公开(公告)号：US20110294893A1

公开(公告)日：2011-12-01

申请号：US13205220

申请日：2011-08-08

Applicant: David F. Woodward ,  Steven W. Andrews ,  Robert M. Burk ,  Michael E. Garst

Inventor： David F. Woodward ,  Steven W. Andrews ,  Robert M. Burk ,  Michael E. Garst

IPC: A61K31/165 ,  A61P27/06 ,  A61P27/02

CPC classification number: A61K31/559 ,  A61K31/381 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/5585 ,  C07C35/21 ,  C07C215/42 ,  C07C235/34 ,  C07C247/10 ,  C07C255/36 ,  C07C405/00 ,  C07C2601/08 ,  Y10S514/913

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract translation: 本发明提供环戊烷庚酸，2-环烷基或芳基烷基化合物，其可以在1-位被氨基，酰氨基，醚或酯基取代，例如1-OH环戊烷庚酸，2-（环烷基或芳烷基 ）化合物。 本发明的环戊烷庚酸2-（环烷基或芳基烷基）化合物是有效的眼部低血压剂，特别适用于治疗青光眼。 此外，本发明的环戊烷庚酸，2-（环烷基或芳基烷基）化合物是广泛应用于全身高血压和肺部疾病的平滑肌松弛剂; 平滑肌松弛剂适用于胃肠道疾病，繁殖，生育，失禁，休克等。

公开(公告)号：US08017655B2

公开(公告)日：2011-09-13

申请号：US12339494

申请日：2008-12-19

Applicant: David F. Woodward ,  Steven W. Andrews ,  Robert M. Burk ,  Michael E. Garst

Inventor： David F. Woodward ,  Steven W. Andrews ,  Robert M. Burk ,  Michael E. Garst

IPC: A61K31/215 ,  A61K31/205 ,  A61K31/19 ,  A61K31/165

CPC classification number: A61K31/559 ,  A61K31/381 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/5585 ,  C07C35/21 ,  C07C215/42 ,  C07C235/34 ,  C07C247/10 ,  C07C255/36 ,  C07C405/00 ,  C07C2601/08 ,  Y10S514/913

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract translation: 本发明提供环戊烷庚酸，2-环烷基或芳基烷基化合物，其可以在1-位被氨基，酰氨基，醚或酯基取代，例如1-OH环戊烷庚酸，2-（环烷基或芳烷基 ）化合物。 本发明的环戊烷庚酸2-（环烷基或芳基烷基）化合物是有效的眼部低血压剂，特别适用于治疗青光眼。 此外，本发明的环戊烷庚酸，2-（环烷基或芳基烷基）化合物是广泛应用于全身高血压和肺部疾病的平滑肌松弛剂; 平滑肌松弛剂适用于胃肠道疾病，繁殖，生育，失禁，休克等。

公开(公告)号：US20110166122A1

公开(公告)日：2011-07-07

申请号：US13063894

申请日：2009-09-21

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

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

IPC: A61K31/5025 ,  A61K31/54 ,  C07D487/04 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  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: 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，是Trk激酶的抑制剂，可用于治疗可用Trk 激酶抑制剂。

公开(公告)号：US20100105894A1

公开(公告)日：2010-04-29

申请号：US12457391

申请日：2009-06-09

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

IPC: C07D243/08 ,  C07C229/02 ,  C07C307/00 ,  C07D409/02 ,  C07D231/10 ,  C07D401/02 ,  C07D261/06 ,  C07D333/34 ,  C07D241/04 ,  C07D271/06 ,  C07D257/04 ,  C07D295/00 ,  C07D215/14 ,  C07D205/04 ,  C07D413/02 ,  C07D241/36 ,  C07D413/14 ,  C07D223/14

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）所示的环丙烷化合物：其中，R 1为 - （CH 2 ）m-X-（CH 2）n -Al等，其中m和n相同或不同，各自为0〜6，X为单键等，而A1为取代的C3-14烃环基， 等等。; R2和R3相同或不同，各自为氢原子， - （CH2）p-X1-（CH2）q-A2等，其中p和q相同或不同，各自为0至6，X1 是单键等，A2是任选取代的C 3-14烃环基等; R4是-CO 2 R 9等，其中R9是氢原子等; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2）m 12 -X 12 - （CH 2）m 12 -R 30等，其中m12和m12相同或不同，各自为0至6， X12为单键等，R30为氢原子等; 或其前药或其药学上可接受的盐。

公开(公告)号：US20090148407A1

公开(公告)日：2009-06-11

申请号：US11996902

申请日：2006-07-17

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: A61K38/21 ,  C07K5/12 ,  A61K38/12 ,  C07D209/18 ,  C12N9/99 ,  A61K39/395

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：US20090099186A1

公开(公告)日：2009-04-16

申请号：US12089903

申请日：2006-10-10

Applicant: Leonid Beigelman ,  Steven W. Andrews ,  Kevin R. Condroski ,  Indrani Gunawaradana ,  Julia Haas

Inventor： Leonid Beigelman ,  Steven W. Andrews ,  Kevin R. Condroski ,  Indrani Gunawaradana ,  Julia Haas

IPC: A61K31/535 ,  C07C233/00 ,  A61K31/165 ,  C07D209/44 ,  A61K31/40 ,  C07D211/60 ,  C12N5/02 ,  C07D265/30 ,  A61K31/445 ,  A61K31/454 ,  C07D405/06 ,  A61K31/496

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: 实施方案提供了通式I-IV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：US06559173B1

公开(公告)日：2003-05-06

申请号：US10256382

申请日：2002-09-26

Applicant: Steven W. Andrews ,  Julie A. Wurster

Inventor： Steven W. Andrews ,  Julie A. Wurster

IPC: A61K314152

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：US06541504B1

公开(公告)日：2003-04-01

申请号：US10116309

申请日：2002-04-03

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

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

IPC: A61K31404

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.

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：US20150166564A1

公开(公告)日：2015-06-18

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: C07D495/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D403/12 ,  C07D417/14

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：US08865726B2

公开(公告)日：2014-10-21

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: C07D487/04 ,  A61K31/519 ,  A61P35/00

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。