Sulfur Attached Directly To Urea Nitrogen By Nonionic Bonding Patents (Class 514/592)
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Patent number: 7285574Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: GrantFiled: April 5, 2005Date of Patent: October 23, 2007Assignee: University of Maryland, BaltimoreInventors: J. Marc Simard, Mingkui Chen
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Patent number: 7241756Abstract: A method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in need thereof.Type: GrantFiled: June 1, 2006Date of Patent: July 10, 2007Assignee: SmithKline Beecham CorporationInventors: Jonathan Robert Sanders Arch, James Martin Lenhard
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Patent number: 6992106Abstract: The present invention provides composition having as active ingredients a stilbene derivative and a platinum coordination compound which is highly efficacious and highly safe for treating tumors, particularly for the treatment of solid or malignant tumors and thus methods of cancer and tumor treatment using the composition are also provided.Type: GrantFiled: June 12, 2002Date of Patent: January 31, 2006Assignee: Ajinomoto Co., Inc.Inventors: Yoshihiro Morinaga, Yukio Nihei, Yasuyo Suga, Manabu Suzuki, Kazuo Ohishi, Akira Okano
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Patent number: 6951844Abstract: New thyroid receptor ligands are provided which have the general formula I wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: September 21, 2004Date of Patent: October 4, 2005Assignee: Bristol Myers Squibb CompanyInventor: Jon J. Hangeland
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Patent number: 6919310Abstract: The invention provides an improved method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome. The method includes administering, by a pharmaceutically effective mode, a drug composition having an opioidergic agent including an opiate antagonist, opiate having ?-agonist activity or combination thereof, and an insulin secretagogue.Type: GrantFiled: March 3, 2003Date of Patent: July 19, 2005Assignee: CPD, LLCInventor: Anton H. Clemens
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Patent number: 6911457Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.Type: GrantFiled: April 11, 2003Date of Patent: June 28, 2005Assignee: Carbomer, Inc.Inventor: Manssur Yalpani
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Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Patent number: 6818765Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.Type: GrantFiled: October 16, 2001Date of Patent: November 16, 2004Assignee: Universite de LiegeInventors: Jacques Delarge, Jean-Michel Dogne, Bernard Masereel
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Patent number: 6794414Abstract: Diseases Mediated by transglutaminase, such as Huntington's Disease, spinobulbar atrophy, spinocerebellar ataxia, and dentatorubralpallidoluysian atrophy, as well as inflammatory diseases of the central nervous system, including mautiple sclerosis, rheumatoid arthritis, and insulin dependent diabetes mellitus, can be treated by administering a transglutaminase inhibitor such as monadansyl cadaverine, monoamines and diamines such as cystamine, putrescine, GABA. (gamma-amino benzoic acid), N-benzyloxy carbonyl, 5-deazp-4-oxonorvaline p-nitrophenylester, glycine methyl ester, CuSO4, and the oral anti-hyperglycemic agent tolbutamide.Type: GrantFiled: September 6, 2001Date of Patent: September 21, 2004Assignee: Yeda Research and Development Co. Ltd.Inventor: Lawrence Steinman
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Publication number: 20040176420Abstract: A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a sub-maximal amount of an insulin secretagogue, to a mammal in need thereof; and a pharmaceutical composition for use in such method.Type: ApplicationFiled: March 15, 2004Publication date: September 9, 2004Applicant: SmithKline Beecham p.l.c.Inventors: Robin Edwin Buckingham, Stephen Alistair Smith
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Publication number: 20040175421Abstract: The present invention relates to a simple and easy method for the preparation of solid oral dosages of the combination of metformin and glyburide. Specifically, glyburide is homogenized in an organic solution whereby about 8 to 15% w/w of glyburide goes into solution and form a slurry. The resulted slurry is then sprayed onto pharmaceutical excipients or metformin granules, and the solid oral dosage of metformin and glyburide is formed. The present invention further relates to the solid oral dosages prepared by the disclosed process, and the method of treating non-insulin dependent diabetes by administering to a patient in need thereof a solid oral dosage prepared by the current invention.Type: ApplicationFiled: March 5, 2004Publication date: September 9, 2004Inventors: Suresh Kumar Gidwani, Purushottam Sharshikant Singnurkar
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Publication number: 20040157927Abstract: A pharmaceutical combination comprising either (S)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy)phenyl]propanoic acid or 3-{4-[4-tert-butoxycarbonylaminophenyl)ethoxy]phenyl}-(S)-2-ethoxy propanoic acid, or a pharmaceutically-acceptable salt thereof and any solvates of either thereof and a sulfonylurea.Type: ApplicationFiled: November 26, 2003Publication date: August 12, 2004Inventor: Peter Ohman
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Publication number: 20040147576Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 15, 2004Publication date: July 29, 2004Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Publication number: 20040147564Abstract: A unit-dose pharmaceutical composition for the treatment of non-insulin dependent diabetes mellitus includes a combination of glimepiride and a thiazolidinedione insulin sensitizer, providing for the simultaneous release of each drug at rates substantially similar to those obtained with the separate administration of immediate release dosage forms of glimepiride and the thiazolidinedione. In addition, processes for the preparation of such combination unit-dose compositions and the use of such compositions for improving glycemic control are described.Type: ApplicationFiled: August 16, 2003Publication date: July 29, 2004Inventors: Vinay U. Rao, Dilip Gopalkrishna Saoji, Sunil Anantrao Mirajkar, Prashant Prabhakarrao Deshmukh, Harshal Prabhakar Bhagwatwar, Manjusha Malhotra, Milind C. Shukla, Noel John De Souza
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Publication number: 20040147430Abstract: The invention concerns the use of at least an antidiabetic selected among compounds stimulation insulin secretion, glucosidase inhibitors, thiazolidine-diones, insulin, agents enhancing insulin sensitivity, the glucagon-like peptide-1 (GLP-1), PPAR&agr;/&ggr; agonists, meglitinide and aP2 inhibitors for making a medicine with cicatrizing effect.Type: ApplicationFiled: December 4, 2003Publication date: July 29, 2004Inventor: Philippe Briet
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Publication number: 20040122060Abstract: A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitizer, an insulin secretagogue and a biguanide antihyperglycaemic agent, to a mammal in need thereof; and composition for use in such method.Type: ApplicationFiled: December 8, 2003Publication date: June 24, 2004Applicant: SmithKline Beecham p.I.c.Inventors: Robin Edwin Buckingham, Stephen Alistair Smith
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Patent number: 6750253Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1Type: GrantFiled: February 22, 2002Date of Patent: June 15, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Publication number: 20040097556Abstract: A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and an insulin secretagogue, to a mammal in need thereof.Type: ApplicationFiled: November 10, 2003Publication date: May 20, 2004Applicant: SmithKline Beecham p.l.c.Inventor: Stephen Alistair Smith
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Publication number: 20040092590Abstract: This invention is directed to methods of treating patients with metabolic syndrome, prediabetes and/or Type II diabetes mellitus by administering docosahexaenoic acid (DHA) alone or in combination with diabetes-related medications.Type: ApplicationFiled: September 29, 2003Publication date: May 13, 2004Inventors: Linda Arterburn, Diane Benisek, James Hoffman, Harry Oken, Mary Van Elswyk
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Publication number: 20040087630Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) HMG-Co-A reductase inhibitors or a pharmaceutically acceptable salt thereof; and (ii) ACE inhibitors or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 18, 2003Publication date: May 6, 2004Inventors: Malcolm Allison, Marjorie Regan Gatlin
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Publication number: 20040039031Abstract: The present invention relates to the field of therapeutic chemistry and more particularly to the preparation of novel medicinal products for treating diabetes. Specifically, a subject of the invention is novel antidiabetic medicinal products consisting of a combination of two active principles that are effective via the oral route, at subliminal doses, formed from an antidiabetic biguanide and an antidiabetic sulfonamide, in combination or as a mixture with one or more inert, pharmaceutically acceptable excipients. The invention also relates to a process for the preparation of such medicinal products formed from a biguanide and a sulfonamide.Type: ApplicationFiled: May 21, 2003Publication date: February 26, 2004Inventors: Nathalie Cugnardey, Nicolas Wiernsperger
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Publication number: 20040034016Abstract: A diuretic, e.g., loop diuretic or thiazide, or a sulphylurea is useful in the treatment of DNA viral infections.Type: ApplicationFiled: March 20, 2003Publication date: February 19, 2004Inventors: Ian Stuart Pardoe, Christopher Edward Hartley
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Publication number: 20040034065Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredients (i) an AT1-receptor antagonist or a pharmaceutically acceptable salt thereof; (ii) (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof or (b) an insulin sensitizer or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 16, 2003Publication date: February 19, 2004Inventors: Malcolm Allison, Marjorie Regan Gatlin
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Publication number: 20040034030Abstract: The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of biguanides (metformin) and/or sulfonylureas in the prevention and treatment of insulin resistance and diabetes mellitus, alone or in combination, as a nutrient for humans. The carefully chosen active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and with the clinical use of biguanides (metformin) and/or the sulfonylureas. These modules are: (1) Mitochondrial Metabolic Group, (2) Plasma and Mitochondrial Membrane Integrity Group, (3) Nocturnal Group and, (4) Insulin Alternative Group. When used in concert with a biguanide, a sulfonylurea or with a combination of both, the invention will broaden the clinical usefulness of these drugs.Type: ApplicationFiled: July 30, 2003Publication date: February 19, 2004Applicant: ChronoRX LLCInventors: Kenneth T. Richardson, Don C. Pearson
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Publication number: 20040002519Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredientsType: ApplicationFiled: March 21, 2003Publication date: January 1, 2004Inventors: Robert Edson Damon, Thomas Edward Hughes
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Publication number: 20040002442Abstract: The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.Type: ApplicationFiled: January 16, 2003Publication date: January 1, 2004Inventors: Clark Pan, James Whelan, Kevin B. Clairmont
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Publication number: 20030228362Abstract: A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials provide for gradual release of the lipoic acid in a manner which makes it possible to substantially increase the period of time over which therapeutic levels of lipoic acid are maintained relative to a quick release formulation. These features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired therapeutic results.Type: ApplicationFiled: April 11, 2003Publication date: December 11, 2003Applicant: Medical Research InstituteInventor: Edward A. Byrd
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Publication number: 20030219482Abstract: A pharmaceutical composition suitable for a once-a-day dosing regimen includes a combination of a biguanide and a sulfonylurea in the form of a multiparticulate, polyphasic system for the treatment of non-insulin dependent diabetes mellitus (NIDDM) and for improving glycemic control.Type: ApplicationFiled: March 20, 2003Publication date: November 27, 2003Inventors: Sunil Sudhakar Chaudhari, Dilip Gopalkrishna Saoji, Harshal Prabhakar Bhagwatwar, Manjusha Malhotra, Milind C. Shukla, Noel John De Souza
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Publication number: 20030216294Abstract: The present invention provides methods of treating non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance, the methods comprising the step of administering to a patient having or at risk of having non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance a synergistic amount of: 1) a sulfonylurea, a non-sulfonylurea K+ ATP channel blocker, or a sulfonylurea and a non-sulfonylurea K+ ATP channel blocker; and 2) a cAMP phosphodiesterase type 3 inhibitor.Type: ApplicationFiled: June 5, 2003Publication date: November 20, 2003Applicant: Pfizer Inc.Inventors: David A. Fryburg, Janice C. Parker
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Publication number: 20030215889Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: ApplicationFiled: March 20, 2003Publication date: November 20, 2003Inventors: J. Marc Simard, Mingkui Chen
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Publication number: 20030212104Abstract: This invention relates to methods of treating or preventing type 2 diabetes, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic microangiopathy, diabetic macroangiopathy, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury and/or insulin resistance syndrome (IRS) in mammals, particularly in humans, by administering a sodium-hydrogen exchanger type 1 (NHE-1) inhibitor or a pharmaceutical composition containing such an inhibitor. This invention also relates to combinations comprising NHE-1 inhibitors and a second pharmaceutical agent, said combinations being useful in treating type 2 diabetes, IRS, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury, diabetic microangiopathy and/or diabetic macroangiopathy.Type: ApplicationFiled: May 1, 2003Publication date: November 13, 2003Applicant: Pfizer Inc.Inventors: W. Ross Tracey, Judith L. Treadway
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Publication number: 20030207823Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.Type: ApplicationFiled: April 11, 2003Publication date: November 6, 2003Inventor: Manssur Yalpani
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Patent number: 6624117Abstract: A heat sensitive recording material, comprising a) at least one colour forming compound, and b) at least one developer of the formula wherein R1 is unsubstituted or substituted phenyl, naphthyl or C1-C20alkyl, X is a group of the formula A is unsubstituted or substituted phenylene, naphthylene or C1-C12alkylene, or is an unsubstituted or substituted heterocyclic group, B is a linking group of formula —O—SO2—, —SO2—O—, —NH—SO2—, —SO2—NH—, —S—SO2—, —O—CO—, —O—CO—NH—, —NH—CO—, —NH—CO—O—, —S—CO—NH—, —S—CS—NH—, —CO—NH—SO2—, —O—CO—NH—SO2—, —NH═CH—, —CO—NH—CO—, —S—, —CO—, —O—, —SO2—NH—CO—, —O&mType: GrantFiled: October 1, 2001Date of Patent: September 23, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Michael Heneghan, Roy Alan Kirk, James Philip Taylor, John Whitworth, Robert Montgomery O'Neil, John Barry Henshall
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Publication number: 20030162816Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) 1Type: ApplicationFiled: January 16, 2003Publication date: August 28, 2003Inventors: Marjorie Regan Gatlin, Michele Ann Ball, Richard Owen Mannion, Anees Abdulquadar Karnachi, Christiane Guitard, Malcolm Allison
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Patent number: 6610746Abstract: The present invention provides methods of treating non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance, the methods comprising the step of administering to a patient having or at risk of having non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance a synergistic amount of:1) a sulfonylurea, a non-sulfonylurea K+ ATP channel blocker, or a sulfonylurea and a non-sulfonylurea K+ ATP channel blocker; and 2) a cAMP phosphodiesterase type 3 inhibitor.Type: GrantFiled: April 10, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: David A. Fryburg, Janice C. Parker
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Publication number: 20030139434Abstract: The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further antidiabetic compound, preferably selected from the group consisting of insulin signalling pathway modulators, like inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), compounds influencing a dysregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, &agr;-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and &agr;2-adrenergic antagonists, for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediatedType: ApplicationFiled: October 10, 2002Publication date: July 24, 2003Inventors: Bork Balkan, Thomas Edward Hughes, David Grenville Holmes, Edwin Bernard Villhauer
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Publication number: 20030114389Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof and at least one antidiabetic agent.Type: ApplicationFiled: November 8, 2002Publication date: June 19, 2003Inventor: Randy Lee Webb
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Publication number: 20030114357Abstract: This invention relates to methods of characterizing subjects and methods of treatment or prevention of diseases and pathological conditions relating to the polymorphic A-C repeat sequence located approximately 2.1 kb upstream from the aldose reductase gene.Type: ApplicationFiled: September 27, 2002Publication date: June 19, 2003Inventors: David A. Fryburg, Solomon S. Klioze, Patrice M. Milos, Peter J. Oates
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Publication number: 20030100504Abstract: Dickkopf-5 (Dkk-5) protein is administered in effective amounts to treat disorders involving insulin resistance, such as non-insulin-dependent diabetes mellitus (NIDDM) or obesity. Also provided is a method of diagnosing insulin resistance and related disorders using Dkk-5 as a measure, and kits for diagnosis and treatment, as well as hybridomas producing antibodies to Dkk-5 and preparations comprising Dkk-5.Type: ApplicationFiled: October 15, 2002Publication date: May 29, 2003Applicant: GENENTECH, INC.Inventors: Venita I. DeAlmeida, Timothy A. Stewart
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Patent number: 6566304Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.Type: GrantFiled: February 6, 2001Date of Patent: May 20, 2003Assignee: Cognis Deutschland GmbHInventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
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Publication number: 20030087814Abstract: Compositions and methods for treating, preventing, or reducing alcoholism, in particular methods for increasing patient compliance with therapies that require the intake of an ALDH inhibitor comprising the step of administering a monoamine oxidase B inhibitor.Type: ApplicationFiled: November 4, 2002Publication date: May 8, 2003Inventor: Seth Lederman
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Publication number: 20030083385Abstract: The present invention is directed to the use of a benzenesulfonyl(thiourea or urea) of formula I 1Type: ApplicationFiled: June 24, 2002Publication date: May 1, 2003Inventors: Uwe Gerlach, Klaus Wirth, Heinrich Christian Englert, Heinz Gogelein
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Publication number: 20030083259Abstract: The invention employs GLP-1 (7-37), GLP-1(7-36)amide, and certain related compounds in combination with an oral hypoglycaemic agent for treating diabetes mellitus.Type: ApplicationFiled: August 22, 2002Publication date: May 1, 2003Inventors: Suad Efendic, Mark Gutniak, Ole Kirk
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Publication number: 20030077335Abstract: The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of biguanides (metformin) and/or sulfonylureas in the prevention and treatment of insulin resistance and diabetes mellitus, alone or in combination, as a nutrient for humans. The carefully chosen active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and with the clinical use of biguanides (metformin) and/or the sulfonylureas. These modules are: (1) Mitochondrial Metabolic Group, (2) Plasma and Mitochondrial Membrane Integrity Group, (3) Nocturnal Group and, (4) Insulin Alternative Group. When used in concert with a biguanide, a sulfonylurea or with a combination of both, the invention will broaden the clinical usefulness of these drugs.Type: ApplicationFiled: November 2, 2001Publication date: April 24, 2003Applicant: ChronoRX LLCInventors: Kenneth T. Richardson, Don C. Pearson
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Publication number: 20030073728Abstract: A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.Type: ApplicationFiled: July 5, 2001Publication date: April 17, 2003Inventors: Paul D. van Poelje, Mark D. Erion, Toshihiko Fujiwara
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Publication number: 20030073614Abstract: The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXR&bgr; selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXR&agr;-selective antagonist.Type: ApplicationFiled: October 17, 2001Publication date: April 17, 2003Inventors: Ira G. Schulman, Eric D. Bischoff, Rajendra K. Tangirala
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Patent number: 6511989Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: November 2, 2001Date of Patent: January 28, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6468963Abstract: Formulations and methods for reducing the unwanted toxicity and complications associated with treatments for diabetes mellitus. The formulations include co-formulations of an anti-diabetic agent and a toxicity reducing agent of the formula described in the specification. The methods include administration of effective amounts of the anti-diabetic agent and the toxicity reducing agent to safely treat the diabetic patient.Type: GrantFiled: May 1, 2000Date of Patent: October 22, 2002Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Aulma Parker, Susan E. Hamilton
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Publication number: 20020123494Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1Type: ApplicationFiled: November 2, 2001Publication date: September 5, 2002Inventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6433009Abstract: A compound of the formula wherein R1 and R2 are as defined above, useful in the treatment and condition selected from the group consisting of meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation, tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzheimers disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including a human.Type: GrantFiled: October 31, 2000Date of Patent: August 13, 2002Assignee: Pfizer IncInventors: Mark Anthony Dombroski, James Frederick Eggler