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：WO2013036434A1

公开(公告)日：2013-03-14

申请号：PCT/US2012/053177

申请日：2012-08-30

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

Inventor： TUNG, Roger ,  MASSE, Craig E. ,  PANDYA, Bhaumik A.

IPC: C07D235/14 ,  A61K31/4184 ,  A61P9/00

CPC classification number: C07D235/16 ,  A61K31/4184 ,  A61K45/06 ,  C07D235/14

Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: [Insert Formulas B, A, I, C, and E] as described herein. 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 selective T-type calcium channel blocker.

Abstract translation: 本发明涉及新的四氢萘衍生物及其药学上可接受的盐，在一个实施方案中：如本文所述的[插入式B，A，I，C和E]。 本发明还提供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选择性T型钙通道阻断剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：WO2011003058A1

公开(公告)日：2011-01-06

申请号：PCT/US2010/040891

申请日：2010-07-02

Applicant: CONCERT PHARMACEUTICALS, INC. ,  MASSE, Craig E. ,  HARBESON, Scott, L. ,  TUNG, Roger, D.

Inventor： MASSE, Craig E. ,  HARBESON, Scott, L. ,  TUNG, Roger, D.

IPC: C07C45/00

CPC classification number: C07C69/734 ,  C07B2200/05 ,  C07B2200/07 ,  C07C59/46 ,  C07C69/732 ,  C07C311/51 ,  C07C2601/14 ,  C07C2602/22 ,  C07D317/34 ,  C07D319/06

Abstract: This invention relates to novel prostacyclin derivatives and acceptable salts thereof. 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 prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.

Abstract translation: 本发明涉及新型前列环素衍生物及其可接受的盐。 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前列环素有益治疗的疾病和病症的方法中的用途，特别是那些由全身和肺动脉血管床的扩张器或血小板有利地治疗的疾病和病症 聚集抑制剂。

公开(公告)号：WO2011116066A1

公开(公告)日：2011-09-22

申请号：PCT/US2011/028631

申请日：2011-03-16

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

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

IPC: A01N43/40 ,  A61K31/44

CPC classification number: C07B59/001 ,  C07B2200/05 ,  C07C49/255

Abstract: The invention relates to compounds of Formula (I) or (Ia), which are depicted herein, or pharmaceutically acceptable salts thereof or tautomers thereof.

Abstract translation: 本发明涉及本文所述的式（I）或（Ia）化合物或其药学上可接受的盐或其互变异构体。

公开(公告)号：WO2011060216A1

公开(公告)日：2011-05-19

申请号：PCT/US2010/056447

申请日：2010-11-12

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

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

IPC: C07B59/00 ,  C07D471/04

CPC classification number: C07B59/002 ,  C07D471/04

Abstract: This invention relates to novel substituted azaindoles 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 showing selective inhibitory activity of oncogenic B-Raf V600E protein kinase.

Abstract translation: 本发明涉及新的取代的阿魏酸和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显示致癌性B-RafV600E蛋白激酶的选择性抑制活性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：WO2011028820A1

公开(公告)日：2011-03-10

申请号：PCT/US2010/047557

申请日：2010-09-01

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

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

IPC: A01N43/90

CPC classification number: C07D487/04 ,  C07B2200/05 ,  C07D513/04

Abstract: This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier.

Abstract translation: 本发明涉及式A，B或C的新化合物及其药学上可接受的盐。 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。

公开(公告)号：WO2011017612A1

公开(公告)日：2011-02-10

申请号：PCT/US2010/044704

申请日：2010-08-06

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

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

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50

CPC classification number: A61K31/50 ,  A61K45/06 ,  C07D241/20 ,  A61K2300/00

Abstract: This invention relates to novel substituted diphenylpyrazines 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 PGI 2 receptor agonist.

Abstract translation: 本发明涉及新型取代的二苯基吡嗪及其药学上可接受的盐。 本发明还提供包含本发明化合物的组合物以及这些组合物在治疗通过施用PGI 2受体激动剂有益治疗的疾病和病症的方法中的用途。

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：WO2007061930A1

公开(公告)日：2007-05-31

申请号：PCT/US2006/044833

申请日：2006-11-17

Applicant: AMGEN INC. ,  XUE, Qiufen ,  ALBRECHT, Brian K. ,  ANDERSEN, Denise Lyn ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  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 ,  YANG, Bryant ,  ZHONG, Wenge

Inventor： XUE, Qiufen ,  ALBRECHT, Brian K. ,  ANDERSEN, Denise Lyn ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  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 ,  YANG, Bryant ,  ZHONG, Wenge

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

CPC classification number: C07D405/12 ,  C07D413/12

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 R 1 , W, B, 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R 1，W，B，R 3，R 4，R 4， SUP> 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：WO2007024680A1

公开(公告)日：2007-03-01

申请号：PCT/US2006/032314

申请日：2006-08-18

Applicant: AMGEN INC. ,  BUCHANAN, John L. ,  BUCKNER, William H. ,  CARDOZO, Mario G. ,  DIMAURO, Erin F. ,  FU, Jiasheng ,  HAO, Xiaolin ,  JIAO, XianYun ,  KAYSER, Frank ,  KOPECKY, David J. ,  MASSE, Craig E. ,  TOMLINSON, Susan A. ,  WHITE, Ryan ,  ZHU, Xiaotian

Inventor： BUCHANAN, John L. ,  BUCKNER, William H. ,  CARDOZO, Mario G. ,  DIMAURO, Erin F. ,  FU, Jiasheng ,  HAO, Xiaolin ,  JIAO, XianYun ,  KAYSER, Frank ,  KOPECKY, David J. ,  MASSE, Craig E. ,  TOMLINSON, Susan A. ,  WHITE, Ryan ,  ZHU, Xiaotian

IPC: C07D487/04 ,  C07D231/56 ,  C07D403/06 ,  C07D405/06 ,  C07D401/14 ,  A61K31/519 ,  A61K31/416 ,  A61P19/00 ,  A61P17/00 ,  A61P35/00

CPC classification number: C07D403/06 ,  C07D231/56 ,  C07D401/14 ,  C07D405/06 ,  C07D487/04

Abstract: The present invention relates to compounds of Formula (I) or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.

Abstract translation: 本发明涉及式（I）的化合物或立体异构体，互变异构体，溶剂化物，药学上可接受的盐或其前药，含有该化合物的药物制剂，使用该化合物的治疗方法，例如蛋白酪氨酸激酶 - 相关疾病如免疫学和肿瘤学疾病以及制备包含该化合物的药物的方法。