Abstract: The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer.
Type:
Grant
Filed:
June 30, 2008
Date of Patent:
November 15, 2011
Assignee:
Florida Atlantic University Broad of Trustees
Inventors:
Amy E. Wright, Susan H. Sennett, Shirley A. Pomponi, Peter J. McCarthy, Esther A. Guzman
Abstract: The present invention relates to novel Tenofovir disoproxil hemifumarate salt, which is prepared by dealkylation of Phosphonate esters by using mineral acids followed by esterification and crystallization to give crystalline Tenofovir disoproxil. The Tenofovir disoproxil is further converted to fumarate salts with improved yield.
Abstract: Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described.
Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.
Type:
Grant
Filed:
December 21, 2007
Date of Patent:
October 25, 2011
Assignee:
UCB Pharma GmbH
Inventors:
Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
Abstract: A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.
Abstract: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N?CH—NR17—??(c-1); or —NR17—CH?N—??(c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
September 27, 2011
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Paulus Joannes Lewi, Marc René de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Jan Heeres, Hendrik Maarten Vinkers, Ruben Gerardus George Leenders, Dirk Alfons Leo Vandenput
Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
Abstract: The present invention relates to a cost effective and industrially advantageous process for the preparation of (3R,4S)-1-(4-fluorophenyl)-3-[3(S)-3-(4-fluorophenyl)-3-hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone, referred to here as Ezetimibe and represented by structural formula (I). The process comprises an multi-step reaction sequence that includes a chiral auxiliary-controlled condensation, a silyl-mediated cyclization, a palladium-catalyzed Negishi cross-coupling, and the enantioselective reduction of a ketone to a hydroxyl group.
Abstract: The present invention provides an improved process for the preparation of Cefixime of formula (I), a cephalosporine antibiotic with an improved quality in regard to color and solubility. This process includes: (i) reaction of 7-?-(4-chloro-2-alkoxycarbonyl methoxyimino-3-oxobutyromido)-3-cephem-4-carboxylic acid (V) with thiourea at pH 5.0 to 6.0 at temperature 25-40° C. in water, (ii) carbon treatment to the reaction mixture in presence of sodium dithionite or ethylenediaminetetraacetic acid (EDTA) followed by filtration, (iii) acidification of the filtrate obtained in step (ii) to pH 2.0 to 3.0 with acid at 50-80° C. to give cefixime ester (IV) (iv) alkaline hydrolysis of cefixime ester of formula (IV) in water followed by acidification to pH 5.0 to 6.0, (v) precipitation of cefixime (I) by adding ketone solvent followed by acidification to pH 2.0 to 3 and (vi) isolation of solid.
Abstract: Provided are certain crystalline hydrates of the formula I in which n has a value of from 0.5 to 1.8. The compound may be suitable, for example, as a hypolipidemic.
Type:
Grant
Filed:
November 12, 2008
Date of Patent:
August 23, 2011
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Theodor Andreas Wollmann, Regina Duffy, Frank Cullmann
Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.
Type:
Grant
Filed:
February 2, 2007
Date of Patent:
August 2, 2011
Assignee:
Pharmacopeia, LLC
Inventors:
Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
Abstract: A method for preparing compounds having the formula(I) by using P(3HB), wherein R is R1, R2, R3 are lower linear or branched C1-C4 alkyl, comprising the steps of: a: obtaining (3R)-3-RO—CH(CH3)CH2COOCH3 by pyrolysis of P(3HB) and protection; b: obtaining (3R)-3-RO—CH(CH3)CH2CHO by reduction of (3R)-3-RO—CH(CH3)CH2COOCH3 ; c: enolizing (3R)-3-RO—CH(CH3)CH2CHO and then reacting with chlorosulfonyl isocyanate, at last getting the final product by reduction; wherein (3R)-3-RO—CH(CH3)CH2CHO is enolized by reacting (3R)-3-RO—CH(CH3)CH2CHO with isopropenyl acetate and p-toluenesulfonic acid by heating under reflux.
Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the following general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for application to mammalian cells, and especially human skin cells, in order to improve the cosmetic appearance of the mammalian cells, especially human skin.
Type:
Grant
Filed:
December 28, 2007
Date of Patent:
June 14, 2011
Assignee:
Institute of Experimental Botany, Academy of Sciences of the Czech Republic
Inventors:
Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
Abstract: This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity in a large scale production.
Abstract: A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.
Type:
Grant
Filed:
March 17, 2006
Date of Patent:
January 6, 2009
Assignee:
Teijin Pharma Limited
Inventors:
Gen Unoki, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi
Abstract: Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstituted or substituted aromatic ring, or alkoxycarbonyl substituent at the end position, or aryloxyalkoxyalkyl group have been found to possess antimalarial activity against Plasmodium falciparum lines, including those resistant against pyrimethamine and other antifolates. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
Type:
Grant
Filed:
March 13, 2003
Date of Patent:
May 13, 2008
Assignee:
National Science & Technology Development Agency
Abstract: A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as kinase modulators.
Type:
Grant
Filed:
November 4, 2003
Date of Patent:
April 22, 2008
Assignee:
Les Laboratoires Servier
Inventors:
Sylvain Rault, Jean-Charles Lancelot, Marina Kopp, Daniel-Henri Caignard, Bruno Pfeiffer, Pierre Renard
Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein
Type:
Grant
Filed:
March 22, 2005
Date of Patent:
October 30, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
James Patrick Dunn, Todd Richard Elworthy, Joan Heather Hogg, Dimitrios Stefanidis
Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubility or pharmaceutical properties of 1,2,3-triazole containing compounds. More particularly, the present disclosure relates to compounds containing N-aminium-1,2,3-triazoles that are useful as antiviral agents and specifically for the treatment of HIV and AIDS.
Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein