C=o Bonded Directly To The Hetero Ring (x Is Chalcogen) Patents (Class 514/448)
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Patent number: 8791049Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.Type: GrantFiled: December 13, 2010Date of Patent: July 29, 2014Assignee: Gowan Co.Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
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Patent number: 8772296Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.Type: GrantFiled: May 31, 2007Date of Patent: July 8, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
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Publication number: 20140187617Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.Type: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicant: AERIE PHARMACEUTICALS, INC.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Patent number: 8765797Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.Type: GrantFiled: June 21, 2011Date of Patent: July 1, 2014Assignee: Board of Regents, The University of Texas SystemInventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
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Patent number: 8759389Abstract: The present invention relates to compounds useful as inhibitors of PLK protein kinase of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: February 15, 2013Date of Patent: June 24, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Keily
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20140171474Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositionsType: ApplicationFiled: February 19, 2014Publication date: June 19, 2014Inventors: Philippe DESBORDES, Ralf DUNKEL, Stephanie GARY, Marie-Claire GROSJEAN-COURNOYER, Benoit HARTMANN, Philippe RINOLFI, Jean-Pierre VORS, Rachel RAMA
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Patent number: 8748479Abstract: A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream is produced that is fed to a crystallization zone followed by a solid-liquid displacement zone to form a low impurity slurry stream. The solids in the low impurity slurry stream are dissolved in a dissolution zone to produce a hydrogenation feed that is hydrogenated in a hydrogenation reactor to generate a hydrogenated FDCA composition. The hydrogenated FDCA composition is routed to a crystallization zone to form a crystallized produce stream that is separated from liquid in a solid-liquid separation zone to generate a purified wet cake stream containing FDCA that can be dried in a drying zone to generate a dry purified FDCA product stream.Type: GrantFiled: February 4, 2013Date of Patent: June 10, 2014Assignee: Eastman Chemical CompanyInventors: Ashfaq Shaikh, Kenny Randolph Parker, Mesfin Ejerssa Janka, Lee Reynolds Partin
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Publication number: 20140155433Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.Type: ApplicationFiled: July 2, 2012Publication date: June 5, 2014Applicant: LUPIN LIMITEDInventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 8741946Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.Type: GrantFiled: July 13, 2012Date of Patent: June 3, 2014Assignee: Gilead Sciences, Inc.Inventors: William J. Watkins, Eda Canales, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith
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Patent number: 8722726Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: GrantFiled: January 21, 2008Date of Patent: May 13, 2014Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20140128437Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicants: President and Fellows of Harvard College, TRUSTEES OF BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITAL, INC., Tufts UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterrev, John A. Proco, JR.
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Publication number: 20140128427Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
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Patent number: 8703811Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: GrantFiled: May 7, 2009Date of Patent: April 22, 2014Assignees: Genzyme Corporation, Massachusetts Institute of Technology, President and Fellows of Harvard CollegeInventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Publication number: 20140107166Abstract: The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: February 13, 2012Publication date: April 17, 2014Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Ralph Mazitschek, James E. Bradner, Melissa Grachan Harman
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Publication number: 20140107134Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
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Publication number: 20140099387Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: August 8, 2013Publication date: April 10, 2014Applicant: Sarcode Bioscience Inc.Inventors: Thomas Gadek, John Burnier, Min Zhong, Wang Shen, Johan D. Oslob, Kenneth Barr
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Patent number: 8691842Abstract: The present invention provides a pharmaceutical composition for preventing or treating rheumatoid arthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg.Type: GrantFiled: October 8, 2009Date of Patent: April 8, 2014Assignees: Catholic University Industry Academic Cooperation Foundation, Hanlim Pharmaceutical Co., Ltd.Inventors: Jun-Ki Min, Mi-La Cho, Yun-Ju Woo, Hye-Jwa Oh, Joo-Yeon Jhun, Geun-Hyeog Lee, Se-Wan Park, Jin-Ha Park, Eun-Young Kwak
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Publication number: 20140094489Abstract: The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) wherein each symbol is as described in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: AJINOMOTO CO., INC.Inventors: Tamotsu SUZUKI, Takahiro KOSHIBA, Munetaka TOKUMASU, Koji OHSUMI
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Patent number: 8680127Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 30, 2009Date of Patent: March 25, 2014Assignee: Bayer Intellectual Property GmbHInventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Publication number: 20140079784Abstract: This invention provides specifically formulated LFA-1 antagonists or pharmaceutically acceptable salts thereof that are suitable for aerosolized delivery. In particular, the LFA-1 antagonists are particularly well suited for localized treatment by having a rapid systemic clearance rate. The invention also encompasses methods of treatment and prevention of immune related disorders using the LFA-1 aerosolized formulations of the present invention.Type: ApplicationFiled: August 7, 2013Publication date: March 20, 2014Applicant: SARCODE BIOSCIENCE INC.Inventors: John Burnier, Thomas Gadek
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Publication number: 20140073666Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: August 8, 2013Publication date: March 13, 2014Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier, Min Zhong, Wang Shen, Johan D. Oslob, Kenneth Barr
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Publication number: 20140057953Abstract: The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (l7beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women.Type: ApplicationFiled: March 2, 2012Publication date: February 27, 2014Inventors: Rolf Hartmann, Sandrine Marchais-Oberwinkler, Kuiying Xu, Ruth Werth
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Publication number: 20140057975Abstract: Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Applicant: ALLERGAN, INC.Inventors: Wha-Bin Im, Robert M. Burk
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Publication number: 20140045850Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: ApplicationFiled: March 14, 2013Publication date: February 13, 2014Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20140031290Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: July 8, 2013Publication date: January 30, 2014Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20140031368Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.Type: ApplicationFiled: July 8, 2013Publication date: January 30, 2014Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
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Publication number: 20140018385Abstract: Pharmaceutical compositions and methods for inhibiting cell growth, modulating function of PCNA, treating prostate cancer, and enhancing PCNA trimer formation are disclosed.Type: ApplicationFiled: September 8, 2011Publication date: January 16, 2014Applicant: UNIVERSITY OF CINCINNATIInventors: Zhongyun Dong, Matthew Wortman, Zonqing Tan, Kelsey Dillehay
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Publication number: 20140005151Abstract: Administering water-soluble or dispersible synthetic analogs or derivatives of astaxanthin, lutein, zeaxanthin, or lycophyll and/or other carotenoids to a subject may reduce some of the adverse effects of inflammation in a body organ or tissue. The analogs or derivatives may be incorporated into pharmaceutical, over-the-counter, or nutraceutical preparations. Administration of the analogs or derivatives described herein may reduce deposition of inflammatory mediators such as C-reactive protein, complement system proteins or the membrane attack complex (MAC) in tissues. Reduced deposition of these molecules in tissues may reduce cell damage and/or lysis in the tissues.Type: ApplicationFiled: June 19, 2013Publication date: January 2, 2014Inventor: Samuel F. Lockwood
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Publication number: 20130338132Abstract: Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: June 14, 2012Publication date: December 19, 2013Applicant: Ajinomoto Co., Inc.Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
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Patent number: 8609715Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: GrantFiled: May 31, 2012Date of Patent: December 17, 2013Assignee: Ajinomoto Co., Inc.Inventors: Atsushi Konishi, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
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Publication number: 20130331411Abstract: The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.Type: ApplicationFiled: September 23, 2011Publication date: December 12, 2013Applicants: BETH ISRAEL DEACONESS MEDICAL CENTER, THE BROAD INSTITUTE, INC.Inventors: Chris Dockendorff, Robert Flaumenhaft, Lawrence MacPherson
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Publication number: 20130331392Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 8, 2011Publication date: December 12, 2013Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
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Publication number: 20130331387Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.Type: ApplicationFiled: February 22, 2012Publication date: December 12, 2013Applicant: Lupin LimitedInventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130323203Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: August 2, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
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Patent number: 8592466Abstract: Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.Type: GrantFiled: July 18, 2012Date of Patent: November 26, 2013Assignee: Neuropill, Inc.Inventor: Ahmed Elkashef
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Publication number: 20130261130Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: October 3, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20130245064Abstract: The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein R1 is phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, R2 is hydrogen or methyl, and R3 and R4 have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: September 19, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Piero Paravidino
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Patent number: 8530465Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: August 1, 2012Date of Patent: September 10, 2013Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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Publication number: 20130231375Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 30, 2009Publication date: September 5, 2013Inventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Publication number: 20130217692Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.Type: ApplicationFiled: September 2, 2011Publication date: August 22, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
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Patent number: 8492434Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel 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 hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: GrantFiled: February 22, 2012Date of Patent: July 23, 2013Assignee: Siga Technologies Inc.Inventors: Dennis E. Hruby, Tove C. Bolken, Sean Amberg, Dongcheng Dai
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Patent number: 8487091Abstract: Disclosed herein are compounds represented by the formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: February 25, 2009Date of Patent: July 16, 2013Assignee: Allergan, Inc.Inventors: Mark Holoboski, Robert M. Burk, Mari Posner, Yariv Donde, David W. Old
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Publication number: 20130172367Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: November 27, 2012Publication date: July 4, 2013Applicant: BAYER CROPSCIENCE AGInventor: Bayer CropScience AG
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Publication number: 20130165493Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel 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 hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: February 22, 2012Publication date: June 27, 2013Applicant: Siga Technologies, Inc,Inventors: Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Dongcheng Dai
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Publication number: 20130165443Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: August 23, 2012Publication date: June 27, 2013Inventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20130158087Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.Type: ApplicationFiled: June 21, 2011Publication date: June 20, 2013Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
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Publication number: 20130137704Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: Addex Pharma, SAInventor: Addex Pharma, SA
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Patent number: 8436013Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.Type: GrantFiled: July 9, 2009Date of Patent: May 7, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: Chen Liu, David A. Ostrov