Spiro Patents (Class 548/958)
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Patent number: 8609858Abstract: The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (?-methylene-?-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 ?M to 93 ?M. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the ?,?-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.Type: GrantFiled: March 5, 2009Date of Patent: December 17, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Mahabalarao Sampath Kumar Halmuthur, Ajit Kumar Saxena, Subhash Chandra Taneja, Shashank Kumar Singh, Vijay Kumar Sethi, Naveed Ahmed Qazi, Sanghapal Damodhar Sawant, Mahendhar Reddy Doma, Abid Hussain Banday, Monika Verma, Ghularn Nabi Qazi
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Publication number: 20110201661Abstract: The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (?-methylene-?-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 ?M to 93 ?M. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the ?,?-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.Type: ApplicationFiled: March 5, 2009Publication date: August 18, 2011Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Mahabalarao Sampath Kumar Halmuthur, Ajit Kumar Saxena, Subhash Chandra Taneja, Shashank Kumar Singh, Vijay Kumar Sethi, Naveed Ahmed Qazi, Sanghapal Damodhar Sawant, Mahendhar Reddy Doma, Abid Hussain Banday, Monika Verma, Ghularn Nabi Qazi
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Publication number: 20090209568Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to spiro[benzopyran] or spiro[benzofuran] derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: April 23, 2007Publication date: August 20, 2009Inventor: Bernhard Wünsch
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Publication number: 20040204394Abstract: Triptolide analogues are described, including compounds of Formula I: 1Type: ApplicationFiled: April 11, 2003Publication date: October 14, 2004Applicant: Aderis Pharmaceuticals, Inc.Inventor: Gevork Minaskanian
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Patent number: 5686484Abstract: Compounds of formula (I): ##STR1## and of formula (I).sub.w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen atoms, halogen atoms, alkyl groups having from 1 to 4 carbon atoms, and alkoxy groups having from 1 to 4 carbon atoms;R.sup.1, R.sub.w.sup.1 and R.sub.w.sup.2 are, for example, hydrogen, halogen, cyano, nitro, optically substituted alkyl, alkoxy or alkoxyalkoxy;X or X.sub.w is hydroxy, alkanoyloxy, substituted alkanoyloxy or hydroxyimino; R.sup.3.sub.w and R.sup.4.sub.w are each hydrogen, alkyl or alkoxy; R.sup.5 and R.sup.5.sub.w are methyl, ethyl, isopropyl or sec-butyl; and salts thereof have valuable anthelmintic, acaricidal and insecticidal activities.Type: GrantFiled: March 1, 1995Date of Patent: November 11, 1997Assignees: Sankyo Co., Ltd., Ciba-Geigy CorporationInventors: Yasuhiro Morisawa, Akio Saito, Satoru Naito, Toshimitsu Toyama, Susumu Kaneko, Louis-Pierre Molleyres, Jean-Claude Gehret
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Patent number: 5545659Abstract: Novel 1-(2-,3- or 4-hydroxylaminobenzensulfonyl-1a,2,6,6 a-tetrahydro-1H,4H-[1,3]-dioxepino[5,6-b]azirines with hypoglycemic activity are prepared by selective reduction of appropriate 1-(2-,3- or 4-nitrobenzenesulfonyl) derivatives.Type: GrantFiled: February 21, 1995Date of Patent: August 13, 1996Assignee: PLIVA farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventors: Miljenko Dumi c, Darko Fili c, Mladen Vinkovi c, Blanka Jamnicky, Mirela E skinja
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Patent number: 5442066Abstract: Novel bleach catalysts, a method for bleaching substrates using these catalysts and detergent compositions containing same are reported. The bleaches are of the quaternary oxaziridinium salt type. Substrates such as fabrics may be bleached in an aqueous solution containing the quaternary oxaziridinium salt.Type: GrantFiled: September 2, 1994Date of Patent: August 15, 1995Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Stephen A. Madison, Janet L. Coope
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Patent number: 5428034Abstract: Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.Type: GrantFiled: June 9, 1993Date of Patent: June 27, 1995Assignees: Sankyo Co., Ltd., Ciba-Geigy CorporationInventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
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Patent number: 5286744Abstract: Starting from cis-2-butene-1,4-diol, via the 4,7-dihydro-1,3-dioxepin and trans-6-acylamino-5-chloro-1,3-dioxepans the novel tetrahydro-[1,3]-dioxepino[5,6-b]-azirines were synthesized, and therefrom the novel hypoglycaemically active N-sulfonyl-tetrahydro-[1,3]-dioxepino[5,6-b]azirines. The inventive compounds are valuable intermediates in the synthesis of other, biologically active substances.Type: GrantFiled: August 20, 1992Date of Patent: February 15, 1994Assignees: Pliva Handels GmbH, PlivaInventors: Miljenko Dumic, Darko Filic, Mladen Vinkovi, Blanka Jamnicky
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Patent number: 5142054Abstract: Disclosed are new 1,3-dioxenones having the formulae ##STR1## in an optically pure state, a process for preparing same and the use thereof.Type: GrantFiled: February 12, 1991Date of Patent: August 25, 1992Assignee: Studiengesellschaft Kohle mbHInventors: Kurt Schaffner, Martin Demuth
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 4900830Abstract: The invention thus provides a process for obtaining the preferential replacement by isotopes, of at least one of the hydrogen atoms selected from the group consisting of those attached to the .alpha.- or .alpha.'-carbon atoms in a compound containing the structural moiety (I) ##STR1## which comprises the steps of oxidizing the compound to the corresponding sulfoxide or sulfone which contains the corresponding structural moiety (II) ##STR2## wherein in the sulfoxide n is 1 and in the sulfone n is 2, effecting the isotopic replacement by a known method of said at least one hydrogen atom, and reducing the resultant isotope-labelled sulfoxide or sulfone to the correspondingly labelled compound containing the structural moiety (I).Type: GrantFiled: October 28, 1987Date of Patent: February 13, 1990Assignee: Israel Institute for Biological ResearchInventors: Abraham Fisher, Ishai Karton
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Patent number: 4725608Abstract: New semicarbazide derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; orR.sup.1 and R.sup.2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,R.sup.Type: GrantFiled: November 21, 1984Date of Patent: February 16, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Osamu Nakaguchi, Norihiko Shimazaki, Yoshio Kawai, Masashi Hashimoto, Michie Nakatuka