G.d. Searle & Company

Continental Pharma Incorporated

Continental Pharma S.a.

Claude L Gillet

Joseph L Roba

Georges E Lambelin

Alexis A Cordi

William R Van Dorsser

Paul J Niebes

Philippe R Bovy

Hugo J Gorissen

Michel P Snyers

Michel Snyers

Michael F Rafferty

Romeo Roncucci

Michel R Franz

Bevyn Jarrott

Philip Mark Beart

Robert G Cavalier

Philippe M Janssens De Varebeke

Alexis H Cordi

Nguyen Phuc Buu-Hoi

Mark A Martens

Romeo R Roncucci

Piedad Calderon

Guy D Jacques

Albert Lenaers

Alex A Cordi

A class of .omega.-amino-.alpha.-phenylalkanonitrile derivatives is described having use in treatment of cardiovascular dysfunctions such as hypertension. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is methoxy, R.sub.3 is hydrido, R.sub.4 is isopropyl, R.sub.5 is methyl and R.sub.6 is selected from linear alkyl, phenylpropyl, phenylbutyl and phenylpentyl.

.omega.-amino-.alpha.-phenylalkanonitrile derivatives

Use of heterocyclic amino-alcohol compounds for treatment of CNS diseases

A class of glycyl urea derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of interest are those of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group independently selected from hydrido, alkyl, aralkyl, aryloxyalkyl and arylthioalkyl, any one of which groups having a substitutable position may be substituted with one or more radicals selected from halo, alkyl of one to about ten carbon atoms, alkenyl of two to about ten carbon atoms, alkynyl of two to about ten carbon atoms, haloalkyl, alkoxy, alkylthio, alkylsulfinyl and alkylsulfonyl; or a pharmaceutically-acceptable salt thereof; with the proviso that when each of R.sup.1 and R.sup.2 is ethyl, then R.sup.3 and R.sup.4 cannot be hydrido simultaneously.

Glycyl urea derivatives as anti-convulsants

A class of diphenylmethylaminoacetamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is independently selected from hydrido and halo; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.

Diphenylmethylaminoacetamide derivatives as anti-convulsants

A class of tricyclic glycinamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is hydrido; wherein Z is selected from methylene, ethylene, ethenylene, thiomethylene and thioethylene; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.

Tricyclic glycinamide derivatives as anti-convulsants

The invention relates to spirohydantoins of the formula I ##STR1## where R.sub.1 and R.sub.2 are defined hereinbelow. Also disclosed are methods of preparation, pharmaceutical compositions containing at least one of these compounds, and methods of using said compounds for treatment and prevention of complications of diabetes and galactosemia.

Spiro-hydantoins as aldose reductase inhibitors

A compound of the formula: ##STR1## wherein X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2, whether or not identical are hydrogen, a halogen such as fluoro, chloro or bromo, linear or branched alkyl of 1 to 3 carbon atoms, linear or branched alkoxy of 1 to 3 carbon atoms, carboxy, alkoxy-carbonyl of 1 to 3 carbon atoms or phenyl;

.alpha..sub.2 -blocking derivatives of imidazole

A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,

Derivatives of glycinamide, their preparation and their use

This invention relates to heterocyclic amino-alcohol derivatives of the formula ##STR1## These compounds are useful as antihypertensives.

Heterocyclic amino-alcohol derivatives

2-Pentanoylaminoacetic acid and pharmaceutically suitable salts thereof are claimed for use as pharmaceuticals. The compounds are useful in producing an effect on the central nervous system, especially in the treatment of various forms of epilepsy, of disninesiae, of parkinsonism, of memory troubles, of psychic troubles and of cerebral anoxia.

Derivatives of 2-aminoacetic acid

The new amino-alcohol derivatives according to the invention have the formula: ##STR1## wherein: (a) R.sub.1 is hydrogen, an alkylthio C.sub.1 -C.sub.5 radical, a cycloalkylthio C.sub.5 -C.sub.6 radical, an alkoxy C.sub.1 -C.sub.5 radical, a cycloalkyloxy C.sub.5 -C.sub.6 radical, an alkyl C.sub.1 -C.sub.5 radical, a cycloalkyl C.sub.5 -C.sub.6 radical or a halogen atom;

Amino-alcohol derivatives

A derivative of benzimidazole of the general formula I: ##STR1## wherein: R.sub.1 represents a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7,C.sub.8,C.sub.9,C. sub.10,C.sub.11,C.sub.12,C.sub.13,C.sub.14,C.sub.15, C.sub.16,C.sub.17 or C.sub.18, a cycloalkyl radical C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7 or C.sub.8, a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4 or C.sub.5 substituted by one or more radicals selected from the group comprising:

Benzimidazole derivatives, their use, and compositions containing these

Amino-alcohols of the formula ##STR1## wherein R.sub.1 represents either a linear or branched chain alkyl radical having 1 to 4 carbon atoms, or a cycloalkyl radical having 5 or 6 carbon atoms; R.sub.2 represents a lower alkyl radical having 1 or 2 carbon atoms; R.sub.3 represents a linear or branched chain alkyl radical having 3 to 10 carbon atoms which radical is optionally substituted by phenyl; R.sub.4 represents hydrogen, or, together with R.sub.3 and the adjacent nitrogen atom, a heterocyclic nucleus of the piperidine type and the corresponding non-toxic salts of said amino-alcohols; preparation of the above and their use as antispasmodic, peripheral vasodilatory and anti-hypertensive agents and as an agent having a protective activity against anoxia of the myocardium.

Alkyl and cycloalkylthiophenylalkylaminoalkanols, their salts and the

The new amino-alcohols according to the invention are represented by the formula ##SPC1## Wherein: R.sub.1 represents a RS, RSO or RSO.sub.2 group in which R is a linear or branched alkyl group (C.sub.1 -C.sub.10), an acetyl radical or hydrogen; R.sub.2 and R.sub.3, which may be identical or different, represent a halogen atom or an alkyl (C.sub.1 -C.sub.3), amino, alkylamino (C.sub.1 -C.sub.4), acylamino, nitro, carboxy, carbalkoxy, trifluoromethyl, alkoxy (C.sub.1 -C.sub.4) or alkylthio (C.sub.1 -C.sub.4) radical; R.sub.4 represents hydrogen or a linear or branched alkyl radical containing 1 - 4 carbon atoms; R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen, a substituted or not, linear or branched alkyl (C.sub.1 -C.sub.16) radical, a cycloalkyl (C.sub.5 -C.sub.6) radical, an alkynyl (C.sub.3 -C.sub.4) radical, an alkenyl (C.sub.3 -C.sub.4) radical or a heterocycle of the kind piperidine, morpholine, pyridine or pyridimine, R.sub.5 and R.sub.6 can also form with adjacent nitrogen atom a heterocyclic radical, substituted or not; one of said R.sub.2 and R.sub.3 can be a hydrogen atom or can be both a hydrogen atom provided that simultaneously R is a lower alkyl (C.sub.1 -C.sub.3) radical in the group RS, R.sub.4 and R.sub.5 are hydrogen atoms and R.sub.6 is an isopropyl or t-butyl radical or if simultaneously R is a methyl radical in the group RSO.sub.2, R.sub.4 and R.sub.5 are hydrogen atoms and R.sub.6 is an isopropyl radical. When R.sub.5 and R.sub.6 represent an alkyl, the latter can be substituted by amino, alkylamino, hydroxy, alkoxy, phenoxy, substituted phenoxy, phenyl, substituted phenyl radical or a heterocycle such as piperidino or morpholino.

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Blanmont, Belgium

Claude L Gillet