公开(公告)号：US10328082B2

公开(公告)日：2019-06-25

申请号：US15314574

申请日：2015-05-18

Applicant: Pfizer Inc.

Inventor： Eugene Lvovich Piatnitski Chekler ,  Adam Matthew Gilbert ,  Rayomand Jal Unwalla ,  Patrick Robert Verhoest ,  James Thomas Anderson

IPC: A61K31/549 ,  A61K45/06 ,  A61K31/277 ,  A61K31/397 ,  A61K31/402 ,  A61K31/433 ,  A61K31/451 ,  A61K31/472 ,  A61K31/4725

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, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

公开(公告)号：US20180002331A1

公开(公告)日：2018-01-04

申请号：US15637071

申请日：2017-06-29

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US20140155390A1

公开(公告)日：2014-06-05

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: C07D417/04 ,  C07C255/59

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-， - （CH 2）q - ， - （CHRs）q-或（CRsRt）q-，其中R 5和R 5独立地是C 1 -C 6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。