DERIVADOS DE EPOTILONES, SU PREPARACION Y UTILIZACION
Derivado de epotilón de la fórmula 1 significando R = H o alquilo C1-4; R1, R2 = H, alquilo C1-6, acilo C1-6, benzoílo, tri-alquil C1-4-sililo, bencilo o fenilo; bencilo o fenilo sustituido con alcoxi C1-6, alquilo C6, hidroxi y halógeno; y realizándose, en el caso de los grupos alquilo y acilo cont...
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| creator | HOFLE, GERHARD, DR KIFFE, MICHAEL |
| description | Derivado de epotilón de la fórmula 1 significando R = H o alquilo C1-4; R1, R2 = H, alquilo C1-6, acilo C1-6, benzoílo, tri-alquil C1-4-sililo, bencilo o fenilo; bencilo o fenilo sustituido con alcoxi C1-6, alquilo C6, hidroxi y halógeno; y realizándose, en el caso de los grupos alquilo y acilo contenidos en los radicales, que se trata de radicales lineales o ramificados; y formando Y y Z uno de los enlaces C-C de un doble enlace C=C.
Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O; (b) R' = C(=X)Me or CH(OX')Me; A = H; B = OR1; and R" = R2; (c) R' = Q; and A+B = bond; X = O, NOR4, N-NR4R5 or N-NHCONR4R5; X' = H, 1-18C alkyl, 1-18C acyl, benzyl, benzoyl or cinnamoyl; Q = a group of formula (i); and R1-R5 = H, 1-6C alkyl, 1-6C acyl, benzoyl, 1-4C trialkylsilyl, or benzyl or phenyl (both optionally substituted by 1-6C alkoxy, 6C alkyl, OH and halo); or R4+R5 = 2-6C alkylene. Epothilone A and B are excluded. Also claimed is the production of epothilone A or B and/or their 12,13-bis-epi derivatives comprising the epoxidation of epothilone C (for A or derivatives) or D (for B or derivatives) especially using dimethyldioxirane or a peracid. |
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Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O; (b) R' = C(=X)Me or CH(OX')Me; A = H; B = OR1; and R" = R2; (c) R' = Q; and A+B = bond; X = O, NOR4, N-NR4R5 or N-NHCONR4R5; X' = H, 1-18C alkyl, 1-18C acyl, benzyl, benzoyl or cinnamoyl; Q = a group of formula (i); and R1-R5 = H, 1-6C alkyl, 1-6C acyl, benzoyl, 1-4C trialkylsilyl, or benzyl or phenyl (both optionally substituted by 1-6C alkoxy, 6C alkyl, OH and halo); or R4+R5 = 2-6C alkylene. Epothilone A and B are excluded. Also claimed is the production of epothilone A or B and/or their 12,13-bis-epi derivatives comprising the epoxidation of epothilone C (for A or derivatives) or D (for B or derivatives) especially using dimethyldioxirane or a peracid.</description><edition>7</edition><language>spa</language><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM ; AGRICULTURE ; ANIMAL HUSBANDRY ; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES ; CHEMISTRY ; FISHING ; FORESTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HUNTING ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PEST REPELLANTS OR ATTRACTANTS ; PLANT GROWTH REGULATORS ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS ; TRAPPING</subject><creationdate>2004</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20041116&DB=EPODOC&CC=ES&NR=2218328T3$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20041116&DB=EPODOC&CC=ES&NR=2218328T3$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>HOFLE, GERHARD, DR</creatorcontrib><creatorcontrib>KIFFE, MICHAEL</creatorcontrib><title>DERIVADOS DE EPOTILONES, SU PREPARACION Y UTILIZACION</title><description>Derivado de epotilón de la fórmula 1 significando R = H o alquilo C1-4; R1, R2 = H, alquilo C1-6, acilo C1-6, benzoílo, tri-alquil C1-4-sililo, bencilo o fenilo; bencilo o fenilo sustituido con alcoxi C1-6, alquilo C6, hidroxi y halógeno; y realizándose, en el caso de los grupos alquilo y acilo contenidos en los radicales, que se trata de radicales lineales o ramificados; y formando Y y Z uno de los enlaces C-C de un doble enlace C=C.
Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O; (b) R' = C(=X)Me or CH(OX')Me; A = H; B = OR1; and R" = R2; (c) R' = Q; and A+B = bond; X = O, NOR4, N-NR4R5 or N-NHCONR4R5; X' = H, 1-18C alkyl, 1-18C acyl, benzyl, benzoyl or cinnamoyl; Q = a group of formula (i); and R1-R5 = H, 1-6C alkyl, 1-6C acyl, benzoyl, 1-4C trialkylsilyl, or benzyl or phenyl (both optionally substituted by 1-6C alkoxy, 6C alkyl, OH and halo); or R4+R5 = 2-6C alkylene. Epothilone A and B are excluded. Also claimed is the production of epothilone A or B and/or their 12,13-bis-epi derivatives comprising the epoxidation of epothilone C (for A or derivatives) or D (for B or derivatives) especially using dimethyldioxirane or a peracid.</description><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</subject><subject>AGRICULTURE</subject><subject>ANIMAL HUSBANDRY</subject><subject>BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES</subject><subject>CHEMISTRY</subject><subject>FISHING</subject><subject>FORESTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HUNTING</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PEST REPELLANTS OR ATTRACTANTS</subject><subject>PLANT GROWTH REGULATORS</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><subject>TRAPPING</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2004</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDB1cQ3yDHN08Q9WcHFVcA3wD_H08fdzDdZRCA5VCAhyDXAMcnT29PdTiFQIBUp5RoF5PAysaYk5xam8UJqbQdHNNcTZQze1ID8-tbggMTk1L7Uk3jXYyMjQwtjIIiTE2JgYNQD8ESgq</recordid><startdate>20041116</startdate><enddate>20041116</enddate><creator>HOFLE, GERHARD, DR</creator><creator>KIFFE, MICHAEL</creator><scope>EVB</scope></search><sort><creationdate>20041116</creationdate><title>DERIVADOS DE EPOTILONES, SU PREPARACION Y UTILIZACION</title><author>HOFLE, GERHARD, DR ; KIFFE, MICHAEL</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_ES2218328TT33</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>spa</language><creationdate>2004</creationdate><topic>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</topic><topic>AGRICULTURE</topic><topic>ANIMAL HUSBANDRY</topic><topic>BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES</topic><topic>CHEMISTRY</topic><topic>FISHING</topic><topic>FORESTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HUNTING</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PEST REPELLANTS OR ATTRACTANTS</topic><topic>PLANT GROWTH REGULATORS</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><topic>TRAPPING</topic><toplevel>online_resources</toplevel><creatorcontrib>HOFLE, GERHARD, DR</creatorcontrib><creatorcontrib>KIFFE, MICHAEL</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>HOFLE, GERHARD, DR</au><au>KIFFE, MICHAEL</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>DERIVADOS DE EPOTILONES, SU PREPARACION Y UTILIZACION</title><date>2004-11-16</date><risdate>2004</risdate><abstract>Derivado de epotilón de la fórmula 1 significando R = H o alquilo C1-4; R1, R2 = H, alquilo C1-6, acilo C1-6, benzoílo, tri-alquil C1-4-sililo, bencilo o fenilo; bencilo o fenilo sustituido con alcoxi C1-6, alquilo C6, hidroxi y halógeno; y realizándose, en el caso de los grupos alquilo y acilo contenidos en los radicales, que se trata de radicales lineales o ramificados; y formando Y y Z uno de los enlaces C-C de un doble enlace C=C.
Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O; (b) R' = C(=X)Me or CH(OX')Me; A = H; B = OR1; and R" = R2; (c) R' = Q; and A+B = bond; X = O, NOR4, N-NR4R5 or N-NHCONR4R5; X' = H, 1-18C alkyl, 1-18C acyl, benzyl, benzoyl or cinnamoyl; Q = a group of formula (i); and R1-R5 = H, 1-6C alkyl, 1-6C acyl, benzoyl, 1-4C trialkylsilyl, or benzyl or phenyl (both optionally substituted by 1-6C alkoxy, 6C alkyl, OH and halo); or R4+R5 = 2-6C alkylene. Epothilone A and B are excluded. Also claimed is the production of epothilone A or B and/or their 12,13-bis-epi derivatives comprising the epoxidation of epothilone C (for A or derivatives) or D (for B or derivatives) especially using dimethyldioxirane or a peracid.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM AGRICULTURE ANIMAL HUSBANDRY BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES CHEMISTRY FISHING FORESTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HUNTING HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEST REPELLANTS OR ATTRACTANTS PLANT GROWTH REGULATORS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS TRAPPING |
| title | DERIVADOS DE EPOTILONES, SU PREPARACION Y UTILIZACION |
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