公开(公告)号：US20230142171A1

公开(公告)日：2023-05-11

申请号：US17938000

申请日：2022-10-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Bjoern BARTELS ,  Giuseppe CECERE ,  Luca GOBBI ,  Maria-Clemencia HERNANDEZ ,  Roland HUMM ,  Andrés Miguel OLIVARES MORALES ,  Angélique PATINY-ADAM ,  Valerie RUNTZ-SCHMITT ,  Christian SCHNIDER

IPC: C07D487/04 ,  C07D243/24 ,  A61K9/20 ,  A61K9/48 ,  A61K9/08 ,  A61K47/12 ,  A61K47/10 ,  A61K9/00

CPC classification number: C07D487/04 ,  C07D243/24 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2013 ,  A61K9/4858 ,  A61K9/485 ,  A61K9/4866 ,  A61K9/08 ,  A61K47/12 ,  A61K47/10 ,  A61K9/0019

Abstract: The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

公开(公告)号：US20240287082A1

公开(公告)日：2024-08-29

申请号：US18611118

申请日：2024-03-20

Applicant: Hoffmann-La Roche Inc.

Inventor： Giuseppe CECERE ,  Luca GOBBI ,  Steven Paul HANLON ,  Maria-Clemencia HERNANDEZ ,  Roland HUMM ,  Andreas KOBLET ,  Andrés Miguel OLIVARES MORALES ,  Valerie RUNTZ-SCHMITT

IPC: C07D487/04 ,  A61K9/16 ,  A61K9/48 ,  A61K31/5513

CPC classification number: C07D487/04 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/4825 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/5513

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R5 and X are as described herein.




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

公开(公告)号：US20230391778A1

公开(公告)日：2023-12-07

申请号：US18451702

申请日：2023-08-17

Applicant: Hoffmann-La Roche Inc.

Inventor： Hans HILPERT ,  Sabine KOLCZEWSKI ,  Roland HUMM ,  Theodor STOLL ,  Thorsten MUSER ,  Jean-Marc PLANCHER ,  Delphine GAUFRETEAU

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D403/04

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D403/04

Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula






wherein
Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−);
R1 is lower alkyl, halogen, cyano or cycloalkyl;
Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−), or is benzo[b]thiophenyl;
R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl;
X is CH or N;
n is 1 or 2;
m is 1 or 2;
as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof




The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, epilepsy, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems.