Patents Represented by Attorney Jon S. Saxe
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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: 4719238Abstract: 1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(alpha-methylstyryl)naphthalene possesses antikeratinizing, antiinflammatory and immunomodulatory properties and can be used in the treatment or prevention of dermatoses which are accompanied by a pathological cornification as well as inflammatory, autoimmune, rheumatic and allergic illnesses.Type: GrantFiled: June 1, 1987Date of Patent: January 12, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Werner Bollag
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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: 4716219Abstract: Adsorbents, which are suitable for the affinity chromatography of proteins, especially of interferons, and which consist of an electroneutral carrier matrix, --O--CH.sub.2 --CH(OH)--CH.sub.2 --NH- groups as the spacer and a triazine coloring substance bonded to the spacer.Type: GrantFiled: January 23, 1986Date of Patent: December 29, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Bernhard Eggimann, Erich Hochuli, Alfred Schacher
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Patent number: 4716148Abstract: A new biological polypeptide hormone has been isolated from mammalian thymus and has been given the designation prothymosin alpha. This peptide contains approximately 107 to 113 amino acid residues depending on species and is distinguished by having the thymosin alpha.sub.1 sequence at its amino-terminus. Prothymosin alpha appears to represent the native polypeptide from which thymosin alpha.sub.1, thymosin alpha.sub.11 and other fragments are generated during the isolation of thymosin fraction 5. Prothymosin alpha is one of several peptides isolated from the thymic tissue which participate in the regulation, differentiation and function of thymic dependent lymphocytes (T cells). The new peptide appears to be more potent on a weight basis than thymosin alpha.sub.1 in the protection of subject animals against opportunistic infections.Type: GrantFiled: November 18, 1986Date of Patent: December 29, 1987Assignee: Hoffman-La Roche Inc.Inventor: Bernard L. Horecker
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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: 4709055Abstract: There is described a novel process for producing hydroquinone derivatives of the formula ##STR1## wherein R is an ether protecting group, and their conversion into d-.alpha.-tocopherol, starting from compounds of the formula ##STR2## wherein R is an ether protecting group and R.sup.1 is hydrogen or an ether protecting group.Type: GrantFiled: January 13, 1986Date of Patent: November 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Richard Barner, Josef Hubscher
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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: 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: 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: 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: 4701540Abstract: A process for producing cycloketones of a 5 or 6 carbon chain length through which said ketones are known intermediates for producing carotenoids.Type: GrantFiled: March 12, 1984Date of Patent: October 20, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Teodor Lukac, Milan Soukup, Erich Widmer
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Patent number: 4699652Abstract: The invention is directed to fungicidal pyridine derivatives and their N-amino salts and acid addition salts, said pyridine derivatives having the formula ##STR1## wherein R is mono-, di- or trisubstituted phenyl, wherein the substituents are the same or different and are selected from the group consisting of 1 to 3 halogen, 1 or 2 C.sub.1-3 -alkyl, 1 or 2 C.sub.1-3 -alkoxy and 1 or 2 trifluoromethyl moieties; R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl; R.sup.2 is hydrogen; R.sup.3 is selected from the group consisting of --CO--R.sup.4, --C(OR.sup.5).dbd.CHR.sup.6, --CH(R.sup.4)OR.sup.5, --C(R.sup.4).dbd.NOR.sup.7 and ##STR2## R.sup.4 is hydrogen or C.sub.1-5 -alkyl; R.sup.5 is C.sub.1-4 -alkyl; R.sup.6 and R.sup.7 are hydrogen or C.sub.1-4 -alkyl; n is 2 or 3; or R.sup.2 taken together with R.sup.4 is equal to the group --CH.dbd.Type: GrantFiled: July 14, 1986Date of Patent: October 13, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Beat Zehnder
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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: 4698315Abstract: A method for determining total digoxin levels in a biological fluid sample containing digoxin-protein complex which method comprises disrupting the digoxin-protein complex by treating said sample solution with an effective amount of a dissociation agent selected from one or more members of the group consisting of a C.sub.3 -C.sub.26 saturated or unsaturated fatty acid, a C.sub.2-7 lower alkanol, quinidine and .alpha.-tocopherol so as to release the bound digoxin from serum protein, passing the treated sample solution through a centrifugal ultrafilter so as to selectively pass digoxin containing sample solution through said filter and retaining said serum proteins and determining the digoxin contents in said sample solution in a fluorescence polarization assay. A kit for carrying out the method is provided.Type: GrantFiled: April 22, 1985Date of Patent: October 6, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Bruce C. Farrenkopf, Richard A. Kaufman
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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