公开(公告)号：US09192612B2

公开(公告)日：2015-11-24

申请号：US14694288

申请日：2015-04-23

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC: A61K31/542 ,  C07D513/04

CPC classification number: A61K31/542 ,  C07D513/04

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 variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09139561B2

公开(公告)日：2015-09-22

申请号：US14638608

申请日：2015-03-04

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: C07D401/12 ,  C07D403/12 ,  A61K31/506 ,  A61K31/444 ,  A61P25/18

CPC classification number: C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  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), age-related cognitive decline, dementia, and Parkinson's disease.

公开(公告)号：US20150224110A1

公开(公告)日：2015-08-13

申请号：US14694288

申请日：2015-04-23

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC: A61K31/542

CPC classification number: A61K31/542 ,  C07D513/04

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 variables R1 and R2 are 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和R2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。

公开(公告)号：US20140323474A1

公开(公告)日：2014-10-30

申请号：US14325409

申请日：2014-07-08

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC: C07D513/04

CPC classification number: A61K31/542 ,  C07D513/04

Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 本发明提供式I化合物及其互变异构体，以及化合物和互变异构体的药学上可接受的盐，其中化合物具有其中变量R1，R2，R3，R4和x如说明书中所定义的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20130296308A1

公开(公告)日：2013-11-07

申请号：US13886405

申请日：2013-05-03

Applicant: PFIZER INC.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC: C07D513/04

CPC classification number: C07D513/04 ,  A61K31/542

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US11964961B2

公开(公告)日：2024-04-23

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: C07D401/12 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  C07D401/14 ,  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：US20230192654A1

公开(公告)日：2023-06-22

申请号：US17969479

申请日：2022-10-19

Applicant: PFIZER, INC.

Inventor： Lei Zhang ,  Erik Alphie LaChapelle ,  Christopher Ryan Butler ,  Natasha Mariam Kablaoui ,  Michael Aaron Brodney ,  Laura Ann McAllister ,  Qingyi Yang ,  Christopher John Helal ,  Damien Webb

IPC: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

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: X1, X2, R1, R2, m and n 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, Parkinson's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US11312713B2

公开(公告)日：2022-04-26

申请号：US16492558

申请日：2018-03-06

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Thomas Allen Chappie ,  Jinshan Michael Chen ,  Jotham Wadsworth Coe ,  Karen Jean Coffman ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Christopher John Helal ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Luis Angel Martinez-Alsina ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Colin Richard Rose ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Joseph Scott Warmus ,  Yuan Zhang

IPC: C07D471/04

Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 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.

公开(公告)号：US11198692B2

公开(公告)日：2021-12-14

申请号：US16625202

申请日：2018-06-14

Applicant: Pfizer Inc.

Inventor： Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Christopher Ryan Butler ,  Adam Matthew Gilbert ,  Erik Alphie Lachapelle ,  Laura Ann McAllister ,  Daniel Paul Uccello ,  Lei Zhang

IPC: C07D471/04

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)a, (R2)b, (R3)c, 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：US10253042B2

公开(公告)日：2019-04-09

申请号：US15678511

申请日：2017-08-16

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill

IPC: A01N43/00 ,  A61K31/553 ,  C07D498/04 ,  C07D498/10

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, R3, R4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.