Patents Represented by Attorney William H. Epstein
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Patent number: 6004965Abstract: Compounds of the formula: ##STR1## where A, B, R.sup.1 -R.sup.8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.Type: GrantFiled: August 15, 1997Date of Patent: December 21, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
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Patent number: 6001855Abstract: Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in claim 1, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasing, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, kidney failure as well as infections caused by viruses, bacteria or fungi.Type: GrantFiled: December 22, 1998Date of Patent: December 14, 1999Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 5990329Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 and X are as described, are disclosed. The compounds are useful for treating dermatological disorders which are accompanied by epithelial lesions, e.g., acne and psoriasis, as well as malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.Type: GrantFiled: April 3, 1997Date of Patent: November 23, 1999Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5986131Abstract: Novel nonatetraenoic acid derivatives which selectively bind to retinoic acid X-receptors (RXR) and which have anti-acne acitvity and which potentiate the activity of retinoids having RAR.alpha. activity are disclosed.Type: GrantFiled: October 17, 1997Date of Patent: November 16, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Allen John Lovey, Peter Mohr, Michael Rosenberger
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Patent number: 5977388Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.Type: GrantFiled: July 9, 1998Date of Patent: November 2, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5973188Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T 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, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitrites.Type: GrantFiled: November 3, 1997Date of Patent: October 26, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
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Patent number: 5969190Abstract: The compound, (E)-(1R,3R)-5-[(R)-11-hydroxy-7,11-dimethyl-dodec-2-enylidene]-cyclohexane -1,3-diol of the formula I: ##STR1## is useful in the treatment or prevention of hyperproliferative skin diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; or for reversing the conditions associated with photodamage.Type: GrantFiled: May 15, 1998Date of Patent: October 19, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Franz Bauer, Lawrence F. Courtney
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Patent number: 5968779Abstract: Proteins which modulate body weight of animals and humans for the treatment, prevention and control of obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.Type: GrantFiled: January 5, 1998Date of Patent: October 19, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Arthur Campfield, Rene Devos, Yves Guisez
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Patent number: 5969139Abstract: The invention relates to new and known tricyclic dione derivatives of the general formula ##STR1## wherein W represents hydrogen or lower alkyl;X represents lower alkyl;Y represents NR1;R.sup.1 represents hydrogen, lower alkyl, lower alkoxycarbonyl or lower alkoxycarbonyl-lower alkyl;Z represents aryl or heteroaryl optionally substituted by one or more halo, cyano, nitro, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, COR.sup.2, OCOR.sup.2, CO.sub.2 R.sup.2, OR.sup.2, S(O).sub.n R.sup.2, NR.sup.2 R.sup.3, N(R.sup.4)COR.sup.5, Ar, Ar-lower alkyl, Het or Het-lower alkyl substituents and/or on adjacent carbon atoms by lower alkylenedioxy;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each individually represent hydrogen, lower alkyl, Ar, Ar-lower alkyl, Het or Het-lower alkyl substituents; or R.sup.2 and R.sup.3 together represent the group --CH.dbd.CH--CH.dbd.CH-- or --CH.dbd.N--CH.dbd.Type: GrantFiled: August 6, 1997Date of Patent: October 19, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Armstrong Martin, Bradley Stuart Sherborne, Gareth Mark Taylor
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Patent number: 5965733Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.Type: GrantFiled: November 16, 1998Date of Patent: October 12, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 5962682Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.Type: GrantFiled: August 18, 1997Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 5962686Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antiftngal properties.Type: GrantFiled: January 8, 1999Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
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Patent number: 5931814Abstract: An improved injection device has a casing containing an active substance reservoir, a cannula communicating with the reservoir, a device for inserting the cannula, and pump means for discharging the reservoir contents through the cannula. The cannula 11 is fixed relative to the casing and projects beyond the underside of the casing to the depth required for injection. The cannula is surrounded by a protective element which is moved by a spring drive from a first end position in which the protective device projects beyond the underside of the casing and beyond the cannula to a second end position in which the protective device does not project beyond the underside of the casing.Type: GrantFiled: May 12, 1997Date of Patent: August 3, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Rainer Alex, Paul Hadvary, Hansjorg Tschirky
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Patent number: 5928636Abstract: The present invention provides a combination of IL-12 and IFN.alpha. together with a pharmaceutically acceptable carrier useful for treatment and prophylaxis of infectious diseases, preferably chronic infectious diseases and more preferably viral infections, e.g. HSV, HIV, Hepatitis B, Hepatitis C, papilloma etc., bacterial infections, e.g. tuberculosis, salmonellosis, listeriosis, etc., and parasite infections, e.g. malaria, leishmaniasis, and schistosomiasis. These compositions are characterized by the synergistic interaction of IL-12 and IFN.alpha.. The present invention also provides the use of the above combination for the treatment and prophylaxis of infectious diseases.Type: GrantFiled: April 30, 1997Date of Patent: July 27, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Gottfried Alber, Jacqueline Anne Carr, Frank Albert Mattner, Michael John Mulqueen, Kathrin Palmer, Jane Andre Louise Rogerson
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Patent number: 5919939Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R.sup.1 is trityl, acetyl, tetrahydropyranyl or cyclopentyl;R.sup.2 is hydrogen, hydroxy, lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, lower alkynyl, aryl, aryloxy, aryl-lower alkyl, aryl-lower alkoxy or heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl, aryloxy, aryl-lower alkoxy, the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.21 R.sup.22, --N(R.sup.22)COOR.sup.23, R.sup.22 CO--, R.sup.22 OCO-- or R.sup.22 COO--, wherein R.sup.21 is hydrogen, lower alkyl, or cycloalkyl; R.sup.22 is hydrogen or lower alkyl; R.sup.23 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Y is --S-- and Z is --CH.sub.2 -- orY is --CH.sub.Type: GrantFiled: May 20, 1998Date of Patent: July 6, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Thomas Oberhauser
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Patent number: 5914404Abstract: The present invention is concerned with a novel process for the manufacture of quinargine ##STR1## (N-(2-quinolylcarbonyl)-asparagine) based on the reaction of the succinimide ester ##STR2## with asparagine or asparagine salts in an aqueous reaction medium at a neutral pH value.Type: GrantFiled: July 18, 1997Date of Patent: June 22, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Wolfgang Gohring
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Patent number: 5907038Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is phenyl or alpha- or beta-naphthyl, which groups can be substituted by hydroxy, lower-alkyl, lower-alkoxy, lower alkoxycarbonyl, phenoxy, acyloxy, hydroxyphenoxy-sulfonyl, halogen, nitro, amino, acylamino or N-lower-alkyl-acylamino;R.sup.2 is phenyl or phenyl substituted by hydroxy or acyloxy;Y is a carbon-carbon bond or is vinylene; andn is 1,2 or 3;and pharmaceutically acceptable acid addition salts thereof are protein kinase inhibitors and can be used for the treatment of disorders mediated by such enzymes, for example, inflammatory diseases.Type: GrantFiled: March 31, 1997Date of Patent: May 25, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Josef Stadlwieser, Sven Taylor
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Patent number: 5902882Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.Type: GrantFiled: April 3, 1997Date of Patent: May 11, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
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Patent number: 5900486Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antifungal properties.Type: GrantFiled: September 9, 1997Date of Patent: May 4, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
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Patent number: 5891900Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, cycloalkyl or phenyl,R.sup.2 is H, OH or C(O)O--A, wherein A is lower-alkyl, cycloalkyl or phenyl, andR.sup.3,R.sup.4 and R.sup.5 are either methyl or R.sup.3 is H and R.sup.4 and R.sup.5 taken together are trimethyleneas well as hydrates or solvates and physiologically usable salts thereof can be used for the production of medicaments for the treatment or prophylaxis of illnesses which are caused by thrombin-induced platelet aggregation or fibrinogen clotting in blood plasma.Type: GrantFiled: July 8, 1997Date of Patent: April 6, 1999Assignee: Hoffman-La Roche IncInventors: Fran.cedilla.ois Diederich, Ulrike Obst, Lutz Weber