Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
Abstract: The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
Type:
Application
Filed:
May 26, 2006
Publication date:
April 1, 2010
Applicant:
METABASIS THERAPEUTICS, INC.
Inventors:
Mark D. Erion, Hongjian Jiang, Serge H. Boyer
Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
Abstract: Disclosed herein are novel electrochromic materials. The electrochromic materials are viologens into which an imidazole derivative is asymmetrically introduced. The electrochromic materials can be used in a variety of electrochromic displays, including electrochromic windows and smart windows. Also disclosed herein are electrochromic devices that use the electrochromic materials.
Type:
Application
Filed:
January 27, 2009
Publication date:
March 4, 2010
Applicant:
SAMSUNG ELECTRONICS CO., LTD.
Inventors:
Rupasree RaginiDAS, Chang-Ho NOH, Jin-Min LEE
Abstract: Disclosed are new compositions consisting of polyphosphonates and specific additive compositions that exhibit superior resistance to degradation due to exposure to air, high temperature and air, moisture or combinations thereof. Also disclosed are polymer mixtures or blends comprising these polyphosphonates/additive compositions and commodity and engineering plastics and articles produced therefrom. Further disclosed are articles of manufacture produced from these materials, such as fibers, films, coated substrates, moldings, foams, fiber-reinforced articles, or any combination thereof.
Abstract: The present invention has for an object a cationic lipophilic compound of the following general formula (I): wherein: a) R1 and R?1 each represent, independently from one another, an alkyl chain, an alkenyl chain or a polyalkenyl chain with from 10 to 24 carbon atoms, with the polyalkenyl chain having from 2 to 4 double links; b) R2 is a hydrogen atom or an alkyl chain having from 1 to 4 carbon atoms; and R3 is a group with the following formula (IIa) —(CH2)n— or following formula (IIb) —C(?NH)—NH—(CH2)n— wherein: n is an integer equal to 0, 1, 2, 3 or 4; and d) A+ is an organic cation; e) X? is an anion.
Type:
Grant
Filed:
November 7, 2003
Date of Patent:
February 23, 2010
Assignees:
Centre National de la Recherche Scientifique (CNRS), Institut National de la Sante de de la Recherche Medicale (INSERM), Universite de Bretagne Occidentale, Centre Hospitalier Universitaire de Brest
Inventors:
Hervé Des Abbayes, Jean-Jacques Yaouanc, Jean-Claude Clement, Karine Le Ny, Claude Ferec, Tristan Montier, Pascal Delepine
Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.
Abstract: 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N,N?,N?-tetrakis(2-chloroethyl)-phosphorodiamidates, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
Type:
Grant
Filed:
November 29, 2006
Date of Patent:
February 2, 2010
Assignee:
Telik, Inc.
Inventors:
Wenli Ma, Kevin T. Weber, Robert M. Yee
Abstract: A novel process for preparing risedronate sodium hemipentahydrate represented by the following formula 1 using 2-(3-pyridyl)-1-hydroxyethane-1,1-bisphosphonic acid (risedronic acid) and an aqueous solution of risedronate sodium is disclosed.
Abstract: A process for the preparation of biphosphonic acids and pharmaceutical acceptable salts thereof, comprises reacting a carboxylic acid with phosphorous trichloride and phosphorous acid in the presence of an aprotic polar solvent.
Abstract: Disclosed herein is a process for producing bisphosphonic acids and salts thereof. The process comprising reacting a carboxylic acid of Formula [I] with phosphorous acid and halophosphorus compound in the presence of a solvent selected from aliphatic hydrocarbon or water miscible cyclic ether. Further, the present invention also provides novel forms of bisphosphonic acids and process for preparation thereof.
Abstract: The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.
Abstract: The monosodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid in new amorphous forms, methods of preparation and a pharmaceutical formulation.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
November 17, 2009
Assignee:
Zentiva, a.s.
Inventors:
Jindrich Richter, Josef Jirman, Hana Petrickova
Abstract: The invention relates to a novel process for the preparation of [1-hydroxy-2-(3-pyridinyl)ethylidene] bisphosphonic acid and hemipentahydrate monosodium salt thereof comprising (a) reacting an aqueous solution of 3-pyridyl acetic acid hydrochloride with phosphorus trichloride; (b) removing unreacted phosphorus trichloride; (c) adding water and hydrolyzing; (d) isolating crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene] bisphosphonic acid; (e) suspending said crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene] bisphosphonic acid in water; (f) adding sodium hydroxide, filtering off, and washing; and (g) drying obtained hemipentahydrate monosodium salt of 1-hydroxy-2-(3-pyridinyl)ethylidene] bisphosphonic acid.
Type:
Application
Filed:
December 28, 2005
Publication date:
November 12, 2009
Applicants:
ZAKLADY FARMACEUTYCZNE POLPHARMA SA, POLITECHNIKA GDANSKA
Inventors:
Leszek Dembkowski, Robert Rynkiewicz, Janusz Rachon, Slawomir Makowiec, Witold Przychodzen, Dariusz Witt
Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
Type:
Application
Filed:
July 17, 2009
Publication date:
November 12, 2009
Inventors:
George Wu, Anantha R. Sudhakar, Tao Wang, Ji Xie, Frank Xing Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia A. Zavialov, Hoa N. Nguyen, Ngiap Kie Lim
Abstract: Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3?-pyridyl or 2?-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.
Type:
Grant
Filed:
January 27, 2004
Date of Patent:
November 3, 2009
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Jozsef Neu, Janos Fischer, Tamas Fodor, Jozsef Törley, Tibor Gizur, Sandor Levai, Adam Demeter, Eva Perenyi
Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
Type:
Application
Filed:
July 16, 2007
Publication date:
October 29, 2009
Inventors:
Joshua Close, Jonathan Grimm, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Paul J. Tempest, Kevin J. Wilson, David J. Witter
Abstract: Tertiary phosphines are prepared by reacting a phosphine (PH3 or a primary or secondary phosphine) with a cyclic alpha,beta-unsaturated carbonyl compound having no more than one C?C double bond conjugated with a carbonyl group. The inventive tertiary phosphines can have R groups that are the same or different. The inventive tertiary phosphines may be used as ligands for metal catalysts or as starting materials for preparing phosphonium salts or ylids.
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
October 27, 2009
Assignee:
Cytec Canada Inc.
Inventors:
Christine J. Bradaric-Baus, Yuehui Zhou
Abstract: The invention concerns electrochromic compounds of the general formula I. These compounds may be used in electrochromic devices, especially electrochromic devices comprising nanostructured films.
Type:
Application
Filed:
June 22, 2009
Publication date:
October 15, 2009
Applicant:
NTERA LIMITED
Inventors:
David CORR, S. N. RAO, Niall STOBIE, Mark KINSELLA
Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
Type:
Grant
Filed:
January 31, 2008
Date of Patent:
October 6, 2009
Assignee:
Pfizer, Inc.
Inventors:
Hengmiao (Henry) Cheng, Rajesh Devraj, Gary A DeCresenzo, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Paul V. Rucker, Ronald Keith Webber
Abstract: The present invention provides compounds that have excellent antifungal action, and are also excellent in terms of properties, such as solubility in water and safety. The compounds are represented by formula (I): The present invention is also directed to a pharmaceutical composition comprising the compound, an antifungal agent comprising the compound as an active ingredient, and a method for preventing or treating a fungal disease by administering the compound.
Abstract: The present invention relates to novel nitrogen-containing monodentate phosphane ligands of formula (I) and to their use in catalytic reactions, especially in the improvement of haloaromatic compounds.
Type:
Grant
Filed:
May 3, 2004
Date of Patent:
September 15, 2009
Assignee:
DEGUSSA GmbH
Inventors:
Alexander Zapf, Mark Sundermeier, Ralf Jackstell, Matthias Beller, Thomas Riermeier, Axel Monsees, Uwe Dingerdissen
Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.
Type:
Application
Filed:
December 4, 2008
Publication date:
September 10, 2009
Inventors:
Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne F. Patton
Abstract: Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phosphorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, an inert support or ortho-phosphoric acid codiluent is advantageously included.
Type:
Application
Filed:
February 10, 2009
Publication date:
August 20, 2009
Inventors:
Rami Lidor-Hadas, Zvi Harel, Revital Lifshitz-Liron, Eti Kovalevski-Ishai
Abstract: A phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified phosphocalcic compound is obtained by adding a gem-bisphosphonic acid or one of its alkali metal or alkaline earth salts to a suspension of a precursor phosphocalcic compound in ultras-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. The compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.
Type:
Application
Filed:
April 14, 2009
Publication date:
August 13, 2009
Applicants:
Centre National de la Recherche Scientifique, Universite de Nantes, Institut National de la Sante et de la Recherche Medicale
Inventors:
Bruno Bujoli, Solen Josse, Jerome Guicheux, Pascal Janvier, Jean-Michel Bouler, Guy Daculsi
Abstract: The present invention relates to a process for the preparation of bisphosphonic acids and salts thereof, in particular monosodium salts thereof. The invention also relates to the conversion of the bisphosphonic acids to their sodium salts using an aqueous-organic solvent system. The present invention further relates to the conversion of variable hydrate forms of risedronic acid monosodium salt into a pharmaceutically acceptable hemipentahydrate form by crystallization using an aqueous-organic solvent system.
Type:
Application
Filed:
December 22, 2008
Publication date:
August 6, 2009
Inventors:
Vinayak G. Gore, Vinay Kumar Shukla, Manoj M. Ghadge, Rekha M. Avadhut
Abstract: The present invention relates to an industrially advantageous process of making bisphosphonic acid or its salt in particular risedronic acid, [1-hydroxy-2(3-pyridinyl)ethylidene]bisphosphonic acid, having formula-(I) or its salts in high purity and high yields.
Abstract: The present invention is related to compounds comprising mannitol or glucitol derivatives which may be used to build up oligomeric compounds. The invention is further related to uses of these oligomeric compounds for hybridization and as probes. In addition, methods for the detection of nucleic acids are disclosed wherein the oligomeric compounds are used.
Type:
Grant
Filed:
December 5, 2003
Date of Patent:
July 14, 2009
Assignee:
Roche Molecular Systems, Inc.
Inventors:
Frank Bergmann, Herbert Von Der Eltz, Christoph Seidel, Kurt Weindel
Abstract: 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N-bis(2-chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.
Type:
Application
Filed:
December 12, 2007
Publication date:
June 18, 2009
Inventors:
Edgardo Laborde, Andrew B. Kelson, Wenli Ma, Kevin T. Weber
Abstract: The present invention is concerned with new hydrated forms of risedronate salts, processes of preparing the new hydrated forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same. In particular, the present invention provides tri-sodium risedronate dihydrate.
Type:
Application
Filed:
September 4, 2006
Publication date:
June 11, 2009
Inventors:
Kreso Mihaljevic, Blazenko Bajic, Drazen Cavuzic, Ernest Mestrovic, Miroslav Zegarac, Nada Kosutic Hulita
Abstract: The present invention provides an optical recording composition comprising a compound denoted by general formula (I) and a holographic recording medium comprising a recording layer, wherein the recording layer comprises a compound denoted by general formula (I). In general formula (I), each of R1, R2, and R3 independently denotes an alkyl group, aryl group, or heterocyclic group, X denotes an oxygen atom or sulfur atom, and n denotes 0 or 1.
Abstract: Methods and compounds are provided for the formation of carbon-nitrogen or carbon-carbon bonds comprising reacting an amine or an aryl boronic acid with an aryl halide in the presence of a palladium catalyst, a base, and a compound of formula II:
Type:
Grant
Filed:
January 24, 2008
Date of Patent:
June 2, 2009
Assignee:
Iowa State University Research Foundation, Inc.
Inventors:
John G. Verkade, Sameer Urgaonkar, JuHua Xu
Abstract: Pyridinium cationic lipids useful as non-viral gene delivery agents are disclosed. The agents are prepared by reaction of pyrylium salts with primary amines. Also disclosed are methods of trasfectind cells using the pyridinium cationic lipids as gene transfer agents.
Type:
Application
Filed:
November 24, 2008
Publication date:
May 28, 2009
Inventors:
Alexandru T. Balaban, William A. Seitz, Marc A. C. Ilies, Edward Bradbridge Thompson, Robert E. Garfield, Betty H. Johnson, Aaron L. Miller, Melissa J. Wentz
Abstract: Disclosed are viologen derivatives as an electrochromic material having improved stability and lifetime, a metal oxide electrode including the same, and an electrochromic device using the viologen derivative as an electrochromic material. The viologen derivative includes a suitable regulator group capable of increasing ?E that is a potential difference between E1 (potential at the first redox reaction) and E2 (potential at the second redox reaction). When ?E increases, the mole fraction of viologen molecules present in the second reduction state decreases. Therefore, it is possible to lower the mole fraction of viologen molecules present in an irreversibly reduced state at an applied potential, thereby increasing the lifetime of an electrochromic material and an electrochromic device.
Type:
Application
Filed:
August 4, 2008
Publication date:
May 28, 2009
Inventors:
Won Jong Kwon, Ki Seok Jang, Sang Ho Kim, Shin Jung Choi, Jin Young Park, Young Hee Lim
Abstract: A manufacturing process for the preparation of bisphosphonic acids and in particular zoledronic acid is provided wherein diglyme, monoglyme, or a mixture thereof, is utilized to produce a homogenous, water soluble, solid reaction mass that upon cooling, dissolving in water and stripping results in a high purity product and comparatively good yield.
Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Type:
Application
Filed:
October 24, 2008
Publication date:
May 28, 2009
Inventors:
Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Type:
Application
Filed:
October 24, 2008
Publication date:
May 21, 2009
Inventors:
Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
Abstract: The present invention concerns a process for hydrocyanating ethylenically unsaturated organic compounds to compounds containing at least one nitrile function. It relates more particularly to the hydrocyanation of diolefins such as butadiene or of substituted olefins such as alkenenitriles, for instance pentenenitriles. According to the process of the invention the reaction is implemented in the presence of a metal complex catalyst comprising a transition metal such as nickel and an organic ligand.
Type:
Grant
Filed:
July 11, 2003
Date of Patent:
May 12, 2009
Assignee:
Rhodia Polyamide Intermediates
Inventors:
Jean-Christophe Galland, Blaise Didillon, Philippe Marion, Damien Bourgeois
Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.
Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Type:
Application
Filed:
October 24, 2008
Publication date:
May 7, 2009
Inventors:
Michael N. Greco, Harold R. Almond, JR., Lawrence Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donaid Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leoperd Sorgi, Eugene Powell
Abstract: The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.
Type:
Application
Filed:
November 19, 2004
Publication date:
May 7, 2009
Inventors:
Mark D. Erion, Hongjian Jiang, Serge H. Boyer
Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Type:
Application
Filed:
October 24, 2008
Publication date:
May 7, 2009
Inventors:
Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
Abstract: The invention concerns a phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified phosphocalcic compound is obtained by adding a gem-bisphosphonic acid or one of its alkali metal or alkaline earth salts to a suspension of a precursor phosphocalcic compound in ultra-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. Said compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.
Type:
Grant
Filed:
February 18, 2003
Date of Patent:
April 21, 2009
Assignees:
Centre National de la Recherche Scientifique, Universite de Nantes, Institut National de la Sante et de la Recherche Medicale
Inventors:
Bruno Bujoli, Solen Josse, Jérôme Guicheux, Pascal Janvier, Jean-Michel Bouler, Guy Daculsi
Abstract: The present application describes deuterium-enriched risedronate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
Abstract: This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
Type:
Grant
Filed:
August 31, 2004
Date of Patent:
February 24, 2009
Assignee:
Merck & Co. Inc.
Inventors:
Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.