公开(公告)号：US20180118680A1

公开(公告)日：2018-05-03

申请号：US15851322

申请日：2017-12-21

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/14 ,  C07D417/12 ,  C07D403/12 ,  C07D451/02 ,  C07D405/14 ,  C07D401/14 ,  C07D491/048 ,  C07D401/12

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US09855269B2

公开(公告)日：2018-01-02

申请号：US15454793

申请日：2017-03-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Nbdubaku ,  Lan Wang

IPC: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The invention provides a method of inhibiting angiogenesis in a patient by administering a compound of formula (I): wherein R1 R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US20170008877A1

公开(公告)日：2017-01-12

申请号：US15200058

申请日：2016-07-01

Applicant: Genentech, Inc.

Inventor： Snahel PATEL ,  Gregory HAMILTON ,  Craig Stivala ,  Huifen Chen ,  Guiling Zhao

IPC: C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D498/04 ,  C07D491/044 ,  C07D413/14 ,  C07D491/048 ,  C07D413/12 ,  C07D491/052

CPC classification number: C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D491/10 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

Abstract translation: 其中R1，X，Z1，L，n，A环，B环和C环如本文所述，包括该化合物的药物组合物和使用该化合物的方法。

公开(公告)号：US09440976B2

公开(公告)日：2016-09-13

申请号：US14743835

申请日：2015-06-18

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  C07D453/02 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US09382257B2

公开(公告)日：2016-07-05

申请号：US14688724

申请日：2015-04-16

Applicant: Genentech, Inc.

Inventor： Daniel Burdick ,  Huifen Chen ,  Shumei Wang ,  Weiru Wang

IPC: A61K31/4985 ,  C07D231/10 ,  C07D241/38 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K45/06

Abstract: Compounds having the formula I wherein R1 and R2 are as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中R 1和R 2如本文所定义，是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：US09382241B2

公开(公告)日：2016-07-05

申请号：US13906626

申请日：2013-05-31

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC: C07D471/04 ,  C07D239/94 ,  C07D403/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D239/95 ,  C07D413/12

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract translation: 本发明提供具有以下通式的新化合物：其中A，R 1，R 2和R 3如本文所定义，包括该化合物的组合物和使用该化合物的方法。

公开(公告)号：US20150368244A1

公开(公告)日：2015-12-24

申请号：US14137972

申请日：2013-12-20

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Charles Goodacre ,  Joseph P. Lyssikatos ,  Calum MacLeod ,  Karen Williams ,  Huifen Chen

IPC: C07D471/14 ,  A61K31/496 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D471/14 ,  A61K31/496 ,  A61K31/519 ,  A61K45/06

Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及有用的式（I），（Ia），（Ib），（Ic），（Id），（Ie），（If），（Ig）和（Ih）的1,5-二氮杂咔唑化合物 作为激酶抑制剂，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US20130261104A1

公开(公告)日：2013-10-03

申请号：US13890949

申请日：2013-05-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  C07D513/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/541 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4375 ,  C07D491/107

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

公开(公告)号：US20130096102A1

公开(公告)日：2013-04-18

申请号：US13712015

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Mark Chambers ,  Bryan K. Chan ,  Huifen Chen ,  Anthony Estrada ,  Janet Gunzner-Toste ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: C07D413/14 ,  C07D498/08 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D403/14 ,  C07D413/12 ,  C07D473/16 ,  C07D498/06 ,  C07D498/08

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 5，R 6和R 7如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US12281101B2

公开(公告)日：2025-04-22

申请号：US17198238

申请日：2021-03-10

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Craig Stivala ,  Huifen Chen ,  Guiling Zhao

IPC: C07D403/12 ,  A61K31/55 ,  A61K31/553 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/06 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D491/10 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D498/16 ,  C07D519/00

Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.