Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
  • Patent number: 5919986
    Abstract: Compounds of formula I: ##STR1## wherein the dotted carbon-carbon bond in the D-ring is C--C or C.dbd.C; C(R,R) is CH.sub.2 or C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently C.sub.1-4 -alkyl or CF.sub.3, or together with the carbon to which they are bound form C.sub.3-6 -cycloalkyl.are useful in the treatment of vitamin D dependent disorders, such as psoriasis, leukemia; acne and seborrhoic dermatitis; osteoporosis hyperparathyroidism accompanying renal failure; and multiple sclerosis.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: July 6, 1999
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Pierre Barbier, Franz Bauer, Peter Mohr, Marc Muller, Wolfgang Pirson
  • Patent number: 5905074
    Abstract: A compound of the formula ##STR1## useful for treating vitamin D dependent disorders.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: May 18, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Fernand Schneider
  • Patent number: 5904148
    Abstract: Delayed release flavorant compositions containing flavor-release additives, namely 1,2-diols of the formula ##STR1## wherein R.sup.1 is one of the radicals ##STR2## where R.sup.2 is H, lower alkylR.sup.3, R.sup.4 are H, lower alkyl, lower alkoxy, hydroxy, or R.sup.3 +R.sup.4 together are methylenedioxy,R.sup.5 is lower alkyland the broken lines represent in the ring one additional bondand in the side chain an optional bond.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: May 18, 1999
    Assignee: Givaduan-Roure (International) SA
    Inventor: Denise Anderson
  • Patent number: 5891901
    Abstract: Compounds of the formula ##STR1## wherein R is alkyl, alkylthio or hydroxy, as well as, pharmaceutically acceptable salts of compounds of formula I are antiproliferative agents useful in the treatment of cancer.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: April 6, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urvashi Hooda Dhingra, Donna Mary Huryn, Dennis Dalton Keith, Giuseppe Federico Weber
  • Patent number: 5888994
    Abstract: A compound of formula I ##STR1## wherein R is hydrogen, fluorine or hydroxy, and X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2 which are useful in the treatment of hyperproliferative disorders, neoplastic diseases and sebaceous gland diseases.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: March 30, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernard Michael Hennessy, Milan Radoje Uskokovic
  • Patent number: 5880285
    Abstract: A process for the manufacture of optically active (R)- or (S)-1-(4-methoxy-benzyl)-1,2,3,4,5,6,7,8-octahydro-isoquinoline adducts of the formula ##STR1## wherein HX signifies a mineral acid from the group of HBF.sub.4, H.sub.2 SO.sub.4, HPF.sub.6, HBr, HI, HCl,HSbF.sub.6 or HClO.sub.4, or a strong organic acid from the group of C.sub.1-8 -alkylSO.sub.3 H, picric acid, formic acid, a lower alkylsulphonic acid or arylcarboxylic acid or a dicarboxylic acid,from a compound of the formula ##STR2## wherein HX has the significance given above, by asymmetric hydrogenation in the presence of a complex consisting of optically active diphosphine ligands with iridium, optionally in the presence of an additive.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: March 9, 1999
    Assignee: Roche Vitamins Inc.
    Inventors: Emil Albin Broger, Michelangelo Scalone, Christof Wehrli
  • Patent number: 5875586
    Abstract: The invention provides a method and apparatus dispensing a liquid bait in a refillable manner. The invention provides a transparent bait station in which is mounted to a structure. A liquid bait is injected into the bait station to initially fill and then refill the bait station. The bait is a slow acting toxicant and attractant. The bait station is formed to allow access by bugs, but not by larger animals. The bait station is also able to protect the bait from wind and rain. The bait station prevents leakage of the toxicant if the bait station is tumbled or placed in an incorrect position. The bait station is able to hold two different liquid baits, which may be two different poisons, or a poison and an attractant. An embodiment of the bait station provides a series of inner walls to minimize the leakage of liquid bait, if the liquid bait station is tumbled.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: March 2, 1999
    Inventors: James Bruce Ballard, Elleen P. McGorman
  • Patent number: 5877193
    Abstract: The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,R.sup.1 -R.sup.4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: March 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrea Cesura, Stephan Rover
  • Patent number: 5877353
    Abstract: The present invention relates to a process for the preparation of benzophenone derivatives and comprises a selective crystallization of alkali salts of compounds of formula (I) ##STR1## wherein R.sup.1 is lower-alkyl and R.sup.2 is hydrogen, lower-alkyl or halogen,from the isomeric alkali salts of the 3-hydroxy compounds of formula (II), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above.
    Type: Grant
    Filed: January 15, 1998
    Date of Patent: March 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jurg Bruhin
  • Patent number: 5861359
    Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controling weeds are disclosed. The novel herbicidal compounds are optionally substituted phenylmethoxy or phenylmethylthio heterocycles of the formula: ##STR1## in which Q is selected from: ##STR2## R=halogen; R.sup.1 =lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, lower alkylthio, lower sulfonyl, or lower alkylsulfinyl; R.sup.2 =lower alkyl, or lower haloalkyl; X=H, halogen, or lower alkyl; W=O or S; Z, Z.sup.1, Z.sup.2 are independently selected from H, halogen, straight or branched chain lower alkyl, lower alkoxy, is lower haloalkoxy, cyano, lower cyanoalkyloxy, or aryl; or Z and Z.sup.1 are adjacent to each other on the benzene ring, and taken together are --(CH.sub.2).sub.4 --; or Z.sup.2 is OA in the 2-, 3-, or 4-position of the phenyl ring; A is a derivative of an alkanoate bonded to the phenoxy oxygen at the alpha carbon; R.sup.3 is H or lower alkyl; R.sup.
    Type: Grant
    Filed: July 18, 1996
    Date of Patent: January 19, 1999
    Assignee: FMC Corporation
    Inventor: George Theodoridis
  • Patent number: 5856317
    Abstract: 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: Grant
    Filed: May 24, 1996
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benoit Thomas Dore, Richard Lewis Momparler, Milan Radoje Uskokovic
  • Patent number: 5856517
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.1' are independently alkyl, aryl, alkenyl or alkynyl;R.sup.2 and R.sup.2' are independently hydrogen or alkyl;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are ##STR2## CH.sub.2 OR.sup.10, CHO, CH.sub.2 NR.sup.11 R.sup.12, hydrogen, halogen, cyano, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl, provided that at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.7 is cyano, ##STR3## CH.sub.2 OR.sup.10, CH.sub.2 NR.sup.11 R.sup.12, or CHO ; R.sup.8 is alkyl, aralkyl or aryl;R.sup.10 is hydrogen, alkyl, aralkyl or aryl;R.sup.11 and R.sup.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Donna Mary Huryn, Dennis Dalton Keith
  • Patent number: 5852176
    Abstract: Antibodies to human IL-12 beta 2 receptor protein or an IL-12 receptor complex, the complex comprising the beta1 receptor protein complexed with a beta2 receptor protein, which complex is capable of binding to human IL-12 with high affinity.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: December 22, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulrich Andreas Gubler, David Howard Presky
  • Patent number: 5840530
    Abstract: A recombinant human IL-12 beta2 receptor protein produced on the surface of a non-human mammalian cell, free from other human proteins, in its active form. In addition, a non-human mammalian cell having expressed on its surface the recombinant human IL-12 beta2 receptor protein, which cell proliferates in the presence of human IL-12. A non-human mammalian cell having the human IL-12 beta2 receptor protein on its surface and which proliferates in response to human IL-12 is useful for determining whether a given compound inhibits biological activity of human IL-12 or is an IL-12 agonist.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: November 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulrich Andreas Gubler, David Howard Presky
  • Patent number: 5827883
    Abstract: A method of using vitamin D derivatives of the formula ##STR1## wherein X is .dbd.CH.sub.2 or H,H;Y is a moiety--CH(CH.sub.3)--(A).sub.n --C(O)--OR.sup.1 (a)--CH(CH.sub.3)--CH.sub.2 --O--C(O)--R.sup.2 (b)or--C(O)--OR.sup.1 (c);A is --CH.dbd.CH-- or CH.sub.2 --CH.sub.2 --R.sup.1 is lower alkyl, cycloalkyl, cycloalkylmethyl, --CH.sub.2 R.sup.3 or --CH.sub.2 --CH.sub.2 R.sup.3 ;R.sup.2 is lower alkyl, cycloalkyl or R.sup.3 ;R.sup.3 is hydroxy-lower alkyl, hydroxy-cycloalkyl or trifluoromethyl-hydroxy-lower-alkyl;n is 0 or 1;and the dotted bond in the five membered ring is optional;in the treatment of dermatological conditions, in particular keratinization disorders such as psoriasis, as well as acne and photodamaged skin, is described.Vitamin D derivatives of the formula I above, wherein X, Y, A, R.sup.1, R.sup.2, R.sup.3 and n are as set forth above; with the proviso that X is H,H when Y is --CH(CH.sub.3)--CH.sub.2 --OC(O)--C(OH)(CH.sub.3).sub.
    Type: Grant
    Filed: July 21, 1997
    Date of Patent: October 27, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Marc Muller, Josef Stadlwieser
  • Patent number: 5817814
    Abstract: This invention describes a method for preparing benzyluracils using methyl benzylcarbamates as intermediates. The method comprises the steps of contacting an alkali metal salt of an ester of 3-amino-4,4,4-trifluoro-2-butenoic acid with a methyl benzylcarbamate I to provide a benzyluracil II. ##STR1## where R, W, V, X and Y are as described in the specification.
    Type: Grant
    Filed: May 1, 1997
    Date of Patent: October 6, 1998
    Assignee: FMC Corporation
    Inventors: Marvin J. Konz, Harvey R. Wendt
  • Patent number: 5811414
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin, produced by photodamage, which disorders include wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein R is hydrogen, fluorine, or hydroxy, R.sub.2 is hydrogen, lower alkyl or halogen, X is .dbd.CH.sub.2 or when R is hydroxy X is hydrogen or .dbd.CH.sub.2, ##STR2## --CH.sub.2 --CH.sub.2 --, provided that when A is --CH.sub.2 --CH.sub.2 --, R.sub.2 is hydrogen or lower alkyl.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: September 22, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic
  • Patent number: 5804574
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin, produced by photodamage, which disorders include wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein R.sub.1 is hydrogen, hydroxy or fluorine, R.sub.2 is hydrogen or halogen and A is --C.tbd.C--, --C.dbd.C-- or --CH.sub.2 --CH.sub.2 --, provided that when A is --CH.sub.2 --CH.sub.2 --, R.sub.2 is hydrogen.
    Type: Grant
    Filed: September 17, 1997
    Date of Patent: September 8, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic
  • Patent number: 5789004
    Abstract: A stabilizer composition, useful for reduced fat frozen desserts and whipped toppings, containing, as a first component, microcrystalline cellulose coprocessed with guar and, as a second component, microcrystalline cellulose coprocessed with carboxymethylcellulose. The method of using the stabilizer composition provides reduced fat food products, particularly products with less than ten percent fat, with many of the desirable body and textural characteristics of full-fat products.
    Type: Grant
    Filed: December 15, 1995
    Date of Patent: August 4, 1998
    Assignee: FMC Corporation
    Inventors: Daniel T. Hogan, Dale T. Bertrand, Marlene T. Tuazon, Domingo C. Tuason
  • Patent number: H1764
    Abstract: This invention relates to a method for controlling the weeds Papever, Matricharia, Viola, and/or Polygonum in cereal crops comprising the step of applying to the locus where the weed control is desired a herbicidal formulation comprised of a benzyluracil having the formula ##STR1## where V is chlorine; W is chlorine or methoxy; X is hydrogen; Y is chlorine or methoxy; and R is methyl or amino. Preferred benzyluracils are those where R is methyl.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: December 1, 1998
    Assignee: FMC Corporation
    Inventors: Frederick W. Hotzman, James T. Bahr