Only Two Ring Oxygens In The Hetero Ring Which Is Not A Polycyclo Ring System (e.g., Dioxolane, Etc.) Patents (Class 514/467)
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Publication number: 20090163576Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R5 is hydrogen or alkyl having from one to six carbon atoms.Type: ApplicationFiled: May 11, 2007Publication date: June 25, 2009Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20090163457Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.Type: ApplicationFiled: November 26, 2008Publication date: June 25, 2009Applicant: pSivida, Inc.Inventors: Paul Ashton, Jianbing Chen, Hong Guo, Grazyna Cynkowska, Tadeusz Cynkowski
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Publication number: 20090163549Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.Type: ApplicationFiled: December 13, 2006Publication date: June 25, 2009Inventor: Hiroyuki Kai
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Publication number: 20090137660Abstract: A method of treating a patient in need of therapy for a cytokine dysregulation comprising administering to that patient a therapeutically effective dose of a compound of general formula: (I) wherein R1 and R2 together form a group —(CH2)n—CR4R5—(CH2)m— wherein n and m are independently selected integers 0, 1 or 2 and R4 and R5 are independently selected from H, C1-18 alkyl, C1-18 alkoxy, C1-18n hydroxyalkyl, C2-18 alkenyl and C6-18 aryl or aralyalkyl and R3 is the fatty acyl group of an essential polyunsaturated fatty acid.Type: ApplicationFiled: March 2, 2006Publication date: May 28, 2009Inventors: Laurence S. Harbige, Michael J. Leach, Paul Barraclough, Anthony P. Dolan
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Publication number: 20090137393Abstract: The invention relates to novel 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) in which X, Y, A, B, Q1, Q2 and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: January 3, 2007Publication date: May 28, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Ulrich Gorgens, Olga Malsam, Alfred Angermann, Guido Bojack, Alan Graff, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Hein Kehne, Christopher Hugh Rosinger, Jan Dittgen
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Publication number: 20090082311Abstract: The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect.Type: ApplicationFiled: April 27, 2007Publication date: March 26, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masatoshi Kiuchi, Mitsuharu Nakamura, Maiko Hamada, Kunio Sugahara
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Publication number: 20090076062Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 13, 2007Publication date: March 19, 2009Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
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Publication number: 20090069416Abstract: The present invention is to provide skin cosmetics and anti-wrinkle agents which are excellent in reducing effect on wrinkle caused by photoaging. Skin cosmetics and anti-wrinkle agents which comprise a sugar alcohol derivative represented by the following formula (1): (wherein n is 1 to 5, preferably n=2.).Type: ApplicationFiled: January 21, 2006Publication date: March 12, 2009Inventors: Kyoko Miura, Akinori Haratake
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Patent number: 7468457Abstract: Novel biaryl compounds having the structural formula (I): are useful in a variety of pharmaceutical applications, whether human or veterinary, and also in cosmetics.Type: GrantFiled: November 19, 2004Date of Patent: December 23, 2008Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Pascal Collette
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Publication number: 20080312317Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Masayuki Miyano, Daisuke Ito, Norio Murai
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Publication number: 20080242721Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof.Type: ApplicationFiled: May 31, 2007Publication date: October 2, 2008Applicant: AROMAGEN CORPORATIONInventor: Sergey Selifonov
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Publication number: 20080125483Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.Type: ApplicationFiled: November 21, 2007Publication date: May 29, 2008Inventors: Jenn-Tsang Hwang, Chrong-Shiong Hwang, Yow-Lone Chang, Chung-Niang Yao
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Publication number: 20080103191Abstract: Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.Type: ApplicationFiled: June 14, 2007Publication date: May 1, 2008Inventors: Klaus Hansen, Robert Kraemer, Thomas Lauterbach, Dirk Schmidt, Fritz Paar, Petra Pfeiffer, Detlef Geffken, Wolfgang Thimann, Katharina Wehner
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Patent number: 7339078Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 10, 2006Date of Patent: March 4, 2008Assignee: G.D. Searle LLCInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Publication number: 20080033036Abstract: The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.Type: ApplicationFiled: August 12, 2004Publication date: February 7, 2008Inventors: Ryuji Ueno, Tsuyoshi Habe, Takashi Sekida
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Patent number: 7323493Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.Type: GrantFiled: June 19, 1998Date of Patent: January 29, 2008Assignee: Sanofi-AventisInventors: Bernard Abramovici, Jean-Claude Gautier, Jean-Claude Gromenil, Jean-Marie Marrier
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Publication number: 20080020071Abstract: A composition protects against, minimizes the effects of, and hastens recovery from the typical symptoms associated with an alcohol induced hangover. The composition includes superoxide dismutase (SOD), and prickly pear cactus (OFI). In addition, sesamin and alpha-lipoic acid work with the SOD and OFI for enhanced antioxidant and therapeutic effects. Other ingredients can be added to the composition for additional treatment of symptoms.Type: ApplicationFiled: July 24, 2006Publication date: January 24, 2008Inventor: Victor H. Diaz
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Patent number: 7307043Abstract: An aqueous composition suitable for applying insecticides or acaricides to plant propagation materials comprising water, an insecticidally or acaricidally effective amount of at least one nitroimino- or nitroguanidino-compound in free form or in agrochemically useful salt form and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 4-20% of at least one inorganic solid carrier; and c) 3-25% of at least one antifreeze agent. In one embodiment, the aqueous composition further comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.Type: GrantFiled: August 17, 2004Date of Patent: December 11, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Christian Schlatter, Ravi Ramachandran
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Patent number: 7271194Abstract: Use of escitalopram (the S-(+)-enantiomer of citalopram) or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment of neurotic disorders is provided, including anxiety states, in particular generalised anxiety disorder and social anxiety disorder, post traumatic stress disorder, obsessive compulsive disorder and panic attacks.Type: GrantFiled: December 12, 2001Date of Patent: September 18, 2007Assignee: H. Lundbeck A/SInventors: Connie Sanchez, Sandra Hogg
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Patent number: 7271274Abstract: The invention relates to compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, wherein the compounds are of the following Formulas: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein the substituents are defined in the application. The invention further provides methods of treatment of inflammatory disorders by administering the compounds.Type: GrantFiled: April 20, 2005Date of Patent: September 18, 2007Assignee: AhteroGenics, Inc.Inventors: Charles Q. Meng, M. David Weingarten
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Patent number: 7264822Abstract: One aspect of the invention is a system for treating vascular conditions, including a catheter, a stent coupled to the catheter, and a polymeric coating on the stent comprising at least one conjugated drug. Each conjugated drug includes a control agent and a bioactive agent, where the control agent controls the elution rate of the bioactive agent.Type: GrantFiled: April 3, 2002Date of Patent: September 4, 2007Assignee: Poly-Med, Inc.Inventors: Shalaby W. Shalaby, Todd Campbell
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Patent number: 7196089Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: January 29, 2004Date of Patent: March 27, 2007Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Patent number: 7105552Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.Type: GrantFiled: April 27, 2001Date of Patent: September 12, 2006Assignee: Theracos, Inc.Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
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Patent number: 7078400Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7026315Abstract: Fungicidal mixtures, comprising as active components a) a morpholine or piperidine derivative I selected from the group of the compounds Ia, Ib, Ic and Id and b) compounds of the formula II in a synergistically effective amount are described.Type: GrantFiled: December 11, 1999Date of Patent: April 11, 2006Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Reinhold Saur, Karl Eicken, Egon Haden, Eberhard Ammermann, Thomas Grote, Gisela Lorenz, Siegfried Strathmann
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Patent number: 7001924Abstract: The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The compounds belong to several classes including mono- and bis-guanylhydrazones, guanylhydrazone mimetics, and benzothiazolium compounds. Exemplary compounds are compounds of formula I: Y—(NR?)k—U1—(NR?)I—A—(NR1)m—U2—(NR2)n—Z??I with substituents as described herein.Type: GrantFiled: September 23, 2002Date of Patent: February 21, 2006Assignee: Message PharmaceuticalsInventors: Tony Giordano, Michael A. Sturgess, Samala J. Rao
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Patent number: 6926913Abstract: The invention provides a composition of matter comprising molecular iodine and tetraglycol.Type: GrantFiled: March 22, 2001Date of Patent: August 9, 2005Assignees: Ben Gurion University of the Negev Research & Development Authority, Yissum Research Development Company of the HebrewInventors: Uri Wormser, Amnon Sintov
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Patent number: 6903086Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: March 1, 2002Date of Patent: June 7, 2005Assignee: SYNTEX (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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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: 6890955Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive.Type: GrantFiled: January 3, 2003Date of Patent: May 10, 2005Assignee: Virbac SAInventors: Ahmed El Hadri, Philippe Archimbault, Gérard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6861539Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 12, 2003Date of Patent: March 1, 2005Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6849626Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Patent number: 6825231Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endotType: GrantFiled: December 12, 2000Date of Patent: November 30, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6800658Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: GrantFiled: January 10, 2002Date of Patent: October 5, 2004Assignees: Children's Medical Center Corporation, President & Fellows of Harvard College, Nuchem Pharmaceuticals, Inc.Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 6790463Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.Type: GrantFiled: March 30, 2001Date of Patent: September 14, 2004Inventors: Robert F. Hofmann, Robert H. Carpenter
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Patent number: 6777440Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1, R2 and B1 are as defined herein.Type: GrantFiled: December 6, 2002Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
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Publication number: 20040138296Abstract: The present invention provides compositions and methods for the treatment or prevention of Alzheimer's disease. More particularly, the invention provides a combination therapy for the treatment or prevention of Alzheimer's disease, wherein the therapy comprises administering to a subject an amyloid beta vaccine in combination with a cyclooxygenase-2 selective inhibitor.Type: ApplicationFiled: July 25, 2003Publication date: July 15, 2004Applicant: Pharmacia CorporationInventors: David W. Robertson, Grant A. Krafft
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040019038Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: July 21, 2003Publication date: January 29, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John Robert Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
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Patent number: 6683210Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 15, 2002Date of Patent: January 27, 2004Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6677330Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.Type: GrantFiled: August 30, 2001Date of Patent: January 13, 2004Assignee: Eisai Co., Ltd.Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
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Publication number: 20040006130Abstract: A compound of the formula [I] 1Type: ApplicationFiled: February 10, 2003Publication date: January 8, 2004Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
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Publication number: 20040006050Abstract: Compounds of Formula I, 1Type: ApplicationFiled: June 9, 2003Publication date: January 8, 2004Applicants: Wyeth, ArQule Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Publication number: 20030225091Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1Type: ApplicationFiled: November 15, 2002Publication date: December 4, 2003Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Patent number: 6653322Abstract: The present invention provides compositions and methods for treating an animal, preferably a human, suffering from or predisposed to a physical disorder by administering an effective amount of a composition comprising at least one RAR antagonist, preferably an RAR&agr; antagonist, and at least one RXR agonist. The combination of an RXR agonist, which has no therapeutic effects alone, with an RAR antagonist allows the use of lower doses of the RAR antagonist than were previously thought to be efficacious; this approach obviates many of the undesirable physiological side-effects of treatment with RAR antagonists.Type: GrantFiled: July 19, 2000Date of Patent: November 25, 2003Assignees: Bristol-Myers Squibb Company, Institut National de la Sante et de la Recherche Medicale, Centre National de la Recherche Scientifique, Universite Louis PasteurInventors: Pierre Chambon, Hinrich Gronemeyer, Peter R. Reczek, Jacek Ostrowski
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Patent number: 6653318Abstract: The present invention relates to pyrimidine nucleoside compounds and their use to treat viral infections of Varicella Zoster virus and Epstein Barr Virus, as well as cancers which are complications of Epstein Barr virus.Type: GrantFiled: July 21, 1999Date of Patent: November 25, 2003Assignees: Yale University, The University of Georgia Research Foundation, Inc.Inventors: Yung-Chi Cheng, Chung K. Chu, Ling Li, Yongseok Chai
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Patent number: 6649652Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I)Type: GrantFiled: July 30, 2002Date of Patent: November 18, 2003Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro