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1. 发明申请

WO1994005625A1 ALCOHOLS AND ETHERS WITH AROMATIC SUBSTITUENTS AS TACHYKININ-ANTAGONISTS 审中-公开
标题翻译：酒精和芳香剂作为TACHYKININ-ANTAGONISTS的人
公开(公告)号：WO1994005625A1
公开(公告)日：1994-03-17
申请号：PCT/GB1993001863
申请日：1993-09-03
申请人： MERCK SHARP & DOHME LIMITED , HUSCROFT, Ian, Thomas , STEVENSON, Graeme, Irvine , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07C235/06
CPC分类号： C07D213/40 , C07C43/1786 , C07C69/708 , C07C235/06
摘要： Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; R1 is H; optionally substituted C1-6alkyl; optionally substituted phenyl(C1-4alkyl); C2-6alkenyl; C2-6alkynyl; CORa; COORa; COHet; COC1-6alkylhalo; COC1-6alkylNRaRb; CONR12C1-6alkylCONRaRb; CONRaRb; or SO2Ra; R2 represents H, C1-6alkyl or C2-6alkenyl; or R1 and R2 together form a chain (CH2)q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NRx, where Rx is H or C1-6alkyl; R3 is C1-3alkyl substituted by optionally substituted phenyl; R4 and R5 are each H, C1-6alkyl or C2-6alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.
摘要翻译：式（I）化合物及其盐和前体药物，其中Q为任选取代的苯基或二苯甲基; R1是H; 任选取代的C 1-6烷基; 任选取代的苯基（C 1-4烷基）; 2-6链烯基; C 2-6炔基; CORA; COORa; COHet; COC1-6alkylhalo; COC1-6alkylNRaRb; CONR12C1-6alkylCONRaRb; CONRaRb; 或SO2Ra; R 2表示H，C 1-6烷基或C 2-6烯基; 或R 1和R 2一起形成任选被氧代取代的链（CH 2）q，其中q是4或5，并且其中一个亚甲基可以任选地被氧原子或基团NR x取代，其中R x是H或C 1-6烷基; R3是被任意取代的苯基取代的C 1-3烷基; R 4和R 5各自为H，C 1-6烷基或C 2-6烯基; Z表示O或S; 是用于治疗的速激肽受体拮抗剂。

2. 发明申请

WO1994010165A1 4-ARYLMETHYLOXYMETHYL PIPERIDINES AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译： 4-ARYLMETHYLOXYMETHYL PIPERIDINES作为TACHYKININ ANTAGONISTS
公开(公告)号：WO1994010165A1
公开(公告)日：1994-05-11
申请号：PCT/GB1993002214
申请日：1993-10-27
申请人： MERCK SHARP & DOHME LIMITED , HARRISON, Timothy , MACLEOD, Angus, Murray , STEVENSON, Graeme, Irvine , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D401/06
CPC分类号： C07D207/08 , C07D211/22 , C07D211/96 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I) wherein 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; X represents O or S; R represents phenyl optionally substituted by 1, 2 or 3 groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, -OR , SR , SOR , SO2R , -NR R , -NR COR , -NR CO2R , -CO2R or -CONR R , where R and R each independently represent H, C1-6alkyl, phenyl or trifluoromethyl; R represents phenyl optionally substituted by 1, 2 or 3 groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, -OR , SR , SOR , SO2R , -NR R , -NR COR , -NR CO2R , -CO2R or -CONR R , where R and R are as previously defined; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each heteroaryl and each phenyl moiety of benzyl and benzhydryl may be substituted by C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl; and 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 phenyl optionally substituted by one or more substituents selected from C1-6alkyl, C1-6alkoxy, halo and trifluoromethyl), Y-R or CO-Z-(CH2)q-R ; R , R , R and R each independently represent H or C1-6alkyl; R represents an optionally substituted aromatic heterocycle; R represents H, C1-6alkyl or phenyl; R and R each independently represent H or C1-6alkyl; 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, phenyl optionally substituted by one or more of C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl or phenylC1-4alkyl optionally substituted in the phenyl ring by one or more of C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl; R represents C1-6alkyl, trifluoromethyl or phenyl optionally substituted by one or more substituents selected from C1-6alkyl, C1-6alkoxy, halo and trifluoromethyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which way optionally be substituted by oxo; Z represents CH2, O, S or NR ; and q represents 0, 1, 2, 3, 4, 5 or 6 and their salts are useful as tachykinin antagonists.
摘要翻译：式（I）的化合物，其中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; X表示O或S; R 1表示任选被1,2或3个选自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，SO 2 R 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各自独立地表示H，C 1-6烷基，苯基或三氟甲基; R 2表示任选被1,2或3个选自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，SO 2 R 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如前所定义; 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; 其中苄基和二苯甲基的每个杂芳基和每个苯基部分可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; 和R 3代表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，任选地被选自（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和任选地被一个或多个选自C 1-6烷基，C 1-6烷氧基，卤代和三氟甲基），YR 8或CO-Z-（CH 2）q R 12; R 4，R 5，R 6和R 7各自独立地表示H或C 1-6烷基; R 8表示任选取代的芳族杂环; R 9表示H，C 1-6烷基或苯基; R 10和R 11各自独立地表示H或C 1-6烷基; 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，任选地被一个或多个C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代的苯基或在苯环中任选被苯基取代的苯基C 1-4烷基，更多的C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基; R 15代表任选被一个或多个选自C 1-6烷基，C 1-6烷氧基，卤素和三氟甲基的取代基取代的C 1-6烷基，三氟甲基或苯基; Y表示任选被氧代取代的1,2,3或4个碳原子的烃链; Z表示CH 2，O，S或NR 10; 和q代表0,1,2,3,4,5或6，它们的盐可用作速激肽拮抗剂。

3. 发明申请

WO1995019344A1 GEM-DISUBSTITUTED AZACYCLIC TACHYKININ ANTAGONISTS 审中-公开
公开(公告)号：WO1995019344A1
公开(公告)日：1995-07-20
申请号：PCT/GB1995000057
申请日：1995-01-12
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STEVENSON, Graeme, Irvine
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D211/22
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12
摘要： The present invention relates to compounds of formula (I), wherein A and A each independently represent hydrogen or C1-4alkyl; m is 2, 3 or 4; n is zero, 1 or 2 when m is 2 or 3 and n is zero or 1 when m is 4; R represents optionally substituted phenyl; R represents phenyl; heteroaryl; benzhydryl; or benzyl; each of which may be substituted; R represents H, COR , CO2R , COCONR R , COCO2R , SO2R , CONR SO2R , optionally substituted C1-6alkyl, Y-R or CO-Z-(CH2)q-R ; R represents C1-6alkyl substituted by a hydroxy group, or (CH2)pNR R , CO2R , CONR R , (CH2)pCO2R , (CH2)pCONR R , (CH2)pNR COR , (CH2)pNR SO2R , (CH2)pOR , (CH2)pOC(O)R or (CH2)pO(CH2)rCOR ; R represents hydrogen or C1-6alkyl or any of the substituents defined for R4; or R4 and R5 together with the carbon atom to which they are attached form an optionally substituted C3-6cycloalkyl ring; R and R each independently represent H or C1-6alkyl; X represents O or NR where R represents hydrogen or C1-6alkyl; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are tachykinin antagonists and 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A 1和A 2各自独立地表示氢或C 1-4烷基; 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表示苯基; 杂; 二苯甲基; 或苄基; 每个可以被替代; 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，YR 8或CO-Z-（CH 2）q R 12; R 4表示被羟基取代的C 1-6烷基，或（CH 2）p NR R R 11，CO 2 R 16，CONR 10 R 11，（CH 2）p CO 2 R 16，（ CH 2）p CONR 10 R 11，（CH 2）p NR 10 COR 18，（CH 2）pNR 10 SO 2 R 15，（CH 2）pOR 16，（CH 2）pOC（O） R 10或（CH 2）p O（CH 2）r COR 17; R 5表示氢或C 1-6烷基或对R 4定义的任何取代基; 或R 4和R 5与它们所连接的碳原子一起形成任选取代的C 3-6环烷基环; R 6和R 7各自独立地表示H或C 1-6烷基; X表示O或NR 19，其中R 19表示氢或C 1-6烷基; 及其药学上可接受的盐和前药。这些化合物是速激肽拮抗剂，特别用于治疗疼痛，炎症，偏头痛和呕吐。

4. 发明申请

WO1994013639A1 4-AMINOMETHYL/THIOMETHYL/SULFONYLMETHYL-4-PHENYLPIPERIDINES AS TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为TACHYKININ受体拮抗剂的4-氨基甲酰基/甲硫醇/磺酰基甲基-4-苯基哌啶
公开(公告)号：WO1994013639A1
公开(公告)日：1994-06-23
申请号：PCT/GB1993002535
申请日：1993-12-10
申请人： MERCK SHARP & DOHME LIMITED , MACLEOD, Angus, Murray , STEVENSON, Graeme, Irvine
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D211/26
CPC分类号： C07D211/20 , C07D211/24 , C07D211/26
摘要： Compounds of formula (I) are tachykinin antagonists and hence useful in medicine.
摘要翻译：式（I）化合物是速激肽拮抗剂，因此可用于药物。

5. 发明申请

WO1997001553A1 PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：哌啶和吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1997001553A1
公开(公告)日：1997-01-16
申请号：PCT/GB1996001478
申请日：1996-06-20
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , ELLIOTT, Jason , STEVENSON, Graeme, Irvine , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D403/14
CPC分类号： C07D401/14
摘要： The present invention provides compounds of formula (I), wherein R is a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms selected from nitrogen, oxygen and sulphur, which group is optionally substituted; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, OCF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substitued by C1-4alkoxy, where R and R each independently represent hydrogen or C1-4alkyl; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by C1-4alkoxy or CF3; R , R , R , R , R , A, X and Y are as defined in the specification; and m is zero or 1, and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明提供式（I）化合物，其中R 1是含有1,2,3或4个选自氮，氧和硫的杂原子的5-或6-元芳族杂环基，该基团任选被取代; R 2是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，OCF 3，NO 2，CN，SR a，SOR a，SO 2 R a，CO 2 R a，CONR C 1-6烷基，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各自独立地表示氢或C 1-4烷基; R 3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 4，R 5，R 6，R 9a，R 9b，A，X和Y如说明书中所定义; 和m为0或1，及其药学上可接受的盐和前药。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。

6. 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。

7. 发明申请

WO1997001554A1 PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：哌啶和吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1997001554A1
公开(公告)日：1997-01-16
申请号：PCT/GB1996001477
申请日：1996-06-20
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , ELLIOTT, Jason , STEVENSON, Graeme, Irvine , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention provides compounds of formula (I), wherein R is phenyl or a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur, which aryl or heteroaryl group is optionally substituted; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, OCF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, where R and R each independently represent hydrogen or C1-4alkyl; R , R , R , R and R , A, X, and Y are as defined in the specification; the dotted line is an optional double bond; Q is oxygen, sulphur or -NH-; Q is -N=, -NH-, -CH= or -CH2-; and m is zero or 1; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明提供式（I）化合物，其中R 1为苯基或含有1,2,3或4个选自氮，氧和硫的杂原子的5或6元芳族杂环基，该芳基或杂芳基任选被取代; R 2是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，OCF 3，NO 2，CN，SR a，SOR a，SO 2 R a，CO 2 R a，CONR 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各自独立地表示氢或C 1-4烷基; R 4，R 5，R 6，R 9a和R 9b，A，X和Y如说明书中所定义; 虚线是可选的双键; Q 1是氧，硫或-NH-; Q 2是-N =，-NH-，-CH =或-CH 2 - ; m为0或1; 及其药学上可接受的盐和前药。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。

8. 发明申请

WO1998001450A1 SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：螺旋哌啶衍生物及其作为治疗剂的用途
公开(公告)号：WO1998001450A1
公开(公告)日：1998-01-15
申请号：PCT/GB1997001710
申请日：1997-06-24
申请人： MERCK SHARP & DOHME LIMITED , CURTIS, Neil, Roy , HUSCROFT, Ian, Thomas , KULAGOWSKI, Janusz, Jozef , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D491/107
CPC分类号： C07D491/10 , A61K31/438
摘要： The present invention relates to compounds of formula (I), wherein R is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalyklC1-4alkyl, which groups are optionally substituted by hydroxy, C1-4alkoxy or NR R , where R and R each independently represent hydrogen or C1-4alkyl; or R is C1-4alkyl substituted by Ar, and optionally further substituted by one or both of R and R ; R , R and R represent a variety of substituents; R and R are each hydrogen, halogen, C1-6alkyl, CH2OR , oxo, CO2R or CONR R where R represents hydrogen, C1-6alkyl or phenyl; X is -CH2, or -CH2CH2-; Y is -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is -CH= or -CH2CH=, the broken line is a double bond; 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R为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，该基团任选被羟基，C 1-4烷氧基或NR 其中R a和R b各自独立地表示氢或C 1-4烷基; 或R为被Ar取代的C 1-4烷基，且任选进一步被R 4和R 5中的一个或两个取代; R 1，R 2和R 3代表各种取代基; R 9和R 10各自为氢，卤素，C 1-6烷基，CH 2 OH，氧代，CO 2 R a或CONR a R b，其中R e表示氢，C 1-6烷基或苯基; X是-CH 2或-CH 2 CH 2 - ; Y是-CH =，-CH 2 - ， - CH 2 CH =或-CH 2 CH 2 - ，条件是X + Y中的碳原子总数为2或3; 当Y为-CH =或-CH 2 CH =时，虚线为双键; 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。

9. 发明申请

WO1998024445A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SCHIZOPHRENIC DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗嗜酸性粒细胞减少症
公开(公告)号：WO1998024445A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006691
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of schizophrenic disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防精神分裂症的药物中的用途，使用这种NK-1 受体拮抗剂和包含它的药物组合物。

10. 发明申请

WO1995011880A1 SUBSTITUTED AMIDES AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译：作为TACHYKININ ANTAGONISTS的替代药物
公开(公告)号：WO1995011880A1
公开(公告)日：1995-05-04
申请号：PCT/GB1994002342
申请日：1994-10-24
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , HARRISON, Timothy , OWENS, Andrew, Pate , TEALL, Martin, Richard , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07C233/29
CPC分类号： C07D233/64 , C07C233/11 , C07C233/13 , C07C233/22 , C07C235/34 , C07C235/46
摘要： A class of substituted amide compounds of formula (I), are antagonists of tachykinins, especially substance P, and are therefore of use in the treatment or prevention of physiological disorders associated with an excess of tachykinins, such as inflammation, pain, migraine and emesis. In formula (I) Ar and Ar each independently represents a phenyl group optionally substituted by one, two or three groups selected from halo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C3-6cycloalkylC1-4alkyl, trifluoromethyl, cyano, nitro, SR , SOR , SO2R , OR , NR R , NR COR , NR CO2R , CO2R or CONR R , wherein R and R are each independently H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C3-6cycloalkylC1-4alkyl, phenyl or trifluoromethyl; Q represents Ar or a group of formula Het-(CH2)n-, where n is 1 or 2 and Het is a five or six membered nitrogen containing heterocyclic group with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulphur with at most one oxygen or sulphur atom, which group may have the residue of a further 5 or 6 membered aromatic ring fused thereto, and which group may be optionally substituted by a group selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, oxo, thioxo, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , SO2R , NR R , NR COR , NR CO2R , CO2R , CONR R or phenyl optionally substituted by 1, 2 or 3 groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , SO2R , NR R , NR COR , CO2R , or CONR R , where R and R are each independently H, C1-6alkyl, trifluoromethyl or phenyl; X represents a -CO-NR- or -NR-CO- group, where R is hydrogen, C1-6alkyl, or methyl substituted by a C2-6alkenyl or C2-6alkynyl group; one of Y and Y is a bond or C1-4alkylene group and the other is a C1-4alkylene group; with the proviso that when Ar and Q are dimethoxyphenyl, -Y -X-Y -Ar is not -CH2CON(CH3)CH2C6H5.
摘要翻译：一类取代的式（I）酰胺化合物是速激肽，特别是物质P的拮抗剂，因此可用于治疗或预防与超速激肽相关的生理紊乱症，例如炎症，疼痛，偏头痛和呕吐。在式（I）中，Ar 1和Ar 2各自独立地表示任选被一个，两个或三个选自卤素，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，C 3 -6环烷基C 1-4烷基，三氟甲基，氰基，硝基，SR a，SOR a，SO 2 R a，OR a，NR a R b，NR a COR b，NR 其中R a和R b各自独立地为H，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3 -C 10环烷基 C 3-6环烷基C 1-4烷基，苯基或三氟甲基; Q表示Ar 1或式Het-（CH 2）n - 的基团，其中n为1或2，Het为含有1,2或3个选自氮，氧或氧的杂原子的5或6元含氮杂环基具有至多一个氧或硫原子的硫，该基团可以具有与其稠合的另外5或6元芳环的残基，该基团可以任选地被选自C 1-6烷基，C 2-6烯基， 6-炔基，C3-7环烷基，C3-7环烷基C 1-4烷基，氧代，硫代，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR c，SR c，SOR c，SO 2 R c，NR c， R d，NR c，C d，NR c CO 2 R d，CO 2 R c，CONR c R d或任选被1,2或3个选自C 1的基团取代的苯基 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，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR c， NR c，R c，R c，R d，CO 2 R c或CONR c R d，其中R c和R d各自独立地为H，Cl -6-烷基，三氟甲基或苯基; X表示-CO-NR-或-NR-CO-基，其中R是氢，C 1-6烷基或被C 2-6烯基或C 2-6炔基取代的甲基; Y 1和Y 2之一是键或C 1-4亚烷基，另一个是C 1-4亚烷基; 条件是当Ar 1和Q是二甲氧基苯基时，-Y 1 -X-Y 2 -Ar 2不是-CH 2 CON（CH 3）CH 2 C 6 H 5。

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