公开(公告)号：US20110130349A1

公开(公告)日：2011-06-02

申请号：US12952713

申请日：2010-11-23

Applicant: Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

Inventor： Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

IPC: A61K38/07 ,  C07K5/062 ,  A61K38/05 ,  C07K5/113 ,  C07F9/09 ,  A61K31/688 ,  A61P37/02 ,  A61P29/00 ,  A61P17/00 ,  A61P17/06 ,  A61P31/00 ,  A61P37/08 ,  A61P9/00

CPC classification number: A61K31/661 ,  A61K31/4045 ,  C07F9/02 ,  C07F9/091 ,  C07F9/5728

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

Abstract translation: 本发明涉及可用于预防或治疗与Toll样受体2激活相关的疾病或病症的化合物和方法。

公开(公告)号：US20110105427A1

公开(公告)日：2011-05-05

申请号：US12917669

申请日：2010-11-02

Applicant: Jane Daun ,  Heather A. Davis ,  Bruce DeCosta ,  Fabian Gusovsky ,  Ieharu Hishinuma ,  Yimin Jiang ,  Toshihiko Kaneko ,  Kouichi Kikuchi ,  Seiichi Kobayashi ,  André Lescarbeau ,  Xiang-Yi Li ,  Kenzo Muramoto ,  Norihito Ohi ,  Marc Pesant ,  Boris M. Seletsky ,  Motohiro Soejima ,  Mark Spyvee ,  Lynda Tremblay ,  Ye Yao ,  Hiromitsu Yokohama ,  Yan (Janet) Zhao ,  Wanjun Zheng

Inventor： Jane Daun ,  Heather A. Davis ,  Bruce DeCosta ,  Fabian Gusovsky ,  Ieharu Hishinuma ,  Yimin Jiang ,  Toshihiko Kaneko ,  Kouichi Kikuchi ,  Seiichi Kobayashi ,  André Lescarbeau ,  Xiang-Yi Li ,  Kenzo Muramoto ,  Norihito Ohi ,  Marc Pesant ,  Boris M. Seletsky ,  Motohiro Soejima ,  Mark Spyvee ,  Lynda Tremblay ,  Ye Yao ,  Hiromitsu Yokohama ,  Yan (Janet) Zhao ,  Wanjun Zheng

IPC: A61K31/437 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/541 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/55 ,  A61K31/439 ,  A61K31/4725 ,  A61K31/695 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P17/06 ,  A61P11/06 ,  A61P9/00

CPC classification number: A61K31/437 ,  C07D471/04

Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.

Abstract translation: 本发明提供了具有式（I）的化合物：其中R 1，R 2，R 3和n如本文中一般和本领域和亚类所述，并且另外提供其药物组合物，及其用于治疗炎症或自身免疫的方法 和增殖性疾病以及作为细胞粘附分子表达和炎性细胞因子信号转导的抑制剂。

公开(公告)号：US20110065916A1

公开(公告)日：2011-03-17

申请号：US12739286

申请日：2008-11-26

Applicant: Mark Spyvee ,  Boris M. Seletsky ,  Shawn Schiller ,  Francis Fang

Inventor： Mark Spyvee ,  Boris M. Seletsky ,  Shawn Schiller ,  Francis Fang

IPC: C07D487/20

CPC classification number: C07D471/20 ,  C07D513/04

Abstract: A method of making a compound of Formula I: is carried out by (a) providing a compound of Formula (II) or (III): wherein ring A is C3-14 aryl or C3-14 heteroaryl such as phenyl or furanyl, and then (b) combining the compound of Formula (II) or (III) with an acid to produce a compound of Formula I.

Abstract translation: 通过（a）提供式（II）或（III）的化合物来进行制备式I化合物的方法：其中环A为C 3-8芳基或C 3-14杂芳基，例如苯基或呋喃基，和 然后（b）将式（II）或（III）的化合物与酸组合以产生式I的化合物。

公开(公告)号：US07868002B2

公开(公告)日：2011-01-11

申请号：US11906056

申请日：2007-09-28

Applicant: Jane Daun ,  Heather A. Davis ,  Bruce DeCosta ,  Fabian Gusovsky ,  Ieharu Hishinuma ,  Yimin Jiang ,  Toshihiko Kaneko ,  Kouichi Kikuchi ,  Seiichi Kobayashi ,  André Lescarbeau ,  Xiang-Yi Li ,  Kenzo Muramoto ,  Norihito Ohi ,  Marc Pesant ,  Boris M. Seletsky ,  Motohiro Soejima ,  Mark Spyvee ,  Lynda Tremblay ,  Ye Yao ,  Hiromitsu Yokohama ,  Yan (Janet) Zhao ,  Wanjun Zheng

Inventor： Jane Daun ,  Heather A. Davis ,  Bruce DeCosta ,  Fabian Gusovsky ,  Ieharu Hishinuma ,  Yimin Jiang ,  Toshihiko Kaneko ,  Kouichi Kikuchi ,  Seiichi Kobayashi ,  André Lescarbeau ,  Xiang-Yi Li ,  Kenzo Muramoto ,  Norihito Ohi ,  Marc Pesant ,  Boris M. Seletsky ,  Motohiro Soejima ,  Mark Spyvee ,  Lynda Tremblay ,  Ye Yao ,  Hiromitsu Yokohama ,  Yan (Janet) Zhao ,  Wanjun Zheng

IPC: C07D413/14 ,  C07D471/02 ,  A61K31/4745 ,  A61K31/5377 ,  A61P11/06 ,  A61P19/02 ,  A61P25/00 ,  A61P3/10 ,  A61P9/00

CPC classification number: A61K31/437 ,  C07D471/04

Abstract: As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I), and pharmaceutical compositions thereof, as described generally and in classes and subclasses herein, as well as methods of making and using such compounds.

Abstract translation: 如上所述，仍然需要开发可用于治疗炎性或自身免疫性和增殖性疾病的新型治疗剂。 本发明提供了通式（I）的新型化合物及其药物组合物，如本文中一般和本课程和亚类所述，以及制备和使用这些化合物的方法。

公开(公告)号：US20090186855A1

公开(公告)日：2009-07-23

申请号：US12416489

申请日：2009-04-01

Applicant: Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

Inventor： Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

IPC: A61K31/675 ,  C07F9/02 ,  C07C69/003 ,  A61K31/66 ,  C07D209/04 ,  A61K31/404 ,  A61P37/00

CPC classification number: A61K31/661 ,  A61K31/4045 ,  C07F9/02 ,  C07F9/091 ,  C07F9/5728

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

Abstract translation: 本发明涉及可用于预防或治疗与Toll样受体2激活相关的疾病或病症的化合物和方法。

公开(公告)号：US20080051434A1

公开(公告)日：2008-02-28

申请号：US11701969

申请日：2007-02-02

Applicant: James Kowalczyk ,  Galina Kuznetsov ,  Shawn Schiller ,  Boris Seletsky ,  Mark Spyvee ,  Hu Yang

Inventor： James Kowalczyk ,  Galina Kuznetsov ,  Shawn Schiller ,  Boris Seletsky ,  Mark Spyvee ,  Hu Yang

IPC: A61K31/445 ,  A61K31/164 ,  A61K31/195 ,  A61K31/221 ,  A61P43/00 ,  C07C233/00 ,  C07D221/00 ,  C07C229/00 ,  A61P35/00 ,  A61K31/40 ,  A61K31/426

CPC classification number: C07K7/06 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  C07C237/22 ,  C07D207/08 ,  C07D207/16 ,  C07D211/60 ,  C07D295/185 ,  C07D401/14 ,  C07K5/06078 ,  C07K5/06156 ,  C07K5/06165 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  C07K5/1016

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract translation: 本发明提供具有式（I）的化合物：另外提供其合成方法及其用于治疗癌症的方法，其中R 1 -R 7 X 1，X 2，R 3，Q 3和n如本文所定义。

公开(公告)号：US20050113345A1

公开(公告)日：2005-05-26

申请号：US10973164

申请日：2004-10-25

Applicant: Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

Inventor： Jesse Chow ,  Fabian Gusovksy ,  Lynn Hawkins ,  Mark Spyvee

IPC: A61K20060101 ,  A61K31/40 ,  A61K31/66 ,  C07F9/141 ,  C07F9/547

CPC classification number: A61K31/661 ,  A61K31/4045 ,  C07F9/02 ,  C07F9/091 ,  C07F9/5728

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

Abstract translation: 本发明涉及可用于预防或治疗与Toll样受体2激活相关的疾病或病症的化合物和方法。

公开(公告)号：US20180086700A1

公开(公告)日：2018-03-29

申请号：US15560743

申请日：2016-03-23

Applicant: Mark SPYVEE ,  UNIVERSITY OF MIAMI ,  UNIVERSITY OF MARYLAND, BALTIMORE

Inventor： Anthony J. Capobianco ,  Alex Mackerell, JR. ,  Mark Spyvee

IPC: C07D207/444 ,  C07D277/54

CPC classification number: C07D207/444 ,  A61K31/4015 ,  A61K31/426 ,  C07D277/36 ,  C07D277/54

Abstract: Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

公开(公告)号：US07915306B2

公开(公告)日：2011-03-29

申请号：US10657910

申请日：2003-09-09

Applicant: Kenichi Chiba ,  Hong Du ,  Yoshihito Eguchi ,  Masanori Fujita ,  Masaki Goto ,  Fabian Gusovsky ,  Jean-Christophe Harmange ,  Atsushi Inoue ,  Megumi Kawada ,  Takatoshi Kawai ,  Yoshiyuki Kawakami ,  Akifumi Kimura ,  Makoto Kotake ,  Yoshikazu Kuboi ,  Tomohiro Matsushima ,  Yoshiharu Mizui ,  Kenzo Muramoto ,  Hideki Sakurai ,  Yong-Chun Shen ,  Hiroshi Shirota ,  Mark Spyvee ,  Isao Tanaka ,  John (Yuan) Wang ,  Ray Wood ,  Satoshi Yamamoto ,  Naoki Yoneda

Inventor： Kenichi Chiba ,  Hong Du ,  Yoshihito Eguchi ,  Masanori Fujita ,  Masaki Goto ,  Fabian Gusovsky ,  Jean-Christophe Harmange ,  Atsushi Inoue ,  Megumi Kawada ,  Takatoshi Kawai ,  Yoshiyuki Kawakami ,  Akifumi Kimura ,  Makoto Kotake ,  Yoshikazu Kuboi ,  Tomohiro Matsushima ,  Yoshiharu Mizui ,  Kenzo Muramoto ,  Hideki Sakurai ,  Yong-Chun Shen ,  Hiroshi Shirota ,  Mark Spyvee ,  Isao Tanaka ,  John (Yuan) Wang ,  Ray Wood ,  Satoshi Yamamoto ,  Naoki Yoneda

IPC: A61K31/335

CPC classification number: C07D493/04 ,  C07D313/00

Abstract: The present invention provides compositions comprising compounds having formula (I): and additionally provides methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein. In certain embodiments, the compositions are for systemic (e.g., oral) administration. In certain embodiments, methods for the treatment of various disorders including inflammatory or autoimmune disorders comprise systemically (e.g., orally) administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I).

Abstract translation: 本发明提供了包含具有式（I）的化合物的组合物：另外提供了其用于治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管发生的疾病的方法，其中R1-R11，X，Y， Z和n如本文所定义。 在某些实施方案中，组合物用于全身（例如口服）给药。 在某些实施方案中，用于治疗各种疾病（包括炎性或自身免疫性疾病）的方法包括全身（例如，口服）向有需要的受试者施用治疗有效量的式（I）化合物。

公开(公告)号：US20100063095A1

公开(公告)日：2010-03-11

申请号：US12394882

申请日：2009-02-27

Applicant: James J. KOWALCZYK ,  Galina KUZNETSOV ,  Shawn SCHILLER ,  Boris M. SELETSKY ,  Mark SPYVEE ,  Hu YANG

Inventor： James J. KOWALCZYK ,  Galina KUZNETSOV ,  Shawn SCHILLER ,  Boris M. SELETSKY ,  Mark SPYVEE ,  Hu YANG

IPC: A61K31/454 ,  C07D211/60 ,  A61K31/445 ,  C07D401/14 ,  A61P35/00

CPC classification number: C07K7/06 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  C07C237/22 ,  C07D207/08 ,  C07D207/16 ,  C07D211/60 ,  C07D295/185 ,  C07D401/14 ,  C07K5/06078 ,  C07K5/06156 ,  C07K5/06165 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  C07K5/1016

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract translation: 本发明提供具有式（I）的化合物：另外提供其合成方法及其用于治疗癌症的方法，其中R1-R7，X1，X2，R，Q和n如本文所定义 。