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公开(公告)号：EP2871957A4
公开(公告)日：2016-01-27
申请号：EP13817154
申请日：2013-07-10
申请人： MERCK SHARP & DOHME
发明人： REGER THOMAS , WALJI ABBAS , SANDERS JOHN , WAI JOHN , WANG LIPING
IPC分类号： C07D487/18 , A61K31/427 , A61K31/513 , A61K31/55 , A61K31/553 , A61K45/06 , C07D498/18 , C07D515/18
CPC分类号： C07D498/18 , A61K31/427 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/18 , C07D515/18 , A61K31/513 , A61K2300/00
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公开(公告)号：EP2488521B1
公开(公告)日：2013-12-18
申请号：EP10772998.0
申请日：2010-10-13
IPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , C07D515/18 , A61K31/547 , A61P31/18 , C07D498/22
CPC分类号： C07D513/18 , C07D471/18 , C07D498/18 , C07D498/22 , C07D515/18
摘要： Compound having formula (I), wherein -W is NH-, -N(CH3)- or piperazine, -X is a bond, -C(=O)- or S(=O)2-, -Y is C3-7alkylene, and -Z is NH-C(=O)- or -O-, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.
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公开(公告)号：EP1557418B1
公开(公告)日：2012-04-04
申请号：EP03758937.1
申请日：2003-10-27
申请人： MSD K.K.
发明人： HIRAI, Hiroshi; c/o BANYU PHARMACEUTICAL CO., LTD , KAWANISHI, Nobuhiko; c/o BANYU PHARMACEUTICAL CO. , HIROSE, Masaaki; c/o BANYU PHARMACEUTICAL CO.,LTD , SUGIMOTO, Tetsuya; c/o BANYU PHARMACEUTICAL CO., , KAMIJYO, Kaori; c/o BANYU PHARMACEUTICAL CO., , SHIBATA, Jun; c/o BANYU PHARMACEUTICAL CO., LTD. , MASUTANI, Kouta; c/o BANYU PHARMACEUTICAL CO.,
IPC分类号： A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D487/18 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22 , A61P35/00
CPC分类号： C07D487/18 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22
摘要： Quinoxaline derivatives represented by the general formula (I) or pharmaceutically acceptable salts or esters thereof: (I) wherein X is NH, S, or the like; Y is O or the like; the group represented by the general formula (II): (II) is, e.g., (III) [wherein B1, B2, ..., Bn-1, and Bn (wherein n is 4, 5, or 6) are each independently CH, N, or the like; and B’1, B’2, ..., B’n-1, and B’n (wherein n is 4, 5, or 6) are each independently hydrogen or the like]; and R is hydrogen, lower alkyl, or the like.
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公开(公告)号：EP1951729A4
公开(公告)日：2009-09-23
申请号：EP06813132
申请日：2006-11-15
申请人： S BIO PTE LTD
发明人： BLANCHARD STEPHANIE , LEE CHENG HSIA ANGELINE , NAGARAJ HARISH KUMAR MYSORE , POULSEN ANDERS , SUN ERIC T , TAN YEE LING EVELYN , WILLIAM ANTHONY DEODAUNIA
IPC分类号： C07D498/02 , A61K31/505 , A61P35/00 , A61P35/02 , C07D495/12 , C07D498/12
CPC分类号： A61K31/519 , A61K31/5377 , C07D498/06 , C07D498/08 , C07D498/16 , C07D498/18 , C07D515/16 , C07D515/18
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公开(公告)号：EP3833672B1
公开(公告)日：2024-09-18
申请号：EP19749375.2
申请日：2019-08-09
IPC分类号： C07D513/14 , C07D515/04 , C07D515/14 , C07D515/18 , C07D519/00 , A61K31/554 , A61P31/20
CPC分类号： C07D513/14 , C07D515/04 , C07D515/14 , C07D515/18 , C07D519/00
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公开(公告)号：EP2871957A1
公开(公告)日：2015-05-20
申请号：EP13817154.1
申请日：2013-07-10
发明人： REGER, Thomas , WALJI, Abbas , SANDERS, John , WAI, John , WANG, Liping
CPC分类号： C07D498/18 , A61K31/427 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/18 , C07D515/18 , A61K31/513 , A61K2300/00
摘要： The present invention relates to Macrocyclic Compounds. The present invention also relates to compositions comprising at least one Macrocyclic Compound, and methods of using the Macrocyclic Compounds for treating or preventing HIV infection in a subject.
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17.发明公开
公开(公告)号：EP2178886A1
公开(公告)日：2010-04-28
申请号：EP08776190.4
申请日：2008-07-09
发明人： CONTE, Immacolata , HABERMANN, Joerg , MACKAY, Angela Claire , NARJES, Frank , RICO FERREIRA, Maria del Rosario , STANSFIELD, Ian
IPC分类号： C07D513/16 , C07D515/16 , A61K31/407 , A61P31/12
CPC分类号： C07D513/08 , C07D513/18 , C07D513/22 , C07D515/18 , C07D515/22
摘要： A class of macrocyclic compounds of formula (I), wherein R7,A,Ar, B,D, F, M, Q1, Q2, W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Alsoprovided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
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18.发明公开
公开(公告)号：EP2178885A1
公开(公告)日：2010-04-28
申请号：EP08776186.2
申请日：2008-07-09
发明人： CONTE, Immacolata , HABERMANN, Joerg , MACKAY, Angela Claire , NARJES, Frank , RICO FERREIRA, Maria del Rosario , STANSFIELD, Ian
IPC分类号： C07D513/16 , C07D515/16 , A61K31/407 , A61P31/12
CPC分类号： C07D513/08 , C07D513/18 , C07D513/22 , C07D515/18 , C07D515/22
摘要： A class of macrocyclic compounds of formula (I), wherein R7, R9, B, F, M, Q, W, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such 5 macrocyclic compounds for treating or preventing HCV infection.
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公开(公告)号：EP1951729A1
公开(公告)日：2008-08-06
申请号：EP06813132.5
申请日：2006-11-15
申请人： S*BIO Pte Ltd
发明人： BLANCHARD, Stéphanie , LEE, Cheng Hsia, Angeline , NAGARAJ, Harish, Kumar, Mysore , POULSEN, Anders , SUN, Eric, T. , TAN, Yee Ling, Evelyn , WILLIAM, Anthony, Deodaunia
IPC分类号： C07D498/02 , A61P35/00 , C07D495/12 , A61K31/505 , A61P35/02 , C07D498/12
CPC分类号： A61K31/519 , A61K31/5377 , C07D498/06 , C07D498/08 , C07D498/16 , C07D498/18 , C07D515/16 , C07D515/18
摘要： The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
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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.
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