Phosphorus Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/22)
  • Patent number: 10174062
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: January 8, 2019
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 10112884
    Abstract: The present invention relates to the technical field of organic chemistry, specifically an asymmetrical hydrogenation of an ?-ketonic acid compound, the technical proposal being as shown by the following formula: Wherein R1 is a phenyl, a substituted phenyl, a naphthyl a substituted naphthyl, a C1-C6 alkyl or aralkyl, the substitute is a C1-C6 alkyl, a C1-C6 alkoxy, a halogen, the number of the substituents is 1-3.
    Type: Grant
    Filed: April 28, 2015
    Date of Patent: October 30, 2018
    Inventors: Pucha Yan, Yuanqiang Li, Daqing Che, Xiangdong Zhang, Kang Chen, Yongliang Yan
  • Patent number: 10065947
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Patent number: 10005805
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: June 26, 2018
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 9988406
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: June 5, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Patent number: 9771385
    Abstract: The present invention is directed to oxidized lipids and pharmaceutical compositions comprising the same. The present invention is also directed to methods of making an oxidized lipid of the invention and to methods of treating or preventing fibrosis or inflammatory diseases or disorders comprising an oxidized lipid of the invention.
    Type: Grant
    Filed: November 25, 2015
    Date of Patent: September 26, 2017
    Assignee: Vascular Biogenics Ltd.
    Inventors: Eti Kovalevski Ishai, Itzhak Mendel, Yaniv Salem, Niva Yacov, Eyal Breitbart
  • Patent number: 9624250
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: April 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Patent number: 9605010
    Abstract: Novel monophosphite compounds having a methyl group, and a process for preparing these compounds, which are especially suitable for use as ligands in hydroformylation reactions.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: March 28, 2017
    Assignee: EVONIK DEGUSSA GMBH
    Inventors: Katrin Marie Dyballa, Robert Franke
  • Patent number: 9181184
    Abstract: The present invention provides a method for increasing the activity of a mutant or wild-type ?-glucosidase enzyme in vitro and in vivo by contacting the enzyme with a specific pharmacological chaperone which is a derivative of 1-deoxynojirimycin. The invention also provides a method for the treatment of Pompe disease by administration of chaperone small molecule compound which is a derivative of 1-deoxynojirimycin. The 1-deoxynojirimycin derivative is substituted at the N or C1 position. Combination therapy with replacement ?-glucosidase gene or enzyme is also provided.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: November 10, 2015
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Benjamin Mugrage, Gary Lee, Xiaoxiang Zhu, Robert Boyd, Kamlesh Sheth
  • Patent number: 9029542
    Abstract: A substituted phenoxyethyl(isopropyl)acyloxyalkyl phosphonate having phosphorusheterocyclic ring and having herbicidal activity, with a general formula of I, wherein R represents 5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one-2-yl, or 1-oxo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl, or 1-sulfo-1-phospha-2,6,7-trioxabicyclo 2,6,7-trioxabicyclo[2,2,2]octan-4-yl; R1 represents H, C1-C4 alkyl, phenyl, furyl, pyridyl, or phenyl substituted with methyl, methoxyl, nitro or chloro; R2 represents H, methyl, and methyl only if R in the general formula I is 1-sulfo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl as phosphorusheterocyclic ring; X and Y represent H, halogen, C1-C4 alkyl or trifluoromethyl, and X and Y are the same or different. The compounds according to the present invention may be used as active component of dicotyledonous broadleaf weed herbicides.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: May 12, 2015
    Assignee: Central China Normal University
    Inventors: Hongwu He, Wei Wang, Na Zuo, Xijun Sheng, Hao Peng, Xiaosong Tan
  • Publication number: 20150097162
    Abstract: Provided is an organic electroluminescent element which has improved driving voltage and improved current efficiency. An organic electroluminescent element having the above-mentioned improved characteristics is provided by using, as a material for organic electroluminescent elements, a polycyclic aromatic compound in which a nitrogen atom and another heteroatom or a metal atom (X) are adjacent to each other in a non-aromatic ring.
    Type: Application
    Filed: September 11, 2013
    Publication date: April 9, 2015
    Applicants: JNC Corporation, Kyoto University
    Inventors: Yohei Ono, Kazushi Shiren, Toshiaki Ikuta, Jingping Ni, Takeshi Matsushita, Takuji Hatakeyama, Masaharu Nakamura, Shiguma Hashimoto
  • Publication number: 20150080345
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 19, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150065466
    Abstract: The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group.
    Type: Application
    Filed: April 18, 2013
    Publication date: March 5, 2015
    Inventor: Yongcheng Song
  • Patent number: 8969560
    Abstract: A novel bidentate ligand of general formula (I) is described together with a process for the carbonylation of ethylenically unsaturated compounds. The group X1 may be defined as a univalent hydrocarbyl radical of up to 30 atoms containing at least one nitrogen atom having a pKb in dilute aqueous solution at 18° C. of between 4 and 14 wherein the said at least one nitrogen atom is separated from the Q2 atom by between 1 and 3 carbon atoms. The group X2 is defined as X1, X3 or X4 or represents a univalent radical of up to 30 atoms having at least one primary, secondary or aromatic ring carbon atom wherein each said univalent radical is joined via said at least one primary, secondary or aromatic ring carbon atom(s) respectively to the respective atom Q2. Q1 and Q2 each independently represent phosphorus, arsenic or antimony.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: March 3, 2015
    Assignee: Lucite International UK Limited
    Inventors: Graham Ronald Eastham, Mark Waugh, Paul Pringle, Thomas Philip William Turner
  • Publication number: 20150057251
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: August 26, 2013
    Publication date: February 26, 2015
    Inventor: Jason R. Harris
  • Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • Patent number: 8962839
    Abstract: The present invention relates to a chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof. The chiral spiro-pyridylamidophosphine compound is a compound having a structure of Formula (I), a racemate or optical isomer thereof, or a catalytically acceptable salt thereof, and is mainly characterized by having a chiral spiro-dihydro-indene skeleton in its structure. The chiral spiro-pyridylamidophosphine compound may be synthesized with optical active 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene or substituted 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene having a spiro-skeleton as chiral starting material. The chiral spiro-pyridylamidophosphine compound may be used as a chiral ligand in asymmetric hydrogenation of a carbonyl compound catalyzed by iridium, in which the reaction activity is very high, the amount of the catalyst may be 0.0001 mol %, and the enantioselectivity of the reaction is up to 99.9% ee.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 24, 2015
    Assignee: Zhejiang Jiuzhou Pharma Science & Technology Co., Ltd.
    Inventors: Qilin Zhou, Jianhua Xie, Xiaoyan Liu, Jianbo Xie, Lixin Wang
  • Publication number: 20150034927
    Abstract: A compound represented by the following formula (1-1):
    Type: Application
    Filed: February 7, 2013
    Publication date: February 5, 2015
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Yuki Nakano, Hiroshi Yamamoto, Ryohei Hashimoto, Hideaki Nagashima
  • Patent number: 8946418
    Abstract: The invention relates to a series of novel chiral nitrogen-phosphorus ligands of formulae (Ia) and (Ib): wherein R1-R3 and X are as defined herein. The invention also relates to chiral metal complexes prepared with these chiral nitrogen-phosphorus ligands. The chiral metal complexes are useful as catalysts for carrying out asymmetric hydrogenation.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Nizar Haddad, Bo Qu, Jolaine Savoie, Chris Hugh Senanayake, Xudong Wei
  • Patent number: 8937055
    Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 20, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
  • Publication number: 20150011758
    Abstract: A novel bidentate ligand of general formula (I) is described together with a process for the carbonylation of ethylenically unsaturated compounds. The group X1 may be defined as a univalent hydrocarbyl radical of up to 30 atoms containing at least one nitrogen atom having a pKb in dilute aqueous solution at 18° C. of between 4 and 14 wherein the said at least one nitrogen atom is separated from the Q2 atom by between 1 and 3 carbon atoms. The group X2 is defined as X1, X3 or X4 or represents a univalent radical of up to 30 atoms having at least one primary, secondary or aromatic ring carbon atom wherein each said univalent radical is joined via said at least one primary, secondary or aromatic ring carbon atom(s) respectively to the respective atom Q2. Q1 and Q2 each independently represent phosphorus, arsenic or antimony.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Inventors: Graham Ronald EASTHAM, Mark WAUGH, Paul PRINGLE, Thomas Philip William TURNER
  • Publication number: 20150004666
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: January 18, 2013
    Publication date: January 1, 2015
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Publication number: 20140349973
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 27, 2014
    Applicant: Viamet Pharmaceuticals, Inc
    Inventors: William J. Hoekstra, Christopher M. Yates
  • Publication number: 20140339098
    Abstract: A process for the catalyzed electrochemical reduction of carbon dioxide wherein a metal organic framework comprising metal ions and an organic ligand is used as a catalyst and novel metal organic frameworks based on bisphosphonic acids.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 20, 2014
    Inventors: Adam Wieslaw Mazur, Jean-Yves Nedelec, Christine Cachet-Vivier, Maniyan Padmanilayam, Armin T. Liebens
  • Publication number: 20140323440
    Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Eric Thomas Miller, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
  • Publication number: 20140309422
    Abstract: The present invention relates to the compound of dialkyl(2-alkoxy-6-aminophenyl)phosphine and the preparation method thereof and the application in the palladium catalyzed coupling reactions of aryl chloride and ketone. The dialkyl(2-alkoxy-6-aminophenyl)phosphine of the present invention could coordinate with the palladium catalyst to highly selectively activate the inert carbon-chlorine bond, and to catalyze direct arylation reaction in the ?-position of ketones to produce corresponding coupling compounds. The preparation method of the present invention is a simple one-step method which produces the air-stable dialkyl(2-alkoxy-6-aminophenyl)phosphine. Compared with the synthetic routes of ligands to be used in the activation of carbon-chlorine bonds in the prior arts, the preparation method of the present invention has the advantages of short route and easy operation.
    Type: Application
    Filed: July 3, 2012
    Publication date: October 16, 2014
    Applicant: ZHEJIANG UNIVERSITY
    Inventors: Shengming Ma, Bo Lv, Chunling Fu
  • Publication number: 20140274961
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: Global Blood Therapeutics, Inc.
    Inventors: Brian W. Metcalf, Jason R. Harris, Zhe Li, Stephen L. Gwaltney, II
  • Publication number: 20140256945
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Patent number: 8828973
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: March 18, 2014
    Date of Patent: September 9, 2014
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, John R. Cappiello
  • Publication number: 20140243291
    Abstract: The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 28, 2014
    Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle
  • Patent number: 8816082
    Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: August 26, 2014
    Assignee: The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
  • Publication number: 20140235584
    Abstract: The present invention relates to a biaryl heterocycle substituted oxazolidinone antibacterials shown by general formula (I), a pharmaceutically acceptable salt thereof, an isomer or a prodrug thereof, wherein R1, R2, R3, R4, R5, A and B are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound in the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 21, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Aichen Wang
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Publication number: 20140228553
    Abstract: The present invention relates to organic compounds that are usable as ligands for preparing complexes of lanthanides or of certain transition metals which are water-soluble, to a method for preparing same, and also to the use thereof as a fluorescent probe.
    Type: Application
    Filed: October 11, 2012
    Publication date: August 14, 2014
    Inventors: Raymond Ziessel, Mathieu Starck, Alexandra Sutter
  • Publication number: 20140221637
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Application
    Filed: November 30, 2011
    Publication date: August 7, 2014
    Inventor: Yoshihito Ueno
  • Publication number: 20140199600
    Abstract: The present invention provides a nonaqueous electrolyte solution, which can improve flame retardancy and ameliorate performances of a battery without deteriorating the basic battery performance as far as possible, and a secondary battery. The nonaqueous electrolyte solution is a nonaqueous electrolyte solution for a secondary battery that contains metal salts including ions of metals belonging to group 1 or 2 of the periodic table and a specific cyclic compound having phosphorus and nitrogen atoms in a non-protonic solvent. The non-protonic solvent is a solvent that contains at least one kind of carboxylic acid ester compound and carbonic acid ester compound, and a ratio (MPN/Ms) between a mass (Ms) of the non-protonic solvent containing the metal salts and a mass (MPN) of the cyclic compound is 0.01 to 1.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Toshihiko YAWATA, Ikuo KINOSHITA
  • Patent number: 8779135
    Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: July 15, 2014
    Assignee: Straitmark Holding AG
    Inventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
  • Publication number: 20140194389
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20140187780
    Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
    Type: Application
    Filed: December 24, 2013
    Publication date: July 3, 2014
    Applicant: Enanta Pharmaceuticals, Inc.
    Inventors: In Jong Kim, Tongzhu Liu, Jiang Long, Guoqiang Wang, Yao-Ling Qiu, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
  • Patent number: 8765722
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 1, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20140171644
    Abstract: A substituted phenoxyethyl(isopropyl)acyloxyalkyl phosphonate having phosphorusheterocyclic ring and having herbicidal activity, with a general formula of I, wherein R represents 5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one-2-yl, or 1-oxo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl, or 1-sulfo-1-phospha-2,6,7-trioxabicyclo 2,6,7-trioxabicyclo[2,2,2]octan-4-yl; R1 represents H, C1-C4 alkyl, phenyl, furyl, pyridyl, or phenyl substituted with methyl, methoxyl, nitro or chloro; R2 represents H, methyl, and methyl only if R in the general formula I is 1-sulfo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl as phosphorusheterocyclic ring; X and Y represent H, halogen, C1-C4 alkyl or trifluoromethyl, and X and Y are the same or different. The compounds according to the present invention may be used as active component of dicotyledonous broadleaf weed herbicides.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: CENTRAL CHINA NORMAL UNIVERSITY
    Inventors: Hongwu He, Wei Wang, Na Zuo, Xijun Sheng, Hao Peng, Xiaosong Tan
  • Publication number: 20140161839
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: PHARMALEADS
    Inventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
  • Patent number: 8741875
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: June 3, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, John Cappiello
  • Publication number: 20140135290
    Abstract: The present invention includes macrocyclic prodrug compounds, pharmaceutical compositions containing them. The present invention also includes use of these compounds in the treatment of various diseases including an autoimmune disease, an inflammatory disease, a neurological or neurodegenerative disease, cancer, a cardiovascular disease, allergy, asthma, a hormone-related disease, and tumors or symptoms resulting from neurofibromatosis.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 15, 2014
    Applicants: ONCOSYNERGY, INC., LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURG
    Inventors: James HECK, Nicolas Winssinger, John C. Chabala, Sofia Barluenga, Ruihong Chen, Allan Rubenstein, Jin-Chen Yu
  • Patent number: 8716265
    Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: May 6, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat, David Nugiel
  • Patent number: 8710215
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: April 29, 2014
    Assignee: Warner Chilcott Company, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Patent number: 8703437
    Abstract: The present invention provides fluorogenic substrates and methods of use in detecting and analyzing phospholipase C isozyme (PLC) activity.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: April 22, 2014
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Qisheng Zhang, Wei Gang Huang, John Sondek, Stephanie Hicks
  • Patent number: 8703745
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: April 22, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen