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1. 发明专利

AT459356T 未知
公开(公告)号：AT459356T
公开(公告)日：2010-03-15
申请号：AT00967789
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JUERGEN , BRUYNEEL ERIK , KAMP GUENTER , PETERS KIRSTEN
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/404 , A61P9/00 , A61P35/00 , A61P35/02 , A61P35/04
摘要： The invention relates to the use of N-substituted indol-3- glyoxylamides of general formula (I) for treating tumors, in particular, in cases of drug resistance and metastatic carcinoma, and as angiogenesis inhibitors having distinctly fewer side effects, in particular, distinctly lower neurotoxicity. The invention also relates to medicaments containing the inventive compounds.

2. 发明专利

SK287533B6 Medicament for the treatment of multidrug-resistant tumors or angiogenesis and metastasis inhibition 未知
公开(公告)号：SK287533B6
公开(公告)日：2011-01-04
申请号：SK4072002
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JURGEN , BRUYNEEL ERIK , KAMP GUNTER , PETERS KIRSTEN
IPC分类号： A61K31/00 , C07D401/12 , A61K31/404 , A61K31/4439 , A61P35/00
摘要： Use of N-substituted indol-3-glyoxylamides of general formula (1) and pharmaceutically acceptable acid addition salts thereof for the manufacture of a medicament for the treatment of multidrug-resistant tumors and angiogenesis and metastasis inhibition. In the general formula (1) R represents hydrogen atom; R1 represents 4-pyridyl group or 4-fluorophenyl group; R2 represents benzyl group, 4-chlorobenzyl group, 4-fluorobenzyl group, 3-pyridylmethyl group or 4-bromobenzyl group; R3 and R4 represent hydrogen atom and Z represents oxygen atom. The preferred compound for that use is N-(pyridin-4-yl)-[1-(4- chlorobenzyl)indol-3-yl]glyoxylamide (indibulin).

3. 发明专利

ES2342042T3 DERIVADOS DEL ACIDO INDOLIL-3-GLIOXILICO CON VALIOSAS PROPIEDADES TERAPEUTICAS. 未知
公开(公告)号：ES2342042T3
公开(公告)日：2010-07-01
申请号：ES00967789
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JURGEN
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/404 , A61P9/00 , A61P35/00 , A61P35/02 , A61P35/04
摘要： Indol-3-glioxilamidas sustituidas en N de la Fórmula 1 siguiente, o bien sus sales de adición fisiológicamente tolerables, para emplear en el tratamiento de tumores resistentes a fármacos antitumorales **(Ver fórmula)** en donde los radicales R, R1, R2, R3, R4 y Z tienen los significados siguientes: Res hidrógeno. R1es una estructura de piridina de Fórmula 2 **(Ver fórmula)** en donde la estructura de piridina está unida a los átomos de carbono 2, 3 ó 4 en el anillo y puede estar sustituida opcionalmente con los sustituyentes R5 y R6, en donde los radicales R5 y R6 pueden ser iguales o distintos y ser alquilo (C1-C6), cicloalquilo (C3-C7), alcoxi (C1-C6), nitro, amino, hidroxi, halógeno, trifluorometilo, etoxicarbonilamino y carboxialquiloxi en el que el grupo alquilo puede tener 1-4 átomos de C, R2es un grupo alquilo (C1-C6), en donde el grupo alquilo está monosustituido o polisustituido con halógeno y fenilo, el cual, por otro lado, puede estar monosustituido o polisustituido con halógeno, alquilo (C1-C6), cicloalquilo (C3-C7), un grupo carboxilo, un grupo carboxilo esterificado con alcanol (C1-C6), un grupo trifluorometilo, un grupo hidroxilo, un grupo metoxi, un grupo etoxi, un grupo benciloxi, un grupo 2-quinolilo o un grupo 2-piridilo, 3-piridilo o 4-piridilo, en donde los grupos 2-piridilo, 3-piridilo o 4-piridilo pueden estar en cada caso, monosustituidos o polisustituidos con halógeno, un grupo alquilo (C1-C4) o un grupo alcoxi (C1-C4), R3 y R4 pueden ser idénticos o diferentes, y representan hidrógeno, alquilo (C1-C6), cicloalquilo (C3-C7), alcanoilo (C1-C6), alcoxi (C1-C6), halógeno y benciloxi, un grupo nitro, un grupo amino, un grupo amino sustituido con monoalquilo o dialquilo (C1-C4), un grupo alcoxi (C1-C6)-carbonilamino y un grupo alcoxi (C1-C6)-carbonilamino-alquilo (C1-C6), Zes O y S.

4. 发明专利

RS51302B DERIVATI INDOLIL-3-GLIOKSILNE KISELINE SA TERAPEUTSKI VREDNIM SVOJSTVIMA 未知
公开(公告)号：RS51302B
公开(公告)日：2010-12-31
申请号：YUP22702
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： ENGEL JUERGEN , NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , BRUYNEEL ERIC , KAMP GRUENTER , PETERS KIRSTEN
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/404 , A61P9/00 , A61P35/00 , A61P35/02 , A61P35/04
摘要： N-supstituisani indol-3-glioksilamidi formule I ili njihove fiziološki prihvatljive kisele adicione soli za upotrebu u lečenje tumora otpornih na lekove(I)gde radikali R, R1, R2, R3, R4, i Z imaju sledeća značenja:R je vodonikR1 je piri din sa strukturom formule IIpri čemu je piridinski deo vezan za ugljenikov atom prstena u položaju 2, 3, ili 4 i opciono supstituisan sa supstituentima R5 i R6 gde R5 i R6 mogu biti isti ili različiti i odabrani od: (C1-C6)-alkila, (C3-C7)-cikloalkila, (C1-C6)-alkoksi, nitro, amino, hidroksil, halogen, trifluorometil, etoksikarbonilamino i karboksialkiloksi grupe gde alkil grupa može imati 1 -4 atoma;R2 je (C1-C6)-alkil grupa koja ima jedan ili više supstituenata, odabranih od halogena i fenila, koji je opciono supstituisan sa jednim ili više supstituenata odabranih od: halogena, (C1-C6)-a1kila, (C3-C7)-cikloalkila, karboksilne grupe, karboksilne grupe esterifikovane sa C1-C6-alkanolom, trifluorometil grupe, hidroksil grupe, metoksi grupe, etoksi grupe, benziloksi grupe; 2-hinolil grupe; ili 2-, 3- ili 4-piridil grupe, pri čemu 2-hinolil i 2-, 3-, ili 4-piridil grupe mogu obe, u svakom slučaju, biti mono- ili polisupstituisane halogenom, (C1-C4)-alkilnom grupom ili (C1-C4)-alkoksi;R3 i R4 mogu biti isti ili različiti i nezavisno su odabrane od: hidrogena, (C1-C6)-alkila, (C3-C7)-cikloalkila, (C1-C6)-alkanoila, (C1-C6)-alkoksi, halogena, benziloksi, nitro grupe, amino grupe, (C1-C4)-mono ili dialkil-supstituisane amino grupe, (C1-C6) alkoksikarbonilamino grupe, i (C1-C6)-alkoksikarbonilamino-(C1-C6)-alkil grupe; i Z je O ili S. Prijava sadrži još 10 patentnih zahteva.

5. 发明专利

DE50015879D1 未知
公开(公告)号：DE50015879D1
公开(公告)日：2010-04-15
申请号：DE50015879
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JUERGEN , BRUYNEEL ERIK , KAMP GUENTER , PETERS KIRSTEN
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/404 , A61P9/00 , A61P35/00 , A61P35/02 , A61P35/04
摘要： The invention relates to the use of N-substituted indol-3- glyoxylamides of general formula (I) for treating tumors, in particular, in cases of drug resistance and metastatic carcinoma, and as angiogenesis inhibitors having distinctly fewer side effects, in particular, distinctly lower neurotoxicity. The invention also relates to medicaments containing the inventive compounds.

6. 发明专利

AU7782900A Indolyl-3-glyoxylic acid derivatives comprising therapeutically valuable properties 未知
公开(公告)号：AU7782900A
公开(公告)日：2001-04-30
申请号：AU7782900
申请日：2000-09-26
申请人： ZIOPHARM ONCOLOGY INC
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JURGEN , BRUYNEEL ERIK , KAMP GUNTER , PETERS KIRSTEN
IPC分类号： C07D401/12 , A61K31/404 , A61K31/4439 , A61P35/00 , A61K31/00
摘要： The invention relates to the use of N-substituted indol-3- glyoxylamides of general formula (I) for treating tumors, in particular, in cases of drug resistance and metastatic carcinoma, and as angiogenesis inhibitors having distinctly fewer side effects, in particular, distinctly lower neurotoxicity. The invention also relates to medicaments containing the inventive compounds.

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