Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
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Patent number: 6040461Abstract: The invention relates to a process for the preparation of vitamin D.sub.3 compounds of formula I. ##STR1## Wherein A is a single or a double bond; B is a single, cis-double, trans double or a triple bond; R.sub.1 and R.sub.2 are independently hydrogen, a lower alkyl, e.g., a C.sub.1 -C.sub.4 alkyl; R.sub.3 and R.sub.4 are independently a lower alkyl, e.g., C.sub.1 -C.sub.4 alkyl, a hydroxyalkyl, and a haloalkyl, e.g., a fluoroalkyl; and X and Y are independently hydrogen or hydroxy in the case when B is a single or a double bond.Type: GrantFiled: May 11, 1999Date of Patent: March 21, 2000Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)Inventors: Andrew David Batcho, Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 6030976Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.Type: GrantFiled: June 3, 1998Date of Patent: February 29, 2000Assignee: Hoffman-La Roche Inc.Inventors: Michael Bos, Thierry Godel, Claus Riemer, Andrew Sleight
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Patent number: 6030994Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.1 ', R.sup.2, R.sup.2 ' R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein;as well as pharmaceutically acceptable prodrugs or salts of acidic compounds of formula I with bases and or basic compounds of formula I with acids are antiproliferative agents useful in the treatment of cancer.Type: GrantFiled: October 5, 1998Date of Patent: February 29, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Donna Mary Huryn, Dennis Dalton Keith
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Patent number: 6030963Abstract: The invention relates to a compound of the formula ##STR1## wherein A is ##STR2## Et is ethyl, and R is hydroxy and R.sup.1 is hydrogen or .dbd.CH.sub.2 or R is hydrogen or fluoro and R.sup.1 is .dbd.CH.sub.2. Compounds of formula I stimulate HL-60 cell differentiation. Accordingly, the compounds of formula I are useful as agents for the treatment of neoplastic diseases, such as leukemia.Type: GrantFiled: July 31, 1998Date of Patent: February 29, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6025007Abstract: The invention is directed to a cellulose composition useful as a texturizing, thickening, stabilizing, gelling or bulking agent for food systems comprising a combination of (1) a finely divided cellulose component and (2) a surfactant component comprising one or more surfactants, in powder aggregate form; to the use of this agent in lipids and in reduced fat foods; and to the method of making the agent. The invention is also directed to the resulting stabilized lipids, which have viscosity and consistency characteristics that were previously only obtainable with use of stabilizers such as fats that have the undesirable effect of increasing LDL and decreasing HDL.Type: GrantFiled: May 28, 1996Date of Patent: February 15, 2000Assignee: FMC CorporationInventor: Gregory R. Krawczyk
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Patent number: 6008209Abstract: This invention provides a method of treating or preventing neoplastic diseases. The method comprises adminstering to a host in need of such treatment or prevention an effective amount of a Vitamin D.sub.3 analog of the Formula I wherein:X is H.sub.2 or CH.sub.2 ;Y is hydrogen, hydroxy or fluorine;Z is hydroxy;R.sub.1 and R.sub.2 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.1 and R.sub.2 together with C.sub.25 form a (C.sub.3 -C.sub.6) cycloalkyl or cyclofluoroalkyl;R.sub.3 and R.sub.4 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.3 and R.sub.4 together with C.sub.25' form a (C.sub.3 -C.sub.6)cycloalkyl or cyclofluoroalkyl;A is a single bond or a double bond;B.sub.1 is a single bond, an E-double bond, a Z-double bond or a triple bond; andB.sub.2 is a single bond, an E-double bond, a Z-double bond or a triple bond; or a prodrug thereof.Type: GrantFiled: April 16, 1998Date of Patent: December 28, 1999Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 6005098Abstract: Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;R.sup.2 is --(CH.sub.2).sub.n -cycloalkyl wherein cycloalkyl contains 3 to 5 carbon atoms and n is an integer from 0 to 4, heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), aralkylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino)-(lower-alkyl) wherein the alkylene chain is unsubstituted or substituted with one or two lower-alkyl group(s); andR.sup.3 is iodo, or a vinyl or ethynyl group which group is unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, cycloalkyl, aralkyl, carbocyclic aromatic ring and heteorcyclic aromatic ring.Type: GrantFiled: January 20, 1999Date of Patent: December 21, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
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Patent number: 5998665Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.Type: GrantFiled: June 3, 1998Date of Patent: December 7, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Claus Riemer, Andrew Sleight
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Patent number: 5994569Abstract: Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula ##STR1## wherein A is a single or double bond,B.sup.1 and B.sup.2 are each independently CH.dbd.CH or C.tbd.C,T is CH.sub.2 or CH.sub.2 CH.sub.2,X 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 lower alkyl or CF.sub.3, orC(R.sup.2,R.sup.3) is C.sub.3-6 -cycloalkyl,are useful in the treatment or prevention of vitamin D dependent disorders and of IL-12-dependent autoimmune diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, multiple sclerosis, transplant rejection, graft vs. host disease, rheumatoid arthritis, insulin-dependent diabetes mellitus, inflammatory bowel disease, septic shock and allergic encephalomyelitis.Type: GrantFiled: July 14, 1998Date of Patent: November 30, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Peter Mohr, Marc Muller, Christopher Self
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Patent number: 5976600Abstract: A pure, smooth microcrystalline cellulose bulking agent for oil containing foods such as nut butters, chocolates, cream containing foods, mayonnaise, and salad dressings. The bulking agent having a loose bulk density greater than 0.40 and a oil absorptivity of less than 1.0.Type: GrantFiled: September 28, 1994Date of Patent: November 2, 1999Assignee: FMC CorporationInventors: Thomas A. Ruszkay, Donald Elliott
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Patent number: 5965070Abstract: A process for fractionating agaroid compositions by dissolving the agaroid in a glycol, precipitating a first fraction by cooling and precipitating a second fraction by incorporating a nonsolvent to form two fractions substantially more soluble in water than the initial agaroid. Optionally the solubility of either fraction can be converted to conventional solubilities.Type: GrantFiled: September 5, 1997Date of Patent: October 12, 1999Assignee: FMC CorporationInventor: Richard B. Provonchee
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Patent number: 5958910Abstract: 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: GrantFiled: November 20, 1998Date of Patent: September 28, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Stephan Rover
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Patent number: 5958956Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.Type: GrantFiled: January 15, 1998Date of Patent: September 28, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5955495Abstract: The invention is concerned with the use of compounds of the general formula ##STR1## wherein R.sup.1 -R.sup.4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R.sup.1 and R.sup.2 together signify the group --O--(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 --O-- andR.sup.5 signifies hydrogen or hydroxy,as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.Type: GrantFiled: April 14, 1997Date of Patent: September 21, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Heinz Stadler, Jurgen Wichmann
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Patent number: 5952344Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula ##STR1## wherein A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.Type: GrantFiled: January 19, 1998Date of Patent: September 14, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Anne Bourson, Bernd Buttelmann, Gunther Fischer, Marie-Paule Heitz Neidhart, Vincent Mutel, Emmanuel Pinard, Stephan Rover, Gerhard Trube, Rene Wyler
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Patent number: 5939408Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, fluorine, or hydroxyl, each R.sub.2 is lower alkyl or C(R.sub.3).sub.3 and R.sub.3 is halogen, X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2, and A is --C.tbd.C-- ##STR2## or --CH.sub.2 --CH.sub.2 --, which are useful in the treatment of hyperproliferative skin disorders, neoplastic diseases, and sebaceous gland diseases.Type: GrantFiled: September 29, 1998Date of Patent: August 17, 1999Assignee: Hoffman-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 5939451Abstract: The present invention is concerned with compounds of formula ##STR1## wherein Z is a substituted indolyl group of formula ##STR2## R.sup.1 is hydrogen, amino, lower alkylamino, lower dialkylamino, lower alkyl, halogen, or trifluoromethyl;R.sup.2 is hydrogen or lower alkyl;R.sup.11 is hydrogen or halogen;R.sup.12 is hydrogen or lower alkyl; anda is a single or double bond;or a pharmaceutically acceptable salt.Type: GrantFiled: June 4, 1997Date of Patent: August 17, 1999Assignee: Hoffmann-la Roche Inc.Inventors: Michael Bos, Claus Riemer, Andrew Sleight
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Patent number: 5932599Abstract: The present invention is concerned with compounds of formula ##STR1## wherein Z is a substituted pyridyl group of formula ##STR2## R.sup.1 is hydrogen, amino, lower alkylamino, lower dialkylamino, lower alkyl, halogen, or trifluoromethyl;R.sup.2 is hydrogen or lower alkyl;R.sup.5 is hydrogen, lower alkyl, lower alkylamino, di-lower alkylamino, lower alkoxy, or halogen;R.sup.6 lower alkylamino, di-lower alkylamino, lower alkoxy, halogen, or CF.sub.3.Type: GrantFiled: June 3, 1998Date of Patent: August 3, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Thierry Godel, Claus Riemer, Andrew Sleight
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Patent number: 5919903Abstract: A recombinant human IL-12 receptor complex produced on the surface of a non-human mammalian cell and free from other human proteins, 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. 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 or the recombinant human IL-12 receptor complex, which cell proliferates in the presence of human IL-12. A non-human mammalian cell having the human IL-12 beta2 receptor protein or the complex expressed 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: GrantFiled: August 19, 1997Date of Patent: July 6, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Ulrich Andreas Gubler, David Howard Presky
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Patent number: H1838Abstract: Compounds for control of insects and arcarids are disclosed and exemplified which are N-(arylalkyl)-4-[bis(substituted aryl)hydroxymethyl]azabicyclo[3.3. 1 .]nonanes and [3.2.1.]octanes, including N-oxides thereof, N-(substituted-oxy) derivatives thereof, and agriculturally acceptable salts thereof, having the formula: ##STR1## Certain novel intermediates for these pesticidal compounds are also disclosed.Type: GrantFiled: December 16, 1998Date of Patent: February 1, 2000Assignee: FMC CorporationInventors: Thomas G. Cullen, Ian Robert Silverman, Walter H. Yeager