Additional Chalcogen Containing Hetero Ring Patents (Class 514/382)
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Publication number: 20120289555Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: February 10, 2011Publication date: November 15, 2012Applicant: N30 PHARMACEUTICALS, LLCInventors: Xicheng Sun, Jian Qiu
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Publication number: 20120283293Abstract: The present invention provides methods for attenuating neuronal inflammation and neuronal damage in case of acute or chronic injury of nerve cells of the central nervous system through prostaglandin E2 EP4 receptor activation. Methods for treating neuropathic pain are also provided.Type: ApplicationFiled: May 6, 2012Publication date: November 8, 2012Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventor: Katrin Andreasson
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Patent number: 8299065Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic raType: GrantFiled: December 12, 2008Date of Patent: October 30, 2012Assignee: Biota Europe Ltd.Inventors: David John Haydon, Lloyd George Czaplewski
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Patent number: 8293776Abstract: The present invention provides compositions and methods for treating inflammatory conditions (e.g., of the bowel). In particular, the present invention provides methods of treating (e.g., therapeutically and/or prophylactically treating) inflammatory conditions (e.g., of the bowel), compositions useful for such methods (e.g., antagonists and/or inhibitors of angiotensin II (AngII) receptor Type 1a (AT1a)), and methods of identifying, characterizing and/or optimizing such compositions. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine) and research applications.Type: GrantFiled: August 5, 2009Date of Patent: October 23, 2012Assignee: The Regents of the University of MichiganInventors: Daniel H. Teitelbaum, Hollis Showalter, Scott Larsen, Peter Lucas, Hiroyuki Koga
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20120238608Abstract: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: Merck Sharp & DohmeInventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
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Publication number: 20120234721Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.Type: ApplicationFiled: September 9, 2011Publication date: September 20, 2012Applicant: Neurotherapeutics Pharma, Inc.Inventors: Daryl W. HOCHMAN, John J. Partridge
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Publication number: 20120214789Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: May 2, 2012Publication date: August 23, 2012Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Patent number: 8217038Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: October 7, 2010Date of Patent: July 10, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120165338Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: December 19, 2011Publication date: June 28, 2012Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
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Publication number: 20120164103Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: March 9, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Publication number: 20120149743Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.Type: ApplicationFiled: June 2, 2009Publication date: June 14, 2012Applicant: Ironwood Pharmaceuticals, IncInventor: Regina Graul
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Publication number: 20120148637Abstract: The present invention is directed to nanostructured (nanoparticulated) Olmesartan or its pharmaceutically acceptable ester, preferable Olmesartan Medoxomil, or co-crystal compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Olmesartan or its pharmaceutically acceptable ester, preferable Olmesartan Medoxomil, or co-crystal according to the invention have an average particle size of less than about 500 nm. Olmesartan Medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. The prodrug Olmesartan Medoxomil is marketed worldwide by Daiichi Sankyo, Ltd. and in the United States by Daiichi Sankyo, Inc.Type: ApplicationFiled: June 18, 2010Publication date: June 14, 2012Inventors: Genovéva Filipcsei, Zsolt Ötvös, Katalin Pongrácz, Ferenc Darvas
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Publication number: 20120149665Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.Type: ApplicationFiled: August 25, 2010Publication date: June 14, 2012Applicant: Bionomics LimitedInventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
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Publication number: 20120149734Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Xiaoxia Qian
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Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
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Publication number: 20120115869Abstract: The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.Type: ApplicationFiled: July 14, 2010Publication date: May 10, 2012Applicant: MERCK SERONO S.A.Inventors: Stefano Crosignani, Christophe Cleva, Anna Quattropani, Gwenaelle Desforges, Agnès Bombrun
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Publication number: 20120108640Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.Type: ApplicationFiled: August 26, 2011Publication date: May 3, 2012Applicant: NEUROTHERAPEUTICS PHARMA, INC.Inventors: Daryl W. Hochman, John J. Partridge
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Patent number: 8153671Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.Type: GrantFiled: July 14, 2006Date of Patent: April 10, 2012Assignee: IRM LLCInventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He
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Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20120071529Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: March 1, 2011Publication date: March 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Monika ERMANN, Doris RIETHER, Renee M. ZINDELL
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Publication number: 20120046312Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.Type: ApplicationFiled: October 19, 2011Publication date: February 23, 2012Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
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Publication number: 20120046327Abstract: Methods for (i) inhibiting the induction and formation of osteoclasts, (ii) inhibiting RANKL expression in osteoblasts, (ii) inhibiting the activation of osteoclasts and (iv) inhibiting a decrease in bone density by administering to a warm-blooded animal in need thereof a pharmacologically effective amount of a compound selected from the group consisting of olmesartan and olmesartan medoxomil, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof.Type: ApplicationFiled: September 19, 2011Publication date: February 23, 2012Applicants: OSAKA UNIVERSITY, DAIICHI SANKYO COMPANY, LIMITEDInventors: Ryuuichi Morishita, Hironori Nakagami, Hideo Shimizu
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Publication number: 20120015944Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: September 22, 2011Publication date: January 19, 2012Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20120010249Abstract: The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: January 12, 2012Applicant: BAYER CROPSCIENCE AGInventors: Rüdiger FISCHER, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Ernst Rudolf GESING, Arnd VOERSTE, Ulrich GÖRGENS
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Publication number: 20110313003Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Patent number: 8080571Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: GrantFiled: April 12, 2006Date of Patent: December 20, 2011Assignee: Vicore Pharma ABInventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
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Publication number: 20110300104Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20110281823Abstract: A pharmaceutical preparation including a pharmacologically effective amount of a combination of active ingredients containing an angiotensin II receptor antagonist, a calcium channel blocker and polyvinyl alcohol, wherein the polyvinyl alcohol is in an amount of 5 to 85% by weight of the total weight of the pharmaceutical preparation. A method for the prophylaxis or treatment of hypertension by administering a pharmaceutically effective amount of the pharmaceutical preparation to a patient.Type: ApplicationFiled: July 19, 2011Publication date: November 17, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Takeshi Hamaura, Mitsuru Kanno
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Publication number: 20110281795Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: January 15, 2010Publication date: November 17, 2011Inventors: Songnian Lin, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
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Publication number: 20110281811Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.Type: ApplicationFiled: November 12, 2009Publication date: November 17, 2011Inventor: Sabine Rupprecht
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Publication number: 20110275683Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.Type: ApplicationFiled: June 2, 2009Publication date: November 10, 2011Applicant: Ironwood Pharmaceuticals, IncInventor: Regina Graul
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Patent number: 8048905Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: GrantFiled: December 17, 2008Date of Patent: November 1, 2011Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8048904Abstract: The present invention provides a process for the preparation of Olmesartan medoxomil by condensing the ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate with 4-[2-(trityl tetrazol-5-yl)phenyl]benzyl bromide to obtain ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate and then hydrolyzing ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methyl imidazole-5-carboxylate to obtain trityl Olmesartan dihydrate followed by reacting trityl Olmesartan dihydrate with 4-chloromethyl-5-methyl-2-oxo-1,3-dioxolene to obtain trityl Olmesartan medoxomil and then deprotecting trityl Olmesartan medoxomil to obtain Olmesartan medoxomil.Type: GrantFiled: June 15, 2007Date of Patent: November 1, 2011Assignee: Matrix Laboratories Ltd.Inventors: Gorantla Seeta Ramanjaneyulu, Bandari Mohan, Purna Chandra Ray, Madhuresh Kumar Sethi, Vijendra Singh Rawat, Yerramalla Raja Krishna, Vemula Lakshminarayana, Mamidi Srinivas
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Publication number: 20110263666Abstract: The present invention relates to a process for the preparation and purification of olmesartan medoxomil hydrohalide salts and optionally converting them to olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.Type: ApplicationFiled: August 7, 2008Publication date: October 27, 2011Applicant: LEK PHARMACEUTICALS D.D.Inventors: Samo Pirc, Lovro Selic
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Publication number: 20110257177Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 22, 2009Publication date: October 20, 2011Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
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Publication number: 20110257178Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: October 7, 2010Publication date: October 20, 2011Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20110256221Abstract: This invention is related to pharmaceutical compositions, which have good flowability properties, comprising olmesartan medoxomil or combination of olmesartan medoxomil and hydrochlorothiazide and a lubricant or mixtures of lubricants and a pharmaceutically acceptable excipient or excipients.Type: ApplicationFiled: December 30, 2008Publication date: October 20, 2011Inventors: Farhad Farshi, Recep Avci, Serdar Soylemez, Fikret Koc, Nadin Narsisoglu
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Patent number: 8039496Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.Type: GrantFiled: January 22, 2008Date of Patent: October 18, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20110224228Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: August 10, 2009Publication date: September 15, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: Mark L Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Ahmed Mamai
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Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8008290Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: GrantFiled: August 9, 2010Date of Patent: August 30, 2011Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
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Publication number: 20110206665Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.Type: ApplicationFiled: March 25, 2011Publication date: August 25, 2011Applicant: PHIGENIX, INC.Inventor: Carlton D. DONALD
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Publication number: 20110201609Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.Type: ApplicationFiled: June 30, 2009Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20110195935Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.Type: ApplicationFiled: September 24, 2009Publication date: August 11, 2011Inventor: Michael Farber
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Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
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Publication number: 20110165259Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.Type: ApplicationFiled: September 15, 2009Publication date: July 7, 2011Applicant: ACTIVUS PHARMA CO., LTD.Inventors: Takashi Hirokawa, Takahiro Tada, Jun Nihira
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Publication number: 20110166114Abstract: A method of treating snoring and/or sleep apnea comprising administering to a patient in need of such treatment a therapeutically effective amount of a leukotriene receptor antagonist.Type: ApplicationFiled: March 14, 2011Publication date: July 7, 2011Inventor: David Gozal