公开(公告)号：US09751895B2

公开(公告)日：2017-09-05

申请号：US15272501

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 ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC: C07D513/04 ,  C07D513/10 ,  C07D513/20

CPC classification number: C07D513/04 ,  C07D513/10 ,  C07D513/20

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, R2 and R3 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：US09745317B2

公开(公告)日：2017-08-29

申请号：US15305384

申请日：2015-04-14

Applicant: PFIZER INC.

Inventor： David Lawrence Firman Gray ,  Lei Zhang ,  Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Ivan Viktorovich Efremov ,  Michael Eric Green ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers

IPC: C07D491/048 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

CPC classification number: C07D491/048 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

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), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

公开(公告)号：US20170151252A1

公开(公告)日：2017-06-01

申请号：US15427350

申请日：2017-02-08

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: A61K31/542

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.

公开(公告)号：US09540352B2

公开(公告)日：2017-01-10

申请号：US14694333

申请日：2015-04-23

Applicant: PFIZER INC.

Inventor： David Lawrence Firman Gray ,  Lei Zhang ,  Michael Aaron Brodney ,  Michael Eric Green ,  Chakrapani Subramanyam

IPC: A61K31/4375 ,  C07D221/04 ,  C07D403/12 ,  C07D471/04 ,  C07D401/12

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D471/04

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), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐; 制备过程; 中间体用于制备; 和含有这些化合物或盐的组合物及其用于治疗D1介导的（或D1相关）疾病的用途，包括例如精神分裂症（例如其认知和阴性症状），分裂型人格障碍，认知障碍（例如，认知障碍相关 精神分裂症，AD，PD或药物治疗），ADHD，帕金森病，焦虑和抑郁。

公开(公告)号：US09527843B2

公开(公告)日：2016-12-27

申请号：US14819541

申请日：2015-08-06

Applicant: PFIZER INC.

Inventor： Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Chakrapani Subramanyam ,  Lei Zhang

IPC: C07D401/14 ,  C07D401/04 ,  A61K31/437 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, 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, and bipolar disorder.

公开(公告)号：US09527831B2

公开(公告)日：2016-12-27

申请号：US14311963

申请日：2014-06-23

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 ,  C07D401/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/501 ,  A61K31/513

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.

Abstract translation: 及其药学上可接受的盐; 制备过程; 中间体用于制备; 和含有这些化合物或盐的组合物及其用于治疗D1介导的（或D1相关）疾病的用途，包括例如精神分裂症（例如，其认知和负面症状），认知障碍（例如，与精神分裂症相关的认知障碍，AD ，PD或药物治疗），ADHD，冲动性，强迫性赌博，暴饮暴食，孤独症谱系障碍，MCl，年龄相关认知衰退，痴呆，RLS，帕金森病，亨廷顿舞蹈症，焦虑症，抑郁症，MDD，TRD，双相情感障碍， 慢性冷漠，慢性疲劳，创伤后应激障碍，季节性情绪障碍，社会焦虑症，产后抑郁症，血清素综合征，药物滥用和毒品依赖，药物滥用复发，Tourette综合征，迟发性运动障碍，嗜睡，白天过度 嗜睡，恶病质，注意力不集中，性功能障碍，偏头痛，SLE，高血糖症，动脉粥样硬化，血脂异常，肥胖，糖尿病，败血症，缺血后小管 坏死，肾衰竭，低钠血症，抗性水肿，发作性睡病，高血压，充血性心力衰竭，术后眼睛低血压，睡眠障碍和疼痛。

公开(公告)号：US20150366874A1

公开(公告)日：2015-12-24

申请号：US14840528

申请日：2015-08-31

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Antonia Friederike Stepan ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 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.

Abstract translation: 本发明提供了式I的新的4,5-二取代的-7H-吡咯并[2,3-d]嘧啶衍生物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义。 本发明还涉及包含式I化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森病或阿尔茨海默病，神经变性疾病或克罗恩病或麻风病的神经变性疾病。

公开(公告)号：US09107923B2

公开(公告)日：2015-08-18

申请号：US14638677

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 ,  A61K31/513 ,  A61K31/501

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.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐; 制备过程; 中间体用于制备; 和含有这些化合物或盐的组合物及其用于治疗D1介导的（或D1相关）疾病的用途，包括例如精神分裂症（例如，其认知和负面症状），认知障碍（例如，与精神分裂症相关的认知障碍，AD ，PD或药物治疗），年龄相关的认知衰退，痴呆和帕金森病。