Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., N-oleoylpyrrolidine, Etc.) Patents (Class 548/540)
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Publication number: 20130108685Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.Type: ApplicationFiled: April 28, 2011Publication date: May 2, 2013Inventors: Takeshi Kuboyama, Tomohiro Era, Tomoyuki Naoi
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Patent number: 8404866Abstract: The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.Type: GrantFiled: September 2, 2009Date of Patent: March 26, 2013Assignee: Florida State University Research FoundationInventors: Martin A. Schwartz, Yonghao Jin, Qing-Xiang (Amy) Sang
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Publication number: 20130059873Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: April 3, 2012Publication date: March 7, 2013Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Publication number: 20130053342Abstract: The invention relates to the cosmetic use, as a skin moisturizer, of a compound of formula (I): with (i) R1 and R2 represent a hydrogen atom or a C1-C6 alkyl group, or (ii) R1 and R2 can form, together with the nitrogen atom which bears them, a saturated heterocycle with 5 to 7 ring members; R5 representing a hydrogen atom or a (C1-C3) alkyl group; R6 representing a hydrogen atom or a (C1-C4) alkyl group; R3 represents a hydrogen atom or a (C1-C6) alkyl group, or —OR3 represents a phosphate group; it being possible for the two groups R3 to form, together, an isopropylidene group; R4 represents a hydrogen atom or —OR4 represents a phosphate group; and the salts, solvates and isomers thereof. The invention also relates to a cosmetic composition comprising a compound (I) and the corresponding new compounds.Type: ApplicationFiled: October 23, 2012Publication date: February 28, 2013Applicant: L'OREALInventor: L'OREAL
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Patent number: 8383833Abstract: The present application relates to a method for producing an optically active ?-amino acid derivative, comprising steps of reacting an ?-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active ?-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.Type: GrantFiled: June 2, 2009Date of Patent: February 26, 2013Assignee: Kaneka CorporationInventors: Shohei Yamamoto, Akio Fujii, Masaru Mitsuda
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Publication number: 20130040998Abstract: Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases).Type: ApplicationFiled: January 5, 2011Publication date: February 14, 2013Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: James Elliot Bradner, Ralph Mazitschek
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Publication number: 20120302719Abstract: New bioresorbable polymers are synthesized from monomer analogs of natural metabolites In particular, polymers are polymerized from analogs of amino acids that contribute advantageous synthesis, processing and material properties to the polymers prepared therefrom, including particularly advantageous degradation profilesType: ApplicationFiled: May 29, 2012Publication date: November 29, 2012Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal
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Publication number: 20120296088Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: ApplicationFiled: March 14, 2012Publication date: November 22, 2012Inventors: Bradford H. Hirth, Craig Siegel
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Publication number: 20120295874Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.Type: ApplicationFiled: October 7, 2010Publication date: November 22, 2012Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATIONInventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
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Publication number: 20120294939Abstract: Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of direct compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus present formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.Type: ApplicationFiled: July 31, 2012Publication date: November 22, 2012Inventors: James Kowalski, Jay Parthiban Lakshman, Arun P. Patal
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Publication number: 20120289710Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a g-amino-d-biphenyl-a-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: January 21, 2011Publication date: November 15, 2012Inventors: David Hook, Jianguang Zhou, Yunzhong Li
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Patent number: 8293926Abstract: The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods.Type: GrantFiled: December 8, 2006Date of Patent: October 23, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Junichi Yasuoka, Shoji Fukuyo, Tetsuya Ikemoto
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Patent number: 8288534Abstract: The invention relates to a novel process for the preparation of Ruthenium metathesis catalysts of the formula Ruthenium metathesis catalysts have been widely applied in the synthesis of macrocyclic drug compounds.Type: GrantFiled: May 6, 2010Date of Patent: October 16, 2012Assignee: Roche Palo Alto LLCInventors: Angelino Doppiu, Ralf Karch, Kurt Puentener, Andreas Rivas-Nass, Michelangelo Scalone, Roland Winde, Eileen Woerner
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Patent number: 8268880Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: GrantFiled: December 15, 2006Date of Patent: September 18, 2012Assignee: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Publication number: 20120213904Abstract: The present invention relates to novel pandan extract articles in powder form, wherein the artice comprises high amounts of precursors of 2-acetyl-1-pyrroline, a novel process of preparing such pandan extract articles in powder form and corresponding methods of using said pandan extract articles.Type: ApplicationFiled: February 22, 2012Publication date: August 23, 2012Applicant: SYMRISE AGInventors: Andreas Degenhardt, Gerhard Krammer, Jens Koch, Mee Yin Tai
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Patent number: 8247404Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.Type: GrantFiled: December 13, 2010Date of Patent: August 21, 2012Assignee: SanofiInventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart
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Patent number: 8242286Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.Type: GrantFiled: July 28, 2008Date of Patent: August 14, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Jin Li, Nicole Lee Kolosko
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Patent number: 8207183Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: GrantFiled: July 8, 2011Date of Patent: June 26, 2012Assignee: Novartis AGInventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Publication number: 20120141496Abstract: The present invention, according to several embodiments, comprises a compound represented by Formula I: in which the substituents BG, B, B1, R1, R100, R2, R200, A, A1, Q and Q1 are defined herein; or a prodrug, or a salt thereof, and which bind to IAP BIR domains. In particular, the compounds of certain embodiments are useful in treating proliferative disorders such as cancer.Type: ApplicationFiled: December 17, 2007Publication date: June 7, 2012Applicant: AEGERA THERAPEUTICS, INC.Inventors: Alain Laurent, Scott Jarvis
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Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Publication number: 20120142916Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: December 21, 2011Publication date: June 7, 2012Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murtidhar Waykole
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Patent number: 8183280Abstract: The present invention concerns compounds, according to general formula (I), which find utility preferably for the treatment of cancer.Type: GrantFiled: August 31, 2006Date of Patent: May 22, 2012Assignee: Vantia LimitedInventors: David Michael Evans, John Horton, Julie Elizabeth Trim
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Publication number: 20120122764Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Qian LIU, Muneto MOGI, Nikolaus SCHIERING, Robert SUN
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Patent number: 8168631Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: February 3, 2009Date of Patent: May 1, 2012Assignee: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20120100274Abstract: The present invention relates to a method for synthetizing a compound of the following formula (I): wherein R is a methyl or ethyl group, n is 1 or 2, and X is a CH2 or CD2 group, from a compound of the following formula (II): wherein R and n are as defined above, and also relates to a method for assaying the compounds of the formula (I) using a corresponding deuterated derivative as an internal reference, as well as to the use of ketal derivatives of compounds of the formula (I) as a stable precursor, in particular in a flavoring composition.Type: ApplicationFiled: June 24, 2010Publication date: April 26, 2012Inventors: Alain Morere, Chantal Menut, Yusuf Ziya Gunata, Abdelhamid Agrebi
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Publication number: 20120101080Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: June 25, 2010Publication date: April 26, 2012Applicant: BioVersys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
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Patent number: 8163792Abstract: Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.Type: GrantFiled: May 16, 2007Date of Patent: April 24, 2012Assignee: Pharmascience Inc.Inventors: Alain Laurent, Scott Jarvis, Patrick Bureau, Alain Boudreault, James Jaquith
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Publication number: 20120077779Abstract: Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer.Type: ApplicationFiled: July 6, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai
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Patent number: 8143259Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: GrantFiled: August 11, 2009Date of Patent: March 27, 2012Assignee: Janssen Pharmaceutica, NVInventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
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Publication number: 20120045509Abstract: The present invention refers to pharmaceutical composition comprising a DPP-IV inhibitor.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Inventors: Bernd Michael Loeffler, Alexander MacDonald, Cynthia Rocha, Eric Worth
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Patent number: 8110598Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.Type: GrantFiled: January 23, 2008Date of Patent: February 7, 2012Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Publication number: 20120029188Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Applicant: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Patent number: 8106191Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.Type: GrantFiled: June 13, 2003Date of Patent: January 31, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Publication number: 20120022263Abstract: The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R1 and R2 each represent, for instance, a C1 to C3 alkoxy group or a C1 to C3 haloalkoxy group; R3 and R4 each represent, for instance, a C1 to C8 alkyl group or a C1 to C8 haloalkyl group; R5 represents, for instance, a C1 to C5 haloalkyl group; R6 and R7 each represent, for instance, a hydrogen atom or a C1 to C5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).Type: ApplicationFiled: February 5, 2010Publication date: January 26, 2012Applicant: AGRO-KANESHO Co., Ltd.Inventors: Shuichi Usui, Toshiki Fukuchi, Sachiko Kinoshita
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Patent number: 8088763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 3, 2012Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
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Publication number: 20110294827Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: ApplicationFiled: June 3, 2011Publication date: December 1, 2011Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8053465Abstract: Summary Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. Solving Means The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).Type: GrantFiled: December 8, 2009Date of Patent: November 8, 2011Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Kohei Ohata, Kazuya Yokota, Koji Murakami, Toshiyuki Matsui
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte
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Publication number: 20110263604Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: ApplicationFiled: April 18, 2011Publication date: October 27, 2011Applicant: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Publication number: 20110257164Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.Type: ApplicationFiled: January 7, 2010Publication date: October 20, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
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Publication number: 20110245250Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X is hydrogeType: ApplicationFiled: July 20, 2009Publication date: October 6, 2011Applicant: Ramot at tel-Aviv University Ltd.Inventors: Simon David Edwards, Meriel Ruth Kimberley, Richard Edward Armer, Nawaz Mohammed Khan
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Publication number: 20110230539Abstract: Compounds having a structure of Formula (A) are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are provided. Uses of compounds having a structure of Formula (F) for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.Type: ApplicationFiled: August 24, 2009Publication date: September 22, 2011Inventors: Marianne D. Sadar, Nasrin R. Mawji, Jun Wang, Raymond J. Andersen, David E. Williams, Mike Leblanc, Lu-Ping Yan
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Patent number: 7999120Abstract: A process for continuously removing a target product X in the form of fine crystals from a liquid phase P comprising the target product X and constituents other than the target product X by cooling suspension crystallization in the secondary chamber, into which the liquid phase P flows continuously, of an indirect heat exchanger with simultaneous continuous flow of a coolant through the primary chamber of the indirect heat exchanger and continuous withdrawal of a crystal suspension S having a degree of crystallization Y from the secondary chamber, in which the degree of crystallization Y is adjusted on the basis of a heat balance conducted continuously with the aid of a process computer.Type: GrantFiled: September 12, 2008Date of Patent: August 16, 2011Assignee: BASF SEInventors: Jörg Heilek, Peter Schlemmer, Ulrich Hammon, Klaus Joachim Müller-Engel
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Publication number: 20110178151Abstract: The present invention relates to novel fatty acid derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as agents for the treatment of obesity and related disorders, and for improving cognition.Type: ApplicationFiled: March 4, 2009Publication date: July 21, 2011Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREWInventors: Jehoshua Katzhendler, Elliot Berry, Yosefa Avraham, Yousef Najajreh, Meir Saidian, Raphael Mevorach
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave