Patents Represented by Attorney, Agent or Law Firm Bruce A. Pokras
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Patent number: 5559232Abstract: The novel carboxamides of the formula ##STR1## wherein A, E, G, L, M, R and Q have the significance given in the description, as well as hydrates or solvates thereof inhibit thrombin-induced platelet aggregation and fibrinogen coagulation in plasma. They can be manufactured starting from the corresponding acid and the corresponding amine H.sub.2 NCH.sub.2 Q.Type: GrantFiled: September 2, 1994Date of Patent: September 24, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
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Tetrasulfonated diphosphine compounds and metal complexes thereof for asymmetric catalytic reactions
Patent number: 5536858Abstract: The invention is concerned with novel water-soluble racemic or optically active compounds of formulae ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently signify lower alkyl or lower alkoxy;m and n are 0, 1 or 2; andX signifies hydrogen, an alkali :metal, the equivalent of an earthalkali metal or an ammonium ion;with the provision that R.sup.3 is in position 4 or 5 and R.sup.4 is in position 4' or 5'. The invention is also concerned with complexes of such compounds with a metal of Group VIII. These complexes are, useful as catalysts for asymmetric hydrogenation and for enantioselective hydrogen displacement in prochiral allylic systems.Type: GrantFiled: December 2, 1994Date of Patent: July 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Michel Lalonde, Rudolf Schmid -
Patent number: 5536816Abstract: A process for the manufacture of amides, including peptides, by reacting a carboxylic acid with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of a N-hydroxy compound.Type: GrantFiled: February 15, 1994Date of Patent: July 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Markus Hohler, Peter Vogt
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Patent number: 5536867Abstract: The present invention is directed to a process, and novel intermediates used in the manufacture of, dicarboxamides of the formula I ##STR1## wherein A, G, L, Q, X and Y have the meaning given in the specification, starting from corresponding N-substituted aspartic acid and from corresponding amines G-NHCH(X,Y), via corresponding N-substituted oxazolidinone and N,N-substituted aspartates.Type: GrantFiled: March 17, 1995Date of Patent: July 16, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Milan Soukup
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Patent number: 5532232Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.Type: GrantFiled: November 22, 1994Date of Patent: July 2, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
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Patent number: 5516944Abstract: The present invention is concerned with novel optically active phosphorus compounds of the general formula ##STR1## wherein R and R.sup.1 each independently signify hydroxy, a protected hydroxy group, lower alkyl or lower alkoxy andR.sup.2 to R.sup.5 each independently signify alkyl with 3 to 7 carbon atoms, cycloalkyl or aryl or R.sup.2 and R.sup.3 or R.sup.4 and R.sup.5 together with the phosphorus form a group of the formula ##STR2## wherein R2 and R3 are different when R4 and R5 are the same, and R4 and R5 are different when R2 and R3 are the same,the manufacture of such compounds, their use for enantioselective reactions, such as, e.g., asymmetric hydrogenations, enantioselective hydrogen displacements in prochiral allylic systems and the like, as well as complexes of the compounds of formula I with Group VIII metals.Type: GrantFiled: September 30, 1994Date of Patent: May 14, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Emil A. Broger, Marco Cereghetti, Alain Rageot
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Patent number: 5514805Abstract: A novel process for the asymmetric hydrogenation of compounds of the formula: ##STR1## wherein R represent aryl or heteroaryl, to compounds of the formula: ##STR2## wherein R has the above significance, is carried out using rhodium-diphosphine complexes.Type: GrantFiled: April 8, 1994Date of Patent: May 7, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Emil A. Broger, Werner Hofheinz, Arthur Meili
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Patent number: 5512683Abstract: Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.Type: GrantFiled: October 18, 1994Date of Patent: April 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5508438Abstract: Novel, racemic and optically active phosphorus compounds of the formula ##STR1## wherein R signifies lower alkyl, lower alkoxy, hydroxy or a protected hydroxy group, R.sup.1 and R.sup.2 are different from each other and represent lower alkyl, cycloalkyl, aryl, a five-membered heteroaromatic or a group of the formula ##STR2## are described. The compounds of formula I are useful in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in prochiral allylic systems.Type: GrantFiled: September 24, 1993Date of Patent: April 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Emil A. Broger, Marco Cereghetti
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Patent number: 5508437Abstract: Analogs of Tyrosine Sulfate or Tyrosine Phosphate containing peptides, the novel intermediate compounds used in the preparation of these analogs, as well as a method for suppressing appetite in subjects by administering to the subject an effective amount of CCK analog wherein one or more of any Tyrosine Sulfate present is substituted with a radical of the invention.Type: GrantFiled: December 17, 1993Date of Patent: April 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Waleed Danho, Jefferson W. Tilley, Joseph Triscari, Rolf Wagner
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Patent number: 5502212Abstract: A process for the manufacture of 5-cyano-4-lower alkyl-oxazoles is described in which a 5-carbamoyl-4-lower alkyl-oxazole is dehydrated in an organic solvent under mild conditions with cyanuric chloride and an N,N-disubstituted-formamide.Type: GrantFiled: February 16, 1994Date of Patent: March 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bonrath, Reinhard Karge, Horst Pauling
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Patent number: 5502236Abstract: Novel processes and intermediates useful for the manufacture of the Wittig ester salts are disclosed. The Wittig ester salts are known as important CS building blocks for the manufacture of various polyenecarboxylic acid esters in the field of carotenoid chemistry.Type: GrantFiled: March 17, 1995Date of Patent: March 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Bruno Burdet, August Ru/ ttimann, Jean-Marie Santer, Theodor Siegfried
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Patent number: 5488172Abstract: Novel chiral phosphorus compounds of the formula ##STR1## wherein R signifies lower alkyl, R.sup.1 signifies phenyl and R.sup.2 and R.sup.3 signify hydrogen or lower alkoxy,which are suitable in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in prochiral allylic systems.Type: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Marco Cereghetti, Joseph Foricher, Bernd Heiser, Rudolf Schmid
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Patent number: 5482718Abstract: A novel delivery system for targeting drugs to the colon is disclosed. The delivery system is a tablet comprised of three parts: (1) an enteric coating to prevent penetration of gastric fluid into the delivery system, thereby preventing any drug release in the stomach; (2) an erodible polymer layer which is exposed and gradually erodes during transit through the upper intestinal tract, and (3) a core, which is a conventional tablet or beadlet containing an active ingredient(s), which readily disintegrates and subsequently releases the drug to the target site, the colon, after erosion of the erodible polymer layer. The erodible polymer layer prevents drug release in the upper portion of the intestinal tract for 4-6 hours after gastric emptying, representing the amount of time needed for the delivery system to reach the colon.Type: GrantFiled: March 23, 1994Date of Patent: January 9, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Navnit H. Shah, Wantanee Phuapradit, Aruna Railkar
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Patent number: 5453547Abstract: A novel process for the manufacture of .gamma.-acetoxytiglic aldehyde ("C.sub.5 -aldehyde"), which is known as an important starting material for the production of vitamin A acetate from a (.beta.-ionylidenethyl)triphenylphosphonium halide and C.sub.5 -aldehyde, comprises treating a pentenyn-3-ol of the formula HC.tbd.C--C(CH.sub.3)(OH)--CH.dbd.C(R).sub.2 (II), wherein both R's signify either hydrogen or methyl, with ozone, preferably in a lower alkanol R.sup.1 OH, wherein R.sup.1 signifies C.sub.1-4 -alkyl, to obtain an aldehyde 2-hydroxy-2-methyl-3-butynal of the formula HC.tbd.C--C(CH.sub.3)(OH)--CHO (III). The aldehyde III may be converted to the C.sub.5 -aldehyde by conventional means.Type: GrantFiled: September 30, 1994Date of Patent: September 26, 1995Assignee: Hoffman-La Roche Inc.Inventor: Ulriche Zutter
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Patent number: 5453546Abstract: A process is described for the manufacture of .beta.-ionone by the sulphuric acid-catalyzed cyclization of pseudoionone in a two-phase solvent system comprising concentrated sulphuric acid and a second solvent essentially immiscible with water, which process comprises using carbon dioxide liquefied under pressure as the second solvent. This process is carried out, inter alia, under a pressure of about 50 bar to about 150 bar and at temperatures from about -15.degree. C. to about +15.degree. C. prior to the subsequent stopping (quenching) of the cyclization reaction. The process in accordance with the invention is preferably carried out continuously and is an important intermediate stage in the synthesis of vitamin A.Type: GrantFiled: June 2, 1994Date of Patent: September 26, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Steiner, Herwig Ertel, Helmut Tiltscher
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Patent number: 5430041Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heterocyclylcarbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl: and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.Type: GrantFiled: April 21, 1992Date of Patent: July 4, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Martin, Gareth J. Thomas
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Patent number: 5420273Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: December 23, 1993Date of Patent: May 30, 1995Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5393875Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significance given in claim 1,in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharamaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be manufactured according to various methods which are known per se.Type: GrantFiled: August 3, 1993Date of Patent: February 28, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Marie-Paule Heitz, Werner Neidhart, Heinz Stadler, Eric Vieira, Wolfgang Wostl
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Patent number: 5391766Abstract: Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.Type: GrantFiled: May 5, 1993Date of Patent: February 21, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr