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1. 发明申请

WO2004046170A3 TUBULYSINS, METHOD FOR PRODUCING THE SAME AND TUBULYSIN PREPARATIONS 审中-公开
标题翻译：微管蛋白抑制剂，的方法和手段微管蛋白抑制剂
公开(公告)号：WO2004046170A3
公开(公告)日：2004-07-01
申请号：PCT/EP0311603
申请日：2003-10-20
申请人： BIOTECHNOLOG FORSCHUNG GMBH , HOEFLE GERHARD , GLASER NICOLE , STEINMETZ HEINRICH , LEIBOLD THOMAS , SASSE FLORENZ
发明人： HOEFLE GERHARD , GLASER NICOLE , STEINMETZ HEINRICH , LEIBOLD THOMAS , SASSE FLORENZ
IPC分类号： A61K38/00 , C07D277/56 , C07D417/12 , C07D417/14 , C07K5/02 , A61K38/08 , C07C271/22 , C07D207/26 , C07D211/60 , C07F7/18
CPC分类号： C07D417/12 , A61K38/00 , C07D417/14 , C07K5/021
摘要： The invention relates to a compound of the following general formula (tubulysin) with the following definitions for R, R , R , R , R , R , R , R , R R , R , R , S, T, U, V, W, X, Y and Z: R = H, C1-4 alkyl, aryl, OR , NR R or NH-(CH2)2-4-; R = H, C1-6 alkyl or aryl; R = H, C1-6 alkyl or aryl; S = H, Hal, NO2 or NHR ; U = H, Hal, NO2 or NHR ; R = H, HCO or C1-4 alkyl-CO; T = H or OR ; R = H, C1-4 alkyl, aryl, COR , P (O) (OR )2 or SO3R ; R = C1-6 alkyl, alkenyl, aryl or heteroaryl; R = H, C1-4 alkyl or metal ion; V = H or R or (if W = O) O; R = H, C1-4 alkyl or COR ; R = C-1-4 alkyl, alkenyl or aryl; W = H or C1-4 alkyl or (if V = O) O; X = H, C1-4 alkyl, alkenyl or CH20R ; R = H, C1-4 alkyl, alkenyl, aryl or COR ; R = C1-6 alkyl, alkenyl, aryl or heteroaryl; Y = (if Z = CH3 or COR ) a free electron pair or (if Z = CH3) O; R = C1-4 alkyl, CF3 or aryl and/or Z = (if Y = O or a free electron pair) CH3 or (if Y = free electron pair) COR .
摘要翻译：本发明涉及下述通式（微管蛋白抑制剂）的化合物与对R，R <1>，R <2>，R <3>，R <4>，R <5> - [R <6>，R的含义如下 <7> - [R <8> - [R <9>，R1 <0>，R <11>，S，T，U，V，W，X，Y和Z：R = H，C 1-4烷基，芳基或<1>，NR <1> [R <2>或NH-（CH2）2-R <1> = H，C 1-6 - 烷基或芳基，R <2> = H，C 1-6烷基或芳基 S = H，哈尔，NO 2或NHR <3> U = H，哈尔，NO 2或NHR <3> [R <3> = H，HCO或C 1-4 - 烷基-CO T = H或或<4> - [R < 4> = H，C 1-4烷基，芳基，COR <5>，P（O）（或<6>）2或SO 3 R <6> - [R <5> = C 1-6烷基，链烯基，芳基或杂芳基 [R <6> = H，C 1-4烷基或金属离子V = H，或R <7>或（对于W = O）或<7> = H，C 1-4烷基或COR <8> - [R <8> = C 1-4烷基，烯基或芳W = H或C 1-4烷基或（对于V = O）OX = H，C 1-4烷基，烯基或CH 2 OR <9> - [R <9> = H ，C 1-4烷基，烯基，芳基或COR <10> - [R <10> = C 1-6烷基，烯基，芳基或杂芳基Y =（Z = CH 3或COR <11>）自由电子对或（Z = CH 3）或<11> = C 1-4烷基，CF 3或芳基和/或Z =（Y = O或自由电子对），或CH 3（= Y为自由电子对）COR <11>。

2. 发明申请

WO9965913A3 EPOTHILONE MINOR CONSTITUENTS 审中-公开
标题翻译：埃博霉素端组件
公开(公告)号：WO9965913A3
公开(公告)日：2000-04-20
申请号：PCT/EP9904244
申请日：1999-06-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH , HOEFLE GERHARD , REICHENBACH HANS , GERTH KLAUS , HARDT INGO , SASSE FLORENZ , STEINMETZ HEINRICH
发明人： HOEFLE GERHARD , REICHENBACH HANS , GERTH KLAUS , HARDT INGO , SASSE FLORENZ , STEINMETZ HEINRICH
IPC分类号： C07D277/24 , C07D413/06 , C07D417/06 , C07D493/04
CPC分类号： C07D413/06 , C07D277/24 , C07D417/06 , C07D493/04
摘要： The invention relates to compounds which are obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.
摘要翻译：本发明涉及作为通过DSM的发酵所得到的6773化合物，尤其是大环内酯类A1，A2，A8，A9，B10，C1，C2，C3，C4，C5，C6，C7，C8，C9，D1，D2，D5， G1，G2，H1，H2，I1，I2，I3，I4，I5，I6和K和反式埃博霉素C1和C2。

3. 发明申请

WO2009103534A3 ELANSOLIDS, NOVEL NATURAL METABOLITES OF FLEXIBACTER AND ANTIBIOTICALLY ACTIVE DERIVATIVES THEREOF 审中-公开
标题翻译： ELANSOLIDIS，灵活性的新型天然代谢物及其抗生素活性衍生物
公开(公告)号：WO2009103534A3
公开(公告)日：2009-10-29
申请号：PCT/EP2009001192
申请日：2009-02-19
申请人： HELMHOLTZ INFEKTIONSFORSCHUNG , GERTH KLAUS , STEINMETZ HEINRICH , HOEFLE GERHARD
发明人： GERTH KLAUS , STEINMETZ HEINRICH , HOEFLE GERHARD
IPC分类号： C07C59/72 , A61K31/202 , A61K31/335 , C07C59/54 , C07C215/76 , C07C225/22 , C07C229/56 , C07D307/54 , C07D313/00 , C07D333/24 , C12P7/42 , C12P13/00 , C12P17/08
CPC分类号： C07C59/72 , C07C59/54 , C07C229/56 , C07C2602/08 , C07D313/00 , C12P7/42 , C12P13/001 , C12P17/08
摘要： The present invention describes Elansolids, a new class of novel anti-bacterial compounds of formula (I).
摘要翻译：本发明描述了Elansolids，一类新的式（I）的新型抗菌化合物。

4. 发明专利

DK0941227T4 未知
公开(公告)号：DK0941227T4
公开(公告)日：2008-05-19
申请号：DK97951233
申请日：1997-11-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： REICHENBACH HANS , HOEFLE GERHARD , GERTH KLAUS , STEINMETZ HEINRICH
IPC分类号： C07D417/06 , A01N43/78 , A01N43/90 , A01N63/02 , A61K31/425 , A61K31/427 , A61P35/00 , C07D303/00 , C07D313/00 , C07D493/04 , C12P1/04 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01
摘要： Epothilone derivatives are obtained by: (1) cultivation of Sorangium cellulosum DSM 6773 in the presence of an absorption resin; (2) separation of the resin and culture followed by washing with aqueous methanol; (3) eluting the washed resin with methanol and reducing the extract; (4) partitioning the extract between methanol and hexane; (5) reducing the methanolic phase and fractionating it on a Sephadex column, and (6) isolation of the epothilones by chromatography using a methanol/water mixture. Epothilone A is followed by epothilone B, and two further fractions.

5. 发明专利

ES2221692T4 EPOTILON, SU PREPARACION Y SU UTILIZACION COMO AGENTE CITOSTATICO O COMO AGENTE FITOPROTECTOR. 未知
公开(公告)号：ES2221692T4
公开(公告)日：2005-10-01
申请号：ES97951233
申请日：1997-11-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： REICHENBACH HANS , HOFLE GERHARD , GERTH KLAUS , STEINMETZ HEINRICH
IPC分类号： A01N43/78 , A01N43/90 , A01N63/02 , A61K31/425 , A61K31/427 , A61P35/00 , C07D417/06 , C07D493/04 , C12P1/04 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01
摘要： LA PRESENTE INVENCION TRATA DE EPOTILONA, EN PARTICULAR EPOTILONA C (R = HIDROGENO) Y EPOTILONA D (R = METILO) DE FORMULA (I), ASI COMO EPOTILONA E (R = HIDROGENO) Y EPOTILONA F (R = METILO) DE FORMULA (II), SU PREPARACION, ASI COMO SU UTILIZACION PARA LA PREPARACION DE AGENTES TERAPEUTICOS, EN PARTICULAR CITOSTATICOS ASI COMO AGENTES FITOSANITARIOS.

6. 发明专利

DE59711647D1 未知
公开(公告)号：DE59711647D1
公开(公告)日：2004-06-24
申请号：DE59711647
申请日：1997-11-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： REICHENBACH HANS , HOEFLE GERHARD , GERTH KLAUS , STEINMETZ HEINRICH
IPC分类号： A01N43/78 , A01N43/90 , A01N63/02 , A61K31/425 , A61K31/427 , A61P35/00 , C07D417/06 , C07D493/04 , C12P1/04 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01
摘要： Epothilone derivatives are obtained by: (1) cultivation of Sorangium cellulosum DSM 6773 in the presence of an absorption resin; (2) separation of the resin and culture followed by washing with aqueous methanol; (3) eluting the washed resin with methanol and reducing the extract; (4) partitioning the extract between methanol and hexane; (5) reducing the methanolic phase and fractionating it on a Sephadex column, and (6) isolation of the epothilones by chromatography using a methanol/water mixture. Epothilone A is followed by epothilone B, and two further fractions.

7. 发明专利

AT267197T 未知
公开(公告)号：AT267197T
公开(公告)日：2004-06-15
申请号：AT97951233
申请日：1997-11-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： REICHENBACH HANS , HOEFLE GERHARD , GERTH KLAUS , STEINMETZ HEINRICH
IPC分类号： A01N43/78 , A01N43/90 , A01N63/02 , A61K31/425 , A61K31/427 , A61P35/00 , C07D417/06 , C07D493/04 , C12P1/04 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01 , C07D313/00 , C07D303/00
摘要： Epothilone derivatives are obtained by: (1) cultivation of Sorangium cellulosum DSM 6773 in the presence of an absorption resin; (2) separation of the resin and culture followed by washing with aqueous methanol; (3) eluting the washed resin with methanol and reducing the extract; (4) partitioning the extract between methanol and hexane; (5) reducing the methanolic phase and fractionating it on a Sephadex column, and (6) isolation of the epothilones by chromatography using a methanol/water mixture. Epothilone A is followed by epothilone B, and two further fractions.

8. 发明专利

AU753546B2 Epothilone C, D, E and F, production process, and their use as cytostatic as well as phytosanitary agents 未知
公开(公告)号：AU753546B2
公开(公告)日：2002-10-24
申请号：AU5483798
申请日：1997-11-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： REICHENBACH HANS , HOFLE GERHARD , GERTH KLAUS , STEINMETZ HEINRICH
IPC分类号： A01N43/78 , A01N43/90 , A01N63/02 , A61K31/425 , A61K31/427 , A61P35/00 , C07D417/06 , C07D493/04 , C12P1/04 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01
摘要： Epothilone derivatives are obtained by: (1) cultivation of Sorangium cellulosum DSM 6773 in the presence of an absorption resin; (2) separation of the resin and culture followed by washing with aqueous methanol; (3) eluting the washed resin with methanol and reducing the extract; (4) partitioning the extract between methanol and hexane; (5) reducing the methanolic phase and fractionating it on a Sephadex column, and (6) isolation of the epothilones by chromatography using a methanol/water mixture. Epothilone A is followed by epothilone B, and two further fractions.

9. 发明专利

DE19826988A1 未知
公开(公告)号：DE19826988A1
公开(公告)日：1999-12-23
申请号：DE19826988
申请日：1998-06-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： HOEFLE GERHARD , REICHENBACH HANS , GERTH KLAUS , HARDT INGO , SASSE FLORENZ , STEINMETZ HEINRICH
IPC分类号： C07D277/24 , C07D413/06 , C07D417/06 , C07D493/04
摘要： The invention relates to compounds which are obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.

10. 发明专利

CA2336189A1 EPOTHILONE MINOR CONSTITUENTS 未知
公开(公告)号：CA2336189A1
公开(公告)日：1999-12-23
申请号：CA2336189
申请日：1999-06-18
申请人： BIOTECHNOLOG FORSCHUNG GMBH
发明人： HOEFLE GERHARD , HARDT INGO , REICHENBACH HANS , GERTH KLAUS , STEINMETZ HEINRICH , SASSE FLORENZ
IPC分类号： C07D277/24 , C07D413/06 , C07D417/06 , C07D493/04 , C07D303/00 , C07D313/00
摘要： The invention relates to compounds which are obtained by fermenting DSM 6773 , especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans- epothilones C1 and C2.

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