公开(公告)号：US20190292203A1

公开(公告)日：2019-09-26

申请号：US16429678

申请日：2019-06-03

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Chistopher John Helal ,  Steven Victor O'Neil ,  Patrick Robert Verhoest

IPC: C07D513/10 ,  A61P37/00 ,  C07D498/10 ,  C07D493/10 ,  C07D471/10 ,  A61P3/00 ,  C07D221/20 ,  A61P35/00 ,  A61P25/00 ,  A61P9/00 ,  C07D401/12

Abstract: The present invention provides, in part, heterocyclic spiro 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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US10329308B2

公开(公告)日：2019-06-25

申请号：US15874987

申请日：2018-01-19

Applicant: PFIZER INC.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Christopher John Helal ,  Steven Victor O'Neil ,  Patrick Robert Verhoest

IPC: C07D513/10 ,  C07D221/20 ,  C07D295/185 ,  C07D401/08 ,  C07D401/12 ,  C07D491/10

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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US20190047997A1

公开(公告)日：2019-02-14

申请号：US16069585

申请日：2017-01-09

Applicant: Pfizer Inc.

Inventor： 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: C07D471/04

Abstract: 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：US10077269B2

公开(公告)日：2018-09-18

申请号：US15426423

申请日：2017-02-07

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

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：US20170305931A1

公开(公告)日：2017-10-26

申请号：US15646572

申请日：2017-07-11

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC: C07D513/04 ,  C07D513/20 ,  C07D513/10

CPC classification number: C07D513/04 ,  C07D513/10 ,  C07D513/20

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

公开(公告)号：US09751895B2

公开(公告)日：2017-09-05

申请号：US15272501

申请日：2016-09-22

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC: C07D513/04 ,  C07D513/10 ,  C07D513/20

CPC classification number: C07D513/04 ,  C07D513/10 ,  C07D513/20

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

公开(公告)号：US20170096428A1

公开(公告)日：2017-04-06

申请号：US15382778

申请日：2016-12-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/4985

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09328104B2

公开(公告)日：2016-05-03

申请号：US14093812

申请日：2013-12-02

Applicant: Pfizer Inc.

Inventor： James Thomas Anderson ,  Eugene Lvovich Piatnitski Chekler ,  Edmund L. Ellsworth ,  Bruce Kipp Erickson ,  Adam Matthew Gilbert ,  Anthony P. Ricketts ,  David P. Thompson ,  Rayomand Jal Unwalla ,  Patrick Robert Verhoest

IPC: C07D207/08 ,  C07D211/22 ,  C07D217/26 ,  C07D285/10 ,  C07D401/04 ,  C07D417/04 ,  C07C255/59 ,  C07C255/58 ,  C07D205/04

CPC classification number: C07D417/04 ,  C07C255/58 ,  C07C255/59 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D217/26 ,  C07D285/10 ,  C07D401/04

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or —(CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

Abstract translation: 本发明涉及式1,2或3的化合物：其中A是N或-CR 0-，其中R 0是氢，C 1 -C 6直链或支链烷基等，Z是-CRe-或 - N-，其中Re为氢，C1-C6直链或支链烷基等; R1是氢，C1-C6直链或支链烷基等; R2独立地为氢或C1-C6直链或支链烷基; R3和R4独立地是氢，C1-C6直链或支链烷基等; R5和R6独立地是氢或C1-C6直链或支链烷基等; R8是氢，C1-C6直链或支链烷基等; R9和R10独立地为氢或C1-C6直链或支链烷基等; Q是-CO - ， - （CH2）q-， - （CHRs）q-或 - （CRsRt）q-，其中Rs和Rt独立地是C1-C6直链或支链烷基，芳基，烷基芳基，杂芳基或烷基杂芳基 ; 其中q是0,1,2或3; 并且其中n为0,1,2,3,4或5; 或其药学上可接受的盐包含含有这些化合物的组合物; 以及这些化合物在治疗各种疾病，特别是受雄激素受体影响或介导的疾病的用途。

公开(公告)号：US20150366874A1

公开(公告)日：2015-12-24

申请号：US14840528

申请日：2015-08-31

Applicant: Pfizer Inc.

Inventor： 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: A61K31/5377

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: 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.

Abstract translation: 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。