Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Publication number: 20150087644Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
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Patent number: 8987267Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.Type: GrantFiled: July 21, 2011Date of Patent: March 24, 2015Assignee: Temple University—of the Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 8987260Abstract: Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.Type: GrantFiled: February 6, 2014Date of Patent: March 24, 2015Assignee: F. Hoffmann-La Roche AGInventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
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Publication number: 20150080393Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.Type: ApplicationFiled: September 5, 2014Publication date: March 19, 2015Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
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Publication number: 20150079079Abstract: The present invention provides compositions and methods of use in the treatment/prevention of chlamydial infection and/or diseases and disorders associated with chlamydial infection in a subject.Type: ApplicationFiled: September 11, 2014Publication date: March 19, 2015Inventors: Allen W. Tsang, Cristina M. Furdui
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Publication number: 20150080392Abstract: A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.Type: ApplicationFiled: July 21, 2012Publication date: March 19, 2015Applicants: HANGZHOU MINSHENG PHARMACEUTICAL CO. LTD, HANGZHOU MINSHENG INSTITUTES FOR PHARMA RESEARCHInventors: Shulong Wang, Jian Cai, Qiufu Ge, Dianwu Guo, Lan Yang, Binnan Huang, Zhenhua Liu, Zhonghua Peng, Ximing Shen, Feiyu Feng
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Publication number: 20150072955Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: October 14, 2014Publication date: March 12, 2015Applicant: Resverlogix Corp.Inventor: Henrik C. Hansen
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Publication number: 20150071919Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Patients to be treated include those that have been treated with Tarceva or other therapeutic compounds and relapsed or are resistant to treatment. The compounds described herein may exhibit a synergistic effect when administered with another agent.Type: ApplicationFiled: September 9, 2014Publication date: March 12, 2015Inventors: Thomas F. WHITE, Dan HOTH
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Publication number: 20150072959Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20150065483Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150065495Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
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Patent number: 8969343Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: December 19, 2013Date of Patent: March 3, 2015Assignee: Quanticel Pharmaceuticals, Inc.Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Patent number: 8969342Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: GrantFiled: March 22, 2010Date of Patent: March 3, 2015Assignees: Brandeis University, University of Georgia Research Foundation, Inc., The Brigham and Women's Hospital, Inc.Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Boris Striepen, Suresh Kumar Gorla, Mandapati Kavitha
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Publication number: 20150057272Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20150057263Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.Type: ApplicationFiled: March 19, 2013Publication date: February 26, 2015Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
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Publication number: 20150056193Abstract: The present disclosure provides methods of that include detecting in a biological sample from a patient having or suspected of having cancer the presence of a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and detecting in the biological sample the presence of a mutant EGFR polypeptide or a polynucleotide encoding the same. In some aspects, the disclosure provides methods of treating a patient for cancer that include determining that a biological sample from a tumor in the patient includes a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and a mutant EGFR polypeptide or a polynucleotide encoding the same and administering to the patient a therapeutically effective amount of a ROS1 inhibitor and an EGFR inhibitor, thereby treating the patient for cancer.Type: ApplicationFiled: April 18, 2013Publication date: February 26, 2015Applicant: CELL SIGNALING TECHNOLOGY, INC.Inventors: Katherine Eleanor Crosby, Victoria McGuinness Rimkunas, Matthew Ren Silver, Herbert Haack
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Publication number: 20150057275Abstract: This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping.Type: ApplicationFiled: September 2, 2014Publication date: February 26, 2015Inventors: Dora Dias-Santagata, Anthony John Iafrate
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Patent number: 8962620Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 24, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150051203Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.Type: ApplicationFiled: March 27, 2013Publication date: February 19, 2015Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
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Publication number: 20150051208Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: August 11, 2014Publication date: February 19, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150045359Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.Type: ApplicationFiled: January 8, 2013Publication date: February 12, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
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Patent number: 8952058Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: GrantFiled: October 12, 2012Date of Patent: February 10, 2015Assignee: Ambit Biosciences CorporationInventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
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Publication number: 20150038486Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: July 7, 2014Publication date: February 5, 2015Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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Publication number: 20150038460Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: October 16, 2014Publication date: February 5, 2015Applicant: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
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Publication number: 20150038510Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.Type: ApplicationFiled: March 25, 2013Publication date: February 5, 2015Inventors: John David Lawson, Mark Sabat, Christopher Smith, Haixia Wang, Young K. Chen, Toufike Kanouni
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Publication number: 20150038506Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.Type: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Applicants: Agency for Science, Technology and Research, University of BaselInventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
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Patent number: 8946217Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: June 17, 2014Date of Patent: February 3, 2015Assignee: F. Hoffmann-La Roche AGInventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Patent number: 8946216Abstract: The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: GrantFiled: August 29, 2011Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Yonqi Deng, Gerald W. Shipps, Jr., Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Kiran Muppalla
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Patent number: 8945510Abstract: Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.Type: GrantFiled: May 24, 2012Date of Patent: February 3, 2015Assignee: Probiodrug AGInventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
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Publication number: 20150030588Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.Type: ApplicationFiled: November 12, 2012Publication date: January 29, 2015Inventors: Katayoun Jessen, Xin Guo, Pingda Ren, Christian Rommel, Yi Liu
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Publication number: 20150031695Abstract: Small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. The compositions may be used for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC).Type: ApplicationFiled: May 12, 2014Publication date: January 29, 2015Inventor: Michael West Brooks
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150031673Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
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Patent number: 8940730Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: GrantFiled: March 16, 2010Date of Patent: January 27, 2015Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Publication number: 20150025071Abstract: Compounds of the formula I in which U, V and W have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.Type: ApplicationFiled: January 14, 2013Publication date: January 22, 2015Applicant: MERCK PATENT GMBHInventors: Hans-Peter Buchstaller, Christina Esdar, Birgitta Leuthner
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Publication number: 20150025072Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).Type: ApplicationFiled: October 7, 2014Publication date: January 22, 2015Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Penelope Jane HUGGINS, Jack Gordon PARSONS
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Publication number: 20150018351Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: ApplicationFiled: July 10, 2014Publication date: January 15, 2015Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20150018313Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT, Armin HECKEL
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Publication number: 20150017156Abstract: The present invention relates to gene regulation. In particular, the present invention provides small compounds capable of modulating ESX-mediated transcription and related methods of therapeutic and research use. In addition, the present invention provides methods for treating conditions associated with aberrant EGFR expression with ESX-mediated transcription modulators (e.g., ESX-mediated transcription inhibitors).Type: ApplicationFiled: September 14, 2012Publication date: January 15, 2015Applicants: THE OHIO STATE UNIVERSITY, THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Anna Mapp, Quintin Pan
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Publication number: 20150018331Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: March 24, 2014Publication date: January 15, 2015Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Patent number: 8933085Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: November 18, 2011Date of Patent: January 13, 2015Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Patent number: 8933070Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.Type: GrantFiled: July 4, 2011Date of Patent: January 13, 2015Assignee: University Health NetworkInventors: Guohua Pan, Jacqueline M. Mason, Xin Wei, Miklos Feher
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Publication number: 20150011547Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: ApplicationFiled: September 2, 2014Publication date: January 8, 2015Applicant: ASANA BIOSCIENCES, LLCInventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
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Publication number: 20150011549Abstract: Provided is a tablet showing improved hygroscopicity, which contains, as a pharmaceutically active ingredient, a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C. A tablet containing a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C. and an additive showing an equilibrium moisture absorption rate at relative humidity 75% at 25 degrees C. of not less than 7 wt % relative to its dry weight.Type: ApplicationFiled: February 14, 2013Publication date: January 8, 2015Inventor: Yuko Deharu
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Publication number: 20150011533Abstract: The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and R1 are as defined in the claims.Type: ApplicationFiled: January 30, 2013Publication date: January 8, 2015Applicant: Vernalis (R&D) LimitedInventors: Stephen Stokes, Christopher John Graham, Stuart Christopher Ray, Emma Jane Stefaniak
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Publication number: 20150011548Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: ApplicationFiled: October 9, 2012Publication date: January 8, 2015Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Publication number: 20150005302Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: December 21, 2012Publication date: January 1, 2015Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
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Publication number: 20150004134Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: December 3, 2013Publication date: January 1, 2015Applicant: CALITHERA BIOSCIENCES, INC.Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren