Phosphorus Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/22)
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Patent number: 11331391Abstract: This invention relates to drug conjugates useful for localized treatment of diseases or disorders of the middle ear and/or inner ear. Methods of treating diseases or disorders of the middle ear and/or inner ear, pharmaceutical compositions comprising the conjugates, and methods of inhibiting a Tropomyosin receptor kinase are also provided.Type: GrantFiled: January 25, 2017Date of Patent: May 17, 2022Assignees: Massachusetts Eye and Ear Infirmary, University of Southern CaliforniaInventors: Charles E. McKenna, Boris A. Kashemirov, Shuting Sun, Kim Nguyen, David Jung, Michael J. McKenna, William Sewell, Judith Kempfle, Woo Seok Kang, Albert Edge
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Patent number: 10550088Abstract: The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R?, R?, R?? R1, R2, R3, R4, R4a, and R20 are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I or II and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors. Certain compounds of the invention are especially useful for treating pain.Type: GrantFiled: October 10, 2014Date of Patent: February 4, 2020Assignee: Purdue Pharma L.P.Inventors: Jeffrey Lockman, Laykea Tafesse, Jae Hyun Park, Mark A. Youngman
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Patent number: 10442829Abstract: 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: GrantFiled: May 3, 2018Date of Patent: October 15, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Patent number: 10174062Abstract: 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: GrantFiled: December 19, 2016Date of Patent: January 8, 2019Assignee: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Patent number: 10112884Abstract: 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: GrantFiled: April 28, 2015Date of Patent: October 30, 2018Inventors: Pucha Yan, Yuanqiang Li, Daqing Che, Xiangdong Zhang, Kang Chen, Yongliang Yan
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Patent number: 10065947Abstract: 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: GrantFiled: May 3, 2018Date of Patent: September 4, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Patent number: 10005805Abstract: 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: GrantFiled: December 19, 2016Date of Patent: June 26, 2018Assignee: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Patent number: 9988406Abstract: 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: GrantFiled: March 10, 2017Date of Patent: June 5, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Patent number: 9771385Abstract: 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: GrantFiled: November 25, 2015Date of Patent: September 26, 2017Assignee: Vascular Biogenics Ltd.Inventors: Eti Kovalevski Ishai, Itzhak Mendel, Yaniv Salem, Niva Yacov, Eyal Breitbart
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Patent number: 9624250Abstract: 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: GrantFiled: December 4, 2015Date of Patent: April 18, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Patent number: 9605010Abstract: 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: GrantFiled: April 28, 2016Date of Patent: March 28, 2017Assignee: EVONIK DEGUSSA GMBHInventors: Katrin Marie Dyballa, Robert Franke
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Patent number: 9181184Abstract: 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: GrantFiled: May 17, 2006Date of Patent: November 10, 2015Assignee: Amicus Therapeutics, Inc.Inventors: Benjamin Mugrage, Gary Lee, Xiaoxiang Zhu, Robert Boyd, Kamlesh Sheth
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Patent number: 9029542Abstract: 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: GrantFiled: February 20, 2014Date of Patent: May 12, 2015Assignee: Central China Normal UniversityInventors: Hongwu He, Wei Wang, Na Zuo, Xijun Sheng, Hao Peng, Xiaosong Tan
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Publication number: 20150097162Abstract: 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: ApplicationFiled: September 11, 2013Publication date: April 9, 2015Applicants: JNC Corporation, Kyoto UniversityInventors: Yohei Ono, Kazushi Shiren, Toshiaki Ikuta, Jingping Ni, Takeshi Matsushita, Takuji Hatakeyama, Masaharu Nakamura, Shiguma Hashimoto
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Publication number: 20150080345Abstract: 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: ApplicationFiled: February 28, 2013Publication date: March 19, 2015Inventor: Mahesh Kandula
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Publication number: 20150065466Abstract: 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: ApplicationFiled: April 18, 2013Publication date: March 5, 2015Inventor: Yongcheng Song
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Patent number: 8969560Abstract: 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: GrantFiled: December 29, 2010Date of Patent: March 3, 2015Assignee: Lucite International UK LimitedInventors: Graham Ronald Eastham, Mark Waugh, Paul Pringle, Thomas Philip William Turner
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Publication number: 20150057251Abstract: 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: ApplicationFiled: August 26, 2013Publication date: February 26, 2015Inventor: Jason R. Harris
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Publication number: 20150057220Abstract: 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: ApplicationFiled: April 16, 2013Publication date: February 26, 2015Inventors: Michel Therien, Yves Leblanc, Yongxin Han
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Patent number: 8962839Abstract: 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: GrantFiled: November 18, 2011Date of Patent: February 24, 2015Assignee: Zhejiang Jiuzhou Pharma Science & Technology Co., Ltd.Inventors: Qilin Zhou, Jianhua Xie, Xiaoyan Liu, Jianbo Xie, Lixin Wang
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Publication number: 20150034927Abstract: A compound represented by the following formula (1-1):Type: ApplicationFiled: February 7, 2013Publication date: February 5, 2015Applicant: Idemitsu Kosan Co., Ltd.Inventors: Yuki Nakano, Hiroshi Yamamoto, Ryohei Hashimoto, Hideaki Nagashima
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Patent number: 8946418Abstract: 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: GrantFiled: July 9, 2014Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Nizar Haddad, Bo Qu, Jolaine Savoie, Chris Hugh Senanayake, Xudong Wei
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Patent number: 8937055Abstract: 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: GrantFiled: July 14, 2011Date of Patent: January 20, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
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Publication number: 20150011758Abstract: 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: ApplicationFiled: September 22, 2014Publication date: January 8, 2015Inventors: Graham Ronald EASTHAM, Mark WAUGH, Paul PRINGLE, Thomas Philip William TURNER
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Publication number: 20150004666Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: January 18, 2013Publication date: January 1, 2015Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Publication number: 20140371176Abstract: 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: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
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Publication number: 20140357599Abstract: 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: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
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Publication number: 20140349973Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 10, 2012Publication date: November 27, 2014Applicant: Viamet Pharmaceuticals, IncInventors: William J. Hoekstra, Christopher M. Yates
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Publication number: 20140339098Abstract: 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: ApplicationFiled: December 13, 2012Publication date: November 20, 2014Inventors: Adam Wieslaw Mazur, Jean-Yves Nedelec, Christine Cachet-Vivier, Maniyan Padmanilayam, Armin T. Liebens
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Publication number: 20140323440Abstract: 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: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Eric Thomas Miller, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Publication number: 20140309422Abstract: 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: ApplicationFiled: July 3, 2012Publication date: October 16, 2014Applicant: ZHEJIANG UNIVERSITYInventors: Shengming Ma, Bo Lv, Chunling Fu
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Publication number: 20140274961Abstract: 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: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Global Blood Therapeutics, Inc.Inventors: Brian W. Metcalf, Jason R. Harris, Zhe Li, Stephen L. Gwaltney, II
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Publication number: 20140256945Abstract: 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: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
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Patent number: 8828973Abstract: 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: GrantFiled: March 18, 2014Date of Patent: September 9, 2014Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, John R. Cappiello
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Publication number: 20140243291Abstract: 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: ApplicationFiled: July 27, 2012Publication date: August 28, 2014Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle
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Patent number: 8816082Abstract: 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: GrantFiled: May 27, 2011Date of Patent: August 26, 2014Assignee: The Royal Institution for the Advancement of Learning/McGill UniversityInventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
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Publication number: 20140235584Abstract: 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: ApplicationFiled: September 28, 2012Publication date: August 21, 2014Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Aichen Wang
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Publication number: 20140228323Abstract: 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: ApplicationFiled: February 12, 2014Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
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Publication number: 20140228553Abstract: 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: ApplicationFiled: October 11, 2012Publication date: August 14, 2014Inventors: Raymond Ziessel, Mathieu Starck, Alexandra Sutter
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Publication number: 20140221637Abstract: 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: ApplicationFiled: November 30, 2011Publication date: August 7, 2014Inventor: Yoshihito Ueno
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Publication number: 20140199600Abstract: 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: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Applicant: FUJIFILM CORPORATIONInventors: Toshihiko YAWATA, Ikuo KINOSHITA
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Patent number: 8779135Abstract: 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: GrantFiled: October 4, 2010Date of Patent: July 15, 2014Assignee: Straitmark Holding AGInventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
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Publication number: 20140194389Abstract: 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: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: WARNER CHILCOTT COMPANY, LLCInventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
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Publication number: 20140187780Abstract: 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: ApplicationFiled: December 24, 2013Publication date: July 3, 2014Applicant: 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
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Patent number: 8765722Abstract: 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: GrantFiled: June 26, 2013Date of Patent: July 1, 2014Assignee: 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
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Publication number: 20140171644Abstract: 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: ApplicationFiled: February 20, 2014Publication date: June 19, 2014Applicant: CENTRAL CHINA NORMAL UNIVERSITYInventors: Hongwu He, Wei Wang, Na Zuo, Xijun Sheng, Hao Peng, Xiaosong Tan
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Publication number: 20140161839Abstract: 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 substiType: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: PHARMALEADSInventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
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Patent number: 8741875Abstract: 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: GrantFiled: February 11, 2013Date of Patent: June 3, 2014Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, John Cappiello
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Publication number: 20140135290Abstract: 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: ApplicationFiled: November 4, 2013Publication date: May 15, 2014Applicants: ONCOSYNERGY, INC., LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: James HECK, Nicolas Winssinger, John C. Chabala, Sofia Barluenga, Ruihong Chen, Allan Rubenstein, Jin-Chen Yu
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Patent number: 8716265Abstract: 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: GrantFiled: November 18, 2011Date of Patent: May 6, 2014Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat, David Nugiel