Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T76685 Target Info
Target Name Cannabinoid receptor 1 (CB1)
Synonyms Cannabinoid CB1 receptor; CNR; CB-R; CANN6
Target Type Successful Target
Gene Name CNR1
Biochemical Class GPCR rhodopsin
UniProt ID
CNR1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014062965
Title 2-Cycloalkyl Resorcinol Cannabinergic Ligands.
Abstract The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
Applicant(s) Northeastern University
Representative Drug(s) D0H0XC Drug Info Ki = 2.6 nM Click to Show More [1]
2 D05CEL Drug Info Ki = 6 nM [1]
Patent ID WO2014039042
Title Novel Cannabinergic Compounds and Uses Thereof.
Abstract Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
Applicant(s) Northeastern University
Representative Drug(s) D09GJQ Drug Info Ki = 0.6 nM Click to Show More [1]
2 D02TOI Drug Info Ki = 2.4 nM [1]
Patent ID WO2014018695
Title Cannabinoid Receptor Antagonists/Inverse Agonists.
Abstract The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.
Applicant(s) Jenrin Discovery, Inc
Patent ID WO2012174362
Title Pyrazole Derivatives As Cannabinoid Receptor 1 Antagonists.
Abstract The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
Applicant(s) Research Triangle Institute
Representative Drug(s) D0Q9AD Drug Info Ki = 36 nM Click to Show More [2]
2 D01WWN Drug Info Ki = 56 nM [2]
3 D09IYH Drug Info Ki = 294 nM [2]
4 D07PIH Drug Info Ki = 3440 nM [2]
Patent ID WO2012117216
Title N- (Arylalkyl) - 1H- Indole- 2 - Sulfonic Acid Amide Compounds and Their Therapeutic Use As Cannabinoid Allosteric Modulators.
Abstract The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain /V-(arylalkyl)-1 H-indole- 2-sulfonic acid amide compounds that, inter alia, inhibit cannabinoid receptor signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cannabinoid receptor signalling; to treat disorders that are ameliorated by the inhibition of cannabinoid receptor signalling; to treat metabolic syndrome, type-2 diabetes, dyslipidaemia, obesity, eating disorders, cardiovascular diseases and disorders, and other conditions as described herein.
Applicant(s) The University Court of the University of Aberdeen
Representative Drug(s) D05GDS Drug Info IC50 = 1 nM Click to Show More [2]
2 D04ZLC Drug Info IC50 = 400 nM [2]
Patent ID WO2012068529
Title Cannabinoid Receptor Antagonists-Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Abstract The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.
Applicant(s) Jenrin Discovery, Inc
Representative Drug(s) D03HHD Drug Info IC50 = 100 to 1000 nM Click to Show More [2]
2 D0S2ME Drug Info IC50 < 100 nM [2]
3 D0CF8Y Drug Info IC50 = 1000 to 10000 nM [2]
Patent ID WO2012030170
Title Novel Compound Acting As A Cannabinoid Receptor-1 Inhibitor.
Abstract Disclosed are a novel compound acting as a cannabinoid receptor-1 inhibitor, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a hydrate thereof or a solvate thereof. The novel compou.
Applicant(s) Amorepacific Corp
Representative Drug(s) D0L2MA Drug Info IC50 = 4 nM Click to Show More [2]
2 D0GH4B Drug Info IC50 = 7 nM [2]
Patent ID WO2010035915
Title Sulfur Containing Pyrazole-Heterocycle Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Abstract A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Applicant(s) Green Cross Corporation
Representative Drug(s) D0NJ0S Drug Info IC50 = 0.87 nM Click to Show More [2]
2 D0UA6W Drug Info IC50 = 4.11 nM [2]
Patent ID WO2010012797
Title Synthesis of 3,4-Diaryl-4,5-Dihydro-(1H)-Pyrazole-1- Carboxamidine Derivatives.
Abstract The invention relates to a novel chemical route to 3,4-diaryl-4,5-dihydro-(1H)-pyrazole-1-carboxamidine derivatives, known as potent cannabinoid-CB1 receptor antagonists, and to novel intermediates of these compounds. The synthetic route produced considerably higher yields than those reported, without the use of corrosive reagents. The process concerns the preparation of a compound of formula (I) wherein the symbols have the meanings given in the description.
Applicant(s) Abbott
Patent ID WO2009141533
Title Pyrrole Derivatives, Preparation of Same and Therapeutic Application Thereof As Cannabinoid Cb1 Receptor Antagonists.
Abstract The subject of the invention is compounds corresponding to the formula (I): in which: - R1 represents a hydrogen atom or a (C1-C4)alkyl group; - R2 represents a homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical, or an amino (C1-C6)alkyl group; - or R1 and R2, together with the nitrogen atom to which they are attached, constitute a piperazin-1-yl, 1,4-diazepan-1-yl, homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical; - one of the two substituents R3, R6 represents a Y-A-R9 group; - Y represents an oxygen atom, or an -S(O)n-, -OSO2- or-N(R18)- group; ...A represents an unsubstituted (C1-C4)alkylene group; - R9 represents an -OR12, -CN, ...O2H, NR12R13, -CONR12R13, -NR15COR12,-CONHNH2, -CONHOH, -CONHSO2R14, ...(O)nR14, -SO2NR12R13, -NR18SO2R14, or-NR15SO2NR12R13 group, or an aromatic heterocycle. The present invention also relates to the methods of preparation and the therapeutic applications of the compounds of formula (I) as cannabinoid CB1 receptor antagonists.
Applicant(s) Sanofi-Aventis
Representative Drug(s) D0CW1J Drug Info IC50 = 500 nM Click to Show More [2]
2 D0NB2K Drug Info IC50 = 500 nM [2]
Patent ID WO2009141532
Title Derivatives of 1,5-Diphenyl Pyrrole-3-Carboxamide, Preparation Thereof and Use of Same As Cannabinoid Cb1 Receptor Antagonists.
Abstract The subject of the invention is compounds corresponding to the formula (I): in which: - A represents an unsubstituted or substituted (C1-C6)alkylene group; - R1 represents a hydrogen atom or an unsubstituted or substituted (C1-C4)alkyl group; - R2 represents a homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical, or an amino (C1-C6)alkyl group; - or R1 and R2, together with the nitrogen atom to which they are attached, constitute a piperazin-1-yl, 1,4-diazepan-1-yl, homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical; - R3, R4, R5, R6, R7, R8 each independently represent a hydrogen atom, a halogen atom, a -CN, ...(O)nR14, or -OS(O)nR14 group, or an unsubstituted or substituted (C1-C6)alkyl group; - R9 represents an -OR12, -CN, -CO2H, NR12R13,-CONR12R13, -NR15COR12, -CONHNH2, -CONHOH, -CONHSO2R14, ...(O)nR14,-SO2NR12R13, ...R18SO2R14, or -NR15SO2NR12R13 group, or an aromatic heterocycle. The present invention also relates to the methods of preparation and the therapeutic applications of the compounds of formula (I) as cannabinoid CB1 receptor antagonists.
Applicant(s) Sanofi-Aventis
Representative Drug(s) D0HD7S Drug Info IC50 = 500 nM Click to Show More [2]
2 D0M6PB Drug Info IC50 = 500 nM [2]
Patent ID WO2009131815
Title 1,5-Diphenyl-Pyrrolidin-2-One Compounds As Cb-1 Ligands.
Abstract CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0VB2M Drug Info Kb = 0.644 nM Click to Show More [2]
2 D09XUI Drug Info Kb = 0.83 nM [2]
Patent ID WO2009078498
Title Biarylpyrazole 4-Carboxamides As Cannabinoid Cb1 Receptor Ligands.
Abstract A novel biarylpyrazole 4-carboxamide compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor ligand, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Applicant(s) Green Cross Corporation
Representative Drug(s) D0KD5X Drug Info IC50 = 1.47 nM Click to Show More [2]
2 D04BXA Drug Info IC50 = 1.64 nM [2]
Patent ID WO2009033125
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Obesity.
Abstract The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.
Applicant(s) Jenrin Discovery, Inc
Patent ID WO2008130616
Title Diaryl Morpholines As Cb1 Modulators.
Abstract The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
Applicant(s) Schering Corp
Representative Drug(s) D0KX8N Drug Info Ki <= 800 nM [2]
Patent ID WO2008105607
Title Heteroaryl-Imidazole Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Abstract A novel heteroaryl-imidazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Applicant(s) Green Cross Corporation
Representative Drug(s) D0JK3V Drug Info IC50 = 1.14 nM Click to Show More [2]
2 D0BI0F Drug Info IC50 = 1.7 nM [2]
3 D05VIN Drug Info IC50 = 8.98 nM [2]
4 D03GLK Drug Info IC50 = 10.5 nM [2]
Patent ID WO2008094476
Title Substituted Pyrano [2, 3 - B] Pyridine Derivatives As Cannabinoid -1 Receptor Modulators.
Abstract Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0R1PX Drug Info IC50 = 1 nM Click to Show More [2]
2 D0U3YY Drug Info IC50 = 2 nM [2]
Patent ID WO2008074982
Title Pyrazole Derivatives As Modulators of Cannabinoid Receptor.
Abstract Compounds of formula (I) suppress the normal signalling activity of CB1 receptors, and are useful in the treatment of, for example obesity or overweight formula (I): wherein A1, A2, A5, A6, R1, R2, R3, and X are as defined in the claims.
Applicant(s) Cooper, Martin
Representative Drug(s) D08WTW Drug Info IC50 = 300 to 3000 nM Click to Show More [2]
2 D0P7HQ Drug Info IC50 < 300 nM [2]
3 D0P7QA Drug Info IC50 < 300 nM [2]
4 D0KT1Q Drug Info IC50 = 3000 to 10000 nM [2]
Patent ID WO2008070305
Title 1, 5-Diphenyl-3-Pyridinylamino-1, 5-Dihydropyrrolidin-2-One As Cbl' Receptor Modulator.
Abstract Compound and pharmaceutical compositions of Forumla by blockade of the CB1 receptors via an inverse agonism mechanism, and are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailabilty.
Applicant(s) Eli Lilly and Company
Patent ID WO2008059207
Title Cannabinoid Receptor Modulators.
Abstract Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful for the treatment of obesity and diseases for which obesity is a risk factor: (I) wherein: X is a bond, Or-C(R10)(R11)-*. -C(R10)(R11)-O-*, -C(R10)(R11)CH2-*, -C(R10)(R11)CH2-O-*, -CH2C(R10)(R11)-*, -CH2C(R10)(R11)-O-*, or -CH2-O-C(R10)(R11)-*; Y is =O, =N(R9), =N(OR9), =CH(CN), =C(CN)2 or =N(CN); Z is a bond, -O- or -NH-; R1 and R2 are hydrogen, (CrC3)alkyl, (C3-C6)cycloalkyl or monocyclic heterocyclic; or R1 and R2 taken together with the nitrogen to which they are attached form a cyclic amino ring; R3 is hydrogen or a radical of formula -(O)a- AIk3 wherein a and AIk3 are as defined in the claims; R4 is a radical of formula -(O)b-(Alk1)p-(Q)r-(L)s-Q2 wherein b, p, r, s AIk1, L, Q1 and Q2 are as defined in the claims; or R3 and R4 taken together with the nitrogen to which they are attached form a cyclic amino ring; R5 is hydrogen -F, -Cl, -Br, -CN, (C1-C3)alkyl, (C1-C3)fluoroalkyl, cyclopropyl, -COOH, tetrazole or -OR9; R6, R7 and R8 are hydrogen -F, -Cl, -Br, -CN, (C1-C3)alkyl, (C1-C3)fluoroalkyl, cyclopropyl, or -OR9; and R9 R10 and R11 are as defined in the claims.
Applicant(s) Cooper, Martin
Representative Drug(s) D00BXK Drug Info IC50 < 500 nM Click to Show More [2]
2 D00XDN Drug Info IC50 < 500 nM [2]
3 D05NUN Drug Info IC50 = 500 to 5000 nM [2]
4 D06MIW Drug Info IC50 = 500 to 5000 nM [2]
5 D0A2PY Drug Info IC50 = 500 to 5000 nM [2]
6 D0T7QY Drug Info IC50 < 500 nM [2]
Patent ID WO2008039023
Title Heteroaryl-Pyrazole Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Abstract A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Applicant(s) Green Cross Corporation
Representative Drug(s) D0BB2F Drug Info IC50 = 1.09 nM Click to Show More [2]
2 D0D5MQ Drug Info IC50 = 1.79 nM [2]
3 D06MPH Drug Info IC50 = 11.6 nM [2]
4 D05TQG Drug Info IC50 = 14.2 nM [2]
5 D0N0XU Drug Info IC50 = 60.9 nM [2]
Patent ID WO2008004698
Title Pyrazolo [1, 5-A] Pyrimidine Compounds As Cb1 Receptor Antagonist.
Abstract The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: -C(=O)- or -SO2-, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
Applicant(s) Mitsubishi Tanabe Pharma Corporation
Representative Drug(s) D0B6NT Drug Info IC50 < 10 nM Click to Show More [2]
2 D0OT3G Drug Info IC50 < 10 nM [2]
Patent ID WO2007145563
Title Benzimidazole Derivatives Which Are To Be Used As Antagonist for The Cb1-Receptor.
Abstract Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D0K6GI Drug Info Ki = 19.17 nM Click to Show More [2]
2 D0V5BV Drug Info Ki = 23.79 nM [2]
Patent ID WO2007138050
Title Sulphur Containing Pyrazole Derivatives As Selective Cannabinoid Cb1 Receptor Antagonists.
Abstract The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
Applicant(s) Solvay Pharmaceuticals Bv
Representative Drug(s) D0GX6V Drug Info Ki = 10 nM Click to Show More [2]
2 D0M2RT Drug Info Ki = 13 nM [2]
3 D0I0VJ Drug Info Ki = 25 nM [2]
Patent ID WO2007062193
Title Heterocycle-Substituted 3-Alkyl Azetidine Derivatives.
Abstract Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CBl) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CBl receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro- inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0I1VK Drug Info IC50 < 1 nM Click to Show More [2]
2 D0SV6D Drug Info IC50 < 1 nM [2]
3 D0TS3S Drug Info IC50 < 1 nM [2]
Patent ID WO2007046550
Title Pyrazole Compounds Having Cannabinoid Receptor (Cb1) Antagonizing Activity.
Abstract The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
Applicant(s) Mitsubishi Tanabe Pharma Corporation
Representative Drug(s) D02SNQ Drug Info IC50 < 10 nM Click to Show More [2]
2 D07QLD Drug Info IC50 = 10 to 100 nM [2]
3 D0H1IX Drug Info IC50 = 10 to 100 nM [2]
4 D0M9FZ Drug Info IC50 = 10 to 100 nM [2]
5 D01KJZ Drug Info IC50 = 100 to 500 nM [2]
Patent ID WO2007046548
Title Pyrazolo[1,5-A]Pyrimidine Compounds As Cannabinoid Receptor Antagonists.
Abstract The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), or a pharmaceutically acceptable salt thereof.
Applicant(s) Mitsubishi Tanabe Pharma Corporation
Representative Drug(s) D06IPV Drug Info IC50 = 10 to 100 nM Click to Show More [2]
2 D07SYY Drug Info IC50 < 10 nM [2]
3 D0EQ3O Drug Info IC50 < 10 nM [2]
4 D0X7DZ Drug Info IC50 = 10 to 100 nM [2]
Patent ID WO2007020388
Title Pyrazole Derivatives As Therapeutic Agents.
Abstract Salts of 1,5-diarylpyrazole-3-carboxamides and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Applicant(s) Astrazeneca Ab
Patent ID WO2013123335
Title Peripherally Restricted Diphenyl Purine Derivatives.
Abstract The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
Applicant(s) Research Triangle Institute
Representative Drug(s) D0DE0C Drug Info Ki = 1.5 nM Click to Show More [2]
2 D0I1XE Drug Info Ki = 1.9 nM [2]
3 D07PND Drug Info Ki = 360 nM [2]
4 D02ZVY Drug Info N.A. [2]
5 D0D1EI Drug Info N.A. [2]
Patent ID WO2009059264
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Abstract The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.
Applicant(s) Jenrin Discovery, Inc
Representative Drug(s) D01XVK Drug Info N.A. Click to Show More [2]
2 D0ET9U Drug Info N.A. [2]
Patent ID WO2009005646
Title Substituted Piperazines As Cb1 Antagonists.
Abstract Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
Applicant(s) Intervet International Bv
Representative Drug(s) D0IG6J Drug Info N.A. Click to Show More [2]
2 D0PK0R Drug Info N.A. [2]
Patent ID WO2009005645
Title Substituted Piperazines As Cb1 Antagonists.
Abstract Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
Applicant(s) Intervet International Bv
Representative Drug(s) D0AM1D Drug Info N.A. Click to Show More [2]
2 D0ZY6C Drug Info N.A. [2]
Patent ID WO2014013117
Title Chromenopyrazole Diones As Cannabinoid Quinone Derivatives Having Anti-Tumour Activity.
Abstract The invention relates to a compound of general formula (I) or a tautomer, pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1 is independently selected from hydrogen or C1-C18 alkyl; R2 is independently selected from hydrogen, C1-C18 alkyl or C5-C18 aryl; and R3 is independently selected from hydrogen or C1-C5 alkyl. The invention also relates to the use of said compound of formula (I) for treating cancer or a malignant tumor, such as a blastoma, carcinoma, glioma, leukemia, lymphoma and melanoma, and to a method for treating said cancer or tumour, comprising the administration of a therapeutically effective quantity of the compound of formula (I). Consequently, the invention further relates to a pharmaceutical composition comprising a therapeutically effective quantity of a compound of general formula (I) and at least one pharmaceutically acceptable excipient. In addition, the invention relates to the method for producing said compound of general formula (I) by means of oxidation with [bis(trifluoroacetoxy)iode]benzene of the corresponding precursor phenolic derivative.
Applicant(s) Consejo Superior De Investigaciones Cient
Representative Drug(s) D07BFP Drug Info IC50 = 15000 nM [1]
Patent ID WO2010104488
Title Novel Hetero Pyrrole Analogs Acting On Cannapinoid Receptors.
Abstract Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.
Applicant(s) University of Connecticut
Representative Drug(s) D0YN2I Drug Info Ki = 0.5 to 100 nM [2]
Patent ID WO2009124950
Title 4-Methyl-4,5-Dihydro-1H-Pyrazole-3-Carboxamide Useful As A Cannabinoid Cb1 Neutral Antagonist.
Abstract The present invention relates to 4-methyl-4, 5-dihydro-1H- pyrazole-3-carboxamide, and pharmaceutically acceptable salts and solvates thereof. It further concerns pharmaceutical compositions comprising this compound as active ingredient as well as processes and intermediates for preparing this compound and compositions. The referred compound is a cannabinoid CB1 neutral antagonist useful in the prophylaxis and treatment of food intake disorders.
Applicant(s) Laboratorios Del Dr. Esteve
Representative Drug(s) D03WCJ Drug Info IC50 = 7.52 nM [2]
Patent ID WO2008154015
Title Cb1 Receptor Antagonists and Uses Thereof.
Abstract Neutral antagonists of the CB1cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects. A method of detecting a neutral CB1 cannabinoid receptor antagonist, including identifying a candidate compound; subjecting the candidate compound to one or more of a cAMP assay, CB1 competitive binding assay, food intake assay, thermoregulation assay, or emesis assay; and selecting the compound if it exhibits neutral antagonist activity.
Applicant(s) Alexandros Makriyannis et al
Patent ID WO2005035488
Title Thiophene-2-Carboxamide Derivatives and Use Thereof As Cannabinoid Cb-1 Receptor Antagonists.
Abstract The invention relates to a compound of formula (I), where R1 = H, or C1-C4 alkyl, R2 = C4-C10 alkyl, a carbocyclic group, a heterocyclic group, an alkylene group supporting a radical, a NR9R10 group, where R1 and R2 together with nitrogen atom of attachment = either a piperazin-1-yl or a 4-substituted 1,4-diazepan-1-yl, R11 = H, ( C1-C4 alkyl or C3-C7 cycloalkyl and the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.
Applicant(s) Sanofi-Aventis
Representative Drug(s) D0GW8L Drug Info IC50 = 500 nM [2]
Patent ID WO2014008567
Title Modified Peptide, Cb Receptor Ligand, Kit, In Vitro Process for Evaluating Cb Receptor Bonds, Uses, Pharmaceutical Composition for Modulating Cb Receptor Activity.
Abstract The present invention discloses new, non-natural and modified peptides that act as ligands for cannabinoid receptors (CB), especially CB1 and/or CB2, and are useful as modulators of the activity of the latter; also described are a kit and an in vitro process for evaluating CB receptor bonds, uses and a pharmaceutical composition for modulating CB receptor activity. The invention covers the non-natural peptide of SEQ. ID. No: 1 and peptides having at least 70% similarity therewith, including, as particularly useful embodiments of the invention, the non-natural peptides of SEQ. ID. No: 2, SEQ. ID. No: 3, SEQ. ID. No: 4, SEQ. ID. No: 5 and SEQ. ID. No: 6.
Applicant(s) Proteimax Biotecnologia Ltda
United States Patent and Trademark Office (USPTO)
Patent ID US8680131
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Disease Conditions, Including Metabolic Disorders and Cancers.
Patent ID US8461184
Title Sulphur Containing Pyrazole Derivatives As Selective Cannabinoid Cb1 Receptor Antagonists.
Representative Drug(s) D0GX6V Drug Info Ki = 10 nM Click to Show More [2]
2 D0M2RT Drug Info Ki = 13 nM [2]
3 D0I0VJ Drug Info Ki = 25 nM [2]
Patent ID US8420654
Title 1,5-Diphenyl-Pyrrolidin-2-One Compounds As Cb-L Ligands.
Representative Drug(s) D0VB2M Drug Info Kb = 0.644 nM Click to Show More [2]
2 D09XUI Drug Info Kb = 0.83 nM [2]
Patent ID US8410097
Title Heteropyrrole Analogs Acting On Cannabinoid Receptors.
Representative Drug(s) D00TBI Drug Info Ki = 1 nM Click to Show More [2]
2 D0K3FJ Drug Info Ki = 1.2 nM [2]
3 D06FOF Drug Info Ki = 5762 nM [2]
Patent ID US8383666
Title Pyrrole Derivatives, Preparation of Same and Therapeutic Application Thereof.
Representative Drug(s) D0CW1J Drug Info IC50 = 500 nM Click to Show More [2]
2 D0NB2K Drug Info IC50 = 500 nM [2]
Patent ID US8309584
Title Sulfur Containing Pyrazole-Heterocycle Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Representative Drug(s) D0NJ0S Drug Info IC50 = 0.87 nM Click to Show More [2]
2 D0UA6W Drug Info IC50 = 4.11 nM [2]
Patent ID US8188097
Title Pyrazolo[1,5-A]Pyrimidine Compounds.
Representative Drug(s) D06IPV Drug Info IC50 = 10 to 100 nM Click to Show More [2]
2 D07SYY Drug Info IC50 < 10 nM [2]
3 D0EQ3O Drug Info IC50 < 10 nM [2]
4 D0X7DZ Drug Info IC50 = 10 to 100 nM [2]
Patent ID US8168659
Title 1,5-Diphenyl-3-Benzylamino-1,5-Dihydropyrolidin-2-One As Cb1 Receptor Modulators.
Patent ID US8124634
Title Cb1 Receptor Modulators.
Representative Drug(s) D04MPV Drug Info IC50 < 300 nM Click to Show More [2]
2 D0Q5FS Drug Info IC50 < 300 nM [2]
3 D0RV2E Drug Info IC50 < 300 nM [2]
4 D0YW3K Drug Info IC50 < 300 nM [2]
Patent ID US7875647
Title Heteroaryl- Pyrazole Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Representative Drug(s) D0BB2F Drug Info IC50 = 1.09 nM Click to Show More [2]
2 D0D5MQ Drug Info IC50 = 1.79 nM [2]
3 D06MPH Drug Info IC50 = 11.6 nM [2]
4 D05TQG Drug Info IC50 = 14.2 nM [2]
5 D0N0XU Drug Info IC50 = 60.9 nM [2]
Patent ID US7875646
Title Derivatives of N-[(1,5-Diphenyl-1H-Pyrazol-3-Yl)Methyl Sulfonamide, Their Preparation and Their Application In Therapeutics.
Patent ID US7872006
Title Pyrazole Compounds Having Cannabinoid Receptor (Cb1) Antagonizing Activity.
Representative Drug(s) D02SNQ Drug Info IC50 < 10 nM Click to Show More [2]
2 D07QLD Drug Info IC50 = 10 to 100 nM [2]
3 D0H1IX Drug Info IC50 = 10 to 100 nM [2]
4 D0M9FZ Drug Info IC50 = 10 to 100 nM [2]
5 D01KJZ Drug Info IC50 = 100 to 500 nM [2]
Patent ID US7786144
Title Sulphur Containing Pyrazole Derivatives As Selective Cannabinoid Cb1 Receptor Antagonists.
Representative Drug(s) D0GX6V Drug Info Ki = 10 nM Click to Show More [2]
2 D0M2RT Drug Info Ki = 13 nM [2]
3 D0I0VJ Drug Info Ki = 25 nM [2]
Patent ID US77055024
Title Oxadiazole Compounds.
Representative Drug(s) D0D7ZU Drug Info IC50 = 1 to 10000 nM Click to Show More [2]
2 D0J5NB Drug Info IC50 = 1 to 10000 nM [2]
3 D0S5NS Drug Info IC50 = 1 to 10000 nM [2]
Patent ID US20148680102
Title Pyrrole Derivatives, Their Preparation and Their Therapeutic Application.
Representative Drug(s) D0HD7S Drug Info IC50 = 500 nM Click to Show More [2]
2 D0M6PB Drug Info IC50 = 500 nM [2]
Patent ID US20140107157
Title Pyrazole Derivatives As Cannabinoid Receptor 1 Antagonists.
Representative Drug(s) D0Q9AD Drug Info Ki = 36 nM Click to Show More [2]
2 D01WWN Drug Info Ki = 56 nM [2]
3 D09IYH Drug Info Ki = 294 nM [2]
4 D07PIH Drug Info Ki = 3440 nM [2]
Patent ID US20140031404
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Disease Conditions, Including Metabolic Disorders and Cancers.
Patent ID US20130158025
Title Novel Compound Acting As A Cannabinoid Receptor-1 Inhibitor.
Representative Drug(s) D0L2MA Drug Info IC50 = 4 nM Click to Show More [2]
2 D0GH4B Drug Info IC50 = 7 nM [2]
Patent ID US20128252791
Title Purine Compounds As Cannabinoid Receptor Blockers.
Representative Drug(s) D04KUJ Drug Info IC50 < 10 nM Click to Show More [2]
2 D06CEA Drug Info IC50 < 10 nM [2]
3 D06STK Drug Info IC50 < 10 nM [2]
Patent ID US20128173680
Title Cannabinoid Receptor Modulators.
Patent ID US2011112097
Title Substituted Imidazoline-2,4-Diones, Process for Preparation Thereof, Medicaments Comprising These Compounds and Use Thereof.
Representative Drug(s) D0LH9E Drug Info Ki = 2 nM Click to Show More [2]
2 D0FZ5R Drug Info Ki = 217 nM [2]
Patent ID US20110160179
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Representative Drug(s) D01HJQ Drug Info Antagonistic activity < 10000 nM Click to Show More [2]
2 D02OBW Drug Info Antagonistic activity < 10000 nM [2]
3 D0C0KI Drug Info Antagonistic activity < 10000 nM [2]
4 D0J8GO Drug Info Antagonistic activity < 10000 nM [2]
5 D0LX2Y Drug Info Antagonistic activity < 10000 nM [2]
6 D0T8VE Drug Info Antagonistic activity < 10000 nM [2]
7 D0U3VU Drug Info Antagonistic activity < 10000 nM [2]
8 D0VL5E Drug Info Antagonistic activity < 10000 nM [2]
Patent ID US20110152320
Title Pyrrole Derivatives, Their Preparation and Their Therapeutic Application.
Representative Drug(s) D0HD7S Drug Info IC50 = 500 nM Click to Show More [2]
2 D0M6PB Drug Info IC50 = 500 nM [2]
Patent ID US20110144157
Title Pyrrole Derivatives, Preparation of Same and Therapeutic Application Thereof.
Representative Drug(s) D0CW1J Drug Info IC50 = 500 nM Click to Show More [2]
2 D0NB2K Drug Info IC50 = 500 nM [2]
Patent ID US20110053983
Title (5R)-1,5-Diaryl-4,5-Dihydro-1H-Pyrazole-3-Carboxamidine Derivatives Having Cbl-Antagonistic Activity.
Patent ID US20110053908
Title Azetidine-Derived Compounds, Preparation Method Therefore and Therapeutic Use of Same.
Representative Drug(s) D0RC5I Drug Info IC50 = 6 nM Click to Show More [2]
2 D0P7LP Drug Info IC50 = 16 nM [2]
Patent ID US20110034484
Title 1,5-Diphenyl-Pyrrolidin-2-One Compounds As Cbl Ligands.
Representative Drug(s) D0VB2M Drug Info Kb = 0.644 nM Click to Show More [2]
2 D09XUI Drug Info Kb = 0.83 nM [2]
Patent ID US20100292273
Title Cannabinoid Receptor Modulators.
Patent ID US20100197564
Title Diaryl Morpholines As Cb1 Modulators.
Representative Drug(s) D0KX8N Drug Info Ki <= 800 nM [2]
Patent ID US20100144734
Title 1,2,3-Triazole Derivatives As New Cannabinoid-1 Receptor Antagonists.
Representative Drug(s) D0FS0D Drug Info IC50 = 11.6 nM Click to Show More [2]
2 D0S3RX Drug Info IC50 = 1173 nM [2]
Patent ID US20100063032
Title Substituted Pyrido[2,3-D]Pyrimidine Derivatives As Cannabinoid-L Receptor Modulators.
Representative Drug(s) D08RCV Drug Info IC50 = 0.6 nM Click to Show More [2]
2 D0J5XM Drug Info IC50 = 11 nM [2]
Patent ID US20100041650
Title Purine Compounds As Cannabinoid Receptor Blockers.
Representative Drug(s) D04KUJ Drug Info IC50 < 10 nM Click to Show More [2]
2 D06CEA Drug Info IC50 < 10 nM [2]
3 D06STK Drug Info IC50 < 10 nM [2]
Patent ID US20100029697
Title Substituted Pyrido[3,2-E][1,2,4]Triazole[4,3-C]Pyrimidine Derivatives As Cannabinoid-L Receptor Modulators.
Representative Drug(s) D0Z8WF Drug Info IC50 = 1 nM Click to Show More [2]
2 D0V0UW Drug Info IC50 = 2 nM [2]
3 D0F1DK Drug Info IC50 = 11 nM [2]
Patent ID US20100022611
Title 1,5-Diaryl-Pyrazoles As Cannabinoid Receptor Neutral Antagonists Useful As Therapeutic Agents.
Representative Drug(s) D07GJH Drug Info KD = 1.4 nM Click to Show More [2]
2 D03FDN Drug Info KD = 2.3 nM [2]
Patent ID US20090286758
Title Substituted N-Phenyl-5-Phenyl-Pyrazolin-3-Yl Amides As Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Obesity.
Representative Drug(s) D0IC3K Drug Info IC50 < 10000 nM Click to Show More [2]
2 D0K0DV Drug Info IC50 < 10000 nM [2]
3 D0QH5I Drug Info IC50 < 10000 nM [2]
Patent ID US20090258867
Title Pyrazolo[1,5-A]Pyrimidine Compounds As Cb1 Receptor Antagonist.
Representative Drug(s) D0B6NT Drug Info IC50 < 10 nM Click to Show More [2]
2 D0OT3G Drug Info IC50 < 10 nM [2]
Patent ID US20090247499
Title Sulfonylated Piperazines As Cannabinoid-L Receptor Modulators.
Representative Drug(s) D0O4RN Drug Info IC50 = 1.24 nM Click to Show More [2]
2 D07NAA Drug Info IC50 = 6.07 nM [2]
3 D0WK8I Drug Info IC50 = 3188 nM [2]
4 D0FR1Q Drug Info IC50 = 3221 nM [2]
5 D0CX1F Drug Info IC50 = 3791 nM [2]
Patent ID US200901917857
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Representative Drug(s) D01HJQ Drug Info Antagonistic activity < 10000 nM Click to Show More [2]
2 D02OBW Drug Info Antagonistic activity < 10000 nM [2]
3 D0C0KI Drug Info Antagonistic activity < 10000 nM [2]
4 D0J8GO Drug Info Antagonistic activity < 10000 nM [2]
5 D0LX2Y Drug Info Antagonistic activity < 10000 nM [2]
6 D0T8VE Drug Info Antagonistic activity < 10000 nM [2]
7 D0U3VU Drug Info Antagonistic activity < 10000 nM [2]
8 D0VL5E Drug Info Antagonistic activity < 10000 nM [2]
Patent ID US20080090810
Title Thiophene Compounds.
Representative Drug(s) D01RIT Drug Info IC50 = 0.1 to 20000 nM Click to Show More [2]
2 D0C4TB Drug Info IC50 = 0.1 to 20000 nM [2]
3 D0FC8P Drug Info IC50 = 0.1 to 20000 nM [2]
4 D0K7XA Drug Info IC50 = 0.1 to 20000 nM [2]
Patent ID US20080081812
Title Heteroaryl- Pyrazole Derivatives As Cannabinoid Cb1 Receptor Antagonists.
Representative Drug(s) D0BB2F Drug Info IC50 = 1.09 nM Click to Show More [2]
2 D0D5MQ Drug Info IC50 = 1.79 nM [2]
3 D06MPH Drug Info IC50 = 11.6 nM [2]
4 D05TQG Drug Info IC50 = 14.2 nM [2]
5 D0N0XU Drug Info IC50 = 60.9 nM [2]
Patent ID US20070293505
Title Heterocyclic-Substituted 3-Alkyl Azetidine Derivatives.
Representative Drug(s) D0I1VK Drug Info IC50 < 1 nM Click to Show More [2]
2 D0SV6D Drug Info IC50 < 1 nM [2]
3 D0TS3S Drug Info IC50 < 1 nM [2]
Patent ID US20110178148
Title Substituted 5-Vinylphenyl-1-Phenyl-Pyrazole Cannabinoid Modulators.
Representative Drug(s) D00XFT Drug Info 53% inhibition = 1000 nM [2]
Patent ID US8623873
Title Substituted Piperazines As Cb1 Antagonists.
Representative Drug(s) D0IG6J Drug Info N.A. Click to Show More [2]
2 D0PK0R Drug Info N.A. [2]
Patent ID US20100105751
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Representative Drug(s) D01XVK Drug Info N.A. Click to Show More [2]
2 D0ET9U Drug Info N.A. [2]
Patent ID US20070259934
Title Cannabinoid Receptor Antagonists/Inverse Agonists Useful for Treating Metabolic Disorders, Including Obesity and Diabetes.
Representative Drug(s) D0D7AJ Drug Info N.A. Click to Show More [2]
2 D0N6GL Drug Info N.A. [2]
Patent ID US8012958
Title Tetrahydro-Lh-1,2,7-Triaza-Azulene Cannabinoid Modulators.
Representative Drug(s) D0SW2Q Drug Info 52% inhibition = 2000 nM [2]
Patent ID US8012957
Title Tetrahydro-Lh-1,2,6-Triaza-Azulene Cannabinoid Modulators.
Representative Drug(s) D0HD6C Drug Info 39% inhibition = 2000 nM [2]
Patent ID US7495108
Title Imidazoline Derivatives Having Cb1-Antagonistic Activity.
Representative Drug(s) D04QVK Drug Info pA2 = 7.7 [2]
Patent ID US20130123229
Title Cb1 Receptor Antagonists and Uses Thereof.
Patent ID US20128293211
Title Cb1 Receptor Antagonists and Uses Thereof.
Patent ID US20110183960
Title Thiophene-2-Carboxamide, Derivatives Thereof and Therapeutic Use Thereof.
Representative Drug(s) D0H2GT Drug Info IC50 = 500 nM [2]
Patent ID US20110028517
Title 4-Methyl-4,5-Dihydro-1H-Pyrazole-3-Carboxamide Useful As A Cannabinoid Cb1 Neutral Antagonist.
Representative Drug(s) D03WCJ Drug Info IC50 = 7.52 nM [2]
Patent ID US20070066587
Title Substituted Azetidine Compounds, Their Preparation and Use As Medicaments.
Representative Drug(s) D0I5SD Drug Info Ki = 264 nM [2]
Patent ID US2012039804
Title Novel Tricyclic Modulators of Cannabinoid Receptors.
Representative Drug(s) D0GQ8W Drug Info N.A. [1]
European Patent Office (EPO)
Patent ID EP2520577
Title Pyrazolo[1,5-A]Pyrimidine Compounds As Cb1 Receptor Antagonists.
Representative Drug(s) D0LU7K Drug Info IC50 = 1 to 100 nM Click to Show More [2]
2 D0LZ1Z Drug Info IC50 = 1 to 100 nM [2]
3 D0F0VY Drug Info IC50 = 10 to 100 nM [2]
4 D0G8LH Drug Info IC50 < 10 nM [2]
5 D0U6PA Drug Info IC50 < 10 nM [2]
Patent ID EP2146997
Title Substituted Furo[2,3-B]Pyridine Derivatives As Cannabinoid-1 Receptor Modulators.
Representative Drug(s) D02XYT Drug Info IC50 = 0.4 nM Click to Show More [2]
2 D0T0OQ Drug Info IC50 = 1 nM [2]
Patent ID EP2109615
Title Substituted Pyrano[2,3-B]Pyridine Derivatives As Cannabinoid-1-Receptor Modulatos.
Representative Drug(s) D0R1PX Drug Info IC50 = 1 nM Click to Show More [2]
2 D0U3YY Drug Info IC50 = 2 nM [2]
Patent ID EP2035427
Title Pyrazolo[1,5-A]Pyrimidine Compounds As Cb1 Receptor Antagonist.
Representative Drug(s) D0B6NT Drug Info IC50 < 10 nM Click to Show More [2]
2 D0OT3G Drug Info IC50 < 10 nM [2]
Patent ID EP1756066
Title Tetrasubstituted Imidazole Derivatives As Cannabinoid Cb1 Receptor Modulators with A High Cb1/Cb2 Receptor Subtype Selectivity.
Representative Drug(s) D0KX2W Drug Info Ki = 5 nM Click to Show More [2]
2 D0TI3Q Drug Info Ki = 12 nM [2]
Patent ID EP1713475
Title 1,3,5-Trisubstituted 4,5-Dihydro-1H-Pyrazole Derivatives Having Cb1-Antagonistic Activity.
Representative Drug(s) D03TDK Drug Info 79% inhibition = 1000 nM Click to Show More [2]
2 D0Z7EV Drug Info 98% inhibition = 1000 nM [2]
Patent ID EP1620395
Title Azetidinecarboxamide Derivatives and Their Use In The Treatment of Cb1 Receptor Mediated Disorders.
Representative Drug(s) D00TMQ Drug Info Ki = 0.6 nM Click to Show More [2]
2 D0ZE8B Drug Info Ki = 1.3 nM [2]
3 D0DF6B Drug Info Ki = 80 nM [2]
Patent ID EP1542678
Title 1H-1,2,4-Triazole-3-Carboxamide Derivatives As Cannabinoid-Cb Sb 1/Sb Receptor Ligands.
Representative Drug(s) D02NNZ Drug Info pA2 = 7.2 Click to Show More [2]
2 D0TT0B Drug Info pA2 = 8.2 [2]
Patent ID EP1494673
Title Compounds Having Unique Cb1 Receptor Binding Selectivity and Methods for Their Production and Use.
Representative Drug(s) D0JW7T Drug Info EC50 = 5270 nM Click to Show More [2]
2 D0R9PD Drug Info EC50 = 73585 nM [2]
Patent ID EP20081725536
Title Imidazoline Derivatives Having Cb1-Antagonistic Activity.
Representative Drug(s) D04QVK Drug Info pA2 = 7.7 [2]
References  Top
REF 1 Cannabinoid receptor 2 (CB2) agonists and antagonists: a patent update.Expert Opin Ther Pat. 2016 Jul;26(7):843-56.
REF 2 A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents. Expert Opin Ther Pat. 2015 Oct;25(10):1093-116.

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