| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2017220799 |
| Title |
Compounds for Treating Disorders Sensitive To Serotoninergic Regulation Controlled By The 5-Ht1A Receptors. |
| Abstract |
The invention concerns compounds that possess a high affinity at 5-HT 1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors. |
| Applicant(s) |
Neurolixis |
| Representative Drug(s) |
D0E7FT |
Drug Info
|
Ki = 0.01 nM |
[1] |
| Patent ID |
WO2016003296 |
| Title |
(Quinoline or Isoquinoline)Sulfonamides of Cyclic Amines As Antipsychotic Drugs. |
| Abstract |
The invention relates to compounds of general formula (I) wherein: one of A1 and A2 represents a nitrogen atom and the other a carbon atom optionally substituted by halogen; the wave line between the sulfonamido moiety and B/C rings represents a single bond linking the sulfur atom to a non-bridgehead carbon atom, with the proviso that the part of ring C being detached by the dashed broken line is unsubstituted; n represents an integer from 0 to 3; Y represents a nitrogen or carbon atom; Z represents a 5-6 membered aromatic/ heteroaromatic ring optionally fused with a further aromatic or non- aromatic 5-6 membered heterocycle, the condensed ring system being linked via a non-bridgehead carbon atom. The compounds display high affinity for the D2, D3, 5-HT1A, 5-HT2A- 5-HT6 and 5-HT7 receptors and are useful for the treatment of psychotropic diseases or disorders associated with disturbances of the dopaminergic/ serotoninergic systems such as schizophrenia and autism. |
| Applicant(s) |
Instytut Farmakologii Polskiej Akademii Nauk |
| Representative Drug(s) |
D09BCJ |
Drug Info
|
Ki = 1 nM |
Click to Show More |
[1] |
|
2
|
D0F4NB
|
Drug Info
|
EC50 = 28.3 nM; Ki = 18 nM
|
[1] |
| Patent ID |
WO2014180165 |
| Title |
Benzoisothiazole Compounds and Use In Preparation of Antipsychotic Drugs. |
| Abstract |
Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D3 receptor, 5-HT1A receptor and 5-HT2A receptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof. |
| Applicant(s) |
Shanghai Inst Pharm Industry |
| Representative Drug(s) |
D0Z9WY |
Drug Info
|
Ki = 0.2 nM |
Click to Show More |
[1] |
|
2
|
D0M1UF
|
Drug Info
|
Ki = 1.3 nM
|
[1] |
| Patent ID |
WO2013102250 |
| Title |
Gravity Assisted Spine Decompressing Apparatus. |
| Abstract |
Commonly referred to as a back stretcher and/or a neck stretcher, the present invention pertains to an apparatus designed to relax the user's back muscles as gravity safely and smoothly decompresses his/her thoracic and lumbar vertebrae while lying chest side on the apparatus; and same said apparatus being made reconfigurable to safely and smoothly decompress the user's cervical vertebrae while lying back side on the apparatus. When configured to decompress the user's thoracic and lumbar vertebrae, the apparatus is equipped with armrests or arm-harnesses to retain the user in place against the down-pull of gravity; said armrests or arm- harnesses made adjustable to fit the user's body length and chest width. Furthermore, the apparatus is equipped with a facial support with opening allowing the user to see through and perform other tasks while lying chest side on the apparatus; said facial support made adjustable to fit the user's facial physical features as well as his/her neck and head lengths. The apparatus is also made adjustable for distinct curvatures, allowing the user to emphasize the effect of the down-pull of gravity to act on his/her thoracic and/or lumbar vertebrae. The apparatus also comprises an abdomen surface adjustment enabling a user who has a medium size or a large size abdomen to obtain as close as possible to the ideal configuration for best spinal decompression geometry which provides enhanced blood circulation within the intervertebral fibrocartilage (discs) and other tissues between his/her vertebrae. The apparatus is also equipped with an adjustable shelf allowing the user to perform other task(s) while lying chest side on the apparatus. When configured to decompress the user's cervical vertebrae, the apparatus comprises an adjustable head-harness to hold the user's head in place while gravity smoothly pulls on the remainder of his/her body. The apparatus is also equipped with an ankle support and an extendable surface to deter the user from using his/her feet to retain position on the apparatus against the down-pull of gravity. The apparatus is further equipped with adjustable legs which can be lengthen or shorten to obtain the desired level of efficiency/comfort relationship. |
| Applicant(s) |
Benoit Launier |
| Representative Drug(s) |
D0SG8X |
Drug Info
|
Ki = 5 nM |
[1] |
| Patent ID |
WO2013102249 |
| Title |
N-Phenylpiperazine Derivatives That Are Antagonists of 1A, 1D Adrenoceptors and 5-Ht1A Receptors for The Treatment of Benign Prostate Hyperplasia. |
| Abstract |
The present invention provided N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of alpha1A adrenoceptors, alpha1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions. |
| Applicant(s) |
Univ Rio De Janeiro |
| Representative Drug(s) |
D0EO8F |
Drug Info
|
Ki = 0.0237 nM |
[1] |
| Patent ID |
WO2010139758 |
| Title |
Novel Derivatives of Aryl-{4-Halogeno-4-[Aminomethyl]-Piperidin-1-Yl}-Methanone, Their Method of Preparation and Their Use As Medicinal Products. |
| Abstract |
The present invention concerns compounds of general formula (1) (I) wherein R1 is: - a hydrogen atom, or a halogen, - a straight or branched C1-C6 alkyl group or a C1-C3 fluoroalkyl group, - a straight or branched C1-C6 alcoxy group, a carbamyl group, N-substituted or not by one or two, straight or branched C1-C3 alkyl groups, or - a cyano group (CN) R2 is: - a hydrogen atom or a straight or branched C1-C6 alkyl group, HaI1, Hal2 and Hal3 are: - a halogen their addition salts and the hydrates of addition salts with pharmaceutically acceptable mineral acids or organic acids, and their enantiomer forms. |
| Applicant(s) |
Pierre Fabre Medicament |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20160244429 |
| Title |
Substituted Piperazine Compounds and Methods of Use Thereof. |
| Representative Drug(s) |
D0F9TY |
Drug Info
|
Ki = 0.1 nM |
Click to Show More |
[1] |
|
2
|
D0T7HK
|
Drug Info
|
Ki = 0.14 nM
|
[1] |
|
3
|
D0M9LM
|
Drug Info
|
IC50 = 0.23 nM
|
[1] |
| Patent ID |
US20160096811 |
| Title |
Benzoisothiazole Compounds and Use In Preparation of Antipsychotic Drugs. |
| Representative Drug(s) |
D0Z9WY |
Drug Info
|
Ki = 0.2 nM |
Click to Show More |
[1] |
|
2
|
D0M1UF
|
Drug Info
|
Ki = 1.3 nM
|
[1] |
| Patent ID |
US20150011566 |
| Title |
N-Phenylpiperazine Derivatives That Are Antagonists of A1A, A1D Adrenoreceptors and 5-Ht1A Receptors for The Treatment of Benign Prostate Hyperplasia. |
| Representative Drug(s) |
D0EO8F |
Drug Info
|
Ki = 0.0237 nM |
Click to Show More |
[1] |
|
2
|
D0SG8X
|
Drug Info
|
Ki = 5 nM
|
[1] |
| Patent ID |
US20150374695 |
| Title |
6-Piperazinyl-3,4-Dihydroquinazolin-2(1H)-Ones. |
| Patent ID |
US20140296528 |
| Title |
4-Aryl-1-(Biarylmethylene)Piperidine Compounds. |
