摘要:
[Constitution] A compound represented by the formula [I], [Chemical Formula 1]
[wherein X stands for a methine group or a nitrogen atom; R¹ stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R² and R³ respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent -C=C-; R⁴ and R⁵ respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or hetero-cyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively], salts thereof, a method of preparing same or pharmaceutical compositions containing same. [Effects] Excellent antiasthmatic agents
摘要翻译:由下式表示的新化合物:其中X代表次甲基(即基团-CH =)或氮原子; R 1表示氢原子,任选取代的低级烷基或卤素原子; R 2和R 3分别表示氢原子或任选取代的低级烷基,或者一起可以形成与相邻的-C = C-结合的5-至7-元环; R 4和R 5分别表示氢原子或任选取代的低级烷基,或者一起形成与相邻碳原子结合的3-至7-元同 - 或杂 - 环; A代表任选取代的氨基; m和n分别表示1至4个或其盐,其具有抗过敏,抗炎和抗PAF活性,并且可用作抗哮喘药。
摘要:
A cephem compound of the general formula: , wherein R, is an amino group which may be protected, Q is nitrogen or a group of C-R 2 in which R2 is hydrogen or a halogen,
R 3 is hydrogen or a hydrocarbon residue which may be substituted, A is a triazolopyridinyl, triazolopyridazinyl or triazolopyrazinyl group which may be substituted, or a salt or ester thereof , and a process for preparing the same and a pharmaceutical composition thereof are disclosed.
摘要:
A compound of the general formula: wherein R° is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S → O, O or CH 2 ; R 4 is hydrogen, methoxy group or formamido group; R 13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with a 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other, or a salt or ester thereof. And a process for preparing the same and a pharmaceutical composition thereof are disclosed.
摘要:
A compound of the formula: wherein R 1 stands for n-propyl or isoprppyl; and R 2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要:
New bicyclic compounds, inclusive of salts thereof, of the formula: wherein R 1 and R 2 , which may be the same or different, each represent hydrogen, halogen, lower alkyl, hydroxyl, lower alkyloxy or aralkyloxy, or R' and R 2 jointly represent lower alkylenedioxy: R 3 and R 4 each represent hydrogen or lower alkyl; R 3 represents hydrogen,lower alkyl or -CH 2 SR 7 (R 7 represents hydrogen or acyl): R 6 represents hydrogen or acyl, or R 6 and R 7 jointly represent a single bond; X represents -CH 2 -, -O- orN-R 5 (R 8 represents hydrogen, acyl or lower alkyl); I and n represents 2, 3 or 4, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.
摘要翻译:其中R 1和R 2可以相同或不同的新的双环化合物,包括其盐,其具有下式:其中R 1和R 2各自表示氢,卤素,低级烷基,羟基,低级烷氧基或芳烷氧基 ,或R 1和R 2共同表示低级亚烷基二氧基; R 3和R 4各自代表氢或低级烷基; R 5表示氢,低级烷基或-CH 2 SR 7(R 7表示氢或酰基); R 6表示氢或酰基,或R 6和R 7共同表示单键; X表示-CH 2 - , - O-或者N-R 8(R 8表示氢,酰基或低级烷基)。 n代表2,3或4,具有血管紧张素转换酶和缓激肽分解酶的抑制活性,可用作抗高血压药。
摘要:
A composition for inhibiting an eosinophil chemotaxis which comprises a compound of the formula:
wherein R¹ represents a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; either A or B represents a nitrogen atom with the other representing a methine group, or both of them represents a methine group; R² and R³ independently represent a hydrogen atom or an optionally substituted lower alkyl group, or R² and R³ taken together with the adjacent -C=C-, may form a 5- to 7-membered ring; X represents a methylene group, an oxygen atom or S(O)p wherein p represents an integer of 0 to 2; Y represents (i) a group of the formula
wherein R⁴ and R⁵ independently represent a hydrogen atom or an optionally substituted lower alkyl group or (ii) a divalent group derived from an optinally substituted 3- to 7-membered homocyclic or heterocyclic ring; R⁶ represents a primary to tertiary amino group; m and n independently represent an integer of 0 to 4, or a salt thereof. Said composition is useful for treating a disease related to eosinophil chemotaxis such as allergic rhinits and/or atopic dermatitis and so on.
wherein R¹ is a hydrogen atom, a lower alkyl group or a halogen atom; R² and R³ are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent -C=C-; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R⁶ and R⁷ are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together with the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.
摘要翻译:下式的化合物:其中R 1是氢原子,低级烷基或卤素原子; R 2和R 3是与相邻的-C≡C-一起形成的氢原子,低级烷基或5-至7-元环基; X是氧原子,硫原子或亚甲基; Y是任选取代的亚甲基,二价3-至7-元均基或杂环基; R 6和R 7是与相邻氮原子一起形成的氢原子,低级烷基,环烷基,芳基或含氮杂环基; m为0〜4的整数。 n为0〜4的整数,或其盐。 所述化合物具有优异的抗PAF活性,抗过敏作用等,因此可用作抗哮喘药。