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41. 发明申请

WO2003000649A1 6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1) 审中-公开
标题翻译： 6-（ARYL-AMIDO或芳基 - 氨基甲酰基） - 磷酸-2-乙酯酸衍生物作为PLASMINOGENA激活剂抑制剂类型1（PAI-1）的抑制剂
公开(公告)号：WO2003000649A1
公开(公告)日：2003-01-03
申请号：PCT/US2002/019193
申请日：2002-06-18
申请人： WYETH
发明人： COMMONS, Thomas, Joseph , CROCE, Susan, Christman , WOODWORTH, Richard, Page , TRYBULSKI, Eugene, John , ELOKDAH, Hassan, Mahmoud , CRANDALL, David, LeRoy
IPC分类号： C07C233/75
CPC分类号： C07D403/12 , C07C233/73 , C07C235/48 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D231/14 , C07D307/68 , C07D307/84 , C07D307/85 , C07D405/12
摘要： This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula (I), wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by one or more groups selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxy, phenyl-(CH 2 ) 0-6 -, phenyl-(CH 2 ) 0-6 O-,C 3 -C 6 cycloalkyl, -(CH 2 )-C 3 -C 6 cycloalkyl, halogen, C 1 -C 3 perflouroalkyl and C 1 -C 3 perfluoroalkoxy where phenyl can be substituted with from one or more groups selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, phenyl, halogen, trifluoromethyl and trifluoromethoxy; R 1 is hydrogen, C 1 -C 6 alkyl or phenyl-(CH 2 ) 1-6 - where phenyl can be substituted with C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R 2 and R 3 are H, C 1 -C 6 alkyl, phenyl-(CH 2 ) 0-3 -, halo and C 1 -C 3 perfluoroalkyl where phenyl can be substituted with C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R 4 is -CHR 5 CO 2 H or -CH 2 -tetrazole where R 5 is H or benzyl; and n = 0 or 1; or a pharmaceutically acceptable salt or ester form thereof.
摘要翻译：本发明提供新的化合物，药物组合物和治疗哺乳动物血栓形成障碍的方法，具有式（I）的化合物，其中：Ar是苯基，萘基，呋喃基，苯并呋喃基，吲哚基，吡唑基，恶唑基，芴基，苯基环烷烃，其中环烷可以是环丙基，环丁基，环戊基或环己基，Ar可任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，苯基 - （CH 0-6 < - ，苯基 - （CH> 2 <）> 0-6 ）-C 3 -C 6环烷基，卤素，C 1 -C 3全氟烷基和C 1 -C 3全氟烷氧基，其中苯基可以被一个或多个选自C 1 -C 3烷基的基团取代， C 1-6烷基，C 1 -C 6烷氧基，苯基，卤素，三氟甲基和三氟甲氧基; R 1是氢，C 1 -C 6烷基或苯基 - （CH 2）1-6 - ，其中苯基可被C 1 -C 6烷基取代，C 卤代，三氟甲基和三氟甲氧基; R 2和R 3是H，C 1 -C 6烷基，苯基 - （CH 2）0-3 - ，卤素和C 1 -C 3全氟烷基其中苯基可被C 1 -C 6烷基取代，C 1 -C 6烷氧基，卤素，三氟甲基和三氟甲氧基; R> 4 <= -CHR> 5 2 - 四唑，其中R 5是H或苄基; 并且n = 0或1; 或其药学上可接受的盐或酯形式。

42. 发明申请

WO2002074768A1 PIPERAZINE DERIVATIVES, THEIR PREPARATION AND USES IN THERAPY (5HT1B RECEPTOR ACTIVITY) 审中-公开
标题翻译：哌嗪衍生物，其制备和治疗用途（5HT1B受体活性）
公开(公告)号：WO2002074768A1
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002634
申请日：2002-03-11
申请人： SMITHKLINE BEECHAM PLC , MARSHALL, Howard , THOMPSON, Mervyn , WYMAN, Paul, Adrian
发明人： MARSHALL, Howard , THOMPSON, Mervyn , WYMAN, Paul, Adrian
IPC分类号： C07D405/08
CPC分类号： C07D333/62 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/84 , C07D405/12 , C07D413/10
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which R a is a group of formula (i) wherein P 1 is phenyl, naphthyl or heteroaryl; R 1 is halogen, C 1-6 alkyl, C 3-6 cycloalkyl, COC 1-6 alkyl, C 1-6 alkoxy, hydroxy, hydroxyC 1-6 alkyl, nitro, haloC 1-6 alkyl, cyano, SR 6 , SOR 6 , SO 2 R 6 , SO 2 NR 6 R 7 , CO 2 R 6 , CONR 6 R 7 , OCONR 6 COR 7 , NR 6 r 7 , NR 6 COR 7 , NR 6 CO 2 R 7 , NR 6 SO 2 R 7 , NR 6 CONR 7 R 8 , CH 2 NR 6 COR 7 , CH 2 NR 6 CO 2 R 7 , CH 2 NR 6 SO 2 R 7 , CR 6 =NOR 7 where R 6 , R 7 and R 8 are independently hydrogen or C 1-6 alkyl, a is 1, 1, 2, or 3; or R a is a group of formula (ii) where P 2 is phenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; P 3 is phenyl, naphthyl or heteroaryl; R 2 is a defined above for R 1 in formula (I) or R 2 is heteroaryl optionally substituted By C 1-6 alkyl, halogen or COC 1-6 alkyl or is a 5-7 membered heterocyclic ring optionally substituted by oxo; R 3 is halogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyl, COC 1-6 alkyl, hydroxy, intro, haloC 1-6 alkyl, cyano, CO 2 R 6 , CONR 6 R 7 , NR 6 R 7 where R 6 and R 7 are as defined above; b and c are independently 0, 1, 2, or 3; Y is a single bond, CH 2 or NH; X is oxygen, sulfur or N-R 5 where R 5 is hydrogen or C 1-6 alkyl; R b is hydrogen, halogen, C 1-6 alkyl, haloC 1-6 alkyl, COC 1-6 alkyl or cyano; R c is hydrogen or C 1-6 alkyl. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy as 5-HT 1B receptor antagonists, for diseases such as depression, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐：其中R a是式（ⅰ）的基团，其中P 1是苯基，萘基或杂芳基; R 1是卤素，C 1-6烷基，C 3-6环烷基，COC 1-6烷基，C 1-6烷氧基，羟基，羟基C 1-6烷基，硝基，卤代C 1-6烷基，氰基，SR 6，SOR 6，SO 2 R 6 >，SO 2 NR 6 R 7，CO 2 R 6，CONR 6 R 7，OCONR 6 COR 7，NR 6 R 7，NR 6 COR 7 ，NR 6 CO 2 R 7，NR 6 SO 2 R 7，NR 6 CONR 7 R 8，CH 2 NR 6 COR 7，CH 2 NR 6 CO 2 R 7， CH 2 NR 6 SO 2 R 7，CR 6 = NOR 7其中R 6，R 7和R 8独立地是氢或C 1-6烷基，a是1,2，或3; 或R a是式（ⅱ）的基团，其中P 2是苯基，萘基，杂芳基或5至7元杂环; P 3是苯基，萘基或杂芳基; R 2为式（I）中R 1定义或R 2为任选被C 1-6烷基，卤素或COC 1-6烷基取代的杂芳基，或为任选被氧代取代的5-7元杂环 ; R 3是卤素，C 1-6烷基，C 3-6环烷基，C 1-6烷基，COC 1-6烷基，羟基，引入，卤代C 1-6烷基，氰基，CO 2 R 6，CONR 6 R 7，NR 6 > R 7，其中R 6和R 7如上定义; b和c独立地为0,1,2或3; Y是单键，CH2或NH; X是氧，硫或N-R 5，其中R 5是氢或C 1-6烷基; R b是氢，卤素，C 1-6烷基，卤代C 1-6烷基，CO C 1-6烷基或氰基; R c是氢或C 1-6烷基。还公开了其制备方法，含有它们的药物组合物及其在治疗中用作5-HT1B受体拮抗剂，用于抑郁症等疾病。

43. 发明申请

WO9919296A8 AMINOBUTANOIC ACID DERIVATIVES 审中-公开
公开(公告)号：WO9919296A8
公开(公告)日：2000-11-02
申请号：PCT/JP9804529
申请日：1998-10-07
申请人： ONO PHARMACEUTICAL CO , TAKAHASHI KANJI , SUGIURA TSUNEYUKI
发明人： TAKAHASHI KANJI , SUGIURA TSUNEYUKI
IPC分类号： A61K31/16 , A61K31/165 , A61P19/00 , A61P43/00 , C07C233/47 , C07C233/63 , C07C233/83 , C07C235/06 , C07C235/16 , C07C235/42 , C07C235/52 , C07C237/22 , C07C243/00 , C07C243/34 , C07C255/41 , C07C255/57 , C07C259/06 , C07C259/08 , C07C271/16 , C07C271/22 , C07C311/21 , C07C323/42 , C07C323/60 , C07C327/30 , C07D207/32 , C07D207/327 , C07D207/34 , C07D207/40 , C07D207/46 , C07D209/18 , C07D209/42 , C07D211/14 , C07D211/46 , C07D211/62 , C07D213/54 , C07D213/56 , C07D213/68 , C07D213/70 , C07D213/81 , C07D215/14 , C07D233/61 , C07D233/74 , C07D253/08 , C07D263/56 , C07D263/57 , C07D277/62 , C07D295/13 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/84 , C07D309/12 , C07D333/16 , C07D333/38 , C07D333/44 , C07D333/60 , C07D405/12 , C07D521/00 , C07F7/18 , C07C275/36 , C07C323/41 , C07C323/43 , C07D209/24 , C07D211/70 , C07D215/02 , C07D233/72 , C07D277/64 , C07D333/24 , C07D339/08 , C07F5/02
CPC分类号： C07D207/327 , C07B2200/07 , C07B2200/09 , C07C233/47 , C07C233/63 , C07C233/83 , C07C235/06 , C07C235/16 , C07C235/42 , C07C235/52 , C07C237/22 , C07C243/34 , C07C255/41 , C07C255/57 , C07C259/06 , C07C259/08 , C07C271/22 , C07C311/21 , C07C323/42 , C07C323/60 , C07C327/30 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D207/40 , C07D207/46 , C07D209/18 , C07D209/42 , C07D211/14 , C07D211/46 , C07D211/62 , C07D213/54 , C07D213/56 , C07D213/68 , C07D213/70 , C07D213/81 , C07D215/14 , C07D231/12 , C07D233/56 , C07D233/74 , C07D249/08 , C07D253/08 , C07D263/57 , C07D277/62 , C07D295/13 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/84 , C07D309/12 , C07D333/16 , C07D333/38 , C07D333/44 , C07D333/60 , C07D405/12 , C07F7/1856
摘要： Aminobutanoic acid derivatives represented by general formula (I) and salts thereof (wherein each symbol is as defined in the description). The derivatives inhibit matrix metalloproteinases and are therefore useful for the prevention and/or treatment of rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontal diseases, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatic cirrhosis, corneal injury, diseases due to metastasis and infiltration of cancer cells or proliferation thereof, autoimmune diseases (such as Crohn's disease and Sjögren's disease), diseases due to transmigration of white blood cells or infiltration thereof, neovascularization, multiple sclerosis, aortic aneurysm, endometritis and so on.

44. 发明申请

WO99059973A1 CARBOXAMIDE COMPOUNDS, COMPOSITIONS, AND METHODS FOR INHIBITING PARP ACTIVITY 审中-公开
标题翻译：羧酰胺化合物，组合物和抑制PARP活性的方法
公开(公告)号：WO99059973A1
公开(公告)日：1999-11-25
申请号：PCT/US1998/018186
申请日：1998-09-02
IPC分类号： A61K9/00 , A61K9/08 , A61K9/107 , A61K9/20 , A61K31/16 , A61K31/18 , A61K31/185 , A61K31/192 , A61K31/343 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/42 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/496 , A61K31/517 , A61K31/662 , A61K31/664 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/10 , A61P13/12 , A61P19/02 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C233/65 , C07C235/84 , C07D209/42 , C07D215/50 , C07D217/24 , C07D217/26 , C07D221/12 , C07D221/18 , C07D239/72 , C07D257/04 , C07D261/12 , C07D307/84 , C07D309/40 , C07D333/68 , C07D495/04
CPC分类号： C07D257/04 , A61K31/16 , A61K31/47 , C07C233/65 , C07C235/84 , C07D209/42 , C07D215/50 , C07D217/24 , C07D217/26 , C07D221/12 , C07D221/18 , C07D239/72 , C07D307/84 , C07D333/68 , C07D495/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof; wherein: Y represents the atoms necessary to form a fused 5-to 6-membered, aromatic or non-aromatic, carbocyclic or N-containing heterocyclic ring, wherein Y and any heteroatom(s) therein are unsubstituted or independently substituted by at least one non-interfering alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, carboxy or halo substituent; X is at the 1-position of ring Y and is -COOR5 or a substituted or unsubstituted moiety selected from the group consisting of (a), (b), (c), (d), (e), (f) and (g) wherein R7 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R1 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R2, R3, R4 and R5 are independently hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl, and are either unsubtsituted or substituted with a moiety selected from the group consisting of alkyl, alkenyl, alkoxy, phenoxy, benzyloxy, cycloalkyl, cycloalkenyl, hydroxy, carboxy, carbonyl, amino, amido, cyano, isocyano, nitro, nitroso, nitrilo, isonitrilo, imino, azo, diazo, sulfonyl, sulfoxy, thio, thiocarbonyl, sulfhydryl, halo, haloalkyl, trifluoromethyl and aryl.
摘要翻译：式（I）化合物或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物; 其中：Y表示形成稠合的5至6元芳族或非芳族，碳环或含氮杂环所必需的原子，其中Y及其中的任何杂原子是未被取代的或独立地被至少一个非干扰性烷基，烯基，环烷基，环烯基，芳烷基，芳基，羧基或卤素取代基; X为环Y的1-位，为-COOR 5或选自（a），（b），（c），（d），（e），（f）和（g）其中R 7是氢，烷基，烯基，环烷基或环烯基，并且本身未被取代或被烷基，链烯基，环烷基或环烯基取代; R1是氢，烷基，烯基，环烷基或环烯基，并且本身是未取代的或被烷基，烯基，环烷基或环烯基取代; R2，R3，R4和R5独立地是氢，烷基，烯基，环烷基，环烯基，芳烷基或芳基，并且是未取代的或被选自烷基，烯基，烷氧基，苯氧基，苄氧基，环烷基，环烯基，羟基，羧基，羰基，氨基，酰胺基，氰基，异氰基，硝基，亚硝基，次氮基，异亚三烯基，亚氨基，偶氮，重氮，磺酰基，亚磺酰基，硫代，硫代羰基，巯基，卤素，卤代烷基，三氟甲基和芳基。

45. 发明申请

WO99042442A1 AMINOGUANIDINE HYDRAZONE DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND DRUGS THEREOF 审中-公开
标题翻译：氨基嘌呤盐酸衍生物，其生产方法及其药物
公开(公告)号：WO99042442A1
公开(公告)日：1999-08-26
申请号：PCT/JP1999/000703
申请日：1999-02-18
IPC分类号： C07D209/06 , C07D209/88 , C07D215/38 , C07D215/60 , C07D221/04 , C07D231/56 , C07D237/28 , C07D239/74 , C07D261/20 , C07D307/79 , C07D307/84 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D209/08 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/47 , A61K31/50 , A61K31/505 , C07D333/36
CPC分类号： C07D221/04 , C07D209/06 , C07D209/88 , C07D215/38 , C07D215/60 , C07D231/56 , C07D237/28 , C07D239/74 , C07D261/20 , C07D307/79 , C07D307/84 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： Compounds represented by general formula (I) or salts thereof having preventive and therapeutic effects on ischemic heart diseases, etc., and being useful as preventives/remedies for ischemic heart diseases such as heart infarction and arrhythmia. In formula (I), A represents optionally substituted 5- or 6-membered heteroaryl; B represents an optionally substituted 5- or 6-membered aromatic homocycle or heterocycle; R represents hydrogen, hydroxy or lower alkyl; and n is 0 or 1.
摘要翻译：由通式（I）表示的化合物或其盐对缺血性心脏病等具有预防和治疗作用，并且可用作缺血性心脏病如心脏梗死和心律失常的预防药物/治疗剂。在式（I）中，A表示任选取代的5或6元杂芳基; B表示任选取代的5或6元芳族共轭或杂环; R 1表示氢，羟基或低级烷基; n为0或1。

46. 发明申请

WO99025684A1 METHOD OF SYNTHESIS OF PYRROLE AMIDES 审中-公开
标题翻译：吡咯类化合物的合成方法
公开(公告)号：WO99025684A1
公开(公告)日：1999-05-27
申请号：PCT/IB1998/001672
申请日：1998-10-21
IPC分类号： C07D307/93 , C07C271/14 , C07D209/42 , C07D209/52 , C07D307/83 , C07D307/84 , C07D401/12 , C07D405/12 , C07D407/12 , A61K31/34 , A61K31/40
CPC分类号： C07D405/12 , C07D209/42 , C07D307/83 , C07D307/84
摘要： A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakanediones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
摘要翻译：制备选择性结合GABAa受体的吡咯 - 羧酰胺的方法; 其包括使1,3-环烷二酮与乙酸乙酯反应，随后将所得产物与酰卤反应，然后与芳族胺反应，最后在升高的温度下与二铵源反应。

47. 发明申请

WO98038167A1 HETEROARYL-HEXANOIC ACID AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS SELECTIVE INHIBITORS OF MIP-1-ALPHA BINDING TO ITS CCR1 RECEPTOR 审中-公开
标题翻译：异烟肼酰胺酰胺衍生物，其制备及其作为MIP-1-ALPHA结合至CCR1受体的选择性抑制剂的用途
公开(公告)号：WO98038167A1
公开(公告)日：1998-09-03
申请号：PCT/US1998/001568
申请日：1998-02-05
IPC分类号： C07D237/28 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4184 , A61K31/428 , A61K31/44 , A61K31/455 , A61K31/47 , A61K31/498 , A61K31/502 , A61P1/00 , A61P3/10 , A61P17/00 , A61P29/00 , A61P37/02 , A61P43/00 , C07C237/22 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/54 , C07D217/26 , C07D221/04 , C07D221/12 , C07D221/16 , C07D235/24 , C07D241/24 , C07D241/44 , C07D277/68 , C07D307/84 , C07D307/85 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D521/00 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/495 , A61K31/50
CPC分类号： C07D213/82 , C07C237/22 , C07D209/42 , C07D213/81 , C07D215/48 , C07D215/54 , C07D217/26 , C07D221/16 , C07D235/24 , C07D237/28 , C07D241/24 , C07D241/44 , C07D277/68 , C07D307/84 , C07D307/85 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Compounds of formula (I) wherein R is optionally substituted (C2-C9)heteroaryl; R is optionally substituted phenyl-(CH2)m-, naphthyl-(CH2)m-, (C3-C10)cycloalkyl-(CH2)m-, (C1-C6)alkyl or (C2-C9)heteroaryl-(CH2)m-, m is an integer from zero to four; R is hydrogen, or optionally substituted (C1-C10)alkyl, (C3-C10)cycloalkyl-(CH2)n-, (C2-C9)heterocycloalkyl-(CH2)n-, (C2-C9)heteroaryl-(CH2)n- or aryl-(CH2)n-, n is an integer from zero to six; or R and the carbon to which it is attached form an optionally substituted and/or fused five to seven membered carbocyclic ring; R is hydrogen, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, hydroxy (C1-C6)alkyl, (C1-C6)alkoxyCO, (C3-C10)cycloalkyl-(CH2)p-, or optionally substituted (C2-C9)heterocycloalkyl-(CH2)p-, (C2-C9)heteroaryl-(CH2)p-, phenyl-(CH2)p- or naphthyl-(CH2)p-, p is an integer from zero to four; or R and R together with the nitrogen atom to which they are attached form an optionally substituted (C2-C9)heterocycloalkyl group; R is hydrogen, (C1-C6)alkyl or amino. The present compounds are potent and selective inhibitors of MIP-1-alpha. binding to its receptor CCR1, and are thus useful to treat inflammation and other immune disorders.
摘要翻译：式（I）的化合物，其中R 1是任选取代的（C 2 -C 9）杂芳基; R 2是任选取代的苯基 - （CH 2）m - ，萘基 - （CH 2）m - ，（C 3 -C 10）环烷基 - （CH 2）m - ，（C 1 -C 6）烷基或（C 2 -C 9）（CH 2）m - ，m是0至4的整数; R 3是氢或任选取代的（C 1 -C 10）烷基，（C 3 -C 10）环烷基 - （CH 2）n - ，（C 2 -C 9）杂环烷基 - （CH 2）n - ，（C 2 -C 9）（CH 2）n - 或芳基 - （CH 2）n - ，n为0至6的整数; 或R 3，并且其连接的碳形成任选取代的和/或稠合的五至七元碳环; R 4是氢，（C 1 -C 6）烷基，羟基，（C 1 -C 6）烷氧基，羟基（C 1 -C 6）烷基，（C 1 -C 6）烷氧基CO，（C 3 -C 10）环烷基 - （CH 2），或任选取代的（C 2 -C 9）杂环烷基 - （CH 2）p - ，（C 2 -C 9）杂芳基 - （CH 2）p - ， - 苯基 - （CH 2）p - 或萘基 - （CH 2）p - 从零到四; 或R 4和R 5与它们所连接的氮原子一起形成任选取代的（C 2 -C 9）杂环烷基; R 5是氢，（C 1 -C 6）烷基或氨基。本发明化合物是MIP-1-α的有效和选择性抑制剂。与其受体CCR1结合，因此可用于治疗炎症和其它免疫疾病。

48. 发明申请

WO1995032949A1 GASTRIN AND CCK ANTAGONISTS 审中-公开
标题翻译： GASTRIN和CCK拮抗剂
公开(公告)号：WO1995032949A1
公开(公告)日：1995-12-07
申请号：PCT/GB1995001194
申请日：1995-05-25
申请人： JAMES BLACK FOUNDATION LIMITED , KALINDJIAN, Sarkis, Barret , SHANKLEY, Nigel, Paul , HULL, Robert, Antony, David , KOTECHA, Atul , ROBERTS, Sonia, Patricia , HARPER, Elaine, Anne
发明人： JAMES BLACK FOUNDATION LIMITED
IPC分类号： C07D235/06
CPC分类号： C07D235/06 , C07C233/65 , C07C233/82 , C07C237/22 , C07C237/48 , C07C2603/74 , C07D207/16 , C07D209/08 , C07D209/42 , C07D209/88 , C07D217/26 , C07D235/24 , C07D307/84 , C07D333/70 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D453/02 , C07D471/04
摘要： Compounds of formula (I) wherein L is =N- or =CH-, one of X and Y is -NH-CH2-R (wherein R is cycloheptyl or 1-adamantyl) and the other is (II) in which R is H or methyl, T and T are independently H or Z(CH2)m-, wherein m is from 0 to 3 and Z is a carboxy group, a tetrazolyl group, CF3CONHSO2-, PhCONHSO2-, isopropyl-OC(O)NHSO2- or a group selected from (a), (b) and (c) (provided that T and T are not both H and that T and T are not both carboxy when L is =CH-); and n is from 0 to 5; and pharmaceutically acceptable salts thereof are potent gastrin and/or CCK antagonists.
摘要翻译：其中L为=或N-或= CH-的式（I）化合物，X和Y之一为-NH-CH 2 -R 2（其中R 2为环庚基或1-金刚烷基），另一个为（ II）其中R 1是H或甲基，T 1和T 2独立地是H或Z（CH 2）m - ，其中m是0-3，Z是羧基，四唑基，CF 3 CONHSO 2 - ，PhCONHSO 2 - ，异丙基-OC（O）NHSO 2 - 或选自（a），（b）和（c）的基团（条件是T 1和T 2不都是H而且T 当L = CH-时，<1>和T 2不同时为羧基; 且n为0至5; 及其药学上可接受的盐是有效的胃泌素和/或CCK拮抗剂。

49. 发明申请

WO1993020057A1 NOVEL DERIVATIVES OF 2,3-DIHYDRO-2,2,4,6,7-PENTAALKYL-5-BENZOFURANOLS 审中-公开
标题翻译： 2,3-二氢-2,2,4,6,7-二戊基-5-苯并呋喃醇的新衍生物
公开(公告)号：WO1993020057A1
公开(公告)日：1993-10-14
申请号：PCT/US1993002107
申请日：1993-03-10
申请人： MERRELL DOW PHARMACEUTICALS INC. , GRISAR, J., Martin , PETTY, Margaret, A. , BOLKENIUS, Frank
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07D307/80
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D307/84 , C07D405/12
摘要： Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.
摘要翻译： 2,3-二氢-5-苯并呋喃醇的衍生物，其中间体及其制备方法。这些化合物是自由基清除剂，可用于治疗能够通过自由基清除剂治疗的病症，例如中风，神经系统创伤和再灌注损伤。

50. 发明申请

WO9100725A3 AMINO ACID ANALOG CCK ANTAGONISTS 审中-公开
标题翻译：氨基酸模拟CCK拮抗剂
公开(公告)号：WO9100725A3
公开(公告)日：1991-02-21
申请号：PCT/US9003630
申请日：1990-06-26
申请人： ABBOTT LAB
发明人： KERWIN JAMES F JR
IPC分类号： A61K31/16 , A61K31/195 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/47 , A61K38/00 , A61P1/00 , A61P3/04 , A61P3/08 , A61P25/00 , A61P25/04 , C07C237/06 , C07C237/20 , C07C237/22 , C07C255/24 , C07C255/29 , C07C255/41 , C07C271/22 , C07C271/24 , C07C275/42 , C07C275/62 , C07C311/13 , C07C311/19 , C07C317/14 , C07C323/58 , C07C327/38 , C07C335/04 , C07D207/16 , C07D209/20 , C07D209/42 , C07D213/56 , C07D213/75 , C07D213/82 , C07D215/48 , C07D215/54 , C07D215/56 , C07D233/54 , C07D295/185 , C07D307/84 , C07D333/20 , C07D333/24 , C07D333/70 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07K5/02 , C07K5/078 , A61K
CPC分类号： C07D213/82 , A61K38/00 , C07C237/06 , C07C237/20 , C07C237/22 , C07C255/29 , C07C255/41 , C07C271/22 , C07C271/24 , C07C275/62 , C07C317/14 , C07C323/58 , C07C2601/14 , C07D207/16 , C07D209/42 , C07D213/56 , C07D215/48 , C07D215/54 , C07D215/56 , C07D233/54 , C07D295/185 , C07D307/84 , C07D333/24 , C07D333/70 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07K5/0202 , C07K5/06139
摘要： A CCK antagonist compound of formula (I) wherein G is (1) NH2 or (2) substituted amino; R9 is (1) hydrogen, (2) loweralkyl, (3) carboxy-substituted alkyl or (4) carboxyester-substituted alkyl; R10 is (1) hydrogen, (2) loweralkyl, (3) functionalized alkyl or (4) cycloalkyl; D is (1) hydrogen, (2) loweralkyl, (3) functionalized alkyl, (4) cycloalkyl, (5) aryl, (6) functionalized oxyalkyl or (7) heterocyclic; with the proviso that D is other than indolylmethyl, indolinylmethyl or oxindolylmethyl; or R10 taken together with D or R9 taken together with D forms a cyclic group; Z is (1) -C(O)-, (2) -C(S)- or (3) -S(O)2-; B is (1) absent, (2) alkylene, (3) alkenylene, (4) substituted alkenylene, (5) -R26-R27- wherein R26 is absent or -CH2- and R27 is -O-, -S-, -NH- or -N(loweralkyl)- or (6) -R27-CH2- wherein R27 is defined as above; and Ar is (1) aryl or (2) a heterocyclic group.

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