公开(公告)号：US09067934B2

公开(公告)日：2015-06-30

申请号：US14053924

申请日：2013-10-15

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Benjamin Adam Fish ,  Michael Eric Green ,  Patrick Bradley Mullins ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Thayalan Navaratnam

IPC: C07D471/04 ,  C07D401/04 ,  A61K31/4985 ,  A61K31/695 ,  A61K45/06 ,  C07D491/048 ,  C07F7/08

CPC classification number: C07D471/04 ,  A61K31/4985 ,  A61K31/695 ,  A61K45/06 ,  C07D401/04 ,  C07D491/048 ,  C07F7/0812

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

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如本文所定义的式I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：US20180148432A1

公开(公告)日：2018-05-31

申请号：US15820679

申请日：2017-11-22

Applicant: Pfizer Inc.

Inventor： Natasha Mariam Kablaoui ,  Michael Eric Green ,  Justin Ian Montgomery ,  Michael Aaron Brodney ,  Patrick Robert Verhoest ,  Gregory Wayne Kauffman ,  Danica Antonia Rankic ,  Scot Richard Mente ,  Bruce Nelsen Rogers ,  Kapildev Kashmirilal Arora ,  Matthew Francis Dunn

IPC: C07D403/04 ,  C07D417/04 ,  A61P25/00 ,  C07D231/20 ,  C07D413/04

CPC classification number: C07D403/04 ,  A61P25/00 ,  C07B2200/13 ,  C07D231/20 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R9, X, m and n 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 kappa opioid (κ-opioid) associated disorders including, e.g., a neurological disorder, or psychiatric disorder such as a neurocognitive disorder, substance abuse disorder, depressive disorder, anxiety disorder, trauma and stressor related disorder and feeding and eating disorder.

公开(公告)号：US09850232B2

公开(公告)日：2017-12-26

申请号：US15077229

申请日：2016-03-22

Applicant: PFIZER INC.

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

IPC: 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.

公开(公告)号：US09822097B2

公开(公告)日：2017-11-21

申请号：US15349075

申请日：2016-11-11

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 ,  C07D403/12 ,  A61K31/501 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  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.

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：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：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：US09193726B2

公开(公告)日：2015-11-24

申请号：US14543020

申请日：2014-11-17

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D241/36 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds 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.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I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：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。

公开(公告)号：US08916564B2

公开(公告)日：2014-12-23

申请号：US14031163

申请日：2013-09-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: A61K31/4985 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds 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.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I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。