公开(公告)号：US20160304450A1

公开(公告)日：2016-10-20

申请号：US14972333

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: C07D205/04 ,  A61K31/404 ,  A61K45/06 ,  A61K31/397 ,  C07D207/04 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D413/12 ,  A61K31/422 ,  C07D417/12 ,  A61K31/427 ,  C07D401/14 ,  A61K31/4439 ,  C07D411/12 ,  C07D403/12

CPC classification number: C07D205/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/416 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5415 ,  A61K45/06 ,  C07D207/04 ,  C07D207/08 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12 ,  C07D403/14 ,  C07D409/02 ,  C07D409/12 ,  C07D411/02 ,  C07D411/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  A61K2300/00

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US12233052B2

公开(公告)日：2025-02-25

申请号：US17185319

申请日：2021-02-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li

IPC: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04 ,  A61P5/30 ,  A61P35/00 ,  A61P43/00

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20230045776A9

公开(公告)日：2023-02-09

申请号：US17185319

申请日：2021-02-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US10399939B2

公开(公告)日：2019-09-03

申请号：US15345958

申请日：2016-11-08

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg

IPC: C07D205/04 ,  A61K31/397 ,  A61K31/40 ,  A61K45/06 ,  C07D207/06 ,  C07D401/12 ,  C07D405/12

Abstract: Described herein are tetrahydronaphthalene compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US09845291B2

公开(公告)日：2017-12-19

申请号：US14972333

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: A61K31/397 ,  C07D205/04 ,  C07D403/12 ,  A61K31/404 ,  A61K45/06 ,  C07D207/04 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D413/12 ,  A61K31/422 ,  C07D417/12 ,  A61K31/427 ,  C07D401/14 ,  A61K31/4439 ,  C07D411/12

CPC classification number: C07D205/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/416 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5415 ,  A61K45/06 ,  C07D207/04 ,  C07D207/08 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12 ,  C07D403/14 ,  C07D409/02 ,  C07D409/12 ,  C07D411/02 ,  C07D411/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  A61K2300/00

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20170320871A1

公开(公告)日：2017-11-09

申请号：US15481757

申请日：2017-04-07

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Maia Vinogradova ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Tao Wang

IPC: C07D471/04 ,  C07D401/14 ,  A61K31/55 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/4745 ,  C07D403/12 ,  C07D401/12

CPC classification number: C07D471/04 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituent and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20160175284A1

公开(公告)日：2016-06-23

申请号：US14972336

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Li ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith

IPC: A61K31/4025 ,  C07D401/12 ,  A61K31/4184 ,  C07D401/14 ,  A61K31/404 ,  A61K45/06 ,  A61K31/397

CPC classification number: A61K31/4025 ,  A61K31/397 ,  A61K31/404 ,  A61K31/4184 ,  A61K45/06 ,  C07D311/14 ,  C07D401/12 ,  C07D401/14

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula I: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract translation: 本文描述的是作为式I的雌激素受体调节剂的化合物：及其立体异构体，互变异构体或其药学上可接受的盐，以及本文所述的取代基和结构特征。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这种雌激素受体调节剂单独使用并与其它化合物联合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

公开(公告)号：US20140194408A1

公开(公告)日：2014-07-10

申请号：US14207966

申请日：2014-03-13

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: C07D513/04 ,  A61K31/4985 ,  C07D487/04 ,  C07D495/04 ,  A61K31/496 ,  A61K31/5377 ,  C07D471/14 ,  A61K31/5025 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/506 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/53 ,  A61K31/501 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供式I的杂芳基吡啶酮和氮杂 - 吡啶酮化合物，其中X1，X2和X3中的一个或两个为N，并且包括可用于抑制Btk激酶和用于治疗免疫疾病的立体异构体，互变异构体及其药学上可接受的盐 例如由Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US20130116246A1

公开(公告)日：2013-05-09

申请号：US13667126

申请日：2012-11-02

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: C07D498/04 ,  A61K31/502 ,  A61K45/06 ,  A61K31/5377 ,  C07D487/04 ,  A61K31/5383 ,  C07D401/14 ,  C07D413/14

CPC classification number: A61K31/506 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供其中X 1，X 2和X 3中的一个或两个为N的式II的8-氟酞嗪-1（2h） - 酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐， 治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式II化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理条件中的这些病症的治疗的方法。

公开(公告)号：US20130116235A1

公开(公告)日：2013-05-09

申请号：US13667133

申请日：2012-11-02

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: C07D487/04 ,  A61K45/06 ,  C07D495/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/53 ,  C07D519/00 ,  A61K31/5025 ,  C07D498/04 ,  A61K31/5383 ,  C07D471/14 ,  A61K31/506 ,  A61K31/4985 ,  C07D495/14

CPC classification number: A61K31/4985 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供式I的杂芳基吡啶酮和氮杂 - 吡啶酮化合物，其中X1，X2和X3中的一个或两个为N，并且包括可用于抑制Btk激酶和用于治疗免疫疾病的立体异构体，互变异构体及其药学上可接受的盐 例如由Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。