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：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：US09434732B2

公开(公告)日：2016-09-06

申请号：US14049458

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D471/02 ,  C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

公开(公告)号：US20210277024A1

公开(公告)日：2021-09-09

申请号：US17156384

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Terry Kellar ,  Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D519/00 ,  C07D471/04 ,  A61P37/04

Abstract: Naphthyridine compounds of formula (I). variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US20210253580A1

公开(公告)日：2021-08-19

申请号：US17156387

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Joy Alison Drobnick ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  C07D487/14 ,  C07D498/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D498/04 ,  A61P37/04

Abstract: Isoquinoline compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

公开(公告)号：US10407424B2

公开(公告)日：2019-09-10

申请号：US15942321

申请日：2018-03-30

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Blake Daniels ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca

IPC: C07D471/04 ,  A61K31/55 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K45/06

Abstract: Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US10053451B2

公开(公告)日：2018-08-21

申请号：US15164102

申请日：2016-05-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Birong Zhang ,  Nicholas D. Smith ,  Steven P. Govek ,  Mehmet Kahraman ,  Andiliy G. Lai ,  Johnny Y. Nagasawa ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: C07D405/14 ,  A61K31/497 ,  A61K31/397 ,  C07D491/052 ,  A61K31/4162 ,  C07D405/12 ,  A61K31/4439 ,  A61K31/416 ,  C07D405/04

CPC classification number: C07D405/14 ,  A61K31/397 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/497 ,  C07D405/04 ,  C07D405/12 ,  C07D491/052

Abstract: Described herein are compounds that are estrogen receptor modulators. 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：US20140206702A1

公开(公告)日：2014-07-24

申请号：US14220409

申请日：2014-03-20

Applicant: Genentech, Inc.

Inventor： Yingjie Lai ,  Jun Liang ,  Steven R. Magnuson ,  Kirk D. Robarge ,  Vickie H. Tsui ,  Birong Zhang

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, Ra, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.

Abstract translation: 本发明提供式Ia-Ib的化合物，其立体异构体或其药学上可接受的盐，其中A，X，Ra，R 1，R 2，R 4，R 5和R 16如本文所定义，药物组合物包含式Ia-Ib的化合物和 药学上可接受的载体，佐剂或载体，以及在治疗中使用该化合物或组合物的方法。

公开(公告)号：US20140171408A1

公开(公告)日：2014-06-19

申请号：US14185700

申请日：2014-02-20

Applicant: Genentech, Inc.

Inventor： Toby Jonathan Blench ,  Charles Ellwood ,  Simon Charles Goodacre ,  Yingjie Lai ,  Jun Liang ,  Calum MacLeod ,  Steven R. Magnuson ,  Vickie Hsiao-Wei Tsui ,  Karen Williams ,  Birong Zhang

IPC: A61K31/5377 ,  C07D513/04 ,  A61K31/519 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506

CPC classification number: A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  C07D513/04

Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.

Abstract translation: 提供式I化合物，立体异构体，互变异构体，溶剂合物，前药和药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义，药物组合物包括式I化合物和药学上可接受的 载体，佐剂或载体，在治疗中使用化合物或组合物的方法，以及制备式I化合物的方法。

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.