摘要:
Novel 7-acetylspirobenzofuranone compound of the formula: ##STR1## has gastric secretion inhibitive, antiinflammatory and analgesic activities, and is of value as drugs.
摘要:
Novel spiro compounds of the formula: ##STR1## wherein Ring A represents a benzene ring or a naphthalene ring, said rings being unsubstituted or substituted by at least one of lower alkyl, nitro, halogen, amino which may optionally be substituted, hydroxyl which may optionally be substituted, acyl, sulfamoyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may optionally be substituted, ureido which may optionally be substituted, thioureido which may optionally be substituted, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminomethyl which may optionally be substituted, cyano and phenyl, have gastric secretion inhibitive, anti-inflammatory and analgesic activities, and are of value as drugs.
摘要:
Novel aminotetralol compounds of the formula ##STR1## wherein Z.sup.1 and Z.sup.2 are hydrogen or an alkyl group and R.sup.1 is a substituted acyclic hydrocarbon group or a cyclic hydrocarbon group, and their pharmaceutically acceptable salts, have excellent pharmacological activities such as strong bronchodilating activity or .beta.-adrenergic blocking activity. They are useful as medicines, for example, for treatment of asthma or arrhythmia.
摘要:
The compounds of the formula ##STR1## wherein G stands for an amidino group or an optionally cyclic amino group, these being respectively optionally substituted; D stands for a spacer having 2 to 6 atomic chain optionally bonded through a hetero-atom and/or a 5- to 6-membered ring (provided that the 5- to 6-membered ring is, depending on its bonding position, counted as 2 to 3 atomic chains); R.sup.1 stands for hydrogen, benzyl group or a lower alkyl group; R.sup.2 and R.sup.3 independently stand for a residual group formed by removing --CH(NH.sub.2)COOH from an .alpha.-amino acid, or R.sup.1 and R.sup.2 may form a 5- to 6-membered ring taken together with the adjacent N and C; X stands for hydrogen or an optionally substituted lower alkyl group; and Z stands for a group capable of forming an anion or a group convertible into an anion in a living body, or salts thereof and agents for inhibiting cell-adhesion, which are characterized by containing these compounds. The novel compounds and pharmaceutical agents are effective for prophylaxis and therapy of various diseases by controlling or inhibiting cell adhesion.
摘要:
Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.
摘要:
Platelet Activating Factor (PAF) antagonists which comprise the compounds of the formula (I): ##STR1## wherein A is an optionally substituted phenyl or an optionally substituted heterocyclic group; X is methylene group, carbonyl group or thiocarbonyl group; R.sup.1, R.sup.2 and R.sup.3 are independently a lower alkyl group, and their salts are excellent in absorption from the intestinal canal.Among the compounds of the formula (I), those wherein A is an optionally substituted 2,3-dihydro-1-benzoxepin-4-yl group are novel compounds and exhibit excellent PAF antagonism.
摘要:
Novel condensed, seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 each represent hydrogen, halogen, trifluoromethyl, lower alkyl or alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or alkyl, aralkyl or cycloalkylalkyl which may be substituted; X is a group represented by the formula S(O).sub.n (where n is an integer of 0 to 2); Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of hypertension.
摘要:
Novel 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives of the formula ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, optionally substituted lower alkyl or optionally substituted aralkyl; R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aralkyl or optionally substituted cycloalkylalkyl; Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds and salts thereof exhibits inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases (e.g. hypertension, cardiopathy, cerebral apoploxy).
摘要翻译:式[IMAGE]的新型3-氨基-4-氧代-2,3,4,5-四氢-1,5-苯并氧氮杂衍生物[其中R1和R2独立地为氢,卤素,三氟甲基,低级烷基或低级烷氧基, 或两者共同形成三亚甲基或四亚甲基; R3是氢,任选取代的低级烷基或任选取代的芳烷基; R 4是氢,任选取代的烷基,任选取代的芳烷基或任选取代的环烷基烷基; Y是可被酯化或酰胺化的羧基; m为1或2]及其盐。 这些化合物及其盐对血管紧张素转换酶等表现出抑制活性,作为循环系统疾病(例如高血压,心脏病,脑酰化氧化物)的诊断,预防和治疗药物具有价值。
摘要:
Novel spirobenzofuranone compounds of the formula: ##STR1## have gastric secretion inhibitive, antiinflammatory and analgesic activities, and are of value as drugs.
摘要:
The present invention relates to novel 1-azaxanthone derivatives, which are shown by the following formula: ##STR1## wherein m is 1 or 2R'.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxycarbonyl, hydroxy, C.sub.1-4 alkoxy, amino or C.sub.1-3 alkylamino;each of R.sub.2 is independently C.sub.1-6 alkyl, C.sub.1-4 alkoxy, halogen, nitro, hydroxy, carboxy, amino, C.sub.1-3 alkylamino or di(C.sub.1-3 alkyl) amino; orwhen m is 2, the two R.sub.2 groups may be independently as defined above or may form together with adjacent rings carbon atoms the butadienylene group;R.sub.3 is cyano, C.sub.1-6 alkoxycarbonyl, carboxamide, N-C.sub.1-3 alkylcarboxamide or N,N-di(C.sub.1-3 alkyl) carboxamide.The novel derivatives are useful as intermediates for 1-azaxanthone-3-carboxylic acid derivatives having effective antiallergic and bronchodilating activities.