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公开(公告)号：EP1495018B3
公开(公告)日：2011-03-16
申请号：EP03718393.6
申请日：2003-04-14
申请人： Schering Corporation
发明人： CHACKALAMANNIL, Samuel , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , XIA, Yan , VELTRI, Enrico, P. , CHELLIAH, Mariappan , WU, Wenxue
IPC分类号： C07D405/06 , A61K31/44 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; (a) represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; each R13 is independently selected from H, (C1-C6)alkyl, (C3-C8)cycloalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, haloalkyl and halogen; each R14 is independently selected from H, (C1-C6)alkyl, -OH, (C1-C6)alkoxy, R27-aryl (C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, halogen and haloalkyl; or R13 and R14 taken together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; wherein at least one of R13 or R14 is selected from the group consisting of -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
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公开(公告)号：EP1294714B1
公开(公告)日：2007-08-01
申请号：EP01944492.6
申请日：2001-06-13
申请人： SCHERING CORPORATION
IPC分类号： C07D405/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Heterocyclic-substituted compounds of formula (I) ]or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is — (CH2)n-; (a) ; (b), wherein R10 is absent; or, (c) wherein R3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is -(CH¿2?)n3-, wherein n3 is 0-5, -CH2-O-, -CH2S-, -CH2-NR?6¿-, -C(O)NR?6-. -NR6¿C(O)-, (d), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR6- when the double dotted line represents a single bond, or X is H, -OH or -NHR20 when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C¿1?-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is =O, =NOR?17¿, (H, H), (H, OH), (H, SH), (H, C¿1?-C6 alkoxy) or (H, substituted-amino); R?22 and R23¿ are independently -OH, -OC(O)R30, OC(O)NR30R31, or optionally substituted alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl, cycloalkyl, cycloalkenyl, carbonyl, amino, alkoxy, alkenyloxy, alkynyloxy, heterocycloalkyloxy, cycloalkyloxy, or cycloalkenyloxy; or R?22 and R10, or R23 and R11¿, can form a carbocyclic or heterocyclic ring; and the remaining variables are as described in the specification. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
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公开(公告)号：EP1294714A2
公开(公告)日：2003-03-26
申请号：EP01944492.6
申请日：2001-06-13
申请人： SCHERING CORPORATION
IPC分类号： C07D405/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Heterocyclic-substituted compounds of formula (I) ]or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is — (CH2)n-; (a) ; (b), wherein R10 is absent; or, (c) wherein R3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is -(CH¿2?)n3-, wherein n3 is 0-5, -CH2-O-, -CH2S-, -CH2-NR?6¿-, -C(O)NR?6-. -NR6¿C(O)-, (d), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR6- when the double dotted line represents a single bond, or X is H, -OH or -NHR20 when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C¿1?-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is =O, =NOR?17¿, (H, H), (H, OH), (H, SH), (H, C¿1?-C6 alkoxy) or (H, substituted-amino); R?22 and R23¿ are independently -OH, -OC(O)R30, OC(O)NR30R31, or optionally substituted alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl, cycloalkyl, cycloalkenyl, carbonyl, amino, alkoxy, alkenyloxy, alkynyloxy, heterocycloalkyloxy, cycloalkyloxy, or cycloalkenyloxy; or R?22 and R10, or R23 and R11¿, can form a carbocyclic or heterocyclic ring; and the remaining variables are as described in the specification. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译： 式（I）的杂环取代的化合物]或其药学上可接受的盐，其中：Z是 - （CH 2）n - （一个） ; （b），其中R 10不存在; 或（c）其中R3不存在; 单点虚线表示可选的双键; 双点线表示可选的单键; n是0-2; Het是任选取代的单环，双环或三环杂芳族基团; B是 - （CH 2 2）n3 - ，其中n3是0-5，-CH2-O - ， - CH2S - ， - CH2-NR6-，-C（O）NR6-。 （O） - ，（d），任选取代的烯基或任选取代的炔基; 当双虚线表示单键时，X是-O-或-NR 6 - ，或当键不存在时X是H，-OH或-NHR 20; 当双点划线表示单键或当键不存在时，Y是= O，= S，（H，H），（H，OH）或（H，C 1 -C 6烷氧基） （H，H），（H，OH），（H，SH），（H，C 1 -C 6烷氧基）或（H，取代的氨基）。 R22和R23独立地为-OH，-OC（O）R30，OC（O）NR30R31或任选取代的烷基，烯基，炔基，杂环烷基，芳基，环烷基，环烯基，羰基，氨基，烷氧基，烯氧基， ，杂环烷氧基，环烷氧基或环烯氧基; 或者R 22和R 10或R 23和R 11可以形成碳环或杂环; 其余变量如说明书中所述。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体结合剂的用途的药物组合物。
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公开(公告)号：EP1495018B1
公开(公告)日：2007-11-14
申请号：EP03718393.6
申请日：2003-04-14
申请人： Schering Corporation
发明人： CHACKALAMANNIL, Samuel , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , XIA, Yan , VELTRI, Enrico, P. , CHELLIAH, Mariappan , WU, Wenxue
IPC分类号： C07D405/06 , A61K31/44 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; (a) represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; each R13 is independently selected from H, (C1-C6)alkyl, (C3-C8)cycloalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, haloalkyl and halogen; each R14 is independently selected from H, (C1-C6)alkyl, -OH, (C1-C6)alkoxy, R27-aryl (C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, halogen and haloalkyl; or R13 and R14 taken together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; wherein at least one of R13 or R14 is selected from the group consisting of -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
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公开(公告)号：EP1495018A1
公开(公告)日：2005-01-12
申请号：EP03718393.6
申请日：2003-04-14
申请人： SCHERING CORPORATION
发明人： CHACKALAMANNIL, Samuel , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , XIA, Yan , VELTRI, Enrico, P. , CHELLIAH, Mariappan , WU, Wenxue
IPC分类号： C07D405/06 , A61K31/44 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; (a) represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; each R13 is independently selected from H, (C1-C6)alkyl, (C3-C8)cycloalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, haloalkyl and halogen; each R14 is independently selected from H, (C1-C6)alkyl, -OH, (C1-C6)alkoxy, R27-aryl (C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, halogen and haloalkyl; or R13 and R14 taken together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; wherein at least one of R13 or R14 is selected from the group consisting of -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
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