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1. 发明申请

WO2009016516A8 CYTOTOXIC AGENTS COMPRISING NEW TOMAYMYCIN DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：包含新霉素衍生物的细胞毒药物及其治疗用途
公开(公告)号：WO2009016516A8
公开(公告)日：2009-04-16
申请号：PCT/IB2008002869
申请日：2008-07-18
申请人： SANOFI AVENTIS , BOUCHARD HERVE , CHARI RAVI V J , COMMERCON ALAIN , DENG YONGHONG , GAUZY LAURENCE
发明人： BOUCHARD HERVE , CHARI RAVI V J , COMMERCON ALAIN , DENG YONGHONG , GAUZY LAURENCE
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention relates to novel tomaymicine derivatives comprising a linker. It also relates to the conjugate molecules that comprise one or more of said tomaymicine derivatives covalently linked to a cell binding agent through a linking group that is present on the linker of the tomaymycin derivative. It also relates to the preparation of the tomaymicine derivatives and of the conjugate molecules.
摘要翻译：本发明涉及包含接头的新颖的托美米丁衍生物。本发明还涉及包含一个或多个通过存在于茅茅霉素衍生物的接头上的连接基团与细胞结合剂共价连接的所述茅草碱衍生物的缀合物分子。它还涉及tomaymicine衍生物和缀合物分子的制备。

2. 发明申请

WO2007144709A3 LEPTOMYCIN DERIVATIVES 审中-公开
标题翻译： LEPTOMYCIN衍生物
公开(公告)号：WO2007144709A3
公开(公告)日：2008-06-12
申请号：PCT/IB2007001328
申请日：2007-05-23
申请人： SANOFI AVENTIS , BOUCHARD HERVE , COMMERCON ALAIN , CHARI RAVI V J
发明人： BOUCHARD HERVE , COMMERCON ALAIN , CHARI RAVI V J
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/6863 , A61K47/6803
摘要： Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.
摘要翻译：公开了具有可与细胞结合试剂如抗体缀合的具有部分例如硫化物或二硫化物的紫霉素衍生物。还描述了这种灵霉素衍生物缀合物的治疗用途; 这样的缀合物具有治疗用途，因为它们可以以靶向的方式将细胞毒性的曲霉素衍生物递送到特定细胞群体。

3. 发明申请

WO2009016516A3 CYTOTOXIC AGENTS COMPRISING NEW TOMAYMYCIN DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：包含新型甲氧嘧啶衍生物及其治疗用途的细胞毒性剂
公开(公告)号：WO2009016516A3
公开(公告)日：2009-06-11
申请号：PCT/IB2008002869
申请日：2008-07-18
申请人： SANOFI AVENTIS , BOUCHARD HERVE , CHARI RAVI V J , COMMERCON ALAIN , DENG YONGHONG , GAUZY LAURENCE
发明人： BOUCHARD HERVE , CHARI RAVI V J , COMMERCON ALAIN , DENG YONGHONG , GAUZY LAURENCE
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention relates to novel tomaymicine derivatives comprising a linker. It also relates to the conjugate molecules that comprise one or more of said tomaymicine derivatives covalently linked to a cell binding agent through a linking group that is present on the linker of the tomaymycin derivative. It also relates to the preparation of the tomaymicine derivatives and of the conjugate molecules.
摘要翻译：本发明涉及包含连接体的新颖的甲氧基衍生物。它还涉及包含一种或多种通过存在于茅屋霉素衍生物的接头上的连接基团与细胞结合剂共价连接的所述柚皮苷衍生物的缀合物分子。它还涉及制备汤姆米明衍生物和共轭分子。

4. 发明申请

WO9905165A8 STREPTOGRAMINES, THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： STREPTOGRAMINES，他们的制备和组合物
公开(公告)号：WO9905165A8
公开(公告)日：1999-04-29
申请号：PCT/FR9801639
申请日：1998-07-24
申请人： RHONE POULENC RORER SA , COMMERCON ALAIN , BOUCHARD HERVE , RIBEILL YVES , BACQUE ERIC , RONAN BAPTISTE , BARRIERE JEAN CLAUDE , PUCHAULT GERARD , TERRIER CORINNE
发明人： COMMERCON ALAIN , BOUCHARD HERVE , RIBEILL YVES , BACQUE ERIC , RONAN BAPTISTE , BARRIERE JEAN-CLAUDE , PUCHAULT GERARD , TERRIER CORINNE
IPC分类号： A61K38/00 , A61K38/05 , A61K38/08 , A61P31/04 , C07K5/078
CPC分类号： C07K5/06182 , A61K38/00
摘要： The invention concerns derivatives of group A of streptogramines of general formula (I) in which R1 is a -NR'R'' radical in which R' is a hydrogen atom or a methyl radical, and R'' is a hydrogen atom, an alkyl, cycloalkyl, allyl, propynyl, benzyl radical or -OR''', R''' being a hydrogen atom, an alkyl, cycloalkyl, allyl, propynyl or benzyl radical, or -NR3R4, R3 and R4 representing a methyl radical, or forming together with the nitrogen atom to which they are bound a saturated or unsaturated heterocyclic compound with 5 or 6 chains, further capable of containing another heteroatom selected among nitrogen, oxygen or sulphur; R2 is a hydrogen atom or a methyl or ethyl radical, and the bond --- represents a single or double bond, and in which, except if it is specified, the alkyl radicals are linear or branched and contain 1 to 6 carbon atoms, the cycloalkyl radicals contain 3 to 4 carbon atoms, and the chain in position 16 means: when R'' is other than -OR''' or -NR3R4, the epimer R or the mixture of epimers R and S in which the epimer R constitutes the major part, and when R'' is -OR''' or -NR3R4, the epimers R and S and their mixtures and their salts. Said novel derivatives are particularly useful as antimicrobial agents, optionally combined with components of group B of streptogramines.
摘要翻译：本发明涉及通式（I）的链霉素A组的衍生物，其中R 1为-NR'R“基，其中R'为氢原子或甲基，R”为氢原子，烷基，环烷基，烯丙基，丙炔基，苄基或-OR“，R”'为氢原子，烷基，环烷基，烯丙基，丙炔基或苄基，或-NR3R4，R3和R4表示甲基，或与其结合的氮原子一起与5或6个链结合的饱和或不饱和杂环化合物，还能够含有选自氮，氧或硫的其它杂原子; R2是氢原子或甲基或乙基，并且键 - 表示单键或双键，并且其中除特定之外，烷基是直链或支链的，并且含有1至6个碳原子，环烷基包含3至4个碳原子，第16位的链表示：当R“不是-OR”或-NR 3 R 4时，差向异构体R或混合物差向异构体R和S，其中差向异构体R构成主要部分，当R“为-OR”或-NR 3 R 4时，差向异构体R和S及其混合物及其盐。所述新型衍生物特别可用作抗微生物剂，任选地与链霉菌B组的组分组合。

5. 发明申请

WO2006010641A3 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：新型环状尿素衍生物及其制备方法和作为激酶抑制剂的药物用途
公开(公告)号：WO2006010641A3
公开(公告)日：2006-10-26
申请号：PCT/EP2005008720
申请日：2005-07-25
申请人： AVENTIS PHARMA SA , STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
发明人： STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
IPC分类号： C07D401/06 , A61K31/4166 , C07D401/14
CPC分类号： C07D403/04
摘要： The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
摘要翻译：本发明涉及式（I）的产物：其中p = 0,1和2; A =芳基，杂芳基，碳环或杂环; X =单键; -N（R 6） - ; -NH-烷 - ; 亚; -O-; -C（O） - ; -儿子-; -N（R 6）-C（O） - ; -NH-CO-alk-，-N（R 6）-C（O）-N（R 6'） - ; -N（R6）-C（S）-N（R6' ） - ; -N（R 6）-C（O）O-; -N（R 6）-SO 2 - ; -N（R6）-SO2-N（R6' ） - ; -C（O）-N（R6） - ; -SO 2 NR 6 - ; 和-C（O）O-; L1 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚杂芳基; 全部任选被取代; R1 =氢，烷基，烯基，炔基或环烷基，芳基，杂芳基，芳基烷基，杂芳基烷基; -SO 2 R 9，-C（O）R 9; -C（O）OR 9，-C（O）NR 10 R 11，-C（S）NR 10 R 11，-SO 2 NR 10 R 11; R 2 =氢，烷基，烯基，炔基，环烷基，R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O，N，S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基，烯基，炔基，环烷基，烷氧基，亚烷基二氧基，杂环，芳基和杂芳基，全部任选被取代; S（O）n-烷基; 氨基，烷基氨基，二烷基氨基，任选与N环形成的二烷基氨基，全部任选被取代; R4，R4'和R4“=氢，卤素，烷基，烯基，炔基，环烷基，芳基，杂芳基，氧代; 其中R4，R4'和R4“中的两个可能与C形成可能含有O，N或S的环; L2 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，-O - ， - NR17-，-C（O） - ，SO2; Y =可能含有O，N或S的N-杂环; R5 =氢，卤素，烷基，烯基，炔基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基; 所有这些基团任选地被取代，这些产物以所有异构形式和盐作为医药产品。

6. 发明申请

WO2004072027A2 CHEMICAL DERIVATIVES BINDING VERY SPECIFICALLY WITH G-QUADRUPLEX DNA STRUCTURES AND USE THEREOF AS A SPECIFIC ANTI-CANCER AGENT 审中-公开
标题翻译：化学衍生物与G-四联体DNA结构结合非常明确，并将其用作特异性抗癌药
公开(公告)号：WO2004072027A2
公开(公告)日：2004-08-26
申请号：PCT/FR2004000260
申请日：2004-02-05
申请人： AVENTIS PHARMA SA , CENTRE NAT RECH SCIENT , MUSEUM NAT D HISTOIRE NATURELL , INST CURIE , COMMISSARIAT ENERGIE ATOMIQUE , UNIV REIMS CHAMPAGNE ARDENNE , HITTINGER AUGUSTIN , CAULFIELD THOMAS , MAILLIET PATRICK , BOUCHARD HERVE , MANDINE ELIANE , MERGNY JEAN-LOUIS , GUITTAT LIONEL , RIOU JEAN-FRANCOIS , GOMEZ DENNIS , BELMOKHTAR CHAFKE
发明人： HITTINGER AUGUSTIN , CAULFIELD THOMAS , MAILLIET PATRICK , BOUCHARD HERVE , MANDINE ELIANE , MERGNY JEAN-LOUIS , GUITTAT LIONEL , RIOU JEAN-FRANCOIS , GOMEZ DENNIS , BELMOKHTAR CHAFKE
IPC分类号： A61K45/06 , A61P35/00 , A61P37/00 , C07D215/38 , C07D401/12 , C07D401/14 , C07D
CPC分类号： C07D401/12 , A61K45/06 , C07D215/38 , C07D401/14
摘要： The invention relates to cancer therapy and concerns novel anti-cancer agents exhibiting a highly specific action mechanism. The invention also relates to novel chemical compounds and the therapeutic use thereof in man. The invention describes the preparation of heterocylic diamides of general formula (IB) as highly specific G quadruplex DNA ligands and the use thereof as telomerase inhibitors in man. (IB) nitrogenous aromatic cycle comprising a nitrogen atom in a quaternary form (NR3)p CO distributor (CO)m NR'3)qu X- aromatic or non-aromatic cycle.
摘要翻译：本发明涉及癌症治疗并且涉及展现出高度特异性作用机制的新型抗癌剂。本发明还涉及新型化合物及其在人体中的治疗用途。本发明描述了通式（IB）的杂环二酰胺作为高度特异的G四链体DNA配体的制备及其在人体中作为端粒酶抑制剂的用途。（IB）包含氮原子的季氮形式（NR 3）p CO分配器（CO）m NR'3）q-芳族或非芳族循环的含氮芳族环。

7. 发明申请

WO02096903A3 CHEMICAL DERIVATIVES AND THE USE THEREOF AS AN ANTI-TELOMERASE AGENT 审中-公开
标题翻译：化学衍生物及其作为抗TELOMERASE剂的用途
公开(公告)号：WO02096903A3
公开(公告)日：2003-04-17
申请号：PCT/FR0201767
申请日：2002-05-27
申请人： AVENTIS PHARMA SA , BOUCHARD HERVE , HITTINGER AUGUSTIN
发明人： BOUCHARD HERVE , HITTINGER AUGUSTIN
IPC分类号： C07D215/22 , A61K31/17 , A61K31/203 , A61K31/255 , A61K31/282 , A61K31/4709 , A61K31/4745 , A61K31/505 , A61K31/506 , A61K31/565 , A61K31/661 , A61K31/704 , A61K31/7068 , A61K31/7076 , A61K33/24 , A61K38/43 , A61K45/00 , A61P35/00 , A61P43/00 , C07D215/38 , C07D215/42 , C07D401/14 , C07D409/14 , A61K31/33
CPC分类号： C07D401/14 , C07D215/38 , C07D215/42 , C07D409/14
摘要： The invention relates to cancer therapy and concerns novel anti-cancer agents having a specific action mechanism. The invention also relates to novel chemical compounds and the use thereof in humans.
摘要翻译：本发明涉及癌症治疗，并涉及具有特定作用机制的新型抗癌剂。本发明还涉及新型化合物及其在人体中的用途。

8. 发明专利

CA2693551C CYTOTOXIC AGENTS COMPRISING NEW TOMAYMYCIN DERIVATIVES AND THEIR THERAPEUTIC USE 未知
公开(公告)号：CA2693551C
公开(公告)日：2016-09-20
申请号：CA2693551
申请日：2008-07-18
申请人： SANOFI-AVENTIS
发明人： BOUCHARD HERVE , CHARI RAVI V J , COMMERCON ALAIN , DENG YONGHONG , GAUZY LAURENCE
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
摘要： The invention relates to tomaymicine comprising a linker. It also relates to the conjugate molecules that comprise one or more of said tomaymicine derivatives covalently linked to a cell binding agent through a linking group that is present on the linker of the tomaymicine derivative. It also relates to the preparation of the tomaymicine derivatives and of the conjugate molecules.

9. 发明专利

JO2744B1 CYTOTOXIC AGENTS COMPRISING NEW TOMAYMYCIN DERIVATIVES AND THEIR THERAPEUTIC USE 未知
公开(公告)号：JO2744B1
公开(公告)日：2014-03-15
申请号：JOP20080323
申请日：2008-07-17
申请人： SANOFI AVENTIS
发明人： COMMERCON ALAIN , GAUZY LAURENCE , CHARI RAVI V J , DENG YONGHONG , BOUCHARD HERVE
摘要： The invention relates to novel tomaymicine derivatives comprising a linker. It also relates the conjugate molecules that comprise one or more of said tomaymicine derivatives covalently linked to a cell binding agent through a linking group that is present on the linker of the tomaymycin derivative. It also relates to the preparation of the tomaymicine derivatives and of the conjugate molecules.

10. 发明专利

ES2435779T3 Agentes citotóxicos que comprenden nuevos derivados de tomaimicina y su uso terapéutico 未知
公开(公告)号：ES2435779T3
公开(公告)日：2013-12-23
申请号：ES07290904
申请日：2007-07-19
申请人： SANOFI AVENTIS , SANOFI SA
发明人： GAUZY LAURENCE , BOUCHARD HERVE , COMMERCON ALAIN , DENG YONGHONG , CHARI RAVI V J
IPC分类号： C07D519/00 , C07D487/04
摘要： Compuestos de fórmula (I) donde: representa un enlace sencillo opcional; representa o un enlace sencillo o un doble enlace; con la condición de que cuando represente un enlace sencillo, U y U', iguales o diferentes, representanindependientemente H, y W y W', iguales o diferentes, se seleccionan independientemente del grupo que consisteen -OH, -OR, -OCOR, -OCOOR, -OCONRR', un carbamato cíclico, tal que N10 y C11 son una parte del ciclo,-NRCONRR', -OCSNHR, un tiocarbamato cíclico tal que N10 y C11 son una parte del ciclo, -SH, -SR, -SOR, -SOOR,-SO3 -, -NRSOOR', -NRR', opcionalmente amina cíclica tal que N10 y C11 son una parte del ciclo, -NROR', -NRCOR',-N3, un ciano, un halo, un trialquilo o triarilfosfonio; y cuando represente un doble enlace, U y U' están ausentes y W y W' representan H; - R1, R2, R1', R2' son iguales o diferentes y se eligen independientemente de: H, Haluro o Alquilo opcionalmentesustituido por uno o más Hal, CN, NRR', CF3, OR, Arilo, Het, S(O)qR o R1 y R2 y R1' y R2' forman juntos un dobleenlace que contiene grupo >=B y >=B' respectivamente. - B y B' son iguales o diferentes y se eligen independientemente entre Alquenilo que está opcionalmente sustituidocon uno o más Hal, CN, NRR', CF3, OR, Arilo, Het, S(O)qR o B y B' representan un átomo de oxígeno. - A y A' son iguales o diferentes y se eligen independientemente de: Alquilo o Alquenilo, estando cada unoopcionalmente sustituido por uno o más Hal, CN, NRR', CF3, OR, S(O)qR, Arilo, Het, Alquilo, Alquenilo. - Y e Y' son iguales o diferentes y se eligen independientemente entre H, OR; - q es 0, 1 ó 2 ; - n, n', iguales o diferentes, son 0 ó 1 ; - R y R' son iguales o diferentes y se eligen independientemente entre H, Alquilo, Arilo, estando cada uno de ellosopcionalmente sustituido con Hal, CN, NRR', CF3, R, OR, S(O)qR, Arilo, Het; - T es -NR- o un arilo, cicloalquilo, heterocíclico o heteroarilo de 4 a 10 miembros, estando cada uno de ellosopcionalmente sustituido con uno o más de Hal, CN, NRR', CF3, R, OR, S(O)qR y estando cada uno sustituido conuno o más ligante(s) no escindible(s) elegidos de la siguiente lista.

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