公开(公告)号：US09227975B2

公开(公告)日：2016-01-05

申请号：US13614968

申请日：2012-09-13

Applicant: Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

Inventor： Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00

Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.

Abstract translation: 治疗哺乳动物选自疼痛，癌症，炎症，神经变性疾病，克氏锥虫感染和溶骨性疾病的疾病或病症的方法，其包括向所述哺乳动物施用治疗有效量的式I化合物，其中R1，R2， R3，R4，X，Y和n具有说​​明书中给出的含义。

公开(公告)号：US20110195948A1

公开(公告)日：2011-08-11

申请号：US13125263

申请日：2009-10-21

Applicant: Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: A61K31/397 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/497 ,  A61K31/496 ,  A61P29/00 ,  A61P35/00 ,  A61P31/00 ,  A61P25/04

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物是Trk激酶的抑制剂，可用于治疗可用Trk激酶治疗的疾病 抑制剂。

公开(公告)号：US07829665B2

公开(公告)日：2010-11-09

申请号：US11491126

申请日：2006-07-21

Applicant: Lawrence M. Blatt ,  Scott D. Seiwert ,  Steven W. Andrews ,  Pierre Martin ,  Andreas Schumacher ,  Bradley Barnett ,  C. Todd Eary ,  Robert Kaus ,  Timothy Kercher ,  Weidong Liu ,  Michael Lyon ,  Paul Nichols ,  Bin Wang ,  Tarek Sammakia ,  April Kennedy ,  Yutong Jiang

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Steven W. Andrews ,  Pierre Martin ,  Andreas Schumacher ,  Bradley Barnett ,  C. Todd Eary ,  Robert Kaus ,  Timothy Kercher ,  Weidong Liu ,  Michael Lyon ,  Paul Nichols ,  Bin Wang ,  Tarek Sammakia ,  April Kennedy ,  Yutong Jiang

IPC: C07K7/50

CPC classification number: C07K5/0806 ,  A61K38/00 ,  A61K38/1793 ,  A61K38/212 ,  A61K38/217 ,  A61K38/2292 ,  A61K38/55 ,  C07D471/04 ,  C07D487/04 ,  C07K5/0804 ,  A61K2300/00

Abstract: The embodiments provide compounds of the general Formulae I through general Formula VIII, 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至通式VIII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：US20090111982A1

公开(公告)日：2009-04-30

申请号：US12341517

申请日：2008-12-22

Applicant: Lawrence M. Blatt ,  Steven W. Andrews ,  Kevin R. Condroski ,  George A. Doherty ,  Yutong Jiang ,  John A. Josey ,  April L. Kennedy ,  Machender R. Madduru ,  Peter J. Stengel ,  Steven M. Wenglowsky ,  Benjamin T. Woodard ,  Laura Woodard

Inventor： Lawrence M. Blatt ,  Steven W. Andrews ,  Kevin R. Condroski ,  George A. Doherty ,  Yutong Jiang ,  John A. Josey ,  April L. Kennedy ,  Machender R. Madduru ,  Peter J. Stengel ,  Steven M. Wenglowsky ,  Benjamin T. Woodard ,  Laura Woodard

IPC: C07D487/04 ,  C07D401/12 ,  C07D403/02

CPC classification number: C07K5/0804

Abstract: The embodiments provide compounds of the general formulas I-XIX, 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.

公开(公告)号：US07491794B2

公开(公告)日：2009-02-17

申请号：US11093884

申请日：2005-03-29

Applicant: Lawrence M. Blatt ,  Steven W. Andrews ,  Kevin R. Condroski ,  Yutong Jiang ,  April L. Kennedy ,  Peter J. Stengel ,  Steven M. Wenglowsky

Inventor： Lawrence M. Blatt ,  Steven W. Andrews ,  Kevin R. Condroski ,  Yutong Jiang ,  April L. Kennedy ,  Peter J. Stengel ,  Steven M. Wenglowsky

IPC: A61K38/12

CPC classification number: C07K5/0804

Abstract: The embodiments provide compounds of the general formulas I-XIX, 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: 实施方案提供了通式I-XIX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：US20080242656A1

公开(公告)日：2008-10-02

申请号：US11765136

申请日：2007-06-19

Applicant: Andrew M. Fryer ,  Makoto Shiozaki ,  Nicole M. Littmann ,  Takashi Inaba ,  Steven W. Andrews ,  Katsutaka Yasue ,  Ellen R. Laird ,  Masahiro Yokota ,  Julia Haas ,  Hiroto Imai ,  Katsuya Maeda ,  Yuichi Shinozaki ,  Yoshikazu Hori

Inventor： Andrew M. Fryer ,  Makoto Shiozaki ,  Nicole M. Littmann ,  Takashi Inaba ,  Steven W. Andrews ,  Katsutaka Yasue ,  Ellen R. Laird ,  Masahiro Yokota ,  Julia Haas ,  Hiroto Imai ,  Katsuya Maeda ,  Yuichi Shinozaki ,  Yoshikazu Hori

IPC: A01N43/00

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 R1 is —W-A1-W1-A2, W is —(CH2)m—X—(CH2)n—, wherein W1 is —(CH2)m1—X1—(CH2)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 C3-14 hydrocarbon ring group, etc. and A2 is a substituted C3-14 hydrocarbon ring group etc.; R2 is —(CH2)r—CO—R8, etc., wherein r is 0 to 6 and R8 is a C1-6 alkoxy group, etc.; R3 and R4 are the same or different and each is a hydrogen atom, a C1-6 alkyl group, etc.; and R5 is —CO2R21, etc.; R30 and R31 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，更具体地，可以使用式（1）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）2 其中W 1 - （CH 2）n - （CH 2）n - 其中W 1是 - （ CH 2 - （CH 2）n1 - - - - - （CH 2）n1 - m，m1，n和n1相同或不同，各自为0〜6，X和X 1相同或不同，分别为单键等。 任选取代的C 3-14-14烃环基等，并且A 2是取代的C 3-14烃基 戒指组等 R 2是 - （CH 2 CH 2）n -CO-R 8等，其中r是0 至6和R 8是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; 和R 5是-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：US07393870B2

公开(公告)日：2008-07-01

申请号：US11282044

申请日：2005-11-17

Applicant: Steven W. Andrews ,  Julie A. Wurster

Inventor： Steven W. Andrews ,  Julie A. Wurster

IPC: A61K31/422 ,  C07D413/12

CPC classification number: C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14

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：US07098236B2

公开(公告)日：2006-08-29

申请号：US10886213

申请日：2004-07-06

Applicant: Steven W. Andrews ,  Julie A. Wurster ,  Clarence E. Hull, III

Inventor： Steven W. Andrews ,  Julie A. Wurster ,  Clarence E. Hull, III

IPC: A61K31/4045 ,  C07D209/34

CPC classification number: C07D295/088 ,  A61K31/404 ,  C07D209/34 ,  C07D295/135 ,  C07D401/10 ,  C07D403/12

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：US08513263B2

公开(公告)日：2013-08-20

申请号：US13125263

申请日：2009-10-21

Applicant: Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物是Trk激酶的抑制剂，可用于治疗可用Trk激酶治疗的疾病 抑制剂。

公开(公告)号：US20100209391A1

公开(公告)日：2010-08-19

申请号：US12769449

申请日：2010-04-28

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

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

IPC: A61K31/404 ,  C07D403/12 ,  A61K31/7052 ,  A61K31/427 ,  A61K38/21 ,  A61K31/7072 ,  A61K31/7068 ,  A61P1/16

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

Abstract: The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments also 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。