Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
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Patent number: 6564083Abstract: A method of identifying, for a patient having pain of a joint, susceptibility to developing progressive osteoarthritis or loss of joint space, by determining in such patient the presence or absence of bone marrow edema about or of the joint. A determination of the presence of bone marrow edema about or of the joint identifies the patient as susceptible to developing progressive osteoarthritis or loss of joint space.Type: GrantFiled: December 12, 2001Date of Patent: May 13, 2003Assignee: Hoffmann-La Roche Inc.Inventor: Randall Marion Stevens
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Patent number: 6506755Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.Type: GrantFiled: January 23, 2001Date of Patent: January 14, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Hans-Willi Krell, Sabine Woelle, Hans-Peter Wolff
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Patent number: 6498252Abstract: Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.Type: GrantFiled: September 29, 2000Date of Patent: December 24, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
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Patent number: 6455279Abstract: A process for the production of a naturally folded eukaryotic polypeptide containing two or several cysteines linked by disulfide bridges by a) culturing prokaryotic cells in which the said prokaryotic cells contain an expression vector which codes for the said polypeptide which contains a prokaryotic signal sequence at the N-terminus, b) secreting the polypeptide into the periplasm or the medium, c) cleaving the signal sequence and isolating the polypeptide from the periplasm or the medium, which is characterized in that a nucleic acid coding for a molecular chaperone is additionally expressed in the said prokaryotic cell and the chaperone is secreted into the periplasm, is suitable for the recombinant production of polypeptides in prokaryotes in a high yield.Type: GrantFiled: July 19, 2000Date of Patent: September 24, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Dorothee Ambrosius, Rainer Rudolph, Joerg Schaeffner, Elisabeth Schwarz
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Patent number: 6452028Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R1 is ethyl, propyl, butyl, isopropyl or t-butyl, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—. These compounds are useful for the treatment of hyperproliferative disorders, skin diseases, and sebaceous gland diseases.Type: GrantFiled: August 25, 2000Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6444829Abstract: The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.Type: GrantFiled: July 6, 2001Date of Patent: September 3, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Eric Argirios Kitas
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Patent number: 6440099Abstract: A hypodermic needleless injection system for injecting a liquid medication, which system comprises: a medication unit configured and dimensioned to store a volume of liquid to be injected, the medication unit having a first region and a second region that are in liquid communication with each other, the first region being deformable and the second region having at least one orifice, a hydrostatic chamber containing a hydrostatic pressure transfer medium, the hydrostatic chamber being so configured and dimensioned that the medication unit is located at least partially within the hydrostatic chamber and so that a pressure exerted on the transfer medium would cause the first region of the medication unit to deform so as to reduce the volume available for the liquid medication within the medication unit, and a first piston having a first end and a second end opposite to the first end, the first end having a surface which forms a closure of the hydrostatic chamber, and is adapted for applying a pressure on the traType: GrantFiled: February 12, 2001Date of Patent: August 27, 2002Assignee: Roche Diagnostics GmbHInventors: Hans-Peter Haar, Hans List, George Bevan Kirby Meacham
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Patent number: 6437118Abstract: The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) wherein Ra is hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II wherein R21 is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3 is bromo, chloro or iodo, and R1 is as above, with a vinyl borane compound in the presence of a Pd complex and a base, and optionally, further reacting a product of formula I wherein R2 is hydrogen with a compound of the formula IV wherein Rb is a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.Type: GrantFiled: May 23, 2000Date of Patent: August 20, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Püntener, Michelangelo Scalone
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Patent number: 6331642Abstract: Compounds of the formula wherein R1 is hydrogen or an alkyl group; R2 is hydrogen or an alkyl group; or R1, R2 and C20 together are cyclopropyl; R3 is alkyl, hydroxy-alkyl or fluoroalkyl; and R4 is alkyl, hydroxy-alkyl or fluoroalkyl which are useful in the treatment of breast cancer, prostate cancer, myeloid leukemia benign prostate growth, baldness and osteoporosis.Type: GrantFiled: May 24, 2000Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Milan Radoje Uskokovic
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Patent number: 6329538Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R2 is independently H or halogen, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—, provided that when A is —CH2—CH2—, R2 is H.Type: GrantFiled: August 25, 2000Date of Patent: December 11, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6316633Abstract: The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) wherein R1 is (C1-C6) alkyl or benzyl, and the novel intermediates used therein.Type: GrantFiled: October 30, 2000Date of Patent: November 13, 2001Assignee: Hoffman-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 6310247Abstract: Novel trienoic retinoid compounds of with apoptotic activity useful for the prevention and treatment of cancer.Type: GrantFiled: December 14, 1999Date of Patent: October 30, 2001Assignee: Hoffmann-LA Roche Inc.Inventors: Adrian Wai-Hing Cheung, Stephen B. Ferguson, Louise Helen Foley, Allen John Lovey
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Patent number: 6307051Abstract: New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.Type: GrantFiled: January 31, 2000Date of Patent: October 23, 2001Assignee: Roche Diagnostics GmbHInventors: Walter-Gunar Friebe, Bernhard Koenig, Hans-Willi Krell, Sabine Woelle
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Patent number: 6294548Abstract: Invented are improved multidose aqueous formulations of endo-N-(9-methyl-9-azabicyclo[3.3.1.]non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride.Type: GrantFiled: April 13, 2000Date of Patent: September 25, 2001Assignee: Hoffmann-La Roche Inc.Inventor: Susan James
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Patent number: 6281356Abstract: Disclosed are substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds.Type: GrantFiled: December 15, 2000Date of Patent: August 28, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Norman Kong, Allen John Lovey
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Patent number: 6268498Abstract: A process for preparing granisetron by cyclising a compound of structure (2).Type: GrantFiled: March 23, 2000Date of Patent: July 31, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Neal Ward, David Alan Jones, Victor Witold Jacewicz
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Patent number: 6268499Abstract: The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof comprisingepoxidation of a compound of formula 2 or a salt thereof wherein A, R1 and R2 are as herein defined. These compounds are useful in the synthesis of renin inhibitors.Type: GrantFiled: July 13, 1999Date of Patent: July 31, 2001Assignee: Hoffman-La Roche Inc.Inventors: Rolf Güller, Bruno Lohri, Rudolf Schmid
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Patent number: 6265578Abstract: A compound of formula I wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy, or a pharmaceutically acceptable salt of an acidic compound of formula I, or a prodrug thereof. The compounds of formula I and their aforementioned salts and prodrugs can be used in the treatment or control of cancer associated with overexpresison of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer. The compounds of the invention are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.Type: GrantFiled: January 17, 2000Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Louise Helen Foley, Robert Edward Palermo, Ping Wang
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Patent number: H2007Abstract: Compounds of the following structure are disclosed as effective insecticides: in which: A and B are independently lower alkyl; U is lower alkylidene, lower alkenylidene, or CH—Z, where Z is hydrogen, lower alkyl, lower cycloalkyl, or phenyl; R is phenyl or a dibenzocyclo(C5-8)alkyl, each optionally substituted, or where R3 and R4 are independently selected from phenyl, optionally substituted with, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkenyl, or phenyl; R1 is selected from a variety of substituents, including 3-R2, where R2 is where D, E, and G are hydrogen, hydroxy, halogen, cyano, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy, nitro, lower haloalkylsuffonyloxy, lower alkylcarboxylato, lower alkylcarbonylamino, lower alkylcarbonyl, lower alkoxycarbonyl, arylcarbonylamino; D and E taken together may form the group —O(CH2)O—; J is hydrogen or lower alkyl; m is 2 or 3, n is 1, 2, or 3; and halogType: GrantFiled: January 9, 1997Date of Patent: December 4, 2001Assignee: FMC CorporationInventors: Ian R. Silverman, Syed F. Ali, Daniel H. Cohen, John W. Lyga, Kirk A. Simmons, Thomas G. Cullen
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Patent number: H2095Abstract: An inulin/colloidal hydrolyzed cellulose composition as a fat substitute. Processes for preparing an inulin/colloidal hydrolyzed cellulose composition by forming a paste or by spray drying. A fat substitute gel. A food containing inulin/colloidal hydrolyzed cellulose.Type: GrantFiled: December 3, 1996Date of Patent: January 6, 2004Assignee: FMC CorporationInventor: Timothy J. Young