公开(公告)号：US08269043B2

公开(公告)日：2012-09-18

申请号：US12588883

申请日：2009-10-30

Applicant: Richard D. Caldwell ,  Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Wen-Cherng Lee ,  Edward Yin-Shiang Lin ,  Xiaogao Liu ,  Bin Ma ,  Daniel M. Scott ,  Zhan Shi ,  Jermaine Thomas ,  Arthur G. Taveras ,  Guo Zhu Zheng

Inventor： Richard D. Caldwell ,  Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Wen-Cherng Lee ,  Edward Yin-Shiang Lin ,  Xiaogao Liu ,  Bin Ma ,  Daniel M. Scott ,  Zhan Shi ,  Jermaine Thomas ,  Arthur G. Taveras ,  Guo Zhu Zheng

IPC: C07C211/00 ,  C09B11/02 ,  A61K31/66

CPC classification number: A61K31/135 ,  A61K31/27 ,  C07C205/26 ,  C07C205/50 ,  C07C217/52 ,  C07C217/60 ,  C07C229/32 ,  C07C271/16 ,  C07D263/38 ,  C07F9/091 ,  C07F9/093 ,  C07F9/653 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：US20100105714A1

公开(公告)日：2010-04-29

申请号：US12525144

申请日：2008-01-30

Applicant: Lihong Sun ,  Wen-Cherng Lee ,  Paul Lyne

Inventor： Lihong Sun ,  Wen-Cherng Lee ,  Paul Lyne

IPC: A61K31/438 ,  C07D307/02 ,  A61K31/34 ,  C07D471/10 ,  C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04 ,  C07D405/04 ,  C07D491/08 ,  C07D519/00

Abstract: The invention features compounds of the general Formula (I): (formula should be inserted here) Compounds of Formula (I) possess unexpectedly high affinity for Alk5 and/or Alk4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.

Abstract translation: 本发明的特征在于通式（I）的化合物：（式中应该插入）式（I）化合物对Alk5和/或Alk4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗多种 疾病，包括纤维化疾病。

公开(公告)号：US20060106033A1

公开(公告)日：2006-05-18

申请号：US10526839

申请日：2003-09-05

Applicant: Wen-Cherng Lee ,  Mary Carter ,  Lihong Sun ,  Claudio Chuaqui ,  Zhongli Zheng ,  Juswinder Singh ,  Paula Boriack-Sjodin ,  Paul Lyne

Inventor： Wen-Cherng Lee ,  Mary Carter ,  Lihong Sun ,  Claudio Chuaqui ,  Zhongli Zheng ,  Juswinder Singh ,  Paula Boriack-Sjodin ,  Paul Lyne

IPC: C07D471/02 ,  A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: Compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I:

Abstract translation: 式I的化合物对Alk 5和/或Alk 4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化疾病在内的许多疾病。 在一个实施方案中，本发明的特征在于式I的化合物：

公开(公告)号：US06630512B2

公开(公告)日：2003-10-07

申请号：US10002341

申请日：2001-10-23

Applicant: Steven P. Adams ,  Ko-Chung Lin ,  Wen-Cherng Lee ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Charles E. Hammond ,  Yu-Sheng Liao ,  Julio Hernan Cuervo ,  Juswinder Singh

Inventor： Steven P. Adams ,  Ko-Chung Lin ,  Wen-Cherng Lee ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Charles E. Hammond ,  Yu-Sheng Liao ,  Julio Hernan Cuervo ,  Juswinder Singh

IPC: A61K31197

CPC classification number: C07D213/75 ,  A61K38/00 ,  C07C237/22 ,  C07C255/19 ,  C07C271/22 ,  C07C275/28 ,  C07C275/42 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C317/50 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/14 ,  C07D209/42 ,  C07D213/55 ,  C07D215/48 ,  C07D277/48 ,  C07D317/60 ,  C07D405/12 ,  C07K7/06

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

公开(公告)号：US06630503B1

公开(公告)日：2003-10-07

申请号：US09638652

申请日：2000-08-14

Applicant: Daniel Scott ,  Wen-Cherng Lee ,  Russell C. Petter ,  Mark Cornebise

Inventor： Daniel Scott ,  Wen-Cherng Lee ,  Russell C. Petter ,  Mark Cornebise

IPC: A61K3140

CPC classification number: C07D401/06 ,  A61K38/00 ,  C07D205/04 ,  C07D207/16 ,  C07D207/48 ,  C07D209/42 ,  C07D211/32 ,  C07D265/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07K5/0215 ,  C07K5/06165 ,  C07K5/06191

Abstract: A cell adhesion inhibitor of the general formula: R3—L—L′—R1 is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing and using such a cell adhesion inhibitor, as well as pharmaceutical compositions containing the same.

Abstract translation: 公开了通式的细胞粘附抑制剂。 本发明的抑制剂与VLA-4分子相互作用并抑制VLA-4依赖性细胞粘附。 还公开了制备和使用这种细胞粘附抑制剂的方法以及含有该细胞粘附抑制剂的药物组合物。

公开(公告)号：US06306840B1

公开(公告)日：2001-10-23

申请号：US08376372

申请日：1995-01-23

Applicant: Steven P. Adams ,  Ko-Chung Lin ,  Wen-Cherng Lee ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Charles E. Hammond ,  Yu-Sheng Liao

Inventor： Steven P. Adams ,  Ko-Chung Lin ,  Wen-Cherng Lee ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Charles E. Hammond ,  Yu-Sheng Liao

IPC: A61K3136

CPC classification number: C07D213/75 ,  A61K38/00 ,  C07C237/22 ,  C07C255/19 ,  C07C271/22 ,  C07C275/28 ,  C07C275/42 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C317/50 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/14 ,  C07D209/42 ,  C07D213/55 ,  C07D215/48 ,  C07D277/48 ,  C07D317/60 ,  C07D405/12 ,  C07K7/06

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

公开(公告)号：US06248713B1

公开(公告)日：2001-06-19

申请号：US08498237

申请日：1995-07-11

Applicant: Ko-Chung Lin ,  Steven P. Adams ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Julio Hernan Cuervo ,  Wen-Cherng Lee ,  Charles E. Hammond ,  Mary Beth Carter ,  Ronald G. Almquist

Inventor： Ko-Chung Lin ,  Steven P. Adams ,  Alfredo C. Castro ,  Craig N. Zimmerman ,  Julio Hernan Cuervo ,  Wen-Cherng Lee ,  Charles E. Hammond ,  Mary Beth Carter ,  Ronald G. Almquist

IPC: A61K3803

CPC classification number: C07K5/0821 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06034 ,  C07K5/06113 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/101 ,  C07K5/1013 ,  C07K5/1016 ,  C07K5/1024 ,  C07K14/78 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/863 ,  Y10S514/866 ,  Y10S514/885 ,  Y10S514/903 ,  Y10S530/868

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract translation: 本发明涉及可用于抑制和预防细胞粘附和细胞粘附介导的病理学的新型化合物。 本发明还涉及包含这些化合物的药物制剂及其用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。 本发明的化合物和药物组合物可用作治疗剂或预防剂。 它们特别适用于治疗许多炎性和自身免疫性疾病。

公开(公告)号：US20140100195A1

公开(公告)日：2014-04-10

申请号：US13646143

申请日：2012-10-05

Applicant: Richard D. Caldwell ,  Kevin M. GUCKIAN ,  Gnanasambandam KUMARA VEL ,  Wen-Cherng LEE ,  Edward Yin-Shiang LIN ,  Xiaogao LlU ,  Bin MA ,  Daniel M. SCOTT ,  Zhan SHl ,  Jermaine THOMAS ,  Arthur G. TAVERAS ,  Guo Zhu ZHENG

Inventor： Richard D. Caldwell ,  Kevin M. GUCKIAN ,  Gnanasambandam KUMARA VEL ,  Wen-Cherng LEE ,  Edward Yin-Shiang LIN ,  Xiaogao LlU ,  Bin MA ,  Daniel M. SCOTT ,  Zhan SHl ,  Jermaine THOMAS ,  Arthur G. TAVERAS ,  Guo Zhu ZHENG

IPC: A61K31/685 ,  A61K31/195 ,  C07C229/36 ,  A61K31/216 ,  C07C217/58 ,  A61K31/137 ,  C07D263/24 ,  A61K31/421 ,  C07D215/20 ,  A61K31/47 ,  C07F9/60 ,  A61K31/675 ,  C07D239/80 ,  A61K31/517 ,  C07D413/04 ,  C07F9/6512 ,  C07D277/64 ,  A61K31/428 ,  A61P37/06 ,  A61P7/00 ,  C07C233/47

CPC classification number: C07F9/6512 ,  C07C217/58 ,  C07C217/74 ,  C07C229/36 ,  C07C233/47 ,  C07C2602/10 ,  C07D215/06 ,  C07D215/20 ,  C07D215/227 ,  C07D233/32 ,  C07D239/74 ,  C07D239/80 ,  C07D263/24 ,  C07D277/64 ,  C07D401/04 ,  C07F9/091 ,  C07F9/60 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：US20120208819A1

公开(公告)日：2012-08-16

申请号：US13499835

申请日：2010-10-05

Applicant: Joseph Arndt ,  Timothy Chan ,  Kevin Guckian ,  Gnanasambandam Kumaravel ,  Wen-Cherng Lee ,  Edward Yin-Shiang Lin ,  Daniel Scott ,  Lihong Sun ,  Jermaine Thomas ,  Kurt van Vloten ,  Deping Wang ,  Lei Zhang ,  Daniel Erlanson

Inventor： Joseph Arndt ,  Timothy Chan ,  Kevin Guckian ,  Gnanasambandam Kumaravel ,  Wen-Cherng Lee ,  Edward Yin-Shiang Lin ,  Daniel Scott ,  Lihong Sun ,  Jermaine Thomas ,  Kurt van Vloten ,  Deping Wang ,  Lei Zhang ,  Daniel Erlanson

IPC: A61K31/53 ,  C07D401/14 ,  C07D409/14 ,  A61P35/00 ,  A61K31/444 ,  A61K31/519 ,  A61K31/4439 ,  A61K31/517 ,  C07D471/04 ,  C07D401/12

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/452 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  C07D213/82 ,  C07D213/85 ,  C07D241/26 ,  C07D241/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D473/34 ,  C07D487/04 ,  C07D491/052 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

Abstract translation: 本发明提供了可用作PDK1抑制剂的化合物。 本发明还提供了其组合物，以及治疗PDK1介导的疾病的方法。

公开(公告)号：US20100166819A1

公开(公告)日：2010-07-01

申请号：US12086954

申请日：2006-12-22

Applicant: Wen-Cherng Lee ,  Lihong Sun ,  Michael Hoemann ,  Deqiang Niu ,  Dingxue Yan ,  Claudio Chuaqui ,  Russell Petter ,  Helen (Xiaomei) Feng

Inventor： Wen-Cherng Lee ,  Lihong Sun ,  Michael Hoemann ,  Deqiang Niu ,  Dingxue Yan ,  Claudio Chuaqui ,  Russell Petter ,  Helen (Xiaomei) Feng

IPC: A61K31/55 ,  A61K9/00 ,  A61K31/502 ,  A61K31/517 ,  A61K31/438 ,  C07D487/10 ,  C07D401/14 ,  C07D403/14 ,  A61P35/00 ,  A61P9/12 ,  A61P9/10 ,  A61P27/02 ,  A61P1/16 ,  A61P13/12

CPC classification number: C07D487/10 ,  C07D471/10

Abstract: The invention is related to compounds of formula (I) that can be used as antagonists of the TGFβ family type I receptors, Alk5 and/or Alk4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable.

Abstract translation: 本发明涉及可用作TGFβb拮抗剂的式（I）化合物; 家族I型受体，Alk5和/或Alk4，组合物和使用方法。 式（I）化合物可用于预防和/或治疗诸如纤维化（例如肾纤维化，肺纤维化和肝纤维化），进行性癌症或其它TGFβb的降低的疾病; 家庭信号传导活动是可取的。