Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
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Patent number: 9034881Abstract: Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions.Type: GrantFiled: September 12, 2013Date of Patent: May 19, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventor: Daniel Magilavy
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Patent number: 9035096Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: October 9, 2013Date of Patent: May 19, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 9034889Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. The oral bioavailabilty of zoledronic acid can be enhanced by administering the zoledronic acid in the disodium salt form.Type: GrantFiled: May 15, 2014Date of Patent: May 19, 2015Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Publication number: 20150133441Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: June 6, 2014Publication date: May 14, 2015Inventor: Gerard M. Housey
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Publication number: 20150133401Abstract: The present invention provides a method for treating a proliferative disease in a patient. The method comprises administering to a patient in need thereof: a) a vascular disrupting agent and (b) at least one hypoxia targeting agent. Preferred combinations are BNC105 and Pazopanib and BNC 105 and Bortezomib.Type: ApplicationFiled: June 3, 2013Publication date: May 14, 2015Inventors: Daniel J. Inglis, Tina C. Lavranos, Gabriel Kremmidiotis
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Publication number: 20150133479Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 13, 2013Publication date: May 14, 2015Inventors: Matthias Broekema, Gang Wu, Dean A. Wacker
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Publication number: 20150133457Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.Type: ApplicationFiled: July 11, 2014Publication date: May 14, 2015Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
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Publication number: 20150133478Abstract: Nucleic acids and proteins having a mutant C-RAF sequence, and methods of identifying patients having cancer who are likely to benefit from a combination therapy and methods of treatment are provided.Type: ApplicationFiled: March 7, 2013Publication date: May 14, 2015Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Caroline Emery, Rajee Antony, Levi A. Garraway
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Patent number: 9028876Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.Type: GrantFiled: March 14, 2012Date of Patent: May 12, 2015Assignee: Janssen R&D IrelandInventors: Thomas Hantke, Bettina Rehbock, Jörg Rosenberg, Jörg Breitenbach
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Patent number: 9029379Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.Type: GrantFiled: March 15, 2013Date of Patent: May 12, 2015Assignee: The University of Utah Research FoundationInventors: Julie Ruth Korenberg, Karen Sue Wilcox, Peter Jeffrey West, Raymond Pierre Kesner
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Patent number: 9029377Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.Type: GrantFiled: June 28, 2010Date of Patent: May 12, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
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Publication number: 20150126504Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: January 12, 2015Publication date: May 7, 2015Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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Publication number: 20150126494Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 30, 2013Publication date: May 7, 2015Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
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Patent number: 9023841Abstract: This disclosure provides methods for treating asthma or an associated disorder in a patient in need thereof, by administering to the patient an effective amount of an autophagy inducing agent, thereby treating the asthma or the associated disorder. Disorders that can be treated include, allergic asthma, chronic obstructive pulmonary disease, lung inflammation, respiratory tolerance and a lung infection or disorder.Type: GrantFiled: August 2, 2012Date of Patent: May 5, 2015Assignee: University of Southern CaliforniaInventor: Omid Akbari
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Publication number: 20150119385Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.Type: ApplicationFiled: October 24, 2014Publication date: April 30, 2015Applicant: Novartis AGInventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
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Publication number: 20150119413Abstract: An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and ?-catenin phosphorylation and/or acetylation while reducing bile duct ?-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.Type: ApplicationFiled: October 24, 2014Publication date: April 30, 2015Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCHInventors: Sergio A. Gradilone, Nicholas F. LaRusso
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Publication number: 20150119414Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.Type: ApplicationFiled: January 2, 2015Publication date: April 30, 2015Applicant: PIVOTAL THERAPEUTICS INC.Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar Ahmad SHAIKH, Jason YANTHA, Valerie B. SCHINI-KERTH
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Publication number: 20150119379Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.Type: ApplicationFiled: December 19, 2014Publication date: April 30, 2015Applicant: AstraZeneca ABInventors: Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, Chandrasekhara Reddy Chintakuntla, Claudio Edmundo Chuaqui, Vasantha Krishna Kadambar, Andiappan Murugan
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Patent number: 9018223Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 20, 2014Date of Patent: April 28, 2015Assignee: Cytokinetics, Inc.Inventors: Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang
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Patent number: 9018133Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 9018224Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: November 9, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Patent number: 9018205Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: GrantFiled: February 13, 2013Date of Patent: April 28, 2015Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
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Publication number: 20150112116Abstract: Provided herein are methods comprising providing a tyrosine derivative and a solid particulate material (and, optionally, melanin) and applying force to said tyrosine derivative and said solid particulate material for a time and under conditions effective to impregnate at least one of said tyrosine derivative and said solid particulate material with the other of said tyrosine derivative and said solid particulate material. The invention also provides compositions comprising at least one of a tyrosine derivative impregnated with a solid particulate material and a solid particulate material impregnated with a tyrosine derivative.Type: ApplicationFiled: October 24, 2013Publication date: April 23, 2015Inventor: STEVEN HOFFMAN
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Publication number: 20150111883Abstract: 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: October 21, 2014Publication date: April 23, 2015Inventors: Jaekyoo Lee, Jang-Sik Choi, Hae-Jun Hwang, Ho-Juhn Song, Jung-Ho Kim, Se-Won Kim, Jong Sung Koh, Jaesang Lee, Tae-Im Lee, Yung-Geun Choi, Sung-Ho Park, In Yong Lee, Byung-Chul Suh, Paresh Devidas Salgaonkar, Dong-Sik Jung
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Publication number: 20150110871Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.Type: ApplicationFiled: January 3, 2015Publication date: April 23, 2015Inventor: David Wong
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Publication number: 20150111860Abstract: The present invention relates to a suspoemulsion comprising the following ingredients (1), (2), (3), (4), (5), and (6): an ingredient (1): low water-soluble liquid pesticidal ingredient, an ingredient (2): low water-soluble pesticidal active ingredient which is solid at normal temperature, an ingredient (3): polyoxyalkylene block copolymer, an ingredient (4): phosphate ester salt and/or sulfate ester salt of polyoxyethylene aryl phenyl ether, an ingredient (5): ligninsulfonic acid salt, and an ingredient (6): water. The suspoemulsion of the present invention is a formulation having excellent storage stability, which suppresses the particle growth of dispersoids of an ingredient (1) and an ingredient (2) during storage at high temperature and low temperature, and causes neither aggregation nor separation of dispersoids, nor formation of a hard cake, nor a change in appearance.Type: ApplicationFiled: February 27, 2013Publication date: April 23, 2015Inventor: Takuya Tanaka
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Publication number: 20150111869Abstract: The invention provides combinations comprising a MEK inhibitor (such as GDC-0973 or GDC-0623), or a pharmaceutically acceptable salt thereof and an ERK inhibitor (such as GDC-0994). The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.Type: ApplicationFiled: August 29, 2014Publication date: April 23, 2015Applicant: Genentech, Inc.Inventors: Marcia Belvin, John Moffat, Mark Merchant
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Publication number: 20150111868Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: June 14, 2013Publication date: April 23, 2015Applicant: Jansen R&D IrelandInventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
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Publication number: 20150111912Abstract: Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.Type: ApplicationFiled: May 15, 2013Publication date: April 23, 2015Applicant: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury, Tarak D. Mody
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Publication number: 20150111879Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: December 24, 2014Publication date: April 23, 2015Applicants: CURIS, INC., GENENTECH, INC.Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
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Publication number: 20150111866Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.Type: ApplicationFiled: April 26, 2013Publication date: April 23, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
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Publication number: 20150111913Abstract: A non-pressurized container that contains one or more of: a foamable composition of minoxidil, or a pharmaceutically acceptable salt thereof, and a dihydrotestosterone blocker in a formulation with a precise density and viscosity to yield a foam with a temperature sensitivity and shear strength designed for inverted application and immediate targeted release at body temperature under a minimal hand applied pressure to the scalp.Type: ApplicationFiled: December 31, 2014Publication date: April 23, 2015Inventor: Nyangenya Maniga
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Patent number: 9012462Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: May 21, 2009Date of Patent: April 21, 2015Assignee: Ariad Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlman, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
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Patent number: 9012456Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: February 22, 2013Date of Patent: April 21, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Bernd Nosse
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Publication number: 20150105414Abstract: The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Longsheng Hu, Virginia Streusand Goldman, Josephine A. Minerva, Susan Wendling
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Publication number: 20150105358Abstract: The invention relates to combinations comprising an HDAC inhibitor and an immunomodulatory drug for the treatment of multiple myeloma in a subject in need thereof. The combinations may, optionally, further comprise an anti-inflammatory agent, such as dexamethasone. Also provided herein are methods for treating multiple myeloma in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations.Type: ApplicationFiled: October 7, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Steven Norman Quayle, Simon Stewart Jones, Kenneth C. Anderson, Teru Hideshima
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Publication number: 20150105401Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: October 7, 2014Publication date: April 16, 2015Applicant: The University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
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Publication number: 20150105383Abstract: The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a PI3K inhibitor.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Steven Norman Quayle, Simon Stewart Jones
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Publication number: 20150105393Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: April 25, 2013Publication date: April 16, 2015Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
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Publication number: 20150105413Abstract: The present invention relates to compounds of formula (I): wherein R1 is NH2 or NHMe; R2 is halo; and one of R3 or R4 is hydrogen and the other is selected from —SO2NH2, —SO2NHMe or —SO2NMe2, —SO2NHEt, or —SO2NEt2; or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula (I) are inhibitors of protein kinases, especially cyclic dependent kinases (CDKs) such as CDK9. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which protein kinase/CDK activity is implicated.Type: ApplicationFiled: April 18, 2013Publication date: April 16, 2015Applicant: CHANGZHOU LE SUN PHARMACEUTICALS LIMITEDInventors: Shudong Wang, Hao Shao
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Publication number: 20150105384Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 9, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Simon Stewart Jones, Min Yang, David Lee Tamang
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Publication number: 20150105390Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: IRM LLC, a Delaware Limited Liability CompanyInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20150104504Abstract: The present disclosure provides pharmaceutical compositions of statins and polyunsaturated fatty acids (PUFAs), in which the statins are dissolved in the PUFAs, the PUFA species being present substantially in the free acid form. Also provided are oral unit dosage forms of the disclosed pharmaceutical compositions and methods of treating blood lipid disorders using the compositions and oral unit dosage forms.Type: ApplicationFiled: May 7, 2013Publication date: April 16, 2015Inventors: Bernardus Machielse, Timothy J. Maines, Michael H. Davidson, Bharat M. Mehta
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Publication number: 20150105409Abstract: The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a BTK inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor.Type: ApplicationFiled: October 7, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceticals, Inc.Inventors: Steven Norman Quayle, Simon Stewart Jones, Eduardo M. Sotomayor, Javier Pinilla-Ibarz, Eva Sahakian
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Publication number: 20150105400Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Haruto NAKAGAWA, Naoko ANDO
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Patent number: 9006228Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: June 11, 2012Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Patent number: 9006243Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compouType: GrantFiled: December 28, 2007Date of Patent: April 14, 2015Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
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Publication number: 20150099744Abstract: The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatrent of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: David Lee Tamang, Min Yang, Simon S. Jones
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Publication number: 20150099749Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: December 10, 2014Publication date: April 9, 2015Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
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Publication number: 20150099743Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN