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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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5.发明授权Catalyzed enantiomeric selection of 1,2-diols and their cyclization to produce oxiranes 失效催化1,2-二醇的对映体选择及其环化生成环氧乙烷
公开(公告)号：US5854062A
公开(公告)日：1998-12-29
申请号：US535134
申请日：1995-12-11
IPC分类号： C07C29/88 , C07C29/92 , C07C67/48 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D521/00 , C12P17/02 , C12P17/10 , C12P41/00
CPC分类号： C07D231/12 , C07C67/48 , C07D233/56 , C07D249/08 , C12C11/02 , C12P17/02 , C12P17/10 , C12P41/004
摘要： Method of preparing an optically active compound of formula, wherein R and R.sup.1 are independently alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl, cycloalkyl, aryl, aralkyl, a heterocyclic group or a C.sub.1 -C.sub.4 alkyl-heterocycle, each being optionally substituted, procided that R and R.sup.1 are not identical and * is an optically active chiral center, from the corresponding racemic ester or diol by treating with a hydrolase enzyme. In particular, racemic 2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-1,2 diol, an intermediate in fluconazole synthesis, is resolved using porcine pancreatic lipase or lipase from Chromobacterium viscosum.
摘要翻译： PCT No.PCT / GB94 / 00793 Sec。 371 1995年12月11日第 102（e）日期1995年12月11日PCT 1994年4月15日PCT PCT。 公开号WO94 / 24305 日期：1994年10月27日制备其中R和R 1独立地为烷基，烯基，炔基，烷氧基，烷氧基烷基，环烷基，芳基，芳烷基，杂环基或C 1 -C 4烷基杂环的光学活性化合物的方法 任选被取代，通过用水解酶处理，通过相应的外消旋酯或二醇处理R和R 1不相同和*是光学活性的手性中心。 特别地，外消旋的2-（2,4-二氟苯基）-3-（1H-1,2,4-三唑-1-基）丙-1,2-二醇是氟康唑合成中的中间体，使用猪胰脂肪酶 或来自粘杆菌（Chromobacterium viscosum）的脂肪酶。
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公开(公告)号：US5912355A
公开(公告)日：1999-06-15
申请号：US968510
申请日：1997-11-12
IPC分类号： C07C29/88 , C07C29/92 , C07C67/48 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D521/00 , C12P17/02 , C12P17/10 , C12P41/00
CPC分类号： C07D231/12 , C07C67/48 , C07D233/56 , C07D249/08 , C12C11/02 , C12P17/02 , C12P17/10 , C12P41/004
摘要： Method of preparing an optically active compound of formula, wherein R and R.sup.1 are independently alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl, cycloalkyl, aryl, aralkyl, a heterocyclic group or a C.sub.1 -C.sub.4 alkyl-heterocycle, each being optionally substituted, procided that R and R.sup.1 are not identical and * is an optically active chiral center, from the corresponding racemic ester or diol by treating with a hydrolase enzyme.
摘要翻译： 制备式的光学活性化合物的方法，其中R和R 1独立地是烷基，烯基，炔基，烷氧基，烷氧基烷基，环烷基，芳基，芳烷基，杂环基或C 1 -C 4烷基杂环， R和R1不相同，*是通过用水解酶处理来自相应的外消旋酯或二醇的光学活性手性中心。
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公开(公告)号：US07709479B1
公开(公告)日：2010-05-04
申请号：US10088814
申请日：2000-09-18
IPC分类号： A61K31/517 , A61K31/535 , C07D239/72 , C07D413/12
CPC分类号： C07D401/04 , A61K31/517 , C07D239/94 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , Y02P20/582
摘要： The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group NHC(O)OR9, NHC(O)R9, NHS(O)2R9, C(O)R9, C(O)OR9, S(O)R9, S(O)OR9, S(O)2OR9, C(O)NR10 R11, S(O)NR10R11 S(O)ONR10R11, where R9, R10 or R11 are various specified organic groups; R6 is hydrogen, optionally substituted hydrocarbyl or optionally substituted heterocyclyl; R7 and R8 are various specified organic groups, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, —N(OH)R13— (wherein R7 is hydrogen, or C1-3alkyl), or R15X1— (wherein X1 represents a direct bond, —O—, —CH2—, —OCO—, carbonyl, —S—, —SO—, —SO2—, —NR16CO—, —CONR16—, —SO2NR16—, —NR17SO2— or —NR18— (wherein R16, R17 and R18 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; in the preparation of a medicament for use in the inhibition of aurora 2 kinase.
摘要翻译： 式（I）化合物或其盐，酯，酰胺或前药的用途; 其中X是O或S，S（O）或S（O）2，NH或NR 12，其中R 12是氢或C 1-6烷基; R 5选自NHC（O）OR 9，NHC（O）R 9，NHS（O）2 R 9，C（O）R 9，C（O）OR 9，S（O）R 9，S（O）OR 9， O）2OR 9，C（O）NR 10 R 11，S（O）NR 10 R 11 S（O）ONR 10 R 11，其中R 9，R 10或R 11是各种规定的有机基团; R 6是氢，任选取代的烃基或任选取代的杂环基; R 7和R 8是各种规定的有机基团，R 1，R 2，R 3，R 4独立地选自卤素，氰基，硝基，C 1-3烷基硫基，-N（OH）R 13 - （其中R 7是氢或C 1-3烷基） 或R 15 X 1-（其中X 1表示直接键，-O - ， - CH 2 - ， - OCO-，羰基，-S-，-SO - ， - SO 2 - ， - NR 16 CO-，-CONR 16 - ， - SO 2 NR 16 - NR 17 SO 2 - 或-NR 18 - （其中R 16，R 17和R 18各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3烷基），并且R 9是氢，任选取代的烃基，任选取代的杂环基或任选取代的烷氧基; 的用于抑制极光2激酶的药物。
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