摘要:
Compounds of the formula whereinHet is a heterocycle;n is an integer from 1 to 4, inclusive, preferably 2 or 3;R.sub.1 is H or acyl;R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN;R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7 ; orR.sub.2 and R.sub.3, together with each other, are ##STR1## N.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ; R.sub.5 and R.sub.6 are each H or --CH.sub.3 ;R.sub.7 is C.sub.1 -C.sub.4 alkyl;R.sub.8 is H or C.sub.1 -C.sub.4 alkyl; andR.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
摘要:
Compounds of the formula ##STR1## wherein R is phenyl; phenyl having one or two substituents attached thereto, said substituents being selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, chlorine and trifluoromethyl; naphthyl; tetrahydronaphthyl; indanyl; pyridyl; isoquinolyl; or thiazolyl;R.sub.1 is ##STR2## where R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms,R.sub.4 and R.sub.5 are each hydrogen or alkyl of 1 to 4 carbon atoms, andQ is oxygen or two hydrogens,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halogen,A is a single carbon-to-carbon bond or --OCH.sub.2 --,R.sub.6 is hydrogen, hydroxyl, alkoxy of 1 to 4 carbon atoms or alkanoyloxy of 1 to 4 carbon atoms, andm is 0, 1, 2, 3, 4 or 5, but other than 0 when R.sub.6 is hydroxyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as CNS-depressants, adrenolytics, antiphlogistics, analgesics, antihistaminics and anticholesteremics.
摘要:
Pharmaceutical compositions containing as an active ingredient a compound of the formula ##SPC1##Wherein R' is in the m- or p-position and is selected from the group consisting of--CH.sub.2 --A, --CHR.sub.1 --CH.sub.2 --Aand ##EQU1## where R.sub.1 is hydrogen or hydroxyl, andA is ##SPC2##WhereR.sub.3 is hydrogen, chlorine, methyl, ethyl, trifluoromethyl or lower alkoxy, andR.sub.4 is hydrogen or methyl, orR.sub.3 and R.sub.4, together with each other and neighboring carbon atoms of the phenyl ring to which they are attached, are naphthyl,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as CNS-depressants, neuroleptics and anticholesteremics.
摘要:
Compounds of the formula ##STR1## wherein Het is ##STR2## n is an integer from 1 to 4, inclusive, preferably 2 or 3, R.sub.1 is H or acyl,R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN,R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7,R.sub.2 and R.sub.3 together with each other are ##STR3## R.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5, R.sub.5 and R.sub.6 are each H or --CH.sub.3,R.sub.7 is C.sub.1 -C.sub.4 alkyl,R.sub.8 is H or C.sub.1 -C.sub.4 alkyl,R.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen,R.sub.10 and R.sub.12 are each H, CH.sub.3, Cl or OCH.sub.3, or together methylenedioxy,X is ##STR4## or N, and Z is --CH.sub.2 or --CO;in the form of racemates, enantiomers, diastereoisomeric antipode pairs, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
摘要翻译:其中Het为+4 u>的化合物,n为1〜4的整数,优选2或3,R 1为H或酰基,R 2为H,R 10,-NHSO 2 R 7, NHCOR 8,-NHCONHR 8,-NH-CH 2 -C 6 H 4 -R 9,-CH 2 OH,-CH 2 SO 2 R 7,-CONHR 8,卤素或-CN,R 3是H,卤素,R 7或-OR 7,R 2和R 3彼此是 R4是H,-CH3或-C2H5,R5和R6分别是H或-CH3,R7是C1-C4烷基,R8是H或C1-C4烷基,R9是H,C1-C4烷基或C1-C4烷氧基 被氧中断,R 10和R 12各自为H,CH 3,Cl或OCH 3,或一起亚甲二氧基,X为或N,Z为-CH 2或-CO; 以外消旋物,对映异构体,非对映异构体对映体对及其无毒的药学上可接受的酸加成盐的形式存在。 化合物和盐可用作支气管解痉药,解痉药,肌肉松弛剂,抗过敏药和低血压药。
摘要:
Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen; alkyl of 1 to 5 carbon atoms; or optionally substituted aralkyl or 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 8 carbon atoms or arylmethyl; orR.sub.1 and R.sub.2, together with each other, are --(CH.sub.2).sub.4 or --(CH.sub.2).sub.5 --; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or arylmethyl; orR.sub.3 and R.sub.4, together with each other, are --CH.sub.3 -- or --CH.sub.2 --CH.sub.2 --;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of cardiovascular diseases, especially hypertension.
摘要:
Compounds of the formula ##STR1## wherein A is a single bond, ##STR2## R.sub.1 is --OH, --0--acyl, chlorine or hydrogen; R.sub.2 is hydrogen, methyl or ethyl;R.sub.3 is ##STR3## m is 2, 3 or 4; n is 1, 2 or 3;R.sub.4 is hydrogen or lower alkyl;R.sub.5 is hydrogen, lower alkyl or, when R.sub.4 is hydrogen, also phenyl;R.sub.6, R.sub.7 and R.sub.8 are each hydrogen or methyl;R.sub.9 is hydrogen, --Ar, --OAr or --NH--CO--Ar;Ar is ##STR4## R.sub.10, R.sub.11 and R.sub.12 which may be identical to or different from each other, are each hydrogen, hydroxyl, methyl, methoxy, halogen, methylenedioxy, --NH--R.sub.13 or --CONH.sub.2 ; andR.sub.13 is hydrogen, acyl or lower alkylsulfonyl;and non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as their salts are useful for the treatment of asthma, bronchitis, urticaria, conjunctivities, hay fever, colds and cardiovascular disorders, and for relaxation of the uterine musculature.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms, or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要:
This invention relates to the novel compound 11-oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid of the formula ##STR1## and non-toxic, pharmacologically acceptable salts thereof, as well as to pharmaceutical composition containing these compounds as active ingredients, and methods of using them as antiallergics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is alkyl of 6 to 19 carbon atoms, andR.sub.2 is methyl or ethyl,And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as the salts are useful as pharmaceuticals for the treatment of cardiac and circulatory insufficiencies.