Abstract: Retinoids with retinoid receptor antagonistic activity, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found efficacious in treating T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.
Type:
Grant
Filed:
November 10, 1998
Date of Patent:
October 17, 2000
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Bollag, Michael Klaus, Paola Panina-Bordignon, Francesco Sinigaglia
Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 each independently represent hydrogen, C.sub.1-7 -alkyl, or C.sub.1-7 -alkoxy,A signifies--CN,a carbanionic R.sup.4 -alkynyl residue, in which R.sup.4 is hydrogen or C.sub.1-7 -alkyl, ora carbanionic residue of the malonic acid derivative of formula III ##STR2## in which B and B' independently represent --CN, --COOR.sup.5, or --C(O)R.sup.5, wherein R.sup.5 is alkyl or aryl.
Abstract: New compounds have the formula: ##STR1## wherein R, R.sup.1, 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:
Grant
Filed:
October 27, 1998
Date of Patent:
August 15, 2000
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
Abstract: The present invention is concerned with a novel process for the carbamoylation of substituted pyridines, especially with a process for the preparation of compounds of formula I ##STR1## wherein R.sup.4 to R.sup.8 represent hydrogen, lower-alkoxy or halogen; or optionally salts thereof.
Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.
Type:
Grant
Filed:
December 22, 1998
Date of Patent:
August 8, 2000
Assignee:
Hoffman-La Roche Inc.
Inventors:
Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
Abstract: A method for the determination of factor IXa in a sample solution using a measurable factor IXa substrate and a water-miscible alcohol and measuring the cleavage of the factor IXa substrate as a measure for factor IXa activity is suitable for the direct determination of factor IXa.
Abstract: 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.
Abstract: Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.
Type:
Grant
Filed:
February 22, 1999
Date of Patent:
April 18, 2000
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alfred Binggeli, Volker Breu, Daniel Bur, Walter Fischli, Rolf Guller, Georges Hirth, Hans-Peter Marki, Marcel Muller, Christian Oefner, Heinz Stadler, Eric Vieira, Maurice Wilhelm, Wolfgang Wostl
Abstract: Tertiary amines of the formula ##STR1## wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.
Type:
Grant
Filed:
December 6, 1996
Date of Patent:
March 7, 2000
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synese Jolidon, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Ku-Hua Ji
Abstract: 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:
Grant
Filed:
August 15, 1997
Date of Patent:
December 21, 1999
Assignee:
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
Abstract: Product containing tetrahydrolipstatin as the active ingredient and pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter of 0.25 to 2 mm; and pharmaceutical preparation s or compositions for oral administration containing the product.
Abstract: 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:
Grant
Filed:
December 22, 1998
Date of Patent:
December 14, 1999
Assignee:
Hoffman-La Roche Inc.
Inventors:
Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
Abstract: 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.
Abstract: 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:
Grant
Filed:
November 3, 1997
Date of Patent:
October 26, 1999
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
Abstract: 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.
Abstract: 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:
Grant
Filed:
August 18, 1997
Date of Patent:
October 5, 1999
Assignee:
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
Abstract: 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.
Abstract: 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:
Grant
Filed:
May 12, 1997
Date of Patent:
August 3, 1999
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rainer Alex, Paul Hadvary, Hansjorg Tschirky
Abstract: 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.