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1. 发明授权

US08217071B2 Use of inhibitors of the degradation of p27, in particular Argyrin and derivatives thereof, for the treatment of proliferative diseases 有权
标题翻译：使用p27降解抑制剂，特别是Argyrin及其衍生物，用于治疗增殖性疾病
公开(公告)号：US08217071B2
公开(公告)日：2012-07-10
申请号：US12527428
申请日：2008-02-27
申请人： Nisar Malek , Florenz Sasse , Irina Nickeleit , Roland Frank , Bettina Hinkelmann , Heinrich Steinmetz
发明人： Nisar Malek , Florenz Sasse , Irina Nickeleit , Roland Frank , Bettina Hinkelmann , Heinrich Steinmetz
IPC分类号： A01N43/48 , A61K31/40 , G01N33/567 , G01N33/574
CPC分类号： A61K31/4045 , A61K31/405 , A61K38/00 , C07D519/04 , C07K7/56 , G01N33/5011
摘要： The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular Argyrin and derivatives thereof, preferably Argyrin A, for the treatment of proliferative diseases, such as cancer, as well as the derivatization of said macrocycles.
摘要翻译：本发明涉及作为p27蛋白酶体降解抑制剂的特别大环化合物的用途，特别是Argyrin及其衍生物，优选Argyrin A，用于治疗增殖性疾病如癌症，以及所述大环化合物的衍生化。

2. 发明申请

US20100144822A1 Use of Inhibitors of the Degradation of P27, in Particular Argyrin and Derivatives Thereof, for the Treatment of Proliferative Diseases 有权
标题翻译：使用抑制剂降低P27，特别是Argyrin及其衍生物，用于治疗增殖性疾病
公开(公告)号：US20100144822A1
公开(公告)日：2010-06-10
申请号：US12527428
申请日：2008-02-27
申请人： Nisar Malek , Florenz Sasse , Irina Nickeleit , Ronald Frank , Bettina Hinkelmann , Heinrich Steinmetz
发明人： Nisar Malek , Florenz Sasse , Irina Nickeleit , Ronald Frank , Bettina Hinkelmann , Heinrich Steinmetz
IPC分类号： A61K31/404 , G01N33/567 , G01N33/574 , C12Q1/68 , A61P35/00
CPC分类号： A61K31/4045 , A61K31/405 , A61K38/00 , C07D519/04 , C07K7/56 , G01N33/5011
摘要： The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular Argyrin and derivatives thereof, preferably Argyrin A, for the treatment of proliferative diseases, such as cancer, as well as the derivatization of said macrocycles.
摘要翻译：本发明涉及作为p27蛋白酶体降解抑制剂的特别大环化合物的用途，特别是Argyrin及其衍生物，优选Argyrin A，用于治疗增殖性疾病如癌症，以及所述大环化合物的衍生化。

3. 发明申请

US20060142584A1 Epothilone side components 有权
标题翻译：埃坡霉素组分
公开(公告)号：US20060142584A1
公开(公告)日：2006-06-29
申请号：US11354769
申请日：2006-02-15
申请人： Gerhard Hoefle , Hans Reichenbach , Klaus Garth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
发明人： Gerhard Hoefle , Hans Reichenbach , Klaus Garth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
IPC分类号： C07D417/02 , C07D413/02
CPC分类号： C07D413/06 , C07D277/24 , C07D417/06 , C07D493/04
摘要： The invention concerns compounds which can be 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：本发明涉及通过发酵DSM 6773，特别是埃坡霉素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以及反式埃坡霉素C1和C2。

4. 发明申请

US20060128754A1 Tubulysins, method for producing the same and tubulysin preparations 有权
公开(公告)号：US20060128754A1
公开(公告)日：2006-06-15
申请号：US10535630
申请日：2003-10-20
申请人： Gerhard Hoefle , Nicole Glaser , Heinrich Steinmetz , Thomas Leibold , Florenz Sasse
发明人： Gerhard Hoefle , Nicole Glaser , Heinrich Steinmetz , Thomas Leibold , Florenz Sasse
IPC分类号： A61K31/454 , C07D417/02
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) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, S, T, U, V, W, X, Y and Z: R=H, C1-4alkyl, aryl, OR1, NR1R2 or NH—(CH2)2-4 R1=H, C1-6alkyl or aryl R2=H, C1-6alkyl or aryl S=H, Hal, NO2 or NHR3 U=H, Hal, NO2 or NHR3 R3=H, HCO or C1-4alkyl-CO T=H or OR4 R4=H, C1-4alkyl, aryl, COR5, P(O)(OR6)2 or SO3R6 R5=C1-6alkyl, alkenyl, aryl or heteroaryl R6=H, alkyl or a metal ion V=H, OR7, Hal or (for W=O)O R7=H, C1-4alkyl or COR8 R5=C1-4alkyl, alkenyl or aryl W=H or C1-4alkyl or (for V=O) O X=H, C1-4alkyl, alkenyl or CH2OR9 R9=H, C1-4alkyl, alkenyl, aryl or COR10 R10=C1-6alkyl, alkenyl, aryl or heteroaryl Y=(for Z=CH3 or COR11) free electron pair or (for Z=CH3)O R11=C1-4alkyl, CF3 or aryl and/or Z=(for Y=O or free electron pair) CH3 or (for Y=free electron pair) COR11.

5. 发明授权

US5610038A Thiangazole, its preparation, compositions and use thereof 失效
公开(公告)号：US5610038A
公开(公告)日：1997-03-11
申请号：US487385
申请日：1995-06-07
申请人： Gerhard Hofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
发明人： Gerhard Hofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
IPC分类号： A01N43/78 , A01N63/02 , C07D417/14 , C12P17/16
CPC分类号： A01N43/78 , A01N63/02 , C07D417/14
摘要： The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.

6. 发明授权

US07235669B2 Epothilone side components 有权
标题翻译：埃坡霉素组分
公开(公告)号：US07235669B2
公开(公告)日：2007-06-26
申请号：US11354769
申请日：2006-02-15
申请人： Gerhard Hoefle , Hans Reichenbach , Klaus Gerth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
发明人： Gerhard Hoefle , Hans Reichenbach , Klaus Gerth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
IPC分类号： C07D417/06
CPC分类号： C07D413/06 , C07D277/24 , C07D417/06 , C07D493/04
摘要： The invention concerns compounds which can be 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：本发明涉及通过发酵DSM 6773，特别是埃坡霉素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以及反式埃坡霉素C1和C2。

7. 发明授权

US5604249A Thiangazole, its preparation, compositions and use thereof 失效
标题翻译：噻唑，其制备方法，组合物及其用途
公开(公告)号：US5604249A
公开(公告)日：1997-02-18
申请号：US487382
申请日：1995-06-07
申请人： Gerhard H ofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
发明人： Gerhard H ofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
IPC分类号： A01N43/78 , A01N63/02 , C07D417/14 , G07D417/14
CPC分类号： A01N43/78 , A01N63/02 , C07D417/14
摘要： The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.
摘要翻译：本发明涉及以下通式I的化合物，其特别是称为噻唑的式Ia化合物（Ia）其药学上可接受的酸加成盐，其制备方法以及可用于作物保护的治疗组合物和组合物。

8. 发明授权

US07754885B2 Tubulysins, method for producing the same and tubulysin preparations 有权
标题翻译： Tubulysins，其制备方法和tubulysin制剂
公开(公告)号：US07754885B2
公开(公告)日：2010-07-13
申请号：US10535630
申请日：2003-10-20
申请人： Gerhard Hoefle , Nicole Glaser , Heinrich Steinmetz , Thomas Leibold , Florenz Sasse
发明人： Gerhard Hoefle , Nicole Glaser , Heinrich Steinmetz , Thomas Leibold , Florenz Sasse
IPC分类号： C07D417/00 , A61K31/445
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) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, S, T, U, V, W, X, Y and Z: R=H, alkyl, aryl, OR1, NR1R2 or R1=H, C1-6alkyl or aryl R2=H, C1-6alkyl or aryl S=H, Hal, NO2 or NHR3 U=H, Hal, NO2 or NHR3 R3=H, HCO or C1-4alkyl-CO T=H or OR4 R4=H, C1-4alkyl, aryl, COR5, P(O)(OR6)2 or SO3R6 R5=C1-6alkyl, alkenyl, aryl or heteroaryl R6=H, alkyl or a metal ion V=H, OR7, Hal or (for W=O) O R7=H, C1-4alkyl or COR8 R5=C1-4alkyl, alkenyl or aryl W=H or C1-4alkyl or (for V=O) O X=H, C1-4alkyl, alkenyl or CH2OR9 R9=H, C1-4alkyl, alkenyl, aryl or COR10 R10=C1-6alkyl, alkenyl, aryl or heteroaryl Y=(for Z=CH3 or COR11) free electron pair or (for Z=CH3)O R11=C1-4alkyl, CF3 or aryl and/or Z=(for Y=O or free electron pair) CH3 or (for Y=free electron pair) COR11.
摘要翻译：本发明涉及对R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，S，T，U，V具有以下含义的下列通式（管状素）的化合物，W，X，Y和Z：R = H，烷基，芳基，OR1，NR1R2或R1 = H，C1-6烷基或芳基R2 = H，C1-6烷基或芳基S = H，Hal，NO2或NHR3 U = H，Hal，NO 2或NHR 3 R 3 = H，HCO或C 1-4烷基-CO T = H或OR 4 R 4 = H，C 1-4烷基，芳基，COR 5，P（O）（OR 6）2或SO 3 R 6 R 5 = ，烯基，芳基或杂芳基R6 = H，烷基或金属离子V = H，OR7，Hal或（对于W = O）O R7 = H，C1-4烷基或COR8 R5 = C1-4烷基，烯基或芳基W = H或C 1-4烷基或（对于V = O）O X = 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 = 对于Z = CH 3或COR 11）自由电子对或（对于Z = CH 3）O R 11 = C 1-4烷基，CF 3或芳基和/或Z =（对于Y = O或自由电子对）CH 3或（对于Y = 对）COR11。

9. 发明授权

US06624310B1 Epothilone minor constituents 有权
标题翻译：埃博霉素次要成分
公开(公告)号：US06624310B1
公开(公告)日：2003-09-23
申请号：US09719932
申请日：2001-03-21
申请人： Gerhard Hoefle , Hans Reichenbach , Klaus Gerth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
发明人： Gerhard Hoefle , Hans Reichenbach , Klaus Gerth , Ingo Hardt , Florenz Sasse , Heinrich Steinmetz
IPC分类号： C07D49304
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：本发明涉及通过发酵DSM6773，特别是埃坡霉素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以及反式埃坡霉素C1和C2。

10. 发明授权

US5622979A Thiangazole, its preparation, compositions and use thereof 失效
公开(公告)号：US5622979A
公开(公告)日：1997-04-22
申请号：US487384
申请日：1995-06-07
申请人： Gerhard H ofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
发明人： Gerhard H ofle , Norbert Bedorf , Edgar Forche , Klaus Gerth , Herbert Irschik , Rolf Jansen , Brigitte Kunze , Hans Reichenbach , Florenz Sasse , Heinrich Steinmetz , Wolfram Trowitzsch-Kienast , Johannes P. Pachlatko
IPC分类号： A01N43/78 , A01N63/02 , C07D417/14
CPC分类号： A01N43/78 , A01N63/02 , C07D417/14
摘要： The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.

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