Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
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Patent number: 7345062Abstract: Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.Type: GrantFiled: February 25, 2004Date of Patent: March 18, 2008Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Patent number: 7329761Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication.Type: GrantFiled: November 16, 2004Date of Patent: February 12, 2008Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Publication number: 20070259867Abstract: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.Type: ApplicationFiled: November 16, 2006Publication date: November 8, 2007Inventors: Yong Seo Cho, Hyunah Choo, Ae Nim Pae, Joo Hwan Cha, Hun Yeong Koh, Hwa-Sil Kim, Hyewhon Rhim, Seon Hee Seo
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Patent number: 7276529Abstract: Methods of treating, managing or preventing exercise-induced asthma are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione alone or in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms are also disclosed.Type: GrantFiled: March 28, 2006Date of Patent: October 2, 2007Assignee: Celgene CorporationInventors: George W. Muller, Peter H. Schafer, Patricia E. W. Rohane
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Patent number: 7244759Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.Type: GrantFiled: July 28, 2004Date of Patent: July 17, 2007Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 7223784Abstract: The invention relates to compounds for the modulation of the glycolysis enzyme complex and of the transaminase complex, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases.Type: GrantFiled: July 11, 2003Date of Patent: May 29, 2007Assignee: ScheBo® Biotech AGInventors: Erich Eigenbrodt, Hans Scheefers, Sybille Mazurek
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7208516Abstract: Methods of treating, managing or preventing psoriatic arthritis are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione alone or in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms are also disclosed.Type: GrantFiled: March 28, 2006Date of Patent: April 24, 2007Assignee: Celgene CorporationInventors: George W. Muller, Peter H. Schafer, Patricia E. W. Rohane
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Patent number: 7199081Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2–10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5–10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4–20% of at least one inorganic solid carrier; and d) 3–20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.Type: GrantFiled: February 28, 2005Date of Patent: April 3, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Christian Schlatter, Ravi Ramachandran
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Patent number: 7173058Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: GrantFiled: December 29, 2003Date of Patent: February 6, 2007Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Patent number: 7173059Abstract: Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.Type: GrantFiled: May 4, 2004Date of Patent: February 6, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Kim Francis Albizati, Srinivasan Babu
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Patent number: 7157078Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: February 2, 2004Date of Patent: January 2, 2007Assignee: The University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garren, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 7119105Abstract: The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (?-protein); and (iv) methods for treating neurodegenerative diseases.Type: GrantFiled: February 5, 2004Date of Patent: October 10, 2006Assignee: The Regents of the University of CaliforniaInventors: Jonathan A. Ellman, Gary Lynch, Irwin D. Kuntz, Xiaoning Bi, Christina E. Lee, A. Geoffrey Skillman, Tasir Haque
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Patent number: 7115624Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.Type: GrantFiled: September 11, 2000Date of Patent: October 3, 2006Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Thomas Kruse Hansen, Lars Fogh Iversen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
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Patent number: 7067550Abstract: The invention involves identification of a mechanism of ?-amyloid peptide cytotoxicity, which enables treatment of conditions caused by ?-amyloid peptide aggregates by administration of compounds which antagonize the mechanism of cytotoxicity. The invention includes the identification and isolation of compounds which can reduce the neurotoxic effects of such aggregates. Methods for treating conditions resulting from neurotoxic ?-amyloid peptide aggregates, such as Alzheimer's disease and pharmaceutical preparations are provided. Also provided are methods for selecting additional compounds which can reduce the neurotoxic effects of ?-amyloid aggregates.Type: GrantFiled: May 10, 2002Date of Patent: June 27, 2006Assignee: Massachusetts Institute of TechnologyInventors: Vernon M. Ingram, Barbara J. Blanchard, Brent R. Stockwell
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6962940Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.Type: GrantFiled: March 19, 2003Date of Patent: November 8, 2005Assignee: Celgene CorporationInventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
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Patent number: 6911464Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.Type: GrantFiled: March 12, 2004Date of Patent: June 28, 2005Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller
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Patent number: 6900194Abstract: Novel 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives, use of substituted 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives as Matrix Metalloprotease Inhibitors for the Treatment of Respiratory Diseases, pharmaceutical compositions containing them, and a process for using them. The compounds of the invention have the generalized formula (I) (T)xA—B—D—E—CO2H wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group, x is 0, 1, or 2; the group D represents (a), (b), (c), or (d); the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.Type: GrantFiled: December 20, 1999Date of Patent: May 31, 2005Assignee: Bayer AktiengesellschaftInventors: Mary F. Fitzgerald, Philip J. Gardiner, Kevin Nash, Graham Sturton, Günter Benz, Rolf Henning, Karl-Heinz Schlemmer, Bernd Riedl, Helmut Haning, Lorenz Mayr
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Patent number: 6884754Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5-10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4-20% of at least one inorganic solid carrier; and d) 3-20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.Type: GrantFiled: September 27, 2002Date of Patent: April 26, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Christian Schlatter, Ravi Ramachandran
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Patent number: 6875760Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: GrantFiled: August 30, 2002Date of Patent: April 5, 2005Assignee: Novo Nordisk A/SInventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jøgensen, Janos Tibor Kodra, Shenghua Shi
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6844359Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2-Phthalimido-3-(3?,4?-dimethoxyphenyl)propane.Type: GrantFiled: March 25, 2002Date of Patent: January 18, 2005Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Publication number: 20040254214Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples inlcude, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.Type: ApplicationFiled: March 12, 2004Publication date: December 16, 2004Inventors: Hon-Wah Man, George W. Muller, Weihong Zhang
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Publication number: 20040248964Abstract: The present invention relates to norketamine and ketamine/norketamine prodrugs, and methods of their use as analgesics. More particularly, the invention relates to norketamine and N-conjugated prodrugs of ketamine and norketamine, and methods of using these agents for the management of chronic pain without requiring administration of narcotics. The invention relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine and/or ketamine/norketamine prodrugs effective to alleviate pain to a subject suffering from pain. Uses of norketamine and ketamine/norketamine prodrugs would also apply, to treating headaches, drug abuse, mood and anxiety disorders, as well as other neuropsychiatric disorders, both motoric and cognitive, such as Alzheimer's disease, Parkinson's syndrome, which are thought to be caused by neurodegeneration.Type: ApplicationFiled: November 18, 2003Publication date: December 9, 2004Inventors: Peter A. Crooks, Miguel Rivera
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Publication number: 20040248963Abstract: This invention relates to synthetic excitatory amino acid prodrugs of formula (I) wherein the residues R11, R12 and R13 are as defined in claim 1. The invention further relates to processes for the preparation of the compounds of formula (I), and to pharmaceutical compositions for the treatment of neurological and psychiatric disorders comprising said compounds.Type: ApplicationFiled: April 30, 2004Publication date: December 9, 2004Inventors: Ana Belen Bueno Melendo, Alfonso De Dios, Carmen Dominguez-Fernandez, Mark Francis Herin, Luisa Maria Martin-Cabrejas, Jose Alfredo Martin, Maria Angeles Martinez-Grau, Steven Marc Massey, James Allen Monn, Carlos Montero Salgado, Concepcion Pedregal-Tercero, Matthew John Valli
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Publication number: 20040235848Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &agr;4 integrin in which &agr;4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Applicant: Ajinomoto Co., Inc.Inventors: Tatsuya Okuzumi, Kazuyuki Sagi, Toshihiko Yoshimura, Yuji Tanaka, Eiji Nakanishi, Miho Ono, Masahiro Murata
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Patent number: 6821960Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: GrantFiled: November 16, 2001Date of Patent: November 23, 2004Assignee: Noyo Nordisk Pharmaceuticals, Inc.Inventors: Anker Steen Jørgensen, Peter Madsen
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Publication number: 20040229871Abstract: This invention relates to phthalimido derivatives of the formula 1Type: ApplicationFiled: September 9, 2003Publication date: November 18, 2004Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20040214869Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: May 11, 2004Publication date: October 28, 2004Applicant: WyethInventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Publication number: 20040167199Abstract: Enantiomerically pure (−)-3-(3,4-dimethoxy-phenyl)-3-(1-oxo-1,3-dihydro-isoindol-2-yl)-propionamide, prodrugs, metabolites, polymorphs, salts, solvates, and clathrates thereof are discussed. Methods of treating and/or preventing various diseases and disorders, such as those ameliorated by the reduction of levels of TNF-&agr; or the inhibition of PDE4, are also disclosed.Type: ApplicationFiled: November 17, 2003Publication date: August 26, 2004Applicant: Celgene CorporationInventors: George W. Muller, Roger Shen-Chu Chen
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Publication number: 20040167174Abstract: Imido and amido substituted acyihydroxamidic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin -2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.Type: ApplicationFiled: February 25, 2004Publication date: August 26, 2004Applicant: CelgeneInventors: Hon-Wah Man, George W. Muller, Shaei Y. Huang
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Publication number: 20040147587Abstract: The invention relates to compounds for the modulation of the glycolysis enzyme complex and of the transaminase complex, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases.Type: ApplicationFiled: July 11, 2003Publication date: July 29, 2004Applicant: ScheBo Biotech AGInventors: Erich Eigenbrodt, Hans Scheefers, Sybille Mazurek
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Publication number: 20040147588Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an &agr;-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF&agr; and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.Type: ApplicationFiled: October 14, 2003Publication date: July 29, 2004Inventors: Hon-Wah Man, George W. Muller
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Publication number: 20040127545Abstract: The invention provides new and useful analogs of 2-phthalimidinoglutaric acid. These analogs include DL-2-methyl-2-phthalimidinoglutaric acid and hydroxylated analogs of 2-phthalimidinoglutaric. The invention also provides processes for making these analogs. The invention also provides the two individual enantiomers of DL-2-methyl-2-phthalimidinoglutaric acid, (R) (+)-2-methyl-2-phthalimidinoglutaric acid and (S)-(−)-2-methyl-2-phthalimidinoglutaric acid, and processes for separating these individual enantiomers from the racemate. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering one or more of these compounds.Type: ApplicationFiled: December 9, 2003Publication date: July 1, 2004Applicant: Childrens' Medical CorporationInventors: Robert J. D'Amato, Shawn J. Green, John W. Madsen, William Fogler, Glenn M. Swartz, Adonia E. Papathanassiu, Jamshed H. Shah
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Publication number: 20040122030Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: ApplicationFiled: October 21, 2003Publication date: June 24, 2004Inventor: Milton L. Brown
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Publication number: 20040082603Abstract: 2,3-Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B.Type: ApplicationFiled: July 22, 2003Publication date: April 29, 2004Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20040077685Abstract: A number of thalidomide metabolites having superior anti-angiogenic properties have now been isolated and identified In addition, thalidomide analogs that mimic the effects of the isolated and identified active thalidomide metabolites, and variations of such thalidomide analogs, have been developed. Such thalidomide analog compounds show enhanced potency in the inhibition of undesirable angiogenesis without the undesirable effects of administration of thalidomide.Type: ApplicationFiled: November 14, 2003Publication date: April 22, 2004Inventors: William D. Figg, Kurt Eger, Uwe Teubert, Michael Weiss, Michael Guetschow, Thomas Hecker, Sunna Hauschildt
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Patent number: 6716421Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: March 5, 2001Date of Patent: April 6, 2004Assignee: University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 6706744Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: GrantFiled: November 16, 2001Date of Patent: March 16, 2004Assignee: Novo Nordisk A/SInventors: Peter Madsen, Jesper Lau, Anthony Ling
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Publication number: 20040048917Abstract: 1Type: ApplicationFiled: May 1, 2003Publication date: March 11, 2004Inventors: Arne Eek, Johan Raud
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Publication number: 20040044052Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: ApplicationFiled: February 24, 2003Publication date: March 4, 2004Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Publication number: 20040024045Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: ApplicationFiled: February 24, 2003Publication date: February 5, 2004Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
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Patent number: 6673965Abstract: A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.Type: GrantFiled: July 16, 2002Date of Patent: January 6, 2004Assignee: SmithKline Beecham P.L.C.Inventors: John Gerard Ward, Andrew Faller
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Patent number: 6673790Abstract: The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.Type: GrantFiled: October 2, 2002Date of Patent: January 6, 2004Assignee: Sanofi-SynthelaboInventors: Loïc Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gérard Valette
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Patent number: 6667316Abstract: A compound of formula I wherein each of R1 and R2, independently of the other, is alkyl, alkoxy, cyano, cycloalkoxy, cycloalkyl or cycloalkylmethoxy; one of X and X′ is ═C═O or ═SO2 and the other of X and X′ is a divalent group selected from ═C═O, ═CH2, ═SO2 or ═CH2C═O; R3 is —SO2—Y, —COZ, —CN, or hydroxyalkyl in which Y is alkyl, phenyl, or benzyl and Z is —NR6″R7″, alkyl, phenyl, or benzyl; one of R4 and R5 is hydrogen and the other of R4 and R5 is imidazolyl, pyrrolyl; oxadiazolyl, triazolyl, or R6R7N(CzH2z)— wherein R6, when taken independently of R7, is cycloalkanoyl which is unsubstituted or substituted with halo, amino, monoalkylamino or dialkylamino; and R7 is hydrogen, alkyl of 1 to 4 carbon atoms, methylsufonyl; or alkoxyalkylcarbonyl.Type: GrantFiled: November 8, 2000Date of Patent: December 23, 2003Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030229128Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, type 1 diabetes, type 2 diabetes, disorders of the lipid metabolism and obesity.Type: ApplicationFiled: December 18, 2002Publication date: December 11, 2003Inventors: Peter Madsen, Carsten Behrens