Additional Hetero Ring Containing Patents (Class 546/187)
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Patent number: 10584136Abstract: Aluminum chloride is separated from a silane mixture containing aluminum chloride by reacting the aluminum chloride with a compound reactive therewith which forms an ionic liquid or solid, and separating the ionic liquid or solid from the now-purified silane.Type: GrantFiled: April 3, 2017Date of Patent: March 10, 2020Assignee: WACKER CHEMIE AGInventors: Andreas Bockholt, Konrad Mautner
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Patent number: 10202362Abstract: This present disclosure is directed to compounds of formula (I): where R1a, R3, Y, and Z are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.Type: GrantFiled: December 11, 2017Date of Patent: February 12, 2019Assignee: Celtaxsys, Inc.Inventors: Kurt Roinestad, William Guilford, Tom Kirkland, Lopa Bhatt, Eric Springman
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Patent number: 9409884Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) in which the variables are as described herein.Type: GrantFiled: January 31, 2013Date of Patent: August 9, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
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Patent number: 9353092Abstract: The present disclosure provides compositions and methods for the synthesis and use of croconaine compounds. The disclosed compounds are easily prepared from croconic acid. A halothiophene is reacted with an alkanolamine, the resulting aminothiophene is modified by appending a desired functional group to the hydroxyl group, and the modified aminothiophene is reacted with croconic acid to form the final compound. Applications of such croconaine compounds include photothermal imaging, photothermal therapy, light-activated drug release, and tissue welding.Type: GrantFiled: June 21, 2014Date of Patent: May 31, 2016Assignee: University of Notre Dame du LacInventor: Bradley Smith
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Patent number: 9029531Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: GrantFiled: November 21, 2013Date of Patent: May 12, 2015Assignee: Agios Pharmaceuticals, Inc.Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Patent number: 9023854Abstract: The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: GrantFiled: December 5, 2008Date of Patent: May 5, 2015Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Publication number: 20150111888Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.Type: ApplicationFiled: April 30, 2013Publication date: April 23, 2015Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
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Patent number: 8987303Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: March 13, 2013Date of Patent: March 24, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
Publication number: 20150079028Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.Type: ApplicationFiled: August 5, 2013Publication date: March 19, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTDInventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo -
Patent number: 8980921Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: March 13, 2013Date of Patent: March 17, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20150065490Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE
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Patent number: 8962845Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.Type: GrantFiled: September 25, 2012Date of Patent: February 24, 2015Assignee: National Health Research InstitutesInventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao
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Publication number: 20150045553Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.Type: ApplicationFiled: December 27, 2012Publication date: February 12, 2015Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Toshio Nakamura, Seiji Masuda
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Patent number: 8952004Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n 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: GrantFiled: January 5, 2011Date of Patent: February 10, 2015Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20150011754Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 17, 2014Publication date: January 8, 2015Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20150005279Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 26, 2014Publication date: January 1, 2015Applicant: ABBVIE INC.Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
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Publication number: 20150005501Abstract: The present disclosure provides compositions and methods for the synthesis and use of croconaine compounds. The disclosed compounds are easily prepared from croconic acid. A halothiophene is reacted with an alkanolamine, the resulting aminothiophene is modified by appending a desired functional group to the hydroxyl group, and the modified aminothiophene is reacted with croconic acid to form the final compound. Applications of such croconaine compounds include photothermal imaging, photothermal therapy, light-activated drug release, and tissue welding.Type: ApplicationFiled: June 21, 2014Publication date: January 1, 2015Applicant: University of Notre Dame du LacInventor: Bradley Smith
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Publication number: 20140378429Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.Type: ApplicationFiled: January 31, 2013Publication date: December 25, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
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Publication number: 20140378471Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: ApplicationFiled: September 9, 2014Publication date: December 25, 2014Inventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 8916555Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: GrantFiled: March 14, 2013Date of Patent: December 23, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20140369961Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
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Patent number: 8907098Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the meanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: GrantFiled: November 18, 2010Date of Patent: December 9, 2014Assignee: MERCK PATENT GmbHInventors: Frank Stieber, Dirk Wienke
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Publication number: 20140349918Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.Type: ApplicationFiled: September 10, 2012Publication date: November 27, 2014Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and ResearchInventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
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Publication number: 20140349989Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.Type: ApplicationFiled: December 20, 2013Publication date: November 27, 2014Applicant: ALZHEIMER'S INSTITUTE OF AMERICAInventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
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Publication number: 20140341851Abstract: 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: April 4, 2014Publication date: November 20, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
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Publication number: 20140343074Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.Type: ApplicationFiled: March 14, 2014Publication date: November 20, 2014Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
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Publication number: 20140343075Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: July 30, 2014Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
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Patent number: 8889670Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 16, 2010Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20140336165Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.Type: ApplicationFiled: November 14, 2012Publication date: November 13, 2014Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
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Publication number: 20140336168Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 13, 2014Inventor: AbbVie Inc.
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Publication number: 20140330010Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.Type: ApplicationFiled: December 7, 2012Publication date: November 6, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Toshio Nakamura, Seiji Masuda
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Publication number: 20140329803Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.Type: ApplicationFiled: November 16, 2012Publication date: November 6, 2014Inventors: Miles Congreve, Giles Brown, Julie Cansfield, Benjamin Tehan
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Patent number: 8877778Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: December 7, 2011Date of Patent: November 4, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20140323458Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
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Patent number: 8871770Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: February 3, 2014Date of Patent: October 28, 2014Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20140314669Abstract: The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi.Type: ApplicationFiled: August 17, 2012Publication date: October 23, 2014Applicant: PIRAMAL IMAGING SAInventors: Markus Berger, Martin Kruger, Jessica Lohrke, Michael Reinhardt, Holger Siebeneicher
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Publication number: 20140315918Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
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Publication number: 20140315914Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: April 14, 2014Publication date: October 23, 2014Inventors: Astrid Netz, Thorsten Oost, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140315893Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediType: ApplicationFiled: November 22, 2012Publication date: October 23, 2014Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
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Patent number: 8865702Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: GrantFiled: July 23, 2008Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20140309193Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.Type: ApplicationFiled: December 5, 2012Publication date: October 16, 2014Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
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Patent number: 8859557Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: GrantFiled: August 21, 2012Date of Patent: October 14, 2014Assignee: Abbott GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Martin Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8859776Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: GrantFiled: October 5, 2010Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew Ernst Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Gerald W. Shipps, Jr., Malcolm MacCoss
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Patent number: 8853205Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.Type: GrantFiled: February 19, 2009Date of Patent: October 7, 2014Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Vemuri
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Publication number: 20140296289Abstract: Thiazolyl oxime ethers and hydrazones of the formula (I), in which the symbols A, L1, L2, Y, W, X, R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also methods for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: February 28, 2014Publication date: October 2, 2014Applicant: Bayer CropScience AGInventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting
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1H-BENZIMIDAZOLE-4-CARBOXAMIDES SUBSTITUTED WITH PHENYL AT THE 2-POSITION ARE POTENT PARP INHIBITORS
Publication number: 20140296235Abstract: Compounds having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).Type: ApplicationFiled: April 11, 2014Publication date: October 2, 2014Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda -
Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Publication number: 20140275110Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: April 11, 2014Publication date: September 18, 2014Inventors: Thorsten Oost, Astrid Netz, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140275068Abstract: The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1. The compounds are useful for the treatment or prevention of a range of conditions including, e.g., migraine, epilepsy, non-epileptic seizures, brain injury, and cardiovascular disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Proximagen LimitedInventors: Edward Savory, Daniel Hill, Oldrich Kocian