公开(公告)号：US11066414B2

公开(公告)日：2021-07-20

申请号：US16717074

申请日：2019-12-17

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Gayatri Balan ,  Chien-Hung Chou ,  Christopher T. Clark ,  Jeromy J. Cottell ,  Musong Kim ,  Thorsten A. Kirschberg ,  John O. Link ,  Gary Phillips ,  Scott D. Schroeder ,  Neil H. Squires ,  Kirk L. Stevens ,  James G. Taylor ,  William J. Watkins ,  Nathan E. Wright ,  Sheila M. Zipfel

IPC: C07D401/14 ,  C07D498/04 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07B59/00

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

公开(公告)号：US10774071B2

公开(公告)日：2020-09-15

申请号：US16510647

申请日：2019-07-12

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Aesop Cho ,  Michael Graupe ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Devan Naduthambi ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC: C07D401/14 ,  C07D471/08 ,  A61K31/444 ,  A61K31/497 ,  A61K31/704 ,  A61K31/7068 ,  A61K39/395 ,  A61P31/20

Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

公开(公告)号：US10710986B2

公开(公告)日：2020-07-14

申请号：US16274106

申请日：2019-02-12

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Aesop Cho ,  Zhimin Du ,  Michael Graupe ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Prasenjit Kumar Mukherjee ,  Devan Naduthambi ,  Eric Q. Parkhill ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Neil H. Squires ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC: C07D403/14 ,  A61P31/20 ,  A61P35/02 ,  A61K31/496 ,  C07D519/00 ,  C07D241/20 ,  C07D487/10 ,  C07D405/14 ,  C07D487/08 ,  A61K31/497 ,  C07D491/107 ,  C07D241/18 ,  A61P35/00 ,  C07K16/28

Abstract: Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

公开(公告)号：US10479770B2

公开(公告)日：2019-11-19

申请号：US15711875

申请日：2017-09-21

Applicant: Gilead Sciences, Inc.

Inventor： Jayaraman Chandrasekhar ,  Devan Naduthambi ,  Leena Patel ,  Stephane Perreault ,  Gary Phillips ,  Kassandra F. Sedillo ,  Nicholas Alexander Till ,  Jennifer Anne Treiberg ,  William J. Watkins ,  Julian A. Codelli ,  Joshua J. Van Veldhuizen

IPC: C07D235/08 ,  C07D413/14 ,  C07D413/04 ,  A61K31/4184 ,  A61K31/5377 ,  A61P35/02 ,  A61P35/04 ,  A61K45/06

Abstract: The present application provides the compounds of formula I or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein t, R1, R2, R3, R4, and R6 are as described herein.

公开(公告)号：US20170298068A1

公开(公告)日：2017-10-19

申请号：US14971825

申请日：2015-12-16

Applicant: Gilead Sciences, Inc.

Inventor： CHRISTIAN GEGE ,  Claus Kremoser ,  Olaf Kinzel ,  Peter A. Blomgren ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Aaron C. Schmitt ,  William J. Watkins ,  Jianjun Xu

IPC: C07D471/08 ,  C07D413/12 ,  C07D261/08 ,  C07D401/14 ,  C07D417/14 ,  C07D413/14

CPC classification number: C07D471/08 ,  C07D261/08 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US20170008873A1

公开(公告)日：2017-01-12

申请号：US15199779

申请日：2016-06-30

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Gayatri Balan ,  Chien-Hung Chou ,  Christopher T. Clark ,  Jeromy J. Cottell ,  Musong Kim ,  Thorsten A. Kirschberg ,  John O. Link ,  Gary Phillips ,  Scott D. Schroeder ,  Neil H. Squires ,  Kirk L. Stevens ,  James G. Taylor ,  William J. Watkins ,  Nathan E. Wright ,  Sheila M. Zipfel

IPC: C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D409/14 ,  C07F7/08 ,  C07D453/02 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07F7/0814

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

Abstract translation: 本公开一般涉及Cot（癌症大阪甲状腺）的调节剂及其使用和制造方法。

公开(公告)号：US20160096827A1

公开(公告)日：2016-04-07

申请号：US14863108

申请日：2015-09-23

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  Juan A. Guerrero ,  Joshua A. Kaplan ,  John E. Knox, JR. ,  Jennifer R. Lo ,  Scott A. Mitchell ,  Devan Naduthambi ,  Barton W. Phillips ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  William J. Watkins ,  Zhongdong Zhao

IPC: C07D405/12 ,  C07D405/14 ,  A61K31/53 ,  C07D403/14 ,  C07D409/14 ,  A61K31/5383 ,  A61K31/5377 ,  C07D417/14 ,  C07D491/107 ,  C07D471/10 ,  C07D413/14 ,  C07D498/04 ,  A61K31/541 ,  C07D403/12

CPC classification number: C07D405/12 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/541 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04

Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:

公开(公告)号：US20150361095A1

公开(公告)日：2015-12-17

申请号：US14735939

申请日：2015-06-10

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  Jerry Evarts ,  Joshua Kaplan ,  Musong Kim ,  Devan Naduthambi ,  Leena Patel ,  Stephane Perreault ,  Barton W. Phillips ,  Gary Phillips ,  Kirk L. Stevens ,  Jennifer A. Treiberg ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC: C07D513/04 ,  C07D473/34 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D513/04 ,  C07D239/91 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D473/34 ,  C07D487/04

Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A′, W1, W2, W3, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Abstract translation: 本申请提供式（J）化合物或其药学上可接受的盐，异构体或其混合物，其中n，m，q，A'，W 1，W 2，W 3，R 1，R 2和R 3在本文中描述。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US20150361054A1

公开(公告)日：2015-12-17

申请号：US14735254

申请日：2015-06-10

Applicant: Gilead Sciences, Inc.

Inventor： Shaopei Cai ,  Zhimin Du ,  Joshua Kaplan ,  Jennifer A. Loyer-Drew ,  Devan Naduthambi ,  Barton W. Phillips ,  Gary Phillips ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC: C07D239/90 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D403/14 ,  C07D513/04

CPC classification number: A61K31/496 ,  C07D239/04 ,  C07D239/80 ,  C07D239/90 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D513/04

Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Abstract translation: 本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中W，B，n，m，A'，R 1，R 2和R 3在本文中描述。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US20230295111A1

公开(公告)日：2023-09-21

申请号：US18297316

申请日：2023-04-07

Applicant: Gilead Sciences, Inc.

Inventor： Gayatri Balan ,  Peter A. Blomgren ,  Chen Chen ,  Julian A. Codelli ,  Zhimin Du ,  Musong Kim ,  Dorothée Saddier Axe ,  Gregg M. Schwarzwalder ,  Rhiannon Thomas-Tran ,  Michael T. Tudesco ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Brian M. Weist ,  Suet C. Yeung ,  Helen Yu

IPC: C07D401/04

CPC classification number: C07D401/04 ,  C07B2200/05

Abstract: The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.