公开(公告)号：WO2010047819A8

公开(公告)日：2010-07-29

申请号：PCT/US2009005773

申请日：2009-10-23

Applicant: CONCERT PHARMACEUTICALS INC ,  HARBESON SCOTT L ,  MASSE CRAIG E

Inventor： HARBESON SCOTT L ,  MASSE CRAIG E

IPC: A01N41/06

CPC classification number: C07D493/04

Abstract: This invention relates to novel hydroxyethylamino sulfonamides and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.

Abstract translation: 本发明涉及新的羟乙基氨基磺酰胺及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用具有作为HIV（人类免疫缺陷病毒）蛋白酶抑制剂的能力的化合物有益治疗的疾病和病症的方法中的用途。

公开(公告)号：WO2010045551A1

公开(公告)日：2010-04-22

申请号：PCT/US2009/060996

申请日：2009-10-16

Applicant: CONCERT PHARMACEUTICALS, INC. ,  MASSE, Craig, E.

Inventor： MASSE, Craig, E.

IPC: C07D311/00 ,  C07D491/04

CPC classification number: C07D311/86

Abstract: This invention relates to novel compounds that are xanthenone-4-acetic acid derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel xanthenone-4-acetic acid derivatives that are derivatives of AS 1404. This invention also provides compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a vascular disrupting agent, such as AS 1404.

Abstract translation: 本发明涉及x吨酮-4-乙酸衍生物及其药学上可接受的盐的新化合物。 更具体地说，本发明涉及作为AS 1404衍生物的新型x吨酮-4-乙酸衍生物。本发明还提供了包含一种或多种本发明化合物和载体的组合物，以及所公开的化合物和组合物在方法 治疗通过施用血管破坏剂如AS 1404有益治疗的疾病和病症。

公开(公告)号：WO2009154754A3

公开(公告)日：2009-12-23

申请号：PCT/US2009/003628

申请日：2009-06-17

Applicant: CONCERT PHARMACEUTICALS, INC. ,  LIU, Julie, F. ,  TANG, Xuejun ,  HARBESON, Scott, L. ,  MASSE, Craig, E.

Inventor： LIU, Julie, F. ,  TANG, Xuejun ,  HARBESON, Scott, L. ,  MASSE, Craig, E.

IPC: C07D295/02 ,  C07D295/06 ,  C07D295/12 ,  A61K31/5377 ,  C07C215/10 ,  C07C215/12 ,  C07D413/10 ,  C07D413/14

Abstract: The present invention is directed to a process for preparing a 2,26,6- d 4 -morpholine derivative represented by Structural Formula (I), or a salt thereof.

公开(公告)号：WO2009154754A2

公开(公告)日：2009-12-23

申请号：PCT/US2009003628

申请日：2009-06-17

Applicant: CONCERT PHARMACEUTICALS INC ,  LIU JULIE F ,  TANG XUEJUN ,  HARBESON SCOTT L ,  MASSE CRAIG E

Inventor： LIU JULIE F ,  TANG XUEJUN ,  HARBESON SCOTT L ,  MASSE CRAIG E

IPC: C07D295/02 ,  A61K31/5377 ,  C07C215/10 ,  C07C215/12 ,  C07D295/06 ,  C07D295/12 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D413/10 ,  A61K31/5377 ,  A61K45/06 ,  C07B2200/05 ,  C07C215/12 ,  C07D263/06 ,  C07D295/02 ,  C07D295/033 ,  C07D295/06 ,  C07D295/12 ,  C07D295/135 ,  C07D413/14

Abstract: The present invention is directed to a process for preparing a 2,26,6-d 4 -morpholine derivative represented by Structural Formula (I), or a salt thereof.

Abstract translation: 本发明涉及一种制备由结构式（I）表示的2,26,6-d-吗啉衍生物或其盐的方法。

公开(公告)号：WO2009051782A1

公开(公告)日：2009-04-23

申请号：PCT/US2008/011856

申请日：2008-10-17

Applicant: CONCERT PHARMACEUTICALS INC. ,  MASSE, Craig E.

Inventor： MASSE, Craig E.

IPC: C07D239/48 ,  A61K31/505 ,  A61P31/18

CPC classification number: C07D239/48

Abstract: This disclosure relates to novel di-aryl-pyrimidine (DAPY) compounds and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a non-nucleoside reverse transcriptase inhibitor (NNRTI).

Abstract translation: 本公开涉及新的二芳基嘧啶（DAPY）化合物及其药学上可接受的盐。 本公开还提供了包含本公开的化合物和这种组合物在治疗通过施用非核苷逆转录酶抑制剂（NNRTI）有益治疗的疾病和病症的方法中的用途的组合物。

公开(公告)号：WO2007061670A1

公开(公告)日：2007-05-31

申请号：PCT/US2006/044058

申请日：2006-11-13

Applicant: AMGEN INC. ,  ZHONG, Wenge ,  HITCHCOCK, Stephen ,  ALBRECHT, Brian K ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HICKMAN, Dean ,  HORNE, Daniel ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  XUE, Qiufen ,  YANG, Bryant

Inventor： ZHONG, Wenge ,  HITCHCOCK, Stephen ,  ALBRECHT, Brian K ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HICKMAN, Dean ,  HORNE, Daniel ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  XUE, Qiufen ,  YANG, Bryant

IPC: C07D405/12 ,  C07D413/12 ,  A61K31/44 ,  A61P25/28

CPC classification number: C07D405/12 ,  C07D311/68 ,  C07D413/12 ,  C07D491/052

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A, B, W, R 3 , R 4 , R 5 , i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式（I）; 其中A，B，W，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式（I）化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过施用式（I）化合物或其组合物，包括它们， 到一个主题。 本发明还包括式（II）和（III）的其它实施方案，可用于制备本发明化合物的中间体和方法。

公开(公告)号：WO2010138889A8

公开(公告)日：2011-02-17

申请号：PCT/US2010036682

申请日：2010-05-28

Applicant: CONCERT PHARMACEUTICALS INC ,  MASSE CRAIG E

Inventor： MASSE CRAIG E

IPC: C07K5/06 ,  A61K38/05 ,  A61P31/14

CPC classification number: C07K5/06052 ,  A61K38/212 ,  A61K2300/00

Abstract: This invention relates to novel compounds that are peptides derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel peptides that are deuterated derivatives of boceprevir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating HCV infection.

Abstract translation: 本发明涉及作为肽衍生物和药学上可接受的盐的新型化合物。 更具体地，本发明涉及作为波普瑞韦的氘代衍生物的新型肽。 本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗HCV感染的方法中的用途。

公开(公告)号：WO2009121042A8

公开(公告)日：2010-11-25

申请号：PCT/US2009038701

申请日：2009-03-27

Applicant: CONCERT PHARMACEUTICALS INC ,  MASSE CRAIG E ,  TUNG ROGER

Inventor： MASSE CRAIG E ,  TUNG ROGER

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/94

Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.

Abstract translation: 本发明涉及新的喹唑啉衍生物及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过抑制细胞表面酪氨酸受体激酶有益治疗的疾病和病症的方法中的用途。

公开(公告)号：WO2010068480A1

公开(公告)日：2010-06-17

申请号：PCT/US2009/065872

申请日：2009-11-25

Applicant: CONCERT PHARMACEUTICALS, INC. ,  SILVERMAN, I., Robert ,  MASSE, Craig, E.

Inventor： SILVERMAN, I., Robert ,  MASSE, Craig, E.

IPC: C07D471/04 ,  A61K31/475 ,  A61P25/28

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/475 ,  A61K31/55 ,  A61K45/06

Abstract: This invention relates to novel tetrahydro-lH-pyrido[4,3-b]indoles, their derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by NMDA antagonists, acetylcholinesterase inhibitors, 5-HT6 antagonists, other neuroprotectors, antihistamines and agents that delay age-related pathologies and conditions.

Abstract translation: 本发明涉及新的四氢-1H-吡啶并[4,3-b]吲哚及其衍生物及其药学上可接受的盐。 本发明还提供了包含本发明化合物和这些组合物在治疗由NMDA拮抗剂，乙酰胆碱酯酶抑制剂，5-HT6拮抗剂，其它神经保护剂，抗组胺剂和延缓衰老的药剂有益治疗的疾病和病症的方法中的用途。 相关病理和病情。

公开(公告)号：WO2009121042A1

公开(公告)日：2009-10-01

申请号：PCT/US2009/038701

申请日：2009-03-27

Applicant: CONCERT PHARMACEUTICALS, INC. ,  MASSE, Craig, E. ,  TUNG, Roger

Inventor： MASSE, Craig, E. ,  TUNG, Roger

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/94

Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.

Abstract translation: 本发明涉及新的喹唑啉衍生物及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过抑制细胞表面酪氨酸受体激酶有益治疗的疾病和病症的方法中的用途。