Patents Issued in January 14, 2003
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Patent number: 6506714Abstract: An aqueous, clear, cleansing composition comprising (a) a cleansing effective amount of a potassium salt of a long chain alkyl carboxylic acid or mixture thereof, the pH of said composition being from about 10.0 to about 11.0.Type: GrantFiled: October 31, 2000Date of Patent: January 14, 2003Assignee: Colgate-Palmolive CompanyInventors: Zenaida Soriano, Ma. Theresa Lumain
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Patent number: 6506715Abstract: An automobile wash and wax composition suitable for simultaneously washing and waxing a soiled exterior surface of a vehicle without buffing. The automotive wash and wax composition being an aqueous emulsion containing an anionic surfactant, a silicone oil, an amino-functional silicone, a wax, and a cationic emulsifier. The wash and wax composition is applied to a pre-wetted exterior surface of a vehicle so as to substantially coat the surface of the vehicle that requires cleaning and polishing. After the coated surface has substantially dried, the surface is washed with a sufficient quantity of water to rinse away the soil particles and the residue of the anionic surfactant, leaving behind a durable, evenly distributed, high-gloss, water resistant protective film of silicones and wax on the vehicle surface, without any buffing of the surface.Type: GrantFiled: January 10, 2002Date of Patent: January 14, 2003Assignee: Turtle Wax, Inc.Inventors: Michael A. Schultz, Denis John Healy
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Patent number: 6506716Abstract: The present invention relates to stable, aqueous heavy duty gel laundry detergent compositions comprising anionic surfactants, fatty acids, and detersive amines. The anionic surfactant component comprises alkyl ethoxylated sulfates and fatty acids.Type: GrantFiled: January 19, 2000Date of Patent: January 14, 2003Assignee: The Procter & Gamble CompanyInventors: Patrick Firmin August Delplancke, Francesco de Buzzaccarini, Abdennaceur Fredj, Pramod Kakumanu Reddy, Robert Walter Boswell, Eugene Steven Sadlowski
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Patent number: 6506717Abstract: The present invention relates to surfactant mixtures, improved detergent and cleaning products containing particular types of modified alkylbenzenesulfonate surfactants.Type: GrantFiled: July 19, 2001Date of Patent: January 14, 2003Assignee: The Procter & Gamble CompanyInventors: Kevin Lee Kott, Jeffrey John Scheibel, Roland George Severson, Thomas Anthony Cripe, James Charles Theophile Roger Burckett-St. Laurent, William Michael Scheper, Chandrika Kasturi
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Patent number: 6506718Abstract: The present invention relates to liquid hypohalite bleach-containing compositions which comprise an alkyl ethoxy sulphate having a low number of moles of ethoxy groups.Type: GrantFiled: February 28, 2001Date of Patent: January 14, 2003Assignee: The Procter & Gamble CompanyInventor: Oreste Todini
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Patent number: 6506719Abstract: A light duty, liquid comprising: a C8-C18 ethoxylated alkyl ether sulfate surfactant, a magnesium salt of a C8-C18 linear alkyl benzene sulfonate, a sodium salt of a C8-C18 linear alkyl benzene sulfonate, a zwitterionic surfactant, a polyalkylglucoside, a preservative, a perfume and water.Type: GrantFiled: July 15, 2002Date of Patent: January 14, 2003Assignee: Colgate-Palmolive CompanyInventors: Evangelia S. Arvanitidou, Barbara Thomas, Gary Jakubicki, Gregory Szewczyk
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Patent number: 6506720Abstract: A process for making a detergent tablet by forming a disintegrating agent by compacting cellulose or a cellulose derivative, forming disintegrating agent particles comprising the disintegrating agent, dry mixing a washing- or cleaning-active substance and an amount of the disintegrating agent particles effective to rapidly dissolve or disperse the composition in water, and shaping the resulting mixture into a tablet. The disintegrating agent particles have a particle size distribution of less than 10% by weight smaller than about 0.2 mm particle size and no more than 1% by weight of dust-fine particles.Type: GrantFiled: September 3, 1999Date of Patent: January 14, 2003Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Gerhard Blasey, Dieter Jung, Hans-Friedrich Kruse, Fred Schambil
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Patent number: 6506721Abstract: A novel composition having the formula: wherein R1 is selected from the group consisting of an alkyl group containing from 1 to 20 carbon atoms and an aryl group, and R2 is selected from the group consisting of an alkyl group containing from 1 to 20 carbon atoms and an aryl group. The composition is made by combining an amine compound, a carbonyl compound, a solvent, and a sulfur-containing compound. The composition is used as a detergent additive in cleaning process.Type: GrantFiled: September 22, 2000Date of Patent: January 14, 2003Assignee: Phillips Petroleum CompanyInventors: Mitchell D. Refvik, David W. Dockter
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Patent number: 6506722Abstract: The invention relates to cogranulates comprising phyllosilicates and disintegrants, in particular cellulose, and to detergents and cleaners which comprise these cogranulates, preferably in tablet form.Type: GrantFiled: September 11, 2000Date of Patent: January 14, 2003Assignee: Clariant GmbHInventors: Harald Bauer, Josef Holz, Guenther Schimmel, Armelle Pelissou
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Patent number: 6506723Abstract: Described is a single phase aqueous surfactant-free nontoxic air freshening composition containing 30-70% water, 5-20% of a fragrance, at least 60% of the components of which has a C log10 P≦2.5 and 30-60 weight percent of a mixture of two glycol ether components: (i) dipropylene glycol methyl ether; and (ii) propylene glycol propyl ether or propylene glycol butyl ether. Also described is an air freshener device comprising a vessel for the aforementioned composition, an emanating surface and a wick for supplying the composition to the emanating surface. In another embodiment of the invention is a stain removal wipe, which contains a fragrant aqueous system with low solvent and substantially free of surfactant.Type: GrantFiled: August 2, 2000Date of Patent: January 14, 2003Assignee: International Flavors & Fragrances Inc.Inventors: Arnoud Van Walsum, Jan-Willem Zacharias Ruizendaal, Richard M. Boden, Andrew John Crossman, Michael John Robert White
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Patent number: 6506724Abstract: Methods for treating gestational diabetes which comprise administration of an effective amount of an exendin or an exendin agonist, alone or in conjunction with other compounds or compositions that lower blood glucose levels.Type: GrantFiled: June 1, 1999Date of Patent: January 14, 2003Assignee: Amylin Pharmaceuticals, Inc.Inventors: Richard A. Hiles, Kathryn S. Prickett
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Patent number: 6506725Abstract: A blood substitute and plasma expander comprising a cross-linked, substantially endotoxin-free hemoglobin solution and process for preparing same. The process comprises fractionating whole blood, separating out a stromal-free, sterile hemoglobulin solution, chromatographically separating endotoxins from said hemoglobin solution and crosslinking the resulting endotoxin-free hemoglobin solution.Type: GrantFiled: May 10, 1999Date of Patent: January 14, 2003Assignee: BioPure CorporationInventors: Carl W. Rausch, Mario Feola
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Patent number: 6506726Abstract: A method is described for separating and purifying a wide variety of fermentation cyclopeptide products containing at least one protonatable amino group (including the deacylated Echinocandin-type compounds) from their fermentation or mixed broths and partially purified process streams by adsorbing the mixture onto a hydrophobic, reversed phase chromatographic media and eluting with a continuous linear acetic acid gradient ranging from 0.1% acetic acid to 10.0% acetic acid by volume in water. A process for removing tripeptide-aldehyde by-products from the fermentation products by means of a derivatizing agent is also described.Type: GrantFiled: December 10, 2001Date of Patent: January 14, 2003Assignee: Eli Lilly and CompanyInventors: John Robert Dobbins, Eugene Paul Kroeff, Jeffrey Thomas Vicenzi
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Patent number: 6506727Abstract: It has been found that the growth factor PDGF, when used in combination with another growth factor such as IGF-I, acts synergistically with the other factor to promote neuronal regeneration.Type: GrantFiled: February 18, 1994Date of Patent: January 14, 2003Assignee: Institute of Molecular Biology, Inc.Inventors: Hans-Arne Hansson, Samuel E. Lynch, Harry N. Antoniades
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Patent number: 6506728Abstract: A novel polypeptide, designated neurotrophic factor-4 (NT-4), has been identified by PCR amplification of human genomic DNA. Provided herein is nucleic acid encoding NT-4 useful in diagnostics and in the recombinant preparation of NT-4. Also provided herein are nucleic acids encoding naturally occurring amino acid sequence variants of NT-4, designated NT-4&bgr;, NT-4&ggr;, and NT-4&Dgr;. The neurotrophic factors of the invention are useful in the treatment of nerve cells and in diagnostic assays.Type: GrantFiled: May 26, 1995Date of Patent: January 14, 2003Assignee: Genentech, Inc.Inventor: Arnon Rosenthal
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Patent number: 6506729Abstract: Disclosed are therapeutic treatment methods, compositions and devices for maintaining neural pathways in a mammal, including enhancing survival of neurons at risk of dying, inducing cellular repair of damaged neurons and neural pathways, and stimulating neurons to maintain their differentiated phenotype. In one embodiment, the invention provides means for stimulating CAM expression in neurons. The invention also provides means for evaluating the status of nerve tissue, including means for detecting and monitoring neuropathies in a mammal. The methods, devices and compositions include a morphogen or morphogen-stimulating agent provided to the mammal in a therapeutically effective concentration.Type: GrantFiled: September 25, 1997Date of Patent: January 14, 2003Assignee: Curis, Inc.Inventors: David C. Rueger, Kuber T. Sampath, Charles M. Cohen, Hermann Oppermann, Roy H. L. Pang
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Patent number: 6506730Abstract: The present invention relates to a pharmaceutical composition for the nasal transmucosal delivery of a biocompatible polymer-biologically active peptide conjugate. The pharmaceutical composition of the present invention increases the water solubility of peptide, which is sparingly soluble in water, improves its stability by protecting it from being degraded by proteases. As a result, the number of administrations of the drug and the side-effects induced by drug abuse are decreased. In addition, since the pharmaceutical composition of the present invention is delivered through the nasal cavity, it allows drug activity to be expressed in a short period of time and improves a bioavailability.Type: GrantFiled: August 15, 2000Date of Patent: January 14, 2003Inventors: Kang Choon Lee, Myung-Ok Park
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Patent number: 6506731Abstract: The present invention is directed to a composition which is used to enhance the elasticity and/or appearance of tissue. Specifically, the present invention is directed to a composition formulated from peptides having low molecular weights and which substantially correspond to sequences found in elastin More preferably, the present invention corresponds to the general formula R1-Leucine-Glycine-Alanine-Glycine-Glycine-Alanine-Glycine-R2.Type: GrantFiled: May 30, 2000Date of Patent: January 14, 2003Assignee: Connective Tissue Imagineering LLCInventors: Lawrence B. Sandberg, Thomas F. Mitts
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Patent number: 6506732Abstract: The present invention relates to a mixture of soluble hydrophobic peptides of an enzymatic hydrolysate of milk having skin hydrating properties and percutaneous absorption levels of 4 to 5%. The mixture also exhibits wound healing properties but does not have the allergenicity of the milk-protein. One fraction of the mixture is capable of increasing in vitro the growth rate of cell-cultured keratinocytes by at least 50%. The soluble peptides of the fraction have a molecular weight of about 900 daltons ranging from 200 to 1400 daltons, and an average hydrophobicity of 11 Kcal/mole. The soluble peptides are constituted of 66% hydrophobic amino acids and 17% aromatic amino acids, and have aromatic amino acids and other hydrophobic amino acids located at the C- and N-terminal ending in proportion over 85%. Another fraction is capable of increasing the growth rate of cell-cultured fibroblasts by 37% and the production of collagen by 73%.Type: GrantFiled: January 27, 2000Date of Patent: January 14, 2003Assignee: Universite LavalInventor: Jean Amiot
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Patent number: 6506733Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.Type: GrantFiled: March 15, 2000Date of Patent: January 14, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
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Patent number: 6506734Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.Type: GrantFiled: October 27, 1999Date of Patent: January 14, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Lerchen, Karsten von dem Bruch, Jörg Baumgarten, Michael Sperzel
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Patent number: 6506735Abstract: The invention provides optimized antisense oligonucleotides complementary to the DNA methyltransferase gene or its RNA transcript. The invention further provides methods for using such antisense oligonucleotides as analytical and diagnostic tools, as potentiators of transgenic plant and animal studies and gene therapy approaches, and as potential therapeutic agents.Type: GrantFiled: May 22, 2000Date of Patent: January 14, 2003Assignee: Methyl Gene, Inc.Inventor: A. Robert MacLeod
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Patent number: 6506736Abstract: A method for treating a human being having or suspected of having sexual dysfunction or a disorder of physiological and/or anatomical response to sexual stimulation, said dysfunction or disorder involving erectile tissue of genitalia comprising administering the nitrogen monoxide donor arginine and at least on nucleotide selected from the group consisting of AMP or ATP.Type: GrantFiled: July 12, 2000Date of Patent: January 14, 2003Inventor: Philippe Gorny
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Patent number: 6506737Abstract: An oxidizing species is described herein as a reaction product through an in situ preparation combining a protonizable phosphorus or sulfur compound, and a halide source at controlled proportions in an aqueous, non-aqueous, gel, aerosol, solid-phase or powdered media. The oxidizing species can be used to reduce microbial and viral populations on a surface or object or in a body or stream of water. The invention thus finds applications as a bleach, sanitizer, oxidant, or in any other application in which an oxidizing agent can be beneficially used alone or in a formulation.Type: GrantFiled: April 5, 2000Date of Patent: January 14, 2003Assignee: Ecolab, Inc.Inventors: Robert D. P. Hei, Kim Smith
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Patent number: 6506738Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: September 14, 2001Date of Patent: January 14, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Rita Civiello, Keith Combrink, Hatice Belgin Gulgeze, Bradley C. Pearce, Xiangdong Wang, Nicholas A. Meanwell, Yi Zhang
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Patent number: 6506739Abstract: Bis-(N,N′-bis-(2-haloethyl)amino)phosphoramidates, pharmaceutical compositions containing them, methods of treatment using them, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities; and this invention relates to the use of the compounds in methods for the treatment of tumors and, especially, for the treatment of cancer.Type: GrantFiled: May 1, 2001Date of Patent: January 14, 2003Assignee: Telik, Inc.Inventors: R. Jason Herr, Robert T. Lum, Steven R. Schow, Fanying Meng, Michael R. Kozlowski, Pavel Zhichkin
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Patent number: 6506740Abstract: The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted at the 7, 8, and/or 9 positions and methods for preparing the 4-dedimethylamino tetracycline compounds. Other tetracycline compounds are the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N—NH-Alkyl group at the C4 position. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified 4-dedimethylamino tetracycline compounds.Type: GrantFiled: May 18, 2000Date of Patent: January 14, 2003Inventors: Robert A. Ashley, Joseph J. Hlavka
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Patent number: 6506741Abstract: An object of the present invention is to provide pharmaceutical compositions for inhibiting mesangial cell proliferation or mesangial matrix production without causing hypercalcemia. According to the present invention, therapeutic agents for glomerulosclerosis containing 1&agr;,3&bgr;-dihydroxy-20&agr;-(3-hydroxy-3-methylbutyloxy)-9,10-seco-5,7,10 (19)-pregnatriene as an active ingredient are provided.Type: GrantFiled: November 13, 2001Date of Patent: January 14, 2003Inventor: Toshio Doi
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Patent number: 6506742Abstract: This invention provides a convenient process for preparing an oral contraceptive liquid formulation having improved solubility, bioavailability and stability useful as a reference standard.Type: GrantFiled: December 1, 2000Date of Patent: January 14, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: George Wong, Shifeng Wei, Herling Uang
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Patent number: 6506743Abstract: Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen, an unsubstituted or substituted C1-C3-C6alkyl, C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: December 11, 2001Date of Patent: January 14, 2003Assignee: Syngenta Investment CorporationInventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Patent number: 6506744Abstract: Compounds of formula I as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations for the treatment or prevention of neoplasms, tumor metastasis, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: July 7, 2000Date of Patent: January 14, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Alexander Chucholowski, Thomas Weller
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Patent number: 6506745Abstract: The present invention relates to a medical composition for atrial fibrillation treatment, comprising a compound represented by the following formula [I]: Formula [I] [wherein R1 represents a hydrogen atom or lower alkoxy group; R2 represents a hydrogen atom, lower alkoxy group or phenyl group (wherein the phenyl group may be substituted with 1 to 3 substituents selected from a group consisting of a hydroxides group and a lower alkoxy group), (wherein R3 represents an acyl group); X represents —CO— or —CH2—, and n represents an integer of 1 or 2.] The present invention also relates to a method of treating atrial fibrillation using said compound, and to the use of said compound for producing a medicine for atrial fibrillation treatment or salts thereof or prodrugs thereof.Type: GrantFiled: June 28, 2001Date of Patent: January 14, 2003Assignee: Noboru KanekoInventors: Kazuo Aisaka, Naoya Imagawa, Hisato Miyai, Satoshi Ogawa
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Patent number: 6506746Abstract: The invention provides a method of treating a cognitive dysfunction comprising administering an effective amount of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno(2,3-b][1,5]benzodiazepine.Type: GrantFiled: November 25, 1997Date of Patent: January 14, 2003Assignee: Eli Lilly and CompanyInventor: Charles M Beasley, Jr.
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Patent number: 6506747Abstract: 1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.Type: GrantFiled: June 3, 1999Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Charles L. Cywin, Karl Hargrave, Mary Ann Hoermann, Thomas M. Kirrane, Thomas M. Parks, Usha R. Patel, John R. Proudfoot, Rajiv Sharma, Sanxing Sun, Xiao-Jun Wang
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Patent number: 6506748Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: June 26, 2001Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Eugene R. Hickey, John R. Regan
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Patent number: 6506749Abstract: The present invention provides compounds of the formula: wherein R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-alkyl, optionally substituted heterocyclyl, spiro-substituted cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl (wherein n is 1 or 2), or —SO2Ar2; and R1, R3, and Ar1 are those defined herein, and methods for preparation and uses thereof.Type: GrantFiled: August 30, 2001Date of Patent: January 14, 2003Assignee: Syntex (U.S.A.) LLCInventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
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Patent number: 6506750Abstract: N-(phenylacetyl)morpholine derivatives useful as NK1 receptor antagonists, a process for the preparation thereof, and pharmaceutical compositions containing them as active principle.Type: GrantFiled: September 24, 2001Date of Patent: January 14, 2003Assignee: Sanofi-SynthelaboInventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
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Patent number: 6506751Abstract: Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.Type: GrantFiled: November 2, 2000Date of Patent: January 14, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Stephanie Elizabeth Ault Justus, Helen Tsenwhei Lee, Jason Keith Pontrello, Bruce David Roth, Karen Elaine Sexton, Michael William Wilson
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Patent number: 6506753Abstract: The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone.Type: GrantFiled: June 11, 2001Date of Patent: January 14, 2003Assignee: Sepracor, Inc.Inventors: Thomas P. Jerussi, Chrisantha H. Senanayake, Paul D. Rubin, Yaping Hong, Roger A. Bakale, Tingjian Xiang, Fran A. McConville
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Patent number: 6506754Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and which feature a six member heterocyclic ring having two ring nitrogen atoms and the remainder of the ring atoms carbon atoms at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.Type: GrantFiled: April 14, 2000Date of Patent: January 14, 2003Assignee: Corvas International, Inc.Inventors: Daniel Vanna Siev, Gian Luca Araldi, Jonathan Zhanqi Ho, John Eugene Reiner, Joseph Edward Semple
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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: 6506756Abstract: The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.Type: GrantFiled: September 18, 2001Date of Patent: January 14, 2003Assignee: Schering CorporationInventors: Neng-Yang Shih, Daniel M. Solomon, John J. Piwinski, Andrew T. Lupo, Jr., Michael J. Green
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Patent number: 6506757Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 11, 2000Date of Patent: January 14, 2003Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 6506758Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxType: GrantFiled: October 11, 2001Date of Patent: January 14, 2003Assignees: SmithKline Beecham Laboratoires Pharmceutiques, SmithKline Beecham SpAInventors: Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler, Pietro A T Novella
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Patent number: 6506759Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 31, 2000Date of Patent: January 14, 2003Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
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Patent number: 6506760Abstract: Compounds of the invention are active as inhibitors of Thrombin and are useful in treating disease states in mammals which are characterized by abnormal thrombosis and have the following structure: as described herein.Type: GrantFiled: April 14, 2000Date of Patent: January 14, 2003Assignee: Corvas International, Inc.Inventors: Gian Luca Araldi, Joseph Edward Semple
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Patent number: 6506761Abstract: Compound of the invention are active as inhibitors of Thrombin and are useful in treating disease states in mammals which are characterized by abnormal thrombosis and have the following structure: as described herein.Type: GrantFiled: April 14, 2000Date of Patent: January 14, 2003Assignee: Corvas International, Inc.Inventors: Gian Luca Araldi, Joseph Edward Semple
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Patent number: 6506762Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: September 29, 2000Date of Patent: January 14, 2003Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 6506763Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: July 30, 2001Date of Patent: January 14, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6506764Abstract: Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y (I) have therapeutic utility as inhibitors of metalloproteinases etc.Type: GrantFiled: September 6, 2000Date of Patent: January 14, 2003Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, Duncan Hannah, John Gary Montana