Patents Represented by Attorney, Agent or Law Firm Ellen Ciambrone Coletti
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Patent number: 5614526Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host in need of such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 and R.sup.3 each independently are hydrogen, aryl, carbamoyl, lower-alkyl-carbonyl, lower-alkyl, halogen, lower-alkyl-carbonyl-amino, lower-alkenyl-carbonyl-amino, amino, arylamino, aryloxy, nitro, aryl-acetyl, lower-alkanoyl-lower-alkyl, alkyl-sulphonyl-amino, ureido or furan-2-yl-carbonyl-amino andR.sup.2 is hydrogen, lower-alkyl, trifluoromethyl, halogen, lower-alkoxy, lower-alkyl-carbonyl or lower-alkyl-carbonyl-amino orR.sup.1 and R.sup.2 together are --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O-- or --(CH.sub.2).sub.3 --,R.sup.4 is hydrogen, halogen, hydroxy, lower-alkyl, lower-alkoxy or nitro,R.sup.5 is hydrogen, halogen or lower-alkoxy,R.sup.Type: GrantFiled: April 29, 1996Date of Patent: March 25, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Deborah Hartman, Claus Riemer
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Patent number: 5612328Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.Type: GrantFiled: February 1, 1996Date of Patent: March 18, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Barbara J. Baggiolini, Shian-Jan Shiuey, Milan R. Uskokovic
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Patent number: 5580574Abstract: A pharmaceutical composition for transdermal delivery comprising an effective amount of an active ingredient selected from a benzodiazepine and a benzodiazepine antagonist; isopropanol; propylene glycol; oleic acid; and water. Additionally, the composition may contain diacetin, Cetiol B.RTM., caprylic acid, Silicon fluid, Miglyol.RTM. 840 or transcutol.Type: GrantFiled: April 28, 1994Date of Patent: December 3, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Charanjit R. Behl, Peter Hofmann
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Patent number: 5578728Abstract: The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4-oxo-3 -phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.Type: GrantFiled: October 21, 1994Date of Patent: November 26, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Paul Spurr
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Patent number: 5567349Abstract: The present invention is concerned with photo cross-linkable liquid crystals of the formula ##STR1## wherein A is a cross-linkable mesogenic residue;X is a single bond, --COO--, --CH.sub.2 O--, --CONH-- or --C.dbd.N--; andQ is n-alkylene, c-alkylene, 1,4-phenylene, 4,4'-biphenylene or 2,6-naphthylene;liquid crystalline mixtures which contain such compounds as well as their use in the cross-linked state for optical building elements.Type: GrantFiled: March 1, 1995Date of Patent: October 22, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Stephen Kelly, Martin Schadt, Klaus Schmitt
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Patent number: 5561150Abstract: Compounds of the formula ##STR1## wherein R.sup.1 to R.sup.4 each are hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy or phenyl;R.sup.5 is hydrogen or lower alkyl,R.sup.6 is hydrogen, lower alkyl or lower alkoxy;X is --(CR.sup.7 R.sup.8).sub.n -- or --CH.dbd.CH--;R.sup.7 and R.sup.8 are hydrogen or lower alkyl andn is 1 or 2,as well as pharmaceutically acceptable salts of basic compounds of formula I, bind to serotonin receptors, and thus are useful in treating central nervous system disorders.Type: GrantFiled: August 2, 1995Date of Patent: October 1, 1996Assignee: Hoffman-La Roche Inc.Inventor: J urgen Wichmann
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Patent number: 5561233Abstract: The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4 -oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.Type: GrantFiled: May 30, 1995Date of Patent: October 1, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Paul Spurr
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Patent number: 5552153Abstract: A pharmaceutical composition for transdermal delivery comprising an effective amount of an active ingredient selected from a benzodiazepine and a benzodiazepine antagonist; ethanol; caprylic acid; and oleic acid. Additionally, the composition may contain silicon fluid, benzyl alcohol, transcutol or dimethyl sulfoxide.Type: GrantFiled: April 28, 1994Date of Patent: September 3, 1996Assignee: Hoffman-La Roche Inc.Inventor: Charanjit R. Behl
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Patent number: 5547947Abstract: A method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 analog, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 analog.In another aspect, a method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 metabolite, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 metabolite.Type: GrantFiled: November 30, 1994Date of Patent: August 20, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Benoit T. Dore, Richard L. Momparler, Milan R. Uskokovic
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Patent number: 5545658Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.Type: GrantFiled: May 25, 1995Date of Patent: August 13, 1996Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Paul Hadvary, Marianne H urzeler, Marcel M uller, Beat Steiner, Thomas Weller
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Patent number: 5534635Abstract: It has been found that pyridine-2-carboxamides of the formula ##STR1## wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formulaR.sup.1 --C.tbd.CH IIIwherein R.sup.1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R.sup.2)(R.sup.3)--COH and R.sup.2 and R.sup.3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl,oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formulaor with carbon monoxide and an amino compound of formula VI or with carbon monoxide and a lower alkanol which is optionally mixed with water and reacting the resulting acid or the resulting ester with an amino compound of formula VI.Type: GrantFiled: September 12, 1994Date of Patent: July 9, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Michelangelo Scalone, Peter Vogt
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Patent number: 5512554Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.Type: GrantFiled: April 11, 1995Date of Patent: April 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, deceased, Shian-Jan Shiuey, Milan R. Uskokovic
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Patent number: 5486310Abstract: Optically active compounds of the formula ##STR1## wherein rings A, B and C each independently are unsubstituted or each are 1,4-phenylene substituted with at least one of halogen-, cyano-, methyl- or methoxy in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; R.sup.1 is a radical of an optically active terpene alcohol after cleavage of the hydroxy group or a group --(CH.sub.2).sub.m --C*HX.sup.1 --R.sup.3 ; R.sup.2 is a radical of an optically active terpene alcohol after cleavage of the hydroxy group or a group --(CH.sub.2).sub.n --C*HX.sup.2 --R.sup.4 ; m and n each independently stand for the number 0 or 1: C* denotes a chiral carbon atom; X.sup.1 and X.sup.2 each independently are fluorine, chlorine, cyano, methyl or methoxy; R.sup.3 and R.sup.4 each independently denote a group R, phenyl or phenyl substituted with R, with the proviso that R.sup.3 is different from X.sup.1 and R.sup.4 is different from X.sup.Type: GrantFiled: February 18, 1994Date of Patent: January 23, 1996Assignees: Hoffmann-La Roche Inc., Niopic Moscow Research and Production AssociationInventors: Richard Buchecker, Nina I. Chernova, Alexander V. Ivaschenko, Marina V. Loseva, Olga S. Petrashevich, Evgeniy P. Pozhidaev, Arnold Z. Rabinovich, Martin Schadt
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Patent number: 5481008Abstract: A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.Type: GrantFiled: August 31, 1994Date of Patent: January 2, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Emil A. Broger, Martin Karpf, Ulrich Zutter
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Patent number: 5470861Abstract: The use of the compound 2-(6-cyano-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)pyridine-1-oxide represented by the formula ##STR1## as well as pharmaceutically acceptable salts, as topical agents to promote hair growth is disclosed.Type: GrantFiled: August 4, 1994Date of Patent: November 28, 1995Assignee: Hoffmann-La Roche Inc.Inventor: Charles S. Harmon
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Patent number: 5451574Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.Type: GrantFiled: January 18, 1994Date of Patent: September 19, 1995Assignee: Hoffman-La Roche Inc.Inventors: Enrico G. Baggiolini, deceased, Barbara J. Baggiolini, Shian-Jan Shiuey, Milan R. Uskokovic
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Patent number: 5447919Abstract: The use of compounds of the formula ##STR1## wherein R is hydrogen or a residue --SO.sub.3 M; M is a cation; and R' and R" are hydrogen or an .alpha.-glycosidically linked sulfated mono- or disaccharide residue; and at least one --SO.sub.3 M group is present per monosaccharide unit,as pharmaceutical compositions for the prevention and/or treatment of arteriosclerotic disorders and for the prevention of restenosis after invasive vascular surgery and after organ transplants.Type: GrantFiled: March 17, 1994Date of Patent: September 5, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Markus Hosang, Niggi Iberg, Thomas B. Tschopp, Hans P. Wessel
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Patent number: 5447929Abstract: Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.Type: GrantFiled: March 17, 1994Date of Patent: September 5, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5420305Abstract: A process for the preparation of a tautomeric mixture of compounds of the formulas ##STR1## wherein W is hydrogen or C.sub.6 H.sub.13, which comprises treating a compound of the formula ##STR2## wherein R is unsubstituted or substituted alkoxy, arylalkoxy, aryloxy or amine and R.sup.1 is hydrogen or when R is alkoxy, substituted alkoxy, substituted amine, unsubstituted or substituted arylalkoxy R.sup.1 can also be metal, with a compound of the formula ##STR3## wherein W is as described above, both X and Y are reducible groups or X is hydrogen and Y is a reducible group or Y is hydrogen and X is a reducible group and, Z is hydroxy or a leaving group to form the compound of formula IV ##STR4## wherein W, X, Y and R are as defined above, the compound of formula IV is treated with a low valent metal to form a tautomeric mixture of compounds of formulas I and Ia, which are useful in the synthesis of tetrahydrolipstatin.Type: GrantFiled: October 4, 1993Date of Patent: May 30, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Keith M. Ramig, John J. Landi, Jr.
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Patent number: 5399702Abstract: Compounds of the formula: ##STR1## wherein the substituents are as defined herein, and enantiomers, diastereomers, racemates and salts with pharmaceutically acceptable bases, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.Type: GrantFiled: September 2, 1993Date of Patent: March 21, 1995Assignee: Hoffmann-La Roche Inc.Inventors: George W. Holland, John R. Vermeulen, William J. Zally