Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
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Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Patent number: 8889881Abstract: Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPAR? and PPAR? activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.Type: GrantFiled: February 8, 2012Date of Patent: November 18, 2014Assignee: Pusan National University Industry —University Cooperation FoundationInventors: Hae Young Chung, Min Hi Park, Young Mi Ha, Yu Kyeong Han, Ji Young Park, Yun Jung Park, Jin Ah Kim, Ji Yeon Lee, Yu Min Song, Hyung Ryong Moon
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Patent number: 8889703Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: GrantFiled: February 23, 2011Date of Patent: November 18, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
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Patent number: 8889710Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: GrantFiled: December 20, 2013Date of Patent: November 18, 2014Assignee: Eli Lilly and CompanyInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Publication number: 20140336174Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: ApplicationFiled: April 17, 2014Publication date: November 13, 2014Applicant: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
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Publication number: 20140335175Abstract: An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least one water swelling polymer other than pregelatinized starch.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Thomas FRIEDL, Wolfram EISENREICH
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Patent number: 8883834Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.Type: GrantFiled: June 6, 2014Date of Patent: November 11, 2014Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8883831Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.Type: GrantFiled: February 4, 2013Date of Patent: November 11, 2014Assignee: PharmoRx Therapeutics, Inc.Inventors: David M. Bear, Robert M. Kessler
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Patent number: 8884023Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: GrantFiled: August 22, 2012Date of Patent: November 11, 2014Assignee: Merck Patent GmbHInventors: Marianne Donnely, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Patent number: 8883833Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: GrantFiled: November 20, 2008Date of Patent: November 11, 2014Assignee: Decode Genetics EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
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Publication number: 20140329869Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.Type: ApplicationFiled: February 28, 2014Publication date: November 6, 2014Applicant: KNOPP BIOSCIENCES, LLCInventors: Michael E. BOZIK, Thomas PETZINGER, JR., James L. MATHER, Donald ARCHIBALD
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Patent number: 8877751Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 8, 2009Date of Patent: November 4, 2014Assignee: Merck Patent GmbHInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20140322278Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.Type: ApplicationFiled: June 19, 2012Publication date: October 30, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
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Publication number: 20140323420Abstract: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subjectType: ApplicationFiled: November 8, 2012Publication date: October 30, 2014Inventors: Stephen Dewhurst, David Easterhoff, Brad Nilsson, John Dimaio, Alan Smrcka, Jerry Yang, Christina Capule
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Publication number: 20140315945Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140315792Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: February 14, 2014Publication date: October 23, 2014Inventors: Rolf Wagner, John K. Pratt, Dachun Liu, Michael D. Tufano, David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Dooner, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, Yi Gao, Allan C. Krueger
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Publication number: 20140315963Abstract: [Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.Type: ApplicationFiled: April 18, 2014Publication date: October 23, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Ryota Shiraki, Takahiko Tobe, Shimpei Kawakami, Hiroyuki Moritomo, Makoto Ohmiya
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Patent number: 8865752Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: GrantFiled: July 4, 2013Date of Patent: October 21, 2014Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J. W. M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
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Patent number: 8865736Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.Type: GrantFiled: November 28, 2011Date of Patent: October 21, 2014Assignee: Biota Scientific Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Publication number: 20140309210Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.Type: ApplicationFiled: February 12, 2014Publication date: October 16, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
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Publication number: 20140308243Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 16, 2014Publication date: October 16, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
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Publication number: 20140309190Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: June 17, 2014Publication date: October 16, 2014Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Patent number: 8859599Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.Type: GrantFiled: February 11, 2010Date of Patent: October 14, 2014Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
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Publication number: 20140303207Abstract: The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.Type: ApplicationFiled: April 3, 2013Publication date: October 9, 2014Applicant: NEUROVANCE, Inc.Inventors: Phil SKOLNICK, Zhengming Chen
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Publication number: 20140296223Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.Type: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Publication number: 20140296257Abstract: The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment.Type: ApplicationFiled: August 10, 2012Publication date: October 2, 2014Applicant: Ascendis Pharma A/SInventors: Ulrich Hersel, Guillaume Maitro, Harald Rau, Dirk Vetter
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Publication number: 20140296205Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: June 27, 2012Publication date: October 2, 2014Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
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Publication number: 20140296219Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: ApplicationFiled: November 14, 2013Publication date: October 2, 2014Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Patent number: 8846685Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: GrantFiled: September 25, 2012Date of Patent: September 30, 2014Assignee: Aerpio Therapeutics Inc.Inventors: Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Publication number: 20140288105Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: EPIZYME, INC.Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
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Publication number: 20140275103Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Aerpio Therapeutics Inc.Inventors: Kevin Peters, Robert Shalwitz, John Janusz, Alexander Smith
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Publication number: 20140275091Abstract: Provided herein is a pharmaceutical formulation comprising a GGA derivative in the form of an eye drop. Also provided herein are methods of treating neural diseases or disorders by administering such pharmaceutical formulations.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Hiroaki Serizawa, Tilmann M. Brotz
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Publication number: 20140275172Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.Type: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Zhihua Sui, Nalin Subasinghe
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Publication number: 20140275028Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein ring A, R1, R5 and R6 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Wenying Chai, Charlotte Deckhut, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Virginia M. Tanis, Kyle T. Tarantino
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Publication number: 20140275022Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: June 27, 2012Publication date: September 18, 2014Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
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Patent number: 8835428Abstract: The present invention relates to isoxazole, thiazole and oxidiazole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, in particular to the use of these compounds in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1.Type: GrantFiled: February 24, 2011Date of Patent: September 16, 2014Assignee: Piramal Enterprises LimitedInventors: Ashok Kumar Gangopadhyay, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Hitesh Mistry, Rajiv Sharma
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Patent number: 8835473Abstract: The present invention provides methods of treating cancer using 2-amino-6-trifluoromethoxybenzothiazole (riluzole). In one aspect, the present invention provides methods of reducing cancer cell growth. In another aspect, the present invention provides a method of inducing apoptosis in a cancer cell. In another aspect, the present invention provides a method of reducing the growth of a glutamate-releasing tumor.Type: GrantFiled: September 15, 2009Date of Patent: September 16, 2014Assignee: Rutgers, The State University of New JerseyInventors: James S. Goydos, Suzie Chen
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Patent number: 8829034Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 8, 2011Date of Patent: September 9, 2014Assignee: Boehringer Ingerlheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Patent number: 8829035Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.Type: GrantFiled: May 28, 2010Date of Patent: September 9, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Junichi Ishikawa, Koichi Saito, Norihisa Ohe, Kentaro Kobayashi
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Publication number: 20140249173Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.Type: ApplicationFiled: May 15, 2014Publication date: September 4, 2014Inventors: Vladimir Coric, John H. Krystal, Gerald Sanacora
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Publication number: 20140249100Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.Type: ApplicationFiled: March 3, 2013Publication date: September 4, 2014Applicant: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
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Patent number: 8822691Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.Type: GrantFiled: July 10, 2010Date of Patent: September 2, 2014Assignee: Bayer CropScience AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Publication number: 20140243282Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.Type: ApplicationFiled: December 12, 2011Publication date: August 28, 2014Inventor: Satish Reddy Kallam
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Publication number: 20140243338Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
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Publication number: 20140243288Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.Type: ApplicationFiled: September 29, 2012Publication date: August 28, 2014Inventors: Hui Zhang, Aichen Wang
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Publication number: 20140243370Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: ApplicationFiled: August 22, 2012Publication date: August 28, 2014Applicant: MERCK PATENT GmbHInventors: Marianne Donnelly, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Publication number: 20140242026Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.Type: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Inventors: Robert Shalwitz, Kevin Gene Peters
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Patent number: 8815864Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: GrantFiled: November 25, 2013Date of Patent: August 26, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Elke Langkopf, Holger Wagner