公开(公告)号：US10421744B2

公开(公告)日：2019-09-24

申请号：US16123072

申请日：2018-09-06

申请人： PFIZER INC.

发明人： 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分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  A61K31/444 ,  A61K31/606 ,  A61K31/513 ,  A61K31/501 ,  A61P25/18 ,  A61P25/28 ,  A61K31/506

摘要： 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), and Parkinson's disease.

公开(公告)号：US09617275B2

公开(公告)日：2017-04-11

申请号：US14820611

申请日：2015-08-07

申请人： PFIZER INC.

发明人： Jotham Wadsworth Coe ,  John Arthur Allen ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Edward Raymond Guilmette ,  Anthony Richard Harris ,  Chris John Helal ,  Jaclyn Louise Henderson ,  Scot Richard Mente ,  Deane Milford Nason ,  Steven Victor O'Neil ,  Chakrapani Subramanyam ,  Wenjian Xu

IPC分类号： C07D491/048 ,  C07D491/04 ,  C07D495/04 ,  C07D519/04 ,  C07D519/00

CPC分类号： A61K31/53 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D519/04

摘要： The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

公开(公告)号：US10590128B2

公开(公告)日：2020-03-17

申请号：US16069585

申请日：2017-01-09

申请人： Pfizer Inc.

发明人： Thomas Allen Chappie ,  Jaclyn Louise Henderson ,  Joseph Michael Young ,  Travis T. Wager ,  Bethany Lyn Kormos ,  Nandini Chaturbhai Patel ,  Simone Sciabola ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Joseph Walter Tucker

IPC分类号： C07D471/04 ,  A61K31/55 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22

摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression.

公开(公告)号：US20190047997A1

公开(公告)日：2019-02-14

申请号：US16069585

申请日：2017-01-09

申请人： Pfizer Inc.

发明人： Thomas Allen Chappie ,  Jaclyn Louise Henderson ,  Joseph Michael Young ,  Travis T. Wager ,  Bethany Lyn Kormos ,  Nandini Chaturbhai Patel ,  Simone Sciabola ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Joseph Walter Tucker

IPC分类号： C07D471/04

摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression.

公开(公告)号：US09822097B2

公开(公告)日：2017-11-21

申请号：US15349075

申请日：2016-11-11

申请人： PFIZER INC.

发明人： 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分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/501 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： 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：US09527831B2

公开(公告)日：2016-12-27

申请号：US14311963

申请日：2014-06-23

申请人： PFIZER INC.

发明人： 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分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/501 ,  A61K31/513

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： 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.

摘要翻译： 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

申请人： Pfizer Inc.

发明人： 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分类号： A61K31/5377

CPC分类号： A61K31/5377 ,  C07D487/04 ,  C07D519/00

摘要： 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.

摘要翻译： 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

申请人： PFIZER INC.

发明人： 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分类号： C07D401/12 ,  C07D403/12 ,  A61K31/506 ,  A61K31/444 ,  A61K31/513 ,  A61K31/501

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20200283407A1

公开(公告)日：2020-09-10

申请号：US16880632

申请日：2020-05-21

申请人： Pfizer Inc.

发明人： 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分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  A61P25/28 ,  A61P25/18 ,  A61K31/444 ,  A61K31/506 ,  A61K31/501 ,  A61K31/513 ,  C07D403/12

摘要： 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), Parkinson's disease and chronic apathy.

公开(公告)号：US10696658B2

公开(公告)日：2020-06-30

申请号：US16539865

申请日：2019-08-13

申请人： Pfizer Inc.

发明人： 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分类号： C07D403/12 ,  C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  A61K31/501 ,  A61K31/444 ,  A61K31/506 ,  A61P25/18 ,  A61P25/28 ,  C07D405/14 ,  A61K31/513

摘要： 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), and Parkinson's disease.