Patents Represented by Attorney, Agent or Law Firm Ellen Ciambrone Coletti
-
Patent number: 5250562Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.Type: GrantFiled: February 3, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
-
Patent number: 5247123Abstract: The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis.Type: GrantFiled: July 2, 1992Date of Patent: September 21, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic
-
Patent number: 5246960Abstract: Racemic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as described herein, enantiomers and diastereomers thereof, and salts of these esters with weak acids, are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipaemia, atherosclerosis and arteriosclerosis.Type: GrantFiled: September 14, 1992Date of Patent: September 21, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
-
Patent number: 5244900Abstract: A compound of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is the group ##STR2## and further wherein the substituents R.sup.1, R.sup.2, and R.sup.3 are as described in the specification, can be used in the treatment of neurological symptoms which are associated with circulatory disorders of the brain, especially in the treatment of neurological symptoms which are associated with cerebrovascular seizures.Type: GrantFiled: December 20, 1991Date of Patent: September 14, 1993Assignee: Hoffmann-La Roche Inc.Inventor: Giuseppe Scollo-Lavizzari
-
Patent number: 5236952Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1991Date of Patent: August 17, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
-
Patent number: 5225557Abstract: A process for preparing optically active naphtho[1.2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.Type: GrantFiled: December 10, 1990Date of Patent: July 6, 1993Assignee: Hoffmann-La Roche Inc.Inventor: Erno Mohacsi
-
Patent number: 5215972Abstract: Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.Type: GrantFiled: May 1, 1992Date of Patent: June 1, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Marie Cassal, Nigel Gains, Eva-Maria Gutknecht, Georges Hirth, Hans Lengsfeld
-
Patent number: 5187293Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, and their hydrates, which inhibit blood platelet activating factor (PAF), are described.Type: GrantFiled: November 19, 1987Date of Patent: February 16, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
-
Patent number: 5175186Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently C.sub.1-17 -alkyl which is saturated or optionally interrupted by up to 8 double or triple bonds and/or optionally interrupted by an O or S atom, which is present in other than the .alpha.-position to an unsaturated C atom; or phenyl, benzyl or --C.sub.6 H.sub.4 --X--C.sub.6 H.sub.5 ring-substituted by 0 to 3 C.sub.1-6 -alkyl-(O or S).sub.1 or 0 groups, and X is oxygen, sulfur or (CH.sub.2).sub.0-3, with the proviso that when R.sup.1 is n-hexyl and R.sup.2 is undecyl or 2Z,5Z-undecadienyl, at least one of the asymmetric C-atoms present in the oxetanone ring and in the .beta.-position to the latter has the R-configuration, an enantiomer or a diastereomer thereof are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipemia, atherosclerosis and arteriosclerosis.Type: GrantFiled: March 19, 1990Date of Patent: December 29, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
-
Patent number: 5149846Abstract: The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis.Type: GrantFiled: November 16, 1989Date of Patent: September 22, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic
-
Patent number: 5145846Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or hydroxy, R.sub.5 is hydrogen, and A is ##STR2## with the proviso that when A is --C.tbd.C--, R.sub.5 may also be deuterium, are described.The compounds of formula I are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne or seborrheic dermatitis.Type: GrantFiled: April 10, 1991Date of Patent: September 8, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, deceased, Bernard M. Hennessy, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
-
Patent number: 5134123Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.Type: GrantFiled: March 3, 1989Date of Patent: July 28, 1992Assignee: Hoffman-La Roche Inc.Inventors: Quirico Branca, Werner Neidhart, Henri Ramuz, Heinz Stadler, Wolfgang Wostl
-
Patent number: 5120722Abstract: The compounds 1.alpha.,25(S), 26-trihydroxy-.DELTA..sup.22 -cholecalciferol; 1.alpha.,25(R), 26-trihydroxy-.DELTA..sup.22 -cholecalciferol; 1.alpha.,25(S),26-trihydroxyergocalciferol, 1.alpha.,25(R),26-trihydroxyergocalciferol and pharmaceutical compositions comprising the compounds as well as methods of making and using these compounds are disclosed.Type: GrantFiled: March 19, 1990Date of Patent: June 9, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Andrew D. Batcho, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
-
Patent number: 5106981Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.Type: GrantFiled: April 19, 1990Date of Patent: April 21, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
-
Patent number: 5104569Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is alkyl or alkenyl; Z.sup.1 denotes a single covalent bond or --CH.sub.2 CH.sub.2 --; ring A represents unsubstituted or halogen- and/or methyl-substituted 1,4-phenylene; Z.sup.2 denotes a single covalent bond, oxygen or --CH.sub.2 O--; and R.sup.2 is an unsubstituted or halogen-substituted alkyl or alkenyl group,their preparation as well as liquid crystalline mixtures and their use for electro-optical purposes.Type: GrantFiled: March 27, 1990Date of Patent: April 14, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Frans Leenhouts, Alois Villiger
-
Patent number: 5087619Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or hydroxy, R.sub.5 is hydrogen, and A is --C.tbd.C--, ##STR2## or --CH.sub.2 --CH.sub.2 --, with the proviso that when A is --C.tbd.C--, R.sub.5 may also be deuterium, are described.The compounds of formula I are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne or seborrheic dermatitis.Type: GrantFiled: March 23, 1990Date of Patent: February 11, 1992Assignee: Hoffman-La Roche Inc.Inventors: Enrico G. Baggiolini, deceased, Barbara J. Baggiolini, Bernard M. Hennessy, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
-
Patent number: 5082842Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are defined in the specification, and the pharmaceutically acceptable acid addition salts of compounds of formula A which have one or more basic substituents are described. The compounds of formula A have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: October 16, 1989Date of Patent: January 21, 1992Assignee: Hoffmann-La Roche Inc.Inventor: Ulrich Widmer
-
Patent number: 5073550Abstract: Antibacterial compounds of the formula ##STR1## wherein R is a mononuclear carbocyclic aromatic group, a 5-membered aromatic heterocyclic group which contains as the hetero (non-carbon) ring member(s) an oxygen or sulphur atom or an imino or lower alkylimino group and, optionally, one or two nitrogen atoms, or a 6-membered aromatic heterocyclic group which contains one to three nitrogen atoms as the hetero ring member(s); R.sup.1 is hydrogen or a 3-substituent which is usable in cephalosporin chemistry; A is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di-(lower alkyl)carbamoyl; Q is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di(lower alkyl)carbamoyl, or the group --NR.sup.2 -- or --NR.sup.2 NR.sup.3 --; R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl; p and m are the zero or 1, n is zero, 1 or 2; R.sup.Type: GrantFiled: August 28, 1990Date of Patent: December 17, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Erwin Gotschi
-
Patent number: 5057614Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Y have the signficance given in the description, are useful in the control or prevention of inflammatory, immunological, bronchopulmonary or cardiovascular disorders.Type: GrantFiled: February 6, 1989Date of Patent: October 15, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Peter D. Davis, Christopher H. Hill, Geoffrey Lawton
-
Patent number: 5057530Abstract: Glycerol derivatives of the formula ##STR1## wherein one of the residues R.sup.1, R.sup.2 and R.sup.3 is a group U of the formula OY.sup.1 or --X.sup.1 --CO--(A.sup.1).sub.n --Z.sup.1, another residue is a group V of the formula OY.sup.2 or --X.sup.2 --CO--(A.sup.2).sub.p --Z.sup.2, and the remaining residue is a group W of the formula --X.sup.3 T--(C.sub.2-6 -alkylene)-N.sup.+ R A.sup.- in which one of X.sup.1, X.sup.2 and X.sup.3 is oxygen or NQ.sup.1 and the other two are oxygen and the remaining symbols have the significance given below, and their hydrates are described and are prepared by introducing or generating the residues R.sup.1, R.sup.2 and R.sup.3 in corresponding glycerol derivatives.The compounds of formula I are active as inhibitors of blood platelet activating factor or as inhibitors of the growth of tumors.Type: GrantFiled: May 19, 1989Date of Patent: October 15, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller