摘要:
Aminoalkylbenzene derivative of the formula: wherein
A is oxygen or sulfur; Y is oxo, thioxo, or cyanoimino; a is an integer of 1 to 3; b is an integer of 0 to 3; c is an integer of 1 to 4; R 1 is alkyl; R 2 is hydrogen or alkyl; or R 1 and R 2 taken together represent pyrrolidinyl; R is hydrogen, cycloalkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: wherein
R 3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy; R 4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; or R 3 and R 4 taken together represent alkylidene or aralkylidene;
with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents and their acid addition salts being useful as histamine H 2 blockers, especially peptic ulcer remedies.
摘要翻译:下式的氨基烷基苯衍生物:... 其中A是氧或硫; Y是氧代,硫代或氰基亚氨基; a是1至3的整数; b是0-3的整数; c为1〜4的整数; R 1为烷基; R 2为氢或烷基; 或R 1和R 2一起代表吡咯烷基; R是氢,环烷基,三卤代烷基,烷氧基,二烷基氨基,芳基,芳酰基,杂环基或下式的基团:其中... R 3是氢,卤素,氨基,烷基,烷基氨基,二烷基氨基,烷硫基或芳氧基; R 4是氢,烷基,烯基,芳基或杂环基; 或R 3和R 4一起代表亚烷基或亚烷叉基;条件是上述芳基,芳酰基和杂环基可被1至3个取代基取代,并且它们的酸加成盐可用作组胺H2 阻滞剂,特别是消化性溃疡补救。
摘要:
Novel antibiotic stalobacins A, B, C, D, E, F and G having physicochemical properties as shown in Tables 1, 2 and 3 are provided, which are excellent antibiotics showing marked effects on Gram-positive bacteria.
摘要:
The present invention relates to the compounds of the formula:
in which R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are independently hydrogen, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, hydroxy, acyloxy, or halogen; R⁹ is hydrogen, hydroxy, acyloxy, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, or lower alkylamino which is optionally substituted; E¹ is hydrogen, or an ester residue; m is an integer of from 1 to 4; or a pharmaceutically acceptable salt thereof. The compounds of the present invention exhibit phospholipase A₂ inhibitory activity, and can be used in treating inflammatory conditions.
摘要翻译:本发明涉及下式的化合物:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7, R 8独立地为氢,任选取代的低级烷基,任选取代的低级烷氧基,羟基,酰氧基或卤素; R 9是氢,羟基,酰氧基,任选被取代的低级烷基,任选被取代的低级烷氧基或任选取代的低级烷基氨基; E 1是氢或酯残基; m为1〜4的整数, 或其药学上可接受的盐。 本发明化合物表现出磷脂酶A2抑制活性,可用于治疗炎性病症。
摘要:
9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: wherein n is 0 or 1, R is -COR 1 , -CONR 4 R 5 or -CH 2 R 6 , R 1 is C 1 -C 5 alkyl, C 3 -C 7 cycloalkyl, allylthio, styryl, phenoxymethyl, thienylmethyl, C 6 -C 10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R 2 and R 3 each is hydrogen, C l -C 5 alkyl, carboxy, C 2 -C 5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R 4 and R 5 each is hydrogen, C l -C 5 alkyl, C 3 -C 7 cycloalkyl or phenyl optionally substituted, and R 6 is pyridyl or phenyl optionally substituted are useful as antiulcer agents and may be provided by several routes.
摘要:
9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: wherein n is 0 or 1, R is -COR 1 , -CONR 4 R 5 or -CH 2 R 6 , R 1 is C 1 -C 5 alkyl, C 3 -C 7 cycloalkyl, allylthio, styryl, phenoxymethyl, thienylmethyl, C 6 -C 10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R 2 and R 3 each is hydrogen, C l -C 5 alkyl, carboxy, C 2 -C 5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R 4 and R 5 each is hydrogen, C l -C 5 alkyl, C 3 -C 7 cycloalkyl or phenyl optionally substituted, and R 6 is pyridyl or phenyl optionally substituted are useful as antiulcer agents and may be provided by several routes.
摘要:
A compound of the formula: wherein the wave line means α-bond or β-bond, which compound is useful as a phospholipase A₂ inhibitor. Process for the production of the compound, pharmaceutical composition containing the compound, and a cell culture of a microorganism Thielavia terricola RF-143 producing the compound are also provided.