Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/308)
  • Patent number: 9422310
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: January 8, 2015
    Date of Patent: August 23, 2016
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20150098902
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20150072006
    Abstract: The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.
    Type: Application
    Filed: March 1, 2013
    Publication date: March 12, 2015
    Inventors: Katrin Moschner, Torsten Hoffmann, Mario Weingart, Annegret Hildebrand-Cyrener
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8962847
    Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are caused by inflammatory processes. The multicomponent crystals according to the invention contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and an arylpropionic acid as the sole active ingredient combination and can be produced by dissolving flupirtine and the arylpropionic acid in an inert organic solvent and subsequently crystallizing the multicomponent crystal.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: February 24, 2015
    Assignee: TEVA GmbH
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
  • Publication number: 20140363588
    Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
  • Patent number: 8889876
    Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: November 18, 2014
    Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Juan Feng, Wangping Cai
  • Patent number: 8883324
    Abstract: Disclosed is an organic electroluminescence device in which an organic thin film which is composed of one or more layers including at least a light-emitting layer is interposed between a cathode and an anode. Since at least one layer of the organic thin film contains a novel aromatic amine derivative, which has an asymmetric structure wherein two different amine units are bonded through a linking group, by itself or as a component of a mixture, molecules are hardly crystallized, thereby improving the production yield of the organic electroluminescence device. This organic electroluminescence device has a long life.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: November 11, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Nobuhiro Yabunouchi, Hisayuki Kawamura
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Publication number: 20140309225
    Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Hideyasu FUJIWARA, Shinsuke MIZUMOTO, Yohei KUBO, Hiyoku NAKATA, Shinji HAGIWARA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Tomoyuki MASHIKO, Mari YAMAMOTO
  • Patent number: 8853230
    Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: October 7, 2014
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Shawn M. Bauer, Jack W. Rose, Yonghong Song, Qing Xu, Mukund Mehrotra, Wolin Huang, Anjali Pandey
  • Publication number: 20140296534
    Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
    Type: Application
    Filed: January 7, 2014
    Publication date: October 2, 2014
    Applicant: AstraZeneca AB
    Inventors: Seth Björk, Peter Johnström, Nils A. Nilsson, Katinka Ruda, Per M. Schou, Britt-Marie Swahn, Vern Delisser
  • Publication number: 20140256775
    Abstract: The present disclosure provides novel compounds capable of functioning as transcription factor modulators, as well as compositions, pharmaceutical formulations, and kits. Also provided are methods of treating a condition regulatable by a transcription factor and/or cofactor using the compounds, compositions, pharmaceutical formulations, and kits provided herein.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 11, 2014
    Inventors: Lin CHEN, Xiaojiang CHEN, Yongqing WU, Dahai GAI
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Patent number: 8722672
    Abstract: The present invention relates to pharmaceutical compositions of 2-Methyl-4?-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: May 13, 2014
    Assignee: Novartis AG
    Inventors: Andreas Fritze, Karine Corcelle, Melinda Eniko Grubesa
  • Publication number: 20140088105
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20140038948
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Publication number: 20140024621
    Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 23, 2014
    Applicant: MS THERAPEUTICS LIMITED
    Inventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
  • Publication number: 20130345240
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Patent number: 8604212
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: December 10, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Publication number: 20130266744
    Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.
    Type: Application
    Filed: May 31, 2013
    Publication date: October 10, 2013
    Inventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
  • Patent number: 8546579
    Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: October 1, 2013
    Assignee: Evotec (US) Inc.
    Inventors: Michael G. Kelly, John Kincaid, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Zhan Wang, Jianhua He
  • Patent number: 8546403
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: October 1, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8486950
    Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: July 16, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Simon Charles Goodacre, Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Mark S. Stanley, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang, Aihe Zhou
  • Patent number: 8415479
    Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: April 9, 2013
    Assignee: Renascience Co., Ltd.
    Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
  • Patent number: 8367689
    Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: February 5, 2013
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Shawn M. Bauer, Jack W. Rose, Yonghong Song, Qing Xu, Mukund Mehrotra, Wolin Huang, Anjali Pandey
  • Patent number: 8367688
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: February 5, 2013
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
  • Patent number: 8222282
    Abstract: Flupirtine acid addition salts having the following formula (2), wherein R represents a substituted or unsubstituted C1-C12-alkyl or a substituted or unsubstituted C6-C10-aryl group, have been prepared.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: July 17, 2012
    Assignee: Teva Pharmaceuticals USA, Inc.
    Inventors: Christoph Martin Hoock, Asal Qadan
  • Publication number: 20120142743
    Abstract: New polymorphic forms of flupirtine maleate are described.
    Type: Application
    Filed: February 9, 2012
    Publication date: June 7, 2012
    Applicant: PLIVA HRVATSKA D.O.O.
    Inventors: Aleksandar DANILOVSKI, Maja DEVCIC, Marina MARINKOVIC, Ernest MESTROVIC, Tina MUNDORFER, Iva TUNJIC
  • Patent number: 8183267
    Abstract: The preparation of flupirtine carboxylate acid addition salts having the following formula (2), wherein R represents hydrogen or a C1-C6 alkyl group, with the proviso that RCOOH is neither maleic acid nor gluconic acid, is described.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: May 22, 2012
    Assignee: AWD. Pharma GmbH & Co. KG
    Inventors: Christoph Martin Hoock, Asal Qadan
  • Patent number: 8138349
    Abstract: The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: March 20, 2012
    Assignee: Pliva Hrvatska D.O.O.
    Inventors: Aleksandar Danilovski, Maja Dev{hacek over (c)}ić, Marina Marinković, Ernest Me{hacek over (s)}trović, Tina Mundorfer, Iva Tunjić
  • Publication number: 20120059039
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Application
    Filed: May 17, 2010
    Publication date: March 8, 2012
    Applicant: Ishihara Sangyo Kaisha Ltd
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Publication number: 20120028930
    Abstract: The present invention includes salts and polymorphs of flupirtine including, but not limited to carboxylic acid salts and sulfonic acid salts and their polymorphs. The present invention also includes pharmaceutical compositions comprising the salts and polymorphs of flupirtine. The invention also relates to the therapeutic use of the flupirtine salts and polymorphs to treat nervous system disorders, pain disorders, musculoskeletal disorders, and other diseases and conditions.
    Type: Application
    Filed: February 25, 2011
    Publication date: February 2, 2012
    Applicant: Bionevia Pharmaceuticals Inc.
    Inventors: Isabel KALOFONOS, William Martin Doyle
  • Patent number: 8084614
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: December 27, 2011
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Publication number: 20110275679
    Abstract: The invention relates to crystalline forms of flupirtine, particularly to 1:1 flupirtine hydrochloride maleic acid cocrystal. The preparation and characterization of 1:1 flupirtine hydrochloride maleic acid cocrystal is described. The invention also relates to the therapeutic use of the flupirtine hydrochloride maleic acid cocrystal to treat nervous system disorders, pain disorders, and musculoskeletal disorders and to pharmaceutical compositions containing the cocrystal.
    Type: Application
    Filed: August 6, 2009
    Publication date: November 10, 2011
    Applicant: Bionevia Pharmaceuticals, Inc.
    Inventors: Isabel Kalofonos, Dimitris Kalofonos, Patrick G. Stahly, Jeffrey S. Stults, Jason A. Hanko, Rex A. Shipplett, William Martin-Doyle
  • Publication number: 20110263612
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: April 12, 2011
    Publication date: October 27, 2011
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110224266
    Abstract: A composition is provided having the formula where R1 in each occurrence is independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.
    Type: Application
    Filed: January 24, 2011
    Publication date: September 15, 2011
    Inventor: Landon C.G. Miller
  • Publication number: 20110184030
    Abstract: The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.
    Type: Application
    Filed: July 13, 2007
    Publication date: July 28, 2011
    Applicant: PLIVA Hrvatska d.o.o
    Inventors: Aleksandar Danilovski, Maja Devcic, Marina Marinkovic, Ernest Mestrovic, Tina Mundorfer, Iva Tunjic
  • Publication number: 20110152323
    Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.
    Type: Application
    Filed: June 9, 2009
    Publication date: June 23, 2011
    Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Jianqi Li, Juan Feng, Wangping Cai
  • Publication number: 20110009454
    Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.
    Type: Application
    Filed: February 27, 2009
    Publication date: January 13, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue
  • Publication number: 20110003867
    Abstract: This invention relates to novel 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.
    Type: Application
    Filed: December 10, 2008
    Publication date: January 6, 2011
    Applicant: NeuroSearch A/S
    Inventors: Carsten Jessen, William Dalby Brown, Dorte Strøbaek
  • Publication number: 20110003859
    Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: February 27, 2009
    Publication date: January 6, 2011
    Applicant: Array Biopharma Inc.
    Inventor: Kateri A. Ahrendt
  • Publication number: 20110003865
    Abstract: This invention relates to novel 2-diethylamino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-diethylamino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-diethylamino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.
    Type: Application
    Filed: December 10, 2008
    Publication date: January 6, 2011
    Inventors: Carsten Jessen, William Dalby Brown, Dorte Strøbæk
  • Publication number: 20110003866
    Abstract: This invention relates to novel 2-dimethylamino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-dimethylamino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-dimethylamino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.
    Type: Application
    Filed: December 10, 2008
    Publication date: January 6, 2011
    Inventors: William Dalby Brown, Carsten Jessen, Dorte Strøbæk
  • Publication number: 20100324092
    Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Richard W. Heidebrecht, JR., Thomas A. Miller, Matthew G. Stanton, David J. Witter
  • Publication number: 20100261623
    Abstract: Provided herein are methods and compositions that include a method comprising contacting a metal surface with an acidic fluid comprising a corrosion inhibitor that comprises a reaction product formed from a direct or an indirect reaction of an aldehyde with a thiol and/or an amine functionalized ring structure. A composition provided includes an acidic treatment fluid that comprises an aqueous-base fluid, and acid, and a corrosion inhibitor that comprises a reaction product formed from a direct or an indirect reaction of an aldehyde with a thiol and/or an amine functionalized ring structure.
    Type: Application
    Filed: April 14, 2009
    Publication date: October 14, 2010
    Inventors: Juanita M. Cassidy, Chad E. Kiser, Jim L. Lane
  • Publication number: 20100234373
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.
    Type: Application
    Filed: May 26, 2010
    Publication date: September 16, 2010
    Applicant: Amgen Inc.
    Inventors: Erin F. Dimauro, Jean E. Bemis, Stuart C. Chaffee, Ning Chen, Essa Hu, Roxanne Kunz, Matthew W. Martin, David C. McGowan, Shannon Rumfelt
  • Publication number: 20100190777
    Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.
    Type: Application
    Filed: July 16, 2008
    Publication date: July 29, 2010
    Applicant: PLEXXIKON INC.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Patent number: 7727996
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: June 1, 2010
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi