公开(公告)号：EP1965824A2

公开(公告)日：2008-09-10

申请号：EP06827878.7

申请日：2006-11-17

申请人： Gloucester Pharmaceuticals, Inc.

发明人： OR, Yat, Sun ,  VERDINE, Gregory, L. ,  KEEGAN, Mitchell

IPC分类号： A61K38/12 ,  C07K5/12

CPC分类号： C07K5/101 ,  A61K38/00 ,  C07D515/08 ,  C07K11/00

摘要： The present invention relates to HDAC inhibitor derivatives, particularly derivatives of the free thiol of metabolites of the HDAC inhibitor FK228, pharmaceutical compositions thereof, and to methods of using such derivatives and pharmaceutical compositions thereof in the treatment of diseases associated with HDAC, in particular, tumor or cell proliferation diseases.

公开(公告)号：EP2802591A1

公开(公告)日：2014-11-19

申请号：EP13700506.2

申请日：2013-01-08

申请人： F.Hoffmann-La Roche AG

发明人： Anselm, Lilli ,  Banner, David ,  Blanc, Jean-Baptiste ,  Gaufreteau, Delphine ,  Haap, Wolfgang ,  Hartmann, Guido ,  Kuhn, Bernd ,  Luebbers,Thomas ,  Peters, Jens-Uwe ,  Spinnler, Beat

IPC分类号： C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07D515/08 ,  C07D515/22 ,  C07D273/01 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4353 ,  A61K31/397 ,  A61P3/10

CPC分类号： C07D273/01 ,  C07D269/00 ,  C07D273/02 ,  C07D413/10 ,  C07D498/06 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07D515/06 ,  C07D515/08 ,  C07D515/22

摘要： The invention relates to a compound of formula (I) wherein A, B, D and R
1 to R
6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

公开(公告)号：EP2331554B1

公开(公告)日：2013-03-06

申请号：EP09806438.9

申请日：2009-08-14

申请人： Janssen R&D Ireland

发明人： MC GOWAN, David, Craig ,  VENDEVILLE, Sandrine, Marie, Helene ,  RABOISSON, Pierre, Jean-Marie, Bernard ,  TAHRI, Abdellah

IPC分类号： C07D515/08 ,  A61K31/407 ,  A61P31/14

CPC分类号： C07D515/08

公开(公告)号：EP2334301B1

公开(公告)日：2018-02-14

申请号：EP09792214.0

申请日：2009-09-03

申请人： Merck Serono SA

发明人： YU, Henry ,  DE SELM, Lizbeth Celeste ,  JIANG, Xuliang ,  ASKEW, JR., Benny C. ,  KARRA, Srinivasa R. ,  GOUTOPOULOS, Andreas

IPC分类号： A61K31/529 ,  C07D239/42 ,  C07D487/08 ,  C07D487/18 ,  C07D498/08 ,  C07D498/18 ,  C07D513/08 ,  C07D513/18 ,  C07D515/08 ,  C07D295/096 ,  A61P35/00 ,  A61P29/00 ,  A61P31/00 ,  A61P37/00

CPC分类号： C07D498/08 ,  C07D487/08 ,  C07D487/18 ,  C07D498/18 ,  C07D513/08 ,  C07D513/18 ,  C07D515/08

摘要： Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.

公开(公告)号：EP1965824A4

公开(公告)日：2011-10-19

申请号：EP06827878

申请日：2006-11-17

申请人： GLOUCESTER PHARMACEUTICALS INC

发明人： OR YAT SUN ,  VERDINE GREGORY L ,  KEEGAN MITCHELL

IPC分类号： A61K38/00 ,  A61K38/12 ,  A61P35/00 ,  C07D515/08

CPC分类号： C07K5/101 ,  A61K38/00 ,  C07D515/08 ,  C07K11/00

公开(公告)号：EP0817787A4

公开(公告)日：2000-09-13

申请号：EP96910605

申请日：1996-03-27

申请人： ISIS PHARMACEUTICALS INC

发明人： COOK PHILLIP DAN ,  AN HAOYUN ,  GUINOSSO CHARLES J ,  KUNG PEI-PEI ,  FRASER ALLISTER S

IPC分类号： G01N33/15 ,  A61K31/33 ,  A61K31/395 ,  A61K31/435 ,  A61K31/53 ,  A61P29/00 ,  A61P31/04 ,  A61P43/00 ,  C07B61/00 ,  C07D255/02 ,  C07D273/00 ,  C07D471/08 ,  C07D471/18 ,  C07D498/08 ,  C07D515/08 ,  C07D521/00 ,  C07D519/00 ,  G01N33/531

CPC分类号： C07D471/08 ,  B01J2219/0072 ,  C07D515/08

摘要： Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring sytem. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

公开(公告)号：EP2836485B1

公开(公告)日：2018-01-10

申请号：EP13709234.2

申请日：2013-03-15

申请人： Polyphor AG

发明人： OBRECHT, Daniel ,  ERMERT, Philipp ,  OUMOUCH, Said ,  PIETTRE, Arnaud ,  GOSALBES, Jean-François ,  THOMMEN, Marc

IPC分类号： C07D273/02 ,  C07D498/04 ,  C07D498/18 ,  C07D515/06 ,  C07D515/18 ,  C07D515/22 ,  C07D291/08 ,  A61K31/395 ,  A61P31/04

CPC分类号： C07D273/02 ,  C07D291/08 ,  C07D498/04 ,  C07D498/08 ,  C07D498/18 ,  C07D515/06 ,  C07D515/08 ,  C07D515/18 ,  C07D515/22

摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

公开(公告)号：EP2981529A4

公开(公告)日：2016-12-07

申请号：EP14778536

申请日：2014-04-05

申请人： UNIV TEXAS

发明人： ZHOU JIA ,  DING CHUNYONG ,  SHEN QIANG

IPC分类号： C07D491/08 ,  A61K31/352 ,  A61P35/00 ,  C07D311/78 ,  C07D405/04 ,  C07D493/08 ,  C07D493/18 ,  C07D498/08 ,  C07D513/08 ,  C07D515/08

CPC分类号： C07D493/18 ,  C07D311/78 ,  C07D405/04 ,  C07D491/08 ,  C07D493/08 ,  C07D498/08 ,  C07D513/08 ,  C07D515/08

公开(公告)号：EP2802591B1

公开(公告)日：2016-03-16

申请号：EP13700506.2

申请日：2013-01-08

申请人： F.Hoffmann-La Roche AG

发明人： Anselm, Lilli ,  Banner, David ,  Blanc, Jean-Baptiste ,  Gaufreteau, Delphine ,  Haap, Wolfgang ,  Hartmann, Guido ,  Kuhn, Bernd ,  Luebbers,Thomas ,  Peters, Jens-Uwe ,  Spinnler, Beat

IPC分类号： C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07D515/08 ,  C07D515/22 ,  C07D273/01 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4353 ,  A61K31/397 ,  A61P3/10

CPC分类号： C07D273/01 ,  C07D269/00 ,  C07D273/02 ,  C07D413/10 ,  C07D498/06 ,  C07D498/08 ,  C07D498/18 ,  C07D498/22 ,  C07D515/06 ,  C07D515/08 ,  C07D515/22

公开(公告)号：EP2836485A1

公开(公告)日：2015-02-18

申请号：EP13709234.2

申请日：2013-03-15

申请人： Polyphor Ag

发明人： OBRECHT, Daniel ,  ERMERT, Philipp ,  OUMOUCH, Said ,  PIETTRE, Arnaud ,  GOSALBES, Jean-François ,  THOMMEN, Marc

IPC分类号： C07D273/02 ,  C07D498/04 ,  C07D498/18 ,  C07D515/06 ,  C07D515/18 ,  C07D515/22 ,  C07D291/08 ,  A61K31/395 ,  A61P31/04

CPC分类号： C07D273/02 ,  C07D291/08 ,  C07D498/04 ,  C07D498/08 ,  C07D498/18 ,  C07D515/06 ,  C07D515/08 ,  C07D515/18 ,  C07D515/22

摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

摘要翻译： 式（I）的构象限制的空间定义的大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.由该环系统描述的大环化合物易于通过平行合成或组合化学在溶液中制备 或固相。 它们被设计为与各种特定的生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR）的激动或拮抗活性，对酶或抗微生物活性的抑制活性。 特别地，这些大环化合物显示对亚型1（ECE-1）和/或半胱氨酸蛋白酶组织蛋白酶S（CatS）的内皮素转化酶的抑制活性，和/或作为催产素（OT）受体的拮抗剂，促甲状腺激素释放激素 （TRH）受体和/或白三烯B4（LTB4）受体和/或作为铃蟾肽3（BB3）受体的激动剂，和/或显示针对至少一种细菌菌株的抗微生物活性。 因此，它们作为各种疾病的药物具有巨大的潜力。