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31. 发明公开

EP1635831A1 COMBINED USE OF ECTEINASCIDIN-743 AND PLATINUM ANTINEOPLASTIC COMPOUNDS 审中-公开
标题翻译：海鞘素743和铂抗肿瘤化合物联合应用
公开(公告)号：EP1635831A1
公开(公告)日：2006-03-22
申请号：EP04735600.1
申请日：2004-06-01
申请人： Pharma Mar, S.A.U.
发明人： D'INCALCI, Maurizio , GIANNI, Luca , GIAVAZZI, Rafaella , GARCIA MARTIN, M., Inst. Catalan de Oncologia , JUDSON, Ian , JIMENO, Donaque Jose Maria, Poligono Ind. La Mina , SESSA, Cristiana
IPC分类号： A61K31/495 , A61K31/282 , A61P35/00
CPC分类号： A61K31/282 , A61K31/4995 , A61K31/555 , A61K33/24 , A61K2300/00
摘要： ET-743 can be used to mitigate resistance to and potentiate the cytotoxic effects of a platinum coordination complex anti-neoplastic agent in a human cancer patient.

32. 发明授权

EP2664623B1 New antitumoral compounds 有权
标题翻译：新的抗肿瘤化合物
公开(公告)号：EP2664623B1
公开(公告)日：2015-03-04
申请号：EP13180582.2
申请日：2004-09-09
申请人： Pharma Mar, S.A.U.
发明人： Fernandez Donis, Ariadna , Giralt Lledó, Ernest , Gracia Cantador, Carolina , López Rodríguez, Pilar , Varon Colomer, Sonia , Cuevas Marchante, Carmen , López Macia, Ángel , Francesch Solloso, Andrés , Jiménez García, José-Carlos , Royo Expósito, Miriam , Albericio Palomera, Fernando
IPC分类号： C07K11/02 , C07K7/64 , A61K38/15
CPC分类号： C07K7/08 , A61K38/00 , C07K7/56 , C07K11/02

33. 发明授权

EP2305689B1 The synthesis of naturally occuring ecteinascidins and related compounds 有权
标题翻译：天然存在的海鞘素和相关化合物的制备
公开(公告)号：EP2305689B1
公开(公告)日：2014-04-09
申请号：EP10181699.9
申请日：2003-02-04
申请人： Pharma Mar S.A.U.
发明人： Menchaca, Roberto , Martinez, Valentin , Rodriguez, Alberto , Rodriguez, Natividad , Gallego, Pilar , Cuevas, Carmen , Munt, Simon , Manzanares, Ignacio
IPC分类号： C07D515/22 , A61K31/50 , A61P35/00
CPC分类号： C07D515/18 , C07D515/22

34. 发明公开

EP2305689A1 The synthesis of naturally occuring ecteinascidins and related compounds 有权
标题翻译： Herstellung vonnatürlichvorkommenden Ecteinascidinen und verwandten Verbindungen
公开(公告)号：EP2305689A1
公开(公告)日：2011-04-06
申请号：EP10181699.9
申请日：2003-02-04
申请人： Pharma Mar S.A.U.
发明人： Menchaca, Roberto , Martinez, Valentin , Rodriguez, Alberto , Rodriguez, Natividad , Gallego, Pilar , Cuevas, Carmen , Munt, Simon , Manzanares, Ignacio
IPC分类号： C07D515/22 , A61K31/50 , A61P35/00
CPC分类号： C07D515/18 , C07D515/22
摘要： The present invention provides compounds of formula:

wherein
R a and R b together with the carbon to which they are attached form a group of formula:

where each X 1 is independently selected from hydrogen or substituted or unsubstituted R', OR', -(C=O)R', substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl; wherein R' is selected from the group consisting of H, OH, NO 2 NH 2 , SH, CN, halogen, C(=O)H, C(=O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic;
where R d is a substituted or unsubstituted R', OR',-(C=O)R', substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; wherein R' is selected from the group consisting of OH, NO 2 , NH 2 , SH, CN, halogen, C(=O)H, C(=O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic;
R 7 is -OCH 3 and R 8 is -OH or R 7 and R 8 together form a group -O-CH 2 -O-;
R 12a is hydrogen, acyl, alkenyl, or alkyl-O-CO-;
R 21 is -H, OH or CN;
X is -O- or -NH-;
R 5 and R 18 are -OX 1 , wherein each X 1 is independently selected from hydrogen, 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, and -C(=O)R' wherein R' is selected from hydrogen, OH, NO 2 , NH 2 , SH, CN, halogen, C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl, and heterocyclic.
摘要翻译：本发明提供下式的化合物：其中R a和R b与它们所连接的碳一起形成下式：其中每个X 1独立地选自氢或取代或未取代的R'，OR'， - （ C = O）R'，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基和取代或未取代的芳烷基; 其中R'选自H，OH，NO 2 NH 2，SH，CN，卤素，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，C C 1 -C 6烷基，烯基，炔基，芳基，芳烷基和杂环基; 其中R d是取代或未取代的R'，OR'， - （C = O）R'，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基或取代的或未取代的芳烷基; 其中R'选自OH，NO 2，NH 2，SH，CN，卤素，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，C 1 -C 6烷基，烯基，炔基，芳基，芳烷基和杂环基; R 7是-OCH 3，R 8是-OH或R 7和R 8一起形成-O-CH 2 -O-基团; R 12a是氢，酰基，烯基或烷基-O-CO-; R 21是-H，OH或CN; X是-O-或-NH-; R 5和R 18是-OX 1，其中每个X 1独立地选自氢，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，取代的或未取代的芳基，和-C（= O）R'，其中R'选自氢，OH，NO 2，NH 2，SH，CN，卤素，C 1 -C 6烷基，烯基，炔基，芳基，芳烷基，和杂环。

35. 发明授权

EP1572726B1 4-METHYLHEXANOIC KAHALALIDE F COMPOUND 有权
标题翻译： 4-甲基己的Kahalalide˚F化合物
公开(公告)号：EP1572726B1
公开(公告)日：2010-12-08
申请号：EP03779140.7
申请日：2003-10-20
申请人： Pharma Mar, S.A.U.
发明人： FAIRCLOTH, Glynn, Thomas , ELICES, Mariano , SASAK, Halina , AVILES MARIN, Pablo, Manuel , CUEVAS MARCHANTE, Maria del Carmen
IPC分类号： C07K7/64 , A61K38/15 , A61P35/00
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.

36. 发明授权

EP1689404B9 COMBINATION OF ET-743 WITH 5-FLUOROURACIL PRO-DRUGS FOR THE TREATMENT OF CANCER 有权
标题翻译： ET-743与5-氟尿嘧啶前体药物用于治疗癌症的组合
公开(公告)号：EP1689404B9
公开(公告)日：2009-04-22
申请号：EP04798717.7
申请日：2004-11-15
申请人： Pharma Mar, S.A.U.
发明人： RYBAK, Mary, Ellen
IPC分类号： A61K31/498 , A61K31/513 , A61K31/7068 , A61P35/00
CPC分类号： A61K31/498 , A61K31/495 , A61K31/513 , A61K31/7068 , A61K2300/00
摘要： Methods of treating a human body for cancer are provided. In one aspect, a therapeutic amount of capecitabine is administered in combination with ET-743 in a dose range between 0.75 and 1.4 mg/m2 for Et-743. In a related aspect, an effective therapeutic amount of ET-743 is administered in combination with capecitabine in a dose range between 1500 to 2500 mg/m/day for capecitabine.

37. 发明授权

EP1532139B1 TOTAL SYNTHESIS OF MYRIAPORONES 有权
标题翻译： MYRIAPORONEN的全合成
公开(公告)号：EP1532139B1
公开(公告)日：2007-06-13
申请号：EP03771210.6
申请日：2003-07-30
申请人： Pharma Mar, S.A.U.
发明人： PEREZ ALVAREZ, Marta, Poligono Industrial La Mina , DEL POZO LOSADA, C., Poligono Industrial La Mina , FRANCESCH SOLLOSO, A., Poligono Industrial La Mina , CUEVAS MARCHANTE, C., Poligono Industrial La Mina
IPC分类号： C07D407/06 , C07D493/08 , C07D303/32 , A61P35/00 , A61K31/35
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', SO2X, 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', S02R', N02, NH2, NHR', N(R')2, NHCOR', N(COR')2, NHS02R', CN, halogen, C(=0)H, C(=0)R', C02H, C02R', CH20R, 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.

38. 发明公开

EP1596879A1 USE OF KAHALALIDE COMPOUNDS FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF PSORIASIS 有权
标题翻译：作者的Kahalalide化合物用于生产药物牛皮癣的治疗
公开(公告)号：EP1596879A1
公开(公告)日：2005-11-23
申请号：EP04714847.3
申请日：2004-02-26
申请人： Pharma Mar, S.A.U.
发明人： IZQUIERDO DELSO, Miguel Angel
IPC分类号： A61K38/12 , A61P17/06
CPC分类号： C07K7/08 , A61K38/00 , C07K7/56 , C07K14/4748
摘要： Kahalalide compounds, in particular kahalalide F, are of use in a method to treat a mammal suffering from skin disease with avoiding toxicity and leading to clinical improvement.

39. 发明公开

EP1572726A2 4-METHYLHEXANOIC KAHALALIDE F COMPOUND 有权
标题翻译： 4-甲基己的Kahalalide˚F化合物
公开(公告)号：EP1572726A2
公开(公告)日：2005-09-14
申请号：EP03779140.7
申请日：2003-10-20
申请人： Pharma Mar, S.A.U.
发明人： FAIRCLOTH, Glynn, Thomas , ELICES, Mariano , SASAK, Halina , AVILES MARIN, Pablo, Manuel , CUEVAS MARCHANTE, Maria del Carmen
IPC分类号： C07K7/64 , A61K38/15 , A61P35/00
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.

40. 发明公开

EP1472261A2 THE SYNTHESIS OF NATURALLY OCCURING ECTEINASCIDINS AND RELATED COMPOUNDS 审中-公开
标题翻译：生产自然发生的海鞘素和相关链接
公开(公告)号：EP1472261A2
公开(公告)日：2004-11-03
申请号：EP03737360.2
申请日：2003-02-04
申请人： Pharma Mar S.A.U.
发明人： MENCHACA, Roberto,Pharma Mar, S.A.U. , MARTINEZ, Valentin,Pharma Mar, S.A.U. , RODRIGUEZ, Alberto,Pharma Mar, S.A.U. , RODRIGUEZ, Natividad,Pharma Mar, S.A.U. , GALLEGO, Pilar,Pharma Mar, S.A.U. , CUEVAS, Carmen,Pharma Mar, S.A.U. , MUNT, Simon,Pharma Mar, S.A.U. , MANZANARES, Ignacio,Pharma Mar, S.A.U.
IPC分类号： C07D515/22 , A61K31/50 , A61P35/00
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.

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