Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 548/966)
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Publication number: 20150057238Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.Type: ApplicationFiled: March 13, 2013Publication date: February 26, 2015Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
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Publication number: 20150025241Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Inventors: Woo Young KWAK, Heung Jae KIM, Jong Pil MIN, Tae Hyun YOON, Moohi YOO, Geun Gho LIM, Sun Ki CHANG
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Publication number: 20140364602Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.Type: ApplicationFiled: February 1, 2013Publication date: December 11, 2014Applicant: Gilead Sciences, Inc.Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
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Publication number: 20140187722Abstract: Described herein is a composition comprising at least one of: X—R—(Z)n wherein X is selected from: an aziridine amide, an aziridine urea, an isocyanate, an alcohol, an amine, an epoxy, or a sulfhydryl, R is a multifunctional organic group, and Z is selected from —N3 or —C?C—R?, wherein R? is a hydrogen or a monofunctional organic group and n is from one to about 10. Also, described are mixtures, curable polymeric compositions, and methods of making cured polymeric compositions.Type: ApplicationFiled: March 5, 2014Publication date: July 3, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: Anthony P. Manzara, Michael D. Crandall, Joshua R. Wurst
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Patent number: 8765982Abstract: A composition is provided that, when utilized in combination with warfarin, greatly improves the anticoagulant effects of warfarin in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K1 and has the general formula: where R1 and R4 are hydrogen or acyl, R2 is a saturated or unsaturated alkyl group with up to 6 carbons, and R3 is a saturated or unsaturated alkyl group with up to 20 carbons, or R2 and R3 are part of a cyclic or polycyclic ring system.Type: GrantFiled: September 30, 2010Date of Patent: July 1, 2014Assignee: Marshfield Clinic Health System, Inc.Inventors: David E. Lewis, Michael D. Caldwell
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Patent number: 8541572Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: September 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Patent number: 8507612Abstract: A crosslinkable, pre-adhesive composition is described comprising an acid-functional (meth)acrylate copolymer and an aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhesive articles.Type: GrantFiled: February 22, 2010Date of Patent: August 13, 2013Assignee: 3M Innovative Properties CompanyInventors: Peiwang Zhu, Zhong Chen, Babu N. Gaddam, Larry R. Krepski, Jingjing Ma, David B. Olson, Andrew Satrijo, Dong-Wei Zhu
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Publication number: 20130172388Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher EducationInventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
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Publication number: 20130023510Abstract: The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.Type: ApplicationFiled: May 25, 2012Publication date: January 24, 2013Applicant: Cytometix, Inc.Inventors: Lane Brostrom, John R. Falck
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Patent number: 8143375Abstract: The present invention relates to unprotected amino aldehydes and applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.Type: GrantFiled: October 22, 2007Date of Patent: March 27, 2012Assignee: The Governing Council of the University of TorontoInventors: Andrei K. Yudin, Ryan Hill
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Publication number: 20120010401Abstract: An industrially advantageous method for producing a 1,5-benzodiazepine compound is provided. A compound (5) is obtained according to the reaction scheme shown below, and this compound is used as an intermediate.Type: ApplicationFiled: March 29, 2010Publication date: January 12, 2012Applicant: Zeria Pharmaceutical Co., Ltd.Inventor: Masaru Terauchi
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Publication number: 20110224431Abstract: Provided herein are triazolium carbine catalysts useful for asymmetric hydration, fluorination, and deuteration, and processes for their preparation. Also provided are synthetic reactions in which these catalysts are used, in particular, in stereoselective formation of carbon-chlorine, carbon-hydrogen, carbon-fluorine, and carbon-deuterium bonds.Type: ApplicationFiled: February 3, 2011Publication date: September 15, 2011Applicant: COLORADO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Tomislav Rovis, Harit U. Vora
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Publication number: 20110112310Abstract: The invention relates to a process for making an aziridine. wherein an aldehyde, a nitroso compound and a Michael acceptor are reacted in the presence of an N-heterocyclic carbene (NHC) catalyst.Type: ApplicationFiled: January 30, 2009Publication date: May 12, 2011Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Pranab K. Patra, Jayasree Seayad, Yugen Zhang, Jackie Y. Ying
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Publication number: 20110105458Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.Type: ApplicationFiled: November 2, 2010Publication date: May 5, 2011Applicant: COMPLEXA, INC.Inventor: Bruce Branchaud
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Publication number: 20110054115Abstract: A pre-adhesive composition is described comprising an acid-functional (meth)acrylate copolymer and an acylaziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhesive articles.Type: ApplicationFiled: August 25, 2009Publication date: March 3, 2011Inventors: Belma Erdogan, Timothy D. Filiatrault, Maureen A. Kavanagh, Larry R. Krepski, Babu N. Gaddam
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Publication number: 20100317832Abstract: The present invention applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.Type: ApplicationFiled: October 22, 2007Publication date: December 16, 2010Inventors: Andrei K. Yudin, Ryan Hili
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Publication number: 20100227969Abstract: A crosslinkable, pre-adhesive composition is described comprising an acid-functional (meth)acrylate copolymer and an aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhesive articles.Type: ApplicationFiled: February 22, 2010Publication date: September 9, 2010Inventors: Peiwang Zhu, Zhong Chen, Babu N. Gaddam, Larry R. Krepski, Jingjing Ma, David B. Olson, Andrew Satrijo, Dong-Wei Zhu
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Publication number: 20100197688Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.Type: ApplicationFiled: May 28, 2009Publication date: August 5, 2010Inventors: Philippe G. Nantermet, Hamaka A. Rajapakse, Takeshi Sagara, John M. Sanders, Hong Zhu
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Publication number: 20090022664Abstract: The present invention relates to novel compounds suitable for or already radiolabelled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging.Type: ApplicationFiled: September 7, 2007Publication date: January 22, 2009Inventors: Ananth Srinivasan, Thomas Brumby, Timo Stellfeld, Keith Graham, Ulrike Voigtmann, Jessica Becaud, Linjing Mu
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Patent number: 7297692Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.Type: GrantFiled: August 3, 2006Date of Patent: November 20, 2007Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7268228Abstract: This invention relates to compounds of Formula I having an aziridine-2-carboxylic group and a menthol group, a process for preparing such compounds, a method for obtaining optically active aziridine-2-carboxylate derivatives by optical resolution of such compounds, and optically active aziridine-2-carboxylate derivatives obtained by the same method: wherein R1 is hydrogen; alkyl; cycloalkyl; 4-chlorophenyl; 4-methoxyphenyl; s-triazinyl or pyridinyl acyl; benzyl; hydrocarbon residue which may be substituted with a substituent selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl and 4-methoxyphenyl; 2,4-dimethoxyphenyl; substituted phenyl including (1R)-phenylethyl or (1S)-phenylethyl. Preferences are given to (1R)-phenylethyl and (1S)-phenylethyl. Menthol is selected from the group consisting of (+)-menthol and (?)-menthol.Type: GrantFiled: August 10, 2001Date of Patent: September 11, 2007Assignee: Imagene Co., Ltd.Inventors: Won Koo Lee, Chan Sun Park, Yeon Hwa Lim, Hyun J on Ha
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Patent number: 7109352Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.Type: GrantFiled: November 20, 2003Date of Patent: September 19, 2006Assignee: Kaneka CorporationInventors: Masanobu Sugawara, Akio Fujii, Kazumi Okuro, Yasuhiro Saka, Nobuo Nagashima, Kenji Inoue, Toshihiro Takeda, Koichi Kinoshita, Tadashi Moroshima, Yoshihide Fuse, Yasuyoshi Ueda
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Patent number: 7084120Abstract: Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.Type: GrantFiled: December 22, 2000Date of Patent: August 1, 2006Assignee: Probiodrug AGInventors: Hans-Ulrich Demuth, Dagmar Schlenzig, Torsten Hoffmann, Susanne Manhart
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6753431Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p (1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH (2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX (3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: June 1, 2001Date of Patent: June 22, 2004Assignee: Sumitomo Chemical Company LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Publication number: 20040030133Abstract: This invention relates to compounds of Formula I having an aziridine-2-carboxylic group and a menthol group, a process for preparing such compounds, a method for obtaining optically active aziridine-2-carboxylate derivatives by optical resolution of such compounds, and optically active aziridine-2-carboxylate derivatives obtained by the same method: 1Type: ApplicationFiled: July 30, 2003Publication date: February 12, 2004Inventors: Won Koo Lee, Chan Sun Park, Yeon Hwa Lim, Hyun Joon Ha
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Patent number: 6559323Abstract: A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I), wherein X is oxygen, NR4 or CHR5; R1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO2R8, CHR14NHR13, heterocyclic or cycloalkyl; or R1 and R2 join together to form a cycloalkyl ring; R3 and R10 are, independently, hydrogen, alkyl, aryl, heteroaromatic, CO2R8, R83Sn, CONR8R9, trialkylsilyl or triarylsilyl; R4 is an electron withdrawing group; R5 is alkyl, cycloalkyl, aryl, heteroaromatic, SO2R8, SO3R8, COR8, CO2R8, CONR8R9, PO(R8)2, PO(OR8)2 or CN; R8 and R9 are independently alkyl or aryl; and R13 and R14 are independently hydrogen, alkyl or aryl is provided. The process comprises degrading a compound of formula (II), (IIa), (IIb) or (IIc): wherein R3 and R10 are as defined above; Y is a cation; depending on the nature of Y, r is 1 or 2; and L is a suitable leaving group, to form a diazo compound.Type: GrantFiled: February 28, 2000Date of Patent: May 6, 2003Assignees: Avecia Limited, University of SheffieldInventors: John Richard Studley, Varinder Kumar Aggarwal
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Patent number: 6476236Abstract: The present invention provides a process for producing an aziridine-1-carboxamide of the formula: from an aziridine of the formula: and an isocyanate of the formula R5—N═C═O, where R1, R2, R3, R4 and R5 are those defined herein. In addition, the present invention also provides a process for producing a 4-imino-1,3-diazabicyclo[3.1.0]-hexan-2-one of the formula: from the aziridine-1-carboxamide of Formula I.Type: GrantFiled: November 26, 2001Date of Patent: November 5, 2002Assignee: The Arizona Board of RegentsInventors: William Remers, Bashyam Iyengar
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Patent number: 6423689Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: December 16, 1998Date of Patent: July 23, 2002Assignees: Warner-Lambert Company, Neurex CorporationInventors: Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
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Publication number: 20020049164Abstract: The present invention relates to prodrug compounds of inhibitors of dipeptidyl peptidase IV (DP IV), which prodrug compounds have the general formula A-B-C, whereinType: ApplicationFiled: December 22, 2000Publication date: April 25, 2002Inventors: Hans-Ulrich Demuth, Dagmar Schlenzig, Torsten Hoffmann, Susanne Manhart
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Patent number: 6297230Abstract: The present invention is directed to novel anti-cancer compounds of the formula. wherein X is CN, R4 is hydrogen or lower alkyl; and R5 is lower alkyl, lower cycloalkyl, alkenyl, alkynyl, aryl, monosubstituted aryl, disubstituted aryl, aryl lower alkyl, lower alkoxycarbonyl lower alkyl, or heterocyclic ring, with the proviso that when X is CN, and R4 is hydrogen, then R5 is not CH3, C6H5, or, p-nitrophenyl. R4, R5 and N taken together form a heterocyclic ring.Type: GrantFiled: April 10, 2000Date of Patent: October 2, 2001Assignee: Amplimed, Inc.Inventors: William A. Remers, Evan M. Hersh, Robert T. Dorr, Bhashyam Iyengar
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Publication number: 20010020092Abstract: The present invention relates to a compound of the formula (I) 1Type: ApplicationFiled: December 7, 2000Publication date: September 6, 2001Inventors: Mark James Ford, Jan Vermehren
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Patent number: 6258960Abstract: The present invention relates to the synthesis of chiral cis-aziridines (IIIa and IIIb) by reacting an imine (I) with a diazo compound (II) in the presence of a chiral vaulted biary-Lewis Acid complex as shown below:Type: GrantFiled: March 17, 2000Date of Patent: July 10, 2001Assignee: Arch Development CorporationInventors: Jon Antilla, William D. Wulff
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Patent number: 6201133Abstract: Disclosed are compound of formula I wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl; R2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl); R3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C2-C7-alkyl interrupted by S, SO, SO2, O or N—R5; R4 represents hydrogen or acyl; R5 represents hydrogen, lower alkyl, aryl-lower alkyl, acyl, or (lower alkyl, aryl or aryl-lower alkyl)-sulfonyl; A together with the carbon to which it is attached forms a ring and reprType: GrantFiled: November 8, 1999Date of Patent: March 13, 2001Assignee: Novartis AGInventor: Cynthia A. Fink
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Patent number: 6177594Abstract: Benzamides of the formula I: wherein R1 and R2 independently of one another are each alkyl having 1-6 C atoms, or R1 and R2 together are alkylene, and their salts, are suitable as intermediates in the synthesis of drugs.Type: GrantFiled: December 9, 1998Date of Patent: January 23, 2001Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Andreas W{umlaut over (a)}chtler, Margit Stern, Volker Reiffenrath
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Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 5668128Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 and Q are independently an optionally esterified or amidated carboxyl group; R.sub.2 is hydrogen, an acyl group or an optionally substituted hydrocarbon residue; X is a divalent hydrocarbon residue which may be substituted; or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as agents for inhibiting thiol protease.Type: GrantFiled: September 5, 1995Date of Patent: September 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigetoshi Tsubotani, Masayuki Takizawa, Mikio Shirasaki, Junji Mizoguchi, Yoshiaki Shimizu
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Patent number: 5633239Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit outstanding effects on the cardiovascular system.Type: GrantFiled: February 16, 1996Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz G ogelein, Joachim Kaiser
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Patent number: 5025005Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: July 23, 1990Date of Patent: June 18, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
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Patent number: 4988688Abstract: 4-(N-Substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: August 2, 1989Date of Patent: January 29, 1991Assignee: Warner-Lambert CompanyInventors: Jeffrey A. Kester, Walter H. Moos, Anthony J. Thomas
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4935527Abstract: Alkaline earth metal salts of aziridine-2-carboxylic acid, typically Ca salt, are produced by a reaction of a 2,3-dihalopropionic acid derivative or an .alpha.-haloacrylic acid derivative with an aqueous ammonia in the presence of an alkaline earth metal hydroxide, typically Ca(OH).sub.2.Salts of aziridine-2-carboxylic acid are recovered from such a reaction product as referred to above by a liquid chromatographic technique in which a weak or weakened cation exchanger is utilized.Type: GrantFiled: December 23, 1988Date of Patent: June 19, 1990Assignee: Research Association for Utilization of Light OilInventors: Sadao Kitagawa, Takashi Yokoi, Mitsumasa Kaitoh
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Patent number: 4900841Abstract: This invention relates to a process for the preparation of substituted sulfonamidobenzamides which compounds are known antiarrhythmic agents and to the novel N-acylaziridine employed therein.Type: GrantFiled: April 20, 1987Date of Patent: February 13, 1990Assignee: Schering A.G.Inventor: Thomas K. Morgan, Jr.
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Patent number: 4795627Abstract: The present invention describes novel tritium labelled nitrogen mustard type compounds, and their aziridinium type analog, and a process for the production of same. The compounds are of value in medical research and development and also as active ingredients of pharmaceutical compositions. The compounds can be used to develop analogs of human disease states and can also be used to evaluate the mechanism of neurotransmitter regulation and function, both in vitro and in vivo.Type: GrantFiled: October 18, 1984Date of Patent: January 3, 1989Assignee: University of PittsburghInventors: Abraham Fisher, Israel Hanin, Donald J. Abraham
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Patent number: 4791133Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.Type: GrantFiled: June 26, 1987Date of Patent: December 13, 1988Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 4788287Abstract: A high performance water and oil repellant composed of a compound comprising at least two terminal segments and an intermediate segment connecting the terminal segments and having a molecular weight of from 800 to 20,000, each terminal segment containing at least one polyfluoroalkyl group connected by a --CONH-- linking group, said intermediate segment being a urethane oligomer containing at least two --CONH-- linking groups in one molecule, and said terminal segments and intermediate segment being connected by a --CONH-- linking group.Type: GrantFiled: September 3, 1986Date of Patent: November 29, 1988Assignee: Asahi Glass Company Ltd.Inventors: Masashi Matsuo, Masayuki Tamura, Katsuji Ito
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Patent number: 4737518Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: September 12, 1986Date of Patent: April 12, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
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Patent number: 4708954Abstract: Pharmaceutical compositions containing an oxaluric acid derivative of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen; an alkyl group or a cycloalkyl group; or R.sub.1 and R.sub.2 are joined to form a heterocyclic ring with the nitrogen atom to which they are both attached; and R.sub.3 is hydrogen or an alkyl group. These compounds have excellent hypoglycemic effects with low toxcicity and safety.Type: GrantFiled: February 7, 1986Date of Patent: November 24, 1987Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kazuharu Ienaga, Ko Nakamura, Akira Ishii
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Patent number: 4696760Abstract: A method for the production of an aqueous dispersion of a water insoluble N-substituted N',N'-alkylene urea having the general formula I: ##STR1## wherein R.sup.1 denotes alkyl having 6 to 20 carbon atoms, phenyl or ##STR2## in case of m=1, or R.sup.1 denotes alkylene having 6 to 20 carbon atoms, phenylene or ##STR3## in case of m=2, where X denotes H, CH.sub.3 or OCH.sub.3 and n is 0 or 1, R.sup.2 denotes H or CH.sub.3, R.sup.3 denotes H, CH.sub.3 or C.sub.2 H.sub.5 and R.sup.4 denotes H or CH.sub.3, by the reaction of an alkylene imine having 2 to 4 carbon atoms with an isocyanate represented by the general formula II:R-NCO (II)wherein R denotes an alkyl having 6 to 20 carbon atoms, ##STR4## wherein X and n are the same as above in the presence of at least one surface active agent selected from the group consisting of anionic surface active agents and nonionic surface active agents under vigorous stirring.Type: GrantFiled: December 5, 1984Date of Patent: September 29, 1987Assignee: Nippon Shokubai Kagaku Kogyo Co., Ltd.Inventors: Yutaka Morimoto, Minoru Saotome, Atsushi Komai