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1. 发明授权

US06391900B1 Cytotoxic tris(oxazole)-containing macrolides 失效
标题翻译：含有细菌毒性的三（恶唑）大环内酯类
公开(公告)号：US06391900B1
公开(公告)日：2002-05-21
申请号：US09601146
申请日：2001-01-12
申请人： Tatsuo Higa , Dolores Garcia Gravalos , Jose Luis Fernandez Puentes
发明人： Tatsuo Higa , Dolores Garcia Gravalos , Jose Luis Fernandez Puentes
IPC分类号： A61P3500
CPC分类号： C07D498/22
摘要： The present invention discloses new cytotoxic tris(oxazole)-containing macrolides having the formula: wherein X represents a lower alkyl; R1 and R2 represent hydrogen or lower alkyl; R3a represents hydrogen, and R3b represents or R3a and R3b together represent oxygen; R4 represents hydrogen, lower alkoxy or lower alkyl; R5 represents hydrogen, carbamoyl, or lower alkanoyl; R6a represents hydrogen, and R6b represents hydroxy, or R6a and R6b together represent oxygen; R7 represents hydrogen, lower alkyl, or hydroxymethyl; R8 represents lower alkoxy or lower alkyl; Y1 represents hydrogen or methyl, and y2 represents hydrogen, or Y1 and Y2 together represent a double bond. Also disclose are methods for treating mammals using the macrolides and pharmaceutical preparations including the macrolides.
摘要翻译：本发明公开了具有下式的新的具有细胞毒性的三（恶唑）的大环内酯类：其中X代表低级烷基; R1和R2表示氢或低级烷基; R3a表示氢，R3b表示R3a和R3b表示氧; R4代表氢，低级烷氧基或低级烷基; R5表示氢，氨基甲酰基或低级烷酰基; R6a表示氢，R6b表示羟基，R6a和R6b表示氧; R7表示氢，低级烷基或羟甲基; R8表示低级烷氧基或低级烷基; Y1表示氢或甲基，y2表示氢，Y1或Y2表示双键。还公开了使用大环内酯类和包括大环内酯类药物制剂治疗哺乳动物的方法。

2. 发明授权

US6087370A Methods of treatment using lamellarin-class alkaloids 失效
标题翻译：使用片剂类生物碱的治疗方法
公开(公告)号：US6087370A
公开(公告)日：2000-07-11
申请号：US216406
申请日：1998-12-18
申请人： Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Ana Rodriguez Quesada
发明人： Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Ana Rodriguez Quesada
IPC分类号： C07D491/147 , A61K31/435 , A61K31/437 , A61K31/4433 , A61K31/4745 , A61K31/475 , A61K31/65 , A61K31/70 , A61K35/56 , A61K38/08 , A61P35/00 , A61P43/00 , A61K31/44
CPC分类号： A61K31/475 , A61K31/437 , A61K31/4745 , A61K31/70 , A61K38/08
摘要： The lamellarin compounds disclosed herein have been found to be inhibitors of MDR, i.e., acquired multidrug resistance, which has become a major problem in the treatment of various cancers. The lamellarin compounds disclosed herein have also been found to be cytotoxic to MDR cells. MDR is believed to be associated with certain alterations in tumor cells, including an over-expression of a certain high molecular weight membrane glycoprotein and a decrease in the ability of the tumor cell to accumulate and retain chemotherapeutic agents. The present invention is thus directed to methods of treating MDR-type tumors with an effective anti-MDR amount (either inhibitory or cytotoxic) of one or more lamellarin compounds, which compounds have been found to be effective antitumoral agents against MDR cells.
摘要翻译：已经发现本文公开的片层蛋白化合物是MDR的抑制剂，即获得性多药耐药性，其已经成为治疗各种癌症的主要问题。已经发现本文公开的片层蛋白化合物对MDR细胞具有细胞毒性。 MDR被认为与肿瘤细胞中的某些改变相关，包括某种高分子量膜糖蛋白的过度表达以及肿瘤细胞累积和保留化学治疗剂的能力的降低。因此，本发明涉及用一种或多种片连蛋白化合物的有效抗MDR量（抑制性或细胞毒性）治疗MDR型肿瘤的方法，该化合物已被发现是抗MDR细胞的有效抗肿瘤药物。

3. 发明授权

US5852033A Methods of treatment using lamellarin-class alkaloids 失效
公开(公告)号：US5852033A
公开(公告)日：1998-12-22
申请号：US496465
申请日：1995-06-29
申请人： Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Ana Rodriguez Quesada
发明人： Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Ana Rodriguez Quesada
IPC分类号： C07D491/147 , A61K31/435 , A61K31/437 , A61K31/4433 , A61K31/4745 , A61K31/475 , A61K31/65 , A61K31/70 , A61K35/56 , A61K38/08 , A61P35/00 , A61P43/00 , A61K31/44
CPC分类号： A61K31/475 , A61K31/437 , A61K31/4745 , A61K31/70 , A61K38/08
摘要： The lamellarin compounds disclosed herein have been found to be inhibitors of MDR, i.e., acquired multidrug resistance, which has become a major problem in the treatment of various cancers. The lamellarin compounds disclosed herein have also been found to be cytotoxic to MDR cells. MDR is believed to be associated with certain alterations in tumor cells, including an over-expression of a certain high molecular weight membrane glycoprotein and a decrease in the ability of the tumor cell to accumulate and retain chemotherapeutic agents. The present invention is thus directed to methods of treating MDR-type tumors with an effective anti-MDR amount (either inhibitory or cytotoxic) of one or more lamellarin compounds, which compounds have been found to be effective antitumoral agents against MDR cells.

4. 发明授权

US07153885B2 Stolonoxides 失效
公开(公告)号：US07153885B2
公开(公告)日：2006-12-26
申请号：US10275377
申请日：2001-05-04
申请人： Rosario Duran , Eva Zubia , Maria J. Ortega , Javier Salva , Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Santiago Naranjo Lozano
发明人： Rosario Duran , Eva Zubia , Maria J. Ortega , Javier Salva , Jose Luis Fernandez Puentes , Dolores Garcia Gravalos , Santiago Naranjo Lozano
IPC分类号： A61K31/335 , C07D407/04
CPC分类号： C07D407/04 , A61K31/341 , A61K31/357
摘要： Naturally occurring stolonoxide compounds, and derivatives thereof, have antitumor activity. Typical compounds are of the formula (I) or a derivative thereof
摘要翻译：天然存在的泛素化合物及其衍生物具有抗肿瘤活性。典型的化合物是式（I）化合物或其衍生物

5. 发明授权

US06559161B1 Cytotoxic pyrido[2,3,4-ki]acridine derivatives, their preparation and their therapeutic use 失效
标题翻译：细胞毒性吡啶并[2,3,4-ki]吖啶衍生物，其制备及其治疗用途
公开(公告)号：US06559161B1
公开(公告)日：2003-05-06
申请号：US10048340
申请日：2002-05-09
申请人： Mercedes Alvarez , Lidia Feliu , Dolores Garcia Gravalos , Jose Luis Fernandez-Puentes
发明人： Mercedes Alvarez , Lidia Feliu , Dolores Garcia Gravalos , Jose Luis Fernandez-Puentes
IPC分类号： A61K314738
CPC分类号： C07D471/06
摘要： The invention provides compounds of formula (I) wherein R1 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a hydroxy group, an alkoxy group having from 1 to 6 carbon atoms, a halogen atom, a nitro group, an amino group, a monoalkylamino group wherein the alkyl moiety has from 1 to 6 carbon atoms, a dialkylamino group wherein each alkyl moiety may be the same or different and each has from 1 to 6 carbon atoms, a dialkoxyamino group wherein each alkoxy moiety may be the same or different and each has from 1 to 6 carbon atoms, an alkanoyalmino group having from 1 to 20 carbon atoms or an alkanesulfonylamino group having from 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms; and R3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an alkoxy group having from 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The compounds exhibit activity against a wide variety of mammalian cancer cell lines.
摘要翻译：本发明提供式（I）化合物，其中R 1表示氢原子，具有1至6个碳原子的烷基，羟基，具有1至6个碳原子的烷氧基，卤素原子，硝基，氨基，其中烷基部分具有1至6个碳原子的单烷基氨基，其中每个烷基部分可以相同或不同并且各自具有1至6个碳原子的二烷基氨基，其中每个烷氧基部分可以是相同或不同，各自具有1至6个碳原子，具有1至20个碳原子的链烷亚氨基或具有1至6个碳原子的烷磺酰氨基; R 2表示氢原子或具有1至6个碳原子的烷基碳原子和R 3表示氢原子，具有1至6个碳原子的烷基或具有1至6个碳原子的烷氧基;及其药学上可接受的盐。该化合物表现出针对各种哺乳动物癌细胞系的活性。

6. 发明授权

US06864283B2 Oxy-and amino-substituted tetrahydrofuryl derivatives with antitumour activity 失效
标题翻译：具有抗肿瘤活性的羟基和氨基取代的四氢呋喃衍生物
公开(公告)号：US06864283B2
公开(公告)日：2005-03-08
申请号：US10203918
申请日：2001-02-16
申请人： Tatsuo Higa , Junichi Tanaka , Dolores Garcia Gravalos
发明人： Tatsuo Higa , Junichi Tanaka , Dolores Garcia Gravalos
IPC分类号： A61K31/341 , A61K35/56 , A61P35/00 , A61P35/02 , A61P43/00 , C07D307/22 , A61K31/34 , C07D307/02 , C07F4/28
CPC分类号： C07D307/22
摘要： Compounds of formula (I) wherein R1is selected from H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or R1 together with R2 forms a saturated or unsaturated heterocyclic ring; R2 and R3 are each, independently, selected from H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or one of R2 or R3 together with R1 forms a saturated or unsaturated heterocyclic ring; or R2 and R3 together form a saturated or unsaturated heterocyclic ring; R4 is selected from H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18, alkynyl, or substituted or unsubstituted aryl, wherein R′ is selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted and unsubstituted aryl; R″ is selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted and unsubstituted aryl; wherein X1, X2 X3 on formula I are independently placed in any particular position of the chain and independently selected from H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, wherein substituent groups defined by R′ are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaromatic; wherein x is 6 to 20; and wherein the dotted lined is one or several optional double bonds placed in any particular position of the side chain; or pharmaceutically acceptable salts thereof are useful as antitumor compounds and include compound IK-8-73-4 of structure (a) which was isolated from a sponge Pachastrissa sp.
摘要翻译：其中R 1选自H，C（= O）R'，P（= O）R'R“，S（= O）R'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炔基或取代或未取代的芳基; 或R 1与R 2一起形成饱和或不饱和杂环; R 2和R 3各自独立地选自H，C（= O）R'，P（= O）R'R“，S（= O）R'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炔基或取代或未取代的芳基; 或R 2或R 3中的一个与R 1一起形成饱和或不饱和杂环; 或R 2和R 3一起形成饱和或不饱和杂环; R 4选自H，C（= O）R'，P（= O）R'R“，S（= O）R'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炔基或取代或未取代的芳基，其中R'选自H，OH，NO 2，NH 2，SH，CN，卤素，C（= O）H，C（ C = O）CH 3，CO 2 H，CO 2 CH 3，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，取代和未取代的芳基; R“选自H，OH，NO 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，取代或未取代的C1- C18烷基，取代或未取代的C2-C18烯基，取代或未取代的C2-C18

7. 发明授权

US06350743B1 Cytotoxic pyridoacridine alkaloids 失效
标题翻译：细胞毒性吡啶并吖啶生物碱
公开(公告)号：US06350743B1
公开(公告)日：2002-02-26
申请号：US09554181
申请日：2001-02-22
申请人： Yoel Kashman , Ganit Koren-Goldshlager , Maurice Aknin , Dolores Garcia Gravalos
发明人： Yoel Kashman , Ganit Koren-Goldshlager , Maurice Aknin , Dolores Garcia Gravalos
IPC分类号： A61K31545
CPC分类号： C07D513/16
摘要： Shermilamine D, a novel cytotoxic pyridoacridine alkaloid of Formula 1, has been isolated from the tunicate Cystodytes violatinctus. The structure of the compound has been established on the basis of 1-D and 2-D NMR data.
摘要翻译：已经从隐孢子虫隐孢子虫（Cystodytes violatinctus）中分离出了具有式1的新型细胞毒性吡啶并吖啶生物碱的Shermilamine D。该化合物的结构是基于1-D和2-D NMR数据建立的。

8. 发明授权

US5925671A Antitumor isocoumarins 失效
标题翻译：抗肿瘤异香豆素
公开(公告)号：US5925671A
公开(公告)日：1999-07-20
申请号：US913099
申请日：1997-11-06
申请人： Librada Canedo Hernandez , Cristina Acebal Sarabia , Dolores Garcia Gravalos
发明人： Librada Canedo Hernandez , Cristina Acebal Sarabia , Dolores Garcia Gravalos
IPC分类号： A61K31/365 , A61K31/37 , A61P35/02 , C07D311/76 , C12P17/06 , C12R1/07 , A61K31/35 , C07D311/04
CPC分类号： C12R1/07 , A61K31/37 , C07D311/76 , C12P17/06
摘要： Antitumor isocoumarins are of general formula (III) where R is --CONH.sub.2 or --CH(CH.sub.3).sub.2, or a pharmaceutically acceptable addition salt thereof. The compound wherein R is --CONH.sub.2 is the known compound amicoumacin A. The compound wherein is --CH(CH.sub.3).sub.2 is a new compound which can be obtained from fermentation of the new marine bacterium Bacillus sp. strain M-00-PHD-090, CECT 4546. ##STR1##
摘要翻译： PCT No.PCT / GB96 / 00537 371日期：1997年11月6日 102（e）日期1997年11月6日PCT提交1996年3月8日PCT公布。公开号WO96 / 27594 日本1996年9月12日抗肿瘤异香豆素具有通式（III），其中R是-CONH 2或-CH（CH 3）2，或其药学上可接受的加成盐。其中R是-CONH 2的化合物是已知的化合物微乳糖素A.其中-CH（CH 3）2的化合物是可以从新型海洋细菌芽孢杆菌属的发酵获得的新化合物。菌株M-00-PHD-090，CECT4546。

9. 发明授权

US5849540A Thiodepsipeptide isolated from a marine actinomycete 失效
标题翻译：从海洋放线菌分离的硫代三肽
公开(公告)号：US5849540A
公开(公告)日：1998-12-15
申请号：US936460
申请日：1997-09-24
申请人： Julia Perez Baz , Francisco Romero Millan , Teresa Garcia De Quesada , Dolores Garcia Gravalos
发明人： Julia Perez Baz , Francisco Romero Millan , Teresa Garcia De Quesada , Dolores Garcia Gravalos
IPC分类号： C12N1/20 , A61K38/00 , C07K7/06 , C12R1/29 , C12P21/00
CPC分类号： C12R1/29 , C07K7/06 , A61K38/00
摘要： The present invention is directed to a novel depsipeptide has been isolated from a new marine strain L-13-ACM2-092 belonging to the family Micromonosporaceae. Its production by aerobic fermentation under controlled conditions of the strain, and the isolation and purification of PM-93135 are described herein. The compound and the fermentation broth demonstrate significant activity against several cancer cell lines. The compound also shows activity against several gram positive bacteria.
摘要翻译：本发明涉及从属于小单孢菌科的新型海洋菌株L-13-ACM2-092中分离出新的脱脂肽。本文描述了在菌株的受控条件下通过需氧发酵的生产以及PM-93135的分离和纯化。化合物和发酵液显示出对几种癌细胞系的显着活性。该化合物还显示针对几种革兰氏阳性菌的活性。

10. 发明授权

US06812245B2 Polycylic xanthones and their use 失效
标题翻译：多晶呫吨酮及其用途
公开(公告)号：US06812245B2
公开(公告)日：2004-11-02
申请号：US10312343
申请日：2003-06-09
申请人： Librada Maria Cañedo , Dolores Garcia Gravalos , Francisco Romero , Fernando Espliego , Julia Perez-Baz
发明人： Librada Maria Cañedo , Dolores Garcia Gravalos , Francisco Romero , Fernando Espliego , Julia Perez-Baz
IPC分类号： A61K3135
CPC分类号： C07D493/04 , C07H17/08 , C12P17/181 , C12R1/03
摘要： A novel class of antitumour compounds has been recognised based on the isolation from a new marine microbe, strain PO13-046, belonging to the genus Actinomadura sp.), of a compound designated IB-00208. The class of the formulae (I) or (II) where R1 can be hydrogen, acyl, alkyl, alkenyl, aryl, benzyl, alkali metal, and/or sugar, and R2 and R3 can be hydrogen, alkyl, or together R2 and R3 form an unsaturated bond. Such compounds demonstrate an interesting activity several cancel cell lines and against Gram-positive bacteria.
摘要翻译：基于与名为IB-00208的化合物的新型海洋微生物属于Actinomadura属植物菌株PO13-046的分离，已经认识到一类新的抗肿瘤化合物。式（I）或（II）的类别，其中R 1可以是氢，酰基，烷基，烯基，芳基，苄基，碱金属和/或糖，R 2和R 3可以是氢，烷基或一起R 2和R 3形成不饱和键。这些化合物表现出一些有趣的活性，一些取消细胞系和革兰氏阳性菌。

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