Abstract:
Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.q phenyl; are tachykinin antagonists useful for treating pain.
Abstract translation:PCT No.PCT / GB92 / 01241 Sec。 371日期:1993年12月17日 102(e)日期1993年12月17日PCT提交1992年7月8日PCT公布。 出版物WO93 / 01165 日期1993年1月21日式(I)化合物及其药学上可接受的盐:其中Q是任选取代的苯基或萘基; X和Y各自为H,C 1-6烷基,C 2-6烯基或X和Y一起= O; Z是O或S; R 1是H,任选取代的C 1-6烷基,任选取代的苯基(C 1-4烷基),C 2-6烯基,COC 1-6烷基卤素,CORA,COORa,CONHRa,COC 1-6烷基NR a R b或CONR a C 1-6烷基CONR a R b; R 2是取代的C 1-6烷基,任选取代的苯基(C 1-4烷基),C 2-6烯基,C 1-6烷基卤代,CORA,COORa,CONHRa,COC 1-6烷基NR a R b或CONR a C 1-6烷基CONR a R b; 或R 1和R 2一起形成任选被氧代取代的链(CH 2)p; R3是H [或C1-6烷基]; R4是H,C1-6烷基或苯基; 并且R 5是任选取代的(CH 2)q苯基; 是用于治疗疼痛的速激肽拮抗剂。
Abstract:
Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
Abstract:
The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I: ##STR1## or pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of neurodegenerative disorders.
Abstract:
A connector assembly including a first connector configured to be movably mounted to a support structure and having a first mating terminal. The first connector is movable with respect to the support structure in an axial direction along an alignment axis. The connector assembly also includes a second connector that is configured to be movably mounted to a support panel and has a second mating terminal. The second connector is movable with respect to the support panel in a radial direction relative to an alignment axis. The second connector shifts in the radial, direction to align the first and second mating terminals when the first and second connectors engage each other in a misaligned manner. The first connector moves between a projected position and a retracted position along the alignment axis to facilitate establishing a communication pathway between the first and second mating terminals.
Abstract:
A class of monomeric or dimeric peptides containing a specific hexa- or heptapeptide unit in either linear or cyclic form are active tachykinin antagonists and are therefore useful in disease states in which these peptides have been implicated, such as allergic conditions, inflammation, migraine, arthritis and CNS disorders.
Abstract:
Compounds of formula (I), or a salt or prodrug thereof, wherein R.sup.1 represents H, C.sub.1-4 alkyl or CH.sub.2 COOH; R.sup.2 represents H or C.sub.1-4 alkyl, with the proviso that R.sup.1 and R.sup.2 are not both H; R.sup.3 and R.sup.4 each independently rely resent H, C.sub.1-, alkyl. C.sub.2-6 alkenyl C.sub.1-6 alkoxy, halo or trifluoromethyl; A.sup.1, A.sup.2, A.sup.3, and A.sup.4 each independently represent H, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 alkoxy, halo or trifluoromethyl; and A.sup.5 and A.sup.6 each independently represent H or C.sub.1-4 are tachykinin antagonists useful ##STR1##
Abstract:
The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are defined herein, and pharmaceutically acceptable salts thereof, which are useful as tachykinin antagonists,
Abstract:
Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.
Abstract:
The present invention relates to compounds of formula (I), and salts and prodrugs thereof, wherein n is 1 , 2 or 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents optionally substituted (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3; R.sup.2 represents optionally substituted aryl, heteroaryl, benzhydryl or benzyl; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.8 represents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a variety of substituents, or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
Abstract translation:PCT No.PCT / EP94 / 00412 Sec。 371日期:1995年7月26日 102(e)日期1995年7月26日PCT 1994年2月10日PCT PCT。 WO94 / 19323 PCT出版物 (I)的化合物本发明涉及式(I)化合物及其盐和前药,其中n为1,2或3,并且其中(CH 2)n的任何碳原子可以是 被R4和/或R5取代; X表示O或S; R 1表示任选取代的(CH 2)q苯基,其中q是0,1,2或3; R 2表示任选取代的芳基,杂芳基,二苯甲基或苄基; 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C 1-6烷基或任选取代的苯基; R8表示H,CORa,CO 2 R a,COCONR a R b,COCO 2 R a,任选被各种取代基取代的C 1-6烷基,或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。 这些化合物是可用于治疗疼痛或炎症,偏头痛或呕吐的速激肽拮抗剂。
Abstract:
m is 0 or 1; andn is 0 or 1, where the sum total of n+m is 1 or 2.The compounds are of particular use in the treatment of pain, inflammation, migraine, emesis and postherpetic neuralgia.