Hypocholesterolemic sugar-substituted 2-azetidinone compounds of the formula: are disclosed, as well as a method of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a sugar-substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents

Use of a compound selected from: pyridoxal-5'-phosphate, pyridoxal, pyridoxamine, 3-acylated pyridoxal analogues, pharmaceutically acceptable acid addition salts thereof, and mixtures thereof, in the preparation of a medicament for the treatment of cardiovascular and related diseases in a mammal undergoing concurrent treatment with an angiotensin II receptor antagonist. The cardiovascular and related diseases include ischemia, congestive heart failure, hypertrophy, ischemia reperfusion injury, and myocardial ischemia reperfusion injury.

Treatment of cardiovascular and related pathologies

A method of treating a cerebrovascular disease, particularly stroke, is described. A method of treating a cerebrovascular disease includes administering pyridoxal-5'-phosphate, pyridoxal, pyridoxine, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, or pharmaceutical compositions thereof.

Treatment of cerebrovascular disease

Disclosed is a composition, therapeutic combination and methods including: (a) at least one sterol absorption inhibitor and (b) at least one cardiovascular agent different from the sterol absorption inhibitor wherein at least one sterol absorption inhibitor is represented by formula I, which can be useful for treating vascular conditions, obesity, diabetes and lowering plasma levels of sterols.

Combinations of sterol absorption inhibitor(s) with cardiovascular agent(s) for the treatment of vascular conditions

The present invention provides methods for the treatment of obesity using sterol or 5α-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5α-stanol absorption inhibitors and at least one obesity control medication.

Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors

Trifluoromethylthiophenylethylamine derivatives, made from the corresponding acid chlorides by successive reduction, condensation with nitroethane, reduction, and condensation with an amine, possess anorexigenic properties, unaccompanied by central stimulant activity or cardiovascular effects.

1-(3'-Trifluoromethylthiophenyl)-2-ethylaminopropane pharmaceutical composition and method for treating obesity

The invention provides vincaminic acid esters of formula ##SPC1## Wherein R1 is hydrogen or hydroxy, R2 is hydrogen or R1 and R2 form an additional bond between the two carbon atoms to which they are attached, and R3, R4 and R5 are hydrogen or methyl, and their salts. The esters are useful in treatment of cardiac-circulatory, cerebal-vascular or respiratory insufficiency.

Vincaminic acid esters

Naphthyridine derivs. of formula (I), as racemates or optical isomers, and their suitable salts with acids are new. In (I) R1=H, 1-4C alkyl, 2-oxopropyl, 2-hydroxypropyl, 3-oxobutyl, 3-hydroxybutyl, cyclopropyl methyl, benzyl (opt. halogenated esp. by F or Cl), acetyl, cyclopropylcarbonyl, benzoyl or (CH2)nR1. R2=H, halo, CH3 or CH3O. R6=H or COR7. R3=CH3 or C2H5, and R4=OH or H and R5=H, or R3+R4=oxo and R5=H, or R3=CH3 or C2H5 and R4+R5=an additional C-C bond. n=1 or 2. R1=(m)ethoxycarbonyl or CN. R7=OH, 1-4C alkoxy, NH2(opt. substd. by 1 or 2 CH3 or by one cyclopropyl). The following cpds. are excluded: R3+R4=oxo; (a) R1=H=R6 and R2=10-CH3O and (b) R1=R2=R6=H; but when R6=alkoxycarbonyl stereoisomers are included. Dose is 10-100 mg/day. In an example methyl 1,2,3,3a,4,5,-hexahydro-3-methyl-6-oxo-6H-indolo 3,2,1-de 1,5 naphthyridine-4-carboxylate was prepd. fron Nb-methyltryptamine and diethyl alpha-formyl succinate.

Indolo-(1,5)-naphthyridine derivs. - having antianoxia and psychotropic activities

The invention provides compound of formula WHEREIN R1 is alkyl or substituted or unsubstituted phenyl or 3-pyridyl, and R2 is hydrogen, halogen, alkoxy or trifluoromethyl, methoxy or methylthio. The compounds are useful as analgesic agents.

2-(4-M-CF{HD 3 {B or -SCF{HD 3 {B phenylpiperazino)-ethyl benzoates

Compounds of the general formula ##SPC1## Wherein R 1 is H or OH and R 2 is H or R 1 and R 2 together represent an additional double bond between the two carbon atoms to which they are attached and m and n are integers of 1 to 5 and 2 to 7 respectively; and pharmaceutically acceptable acid addition salts thereof. The compounds are useful for the treatment of vascular disorders in mammals.

Don Pierre Rene Luc Giudicelli

Papers

1-(3'-Trifluoromethylthiophenyl)-2-ethylaminopropane pharmaceutical composition and method for treating obesity

Vincaminic acid esters

Indolo-(1,5)-naphthyridine derivs. - having antianoxia and psychotropic activities

2-(4-M-CF{HD 3 {B or -SCF{HD 3 {B phenylpiperazino)-ethyl benzoates

Vinvamine series cycloalkyl-alkyl esters