Patents Represented by Attorney William H. Epstein
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Patent number: 6284785Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.Type: GrantFiled: March 24, 2000Date of Patent: September 4, 2001Assignee: Hoffmann- La Roche Inc.Inventors: Vincent Mutel, Eric Vieira, Jürgen Wichmann
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Patent number: 6281353Abstract: The present invention relates to a process for manufacturing diazepine derivatives of the general formula I wherein R1 is lower alkyl and R2 is hydrogen, or R1 and R2 are together —(CH2)n— and n is 2 or 3; R3 is halogen, lower alkyl, lower alkoxy and m is 0, 1 or 2; R4 is hydrogen or lower alkyl. The compounds of general formula I are valuable intermediate products for the manufacture of imidazo [1,5-a][1,4]diazepine derivatives, like for instance 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazepin-6-one, which diazepine derivatives show excellent psychopharmacological properties as agonists of the central benzodiazepine receptors.Type: GrantFiled: May 8, 2000Date of Patent: August 28, 2001Assignee: Hoffmann-la Roche Inc.Inventor: Fabienne Hoffmann-Emery
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Patent number: 6281363Abstract: Hydrazine derivatives and their pharmaceutically acceptable salts useful for the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumors, cachexia, cardiovascular disease, fever, hemorrhage, and sepsis.Type: GrantFiled: December 9, 1999Date of Patent: August 28, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6277997Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.Type: GrantFiled: October 20, 2000Date of Patent: August 21, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michelangelo Scalone, Ulrich Zutter
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Patent number: 6274734Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: wherein R1, R2, R3 each independently represent hydrogen, C1-7-alkyl, or C1-7-alkoxy, A signifies —CN, a carbanionic R4-alkynyl residue, in which R4 is hydrogen or C1-7-alkyl, or a carbanionic residue of the malonic acid derivative of formula III in which B and B′ independently represent —CN, —COOR5, or —C(O)R5, wherein R5 is alkyl or aryl.Type: GrantFiled: March 16, 2000Date of Patent: August 14, 2001Assignee: Hoffman-La Roche Inc.Inventor: Wolfgang Göhring
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Patent number: 6265572Abstract: Compounds of the formula: are described which have activity as anti-inflammatory agents. Cyclic disulfide compounds are provided which inhibit of binding of cells to endothelium. Such compounds are useful for treating inflammatory diseases, such as asthma, whose symptoms and/or damage are related to the binding of cell adhesion molecules to integrin expressing cells.Type: GrantFiled: April 14, 2000Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Nader Fotouhi, David Young Jackson, Jefferson Wright Tilley
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Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6265426Abstract: The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.Type: GrantFiled: July 19, 2000Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Büttelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, René Wyler
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Patent number: 6262089Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: February 16, 2000Date of Patent: July 17, 2001Assignee: Hoffman-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6258063Abstract: A hypodermic injection system allows for the generation of a high pressure liquid jet capable of passing through the skin. The system uses two regions, the first region being flexible or squeezable and the second region having at least one exiting orifice through which the liquid jet can be expelled. The flexible region can be deformed by a pressure change in the surrounding container generated by an activatable gas generator that generates pressure within the first region that causes the liquid to be expelled.Type: GrantFiled: September 24, 1999Date of Patent: July 10, 2001Assignee: Roche Diagnostics GmbHInventors: Hans-Peter Haar, Manfred Beuttenmüller, Markus Mattern, George Bevan Meacham
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Patent number: 6258832Abstract: Improved process of compound of formula III in which A denotes CH═CH or S W denotes O X denotes S, O or NR2 in which the residue R2 is hydrogen or C1-C6 alkyl, Y denotes CH or N R denotes naphthyl, thienyl or phenyl which is optionally monosubstituted or disubstituted with C1-C3 alkyl, CF3, C1-C3 alkoxy, F, Cl or bromine, R1 denotes hydrogen or C1-C6 alkyl and n denotes 1-3 by reducing a compound of the general formula IV, in which A, W, X, Y, R, R1 and n have the meanings stated above with activated aluminium in a protic solvent, as well as new compounds of formula III and pharmaceutical preparations containing these compounds.Type: GrantFiled: September 14, 1999Date of Patent: July 10, 2001Assignee: Roche Diagnostics GmbHInventors: Hans-Frieder Kühnle, Ernst-Christian Witte, Hans-Peter Wolff
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Patent number: 6255501Abstract: Methods for preparing antiosteoportic agents are disclosed. Compounds useful in the methods are also disclosed.Type: GrantFiled: April 13, 2000Date of Patent: July 3, 2001Assignee: Hoffman-La Roche Inc.Inventors: Andrzej Robert Daniewski, Roumen Nikolaev Radinov
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Patent number: 6242601Abstract: The compounds of formula (I) wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.Type: GrantFiled: January 13, 2000Date of Patent: June 5, 2001Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Philippe Coassolo, Rolf Huber, Werner Neidhart, Henri Ramuz, Sébastien Roux, Hans Peter Wessel
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Patent number: 6242644Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.Type: GrantFiled: December 14, 1999Date of Patent: June 5, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
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Patent number: 6238664Abstract: An aqueous protein solution buffered with a potassium phosphate buffer, in which the ratio of potassium ions to sodium ions in the solution is at least 10:1, is resistant to the formation of protein aggregates and particles under conditions of freezing, thawing, lyophilization, and reconstitution.Type: GrantFiled: November 19, 1998Date of Patent: May 29, 2001Assignee: Boehringer Mannheim GmbHInventors: Klaus Hellerbrand, Appollon Papadimitriou, Gerhard Winter
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Patent number: 6239296Abstract: Intermediate compounds useful for making phenylthiobutyl-isoquinoline compounds of formulaType: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 6239151Abstract: The invention provides hydrazine derivatives of the formula wherein R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is an acyl group derived from an &agr;-, &bgr;-, &ggr;- or &dgr;-(amino, hydroxy or thiol)carboxylic acid in which the amino, hydroxy or thiol group is optionally lower alkylated or the amino group is optionally acylated, sulphonylated or amidated and in which any functional group present in a side-chain is optionally protected, or a group of the formula Het(CH2)mCO; R3 is hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl-lower alkenyl, aryl or heterocyclyl; R4 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a groupinType: GrantFiled: June 14, 1999Date of Patent: May 29, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6222039Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.Type: GrantFiled: July 7, 1999Date of Patent: April 24, 2001Assignee: Hoffman-La Roche Inc.Inventors: Michelangelo Scalone, Ulrich Zutter
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Patent number: 6197959Abstract: Compounds of formula (I) wherein R1 and R2 are as defined in the description and claims and pharmaceutically acceptable salts thereof, are useful for the treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, for example, cardiac insufficiency and kidney insufficiency.Type: GrantFiled: April 4, 2000Date of Patent: March 6, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Daniel Bur, Hans-Peter Märki, Eric Vieira, Wolfgang Wostl
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Patent number: 6197759Abstract: Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. These compounds include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds, and derivatives of said compounds, salts, esters, optically active forms and racemates which can be metabolized in vivo to yield the corresponding compound of formula (I).Type: GrantFiled: April 11, 2000Date of Patent: March 6, 2001Assignee: Roche Diagnostics GmbHInventors: Angelika Esswein, Lothar Kling