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US9751870B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9751870-B2 |
| Application number | US-201514802469-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 17, 2015 |
| Priority date | Jan 17, 2013 |
| Publication date | Sep 5, 2017 |
| Grant date | Sep 5, 2017 |
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Abstract
Official abstract text for this publication.
The invention relates to the use of a compound of formula I wherein A 1 is phenyl or a five or six membered hereroaryl group, containing 1, 2 or 3 heteroatoms, selected from N or S; R 1 is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen or cycloalkyl; A 2 is phenyl; R 2 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, S-lower alkyl substituted by halogen, S(O) 2 -lower alkyl substituted by halogen; n is 1 or 2; or a pharmaceutically acceptable acid addition salt, or a racemic mixture or its corresponding enantiomer and/or optical isomers thereof, for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.
First claim
Opening claim text (preview).
The invention claimed is: 1. A method of treating a condition selected from the group consisting of autism, stress, post traumatic stress disorder, anxiety disorders, depression, schizophrenia, psychiatric disorders, memory loss, alcohol withdrawal, drug addiction and Prader-Willi Syndrome, comprising administering a compound of formula I wherein A 1 is phenyl or a five or six membered heteroaryl group, containing 1, 2 or 3 heteroatoms, selected from N or S; R 1 is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen or cycloalkyl; A 2 is phenyl; R 2 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, S-lower alkyl substituted by halogen, S(O) 2 -lower alkyl substituted by halogen; n is 1 or 2; or a pharmaceutically acceptable acid addition salt, a racemic mixture or its corresponding enantiomer and/or optical isomers thereof, to a patient in need thereof. 2. A method of treating a condition selected from the group consisting of autism, stress, post traumatic stress disorder, anxiety disorders, depression, schizophrenia, psychiatric disorders, memory loss, alcohol withdrawal, drug addiction and Prader-Willi Syndrome, comprising administering a compound selected from the group consisting of 4-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Ethyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Propyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 2-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Difluoromethoxy-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-N-[2-(4-fluoro-phenyl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyrimidin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 2,4-Dichloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-2-fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-(1-Fluoro-ethyl)-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethylsulfanyl-benzenesulfonamide 4-Trifluoromethyl-N-[2-(2-trifluoromethyl-pyrimidin-4-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 2-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethanesulfonyl-benzenesulfonamide 3-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-[2-(3-Cyclopropyl-[1,2,4]thiadiazol-5-yl)-2H-pyrazol-3-yl]-4-ethyl-benzenesulfonamide and 4-Chloro-2-fluoro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide to a patient in need thereof. 3. A pharmaceutical composition comprising a compound selected from the group consisting of 4-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Ethyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Propyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 2-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Difluoromethoxy-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-N-[2-(4-fluoro-phenyl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyrimidin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 2,4-Dichloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-2-fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-(1-Fluoro-ethyl)-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethylsulfanyl-benzenesulfonamide 4-Trifluoromethyl-N-[2-(2-trifluoromethyl-pyrimidin-4-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 2-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethanesulfonyl-benzenesulfonamide 3-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-[2-(3-Cyclopropyl-[1,2,4]thiadiazol-5-yl)-2H-pyrazol-3-yl]-4-ethyl-benzenesulfonamide and 4-Chloro-2-fluoro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide, or a pharmaceutically acceptable acid addition salt, a racemic mixture or its corresponding enantiomer and/or optical isomers thereof, and a therapeutically inert carrier. 4. A compound selected from the group consisting of 4-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Ethyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Propyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 2-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 4-Difluoromethoxy-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-N-[2-(4-fluoro-phenyl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyrimidin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide 2,4-Dichloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-Chloro-2-fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide 4-(1-Fluoro-ethyl)-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide N-[2-(4-Methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide 4-Chloro-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Ethyl-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 4-Cyano-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethylsulfanyl-benzenesulfonamide 4-Trifluoromethyl-N-[2-(2-trifluoromethyl-pyrimidin-4-yl)-2H-pyrazol-3-yl]-benzenesulfonamide 2-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethanesulfonyl-benzenesulfonamide 3-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide N-[2-(3-Cyclopropyl-[1,2,4]thiadiazol-5-yl)-2H-pyrazol-3-yl]-4-ethyl-benzenesulfonamide and 4-Chloro-2-fluoro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide or a pharmaceutically acceptable acid addition salt, a racemic mixture or its corresponding enantiomer and
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Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title
for treating abuse or dependence · CPC title
Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title
Anxiolytics · CPC title
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- What does patent US9751870B2 cover?
- The invention relates to the use of a compound of formula I wherein A 1 is phenyl or a five or six membered hereroaryl group, containing 1, 2 or 3 heteroatoms, selected from N or S; R 1 is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen or cycloalkyl; A 2 is phenyl; R 2 is halogen, lower alkyl, lower alkyl substituted by halogen, lowe…
- Who is the assignee on this patent?
- Hoffmann La Roche, Hoffman-La Roche Inc
- What technology area does this patent fall under?
- Primary CPC classification C07D417/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 05 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).