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公开(公告)号：US5728701A
公开(公告)日：1998-03-17
申请号：US820003
申请日：1997-03-18
申请人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
发明人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
IPC分类号： C07D213/74 , A61K31/495 , C07D401/04
CPC分类号： C07D213/74
摘要： Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
摘要翻译： 式I的化合物（I）及其代谢不稳定的酯和酰胺及其药学上可接受的盐，其中R13，M2，X1，Z1，Z1a，X2和A1具有说明书中给出的含义。 该化合物可用作纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂。 还公开了新的中间体。
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2.发明授权Certain�(piperidin-4-yl-alkanoyl)carbazoyl!-carboxy-phenoxy derivatives 失效某些[（哌啶-4-基 - 烷酰基）咔唑基] - 羧基 - 苯氧基衍生物
公开(公告)号：US5760057A
公开(公告)日：1998-06-02
申请号：US767443
申请日：1996-12-16
申请人： Andrew George Brewster , Peter William Rodney Caulkett , Alan Wellington Faull , Robert James Pearce , Richard Eden Shute
发明人： Andrew George Brewster , Peter William Rodney Caulkett , Alan Wellington Faull , Robert James Pearce , Richard Eden Shute
IPC分类号： C07D295/14 , A61K31/195 , A61K31/215 , A61K31/445 , A61K31/4465 , A61P7/02 , A61P9/08 , A61P9/10 , A61P25/04 , A61P43/00 , C07C243/38 , C07C257/18 , C07D211/34 , C07D211/42 , C07D211/46 , C07D211/62 , C07D295/20 , C07D295/215 , C07D211/44 , C07D211/64 , C07D211/66
CPC分类号： C07D295/215 , C07C243/38 , C07C257/18 , C07D211/34 , C07D211/46 , C07D211/62
摘要： The invention concerns acid derivatives of formula I R.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --G(I) and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
摘要翻译： 本发明涉及式IR1-CON（R2）-N（R3）CO-X1-Q-X2-G（I）的酸衍生物及其药学上可接受的代谢不稳定酯或酰胺及其药学上可接受的盐，其中R1， R2，R3，X1，Q，X2和G具有说明书中给出的含义。 本发明还涉及制备式I酸衍生物的方法，药物组合物含有它们作为纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂的用途。
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公开(公告)号：US5652242A
公开(公告)日：1997-07-29
申请号：US457538
申请日：1995-06-01
申请人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
发明人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
IPC分类号： C07D213/74 , A61K31/495 , C07D401/04
CPC分类号： C07D213/74
摘要： Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
摘要翻译： 式I的化合物（I）及其代谢不稳定的酯和酰胺及其药学上可接受的盐，其中R13，M2，X1，Z1，Z1a，X2和A1具有说明书中给出的含义。 该化合物可用作纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂。 还公开了新的中间体。
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公开(公告)号：US5981531A
公开(公告)日：1999-11-09
申请号：US86408
申请日：1998-05-29
申请人： Andrew George Brewster , Peter William Rodney Caulkett , Alan Wellington Faull , Robert James Pearce , Richard Eden Shute
发明人： Andrew George Brewster , Peter William Rodney Caulkett , Alan Wellington Faull , Robert James Pearce , Richard Eden Shute
IPC分类号： C07D295/14 , A61K31/195 , A61K31/215 , A61K31/445 , A61K31/4465 , A61P7/02 , A61P9/08 , A61P9/10 , A61P25/04 , A61P43/00 , C07C243/38 , C07C257/18 , C07D211/34 , C07D211/42 , C07D211/46 , C07D211/62 , C07D295/20 , C07D295/215 , C07D241/04 , A61K31/495 , C07D401/12 , C07D403/12
CPC分类号： C07D295/215 , C07C243/38 , C07C257/18 , C07D211/34 , C07D211/46 , C07D211/62
摘要： The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --Gand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
摘要翻译： 本发明涉及式I的酸衍生物R1-CON（R2）-N（R3）CO-X1-Q-X2-G及其药学上可接受的代谢不稳定的酯或酰胺及其药学上可接受的盐，其中R1，R2， R3，X1，Q，X2和G具有说明书中给出的含义。 本发明还涉及制备式I的酸衍生物的方法，含有它们的药物组合物及其作为纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂的用途。
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公开(公告)号：US06953809B2
公开(公告)日：2005-10-11
申请号：US10194969
申请日：2002-07-15
IPC分类号： C07D401/04 , A61K31/00 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/06 , A61P43/00 , C07D209/04 , C07D209/42 , C07D405/06 , C07D409/04 , C07D413/12
CPC分类号： A61K31/00
摘要： The invention concerns the use of a compound of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.
摘要翻译： 本发明涉及式（I）化合物的用途，其中Z，X，T，A，R 1，R 2，p和q具有 本文定义的含义及其药学上可接受的盐或体内可水解的酯，用于治疗由单核细胞趋化蛋白-1（MCP-1）介导的疾病或病症。 式（I）的某些组分是新的，并且与其药物组合物一起提供作为本发明的进一步特征。
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公开(公告)号：US6022869A
公开(公告)日：2000-02-08
申请号：US117673
申请日：1998-08-04
IPC分类号： C07D401/04 , C07D409/14 , A61K31/495 , C07D295/04
CPC分类号： C07D401/04 , C07D409/14
摘要： The invention relates to compounds of formula (I), and pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties; processes for preparing compounds of formula (I) and pharmaceutical compositions.
摘要翻译： PCT No.PCT / GB97 / 00270 Sec。 371日期：1998年8月4日 102（e）1998年8月4日PCT PCT 1997年1月31日PCT公布。 第WO97 / 29104号PCT公告 日期1997年8月14日本发明涉及具有抗血栓形成和抗凝血性质的式（I）化合物及其药学上可接受的盐; 制备式（I）化合物和药物组合物的方法。
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7.发明申请(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES 审中-公开（4-叔丁基哌嗪-2-基）（哌嗪-1-基）甲酮-N-羧酰胺衍生物公开(公告)号：US20120289513A1
公开(公告)日：2012-11-15
申请号：US13557559
申请日：2012-07-25
IPC分类号： C07D403/06 , A61P29/00 , A61P25/00 , A61K31/496
CPC分类号： C07D295/195 , C07D241/04 , C07D417/12
摘要： The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.
摘要翻译： 本发明涉及式（I）化合物。该化合物通过CCR2b受体的拮抗作用，并可用于治疗炎性疾病和/或神经性疼痛。
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8.发明申请Piperidine Derivative Used for Treating Chemokine Receptor 5 Mediated Diseases 审中-公开哌啶衍生物用于治疗趋化因子受体5介导的疾病公开(公告)号：US20100099708A1
公开(公告)日：2010-04-22
申请号：US12518489
申请日：2007-12-10
IPC分类号： A61K31/4545 , C07D401/14 , A61P11/06
CPC分类号： C07D401/14
摘要： The present invention relates to 4-[3-(1,1-difluoroethyl)-5-methyl-4H-1,2,4-triazol-4-yl]-1-{(1R,3R)-3-(3,5-difluorophenyl)-1-methyl-3-[1-(methylsulfonyl)ρiperidin-4-yl]propyl}piperidine formula (I): or a pharmaceutically acceptable salt thereof, as well as processes for the preparation of this compound and its use in the treatment of CCR5 disease states.
摘要翻译： 本发明涉及4- [3-（1,1-二氟乙基）-5-甲基-4H-1,2,4-三唑-4-基] -1 - {（1R，3R）-3-（3 ，5-二氟苯基）-1-甲基-3- [1-（甲基磺酰基）哌嗪-4-基]丙基}哌啶式（I）：或其药学上可接受的盐，以及其制备方法 化合物及其用于治疗CCR5疾病状态。
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9.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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10.发明授权公开(公告)号：US06730672B2
公开(公告)日：2004-05-04
申请号：US09800745
申请日：2001-03-08
IPC分类号： C07D40114
CPC分类号： C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The invention concerns compounds of formula (I) wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)r—L2—T3R5 in which r is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
摘要翻译： 本发明涉及式（I）化合物，其中G 1，G 2和G 3各自为CH或N; m为1或2; R 1包括氢，卤素和（1-4C）烷基; M 1是下式的基团：其中R 2和R 3一起形成（1-4C）亚烷基，其中R 2，R 2，R 3，R 3， ，L 1包括（1-4C）亚烷基，T 1是CH或N; A可能是直接链接; M 2是下式的基团：（T 2 R 4）r L 2 -T 3 R 5，其中r是0或1，每个T 2和T R 3和R 5分别是氢或（1-4C）烷基，或者R 4和R 5一起形成（1-4C）亚烷基， 和L 2包括（1-4C）亚烷基; M 3可以直接连接到X; X包括磺酰基; 且Q包括萘基和杂环部分; 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作为抗血栓形成或抗凝血剂的用途。
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