Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
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Patent number: 8557816Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: GrantFiled: June 9, 2011Date of Patent: October 15, 2013Assignee: Amgen Inc.Inventors: Stephanie Geuns-Meyer, Victor J. Cee, Isaac Marx, Laurie Schenkel, Ryan White
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Patent number: 8557815Abstract: This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective ?5 receptor partial or full inverse agonists.Type: GrantFiled: August 13, 2010Date of Patent: October 15, 2013Assignee: Concert Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Publication number: 20130267521Abstract: 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: March 15, 2013Publication date: October 10, 2013Applicants: Intellikine LLC, Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Patent number: 8546393Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: GrantFiled: January 26, 2010Date of Patent: October 1, 2013Assignee: SanofiInventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
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Publication number: 20130252936Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: Usher III InitiativeInventors: Roland Werner BÜRLI, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
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Publication number: 20130252961Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.Type: ApplicationFiled: March 5, 2013Publication date: September 26, 2013Applicant: PFIZER INC.Inventors: Simon BAILEY, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
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Patent number: 8541403Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.Type: GrantFiled: February 3, 2011Date of Patent: September 24, 2013Assignee: BioMarin Pharmaceutical Inc.Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard Edwin Post
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Publication number: 20130245021Abstract: Imidazo[1,2-b]pyridazine-based compounds of the formula: are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Inventors: Yingzhi BI, Kenneth Gordon CARSON, Giovanni CIANCHETTA, Michael Alan GREEN, Godwin KUMI, Zhi LIANG, Ying Jade LIU, Alan MAIN, Yulian ZHANG, Gregory Glenn ZIPP
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130245025Abstract: 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: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130245023Abstract: The invention relates to the 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Applicant: SANOFIInventors: Frederic PUECH, Yulin CHIANG, Sylvain COTE DES COMBES, Adrien Tak LI, Philippe BURNIER
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Patent number: 8536168Abstract: The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:Type: GrantFiled: March 13, 2008Date of Patent: September 17, 2013Assignee: Novartis AGInventors: Miao Dai, Feng He, Rishi Kumar Jain, Rajesh Karki, Joseph Kelleher, III, John Lei, Luis Llamas, Michael A. Mcewan, Karen Miller-Moslin, Lawrence Bias Perez, Stefan Peukert, Naeem Yusuff
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Patent number: 8536171Abstract: The invention is related to a method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals of the formula II wherein 5-nitro-2,3-dihydrophthalazine-1,4-dione is solved in water solution of MOH1 where M has the below mentioned meaning, with formation of solution of 5-nitro-2,3-dihydrophthalazine-1,4-dione alkali metal salt, which is catalytically transformed into 5-amino-2,3-dihydrophthalazine-1,4-dione salt at the temperature 40-900C by means of hydrogen under the pressure 1-4 MPa in at the presence of a transition metal catalyst (Pt, Pd) on activated carbon, and separation of crystalline 5-amino-2,3-dihydrophthalazine-1,4-dione salt is performed by water solution diluting with lower alcohol or cyclic lower ether with cooling to the temperature ?5° C. to ?15° C., providing that there is used 5-nitro-2,3-dihydrophthalazine-1,4-dione formed in the reaction of anhydride of 3-nitrophthalic acid with hydrazine hydrate in anhydrous acetic acid at the temperature 100-110° C.Type: GrantFiled: January 15, 2010Date of Patent: September 17, 2013Assignee: Abidopharma PL SP. Z.O.O.Inventors: Admir Musaevich Abidov, Aleksei Silantievich Ishmuratov, Vitalij Vilkin, Irina Georgievna Danilova
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Patent number: 8536166Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: GrantFiled: July 1, 2009Date of Patent: September 17, 2013Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
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Patent number: 8530387Abstract: The present invention relates to new dithiinopyridazinedione derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinedione derivatives.Type: GrantFiled: April 14, 2011Date of Patent: September 10, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Jürgen Benting
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Publication number: 20130231337Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: September 5, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20130231343Abstract: The invention described herein pertains to the treatment of multiple sclerosis. In particular, the invention described herein pertains to the treatment of multiple sclerosis using compounds that modulate the action of acrolein.Type: ApplicationFiled: November 10, 2011Publication date: September 5, 2013Applicant: PURDUE RESEARCH FOUNDATIONInventor: Riyi Shi
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Patent number: 8524713Abstract: The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.Type: GrantFiled: July 29, 2010Date of Patent: September 3, 2013Assignee: Cephalon, IncInventors: Reddeppa reddy Dandu, Robert L. Hudkins, Babu G. Sundar
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Patent number: 8524900Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 1, 2011Date of Patent: September 3, 2013Assignee: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20130225590Abstract: This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABA-A receptor antagonist and/or a ?2, ?3 and ?5 GABA-A receptor agonist.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: CONCERT PHARMACEUTICALS, INC.Inventor: Concert Pharmaceuticals, Inc.
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Publication number: 20130224114Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: ApplicationFiled: March 25, 2013Publication date: August 29, 2013Applicant: The University of SydneyInventor: The University of Sydney
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Publication number: 20130225580Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: CHEMOCENTRYX, INC.Inventor: ChemoCentryx, Inc.
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Publication number: 20130224107Abstract: Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed.Type: ApplicationFiled: December 2, 2010Publication date: August 29, 2013Applicant: SHANGHAI DE NOVO PHARMATECH CO LTD.Inventor: Daxin Gao
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Publication number: 20130224312Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.Type: ApplicationFiled: November 16, 2012Publication date: August 29, 2013Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCHInventor: Mayo Foundation for Medical Education and Research
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Patent number: 8518943Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: August 27, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Publication number: 20130217693Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.Type: ApplicationFiled: April 1, 2011Publication date: August 22, 2013Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
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Publication number: 20130217690Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, 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 p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
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Publication number: 20130217685Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: January 8, 2013Publication date: August 22, 2013Applicant: UNIVERSITY OF MASSACHUSETTSInventor: University of Massachusetts
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Publication number: 20130217662Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
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Publication number: 20130210825Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.Type: ApplicationFiled: July 27, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Publication number: 20130210779Abstract: The present invention provides means for identifying or classifying breast tumors based on the levels of nuclear cathepsin-L (CTSL) and nuclear p53 binding protein (53BP1), and methods of treating thereof.Type: ApplicationFiled: February 15, 2013Publication date: August 15, 2013Applicant: The Washington UniversityInventor: The Washington University
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Patent number: 8507489Abstract: The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: GrantFiled: October 18, 2007Date of Patent: August 13, 2013Assignee: SGX Pharmaceuticals, Inc.Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth Anne Jefferson
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Publication number: 20130203714Abstract: The invention concerns bicyclic compounds of Formula I wherein R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: ApplicationFiled: August 1, 2012Publication date: August 8, 2013Applicant: ASTRAZENECA R&DInventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
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Publication number: 20130202573Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: August 8, 2013Applicant: Ardea Biosciences, Inc.Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
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Patent number: 8501765Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), which are useful as kinase inhibitors, more specifically useful as checkpoint kinase I (chk1) inhibitors, thus useful as cancer therapeutics.Type: GrantFiled: June 10, 2009Date of Patent: August 6, 2013Assignee: Genentech, Inc.Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
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Patent number: 8501731Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: GrantFiled: March 18, 2009Date of Patent: August 6, 2013Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
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Patent number: 8501056Abstract: The invention relates to a method for the solvent-free preparation of a homogenizate, especially for implants or microparticles, wherein one or more polymers and one or more active constituents, as raw materials, are homogenized together below the glass transition temperature of the polymer(s) and, when homogenization is complete, brought to room temperature.Type: GrantFiled: May 23, 2002Date of Patent: August 6, 2013Assignee: Hexal AGInventors: Gregor Schütz, Brigitte Freudensprung
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Patent number: 8501940Abstract: Provided herein are compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof, which are useful as pharmaceutical compositions for the treatment of metabolic diseases and disorders.Type: GrantFiled: June 25, 2009Date of Patent: August 6, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
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Patent number: 8501738Abstract: This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABAA receptor antagonist or an ?2- and/or an ?3-GABAA receptor partial agonist.Type: GrantFiled: June 22, 2010Date of Patent: August 6, 2013Assignee: Concert Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Julie F. Liu
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Publication number: 20130196979Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Patent number: 8497266Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: May 25, 2009Date of Patent: July 30, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8497368Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 10, 2010Date of Patent: July 30, 2013Assignee: Novartis AGInventors: Feng He, Miao Dai, Xingnian Fu, Yue Li, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Zhengtian Yu, Ji Yue Zhang
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Publication number: 20130190306Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: March 6, 2013Publication date: July 25, 2013Applicant: BioMarin Pharmaceutical Inc.Inventor: BioMarin Pharmaceutical Inc.
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Publication number: 20130190172Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 5, 2011Publication date: July 25, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Francis Pahutski, JR.
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Publication number: 20130190309Abstract: 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: December 16, 2009Publication date: July 25, 2013Inventor: Chi B. Vu
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Publication number: 20130190314Abstract: The invention relates to derivatives of 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine and 6-cycloamino-2-furanyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment or prevention of illnesses involving casein kinase 1 epsilon and/or casein kinase 1 delta.Type: ApplicationFiled: December 17, 2009Publication date: July 25, 2013Inventors: Yulin Chiang, Cecile Enguehard-Gueiffier, Pascal George, Alaim Gueiffier, Frederic Puech, Mireille Sevrin, Qiuxia Zhao
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Patent number: 8492379Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: GrantFiled: December 2, 2008Date of Patent: July 23, 2013Assignee: The University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Patent number: 8492373Abstract: Bicyclic aryl substituted triazoles or heteroaryl 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: GrantFiled: December 1, 2010Date of Patent: July 23, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
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Publication number: 20130184240Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.Type: ApplicationFiled: September 8, 2011Publication date: July 18, 2013Applicant: Shionogi & Co., Ltd.Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
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Patent number: 8486901Abstract: Novel sodium channel blocking compounds tetrodotoxm galactopyranosides of formula I were isolated and purified by HPLC and identified further through IR, NMR, GC, and MS. The compounds have a galactopyranosyl moiety attached to C11 of tetrodotoxin and retain the analgesic activity of the latter. Pharmaceutical compositions and medical uses thereof are further disclosed.Type: GrantFiled: March 26, 2010Date of Patent: July 16, 2013Assignee: Wex Medical LimitedInventor: Weiyang Lin