| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2015118019 |
| Title |
Substituted Thiazole or Oxazole P2X7 Receptor Antagonists. |
| Abstract |
The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. |
| Applicant(s) |
Axxam Spa |
| Representative Drug(s) |
D0T1JN |
Drug Info
|
pIC50(hP2X7R) = 8.1 |
[1] |
| Patent ID |
WO2014097140 |
| Title |
Indole Carboxamide Derivatives As P2X7 Receptor Antagonists. |
| Abstract |
The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds. |
| Applicant(s) |
Actelion Pharmaceuticals Ltd |
| Representative Drug(s) |
D0ZY5M |
Drug Info
|
pIC50(hP2X7R) = 8.5 |
[1] |
| Patent ID |
WO2014057080 |
| Title |
N-(2-(Cyclic Amine)Ethyl)Benzamide Derivatives As P2X7 Inhibitors. |
| Abstract |
The present invention is directed to N-(2-(cyclic amine)ethyl)benzamide derivatives of formula (I), as P2X7 inhibitors, pharmaceutical compositions comprising said compounds and uses of the compounds to treat pain, inflammation, neurological disorders, or neuropsychiatric disorders. |
| Applicant(s) |
H. Lundbeck A / S |
| Representative Drug(s) |
D0FR8L |
Drug Info
|
pIC50(hP2X7R) = 9.5 |
[1] |
| Patent ID |
WO2014057078 |
| Title |
Benzamides. |
| Abstract |
The present application relates to compounds of formula (I), wherein R1 to R5 are as defined in claim 1, a pharmaceutical composition thereof and said compounds for use in the treatment of diseases related with the activity of P2X7 receptor. |
| Applicant(s) |
H. Lundbeck A / S |
| Representative Drug(s) |
D0RG4J |
Drug Info
|
pIC50(hP2X7R) = 10 |
[1] |
| Patent ID |
WO2012114268 |
| Title |
Benzamide Derivatives As P2X7 Receptor Antagonists. |
| Abstract |
The invention relates to benzamide derivatives of formula (I),wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds. |
| Applicant(s) |
Actelion Pharmaceuticals Ltd |
| Representative Drug(s) |
D0N2TV |
Drug Info
|
pIC50(hP2X7R) = 8.1 |
[1] |
| Patent ID |
WO2012040048 |
| Title |
Triazolopyrazinones As P2X7 Receptor Antagonists. |
| Abstract |
The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptabl salts, wherein R1, R2, R3, R8, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating pain or an inflammatory disease. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Representative Drug(s) |
D0N4RJ |
Drug Info
|
pIC50(hP2X7R) = 8.2 |
[1] |
| Patent ID |
WO2011054947 |
| Title |
Thiadiazolidinedioxide P2X7 Receptor Antagonists. |
| Abstract |
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: R1 is C1-3alkyl or C1fluoroalkyl-CH2; R2 is hydrogen, C1-4alkyl, C1fluoroalkyl-CH2-, C3-6cycloalkyl, C3-6cycloalkyl-methyl-, optionally substituted benzyl, or optionally substituted heteroaryl-(CH2)n-, wherein n is 0 or 1, wherein in R2 the benzyl is optionally substituted on the ring with one or two substituents independently being methyl, methoxy, fluorine or chlorine, and wherein in R2 the heteroaryl-(CH2)n- optionally substituted on the heteroaryl ring with one or two substituents independently being C1-3alkyl, CF3, methoxy, a halogen atom, or cyano; and wherein: R3, R4, R5, R6 and R7 independently are hydrogen, a halogen atom, C1-4alkyl, trifluoromethyl, or cyano, such that one or both of R3 and R7 is or are a group other than hydrogen. |
| Applicant(s) |
Glaxo Group Limited |
| Representative Drug(s) |
D04SHK |
Drug Info
|
pIC50(hP2X7R) > 7.5 |
[1] |
| Patent ID |
WO2012036193 |
| Title |
Therapeutic Agent for Fatty Liver Disease Containing P2X7 Receptor Inhibitory Substance As Active Ingredient. |
| Abstract |
[Problem] To provide a therapeutic agent for fatty liver disease (FLD), preferably for nonalcoholic fatty liver disease (NAFLD), in particular, for nonalcoholic steatohepatitis (NASH), said agent comp. |
| Applicant(s) |
Astellas Pharma Inc |
| Patent ID |
WO2010018280 |
| Title |
Use of P2X7 Receptor Antagonists To Promote Axonal Growth and Ramification. |
| Abstract |
The present invention relates to the use of P2X7 receptor antagonists capable of crossing the hematoencephalic barrier and pharmaceutically-acceptable vehicles, in addition to pharmaceutical compositions thereof, to produce medicaments intended for the treatment of illnesses or conditions associated with: a) absence of or reduction in axonal growth; b) axonal collateral loss; c) nervous lesion; d) loss or degeneration of synaptic connections. In addition, the use is described of said antagonists to promote axonal growth both in cultivated neurons and in transplanted neurons. A method is also included for producing neurons differentiated in vitro commencing from stem cells, comprising culturing said cells in the presence of a P2X7 antagonist, together with the culture obtained through the previously described method, and use thereof for production of medicaments intended for the previously detailed illnesses. |
| Applicant(s) |
Univ Madrid Complutense |
| Patent ID |
WO2014174282 |
| Title |
P2X7 Receptor Agonist for Use In Preventing or Treating Kidney Injury. |
| Applicant(s) |
Ucl Business Plc |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US8106073 |
| Title |
Quinoline Derivatives 057. |
| Applicant(s) |
AstraZeneca |
| Representative Drug(s) |
D01EBW |
Drug Info
|
pIC50(hP2X7R) = 8.4 |
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[1] |
|
2
|
D0L2KM
|
Drug Info
|
pIC50(hP2X7R) = 8.4
|
[1] |
| Patent ID |
US8580812 |
| Title |
Heteroaryl Amide Analogues As P2X7 Antagonists. |
| Applicant(s) |
H. Lundbeck A / S |
| Representative Drug(s) |
D0OG3Z |
Drug Info
|
pIC50(hP2X7R) < 5.7 |
[1] |
| Patent ID |
US7964616 |
| Title |
Compounds 679. |
| Applicant(s) |
Astrazeneca |
| Representative Drug(s) |
D0B7KM |
Drug Info
|
pIC50(hP2X7R) = 8.1 |
[1] |
| Patent ID |
US7741493 |
| Title |
Heterocyclic Compounds As P2X7 Ion Channel Blockers. |
| Applicant(s) |
Aventis Pharmaceuticals, Inc |
| Representative Drug(s) |
D08PQU |
Drug Info
|
pIC50(hP2X7R) = 8 |
[1] |
| Patent ID |
US7723367 |
| Title |
Amino-Tetrazoles Analogues and Methods of Use. |
| Applicant(s) |
Abbott |
| Representative Drug(s) |
D0UC8I |
Drug Info
|
pIC50(hP2X7R) < 5 |
[1] |
| Patent ID |
US7709469 |
| Title |
P2X7 Receptor Antagonists and Methods of Use. |
| Applicant(s) |
Abbott |
| Representative Drug(s) |
D00PVH |
Drug Info
|
pIC50hIL-1 < 6 |
[1] |
| Patent ID |
US20150025075 |
| Title |
Heterocyclic Amide Derivatives As P2X7 Receptor Antagonists. |
| Applicant(s) |
Actelion Pharmaceuticals Ltd |
| Representative Drug(s) |
D06MSZ |
Drug Info
|
pIC50(hP2X7R) = 8.9 |
[1] |
| Patent ID |
US20140275120 |
| Title |
P2X7 Modulators. |
| Applicant(s) |
Janssen Pharmaceutica |
| Representative Drug(s) |
D08SFW |
Drug Info
|
pIC50(hP2X7R) = 8.6 |
[1] |
| Patent ID |
US20140275096 |
| Title |
[1,2,4]Triazolo[4,3-A]Pyrazines As P2X7 Modulators. |
| Applicant(s) |
Janssen Pharmaceutica |
| Representative Drug(s) |
D07EBW |
Drug Info
|
pIC50(hP2X7R) = 9.5 |
[1] |
| Patent ID |
US20140275056 |
| Title |
5,6,7,8,9,10-Hexahydro-6,10 Epimino[1,2,4]Triazolo[4,3-A]Azocines As P2X7 Modulators. |
| Applicant(s) |
Janssen Pharmaceutica |
| Representative Drug(s) |
D09REZ |
Drug Info
|
pIC50(hP2X7R) = 9 |
[1] |
| Patent ID |
US20140163035 |
| Title |
Heterocyclic Amide Derivatives As P2X7 Receptor Antagonists. |
| Applicant(s) |
Actelion Pharmaceuticals Ltd |
| Representative Drug(s) |
D0C9WD |
Drug Info
|
pIC50(hP2X7R) = 8.7 |
[1] |
| Patent ID |
US20120190680 |
| Title |
Heteroaryl Amide Analogues. |
| Applicant(s) |
H. Lundbeck A / S |
| Representative Drug(s) |
D0PI1X |
Drug Info
|
pIC50(hP2X7R) < 5.7 |
[1] |
| Patent ID |
US20120172366 |
| Title |
Heteroaryl Amide Derivatives. |
| Applicant(s) |
H. Lundbeck A / S |
| Representative Drug(s) |
D08OKB |
Drug Info
|
pIC50(hP2X7R) < 5.7 |
[1] |
| Patent ID |
US20120157494 |
| Title |
Isoindolyl Compounds. |
| Applicant(s) |
Roche |
| Representative Drug(s) |
D0EY5F |
Drug Info
|
pIC50(hP2X7R) = 7.5 |
[1] |
| Patent ID |
US20120157436 |
| Title |
5,6,7,8-Tetrahydro[1,2,4]Triazolo[4,3-A]Pyrazine Derivatives As P2X7 Modulators. |
| Applicant(s) |
Gsk |
| Representative Drug(s) |
D0R4IT |
Drug Info
|
pIC50(hP2X7R) > 8 |
[1] |
| Patent ID |
US20120149718 |
| Title |
Amido Compounds. |
| Applicant(s) |
Roche |
| Representative Drug(s) |
D0GQ6D |
Drug Info
|
pIC50(hP2X7R) = 7.7 |
[1] |
| Patent ID |
US20110092481 |
| Title |
Quinoline or Isoquinoline Substituted P2X7 Antagonists. |
| Applicant(s) |
Janssen Pharmaceutica |
| Representative Drug(s) |
D05KRX |
Drug Info
|
pIC50(hP2X7R) = 9.1 |
[1] |
| Patent ID |
US20110071143 |
| Title |
[1,2,4]Triazolo[3,4-C][1,4]Oxazines As P2X7 Modulators. |
| Applicant(s) |
Roche |
| Representative Drug(s) |
D0AI1I |
Drug Info
|
pIC50(hP2X7R) = 8.3 |
[1] |
| Patent ID |
US20110046137 |
| Title |
Pyrazole Derivatives As P2X7 Modulators. |
| Applicant(s) |
Gsk |
| Representative Drug(s) |
D0NG6O |
Drug Info
|
pIC50(hP2X7R) > 7.9 |
[1] |
| Patent ID |
US20110028502 |
| Title |
Dihydropyrimidone Amides As P2X7 Modulators. |
| Applicant(s) |
Roche |
| Representative Drug(s) |
D07VLC |
Drug Info
|
pIC50(hP2X7R) = 8.6 |
[1] |
| Patent ID |
US20100311749 |
| Title |
4-Benzoyl-1-Substituted-Piperazin-2-One Derivatives As P2X7 Modulators. |
| Applicant(s) |
Gsk |
| Representative Drug(s) |
D0QC5O |
Drug Info
|
pIC50(hP2X7R) > 7 |
[1] |
| Patent ID |
US20100286390 |
| Title |
Pyridazinone Compounds and P2X7 Receptor Inhibitors. |
| Applicant(s) |
Nissan Chemical Industries, Ltd |
| Representative Drug(s) |
D0L8QD |
Drug Info
|
pIC50(hP2X7R) = 8.9 |
[1] |
| Patent ID |
US20100184802 |
| Title |
Bicycloheteroaryl Compounds As P2X7 Modulators and Uses Thereof. |
| Applicant(s) |
Evotec |
| Representative Drug(s) |
D0O8DL |
Drug Info
|
pIC50hIL-1 = 10 |
[1] |
| Patent ID |
US20100075968 |
| Title |
Imidazolidine Carboxamide Derivatives As P2X7 Modulators. |
| Applicant(s) |
Gsk |
| Representative Drug(s) |
D0WI9M |
Drug Info
|
pIC50(hP2X7R) > 7.5 |
[1] |
| Patent ID |
US20100022531 |
| Title |
Novel Compounds As P2X7 Modulators and Uses Thereof. |
| Applicant(s) |
Evotec |
| Representative Drug(s) |
D0S9HE |
Drug Info
|
N.A. |
[1] |
| Patent ID |
US7923448 |
| Title |
Purine Receptor Inhibition As A Therapeutic Strategy In Spinal Cord and Brain. |
| Applicant(s) |
Cornell Research Foundation, Inc |
| Patent ID |
US20140037576 |
| Title |
P2X7: Inhibition of Epithelial Cancers and Papillomas. |
| Applicant(s) |
University Hospitals of Cleveland |
| Patent ID |
US20120034165 |
| Title |
Imaging The Central Nervous System with Purinergic P2X7 Receptor Binding Agents. |
| Applicant(s) |
Jackson Alexander |
| Patent ID |
US20110269708 |
| Title |
P2X7 Antagonists To Treat Affective Disorders. |
| Applicant(s) |
Abbott |
| Patent ID |
US20140322193 |
| Title |
Therapies for Disorders of The Cornea and Conjunctiva. |
| Patent ID |
US20120264708 |
| Title |
Method for Treatment of Macular Degeneration By Modulating P2Y12 or P2X7 Receptors. |
| European Patent Office (EPO) |
| Patent ID |
EP1448535 |
| Title |
Benzamide and Heteroarylamide As P2X7 Receptor Antagonists. |
| Applicant(s) |
Pfizer Product Inc |
| Representative Drug(s) |
D04QLC |
Drug Info
|
pIC50(hP2X7R) = 6 |
[1] |
| Patent ID |
EP2604265 |
| Title |
P2X7 Antagonists As Frontline or Adjunctive Treatment Against Status Epilepticus. |
| Applicant(s) |
Royal College of Surgeons In Ireland |
