Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/70)
  • Patent number: 9890136
    Abstract: 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: Grant
    Filed: December 23, 2014
    Date of Patent: February 13, 2018
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Ronald Breslow, Paul Marks, Adaickapillai Mahendran, Yuanshan Yao
  • Patent number: 9847220
    Abstract: 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: Grant
    Filed: June 30, 2014
    Date of Patent: December 19, 2017
    Assignee: BASF SE
    Inventors: Mi Zhou, Fulvio G. Brunetti, Emmanuel Martin, Stefan Becker, Iori Doi, Raissa Nathania Santoso, Mei Shan Lam
  • Patent number: 9149800
    Abstract: 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: Grant
    Filed: February 1, 2013
    Date of Patent: October 6, 2015
    Assignee: Kyoto University
    Inventors: Kenji Wada, Hiroki Miura, Masahiro Nagao, Saburo Hosokawa, Masashi Inoue
  • Patent number: 9006568
    Abstract: 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: Grant
    Filed: February 12, 2013
    Date of Patent: April 14, 2015
    Assignees: 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
  • Patent number: 8889732
    Abstract: 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: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20140228579
    Abstract: 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: Application
    Filed: September 11, 2013
    Publication date: August 14, 2014
    Applicant: Brock Unviersity
    Inventors: Georgii Nikonov, Dmitry Gutsulyak, Sun Hwa Lee
  • Patent number: 8802720
    Abstract: 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: Grant
    Filed: April 22, 2013
    Date of Patent: August 12, 2014
    Assignee: Sanofi
    Inventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek
  • Patent number: 8759389
    Abstract: 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: Grant
    Filed: February 15, 2013
    Date of Patent: June 24, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Keily
  • Publication number: 20140170564
    Abstract: 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: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Tomoki MATSUDA, Yoko TOKUGAWA, Akinori SHIBUYA
  • Publication number: 20130245127
    Abstract: 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: Application
    Filed: March 1, 2013
    Publication date: September 19, 2013
    Applicant: Avexxin AS
    Inventors: Astrid Jullumstro Feuerherm, Berit Johansen
  • Publication number: 20130123514
    Abstract: 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: Application
    Filed: May 27, 2011
    Publication date: May 16, 2013
    Applicant: GRAPHEA, INC.
    Inventors: Christopher W. Bielawski, Daniel R. Dreyer, Hong-Peng Jia
  • Patent number: 8372982
    Abstract: 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: Grant
    Filed: February 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Patent number: 8324401
    Abstract: 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: Grant
    Filed: August 18, 2009
    Date of Patent: December 4, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang
  • Patent number: 8283383
    Abstract: 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: Grant
    Filed: June 22, 2010
    Date of Patent: October 9, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8258162
    Abstract: 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: Grant
    Filed: June 26, 2009
    Date of Patent: September 4, 2012
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
  • Publication number: 20120203012
    Abstract: 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: Application
    Filed: December 16, 2010
    Publication date: August 9, 2012
    Applicant: CANON KABUSHIKI KAISHA
    Inventor: Terunobu Saitoh
  • Patent number: 8158675
    Abstract: 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: Grant
    Filed: July 24, 2009
    Date of Patent: April 17, 2012
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Patent number: 8133910
    Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: March 13, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
  • Patent number: 8039496
    Abstract: 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: Grant
    Filed: January 22, 2008
    Date of Patent: October 18, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 8030327
    Abstract: 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: Grant
    Filed: November 7, 2005
    Date of Patent: October 4, 2011
    Assignee: MDS K.K.
    Inventors: Yoshiyuki Sato, Hideki Kurihara, Kaori Kamijo, Yu Onozaki, Toshiaki Tsujino, Tetsuya Sugimoto, Akiko Watanabe, Morihiro Mitsuya, Hideya Komatani
  • Patent number: 7935696
    Abstract: 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: Grant
    Filed: October 25, 2007
    Date of Patent: May 3, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Publication number: 20110098309
    Abstract: 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: Application
    Filed: July 11, 2008
    Publication date: April 28, 2011
    Applicant: 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: 7932283
    Abstract: 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: Grant
    Filed: April 5, 2007
    Date of Patent: April 26, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
  • Patent number: 7872146
    Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.
    Type: Grant
    Filed: May 6, 2006
    Date of Patent: January 18, 2011
    Assignee: Bayer CropScience AG
    Inventors: Thierry Eynard, Cécile Franc
  • Publication number: 20100233106
    Abstract: 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: Application
    Filed: March 28, 2008
    Publication date: September 16, 2010
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Benjamin L. Miller, Brian R. McNaughton, Peter Gareiss, Glynis Scott
  • Patent number: 7759502
    Abstract: 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: Grant
    Filed: October 29, 2007
    Date of Patent: July 20, 2010
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
  • Patent number: 7741479
    Abstract: 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: Grant
    Filed: December 7, 2005
    Date of Patent: June 22, 2010
    Assignee: 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
  • Patent number: 7691898
    Abstract: 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: Grant
    Filed: October 5, 2005
    Date of Patent: April 6, 2010
    Assignee: Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Tomiyama, Masayuki Yokota, Kazuo Tokuzaki, Ryoko Tomita
  • Publication number: 20100048648
    Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Application
    Filed: July 10, 2007
    Publication date: February 25, 2010
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
  • Patent number: 7659411
    Abstract: 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: Grant
    Filed: December 13, 2004
    Date of Patent: February 9, 2010
    Assignee: Sumitomo Seika Chemicals Co., Ltd.
    Inventors: Seiji Bando, Syuzo Satake, Hirokazu Kagano
  • Patent number: 7645799
    Abstract: 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: Grant
    Filed: November 7, 2008
    Date of Patent: January 12, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
  • Patent number: 7625944
    Abstract: 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: Grant
    Filed: July 30, 2007
    Date of Patent: December 1, 2009
    Assignee: Activesite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Publication number: 20090221832
    Abstract: 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: Application
    Filed: February 19, 2009
    Publication date: September 3, 2009
    Applicant: SALTIGO GMBH
    Inventors: Alain Cotte, Matthias Gotta, Lukas Goossen, Felix Rudolphi, Christoph Oppel, Nuria Rodriguez Garrido
  • Patent number: 7569600
    Abstract: 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: Grant
    Filed: May 15, 2006
    Date of Patent: August 4, 2009
    Assignee: ViroChem Pharma Inc.
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Patent number: 7553970
    Abstract: 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: Grant
    Filed: September 24, 2003
    Date of Patent: June 30, 2009
    Assignee: Lanxess Deutschland GmbH
    Inventors: Frank Berendes, Markus Eckert, Nils Brinkmann, Claus Dreisbach, Ruth Meissner, Rainhard Koch
  • Patent number: 7528274
    Abstract: 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: Grant
    Filed: July 25, 2002
    Date of Patent: May 5, 2009
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: John K. Inman, Atul Goel, Ettore Appella, Jim Turpin, Marco Schito
  • Patent number: 7476686
    Abstract: 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: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 7439372
    Abstract: A compound having a structure is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.
    Type: Grant
    Filed: May 1, 2007
    Date of Patent: October 21, 2008
    Assignee: Allergan, Inc.
    Inventors: Donde Yariv, Jeremiah H. Nguyen
  • Patent number: 7423030
    Abstract: 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: Grant
    Filed: October 11, 2006
    Date of Patent: September 9, 2008
    Assignee: Sanofi-Aventis
    Inventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
  • Patent number: 7396843
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: July 8, 2008
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Suzanne Joy Merrick, Ann Louise Walker
  • Patent number: 7388012
    Abstract: 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: Grant
    Filed: September 15, 2005
    Date of Patent: June 17, 2008
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Crew, An-Hu Li, Hanqing Dong, Tao Zhang
  • Patent number: 7381688
    Abstract: 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: Grant
    Filed: April 15, 2003
    Date of Patent: June 3, 2008
    Assignee: Bayer CropScience AG
    Inventors: Ralf Dunkel, Heiko Rieck, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
  • Patent number: 7365094
    Abstract: 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: Grant
    Filed: December 17, 2003
    Date of Patent: April 29, 2008
    Assignee: 4SC AG
    Inventors: Johann Leban, Stefan Tasler
  • Patent number: 7351841
    Abstract: 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: Grant
    Filed: December 6, 2005
    Date of Patent: April 1, 2008
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Patent number: 7342116
    Abstract: 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: Grant
    Filed: March 25, 2003
    Date of Patent: March 11, 2008
    Assignee: Koei Chemical Co., Ltd.
    Inventors: Yasuhiro Shiomi, Osamu Uno, Akio Ohta, Takeshi Sunakami
  • Patent number: 7312181
    Abstract: 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: Grant
    Filed: March 22, 2006
    Date of Patent: December 25, 2007
    Assignee: Cropsolution, Inc.
    Inventors: Shy-Fuh Lee, Vivian Du, Richard Anderson
  • Patent number: 7259172
    Abstract: 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: Grant
    Filed: July 2, 2004
    Date of Patent: August 21, 2007
    Assignee: MethylGene Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 7244763
    Abstract: 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: Grant
    Filed: February 6, 2004
    Date of Patent: July 17, 2007
    Assignee: Warner Lambert Company LLC
    Inventors: Larry D. Bratton, Xue-Min Cheng, Noe Erasga, Gary F. Filzen, Andrew G. Geyer, Chitase Lee, Bharat K. Trivedi, Paul C. Unangst
  • Patent number: 7183297
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: February 27, 2007
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Stephen Sean Flack, Dramane Ibrahim Lainé, Ann Louise Walker
  • Patent number: 7173060
    Abstract: The present invention relates to compounds of formula I, their pharmaceutically acceptable salts as well as their enantiomeric forms, diastereoisomers and racemates; the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds as inhibitors of histone deacetylase (HDAC) and therefore in the control or prevention of illnesses and disorders as mentioned above, or in the manufacture of corresponding pharmaceutical compositions.
    Type: Grant
    Filed: March 31, 2004
    Date of Patent: February 6, 2007
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner