Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/70)
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Patent number: 11338271Abstract: A porous carbon material including a porous carbon material having a specific resistance value of 30 ?cm or less at a packing density of 0.3 g/cc, wherein a mesopore volume (cm3/g) of the porous carbon material as measured by the BJH method is 0.5 cm3/g or greater.Type: GrantFiled: January 24, 2019Date of Patent: May 24, 2022Assignee: Dexerials CorporationInventors: Katsuya Tanba, Yoshiharu Okuda, Teiko Kuroda
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Patent number: 9890136Abstract: The present invention provides a compound having the structure: wherein R1 is halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5) R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-5 alkyl-aryl, or C1-5 alkyl-NH-aryl; Ar1 is phenyl or thiophene; wherein when Ar1 is phenyl, then R1 is other than —C(?O)—NR5R6, where one of R5 or R6 is phenyl or quinoline and the other of R5 or R6 is hydroxyalkyl, or where one of R5 or R6 is quinoline and the other of R5 or R6 is H; and wherein when Ar1 is phenyl, then R1 is other than —NR5—C(?O)—R6, where one of R5 is H and R6 is quinoline, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 23, 2014Date of Patent: February 13, 2018Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK MEMORIAL SLOAN-KETTERING CANCER CENTERInventors: Ronald Breslow, Paul Marks, Adaickapillai Mahendran, Yuanshan Yao
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Patent number: 9847220Abstract: The present invention provides compounds of formula a process for their preparation, a solution comprising these compounds, a process for the preparation of a device using the solution, devices obtainable by the process and the use of the bis-azide-type compounds as cross-linkers.Type: GrantFiled: June 30, 2014Date of Patent: December 19, 2017Assignee: BASF SEInventors: Mi Zhou, Fulvio G. Brunetti, Emmanuel Martin, Stefan Becker, Iori Doi, Raissa Nathania Santoso, Mei Shan Lam
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Patent number: 9149800Abstract: This invention relates to a method for producing a ruthenium catalyst in which ruthenium supported on at least one metal oxide is pretreated with an aldehyde compound, a phosphorus compound, and a lower alcohol compound, and a method for producing alkyl- or alkenyl-substituted compound using the ruthenium catalyst.Type: GrantFiled: February 1, 2013Date of Patent: October 6, 2015Assignee: Kyoto UniversityInventors: Kenji Wada, Hiroki Miura, Masahiro Nagao, Saburo Hosokawa, Masashi Inoue
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Patent number: 9006568Abstract: A method of making a fluorothieno[3,4-b]thiophene derivatives and photovoltaic polymers containing same using 3-bromothiophene-2-carboxylic acid as a starting material. This synthetic route provides an easier synthesis as well as greater yield and a purer product, which produces superior results over the prior art less pure products. The resulting materials can be used in a variety of photovoltaic applications and devices, especially solar cells.Type: GrantFiled: February 12, 2013Date of Patent: April 14, 2015Assignees: Phillips 66 Company, Solarmer Energy, Inc.Inventors: Shuangxi Wang, Chenjun Shi, Ruby Chen, Junlian Zhang, Hui Huang, Yue Wu, Wei Wang, Amit Palkar, Ting He
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Patent number: 8889732Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: October 22, 2010Date of Patent: November 18, 2014Assignee: Nissan Chemical Industries, Ltd.Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
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Publication number: 20140228579Abstract: The present application relates to methods for the catalytic reduction of acid chlorides and/or imidoyl chlorides. The methods comprise reacting the acid chloride or imidoyl chloride with a silane reducing agent in the presence of a catalyst such as [Cp(Pri3P)Ru(NCMe)2]+[PF6]?.Type: ApplicationFiled: September 11, 2013Publication date: August 14, 2014Applicant: Brock UnviersityInventors: Georgii Nikonov, Dmitry Gutsulyak, Sun Hwa Lee
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8802720Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: April 22, 2013Date of Patent: August 12, 2014Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Patent number: 8759389Abstract: The present invention relates to compounds useful as inhibitors of PLK protein kinase of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: February 15, 2013Date of Patent: June 24, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Keily
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Publication number: 20140170564Abstract: There is provided an actinic ray-sensitive or radiation-sensitive resin composition containing (A) a compound represented by the following formula (1-1); an actinic ray-sensitive or radiation-sensitive film using the composition; and a pattern forming method: in the formula, R1, R2, R3, R4 and Y? are the same as those in formula (1-1) set forth in the description.Type: ApplicationFiled: February 20, 2014Publication date: June 19, 2014Applicant: FUJIFILM CorporationInventors: Tomoki MATSUDA, Yoko TOKUGAWA, Akinori SHIBUYA
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Publication number: 20130245127Abstract: A compound of formula (I) R-L-CO—X ??(I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) for use in the treatment of rheumatoid arthritis.Type: ApplicationFiled: March 1, 2013Publication date: September 19, 2013Applicant: Avexxin ASInventors: Astrid Jullumstro Feuerherm, Berit Johansen
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Publication number: 20130123514Abstract: The disclosure relates to catalytically active carbocatalysts, e.g., a graphene oxide or graphite oxide catalyst suitable for use in a variety of chemical transformations. In one embodiment, it relates to a method of catalyzing a chemical reaction of an organic molecule by reacting the organic molecule in the presence of a sufficient amount of graphene oxide or graphite oxide for a time and at a temperature sufficient to allow catalysis of a chemical reaction. According to other embodiments, the reaction may be an oxidation reaction, a hydration reaction, a dehydrogenation reaction, a condensation reaction, or a polymerization reaction. Some reactions may include auto-tandem reactions. The disclosure further provides reaction mixtures containing an organic molecule and graphene oxide or graphite oxide in an amount sufficient to catalyze a reaction of the organic molecule.Type: ApplicationFiled: May 27, 2011Publication date: May 16, 2013Applicant: GRAPHEA, INC.Inventors: Christopher W. Bielawski, Daniel R. Dreyer, Hong-Peng Jia
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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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Patent number: 8324401Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: GrantFiled: August 18, 2009Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang
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Patent number: 8283383Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Patent number: 8258162Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: GrantFiled: June 26, 2009Date of Patent: September 4, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Publication number: 20120203012Abstract: There are provided a heteroaromatic-containing compound represented by the following general formula (1), and an optical material including the heteroaromatic-containing compound. wherein R1 and R2 are each independently a hydrogen atom or a methyl group, Ar1 is an aryl group which may have a substituent, and A is an aromatic hydrocarbon group. The R1 and R2 can be a hydrogen atom, and Ar1 can be a phenyl group.Type: ApplicationFiled: December 16, 2010Publication date: August 9, 2012Applicant: CANON KABUSHIKI KAISHAInventor: Terunobu Saitoh
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Patent number: 8158675Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: July 24, 2009Date of Patent: April 17, 2012Assignee: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Patent number: 8133910Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: GrantFiled: July 10, 2007Date of Patent: March 13, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Patent number: 8039496Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.Type: GrantFiled: January 22, 2008Date of Patent: October 18, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Patent number: 8030327Abstract: The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6?, are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: November 7, 2005Date of Patent: October 4, 2011Assignee: MDS K.K.Inventors: Yoshiyuki Sato, Hideki Kurihara, Kaori Kamijo, Yu Onozaki, Toshiaki Tsujino, Tetsuya Sugimoto, Akiko Watanabe, Morihiro Mitsuya, Hideya Komatani
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Patent number: 7935696Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: GrantFiled: October 25, 2007Date of Patent: May 3, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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METHODS OF INHIBITING THE FORMATION OF AMYLOID-BETA DIFFUSABLE LIGANDS USING ACYLHYDRAZIDE COMPOUNDS
Publication number: 20110098309Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.Type: ApplicationFiled: July 11, 2008Publication date: April 28, 2011Applicant: ACUMEN PHARMACEUTICALS, INC.Inventors: Gary Charles Look, Lauri Schultz, Alexandre Mikhaylovich Polozov, Nikhil Bhagat, Jian Wang, David E. Zembower, William F. Goure, Todd Pray, Grant A. Krafft -
Patent number: 7932283Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, 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: April 5, 2007Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
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Patent number: 7872146Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.Type: GrantFiled: May 6, 2006Date of Patent: January 18, 2011Assignee: Bayer CropScience AGInventors: Thierry Eynard, Cécile Franc
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Publication number: 20100233106Abstract: The present invention relates to small molecule modulators of melanin expression and methods of making the small molecules. Also disclosed are methods of increasing pigmentation in a cell which involve providing compounds of the present invention and contacting a cell with the compounds under conditions effective to induce melanin expression in the cell, thereby increasing pigmentation. The present invention also relates to compositions containing compounds of the present invention and a carrier.Type: ApplicationFiled: March 28, 2008Publication date: September 16, 2010Applicant: UNIVERSITY OF ROCHESTERInventors: Benjamin L. Miller, Brian R. McNaughton, Peter Gareiss, Glynis Scott
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Patent number: 7759502Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: October 29, 2007Date of Patent: July 20, 2010Assignee: The Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
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Patent number: 7741479Abstract: The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.Type: GrantFiled: December 7, 2005Date of Patent: June 22, 2010Assignee: Locus Pharmaceuticals, Inc.Inventors: Enrique Luis Michelotti, Eric Bruce Springman, Duyan Nguyen, Rupa S. Shetty, Younghee Lee, Kristofer Kent Moffett, Jennifer Lee Ludington, Ted Tsutomis Fujimoto, Zenon D. Konteatis, Bin Liu, Frank Hollinger, Bruce D. Dorsey
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Patent number: 7691898Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.Type: GrantFiled: October 5, 2005Date of Patent: April 6, 2010Assignee: Kotobuki Pharmaceutical Co., Ltd.Inventors: Hiroshi Tomiyama, Masayuki Yokota, Kazuo Tokuzaki, Ryoko Tomita
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Publication number: 20100048648Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: July 10, 2007Publication date: February 25, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
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Patent number: 7659411Abstract: The present invention provides a process for producing a 2-acylthiophene compound which has a low content of the 3-isomer generated as a by-product, the process comprising reacting a thiophene compound represented by formula (1): wherein R1is a hydrogen atom, a C1-6 alkyl group, a phenyl group, or a halogen atom, with at least one member selected from the group consisting of acid anhydrides represented by formula (2): wherein R2 is a C1-6 alkyl group or a phenyl group, and acid halides represented by formula (3): wherein R2 is as defined above and X is a halogen atom, in the presence of a solid acid catalyst at a temperature less than 75° C. in the absence of solvent, thus producing a 2-acylthiophene compound represented by formula (4): wherein R1 and R2 are as defined above.Type: GrantFiled: December 13, 2004Date of Patent: February 9, 2010Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Seiji Bando, Syuzo Satake, Hirokazu Kagano
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as 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. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Patent number: 7625944Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: July 30, 2007Date of Patent: December 1, 2009Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20090221832Abstract: A process for preparing ketones of the general formula (III) where R is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, and R1 is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, by reacting alpha-oxo carboxylates of the general formula (I) wherein n and m is a number in the range from 1 to 6, M(m+) is a cation, and R has the meaning indicated for formula (III), with aryl bromides of the general formula (II) R1—Br ??(II) where R1 has the meaning indicated for formula (III), in the presence of two transition metals or compounds thereof as catalyst, is described.Type: ApplicationFiled: February 19, 2009Publication date: September 3, 2009Applicant: SALTIGO GMBHInventors: Alain Cotte, Matthias Gotta, Lukas Goossen, Felix Rudolphi, Christoph Oppel, Nuria Rodriguez Garrido
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Patent number: 7569600Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: May 15, 2006Date of Patent: August 4, 2009Assignee: ViroChem Pharma Inc.Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Patent number: 7553970Abstract: The invention relates to a process for preparing enantiomer-enriched 3-heteroaryl-3-hydroxypropanoic acid derivatives and 3-heteroaryl-1-aminopropan-3-ols, and to their use.Type: GrantFiled: September 24, 2003Date of Patent: June 30, 2009Assignee: Lanxess Deutschland GmbHInventors: Frank Berendes, Markus Eckert, Nils Brinkmann, Claus Dreisbach, Ruth Meissner, Rainhard Koch
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Patent number: 7528274Abstract: Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.Type: GrantFiled: July 25, 2002Date of Patent: May 5, 2009Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: John K. Inman, Atul Goel, Ettore Appella, Jim Turpin, Marco Schito
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Patent number: 7476686Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Achillion Pharmaceuticals, Inc.Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 7439372Abstract: A compound having a structure is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.Type: GrantFiled: May 1, 2007Date of Patent: October 21, 2008Assignee: Allergan, Inc.Inventors: Donde Yariv, Jeremiah H. Nguyen
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Patent number: 7423030Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).Type: GrantFiled: October 11, 2006Date of Patent: September 9, 2008Assignee: Sanofi-AventisInventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
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Patent number: 7396843Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: October 16, 2002Date of Patent: July 8, 2008Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Suzanne Joy Merrick, Ann Louise Walker
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Patent number: 7388012Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.Type: GrantFiled: September 15, 2005Date of Patent: June 17, 2008Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Crew, An-Hu Li, Hanqing Dong, Tao Zhang
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Patent number: 7381688Abstract: This invention relates to novel methylthiophenecarboxanilides of the formula (I) in which R1, R2, R3, R4, R5 and R6 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted micro-organisms, and to novel intermediates and their preparations.Type: GrantFiled: April 15, 2003Date of Patent: June 3, 2008Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Heiko Rieck, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Patent number: 7365094Abstract: The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: GrantFiled: December 17, 2003Date of Patent: April 29, 2008Assignee: 4SC AGInventors: Johann Leban, Stefan Tasler
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Patent number: 7351841Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: December 6, 2005Date of Patent: April 1, 2008Assignee: Nissan Chemical Industries, Ltd.Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Patent number: 7342116Abstract: A process is disclosed for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.Type: GrantFiled: March 25, 2003Date of Patent: March 11, 2008Assignee: Koei Chemical Co., Ltd.Inventors: Yasuhiro Shiomi, Osamu Uno, Akio Ohta, Takeshi Sunakami
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Patent number: 7312181Abstract: The present invention provides compounds of Formula I: wherein Ar1 is aryl or heteroaryl, Ar2 is aryl or heteroaryl, and R is a suitable organic group. Herbicidal composition comprising such active compounds, and methods for controlling undesirable plants by applying such compounds, are also described.Type: GrantFiled: March 22, 2006Date of Patent: December 25, 2007Assignee: Cropsolution, Inc.Inventors: Shy-Fuh Lee, Vivian Du, Richard Anderson
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 7244763Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.Type: GrantFiled: February 6, 2004Date of Patent: July 17, 2007Assignee: Warner Lambert Company LLCInventors: Larry D. Bratton, Xue-Min Cheng, Noe Erasga, Gary F. Filzen, Andrew G. Geyer, Chitase Lee, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 7183297Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: October 16, 2002Date of Patent: February 27, 2007Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Stephen Sean Flack, Dramane Ibrahim Lainé, Ann Louise Walker