The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Publication number: 20130225599Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).Type: ApplicationFiled: October 24, 2011Publication date: August 29, 2013Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmonson
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Publication number: 20130225819Abstract: Described herein are inventive methods for synthesis of tetrazoles. In some embodiments, the method involves the use of a flow reactor. The methods provided herein are capable at being carried out in short reaction times, with high yields, with minimal side reactions, and/or with minimal chance of explosions caused by the presence of azides.Type: ApplicationFiled: August 18, 2011Publication date: August 29, 2013Applicant: Massachusetts Institute of TechnologyInventors: Timothy F. Jamison, Prakash B. Palde
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Publication number: 20130225644Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.Type: ApplicationFiled: April 1, 2013Publication date: August 29, 2013Applicant: Zealand Pharma A/SInventor: Zealand Pharma A/S
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Patent number: 8519188Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: GrantFiled: June 15, 2009Date of Patent: August 27, 2013Assignee: Marc-Henry PittyInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Publication number: 20130210874Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 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: November 20, 2012Publication date: August 15, 2013Applicant: THERAVANCE, INC.Inventor: THERAVANCE, INC.
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Publication number: 20130203815Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.Type: ApplicationFiled: March 25, 2011Publication date: August 8, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
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Publication number: 20130196971Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.Type: ApplicationFiled: September 15, 2011Publication date: August 1, 2013Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
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Publication number: 20130190506Abstract: The present invention provides a process for the preparation of substantially pure trityl olmesartan medoxomil. The present invention also provides a process for purification of trityl olmesartan medoxomil. The present invention further provides a process for purification of olmesartan medoxomil.Type: ApplicationFiled: June 28, 2010Publication date: July 25, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Matta Ramakrishna Reddy, Bandi Vamsi Krishna
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Patent number: 8487129Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: November 11, 2011Date of Patent: July 16, 2013Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20130178471Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Vextex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130165446Abstract: The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).Type: ApplicationFiled: May 11, 2011Publication date: June 27, 2013Inventors: Takashi Fujita, Hiroyoshi Horikoshi, Michael Anthony Cawthorne
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Patent number: 8466145Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.Type: GrantFiled: January 7, 2010Date of Patent: June 18, 2013Assignee: Orchid Chemicals & Pharmaceuticals LimitedInventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
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Publication number: 20130144067Abstract: The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (Ia), (Ib), and (Ic), which comprises: (i) condensing 2-(4?-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2?-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2?-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(1-oxopentyl)-N-[[2?-(2-tributyltinte-trazol-5-yType: ApplicationFiled: June 24, 2011Publication date: June 6, 2013Inventors: Raveendra Reddy Chinta, Gangadhara Bhima Shankar Nangi, Mahendar Reddy Nayini, Somappa Somannavar Yallapa, Shankar Reddy Budidet, Islam Aminul, Sivakumaran Meenakshisunderam
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Publication number: 20130137737Abstract: The present invention describes a highly crystalline form of valsartan, pharmaceutical compositions thereof and process for the preparation thereof.Type: ApplicationFiled: August 1, 2011Publication date: May 30, 2013Applicant: NOVARTIS AGInventors: Jens Burgbacher, Björn Thomas Hahn, Florian Andreas Rampf, Ricardo Schneeberger
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Publication number: 20130131351Abstract: 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: October 5, 2012Publication date: May 23, 2013Applicant: Metabolex, Inc.Inventor: Metabolex, Inc.
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8410097Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: GrantFiled: December 22, 2011Date of Patent: April 2, 2013Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Rajesh Thotapally, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Publication number: 20130071328Abstract: This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2.Type: ApplicationFiled: March 22, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Nouri NEAMATI, Nicos A. PETASIS, Roppei YAMADA
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Publication number: 20130066252Abstract: The invention relates to a method for diagnosis of multiple sclerosis (MS) wherein, presence or absence of an anti-AT1 receptor antibody is determined in a sample from a patient to be diagnosed and wherein, the presence of an anti-AT1-receptor antibody is indicative of the disease.Type: ApplicationFiled: April 12, 2011Publication date: March 14, 2013Applicant: CELLTREND GMBHInventor: Harald Heidecke
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Patent number: 8394799Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.Type: GrantFiled: July 3, 2007Date of Patent: March 12, 2013Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Jung Joon Lee, Jeong-Hyung Lee, Kyeong Lee, Young-Soo Hong, B. K. Shanthaveerappa, Yinlan Jin, Jin Hwan Kim, Xuejun Jin
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Patent number: 8394967Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: February 23, 2011Date of Patent: March 12, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Xin Jiang, Xiaofeng Liu, Jack Greiner, Stephen S. Szucs, Melean Visnick
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Patent number: 8383654Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: November 16, 2009Date of Patent: February 26, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
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Patent number: 8378118Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: GrantFiled: January 10, 2012Date of Patent: February 19, 2013Assignee: Torrent Pharmaceuticals Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
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Publication number: 20130041001Abstract: Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases.Type: ApplicationFiled: April 18, 2011Publication date: February 14, 2013Inventors: Dirk Sartor, Armin Scherhag
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Patent number: 8367710Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: GrantFiled: January 4, 2009Date of Patent: February 5, 2013Assignees: Jiangsu Hengrui Medicine Co. Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fei, Shenglan Wang, Li Wang
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Patent number: 8367709Abstract: Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.Type: GrantFiled: June 11, 2008Date of Patent: February 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Mimi L. Quan, Leon M. Smith, II, Michael J. Orwat, Paul J. Gilligan
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Patent number: 8362017Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.Type: GrantFiled: August 27, 2004Date of Patent: January 29, 2013Assignee: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew, John M. Nuss, Wei Xu, William Bajjalieh
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Patent number: 8357705Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.Type: GrantFiled: March 25, 2009Date of Patent: January 22, 2013Assignee: Gruenenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schröder, Werner Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
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Publication number: 20130012434Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
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Publication number: 20130012493Abstract: The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: He Zhao, Ping Chen, Peishan Lin, Peng Dai, Jason Louis Davis, Duane E. DeMong, Michael W. Miller, Xing Dai, Michael K. Wong, Brian J. Lavey, Wensheng Yu, Guowei Zhou, Andrew W. Stamford, Joseph A. Kozlowski, William J. Greenlee
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Publication number: 20130012708Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: Nissan Chemical Industries LimitedInventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Publication number: 20130005784Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: December 23, 2011Publication date: January 3, 2013Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 8343970Abstract: 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: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8344002Abstract: A novel compound represented by the formula (1) below which has ?-secretase inhibitory activity, its pharmaceutically acceptable salt or a prodrug thereof. wherein Ar is a substituted or unsubstituted 5 to 6 membered mono cyclic aromatic group; R1, R2 and R3 are hydrogen atom, substituted or unsubstituted alkyl group or the like, or R2 and R3 may be taken together with the adjacent nitrogen atom and carbon atom respectively to form a 3 to 6 membered ring; R4 is C1-6 alkyl group, C1-6 alkyl group substituted by phenyl, phenylthio, or a hetero ring, or the like; A is represented by the formula below: wherein X and Y are oxygen atom, NH or sulfur atom, Z is hydrogen atom, hydroxy group which may be substituted, amino group, thiol group, or the like; and B is hydroxy group, substituted or unsubstituted amino group, substituted or unsubstituted aliphatic or aromatic amino group, or the like.Type: GrantFiled: June 18, 2008Date of Patent: January 1, 2013Inventor: Yoshiaki Kiso
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120330026Abstract: The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Inventor: Gottfried Sedelmeier
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Publication number: 20120330027Abstract: The present invention relates to a process for the preparation of 5-substituted 1-alkyltetrazoles.Type: ApplicationFiled: March 11, 2011Publication date: December 27, 2012Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stephane Caillon-Morisseau, Pierre-Yves Coqueron, Jens-Dietmar Heinrich, Robert Lui
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Publication number: 20120329844Abstract: The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.Type: ApplicationFiled: August 30, 2012Publication date: December 27, 2012Inventors: Erwin Marti, Hans Rudolf Oswald, Peter Bülmayer, Wolfgang Marterer
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Publication number: 20120316197Abstract: This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 22, 2011Publication date: December 13, 2012Applicant: RAQUALIA PHARMA INC.Inventors: Kiyoshi Kanazawa, Kazuhiko Nonomura, Takako Okumura, Shinichi Koizumi
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Patent number: 8329919Abstract: The invention relates to new forms of salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.Type: GrantFiled: September 28, 2011Date of Patent: December 11, 2012Assignee: Novartis AGInventor: Erwin E Marti
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120309794Abstract: The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.Type: ApplicationFiled: November 5, 2010Publication date: December 6, 2012Applicant: UNIVERSITÀ DI PISAInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Sarabindu Roy, Gino Giannaccini, Antonio Lucacchini
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Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120309944Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there altered profile considered particular useful in therapy.Type: ApplicationFiled: January 24, 2011Publication date: December 6, 2012Applicant: Novo Nordisk Health Care AGInventors: Carsten Behrens, Nils Langeland Johansen, Henrik Sune Andersen, Leif Noerskov-Lauritsen, Jens Buchardt
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Publication number: 20120309757Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120302562Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
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Publication number: 20120302597Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.Type: ApplicationFiled: July 13, 2012Publication date: November 29, 2012Applicant: AFFECTIS PHARMACEUTICALS AGInventor: Michael Bös
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic