Abstract:
This invention relates to a threaded valved inflation needle designed for controlled inflation or deflation of balls and toys by communicating with standard air sources, inflation methods and pressure monitoring devices. The invention is useful for adjustment and monitoring of internal pressure in balls that utilize a rubber valve of the type that commonly appears in recreational balls. The invention is also useful for controlled inflation of toys that utilize plastic pull out valves for communicating with external air sources. The utility and convenience of the threaded valved inflation needle is further enhanced by a cover designed to hold, protect, and lubricate the threaded valved inflation needle when not in use.
Abstract:
This invention relates to a threaded valved inflation needle designed for controlled inflation or deflation of balls and toys by communicating with standard air sources, inflation methods and pressure monitoring devices. The invention is useful for adjustment and monitoring of internal pressure in balls that utilize a rubber valve of the type that commonly appears in recreational balls. The invention is also useful for controlled inflation of toys that utilize plastic pull out valves for communicating with external air sources. The utility and convenience of the threaded valved inflation needle is further enhanced by a cover designed to hold, protect, and lubricate the threaded valved inflation needle when not in use.
Abstract:
This invention relates to compounds of the formulae (I), (II), (III), wherein R'- R e , A, X, and Z are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.
Abstract:
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Abstract:
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, -C(A)Y, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C l-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; Y is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; aryl is independently selected from phenyl, naphthyl, anthracyl or phenanthryl; het is independently selected from an aromatic or non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R 2 is aryl 1 or het 1 , each optionally substituted; aryl 1 is independently selected from phenyl, naphthyl, anthracyl, phenanthryl, or indanyl; het 1 is an aromatic 5 to 10 membered heterocyclic ring system which contains at least one N, O or S heteroatom, optionally containing an aryl group; R 3 is H, C 1-8 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, C 1-8 alkylSC 1-8 alkyl, het 3 , or het 3 -C 1-4 alkyl, wherein the alkyl, cycloalkyl and het 3 groups are each optionally substituted; het 3 is a non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; or R 3 is (CH 2 ) a
Abstract translation:式(I)化合物及其药学和/或兽医学上可接受的衍生物,其中:R 1是H,C 1-6烷基,-C(A)Y C 3-8环烷基,芳基,苯基,芳基-C 1-4烷基或叔-C 1-4烷基,其中 环烷基,芳基或苯基基团任选被取代; A是S或O; Y是H,C 1-6烷基,芳基,苯基,芳基-C 1-4烷基或叔丁基C 1-4烷基 ; 芳基独立地选自苯基,萘基,蒽基或菲基; 独立地选自芳族或非芳族的4-,5-或6-元杂环,其含有至少一个N,O或S杂原子,任选地与5-或6-元碳环基团或第二4- 含有至少一个N,O或S杂原子的5-或6-元杂环; R 2是每个任选被取代的芳基1或1或1; 芳基1独立地选自苯基,萘基,蒽基,菲基或茚满基; 包含至少一个任选含有芳基的N,O或S杂原子的芳族5至10元杂环系统; R 3是H,C 1-8烷基,C 3-8环烷基,C 3-8环烷基 C 1-6烷基,C 1-8烷基,C 1-6烷基,H 3或H 3 其中烷基,环烷基和叔丁基各自任选被取代; 它是非芳族的4-,5-或6-元杂环,其含有至少一个N,O或S杂原子,任选地与5-或6-元碳环基团或 含有至少一个N,O或S杂原子的第二个4-,5-或6-元杂环; 或者R 3是(CH 2)2。
Abstract:
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, -C(A)Y, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C l-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; Y is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; aryl is independently selected from phenyl, naphthyl, anthracyl or phenanthryl; het is independently selected from an aromatic or non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R 2 is aryl 1 or het 1 , each optionally substituted; aryl 1 is independently selected from phenyl, naphthyl, anthracyl, phenanthryl, or indanyl; het 1 is an aromatic 5 to 10 membered heterocyclic ring system which contains at least one N, O or S heteroatom, optionally containing an aryl group; R 3 is H, C 1-8 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, C 1-8 alkylSC 1-8 alkyl, het 3 , or het 3 -C 1-4 alkyl, wherein the alkyl, cycloalkyl and het 3 groups are each optionally substituted; het 3 is a non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; or R 3 is (CH 2 ) a , K, wherein a' is 0, 1 or 2 and K is a group selected from: Formula (i) wherein: Z is O, S, NR 12 , (CH 2 ) V or a bond; a is 1, 2, 3 or 4; b is 1, 2 or 3; v is 1 or 2; R 10 and R 11 are each independently H or C 1-4 alkyl; R 12 is H, C 1-6 alkyl, C(O)C 1-6 alkyl, SO 2 -C 1-6 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula(iii) wherein: c is 1, 2, 3 or 4; d is 1, 2 or 3; e is 1 or 2; and R 30 is H or C 1-4 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: f is 0, 1, 2 or 3; L is SO, SO 2 or NR 40 ; and R 40 is H, C 1-6 alkyl, C(O)C 1-6 alkyl, SO 2 -C 1-6 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (v) wherein: g is 0, 1, 2 or 3; and R 50 is H, C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCHF 2 , OCF 3, SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; and Formula (vi) CH(cyclopropane) 2 ; X is a covalent bond, C 1-8 alkyl or C 3-8 cycloalkyl, wherein if X is C 3-8 cycloalkyl, then R 2 -X may form a fused aryl-cycloalkyl ring system; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre.
Abstract translation:式(I)化合物及其药学和/或兽医学上可接受的衍生物,其中:R 1是H,C 1-6烷基,-C(A)Y C 3-8环烷基,芳基,苯基,芳基-C 1-4烷基或叔-C 1-4烷基,其中 环烷基,芳基或苯基基团任选被取代; A是S或O; Y是H,C 1-6烷基,芳基,苯基,芳基-C 1-4烷基或叔丁基C 1-4烷基 ; 芳基独立地选自苯基,萘基,蒽基或菲基; 独立地选自芳族或非芳族的4-,5-或6-元杂环,其含有至少一个N,O或S杂原子,任选地与5-或6-元碳环基团或第二4- 含有至少一个N,O或S杂原子的5-或6-元杂环; R 2是每个任选被取代的芳基1或1或1; 芳基1独立地选自苯基,萘基,蒽基,菲基或茚满基; 包含至少一个任选含有芳基的N,O或S杂原子的芳族5至10元杂环系统; R 3是H,C 1-8烷基,C 3-8环烷基,C 3-8环烷基 C 1-6烷基,C 1-8烷基,C 1-6烷基,H 3或H 3 其中烷基,环烷基和叔丁基各自任选被取代; 它是非芳族的4-,5-或6-元杂环,其含有至少一个N,O或S杂原子,任选地与5-或6-元碳环基团或 含有至少一个N,O或S杂原子的第二个4-,5-或6-元杂环; 或R 3是(CH 2)2,...,