Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/156)
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Publication number: 20120270863Abstract: 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: October 25, 2012Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Patent number: 8288549Abstract: The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: GrantFiled: September 30, 2009Date of Patent: October 16, 2012Assignee: Merz Pharma GmbH & Co. KGaAInventors: Markus Henrich, Angela Bauer, Jens Nagel, Meik Sladek, Christopher Graham Raphael Parsons, Wojciech Danysz, Valerjans Kauss, Jevgenijs Rozhkovs, Igors Starchenkovs, Dina Trifanova
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Publication number: 20120258982Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: April 3, 2012Publication date: October 11, 2012Inventors: Adrian Wai-Hing Cheung, Kevin Richard Guertin, Nancy-Ellen Haynes, Eric Mertz, Lida Qi, Yimin Qian, Nathan Robert Scott
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Publication number: 20120252841Abstract: The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: June 15, 2012Publication date: October 4, 2012Applicant: DRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER
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Patent number: 8273892Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: April 20, 2010Date of Patent: September 25, 2012Assignee: Abbott LaboratoriesInventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Publication number: 20120238758Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: March 6, 2012Publication date: September 20, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Eric Dowdy, Steven Pfeiffer
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Patent number: 8252813Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: February 5, 2010Date of Patent: August 28, 2012Assignee: Abbott LaboratoriesInventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Publication number: 20120214841Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: ApplicationFiled: January 26, 2012Publication date: August 23, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20120208843Abstract: The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to a method for treating or preventing a metabolic-related disorder, comprising administering to an individual in need thereof an effective amount of a GPR35 modulator.Type: ApplicationFiled: September 16, 2011Publication date: August 16, 2012Inventors: James N. Leonard, Zhi Liang Chu
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Publication number: 20120208841Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: April 4, 2012Publication date: August 16, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20120197005Abstract: The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.Type: ApplicationFiled: January 30, 2012Publication date: August 2, 2012Applicant: UCHICAGO ARGONNE, LLCInventors: Chris J. Benmore, Johann R. Weber
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Publication number: 20120196894Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.Type: ApplicationFiled: September 28, 2010Publication date: August 2, 2012Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
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Patent number: 8232401Abstract: An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.Type: GrantFiled: June 5, 2006Date of Patent: July 31, 2012Assignee: Japan Tobacco Inc.Inventors: Motohide Satoh, Hiroshi Kawakami, Yoshiharu Itoh, Hisashi Shinkai, Takahisa Motomura, Hisateru Aramaki, Yuji Matsuzaki, Wataru Watanabe, Shuichi Wamaki
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Publication number: 20120190707Abstract: The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to prevent and treat cancer and other conditions.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Inventors: Ze'ev Ronai, Maurizio Pellecchia, Gary Chiang
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Publication number: 20120184548Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer.Type: ApplicationFiled: January 11, 2012Publication date: July 19, 2012Inventors: Romyr Dominique, Kin-Chun Luk, Qi Qiao, Pamela Loreen Rossman
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Patent number: 8222407Abstract: To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.Type: GrantFiled: May 23, 2008Date of Patent: July 17, 2012Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Masanori Takadoi, Yoshikazu Asahina, Taro Sato, Haruaki Kurasaki, Hiroyuki Ebisu, Masaya Takei, Hideyuki Fukuda
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Patent number: 8211910Abstract: A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided.Type: GrantFiled: April 13, 2009Date of Patent: July 3, 2012Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
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Publication number: 20120165372Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.Type: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: John DeMattei, Yushi Feng, Cristian Harrison, Adam Looker, Praveen Mudunuri, Stefanie Roeper, Yuegang Zhang
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Publication number: 20120157447Abstract: A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.Type: ApplicationFiled: September 28, 2007Publication date: June 21, 2012Inventor: Arthur E. Harms
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Publication number: 20120142635Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120135961Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: January 10, 2011Publication date: May 31, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Publication number: 20120122921Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: September 20, 2011Publication date: May 17, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John DeMattei, Adam R. Looker, Bobbianna J. Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Lao Yap Guerette, Brian R. Krueger, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
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Patent number: 8178667Abstract: The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the M1 receptor is involved.Type: GrantFiled: June 27, 2007Date of Patent: May 15, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Craig Lindsley, William D. Shipe, Feng Yang, Jaime Lynn Bunda
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Publication number: 20120108582Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.Type: ApplicationFiled: July 2, 2009Publication date: May 3, 2012Inventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
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Patent number: 8163922Abstract: 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride of formula (I) may be conveniently prepared in a diastereomeric pure form from optically pure precursors that are readily available by simple resolution and asymmetric reduction.Type: GrantFiled: July 30, 2009Date of Patent: April 24, 2012Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fausto Pivetti, Monica Bocchi, Maurizio Delcanale
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Publication number: 20120094833Abstract: The present invention relates to novel herbicidal oxopyridine and thionopyridine derivatives of Formula (I), or an agronomically acceptable salt of said compound wherein R1, R5, R6, R7, X1, X2 and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the oxopyridine derivatives, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: March 31, 2010Publication date: April 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Roger Salmon, Glynn Mitchell, James Alan Morris
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Patent number: 8158798Abstract: Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.Type: GrantFiled: October 27, 2008Date of Patent: April 17, 2012Assignee: TaiGen Biotechnology Co., Ltd.Inventor: Michael Reilly
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Patent number: 8158797Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.Type: GrantFiled: December 20, 2004Date of Patent: April 17, 2012Assignee: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Patent number: 8153801Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: September 11, 2008Date of Patent: April 10, 2012Assignee: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Publication number: 20120071466Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: ApplicationFiled: June 4, 2010Publication date: March 22, 2012Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
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Publication number: 20120071504Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.Type: ApplicationFiled: September 20, 2011Publication date: March 22, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
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Publication number: 20120071505Abstract: Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: October 21, 2011Publication date: March 22, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel, Samuel Victory
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Publication number: 20120053206Abstract: The invention relates to substituted 2-oxo- and 2-thioxo-dihydroquinoline-3-carboxamides to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: August 26, 2011Publication date: March 1, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Publication number: 20120053192Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.Type: ApplicationFiled: May 4, 2010Publication date: March 1, 2012Applicants: Nanjing Luyesike Pharmaceutical Co., Ltd., Jiangsu Provincial Institute of Materia Medica Co. Ltd.Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
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Publication number: 20120041208Abstract: The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.Type: ApplicationFiled: September 23, 2009Publication date: February 16, 2012Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Roger Hanselmann, Maxwell M. Reeve, Graham Johnson
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Publication number: 20120041001Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Janssen Pharmaceutica, NVInventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
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Publication number: 20120029015Abstract: The invention relates to the use of kynurenic acid derivatives of general formula (I), wherein R1 is hydroxy, NHR2, NR2R2 or C1-10 straight or branched alkoxy or glyceryl group; R2 is hydrogen atom or C1-10 straight or branched alkyl group; R3-R6 are independently of each other hydrogen atom, halogen atom, C1-10 alkyl, C2-10 alkenyl or alkynyl group optionally substituted with a halogen atom, and a pharmaceutically acceptable salt, ester or amide thereof in manufacturing of a drug used in prevention and therapy of pancreas disorders characterized by edema and/or vacuolization and/or destruction of pancreatic tissue and/or pancreas necrosis leading to release of pancreatic ?-amylase. Preferably, in the compound represented by formula (I) R1 is a hydroxy, NH2, NH—(C1-5 straight or branched alkyl) or C1-5 straight or branched-alkoxy or glyceryl group; R2 is a hydrogen atom; R3-R6 are independently of each other a hydrogen atom, halogen atom or CF3 group.Type: ApplicationFiled: March 23, 2010Publication date: February 2, 2012Inventors: Andrzej Marciniak, Waldemar Turski
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Patent number: 8106072Abstract: Object To provide novel quinolinecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. Solving Means There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe.Type: GrantFiled: February 26, 2009Date of Patent: January 31, 2012Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yoshikazu Asahina, Masaya Takei
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Patent number: 8101766Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.Type: GrantFiled: February 11, 2009Date of Patent: January 24, 2012Assignee: Theravance, Inc.Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
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Publication number: 20120010238Abstract: The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Inventors: Victor Piryatinsky, Avital Laxer
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Patent number: 8093381Abstract: The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.Type: GrantFiled: May 22, 2008Date of Patent: January 10, 2012Assignee: BiocodexInventors: Laurence Berthon-Cedille, Marie-Emmanuelle Leguern, Gilles Renaud, Francis Tombret
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Publication number: 20110312995Abstract: This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Robert Jason Herr, Jason L. Davis, Kai Deng, Ming Min Hsia, Shuangyi Wan
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Patent number: 8071615Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: September 19, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
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Publication number: 20110288121Abstract: The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).Type: ApplicationFiled: May 20, 2011Publication date: November 24, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lifang Sun, Khisal Ahmed Alvi, Caroline Joyce Decker, Yongmin Li
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Publication number: 20110287937Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.Type: ApplicationFiled: February 2, 2010Publication date: November 24, 2011Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
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Patent number: 8063221Abstract: Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.Type: GrantFiled: March 13, 2007Date of Patent: November 22, 2011Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Oana Cociorva, Bei Li, Anna Katrin Szardenings, Yasumichi Fukuda, Masahiro Nomura, Shigeki Seto, Kazuhiro Yumoto, Kyoko Okada, Ayako Nakamura
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Publication number: 20110269741Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: March 28, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Huanming CHEN, Jianlin SONG, Jean-Michel VERNIER, Anthony B. PINKERTON, Johnny Y. NAGASAWA