公开(公告)号：US20240238425A1

公开(公告)日：2024-07-18

申请号：US18541015

申请日：2023-12-15

Applicant: Pfizer Inc.

Inventor： Jan Antoinette Cusi Romero Adams ,  Yotam Ashkenazi ,  Matthew Frank Brown ,  Jason Kenneth Dutra ,  Michelle Renee Garnsey ,  Xinjun Hou ,  Jisun Lee ,  Yajing Lian ,  Deane Milford Nason, II ,  Steven Victor O'Neil ,  Amanda Brooke Pecora ,  Alistair Dean Richardson ,  Matthew Forrest Sammons ,  Yang Wang ,  Ann Sorrentino Wright ,  Jun Xiao ,  Lei Zhang ,  Liying Zhang

IPC: A61K47/55 ,  A61K45/06

CPC classification number: A61K47/55 ,  A61K45/06

Abstract: Described herein are 3-fluoro-4-hydroxybenzamide-containing inhibitors and/or degraders, and pharmaceutical compositions containing 3-fluoro-hydroxybenzamide-containing inhibitors and/or degraders. In some embodiments, the 3-fluoro-4-hydroxybenzamide-containing compounds of the disclosure can be used to treat a condition, for example, nonalcoholic fatty liver disease and nonalcoholic steatohepatitis.

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.

公开(公告)号：US09617275B2

公开(公告)日：2017-04-11

申请号：US14820611

申请日：2015-08-07

Applicant: PFIZER INC.

Inventor： 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: C07D491/048 ,  C07D491/04 ,  C07D495/04 ,  C07D519/04 ,  C07D519/00

CPC classification number: 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

Abstract: 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：US20240366598A1

公开(公告)日：2024-11-07

申请号：US18634154

申请日：2024-04-12

Applicant: Pfizer Inc.

Inventor： Kevin James Filipski ,  Matthew Forrest Sammons ,  Samuel Michael Levi ,  Yang Wang ,  Advaita Panchagnula ,  Yanfei Guan ,  Matthew Richard Reese ,  Luis Angel Martinez Alsina ,  Steven Victor O'Neil ,  Lei Zhang ,  Qifang Li ,  Ethan Lawrence Fisher ,  Danica Antonia Rankic

IPC: A61K31/506 ,  A61K31/403 ,  A61K31/4439 ,  A61K31/444 ,  A61P3/04 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, L1, T1, T2, T3, T4, t1, and t2 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and/or T2DM.

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：US10093655B2

公开(公告)日：2018-10-09

申请号：US15729111

申请日：2017-10-10

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 ,  A61K31/506 ,  A61K31/513 ,  A61P25/18 ,  A61P25/28 ,  A61K31/501

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：US10077272B2

公开(公告)日：2018-09-18

申请号：US15822493

申请日：2017-11-27

Applicant: PFIZER INC.

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

IPC: C07D471/04 ,  C07D491/048 ,  C07D498/04

CPC classification number: C07D491/048 ,  C07D471/04 ,  C07D498/04

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：US09868744B2

公开(公告)日：2018-01-16

申请号：US15305372

申请日：2015-04-13

Applicant: PFIZER INC.

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

IPC: C07D471/04 ,  C07D491/048 ,  C07D498/04

CPC classification number: C07D491/048 ,  C07D471/04 ,  C07D498/04

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：US20210309669A1

公开(公告)日：2021-10-07

申请号：US17260247

申请日：2019-07-10

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Steven Victor O'Neil

IPC: C07D491/107

Abstract: The present invention provides, in part, a compound selected from the group consisting of: 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-[(cyclopropylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-1; and 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-2, 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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, steatohepatitis [e.g. nonalcoholic Steatohepatitis (NASH)], stroke, or cancer.

公开(公告)号：US20200283407A1

公开(公告)日：2020-09-10

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: 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), Parkinson's disease and chronic apathy.