公开(公告)号：US09562055B2

公开(公告)日：2017-02-07

申请号：US14117615

申请日：2012-05-09

Applicant: Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

Inventor： Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

IPC: C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D495/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377

CPC classification number: C07D403/12 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  Y02A50/414

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract translation: 其中R1，R2，Ra，Rb，Rc，Rd，X，Y，B和环C如本文所定义的式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物或前药，其中 Y-B部分和NH-C（= X）-NH部分是反式构型，是TrkA激酶的抑制剂，可用于治疗可用TrkA激酶抑制剂如疼痛，癌症治疗的疾病 ，炎症，神经变性疾病和某些传染病。

公开(公告)号：US20130217662A1

公开(公告)日：2013-08-22

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: C07D487/04

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：US20120178715A1

公开(公告)日：2012-07-12

申请号：US13393767

申请日：2010-09-03

Applicant: Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

IPC: A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61K31/5386 ,  A61K31/675 ,  C07D487/04 ,  C07D498/08

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.

Abstract translation: 式I化合物及其盐，其中R 1，R 2，R 2a，R 3，n，X和环B具有本说明书中给出的含义，是mTOR的抑制剂，可用于治疗对抑制作用敏感的疾病 mTOR，如癌症。

公开(公告)号：US07932277B2

公开(公告)日：2011-04-26

申请号：US12118624

申请日：2008-05-09

Applicant: Scott Seiwert ,  Steven W. Andrews ,  Leonid Beigelman ,  Lawrence M. Blatt ,  Brad Buckman ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timothy S. Kercher ,  Michael A. Lyon ,  Bin Wang

Inventor： Scott Seiwert ,  Steven W. Andrews ,  Leonid Beigelman ,  Lawrence M. Blatt ,  Brad Buckman ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timothy S. Kercher ,  Michael A. Lyon ,  Bin Wang

IPC: A61K31/4035 ,  A61K31/428 ,  A61K31/4025 ,  A61K31/401 ,  C07D207/09 ,  C07D403/12 ,  C07D417/12

CPC classification number: C07D217/26 ,  C07D401/12 ,  C07D417/14

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 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：US07781474B2

公开(公告)日：2010-08-24

申请号：US11773912

申请日：2007-07-05

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: A61K31/40 ,  C07D207/00

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：US20090297476A1

公开(公告)日：2009-12-03

申请号：US12118624

申请日：2008-05-09

Applicant: SCOTT SEIWERT ,  STEVEN W. ANDREWS ,  LEONID BEIGELMAN ,  LAWRENCE M. BLATT ,  BRAD BUCKMAN ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timonthy S. Kercher ,  Michael A. Lyon ,  Bin Wang

Inventor： SCOTT SEIWERT ,  STEVEN W. ANDREWS ,  LEONID BEIGELMAN ,  LAWRENCE M. BLATT ,  BRAD BUCKMAN ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timonthy S. Kercher ,  Michael A. Lyon ,  Bin Wang

IPC: A61K38/21 ,  C12N9/99 ,  A61K31/7088 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/427 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D217/26 ,  C07D401/12 ,  C07D417/14

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 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：US20090286843A1

公开(公告)日：2009-11-19

申请号：US12254736

申请日：2008-10-20

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: A61K31/407 ,  C07D245/00 ,  A61P31/12

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：US07414054B2

公开(公告)日：2008-08-19

申请号：US11274681

申请日：2005-11-15

Applicant: Steven W. Andrews ,  Julie A. Wurster ,  Edward H. Wang ,  Thomas Malone

Inventor： Steven W. Andrews ,  Julie A. Wurster ,  Edward H. Wang ,  Thomas Malone

IPC: A61K31/404 ,  A61K31/5377 ,  C07D413/02 ,  C07D209/04

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：US07351825B2

公开(公告)日：2008-04-01

申请号：US11011773

申请日：2004-12-15

Applicant: Takashi Inaba ,  Julia Haas ,  Makoto Shiozaki ,  Nicole M. Littmann ,  Katsutaka Yasue ,  Steven W. Andrews ,  Atushi Sakai ,  Andrew M. Fryer ,  Takafumi Matsuo ,  Ellen R. Laird ,  Akira Suma ,  Yuichi Shinozaki ,  Yoshikazu Hori ,  Hiroto Imai ,  Tamotsu Negoro

Inventor： Takashi Inaba ,  Julia Haas ,  Makoto Shiozaki ,  Nicole M. Littmann ,  Katsutaka Yasue ,  Steven W. Andrews ,  Atushi Sakai ,  Andrew M. Fryer ,  Takafumi Matsuo ,  Ellen R. Laird ,  Akira Suma ,  Yuichi Shinozaki ,  Yoshikazu Hori ,  Hiroto Imai ,  Tamotsu Negoro

IPC: C07D265/00 ,  C07D295/00 ,  C07D237/00 ,  C07D409/00 ,  C07D411/00 ,  C07D217/00 ,  C07D211/00 ,  C07D213/00 ,  C07D271/00 ,  C07D413/00 ,  C07D498/00 ,  C07D277/00 ,  C07D257/00 ,  C07D233/00 ,  C07D231/00 ,  C07D207/00 ,  C07D333/00 ,  C07D307/00 ,  C07D303/00 ,  C07D309/00 ,  C07D311/00

CPC classification number: C07C311/29 ,  C07C311/13 ,  C07C311/20 ,  C07C311/22 ,  C07C311/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2603/08 ,  C07C2603/18 ,  C07C2603/30 ,  C07D205/04 ,  C07D207/48 ,  C07D209/44 ,  C07D211/58 ,  C07D211/96 ,  C07D213/18 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D217/08 ,  C07D231/12 ,  C07D233/64 ,  C07D237/12 ,  C07D239/22 ,  C07D243/08 ,  C07D257/04 ,  C07D261/08 ,  C07D271/06 ,  C07D271/107 ,  C07D277/26 ,  C07D277/36 ,  C07D277/82 ,  C07D295/26 ,  C07D307/79 ,  C07D307/91 ,  C07D333/18 ,  C07D333/34 ,  C07D333/36 ,  C07D333/38 ,  C07D333/62 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

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 R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 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）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X为单键等，而A 1为取代的C _{3-14个烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基， 烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12） 相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。}

公开(公告)号：US07060844B2

公开(公告)日：2006-06-13

申请号：US10405577

申请日：2003-04-01

Applicant: Steven W. Andrews ,  Xialing Guo ,  Zhen Zhu ,  Clarence E. Hull, III ,  Julie A. Wurster ,  Shimiao Wang ,  Edward H. Wang ,  Thomas Malone

Inventor： Steven W. Andrews ,  Xialing Guo ,  Zhen Zhu ,  Clarence E. Hull, III ,  Julie A. Wurster ,  Shimiao Wang ,  Edward H. Wang ,  Thomas Malone

IPC: C07D405/04

CPC classification number: C07D405/04 ,  C07D405/14 ,  C07D491/10

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.