Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
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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: 7220749Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel compositions comprising at least one COX-2 selective inhibitor, that is optionally sitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: GrantFiled: June 10, 2003Date of Patent: May 22, 2007Assignee: NitroMed, Inc.Inventors: L. Gordon Letts, David S. Garvey
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Patent number: 7208467Abstract: SR-BI is present at relatively high levels on the membranes of hepatocytes and steroidogenic tissues, including the adrenal gland, testes, and ovaries, where it mediates the uptake and transport of cholesteryl ester from high density lipoproteins. It has been demonstrated that transgenic animals which do not produce SR-BI are healthy, with the exception that the females are infertile. SR-BI KO females have abnormal HDLs, ovulate dysfunctional oocytes and are infertile. Surgical, genetic and pharmacologic methods were used to show that the fertility of SR-BI KO females (or their transplanted oocytes) can be restored in the absence of ovarian and/or extraovarian SR-BI expression by manipulations that modify the structure, composition and/or abundance of their abnormal plasma lipoproteins. These manipulations included inactivation of the apolipoprotein A-I gene and administration of the cholesterol-lowering drug PROBUCOL™.Type: GrantFiled: June 7, 2002Date of Patent: April 24, 2007Inventors: Monty Krieger, Helena E. Miettinen
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Patent number: 7189758Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: October 5, 2005Date of Patent: March 13, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David Thomson, Yan Zhang, Renee Michele Zindell
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Patent number: 7189761Abstract: A pharmaceutical composition contains a nitric oxide donor and advantageously an optional corticosteroid and/or topical anesthetic. The composition is useful in a method for treating anal disorders such as anal fissure, anal ulcer, hemorrhoidal disease, levator spasm, and so forth, by topical application to or proximate the affected area.Type: GrantFiled: September 22, 2003Date of Patent: March 13, 2007Inventor: Stephen R. Gorfine
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Patent number: 7179791Abstract: Patients needing NO donor therapy or inhibition of pathologically proliferating cells or increased NO bioactivity are treated with a therapeutically effective amount of an inhibitor of glutathione-dependent formaldehyde dehydrogenase.Type: GrantFiled: January 11, 2001Date of Patent: February 20, 2007Assignee: Duke UniversityInventors: Jonathan S. Stamler, Limin Liu, Alfred Hausladen, Raphael Nudelman
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Patent number: 7169768Abstract: A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease wherein the method involves administering to a human or an animal an amount of an inhibitor of the release of LHRH or GnRH.Type: GrantFiled: June 3, 1998Date of Patent: January 30, 2007Inventors: Kenneth M. Weisman, Michael Goldberg
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Patent number: 7153871Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.Type: GrantFiled: July 18, 2003Date of Patent: December 26, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7129270Abstract: Compounds of Formula 1 are useful in the treatment of inflammation.Type: GrantFiled: October 20, 2005Date of Patent: October 31, 2006Assignee: Schėring AGInventors: Stefan JaRoch, Manfred Lehmann, Norbert Schmees, Bernd Buchmann, Harmur Rehwinkel, Peter Droescher, Werner Skuballa, Konrad Krolikiewicz, Hartwig Hennekes, Heike Schaecke, Arndr Schottelius
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Patent number: 7126012Abstract: The invention concerns compounds of formula (I): R-A-R? wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t-R5 group wherein t and R5 are as defined in the descriptionType: GrantFiled: September 23, 2004Date of Patent: October 24, 2006Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renaud, Philippe Delagrange
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Patent number: 7115252Abstract: A method and composition for the restoration and maintenance of gingival and periodontal health are provided. The composition includes a potassium as an essential ingredient, which acts as an anti-bacterial agent. In some embodiments, the compositions include an osmotic agent other than potassium.Type: GrantFiled: May 13, 2002Date of Patent: October 3, 2006Inventor: Milton Hodosh
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Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 7005428Abstract: Novel methods for the medical treatment and/or inhibition of the development of hypercholesterolemia in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing precursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.Type: GrantFiled: September 24, 1999Date of Patent: February 28, 2006Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6969730Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.Type: GrantFiled: February 25, 2002Date of Patent: November 29, 2005Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
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Patent number: 6964784Abstract: A method for isolating the bioactive component of the water-soluble extract of Uncaria tomentosa known as C-MED-100®, comprising (i) precipitating the spray drying carrier from C-MED-100®; (ii) using the resulting C-MED-100® to obtain a spotting mixture for thin layer chromatography (TLC); (iii) spotting the C-MED-100® spotting mixture on pre-run TLC plates and eluting the plates to obtain the fluorescing band with Rf=0.2-0.3; (iv) scraping off the Rf=0.2-0.3 band, eluting it in ammonia and freeze drying the eluted band to form a powder; and (v) extracting the powder with methanol to remove solubilized silica gel, concentrating the methanol solution and crystalizing the concentrated solution to obtain the bioactive component. The isolated bioactive component is a quinic acid analog, preferably quinic acid lactone. A pharmaceutical composition comprising a pharmaceutically effective amount of the bioactive component and a nontoxic inert carrier or diluent.Type: GrantFiled: March 7, 2002Date of Patent: November 15, 2005Assignee: Optigenex, Inc.Inventor: Ronald W. Pero
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Patent number: 6958358Abstract: Compounds of general formula (I): wherein R1, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.Type: GrantFiled: January 17, 2002Date of Patent: October 25, 2005Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, Manoj Kumar Ramjee
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Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6903134Abstract: The invention relates to a cosmetic or pharmaceutical formulation comprising at least one compound of formula (I). The cosmetics or pharmaceutical products are particularly suitable for the care of the skin in protecting against oxidative stress and ageing phenomena.Type: GrantFiled: January 22, 2001Date of Patent: June 7, 2005Assignee: Merck Patent GmbHInventors: Frank Pflücker, Herwig Buchholz, Ralf Rosskopf, Joachim Bünger
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Patent number: 6894074Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X?, Y?, Z?, n, G?, A? and B? are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.Type: GrantFiled: September 29, 2003Date of Patent: May 17, 2005Assignee: Bayer AktiengesellschaftInventors: Thomas Bretschneider, Reiner Fischer, Christoph Erdelen, Ernst Brück
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Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6878745Abstract: Drugs for preventing and/or treating progressive lesions after organ damage without inhibiting the function of the organ or the regeneration function thereof, by selectively regulating the induction of cytotoxic effecter macrophages which are induced into damaged organ tissues in response to chemokines or cytokines expressed depending on the type of the damaged organ tissues.Type: GrantFiled: March 27, 2001Date of Patent: April 12, 2005Inventors: Michio Ishibashi, Alain Wagner, Charles Mioskowski, Catherine Sylvain
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Patent number: 6878728Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.Type: GrantFiled: June 9, 2000Date of Patent: April 12, 2005Assignee: Vertex Pharmaceutical IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger
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Patent number: 6858632Abstract: Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I) in which A and B independently represent any of the groups —ONO2 and —Z—CO—R, wherein Z is an oxygen atom or sulphur atom and R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, or the group in which R1 is hydrogen, or an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, with the proviso that one of A or B is always —ONO2, but never both of them at the same time, when Z is an sulphur atom R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, and when Z is an oxygen atom R is the groupType: GrantFiled: April 28, 2003Date of Patent: February 22, 2005Assignee: Lacer, S.A.Inventors: Jose Repolles Moliner, Francisco Pubill Coy, Lydia Cabeza Llorente, Marcel.li Carbo Banus, Cristina Negrie Rofes, Juan Antonio Cerda Riudavets, Alicia Ferrer Siso, Marek W. Radomski, Eduardo Perez-Rasilla, Juan Martinez Bonnin
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Patent number: 6828341Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.Type: GrantFiled: March 27, 2002Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer
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Publication number: 20040192753Abstract: A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas: 1Type: ApplicationFiled: November 10, 2003Publication date: September 30, 2004Inventors: Samuel Chackalamannil, Yan Xia, Enrico P. Veltri, Mariappan V. Chelliah, Wenxue Wu, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala
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Publication number: 20040171658Abstract: Novel compounds of the formula I in which Y, T, W, R1 and R2 are as defined in Patent Claim (1), are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: ApplicationFiled: December 23, 2003Publication date: September 2, 2004Inventors: Peter Raddatz, Dieter Dorsch, Johannes Gleitz, Chistopher Barnes, Ulrich Koert, Marko Vogler
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Patent number: 6784177Abstract: The present invention provides methods of treating and preventing mortality associated with heart failure in an African American patient with hypertension, and improving oxygen consumption, quality of life and exercise tolerance by administering a therapeutically effective amount of at least one hydralazine compound and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, one or more compounds, such as, for example, a digitalis, a diuretic compound, or a compound used to treat cardiovascular diseases. In the present invention, the hydralazine compound is preferably hydralazine or a pharmaceutically acceptable salt thereof. Preferred methods of the invention comprise administering hydralazine or a pharmaceutically acceptable salt thereof and isosorbide dinitrate.Type: GrantFiled: August 2, 2002Date of Patent: August 31, 2004Assignee: Nitro Med, Inc.Inventors: Jay N. Cohn, Peter Carson
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Patent number: 6777409Abstract: The compound of formula 1 useful in the treatment of inflammation.Type: GrantFiled: July 27, 2001Date of Patent: August 17, 2004Assignee: Schering Aktiengesellschaft PatentsInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Bernd Buchmann, Harmur Rehwinkel, Peter Droescher, Werner Skuballa, Konrad Krolikiewicz, Hartwig Hennekes, Heike Schaecke, Arndt Schottelius
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Patent number: 6770663Abstract: Provided is a method of treating or ameliorating a number of indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.Type: GrantFiled: May 19, 2003Date of Patent: August 3, 2004Assignee: Alteon, Inc.Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
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Patent number: 6762183Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.Type: GrantFiled: October 7, 2002Date of Patent: July 13, 2004Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Publication number: 20040122007Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I 1Type: ApplicationFiled: November 21, 2003Publication date: June 24, 2004Inventors: Yong-Jin Wu, Li-Qiang Sun, Huan He, Alexandre L'Heureux
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Publication number: 20040122085Abstract: A liver function protecting or improving agent which comprises a compound represented by the formula (I) 1Type: ApplicationFiled: October 3, 2003Publication date: June 24, 2004Inventors: Yasushi Sakai, Shun Kayahashi, Erika Hashizume, Ryusuke Nakagiri
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Patent number: 6713506Abstract: Disclosed herein are ester-bond containing tea polyphenols that has a susceptibility to nucleophilic attack, their analogs and pharmaceutically acceptable salts, method for inhibiting proteasomal chymotrypsin-like activity in vivo and in vitro, methods for cancer treatment with tea-derived polyphenols, such as EGCG, ECG, GCG, or CG, as well as pharmaceutical compositions comprising the same.Type: GrantFiled: October 11, 2001Date of Patent: March 30, 2004Assignee: University of South FloridaInventors: Q. Ping Dou, Sangkil Nam, David M. Smith
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Publication number: 20040044059Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.Type: ApplicationFiled: April 29, 2003Publication date: March 4, 2004Inventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Mallinath Hadimani, Raymond Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Anjan Ghatak, Usha Ghatak
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Publication number: 20040039033Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: December 10, 2002Publication date: February 26, 2004Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
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Publication number: 20040023999Abstract: Compounds of Formula (IA) and Formula (IB) 1Type: ApplicationFiled: March 21, 2003Publication date: February 5, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Rajashehar Betageri, Mario G. Cardozo, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, Hossein Razavi
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Patent number: 6686388Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.Type: GrantFiled: May 29, 2001Date of Patent: February 3, 2004Assignee: Curis, Inc.Inventors: Henryk Dudek, Benxiu Ji
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Patent number: 6677372Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.Type: GrantFiled: May 24, 2002Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Gabriele Bräunlich, Rüdiger Fischer, Mazen Es-Sayed, Rolf Henning, Michael Sperzel, Karl-Heinz Schlemmer, Ulrich Nielsch, Stephen Tudhope, Graham Sturton, Trevor S. Abram, Mary F. Fitzgerald
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Patent number: 6670355Abstract: This invention provides a method of treating or inhibiting cardiovascular, cerebral vascular, or peripheral vascular disease in a mammal in need thereof, which comprises providing said mammal with an effective amount of a rapamycin.Type: GrantFiled: December 6, 2002Date of Patent: December 30, 2003Assignee: WyethInventors: Neal I. Azrolan, Steven J. Adelman, Surendra N. Sehgal
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Publication number: 20030232824Abstract: The present invention relates to non-steroidal progestins of the general formula (I) 1Type: ApplicationFiled: March 11, 2003Publication date: December 18, 2003Applicant: Schering AGInventors: Norbert Schmees, Manfred Lehmann, Ulrike Fuhrmann, Peter Muhn, Christa Hegele-Hartung, Michael Klotzbuecher
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Publication number: 20030232823Abstract: A compound of Formula (I) 1Type: ApplicationFiled: January 3, 2003Publication date: December 18, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David S. Thomson, Yan Zhang, Renee Michele Zindell
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Publication number: 20030232879Abstract: SR-BI is present at relatively high levels on the membranes of hepatocytes and steroidogenic tissues, including the adrenal gland, testes, and ovaries, where it mediates the uptake and transport of cholesteryl ester from high density lipoproteins. It has been demonstrated that transgenic animals which do not produce SR-BI are healthy, with the exception that the females are infertile. SR-BI KO females have abnormal HDLs, ovulate dysfunctional oocytes and are infertile. Surgical, genetic and pharmacologic methods were used to show that the fertility of SR-BI KO females (or their transplanted oocytes) can be restored in the absence of ovarian and/or extraovarian SR-BI expression by manipulations that modify the structure, composition and/or abundance of their abnormal plasma lipoproteins. These manipulations included inactivation of the apolipoprotein A-I gene and administration of the cholesterol-lowering drug PROBUCOL™.Type: ApplicationFiled: June 7, 2002Publication date: December 18, 2003Applicant: Massachusetts Institute of TechnologyInventors: Monty Krieger, Helena E. Miettinen
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Publication number: 20030220393Abstract: The invention relates to compounds of formula (I): wherein R1 represents an alkyl or ureido group, R2 represents an alkyl group or a hydrogen atom, or R1 and R2 together form a 5- or 6-membered ring, R3 represents a group CN, NO2, NRaR′a, NRaSO2,R′aCZR5 or CZNRaR′a, R4 represents a hydrogen atom or a group R3.Type: ApplicationFiled: December 26, 2002Publication date: November 27, 2003Inventors: Zongru Guo, Fengming Chu, Juntian Zhang, Guangzhong Yang, Bailing Xu, Xinyi Niu, Zhihong Ren, Pierre Lestage, Pierre Renard
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Publication number: 20030203902Abstract: This invention describes the new, nonsteroidal gestagens of general formula I 1Type: ApplicationFiled: February 5, 2003Publication date: October 30, 2003Applicant: SCHERING AKTIENGESELLSCHAFTInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Publication number: 20030203028Abstract: A multiplex drug delivery system suitable for oral administration containing at least two distinct drug dosage packages, which exhibit equivalent dissolution profiles for an active agent when compare to one another and when compared to that of the entire multiplex drug delivery unit, and substantially enveloped by a scored film coating that allows the separation of the multiplex drug delivery system into individual drug dosage packages can provide a convenient and cost effective drug delivery unit, particularly for patients with a regimen of prescribed dosages that varies during their treatment period.Type: ApplicationFiled: May 12, 2003Publication date: October 30, 2003Applicant: IMPAX Pharmaceuticals, Inc.Inventors: Richard Ting, Charles Hsiao
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Patent number: 6635273Abstract: The present invention provides methods of treating vascular diseases where nitric oxide insufficiency is a contributing factor by administering a therapeutically effective amount of at least one antioxidant, or a pharmaceutically acceptable salt thereof, and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and/or at least one compound used to treat cardiovascular diseases. The antioxidant is preferably a hydralazine compound or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 27, 2000Date of Patent: October 21, 2003Assignees: Trustees of Boston University, NitroMed, Inc.Inventors: Joseph Loscalzo, Joseph A. Vita, Michael D. Loberg, Manuel Worcel
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Patent number: 6617350Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: August 9, 2001Date of Patent: September 9, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, François Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano