公开(公告)号：WO2017015496A1

公开(公告)日：2017-01-26

申请号：PCT/US2016/043406

申请日：2016-07-21

Applicant: IMMUNOGEN, INC.

Inventor： GÉRARD, Baudouin ,  SHIZUKA, Manami ,  MILLER, Michael Louis ,  SILVA, Richard A.

IPC: C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04 ,  C07K5/0804

Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

公开(公告)号：WO2017015495A1

公开(公告)日：2017-01-26

申请号：PCT/US2016/043402

申请日：2016-07-21

Applicant: IMMUNOGEN, INC.

Inventor： GÉRARD, Baudouin ,  SHIZUKA, Manami ,  MILLER, Michael, Louis ,  SILVA, Richard, A.

IPC: C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04 ,  C07K5/0804

Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Abstract translation: 本发明涉及制备吲哚并苯并二氮杂二聚体化合物及其合成前体的新方法。

公开(公告)号：WO2011089396A3

公开(公告)日：2012-04-26

申请号：PCT/GB2011000079

申请日：2011-01-21

Applicant: ST GEORGE S HOSPITAL MEDICAL SCHOOL ,  UNIV MANCHESTER ,  ROBINSON CLIVE ,  ZHANG JIHUI ,  GARROD DAVID RONALD ,  PERRIOR TREVOR ROBERT ,  NEWTON GARY KARL ,  JENKINS KERRY ,  BEEVERS REBEKAH ELISABETH ,  KIMBERLEY MERIEL RUTH ,  STEWART MARK RICHARD

Inventor： ROBINSON CLIVE ,  ZHANG JIHUI ,  GARROD DAVID RONALD ,  PERRIOR TREVOR ROBERT ,  NEWTON GARY KARL ,  JENKINS KERRY ,  BEEVERS REBEKAH ELISABETH ,  KIMBERLEY MERIEL RUTH ,  STEWART MARK RICHARD

IPC: C07K5/06 ,  A01N43/00 ,  A61K38/06 ,  A61P37/08 ,  C07K5/08

CPC classification number: C07K5/0202 ,  A01N37/46 ,  A01N43/16 ,  A01N43/30 ,  A01N43/36 ,  A01N43/38 ,  A01N43/40 ,  A01N43/42 ,  A01N43/48 ,  A01N43/60 ,  A01N43/72 ,  A01N43/84 ,  A61K38/00 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07K5/06008 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.

Abstract translation: 本发明一般涉及治疗化合物领域，更具体地涉及式（X）的某些丙酮酰胺化合物（为了方便起见，统称为“PVA化合物”），其特别是抑制尘螨组 1肽酶变应原（例如，Der p 1，Der f 1，Eur m 1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制尘螨组1肽酶变应原和治疗由 尘螨组1肽酶变应原; 通过抑制尘螨组1肽酶变应原而得到改善; 哮喘; 鼻炎; 过敏性结膜炎 特应性皮炎; 由尘螨触发的过敏状况; 由尘螨组1肽酶变应原触发的过敏状况; 和犬特应性

公开(公告)号：WO2011063502A1

公开(公告)日：2011-06-03

申请号：PCT/CA2010/001820

申请日：2010-11-18

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  LLINAS-BRUNET , Montse ,  BORDELEAU, Josée ,  GODBOUT, Cédrickx ,  LEBLANC, Mélissa ,  MOREAU, Benoît ,  O'MEARA, Jeffrey

Inventor： LLINAS-BRUNET , Montse ,  BORDELEAU, Josée ,  GODBOUT, Cédrickx ,  LEBLANC, Mélissa ,  MOREAU, Benoît ,  O'MEARA, Jeffrey

IPC: C07D487/04 ,  A61K31/4709 ,  A61P31/14

CPC classification number: C07D487/04 ,  A61K31/4709 ,  A61K38/00 ,  C07K5/0804 ,  C07K5/1024

Abstract: Compounds of Formula (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined herein, maintain good activity against NS3 proteases containing clinically relevant genotype 1 a R155K and genotype 1 b D168V resistance mutations. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.

Abstract translation: 其中R 1，R 2，R 3，R 4和R 5在本文中定义的式（I）化合物对于含有临床相关基因型1的R155K和基因型1B D168V抗性突变的NS3蛋白酶保持良好的活性。 该化合物可用作用于治疗丙型肝炎病毒感染的HCV NS3蛋白酶的抑制剂。

公开(公告)号：WO2011038283A1

公开(公告)日：2011-03-31

申请号：PCT/US2010/050284

申请日：2010-09-24

Applicant: HOFFMANN-LA ROCHE INC. ,  F. HOFFMANN-LA ROCHE LTD ,  SEIWERT, Scott, D. ,  NICHOLAS, John, B. ,  BUCKMAN, Brad ,  SEREBRYANY, Vladimir

Inventor： SEIWERT, Scott, D. ,  NICHOLAS, John, B. ,  BUCKMAN, Brad ,  SEREBRYANY, Vladimir

IPC: C07D487/04 ,  A61K38/05 ,  A61P31/14 ,  A61K31/4035 ,  A61P1/16 ,  C07K5/072

CPC classification number: A61K31/4035 ,  A61K38/212 ,  A61K38/217 ,  C07D487/04 ,  C07K5/0804

Abstract: The embodiments provide compounds of the general Formula I, 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：WO2011034518A1

公开(公告)日：2011-03-24

申请号：PCT/US2009/056937

申请日：2009-09-15

Applicant: TAIGEN BIOTECHNOLOGY CO., LTD. ,  LIU, Chen-Fu ,  LEE, Kuang-Yuan ,  CHENG, Pei-Chin ,  LIU, Yo-Chin ,  LO, Pin ,  TSENG, Kuo-Feng ,  CHEN, Chih-Ming ,  KING, Chi-Hsin Richard ,  LIN, Chu-Chung

Inventor： LIU, Chen-Fu ,  LEE, Kuang-Yuan ,  CHENG, Pei-Chin ,  LIU, Yo-Chin ,  LO, Pin ,  TSENG, Kuo-Feng ,  CHEN, Chih-Ming ,  KING, Chi-Hsin Richard ,  LIN, Chu-Chung

IPC: C07D403/12 ,  C07D401/12 ,  A61K31/4355 ,  A61P31/12

CPC classification number: C07K5/0804 ,  A61K31/4355 ,  A61K31/519 ,  A61K38/00 ,  C07D491/048 ,  C07D519/00

Abstract: This invention relates to macrocyclic compounds shown in the specification. These compounds can be used to treat hepatitis C virus infection.

Abstract translation: 本发明涉及说明书中所示的大环化合物。 这些化合物可用于治疗丙型肝炎病毒感染。

公开(公告)号：WO2011002807A1

公开(公告)日：2011-01-06

申请号：PCT/US2010/040473

申请日：2010-06-29

Applicant: AVILA THERAPEUTICS, INC. ,  PETTER, Russell, C. ,  SINGH, Juswinder ,  KLUGE, Arthur, F. ,  NIU, Deqiang ,  QIAO, Lixin ,  GHOSH, Shomir

Inventor： PETTER, Russell, C. ,  SINGH, Juswinder ,  KLUGE, Arthur, F. ,  NIU, Deqiang ,  QIAO, Lixin ,  GHOSH, Shomir

IPC: C07D487/00 ,  A61K31/40

CPC classification number: A61K47/48246 ,  A61K38/00 ,  A61K38/005 ,  A61K38/06 ,  A61K38/12 ,  A61K47/64 ,  C07D401/12 ,  C07K5/0202 ,  C07K5/06165 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0821 ,  C12N9/506 ,  C12N9/96 ,  C12Y304/00

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract translation: 本发明提供了化合物，其药学上可接受的组合物及其使用方法。

公开(公告)号：WO2010021717A3

公开(公告)日：2010-04-15

申请号：PCT/US2009004743

申请日：2009-08-20

Applicant: SEQUOIA PHARMACEUTICALS INC ,  EISSENSTAT MICHAEL ,  LU RONGJIAN ,  KANG SANG UK

Inventor： EISSENSTAT MICHAEL ,  LU RONGJIAN ,  KANG SANG UK

IPC: C07D487/14 ,  A61K31/407 ,  A61P31/14 ,  C07K5/08

CPC classification number: C07D487/14 ,  C07K5/0804

Abstract: Novel compounds that are potent inhibitors of hepatitis C virus protease are provided. Pharmaceutical compositions containing one or more of these inhibitors, methods of preparing the inhibitors and methods of using the inhibitors to treat hepatitis C and related disorders also are provided.

Abstract translation: 提供了作为丙型肝炎病毒蛋白酶的有效抑制剂的新型化合物。 还提供了含有这些抑制剂中的一种或多种的药物组合物，制备抑制剂的方法和使用该抑制剂治疗丙型肝炎和相关疾病的方法。

公开(公告)号：WO2010021717A2

公开(公告)日：2010-02-25

申请号：PCT/US2009/004743

申请日：2009-08-20

Applicant: SEQUOIA PHARMACEUTICALS, INC. ,  EISSENSTAT, Michael ,  LU, Rongjian ,  KANG, Sang, Uk

Inventor： EISSENSTAT, Michael ,  LU, Rongjian ,  KANG, Sang, Uk

IPC: C07D471/14 ,  A61K31/395 ,  A61P31/12

CPC classification number: C07D487/14 ,  C07K5/0804

Abstract: Novel compounds that are potent inhibitors of hepatitis C virus protease are provided. Pharmaceutical compositions containing one or more of these inhibitors, methods of preparing the inhibitors and methods of using the inhibitors to treat hepatitis C and related disorders also are provided.

Abstract translation: 提供了作为丙型肝炎病毒蛋白酶的有效抑制剂的新型化合物。 还提供了含有一种或多种这些抑制剂的药物组合物，制备该抑制剂的方法以及使用该抑制剂治疗丙型肝炎和相关病症的方法。

公开(公告)号：WO2009137432A1

公开(公告)日：2009-11-12

申请号：PCT/US2009/042773

申请日：2009-05-05

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG ,  SHU, Chutian ,  SENANAYAKE, Chris, Hugh ,  TAN, Zhulin ,  YEE, Nathan ,  ZENG, Xingzhong

Inventor： SHU, Chutian ,  SENANAYAKE, Chris, Hugh ,  TAN, Zhulin ,  YEE, Nathan ,  ZENG, Xingzhong

IPC: C07K1/00 ,  C07K5/12 ,  C07C6/06

CPC classification number: C07K5/0804 ,  C07K1/107

Abstract: The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R 1 -R 6 , A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula (II).

Abstract translation: 本发明涉及一种制备式（I）的大环化合物的方法，包括在催化剂存在下使式（II）二烯环化的步骤，其中R 1 -R 6，A，W和V 如本文所定义。 本发明还涉及式（II）的中间体化合物。