Thiocarbazones Or Thiosemicarbazones (i.e., Hch=n-nh-c(=s)-hnh, Wherein Substitution May Be Made For Hydrogen Only) Patents (Class 564/19)
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Publication number: 20150093328Abstract: The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.Type: ApplicationFiled: April 17, 2013Publication date: April 2, 2015Applicant: MERRIMACK PHARMACEUTICALS, INC.Inventors: Daryl C. Drummond, Dmitri B. Kirpotin, Thomas Wickham, Bart S. Hendricks, Samuel Agresta, Helen Lee
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Patent number: 8765480Abstract: A method for recovering a metal, capable of recovering a metal easily without requiring the use of an organic medium, is provided. A first complex between a first chelating agent and a metal present in a sample is formed in a first mixture prepared by mixing the first chelating agent and the sample. Then, the first complex is recovered from the first mixture, and a second complex between the metal derived from the first complex and a second chelating agent is formed in a second mixture prepared by mixing the first complex and an aqueous solution of the second chelating agent. The aqueous solution is under the pH conditions where the first chelating agent can be insoluble in the aqueous solution. Then, a liquid fraction containing the second complex is recovered from the second mixture. Thus, the metal can be recovered.Type: GrantFiled: April 2, 2012Date of Patent: July 1, 2014Assignee: ARKRAY, Inc.Inventor: Yuka Shimomura
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Publication number: 20120251417Abstract: A method for recovering a metal, capable of recovering a metal easily without requiring the use of an organic medium, is provided. A complex between a chelating agent and a metal present in a sample is formed in a mixture prepared by mixing the chelating agent and the sample under pH conditions where the chelating agent can be insoluble in an aqueous medium. Then, the complex is recovered from the mixture, and further, the metal is recovered by dissolving the recovered complex in an aqueous medium under pH conditions that are different from the pH conditions where the chelating agent can be insoluble in an aqueous medium. By this method, a metal can be recovered easily without requiring the use of the use of an organic medium.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: ARKRAY, INC.Inventors: Yuka Shimomura, Mayumi Yamada
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Publication number: 20110305632Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).Type: ApplicationFiled: December 11, 2009Publication date: December 15, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Brett Michael Paterson
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Publication number: 20090203747Abstract: The present invention relates to the field of pharmacy, especially the treatment of neurodegenerative diseases. The invention specifically relates to a family of chemical compounds for which a neuroprotective activity has been demonstrated. Given that certain members of said family are novel compounds which have never been described, the invention relates to said novel products, the synthesis method thereof and certain novel intermediate synthesis products. The present invention further relates to compositions comprising the compounds of said family, and the use of said compounds as medicaments, especially for the preparation of a medicament for the treatment of neurodegenerative diseases.Type: ApplicationFiled: June 29, 2006Publication date: August 13, 2009Applicant: Trophos Parc Scientifique LuminyInventors: Corinne Chaimbault, Cyrille Drouot, Laure Jamot, Rebecca Pruss, Celine Simon
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Patent number: 7462689Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.Type: GrantFiled: November 24, 2003Date of Patent: December 9, 2008Assignee: Solulink Biosciences, Inc.Inventor: David A. Schwartz
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Patent number: 6649796Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.Type: GrantFiled: April 2, 2002Date of Patent: November 18, 2003Assignee: Chemagis, Ltd.Inventors: Vladimir Naddaka, Naim Menashe, Jael Lexner, Shadi Saeed, Joseph Kaspi, Ori Lerman
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Publication number: 20030114531Abstract: Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized.Type: ApplicationFiled: September 9, 2002Publication date: June 19, 2003Inventors: Farzad Kobarfard, Joel M. Kauffman
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Patent number: 6316467Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.Type: GrantFiled: November 16, 1998Date of Patent: November 13, 2001Assignee: American Home Products CorporationInventor: Thomas J. Commons
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Patent number: 6049006Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, tifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: April 11, 2000Assignee: American Home Products Corp.Inventors: Thomas Joseph Commons, Susan Christman
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Patent number: 6034272Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: March 7, 2000Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Susan Christman
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Patent number: 5843400Abstract: A diagnostic agent for hypoxia or mitochondrial dysfunction is disclosed, comprising a radioactive copper complex of a dithiosemicarbazone derivative or a radioactive copper complex of a diamine diol schiff base derivative. This agent has good transferability to the target tissue, reduction reaction affinity at a hypoxic site, high stability in a non-target site and rapidly disappears.Type: GrantFiled: January 11, 1996Date of Patent: December 1, 1998Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Yasuhisa Fujibayashi, Akira Yokoyama
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Patent number: 5571843Abstract: Therapeutic compounds having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR.sub.4 or R and R.sub.1 together denote .dbd.N--NH--CX--NHR.sub.5, .dbd.N--NH--CX--N(phenyl).sub.2, .dbd.N--NH--CX--NH--NH--R.sub.5, .dbd.N--NH--C(SCH.sub.3).dbd.N--R.sub.6 or .dbd.N--N.dbd.C(SCH.sub.3)--NH--R.sub.6 ; or (A, B)=(N--OH, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2 ; or (A, B)=(N--NH--CX--NHR.sub.5, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 ; or (A, B)=(N--OH, N--OH) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2.Type: GrantFiled: March 24, 1994Date of Patent: November 5, 1996Assignee: InnotheraInventors: Michel P. Cugnon de Sevricourt, Catherine G. Dacquet, Michel A. Finet, Florence J. Le Marquer, Max F. Robba, Norbert O. Tembo, Sylvie J. Yannic-Arnoult, Jean-Luc Torregrosa
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Patent number: 5461076Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: November 30, 1994Date of Patent: October 24, 1995Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5395855Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: March 28, 1994Date of Patent: March 7, 1995Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5118830Abstract: Triazolone derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently represents alkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkoxyalkyl, cycloalkylalkyl, cycloalkyl or represents aralkyl or aryl, which may be substitutedR.sup.2 also represents heteroaryl which may be substituted andX represents oxygen or sulphur,are obtained in good yields and at high purity by reacting an iso(thio)cyanate of the formulaX.dbd.C.dbd.N--R.sup.1if desired in the presence of a diluent, with an amionoguanidine of the formula ##STR2## in which R.sup.3 and R.sup.4, independently of one another, represent alkyl, or with acid adducts thereof to form a (thio)ureidoguanidine of the formula ##STR3## followed by condensation with elimination of dialkylamine (HNR.sup.3 R.sup.4) to form the triazolone derivative and new (thio)ureidoguanidines.Type: GrantFiled: April 17, 1991Date of Patent: June 2, 1992Assignee: Bayer AktiengesellschaftInventors: Kurt Findeisen, Markus Lindig
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Patent number: 4593027Abstract: 3-Aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives of the formula I ##STR1## and their physiologically tolerated acid addition and ammonium salts are described, as is a process for their preparation. The new compounds are chemotherapeutic agents and are active against protozoa, especially malaria plasmodia.Type: GrantFiled: October 11, 1983Date of Patent: June 3, 1986Assignee: Hoechst AktiengesellschaftInventors: Erhardt Winklemann, Walter Durckheimer, Wolfgang Raether
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Patent number: 4474984Abstract: A radioactive diagnostic agent which comprises a physiologically active substance and a radioactive metallic element combined with a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.3 alkyl or phenyl. The agent is characteristic in having a high stability even after being administered into a human body and showing the substantially the same behavior as the physiologically active substance itself in a human body.Type: GrantFiled: December 18, 1981Date of Patent: October 2, 1984Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Nobuo Ueda, Susumu Kondo, Masaaki Hazue
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Patent number: 4444743Abstract: A radioactive diagnostic agent for imaging of various organs, particularly of brain, which comprises a radioactive element such as .sup.Type: GrantFiled: September 15, 1981Date of Patent: April 24, 1984Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Akira Yokoyama, Hisashi Tanaka, Akira Yamada, Yasushi Arano
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Patent number: 4400517Abstract: 1,2,4-triazol-(5)-yl-[thio] phosphates are disclosed having the formula ##STR1## wherein R.sup.1 =alkyl with from 1 to 5 carbon atoms;R.sup.2 =OR.sup.1, R.sup.1, C.sub.6 H.sub.5, NHR.sup.1, N(R.sup.1).sub.2 ;X=O, SR.sup.3 =H, alkyl with from 1 to 5 carbon atoms, C.sub.6 H.sub.5, benzyl, alkenyl with from 2 to 6 carbon atoms, alkynyl with from 2 to 6 carbon atoms; andR.sup.4 =vinyl, halovinyl, polyhalovinyl, vinyl substituted with aryl groups, alkyl groups with from 1 to 4 carbon atoms, O-alkyl groups with from 1 to 4 carbon atoms, S-alkyl groups with from 1 to 4 carbon atoms; haloalkyl, acetyl, cyclohexenyl, benzoyl ##STR2## Also disclosed are 1,2,4-triazole intermediates having the formula ##STR3## wherein: X, R.sup.3 and R.sup.4 have the same meanings as indicated above. The phosphate esters are useful in combatting infestations of pests such as orthoptera, aphides, diptera, lepidoptera, coleoptera, acari, nematodes.Type: GrantFiled: January 29, 1980Date of Patent: August 23, 1983Assignee: Montedison S.p.A.Inventors: Franco Gozzo, Pier M. Boschi, Angelo Longoni