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![3,4-disubstituted-1 H-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazines as LRRK2 inhibitors](/abs-image/US/2017/07/04/US09695171B2/abs.jpg.150x150.jpg)
公开(公告)号：US09695171B2
公开(公告)日：2017-07-04
申请号：US15104659
申请日：2014-12-03
Applicant: Pfizer Inc.
Inventor： Paul Galatsis , Matthew Merrill Hayward , Bethany Lyn Kormos , Travis T. Wager , Lei Zhang , Jaclyn Louise Henderson , Ravi G. Kurumbail , Patrick Robert Verhoest , Antonia Friederike Stepan
IPC: C07D471/04 , C07D487/04 , C07D519/00 , C07D491/08 , C07D498/08
CPC classification number: C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D519/00
Abstract: The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
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![N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides](/abs-image/US/2017/04/04/US09611264B1/abs.jpg.150x150.jpg)
12.发明授权公开(公告)号：US09611264B1
公开(公告)日：2017-04-04
申请号：US15272820
申请日：2016-09-22
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Patrick Robert Verhoest , Romelia del Carmen Salomon Ferrer
IPC: C07D417/14
CPC classification number: C07D417/14
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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![2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides](/abs-image/US/2017/03/28/US09605007B2/abs.jpg.150x150.jpg)
13.发明授权公开(公告)号：US09605007B2
公开(公告)日：2017-03-28
申请号：US15215193
申请日：2016-07-20
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D513/04 , C07D519/00
CPC classification number: A61K31/542 , C07D513/04 , C07D519/00
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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![2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides](/abs-image/US/2016/04/19/US09315520B2/abs.jpg.150x150.jpg)
14.发明授权2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides 有权2-氨基-6-甲基-4,4a，5,6-四氢吡喃并[3,4-d] [1,3]噻嗪-8a（8H） - 基-1,3-噻唑-4-基酰胺公开(公告)号：US09315520B2
公开(公告)日：2016-04-19
申请号：US14682151
申请日：2015-04-09
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D513/04
CPC classification number: A61K31/542 , C07D513/04 , C07D519/00
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Abstract translation: 本发明涉及所公开的化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有式I的结构，并且变量R1如说明书中所定义。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。
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![2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,3-Thiazol-4-yl Amides](/abs-image/US/2015/10/15/US20150291621A1/abs.jpg.150x150.jpg)
15.发明申请2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,3-Thiazol-4-yl Amides 审中-公开2-氨基-6-甲基-4,4a，5,6-四氢吡喃并[3,4-d] [1,3]噻唑-8a（8H） - 基] - 噻唑-4-基酰胺公开(公告)号：US20150291621A1
公开(公告)日：2015-10-15
申请号：US14682151
申请日：2015-04-09
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D513/04
CPC classification number: A61K31/542 , C07D513/04 , C07D519/00
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Abstract translation: 本发明涉及所公开的化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有式I的结构，并且变量R1如说明书中所定义。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。
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Patent Agency Ranking
公开(公告)号：US20240317713A1
公开(公告)日：2024-09-26
申请号：US18607834
申请日：2024-03-18
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Jennifer Elizabeth Davoren , Amy Beth Dounay , Ivan Viktorovich Efremov , David Lawrence Firman Gray , Michael Eric Green , Jaclyn Louise Henderson , Chewah Lee , Scot Richard Mente , Steven Victor O'Neil , Bruce Nelsen Rogers , Lei Zhang
IPC: C07D401/14 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/513 , A61P25/18 , A61P25/28 , C07D401/12 , C07D403/12 , C07D405/14
CPC classification number: C07D401/14 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/513 , A61P25/18 , A61P25/28 , C07D401/12 , C07D403/12 , C07D405/14
Abstract: The present invention provides, in part, compounds of Formula I:
and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, bipolar disorder, chronic apathy, anhedonia, chronic fatigue, post-traumatic stress disorder, seasonal affective disorder, social anxiety disorder, post-partum depression, serotonin syndrome, substance abuse and drug dependence, drug abuse relapse, Tourette's syndrome, tardive dyskinesia, drowsiness, excessive daytime sleepiness, cachexia, inattention, sexual dysfunction, migraine, SLE, hyperglycemia, atherosclerosis, dislipidemia, obesity, diabetes, sepsis, post-ischemic tubular necrosis, renal failure, hyponatremia, resistant edema, narcolepsy, hypertension, congestive heart failure, postoperative ocular hypotonia, sleep disorders, and pain.-
公开(公告)号：US20240190869A1
公开(公告)日：2024-06-13
申请号：US18532547
申请日：2023-12-07
Applicant: Pfizer Inc.
Inventor： Lei Zhang , Christopher Ryan Butler , Elizabeth Mary Beck , Michael Aaron Brodney , Matthew Frank Brown , Laura Ann McAllister , Erik Alphie LaChapelle , Adam Matthew Gilbert
IPC: C07D471/04 , A61K31/437 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28
CPC classification number: C07D471/04 , A61K31/437 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28
Abstract: The present invention provides, in part, compounds of Formula I:
or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.-
公开(公告)号：US20240150334A1
公开(公告)日：2024-05-09
申请号：US18482129
申请日：2023-10-06
Applicant: Pfizer Inc.
Inventor： Jan Antoinette Cusi Romero Adams , Bruce Michael Bechle , Jason Kenneth Dutra , Michelle Renee Garnsey , Xinjun Hou , Jisun Lee , Deane Milford Nason, II , Steven Victor O'Neil , Danica Antonia Rankic , Yang Wang , Ann Sorrentino Wright , Lei Zhang , Liying Zhang , David James Edmonds
IPC: C07D413/04 , C07D231/56 , C07D263/56 , C07D401/04 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04
CPC classification number: C07D413/04 , C07D231/56 , C07D263/56 , C07D401/04 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04
Abstract: Described herein are compounds of Formula I,
wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.-
公开(公告)号：US20210309659A1
公开(公告)日：2021-10-07
申请号：US17335666
申请日：2021-06-01
Applicant: PFIZER INC.
Inventor： Lei Zhang , Christopher Ryan Butler , Elizabeth Mary Beck , Michael Aaron Brodney , Matthew Frank Brown , Laura Ann McAllister , Erik Alphie LaChapelle , Adam Matthew Gilbert
IPC: C07D471/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , A61K31/437
Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
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公开(公告)号：US20210300899A1
公开(公告)日：2021-09-30
申请号：US17204095
申请日：2021-03-17
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Jennifer Elizabeth Davoren , Amy Beth Dounay , Ivan Viktorovich Efremov , David Lawrence Firman Gray , Michael Eric Green , Jaclyn Louise Henderson , Chewah Lee , Scot Richard Mente , Steven Victor O'Neil , Bruce Nelsen Rogers , Lei Zhang
IPC: C07D401/14 , C07D401/12 , C07D405/14 , A61P25/28 , A61P25/18 , A61K31/444 , A61K31/506 , A61K31/501 , A61K31/513 , C07D403/12
Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, bipolar disorder, chronic apathy, anhedonia, chronic fatigue, post-traumatic stress disorder, seasonal affective disorder, social anxiety disorder, post-partum depression, serotonin syndrome, substance abuse and drug dependence, drug abuse relapse, Tourette's syndrome, tardive dyskinesia, drowsiness, excessive daytime sleepiness, cachexia, inattention, sexual dysfunction, migraine, SLE, hyperglycemia, atherosclerosis, dislipidemia, obesity, diabetes, sepsis, post-ischemic tubular necrosis, renal failure, hyponatremia, resistant edema, narcolepsy, hypertension, congestive heart failure, postoperative ocular hypotonia, sleep disorders, and pain.
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