1,2,4 - Benzothiadiazine - 1,1 - Dioxides (including Hydrogenated) Patents (Class 514/223.2)
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Patent number: 7524841Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides 4,4-(disubstituted)piperidine derivatives represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.Type: GrantFiled: April 16, 2003Date of Patent: April 28, 2009Assignee: Teijin LimitedInventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
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Patent number: 7517876Abstract: Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.Type: GrantFiled: February 27, 2006Date of Patent: April 14, 2009Assignee: Abbott LaboratoriesInventors: Larry L. Klein, Peggy P. Huang, John T. Randolph, Douglas K. Hutchinson, Ming C. Yeung, Charles A. Flentge
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Patent number: 7517875Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.Type: GrantFiled: April 16, 2003Date of Patent: April 14, 2009Assignee: Teijin LimitedInventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
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Patent number: 7504409Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.Type: GrantFiled: May 5, 2004Date of Patent: March 17, 2009Assignee: Genaera CorporationInventors: Yuhong Zhou, Roy C. Levitt, Nicholas C. Nicolaides, Steve Jones, Mike McLane
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Publication number: 20090062264Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: ApplicationFiled: July 1, 2008Publication date: March 5, 2009Inventors: Neil M. Cowen, Iain Dukes
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Publication number: 20090062263Abstract: The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: August 27, 2007Publication date: March 5, 2009Inventors: David Ellis, Liansheng Li, Chinh V. Tran, Frank Ruebsam, Yuefen Zhou
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Publication number: 20090012067Abstract: Provided are methods of increasing KATP activity in the hypothalamus of a mammal, methods of reducing glucose production and peripheral blood glucose levels in a mammal, methods of inhibiting gluconeogenesis in the liver of a mammal, and methods of increasing glucose production and peripheral blood glucose levels in a mammal.Type: ApplicationFiled: February 13, 2006Publication date: January 8, 2009Inventors: Luciano Rossetti, Alessandro Pocai
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METHODS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES USING NMDA RECEPTOR GLYCINE SITE ANTAGONISTS
Publication number: 20090004112Abstract: The disclosure provides methods for treating a neurodegenerative disease by administering a NMDA receptor glycine site antagonist. Compounds that can be used in the methods are also provided. Methods are also provided for determining whether a compound inhibits activity of a Parkinson's Disease-associated mutant of leucine-rich repeat kinase-2 (LRRK2). The methods include assessing accumulation of axonal spheroid inclusions, branching and length of neuronal processes, and neuronal cell death.Type: ApplicationFiled: March 17, 2008Publication date: January 1, 2009Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventor: Asa ABELIOVICH -
Publication number: 20080312218Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.Type: ApplicationFiled: September 21, 2006Publication date: December 18, 2008Inventors: Duane A. Burnett, Wen-Lian Wu
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Patent number: 7462611Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R4 is selected from Ring A is 5 or 6- membered aryl or heterocyclyl, and the remaining substituents are defined herein.Type: GrantFiled: June 21, 2007Date of Patent: December 9, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Frank Ruebsam, Martin Tran, Stephen E. Webber, Peter Dragovich, Liansheng Li, Douglas Murphy, David Kucera, Zhongxiang Sun, Chinh Viet Tran
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Publication number: 20080300239Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: May 16, 2008Publication date: December 4, 2008Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerrard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
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Publication number: 20080292588Abstract: The invention is directed to 1-methyl-benzo[1,2,4]thiadiazine 1-oxide derivatives and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: May 16, 2008Publication date: November 27, 2008Applicant: Anadys Pharmaceuticals, Inc.Inventors: Yuefen Zhou, Thomas Bertolini, Liansheng Li
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Publication number: 20080255101Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.Type: ApplicationFiled: June 10, 2008Publication date: October 16, 2008Applicant: NITROMED, INC.Inventors: David S. GARVEY, L. Gordon LETTS, Richard A. EARL, Maiko EZAWA, Xinqin FANG, Ricky D. GASTON, Subhash P. KHANAPURE, Chia-En LIN, Ramani R. RANATUNGE, Cheri A. STEVENSON, Shiow-Jyi WEY
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Publication number: 20080241251Abstract: A method of producing microparticles having a median diameter up to 100 ?m and the microparticles so produced are described. The method includes the steps of providing a solvent having a bioactive dispersed or dissolved therein and a vehicle dissolved therein, carrying out an emulsification in a non-solvent phase to produce an emulsion containing the bioactive and the vehicle in a solvent phase, and evaporating the solvent to leave the microparticles, wherein a mixture of at least two surfactants is employed to stabilize the emulsion and wherein the mixture has a hydrophilic-lipophilic balance (HLB) of up to 8.Type: ApplicationFiled: January 19, 2005Publication date: October 2, 2008Inventors: Abdul Waseh Basit, Richard Andrew Kendall, Sudax Shina Murdan
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Publication number: 20080227774Abstract: The invention is directed to 5,5-disubstituted-indolizinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: March 14, 2008Publication date: September 18, 2008Inventors: Frank Ruebsam, Peter Dragovich
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Patent number: 7425552Abstract: The invention is directed to pyridazinone compounds of Formula I and pharmaceutical compositions containing compounds of Formula I wherein R1 and R2 are independently H, alkyl, cycloalkyl, aryl, or heterocyclyl; and Ring A is 5 or 6-membered aryl or heterocyclyl. The invention also encompasses methods of using a compound of Formula I in the treatment of hepatitis C virus infections.Type: GrantFiled: December 16, 2005Date of Patent: September 16, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Yuefen Zhou, Liansheng Li, Stephen E. Webber
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Patent number: 7423034Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, a halogen or alkyl, R1a represents hydrogen or alkyl, R2 represents hydrogen, a halogen or hydroxy, A represents NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, X is as defined in the description, their isomers, and also addition salts thereof. Medicinal products containing the same which are useful in treating disorders of the AMPA system.Type: GrantFiled: June 27, 2007Date of Patent: September 9, 2008Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alex Cordi, Pierre Lestage
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Publication number: 20080214529Abstract: The invention is directed to saturated fused [1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: December 12, 2007Publication date: September 4, 2008Inventors: Frank Ruebsam, Zhongxiang Sun, Benjamin Ayida, Yuefen Zhou, Alan X. Xiang
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Tricyclic compounds, a process for their preparation and pharmaceutical compositions containing them
Publication number: 20080188460Abstract: Compounds of formula (I): wherein A represents a 5, 6 or 7-membered (hetero)aromatic or non-aromatic ring, n and n? represent 0, 1 or 2 X represents an alkylene chain as defined in the description, R3 represents an aryl or heteroaryl group, one of the groups R1 and R2 represents a hydrogen atom and the other represents a group of formula (II) as defined in the description. Medicinal products containing the same which are useful in treating conditions involving a defect in apoptosis.Type: ApplicationFiled: January 24, 2008Publication date: August 7, 2008Applicant: LES LABORATOIRES SERVIERInventors: Patrick Casara, Thierry Le Diguarher, Olivier Geneste, John Hickman -
Publication number: 20080188466Abstract: The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: September 26, 2007Publication date: August 7, 2008Applicant: ANADYS PHARMACEUTICALS, INC.Inventors: Peter Dragovich, Yuefen Zhou, Stephen E. Webber
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Patent number: 7396829Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.Type: GrantFiled: February 24, 2006Date of Patent: July 8, 2008Assignee: Nitromed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20080139472Abstract: This invention provides methods of preserving, improving, or restoring cognitive function in mammal having one or more mutations in the FMR1 gene (e.g. at risk for or having fragile x syndrome), where the methods involve the brain derived neurotrophic factor (BDNF) level or activity in the brain of said mammal. In certain embodiments the methods involve administering one or more AMPA potentiators (e.g., ampakines) to the mammal in an amount sufficient to increase BDNF levels in the brain of the mammal.Type: ApplicationFiled: October 5, 2007Publication date: June 12, 2008Inventors: JULIE LAUTERBORN, GARY LYNCH, CHRISTINE GALL, CHRISTOPHER REX
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Patent number: 7378414Abstract: Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.Type: GrantFiled: August 24, 2004Date of Patent: May 27, 2008Assignee: Abbott LaboratoriesInventors: Douglas K. Hutchinson, John R. Bellettini, David A. Betebenner, Richard D. Bishop, Thomas B. Borchardt, Todd D. Bosse, Russell D. Cink, Charles A. Flentge, Bradley D. Gates, Brian E. Green, Mira M. Hinman, Peggy P. Huang, Larry L. Klein, Allan C. Krueger, Daniel P. Larson, M. Robert Leanna, Dachun Liu, Darold L. Madigan, Keith F. McDaniel, John T. Randolph, Todd W. Rockway, Teresa A. Rosenberg, Kent D. Stewart, Vincent S. Stoll, Rolf Wagner, Ming C. Yeung
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Patent number: 7268130Abstract: The invention relates to compounds of formula (I): wherein: R1 represents alkyl substituted by one or more halogen atoms, R2 represents hydrogen, halogen or hydroxy, R3 represents unsubstituted or substituted aryl, their isomers, and also addition salts thereof. and medicinal products containing the same which are useful in treating or preventing disorders associated with AMPA flux.Type: GrantFiled: November 2, 2005Date of Patent: September 11, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7268129Abstract: Compounds of formula (I): wherein: RF represents monofluoro- or polyfluoro-alkyl or monofluoro- or polyfluoro-cycloalkylalkyl, R1 represents hydrogen or a group selected from alkylaminocarbonyl and optionally substituted alkyl, R2 represents hydrogen, halogen or a group selected from cycloalkyl and optionally substituted alkyl, R3 to R6, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, nitro, cyano, alkylsulphonyl, hydroxy, alkoxy, optionally substituted alkyl and optionally substituted amino, its optical isomers when they exist, and also their addition salts with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as AMPA modulators.Type: GrantFiled: January 24, 2005Date of Patent: September 11, 2007Assignee: Les Laboratoires ServierInventors: Pierre Francotte, Pierre Fraikin, Pascal De Tullio, Bernard Pirotte, Pierre Lestage, Laurence Danober, Daniel-Henri Caignard, Pierre Renard
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Patent number: 7262190Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.Type: GrantFiled: December 8, 2005Date of Patent: August 28, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage, Laurence Danober
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Patent number: 7262191Abstract: The invention relates to compounds of formula (I): wherein: X represents oxygen or sulphur, R1 represents linear or branched (C1-C6)alkyl substituted by one or more halogen atoms, R2 represents hydrogen, halogen or hydroxy, R3 represents a group R4 or —Y—R5 wherein R4, Y and R5 are as defined in the description, and medicinal products containing the same which are useful in treating or preventing disorders associated with AMPA flux.Type: GrantFiled: November 3, 2005Date of Patent: August 28, 2007Assignee: Les Laboratories ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7250411Abstract: Compounds of formula (I): wherein: R1 represents hydroxy or RCO—O—, R2 represents hydrogen, halogen, hydroxy or R?CO—O, R, R?, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, R3 represents hydrogen, linear or branched (C1-C6)alkyl or (C3-C7)cycloalkyl, A represents CR4R5 or NR4, R4 represents hydrogen or linear or branched (C1-C6)alkyl, their isomers and also their addition salts with a pharmaceutically acceptable acid or base. Medicaments.Type: GrantFiled: December 20, 2002Date of Patent: July 31, 2007Assignee: Les Laboratoires ServierInventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Patent number: 7235548Abstract: The invention provides novel compounds represented by the general formula compound represented by the formula: wherein the bond represented by the broken line may be a single, a double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O or CH2; Y represents —CH(R4)—, —N(R4)— or —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application The compounds are useful as positive modulators of the AMPA-receptor.Type: GrantFiled: August 18, 2003Date of Patent: June 26, 2007Assignee: NeuroSearch A/SInventors: Alex Haaht Gouliaev, Mogens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Jorgen Scheel-Kruger, Gunnar M. Olsen, Elsesbet Ostergaard Nielsen
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Patent number: 7091200Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, 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: October 22, 2004Date of Patent: August 15, 2006Assignee: Syntex U.S.A. LLCInventors: Cyrus Kephra Becker, Joan Marie Caroon, Chris Richard Melville, Fernando Padilla, Jürg Roland Pfister, Xiaoming Zhang
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Patent number: 7026317Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.Type: GrantFiled: November 21, 2001Date of Patent: April 11, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul J. Gilligan, Richard G. Wilde
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Patent number: 6943159Abstract: The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O of CH2; Y represents —CH(R4)—, —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.Type: GrantFiled: August 18, 2000Date of Patent: September 13, 2005Assignee: Neurosearch A/SInventors: Alex Haahr Gouliaev, Mogens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Jørgen Scheel-Krüger, Gunnar M. Olsen, Elsebet Østergaard Nielsen
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Patent number: 6939870Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: August 29, 2003Date of Patent: September 6, 2005Assignee: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6894043Abstract: Compound selected from those of formula (I): wherein: X represents flourine, bromine, iodine or methyl, each of R1 and R2, which may be identical or different, represents hydrogen or alkyl, its isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid Medicinal products containing the same which are useful as AMPA modulators.Type: GrantFiled: November 28, 2000Date of Patent: May 17, 2005Assignee: Les Laboratoires ServierInventors: Bernard Pirotte, Pascal De Tullio, Stéphane Boverie, Isabelle Kempen, Pierre Lestage
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Patent number: 6858228Abstract: The present invention is concerned with solid oral dosage forms of comprising a) an active agent selected from valsartan and optionally HCTZ, and b) Pharmaceutically acceptable additives suitable for the preparation of solid oral dosage forms by compression methods.Type: GrantFiled: September 20, 2002Date of Patent: February 22, 2005Assignee: Novartis AGInventors: Yoshimitsu Katakuse, Manfred Kohlmeyer, Takashi Taike, Robert Frank Wagner, Fujiki Yamato
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Publication number: 20040253276Abstract: An emulsion composition comprising (1) a compound (I) represented by the formula (I) wherein each symbol is as defined in the specification (2) an anionic synthetic phospholipid in a proportion of about 0.0001 about 5% (W/V) relative to the composition in total, and (3) a naturally-occurring phospholipid in a proportion of about 0.1 about 10% (W/V) relative to the composition in total is provided.Type: ApplicationFiled: August 5, 2004Publication date: December 16, 2004Inventors: Jun Sato, Hikaru Taira, Eiji Nara, Harold Jack Stevens
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Publication number: 20040242566Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and othe S9 proteases that comprise a compound comprising the formula: 1Type: ApplicationFiled: March 24, 2004Publication date: December 2, 2004Applicant: Syrrx, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Publication number: 20040204402Abstract: A compound represented by the formula I: 1Type: ApplicationFiled: August 29, 2003Publication date: October 14, 2004Applicant: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
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Publication number: 20040167123Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) 1Type: ApplicationFiled: October 31, 2003Publication date: August 26, 2004Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
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Publication number: 20040162285Abstract: Compounds having the formula 1Type: ApplicationFiled: July 23, 2003Publication date: August 19, 2004Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
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Publication number: 20040147739Abstract: Compounds useful as HCV anti-infectives having the formula: wherein the formula variables are as defined herein, are disclosed. Also disclosed are methods of making and using the same.Type: ApplicationFiled: December 2, 2003Publication date: July 29, 2004Inventors: Deping Chai, Michael G. Darey, Dashyant Dhanak, Kevin J. Duffy, Greg A. Erickson, Duke M. Fitch, Adam T. Gates, Victor K. Johnston, Robert T. Sarisky, Matthew J. Sharp, Antony N. Shaw, Rosanna Tedesco, Kenneth J. Wiggall, Michael N. Zimmerman
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Publication number: 20040097492Abstract: Compounds having the formula 1Type: ApplicationFiled: November 1, 2002Publication date: May 20, 2004Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
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Patent number: 6737427Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.Type: GrantFiled: January 31, 2001Date of Patent: May 18, 2004Assignee: Genaera CorporationInventors: Yuhong Zhou, Roy C. Levitt, Nicholas C. Nicolaides, Steve Jones, Mike McLane
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Publication number: 20040087577Abstract: Compounds having the formula 1Type: ApplicationFiled: April 10, 2003Publication date: May 6, 2004Inventors: John K. Pratt, David A. Betebenner, Pemela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
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Patent number: 6730668Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ringType: GrantFiled: September 18, 2002Date of Patent: May 4, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Michael George Natchus, Biswanath De
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Publication number: 20040006074Abstract: Certain derivatives of acridones and benzothiadiazines have been found to have anti-cancer properties by virtue of their specific inhibition of the cyclin D dependent kinase CDK4. These molecules inhibit CDK4 activity more than they inhibit the activity of other such kinases (e.g. CDC2 and CDK2). This specificity results in an improved therapeutic index when used as drugs to treat susceptible cancers.Type: ApplicationFiled: December 2, 2002Publication date: January 8, 2004Applicant: The Government of the United States of AmericaInventors: Michael J. Kelley, Kazuhiko Nakagawa, Barry Roy Dent
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Patent number: 6656932Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.Type: GrantFiled: February 13, 2002Date of Patent: December 2, 2003Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Publication number: 20030220329Abstract: The present invention relates to a method of increasing the sensitivity of a hyperinsulinemic patient to the anti-obesity and antidiabetic effects of a &bgr; adrenergic receptor (&bgr;AR) agonist. The method comprises administering to the patient the &bgr;AR agonist and an agent that reduces plasma insulin levels and thereby increases the sensitivity of the patient to the effects of the &bgr;AR agonist.Type: ApplicationFiled: March 24, 2003Publication date: November 27, 2003Applicant: DUKE UNIVERSITYInventors: Richard S. Surwit, Sheila A. Collins
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Patent number: RE40000Abstract: A method of treatment using a compound of Formula I: wherein: R1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R3 is hydrogen or lower alkyl of up to 6 carbon atoms; R4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R4 together with R5 can represent —CH2—O—; X is a valency bond, —CH2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronapthyl; R5 and R6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a —CONH2— group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R5 and R6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction wType: GrantFiled: November 25, 2003Date of Patent: January 8, 2008Assignee: SB Pharmco Puerto Rico Inc.Inventors: Mary Ann Lukas-Laskey, Robert Ruffolo, Jr., Neil Howard Shusterman, Gisbert Sponer, Klaus Strein