摘要:
Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl, ethyl or n-propyl; andY is hydrogen, methyl, methoxy, fluorine or chlorine;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiphlogistics.
摘要:
Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, methyl or ethyl, andAr is phenyl, 3-chlorophenyl, 3-bromophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-tolyl, 2-methoxyphenyl, 3-methoxyphenyl, 2-pyridyl, 4-methyl-2-pyridyl, 6-methyl-2-pyridyl, 3-hydroxy-2-pyridyl, 3-pyridyl, 4-pyridyl, 6-chloro-3-pyridazinyl, 2-pyrazinyl, 6-chloro-2-pyrazinyl, 6-chloro-4-pyrimidinyl, 2-thiazolyl, 4-methyl-2-thiazolyl, 4-ethyl-2-thiazolyl, 5-methyl-2-thiazolyl, 5-ethyl-2-thiazolyl, 4,5-dimethyl-2-thiazolyl, 4-ethyl-5-methyl-2-thiazolyl, 5-ethyl-4-methyl-2-thiazolyl, 2-benzothiazolyl, 4,5,6,7-tetrahydro-2-benzothiazolyl, 5,6-dihydro-7H-thiopyrano[4,3-d]thiazol-2-yl, 3-methyl-5-isothiazolyl, 1,3,4-thiadiazolyl, 5-methyl-1,3,4-thiadiazol-2-yl or 5-methyl-3-isoxazolyl,And non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds as well as their salts are useful as inhibitors of platelet adhesion and aggregation.
摘要:
Compounds of the formula ##SPC1##WhereinR.sub.1 is isobutyl, phenyl, o-fluoro-phenyl, o-chloro-phenyl, cyclopentyl, cyclohexyl, methyl-cyclo-hexyl or cycloheptyl,R.sub.2 is hydrogen, fluorine, chlorine or bromine,R.sub.3 is methyl, ethyl or, when R.sub.1 is phenyl, fluoro-phenyl or chloro-phenyl, or R.sub.1 is cyclohexyl and R.sub.2 is halogen, also hydrogen,Z.sub.1 and Z.sub.2 are hydrogen or together form an additional carbon-to-carbon bond,A is ##EQU1## or ##EQU2## and M IS 2, 4, 6, 8 OR WHEN R.sub.1 is halo-phenyl, isobutyl, cyclohexyl, methyl-cyclohexyl, cyclopentyl or cycloheptyl and/or R.sub.2 is halogen and/or R.sub.3 is methyl or ethyl and/or A is --CH(OH)--, also O; the compounds are useful as antiphlogistics.
摘要:
New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
摘要:
New diazepinones of formula I ##STR1## wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human and veterinary medicine.
摘要:
New condensed diazepinones of general formula I are described ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A, R.sup.1 to R.sup.10 and Z are defined as in the specification.
摘要:
The specification describes a process for preparing 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide, a sweetener, from 1,2-benzisothiazol-3(2H)-one-1,1-dioxide by anodic oxidation in the presence of trifluoroacetic acid or trifluoromethanesulfonic acid and, optionally, in the presence of salts which increase the conductivity. The oxidation is effected in an anhydrous medium and the 4-trifluoroacetoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide formed as an intermediate when, for example, trifluoroacetic acid is used is decomposed with water to obtain the desired end product.
摘要:
Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.4 together represent an ethylene bridge,are suitable for the treatment of cholinergically induced spasms and motility disorders of the gastrointestinal tract and in the region of the evacuating bile ducts, for the symptomatic treatment of cystitis and of spasms from urelithiasis, for the treatment of relative incontinence, for the symptomatic treatment of bronchial asthma and bronchitis, and for the treatment of ischaemic heart diseases. The compounds are characterized by good selectivity.
摘要翻译:(I)其中] + E,crc / B /表示二价基团之一的通式I的缩二氮杂酮类(I)其中一个二价基团(S)(T) V)X是= CH-基或氮原子,R表示低级烷基,其可以任选地被任选地带有卤素,甲基或甲氧基的苯基进一步取代,R4和R5代表氢,卤素或低级烷基,R6 是氢,氯或甲基,R7和R8表示低级烷基,R8还另外表示卤素,m,n,o和p表示数字0,1,2或3,具有以下限制:m + n和 o + p的和表示数字1,2或3,n + o和m + p之和各自表示数字1,2,3,4或5,其中,然而, m + n + o + p必须始终大于2,A1,A2,A3和A4表示氢,或者对于m,n,o和p分别表示数字1,A1和A2一起或A3 和A4一起代表乙烯桥,适合于处理o f胆碱能诱发胃肠道的痉挛和运动障碍以及排空胆管区域,用于膀胱炎和尿毒症痉挛的症状治疗,用于治疗相对失禁,用于支气管哮喘和支气管炎的症状治疗, 并用于治疗缺血性心脏病。 该化合物的特征在于良好的选择性。
摘要:
Novel condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, A.sup.1, A.sup.2 and R.sup.1 -R.sup.10 are as defined herein. The condensed diazepinones are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia and they have spasmolytic effects on peripheral organs, particularly the colon, bladder and bronchi.