公开(公告)号：US20140336170A1

公开(公告)日：2014-11-13

申请号：US14338816

申请日：2014-07-23

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Xuqing Zhang ,  Marta C. Abad ,  Alan C. Gibbs ,  Gee-Hong Kuo ,  Fengbin Song ,  Zhihua Sui

IPC: C07D491/08 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D491/08 ,  C07D231/56 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10

Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.

Abstract translation: 本发明涉及取代的吲唑化合物，这些化合物的药物组合物及其使用方法。 本发明的化合物是用于治疗或改善KHK介导的代谢紊乱和/或疾病如肥胖，II型糖尿病和代谢综合征X的酮基己糖激酶（KHK）抑制剂。

公开(公告)号：US10815210B2

公开(公告)日：2020-10-27

申请号：US16348304

申请日：2017-11-08

Applicant: Janssen Pharmaceutica NV

Inventor： Micheal Gaul ,  Gee-Hong Kuo ,  Guozhang Xu ,  Yin Liang

IPC: C07D309/10

Abstract: The present invention is directed to benzocyclobutane derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity. More particularly, the compounds of the present invention are useful in the treatment of for example, Type II diabetes mellitus, Syndrome X, and complications and symptoms associated with said disorders.

公开(公告)号：US20190055226A1

公开(公告)日：2019-02-21

申请号：US16106104

申请日：2018-08-21

Applicant: Janssen Pharmaceutica NV

Inventor： Guozhang Xu ,  Gee-Hong Kuo ,  Micheal Gaul

IPC: C07D409/10 ,  C07D513/04 ,  C07D407/14 ,  C07D411/14 ,  C07D405/14

CPC classification number: C07D409/10 ,  C07D405/14 ,  C07D407/14 ,  C07D411/14 ,  C07D513/04

Abstract: The present invention is directed to 5-fluoro-C-(aryl or hetercyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.

公开(公告)号：US20170362196A1

公开(公告)日：2017-12-21

申请号：US15697867

申请日：2017-09-07

Applicant: Janssen Pharmaceutica NV

Inventor： Hui Huang ,  Gee-Hong Kuo ,  Mark R. Player ,  Shyh-Ming Yang ,  Yue-Mei Zhang

IPC: C07D333/54 ,  C07D409/14 ,  C07D409/12 ,  C07D409/10 ,  C07D409/04 ,  C07D409/02 ,  C07D333/56 ,  C07D233/56 ,  A61K31/4436 ,  C07D495/10 ,  A61K31/381

CPC classification number: C07D333/54 ,  A61K31/381 ,  A61K31/4436 ,  C07D233/56 ,  C07D333/56 ,  C07D409/02 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D495/10

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.

公开(公告)号：US20160102071A1

公开(公告)日：2016-04-14

申请号：US14877972

申请日：2015-10-08

Applicant: Janssen Pharmaceutica NV

Inventor： Hui Huang ,  Gee-Hong Kuo ,  Mark R. Player ,  Shyh-Ming Yang ,  Yue-Mei Zhang

IPC: C07D333/54 ,  C07D409/04 ,  C07D333/56 ,  C07D409/14 ,  C07D409/10 ,  C07D409/12 ,  C07D495/10

CPC classification number: C07D333/54 ,  A61K31/381 ,  A61K31/4436 ,  C07D233/56 ,  C07D333/56 ,  C07D409/02 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D495/10

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.

Abstract translation: 公开了用于治疗受GPR40受体调节影响的病症的化合物，组合物和方法。 这样的化合物由式（I）表示如下：其中R1，R2，R3，R5，R6，W和A如本文所定义。

公开(公告)号：US09012412B2

公开(公告)日：2015-04-21

申请号：US14200051

申请日：2014-03-07

Applicant: Janssen Pharmaceutica NV

Inventor： Micheal Gaul ,  Gee-Hong Kuo ,  Guozhang Xu ,  Bao-Ping Zhao

IPC: C07H7/04 ,  C07D417/10 ,  C07D407/10 ,  C07D409/10 ,  C07D409/14

CPC classification number: C07D417/10 ,  C07D407/10 ,  C07D409/10 ,  C07D409/14

Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein A, R1, R2, R3, R4, and R5 are as defined herein, useful as dual SGLT1/SGLT2 inhibitors.

Abstract translation: 本发明涉及式（I）化合物或其形式，其中A，R 1，R 2，R 3，R 4和R 5如本文所定义，可用作双重SGLT1 / SGLT2抑制剂。

公开(公告)号：US20210238170A1

公开(公告)日：2021-08-05

申请号：US17053363

申请日：2019-05-08

Applicant: Janssen Pharmaceutica NV

Inventor： Guozhang Xu ,  Gee-Hong Kuo ,  Michael Gaul

IPC: C07D407/10 ,  C07D409/10 ,  C07D309/10 ,  A61K9/00 ,  A61K9/48 ,  A61P3/10

Abstract: The present invention is directed to 5,5-difluoro- and 5-fluoro-5-methyl-C-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.

公开(公告)号：US20200291004A1

公开(公告)日：2020-09-17

申请号：US16890331

申请日：2020-06-02

Applicant: Janssen Pharmaceutica NV

Inventor： Guozhang Xu ,  Gee-Hong Kuo ,  Micheal Gaul

IPC: C07D409/10 ,  C07D513/04 ,  C07D405/14 ,  C07D411/14 ,  C07D407/14

Abstract: The present invention is directed to 5-fluoro-C-(aryl or heterocyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.

公开(公告)号：US20190062300A1

公开(公告)日：2019-02-28

申请号：US16174378

申请日：2018-10-30

Applicant: Janssen Pharmaceutica NV

Inventor： Hui Huang ,  Gee-Hong Kuo ,  Mark R. Player ,  Shyh-Ming Yang ,  Yue-Mei Zhang

IPC: C07D333/54 ,  C07D409/02 ,  C07D233/56 ,  C07D495/10 ,  C07D409/14 ,  C07D409/12 ,  A61K31/381 ,  C07D409/04 ,  C07D333/56 ,  A61K31/4436 ,  C07D409/10

CPC classification number: C07D333/54 ,  A61K31/381 ,  A61K31/4436 ,  C07D233/56 ,  C07D333/56 ,  C07D409/02 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D495/10

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.

公开(公告)号：US20140364393A1

公开(公告)日：2014-12-11

申请号：US14363033

申请日：2012-12-05

Applicant: Janssen Pharmaceutica NV

Inventor： Shyh-Ming Yang ,  Gee-Hong Kuo ,  Micheal D. Gaul ,  Thomas A. Rano

IPC: C07D513/04 ,  C07D401/04 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04

CPC classification number: C07D513/04 ,  C07D209/08 ,  C07D209/34 ,  C07D231/56 ,  C07D261/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D407/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.

Abstract translation: 本发明涉及新颖的哌啶基 - 甲酰胺衍生物，含有它们的药物组合物及其作为SCD1抑制剂的用途，可用于治疗肥胖症，II型糖尿病和其它相关的代谢紊乱。