摘要:
Novel xanthine derivatives of the formula (1): wherein R 1 , which may be optionally bound through a hetero atom, is a hydrocarbon residue which may be substituted; one of R 2 and R 3 is a hydrocarbon residue which may be substituted, and the other is hydrogen or a hydrocarbon residue which may be substituted; R 4 is hydrogen, halogen or nitro; R 5 is a residue capable of forming an anion or a residue convertible into the anion; A is a direct bond or a spacer having atomic length of two or less; n is an integer of 1 or 2; and Y and Z, which may be the same or different, are an oxygen atom or a sulfur atom; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonist activity and hypotensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
摘要翻译:式(I)的新型黄嘌呤衍生物:其中R 1可以任选地通过杂原子结合,是可以被取代的烃残基: R 2和R 3之一是可被取代的烃残基,另一个是氢或可被取代的烃残基; R 4是氢,卤素或硝基; R 5是能够形成阴离子或可转化成阴离子的残基的残基; A是原子长度为2以下的直接键合或间隔物; n为1或2的整数; Y和Z可以相同或不同,为氧原子或硫原子; 其药学上可接受的盐具有有效的血管紧张素II拮抗剂活性和降血压活性,因此可用作治疗循环系统疾病如高血压疾病,心脏病,中风等的治疗剂。
摘要:
Nitrogen-containing heterocyclic compounds of the formula (I): wherein Y is N or CH; R 1 , which may be optionally bound through a hetero atom, is a hydrocarbon residue which may be substituted; R 2 and R 3 which may be same or different, are each independently hydrogen, cyano, nitro, optionally substituted lower alkyl, or -COD wherein D is alkoxy, hydroxy, halogen, or optionally substituted amino; or R 2 and R 3 are taken together to form a benzene ring which may be substituted; the dotted line is a chemical bond; Z is bound to a hetero nitrogen atom and is a group having the formula: wherein R 4 is hydrogen, halogen or nitro, and R 5 is a residue capable of forming an anion or a residue convertible into an anion; A is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonist activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
摘要:
Novel fused thiophene derivatives of the formula (I):
wherein W is or
R¹ and R² which may be same or different, are each independently hydrogen, halogen, cyano, nitro, acylamino, or a hydrocarbon residue which may be substituted; R³ is hydrogen, optionally substituted alkyl or alkenyl, or -COD wherein D is hydrogen, alkoxy, hydroxy, halogen, or optionally substituted amino; R⁴ is hydrogen, halogen or nitro; R⁶ is a residue capable of forming an anion or a residue convertible into an anion; R⁶ is hydrogen or optionally substituted alkyl or alkenyl; R⁷ is a hydrocarbon residue which may be substituted; A is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonist activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
摘要翻译:式(I)的新型稠合噻吩衍生物:其中W是或 R 1和R 2可以相同或不同,各自独立地为氢,卤素,氰基,硝基 ,酰氨基或可被取代的烃残基; R 3是氢,任选取代的烷基或烯基或-COD,其中D是氢,烷氧基,羟基,卤素或任选取代的氨基; R 4是氢,卤素或硝基; R 6是能够形成阴离子或可转化为阴离子的残基的残基; R 6是氢或任选取代的烷基或链烯基; R 7是可以被取代的烃残基; A是在亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; n为1或2的整数; 其药学上可接受的盐具有有效的血管紧张素II拮抗剂活性和抗高血压活性,因此可用作治疗循环系统疾病如高血压疾病,心脏病,中风等的治疗剂。
摘要:
Nitrogen-containing heterocyclic compounds of the formula (I): wherein Y is N or CH; R 1 , which may be optionally bound through a hetero atom, is a hydrocarbon residue which may be substituted; R 2 and R 3 which may be same or different, are each independently hydrogen, cyano, nitro, optionally substituted lower alkyl, or -COD wherein D is alkoxy, hydroxy, halogen, or optionally substituted amino; or R 2 and R 3 are taken together to form a benzene ring which may be substituted; the dotted line is a chemical bond; Z is bound to a hetero nitrogen atom and is a group having the formula: wherein R 4 is hydrogen, halogen or nitro, and R 5 is a residue capable of forming an anion or a residue convertible into an anion; A is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonist activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
摘要翻译:式(I)的含氮杂环化合物:其中Y是N或CH; R 1可以任选地通过杂原子结合,是可以被取代的烃残基; R 2和R 3可以相同或不同,各自独立地为氢,氰基,硝基,任选取代的低级烷基或-COD,其中D为烷氧基,羟基,卤素或任选取代的氨基; 或R 2和R 3一起形成可被取代的苯环; 虚线是化学键; Z结合杂氮原子,并且是具有下式的基团:其中R 4是氢,卤素或硝基,R 5是能够形成阴离子的残基或可转化为 阴离子; A是在亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; n为1或2的整数; 及其药学上可接受的盐具有有效的血管紧张素II拮抗剂活性和抗高血压活性,因此可用作治疗循环系统疾病如高血压疾病,心脏病,中风等的治疗剂。
摘要:
The compounds having a 4,11-dioxo-3-oxa8(or 7)-thia-1- azatricyclo[7,2,0,0 2,6 ]undecane-2-carboxylic acid skeleton as the base structure, their esters and their salts are useful antibacterial agents.
摘要:
The compound represented by the formula: where R' stands for amino or an organic residue bonded through nitrogen; R 2 stands for carooxyl ora group derivable therefrom; R 3 , R 4 , R 5 , R 6 , R 7 and R 8 independently stand for hydrogen or an organic residue, including the case where R 5 or R 6 forms a chemical bond or a ring with R 7 or R 8 : X stands for hvdrogen, methoxy or formylamino; or a salt thereof, pro- duceaole by the present method. exnibits excellent antimicrobial activity, and is utilized as antimicrobial agents.
摘要:
Novel xanthine derivatives of the formula (1): wherein R 1 , which may be optionally bound through a hetero atom, is a hydrocarbon residue which may be substituted; one of R 2 and R 3 is a hydrocarbon residue which may be substituted, and the other is hydrogen or a hydrocarbon residue which may be substituted; R 4 is hydrogen, halogen or nitro; R 5 is a residue capable of forming an anion or a residue convertible into the anion; A is a direct bond or a spacer having atomic length of two or less; n is an integer of 1 or 2; and Y and Z, which may be the same or different, are an oxygen atom or a sulfur atom; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonist activity and hypotensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
摘要翻译:式(I)的新型黄嘌呤衍生物:其中R 1可以任选地通过杂原子结合,是可以被取代的烃残基: R 2和R 3之一是可被取代的烃残基,另一个是氢或可被取代的烃残基; R 4是氢,卤素或硝基; R 5是能够形成阴离子或可转化成阴离子的残基的残基; A是原子长度为2以下的直接键合或间隔物; n为1或2的整数; Y和Z可以相同或不同,为氧原子或硫原子; 其药学上可接受的盐具有有效的血管紧张素II拮抗剂活性和降血压活性,因此可用作治疗循环系统疾病如高血压疾病,心脏病,中风等的治疗剂。