Nitrogen In Aglycone Moiety Patents (Class 536/17.4)
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Publication number: 20100145036Abstract: The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.Type: ApplicationFiled: December 28, 2007Publication date: June 10, 2010Applicant: Medarex, Inc.Inventors: Bilal Sufi, Vincent Guerlavais, Liang Chen, Sanjeev Gangwar, Qian Zhang, David B. Passmore
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Publication number: 20100144655Abstract: This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.Type: ApplicationFiled: August 6, 2009Publication date: June 10, 2010Applicant: NOVARTIS AGInventors: Yen Liang CHEN, Jeyaraj DURAISWAMY, Sarah HALLER, Matthias KEIM, Ravinder Reddy KONDREDDI, Zheng YIN
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Patent number: 7718782Abstract: A sophorolid produced by a method involving reacting a compound of formula I with a compound of formula II wherein R1 and R2 are H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, phenyl, or C1 through C18 acyl or alkoxycarbonyl, R1 and R2 are not both acyl, R3 is H, CH3, CH2-phenyl, CH2—C6H4—OH, CH2CO2H, CH2CH2CO2H, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2OH, CH(CH3)OH, CH2CH2CH2CH2NH2, CH2CH2CONH2, CH2CONH2, CH2—C3N2H3(histidine), CH2CH2CH2NHC(NH)NH2, CH2CH2SCH3, R2 and R3 may be joined in a ring, R4 is H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, or phenyl, n is 0-6, R5 and R6 are H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, or phenyl, and X is C1-C18 alkyl or C1-C18 alkenyl; optionally followed by acidolytic (treating with an acid) or hydrogenolytic deprotection (treating with a hydrogenolysis catalyst) which removes one of the groups R1 or R2 and replaces it with hydrogen.Type: GrantFiled: July 11, 2006Date of Patent: May 18, 2010Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Jonathan Zerkowski, Daniel Solaiman, Richard D. Ashby, Thomas A. Foglia
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Publication number: 20100121028Abstract: The invention relates to Fmoc (9-fluorenyl-methoxycarbonyl)-based polymeric conjugates. These conjugates are useful for extending the in-vivo circulation of protein and peptide drugs.Type: ApplicationFiled: January 18, 2010Publication date: May 13, 2010Applicants: BAXTER INTERNATIONAL INC., BAXTER HEALTHCARE S.A.Inventors: Peter Turecek, Juergen Siekmann
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Publication number: 20100113542Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: December 11, 2007Publication date: May 6, 2010Applicant: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Publication number: 20100113371Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds of this invention can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases, for example, bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection or psoriasis. The present invention also relates to pharmacological compositions containing these monosaccharide derivatives, as well as methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, and other inflammatory and/or auto immune disorders.Type: ApplicationFiled: December 22, 2005Publication date: May 6, 2010Applicant: RANBAXY LABORATORIES LIMITED INC.Inventors: Viswajanani Jitendra Sattigeri, Sudershan K. Arora, Mohammad Salman, Venkata P. Palle, Muthukaman Nagarajan, Rajkumar Shirumalla, Gurpreet Kaur Aulakh, Abhijit Ray
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Publication number: 20100105149Abstract: The present invention relates to a fluorescent dye-labeled glucose analog, and a synthesis method and usage of the same, and more particularly, to novel glucose ? and ? anomers in which a fluorescent dye is labeled by O-1-glycosylation, an asymmetric synthesis method of the anomers, a molecular bioimaging method of the anomers, and a screening method of curing or preventing drugs for diseases related to glucose metabolism.Type: ApplicationFiled: December 21, 2007Publication date: April 29, 2010Applicant: SNU R&DB FOUNDATIONInventors: Seung Bum Park, Myung Haing Cho, Hyang Yeon Lee, Jong Min Park
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Patent number: 7704988Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.Type: GrantFiled: October 4, 2006Date of Patent: April 27, 2010Assignee: Merck & Co., Inc.Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
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Publication number: 20100075912Abstract: The present invention relates to new morphine-6-glucuronide derivatives, to pharmaceutical compositions thereof and uses thereof.Type: ApplicationFiled: October 11, 2007Publication date: March 25, 2010Inventors: Karine Larbouret, Roger Lahana, Cedric Castex
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Publication number: 20100062971Abstract: Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.Type: ApplicationFiled: September 22, 2009Publication date: March 11, 2010Inventors: Mona Patel, Philip J. Rybczynski, Maud Urbanski, Xiaoyan Zhang
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Publication number: 20100063120Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl.Type: ApplicationFiled: May 31, 2007Publication date: March 11, 2010Inventors: Francois Nique, Catherine Robin-Jagerschmidt, Philippe Clement-Lacroix
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Patent number: 7674773Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.Type: GrantFiled: June 17, 2005Date of Patent: March 9, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Heiner Glombik, Werner Kramer, Stefanie Flohr, Wendelin Frick, Hubert Heuer, Gerhard Jaehne, Andreas Lindenschmidt, Hans-Ludwig Schäfer
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Publication number: 20100029919Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group selected from the following groups: , and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc.Type: ApplicationFiled: August 3, 2009Publication date: February 4, 2010Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Norihiko Kikuchi, Shigeki Tazawa, Tokuhisa Yamato, Masayuki Isaji
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Patent number: 7655633Abstract: The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.Type: GrantFiled: December 19, 2003Date of Patent: February 2, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masayuki Isaji
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Publication number: 20100009900Abstract: Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.Type: ApplicationFiled: September 22, 2009Publication date: January 14, 2010Inventors: Mary Pat Beavers, Mona Patel, Philip Rybczynski, Maud Urbanski, Xiaoyan Zhang
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Publication number: 20100004188Abstract: This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.Type: ApplicationFiled: September 11, 2009Publication date: January 7, 2010Inventor: Maud Urbanski
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Publication number: 20090318373Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Type: ApplicationFiled: June 8, 2009Publication date: December 24, 2009Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
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Publication number: 20090318668Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: February 2, 2007Publication date: December 24, 2009Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus De Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
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Patent number: 7635684Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.Type: GrantFiled: August 21, 2003Date of Patent: December 22, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
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Publication number: 20090306000Abstract: A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.Type: ApplicationFiled: June 26, 2009Publication date: December 10, 2009Applicant: WyethInventors: Li Shen, Kelly Keating, Oliver McConnell, William DeMaio, Appavu Chandrasekaran
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Patent number: 7622449Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.Type: GrantFiled: June 15, 2005Date of Patent: November 24, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Feroze Ujjainwalla, Anthony Ogawa, Derek Von Langen
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Publication number: 20090275524Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agentsType: ApplicationFiled: May 7, 2009Publication date: November 5, 2009Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
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Publication number: 20090270590Abstract: A surface-modified inorganic material and a preparation method thereof. A surface-modified inorganic material is provided which is obtained by allowing an organosilane compound having allyl or an allyl derivative to react with an inorganic material, particularly solid silica or ITO glass, in the presence of an acid and an organic solvent, to introduce an organic group into the inorganic material even at room temperature, as well as a preparation method thereof. The invention can effectively introduce the organic group into the inorganic material even at room temperature, and thus is very effective in introducing compounds having a thermally sensitive functional group, for example, natural compounds or proteins. It is possible to introduce various organic groups into an inorganic material and to separate and purify organic molecule-bonded organosilane compounds using a silica gel column to effectively bond them to inorganic materials. Accordingly, the invention is very useful in the chemical industry.Type: ApplicationFiled: May 16, 2006Publication date: October 29, 2009Applicant: Industry-Academic Cooperation Foundation Yonsei UniversityInventors: Chul-Ho Jun, Ye-Lim Yeon, Ji-Sung Lee, Young-Jun Park
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Patent number: 7605136Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.Type: GrantFiled: December 5, 2003Date of Patent: October 20, 2009Assignee: Bayer Schering Pharma AGInventors: Klaus Bosslet, Holger Hess-Stumpp, Jens Hoffmann, Ulrich Klar, Andrea Rotgeri
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Publication number: 20090258315Abstract: The invention provides various photoacid generator compounds and ionic components thereof. Photoresist compositions that include the ions and non-ionic photoacid generator compounds are also provided. The invention further provides methods of making and using the photoacid generator compounds and photoresist compositions disclosed herein. The compounds and compositions are useful as photoactive components in chemically amplified resist compositions for use in, for example, various microfabrication applications.Type: ApplicationFiled: April 9, 2009Publication date: October 15, 2009Applicant: Cornell Research Foundation, Inc.Inventors: Christopher K. Ober, Yi Yi
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Publication number: 20090253646Abstract: Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described.Type: ApplicationFiled: April 6, 2009Publication date: October 8, 2009Applicant: GlycoMimetics, Inc.Inventor: John L. MAGNANI
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Patent number: 7598286Abstract: This invention provides anti-inflammatory agents of formula I, having the structure wherein A and R1-R10 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: October 27, 2005Date of Patent: October 6, 2009Assignee: WyethInventors: Robert John Steffan, Edward Martin Matelan
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Publication number: 20090246763Abstract: Disclosed are tri-nuclear metal complexes and salts thereof, such as tri-nuclear osmium or ruthenium complexes or salts thereof, suitable for use as electrochemical labels. Also disclosed are oligonucleotide probes with an attached electrochemical label, methods of nucleic acid amplification, methods of sequencing, and kits for nucleic acid amplification and sequencing having oligonucleotide probes including an electrochemical label. The electrochemical labels are synthesized from siderophores.Type: ApplicationFiled: March 31, 2008Publication date: October 1, 2009Applicant: APPLERA CORPORATION, APPLIED BIOSYSTEMS GROUPInventor: Robert G. Eason
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Publication number: 20090239814Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.Type: ApplicationFiled: December 4, 2008Publication date: September 24, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash K. Narayanannair, Martin Maier
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Patent number: 7589068Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: February 10, 2006Date of Patent: September 15, 2009Assignee: Merck & Co., Inc.Inventors: Nicholas D. P. Cosford, Mark E. Layton, Jun Liang, Craig W. Lindsley, Philip E. Sanderson, Zhijian Zhao
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Publication number: 20090227530Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: July 24, 2008Publication date: September 10, 2009Applicant: PARION SCIENCES, INC.Inventor: Michael R. JOHNSON
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Publication number: 20090226948Abstract: The present invention relates to a time temperature indicator for indicating temperature change over time, comprising an immobilized enzyme and a substrate of the enzyme, wherein the reaction of the substrate catalyzed by the enzyme produces a reaction product in a time and temperature dependent manner and wherein the formation of the reaction product can be detected by monitoring a physical characteristic of the substrate and/or the product which is linked to its concentration. The invention further relates to a method of time temperature indication comprising the step of an enzyme-catalyzed reaction, a method of printing the enzyme-based time temperature indicator on a packaging material or a label, a printing ink or printing ink concentrate comprising components of the enzyme-based time temperature indicator and a packaging material or a label comprising the enzyme-based time temperature indicator.Type: ApplicationFiled: August 3, 2005Publication date: September 10, 2009Inventors: Hans Reichert, Peter Simmendinger, Thomas Bolle
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Publication number: 20090215705Abstract: The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.Type: ApplicationFiled: June 7, 2006Publication date: August 27, 2009Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventors: William R. Kem, Ferenc Soti
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Publication number: 20090215707Abstract: The present invention relates to a compound represented by the following formula (1?) wherein R is an aldopyranose residue, R2 is a C2-18 hydrocarbon group optionally having substituent(s), R3 is an acyl group, X is an oxygen atom, a sulfur atom or —NH—, and p is an integer of 0-4, or a salt thereof. The compound of the present invention has a specific immunoregulatory ability, and is useful for the prophylaxis or treatment of autoimmune diseases and the like.Type: ApplicationFiled: March 3, 2006Publication date: August 27, 2009Applicant: RIKENInventors: Ken-ichi Fuhshuku, Kenji Mori, Takuya Tashiro, Masaru Taniguchi, Ken-ichiro Seino
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Publication number: 20090209476Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.Type: ApplicationFiled: February 11, 2009Publication date: August 20, 2009Applicant: Dow AgroSciences LLCInventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLead, David A. Demeter, Kristy Bryan, Annette V. Brown, William H. Dent, III, Denise P. Cudworth, Jaime S. Nugent, Ricky Hunter, Jack G. Samaritoni
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Publication number: 20090209745Abstract: The present invention discloses a radiographic contrasting agent containing multiple aromatic groups, each of which is substituted with at least three halogen atoms. The radiographic contrasting agent can initiate a polymerization process. The present invention also discloses a radio-opaque polymeric material that comprises a biodegradable polymer having at least one radiographic contrasting moiety covalently attached thereto. The radio-opaque polymeric material provides enhanced contrasting intensity in radiographic imaging. The radio-opaque polymeric material can be applied on at least a portion of one surface of a medical device. The radio-opaque polymeric material can also be used to construct a medical device, a component thereof, or a portion of a component thereof.Type: ApplicationFiled: March 26, 2009Publication date: August 20, 2009Inventor: Jonathon Z. Zhao
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Patent number: 7569679Abstract: A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.Type: GrantFiled: August 11, 2005Date of Patent: August 4, 2009Assignee: WyethInventors: Li Shen, Kelly Keating, Oliver McConnell, William DeMaio, Appavu Chandrasekaran
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Patent number: 7566699Abstract: The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.Type: GrantFiled: March 24, 2004Date of Patent: July 28, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Hideyuki Muranaka, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Fumiaki Ito, Masayuki Isaji
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Publication number: 20090181905Abstract: The invention relates to a crystalline form of 1?-(1-methylethyl)-4?-[(2-fluoro-4-methoxyphenyl)methyl]-5?-methyl-1H-pyrazol-3?-O-?-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.Type: ApplicationFiled: March 16, 2009Publication date: July 16, 2009Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, AJINOMOTO CO., INC.Inventors: Gerd KRAEMER, Hans-Juergen MARTIN, Gebhard ADELGOSS, Klaus DUGI, Adil DURAN, Peter EICKELMANN, Steffen MAIER, Sabine PINNETTI, Regine RITTER, Gebhard SCHILCHER, Ruediger STREICHER, Leo THOMAS
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Patent number: 7556967Abstract: Disclosed herein are novel probes, which can be used to detect and identify target molecules of interest in a sample. The disclosed probes can be used to monitor conformational changes induced by molecular recognition events in addition to providing signaling the presence and/or identity of a target molecule. Methods, including solid phase synthesis techniques, for making probe molecules that exhibit changes in their optical properties upon target molecule binding are described in the disclosure. Also disclosed herein are novel chromophore moieties, which have tailored fluorescent emission spectra.Type: GrantFiled: April 24, 2007Date of Patent: July 7, 2009Assignee: Washington State University Research FoundationInventors: Alexander D. Q. Li, Wei Wang
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Publication number: 20090156514Abstract: The invention relates generally to novel macrolactams and their analogs, to processes for the preparation of these novel macrolactams, to pharmaceutical compositions comprising the novel macrolactams; and to methods of using the novel macrolactams to treat or inhibit various disorders.Type: ApplicationFiled: August 22, 2008Publication date: June 18, 2009Applicant: NovoBiotic Pharmaceuticals LLCInventors: Aaron PEOPLES, Qibo ZHANG, Charles MOORE, Losee Lucy LING, Mithra ROTHFEDER, Kim Lewis
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Publication number: 20090137498Abstract: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4?-bromo-2?-[(5-chloro-2-pyridyl)carbamoyl]-6?-?-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2?-(2-acetamido-2-deoxy-?-D-glucopyranosyloxy)-4?-bromo-6?-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.Type: ApplicationFiled: January 20, 2009Publication date: May 28, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Tsukasa Ishihara, Fukushi Hirayama, Keizo Sugasawa, Yuji Koga, Takeshi Kadokura, Takeshi Shigenaga
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Publication number: 20090124562Abstract: Provided is a new anti-cancer agent lower in cell toxicity. The present invention provides the compounds represented by the general formula of “Formula 1” or the salt thereof. The compounds are compounds having an organic group introduced on a particular ketone group of VST that functions to inhibit induction of GRP 78 expression, similarly to VST, and is applicable, for example, as an anti-cancer agent. The compounds are also advantageous in that it is less toxic than VST and has lower adverse reaction.Type: ApplicationFiled: July 3, 2006Publication date: May 14, 2009Applicant: TOUDAI TLO, LTD.Inventor: Kazuo Shinya
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Publication number: 20090111769Abstract: The present invention relates compounds of the formula I: oligosaccharide-spacer-GpIIb/IIIa antagonist I, wherein the oligosaccharide is a negatively charged pentasaccharide residue of the structure (I), the charge being compensated by positively charged counterions; the spacer is an essentially pharmacologically inactive linking residue of a length of 15-50 atoms; the GpIIb/IIIa antagonist is a residue derived from tirofiban or an analogue thereof; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases.Type: ApplicationFiled: October 6, 2006Publication date: April 30, 2009Inventor: Martin De Kort
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Publication number: 20090105128Abstract: Compounds of the following formula: wherein X is H or substituted with with at least one X being substituted; and halo is fluorine, chlorine, bromine, iodine; and stereoisomers and conjugable analogs thereof.Type: ApplicationFiled: August 28, 2008Publication date: April 23, 2009Inventors: Darryl J. Bornhop, Mingfeng Bai, Nephi Stella
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Publication number: 20090092980Abstract: The invention relates to assays for assessing miRNA maturation effector (preferably: inhibitor) efficacy, and to substances useful for influencing, particularly for inhibiting, maturation of miRNA. According to the invention there is provided assay of miRNA processing inhibitor efficacy, comprising the steps of: a) providing a target miRNA precursor, b) providing a potential inhibitor of one or more processing steps of the target miRNA precursor, c) bringing together of the target miRNA precursor and the potential inhibitor under miRNA maturation conditions, and d) determining inhibition efficiency. The assay of the present invention allows for a very fast and easy assessment of the efficacy of a potential inhibitor in inhibiting processing of a miRNA precursor into miRNA.Type: ApplicationFiled: July 18, 2008Publication date: April 9, 2009Inventors: Christoph Arenz, Brian Patrick Davies, Saskia Neubacher, Claudine Mercedes Klemm
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Publication number: 20090075909Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds of this invention can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases, for example, bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection or psoriasis. The present invention also relates to pharmacological compositions containing these monosaccharide derivatives, as well as methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, and other inflammatory and/or auto immune disorders.Type: ApplicationFiled: December 22, 2005Publication date: March 19, 2009Applicant: RANBAXY LABORATORIES LIMITED INC.Inventors: Viswajanani Jitendra Sattigeri, Sudershan K. Arora, Mohammad Salman, Venkata P. Palle, Muthukaman Nagarajan, Rajkumar Shirumalla, Gurpreet Kaur Aulakh, Abhijit Ray
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Patent number: 7504489Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: December 5, 2005Date of Patent: March 17, 2009Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauve, Vern L. Schramm
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Publication number: 20090068267Abstract: The present invention relates to novel lamivudine/cyclodextrin complexes and processes for preparing said complexes. The present invention also relates to novel solid pharmaceutical compositions comprising lamivudine, wherein lamivudine is present in the form of said lamivudine/cyclodextrin complexes. The present invention further relates to processes for preparing said compositions.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Applicant: Combino Pharm, S.L.Inventors: Sergio Lloret Perez, Marina Puigvert Colomer
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Publication number: 20090062518Abstract: The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.Type: ApplicationFiled: March 16, 2006Publication date: March 5, 2009Applicant: Kissei Pharmaceutical Co., Ltd,Inventors: Kiyoshi Kasai, Tetsuji Ozawa, Nobuhiko Fushimi, Hidetoshi Isawa, Ken Kikuchi, Masahiro Kobayashi, Junichi Sonehara, Minoru Kubota