1,2,5-thiadiazoles (including Hydrogenated) Patents (Class 514/362)
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Publication number: 20100113331Abstract: The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.Type: ApplicationFiled: January 11, 2010Publication date: May 6, 2010Applicant: TRANSTECH PHARMA, INC.Inventors: ADNAN M. M. MJALLI, DHARMA R. POLISETTI, GOVINDAN SUBRAMANIAN, JAMES C. QUADA, RAVINDRA R. YARRAGUNTA, ROBERT C. ANDREWS, RONGYUAN XIE
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Patent number: 7700633Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: GrantFiled: December 6, 2006Date of Patent: April 20, 2010Assignee: Novartis AGInventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing, Katsumasa Nakajima
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Patent number: 7700635Abstract: This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.Type: GrantFiled: May 7, 2007Date of Patent: April 20, 2010Assignee: Aegera Therapeutics Inc.Inventor: James B. Jaquith
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Patent number: 7666885Abstract: Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.Type: GrantFiled: August 12, 2004Date of Patent: February 23, 2010Assignees: Consejo Superior de Investigaciones Cientificas, Universidad Autonoma de Madrid (UAM)Inventors: Ana Gil Martinez, Ana Castro Morera, Maria Concepcion Martin Perez, Mercedes Alonso Cascon, Isabel Dorronsoro Diaz, Francisco Jose Moreno Munoz, Francisco Wandosell Jurado
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Publication number: 20100035942Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: ApplicationFiled: December 6, 2006Publication date: February 11, 2010Inventors: David Barnes, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol
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Publication number: 20100035860Abstract: The invention relates to the use of protein tyrosine phosphatase inhibitors for the promotion of physiological cardiac hypertrophy and the treatment of pathological cardiac hypertrophy.Type: ApplicationFiled: November 30, 2007Publication date: February 11, 2010Inventors: Jey Raju Jeyaseelan, Mie Abe
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Publication number: 20100029641Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: August 27, 2009Publication date: February 4, 2010Applicant: WyethInventors: Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Goldberg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, JR., Puwen Zhang
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Publication number: 20100029618Abstract: Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.Type: ApplicationFiled: December 14, 2007Publication date: February 4, 2010Inventors: Daniel W. Gil, John E. Donello
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Publication number: 20100022525Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: October 4, 2007Publication date: January 28, 2010Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20100022482Abstract: The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.Type: ApplicationFiled: August 21, 2007Publication date: January 28, 2010Inventors: Karl Baumann, Andreas Billich, Berndt Oberhausen
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Patent number: 7652143Abstract: The present invention relates to a novel compound of the formula I: and/or all stereoisomeric forms of the compound of the formula I and/or mixtures of these forms in any ratio, and/or a physiologically tolerated salt of the compound of the formula I, in which R1 to R5 and V1, V2 have the meanings stated in the claims and specification. The inventive compounds are suitable as inhibitors of metalloproteases, especially of ADAMTS proteases and TNF-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.Type: GrantFiled: June 15, 2007Date of Patent: January 26, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Andreas Lindenschmidt, Holger Wagner, Jochen Beninga, Sven Grueneberg, Klaus-ulrich Weithmann
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Patent number: 7645781Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: September 21, 2006Date of Patent: January 12, 2010Assignee: Pfizer IncInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Negandra Josyula
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Publication number: 20090324511Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: May 20, 2009Publication date: December 31, 2009Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, JR.
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Patent number: 7632851Abstract: The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)—(CH2)n18F, O—(CH2)nF, O—(CH2)n18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.Type: GrantFiled: April 2, 2004Date of Patent: December 15, 2009Assignee: Novartis AGInventors: Yves Auberson, Samuel Hintermann, Kaspar Zimmermann
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Publication number: 20090253707Abstract: A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1=n=12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.Type: ApplicationFiled: August 18, 2008Publication date: October 8, 2009Applicant: NATIONAL DEFENSE MEDICAL CENTERInventor: Hsu-Shan HUANG
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Publication number: 20090208449Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Inventors: Sharada Shenvi Labadie, Clara Jeou Jen Lin, Francisco Xavier Talamas, Robert James Weikert
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Publication number: 20090202572Abstract: The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a ?-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and/or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and/or growth in a mammal by administering a composition comprising a ?2-selective antagonist or agonist.Type: ApplicationFiled: May 13, 2006Publication date: August 13, 2009Inventors: Gerard Karsenty, Bruce Devens
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Publication number: 20090197904Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.Type: ApplicationFiled: May 16, 2006Publication date: August 6, 2009Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
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Publication number: 20090181928Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: ApplicationFiled: March 29, 2007Publication date: July 16, 2009Inventors: Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
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Publication number: 20090175938Abstract: This invention is a novel controlled release (CR) flurbiprofen and muscle relaxant combinations for oral administration with anti-inflammatory, analgesic, myorelaxant activity and methods of its manufacture. The pharmaceutical composition of the present invention is administered orally in tablet, multilayer tablet, multicoated tablet and capsule form.Type: ApplicationFiled: December 24, 2008Publication date: July 9, 2009Applicant: SANOVEL ILAC SANAYI VE TICARET A.S.Inventors: Umit Cifter, Ali Turkyilmaz, Hasan Ali Turp
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Publication number: 20090170911Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.Type: ApplicationFiled: February 20, 2009Publication date: July 2, 2009Applicant: AJINOMOTO CO. INCInventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7550492Abstract: Certain amidophenyl-sulfanylamino-benzo[1,2,5]thiadiazole compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.Type: GrantFiled: July 10, 2007Date of Patent: June 23, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Brett Allison, Laura C. McAfee, Victor K. Phuong, Michael H. Rabinowitz, Nigel P. Shankley
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Patent number: 7528173Abstract: Compounds of the following formula (I), for example: (1), wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: March 21, 2003Date of Patent: May 5, 2009Assignee: Schering AktiengesellshaftInventors: Brad Buckman, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendong Yuan
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Publication number: 20090105222Abstract: Methods for the prevention or treatment of stress-related disorders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress-related disorders in an individual at risk.Type: ApplicationFiled: September 19, 2008Publication date: April 23, 2009Applicant: Cypress Bioscience, Inc.Inventors: Jay D. Kranzler, Srinivas G. Rao
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Publication number: 20090105230Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: April 23, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20090088452Abstract: The present invention is directed to substituted indole compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: November 17, 2006Publication date: April 2, 2009Inventors: Paul J. Coleman, Anthony J. Roecker, Jeffrey M. Bergman
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Publication number: 20090075986Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: March 19, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20090069345Abstract: The present invention is related to ophthalmic formulations for the treatment of ocular ailments. More specifically, it is related to the pharmaceutical industry in the production of ophthalmic medication for the treatment of ocular hypertension. The advantage of the present invention over other state of the art treatments is that it achieves a composition of Dorzolamide Hydrochloride, Timolol Maleate and Brimonidine Tartrate with excellent properties of stability; it does not give rise to chemical reactions which produce modifications in the active molecules; with no antagonistic effects among the components. The present invention consists of a stable pharmaceutical composition for the treatment of ocular hypertension characterized by consisting of the following excipients: Polyoxyl 40 Stearate, Sodium Borate crystals, Sodium Chloride, Mannitol and Benzalkonium chloride.Type: ApplicationFiled: January 11, 2008Publication date: March 12, 2009Inventors: Jose Ruben Tornero Montano, Leopoldo Martin Baiza Duran, Juan De Dios Quintana Hau
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Publication number: 20090062354Abstract: An article and method for increasing the extent of tizanidine absorption in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release tablet composition at or around the time food is consumed. The composition may be packaged in a container for distribution.Type: ApplicationFiled: December 12, 2007Publication date: March 5, 2009Inventor: Cara A. Pellegrini
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Patent number: 7498351Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: November 15, 2005Date of Patent: March 3, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Lan Shen, Aihua Wang, Yan Zhang
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Publication number: 20090054442Abstract: A method is provided of treating an eye with ophthalmologically active compounds, particularly with intra-ocular pressure lowering (IOP) compounds, where a dose of 5-15 microliters is delivered at a standard concentration.Type: ApplicationFiled: October 28, 2008Publication date: February 26, 2009Inventors: BEN Z. COHEN, NIGEL KELLY
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Publication number: 20090048261Abstract: The present invention is related to the pharmaceutical industry in general and in particular with the pharmaceutical industry of production of ophthalmic compositions. More specifically, the present invention relates to the pharmaceutical industry of production of ophthalmologic compositions for the treating of ocular hypertension. The advantage of the present invention against the present state of the technique is the fulfilling of a synergic effect of its components for the decreasing of ocular hypertension with no antagonistic effect between its components. The present invention consists of a pharmaceutical composition for the treatment of ocular hypertension characterized by comprising a pharmacologically effective amount of dorzolamide, with a pharmacologically effective amount of timolol and a pharmacologically effective amount of brimonidine.Type: ApplicationFiled: January 11, 2008Publication date: February 19, 2009Inventors: Jose Ruben Tornero Montano, Leopoldo Martin Baiza Duran, Juan De Dios Quintana Hau
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Publication number: 20090023742Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. 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 substituted thiazolones.Type: ApplicationFiled: March 2, 2007Publication date: January 22, 2009Inventors: Dashyant Dhanak, Steven David Knight
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Publication number: 20090017109Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.Type: ApplicationFiled: March 11, 2008Publication date: January 15, 2009Inventors: Cara A. Pellegrini, Paul Stark
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Patent number: 7459473Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: December 3, 1998Date of Patent: December 2, 2008Assignee: Glia Med, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Publication number: 20080293776Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
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Publication number: 20080293782Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: David Barnes, Gary Mark Coppola, Robert Edson Damon, Katsumasa Nakajima, Brian Christopher Raudenbush, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda
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Publication number: 20080279819Abstract: The present invention provides novel methods and compositions for the treatment and prevention of demyelinating conditions. One demyelinating condition treated by the methods and compositions of the invention is multiple sclerosis. Also treated are symptoms associated with multiple sclerosis.Type: ApplicationFiled: February 15, 2006Publication date: November 13, 2008Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson, David Chernoff
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Publication number: 20080279933Abstract: This invention is a novel pharmaceutical composition comprising flurbiprofen or a pharmaceutically acceptable salt thereof in combination with an ?-2 adrenergic receptor agonist or a gamma-aminobutiric acid receptor agonist with anti-inflammatory, analgesic and myorelaxant activity.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: Sanovel Ilac Sanayi Ve Ticaret A.S.Inventors: Umit Cifter, Ali Turkyilmaz, Hasan Ali Turp
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Publication number: 20080267908Abstract: The present invention relates to methods of screening for modulators of interleukin 32 (IL-32), to modulators of IL-32 and to their use. Proteinase 3 has been identified as an IL-32 binding protein capable of deavege thereof. Inhibition of PR 3 activity to process IL-32 or neutralization of IL-32 by-inactive PR3 or its fragments may reduce the consequences of IL-32 in immune regulated diseases (e.g. inflammatory diseases).Type: ApplicationFiled: July 10, 2006Publication date: October 30, 2008Applicants: YEDA RESEARCH AND DEVELOPMENT CO. LTD, THE REGENTS OF THE UNIVERSITY OF COLORADOInventors: Daniela Novick, Menachem Rubinstein, Charles A. Dinarello, Soo-Hyun Kim
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Publication number: 20080262050Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: ApplicationFiled: December 6, 2006Publication date: October 23, 2008Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Katsumasa Nakajima, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Patent number: 7432292Abstract: The present invention relates to novel phosphate isosteres. The invention relates to compounds having a sulfhydantoin or a reverse sulfhydantoin moiety, uses thereof, and related methods. The present invention relates to compounds of formula I or II: or pharmaceutically acceptable salts thereof; wherein Q, T, m, and X are as described herein. These compounds are inhibitors of phosphatases, particularly inhibitors of SHP-2. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing these compounds and compositions in the treatment of various phosphatase-mediated diseases.Type: GrantFiled: December 30, 2003Date of Patent: October 7, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, Gregory F. Miknis, James F. Blake
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Patent number: 7427621Abstract: Compounds of formula I: inhibit the processing of AP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.Type: GrantFiled: October 31, 2003Date of Patent: September 23, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Joanne Clare Hannam, Timothy Harrison, Andrew Madin, Mark Peter Ridgill
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Publication number: 20080214629Abstract: The present invention relates to a novel controlled release formulations of tizanidine. The invention also provides methods of using novel controlled release formulations of tizanidine to treat a patient.Type: ApplicationFiled: January 16, 2008Publication date: September 4, 2008Inventors: Scott Bull, Suneel Gupta, Rhea Donley, Nishit Modi, Noymi Yam
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Publication number: 20080207703Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.Type: ApplicationFiled: July 23, 2007Publication date: August 28, 2008Applicant: Replidyne, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
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Publication number: 20080194655Abstract: The present invention relates to a novel controlled release formulations of tizanidine. The invention also provides methods of using novel controlled release formulations of tizanidine to treat a patient.Type: ApplicationFiled: January 17, 2008Publication date: August 14, 2008Inventors: Scott Bull, Suneel Gupta, Rhea Donley, Nishit Modi, Noymi Yam
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Publication number: 20080182850Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: October 16, 2007Publication date: July 31, 2008Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko