公开(公告)号：WO2008005511A2

公开(公告)日：2008-01-10

申请号：PCT/US2007/015530

申请日：2007-06-05

Applicant: INTERMUNE, INC. ,  ARRAY BIOPHARMA, INC. ,  BLATT, Lawrence M. ,  SEIWERT, Scott ,  BEIGELMAN, Leonid ,  KERCHER, Timothy ,  KENNEDY, April L. ,  ANDREWS, Steven W.

Inventor： BLATT, Lawrence M. ,  SEIWERT, Scott ,  BEIGELMAN, Leonid ,  KERCHER, Timothy ,  KENNEDY, April L. ,  ANDREWS, Steven W.

IPC: C07D231/56 ,  C07D403/14 ,  C07D471/04 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/437 ,  A61P31/14

CPC classification number: C07D403/14 ,  C07D231/56 ,  C07D471/04

Abstract: The embodiments provide compounds of the general Formula (I), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula (II), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula (III), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了通式（I）的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案提供了通式（II）的化合物以及包含主题化合物的组合物，包括药物组合物。 实施方案提供了通式（III）的化合物以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：WO2007047146A2

公开(公告)日：2007-04-26

申请号：PCT/US2006/039044

申请日：2006-10-10

Applicant: INTERMUNE, INC. ,  ARRAY BIOPHARMA, INC. ,  BEIGELMAN, Leonid ,  ANDREWS, Steven, W. ,  CONDROSKI, Kevin, R. ,  GUNAWARADANA, Indrani ,  HAAS, Julia

Inventor： BEIGELMAN, Leonid ,  ANDREWS, Steven, W. ,  CONDROSKI, Kevin, R. ,  GUNAWARADANA, Indrani ,  HAAS, Julia

CPC classification number: C07D409/04 ,  C07C233/11 ,  C07C233/22 ,  C07C323/62 ,  C07D205/04 ,  C07D207/09 ,  C07D207/27 ,  C07D211/58 ,  C07D211/62 ,  C07D231/12 ,  C07D233/56 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  C07D233/78 ,  C07D235/02 ,  C07D249/08 ,  C07D295/13 ,  C07D295/185 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04

Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供通式I-IV的化合物，以及包含药物组合物的组合物，其包含主题化合物。 所述实施方案进一步提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常包括向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：WO2005095403A3

公开(公告)日：2005-12-01

申请号：PCT/US2005010494

申请日：2005-03-29

Applicant: INTERMUNE INC ,  BLATT LAWRENCE M ,  WENGLOWSKY STEVEN M ,  ANDREWS STEVEN W ,  CONDROSKI KEVIN R ,  JIANG YUTONG ,  KENNEDY APRIL L ,  DOHERTY GEORGE A ,  JOSEY JOHN A ,  STENGEL PETER J ,  WOODARD BENJAMIN T ,  MADDURU MACHENDER R

Inventor： BLATT LAWRENCE M ,  WENGLOWSKY STEVEN M ,  ANDREWS STEVEN W ,  CONDROSKI KEVIN R ,  JIANG YUTONG ,  KENNEDY APRIL L ,  DOHERTY GEORGE A ,  JOSEY JOHN A ,  STENGEL PETER J ,  WOODARD BENJAMIN T ,  MADDURU MACHENDER R

IPC: A61K31/495 ,  A61P31/12 ,  C07D487/00 ,  C07D487/04 ,  C07K5/08 ,  C07K5/083 ,  C07D209 ,  C07D245

CPC classification number: C07K5/0804 ,  C07D487/04

Abstract: The embodiments provide macrocylic compounds, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了大环化合物以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：WO2005058808A1

公开(公告)日：2005-06-30

申请号：PCT/US2004/041851

申请日：2004-12-14

Applicant: JAPAN TOBACCO INC. ,  FRYER, Andrew, M. ,  SHIOZAKI, Makoto ,  LITTMANN, Nicole, M. ,  INABA, Takashi ,  ANDREWS, Steven, W. ,  YASUE, Katsutaka ,  LAIRD, Ellen, R. ,  YOKOTA, Masahiro ,  HAAS, Julia ,  IMAI, Hiroto ,  MAEDA, Katsuya ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu

Inventor： FRYER, Andrew, M. ,  SHIOZAKI, Makoto ,  LITTMANN, Nicole, M. ,  INABA, Takashi ,  ANDREWS, Steven, W. ,  YASUE, Katsutaka ,  LAIRD, Ellen, R. ,  YOKOTA, Masahiro ,  HAAS, Julia ,  IMAI, Hiroto ,  MAEDA, Katsuya ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu

IPC: C07C311/20

CPC classification number: C07C311/20 ,  C07C311/51 ,  C07C381/06 ,  C07C381/08 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/34 ,  C07D209/52 ,  C07D211/46 ,  C07D211/60 ,  C07D213/42 ,  C07D213/65 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D231/14 ,  C07D231/20 ,  C07D233/90 ,  C07D235/14 ,  C07D249/10 ,  C07D257/04 ,  C07D257/06 ,  C07D261/18 ,  C07D271/07 ,  C07D277/56 ,  C07D285/06 ,  C07D285/08 ,  C07D295/088 ,  C07D295/13 ,  C07D295/15 ,  C07D295/185 ,  C07D307/68 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) : wherein R 1 is -W-A 1 -W 1 -A 2 , W is (CH 2 ) m -X-(CH 2 )n-, wherein W 1 is -(CH 2 ) m1 -X 1 -(CH 2 ) n1 -, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C 3-14 hydrocarbon ring group, etc. and A 2 is a substituted C 3-14 hydrocarbon ring group etc.; R 2 is -(CH 2 ) r -CO-R 8 , etc., wherein r is 0 to 6 and R 8 is a C 1-6 alkoxy group, etc.; R 3 and R 4 are the same or different and each is a hydrogen atom, a C 1-6 alkyl group, etc.; and R 5 is -CO 2 R 21 , etc.; R 30 and R 31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）所示的N-取代-N-磺酰氨基环丙烷化合物： 其中R 1是-WA 1 -W 1 -A 2，W是（CH 2）m X-（CH 2）n - ，其中W 1是 - （CH 2）m1-X 1 - （CH 2）n - ，m ，m1，n和n1相同或不同，分别为0〜6，X和X1相同或不同，均为单键等，A1为任选取代的C3-14烃环基等。 A 2是取代的C 3-14烃环基等。 R 2为 - （CH 2）r -CO-R 8等，其中r为0至6，R 8为C 1-6烷氧基等; R 3和R 4相同或不同，各自为氢原子，C 1-6烷基等; R 5为-CO 2 R 21等; R 30和R 31相同或不同，各自为氢原子等; 或其前药或其药学上可接受的盐。

公开(公告)号：WO2018071447A1

公开(公告)日：2018-04-19

申请号：PCT/US2017/055983

申请日：2017-10-10

Applicant: ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  MCNULTY, Oren T. ,  METCALF, Andrew T. ,  MORENO, David A. ,  TANG, Tony P. ,  REN, Li

Inventor： ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  MCNULTY, Oren T. ,  METCALF, Andrew T. ,  MORENO, David A. ,  TANG, Tony P. ,  REN, Li

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: Provided herein are compounds of the Formula I and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X 1 , X 2 , X 3 , X 4 , Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Abstract translation: 本文提供了式I的化合物及其立体异构体和药学上可接受的盐或溶剂合物，其中A，B，X 1，X 2， X 3，X 4，D环和E具有在说明书中给出的含义，其是RET激酶的抑制剂并且可用于治疗和预防 可以用RET激酶抑制剂治疗的疾病，包括与RET相关的疾病和病症。

公开(公告)号：WO2008100867A2

公开(公告)日：2008-08-21

申请号：PCT/US2008053617

申请日：2008-02-11

Applicant: INTERMUNE INC ,  BEIGELMAN LEONID ,  BUCKMAN BRAD ,  WANG GUANGYI ,  MATULIC-ADAMIC JASENKA ,  STOYCHEVA ANTITSA DIMITROVA ,  ANDREWS STEVEN W ,  MISIALEK SHAWN MAURICE ,  RAJAGOPALAN P T RAVI ,  FRYER ANDREW M ,  GUNAWARDANA INDRANI ,  HAAS JULIA ,  HUANG LILY ,  MADDURU MACHENDER R ,  ZHANG GAN ,  KOSSEN KARL ,  SEREBRYANY VLADIMIR

Inventor： BEIGELMAN LEONID ,  BUCKMAN BRAD ,  WANG GUANGYI ,  MATULIC-ADAMIC JASENKA ,  STOYCHEVA ANTITSA DIMITROVA ,  ANDREWS STEVEN W ,  MISIALEK SHAWN MAURICE ,  RAJAGOPALAN P T RAVI ,  FRYER ANDREW M ,  GUNAWARDANA INDRANI ,  HAAS JULIA ,  HUANG LILY ,  MADDURU MACHENDER R ,  ZHANG GAN ,  KOSSEN KARL ,  SEREBRYANY VLADIMIR

IPC: C07D209/18 ,  C07D209/30 ,  C07D209/32 ,  C07D307/79 ,  C07D333/60 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D407/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06

CPC classification number: C07F9/65583 ,  C07D209/18 ,  C07D209/30 ,  C07D209/32 ,  C07D307/79 ,  C07D333/60 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D407/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D417/06 ,  C07D487/04 ,  C07F9/5728 ,  C12Q1/707 ,  G01N2333/186 ,  G01N2333/914

Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：WO2005058884A3

公开(公告)日：2005-06-30

申请号：PCT/US2004/041852

申请日：2004-12-14

Applicant: JAPAN TOBACCO INC. ,  INABA, Takashi ,  HAAS, Julia ,  SHIOZAKI, Makoto ,  LITTMAN, Nicole, M. ,  YASUE, Katsutaka ,  ANDREWS, Steven, W. ,  SAKAI, Atushi ,  FRYER, Andrew, M. ,  MATSUO, Takafumi ,  LAIRD, Ellen, R. ,  SUMA, Akira ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu ,  IMAI, Hiroto ,  NEGORO, Tamotsu

Inventor： INABA, Takashi ,  HAAS, Julia ,  SHIOZAKI, Makoto ,  LITTMAN, Nicole, M. ,  YASUE, Katsutaka ,  ANDREWS, Steven, W. ,  SAKAI, Atushi ,  FRYER, Andrew, M. ,  MATSUO, Takafumi ,  LAIRD, Ellen, R. ,  SUMA, Akira ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu ,  IMAI, Hiroto ,  NEGORO, Tamotsu

IPC: A61P19/02

Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R 1 is - (CH 2 ) m -X- (CH 2 ) n -A 1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A 1 is a substituted C 3-14 hydrocarbon ring group, etc.; R 2 and R 3 are the same or different and each is a hydrogen atom, -(CH 2 ) p -X 1 -(CH 2 ) q -A 2 , etc., wherein p and q are the same or different and each is 0 to 6, X 1 is a single bond, etc. and A 2 is an optionally substituted C 3-14 hydrocarbon ring group, etc.; R 4 is -C0 2 R 9 , etc., wherein R 9 is a hydrogen atom, etc.; and R 20 and R 21 are the same or different and each is a hydrogen atom, - (CH 2 ) m12- X 12- (CH 2 ) m12 -R 30 , etc., wherein m12 and m12 are the same or different and each is 0 to 6, X 12 is a single bond, etc. and R 30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.

公开(公告)号：WO2003027109A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/029630

申请日：2002-09-18

Applicant: ALLERGAN, INC. ,  ANDREWS, Steven, W. ,  WURSTER, Julie, A. ,  HULL, III, C., Eugene

Inventor： ANDREWS, Steven, W. ,  WURSTER, Julie, A. ,  HULL, III, C., Eugene

IPC: C07D417/12

CPC classification number: C07D405/12 ,  C07D409/12

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract translation: 本发明涉及能够调节酪氨酸激酶信号转导以调节，调节和/或抑制异常细胞增殖的有机分子。

公开(公告)号：WO2018071454A1

公开(公告)日：2018-04-19

申请号：PCT/US2017/055993

申请日：2017-10-10

Applicant: ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  COLLIER, James ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  MCNULTY, Oren T. ,  METCALF, Andrew T. ,  MORENO, David A. ,  RAMANN, Ginelle A. ,  TANG, Tony P. ,  REN, Li ,  WALLS, Shane M.

Inventor： ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  COLLIER, James ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  MCNULTY, Oren T. ,  METCALF, Andrew T. ,  MORENO, David A. ,  RAMANN, Ginelle A. ,  TANG, Tony P. ,  REN, Li ,  WALLS, Shane M.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X 1 , X 2 , X 3 , X 4 , Ring D, E, R a , R b , n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Abstract translation: 本文提供了式I的化合物：（I）或其药学上可接受的盐或溶剂合物，其中A，B，X 1，X 2， X 3，X 4，D环，E，R a，R b，n和 m具有在说明书中给出的含义，它们是RET激酶的抑制剂，并且可用于治疗和预防可以用RET激酶抑制剂治疗的疾病，包括RET相关的疾病和病症。

公开(公告)号：WO2008005511A8

公开(公告)日：2009-03-19

申请号：PCT/US2007015530

申请日：2007-07-05

Applicant: INTERMUNE INC ,  ARRAY BIOPHARMA INC ,  BLATT LAWRENCE M ,  SEIWERT SCOTT ,  BEIGELMAN LEONID ,  KERCHER TIMOTHY ,  KENNEDY APRIL L ,  ANDREWS STEVEN W

Inventor： BLATT LAWRENCE M ,  SEIWERT SCOTT ,  BEIGELMAN LEONID ,  KERCHER TIMOTHY ,  KENNEDY APRIL L ,  ANDREWS STEVEN W

IPC: C07D231/56 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/437 ,  A61P31/14 ,  C07D403/14 ,  C07D471/04

CPC classification number: C07D403/14 ,  C07D231/56 ,  C07D471/04

Abstract: The embodiments provide compounds of the general Formula (I), as well as compositions, including pharmaceutical compositions, comprising a, subject compound. The embodiments provide compounds of the general Formula (II), as well as compositions, including pharmaceutical compositions, comprising a subject compound, The embodiments provide compounds of the general Formula (III), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了通式（I）的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案提供了通式（II）的化合物，以及包含主题化合物的组合物，包括药物组合物。实施方案提供了通式（III）的化合物，以及包含药物组合物的组合物，其包含受试者 复合。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。