Sulfonamides (i.e., Q-(o=)s(=o)-n, Wherein Q Is A Substituent And Wherein Any Substituent Attached To The Nitrogen Will Be Referred To As E) Patents (Class 514/601)
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Patent number: 8044240Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.Type: GrantFiled: March 6, 2009Date of Patent: October 25, 2011Assignee: Ardea Biosciences Inc.Inventor: Stuart Dimock
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Publication number: 20110245324Abstract: The present invention relates to compounds that modulate the shikimate pathway and/or a pathway branching from the shikimate pathway in members of the Amoebida Order. In particular these compounds may be useful in the treatment or prevention of diseases caused or contributed to by members of the Amoebida Order.Type: ApplicationFiled: May 23, 2011Publication date: October 6, 2011Applicant: University of StrathclydeInventors: Craig William Roberts, Fiona Roberts, Fiona Luisa Henriquez, Paul Richard Ingram
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Patent number: 8030335Abstract: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.Type: GrantFiled: May 10, 2006Date of Patent: October 4, 2011Assignee: Laboratoires Fournier S.A.Inventors: Bernadette Husson, Pierre Broqua, Jean-Louis Junien
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Publication number: 20110218214Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: September 9, 2010Publication date: September 8, 2011Applicant: ABBOTT LABORATORIESInventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
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Publication number: 20110195945Abstract: Compositions and methods of treating or preventing disease or injury to a human patient or biological material undergoing ischemic or hypoxic conditions.Type: ApplicationFiled: February 11, 2011Publication date: August 11, 2011Applicant: Ikaria, Inc.Inventors: Fuqiang Ruan, Edward A. Wintner, Thomas L. Deckwerth
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Patent number: 7981401Abstract: Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described.Type: GrantFiled: February 2, 2007Date of Patent: July 19, 2011Assignee: Alexza Pharmaceuticals, Inc.Inventors: Nathan R. Every, Ron L. Hale, Amy T. Lu, Joshua D. Rabinowitz
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Patent number: 7981839Abstract: A herbicidal suspension comprising (1) a sulfonylurea compound or its salt as a herbicidal component, (2) at least one surfactant selected from the group consisting of an alkoxylated sorbitol fatty acid ester and an alkoxylated sorbitan fatty acid ester, and (3) a water-immiscible diluent. A method for controlling undesired plants or inhibiting their growth, which comprises applying a herbicidally effective amount of the herbicidal suspension to the undesired plants or to a place where they grow.Type: GrantFiled: February 23, 2006Date of Patent: July 19, 2011Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Hiroshi Yoshii, Yoshiaki Ishihara, Ryu Yamada, Tatsuhiko Tsuruta
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Patent number: 7973078Abstract: A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular a lower urinary tract symptom. It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.Type: GrantFiled: August 9, 2007Date of Patent: July 5, 2011Assignee: Astellas Pharma Inc.Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
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Publication number: 20110150859Abstract: The present invention relates to a method for identifying responders to a blockade of integrin receptors, as well as to a method for determining responsiveness to a treatment involving with said blockade in a patient in need of such treatment. Furthermore, the present invention relates to a kit for use in said methods.Type: ApplicationFiled: April 16, 2008Publication date: June 23, 2011Inventors: Anne Marjamaki, Liisa Nissinen
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Patent number: 7951831Abstract: The invention relates to methods, compositions, and uses of those compositions for making medicaments, for potentiating the beneficial effects of inhibitors of COX-1, COX-2, and 5-LOX, and reducing adverse effects, by also administering inhibitors of soluble epoxide hydrolase (“sEH”), with or without also administering one or more cis-epoxyeicosantrienoic acids. The invention further relates to the use of inhibitors of sEH as analgesics and to methods and compositions of epoxides of eicosapentaenoic acid and docosahexaenoic acid, optionally with an inhibitor of sEH, to reduce pain or inflammation or both.Type: GrantFiled: January 10, 2006Date of Patent: May 31, 2011Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Kara Schmelzer, Ahmet Bora Inceoglu
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Publication number: 20110117015Abstract: The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.Type: ApplicationFiled: July 21, 2009Publication date: May 19, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Stanislava Ivanova Avramova, Fulvio Uggeri, Alessandro Maiocchi
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Patent number: 7932242Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.Type: GrantFiled: March 15, 2005Date of Patent: April 26, 2011Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics Inc.Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
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Patent number: 7915316Abstract: The present invention provides R, R1, R2, R3, X, c, d, e, f, g, x, y, a, b, z and n are defined in the specification. These compounds are useful in lowering IOP and/or treating glaucoma or providing neuroprotection to the eye of a human patient.Type: GrantFiled: August 21, 2006Date of Patent: March 29, 2011Assignee: Allergan, IncInventor: Robert M. Burk
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Publication number: 20110060049Abstract: This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.Type: ApplicationFiled: July 28, 2008Publication date: March 10, 2011Applicant: Ardea Biosciences, Inc.Inventors: Jean-Michel Vernier, Colin Edward Rowlings, Jean-Luc Girardet, Stuart Dimock, Barry Quart, Jeffrey N. Miner
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Publication number: 20110053901Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.Type: ApplicationFiled: February 13, 2009Publication date: March 3, 2011Applicants: SIGNUM BIOSCIENCES, INC., Signum Biosciences, Inc.Inventors: Seung-Yub Lee, Michael Voronkov, Peter Wolanin
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Publication number: 20110033539Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.Type: ApplicationFiled: April 14, 2009Publication date: February 10, 2011Applicant: ARDEA BIOSCIENCES, INCInventors: Barry D. Quart, Colin Edward Rowlings
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Patent number: 7868046Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: GrantFiled: December 15, 2009Date of Patent: January 11, 2011Assignee: Dompe' Pha.r.ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
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Publication number: 20100311791Abstract: The present invention relates to active bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and antiviral compounds and compositions and to new uses of these compositions in therapy. This specification also describes methods of use for the new compounds and compositions. The specification further describes methods for preparing these compounds.Type: ApplicationFiled: December 28, 2007Publication date: December 9, 2010Inventors: Ramin Najafi, Rakesh K. Jain, Timothy P. Shiau, Eddy Low, Satheesh K. Nair
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Patent number: 7820158Abstract: Initiator polymers having an initiator group and a ligand group are provided. The initiator polymers are capable of specifically binding to a receptor on a surface. Using a macromer system, the initiator polymers are useful for the formation of a polymeric matrix on the surface of a material. In particular, initiator polymers are provided that have specificity to pancreatic ? cells and can be used to encapsulate cells for transplantation and the treatment of diabetes.Type: GrantFiled: April 10, 2003Date of Patent: October 26, 2010Assignee: SurModics, Inc.Inventors: Stephen J. Chudzik, Dale G. Swan
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Publication number: 20100256209Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 15, 2009Publication date: October 7, 2010Inventor: Jean-Louis Henri Dasseux
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Publication number: 20100247485Abstract: Described herein are formulations and devices for delivering compounds to arthropods and microorganisms within the arthropods. The formulations are generally composed of a sugar and the compound, wherein the compound targets a particular pathogen or other microorganism within the arthropod, kills the arthropod, or a combination thereof.Type: ApplicationFiled: September 5, 2008Publication date: September 30, 2010Applicant: MEVLABS, INC.Inventor: Thomas Kollars
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Patent number: 7786220Abstract: The present invention relates to a block copolymer formed by coupling the following components with each other, as well as a hydrogel composition comprising the block copolymer and a hydrogel formed from the composition: (a) a copolymer of a polyethylene glycol (PEG)-based compound with a biodegradable polymer; and (b) a sulfonamide-based oligomer. The inventive block copolymer shows the sol-gel transition behavior sensitive to changes in not only temperature but also pH. Thus, the inventive block copolymer overcomes the shortcomings of temperature-sensitive copolymers, form a more strong and stable hydrogel, and is stable in vivo. Accordingly, the inventive block copolymer can be used in various applications in the medical and drug delivery fields.Type: GrantFiled: January 26, 2005Date of Patent: August 31, 2010Assignee: Sungyunkwan University Foundation for Corporate CollaborationInventors: Doo Sung Lee, Woo Sun Shim, You Han Bae, Je Sun You, Min Sang Kim, Huynh Dai Phu
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Publication number: 20100189685Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: May 23, 2008Publication date: July 29, 2010Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Patent number: 7759518Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: November 25, 2008Date of Patent: July 20, 2010Assignee: Ardea BiosciencesInventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan el Abdellaoui, Zhi Hong
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Patent number: 7750184Abstract: The present invention relates to novel, non-secosteroidal, sulfonate and sulfonamide functional diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: GrantFiled: November 8, 2004Date of Patent: July 6, 2010Assignee: Eli Lilly and CompanyInventors: Robert Peter Gajewski, Charles David Jones, Jared Harris Linebarger, Jianliang Lu, Tianwei Ma, Sunil Nagpal, Ying Kwong Yee
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Publication number: 20100113449Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Patent number: 7705052Abstract: The present invention is related to the use of sulfonamide derivatives in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). Formula (I). R1 is selected from the group comprising or consisting of hydrogen, C1-C6-alkoxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, amino, sulfanyl, sulfinyl, sulfonyl, sulfonyloxy, sulfonamide, acylamino, aminocarbonyl, C1-C6 alkoxycarbonyl, aryl, heteroaryl, carboxy, cyano, halogen, hydroxy, nitro, hydrazides. R2 is selected from the group comprising or consisting of hydrogen, COOR3, —CONR3R3?, OH, a C1-C4 alkyl substituted with an OH or amino group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt.Type: GrantFiled: September 13, 2004Date of Patent: April 27, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Pierre-Alain Vitte, Jean-Pierre Gotteland
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Publication number: 20100035996Abstract: A compound of the formula I: wherein R1 is lower alkyl, R2 is hydrogen or lower alkyl, Z is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted amino, optionally substituted lower alkoxy, optionally substituted carbocyclyl or optionally substituted heterocyclyl can stimulate the glucose metabolism independent of change in body weight. The compound can be used as a glucose metabolism stimulating agent.Type: ApplicationFiled: October 16, 2007Publication date: February 11, 2010Applicant: Shionogi & Co LtdInventor: Hideo Yukioka
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Patent number: 7659312Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.Type: GrantFiled: June 1, 2007Date of Patent: February 9, 2010Assignee: Niigata UniversityInventors: Tsutomu Nakada, Vincent J. Huber
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Patent number: 7655681Abstract: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.Type: GrantFiled: February 15, 2005Date of Patent: February 2, 2010Inventors: Ludger Grote, Kaj Stenlof, Jan Hedner
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Patent number: 7652169Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: GrantFiled: May 17, 2007Date of Patent: January 26, 2010Assignee: Dompe' Pha. R. Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
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Publication number: 20100015079Abstract: The present invention relates to a cosmetic composition which comprises a compound of the formula R2R3N—(CH2)n—SO2R1, in which R1 is OR4 or NR5R6; R2 and R3, independently of one another, are H, C1-C6-alkyl, phenyl-C1-C4-alkyl, HCO or C1-C4-alkyl-CO; R4 is C1-C6-alkyl; R5 and R6, independently of one another, are H or C1-C6-alkyl; and n is 2, 3 or 4. The cosmetic compositions can be used for protecting the hair and the skin against oxidative damage and for regenerating oxidatively damaged hair or oxidatively damaged skin.Type: ApplicationFiled: April 19, 2007Publication date: January 21, 2010Inventor: Karl-Heinz Schrader
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Publication number: 20100004244Abstract: The present invention relates to ligands of the peripheral cannabinoid receptor CB2, especially (+)-?-pinene derivatives, and to pharmaceutical compositions thereof, which are useful for promoting, inducing and enhancing neurogenesis including neural cell regeneration. In particular, pharmaceutical compositions of the invention will be useful for preventing, alleviating or treating neurological injuries or damages to the CNS or the PNS associated with physical injury, ischemia, neurodegenerative disorders, certain medical procedures or medications, tumors, infections, metabolic or nutritional disorders, cognition or mood disorders, and various medical conditions associated with neural damage or destruction.Type: ApplicationFiled: June 27, 2007Publication date: January 7, 2010Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEMInventors: Ismael Galve-Roperh, Manuel Guzman, Raphael Mechoulam, Javier Palazuelos, Tania Aguado
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Publication number: 20100004339Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.Type: ApplicationFiled: September 14, 2009Publication date: January 7, 2010Applicant: OY JUVANTIA PHARMA LTD.Inventors: Jussi Tomperi, Päivi Hautamäki, Harri Salo, Mia Engström, Andrei Tauber, Anna-Marja Hoffrén, Siegfried Wurster
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Patent number: 7625949Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein.Type: GrantFiled: April 22, 2005Date of Patent: December 1, 2009Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Donald Roy Hirschfeld, Tania Silva, Zachary Kevin Sweeney, Harit Vora
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Publication number: 20090227681Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.Type: ApplicationFiled: March 6, 2009Publication date: September 10, 2009Applicant: ARDEA BIOSCIENCES, INC.Inventor: Stuart DIMOCK
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Patent number: 7572833Abstract: The present invention provides a preparation containing a compound of the formula (I) wherein R1 is an alkyl group having 1 to 4 carbon atoms or an optionally substituted aryl group having 6 to 10 carbon atoms; R2 and R3 are the same or different and each is hydrogen or an alkyl group having 1 to 4 carbon atoms, or R2 and R3 in combination form a ring having 3 to 7 carbon atoms; and R4 is a lower alkyl group optionally substituted by aryl, cycloalkyl or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof together with a lipid. The preparation shows improved stability and improved absorption and penetration into tissue.Type: GrantFiled: September 27, 2001Date of Patent: August 11, 2009Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Jun Inoue, Masazumi Yamaguchi
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Publication number: 20090163594Abstract: The invention provides assays and methods for determining whether a compound inhibits gamma secretase in a substrate specific manner. The invention provides an isolated cell wherein the cell stably expresses APP and at least one gamma secretase substrate other than APP. The invention provides assays and methods comprising contacting a cell with gamma secretase and detecting production of Abeta, detecting production of intracellular domain (ICD), and detecting a signal from a reporter gene under transcriptional control of the ICD. The invention also provides compounds that inhibit gamma secretase, pharmaceutical compositions comprising such compounds, and methods of treating Alzheimer's disease using such compounds.Type: ApplicationFiled: October 31, 2008Publication date: June 25, 2009Applicant: ELAN PHARMACEUTICALS, INC.Inventors: I. Paul Shapiro, Guriqbal S. Basi, Zhao Ren, Xiao-Hua Chen
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Patent number: 7544717Abstract: Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: GrantFiled: March 25, 2005Date of Patent: June 9, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, John Tucker, Varghese John, Neerav Shah
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Patent number: 7531538Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 15, 2006Date of Patent: May 12, 2009Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Publication number: 20090088459Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: ApplicationFiled: September 17, 2008Publication date: April 2, 2009Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Publication number: 20090082457Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: November 25, 2008Publication date: March 26, 2009Applicant: Andrea Biosciences, Inc.Inventors: Andreas MADERNA, Jean-Michel VERNIER, Dinesh BARAWKAR, Varaprasad CHAMAKURA, Hassan EL ABDELLAOUI, Zhi HONG
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Patent number: 7504422Abstract: This invention relates to methods for treating retinopathy and repairing tissue damage. The methods include administering to a subject in need thereof an effective amount of one or more compounds of the following formula. Each variable in this formula is defined in the specification.Type: GrantFiled: August 6, 2007Date of Patent: March 17, 2009Assignee: Taigen Biotechnology Co. Ltd.Inventors: Chi-Feng Yen, Chi-Hsin Richard King, Hua-Chien Chen, Gholam Hossein Hakimelahi, Shu-Jen Chen, Ying-Huey Huang, Chien-Huang Wu
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Publication number: 20090047244Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: July 25, 2008Publication date: February 19, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Dominique Surleraux, Francois-Rene Alexandre, Michel Derock, Frederic Leroy
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Patent number: 7479508Abstract: This invention relates to compositions of nimesulide for topical application.Type: GrantFiled: August 25, 2004Date of Patent: January 20, 2009Assignee: EDKO Trading and Representation Company LimitedInventors: Koral Embil, Ray Figueroa
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Publication number: 20090012074Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition saltsType: ApplicationFiled: October 14, 2005Publication date: January 8, 2009Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
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Publication number: 20080317815Abstract: One aspect of the present invention is directed to a composition. The composition includes a dispersion inducer comprising: H3C—(CH2)n—CHmCHmR, where is a single or double carbon-carbon bond, m is 1 or 2, n is 2 to 15, and R is a carboxylic acid, a salt, an ester, or an amide, where the ester or amide is an isostere or biostere of the carboxylic acid. The composition additionally contains an additive component selected from one or more of the group consisting of biocides, surfactants, antibiotics, antiseptics, detergents, chelating agents, virulence factor inhibitors, gels, polymers, pastes, edible products, and chewable products. The composition is formulated so that when it is contacted with a biofilm produced by a microorganism, where the biofilm comprises a matrix and microorganism on a surface, the dispersion inducer selectively acts on the microorganism and has a suitable biological response without a required direct effect on the matrix to disperse the biofilm.Type: ApplicationFiled: May 14, 2008Publication date: December 25, 2008Applicant: Research Foundation of State University of New YorkInventor: David G. Davies
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Publication number: 20080274169Abstract: Highly flexible penetrating liposomal carrier systems are formulated with enhanced skin penetration properties. These specialized formulations of highly flexible penetrating liposomal delivery systems comprise one or more phospholipids, lysophosphatides and hydrophobic photosensitizer. This new formulations can squeeze liposomal particles through intercellular regions of stratum corneum as intact structures, and, in this way, deliver encapsulated photosensitizer to the epidermis, dermis, hypodermis and surroundings. The penetrating liposomal formulation provides therapeutically effective amounts of the hydrophobic photosensitizer through topical application with better skin penetration thus improving drug targeting and the efficacy of photodynamic therapy (PDT).Type: ApplicationFiled: May 4, 2007Publication date: November 6, 2008Inventors: Gerard Farmer, Dietrich Scheglmann, Volker Albrecht, Nikolay E. Nifantiev
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Publication number: 20080274184Abstract: This invention is directed to graft materials comprising an extracellular matrix (ECM) and therapeutic agents. This invention is also directed to methods of using the graft materials for healing of damaged or diseased tissues on a patient's body.Type: ApplicationFiled: March 31, 2005Publication date: November 6, 2008Inventor: James B. Hunt