Patents Represented by Attorney, Agent or Law Firm Ellen Ciambrone Coletti
  • Patent number: 5250562
    Abstract: 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: Grant
    Filed: February 3, 1992
    Date of Patent: October 5, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5247123
    Abstract: 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: Grant
    Filed: July 2, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic
  • Patent number: 5246960
    Abstract: 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: Grant
    Filed: September 14, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
  • Patent number: 5244900
    Abstract: 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: Grant
    Filed: December 20, 1991
    Date of Patent: September 14, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Giuseppe Scollo-Lavizzari
  • Patent number: 5236952
    Abstract: 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: Grant
    Filed: April 16, 1991
    Date of Patent: August 17, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
  • Patent number: 5225557
    Abstract: 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: Grant
    Filed: December 10, 1990
    Date of Patent: July 6, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erno Mohacsi
  • Patent number: 5215972
    Abstract: 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: Grant
    Filed: May 1, 1992
    Date of Patent: June 1, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Marie Cassal, Nigel Gains, Eva-Maria Gutknecht, Georges Hirth, Hans Lengsfeld
  • Patent number: 5187293
    Abstract: 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: Grant
    Filed: November 19, 1987
    Date of Patent: February 16, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 5175186
    Abstract: 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: Grant
    Filed: March 19, 1990
    Date of Patent: December 29, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
  • Patent number: 5149846
    Abstract: 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: Grant
    Filed: November 16, 1989
    Date of Patent: September 22, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic
  • Patent number: 5145846
    Abstract: 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: Grant
    Filed: April 10, 1991
    Date of Patent: September 8, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, deceased, Bernard M. Hennessy, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
  • Patent number: 5134123
    Abstract: 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: Grant
    Filed: March 3, 1989
    Date of Patent: July 28, 1992
    Assignee: Hoffman-La Roche Inc.
    Inventors: Quirico Branca, Werner Neidhart, Henri Ramuz, Heinz Stadler, Wolfgang Wostl
  • Patent number: 5120722
    Abstract: 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: Grant
    Filed: March 19, 1990
    Date of Patent: June 9, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Andrew D. Batcho, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 5106981
    Abstract: 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: Grant
    Filed: April 19, 1990
    Date of Patent: April 21, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5104569
    Abstract: 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: Grant
    Filed: March 27, 1990
    Date of Patent: April 14, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frans Leenhouts, Alois Villiger
  • Patent number: 5087619
    Abstract: 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: Grant
    Filed: March 23, 1990
    Date of Patent: February 11, 1992
    Assignee: 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: 5082842
    Abstract: 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: Grant
    Filed: October 16, 1989
    Date of Patent: January 21, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ulrich Widmer
  • Patent number: 5073550
    Abstract: 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: Grant
    Filed: August 28, 1990
    Date of Patent: December 17, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erwin Gotschi
  • Patent number: 5057614
    Abstract: 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: Grant
    Filed: February 6, 1989
    Date of Patent: October 15, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter D. Davis, Christopher H. Hill, Geoffrey Lawton
  • Patent number: 5057530
    Abstract: 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: Grant
    Filed: May 19, 1989
    Date of Patent: October 15, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller