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1. 发明申请

WO2005103072A1 CONVERGENT SYNTHESIS FOR KAHALALIDE COMPOUNDS 审中-公开
标题翻译：卡拉沙利特化合物的合成合成
公开(公告)号：WO2005103072A1
公开(公告)日：2005-11-03
申请号：PCT/GB2005/001537
申请日：2005-04-22
申请人： PHARMA MAR, S.A.U. , TUBBY, David, George , FRANCESCH SOLLOSO, Andrés , LÓPEZ MACIA, Ángel , CUEVAS MARCHANTE, Carmen , ALBERICIO PALOMERA, Fernando , ACOSTA CRESPO, Gerardo , CRUZ RICONDO, Luis, Javier , GIRALT LLEDÓ, Ernest , GRACIA CANTADOR, Carolina , ISIDRO LOBET, Albert
发明人： TUBBY, David, George , FRANCESCH SOLLOSO, Andrés , LÓPEZ MACIA, Ángel , CUEVAS MARCHANTE, Carmen , ALBERICIO PALOMERA, Fernando , ACOSTA CRESPO, Gerardo , CRUZ RICONDO, Luis, Javier , GIRALT LLEDÓ, Ernest , GRACIA CANTADOR, Carolina , ISIDRO LOBET, Albert
IPC分类号： C07K7/08
CPC分类号： C07K7/08
摘要： New synthetic routes to kahalalide compounds are provided. These are based on convergent approaches using orthogonal protecting schemes, where a better control of the intermediates is taken. Kahalalide F or a mimic of kahalalide F is synthesised by coupling a cyclic part with a side chain fragment, e.g. according to the reaction (1)
摘要翻译：提供了新的合成kahalalide化合物的途径。这些基于使用正交保护方案的收敛方法，其中采用更好的控制中间体。卡哈拉肽F或卡拉沙利汀F的模拟物通过将环状部分与侧链片段偶联而合成。根据反应（1）

2. 发明申请

WO2004073598A2 SOLID PHASE SYNTHESIS OF ANTITUMORAL COMPOUNDS 审中-公开
标题翻译：抗坏血酸化合物的固相合成
公开(公告)号：WO2004073598A2
公开(公告)日：2004-09-02
申请号：PCT/GB2004/000683
申请日：2004-02-20
申请人： PHARMA MAR, S.A.U. , RUFFLES, Graham, Keith , ALVAREZ, Mercedes , ALBERICIO, Fernando , CIRONI, Pablo , CUEVAS, Carmen , FRANCESCH, Andrés , MARFIL, Marta
发明人： ALVAREZ, Mercedes , ALBERICIO, Fernando , CIRONI, Pablo , CUEVAS, Carmen , FRANCESCH, Andrés , MARFIL, Marta
IPC分类号： A61K
CPC分类号： C07D491/14 , C07D207/34 , Y02P20/55
摘要： Lamellarins are prepared using a solid phase synthesis. In a first aspect, the process includes a step as follows: Formula (I) where R 1 to R 15 are as defined, and X is halogen, provided that one of R 2 , R 3 or R 4 is immobilised to a resin. In a second aspect, the process includes a step as follows: Formula (II) where R 1 ' to R 5 ', R 11 ' and R 13 ' are as defined, X 1 and X 2 are halogen, M is a metal function and PG is an amino protecting group, provided that one of that R 2 ', R 3 ' or R 4 ' is immobilised to a resin.
摘要翻译：采用固相合成法制备片美兰。在第一方面，该方法包括如下步骤：其中R1至R15如所定义且X为卤素的式（I），条件是以下之一： R 2，R 3或R 4固定到树脂上。第二方面，该方法包括如下步骤：式（II）其中R 1至R 5'，R 11'，和R 13'如定义，X 1和X 2是卤素，M是金属官能团，PG是氨基保护基，条件是该R 2'，R 3'或R 4'中的一个固定在树脂上。

3. 发明申请

WO2004014917A2 ANTITUMORAL ANALOGS OF LAMELLARINS 审中-公开
标题翻译：玉米淀粉的抗肿瘤模拟
公开(公告)号：WO2004014917A2
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003541
申请日：2003-08-13
申请人： PHARMA MAR, S.A.U. , RUFFLES, Graham, Keith , BAILLY, Christian , FRANCESCH SOLLOSO, Andrés , MATEO URBANO, Maria, Cristina , JIMENEZ GUERRERO, José, Antonio , PASTOR DEL CASTILLO, Alfredo , CUEVAS MARCHANTE, Carmen
发明人： BAILLY, Christian , FRANCESCH SOLLOSO, Andrés , MATEO URBANO, Maria, Cristina , JIMENEZ GUERRERO, José, Antonio , PASTOR DEL CASTILLO, Alfredo , CUEVAS MARCHANTE, Carmen
IPC分类号： C07D491/00
CPC分类号： C07D471/14 , C07D491/14
摘要： New lamellarins are provided of the general formula III wherein X is selected from the group consisting of N, O and S; wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are each independently selected from the group consisting of H, OH, OR’, SH, SR’, SO 2 R’, NHR’, N(R’) 2 , N=R', NHCOR', N(COR’) 2 , NHS0 2 R’, N0 2 , PO(R’ 2 , P0 2 R', C(=0)H, C(=0)R', C0 2 H, C0 2 R’, OPO(R’) 2 , OP0 2 R', OC(=0)H, OC(=0)R’, N=C(R') 2 , substituted or unsubstituted C 1 -C 12 alkyl, substituted or unsubstituted C 1 -C 12 haloalkyl, substituted or unsubstituted C 2 -C 12 alkenyl, substituted or unsubstituted C 2 -C 12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R' groups is independently selected from the group consisting of H, OH, N0 2 , NH 2 , SH, CN, halogen, =0, C(=0)H, C(=O)CH 3 , C0 2 H, C(=0)R', substituted or unsubstituted C 1 -C 18 alkyl, substituted or unsubstituted C 2 -C 18 alkenyl, substituted or unsubstituted C 2 -C 18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted C 1 -C 18 alkoxyl, substituted or unsubstituted C 1 -C 18 aminoalkyl, substituted or unsubstituted C 1 -C 18 aminoacid, substituted or unsubstituted C 1 -C 18 thioalkyl, substituted or unsubstituted C 1 -C 18 alkylsulfinyl, substituted or unsubstituted C 1 -C 18 alkylsulfonyl; wherein the pairs of groups R 1 and R 2 , R 2 and R 3 , R 3 and R 4 , R 3 and R 9 , R 4 and R 9 , R 9 and R 5 , R 9 and R 6 , or R 6 and R 7 , R 7 and R 8 may be joined into a carbocyclic or heterocyclic ring system; and the dotted line represents an single or double bond; or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof.
摘要翻译：提供通式III的新层合体，其中X选自N，O和S; 其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自H，OH，OR'，SH，SR'，SO2R'，NHR'，N（R' 2，N = R'，NHCOR'，N（COR'）2，NHS02R'，N02，PO（R'2，P02R'，C（= O）H，C（= O）R'，CO 2 H，CO 2 R' ，OPO（R'）2，OPO 2 R'，OC（= O）H，OC（= O）R'，N = C（R'）2，取代或未取代的C 1 -C 12烷基，取代或未取代的C 1 -C 12卤代烷基取代或未取代的C 2 -C 12烯基，取代或未取代的C 2 -C 12炔基，取代或未取代的芳基，取代或未取代的芳烷基和取代或未取代的杂芳族化合物;其中每个R'基团独立地选自H，OH ，N 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，C（= O）R'，取代或未取代的C 1 -C 18烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基，取代或未取代的C 1 -C 18烷氧基，取代或未取代的C 1 -C 18氨基烷基，亚取代或未取代的C1-C18氨基酸，取代或未取代的C1-C18硫代烷基，取代或未取代的C1-C18烷基亚磺酰基，取代或未取代的C1-C18烷基磺酰基; 其中基团R 1和R 2，R 2和R 3，R 3和R 4，R 3和R 9，R 4和R 9，R 9和R 5，R 9和R 6，或R 6和R 7，R 7和R 8可以连接成碳环或杂环系统; 虚线表示单键或双键; 或其药学上可接受的盐，衍生物，前药或立体异构体。

4. 发明申请

WO2004035613A2 NEW ANTITUMORAL COMPOUNDS 审中-公开
标题翻译：新型抗菌化合物
公开(公告)号：WO2004035613A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/033207
申请日：2003-10-20
申请人： PHARMA MAR, S.A.U. , FAIRCLOTH, Glynn, Thomas , ELICES, Mariano , SASAK, Halina , AVILÉS MARIN, Pablo, Manuel , CUEVAS MARCHANTE, Maria del Carmen
发明人： FAIRCLOTH, Glynn, Thomas , ELICES, Mariano , SASAK, Halina , AVILÉS MARIN, Pablo, Manuel , CUEVAS MARCHANTE, Maria del Carmen
IPC分类号： C07K7/00
CPC分类号： C07K7/08 , A61K38/00 , C07K7/56 , C07K14/4748
摘要： The present invention is directed to new kahalalide antitumoral compounds, in particular to analogues of kahalalide F, useful as antitumoral, antiviral, antifungal agents and in the treatment of psoriasis.
摘要翻译：本发明涉及新的卡伐拉定抗肿瘤化合物，特别是可用作抗肿瘤，抗病毒，抗真菌剂和治疗牛皮癣的卡拉沙利肽F的类似物。

5. 发明申请

WO2004015143A2 SEQUENCES FROM AN ENDOSYMBIONT AND THEIR USES 审中-公开
标题翻译：来自内皮细胞的序列及其用途
公开(公告)号：WO2004015143A2
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003538
申请日：2003-08-13
申请人： PHARMA MAR, S.A.U. , PEREZ ESTEBAN, Beatriz , APARICIO PEREZ, Tomás , VELASCO IGLESIAS, Ana , HENRIQUEZ PELAEZ, Rubén , MUÑOZ MORENO, Rosario , MOSS, Claire , MCKENZIE, Douglas
发明人： PEREZ ESTEBAN, Beatriz , APARICIO PEREZ, Tomás , VELASCO IGLESIAS, Ana , HENRIQUEZ PELAEZ, Rubén , MUÑOZ MORENO, Rosario , MOSS, Claire , MCKENZIE, Douglas
IPC分类号： C12R1/00
CPC分类号： C07K14/43504 , A61K38/00
摘要： rDNA corresponding to an endosymbiotic bacteria associated with Ecteinascidia turbinata has been identified. The bacterium appears to be responsible for the biosynthesis of ecteinascidin compounds. The 16S rDNA sequence corresponding to Candidatus Endoecteinascidia frumentensis SEQ ID NO: 1 has been deposited in GeneBank with the accession number AY054370.
摘要翻译：已经鉴定出与Ecteinascidia turbinata相关的内分泌细菌相应的rDNA。该细菌似乎是对ecteinidinidin化合物的生物合成的责任。对应于Candidatus Endoecteinascidia frumentensis SEQ ID NO：1的16S rDNA序列已经保藏在GeneBank中，登录号为AY054370。

6. 发明申请

WO2003066638A2 THE SYNTHESIS OF NATURALLY OCCURING ECTEINASCIDINS AND RELATED COMPOUNDS 审中-公开
标题翻译：天然抗氧化剂及相关化合物的合成
公开(公告)号：WO2003066638A2
公开(公告)日：2003-08-14
申请号：PCT/GB2003/000481
申请日：2003-02-04
申请人： PHARMA MAR, S.A.U. , MENCHACA, Roberto , MARTÍNEZ, Valentin , RODRÍGUEZ, Roberto , RODRÍGUEZ, Natividad , GALLEGO, Pilar , CUEVAS, Carmen , MUNT, Simon , MANZANARES, Ignacio
发明人： MENCHACA, Roberto , MARTÍNEZ, Valentin , RODRÍGUEZ, Roberto , RODRÍGUEZ, Natividad , GALLEGO, Pilar , CUEVAS, Carmen , MUNT, Simon , MANZANARES, Ignacio
IPC分类号： C07D515/22
CPC分类号： C07D515/18 , C07D515/22
摘要： Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
摘要翻译：具有环E的醌环的白in素化合物作为抗癌剂是有活性的。提供相关方法和化合物。

7. 发明申请

WO2007101235A2 IMPROVED ANTITUMORAL TREATMENTS 审中-公开
标题翻译：改善抗肿瘤治疗
公开(公告)号：WO2007101235A2
公开(公告)日：2007-09-07
申请号：PCT/US2007/062936
申请日：2007-02-28
申请人： PHARMA MAR, S.A.U. , FAIRCLOTH, Glynn Thomas , AVILES MARIN, Pablo Manuel , LEPAGE, Doreen , SAN MIGUEL IZQUIERDO, Jesus , PANDIELLA, Atanasio
发明人： FAIRCLOTH, Glynn Thomas , AVILES MARIN, Pablo Manuel , LEPAGE, Doreen , SAN MIGUEL IZQUIERDO, Jesus , PANDIELLA, Atanasio
CPC分类号： A61K45/06 , A61K38/15 , A61K38/2013 , A61K38/212 , A61K2300/00
摘要： The present invention relates to combinations of aplidine or aplidine analogues with other antitumoral agents, and the use of these combinations in the treatment of cancer, in particular in the treatment of lung cancer, breast cancer, colon cancer, prostate cancer, renal cancer, melanoma, multiple myeloma, leukemia and lymphoma.
摘要翻译：本发明涉及aplidine或aplidine类似物与其他抗肿瘤剂的组合，以及这些组合在治疗癌症中的用途，特别是在治疗肺癌，乳腺癌，结肠癌，前列腺癌，肾癌，黑素瘤中的用途，多发性骨髓瘤，白血病和淋巴瘤。

8. 发明申请

WO2005039584A1 IMPROVED ANTITUMORAL COMBINATIONS CONTAINING ET-743 AND A CRUCIFEROUS AND A CRUCIFEROUS INDOLE COMPOUND 审中-公开
标题翻译：含有ET-743和CRUCIFEROUS和CRUCIFEROUS INDOLE化合物的改进的抗肿瘤组合
公开(公告)号：WO2005039584A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004358
申请日：2004-10-14
申请人： PHARMA MAR, S.A.U. , DONALD, Sarah , GESCHER, Andreas , JIMENO DONAQUE, José, María
发明人： DONALD, Sarah , GESCHER, Andreas , JIMENO DONAQUE, José, María
IPC分类号： A61K31/495
CPC分类号： A61K31/404 , A61K31/495 , A61K2300/00
摘要： Administration of a cruciferous indole compound can reduce undesirable toxic side effects inherent in the anti-tumor therapy with ET-743 before during or after administration of the ET-743.
摘要翻译：在施用ET-743之前或之后，施用十字花科吲哚化合物可以减少ET-743在抗肿瘤治疗中固有的不良毒性副作用。

9. 发明申请

WO2004011458A1 TOTAL SYNTHESIS OF MYRIAPORONES 审中-公开
标题翻译： MYRIAPORONES的总合成
公开(公告)号：WO2004011458A1
公开(公告)日：2004-02-05
申请号：PCT/GB2003/003327
申请日：2003-07-30
申请人： PHARMA MAR, S.A.U. , RUFFLES, Graham, Keith , PEREZ ALVAREZ, Marta , DEL POZO LOSADA, Carlos , FRANCESCH SOLLOSO, Andres , CUEVAS MARCHANTE, Carmen
发明人： PEREZ ALVAREZ, Marta , DEL POZO LOSADA, Carlos , FRANCESCH SOLLOSO, Andres , CUEVAS MARCHANTE, Carmen
IPC分类号： C07D407/06
CPC分类号： C07D407/06 , A61K31/35 , C07D493/08 , Y02P20/55
摘要： Compounds of the general formula (I) or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR' 3 , SOR', SO 2 X, C(=0)R', C(=O)OR', C(=O)NR', substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R' is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R" is selected from the group consisting of H, OH, OR', OCOR', SH, SR', SOR', S0 2 R', N0 2 , NH 2 , NHR', N(R') 2 , NHCOR', N(COR') 2 , NHS0 2 R', CN, halogen, C(=0)H, C(=0)R', C0 2 H, C0 2 R', CH 2 0R, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of US 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.
摘要翻译：提供了通式（I）的化合物或其药学上可接受的盐，衍生物，前药或立体异构体：其中由R定义的取代基各自独立地选自H，SiR'3，SOR'，SO2X， C（= O）R'，C（= O）OR'，C（= O）NR'，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，芳基，杂芳基或芳烷基; 基团R'选自取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，氨基烷基，芳基，芳烷基和杂环基; 并且基团R“选自H，OH，OR'，OCOR'，SH，SR'，SOR'，SO 2 R'，NO 2，NH 2，NHR'，N（R'）2，NHCOR' N（COR'）2，NHS02R'，CN，卤素，C（= O）H，C（= O）R'，CO 2 H，CO 2 R'，CH 20 R，取代或未取代的烷基，取代或未取代的卤代烷基，取代或未取代的亚烷基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的芳烷基和取代或未取代的杂芳族化合物;条件是该化合物不是US 5,514,708的化合物1,3或4，这些化合物具有抗肿瘤活性。还提供了合成路线。

10. 发明申请

WO2005049029A1 COMBINATION THERAPY COMPRISING THE USE OF ET-743 AND DOXORUBICIN FOR TREATING CANCER 审中-公开
标题翻译：结合使用ET-743和DOXORUBICIN治疗癌症的联合治疗
公开(公告)号：WO2005049029A1
公开(公告)日：2005-06-02
申请号：PCT/GB2004/050025
申请日：2004-11-12
申请人： PHARMA MAR, S.A.U. , RUFFLES, Graham , GIANNI, Luca , D'INCALCI, Maurizio , DE BRAUD, Flippo , MARSONI, Silvia , JIMENO DONAQUE, José María , LOPEZ LAZARO, Luis
发明人： GIANNI, Luca , D'INCALCI, Maurizio , DE BRAUD, Flippo , MARSONI, Silvia , JIMENO DONAQUE, José María , LOPEZ LAZARO, Luis
IPC分类号： A61K31/495
CPC分类号： A61K31/704 , A61K31/495 , A61K45/06
摘要： Methods of treating a human body for cancer are provided. In one aspect, a therapeutic amount of doxorubicin is administered in combination with ET-743 in a dose range between 0.5 and 1 mg/m 2 . In a related aspect, an effective therapeutic amount of ET-743 is administered in combination with doxorubicin in a dose range between 40 and 80 mg/m 2 .
摘要翻译：提供了治疗人体癌症的方法。一方面，治疗量的多柔比星与ET-743联合施用，剂量范围为0.5至1mg / m 2。在相关方面，ET-743的有效治疗量与多柔比星联合施用，剂量范围为40-80mg / m 2。

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