公开(公告)号：US20150336962A1

公开(公告)日：2015-11-26

申请号：US14720323

申请日：2015-05-22

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-Wai Yuen

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

Abstract translation: 本文描述了式（00A）的化合物和用作Janus激酶抑制剂的方法。

公开(公告)号：US10966963B2

公开(公告)日：2021-04-06

申请号：US15955539

申请日：2018-04-17

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

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：US10654867B2

公开(公告)日：2020-05-19

申请号：US16565041

申请日：2019-09-09

Applicant: Genentech, Inc.

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

IPC: A61K31/4985 ,  A61K31/397 ,  C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  C07F7/18 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  A61K31/55

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US20200002353A1

公开(公告)日：2020-01-02

申请号：US16565041

申请日：2019-09-09

Applicant: Genentech, Inc.

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

IPC: C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  A61K31/55 ,  A61K31/4985 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  C07F7/18

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US20190337946A1

公开(公告)日：2019-11-07

申请号：US16515253

申请日：2019-07-18

Applicant: Genentech, Inc.

Inventor： Simon Charles Goodacre ,  Nicholas Charles Ray ,  Mark Edward Zak ,  Yun-Xing Cheng ,  Wei Li

IPC: C07D471/04 ,  C07D471/10

Abstract: Triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where R1a, R1b, R1c, R2, R3, R4 and R5 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by a JAK kinase in a patient.

公开(公告)号：US20190322661A1

公开(公告)日：2019-10-24

申请号：US16438135

申请日：2019-06-11

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-wai Yuen

IPC: C07D471/04 ,  C07D487/04 ,  C07D403/14 ,  A61K31/519 ,  C07D519/00 ,  A61P11/06

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US20190152970A1

公开(公告)日：2019-05-23

申请号：US16250879

申请日：2019-01-17

Applicant: Genentech, Inc.

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

IPC: C07D471/04 ,  A61K31/437 ,  A61K45/06

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：US20180002344A1

公开(公告)日：2018-01-04

申请号：US15623904

申请日：2017-06-15

Applicant: Genentech, Inc.

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

IPC: C07D495/04 ,  C07D491/048 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  A61K31/695 ,  A61K31/4355 ,  A61K31/55 ,  A61K31/4985 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/4365 ,  C07F7/18 ,  A61K45/06

CPC classification number: C07D495/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/55 ,  A61K31/695 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/048 ,  C07F7/1804

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US09604984B2

公开(公告)日：2017-03-28

申请号：US15139164

申请日：2016-04-26

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-Wei Yuen

IPC: C07D487/04 ,  A61K31/519 ,  A61P11/06 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

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.