Nitrogen Containing Patents (Class 514/466)
  • Patent number: 9884832
    Abstract: Provided are compounds according to formula (Ia) or (Ib) as described herein, that are capable of modulating the activity of influenza viruses (e.g., influenza A virus), for example, via interaction with the M2 transmembrane protein, and other similar viroporins. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds according to according to formulas (Ia?) or (Ib), as described herein.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: February 6, 2018
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jizhou Wang, Jun Wang, Hyunil Jo, Belgin Canturk
  • Patent number: 9545393
    Abstract: Methods and compositions are provided for treating pain in an individual. Aspects of the methods include administering to the individual an agent that promotes ALDH activity. These methods find many uses, for example in treating and preventing nociceptive pain, inflammatory pain, and neuropathic pain.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: January 17, 2017
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Vanessa Zambelli, Che-Hong Chen, Daria Mochly-Rosen
  • Patent number: 9453004
    Abstract: Formylated xanthocillin analogs can be used in the treatment of neurodegenerative diseases. The analogs can be prepared synthetically, and at least some of the analogs can be obtained from a microorganism strain of the Penicillium chrysogenum species.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: September 27, 2016
    Assignee: NEURON BIOPHARMA, S.A.
    Inventors: Maria del Carmen Ramos Martin, Sonia Campoy Garcia, Javier Santos Burgos Muñoz, José Luis Adrio Fondevila, Javier Velasco Alvarez
  • Patent number: 9133110
    Abstract: A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: September 15, 2015
    Assignee: Hanall Biopharma Co., Ltd.
    Inventors: Sung Wuk Kim, Sung Soo Jun, Chang Hee Min, Se Hwan Park, Yong Eun Kim, Duck Kim, Ji Sun Lee, Ju Hoon Oh
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150133515
    Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery based upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: ALEXANDRE CHIGAEV, LARRY A. SKLAR
  • Publication number: 20150126436
    Abstract: The present invention provides a method of treatment of Scedosporium spp.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: BIODIEM LIMITED
    Inventors: Julie Phillips, Tania Sorrell, Sharon Chen
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Publication number: 20150105456
    Abstract: The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 16, 2015
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Xiaohu Ouyang
  • Publication number: 20150099636
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 9, 2015
    Inventors: Robert Eugene HORMANN, Bing Li
  • Publication number: 20150080439
    Abstract: Various embodiments of the present invention relate to, among other things, compounds that are inhibitors of Memapsin 1 and, as a result, are effective in the treatment of Alzheimer's disease or diabetes (e.g., Type 2 diabetes).
    Type: Application
    Filed: September 12, 2014
    Publication date: March 19, 2015
    Inventor: Arun K. Ghosh
  • Publication number: 20150038512
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, or reduce biofilms, or to inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: Ryan Looper, Dustin Williams, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hariprasada R. Kanna Reddy
  • Publication number: 20150018335
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 15, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150011621
    Abstract: Formylated xanthocillin analogs can be used in the treatment of neurodegenerative diseases. The analogs can be prepared synthetically, and at least some of the analogs can be obtained from a microorganism strain of the Penicillium chrysogenum species.
    Type: Application
    Filed: February 2, 2013
    Publication date: January 8, 2015
    Inventors: Maria del Carmen Ramos Martin, Sonia Campoy García, Javier Santos Burgos Muñoz, José Luis Adrio Fondevila, Javier Velasco Alvarez
  • Publication number: 20140378460
    Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140371271
    Abstract: The present invention provides novel piperine derivatives. The present pharmaceutical or food composition containing a piperine derivative as an active ingredient is very effective in preventing or treating metabolic diseases including obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome. Piperine derivatives of the present invention useful as pharmaceuticals compositions or functional food compositions has therapeutic efficacies for metabolic syndrome selected from the group consisting of obesity, diabetes, hyperlipidemia, fatty liver and insulin resistance syndrome, and also suppress the differentiation of progenitor cells and reduce the accumulation of triglycerides.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 18, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Tae Sun Park, Nak Shin Jeong
  • Patent number: 8906945
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: December 9, 2014
    Assignee: Microbiotix, Inc.
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
  • Publication number: 20140350017
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: November 8, 2013
    Publication date: November 27, 2014
    Applicants: The University of Utah, Curza Global, LLC
    Inventors: Dustin Williams, Ryan Looper, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hari Kanna Reddy
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Publication number: 20140343118
    Abstract: Described herein are methods of treating breast cancer using arylcyclopropylamine compounds.
    Type: Application
    Filed: March 14, 2014
    Publication date: November 20, 2014
    Inventors: Dewey G. McCafferty, Sunhee Hwang, Julie A. Pollock, David M. Gooden
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20140323520
    Abstract: The present disclosure provides methods of increasing proliferation of adult salivary stem cells. The methods include contacting adult salivary stem cells in vivo, in vitro, or ex vivo with an aldehyde dehydrogenase (ALDH) agonist. Increasing proliferation of adult salivary stem cells can be carried out to provide for an increase in the number of adult salivary stem cells in an indi vidual undergoing radiotherapy for head and neck cancer.
    Type: Application
    Filed: April 26, 2012
    Publication date: October 30, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Che-Hong Chen, Daria Mochly-Rosen, Quynh-Thu Le
  • Publication number: 20140314787
    Abstract: The present application provides a method for treating a neurodegenerative disease in a subject characterised in that the endoplasmic reticulum protein retrotranslocation machinery and/or VCP is modulated by administering to said subject a therapeutically effective amount of a modulator of said endoplasmic reticulum protein retrotranslocation machinery and/or of VCP.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 23, 2014
    Inventors: Pico Caroni, Francesco Roselli
  • Publication number: 20140271955
    Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: The Scripps Research Institute, The California Institute for Biomedical Research
    Inventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
  • Publication number: 20140243324
    Abstract: The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.
    Type: Application
    Filed: November 17, 2011
    Publication date: August 28, 2014
    Applicant: LIGAND PHARMACEUTICALS INCORPORATED
    Inventors: Reid P. Bissonnette, Andrew R. Hudson, Keith B. Marschke, Deepa Rungta, Lin Zhi
  • Publication number: 20140243366
    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: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20140219995
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: July 13, 2012
    Publication date: August 7, 2014
    Applicant: MICROBIOTIX, INC.
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
  • Publication number: 20140205688
    Abstract: The present invention relates to a stimulating agent comprising a pungent component having astringency, a stimulating composition including the agent, as well as a flavor or fragrance composition, a food, a drink, an oral care product and an external skin preparation containing the agent or the composition, and also relates to the use of a pungent component having astringency as a stimulating agent. Examples of the pungent component having astringency include a plant extract of Asteraceae Spilanthes, Rutaceae Zanthoxyium, Rutaceae Fagara, or Piperaceae Piper, or an amide derivative represented by general formula (1) (where R1 represents an alkenyl group having 2 to 12 carbon atoms which may be substituted by a methylenedioxyphenyl at the end, R2 and R3 may be the same or different from each other and each are a hydrogen atom or a lower alkyl group in which a hydroxyl group may be substituted, and R2 and R3, together with the nitrogen atom adjacent thereto, may form a heterocyclic ring).
    Type: Application
    Filed: May 29, 2012
    Publication date: July 24, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Kaori Takahashi, Miyuki Takayanagi
  • Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20140179735
    Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 26, 2014
    Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Publication number: 20140142134
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Psendomonas spp., Yersinia spp., en tero pathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 22, 2014
    Applicant: MICROBIOTIX, INC.
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
  • Publication number: 20140135360
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc
    Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Publication number: 20140121242
    Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.
    Type: Application
    Filed: June 26, 2012
    Publication date: May 1, 2014
    Applicant: TASLY PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
  • Publication number: 20140080876
    Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Applicant: Biodiem Ltd
    Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
  • Publication number: 20140044810
    Abstract: Use of amide compounds represented by formula (I), for preventing or reducing settlement and/or fouling of marine fouling organisms on a surface of a submerged object is provided, wherein “-A-” has a formula -(CnH2(n?m))- which is either unsubstituted or substituted by one or more C1 to C4 alkyls, and wherein the formula -(CnH2(n?m))- represents a divalent alkyl, or a divalent alkenyl having one or more double bonds, n is 1 to 15, m is 0 to 4, and 2(n?m)=2, and R is selected from piperidinyl, pyrrolidinyl, isobutylamino, piperazinyl or morpholinyl. Amide compounds of formula (I), a category of antifouling compounds, can be either isolated from natural resources or synthesized, which are nontoxic and environmental-friendly.
    Type: Application
    Filed: April 17, 2012
    Publication date: February 13, 2014
    Applicants: YUNNAN UNIVERSITY OF NATIONALITIES, THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Peiyuan Qian, Xiangzhong Huang, Ying Xu, Yu Zhang, Yue Him Wong, Yan Yin, Zhuang Han
  • Patent number: 8648071
    Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: February 11, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
  • Patent number: 8642647
    Abstract: The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 4, 2014
    Assignees: Hanall Biopharma Co., Ltd., Korea Research Institute of Chemical Technology
    Inventors: Sung Wuk Kim, Sung Soo Jun, Hyae Gyeong Cheon, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong Cheol Lee
  • Publication number: 20130338095
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130331390
    Abstract: Nitrogen-containing biphenyl compounds as represented by formula (I), pharmaceutically acceptable salts or derivatives thereof, pharmaceutical compositions, and preparation methods therefore, and anti-HIV-1 use of the compound. Each substituent group in formula (I) is as defined in the description.
    Type: Application
    Filed: October 13, 2011
    Publication date: December 12, 2013
    Applicants: Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming Institute of Zoology, The Chinese Academy of Sciences, Yunnan University
    Inventors: Jingping Liu, Handong Sun, Hongbin Zhang, Yongtong Zheng, Weilie Xiao, Jianxin Pu, Ruirui Wang, Liumeng Yang
  • Patent number: 8598225
    Abstract: The present invention discloses the use of L-butylphthalide of formula (I) in the manufacture of medicaments for the prevention and treatment of cerebral infarct, especially induced by focal cerebral ischemia.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: December 3, 2013
    Assignee: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.
    Inventors: Yipu Feng, Xiaoliang Wang, Jinghua Yang, Ying Peng
  • Publication number: 20130303568
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Application
    Filed: April 22, 2013
    Publication date: November 14, 2013
    Inventors: Nancy C. LAN, Yan Wang, Sui Xiong Cai
  • Publication number: 20130296306
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: June 27, 2013
    Publication date: November 7, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20130295009
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof;
    Type: Application
    Filed: March 14, 2013
    Publication date: November 7, 2013
    Inventors: Torbjorn LUNDSTEDT, Anna SKOTTNER, Elisabeth SEIFERT
  • Patent number: 8569363
    Abstract: Disclosed is a method of treatment and/or prophylaxis of a microbial infection, employing compounds of formula (I), in which X and Y are either the same of different and selected from a hereroatiom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 to R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 to R7 are absent when there is a double bond present. Also disclosed are methods for protecting a subject from radiation damage, methods of cancer radiotherapy, and use of the disclosed compounds as an antimicrobial or radioprotective agent.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: October 29, 2013
    Assignee: Biodiem Ltd.
    Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
  • Publication number: 20130281490
    Abstract: The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.
    Type: Application
    Filed: November 21, 2012
    Publication date: October 24, 2013
    Inventors: The Regents of the University of California, Fondazione Istituto Italiano Di Tecnologia, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino "Carlo Bo"
  • Publication number: 20130281394
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: October 24, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Patent number: 8518940
    Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: August 27, 2013
    Assignee: The Wistar Institute
    Inventor: Emmanuel Skordalakes