The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/341.5)
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Patent number: 11912665Abstract: A 4-(2,4,5-tris(4-chlorophenyl)-1H-imidazol-1-yl)butanoic acid compound, its synthesis, and its use as an antimicrobial agent.Type: GrantFiled: October 25, 2023Date of Patent: February 27, 2024Assignee: KING FAISAL UNIVERSITYInventors: Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
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Patent number: 10868329Abstract: To provide an all solid state secondary battery capable of realizing favorable bonding properties and a favorable ion conductivity. Provided is an all solid state secondary battery having a structure in which an electrode layer is located between a collector and an inorganic solid electrolyte layer, in which the electrode layer contains an inorganic solid electrolyte having a conductivity of ions of metals belonging to Group I or II of the periodic table, an active material, and a specific polymer described below, specific polymer: a polymer having at least one specific functional group selected from acidic functional groups, amide groups, or hydroxyl groups.Type: GrantFiled: June 28, 2017Date of Patent: December 15, 2020Assignee: FUJIFILM CorporationInventors: Tomonori Mimura, Hiroaki Mochizuki, Masaomi Makino, Katsuhiko Meguro
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Patent number: 9586933Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.Type: GrantFiled: December 22, 2015Date of Patent: March 7, 2017Assignee: Gilead Sciences, Inc.Inventor: Gregory Notte
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Patent number: 9168206Abstract: Presently described are curable dental compositions comprising a polymerizable ionic liquid. The polymerizable ionic liquid comprises one or more ethylenically unsaturated (e.g. free-radically polymerizable) groups. Various embodiments of curable dental compositions are described. In some embodiments, the polymerizable ionic liquid is a monofunctional polymerizable ionic liquid comprising an ethylenically unsaturated group. In other embodiments, the polymerizable ionic liquid is a multifunctional polymerizable ionic liquid comprising at least two ethylenically unsaturated groups. The curable dental compositions describe herein can be utilized as dental primers, dental adhesives, dental sealants, and dental composites. In many embodiments, the curable dental compositions further comprise an initiator such as a photoinitiator.Type: GrantFiled: September 8, 2014Date of Patent: October 27, 2015Assignee: 3M Innovative Properties CompanyInventors: Yizhong Wang, Joel D. Oxman, Larry R. Krepski, Peiwang Zhu, Kevin M. Lewandowski, Brian N. Holmes
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Patent number: 9127101Abstract: Presently described are curable compositions comprising a mixture of at least one (e.g. free-radically) polymerizable ionic liquid and at least one other ethylenically unsaturated monomer, oligomer, or polymer. The polymerizable ionic liquid is characterized as having an air to nitrogen curing exotherm ratio of at least 0.70. Also described are articles and methods of making articles from such curable compositions. A monofunctional polymerizable ionic liquid is also described comprising a non-polymerizable substituted imidazolium cationic group and a polymerizable sulfonate anion.Type: GrantFiled: July 15, 2014Date of Patent: September 8, 2015Assignee: 3M Innovative Properties CompanyInventors: Yizhong Wang, Joel D. Oxman, Larry R. Krepski, Peiwang Zhu, Kevin M. Lewandowski, Brian N. Holmes, Richard L. Severance, Joseph D. Rule, Thomas P. Klun
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Patent number: 9040653Abstract: This disclosure provides methods of controlled polymerization of cyclic compounds catalyzed by carbene derivatives having a general formula as shown below, and to obtain a biodegradable polymeric material having a large molecular weight, a narrow dispersity, and no metallic impurity.Type: GrantFiled: February 24, 2011Date of Patent: May 26, 2015Assignee: NANJING UNIVERSITY OF TECHNOLOGYInventors: Zhenjiang Li, Pingkai Ouyang, He Huang
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Publication number: 20150064111Abstract: The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di-acid moiety comprises a di-tetrazole.Type: ApplicationFiled: April 3, 2013Publication date: March 5, 2015Applicant: APOSENSE LTD.Inventors: Joel M. Van Gelder, Menashe Levy, Mirit Argov, Miri Ben-Ami, Ilan Ziv
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Patent number: 8962599Abstract: Therapeutic compositions comprising substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.Type: GrantFiled: September 9, 2014Date of Patent: February 24, 2015Assignee: Antecip Bioventures II LLCInventor: Herriot Tabuteau
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Patent number: 8901162Abstract: The present disclosure relates to therapeutic compositions comprising substituted imidazoliums having multiple acidic groups. The compounds may be used to treat diseases or conditions such as those associated with bone, cancer, or pain. Compositions, dosage forms, methods of treating diseases or conditions, methods of preparation, and other related embodiments related to the substituted imidazoliums are also described herein.Type: GrantFiled: May 28, 2014Date of Patent: December 2, 2014Assignee: Antecip Bioventures II LLCInventor: Herriot Tabuteau
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Patent number: 8901161Abstract: Therapeutic compositions comprising at least two substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.Type: GrantFiled: May 27, 2014Date of Patent: December 2, 2014Assignee: Antecip Bioventures II LLCInventor: Herriot Tabuteau
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Publication number: 20140315960Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.Type: ApplicationFiled: October 31, 2012Publication date: October 23, 2014Inventor: Claus Selch LARSEN
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Patent number: 8865757Abstract: Therapeutic compositions comprising at least two substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.Type: GrantFiled: May 28, 2014Date of Patent: October 21, 2014Assignee: Antecip Bioventures II LLPInventors: Herriot Tabuteau, Eric K. H. Dinkla
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Patent number: 8785655Abstract: A chiral ionic compound comprising an alkyl substituted imidazolium or pyridinium cationic core having an alkyl ester side chain (-alkyl-C(O)O—) directly linked to the core and an associated counter anion, characterized in that the —O— atom of the ester side chain is linked to an alpha, a beta or a gamma hydroxycarboxylic acid functionality via the alpha, beta or gamma hydroxy of the acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon, or characterized in that an —N? atom of the alkyl substituted imidazolium or pyridinium cationic core is substituted with an alpha, a beta or a gamma hydroxy group of a alpha, a beta or a gamma hydroxycarboxylic acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon. The chiral ionic liquids (CILs) may be used as novel solvents, in particular for organic synthesis. The CILs have the potential to induce asymmetry into substrates or catalysts in a variety of organic transformations.Type: GrantFiled: February 24, 2010Date of Patent: July 22, 2014Assignee: Dublin City UniversityInventors: Nicholas Gathergood, Bruce Pegot, Ian Beadham, Monika Gurbisz, Mukund D. Ghavre, Saibh Morrissey
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Patent number: 8759385Abstract: Hair treatment composition comprising an azole fungicide and zinc gluconate and wherein the composition does not comprise Trichogen®.Type: GrantFiled: April 13, 2010Date of Patent: June 24, 2014Assignee: Conopco Inc.Inventors: Jason Shaun Burry, Richard Livesey Evans, Graham Andrew Turner
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20140135503Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl- group, optionally substituted with —ONO2 group, or an aralkyl- or aryl- group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl- group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl- group, Y represents (CH2), group or 0 atom or S atom, and where n=0-3.Type: ApplicationFiled: May 25, 2012Publication date: May 15, 2014Applicant: CHINOIN ZRT.Inventors: Gábor Havasi, Tibor Kiss, Irén Hortobágyi, Zsuzsanna Kardos, István Lászlófi, Zoltán Bischof, Ádám Bódis
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Patent number: 8633182Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: GrantFiled: May 22, 2013Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
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Patent number: 8623942Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.Type: GrantFiled: March 9, 2010Date of Patent: January 7, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
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Patent number: 8604056Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: July 3, 2012Date of Patent: December 10, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
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Patent number: 8604073Abstract: An antimicrobial composition comprising (a) a cationic surfactant derived from the condensation of fatty acids and esterified dibasic amino acids, such as lauric arginate and (b) an antibiotic, such as of ?-lactam antibiotics, polypeptides, quinolones. The composition may be used as a stand alone antimicrobial formulation, or in combination with medical articles or medical devices.Type: GrantFiled: March 27, 2006Date of Patent: December 10, 2013Assignee: Ethicon, Inc.Inventors: Xintian Ming, Stephen J. Rothenburger
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Publication number: 20130324506Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.Type: ApplicationFiled: June 5, 2013Publication date: December 5, 2013Inventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU
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Publication number: 20130303572Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lõrincz, György Dormán, Anikó Görbe
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Patent number: 8575359Abstract: The invention is in general directed to acid-sensitive linkers, and methods of use thereof, such as, for example, in drug delivery methods.Type: GrantFiled: April 4, 2007Date of Patent: November 5, 2013Assignee: The Regents of the University of CaliforniaInventors: Jerry Yang, Seong Deok Kong, Alice Luong, Stephen Howell
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Patent number: 8557856Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.Type: GrantFiled: March 31, 2009Date of Patent: October 15, 2013Assignee: The General Hospital CorporationInventors: Douglas E. Raines, Stuart A. Forman, Keith W. Miller, Syed Shaukat Husain, Joseph F. Cotten
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Publication number: 20130252930Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.Type: ApplicationFiled: December 16, 2011Publication date: September 26, 2013Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel Chu, Bing Wang, Tao Ye
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Patent number: 8541598Abstract: This invention relates to ionic liquid (ILs) solvents for chemical synthesis based on an alkyl-imidazolium cation core containing ionic liquids which have enhanced biodegradability and reduced toxicity relative to existing imidazolium bases ILs such as 1-butyl-3-methylimidazolium (bmmim) salts. Many of the described ILs produce a score of over 60% biodegradability over 28 days in a biodegradability test such as the Sturm Test, the Closed Bottle Test (OECD 301D) or the CO2 Headspace Test (ISO 14593). The ILs of the invention comprise an alkyl substituted imidazolium cationic core having a —C?OX— side chain in the 3-position of the imidazole ring, wherein X?O, NH, N or S and an associated counteranion characterized in that the —C?OX side chain comprises at least one ether linkage. The biodegradable and non-toxic IL may be used as green solvents for the chemical, pharmaceutical, biofuel and biomass industries. The ILs of the invention are particularly useful in hydrogenation, pericyclic and metathesis reactions.Type: GrantFiled: August 21, 2008Date of Patent: September 24, 2013Assignee: Dublin City UniversityInventors: Nick Gathergood, Saibh Morrissey, Bruce Pegot
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Publication number: 20130245274Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.Type: ApplicationFiled: May 8, 2013Publication date: September 19, 2013Applicant: SANOFIInventors: Claudius BOEHM, Susanne KLEIN, Bernard NAPIERSKI, Christian SOMMER
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Publication number: 20130203829Abstract: The present application is directed to novel imidazole-substituted fatty acids that have been functionalized with an alkyl triphenylphosphonium group, compositions comprising these compounds and their use as inhibitors of cytochrome c peroxidase, in particular for the treatment and prevention of apoptosis.Type: ApplicationFiled: November 13, 2012Publication date: August 8, 2013Inventors: Jeffrey Atkinson, Jeffrey Stuart, Valarian E. Kagan, Detcho A. Stoyanovsky, Michael W. Epperly, Joel S. Greenberger
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Patent number: 8492384Abstract: Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.Type: GrantFiled: June 26, 2009Date of Patent: July 23, 2013Assignee: Korea Institute of Science and TechnologyInventors: Kyung Il Choi, Ghilsoo Nam, Hye Ran Kim, Hyewhon Rhim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Yong Seo Cho, Hyunah Choo, Eun Joo Roh, Soon Bang Kang, Kye Jung Shin, Hoh Gyu Hahn, Dong Yun Shin, Chan Seong Cheong, Kee Dal Nam, Yong Koo Kang, Jae Kyun Lee, Woong Seo Park, Youngsoo Kim, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Gyo Chang Keum, Cheolju Lee, Kee Hyun Choi
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Patent number: 8492422Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: September 15, 2011Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Mohammad I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
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Patent number: 8476387Abstract: Provided is a process for preparing a (meth)acrylic ester (F) of an N-hydroxyalkylated lactam, in which a cyclic N-hydroxyalkylated lactam (L): where the structural variables as defined herein, in the presence of at least one metal salt of C1-C10-alkoxides (A), is esterified with (meth)acrylic acid (S) or transesterified with at least one (meth)acrylic ester (D), in which the metal salt of C1-C10-alkoxides (A) used as a catalyst is added in the absence of solvents and completely at the start of the reaction.Type: GrantFiled: February 11, 2008Date of Patent: July 2, 2013Assignee: BASF SEInventors: Hermann Bergmann, Frank Hoefer, Maximilian Angel
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Publication number: 20130123338Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.Type: ApplicationFiled: May 12, 2011Publication date: May 16, 2013Applicant: Protiva Biotherapeutics, Inc.Inventors: James Heyes, Mark Wood, Alan Martin
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Publication number: 20130071439Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using D-amino acids are described.Type: ApplicationFiled: January 10, 2011Publication date: March 21, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Richard Losick, Jon Clardy, Roberto Kolter, Illana Kolodkin-Gal, Diego Romero, Shugeng Cao
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Patent number: 8372982Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: February 16, 2010Date of Patent: February 12, 2013Assignee: Bayer Cropscience AGInventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20130018194Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.Type: ApplicationFiled: April 1, 2011Publication date: January 17, 2013Applicants: AMINOLUX, INC, EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventor: Kwan-Mook Kim
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Publication number: 20120322769Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.Type: ApplicationFiled: February 16, 2011Publication date: December 20, 2012Applicants: DUKE UNIVERSITY, UWM RESEARCH FOUNDATIONInventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
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Patent number: 8329745Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: GrantFiled: September 6, 2011Date of Patent: December 11, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20120245358Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with an oxalic acid diester and to novel intermediate compounds used therein.Type: ApplicationFiled: May 11, 2010Publication date: September 27, 2012Applicant: SANOFIInventors: Kai Rossen, Volker Kraft, Hermut Wehlan, Antony Bigot, Veronique Crocq-Stuerga
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Publication number: 20120142746Abstract: The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: September 15, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Mohammed I. Dibas, Daniel W. Gil, John E. Donello, Ken Chow, Liming Wang, Michael E. Garst
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Publication number: 20120136036Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: September 15, 2011Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventors: Mohammed I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
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Publication number: 20120122945Abstract: The present invention relates to novel compounds, ester pro-drugs of [3-(1-1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals in the treatment of conditions mediated by adrenergic receptors.Type: ApplicationFiled: September 15, 2011Publication date: May 17, 2012Applicant: ALLERGAN, INC.Inventors: Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil, Mohammad I. Dibas
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Publication number: 20120116097Abstract: There is provided a preparation process in which a N—H group of a heteroaromatic ring compound having a N—H group in its ring is converted directly to a N—Rf group at a high reaction efficiency without using a catalyst. The preparation process is a process for preparing a compound comprising a heteroaromatic ring structure having a N—Rf group (—Rf is a fluorine-containing organic group) in its ring and is characterized in that the heteroaromatic ring compound having a N—H group in its ring is allowed to react with fluoroalkene in the absence of an alkali metal.Type: ApplicationFiled: January 13, 2012Publication date: May 10, 2012Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Yuzo KOMATSU, Haruhiko MOHRI, Hirokazu AOYAMA
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Publication number: 20120071661Abstract: A chiral ionic compound comprising an alkyl substituted imidazolium or pyridinium cationic core having an alkyl ester side chain (-alkyl-C(O)O—) directly linked to the core and an associated counter anion, characterized in that the —O— atom of the ester side chain is linked to an alpha, a beta or a gamma hydroxycarboxylic acid functionality via the alpha, beta or gamma hydroxy of the acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon, or characterized in that an —N? atom of the alkyl substituted imidazolium or pyridinium cationic core is substituted with an alpha, a beta or a gamma hydroxy group of a alpha, a beta or a gamma hydroxycarboxylic acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon. The chiral ionic liquids (CILs) may be used as novel solvents, in particular for organic synthesis. The CILs have the potential to induce asymmetry into substrates or catalysts in a variety of organic transformations.Type: ApplicationFiled: February 24, 2010Publication date: March 22, 2012Inventors: Nicholas Gathergood, Bruce Pegot, Ian Beadham, Monika Gurbisz, Mukund D. Ghavre, Saibh Morrissey
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Publication number: 20120020915Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.Type: ApplicationFiled: January 13, 2011Publication date: January 26, 2012Applicants: QUEENS UNIVERSITY AT KINGSTON, THE SIR MORTIMER B. DAVIS JEWISH GENERAL HOSPITAL, OSTA BIOTECHNOLOGIES, INC.Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
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Publication number: 20110318807Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: ApplicationFiled: September 6, 2011Publication date: December 29, 2011Inventors: Patrick G. Harran, Michael S. Brown, Joseph L. Goldstein, Jin Yang, Tong-Jin Zhao
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Patent number: 8026374Abstract: A process for preparing (meth)acrylic esters (F) of N-hydroxyalkylated imidazoles, wherein N-hydroxyalkylated imidazoles (I), in which R1 and R2 may each independently be hydrogen or C1-C20-alkyl, R3, R4 and R5 are each independently hydrogen or C1-C20-alkyl, C1-C20-alkylcarbonyl, C2-C20-alkenyl, C2-C20-alkenylcarbonyl, C2-C20-alkynyl, C2-C20-alkynylcarbonyl, C3-C15-cycloalkyl, C3-C15-cycloalkylcarbonyl, aryl, arylcarbonyl, a heterocycle or a halogen atom, and m and n are each integers in the range of in each case from 0 to 20, where m and n cannot simultaneously be 0, and in which the particular units bracketed by the variables m and n are present in any sequence, and in which, in the case that m?2, the R1 and R2 radicals are in each case independent in the particular units, in the presence of at least one catalyst (K), are esterified with (meth)acrylic acid (S) or transesterified with at least one (meth)acrylic ester (D).Type: GrantFiled: February 11, 2008Date of Patent: September 27, 2011Assignee: BASF SEInventors: Hermann Bergmann, Frank Hoefer
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Publication number: 20110201824Abstract: This invention relates to ionic liquid (ILs) solvents for chemical synthesis based on an alkyl-imidazolium cation core containing ionic liquids which have enhanced biodegradability and reduced toxicity relative to existing imidazolium bases ILs such as 1-butyl-3-methylimidazolium (bmmim) salts. Many of the described ILs produce a score of over 60% biodegradability over 28 days in a biodegradability test such as the Sturm Test, the Closed Bottle Test (OECD 301D) or the CO2 Headspace Test (ISO 14593). The ILs of the invention comprise an alkyl substituted imidazolium cationic core having a —C?OX— side chain in the 3-position of the imidazole ring, wherein X?O, NH, N or S and an associated counteranion characterized in that the —C?OX side chain comprises at least one ether linkage. The biodegradable and non-toxic IL may be used as green solvents for the chemical, pharmaceutical, biofuel and biomass industries. The ILs of the invention are particularly useful in hydrogenation, pericyclic and metathesis reactions.Type: ApplicationFiled: August 21, 2008Publication date: August 18, 2011Applicant: DUBLIN CITY UNIVERSITYInventors: Nick Gathergood, Saibh Morrissey, Bruce Pegot
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Patent number: 7977367Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: GrantFiled: September 9, 2009Date of Patent: July 12, 2011Assignee: Pfizer IncInventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 7964620Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.Type: GrantFiled: September 17, 2008Date of Patent: June 21, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7964626Abstract: The present invention provides a process for producing N,N?-carbonyldiimidazole, comprising: reacting phosgene, diphosgene, or triphosgene with imidazole in an inert solvent to produce N,N?-carbonyldiimidazole; to imidazole hydrochloride yielded as a by-product in the above step, adding a gaseous or liquid basic compound represented by the below-shown general formula (1) in an inert solvent to conduct neutralization reaction; and circulating the imidazole thus generated to use it as a starting material for N,N?-carbonyldiimidazole production. In the general formula (1), R1, R2, and R3 each independently represents a hydrogen atom, a methyl group, or an ethyl group. The CDI produced by the production process of the invention is a compound useful in the fields of synthesis of pharmaceutical agents, synthesis of agricultural chemicals, peptide synthesis, and the like, e.g.Type: GrantFiled: March 29, 2005Date of Patent: June 21, 2011Assignee: Hodogaya Chemical Co., Ltd.Inventors: Yoshikazu Aoki, Norimasa Yokoyama, Masateru Yasumura