公开(公告)号：US20210188829A1

公开(公告)日：2021-06-24

申请号：US17126358

申请日：2020-12-18

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  Agustin Casimiro-Garcia ,  Xiayun Cheng ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D413/14 ,  A61K45/06 ,  A61P17/00

Abstract: The invention relates to benzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.

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：US09856263B2

公开(公告)日：2018-01-02

申请号：US15305390

申请日：2015-04-15

Applicant: PFIZER INC.

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

IPC: C07D487/04 ,  C07D519/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D519/00

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：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：US08822456B2

公开(公告)日：2014-09-02

申请号：US14101462

申请日：2013-12-10

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC: C07D513/04 ,  A61K31/542

CPC classification number: A61K31/542 ,  C07D513/04

Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 本发明提供式I化合物及其互变异构体，以及化合物和互变异构体的药学上可接受的盐，其中化合物具有其中变量R1，R2，R3，R4和x如说明书中所定义的结构。 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：US20240132477A1

公开(公告)日：2024-04-25

申请号：US18257136

申请日：2021-12-13

Applicant: PFIZER INC.

Inventor： Scott William Bagley ,  Agustin Casimiro Garcia ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: The invention relates to benzimidazoles of Formula (I)




and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.

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：US11661419B2

公开(公告)日：2023-05-30

申请号：US17126358

申请日：2020-12-18

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  Agustin Casimiro-Garcia ,  Xiayun Cheng ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D413/14 ,  A61P17/00 ,  A61K45/06

CPC classification number: C07D413/14 ,  A61K45/06 ,  A61P17/00

Abstract: The invention relates to benzimidazoles of Formula (I)




and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.

The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.

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.