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：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.

公开(公告)号：US11014909B2

公开(公告)日：2021-05-25

申请号：US16880632

申请日：2020-05-21

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: A61K31/513 ,  A61K31/506 ,  A61K31/501 ,  A61K31/444 ,  A61P25/18 ,  A61P25/28 ,  A61P25/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  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), Parkinson's disease and chronic apathy.

公开(公告)号：US20190367485A1

公开(公告)日：2019-12-05

申请号：US16539865

申请日：2019-08-13

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 ,  C07D403/12 ,  A61K31/513 ,  A61K31/501 ,  A61K31/506 ,  A61K31/444 ,  C07D405/14 ,  C07D401/12

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), and Parkinson's disease.

公开(公告)号：US10426135B2

公开(公告)日：2019-10-01

申请号：US16268857

申请日：2019-02-06

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand Jal Unwalla

IPC: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  A01K5/01 ,  B65D77/20 ,  B65D25/04 ,  B65D1/34 ,  A01K7/00 ,  A23K20/00 ,  A23K50/48 ,  B65D1/36 ,  B65D25/18 ,  B65D85/00

Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

公开(公告)号：US10316021B2

公开(公告)日：2019-06-11

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 ,  C07D231/20 ,  C07D413/04 ,  C07D417/04 ,  A61P25/00

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：US09688698B2

公开(公告)日：2017-06-27

申请号：US14694039

申请日：2015-04-23

Applicant: PFIZER INC.

Inventor： David Lawrence Firman Gray ,  Lei Zhang ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  Scot Richard Mente ,  Chakrapani Subramanyam

IPC: C07D495/14 ,  C07D519/00 ,  C07D471/04 ,  C07D491/147 ,  C07D513/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  C07D491/048 ,  C07D495/04 ,  A61K31/4985

CPC classification number: C07D519/00 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  C07D471/04 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D495/14 ,  C07D513/04

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：US09133190B2

公开(公告)日：2015-09-15

申请号：US14339123

申请日：2014-07-23

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: A61K31/437 ,  C07D471/04 ,  C07D401/04 ,  C07D401/14

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.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐和上述的N-氧化物; 制备过程; 中间体用于制备; 和含有这些化合物，盐或N-氧化物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，认知障碍相关 精神分裂症，AD，PD或药物治疗），ADHD，冲动，强迫性赌博，暴饮暴食，孤独症谱系障碍，MCI，年龄相关认知衰退，痴呆，RLS，帕金森病，亨廷顿舞蹈病，焦虑，抑郁，MDD，TRD 和双相情感障碍。

公开(公告)号：US20190387710A1

公开(公告)日：2019-12-26

申请号：US16563022

申请日：2019-09-06

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand Jal Unwalla

IPC: A01K5/01 ,  B65D25/18 ,  B65D25/04 ,  B65D1/36 ,  B65D1/34 ,  A01K7/00 ,  B65D77/20 ,  A23K20/00 ,  A23K50/48 ,  C07D471/04 ,  C07D401/14

Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

公开(公告)号：US10421744B2

公开(公告)日：2019-09-24

申请号：US16123072

申请日：2018-09-06

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 ,  C07D405/14 ,  A61K31/444 ,  A61K31/606 ,  A61K31/513 ,  A61K31/501 ,  A61P25/18 ,  A61P25/28 ,  A61K31/506

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), and Parkinson's disease.