公开(公告)号：US11129832B2

公开(公告)日：2021-09-28

申请号：US16666273

申请日：2019-10-28

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Liting Dong ,  Kevin X. Chen ,  Paul Gibbons ,  Malcolm Huestis ,  Terry Kellar ,  Wen Liu ,  Changyou Ma ,  Joseph P. Lyssikatos ,  Alan G. Olivero ,  Snahel Patel ,  Daniel Shore ,  Michael Siu

IPC: C07D471/08 ,  A61K31/506 ,  A61K45/06 ,  A61K31/5386 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  A61K35/30 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  A61K31/553 ,  C07D417/14 ,  C07D487/14 ,  C07D487/18 ,  A61K31/444

Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.

公开(公告)号：US10675367B2

公开(公告)日：2020-06-09

申请号：US16050453

申请日：2018-07-31

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

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：US20160060262A1

公开(公告)日：2016-03-03

申请号：US14928973

申请日：2015-10-30

Applicant: Genentech, Inc.

Inventor： Joseph P. Lyssikatos ,  Lewis J. Gazzard ,  Emily Hanan ,  Samuel S. Kintz ,  Hans Edward Purkey

IPC: C07D471/04 ,  C07D417/04 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D217/22 ,  C07D401/12

CPC classification number: C07D471/04 ,  A61K31/47 ,  A61K31/4725 ,  C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04

Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.

Abstract translation: 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。

公开(公告)号：US20150328195A1

公开(公告)日：2015-11-19

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

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：US20190201561A1

公开(公告)日：2019-07-04

申请号：US16050453

申请日：2018-07-31

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07D487/04 ,  C07B59/00

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

公开(公告)号：US09580411B2

公开(公告)日：2017-02-28

申请号：US14671643

申请日：2015-03-27

Applicant: Hoffmann-La Roche Inc. ,  GENENTECH, INC.

Inventor： Christine E. Brotherton-Pleiss ,  Huifen Chen ,  Shaoqing Chen ,  Zhi Chen ,  Shawn David Erickson ,  Anthony Estrada ,  Kyungjin Kim ,  Hongju Li ,  Allen John Lovey ,  Joseph P. Lyssikatos ,  Yimin Qian ,  Sung-Sau So ,  Peter Michael Wovkulich ,  Lin Yi

IPC: C07D305/08 ,  C07D409/12 ,  C07D231/18 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D237/08 ,  C07D239/42 ,  C07D409/14 ,  C07D241/12 ,  C07D213/26 ,  C07D213/40 ,  C07C311/19 ,  C07C311/16 ,  C07C311/17 ,  C07C311/20 ,  C07D239/26 ,  C07D305/06 ,  C07D403/12

CPC classification number: C07D409/12 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/20 ,  C07C2601/02 ,  C07D213/26 ,  C07D213/40 ,  C07D231/18 ,  C07D237/08 ,  C07D239/26 ,  C07D239/42 ,  C07D241/12 ,  C07D305/06 ,  C07D305/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/14

Abstract: The invention is concerned with the compounds of formula (I): and salts thereof, wherein X, Y, Z, R1, R2, R3, R3′, R4, R5 and R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract translation: 本发明涉及式（I）化合物及其盐，其中X，Y，Z，R 1，R 2，R 3，R 3，R 4，R 5和R 6在详细说明书和权利要求书中定义。 此外，本发明涉及制备和使用式（I）化合物的方法以及含有这些化合物的药物组合物。 该化合物可用于治疗TRPA1介导的疾病和病症，例如疼痛。

公开(公告)号：US20150175619A1

公开(公告)日：2015-06-25

申请号：US14576890

申请日：2014-12-19

Applicant: Genentech, Inc.

Inventor： Michael Siu ,  Anthony Estrada ,  Wen Liu ,  Joseph P. Lyssikatos ,  Snahel Patel ,  Guibai Liang ,  Kevin Chen

IPC: C07D491/107 ,  C07D401/04 ,  C07D491/08 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D407/14

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention provides for compounds of formula 0 and various embodiments thereof, and compositions comprising compounds of formula 0 and various embodiments thereof. In compounds of formula 0, the groups R1A, R1B, R1C, R1D, R2, R3, R4, R5 and R6 have the meaning as described herein. The present invention also provides for methods of using compounds of formula 0 and compositions comprising compounds of formula 0 as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract translation: 本发明提供式0化合物及其各种实施方案，以及包含式0化合物及其各种实施方案的组合物。 在式0的化合物中，基团R1A，R1B，R1C，R1D，R2，R3，R4，R5和R6具有如本文所述的含义。 本发明还提供使用式0化合物和包含式0化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症的方法。

公开(公告)号：US20200297875A1

公开(公告)日：2020-09-24

申请号：US16895352

申请日：2020-06-08

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

公开(公告)号：US20200002345A1

公开(公告)日：2020-01-02

申请号：US16561432

申请日：2019-09-05

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. 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 a Janus kinase activity in a patient are disclosed.