公开(公告)号：WO2011159854A1

公开(公告)日：2011-12-22

申请号：PCT/US2011/040610

申请日：2011-06-16

Applicant: JANSSEN PHARMACEUTICA NV ,  LANTER, James, C. ,  MARKOTAN, Thomas, P. ,  SUBASINGHE, Nalin ,  SUI, Zhihua

Inventor： LANTER, James, C. ,  MARKOTAN, Thomas, P. ,  SUBASINGHE, Nalin ,  SUI, Zhihua

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/517 ,  A61K31/4709 ,  A61K31/502 ,  A61K31/4375 ,  A61P29/00

CPC classification number: C07D471/04 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/502 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention comprises compounds of Formula (I). Wherein: R 1 , R 2 , R 4 , J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract translation: 本发明包括式（I）的化合物。 其中R1，R2，R4，J，Q和A如说明书中所定义。 本发明还包括预防，治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是II型糖尿病，肥胖症和哮喘。 本发明还包括通过施用治疗有效量的至少一种式（I）化合物来抑制哺乳动物CCR2活性的方法。

公开(公告)号：WO2011156554A1

公开(公告)日：2011-12-15

申请号：PCT/US2011/039724

申请日：2011-06-09

Applicant: JANSSEN PHARMACEUTICA NV ,  ZHANG, Xuquing ,  SUI, Zhihua ,  LANTER, James, C.

Inventor： ZHANG, Xuquing ,  SUI, Zhihua ,  LANTER, James, C.

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/416 ,  A61K31/423 ,  A61K31/437 ,  A61P1/02 ,  A61P3/10 ,  A61P11/06

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention comprises compounds of Formula (I). wherein: R 1 , R 2 , X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract translation: 本发明包括式（I）的化合物。 其中：R1，R2，X和Z如说明书中所定义。 本发明还包括预防，治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是II型糖尿病，肥胖症和哮喘。 本发明还包括通过施用治疗有效量的至少一种式（I）化合物来抑制哺乳动物CCR2活性的方法。

公开(公告)号：WO2019171278A1

公开(公告)日：2019-09-12

申请号：PCT/IB2019/051780

申请日：2019-03-05

Applicant: JANSSEN PHARMACEUTICA NV ,  LANTER, James C.

Inventor： LANTER, James C. ,  WALL, Mark ,  SUI, Zhihua

IPC: C07D309/22 ,  C07D313/04 ,  C07D333/06 ,  C07D333/48 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12 ,  C07D307/28 ,  A61P3/10 ,  A61K31/165

Abstract: The present invention is directed to heterocycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and / or GPR40 receptors. 5 More particularly, the compounds of the present invention are agonists of GPR120 and / or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc.

公开(公告)号：WO2019171277A1

公开(公告)日：2019-09-12

申请号：PCT/IB2019/051779

申请日：2019-03-05

Applicant: JANSSEN PHARMACEUTICA NV ,  LANTER, James C.

Inventor： LANTER, James C. ,  MACIELAG, Mark J. ,  WALL, Mark ,  WINTERS, Michael P. ,  ZHANG, Yue-Mei ,  SUI, Zhihua

IPC: C07D333/16 ,  C07D233/70 ,  C07D239/26 ,  C07D277/24 ,  C07D213/55 ,  C07D307/40 ,  C07C59/72 ,  A61P3/10 ,  A61K31/165

Abstract: The present invention is directed to cycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and / or GPR40 receptors. 5 More particularly, the compounds of the present invention are agonists of GPR120 and / or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc.

公开(公告)号：WO2012075115A1

公开(公告)日：2012-06-07

申请号：PCT/US2011/062593

申请日：2011-11-30

Applicant: JANSSEN PHARMACEUTICA NV ,  LANTER, James, C. ,  MARKOTAN, Thomas, P. ,  SUBASINGHE, Nalin ,  SUI, Zhihua ,  ZHANG, Xuqing

Inventor： LANTER, James, C. ,  MARKOTAN, Thomas, P. ,  SUBASINGHE, Nalin ,  SUI, Zhihua ,  ZHANG, Xuqing

IPC: C07D401/12 ,  C07D471/04 ,  A61K31/404 ,  A61K31/437 ,  A61P3/00 ,  A61P11/00

CPC classification number: C07D401/12 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention comprises compounds of Formula (I). wherein: R 1 , R 2 , R 3 , R 4 , X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract translation: 本发明包括式（I）的化合物。 其中：R1，R2，R3，R4，X，Y和Z如说明书中所定义。 本发明还包括预防，治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是II型糖尿病，肥胖症和哮喘。 本发明还包括通过施用治疗有效量的至少一种式（I）化合物来抑制哺乳动物CCR2活性的方法。

公开(公告)号：WO2014028805A1

公开(公告)日：2014-02-20

申请号：PCT/US2013/055275

申请日：2013-08-16

Applicant: JANSSEN PHARMACEUTICA NV ,  WINTERS, Michael, P.

Inventor： WINTERS, Michael, P. ,  SUI, Zhihua

IPC: C07D487/04 ,  A61K31/4162 ,  A61P29/00

CPC classification number: C07D487/04

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: Formula. (I) wherein R 1 , R 2 R 3 , Q, and G are defined herein.

Abstract translation: 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：式。 （I）其中R1，R2 R3，Q和G如本文所定义。

公开(公告)号：WO2005111028A1

公开(公告)日：2005-11-24

申请号：PCT/US2005/011106

申请日：2005-04-01

Applicant: JANSSEN PHARMACEUTICA N.V. ,  LANTER, James C. ,  SUI, Zhihua ,  FIORDELISO, James J. ,  JIANG, Weiqin ,  ZHANG, Xuqing

Inventor： LANTER, James C. ,  SUI, Zhihua ,  FIORDELISO, James J. ,  JIANG, Weiqin ,  ZHANG, Xuqing

IPC: C07D409/04

CPC classification number: C07D209/12 ,  C07D401/04 ,  C07D409/04

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. Formula (II): (II)

Abstract translation: 本发明涉及新的吲哚衍生物，含有它们的药物组合物及其用于治疗由雄激素受体调节的病症和状况。 式（II）：（II）

公开(公告)号：WO2006039243A1

公开(公告)日：2006-04-13

申请号：PCT/US2005/034462

申请日：2005-09-26

Applicant: JANSSEN PHARMACEUTICA N.V. ,  NG, Raymond ,  SUI, Zhihua ,  GUAN, Jihua ,  LANTER, James C. ,  ALFORD, Vernon C. Jr.

Inventor： NG, Raymond ,  SUI, Zhihua ,  GUAN, Jihua ,  LANTER, James C. ,  ALFORD, Vernon C. Jr.

IPC: C07D235/16 ,  C07D235/12 ,  C07D235/10 ,  C07D401/06 ,  C07D409/14 ,  C07D405/06 ,  C07D413/06 ,  C07D417/10 ,  C07D403/10 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/42 ,  A61K31/433 ,  A61P5/26 ,  A61P5/28

CPC classification number: C07D403/06 ,  C07D235/10 ,  C07D235/12 ,  C07D235/16 ,  C07D401/06 ,  C07D403/10 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/10

Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract translation: 本发明涉及新型苯并咪唑衍生物，含有它们的药物组合物及其在治疗由雄激素受体调节的病症和病症中的用途。

公开(公告)号：WO2006039215A2

公开(公告)日：2006-04-13

申请号：PCT/US2005/034277

申请日：2005-09-26

Applicant: JANSSEN PHARMACEUTICA N.V. ,  NG, Raymond ,  SUI, Zhihua ,  GUAN, Jihua ,  LANTER, James C. ,  ALFORD, Vernon C., Jr.

Inventor： NG, Raymond ,  SUI, Zhihua ,  GUAN, Jihua ,  LANTER, James C. ,  ALFORD, Vernon C., Jr.

IPC: C07D235/16 ,  C07D235/12 ,  C07D235/10 ,  C07D401/06 ,  C07D409/14 ,  C07D405/06 ,  C07D413/06 ,  C07D417/10 ,  C07D403/10 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/42 ,  A61K31/433 ,  A61P5/26 ,  A61P5/28

CPC classification number: C07D405/06 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D401/06 ,  C07D403/10 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/10

Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract translation: 本发明涉及新的苯并咪唑衍生物，含有它们的药物组合物及其在治疗由雄激素受体调节的病症和状况中的用途。

公开(公告)号：WO2006023242A1

公开(公告)日：2006-03-02

申请号：PCT/US2005/026944

申请日：2005-07-28

Applicant: JANSSEN PHARMACEUTICA N.V. ,  LANTER, James C. ,  SUI, Zhihua ,  FIORDELISO, James J.

Inventor： LANTER, James C. ,  SUI, Zhihua ,  FIORDELISO, James J.

IPC: C07D267/14 ,  A61K31/553 ,  A61P35/00

CPC classification number: C07D267/10 ,  C07D267/14

Abstract: The present invention is directed to novel benzoxazepine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and diseases mediated by an estrogen receptor.

Abstract translation: 本发明涉及新的苯并氧氮杂衍生物，含有它们的药物组合物及其在治疗由雌激素受体介导的疾病和疾病中的用途。