专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1993001169A2 AROMATIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN THERAPY 审中-公开
标题翻译：芳香化合物，含有它们的药物组合物及其在治疗中的使用
公开(公告)号：WO1993001169A2
公开(公告)日：1993-01-21
申请号：PCT/GB1992001214
申请日：1992-07-03
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , MACLEOD, Angus, Murray , MERCHANT, Kevin, John , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D209/14
CPC分类号： C07D333/58 , A61K38/00 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/47 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/13 , C07C255/54 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C2601/02 , C07D207/28 , C07D209/14 , C07D209/20 , C07D231/56 , C07D241/08 , C07D295/092 , C07D295/185 , C07D333/60 , C07K5/06026
摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR ; X and Y are H or are together =O; R and R are H; optionally substituted C1-6alkyl; optionally substituted phenyl(C1-4alkyl); COR ; CO2R ; CONR R ; CONR COOR ; or SO2R ; R is H or C1-6alkyl, R is H, C1-6alkyl or optionally substituted phenyl; and R represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.
摘要翻译：式（I）化合物及其盐和前药，其中Q表示任选取代的苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基，苄基或吲唑基; Z表示O，S或NR 8; X和Y为H或一起= O; R 1和R 2是H; 任选取代的C 1-6烷基; 任选取代的苯基（C 1-4烷基）; COR ; CO 2 ; CONR - [R ; CONR COOR ; 或SO2R ; R 3是H或C 1-6烷基，R 4是H，C 1-6烷基或任选取代的苯基; 且R 5表示任选取代的苯基; 速激肽拮抗剂。它们及其组合物可用于治疗。

2. 发明申请

WO1995021819A1 ARALKOXY AND ARALKYLTHIO SUBSTITUTED AZACYCLIC COMPOUNDS AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译：阿卡洛昔康和阿拉奇菌素替代亚甲基化合物作为TACHYKININ拮抗剂
公开(公告)号：WO1995021819A1
公开(公告)日：1995-08-17
申请号：PCT/GB1995000228
申请日：1995-02-06
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , MACLEOD, Angus, Murray , SEWARD, Eileen, Mary , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D211/42
CPC分类号： C07D401/06 , C07D211/42 , C07D211/54
摘要： The present invention relates to compounds of formula (I) wherein n is 1, 2 or 3 and where any carbon atom of (CH2)n may be substituted by R and/or R ; X represents O or S; R represents (CH2)qphenyl, wherein q is 0, 1, 2 or 3, which may be optionally substituted in the phenyl ring; R represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R and R each independently represent H, halo, C1-6alkyl, oxo, CO2R or CONR R ; R represents H or C1-6alkyl; R represents trifluoromethyl, C2-6alkenyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, (CH2)pNR R , CO2R , CONR R , (CH2)pCO2R , (CH2)pCONR R , (CH2)pNR COR , (CH2)pNHSO2R , (CH2)pOR , (CH2)pOC(O)R or (CH2)pOC1-4alkylCOR or C1-6alkyl substituted by a hydroxy group; R represents H, COR , CO2R , COCONR R , COCO2R , C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkyl optionally substituted by a group selected from (CO2R , CONR R , hydroxy, cyano, COR , NR R , C(NOH)NR R , CONHphenyl(C1-4alkyl), COCO2R , CONHNR R , C(S)NR R , CONR C1-6alkylR , CONR C2-6alkynyl, CONR C2-6alkenyl, COCONR R , CONR C(NR )NR R , CONR heteroaryl, and optionally substituted phenyl or C1-6alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; R and R each independently represent H, C1-6alkyl, trifluoromethyl or phenyl optionally substituted by C1-6alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
摘要翻译：本发明涉及其中n为1,2或3并且（CH 2）n的任何碳原子可以被R 4和/或R 5取代的式（I）化合物。 X表示O或S; R 1表示（CH 2）q苯基，其中q是0,1,2或3，其可以在苯环中任选被取代; R 2表示选自苯基和萘基的芳基; 选自吲唑基，噻吩基，呋喃基，吡啶基，噻唑基，四唑基和喹啉基的杂芳基。二苯甲基; 或苄基; 其中每个芳基或杂芳基部分可以被取代; R 4和R 5各自独立地表示H，卤素，C 1-6烷基，氧代，CO 2 R a或CONR a R b; R 6表示H或C 1-6烷基; R 7表示三氟甲基，C 2-6烯基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，（CH 2）p NR R 10，CO 2 R 16，CONR 9 R 10，（CH 2） pCO 2 R 16，（CH 2）p CONR 9 R 10，（CH 2）p NR 9 COR 16，（CH 2）p NHSO 2 R 11，（CH 2）pOR 16，（CH 2）pOC O）R 9或（CH 2）pOC 1-4烷基COR 17或被羟基取代的C 1-6烷基; R 8表示H，COR a，CO 2 R a，COCONR a R b，COCO 2 R a，C 3-7环烷基，C 3-7环烷基C 1-4烷基，任选被选定的基团取代的C 1-6烷基由（CO 2 R a，CONR a R b，羟基，氰基，COR a，NR a R b，C（NOH）NR a R b，CONH苯基（C 1 烷基），COCO 2 R a，CONHNR a R b，C（S）NR a R b，CONR a C 1-6烷基R 12，CONR 13 C 2-6炔基， CONR 13 C 2-6烯基，COCONR a R b，CONR a C（NR b）NR a R b，CONR 1杂芳基和任选取代的苯基或C1- 任选被氧代取代的被任选取代的芳族杂环取代的C 1-6烷基; R a和R b各自独立地代表H，C 1-6烷基，三氟甲基或任选被C 1-6烷基，卤素或三氟甲基取代的苯基，化合物是特别用于治疗疼痛，炎症，偏头痛和呕吐。

3. 发明申请

WO1995018124A1 SUBSTITUTED MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：取代的吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1995018124A1
公开(公告)日：1995-07-06
申请号：PCT/GB1994002819
申请日：1994-12-23
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , HARRISON, Timothy , MACLEOD, Angus, Murray , OWENS, Andrew, Pate , SEWARD, Eileen, Mary , SWAIN, Christopher, John , TEALL, Martin, Richard
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06 , C07D413/14 , C07F9/6533 , C07F9/65583
摘要： The present invention relates to compounds of formula (I), wherein R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, CF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6 alkenyl, C2-6 alkynyl or C1-4 alkyl substituted by C1-4 alkoxy, where R and R are hydrogen or C1-4 alkyl; R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy substituted by C1-4 alkoxy or CF3; R is hydrogen, halogen or CF3; R is selected from the definitions of R ; R is selected from the definitions of R ; R is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by =O, =S or a C1-4 alkyl group, and optionally substituted by an aminoalkyl group; R and R are hydrogen or C1-4 alkyl, or R and R are joined to form a C5-7 ring; X is C1-4 alkylene optionally substituted by oxo; and Y is a C1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C1-4 alkyl, R is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，NO 2，CN，SR a，SOR a，SO 2 R， α，CO 2 R a，CONR a R b，C 2-6烯基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b是氢或C 1-4烷基; R 2是氢，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R 3是氢，卤素或CF 3; R 4选自R 1的定义; R 5选自R 2的定义; R 6是含有2或3个氮原子的5元或6元杂环，其任选被= O，= S或C 1-4烷基取代，并且任选被氨基烷基取代; R 9a和R 9b是氢或C 1-4烷基，或R 9a和R 9b连接形成C5-7环; X是任选被氧代取代的C 1-4亚烷基; Y是任选被羟基取代的C 1-4烷基; 条件是如果Y是C 1-4烷基，则R 6至少被氨基烷基取代; 及其药学上可接受的盐和前药。该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

4. 发明申请

WO1996005203A1 SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：螺旋取代的亚氨基衍生物及其作为治疗剂的用途
公开(公告)号：WO1996005203A1
公开(公告)日：1996-02-22
申请号：PCT/GB1995001867
申请日：1995-08-07
申请人： MERCK SHARP & DOHME LIMITED , LADDUWAHETTY, Tamara , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C1-6alkyl, C1-6alkoxy, hydroxy, halogen, cyano, trifluoromethyl, SO2C1-6alkyl, NR R , NR COR or CONR R , where R and R are each H, C1-6alkyl, phenyl or trifluoromethyl; R represents phenyl optionally substituted by 1, 2 or 3 of C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, -O(CH2)pO- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , SO2R , NR R , NR COR , NR CO2R , COR , CO2R or CONR R ; naphthyl; benzhydryl; or benzyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R represents hydrogen, a substituent as defined for R or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R and R are each H or C1-6alkyl or R and R together are linked so as to form a C1-3alkylene chain; R represents H, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenylC1-4alkyl, CO2R , CONR R , SOR or SO2R , wherein the phenyl moiety may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represent =O; and Z represents a bond, O, S, SO, SO2, NR , or -(CR R )- where R is H or C1-6alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明涉及式（I）化合物，其中n为0,1,2或3; R表示C 1-6烷基，C 1-6烷氧基，羟基，卤素，氰基，三氟甲基，SO 2 C 1-6烷基，NR a R b，NR a COR b或CONR a R b，其中 R a和R b各自为H，C 1-6烷基，苯基或三氟甲基; R 1表示任选被1,2或3个C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，-O（CH 2）p O--（其中p为1或 2），卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a，SO 2 R a，NR a R b，NR a COR b，，NR a CO 2 R b，COR a，CO 2 R a或CONR a R b; 萘; 二苯甲基; 或苄基，其中苄基和二苯甲基的萘基或每个苯基部分可被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 2表示氢，R 1所定义的取代基或选自吲唑基，噻吩基，呋喃基，吡啶基，噻唑基，四唑基和喹啉基的杂芳基; 其中每个杂芳基可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 3和R 4各自为H或C 1-6烷基或R 3和R 4一起连接形成C 1-3亚烷基链; R 5表示H，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基C 1-4烷基，CO 2 R a，CONR a R b，SOR a或SO 2 R a，其中苯基部分可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; X和Y各自为H，或一起表示= O; 和Z表示键，O，S，SO，SO 2，NR 6或 - （CR 6 R 6） - ，其中R 6是H或C 1-6烷基; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。

5. 发明申请

WO1995004042A1 4-PHENYL-4-PHENYLPROPYL(ENYL)-PIPERIDINES AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译： 4-苯基-4-苯丙氨酸（ENYL）-PIPERIDINES作为TACHYKININ ANTAGONISTS
公开(公告)号：WO1995004042A1
公开(公告)日：1995-02-09
申请号：PCT/GB1994001576
申请日：1994-07-21
申请人： MERCK SHARP & DOHME LIMITED , MACLEOD, Angus, Murray , MERCHANT, Kevin, John , STEVENSON, Graeme, Irvine
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D211/22
CPC分类号： C07D401/06 , C07D211/18 , C07D211/22 , C07D211/32
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R , R , R and R ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R represents optionally substituted phenyl; R represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R represents H, COR , CO2R , COCONR R , COCO2R , SO2R , CONR SO2R , C1-6alkyl optionally substituted by a group selected from (CO2R , CONR R , hydroxy, cyano, COR , NR R , C(NOH)NR R , CONHphenyl(C1-4alkyl), COCO2R , COCONR R , SO2R , CONR SO2R and optionally substituted phenyl), Y-R or CO-Z-(CH2)q-R ; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy, or R and R together form a group =0; R and R each independently represents H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy or R and R together form a group =0; R represents an optionally substituted aromatic heterocycle; R represents H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, or phenyl; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl or C3-5cycloalkylmethyl; R represents NR R or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R and R each independently represent H, C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, optionally substituted phenyl or phenylC1-4alkyl; R represents C1-6alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH2, O, S or NR ; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和前药，其中X表示任选被一个或多个R 4，R 5，R 6和R 6取代的丙烯或亚丙烯基链 [R <7>; m为2,3或4; 当m为2或3时，n为0,1或2，m为4时，n为0或1; R 1表示任选取代的苯基; R 2表示任选取代的苯基，杂芳基，二苯甲基或苄基; R 3表示H，COR 9，CO 2 R 10，COCONR 10 R 11，COCO 2 R 10，SO 2 R 15，CONR 10 SO 2 R 15，任选取代的C 1-6烷基通过选自（CO 2 R 10，CONR 10 R 11，羟基，氰基，COR 9，NR 10 R 11，C（NOH）NR 10 R 11，，CONH苯基（C 1-4烷基），COCO 2 R 10，COCONR 10 R 11，SO 2 R 15，CONR 10 SO 2 R 15和任选取代的苯基），YR 8或CO-Z- （CH 2）q或r <12>; R 4和R 5各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，羟基或C 1-6烷氧基，或者R 4和R 5一起形成基团= 0; R 6和R 7各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，羟基或C 1-6烷氧基或R 6和R 7一起形成基团= 0; R 8表示任选取代的芳族杂环; R 9表示H，C 1-6烷基，C 3-6环烷基，C 3-5环烷基甲基或苯基; R 10和R 11各自独立地表示H，C 1-6烷基，C 3-6环烷基或C 3-5环烷基甲基; R 12表示NR 13 R 14或任选取代的芳族或非芳族氮杂环或氮杂双环基; R 13和R 14各自独立地表示H，C 1-6烷基，C 3-6环烷基，C 3-8环烷基甲基，任选取代的苯基或苯基C 1-4烷基; R 15表示C 1-6烷基，C 3-6环烷基，C 3-5环烷基甲基，三氟甲基或任选取代的苯基; Y表示可任选被氧代取代的1,2,3或4个碳原子的烃链; Z表示CH 2，O，S或NR 10; q表示0,1,2,3,4,5或6.化合物是用于治疗疼痛或炎症，偏头痛或呕吐的速激肽拮抗剂。

6. 发明申请

WO1994001402A1 HETEROCYCLIC AMIDE DERIVATIVES AS TACHYKININ DERIVATIVES 审中-公开
标题翻译：作为TACHYKININ衍生物的杂环酰胺衍生物
公开(公告)号：WO1994001402A1
公开(公告)日：1994-01-20
申请号：PCT/GB1993001415
申请日：1993-07-06
申请人： MERCK SHARP & DOHME LIMITED , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D209/16
CPC分类号： C07D213/81 , C07D209/14 , C07D295/15 , C07D401/12 , C07D403/12 , C07D409/12 , C07D453/02
摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional covalent bond; one of X and Y is H and the other is hydroxy or C1-6alkoxy, or X and Y together form a group =O or =NOR where R is H or C1-6alkyl; R is H or C1-6alkyl. R is CO-W-R where W represents a bond or a hydrocarbon chain of 1-6 carbon atoms and R is an azacyclic or azabicyclic group; R is H, C1-6alkyl or C2-6alkenyl; and R is phenyl optionally substituted by 1-3 of C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , NR R , NR COR , NR CO2R , CO2R or CONR R , where R and R are H, C1-6alkyl, phenyl or trifluoromethyl; are tachykinin antagonists useful in therapy.
摘要翻译：式（I）化合物及其盐和前药，其中Q 1是被一个或多个卤素取代的苯基; 任选取代的萘基，吲哚基，苯并噻吩基，苯并呋喃基，苄基或芴基; 虚线表示任选的共价键; X和Y之一是H，另一个是羟基或C 1-6烷氧基，或X和Y一起形成基团= O或= NOR 5，其中R 5是H或C 1-6烷基; R 1是H或C 1-6烷基。 R 2是CO-W-R 6，其中W表示1-6个碳原子的键或烃链，R 6是氮杂环或氮杂双环基; R 3是H，C 1-6烷基或C 2-6烯基; 并且R 4是任选被1-3个C 1-6烷基，C 2-6烯基，C 2-6炔基，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a ，NR a R b，NR a COR b，NR a CO 2 R b，CO 2 R a或CONR a R b，其中R a和R b， b是H，C 1-6烷基，苯基或三氟甲基; 是用于治疗的速激肽拮抗剂。

7. 发明申请

WO1993018023A1 HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：杂环化合物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1993018023A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000411
申请日：1993-02-26
申请人： MERCK SHARP & DOHME LIMITED , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D333/58
CPC分类号： C07D333/58 , C07D209/16
摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; .... is an optional covalent bond; one of X and Y is H and the other is hydroxy or C1-6alkoxy, or X and Y are together =0 or =NOR ; R and R are H; C1-6alkyl optionally substituted by hydroxy, cyano, COR , CO2R , CONR R , or NR R (where R and R are H, C1-6 alkyl or phenyl (C0-4alkyl) optionally substituted by C1-6alkyl, C1-6alkoxy, halo and trifluoromethyl); phenyl (C1-4alkyl) (optionally substituted by C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl); COR ; CO2R ; CONR R ; COC1-6alkylNR R ; CONR COOR ; or SO2R ; R is H, C1-6alkyl or C2-6alkenyl; and R is phenyl optionally substituted by C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , NR R , NR COR , NR CO2R , CO2R or CONR R , where R and R are H, C1-6alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
摘要翻译：式（I）化合物及其盐和前药，其中Q 1是卤素取代的苯基; 萘; 吲哚基; 苯并噻吩基; 苯并呋喃基; 苄基; 或芴基; ....是可选的共价键; X和Y之一是H，另一个是羟基或C 1-6烷氧基，或X和Y一起= 0或= NOR 5。 R 1和R 2是H; 任选被羟基，氰基，COR c，CO 2 R c，CONR c R d或NR c R d取代的C 1-6烷基（其中R c和R d分别为任选被C 1-6烷基，C 1-6烷氧基，卤素和三氟甲基取代的C 1-6烷基或苯基（C 0-4烷基）; 苯基（C 1-4烷基）（任选被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代）; COR ; CO 2 ; CONR - [R ; COC1-6alkylNR - [R ; CONR COOR ; 或SO2R ; R 3是H，C 1-6烷基或C 2-6烯基; R 4是任选被C 1-6烷基，C 2-6烯基，C 2-6炔基，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a，NR a取代的苯基 R b，NR a R c，NR a CO 2 R b，CO 2 R a或CONR a R b，其中R a和R b是H ，C 1-6烷基，苯基或三氟甲基; 速激肽拮抗剂。

8. 发明申请

WO1997019073A1 PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES 审中-公开
标题翻译：哌啶和四氢吡啶衍生物
公开(公告)号：WO1997019073A1
公开(公告)日：1997-05-29
申请号：PCT/GB1996002795
申请日：1996-11-14
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , HOBBS, Sarah, Christine , LADDUWAHETTY, Tamara , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D401/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D413/14
摘要： A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D beta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译：一类通过其4-位通过亚烷基链连接到稠合双环杂芳族部分如吲哚基并在1位被进一步被任选取代的烷基，烯基，炔基，环烷基 - 取代的烷基取代的哌啶和四氢吡啶衍生物，烷基，芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂，它是人类5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dαα进行至少10倍的选择性亲和力受体亚型相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

9. 发明申请

WO1994010167A1 TACHYKININ ANTAGONISTS 审中-公开
公开(公告)号：WO1994010167A1
公开(公告)日：1994-05-11
申请号：PCT/GB1993002213
申请日：1993-10-27
申请人： MERCK SHARP & DOHME LIMITED , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D209/16 , C07D453/02
摘要： Compounds of formula (I), wherein Q represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C1-6alkoxy, or X and Y together form a group =O or =NOR where R is H or C1-6alkyl; Z represents O, S or NR , where R is H or C1-6alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R represents H or C1-6alkyl. R represents H, C1-6alkyl or C2-6alkenyl; R represents an optionally substituted phenyl group; and R represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.
摘要翻译：式（I）的化合物，其中Q 1表示芳基; 虚线表示任选的共价键; X和Y之一表示H，另一个表示羟基或C 1-6烷氧基，或X和Y一起形成基团= O或= NOR 5，其中R 5为H或C 1-6烷基; Z表示O，S或NR 2，其中R 2是H或C 1-6烷基; W表示具有1,2,3,4,5或6个碳原子的键或饱和或不饱和烃链; R 1表示H或C 1-6烷基。 R 3表示H，C 1-6烷基或C 2-6烯基; R 4表示任选取代的苯基; 并且R 6表示指定的氨基或任选取代的芳族或非芳族氮杂环或氮杂双环基; 盐和前药是速激肽受体拮抗剂。

10. 发明申请

WO1997011695A1 SUBSTITUTED INDOLYLPROPYL-PIPERAZINE DERIVATIVES AS 5-HT1DALPHA AGONISTS 审中-公开
标题翻译：作为5-HT1DALPHA激动剂的取代的吲哚丙氨酸哌嗪衍生物
公开(公告)号：WO1997011695A1
公开(公告)日：1997-04-03
申请号：PCT/GB1996002309
申请日：1996-09-19
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CHAMBERS, Mark, Stuart , HOBBS, Sarah, Christine , MACLEOD, Angus, Murray , REEVE, Austin, John , STERNFELD, Francine , STREET, Leslie, Joseph
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/40
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： A class of 1-[3-(1H-indol-3-yl)propyl]-4-(2-phenylethyl)piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D beta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译：一类在吲哚核的5-位被五元杂芳族部分取代的1- [3-（1H-吲哚-3-基）丙基] -4-（2-苯基乙基）哌嗪衍生物，一或卤素，三氟甲基，烷基，羟基烷基或烷氧基烷基的苯乙基部分的其它乙烯碳原子，以及任选地在苯乙基部分的苯环上被卤素，三氟甲基，烷氧基或恶唑烷酮基团任选取代，并且任选地被一个或两个其它取代基是5-HT1样受体的选择性激动剂，它是人5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dβ亚型具有至少10倍的5-HT1Dα受体亚型的选择性亲和力 ; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式