Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.3)
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Publication number: 20140249151Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11?-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11?-HSD1.Type: ApplicationFiled: October 17, 2012Publication date: September 4, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Shimpei Kawakami, Minoru Sakurai, Noriyuki Kawano, Takayuki Suzuki, Nobuyuki Shiraishi, Wataru Hamaguchi, Ryuichi Sekioka, Hiroyuki Moritomo, Ayako Motitomo
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Patent number: 8815878Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.Type: GrantFiled: July 27, 2011Date of Patent: August 26, 2014Assignee: NovaDrug, LLCInventor: Eliezer Huberman
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Patent number: 8802666Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140221298Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.Type: ApplicationFiled: September 24, 2012Publication date: August 7, 2014Inventor: Raito Kuwahara
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Publication number: 20140221201Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one active compound II selected from a group M comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, allosteric nicotinic acetylcholine receptor activators, chloride channel activators, juvenile hormone mimics, homopteran feeding blockers, mit grow inhibitors, inhibitors of mitochondrial bATP synthase, uncouplers of the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, ecdyson receptor agonists, octamin receptor agonists, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis, ryanodine receptor modulators and other compounds as defined in the description, in syneType: ApplicationFiled: August 30, 2012Publication date: August 7, 2014Applicant: BASF SEInventors: Florian Kaiser, Steffen Groß, Jürgen Langewald, Arun Narine
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Publication number: 20140213445Abstract: The present invention relates to agricultural methods and the use of 3-arylquinazolin-4-one derivatives of formula (I) wherein R1, R2, R3, R4, k and n are defined in the description in soil application methods. The compounds of the formula (I) are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.Type: ApplicationFiled: August 31, 2012Publication date: July 31, 2014Applicant: BASF SEInventors: Florian Kaiser, Steffen Gross, Arun Narine, Koshi Gunjima
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Publication number: 20140206693Abstract: Certain embodiments are directed to methods of treating a pathophysiological state or symptoms thereof resulting from aldose reductase-mediated signaling in a cytotoxic pathway using an aldose reductase specific inhibitor.Type: ApplicationFiled: January 27, 2014Publication date: July 24, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Satish K Srivastava, Kota V Ramana
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Publication number: 20140206705Abstract: Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).Type: ApplicationFiled: March 12, 2014Publication date: July 24, 2014Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Riho KODAMA, Akinori TATARA
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Publication number: 20140200136Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: August 31, 2012Publication date: July 17, 2014Applicant: BASF SEInventors: Florian Kaiser, Steffen Gross, Egon Haden, Arun Narine
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Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
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Patent number: 8759097Abstract: The present invention relates to compositions and methods for reducing cell proliferation and/or promoting cell death by inhibiting Drp1. It is based, at least in part, on the discoveries that (i) Drp1 disruption-induced mitochondrial hyperfusion is functionally linked to the cell cycle regulation apparatus, so that Drp1 inhibition results in a disruption of the cell cycle and DNA aberrancies; (ii) inhibition of both Drp1 and ATR are synthetic lethal causing increased DNA damage and apoptotic cell death; and (iii) even in resistant cell lines, Drp1 inhibitor (e.g., mdivi-1) together with a second antiproliferative agent (e.g., cisplatin or carboplatin) act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.Type: GrantFiled: April 18, 2012Date of Patent: June 24, 2014Assignee: University of Pittsburgh—of the Commonwealth System of Higher EductionInventors: Wei Qian, Bennett Van Houten
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Publication number: 20140171455Abstract: Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds.Type: ApplicationFiled: June 8, 2012Publication date: June 19, 2014Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Lee-Way Jin, Izumi Meezawa
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Publication number: 20140163050Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment or prevention of photosensitive epilepsy.Type: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Inventors: Donald JOHNS, Georges IMBERT, Klaus KUCHER
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Patent number: 8748422Abstract: The present invention relates to a pharmaceutical composition containing one or more quinazoline compounds as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.Type: GrantFiled: August 21, 2008Date of Patent: June 10, 2014Assignee: Korea Institute of Science and TechnologyInventors: Ghil Soo Nam, Hye Whon Rhim, Ae Nim Pae, Hyun Ah Choo, Kyung Il Choi, Seung Yeol Nah
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Publication number: 20140155417Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: August 30, 2013Publication date: June 5, 2014Applicant: HYDRA BIOSCIENCES, INC.Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis Underwood, Manfred Weigele, Xiaoguang Zhen
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Publication number: 20140155396Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: June 27, 2013Publication date: June 5, 2014Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20140147448Abstract: The invention includes compositions and methods useful for treating preventing abnormal thrombus formation and subsequent cardiovascular disease in diabetic patients and patients with increased cardiovascular risk.Type: ApplicationFiled: June 5, 2012Publication date: May 29, 2014Applicant: Yale UniversityInventors: John Hwa, WaiHo Tang
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Patent number: 8722659Abstract: The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.Type: GrantFiled: October 7, 2011Date of Patent: May 13, 2014Assignee: SanofiInventors: Annie Clauss, Christophe Glaess, Gilbert Marciniak, Jean-Francois Nave, Bertrand Vivet
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Publication number: 20140105920Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.Type: ApplicationFiled: May 23, 2013Publication date: April 17, 2014Inventor: David Sherris
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Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Patent number: 8658656Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: September 12, 2012Date of Patent: February 25, 2014Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustav S Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
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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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Patent number: 8633211Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: GrantFiled: March 4, 2008Date of Patent: January 21, 2014Assignee: Novartis AGInventor: Roger John Taylor
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Publication number: 20140018376Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.Type: ApplicationFiled: October 20, 2010Publication date: January 16, 2014Inventors: Hans Allgeier, Yves Auberson, Thomas Blaettler, David Carcache, Philipp Floersheim, Wolfgang Froestl, Christel Guibourdenche, Hans o Kalkman, Joerg Kallen, Manuel Koller, Kurt Lingenhohl, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud, Christine Strohmaier
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Patent number: 8623884Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: GrantFiled: November 17, 2011Date of Patent: January 7, 2014Assignee: Janssen Pharmaceutica, NVInventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20130345231Abstract: The invention described herein pertains to anticancer therapeutic agents that exhibit preferential cytotoxicity to malignant cells that express a cancer specific isoform of proliferating cell nuclear antigen (caPCNA) compared to cytotoxicity to comparable non-malignant cells, pharmaceutical compositions comprising the agents, and their use in cancer therapy.Type: ApplicationFiled: March 21, 2012Publication date: December 26, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Robert J. Hickey, Linda H. Malkas
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Publication number: 20130338151Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: December 19, 2013Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Patent number: 8609667Abstract: Disclosed is a kind of E-type phenyl acrylic ester compound containing substituted anilino pyrimidine group, which is shown by general structure formula I, wherein each substituent is defined as that in the description. The compounds of general formula I show high insecticidal and acaricidal activities to adults and nymphs of harmful insects and mites in agricultural, civil and zoic technical fields, especially to Tetranychus cinnabarinus, Tetranychidae, and the like. The said compounds show more excellent performance on inhibiting the incubation of eggs of harmful mites. The uses of the said compounds as insecticides and/or acaricides in agricultural and other fields also are disclosed.Type: GrantFiled: June 3, 2010Date of Patent: December 17, 2013Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.Inventors: Changling Liu, Huichao Li, Hong Zhang, Baoshan Chai, Yanmei Luo, Xiaomin He, Guang Huang, Shaowu Liu, Baoxiang Sun
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Patent number: 8609674Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein G1, R2, R1a, R1b, X, X1, X2, X3, Rx, J, k, n, q, and t are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: November 2, 2011Date of Patent: December 17, 2013Assignee: AbbVie Inc.Inventors: Arturo Perez-Medrano, Sridhar Peddi, David DeGoey
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Publication number: 20130324545Abstract: AKR1B1 (EC 1.1.1.21) is an aldose reductase that has mainly been associated with the polyol pathway, and more recently with lipid deperoxidation. We have discovered that the primary activity of this enzyme is rather a PGFS activity, catalyzing the transformation of PGH2 into PGF2?. AKR1B1 as a therapeutic target, and method for modulating its expression and activity are provided. Methods for regulating the expression and activity of PGF2? are also provided.Type: ApplicationFiled: July 17, 2013Publication date: December 5, 2013Applicant: UNIVERSITE LAVALInventors: Michael Fortier, Pierre Chapdelaine, Eva Bresson, Éric Madore
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Patent number: 8586597Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform PI3K? activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed. An exemplary compound disclosed in this application is shown below.Type: GrantFiled: December 27, 2012Date of Patent: November 19, 2013Assignee: ICOS CorporationInventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
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Publication number: 20130303491Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Applicant: Siga Technologies Inc.Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20130296349Abstract: Compounds of formula (I) in which R3 is chosen from hydrogen, cyano, nitro, acetyl and C(?O)NH2, and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl, are useful as antitumor agents.Type: ApplicationFiled: January 18, 2012Publication date: November 7, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Tarun M. Kapoor, Ari J. Firestone, Joshua S. Weinger
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Patent number: 8575185Abstract: The present invention provides quinazolinedione derivatives of Formulae Ia and Ib, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia.Type: GrantFiled: February 26, 2010Date of Patent: November 5, 2013Assignee: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Sureshbabu Dadiboyena, Kouacou Adiey
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Publication number: 20130274101Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Ulrike WACHENDORFF-NEUMANN, Peter Dahmen, Ralf Dunkel
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Publication number: 20130267542Abstract: Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed.Type: ApplicationFiled: April 2, 2013Publication date: October 10, 2013Applicant: Annji Pharmaceutical Co., Ltd.Inventors: Ji-Wang CHERN, Chao-Wu YU, Pei-Teh CHANG
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Patent number: 8552015Abstract: Novel quinazolinone derivatives of formula I wherein R1-R9 are as defined in the description, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: GrantFiled: June 26, 2007Date of Patent: October 8, 2013Assignee: Novartis AGInventors: Christopher T Brain, Edward K Dziadulewicz, Terance W Hart
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Patent number: 8551950Abstract: A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT2 receptor) antagonists is disclosed. The AT2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.Type: GrantFiled: March 20, 2007Date of Patent: October 8, 2013Assignee: Spinifex Pharmaceuticals Pty LtdInventor: Maree Therese Smith
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Patent number: 8524721Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 10, 2011Date of Patent: September 3, 2013Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Patent number: 8518960Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: GrantFiled: May 23, 2008Date of Patent: August 27, 2013Assignee: Siga Technologies, Inc.Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Patent number: 8518441Abstract: The present invention provides solid dispersions or solid dispersion pharmaceutical preparations containing a water-soluble polymeric substance(s) and a phenylalanine compound of the formula (1) or pharmaceutically acceptable salts thereof, wherein A represents the formula (2) and the like, B represent an alkoxy group and the like, E represents a hydrogen atom and the like, D represents a substituted phenyl group and the like, T, U and V represent a carbonyl group and the like, Arm represents a benzene ring and the like, R1 represents an alkyl group and the like, R2, R3, and R4 may be the same or different from one another and each represent a hydrogen atom, a substituted amino group and the like, and J and J? represent a hydrogen atom and the like; production methods thereof; and solubilized pharmaceutical preparations containing a solubilizer(s) and the compound (I) or pharmaceutically acceptable salts thereof.Type: GrantFiled: May 15, 2006Date of Patent: August 27, 2013Assignee: Ajinomoto Co., Inc.Inventors: Hiroyuki Higuchi, Hirokazu Hagio, Kenichi Ogawa, Akira Yabuki
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Patent number: 8513268Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: GrantFiled: July 28, 2011Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Publication number: 20130210805Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.Type: ApplicationFiled: October 6, 2011Publication date: August 15, 2013Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
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Publication number: 20130210733Abstract: Provided herein are methods of treating lung disease in a subject by administering to the subject a therapeutically effective amount of a mitotic kinesin inhibitor, optionally in combination with another therapy.Type: ApplicationFiled: June 16, 2011Publication date: August 15, 2013Inventors: David J. Morgans, JR., Fady Malik, Kenneth Wood, Malar Pannirselvan
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Publication number: 20130210844Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: February 7, 2013Publication date: August 15, 2013Applicant: Glenmark Pharmaceuticals S.A.Inventor: Glenmark Pharmaceuticals S.A.
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Publication number: 20130184296Abstract: Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylacetamide, polyethylene glycol and D5W useful in the treatment of hypertension, heart failure and renal disease leading to edematous states. Also disclosed are methods for preparing such solutions.Type: ApplicationFiled: December 17, 2012Publication date: July 18, 2013Applicant: Academic Pharmaceuticals IncorporatedInventor: Academic Pharmaceuticals Incorporated
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Publication number: 20130172334Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 17, 2012Publication date: July 4, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Patent number: 8475776Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.Type: GrantFiled: February 28, 2007Date of Patent: July 2, 2013Assignee: Paloma Pharmaceuticals, Inc.Inventor: David I. Sherris