Carbocyclic Ring Attached Indirectly To The Morpholine Ring By Nonionic Bonding Patents (Class 514/239.5)
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Publication number: 20100261695Abstract: The present invention generally relates to the treatment of onychomycosis. More specifically, it relates to combination therapies for the treatment of onychomycosis and related compositions. In a composition aspect, the present invention provides a composition for the treatment of onychomycosis, wherein the composition includes Ciclopirox and at least one other antifungal agent. In a method aspect, the present invention provides a method for treating onychomycosis in a patient suffering from the disease. The method involves topically administering a composition to at least one toe or fingernail of the patient and the composition includes Ciclopirox and at least one other antifungal agent.Type: ApplicationFiled: April 9, 2010Publication date: October 14, 2010Inventor: Reza BABAPOUR
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100256150Abstract: A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: formula (II), (III) and (IV); or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: (V) and (VI); wherein R1 and R2 together represent an oxo group, or R1 and R2 each represent hydrogen, methoxy or ethoxy, or R1 and R2 together with the interjacent carbon atom represent a 1,3-dioxolane or 1,3-dioxane ring, attached via the 2 position and optionally bearing one or more methyl or ethyl groups; or a salt thereof, is suitable for the treatment of anxiety and depression.Type: ApplicationFiled: June 15, 2010Publication date: October 7, 2010Applicant: BTG International LimitedInventors: Phillip Parsons, Silvia Trasciatti, Sergio Rosini, Michael Annis
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Publication number: 20100249135Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting ofType: ApplicationFiled: December 11, 2007Publication date: September 30, 2010Applicant: THE GENETICS COMPANY, INC.Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Jaschinskin Frank, Guy Lemaillet, Cornelia Marty-Ernest, Elena Marzi, Leonardo Scapozza
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Publication number: 20100240660Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Applicant: DAC S.R.L.Inventors: Saverio MINUCCI, Pier Giuseppe PELICCI, Antonello MAI, Marco BALLARINI, Gaetano GARGIULO, Silvio MASSA
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Publication number: 20100216640Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of Formula (I) wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.Type: ApplicationFiled: April 23, 2008Publication date: August 26, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
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Publication number: 20100197564Abstract: The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: April 17, 2008Publication date: August 5, 2010Inventors: Jack D. Scott, Andrew Stamford
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Patent number: 7737135Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: GrantFiled: August 22, 2005Date of Patent: June 15, 2010Assignee: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20100143441Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.Type: ApplicationFiled: November 12, 2009Publication date: June 10, 2010Applicant: OsteoGeneX Inc.Inventors: Debra Ellies, William Rosenberg
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Publication number: 20100129311Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100068307Abstract: A foaming gelled composition in the form of a stable oil-in-water microemulsion comprising a fatty phase of microdroplets dispersed in an aqueous phase and a dermatological active ingredient, characterized in that it comprises a surfactant system comprising:—at least one ethoxylated nonionic surfactant;—at least one cosurfactant for stabilizing the ethoxylated nonionic surfactant;—at least one nonethoxylated hydrophilic nonionic surfactant;—at least one foaming agent chosen from the group of anionic surfactants.Type: ApplicationFiled: January 25, 2008Publication date: March 18, 2010Applicant: PIERRE FABRE DERMO-COSMETIQUEInventor: Francoise Nielloud
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Publication number: 20100048573Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. Because their mechanism of action does not involve killing of bacteria or inhibiting their growth, the potential for these compounds to induce drug resistance in bacteria is minimized. Through inhibiting bacterial virulence, the present invention provides a novel means of treating bacterial infections.Type: ApplicationFiled: October 20, 2008Publication date: February 25, 2010Inventors: Vanessa Sperandio, John R. Falck, Donald R. Stewart
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Publication number: 20100029639Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: ApplicationFiled: April 15, 2009Publication date: February 4, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Publication number: 20100009970Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.Type: ApplicationFiled: March 18, 2009Publication date: January 14, 2010Applicant: Combinatorx (Singapore) Pte. Ltd.Inventors: Lisa M. Johansen, Christopher M. Owens, Christina Mawhinney, Todd W. Chappell, Alexander T. Brown, Michael G. Frank, Michael A. Foley, Ralf Altmeyer, Yu Chen
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Publication number: 20090312329Abstract: A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: formula (II), (III) and (IV); or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: (V) and (VI); wherein R1 and R2 together represent an oxo group, or R1 and R2 each represent hydrogen, methoxy or ethoxy, or R1 and R2 together with the interjacent carbon atom represent a 1,3-dioxolane or 1,3-dioxane ring, attached via the 2 position and optionally bearing one or more methyl or ethyl groups; or a salt thereof, is suitable for the treatment of anxiety and depression.Type: ApplicationFiled: August 18, 2009Publication date: December 17, 2009Applicant: BTG International LimitedInventors: Phillip Parsons, Silvia Trasciatti, Sergio Rosini, Michael Annis
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Publication number: 20090312328Abstract: [Object] 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. [Means for Solution] 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: ApplicationFiled: August 9, 2007Publication date: December 17, 2009Applicant: 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: 20090253703Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, Holger Sellner
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Publication number: 20090247529Abstract: Single phase pharmaceutical compositions for topical application, in addition to kits and methods of use and administration are provided. The compositions comprise a biologically active agent; a delivery vehicle comprising at least a non-polymeric crystallization inhibitor and a film-former; and a volatile solvent; wherein the biologically active agent is present in the composition in a subsaturated state, the biologically active agent is present in the delivery vehicle in a supersaturated state, and the crystallization inhibitor is capable of delaying crystallization of the biologically active agent in the delivery vehicle. Biologically active agents include terbinafine and acyclovir. Treatments for onychomycosis and Varicella zoster infection, HSV-1 infection or HSV-2 infection are provided.Type: ApplicationFiled: June 14, 2007Publication date: October 1, 2009Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Ake Lindahl, Birgitta Svensson, Anna Holmberg, Johan Engblom
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Patent number: 7595397Abstract: Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula wherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.Type: GrantFiled: December 8, 2006Date of Patent: September 29, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Renee Zindell, Doris Riether, David S. Thomson, Eugene Richard Hickey, Innocent Mushi, Monika Ermann
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Patent number: 7595315Abstract: Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.Type: GrantFiled: December 10, 2004Date of Patent: September 29, 2009Assignee: Eli Lilly and CompanyInventors: Peter Thaddeus Gallagher, Carlos Lamas-Peteira, Francisco Javier Agejas-Chicharro
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Publication number: 20090209514Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydronaphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: April 29, 2009Publication date: August 20, 2009Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20090192141Abstract: The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: ABBOTT LABORATORIESInventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, James T. Link, Yixian Chen, Hwan-soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
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Publication number: 20090192163Abstract: The invention relates to substituted phenylacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: October 5, 2006Publication date: July 30, 2009Applicant: ASTRAZENECA ABInventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Stephen Thom, Anil Patel
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Patent number: 7563789Abstract: The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], wherein the substituents are as defined in the specification.Type: GrantFiled: April 7, 2006Date of Patent: July 21, 2009Inventors: Gloria Long Anderson, Tawfeq Abdul-Raheem Kaimari
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Publication number: 20090143369Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: ApplicationFiled: January 28, 2009Publication date: June 4, 2009Applicant: H. LUNDBECK A/SInventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
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Patent number: 7534790Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: GrantFiled: November 21, 2007Date of Patent: May 19, 2009Assignee: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Patent number: 7531651Abstract: Compounds of formula (I): wherein A? represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.Type: GrantFiled: March 27, 2003Date of Patent: May 12, 2009Assignee: Glaxo Group LimitedInventors: John Spencer Cook, Robert Philip Landon, Andrew John Walker, Mark Wilkinson
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Publication number: 20090099187Abstract: The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: April 16, 2009Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Carl Petersson, Laszlo Rakos, Daniel Sohn
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Publication number: 20090093484Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: December 21, 2006Publication date: April 9, 2009Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Publication number: 20090088435Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.Type: ApplicationFiled: September 15, 2008Publication date: April 2, 2009Applicant: SIRION THERAPEUTICS, INC.Inventors: Nathan L. MATA, Kim B. PHAN, Tam V. BUI, Mustapha HADDACH
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Publication number: 20090088434Abstract: The invention provides a topical liquid antifungal composition containing an antifungal agent, a film-forming agent and a solvent. The composition is applied on the infected skin area to form a film that delivers the active agent. The invention also provides a method for treating a fungal infection on the skin by applying the topical antifungal composition that forms a film on the skin.Type: ApplicationFiled: September 27, 2006Publication date: April 2, 2009Applicant: NOVARTIS AGInventor: Friedrich Karl Mayer
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Publication number: 20090075975Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: November 24, 2008Publication date: March 19, 2009Inventors: Michael R. DeGraffenreid, JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090048258Abstract: The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: January 31, 2006Publication date: February 19, 2009Inventors: Masaki Ogino, Yoshihisa Nakada, Mitsuyuki Shimada, Kouhei Asano, Norikazu Tamura, Minori Masago
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Publication number: 20090012066Abstract: The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors.Type: ApplicationFiled: August 9, 2006Publication date: January 8, 2009Inventors: Seigo Izumo, Suraj Shivappa Shetty
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Publication number: 20080305051Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.Type: ApplicationFiled: February 23, 2006Publication date: December 11, 2008Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
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Publication number: 20080306072Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cy-cloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.Type: ApplicationFiled: July 26, 2006Publication date: December 11, 2008Applicant: NABRIVA THERAPEUTICS FORSCHUNGS GMBHInventors: Rosemarie Mang, Heinz Berner
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Publication number: 20080275016Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: May 2, 2008Publication date: November 6, 2008Inventor: Jack L. Arbiser
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Publication number: 20080261985Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.Type: ApplicationFiled: November 16, 2007Publication date: October 23, 2008Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
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Ungual/periungual compositions comprising morpholine compounds and water-soluble film-forming agents
Publication number: 20080260656Abstract: Pharmaceutical compositions suited for ungual and periungual application and useful for the treatment of dermatological conditions/afflictions, in particular onychomycosis, contain an anti-mycotic agent of the family of the morpholines and a water-soluble film-forming agent.Type: ApplicationFiled: April 11, 2008Publication date: October 23, 2008Applicant: GALDERMA S.A.Inventor: Claire Mallard -
Publication number: 20080261986Abstract: Pharmaceutical formulations suitable for iontophoresis thereof that provide enhanced iontophoretic delivery of an anti-fungal drug to at least one body surface are described. Also described are pharmaceutical formulations suitable for iontophoresis comprising terbinafine and methods for administering terbinafine to a body surface via iontophoresis. In one embodiment, the body surface includes a nail plate and/or the skin.Type: ApplicationFiled: March 27, 2008Publication date: October 23, 2008Inventors: Phillip M. Friden, Hyun Kim, Bireswar Chakraborty
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Publication number: 20080207537Abstract: Application of a reducing agent followed by an oxidising agent to a nail substantially increases the permeability thereof, thereby enabling the passage of drugs across the nail.Type: ApplicationFiled: June 6, 2006Publication date: August 28, 2008Applicant: MedPharm LimitedInventors: Robert Turner, Marc Barry Brown, Stuart Allen Jones
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Publication number: 20080167312Abstract: Disclosed herein are substituted allylamines having structural Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080132480Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: August 22, 2005Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 7273867Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disordersType: GrantFiled: December 5, 2001Date of Patent: September 25, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
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Patent number: 7232821Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: GrantFiled: April 7, 2003Date of Patent: June 19, 2007Assignee: Glaxo Group LimitedInventors: Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Xiao Qing Lewell, Alan Naylor, Riccardo Novelli
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Patent number: 7223755Abstract: A compound represented by the following formula (I) wherein R1 and R2 are each a lower alkyl group optionally having substituents, which has a calpain inhibitory activity, or a salt thereof is provided.Type: GrantFiled: March 27, 2003Date of Patent: May 29, 2007Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Masayuki Nakamura, Jun Inoue
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou