Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The 1,3-diazine Ring By Nonionic Bonding Patents (Class 514/252.19)
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Publication number: 20140186452Abstract: The present disclosure generally relates to a process for preparing therapeutic nanoparticles, where the process includes combining a therapeutic agent with an organic acid. The therapeutic nanoparticles may have, for example, improved drug loading and/or drug release properties.Type: ApplicationFiled: September 16, 2013Publication date: July 3, 2014Applicant: BIND THERAPEUTICS, INC.Inventors: Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
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Publication number: 20140179711Abstract: The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jean Lajeunesse, John D. DiMarco, Michael Galella, Ramakrishnan Chidambaram
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Publication number: 20140178475Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.Type: ApplicationFiled: September 16, 2013Publication date: June 26, 2014Applicant: BIND Therapeutics, Inc.Inventors: Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
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Publication number: 20140179670Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.Type: ApplicationFiled: July 31, 2012Publication date: June 26, 2014Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
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Publication number: 20140141099Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Inventors: Julian Golec, John Pollard, James Westcott, Hayley Binch, Michael Mortimore, Daniel Robinson
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Publication number: 20140135341Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: January 10, 2014Publication date: May 15, 2014Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Laurence Francoise Bernadette MARCONNET-DECRANE, Sandrine Francoise Dominique GAURRAND, Patrick René ANGIBAUD
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Publication number: 20140135308Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 23, 2014Publication date: May 15, 2014Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20140128406Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140128410Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: March 18, 2013Publication date: May 8, 2014Applicant: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20140120185Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.Type: ApplicationFiled: April 4, 2012Publication date: May 1, 2014Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
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Publication number: 20140107128Abstract: Novel heterocyclic compounds having the Formula I: wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.Type: ApplicationFiled: December 17, 2013Publication date: April 17, 2014Inventors: Dmitry TWOROWSKI, Ron Matsievitch, Vladimir Kogan
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Publication number: 20140087992Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.Type: ApplicationFiled: September 20, 2013Publication date: March 27, 2014Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
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Patent number: 8680103Abstract: The invention relates to a pharmaceutical composition of a crystalline monohydrate of the compound of formula (IV) wherein the crystalline monohydrate is characterized by certain unit cell parameters.Type: GrantFiled: July 31, 2012Date of Patent: March 25, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jean Lajeunesse, John D. DiMarco, Michael Galella, Ramakrishnan Chidambaram
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Publication number: 20140080799Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: September 20, 2013Publication date: March 20, 2014Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20140079636Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: March 15, 2013Publication date: March 20, 2014Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
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Patent number: 8664219Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: June 2, 2010Date of Patent: March 4, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20140057915Abstract: There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: August 16, 2013Publication date: February 27, 2014Applicants: TOPIVERT PHARMA LIMITED, RESPIVERT LIMITEDInventors: CLAIRE ANNE MARIE CARIOU, CATHERINE ELISABETH CHARRON, EUAN ALEXANDER FRASER FORDYCE, MATTHEW COLIN THOR FYFE, DANIEL HAMZA, KAZUHIRO ITO, JOHN KING-UNDERWOOD, PETER JOHN MURRAY, STUART THOMAS ONIONS, STEPHEN MALCOLM THOM, HAYLEY TEGAN ANGELA WATSON, JONATHAN GARETH WILLIAMS
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Publication number: 20140057911Abstract: Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Inventors: Franco Lori, James Chafouleas, Davide De Forni, Antonio Solinas, Zoltán Varga, Zoltán Greff, László Örfi, György Kéri
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Publication number: 20140051708Abstract: The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: April 3, 2012Publication date: February 20, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Maria Gabriella Brasca, Marina Caldarelli, Giovanni Cervi, Teresa Disingrini, Francesca Quartieri
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Publication number: 20140045845Abstract: The invention provides novel pyrimidine derivatives of formula (I), methods of preparing such compounds, pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer; wherein R1-R11, Z, and Y are as defined in the specification.Type: ApplicationFiled: March 23, 2012Publication date: February 13, 2014Applicant: CHEMILIA ABInventors: Marita Högberg, Emma Dahlstedt, Olof Smitt, Tommy Johansson
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Publication number: 20140038938Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Mario JESKE, Ingo FLAMME, Friederike STOLL, Hartmut BECK, Metin AKBABA
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Publication number: 20140037647Abstract: Disclosed herein are new prognostic molecular markers for prostate cancer. More specifically, the invention has identified that overexpression or amplification of at least one of AURKA or MYCN define a distinct subgroup of prostate cancer that is predisposed to the development of lethal NEPC, who will benefit from early intervention.Type: ApplicationFiled: March 28, 2012Publication date: February 6, 2014Applicant: CORNELL UNIVERSITYInventors: Mark A. Rubin, Himisha Beltran
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Publication number: 20140031354Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: ApplicationFiled: July 30, 2012Publication date: January 30, 2014Applicant: Astar Biotech LLCInventors: Chunrong YU, Haihong Huang, Dongfeng Zhang, Peng Li
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Publication number: 20140031329Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: February 18, 2013Publication date: January 30, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GmbH
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Publication number: 20140024641Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.Type: ApplicationFiled: January 7, 2013Publication date: January 23, 2014Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
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Publication number: 20140023642Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.Type: ApplicationFiled: March 31, 2012Publication date: January 23, 2014Applicant: Impact Therapeutics, Inc.Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
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Publication number: 20140018368Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.Type: ApplicationFiled: July 1, 2013Publication date: January 16, 2014Applicants: Genetech, Inc., Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 8629132Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.Type: GrantFiled: November 12, 2010Date of Patent: January 14, 2014Assignees: Genosco, Oscotec, Inc.Inventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Koh, Hee Kyu Lee, Youngsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
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Publication number: 20140010866Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: December 29, 2011Publication date: January 9, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20140011770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130344140Abstract: Methods of selectively targeting a p53-deficient cancer cell, comprising administering to a patient suffering from cancer (i) a reversible cell cycle arrest-inducing agent for inducing cell cycle arrest in a p53-positive cell; and (ii) an aurora kinase inhibitor, wherein said reversible cell cycle arrest-inducing agent is administered prior to administration of said aurora kinase inhibitor, and pharmaceutical combinations, kits and oral dosage forms for the same.Type: ApplicationFiled: March 4, 2011Publication date: December 26, 2013Applicant: Agency for Science, Technology and ResearchInventors: Chit Fang Cheok, David Lane
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Publication number: 20130338111Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicants: Icagen, Inc., Pfizer LimitedInventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130324532Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.Type: ApplicationFiled: February 17, 2012Publication date: December 5, 2013Applicant: Cancer Therapeutics CRC Pty LimitedInventors: Ian Peter Holmes, Yiva Bergman, Gillian Elizabeth Lunniss, Marcia Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
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Publication number: 20130324533Abstract: We describe a polymorphic variant of a BIM {BCL2L11) gene which comprises, in 5? to 3? order, the nucleotide sequence set out in SEQ ID NO: 5 followed immediately by the nucleotide sequence set out in SEQ ID NO: 7. The BIM polymorphic variant may be characterised by lacking the nucleotide sequence set out in SEQ ID NO: 6. It may be used to detect BCR-ABL-independent TKI-resistance (resistance to treatment with tyrosine kinase inhibitors) for chronic myelogenous leukaemia, c-KIT/PDGFR-independent TKI-resistance for gastrointestinal stromal tumours (GIST), EGFR-independent TKI-resistance for non-small cell lung cancer (NSCLC) or JAK2-independent TKI-resistance for a myeloproliferative disorder, in an individual comprising such a polymorphism.Type: ApplicationFiled: December 14, 2011Publication date: December 5, 2013Applicants: NATIONAL UNIVERSITY OF SINGAPORE, AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, SINGAPORE HEALTH SERVICES PTE LTDInventors: Yijun Ruan, Sin Tiong Ong, King-Pan Ng, Charles Thuan Heng Chuah, Axel Maximilian Hillmer, Wen Chun Juan
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Publication number: 20130310364Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: July 16, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20130303497Abstract: The present invention relates to new deuterated derivatives of serotonin 5-HT1A receptor agonists of formula 1 and in particular to compositions and methods for therapeutic use.Type: ApplicationFiled: August 4, 2011Publication date: November 14, 2013Applicant: Conrig Pharma ApSInventors: John Bondo Hansen, Mikael Søndergaard Thomsen
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Patent number: 8580778Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: October 12, 2011Date of Patent: November 12, 2013Assignee: Bayer Intellectual Property GmbHInventors: Mario Jeske, Ingo Flamme, Friederike Stoll, Hartmut Beck, Metin Akbaba
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Patent number: 8580795Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.Type: GrantFiled: January 21, 2010Date of Patent: November 12, 2013Assignee: Orchid Chemicals & Pharmaceuticals LimitedInventors: Gopalan Balasubramanian, Sukunath Narayanan, Ganapavarapu Veera Raghava Sharma, Lavanya Andiappan, Shridhar Narayanan, Sanjeev Saxena, Sridharan Rajagopal, Santosh Lolaknath Vishwakarma, Saravanan Thirunavukkarasu
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Publication number: 20130281447Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventors: Stephen S. Palmer, Selvaraj Nataraja
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Publication number: 20130281430Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.Type: ApplicationFiled: April 17, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
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Publication number: 20130281429Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 26, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
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Patent number: 8563539Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: December 23, 2010Date of Patent: October 22, 2013Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20130274242Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).Type: ApplicationFiled: January 18, 2013Publication date: October 17, 2013Inventors: Jang-Sik Choi, Hae-Jun Hwang, Eunho Lee, Jaekyoo Lee, Ho-Juhn Song, Se Won Kim, Jung-Ho Kim, Jong Sung Koh, Sunhwa Chang, Tae-im Lee, Yung-geun Choi, Ik-hwan Han, Jaesang Lee
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Patent number: 8551999Abstract: The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5—Z1—, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group —CO—, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.Type: GrantFiled: October 29, 2008Date of Patent: October 8, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takumi Sumida, Fujio Tabusa, Kazuo Sekiguchi, Takeshi Kodama, Koichi Yasumura, Yutaka Kojima, Masaaki Motoyama, Keisuke Miyajima, Kenji Yoshida, Keizo Kan, Makoto Sakamoto, Hideki Takasu, Takashi Nakagawa, Naoto Ohi, Yasuo Harada, Norikazu Hashimoto, Hironori Matsuyama, Masatoshi Iida, Shigekazu Fujita, Tae Fukushima
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Patent number: 8551992Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: May 23, 2012Date of Patent: October 8, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8551984Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: GrantFiled: December 15, 2010Date of Patent: October 8, 2013Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou