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1. 发明申请

WO2000049020A2 NOVEL EPOTHILON DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译：新型爱替酮衍生物，其制备方法及其药物应用
公开(公告)号：WO2000049020A2
公开(公告)日：2000-08-24
申请号：PCT/EP2000001332
申请日：2000-02-18
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , SCHWEDE, Wolfgang , BUCHMANN, Bernd , SKUBALLA, Werner , SCHIRNER, Michael , GRIMM, Michael
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D493/00
CPC分类号： C07D417/06 , Y02P20/55
摘要： The invention relates to novel epothilon derivatives of general formula (I), wherein the substituents Y, Z, R1a¿, R1b¿, R2a¿, R2b¿, R3a¿, R3b¿, E, R5¿, R6¿, R7¿, R8¿, R14¿ and X have the meanings cited more specifically in the description. The novel compounds interact with tubulin by stabilizing the formed microtubuli. The compounds are able to influence the cell division in a phase-specific manner and are suited for treating malignant tumors, for example, ovarian cancer, gastric carcinoma, colon cancer, breast cancer, lung cancer, head and neck cancer, malignant melanoma, and acute lymphocytic and myelocytic leukemia. The inventive compounds are suited for use in anti-angiogenic therapy as well as for treating chronic inflammatory diseases (psoriasis, arthritis). In order to prevent uncontrolled cell proliferations and to improve the compatibility of medical implants, the inventive compounds can be applied or incorporated in polymeric materials. The inventive compounds can be used alone or, in order to achieve additive or synergistic effects, in conjunction with additional constituents and substance classes which can be use in tumor therapy.
摘要翻译：本发明涉及通式（I）的新型埃博霉素衍生物，其中取代基Y，Z，R 1a和取代基R 1b和取代基R 2a和取代基R 2b和取代基R 3a和取代基R 3b和取代基E， ;，R6＆Iquest; R7＆Iquest; R8＆Iquest; R14＆Iquest; 和X具有在说明书中更具体引用的含义。新化合物通过稳定形成的微管与微管蛋白相互作用。这些化合物能够以相特异性方式影响细胞分裂，并且适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤和急性淋巴细胞和粒细胞白血病。本发明化合物适用于抗血管生成疗法以及治疗慢性炎症疾病（牛皮癣，关节炎）。为了防止不受控制的细胞增殖并改善医用植入物的相容性，可以将本发明的化合物应用或掺入聚合物材料中。本发明的化合物可以单独使用，或者为了实现累加或协同效应，可以与可用于肿瘤治疗的其他成分和物质类别结合使用。

2. 发明申请

WO2001066154A2 RADIOACTIVELY LABELED EPOTHILONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, AND THEIR BIOCHEMICAL AND PHARMACEUTICAL USE 审中-公开
标题翻译：放射性注明埃博霉素衍生物，进程中为其及其生化和制药用
公开(公告)号：WO2001066154A2
公开(公告)日：2001-09-13
申请号：PCT/EP2001002699
申请日：2001-03-09
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GAY, Jürgen , SKUBALLA, Werner , SCHWEDE, Wolfgang , BUCHMANN, Bernd , BUNTE, Thomas , LICHTNER, Rosemarie
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K51/00
CPC分类号： A61K51/0455 , A61K51/0453
摘要： The invention relates to novel radioactively labeled pharmacologically effective epothilone derivatives of general formula (I), wherein: R1 represents O-PG and hydroxyl, wherein PG is a protective group; R2a, R2b are the same or different and represent, independent of one another, hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl or, together, represent a (CH2)m group, wherein m is equal to 1, 2, 3, 4 or 5; R3 represents a C2-C10 alkyl group, a C2-C10 alkenyl group or a C8-C20 aralkyl each containing 2n tritium atoms, wherein n equals 1 or 2; R4 represents O-PG and hydroxyl; R5 represents hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl and halogen; W-Z represents a CH2-CH2, CH2-O or O-CH2 group; R6 represents hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl, (CH2)s-V and halogen, wherein s equals 1, 2, 3 or 4 and V represents O-PG, hydroxyl or halogen; R7, R8 each represent a hydrogen atom and, together, represent an additional bond or an oxygen atom; A represents aryl, C7-C20 aralkyl, and a group R10-CH=C9-, wherein R9 represents hydrogen, halogen, CN, C1-C20 alkyl, aryl, and C7-C20 aralkyl, and R10 represents hydrogen, C1-C20 alkyl-, aryl-, C7-C20 aralkyl, and; X-Y represents an O-C(=O), an O-CH2, a CH2-C(=O), an NR11-C(=O) and an NR11-SO2 group, wherein R11 represents hydrogen and C1-C10 alkyl. The novel compounds of formula (I) are valuable pharmaceuticals and valuable diagnostic probes for elucidating, for example, active mechanisms and biochemical, pharmacocinketic and/or pharmacodynamic processes.
摘要翻译：本发明涉及通式的新颖放射性标记的药理学活性的埃坡霉素衍生物，其中R <1> O型PG，羟基，其中PG是保护基，R <2A>，R <2B>是相同的或不同的，并独立地氢，C1-C10烷基，芳基，C7-C20芳烷基，或一起为 - （CH 2）M组，其中m是1，2，3，4或5，R <3> C 2 -C 10 - 烷基，C2-C10链烯基或C 8 -C 20 - 芳烷基，各自含有的2n氚原子，其中n是1或2，R <4> O型PG，羟基，R <5>为氢，C1-C10-烷基，芳基，C7-C20芳烷基，卤素，WZ一个CH2-CH2，CH2-O或O-CH 2基团，R <6>是氢，C1-C10烷基，芳基，C7-C20芳烷基，（CH 2）SV，卤素，其中s为1，2，3或4和V O型PG，是羟基或卤素，R <7> - [R <8>是氢原子，一起附加的键或氧原子，a为芳基，C7-C20 芳烷基，基团R <10> -CH = CR <9> - ，其中R <9>为氢，卤素，CN，C1-C20烷基，芳基，C7-C20芳烷基，并且R <10>为氢，C 1 -C C20 是烷基，芳基，C7-C20芳烷基，一个XY OC（= O），O-CH 2，CH 2 C（= O），NR <11> -C（= O），NR <11> -SO 2基团，其中R <11>为氢，C1-C10烷基，式bedeuten.Die新化合物是有价值的药物和用于作用机制的阐明有价值的诊断探针，例如，生物化学，药代动力学和/或药效学过程。

3. 发明申请

WO1995006634A1 NEW 9-CHLORO-PROSTAGLANDIN DERIVATIVES 审中-公开
标题翻译：新的9-氯前列腺素衍生物
公开(公告)号：WO1995006634A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002855
申请日：1994-08-29
申请人： SCHERING AKTIENGESELLSCHAFT , BUCHMANN, Bernd , SKUBALLA, Werner
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C405/00
CPC分类号： B82Y5/00 , A61K47/6951 , C07C405/00 , C07C405/0025
摘要： 9-chloro-prostaglandin derivatives having the formula (I), in which X stands for oxygen or CH2, R stands for hydrogen or straight or branched chain alkyl with 1-6 C atoms and A stands for trans-CH=CH- or -CH2-CH2-, are disclosed, as well as their salts with physiologically neutral bases, when R stands for hydrogen, their clathrates with alpha -, beta - or gamma -cyclodextrin, a process for preparing the same and their pharmaceutical use.
摘要翻译：本发明涉及式（I）其中X为氧或9-氯前列腺素衍生物CH2，R <1>是具有1-6个C原子并且A是反式-CH = CH-或-CH 2氢或直链或支链烷基意味着-CH 2 - ，以及它们与生理上可耐受的碱的盐，当R <1>是氢和它们的具有α-笼形物 - ，β - 或γ-环糊精，其制备和它们的药物用途。

4. 发明申请

WO1994005631A1 9-CHLOROPROSTAGLANDIN ESTERS AND AMIDES AND THEIR USE IN THE PREPARATION OF DRUGS 审中-公开
标题翻译： 9-氯前列腺素的酯和酰胺和它们用于药物的生产
公开(公告)号：WO1994005631A1
公开(公告)日：1994-03-17
申请号：PCT/DE1993000809
申请日：1993-08-31
申请人： SCHERING AKTIENGESELLSCHAFT , BUCHMANN, Bernd , SKUBALLA, Werner , EKERDT, Roland , McDONALD, Fiona , THIERAUCH, Karl-Heinz
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C405/00
CPC分类号： B82Y5/00 , A61K31/557 , A61K47/6951 , C07C405/00 , C07C405/0041
摘要： The invention concerns 9-chloroprostaglandin esters and amides of general formula (I), methods of preparing them and their use as drugs.

5. 发明申请

WO1988007037A1 6-OXOPROSTAGLANDIN-E DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译： 6-OXOPROSTAGLANDIN-E衍生物，其生产方法及其药物应用
公开(公告)号：WO1988007037A1
公开(公告)日：1988-09-22
申请号：PCT/DE1988000151
申请日：1988-03-11
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , SKUBALLA, Werner , VORBRÜGGEN, Helmut , STÜRZEBECHER, Claus-Steffen , THIERAUCH, Karl-Heinz , SCHILLINGER, Ekkehard
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07C405/00
摘要： 6-Oxoprostaglandin-E, derivatives having the formula (I), in which R signifies the residue COOR where R signifies a hydrogen atom, a C1-10 alkyl, a C5-6 cycloalkyl, a C6-C10 aryl group, a heterocyclic residue or the residue CONHSO2R where R signifies a C1-10 alkyl, C5-6 cycloalkyl or C6-10 aryl; A signifies a CH=CH or a -C=C- group in an E configuration; W signifies a free or functionally modified hydroxymethylene group or a free or functionally modified group having the formula (II), in which the group OH may be either alpha - or beta - permanent; D signifies a straight-chain or branched-chain alkylene group with between 1 and 5 C atoms; E signifies a -C=C- group or a C2-C4 alkenyl group; R signifies a C1-C10 alkyl group, a C3-C10 cycloalkyl group or a C6-C10 aryl -C=C- group which may have been substituted, or a heterocyclic group; R signifies a free or functionally modified hydroxy and R and, where R signifies a hydrogen atom, the salts of said group with physiologically compatible bases; also the alpha -, beta - or gamma - cyclodextrinclothrate of the compounds having the formula (I). Process for their production and their pharmaceutical application.
摘要翻译： 6-氧前列腺素E，具有式（I）的衍生物，其中R 1表示残基COOR 2，其中R 2表示氢原子，C1-10烷基，C5-6环烷基， C 6 -C 10芳基，杂环残基或残基CONHSO 2 R 5，其中R 5表示C1-10烷基，C5-6环烷基或C6-10芳基; A表示E配置中的CH = CH或-C = C-基团; W表示游离或官能改性的羟基亚甲基或具有式（II）的游离或官能改性基团，其中基团OH可以是α-或β-永久的; D表示具有1至5个C原子的直链或支链亚烷基; E表示-C = C-基或C 2 -C 4烯基; R 3表示可以被取代的C1-C10烷基，C3-C10环烷基或C6-C10芳基-C = C-基或杂环基; R 4表示游离或官能改性的羟基和R 4，并且其中R 2表示氢原子，所述基团的盐与生理上相容的碱基相同; 还有具有式（I）的化合物的α，β或γ-环糊精碱。生产过程及其药物应用。

6. 发明申请

WO1995020563A1 NEW LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS 审中-公开
标题翻译：新白三烯B4衍生物，用于生产及其作为药物
公开(公告)号：WO1995020563A1
公开(公告)日：1995-08-03
申请号：PCT/EP1994000215
申请日：1994-01-27
申请人： SCHERING AKTIENGESELLSCHAFT , SKUBALLA, Werner , BUCHMANN, Bernd , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C59/54
CPC分类号： C07C69/007 , C07C59/46 , C07C59/54 , C07C59/56 , C07C405/00
摘要： Described are pharmacologically active leukotriene B4 derivatives of the general formula I in which R1 is CH2OH, CH3, CF3, COOR4 or CONR5R6, R2 is H or an organic-acid group with 1 to 15 C-atoms, R3 is H, a C1-C14 alkyl group, optionally with one or more substituents, a C3-C10 cycloalkyl group, a C6-C10 aryl group optionally substituted, independently of each other, with one or more halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy groups or R3 is a 5- to 6-membered aromatic heterocyclic ring with at least one hetero atom, R4 is H, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl group optionally substituted with 1 to 3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy groups or R4 is CH2-CO-(C6-C10) aryl or a 5- to 6-membered ring with at least one hetero atom, A is a trans,trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B is a straight-chain or branched-chain C1-C10 alkylene group, which may be substituted with fluorine, or the group (a), D is a direct bond, oxygen, sulphur, -CC- or -CH=CR7 or, together with B, may also form a direct bond, R5 and R6 which may be the same or different, are H or C1-C4 alkyl, optionally substituted with hydroxy groups, or R6 is H and R5 is C1-C15 alkanoyl or R8SO2-, R7 is H, C1-C5 alkyl, chlorine or bromine, R8 is defined in the same way as R3, m is 1 to 3, n is 2 to 5 plus, when R4 is hydrogen, salts of these compounds with physiologically tolerated bases, as well as their cyclo-dextrin clathrates X and Y together form a direct bond, the resulting olefin being E or Z configured, or X is an alpha - or beta - fluorine atom and Y a beta - hydrogen atom.
摘要翻译：本发明涉及式（I）其中R 1 CH 2 OH，CH 3，CF 3，COOR 4，CONR 5 R 6，并且R 2是H或有机残基与1-15个碳原子的白三烯B4衍生物，R 3是H，任选地单取代或多取代 C1-C14烷基，C3-C10环烷基，任选独立地单独使用或乘以卤素，苯基，C1-C4烷基，C1-C4烷氧基，氟甲基，氯甲基，三氟甲基，羰基，羧基或羟基C 6 -C 10取代的芳基或具有至少1个杂原子象征着的5-6元芳族杂环，R 4是氢，C1-C10烷基，C3-C10环烷基，任选地被1-3个卤素，苯基取代，C1-C4烷基，C1-C4烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10 - 芳基，CH 2 -CO-（C6-C10）芳基或具有至少1个杂原子的5-6元环，是反式，反式 - CH = CH- CH = CH，-CH 2 CH 2一个-CH = CH-或四亚甲基，B是直链C 1 -C 10或版本其可任选被氟取代的支链亚烷基，或（a）象征团，D是一个直接键，氧，硫， - CC-，-CH = CR 7，或与B也可以表示直接键合在一起，R5和R6是相同的或是不同的，它们是H或者未取代的或羟基取代的C1-C4烷基或R 6是H，R5是C1-C15烷酰基或R8SO2-，R 7是H，C1-C5烷基，氯，溴，R8具有相同的含义R3具有中，m是1-3，n是2-5，并且当R 4是氢，其与生理学上可接受的碱及其环糊精笼形物的盐。 X和Y表示直接键合，其特征在于，所得到的烯烃可以被配置E或Z或X是α - 或β--ständiges氟原子，和Y表示氢原子的β-ständiges。

7. 发明申请

WO1995020562A1 LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS 审中-公开
标题翻译：新白三烯B4衍生物，用于生产及其作为药物
公开(公告)号：WO1995020562A1
公开(公告)日：1995-08-03
申请号：PCT/EP1994000214
申请日：1994-01-27
申请人： SCHERING AKTIENGESELLSCHAFT , SKUBALLA, Werner , BUCHMANN, Bernd , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C59/46
CPC分类号： C07F9/4018 , C07C59/46 , C07C59/54 , C07C69/007 , C07C69/732 , C07C235/30 , C07C405/0066 , C07C2601/04 , C07C2601/14 , C07D309/30 , C07F9/4015
摘要： The invention concerns leukotriene B4 derivatives of the formula (I), in which R1 is CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 together with R2 is a carbonyl group, R2 and R3, which may be the same or different, are H or an organic-acid group with 1 to 15 C-atomes, R4 is H, a C1-C14 alkyl group, optionally with one or more substituents, a C3-C10 cycloalkyl group, a C6-C10 aryl group optionally substituted, independently of each other, with one or more halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl oder hydroxy groups or R4 is a 5- or 6-membered aromatic heterocyclic ring with at least one hetero atom, R5 is H, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl group optionally substituted with 1 to 3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy groups or R5 is CH2-CO-(C6-C10 aryl) or a 5- to 6-membered ring with at least one hetero atom, A is a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B is a straight-chain or branched-chain C1-C10 alkylene group, which may be substituted with fluorine, or the group (a), D is a direct bond, oxygen, sulphur, -C=C-, -CH=CR8, or together with B, may also form a direct bond, R6 and R7, which may be the same or different, are H or C1-C4 alkyl, or R is H and R is C1-C15 alkanoyl or C1-C10 alkane sulphonyl, optionally substituted with OH, R8 is H, C1-C5 alkyl, chlorine, bromine and n is 2 to 5 plus, when R5 is hydrogen, salts of these compounds with physiologically tolerated bases, as well as their cyclodextrin clathrates.
摘要翻译：本发明涉及其中R 1 CH 2 OH，CH 3，CF 3，COOR 5，CONR 6 R 7，或R 1与R 2一起表示羰基，R 2和R 3是相同或不同的H或有机残基与1-15的式（I）的白三烯B4衍生物表示碳原子，R 4是H，任选地单取代或多取代的C1-C14烷基，C3-C10环烷基，任选独立地被取代地被卤素，苯基，C1-C4烷基，C1-C4烷氧基，氟甲基一次或多次氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10芳基或具有至少1个杂原子象征着的5-6元芳族杂环，R 5是氢，C1-C10烷基，C3-C10环烷基，任选被1-3个卤素取代的，苯基，指C1-C4烷基，C1-C4烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10 - 芳基，CH 2 -CO-（C6-C10）芳基或具有至少1个杂原子的5-6元环中，是反式，反式CH = CH-CH = CH，一-C H2CH2-CH = CH-或四亚甲基，B是直链或支链C，其可任选被氟取代的1〜10的亚烷基，或（a）象征团，D是一个直接键，氧，硫，-C = C- ，-CH = CR 8，或连同B也可以表示直接键合，R 6和R 7相同或不同并且是H或C1-C4烷基，或者R <7>为H，R <6> C1-C15烷酰基或C1 C10链烷磺酰基代表任选被OH取代，R8是H，C1-C5烷基，氯，溴，n是2-5和，当R 5是氢，其与生理学上可接受的碱及其环糊精笼形物的盐。

8. 发明申请

WO1994004522A1 NEW LEUKOTRIENE-B4 ANTAGONISTS, PROCESS FOR PREPARING THE SAME AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：新白三烯B4拮抗剂，其制造方法相同，它们作为药物
公开(公告)号：WO1994004522A1
公开(公告)日：1994-03-03
申请号：PCT/EP1993002225
申请日：1993-08-19
申请人： SCHERING AKTIENGESELLSCHAFT , BUCHMANN, Bernd , SKUBALLA, Werner , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D317/22
CPC分类号： C07C69/712 , C07D317/22
摘要： Antagonists of the leukotrienes-B4 have formula (I), in which n is an integer between 2 and 5, X is a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridin ring; Y is a bond to a hydrogen atom and at the same time to a hydroxy group, an oxygen atom with a double bond or -O-CH2-CH2-O-; R1 and R2 stand for the rest OH, -O-(C1-C4)-alkyl, O-(C3-C6)-cycloalkyl, -O-(C6-C10)-aryl, -O-(C7-C12)-aralkyl, O-(CH2)-CO-(C6-C10)-aryl or the residue NHR3, in which R3 stands for hydrogen, (C1-C4)-alkyl, (C3-C6)-cycloalkyl or (C7-C12)-aralkyl. Also disclosed are the salts of said antagonists with physiologically tolerable bases and their cyclodextrin clathrates.

9. 发明申请

WO1994002464A1 NEW PYRIDINE DERIVATIVES AS LEUKCOTRIENE B4 ANTAGONISTS 审中-公开
标题翻译：白三烯B4的拮抗作用的新的吡啶衍生物
公开(公告)号：WO1994002464A1
公开(公告)日：1994-02-03
申请号：PCT/DE1993000593
申请日：1993-07-01
申请人： SCHERING AKTIENGESELLSCHAFT , HEINDL, Josef , SKUBALLA, Werner , BUCHMANN, Bernd , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D213/65
CPC分类号： C07D213/61 , C07D213/65
摘要： The invention pertains to new pyridine derivatives of formula (I) where .Ÿ .Ÿ .Ÿ denotes a single bond or a double bond, m, n, p and r in each case stands for a number from 0 to 5, q is 1 or 2, U denotes a single bond or the grouping -CH2-CH2-, -CHOH-, -CO- -CH=CH-, -C=C-, -CO-CO- or -CHOH-CHOH-, V stands for a single bond, phenyl residue or pyridyle residue, W is a hydrogen atom, a halogen atom, an alkyl group with up to four carbon atoms, a trifluoromethyl group, an alkylsulfonylamino group, a trifluoromethylsulfonylamino group, an arylsulfonylaminocarbonyl group, a free, esterified or amidated carboxyl group, or a hydroxy group, X denotes a free, esterified or amidated carboxyl group, Y is an oxygen atom or a methylene group, and Z is a single bond if q is 2 or otherwise an alkyl group or alkylene group with at most 8 carbon atoms or a phenyl, phenoxy or styryl residue substituted by alkyl groups with at most 4 carbon atoms, alkoxy groups with at most 4 carbon atoms, 1-oxoalkyl groups with at most 4 carbon atoms, halogen atoms and/or trifluoromethyl groups. The invention also concerns salts of these derivatives with bases which are generally recognized as physiologically safe.

10. 发明申请

WO1993011105A1 LEUKOTRIENE-B4 DERIVATIVES, PROCESS FOR PREPARING THE SAME AND MEDICAMENTS 审中-公开
标题翻译： LEKOTRIENE-B4衍生物，其制备方法和药物
公开(公告)号：WO1993011105A1
公开(公告)日：1993-06-10
申请号：PCT/EP1992002653
申请日：1992-11-19
申请人： SCHERING AKTIENGESELLSCHAFT , SKUBALLA, Werner , BUCHMANN, Bernd , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C405/00
CPC分类号： C07C405/0058 , C07C2601/04 , C07C2601/18 , C07D309/30
摘要： Leukotriene-B4 derivatives have the formula (I), in which R stands for CH2OH, CH3, CF3, COOR , CONR R , or R represents together with R a carbonyl group; R and R are different or the same and stand for H or an organic acid residue with 1-15 C atoms; R stands for H, C1-C10-alkyl, possibly substituted one or several times by chlorine or bromine, C3-C10-cycloalkyl, a C6-C10-aryl residue possibly independently substituted one or several times by chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy or a 5-6 membered aromatic heterocyclic ring with at least 1 heteroatom; R stands for hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, an aryl residue possibly substituted by 1-3 chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, CH2-CO-(C6-C10)aryl or a 5-6 membered ring with at least 1 heteroatom; A stands for a trans, trans-CH=CH-CH=CH, -CH2CH2-CH=CH- or a tetramethylene group; B stands for a straight or branched chain C1-C10alkylene group, possibly substituted with fluorine or the group (a); D is a direct bond, oxygen, sulphur, -C=C-, -CH=CR or it may represent together with B a direct bond; R and R are different or the same and stand for H or C1-C4-alkyl or R stands for H and R stands for C1-C10-alkanoyl or C1-C10-alkansulphonyl; R stands for H, C1-C5-alkyl, chlorine, bromine; m stands for the digits 1 or 4 and n equals 3-5. Also disclosed are the salts of these derivates with physiologically tolerable bases, when R stands for hydrogen, and their cyclodextrine clathrates.
摘要翻译：白三烯-B4衍生物具有式（I），其中R 1代表CH 2 OH，CH 3，CF 3，COOR 5，CONR 6 R 7或R 1代表R 2 >羰基; R 2和R 3不同或相同，代表H或具有1-15个C原子的有机酸残基; R 4代表H，C 1 -C 10 - 烷基，可能被氯或溴取代一次或几次，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基残基，其可以独立地被氯，溴，苯基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基或具有至少1个杂原子的5-6元芳族杂环; R 5代表氢，C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，可被1-3个氯，溴，苯基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基，CH 2 -CO-（C 6 -C 10）芳基或具有至少1个杂原子的5-6元环; A代表反式，CH = CH-CH = CH，-CH 2 CH 2 -CH = CH-或四亚甲基; B代表直链或支链C1-C10亚烷基，可能被氟取代或（a）组; D是直接键，氧，硫，-C = C-，-CH = CR 8，或者可以与B一起直接键合; R 6和R 7不同或相同，代表H或C 1 -C 4 - 烷基或R 7代表H且R 6代表C 1 -C 10 - 烷酰基或C 1 -C 10 - 烷基磺酰基 ; R 8代表H，C 1 -C 5 - 烷基，氯，溴; m代表数字1或4，n代表3-5。还公开了这些衍生物与生理上可耐受的碱的盐，当R 5代表氢时，它们的环糊精包合。

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