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1.发明授权
公开(公告)号：EP1492534B1
公开(公告)日：2008-06-25
申请号：EP03722719.6
申请日：2003-04-03
发明人： WATKINS, Clare, J. , ROMERO-MARTIN, Maria-Rosario , RITCHIE, James , FINN, Paul, W. , KALVINSH, Ivars Latvian Inst. of Organic Synthesis , LOZA, Einars Latvian Inst. of Organic Synthesis , DIKOVSKA, Klara Latvian Inst. of Organic Synthesis , STARCHENKOV,Igor Latvian Ins.of Organic Synthesis , LOLYA, Daina Latvian Inst. of Organic Synthesis , GAILITE, Vija Latvian Inst. of Organic Synthesis
IPC分类号： A61K31/495 , A61K31/496 , C07D295/18 , C07D295/22 , C07D317/58 , C07D239/42 , C07D209/20 , C07D333/60
CPC分类号： C07D213/74 , C07D239/42 , C07D295/185 , C07D295/192 , C07D295/26 , C07D317/58 , C07D333/60
摘要： This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula:[Insert formula]wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or -C(=O)- ; J2 is independently -C(=O)- or -S(=O)2- ; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X-C1-7alkylene, -X-C1-7alkylene, or C1-7alkylene-X-, wherein X is -O- or -S-; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. 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 HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
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公开(公告)号：EP1335898B1
公开(公告)日：2005-11-23
申请号：EP01970014.5
申请日：2001-09-27
发明人： WATKINS, Clare, J. , ROMERO-MARTIN, Maria-Rosario , MOORE, Kathryn, G., Prolifix Ltd , RITCHIE, James, c/o Prolifix Ltd , FINN, Paul, W., c/o Prolifix Ltd , KALVINSH, Ivars, c/o Latvian Inst. Organic Synth. , LOZA, Einars, c/o Latvian Inst. Organic Synth. , STARCHENKOV, Igor, c/o Latvian Inst. Organic Synth , DIKOVSKA, Klara, c/o Latvian Inst. Organic Synth. , BOKALDERE, Rasma M., c/o Latvian Inst. Orga. Synth , GAILITE, Vija, c/o Lativan Inst. Organic Synth. , VORONA, Maxim, c/o Latvian Inst. Organic Synth. , ANDRIANOV, Victor, c/o Latvian Inst. Organic Synth , LOLYA, Daina, c/o Latvian Inst. Organic Synth. , SEMENIKHINA, Valentina, c/o Latvian Inst. Org. Syn , AMOLINS, Andris, c/o Latvian Inst. Organic Synth. , HARRIS, C., John, c/o BioFocus plc , DUFFY, James, E., S., c/o BioFocus plc
IPC分类号： C07C233/03 , C07C233/05 , C07C233/09 , C07C233/08 , C07D207/40 , C07D213/06 , C07D209/14 , C07D235/24 , C07D307/34 , C07D333/24 , C07D333/60 , A61P35/00
CPC分类号： C07D207/337 , A61K31/16 , A61K31/195 , A61K31/198 , A61K31/277 , A61K31/38 , A61K31/381 , A61K31/426 , C07C233/49 , C07C233/83 , C07C235/34 , C07C237/36 , C07C255/57 , C07C259/06 , C07C259/08 , C07C2603/18 , C07D207/40 , C07D207/404 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/22 , C07D213/06 , C07D213/55 , C07D213/56 , C07D233/04 , C07D233/08 , C07D235/14 , C07D235/24 , C07D271/06 , C07D307/34 , C07D307/54 , C07D317/60 , C07D333/24 , C07D333/60 , C07D403/12 , Y02A50/411
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is an aryl group; Q is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: -NR C(=O)- and -C(=O)NR -; R is an amido substituent; and, Q is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof, for use in the treatment of parasitic infections, such as malaria.
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3.发明公开
公开(公告)号：EP1492534A1
公开(公告)日：2005-01-05
申请号：EP03722719.6
申请日：2003-04-03
发明人： WATKINS, Clare, J. , ROMERO-MARTIN, Maria-Rosario , RITCHIE, James , FINN, Paul, W. , KALVINSH, IvarsLatvian Inst. of Organic Synthesis , LOZA, EinarsLatvian Inst. of Organic Synthesis , DIKOVSKA, KlaraLatvian Inst. of Organic Synthesis , STARCHENKOV,IgorLatvian Ins.of Organic Synthesis , LOLYA, DainaLatvian Inst. of Organic Synthesis , GAILITE, VijaLatvian Inst. of Organic Synthesis
IPC分类号： A61K31/495 , A61K31/496 , C07D295/18 , C07D295/22 , C07D317/58 , C07D239/42 , C07D209/20 , C07D333/60
CPC分类号： C07D213/74 , C07D239/42 , C07D295/185 , C07D295/192 , C07D295/26 , C07D317/58 , C07D333/60
摘要： This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula:[Insert formula]wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or -C(=O)- ; J2 is independently -C(=O)- or -S(=O)2- ; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X-C1-7alkylene, -X-C1-7alkylene, or C1-7alkylene-X-, wherein X is -O- or -S-; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. 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 HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
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