Oxy In Acid Moiety Patents (Class 560/42)
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Patent number: 7935843Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: GrantFiled: December 8, 2006Date of Patent: May 3, 2011Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110014479Abstract: Substrates, particularly low surface energy substrates, can be bonded using certain solvent-free liquid polyurethane adhesives. The adhesive cures through reaction with moisture and/or an active hydrogen-containing curing agent to form a tough, strong, thermoset polymer having excellent chemical and heat resistance. The adhesive is based on a polyurethane prepolymer obtained by reacting a stoichiometric excess of at least one polyfunctional isocyanate having a functionality of less than 2.2 with at least one polyether polyol and at least one polyester polyol containing isophthalic acid moieties but relatively few if any phthalic acid or terephthalic acid moieties.Type: ApplicationFiled: July 22, 2010Publication date: January 20, 2011Applicant: Henkel CorporationInventors: Zhengzhe Song, Yingjie Li
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Publication number: 20100331345Abstract: The present invention relates to compounds represented by formula (I), or isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof: in which each substituent of formula (I) is as defined in the specification. The present invention also relates to preparation methods of compounds represented by formula (I), a pharmaceutical composition comprising compounds represented by formula (I) and usage of compounds represented by formula (I) for treating chronic neurodegenerative diseases such as Alzheimer's disease and other diseases induced by aggregation or deposition of ?-amyloid peptide.Type: ApplicationFiled: February 5, 2007Publication date: December 30, 2010Inventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
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Publication number: 20100298330Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: PHARMAXIS LTD.Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
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Publication number: 20100298402Abstract: Described are novel compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These novel compounds can inhibit pSTAT3/IL-6 and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.Type: ApplicationFiled: November 4, 2008Publication date: November 25, 2010Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Sridharan Rajagopal, Thangapazham Selvakumar, Kuppusamy Bharathimohan, Virendra Kachhadia, Sriram Rajagopal, Rajendran Praveen, Ramachandran Balaji
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Patent number: 7829592Abstract: Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.Type: GrantFiled: December 20, 2007Date of Patent: November 9, 2010Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Patent number: 7799941Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) wherein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, characterized by comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid.Type: GrantFiled: July 9, 2004Date of Patent: September 21, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
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Patent number: 7781609Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) therein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid by using as a catalyst a rhodium complex containing as a ligand an optically active compound of formula (4), (4?) or (5) characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.Type: GrantFiled: January 12, 2006Date of Patent: August 24, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
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Patent number: 7763654Abstract: The present invention provides a novel crystal polymorph of ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.Type: GrantFiled: April 24, 2006Date of Patent: July 27, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kiyoshi Kasai, Michio Toda
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Publication number: 20100144881Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.Type: ApplicationFiled: December 9, 2009Publication date: June 10, 2010Inventors: Sean M. Dalziel, Miroslav Rapta
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Publication number: 20100130545Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Publication number: 20100113778Abstract: An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.Type: ApplicationFiled: April 10, 2008Publication date: May 6, 2010Inventors: John-Matthias Wiegand, Karsten Luettgen, Wolfgang Skranc
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Publication number: 20100113820Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 7, 2010Publication date: May 6, 2010Inventors: Takayuki KAWAGUCHI, Sumihiro NOMURA, Mikiko TSUKIMOTO, Toshiyuki KUME, Ila SIRCAR
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Publication number: 20100075977Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.Type: ApplicationFiled: August 3, 2007Publication date: March 25, 2010Inventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
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Patent number: 7671059Abstract: Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.Type: GrantFiled: September 28, 2006Date of Patent: March 2, 2010Assignee: Novartis AGInventors: Timothy D. Machajewski, Cynthia M. Shafer, Christopher McBride, William Antonios-McCrea, Brandon M. Doughan, Barry H. Levine, Yi Xia, Maureen McKenna, X. Michael Wang, Kris Mendenhall, Yasheen Zhou, Kristin Brinner, Zhenhai Gao, Daniel Poon, Paul Barsanti, Xiaodong Lin, Abran Costales, Alice Rico, Nathan Brammeier, Teresa Pick, Paul A. Renhowe
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Publication number: 20100041904Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: April 20, 2009Publication date: February 18, 2010Inventors: Xin Jiang, Xiaofeng Liu, Jack Greiner, Stephen S. Szucs, Melean Visnick
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Publication number: 20100016379Abstract: Described herein are compounds having a terephthalamate structural feature. Also described herein, are methods of making such compounds, methods of using such compounds to modulate the activity of HIV integase, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology of AIDS or infection with HIV.Type: ApplicationFiled: April 18, 2007Publication date: January 21, 2010Applicant: IRM LLCInventors: Yun He, Zhiwei Wang, Baogen Wu
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Publication number: 20100004326Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: ApplicationFiled: June 19, 2009Publication date: January 7, 2010Inventor: Karen A. VEVERKA
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Patent number: 7598412Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: GrantFiled: October 8, 2004Date of Patent: October 6, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Ashvani K. Singh, Mark T. Miller, Matthew Hamilton, Peter D. J. Grootenhuis
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Publication number: 20090247781Abstract: The present invention relates to an improved process for the preparation of substituted 2-(4-carbonylmethoxy-optionally 2,5-disubstituted-phenyl-acetaldehydes, in particular 2-(4-alkoxycarbonylmethoxy-optionally 2,5-disubstituted-phenyl)-acetaldehydes and their use in the synthesis of optionally substituted 2-[4-[2-[[-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-amino]ethyl]-optionally 2,5-disubstituted-phenoxy]acetic acid derivatives or the salts thereof, which may be used as pharmaceutically active substances.Type: ApplicationFiled: October 20, 2005Publication date: October 1, 2009Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Eric Winter, Carsten Reichel, Dieter Gutheil
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Patent number: 7560586Abstract: Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.Type: GrantFiled: March 26, 2003Date of Patent: July 14, 2009Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, Lara S. Kallander, Chun Ma, Joseph Marino, Dennis Lee
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Publication number: 20090149535Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 10, 2008Publication date: June 11, 2009Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
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Patent number: 7531569Abstract: A method and apparatus for preventing board warpage during the application and curing or drying of liquid epoxies, or the like, on printed circuit boards using a clamping fixture assembly, which includes at least one clamping fixture support and at least one clamping fixture overlay. If desired, a plurality of printed circuit boards may be processed using an appropriate clamping fixture assembly. Furthermore, the clamping fixture may be constructed so a slight bow or curvature thereof can counter either a convex or concave bow or curvature of the printed circuit board. In the method, at least one printed circuit board is mounted to a clamping fixture support whereby a clamping fixture overlay is placed on top of the first printed circuit board.Type: GrantFiled: December 1, 2004Date of Patent: May 12, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Gerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
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Publication number: 20090098180Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: October 10, 2006Publication date: April 16, 2009Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20090099366Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: September 11, 2008Publication date: April 16, 2009Applicant: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Publication number: 20090069421Abstract: The present invention provides a novel crystal polymorph of ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.Type: ApplicationFiled: April 24, 2006Publication date: March 12, 2009Applicant: Kissei Pharmaceutical Co., Ltd,Inventors: Kiyoshi Kasai, Michio Toda
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Publication number: 20090054543Abstract: A monomer is provided which is excellent in reactivity, can give high heat resistance and high refractive index, and has two or more polymerizable functional groups with different polymerization properties and an aromatic ring in the molecule. An industrial advantageous process for producing the monomer is also provided. The monomer is an aromatic isocyanate compound containing a (meth)acryloyl group, and is represented by Formula (I): wherein R1 is a single bond or a linear or branched alkylene group of 1 to 5 carbon atoms, R2 is a hydrogen atom or a methyl group, R3 is a single bond or a linear or branched alkylene group of 1 to 3 carbon atoms, X is independently a halogen atom or an electron-withdrawing group, m is an integer ranging from 0 to 4, n is an integer ranging from 1 to 3, and 1?m+n?5.Type: ApplicationFiled: March 15, 2006Publication date: February 26, 2009Applicant: SHOWA DENKO K.K.Inventors: Kaneo Nozawa, Katsutoshi Ohno, Yotaro Hattori
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Patent number: 7488844Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.Type: GrantFiled: December 30, 2004Date of Patent: February 10, 2009Assignee: AstraZeneca ABInventors: Eva-Lotte Lindstedt Alstermark, Anna Christina Olsson, Lanna Li
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Publication number: 20090036525Abstract: Compounds of formula (I) have activity in alleviating the effects of impaired dopaminergic signaling, for example in the treatment of Parkinsons Disease: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 and R3 are independently hydrogen, or a group —C(?O)R6 or —C(?O)OR6 wherein R6 is C1-C6 alkyl, or a group —CH2Q wherein Q is an optionally substituted monocyclic cycloalkyl or heterocyclyl ring of 3 to 6 ring atoms; R7 is (i) optionally substituted phenyl or monocyclic heteroaryl, or (ii) a radical of formula —CHR4R5; R4 is (a) optionally substituted C1-C4 alkyl, C1-C4 alkoxy, C2-C4 alkenyl, C2-C4 alkenyloxy, or C2-C4 alkynyl, or (b) —CH2XCH3, —CH2CH2XCH3, or —CH2XCH2CH3, wherein X is —O—, S, or —NR7 wherein R7 is hydrogen, methyl or ethyl; or —CH2Q or CH2OQ wherein Q is as defined in relation to R6; and R5 is hydrogen, methyl, ethyl, or methyl substituted by 1, 2 or 3 fluoro atoms; or R4 and R5 taken together with the carbon atom to which they are attached form an optionally substitutedType: ApplicationFiled: January 23, 2007Publication date: February 5, 2009Applicant: POXIMAGEN LTD.Inventor: Christopher Hobbs
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Publication number: 20090036526Abstract: The present invention provides ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride ¼ hydrate or a crystal thereof which can be determined by characteristic diffraction peaks of the powder X-ray diffraction, thermogravimetry-differential thermal analysis or the like, and obtained by manufacturing ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.Type: ApplicationFiled: April 24, 2006Publication date: February 5, 2009Inventors: Hidetoshi Isawa, Michio Toda
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Publication number: 20080306150Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I), wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; t is 0 or 1; R is hydrogen, halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; R is alkyl having from 1 to 3 carbon atoms; R3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R4 and R5 is hydrogen or hydroxy and the other is hydrogen; or R4 and R5 together are ?O; R6 is hydrogen or alkyl having one, two, three, four or five carbon atoms; or a pharmaceutically acceptable salt of the compound. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).Type: ApplicationFiled: January 22, 2007Publication date: December 11, 2008Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20080217580Abstract: The present invention relates to compounds of formula (I) a process for their production and to their use for coloring high molecular weight organic materials, as fluorescent tracers, in solid dye lasers, EL lasers, in EL devices and lighting. The compounds of formula I show unique broadband luminescence in visible region.Type: ApplicationFiled: April 11, 2005Publication date: September 11, 2008Inventors: Junichi Tanabe, Hiroshi Yamamoto, Norihisa Dan
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Patent number: 7402692Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus.Type: GrantFiled: October 24, 2007Date of Patent: July 22, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuyuki Tanaka, Tetsuro Tamai, Harunobu Mukaiyama, Takehiro Ishikawa, Junichi Kobayashi, Satoshi Akahane, Hiromu Harada
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Publication number: 20080161592Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.Type: ApplicationFiled: March 6, 2008Publication date: July 3, 2008Applicant: CEPTYR, INC.Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Marie Schultz, Feng Hong, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffrey Howbert
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Publication number: 20080064748Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.Type: ApplicationFiled: May 5, 2005Publication date: March 13, 2008Inventors: Derk J. Hogenkamp, Timothy B.C. Johnstone, Kelvin W. Gee
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Patent number: 7323585Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: GrantFiled: June 3, 2005Date of Patent: January 29, 2008Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy
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Publication number: 20080020981Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, X1 and X2 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: July 20, 2007Publication date: January 24, 2008Inventor: Zachary Kevin Sweeney
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Patent number: 7208520Abstract: The present invention provides ethyl (?)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent ?3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.Type: GrantFiled: August 27, 2002Date of Patent: April 24, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hidetoshi Isawa, Yukihiko Hotei, Kiyoshi Kasai, Junichi Sonehara, Satoshi Akahane, Hiromu Harada
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7138538Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.Type: GrantFiled: May 7, 2004Date of Patent: November 21, 2006Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
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Patent number: 7015346Abstract: The invention provides a process for preparing a compound useful for inducing or maintaining general anesthesia or sedation in mammals.Type: GrantFiled: November 3, 2004Date of Patent: March 21, 2006Assignee: Theravance, Inc.Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
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Patent number: 6919343Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: January 30, 2003Date of Patent: July 19, 2005Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
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Patent number: 6916956Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.Type: GrantFiled: August 10, 2001Date of Patent: July 12, 2005Assignee: Japan Tobacco, Inc.Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
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Esters derived from (RR,SS)-2-hydroxybenzoate of 3-(2-dimethylaminomethyl-1-hydroxycyclohexyl)phenyl
Patent number: 6894076Abstract: New esters derived from (RR, SS)-3-(2-dimethylaminomethyl-1-hydroxycyclohexyl)phenyl 2-hydroxybenzoate, analog to Tramadol, a process for obtaining them and the use of these compounds for the production of a medicament with analgesic properties. These new products of general formula (I) exhibit an analgesic activity higher than that of tramadol.Type: GrantFiled: December 26, 2000Date of Patent: May 17, 2005Assignee: Vita-Invest, S.A.Inventors: Marisabel Mourelle Mancini, Elisabet De Ramon Amat, Juan Huguet Clotet -
Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6870065Abstract: A reagent having the general formula of General Formula I: wherein group R is an electrophilic or a nucleophilic moiety suitable for reaction of the reagent with a biologically active species; group R2 is one of H and OH moieties; group R3 is one of an alkyl and a methylene bearing an electronegative substituent; group Z is one of (CH2)n and CH2O(CH2CH2O)n2, and n is an integer of from 1 to 5, and n2 is an integer of from 1 to 4; and each of group Z2 and Z3 are (CH2)CONH(CH2)3CONH(CH2)2. Also, a reagent having the general formula of General Formula II: group R2 is one of H and OH moieties; group Z is one of (CH2)n and CH2O(CH2CH2O)n2, and n is an integer of from 1 to 5, and n2 is an integer of from 1 to 4; each of group Z2 and group Z3 include one of (CH2)CONH(CH2)3CONH(CH2)2; and (CH2)CONH(CH2); and group R is an electrophilic or a nucleophilic moiety suitable for reaction of the reagent with the biologically active species.Type: GrantFiled: June 28, 2002Date of Patent: March 22, 2005Assignee: Cambrex Bio Science Rockland, Inc.Inventors: Clarence N. Ahlem, Robert J. Kaiser, Kevin P. Lund, Mark L. Stolowitz
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Patent number: 6861561Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: GrantFiled: September 26, 2002Date of Patent: March 1, 2005Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel