摘要:
Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen or methyl, m is 0 or an integer from 1 to 8, inclusive, andAr is ##STR2## WHERE R is hydrogen or acyl, andR.sub.2 is hydrogen or --OR, as defined above, ##STR3## WHERE R has the meanings defined above, andR.sub.3 is hydroxy-lower alkyl, --NH--CO--R.sub.4, --NH--SO.sub.2 --R.sub.5, --CH.sub.2 --NH--CO--R.sub.4, --CH.sub.2 --NH--SO.sub.2 --R.sub.5 or --CH.sub.2 --NH--CO--NH--R.sub.4, whereR.sub.4 is hydrogen or lower alkyl, andR.sub.5 is lower alkyl or di-lower alkyl-amino, ##STR4## WHERE R.sub.6 is hydrogen, amino or hydroxyl,X is chlorine or bromine, andY is hydrogen, chlorine or bromine or ##STR5## WHERE R has the meanings defined above, andA is a saturated or unsaturated 5- to 6-membered ring,And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as bronchospasmolytics, uterine spasmolytics, antipruritics and antiallergics.
摘要:
The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.
摘要:
Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.
摘要:
Compounds of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is hydrogen, --CO--R.sub.2 or --SO.sub.2 R.sub.3,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or (alkyl of 1 to 4 carbon atoms)amino, andR.sub.3 is alkyl of 1 to 4 carbon atoms,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bronchospasmolytics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms or trifluoromethyl;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, methyl or ethyl;R.sub.5 is hydrogen, alkyl of 1 to 8 carbon atoms, phenyl-(alkyl of 1 to 8 carbon atoms), cycloalkyl of 3 to 7 carbon atoms, (alkoxy of 1 to 4 carbon atoms) carbonyl-methyl, phenyl, substituted phenyl, naphthyl or substituted naphthyl; orR.sub.4 and R.sub.5, together with each other, are alkylene of 4 to 5 carbon atoms, optionally interrupted by --O-- or --NR.sub.6 --, where R.sub.6 is alkyl of 1 to 4 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics.
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:
Racemic or optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl, orR.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy;n is an integer from 2 to 6, inclusive; andR is hydrogen, benzyl or ##STR2## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS-stimulators.
摘要翻译:其中Q为氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,三氟甲基或氨基,R 2为式Q-C n H 2n-NH-R的外消旋或旋光活性化合物 氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或三氟甲基,或R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基; n为2〜6的整数,包括0〜6; 并且R是氢,苄基或者它们的无毒的药学上可接受的酸加成盐。 化合物及其盐可用作血管扩张剂和CNS刺激剂。
摘要:
Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--RwhereinQ is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atomsor trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,n is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, R.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also--NR.sub.3 R.sub.9, whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms, or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 or 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --CONH-- or --O--CO--NH--, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS- stimulators.
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:
Compounds of the formula ##STR1## wherein R.sub.1 is halogen, hydroxyl, amino, alkyl, alkoxy or acylamido,R.sub.2 is hydrogen, hydroxyl, alkyl, alkoxy or carboxamido,R.sub.3 is hydrogen, halogen, alkyl or alkoxy,R.sub.4 is hydrogen, methyl or ethyl, andR.sub.5 and R.sub.6 are each hydrogen, halogen, alkyl, alkoxy, benzyloxy, hydroxyl, amino, cyano, carboxyl, carbalkoxy, carboxamido, alkylenecarboxamido or acylamido,Provided, however, that, when R.sub.1 is 4-hydroxyl or 4-chloro, R.sub.2 and R.sub.3 are hydrogen, R.sub.4 is methyl and R.sub.5 is halogen or 2-halo, R.sub.6 is other than 4-hydroxyl or 4-benzyloxy; and nontoxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, vasodilators, hypotensives and antiarrhythmics.