Abstract: 7-Substituted lower alkyl hept-6-enoates and 4-hydroxytetrahydropyran-2-ones bearing 6-olefinic substituents (e.g.,) ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enoates are prepared by a multi-step process. The process involves 3-protected-lower alkyl 3,5-dihydroxy-hept-6-enoates, which are obtained by cleaving corresponding 6.alpha.-vinyl-4.beta.-protected hydroxy-tetrahydro 2H-pyran-2-ones. The final products are useful as anti hypercholesteremic agents.
Type:
Grant
Filed:
July 26, 1985
Date of Patent:
June 30, 1987
Assignee:
Sandoz Pharmaceuticals Corp.
Inventors:
Charles F. Jewell, Jr., James R. Wareing
Abstract: A compound of formula I ##STR1## wherein R.sub.1 represents ethyl or vinyl andR.sub.2 represents a five membered saturated heterocycle or aminoalkyl unsubstituted or substituted in its alkyl moiety by hydroxy,in free or in the form of an acid addition or quaternary salt, which compounds are indicated for use as chemotherapeutic agents e.g. as anti-bacterially active antibiotics and as veterinary agents e.g. in combatting microorganism infections and promoting growth in domestic animals.
Abstract: 7-Substituted lower alkyl hept-6-enoates and 4-hydroxy-tetrahydropyran-2-ones bearing 6-olefinic substituents (E), (Z), ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enates are prepared by a multi-step process involving lower alkyl 3,5-dihydroxy-hept-6-enates. The final products are useful as anti hypercholesteremic agents.
Type:
Grant
Filed:
July 26, 1985
Date of Patent:
March 17, 1987
Assignee:
Sandoz Corp.
Inventors:
Charles F. Jewell, Jr., James R. Wareing
Abstract: 6-trans-indol-2-yl-ethenyl)-4-hydroxy-tetrahydro-2H-pyran-2-ones of formula I are obtained by a multi-step reaction involving the procedure: ##STR1## wherein p.sup.1 is trisubstituted silyl protective group, and Z is a 2-indolyl radical which may be bear at the 4, 5, 6 and 7-positions up to two substituents such as alkyl, alkoxy, halo and CF.sub.3, and at either one the 1 or 3-positions a substituted or unsubstituted phenyl; and at the other an assymetric alkyl, cycloalkyl or aralkyl radical. Compounds I, e.g. (E)-trans-6-[1'-methyl-3'-(4"-fluorophenyl)indol-2'-ylethenyl]3,4,5,6 -tetrahydro-4-hydroxy-2H-pyran-2-one(4R,6S); are useful as anti-atheroselerotic agents.
Type:
Grant
Filed:
December 21, 1983
Date of Patent:
November 25, 1986
Assignee:
Sandoz Pharm. Corp.
Inventors:
Charles F. Jewell, Jr., James R. Wareing
Abstract: Compounds of the formula I: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 is, independently, (a) alkyl having from 1 to 22 carbon atoms; or(b) of the formula ##STR2## in which m is 0, 1 or 2, and each of R' and R" is independently a hydrogen atom, alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, or halo having an atomic weight of from about 19 to 127; and R is of an aralkyl-, phenyl- tryptophanyl- or benzocycloalkyl-type, are obtained by hydrogenating corresponding .alpha.-.beta. ethylenically-unsaturated analogs (II), which in turn are obtained by hydrogenating corresponding .alpha.-.beta. acetylenically-unsaturated analogs. Compounds I and II are useful as anti-atheroslerotic agents.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are alkyl or aryl groups, A, B, C and D are non-reactive substituents or two are joined to form an additional ring, and Z is either of the formula Z': ##STR2## wherein R.sup.4 is H, lower alkyl or a cation; or a -6-oxotetrahydropyran-2-yl ring of the formula Z": ##STR3## e.g. 4-hydroxy-6-{2-[2-(methyldiphenylsilyl)phenyl]ethenyl]ethyenyl}-tetrahydro -2H-pyran-2-one, (trans, trans). The compounds inhibit cholesterol biosynthesis and are useful as anti-atherosclerotic agents.
Abstract: 6-Substituted-4-hydroxy-tetrahydropyran-2-ones, useful as anti-atherosclerotic agents, are obtainable by the process of the invention. The 6-substituents have a phenyl, naphthyl, tetrahydronaphthyl or indolyl nucleus bound through an ethenyl unit. The invention includes novel intermediates.
Abstract: De-acylation of Penicillins and Cephalosporins to obtain the corresponding 6-aminopenicillanic acid or 7-aminocephalosporanic acid by the imino halide/imino ether process using long chain bases.
Type:
Grant
Filed:
August 3, 1983
Date of Patent:
December 31, 1985
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Bernhard C. Prager, Peter Punk, Heinrich Thaler
Abstract: A process for the preparation of condensed triazoles of formula I ##STR1## in which R together with the triazole group form an aromatic group R.sub.1 is hydrogen or a hydrocarbon groupthe process comprisingreacting in a medium containing an organic phase a compound of formula II ##STR2## with a nitrite and an acid. The reaction is preferably carried out at a raised temperature.
Abstract: The invention provides a method of facilitating vegetation with the aid of a fungal mycelium biomass in admixture with a polybutadiene and application forms comprising such components.
Abstract: Single enanitiomers of 6-(2-hydrocarbyl-substituted ethenyl)-bearing, 4-hydroxy tetrahydro-2H-pyran-2-ones, e.g., 6.alpha.-[2-(2-methyl-1-naphthyl)ethenyl]-3,4,5,6-tetrahydro-4.beta.-hydro xy-2H-pyran-2-one (4R,6S) are obtained by a multi-step process which includes protecting and deprotecting hydroxy groups at various stages.
Abstract: The invention provides a method of converting ethylenically unsaturated units of an olefinic substrate to corresponding cyclopropanyl units, comprising treating the olefinic substrate, in an ether medium, with zinc and diiodomethane and a catalytic amount of a metallo-hydride reducing agent. Preferred substrates are olefinic fatty acids or their functional derivatives, e.g. oleic acid esters.
Abstract: Asymmetrical phosphate esters of formula I ##STR1## in which R is C.sub.1-20 alkyl,R.sub.1 is C.sub.1-20 alkyl,R.sub.2 is hydrogen or methylx is 1-15and M is hydrogen, an alkali metal ion or an equivalent of an alkali earth metal or zinc ionare effective inhibitors of oxidative corrosion of metals in the presence of electrolytes. They may be used alone or in conjunction with further additives, and are preferably dissolved in the electrolyte with which the metal is to come in contact.
Type:
Grant
Filed:
March 10, 1983
Date of Patent:
August 14, 1984
Assignee:
Sandoz Ltd.
Inventors:
Bernard Danner, Hartmut Mau, Hans Stettler
Abstract: The compounds are secondary amides of the formulaA--C.tbd.CO--NH--BwhereinA is alkyl, a mono- or poly-ethylenically unsaturated acyclic hydrocarbon chain, or a hydrocarbon chain having from 1 to 4 cyclopropanyl units thereon; andB is a radical which may be of the phenyl, benzyl, phenylalkyl, benzocycloalkyl or indol- type, e.g., N-[1-phenyl-2-(p-methylphenyl)-ethyl]-oct-2-ynoylamide.The compounds are useful as pharmaceutical agents.
Abstract: Ethylenically unsaturated fatty acid amides of tryptophan derivatives e.g. .alpha.-[1-oxo-9-octadecenylamino)]-1H-indole-3-propanoic acid, ethyl ester, are useful as pharmaceutical agents and are obtainable by reacting a mixed anhydride of a long chain unsaturated carboxylic acid with an appropriate tryptophan ester.
Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are defined in the text, are useful as light stabilizers for polymeric materials, particularly for thermoplastic polymers and automotive finishes. Preferred compounds are those in which R.sub.1 is hydrogen and R.sub.2 and R.sub.3 are identical (C.sub.8-17 alkyl)carbonyl groups.
Type:
Grant
Filed:
January 22, 1982
Date of Patent:
April 3, 1984
Assignee:
Sandoz Ltd.
Inventors:
Hans Hinsken, Wolfgang Mueller, Hermann Schneider
Abstract: 7-[(Carboxymethoximino)-1H-pyrazol-3yl-acetyl]amino-3-desacetoxy-3-(1-methy l-1H-tetrazol-5yl-thio)cephalosporanic acid and salts and solvates thereof which possess chemotherapeutical in particular antibiotic activity.
Abstract: Sulfur and silicon-containing amides, e.g. N-5-sila-3-thia-5,5-dimethyl-pentadecanoyl-1-phenyl-2-(4-methylphenyl)-eth ylamine, are useful as anti-atherosclerotic agents. The amides are obtainable by acylation of a primary amine (the substituents on the amine being of the aralkyl phenyl, tryptophanyl, benzocycloalkyl-type) with a corresponding sulfur and silicon-containing carboxylic acid (or active form thereof).