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公开(公告)号：US11819532B2
公开(公告)日：2023-11-21
申请号：US16389292
申请日：2019-04-19
发明人： Konrad Bleicher , Daniella Cheang , Patrick Di Giorgio , Patrizio Mattei , Petra Schmitz , Theodor Stoll
摘要： The present invention provides compounds of formula (I)
wherein X1, X2, R1 to R6 and A are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by bacteria.-
公开(公告)号：US20220411468A1
公开(公告)日：2022-12-29
申请号：US17377338
申请日：2021-07-15
发明人： Alexander Alanine , Julien Beignet , Konrad Bleicher , Bernhard Fasching , Hans Hilpert , Taishan Hu , Dwight MacDonald , Stephen Jackson , Sabine Kolczewski , Carsten Kroll , Adrian Schaeublin , Hong Shen , Theodor Stoll , Helmut Thomas , Amal Wahhab , Claudia Zampaloni
摘要： The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
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公开(公告)号：US20160095844A1
公开(公告)日：2016-04-07
申请号：US14971120
申请日：2015-12-16
发明人： Daniela Brunner , Hans Hilpert , Sabine Kolczewski , Anja Limberg , Jessica Malberg , Eric Prinssen , Claus Riemer , Bavani G. Shankar , Theodor Stoll
IPC分类号： A61K31/4439 , C07D403/04 , A61K31/506 , C07D403/14 , A61K31/501 , A61K31/438 , C07D498/04 , A61K31/5383 , C07D471/04 , A61K31/437 , C07C53/06 , A61K31/19 , C07D405/14 , A61K31/4178 , C07D413/04 , A61K31/4245 , A61K31/422 , C07D417/04 , A61K31/433 , A61K31/496 , A61K31/5377 , C07D487/04 , A61K31/519 , C07D471/10 , C07D413/14 , A61K31/497 , C07H19/044 , A61K31/7064 , A61K31/55 , A61K45/06 , C07D401/04
CPC分类号： A61K31/4439 , A61K31/19 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/437 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61K31/7064 , A61K45/06 , C07C53/06 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07H19/044
摘要： The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o—S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line indicates a bond may or may not be present; or, a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are 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, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
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公开(公告)号：US11505573B2
公开(公告)日：2022-11-22
申请号：US16358371
申请日：2019-03-19
发明人： Konrad Bleicher , Daniella Cheang , Patrick Di Giorgio , Taishan Hu , Patrizio Mattei , Petra Schmitz , Theodor Stoll
IPC分类号： C07K5/09 , C07K5/00 , C07K5/08 , C07K5/083 , C07K5/093 , A61K38/00 , C07K5/087 , C07K5/02 , C07K5/097 , C07K7/50 , A61K38/12
摘要： The present invention provides compounds of formula (I) wherein X, L1 and R1 to R10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
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公开(公告)号：US20220033395A1
公开(公告)日：2022-02-03
申请号：US17238013
申请日：2021-04-22
发明人： Hans Hilpert , Sabine Kolczewski , Roland Humm , Theodor Stoll , Thorsten Muser , Jean-Marc Plancher , Delphine Gaufreteau
IPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D417/14 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D403/04
摘要： 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.
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公开(公告)号：US11098080B2
公开(公告)日：2021-08-24
申请号：US16006564
申请日：2018-06-12
发明人： Alexander Alanine , Julien Beignet , Konrad Bleicher , Bernhard Fasching , Hans Hilpert , Taishan Hu , Dwight MacDonald , Stephen Jackson , Sabine Kolczewski , Carsten Kroll , Adrian Schaeublin , Hong Shen , Theodor Stoll , Helmut Thomas , Amal Wahhab , Claudia Zampaloni
摘要： The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
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![Indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives](/abs-image/US/2019/08/20/US10385050B2/abs.jpg.150x150.jpg)
公开(公告)号：US10385050B2
公开(公告)日：2019-08-20
申请号：US16100181
申请日：2018-08-09
发明人： Hans Hilpert , Sabine Kolczewski , Anja Limberg , Theodor Stoll
IPC分类号： C07D471/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D411/12 , C07D413/14 , C07D417/14 , A61K31/416 , A61K31/4162 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/506 , C07D403/04 , A61K45/06
摘要： The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disorders
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公开(公告)号：US20180251451A1
公开(公告)日：2018-09-06
申请号：US15971399
申请日：2018-05-04
发明人： Delphine Gaufreteau , Hans Hilpert , Roland Humm , Sabine Kolczewski , Thorsten Muser , Jean-Marc Plancher , Theodor Stoll
IPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D498/04 , A61P25/32 , A61P25/36 , A61P25/28 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/16
CPC分类号： C07D403/14 , A61K31/506 , A61K45/06 , A61K2300/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D413/14 , C07D498/04
摘要： The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; 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, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co morbid epilepsy.
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公开(公告)号：US20180251450A1
公开(公告)日：2018-09-06
申请号：US15971368
申请日：2018-05-04
IPC分类号： C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , A61P25/32 , A61P25/36 , A61P25/28 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/16
CPC分类号： C07D403/14 , A61K45/06 , A61K2300/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/08 , C07D498/04
摘要： The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. 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, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.
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公开(公告)号：US11066393B2
公开(公告)日：2021-07-20
申请号：US16897879
申请日：2020-06-10
IPC分类号： C07D403/14 , C07D401/14 , A61P25/36 , A61P25/28 , A61P25/22 , A61P25/32 , A61P25/18 , A61P25/24 , A61P25/08 , A61P25/16 , A61K31/506 , C07D471/04 , A61K45/06
摘要： The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. 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, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.
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