公开(公告)号：US20170342076A1

公开(公告)日：2017-11-30

申请号：US15538910

申请日：2015-12-17

Applicant: JIAN LIU ,  JOSEPH A. KOZLOWSKI ,  BRIAN M. ANDRESEN ,  SOBHANA BABU BOGA ,  XIAOLEI GAO ,  DEODIAL GUY GUIADEEN ,  JIAQIANG CAI ,  SHILAN LIU ,  DAHAI WANG ,  HAO WU ,  CHUNDAO YANG

Inventor： JIAN LIU ,  JOSEPH A. KOZLOWSKI ,  BRIAN M. ANDRESEN ,  SOBHANA BABU BOGA ,  XIAOLEI GAO ,  DEODIAL GUY GUIADEEN ,  JIAQIANG CAI ,  SHILAN LIU ,  DAHAI WANG ,  HAO WU ,  CHUNDAO YANG

IPC: C07D487/04 ,  A61K31/4985

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

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.

公开(公告)号：US20170226120A1

公开(公告)日：2017-08-10

申请号：US15514537

申请日：2015-09-23

Applicant: JIAQIANG CAI ,  ALEJANDRO CRESPO ,  XIAOXING DU ,  BYRON GABRIEL DUBOIS ,  PING LIU ,  RONGQIANG LIU ,  WEIGUO QUAN ,  CHRISTOPHER SINZ ,  LIPING WANG

Inventor： JIAQIANG CAI ,  ALEJANDRO CRESPO ,  XIAOXING DU ,  BYRON GABRIEL DUBOIS ,  PING LIU ,  RONGQIANG LIU ,  WEIGUO QUAN ,  CHRISTOPHER SINZ ,  LIPING WANG

IPC: C07D491/048

CPC classification number: C07D491/048 ,  A61P7/06 ,  A61P9/10

Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：US10233193B2

公开(公告)日：2019-03-19

申请号：US15575433

申请日：2016-05-20

Applicant: MERCK SHARP & DOHME CORP. ,  Tao Yu ,  Thomas H. Graham ,  Sherman T. Waddell ,  John A. McCauley ,  Andrew W. Stamford ,  John M. Sanders ,  Lihong Hu ,  Jiaqiang Cai ,  Lianyun Zhao

Inventor： Tao Yu ,  Thomas H. Graham ,  Sherman T. Waddell ,  John A. McCauley ,  Andrew W. Stamford ,  John M. Sanders ,  Lihong Hu ,  Jiaqiang Cai ,  Lianyun Zhao

IPC: A61K31/4375 ,  C07D491/147 ,  A61K31/4355 ,  A61K31/437 ,  C07D471/14 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/675 ,  A61P31/18

Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.

公开(公告)号：US10208060B2

公开(公告)日：2019-02-19

申请号：US15513854

申请日：2015-09-23

Applicant: Jiaqiang Cai ,  Alejandro Crespo ,  John Debenham ,  Xiaoxing Du ,  Ping Liu ,  Rongqiang Liu ,  Christina B. Madsen-Duggan ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

Inventor： Jiaqiang Cai ,  Alejandro Crespo ,  John Debenham ,  Xiaoxing Du ,  Ping Liu ,  Rongqiang Liu ,  Christina B. Madsen-Duggan ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

IPC: C07D491/048 ,  C07D495/04 ,  A61P7/06

Abstract: The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：US10208047B2

公开(公告)日：2019-02-19

申请号：US15538910

申请日：2015-12-17

Applicant: Jian Liu ,  Joseph A. Kozlowski ,  Brian M. Andresen ,  Sobhana Babu Boga ,  Xiaolei Gao ,  Deodial Guy Guiadeen ,  Jiaqiang Cai ,  Shilan Liu ,  Dahai Wang ,  Hao Wu ,  Chundao Yang

Inventor： Jian Liu ,  Joseph A. Kozlowski ,  Brian M. Andresen ,  Sobhana Babu Boga ,  Xiaolei Gao ,  Deodial Guy Guiadeen ,  Jiaqiang Cai ,  Shilan Liu ,  Dahai Wang ,  Hao Wu ,  Chundao Yang

IPC: C07D487/04 ,  A61K31/4985 ,  A61K45/06

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.

公开(公告)号：US20170362242A1

公开(公告)日：2017-12-21

申请号：US15538902

申请日：2015-12-17

Applicant: JIAN LIU ,  JOSEPH A. KOZLOWSKI ,  ABDUL-BASIT ALHASSAN ,  SOBHANA BABU BOGA ,  XIAOLEI GAO ,  DEODIAL GUY GUIADEEN ,  JYHSHING WANG ,  WENSHENG YU ,  JIAQIANG CAI ,  SHILAN LIU ,  DAHAI WANG ,  HAO WU ,  CHUNDAO YANG

Inventor： JIAN LIU ,  JOSEPH A. KOZLOWSKI ,  ABDUL-BASIT ALHASSAN ,  SOBHANA BABU BOGA ,  XIAOLEI GAO ,  DEODIAL GUY GUIADEEN ,  JYHSHING WANG ,  WENSHENG YU ,  JIAQIANG CAI ,  SHILAN LIU ,  DAHAI WANG ,  HAO WU ,  CHUNDAO YANG

IPC: C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  A61P37/02 ,  C07D519/00

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

公开(公告)号：US07687515B2

公开(公告)日：2010-03-30

申请号：US11653600

申请日：2007-01-16

Applicant: Jiaqiang Cai ,  Zoran Rankovic ,  Philip Stephen Jones ,  David Jonathan Bennett ,  Iain Cumming ,  Jonathan Gillespie

Inventor： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Stephen Jones ,  David Jonathan Bennett ,  Iain Cumming ,  Jonathan Gillespie

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

Abstract translation: 本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物 包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途 ，如神经性疼痛。

公开(公告)号：US20070179138A1

公开(公告)日：2007-08-02

申请号：US11653600

申请日：2007-01-16

Applicant: Jiaqiang Cai ,  Zoran Rankovic ,  Philip Jones ,  David Bennett ,  Iain Cumming ,  Jonathan Gillespie

Inventor： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Jones ,  David Bennett ,  Iain Cumming ,  Jonathan Gillespie

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

Abstract translation: 本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物 包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途 ，如神经性疼痛。

公开(公告)号：US20170313718A1

公开(公告)日：2017-11-02

申请号：US15513854

申请日：2015-09-23

Applicant: JIAQIANG CAI ,  ALEJANDRO CRESPO ,  JOHN DEBENHAM ,  XIAOXING DU ,  PING LIU ,  RONGQIANG LIU ,  CHRISTINA B. MADSEN-DUGGAN ,  WEIGUO QUAN ,  CHRISTOPHER SINZ ,  LIPING WANG

Inventor： JIAQIANG CAI ,  ALEJANDRO CRESPO ,  JOHN DEBENHAM ,  XIAOXING DU ,  PING LIU ,  RONGQIANG LIU ,  CHRISTINA B. MADSEN-DUGGAN ,  WEIGUO QUAN ,  CHRISTOPHER SINZ ,  LIPING WANG

IPC: C07D495/04 ,  C07D491/048

CPC classification number: C07D495/04 ,  A61P7/06 ,  C07D491/048

Abstract: The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：US20120283239A1

公开(公告)日：2012-11-08

申请号：US13519924

申请日：2011-01-13

Applicant: Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

Inventor： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/54 ,  A61P25/00 ,  A61P19/10 ,  A61P9/10 ,  A61P29/00 ,  A61P37/00 ,  A61P17/06 ,  A61K31/437 ,  A61K31/551

CPC classification number: C07D471/04

Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

Abstract translation: 本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R 2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与Sn相互作用的组。 。 。 组织蛋白酶S活性位点的S2位点; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途 关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。