Sulfur Attached Directly To Urea Nitrogen By Nonionic Bonding Patents (Class 514/592)
  • Patent number: 6919310
    Abstract: 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: Grant
    Filed: March 3, 2003
    Date of Patent: July 19, 2005
    Assignee: CPD, LLC
    Inventor: Anton H. Clemens
  • Patent number: 6911457
    Abstract: 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: Grant
    Filed: April 11, 2003
    Date of Patent: June 28, 2005
    Assignee: Carbomer, Inc.
    Inventor: Manssur Yalpani
  • Patent number: 6822001
    Abstract: 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: Grant
    Filed: November 2, 2001
    Date of Patent: November 23, 2004
    Assignee: Tularik Inc.
    Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
  • Patent number: 6818765
    Abstract: 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: Grant
    Filed: October 16, 2001
    Date of Patent: November 16, 2004
    Assignee: Universite de Liege
    Inventors: Jacques Delarge, Jean-Michel Dogne, Bernard Masereel
  • Patent number: 6794414
    Abstract: 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: Grant
    Filed: September 6, 2001
    Date of Patent: September 21, 2004
    Assignee: Yeda Research and Development Co. Ltd.
    Inventor: Lawrence Steinman
  • Publication number: 20040176420
    Abstract: 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: Application
    Filed: March 15, 2004
    Publication date: September 9, 2004
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Robin Edwin Buckingham, Stephen Alistair Smith
  • Publication number: 20040175421
    Abstract: 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: Application
    Filed: March 5, 2004
    Publication date: September 9, 2004
    Inventors: Suresh Kumar Gidwani, Purushottam Sharshikant Singnurkar
  • Publication number: 20040157927
    Abstract: 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: Application
    Filed: November 26, 2003
    Publication date: August 12, 2004
    Inventor: Peter Ohman
  • Publication number: 20040147564
    Abstract: 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: Application
    Filed: August 16, 2003
    Publication date: July 29, 2004
    Inventors: Vinay U. Rao, Dilip Gopalkrishna Saoji, Sunil Anantrao Mirajkar, Prashant Prabhakarrao Deshmukh, Harshal Prabhakar Bhagwatwar, Manjusha Malhotra, Milind C. Shukla, Noel John De Souza
  • Publication number: 20040147576
    Abstract: 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: Application
    Filed: January 15, 2004
    Publication date: July 29, 2004
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
  • Publication number: 20040147430
    Abstract: 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: Application
    Filed: December 4, 2003
    Publication date: July 29, 2004
    Inventor: Philippe Briet
  • Publication number: 20040122060
    Abstract: 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: Application
    Filed: December 8, 2003
    Publication date: June 24, 2004
    Applicant: SmithKline Beecham p.I.c.
    Inventors: Robin Edwin Buckingham, Stephen Alistair Smith
  • Patent number: 6750253
    Abstract: 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, (C1
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: June 15, 2004
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventor: Erik Rytter Ottosen
  • Publication number: 20040097556
    Abstract: 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: Application
    Filed: November 10, 2003
    Publication date: May 20, 2004
    Applicant: SmithKline Beecham p.l.c.
    Inventor: Stephen Alistair Smith
  • Publication number: 20040092590
    Abstract: 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: Application
    Filed: September 29, 2003
    Publication date: May 13, 2004
    Inventors: Linda Arterburn, Diane Benisek, James Hoffman, Harry Oken, Mary Van Elswyk
  • Publication number: 20040087630
    Abstract: 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: Application
    Filed: June 18, 2003
    Publication date: May 6, 2004
    Inventors: Malcolm Allison, Marjorie Regan Gatlin
  • Publication number: 20040039031
    Abstract: 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: Application
    Filed: May 21, 2003
    Publication date: February 26, 2004
    Inventors: Nathalie Cugnardey, Nicolas Wiernsperger
  • Publication number: 20040034030
    Abstract: 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: Application
    Filed: July 30, 2003
    Publication date: February 19, 2004
    Applicant: ChronoRX LLC
    Inventors: Kenneth T. Richardson, Don C. Pearson
  • Publication number: 20040034016
    Abstract: A diuretic, e.g., loop diuretic or thiazide, or a sulphylurea is useful in the treatment of DNA viral infections.
    Type: Application
    Filed: March 20, 2003
    Publication date: February 19, 2004
    Inventors: Ian Stuart Pardoe, Christopher Edward Hartley
  • Publication number: 20040034065
    Abstract: 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: Application
    Filed: June 16, 2003
    Publication date: February 19, 2004
    Inventors: Malcolm Allison, Marjorie Regan Gatlin
  • Publication number: 20040002442
    Abstract: 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: Application
    Filed: January 16, 2003
    Publication date: January 1, 2004
    Inventors: Clark Pan, James Whelan, Kevin B. Clairmont
  • Publication number: 20040002519
    Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredients
    Type: Application
    Filed: March 21, 2003
    Publication date: January 1, 2004
    Inventors: Robert Edson Damon, Thomas Edward Hughes
  • Publication number: 20030228362
    Abstract: 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: Application
    Filed: April 11, 2003
    Publication date: December 11, 2003
    Applicant: Medical Research Institute
    Inventor: Edward A. Byrd
  • Publication number: 20030219482
    Abstract: 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: Application
    Filed: March 20, 2003
    Publication date: November 27, 2003
    Inventors: Sunil Sudhakar Chaudhari, Dilip Gopalkrishna Saoji, Harshal Prabhakar Bhagwatwar, Manjusha Malhotra, Milind C. Shukla, Noel John De Souza
  • Publication number: 20030216294
    Abstract: 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: Application
    Filed: June 5, 2003
    Publication date: November 20, 2003
    Applicant: Pfizer Inc.
    Inventors: David A. Fryburg, Janice C. Parker
  • Publication number: 20030215889
    Abstract: 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: Application
    Filed: March 20, 2003
    Publication date: November 20, 2003
    Inventors: J. Marc Simard, Mingkui Chen
  • Publication number: 20030212104
    Abstract: 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: Application
    Filed: May 1, 2003
    Publication date: November 13, 2003
    Applicant: Pfizer Inc.
    Inventors: W. Ross Tracey, Judith L. Treadway
  • Publication number: 20030207823
    Abstract: 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: Application
    Filed: April 11, 2003
    Publication date: November 6, 2003
    Inventor: Manssur Yalpani
  • Patent number: 6624117
    Abstract: 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&m
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: September 23, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Michael Heneghan, Roy Alan Kirk, James Philip Taylor, John Whitworth, Robert Montgomery O'Neil, John Barry Henshall
  • Publication number: 20030162816
    Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) 1
    Type: Application
    Filed: January 16, 2003
    Publication date: August 28, 2003
    Inventors: Marjorie Regan Gatlin, Michele Ann Ball, Richard Owen Mannion, Anees Abdulquadar Karnachi, Christiane Guitard, Malcolm Allison
  • Patent number: 6610746
    Abstract: 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: Grant
    Filed: April 10, 2001
    Date of Patent: August 26, 2003
    Assignee: Pfizer Inc.
    Inventors: David A. Fryburg, Janice C. Parker
  • Publication number: 20030139434
    Abstract: 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 mediated
    Type: Application
    Filed: October 10, 2002
    Publication date: July 24, 2003
    Inventors: Bork Balkan, Thomas Edward Hughes, David Grenville Holmes, Edwin Bernard Villhauer
  • Publication number: 20030114357
    Abstract: 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: Application
    Filed: September 27, 2002
    Publication date: June 19, 2003
    Inventors: David A. Fryburg, Solomon S. Klioze, Patrice M. Milos, Peter J. Oates
  • Publication number: 20030114389
    Abstract: 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: Application
    Filed: November 8, 2002
    Publication date: June 19, 2003
    Inventor: Randy Lee Webb
  • Publication number: 20030100504
    Abstract: 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: Application
    Filed: October 15, 2002
    Publication date: May 29, 2003
    Applicant: GENENTECH, INC.
    Inventors: Venita I. DeAlmeida, Timothy A. Stewart
  • Patent number: 6566304
    Abstract: 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: Grant
    Filed: February 6, 2001
    Date of Patent: May 20, 2003
    Assignee: Cognis Deutschland GmbH
    Inventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
  • Publication number: 20030087814
    Abstract: 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: Application
    Filed: November 4, 2002
    Publication date: May 8, 2003
    Inventor: Seth Lederman
  • Publication number: 20030083385
    Abstract: The present invention is directed to the use of a benzenesulfonyl(thiourea or urea) of formula I 1
    Type: Application
    Filed: June 24, 2002
    Publication date: May 1, 2003
    Inventors: Uwe Gerlach, Klaus Wirth, Heinrich Christian Englert, Heinz Gogelein
  • Publication number: 20030083259
    Abstract: 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: Application
    Filed: August 22, 2002
    Publication date: May 1, 2003
    Inventors: Suad Efendic, Mark Gutniak, Ole Kirk
  • Publication number: 20030077335
    Abstract: 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: Application
    Filed: November 2, 2001
    Publication date: April 24, 2003
    Applicant: ChronoRX LLC
    Inventors: Kenneth T. Richardson, Don C. Pearson
  • Publication number: 20030073728
    Abstract: A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.
    Type: Application
    Filed: July 5, 2001
    Publication date: April 17, 2003
    Inventors: Paul D. van Poelje, Mark D. Erion, Toshihiko Fujiwara
  • Publication number: 20030073614
    Abstract: 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: Application
    Filed: October 17, 2001
    Publication date: April 17, 2003
    Inventors: Ira G. Schulman, Eric D. Bischoff, Rajendra K. Tangirala
  • Patent number: 6511989
    Abstract: 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: Grant
    Filed: November 2, 2001
    Date of Patent: January 28, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Holger Heitsch, Heinrich Christian Englert
  • Patent number: 6468963
    Abstract: 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: Grant
    Filed: May 1, 2000
    Date of Patent: October 22, 2002
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Aulma Parker, Susan E. Hamilton
  • Publication number: 20020123494
    Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1
    Type: Application
    Filed: November 2, 2001
    Publication date: September 5, 2002
    Inventors: Holger Heitsch, Heinrich Christian Englert
  • Patent number: 6433009
    Abstract: 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: Grant
    Filed: October 31, 2000
    Date of Patent: August 13, 2002
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, James Frederick Eggler
  • Patent number: 6414030
    Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I in which R1, R2, E, X, Y and Z have the meanings described herein, show effects on the autonomous nervous system. The invention relates to the use of the compounds of the formula I in the treatment and prophylaxis of dysfunctions of the autonomous nervous system, in particular of vagal dysfunctions, for example in the case of cardiovascular diseases. The invention also relates to the use of compounds of the formula I in combination with beta-receptor blockers and to products and pharmaceutical preparations which comprise at least one compound of the formula I and at least one beta-receptor blocker, and to novel compounds.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: July 2, 2002
    Assignee: Aventis Pharma Deutschland, GmbH
    Inventors: Klaus Wirth, Heinrich Christian Englert, Helmut Bohn, Heinz Gögelein, Holger Heitsch, Uwe Gerlach
  • Patent number: 6410573
    Abstract: Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are suitable for the treatment of cardiovascular disorders, especially the treatment of arrhythmias, prevention of sudden death from heart disease or affect diminished contractility of the heart. The invention also relates to methods for producing compounds of formula (I), the use thereof and pharmaceutical preparations containing said compounds.
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: June 25, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Holger Heitsch, Heinrich Christian Englert, Heinz Gögelein
  • Patent number: 6399824
    Abstract: Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by reaction of a compound II with guanidine.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: June 4, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Armin Hofmeister, Max Hropot, Uwe Heinelt, Markus Bleich, Hans-Jochen Lang
  • Publication number: 20020045636
    Abstract: 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 &mgr;-agonist activity or combination thereof, and an insulin secretagogue.
    Type: Application
    Filed: June 11, 2001
    Publication date: April 18, 2002
    Applicant: CPD, LLC
    Inventor: Anton H. Clemens