Patents Represented by Attorney Bernard S. Leon
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Patent number: 4732979Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: January 21, 1987Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4732902Abstract: The invention relates to long-acting depot producing antipsychotic pyrroloisoquinolinyl-dimethyloxoalkyl alkanoates of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R.sub.3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoxyhydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R.sub.4 is alkyl; and n is the integer 2 or 3,their corresponding optical isomers, geometric isomers, and mixtures thereof, and the pharmaceutically acceptable acid additional salts.The compounds of formula I are useful as antipsychotic agents.Type: GrantFiled: May 23, 1986Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Gary L. Olson
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Patent number: 4732753Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.Type: GrantFiled: February 11, 1985Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Walter Fuller
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Patent number: 4731373Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.Type: GrantFiled: December 10, 1984Date of Patent: March 15, 1988Assignee: Hoffman-La Roche Inc.Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
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Patent number: 4731363Abstract: The present disclosure relates to the use of thromboxane synthase inhibitors as antiobesity agents and insulin lowering agents. Such compounds fall into a variety of classes among which are 1-substituted imidazoles, 4-substituted imidazoles, 3-substituted pyridines, 3-substituted indoles, 4-substituted pyrimidines, 5-substituted tetrazoles, pyrazolidines, quinazolines, and substituted xanthene carboxylic acids.Type: GrantFiled: January 16, 1986Date of Patent: March 15, 1988Assignee: Hoffmann-La Roche Inc.Inventors: James G. Hamilton, Ann C. Sullivan, Lawrence D. Tobias, Joseph Triscari
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Patent number: 4729903Abstract: The invention relates to a process for depositing I-125 on a substrate which comprises contacting a predetermined surface area of substrate with Xe-125 gas, whereby the Xe-125 decays to I-125 and the I-125 in turn deposits as a solid on the surface of the substrate, the contact being for a time sufficient to deposit at least about 1 microcurie of I-125. I-125 is thereby deposited in a relatively uniform amount over the surface area of the substrate. The substrate is then assayed to determine how much I-125 has been deposited. The substrate is then divided into pieces of measured surface area, each piece therefore containing a measured amount of deposited I-125, and each piece can then be used in the manufacture of an I-125 source.Type: GrantFiled: June 10, 1986Date of Patent: March 8, 1988Assignee: Midi-Physics, Inc.Inventors: James J. McGovern, Joseph M. Olynyk
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Patent number: 4725554Abstract: Method for measuring the coagulation time of a blood sample in which a sample-reagent mixture is formed by introducing the sample and at least one reagent into a cuvette. To reduce the operating and material costs, the sample-reagent mixture is so moved in a stationary cuvette that the mixture flows back and forth around an edge projecting into the cuvette, whereby a clot forms on this edge.Type: GrantFiled: December 5, 1986Date of Patent: February 16, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Kurt Schildknecht
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Patent number: 4721137Abstract: An apparatus for withdrawing liquid from a receptacle which is closed with a penetrable cover, which comprises a puncturing tool for creating an aperture in the receptacle cover, a cannula for entering the receptacle through the aperture and withdrawing liquid from the receptacle, a holding arm to which the puncturing tool and cannula are affixed in parallel and at a certain distance apart, and a motor drive for effecting horizontal and vertical movements of the holding arm relative to the covered receptacle to align, lower and raise the puncturing tool and cannula in succession through the cover.Type: GrantFiled: October 7, 1986Date of Patent: January 26, 1988Assignee: Kontron Holding A.G.Inventor: Paul Muller
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Patent number: 4720546Abstract: The compounds of the formula ##STR1## wherein one of the symbols Q and Q' is the group --CH.dbd. and the other is the group --CH.dbd. or --N.dbd., R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or halogen and n is the integer 0, 1 or 2, and their pharmaceutically acceptable acid addition salts, which have valuable antimycotic properties and can be used for the control of infections caused by pathogenic fungi, are described.Type: GrantFiled: November 4, 1986Date of Patent: January 19, 1988Assignee: Hoffman-La Roche Inc.Inventors: Ivan Kompis, Ekkehard Weiss
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Patent number: 4718762Abstract: A two-beam spectrophotometer comprising a monochromator and a beam splitter is provided. In addition to being inclined to the optical axis by an angle .alpha./2 lying in the optical plane, the beam splitter is inclined to the direction perpendicular to the optical plane, so that the reference beam is deflected out of the optical plane by an angle .beta.. This improves the spectral intensity distribution.A spectrophotometric method employing this apparatus is also provided.Type: GrantFiled: August 19, 1986Date of Patent: January 12, 1988Assignee: Kontron Holding A.G.Inventors: Peter Wiget, Robert Wolf
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Patent number: 4716227Abstract: Cephalosporin esters of the formula ##STR1## wherein R.sup.2 is hydrogen or acyl and R.sup.1 is a group which is readily removable by hydrolysis,and pharmaceutically acceptable acid addition salts of basic compounds of formula I in which R.sup.2 is an acyl group, may be prepared by reacting 7-amino-3-methyl-3-cephem-4-carboxylic acid (7-ADCA) in a partially chlorinated lower alkane with a bicyclic amidine of the formula ##STR2## wherein n is the integer 3, 4 or 5, and a halide of the formulaX--R.sup.1 IIIwherein X is halogen and R.sup.1 has the above significance,if desired, treating the resulting compound of formula I in which R.sup.2 is hydrogen with an unprotected or optionally protected acylating agent, cleaving off a protecting group which may be present and, if desired, treating a resulting basic compound of formula I in which R.sup.2 is an acyl group into a pharmaceutically acceptable acid addition salt.Type: GrantFiled: November 7, 1985Date of Patent: December 29, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Andre Furlenmeier
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Patent number: 4711889Abstract: The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,R.sup.2 is hydrogen or lower alkyl,one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond,A is lower alkylene,R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.Type: GrantFiled: July 18, 1986Date of Patent: December 8, 1987Assignee: Hoffman-La Roche Inc.Inventors: Urs Brombacher, Helmut Link, Marc Montavon
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Patent number: 4708441Abstract: Compounds of the formula ##STR1## wherein X.sup.2 is a single covalent bond or --COO--; X.sup.1 is a single covalent bond, --COO--, --CH.sub.2 CH.sub.2 -- or when X.sup.2 is --COO--, X.sup.1 also can be p--C.sub.6 H.sub.4 --, p--C.sub.6 H.sub.4 --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --p--C.sub.6 H.sub.4, p--C.sub.6 H.sub.4 --COO-- or --COO--p--C.sub.6 H.sub.4 ; ring A is a benzene ring or trans-1,4-cyclohexylene; ring B is a benzene ring or when X.sup.2 is --COO-- and X.sup.1 is a single covalent bond, --COO-- or --CH.sub.2 CH.sub.2 --, ring B also can be trans-1,4-cyclohexylene; Z.sup.1, Z.sup.2 and Z.sup.3 individually are hydrogen or when positioned on a benzene ring which is not linked directly with a further ring via a single covalent bond, Z.sup.1, Z.sup.2 and Z.sup.3 also can be halogen, cyano or methyl; Y.sup.2 is cyano, nitro, 2,2-dicyanovinyl or when Y.sup.1 is hydrogen Y.sup.2 also can be 2,2-dicyano-1-methylvinyl; Y.sup.1 is halogen, cyano, C.sub.1 -C.sub.3 -alkyl or, when X.sup.Type: GrantFiled: August 16, 1985Date of Patent: November 24, 1987Assignee: Hoffman-La Roche Inc.Inventors: Martin Petrzilka, Martin Schadt, Alois Villiger
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Patent number: 4709030Abstract: Liquid crystalline mixtures containing compounds of the formula ##STR1## wherein n stands for the number 0 or 1; X.sup.1 and X.sup.2 denote single covalent bonds or one of the symbols X.sup.1 and X.sup.2 also denotes --COO--, --OOC-- or --CH.sub.2 CH.sub.2 --; the rings A.sup.1, A.sup.2 and A.sup.3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; R.sup.1 signifies 4-alkenyl or on a cyclohexyl ring also 2Z-alkenyl; and R.sup.2 denotes alkyl, alkoxy, --CN or --NCS,as well as the manufacture of these compounds and the use for electro-optical purposes are described.Type: GrantFiled: July 11, 1986Date of Patent: November 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Martin Petrzilka, Martin Schadt
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Patent number: 4707555Abstract: New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.Type: GrantFiled: July 12, 1985Date of Patent: November 17, 1987Assignee: Hoffmann-La Roche Inc.Inventors: David L. Coffen, George W. Holland, W. Harry Mandeville, Perry Rosen, Frederick Wong
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Patent number: 4707484Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or acyl; R.sub.2 and R.sub.3 independently are lower alkyl, aralkyl or alkenyl or R.sub.2 and R.sub.3 together form a ring of 5 to 8 carbon atoms; R.sub.4 is phenyl, substituted phenyl, cyclohexyl, substituted cyclohexyl, cyclopentyl, substituted cyclopentyl, cycloheptyl, or substituted cycloheptyl; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is hydrogen, lower alkyl or acyl; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I and pharmaceutically acceptable acid addition salts thereof are anti-emetic agents which lack central nervous system side effects.Type: GrantFiled: November 25, 1986Date of Patent: November 17, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Wallace M. Dairman, Thomas F. Mowles, Gary L. Olson
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Patent number: 4704005Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently straight-chain C.sub.1 -C.sub.12 -alkyl or when positioned on an aromatic ring R.sup.1 and R.sup.2 may also independently be straight-chain C.sub.1 -C.sub.12 -alkoxy, or one of R.sup.1 and R.sup.2 may also be a group of the formula: ##STR2## X.sup.1 and X.sup.2 are independently single covalent bonds or one of X.sup.1 and X.sup.2 may also be --CH.sub.2 CH.sub.2 --; rings A.sup.1 and A.sup.2 are independently 1,4-phenylene or, when X.sup.1 or X.sup.2 is --CH.sub.2 CH.sub.2 --, rings A.sup.1 and A.sup.2 may also independently be trans-1,4-cyclohexylene; and R.sup.3 is straight-chain C.sub.1 -C.sub.12 -alkyl or when positioned on an aromatic ring R.sup.3 may also be straight-chain C.sub.1 -C.sub.12 -alkoxy. Their manufacture and use in liquid crystalline mixtures are described.Type: GrantFiled: October 14, 1983Date of Patent: November 3, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Arthur Boller, Martin Petrzilka, Martin Schadt
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Patent number: 4699986Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.Type: GrantFiled: August 26, 1985Date of Patent: October 13, 1987Assignee: Hofmann-La Roche Inc.Inventors: Christian N. Hubschwerlen, Gerard Schmid
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Patent number: 4700009Abstract: The present disclosure is concerned with a novel process for the manufacture of substituted benzaldehydes, namely of benzaldehydes of the formula ##STR1## wherein R represents a methoxy or tert.butyl group. The compounds of formula I are known substances, useful as, e.g. intermediates.Type: GrantFiled: January 28, 1986Date of Patent: October 13, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Nosberger, Paul
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Patent number: 4696921Abstract: Mixtures of active substances and pharmaceutical compositions useful in malaria therapy comprising a quinolinemethanol derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, fluorine, chlorine, bromine, methyl or trifluoromethyl, R.sup.2 is hydrogen, fluorine, chlorine, bromine, methyl or methoxy (at least one of R.sup.1 and R.sup.2 is other than hydrogen), and R.sup.3 is C.sub.1-6 -alkylamino-C.sub.1-3 -alkyl, di-C.sub.1-6 -alkylamino-C.sub.1-3 -alkyl, 2-piperidyl or 3-piperidyl, or a pharmaceutically acceptable acid addition salt thereof; a compound which acts as a p-aminobenzoic acid antagonist; and a compound which acts as a dihydrofolic acid reductase inhibitor, are described.Type: GrantFiled: November 7, 1983Date of Patent: September 29, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Bernhard Merkli