Ring Sulfur In The Additional Hetero Ring Patents (Class 514/342)
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Patent number: 8501746Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: June 4, 2007Date of Patent: August 6, 2013Assignees: Xenon Pharmaceuticals Inc., Novartis AGInventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 8501786Abstract: 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 ?3-adrenoceptor.Type: GrantFiled: March 23, 2009Date of Patent: August 6, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Patent number: 8501812Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: GrantFiled: March 1, 2011Date of Patent: August 6, 2013Assignee: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Patent number: 8501794Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: GrantFiled: November 4, 2009Date of Patent: August 6, 2013Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130196967Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 29, 2013Publication date: August 1, 2013Inventors: Alessandra BARTOLOZZI, Zhidong CHEN, Jonathon Alan DINES, Ho Yin LO, Pui Leng LOKE, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20130190312Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.Type: ApplicationFiled: November 29, 2012Publication date: July 25, 2013Inventors: Jiann-Jyh HUANG, Shih-Hsien CHUANG, Ying-Shuan Eda LEE, Yu-Ling HUANG, Johnson LAU
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Patent number: 8492411Abstract: A compound of formula (I): or a pharmaceutically acceptable salt, prodrug and/or solvate thereof, and a method for the treatment of an acute or chronic inflammatory disease by inhibiting the production of at least one pro-inflammatory cytokine selected from TNF-alpha, IFN-gamma, IL-8 and IL-10, involving administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (I) as defined above.Type: GrantFiled: July 17, 2010Date of Patent: July 23, 2013Assignee: Faes Farma, S.A.Inventors: Victor Rubio Royo, Antonio De La Hera Martinez, Melchor Alvarez De Mon Soto, Ana Munoz Munoz
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Publication number: 20130183269Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130184258Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130184312Abstract: The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a power X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventor: Otsuka Pharmaceutical Co., Ltd.
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Patent number: 8481572Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.Type: GrantFiled: August 10, 2008Date of Patent: July 9, 2013Assignee: Urifer Ltd.Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
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Patent number: 8481456Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: November 17, 2010Date of Patent: July 9, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
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Patent number: 8481574Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: October 12, 2007Date of Patent: July 9, 2013Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Patent number: 8481524Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: GrantFiled: March 31, 2010Date of Patent: July 9, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
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Publication number: 20130172391Abstract: The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.Type: ApplicationFiled: February 1, 2013Publication date: July 4, 2013Applicant: ARES TRADING S.A.Inventor: Ares Trading S.A.
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Publication number: 20130172248Abstract: The invention relates to 3-[4-(phenylaminooxalylamino)phenyl]hex-4-ynoic acids, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3 and R4 are each defined as specified, and to physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: January 4, 2013Publication date: July 4, 2013Inventors: Elisabeth DEFOSSA, Viktoria DIETRICH, Thomas KLABUNDE, Stefanie KEIL, Siegfried STENGELIN, Guido HASCHKE, Andreas HERLING, Johanna KUHLMANN-GOTTKE, Stefan BARTOSCHEK, Simon GESSLER, Angela DUDDA, Guenter BILLEN, Thomas OLPP, Joerg RIEKE-ZAPP
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Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
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Patent number: 8476287Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: December 24, 2010Date of Patent: July 2, 2013Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Patent number: 8476257Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: December 3, 2008Date of Patent: July 2, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Patent number: 8476302Abstract: The present invention is directed to ?-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: GrantFiled: September 26, 2011Date of Patent: July 2, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Michael N. Greco, Margery A. Connelly, Shyamali Ghosh, Dennis J. Hlasta, Edward C. Lawson, Eric Strobel, Michele A. Weidner-Wells, Hong Ye
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Publication number: 20130165451Abstract: The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 19, 2012Publication date: June 27, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
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Patent number: 8470855Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residuType: GrantFiled: November 10, 2006Date of Patent: June 25, 2013Assignee: IMTM GmbHInventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
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Publication number: 20130157950Abstract: The present invention was accomplished for the purpose of developing a method for effectively treating and/or preventing synucleinopathies, and is based on a discovery that an adiponectin receptor agonist suppresses ? (alpha)-synuclein aggregation, tau phosphorylation and a decrease in proteasomal activity. The method of the present invention for treating and/or preventing neurodegenerative diseases includes a step of administering an effective dose of at least one effective element selected from a group consisting of: adiponectin as an adiponectin receptor agonist; a compound inducing expression of adiponectin; globular adiponectin; and a compound inducing expression of globular adiponectin. The present invention further provides a screening method of the adiponectin receptor agonist for treating and/or preventing neurodegenerative diseases.Type: ApplicationFiled: August 20, 2012Publication date: June 20, 2013Applicant: TOKYO METROPOLITAN INSTITUTE OF MEDICAL SCIENCEInventors: Makoto HASHIMOTO, Kazunari SEKIYAMA, Yoshiki TAKAMATSU, Masayo FUJITA, Akio SEKIGAWA
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Publication number: 20130158077Abstract: The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.Type: ApplicationFiled: October 18, 2012Publication date: June 20, 2013Applicant: ARES TRADING S.A.Inventor: Ares Trading S.A.
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Publication number: 20130158078Abstract: Heterocyclic sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: May 12, 2011Publication date: June 20, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Patent number: 8466177Abstract: Compounds that are useful in treating or preventing viral infections, such as influenza, are described herein. Further described are compositions made from these compounds and methods for using the compounds and their compositions in treating or preventing viral infections.Type: GrantFiled: October 31, 2008Date of Patent: June 18, 2013Assignee: The UAB Research FoundationInventors: Ming Luo, Zhen Yang
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Publication number: 20130150339Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: December 6, 2012Publication date: June 13, 2013Applicant: Amgen Inc.Inventor: Amgen Inc.
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Publication number: 20130149386Abstract: A method is provided for early treatment of steatosis, which method is based on early detection of steatosis based on the detection of CD36. CD36 is determined in a body fluid, and CD36 levels above a predetermined value is indicative of steatosis.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: REGION NORDJYLLANDInventor: REGION NORDJYLLAND
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Publication number: 20130150311Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.Type: ApplicationFiled: December 13, 2011Publication date: June 13, 2013Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
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Publication number: 20130143927Abstract: 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 or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 8, 2012Publication date: June 6, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Publication number: 20130143930Abstract: The present invention relates to oxaloacetate compounds that activate AMP-activated protein kinase (AMPK), including the preparation of the compounds, compositions containing the compounds, preserving said compounds and the use of the compounds in the prevention or treatment of disorders such as diabetes, metabolic syndrome, obesity, cardiovascular disease, Alzheimer's disease, and cancer.Type: ApplicationFiled: June 22, 2011Publication date: June 6, 2013Inventor: Alan B. Cash
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Patent number: 8455523Abstract: The present invention is directed to a composition and method for the treatment of hyperlipidemias by targeting Microsomal triglyceride transfer protein (MTP). In particular, the present invention is directed to a combination of at least one MTP inhibitor and at least one lipid-lowering agent, both in an amount effective to treat hyperlipidemias.Type: GrantFiled: January 7, 2011Date of Patent: June 4, 2013Assignee: The Research Foundation of State University of New YorkInventors: M. Mahmood Hussain, Jahangir Igbal, Joby Josekutty
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Patent number: 8455480Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the neonicotinoids, and which are highly suitable for controlling animal pests such as insects and undesired acarids.Type: GrantFiled: September 13, 2008Date of Patent: June 4, 2013Assignee: Bayer Cropscience AGInventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
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Publication number: 20130137728Abstract: Disclosed are compounds or pharmaceutically acceptable salts thereof, having the structure of formula I. Also disclosed are methods of preventing and/or treating degenerative disease in a subject, comprising administering to said subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions for preventing and/or treating de-generative disease in a subject comprising a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 24, 2011Publication date: May 30, 2013Applicant: MUSC Foundation For Research And DevelopmentInventors: Craig Cano Beeson, Baerbel Rohrer, Nathan Perron
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Publication number: 20130137682Abstract: A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q1, Q2, Q3, Q4, R2, R4, R5, R6 and m have the same meanings described in the specification) and a neonicotinoid compound selected from the group consisting of imidacloprid, thiacloprid, acetamiprid, nitenpyram, clothianidin, and thiamethoxam, and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and a neonicotinoid compound selected from the group consisting of imidacloprid, thiacloprid, acetamiprid, nitenpyram, clothianidin, and thiamethoxam is applied to a pest or a pest habitat.Type: ApplicationFiled: July 25, 2011Publication date: May 30, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Kaori Ikari
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130131099Abstract: Nitrated and non-nitrated compounds capable of protecting brain tissue from injury and useful as therapeutic agents to treat neurodegenerative diseases and conditions are disclosed. Methods of using the compounds in therapeutic treatments, and methods of preparing the compounds, also are disclosed.Type: ApplicationFiled: May 4, 2011Publication date: May 23, 2013Inventors: Gregory R.J. Thatcher, Zhihui Qin, Jia Luo
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Publication number: 20130131085Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.Type: ApplicationFiled: December 13, 2012Publication date: May 23, 2013Applicant: ABBOTT LABORATORIESInventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
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Patent number: 8445690Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: February 16, 2011Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130123254Abstract: The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.Type: ApplicationFiled: September 14, 2012Publication date: May 16, 2013Inventors: Barbara Biemans, Georg Jaeschke, Lothar Lindemann, Wolfgang Muster, Heinz Stadler, Eric Vieira
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Publication number: 20130123106Abstract: Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III).Type: ApplicationFiled: November 7, 2012Publication date: May 16, 2013Inventor: Paresh T. Gandhi
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Patent number: 8435976Abstract: The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: September 8, 2010Date of Patent: May 7, 2013Assignee: F. Hoffmann-La RocheInventors: Xiaojing Wang, Allen J. Ebens, Jr.
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Publication number: 20130108693Abstract: A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.Type: ApplicationFiled: September 24, 2012Publication date: May 2, 2013Applicant: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFTInventors: Juan A. VERGEZ, Marcelo A. RICCI
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Publication number: 20130109696Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 1, 2011Publication date: May 2, 2013Applicant: Pfizer LimitedInventors: Benjamin Scott Greener, Brian Edward Marron, David Simon Millan, David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Publication number: 20130109667Abstract: The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: June 28, 2011Publication date: May 2, 2013Applicants: Pfizer Limited, Icagen ,Inc.Inventors: Christopher John Markworth, Brian Edward Marron, David James Rawson, Robert Ian Storer, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130109675Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-cat oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.Type: ApplicationFiled: August 27, 2012Publication date: May 2, 2013Inventors: Ramanuj Dasgupta, Foster Gonsalves
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Publication number: 20130102637Abstract: Provided is a novel pest control agent using at least one imino derivative represented by the following chemical formula (I):Type: ApplicationFiled: July 4, 2011Publication date: April 25, 2013Applicants: GIFU UNIVERSITY, MEIJI SEIKA PHARMA CO., LTD.Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Masahiro Nomura, Satoshi Nakamura, Kazumi Yamamoto
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Publication number: 20130102605Abstract: The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 21, 2011Publication date: April 25, 2013Inventors: Peng Liang, Morihiro Mitsuya, Yoshio Ogino, Changhe Qi, Hidekazu Takahashi, Paul Tempest, Jiabing Wang, Yuguang Wang, Zhenzhen Wang, Shaohua Zhang, Nanyan Zhou, Jiuxiang Zhu