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公开(公告)号：US07906645B2
公开(公告)日：2011-03-15
申请号：US11793606
申请日：2005-12-19
IPC分类号： C07D241/02 , A61K31/495
CPC分类号： C07D295/195 , C07D207/09 , C07D211/26 , C07D211/46 , C07D211/60 , C07D265/30 , C07D295/02 , C07D295/215 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I) Q-L-W—C(═X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C-C chemokine mediated conditions.
摘要翻译： 式（I）化合物Q-L-W-C（= X）-Z-P其中Q是式-N（R1）（R2）的胺; L是烷基或杂环基 - 烷基接头; W是分别连接到基团L和C（X）的环原子Y1和Y2的6或7元脂肪环，Y1和Y2独立地选自N和C; X是O，N，N-CN或S; Z为NR3; P是任选取代的单环或双环芳基或杂芳基; 和其药学上可接受的盐或溶剂化物，可用于治疗C-C趋化因子介导的病症。
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公开(公告)号：US20120264762A1
公开(公告)日：2012-10-18
申请号：US13490765
申请日：2012-06-07
IPC分类号： A61K31/496 , A61P1/00 , A61P11/00 , A61P9/10 , A61K31/506 , A61P29/00
CPC分类号： C07D295/195 , C07D207/09 , C07D211/26 , C07D211/46 , C07D211/60 , C07D265/30 , C07D295/02 , C07D295/215 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I) Q-L-W—C(═X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions.
摘要翻译： 式（I）化合物Q-L-W-C（= X）-Z-P其中Q是式-N（R1）（R2）的胺; L是烷基或杂环基 - 烷基接头; W是分别连接到基团L和C（X）的环原子Y1和Y2的6或7元脂肪环，Y1和Y2独立地选自N和C; X是O，N，N-CN或S; Z为NR3; P是任选取代的单环或双环芳基或杂芳基; 和其药学上可接受的盐或溶剂化物，可用于治疗C-C趋化因子介导的病症。
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公开(公告)号：US20110136820A1
公开(公告)日：2011-06-09
申请号：US13018783
申请日：2011-02-01
IPC分类号： A61K31/496 , A61K31/506 , A61P11/00 , A61P11/06 , A61P29/00 , A61P19/10 , A61P19/02
CPC分类号： C07D295/195 , C07D207/09 , C07D211/26 , C07D211/46 , C07D211/60 , C07D265/30 , C07D295/02 , C07D295/215 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I) Q-L-W—C(═X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions.
摘要翻译： 式（I）化合物Q-L-W-C（= X）-Z-P其中Q是式-N（R1）（R2）的胺; L是烷基或杂环基 - 烷基接头; W是分别连接到基团L和C（X）的环原子Y1和Y2的6或7元脂肪环，Y1和Y2独立地选自N和C; X是O，N，N-CN或S; Z为NR3; P是任选取代的单环或双环芳基或杂芳基; 和其药学上可接受的盐或溶剂化物，可用于治疗C-C趋化因子介导的病症。
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公开(公告)号：US20090099156A1
公开(公告)日：2009-04-16
申请号：US11793606
申请日：2005-12-19
IPC分类号： A61K31/551 , C07D401/06 , A61K31/5377 , A61P1/00 , A61P35/00 , A61P19/02 , C07D413/06 , A61K31/496
CPC分类号： C07D295/195 , C07D207/09 , C07D211/26 , C07D211/46 , C07D211/60 , C07D265/30 , C07D295/02 , C07D295/215 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I) Q-L-W—C(═X)-Z-P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C-C chemokine mediated conditions.
摘要翻译： 式（I）化合物Q-L-W-C（-X）-Z-P其中Q是式-N（R1）（R2）的胺; L是烷基或杂环基 - 烷基接头; W是分别连接到基团L和C（X）的环原子Y1和Y2的6或7元脂肪环，Y1和Y2独立地选自N和C; X是O，N，N-CN或S; Z为NR3; P是任选取代的单环或双环芳基或杂芳基; 和其药学上可接受的盐或溶剂化物，可用于治疗C-C趋化因子介导的病症。
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5.发明授权Piperazine compounds useful as antagonists of C-C chemokines (Ccr2b and CcrS) for the treatment of inflammatory diseases 失效可用作C-C趋化因子（Ccr2b和CcrS）拮抗剂治疗炎性疾病的哌嗪化合物公开(公告)号：US07943768B2
公开(公告)日：2011-05-17
申请号：US12158248
申请日：2006-12-18
IPC分类号： C07D239/72 , C07D403/00 , C07D401/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D405/00 , C07D409/00 , C07D295/00 , C07D411/00 , C07D213/46 , C07D211/60
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14
摘要： A compound of formula (I) P—W—C(═X)-L-Q (I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
摘要翻译： 式（I）化合物P-W-C（= X）-L-Q（I）其中P是任选取代的芳基或杂芳基; W是任选取代的6或7元脂环，其包含独立选自氧和氮的环原子Y 1和Y 2，X选自氧，氮和硫; L是可选的C1-4连接体; 和Q是任选取代的4-7元脂族环：用于治疗趋化因子介导的疾病或病症。
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6.发明申请Piperazine Compounds Useful as Antagonists of C-C Chemokines (Ccr2b and Ccr5) for the Treatment of Inflammatory Diseases 失效可用作C-C趋化因子（Ccr2b和Ccr5）拮抗剂治疗炎性疾病的哌嗪化合物公开(公告)号：US20080287453A1
公开(公告)日：2008-11-20
申请号：US12158248
申请日：2006-12-18
IPC分类号： A61K31/496 , C07D401/06 , A61K31/506 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14
摘要： A compound of formula (I) P—W—C(═X)-L-Q (I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
摘要翻译： 式（I）的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> PWC（-X）-LQ（I）<？in-line-formula description =“In 其中P是任选取代的芳基或杂芳基; W是任选取代的6或7元脂环，其包含独立地选自氧和氮的环原子Y 1和Y 2，X选自氧，氮和硫 ; L是可选的C 1-4 - 连接基; 和Q是任选取代的4-7元脂族环：用于治疗趋化因子介导的疾病或病症。
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7.发明授权Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2 失效噻吩 - 甲酰胺衍生物及其作为IKK-2酶抑制剂的用途公开(公告)号：US07572826B2
公开(公告)日：2009-08-11
申请号：US10542326
申请日：2004-01-13
IPC分类号： A61K31/381 , C07D333/36
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途 。
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8.发明申请THIOPHENE-CARBOXAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE ENZYME IKK-2 审中-公开三苯甲酰胺衍生物及其作为酶的抑制剂IKK-2公开(公告)号：US20100029754A1
公开(公告)日：2010-02-04
申请号：US12537532
申请日：2009-08-07
IPC分类号： A61K31/381 , C07D333/38 , A61P29/00 , A61P11/00
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途 。
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9.发明授权Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases 失效胍衍生物喹唑啉和喹啉用于治疗自身免疫性疾病公开(公告)号：US07001904B1
公开(公告)日：2006-02-21
申请号：US10311587
申请日：2001-06-19
IPC分类号： C07D403/12 , C07D413/12 , A61K31/505
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
摘要翻译： 本发明涉及式（I）的喹唑啉和喹啉衍生物，其中Q 1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉或喹啉，或下式的基团： 其中X 1包括直接键，O和Q 3包括芳基，芳基 - （ 1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R 2，R 3和R 5各自为氢或（1-6C）烷基，提供基团R的一部分 R 2和R 4一起，R 3和R 4一起和R 5， 和R 4一起形成键; R 6是选自（2-6C）烯基，（2-6C）炔基，（3-7C）环烷基和（3-7C）环烯基中的任选取代的基团，或R 6 取代的（1-6C）烷基; 并且Q 2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。
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公开(公告)号：US06806274B1
公开(公告)日：2004-10-19
申请号：US10019945
申请日：2002-01-07
申请人： Graham C Crawley , Laurent F A Hennequin , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine M P Lambert
发明人： Graham C Crawley , Laurent F A Hennequin , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine M P Lambert
IPC分类号： A61K31517
CPC分类号： C07D231/12 , C07D215/54 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/12 , C07D403/12 , C07D417/12 , C07D487/04
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中Q 1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式：Q 3 -X 1 - 的基团，其中 X 1包括直接键，O和Q 3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R 2和R 3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q 2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。
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