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1. 发明申请

WO2009037296A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体具有活性的化合物及其在医学中的用途
公开(公告)号：WO2009037296A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062403
申请日：2008-09-18
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
IPC分类号： A61K31/423 , C07D401/04 , C07D413/04 , C07D498/04 , A61P25/28
CPC分类号： C07D413/04
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R 4 , R 5 , R 6 , Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6， Q，A，Y和R如说明书中所定义。公开了这些化合物作为药物的用途以及在制造用于治疗精神障碍，认知障碍和阿尔茨海默病的药物中的用途。本发明还公开了包含这些化合物的药物组合物。

2. 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。

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

WO0166564A3 GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译： GAMMA-分泌酶抑制剂
公开(公告)号：WO0166564A3
公开(公告)日：2002-01-03
申请号：PCT/GB0100855
申请日：2001-02-28
申请人： MERCK SHARP & DOHME , CASTRO PINEIRO JOSE LUIS , SMITH ADRIAN LEONARD , STEVENSON GRAEME IRVINE
发明人： CASTRO PINEIRO JOSE LUIS , SMITH ADRIAN LEONARD , STEVENSON GRAEME IRVINE
IPC分类号： A61K38/55 , A61K38/00 , A61K38/05 , A61P25/28 , A61P43/00 , C07K5/06 , C07K5/065
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/06026 , C07K5/06078
摘要： Novel urea derivatives of formula (I) are disclosed: The compounds are inhibitors of gamma -secretase, and hence useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的新型脲衍生物：该化合物是γ-分泌酶的抑制剂，因此可用于治疗或预防阿尔茨海默氏病。

5. 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。

6. 发明申请

WO2009037294A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的化合物及其在医学中的用途
公开(公告)号：WO2009037294A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062400
申请日：2008-09-18
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
IPC分类号： A61K31/423 , C07D401/04 , C07D413/04 , C07D498/04 , A61P25/28
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R 4 , R 5 , R 6 , Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

7. 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。

8. 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。

9. 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。

10. 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。

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