摘要:
Novel pyridone-acetic acid derivative, viz. 3,5-dichloro-4-pyridone-1-acetic acid (I) is used as an intermediate in the production of certain cephem derivatives having anti-bacterial activity against gram-negative and gram-positive bacteria. The acid (I) is prepared by methods generally known in the art, e.g. by reacting 3,5-dichloro-4-pyridone with chloracetic acid or bromoacetic acid.
摘要:
Cephem derivatives of the formula ##STR1## wherein Z is 1,4-dihydro-4-oxo-1-pyridyl or the corresponding group substituted by one or more of alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, OH, F, Cl, Br, I, NO.sub.2 and NH.sub.2 ; and R is H, --OCOCH.sub.3 or -S-Het, wherein Het is 3-methyl-1,2,4-thiadiazolyl-5, 5-methyl-1,3,4-oxadiazolyl-2, 5-hydroxymethyl-1,3,4-oxadiazolyl-2, 5-methyl-1,3,4-thiadiazolyl-2, 5-hydroxymethyl-1,3,4-thiadiazolyl-2, tetrazolyl-5, 1-methyltetrazolyl-5, 1,2,3-triazolyl-4, 4-methyl-oxazolyl-2 or 1-oxidopyridinio-2, and the readily cleavable esters thereof and the physiologically acceptable salts thereof, possess anti-bacterial activity and can be prepared by reacting a 3-CH.sub.2 R-7-amino-3-cephem-4-carboxylic acid or a functional derivative thereof with a pyridone acetic acid of the formula Z-CH.sub.2 -COOH or a functional derivative thereof.
摘要:
Novel .beta.-lactam antibiotics are compounds of the formula: ##STR1## wherein R is alkyl of up to 6 carbon atoms or, when A is oxygen, R is hydrogen; A is oxygen or --OCO--; Z is ##STR2## R.sup.1 is hydrogen, acetoxy or S-Het; Het is 1,2,3-triazol-5-yl, 1-methyltetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl; and n is an integer from 0 to 8; or a readily-cleavable ester or physiologically-acceptable salt thereof.
摘要:
New flavanone derivatives of the formula I ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each phenyl which is unsubstituted or monosubstituted to trisubstituted by OH, alkyl, alkoxy, acylamino, halogen, COOalkyl and/or NO.sub.2 and/or substituted by a methylenedioxy group, and the alkyl, alkoxy and acyl groups each have 1-7 C atoms, but wherein the HO group is only in the 6-position if at least one of the radicals Ar.sup.1 and Ar.sup.2 is substituted phenyl, and the phosphoric acid esters thereof and the salts of these compounds display antiallergic effects. Salts of the I-phosphoric acid esters with aminoglycoside antibiotics are outstandingly stable and possess advantageous kinetics of liberation.
摘要:
The invention relates to chroman derivatives of the formula I ##STR1## in which R.sup.1 is A,R.sup.2 is OA,R.sup.3 is OH,R.sup.4 is H, orR.sup.3 and R.sup.4 together are a bond,R.sup.5 is a 2-oxo-1,2-dihydro-1-pyridyl or 2-oxo-2,3-dihydro-4-pyrodyl radical which is optionally monosubstituted by A,R.sup.6 is CN,R.sup.7 and R.sup.8 are each H,Z is O, NH or a bond, andA is alkyl having 1-6 C atoms,or a physiologically acceptable salt thereof.
摘要:
Novel chroman derivatives of the formula I ##STR1## in which R.sup.1 to R.sup.10 have the meanings given in patent claim 1, and their salts show effects on the cardiovascular system and can be used for the treatment or prophylaxis of cardiac insufficiency, angina pectoris, high blood pressure, incontinence and alopecia.
摘要:
Chroman derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 have the meanings defined herein, and their salts have an effect on the cardiovascular system.
摘要:
A compound of the formula: ##STR1## where in x-y is --CO--CH.sub.2 --, --COCR.sup.10-, --CHOHCHR.sup.8-, --CH.dbd.CR.sup.8 -- or ##STR2## and R.sup.9 is various, R.sup.1 and R.sup.8 are alkyl, R.sub.2 is H or alkyl and R.sup.1 and R.sup.2 are alkylene, are disclosed as useful as intermediates for cardiovascular agents.
摘要:
New tetralin derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 and Z have the meanings indicated herein and salts thereof, exhibit an effect on the cardiovascular system.
摘要:
An azachroman derivative of the formula ##STR1## wherein Z is(a) --N.dbd.CH--CH.dbd.CH--,(b) --CH.dbd.N--CH.dbd.CH--,(c) --CH.dbd.CH--N.dbd.CH-- or(d) --CH.dbd.CH--CH.dbd.N--;R.sup.1 is A,R.sup.2 is H or A, orR.sup.1 and R.sup.2 together are alkylene with 3-6 C atoms;R.sup.3 is OH or OAc,R.sup.4 is H, orR.sup.3 and R.sup.4 together are a bond;R.sup.5 is 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl, or 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl mono- or disubstituted by A, F, Cl, Br, I, OH, OA, OAc, NO.sub.2, NH.sub.2, AcNH, HOOC or AOOC;A is C.sub.1-6 -alkyl andAc is C.sub.1-18 -alkanoyl or C.sub.7-11 -aroyl;or a pharmaceutically acceptable salt thereof is claimed. This compound exhibits vasodilatory and anti-hypertensive effects and is suitable for the treatment of alopecia.