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1. 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。

2. 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>。

3. 发明申请

WO2004022586A3 TUBULYSIN BIOSYNTHESIS GENE 审中-公开
标题翻译：微管蛋白抑制剂生物合成基因
公开(公告)号：WO2004022586A3
公开(公告)日：2004-11-11
申请号：PCT/EP0309780
申请日：2003-09-03
申请人： BIOTECHNOLOG FORSCHUNG GMBH , HOEFLE GERHARD , MUELLER ROLF , SASSE FLORENZ , SANDMANN AXEL , BLOECKER HELMUT
发明人： HOEFLE GERHARD , MUELLER ROLF , SASSE FLORENZ , SANDMANN AXEL , BLOECKER HELMUT
IPC分类号： C12N15/52 , C12P17/14 , C12P21/02 , C12P1/04 , A61K38/05 , C07K5/078 , C12N1/20 , C12R1/01
CPC分类号： C12P21/02 , C12N15/52 , C12P17/14
摘要： The invention relates to an ss-DNA molecule, a ds-DNA molecule, an RNA, a vector, the use of the same, and a cell, especially for expressing tubulysin genes.
摘要翻译：本发明涉及一种单链DNA分子，一个双链DNA分子，RNA，载体，其用途，以及作为细胞，特别是用于微管溶素基因的表达。

4. 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。

5. 发明申请

WO02072858A3 DEGRADATION OF EPOTHILONES AND ETHYNYL SUBSTITUTED EPOTHILONES 审中-公开
标题翻译：苯乙烯和乙烯取代的EPOTHILONES的降解
公开(公告)号：WO02072858A3
公开(公告)日：2002-12-19
申请号：PCT/EP0202105
申请日：2002-02-27
申请人： BIOTECHNOLOG FORSCHUNG GMBH , HOEFLE GERHARD , KARAMA USAMA
发明人： HOEFLE GERHARD , KARAMA USAMA
IPC分类号： C12P17/00 , C07B61/00 , C07C51/09 , C07C51/353 , C07C59/90 , C07D277/20 , C07D277/24 , C07D277/30 , C07D417/06 , C07D493/04 , C07F7/18 , C12P7/62 , C12P17/14 , C12P17/18
CPC分类号： C07D417/06 , C07D277/24 , C07D493/04 , C07F7/1852 , C07F7/188 , C07F7/1892 , C12P7/62 , C12P17/14 , C12P17/181 , Y10T436/141111
摘要： The invention concerns a process for a degradation of an epothilone C or a epothilone D, wherein an epothilone C or epothilone D is subjected to an olefin metathesis in the presence of ethylene and subsequently an optional ester hydrolysis. The invention further concerns (2-methyl-1,3-thiazol-4-yl)-ethynyl substitued epothilones (9). Formula (9).
摘要翻译：本发明涉及埃坡霉素C或埃坡霉素D降解的方法，其中埃博霉素C或埃坡霉素D在乙烯存在下进行烯烃复分解，随后进行任选的酯水解。本发明还涉及（2-甲基-1,3-噻唑-4-基） - 乙炔基取代的埃坡霉素（9）。公式（9）。

6. 发明申请

WO0112615A3 FUNGICIDAL HETEROARYL HEPTA-2,6-DIENOIC ACID DERIVATIVES 审中-公开
公开(公告)号：WO0112615A3
公开(公告)日：2001-09-13
申请号：PCT/US0021536
申请日：2000-08-07
申请人： AMERICAN CYANAMID CO , BIOTECHNOLOG FORSCHUNG GMBH , SIMON WERNER , CARTER PAUL , HOEFLE GERHARD , SOEKER UDO
发明人： SIMON WERNER , CARTER PAUL , HOEFLE GERHARD , SOEKER UDO
IPC分类号： A01N43/10 , A01N43/74 , C07D213/55 , C07D213/61 , C07D233/54 , C07D233/64 , C07D233/68 , C07D239/26 , C07D239/30 , C07D263/32 , C07D263/34 , C07D277/30 , C07D277/32 , C07D307/54 , C07D307/56 , C07D333/24 , C07D333/28 , C07F5/02 , A01N43/08 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/76 , A01N43/78
CPC分类号： C07D233/64 , A01N43/10 , A01N43/74 , C07D213/55 , C07D213/61 , C07D233/68 , C07D239/26 , C07D239/30 , C07D263/32 , C07D263/34 , C07D277/30 , C07D277/32 , C07D307/54 , C07D307/56 , C07D333/24 , C07D333/28 , C07F5/025
摘要： Compounds of formula (I) show excellent fungicidal activity and systemicity; wherein A represents an organic radical which is bonded directly or via an oxy, iminoxy, mercapto, amino, carbamoyl, thiocarbamoyl, imidoyl or thioimidoyl group; R represents a hydrogen atom or an alkyl group; R represents an alkoxy group; R and R each independently represent a hydrogen atom or an alkyl group; R represents an alkyl group, and R represents a group of formula -COOR or -CONR R , in which R and R each independently represent a hydrogen atom or an alkyl group; X and Y each independently represent S, O, N, NR , CL , CL -N, N-CL or CL -CL , in which R represents a hydrogen atom or an alkyl group, and L and L each independently represent a hydrogen or halogen atom or an alkyl group; with the proviso that one of X and Y represents S, O, N or NR ; W represents S, N or CL , with the proviso that X represents CL , when W represents S; and wherein the zigzag lines indicate that the connected groups may have the (E)- or (Z)-configuration.
摘要翻译：式（I）化合物显示出优异的杀真菌活性和系统性; 其中A表示直接或通过氧基，亚氨基，巯基，氨基，氨基甲酰基，硫代氨基甲酰基，亚氨基或亚氨基亚氨基结合的有机基团。 R 2表示氢原子或烷基; R 3表示烷氧基; R 4和R 5各自独立地表示氢原子或烷基; R 6表示烷基，R 7表示式-COOR 8或-CONR 8 R 9的基团，其中R 8和R 9各自独立地表示氢原子或烷基; X和Y各自独立地表示S，O，N，NR 10，CL 1，CL 1，N-CL 1或CL 1 -CL 2， 10“表示氢原子或烷基，L 1和L 2各自独立地表示氢或卤素原子或烷基; 条件是X和Y中的一个表示S，O，N或NR 10; W表示S，N或CL <1>，条件是X表示CL 1，当W表示S时; 并且其中之字形线表示连接的组可以具有（E） - 或（Z） - 构型。

7. 发明申请

WO0138317A3 FUNGICIDAL MELITHIAZOLE DERIVATIVES 审中-公开
标题翻译：杀真菌剂MELITHIAZOLE DORIVATIVES
公开(公告)号：WO0138317A3
公开(公告)日：2001-11-08
申请号：PCT/EP0011643
申请日：2000-11-23
申请人： BASF CORP , BASF AG , BIOTECHNOLOG FORSCHUNG GMBH
发明人： MEYER OLIVER , SIMON WERNER , HOEFLE GERHARD , SOEKER UDO
IPC分类号： A01N43/78 , C07D277/24 , C07D277/28 , A01N43/28
CPC分类号： A01N43/78 , C07D277/24 , C07D277/28
摘要： Compounds with contain essentially equimolar amounts of the enantiomer pair of formulae (IA and IB), wherein R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, or aryl group; R , R , R and R each independently represent an alkyl group; and R represents a group of formula -COOR or -CONR R , in which R and R each independently represent a hydrogen atom or an alkyl group; L represents a hydrogen or halogen atom or an optionally substituted alkyl group; and wherein th ezigzag line indicates that the alkoximino group may have the (E)- or (Z)-configuration show excellent fungicidal activity and systemicity.
摘要翻译：含有基本上等摩尔量的式（IA和IB）的对映体对的化合物，其中R 1表示氢原子或任选取代的烷基，烯基或芳基; R 2，R 3，R 4和R 5各自独立地表示烷基; 并且R 6表示式-COOR 7或-CONR 7 R 8的基团，其中R 7和R 8各自独立地表示氢原子或烷基; L 1表示氢或卤素原子或任选取代的烷基; 并且其中之字形线表示该肟基可以具有（E） - 或（Z） - 构型具有优异的杀真菌活性和系统性。

8. 发明专利

DE60326348D1 未知
公开(公告)号：DE60326348D1
公开(公告)日：2009-04-09
申请号：DE60326348
申请日：2003-07-15
申请人： BIOTECHNOLOG FORSCHUNG GMBH , RICHTER WOLFGANG
发明人： HOEFLE GERHARD , RICHTER WOLFGANG
IPC分类号： A61K31/426 , C07D417/06 , A61K31/427 , A61P35/00 , C07C323/22 , C07D277/26 , C07D327/06 , C07D417/04 , C07D497/04
摘要： The present invention relates to new Macro-cycles of Formula (I), and their use for the treatment of cancer.

9. 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.

10. 发明专利

EE04852B1 未知
公开(公告)号：EE04852B1
公开(公告)日：2007-06-15
申请号：EEP200100437
申请日：2000-02-17
申请人： BIOTECHNOLOG FORSCHUNG GMBH , SQUIBB BRISTOL MYERS CO
发明人： HOEFLE GERHARD , GLASER NICOLE , LEIBOLD THOMAS , VITE GREGORY D , KIM SOONG-HOON
IPC分类号： A01N43/78 , A01N43/90 , A61K31/425 , A61P35/00 , C07D417/06 , C07D493/04
摘要： The invention is concerned with epothilones in which the thiazole substituent has been modified, with methods for their preparation and with antifungal or therapeutic agents which contain these epothilones.

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