Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Cyano Group By Nonionic Bonding Patents (Class 558/404)
Two carbons bonded directly to the carbon of the -c(=x)- group (e.g., ketones, etc.) (Class 558/405)
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Patent number: 9029401Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: GrantFiled: February 14, 2012Date of Patent: May 12, 2015Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20150044149Abstract: The present disclosure relates, according to some embodiments, to molecules, including substituted propenoic amides (e.g., aryl substituted propenoic amides), that may receive excited state energy from light-absorbing molecules. According to some embodiments, the present disclosure relates to molecules, including substituted propenoic amides (e.g., aryl substituted propenoic amides), that may quench, dissipate, and/or otherwise resolve excited state energy (e.g., as heat).Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Craig Bonda, Shengkui Hu, Gary A. Neudahl, Stephen O'Rourke, Stephen J. Semlow, Zhihui Zhang
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Publication number: 20140107368Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: December 11, 2013Publication date: April 17, 2014Applicant: Mitsui Chemicals Agro, Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20140088156Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: ApplicationFiled: February 14, 2012Publication date: March 27, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Patent number: 8633228Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: GrantFiled: June 29, 2009Date of Patent: January 21, 2014Assignee: Mitsui Chemicals Agro, Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20130216486Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.Type: ApplicationFiled: March 20, 2013Publication date: August 22, 2013Applicant: The Procter & Gamble CompanyInventor: The Procter & Gamble Company
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Publication number: 20130123356Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof,Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Applicant: UNIVERSITY COLLEGE LONDONInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
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Publication number: 20130109750Abstract: The invention relates to novel arylamide derivatives having formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, where R1-R11, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.Type: ApplicationFiled: July 14, 2011Publication date: May 2, 2013Applicant: MEDEIA THERAPEUTICS LTDInventors: Jari Ratilainen, Milla Koistinaho, Anu Muona
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Publication number: 20110136878Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: Mitsui Chemicals Agro., Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20110104765Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.Type: ApplicationFiled: October 29, 2010Publication date: May 5, 2011Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 7893110Abstract: The present invention refers to cooling compounds of formula I wherein R1, R2, R3, X, Y, Z, and m have the same meaning as given in the specification. The present invention refers furthermore to a process for their production and to product compositions comprising them.Type: GrantFiled: February 27, 2006Date of Patent: February 22, 2011Assignee: Givaudan S.A.Inventors: Christophe C. Galopin, Stefan Michael Furrer, Lori W. Tigani, Jay Patrick Slack, Pablo Victor Krawec, Lucienne Cole
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Publication number: 20100240712Abstract: Novel aromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, R5, G1, G2, Q1, Q2, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: ApplicationFiled: October 13, 2008Publication date: September 23, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Denis Stoller, Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
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Publication number: 20100185000Abstract: The present invention relates to titanium catalysts for asymmetric synthesis reactions produced by bringing a reaction mixture obtained by contacting water and a titanium alkoxide into contact with an optically active ligand represented by the general formula (a), wherein R1, R2, R3, and R4 are independently a hydrogen atom, an alkyl group, or the like, and A* represents a group with two or more carbon atoms having an asymmetric carbon atom or axial asymmetry. The invention further relates to a process for asymmetric cyanation of imines, wherein the process comprises reacting an imine with a cyanating agent in the presence of the titanium catalyst.Type: ApplicationFiled: September 28, 2007Publication date: July 22, 2010Applicants: Agency for Science, Technology and Research, Mitsui Chemicals Inc.Inventors: Abdul Majeed Seayad, Christina Chai, Balamurugan Ramalingam, Takushi Nagata, Kazuhiko Yoshinaga
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Patent number: 7547701Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: September 17, 2004Date of Patent: June 16, 2009Assignee: Virobay, Inc.Inventors: John O. Link, Craig J. Mossman, Soon H. Woo, Sheila M. Zipfel
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Patent number: 7468453Abstract: A process for the preparation of gamma-cyahlothrin comprising a) chlorinating 1R cis-Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid to give 1R cis-Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid chloride; b) esterifying 1R cis-Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid chloride with 3-phenoxy benzaldehyde in the presence of a source of cyanide to form a diastereoisomeric mixture of cyhalothrin isomers and c) epimerising the diastereoisomeric mixture under conditions in which the least soluble diastereoisomer crystallises from solution.Type: GrantFiled: December 9, 2003Date of Patent: December 23, 2008Assignee: Syngenta LimitedInventors: Stephen Martin Brown, Brian David Gott
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Patent number: 7459585Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 24, 2005Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Patent number: 7407959Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: November 18, 2005Date of Patent: August 5, 2008Assignee: Merck Frosst Canada & Co.Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
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Publication number: 20080176945Abstract: The present invention refers to cooling compounds of formula I wherein R1, R2, R3, X, Y, Z, and m have the same meaning as given in the specification. The present invention refers furthermore to a process for their production and to product compositions comprising them.Type: ApplicationFiled: February 27, 2006Publication date: July 24, 2008Inventors: Christophe C. Galopin, Stefan Michael Furrer, Lori W. Tigani, Jay Patrick Slack, Pablo Victor Krawec, Lucienne Cole
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Patent number: 7375134Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: February 28, 2003Date of Patent: May 20, 2008Assignees: Axys Pharmaceuticals, Inc., Merck Frosst Canada & Co.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien
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Publication number: 20080114062Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C?—C—(CH2)2CO2H, meta-C?—C—(CH2)2OH, meta-C?C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C?Type: ApplicationFiled: February 21, 2005Publication date: May 15, 2008Applicant: UNIVERSITY COLLEGE LONDON Wolfson Institute for Biomedical ResearchInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
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Publication number: 20070238710Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Applicant: ARDEA BIOSCIENCESInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
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Publication number: 20040171881Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: November 8, 2002Publication date: September 2, 2004Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, James Beck, Andrea Gailunas, John Freskos, John Mickelson, Lakshman Samala, Jennifer Sealy, Ruth TenBrink, Lawrence Fang, Roy Hom
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Publication number: 20040062726Abstract: Derivatives of fluorene, including ester derivatives of cyano(9H-fluoren-9-ylidene) acetic acid, and sunscreen compositions including a mixture of a photoactive compound and an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid are disclosed herein. Also disclosed are methods for terminating a polymer chain with an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid and methods of filtering out ultra-violet light from a substrate by the use of one or more such derivatives.Type: ApplicationFiled: June 10, 2003Publication date: April 1, 2004Inventors: Craig A. Bonda, Anna B. Pavlovic
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Patent number: 6703379Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 12, 2001Date of Patent: March 9, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Patent number: 6699904Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: February 14, 2002Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Cheryl M. Hayward, David A. Perry
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Publication number: 20030149146Abstract: A yellow colorant comprising a chromophore having at least one poly(oxy-C2-C4-alkylene) chain attached to an aromatic methine backbone having at least one cyanoester moiety attached thereto is provided. The ester portion must include a C1-C8 (such as ethyl, butyl, hexyl, or ethyl-hexyl) pendant group and the poly(oxyalkylene) chain must be at most 10 monomers and at least 3 monomers, with ethylene oxide as the capping group. Such a specific group of coloring agents provides the best overall yellow colorations or effects (either alone or in blends with other coloring agents, particularly at low color loadings) as well as the best overall low extraction levels when present within clear polyester (such as polyethylene terephthalate, for example), when compared to all other known polymeric yellow colorants for the same end-use. Compositions and articles comprising such colorants are provided as well as methods for producing such inventive colorants.Type: ApplicationFiled: February 6, 2003Publication date: August 7, 2003Inventor: Eric B. Stephens
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Patent number: 6596878Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.Type: GrantFiled: September 18, 2001Date of Patent: July 22, 2003Assignees: Yissum Research & Development Company of the Hebrew University, Sugen, Inc.Inventors: Hui Chen, Aviv Gazit, Alexander Levitzki, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
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Patent number: 6465657Abstract: There is disclosed a method of preparing a refined organic compound, comprising the steps of adding water to an organic reaction mixture and mixing them, and then subjecting the mixture to filtration processing using a filter, to separate an organic phase from an aqueous phase, and then isolating the intended organic compound from said organic phase. The method enables highly precise removal of a water-easily soluble compound from an organic reaction mixture, and it further enables obtaining the intended synthesized organic compound in high yield with a high quality.Type: GrantFiled: March 30, 2000Date of Patent: October 15, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Masayuki Goto, Noboru Tanaka
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Patent number: 6294573Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: January 27, 2000Date of Patent: September 25, 2001Assignee: Abbott LaboratoriesInventors: Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Joseph F. Dellaria, Jr., Alan S. Florjancic, Jianchun Gong, Yan Guo, Howard R. Heyman, James H. Holms, Michael R. Michaelides, Jamie R. Stacey, Douglas H. Steinman, Carol K. Wada, Lianhong Xu
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Patent number: 6288261Abstract: Compounds having the formula and pharmaceutically acceptable salts and prodrugs thereof are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: December 14, 1999Date of Patent: September 11, 2001Assignee: Abbott LaboratoriesInventors: David J. Augeri, David A. Betebenner, Richard Craig, Steven K. Davidsen, Stephen W. Fesik, Jamie R. Giesler-Stacey, Yan Guo, Philip J. Hajduk, Michael R. Michaelides, David G. Nettesheim
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Patent number: 6194463Abstract: &agr;-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is a number zero or one; R1 to R7 are as defined herein; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other a number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; X is hydrogen, in which case p and q must have the value zero; phenyl, unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkenyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalkoxy, C1-C6alkylthio, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6or by C1-C6alkoxy, cyano, —COOR17; —COR18 or a group (b) wherein R17 and R21 are each independently of the otherType: GrantFiled: August 24, 1999Date of Patent: February 27, 2001Assignee: Novartis Crop Protection, Inc.Inventor: Martin Zeller
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Patent number: 6083986Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: July 15, 1997Date of Patent: July 4, 2000Assignees: ICAgen, Inc., Eli Lilly & CompanyInventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
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Patent number: 5968977Abstract: The present invention is directed to a ketonitrile derivative represented by the following formula (1): ##STR1## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group; each of R.sup.2, R.sup.3, R.sup.4, and R.sup.Type: GrantFiled: December 29, 1997Date of Patent: October 19, 1999Assignee: Tokuyama CorporationInventors: Shozo Kato, Hidenobu Itahana, Masao Yamaguchi, Makiko Furuki, Seiji Nagata, Toshio Kitajima
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Patent number: 5932766Abstract: The present invention discloses a process for the preparation of a compound having formula 4: ##STR1## The process comprises the step of reacting an enolate having the formula: ##STR2## with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is an alkali metal. R.sub.6 and R.sub.7 are each hydrogen or are independently selected from ##STR3## wherein R.sub.a and R.sub.b are independently selected from hydrogen, lower alkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, lower alkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR4## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from lower alkyl, trifluoromethyl, alkoxy and halo. Alternatively, R.sub.6 is as defined above and R.sub.7 is R.sub.12 OC(O)-- wherein R.sub.12 is benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded form ##STR5## wherein R.sub.Type: GrantFiled: May 30, 1997Date of Patent: August 3, 1999Assignee: Abbott LaboratoriesInventors: Anthony R. Haight, Timothy L. Stuk, Jerome A. Menzia
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Patent number: 5925676Abstract: An ester compound represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represent a C.sub.1 -C.sub.6 alkyl group, or other specified groups, which may be optionally substituted with one or more halogen atoms; and R.sub.3 represents a pyrethroid acid residue (a group resulting from elimination of the carboxyl group from pyrethroid acid), and a pesticidal composition containing the ester compound as an active ingredient.Type: GrantFiled: September 11, 1997Date of Patent: July 20, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Tomonori Iwasaki, Kazunori Tsushima, Masayo Sugano
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Patent number: 5888481Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).Type: GrantFiled: September 29, 1995Date of Patent: March 30, 1999Assignee: AlliedSignal Inc.Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind
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Patent number: 5859279Abstract: A process for the preparation of a compound of formula (VI), optionally in enantiomerically-enriched form (R or S), comprises chemoselective reduction of a novel compound of formula (V), wherein Ar.sup.1 and Ar.sup.2 are independently selected from optionally-substituted aromatic or heteroaromatic groups having upto 20 C atoms, Ak is C.sub.1-20 alkyl, and R is H or C.sub.1-20 alkyl.Type: GrantFiled: September 10, 1997Date of Patent: January 12, 1999Assignee: Darwin Discovery LimitedInventors: Robin Mark Bannister, Graham Evans
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Patent number: 5847147Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0, 1, 2 or 3;Z is CN, CO-A or CS-A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R.sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.Type: GrantFiled: March 13, 1998Date of Patent: December 8, 1998Assignee: Novartis Corp.Inventors: Walter Kunz, Beat Jau
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Patent number: 5750726Abstract: There is provided a single step procedure to prepare 2-aryl-5-perfluoroalkylpyrrole derivatives directly from the perfluoroacetylated Strecker reaction product. Said pyrrole derivatives are insecticidal and also useful as precursors to other insecticidal arylpyrrole compounds.Further provided are amide nitrile intermediates, useful in the preparation of insecticidal arylpyrrole compounds.Type: GrantFiled: June 27, 1997Date of Patent: May 12, 1998Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5696161Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Br, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: May 13, 1996Date of Patent: December 9, 1997Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5650511Abstract: Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.Type: GrantFiled: December 12, 1995Date of Patent: July 22, 1997Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Arthur J. Elliott, David A. Walsh
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Patent number: 5637770Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.Type: GrantFiled: May 31, 1995Date of Patent: June 10, 1997Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hirofumi Terasawa, Akio Ejima, Satoru Ohsuki, Kouichi Uoto
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Patent number: 5563278Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 30, 1995Date of Patent: October 8, 1996Assignee: Eli Lilly and CompanyInventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
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Patent number: 5545664Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.C--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 --C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Dr, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: March 23, 1995Date of Patent: August 13, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5530014Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.Type: GrantFiled: August 18, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Hartmund Wollweber, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5446194Abstract: A compound according to formula 1 ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, carbamoyl which is substituted by an alkyl of 1 to 4 carbon atoms, alkylcarbonyl of 2 to 5 carbon atoms or phenyl carbonyl, X represents halogen nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms or which is substituted with hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable esters and salts thereof, and a pharmaceutically acceptable carrier therefor, as well as pharmaceutical compositions containing said compounds as COMT inhibitors.Type: GrantFiled: September 16, 1993Date of Patent: August 29, 1995Assignee: Orion-yhtyma OyInventors: Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo J. Pystynen
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Patent number: 5430060Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: September 15, 1993Date of Patent: July 4, 1995Assignee: Zeneca LimitedInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
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Patent number: 5405987Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.Type: GrantFiled: March 28, 1991Date of Patent: April 11, 1995Assignee: Hoechst Celanese CorporationInventors: Varadaraj Elango, Donald R. Larkin, John R. Fritch, Michael P. Bodman, Werner H. Mueller, Bernard F. Gupton, John C. Saukaitis
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles