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31. 发明申请

WO1993022278A1 PROCESS FOR PRODUCING HYDROXYALKANE CARBOXYLIC ACID AMIDES 审中-公开
标题翻译：用于生产HYDROXYALKANCARBONSÄUREAMIDEN
公开(公告)号：WO1993022278A1
公开(公告)日：1993-11-11
申请号：PCT/DE1993000413
申请日：1993-05-05
申请人： SCHERING AKTIENGESELLSCHAFT , SCHOLZ, Stefan , HARRE, Michael , VIDIC, Hans-Jörg , NEEF, Günter , KIRSCH, Gerald
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C231/02
CPC分类号： C07D295/182 , C07C231/02
摘要： The description relates to a process for producing hydroxyalkane carboxylic acid amides of the general formula (I), in which n is a whole number from 1 to 20 and R1 and R2 are alkyl groups with a maximum of 8 carbon atoms or together represent an alkylene group with 4 to 8 carbon atoms, possibly interrupted by an oxygen or a nitrogen atom, from hydroxyalkane carboxylic acids of the general formula (II): HO-CnH2n-COOH, in which n has the significance given above and amines of the general formula (III), in which R1 and R2 have the significance given above, characterized in that the hydroxylalkane carboxylic acid is heated with reflux in a one-pot reaction with 10 to 30 mol acetyl chloride per mol acid, the superfluous acetyl chloride is distilled off after acetylisation, the residue is heated with reflux with 1.5 to 5 mol thionyl chloride per mol acid, after the formation of acid chloride the thionyl chloride is distilled off, the residue is dissolved in a dialkyl ether with 4 to 8 carbon atoms, the solution obtained is added proportionately to an aqueous solution of the amine cooled to 0 to 10 °C and, after amide formation, the acetal group is separated off by treatment with aqueous sodium hydroxide solution at a reaction temperature of 10 to 30 °C.

32. 发明申请

WO1991015448A1 24-OXA DERIVATIVES IN THE VITAMIN D SERIES 审中-公开
标题翻译：维生素D系列中的24-OXA衍生物
公开(公告)号：WO1991015448A1
公开(公告)日：1991-10-17
申请号：PCT/EP1991000657
申请日：1991-04-08
申请人： SCHERING AKTIENGESELLSCHAFT , NEEF, Günter , KIRSCH, Gerald , STEINMEYER, Andreas , SCHWARZ, Katica , BRÄUTIGAM, Matthias , THIEROFF-Ekerdt, R. , RACH, Petra
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The description relates to novel 24-oxa derivatives in the vitamin D series of the general formula I in which : R , R and R are mutually independently a hydrogen atom or an acyl group with 1 to 9 carbon atoms; R is a hydrogen atom of a linear or branched alkyl group with 1 to 4 carbon atoms; and R may be a hydrogen atom or a linear or branched alkyl group with 1 to 4 carbon atoms; a process for manufacturing them, pharmaceutical preparations containing these compounds and their use in the production of medicaments.
摘要翻译：该描述涉及通式I的维生素D系中的新型24-氧杂衍生物，其中：R 1，R 2和R 5相互独立地为氢原子或具有1至9个碳原子的酰基碳原子 R 3是具有1至4个碳原子的直链或支链烷基的氢原子; 和R 4可以是氢原子或具有1至4个碳原子的直链或支链烷基; 制造它们的方法，含有这些化合物的药物制剂及其在制备药物中的用途。

33. 发明申请

WO1993007118A1 9-SUBSTITUTED BICYCLO[3.3.0]OCTANE DERIVATIVES, FOR USE AS TXA2 ANTAGONISTS 审中-公开
标题翻译： 9-替代双酚A [3.3.0] OCTANE衍生物，用作TXA2拮抗剂
公开(公告)号：WO1993007118A1
公开(公告)日：1993-04-15
申请号：PCT/DE1992000865
申请日：1992-10-09
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , VORBRÜGGEN, Helmut , REHWINKEL, Hartmut , THIERAUCH, Karl-Heinz , VERHALLEN, Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C405/00
CPC分类号： C07C405/0083
摘要： The invention concerns 9-substituted bicylo[3.3.0]octane derivaties of formula (I) and their physiologically acceptable bases, and also the α-, β- or η-cyclodextrin clathrates, and the compounds of formula (I) encapsulated in liposomes. The invention also concerns methods of preparing such compounds and their use in pharmaceuticals.

34. 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。

35. 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。

36. 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。

37. 发明申请

WO1997035839A1 NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：新冰片，PROCESS FOR THEIR和制药用
公开(公告)号：WO1997035839A1
公开(公告)日：1997-10-02
申请号：PCT/EP1996001324
申请日：1996-03-27
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , BLECHERT, Siegfried , SACHSE, Anke
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/02
CPC分类号： C07D303/16 , C07C233/83 , C07C271/22 , C07C2602/42 , C07F7/1804
摘要： The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.
摘要翻译： Borneolderivate通式（I）中有所描述，其中R <1>表示任选被卤原子，C1-C4烷基，C1-C4烷氧基，C1-C6烷氧羰基或C 1 -C 8 - 酰氧基苯基取代; [R <2>表示一个氢原子，一个C1-C4烷基，取代的芳基，一个C1-C6烷氧基羰基或C1-C8酰基基团; [R <3>代表氢原子，C1-C4烷基，C1-C4酰基或三C1-C4烷基甲硅烷基，并且其中; [R <4>和R <7>代表氢原子，C1-C4烷基或任选地被卤素原子，C1-C4烷基，C1-C9烷氧基，C1-C4烷氧羰基或C 1 -C 8 - 酰氧基苯基取代的且R <5>和R <6>代表氢原子，羟基或C1-C8-酰氧基或一起代表碳 - 碳键或氧原子，或R <4>和R <5>和/或R <6> 且R <7>的每个一起表示羰基，C1-C4亚烷基，或者，如果需要的话，由一个C1-C3烷基取代的环氧乙烷基团，和任选地它们的盐与生理上可接受的酸，以及它们的α - ，β - 或伽马-Cyclodextrinclathrate和通式（I）的脂质体包裹的化合物的意思。

38. 发明申请

WO1999001160A1 SACCHARIDE CONJUGATES, PHARMACEUTICALS CONTAINING THE SAME, PROCESS FOR PREPARING THE SAME AND THEIR USE 审中-公开
标题翻译：糖缀合物，含制药，制造方法相同，它们的用途
公开(公告)号：WO1999001160A1
公开(公告)日：1999-01-14
申请号：PCT/EP1998003142
申请日：1998-05-27
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , MARESKI, Peter , PLATZEK, Johannes , RADÜCHEL, Bernd , BERNDORFF, Dietmar , WEINMANN, Hanns-Joachim
IPC分类号： A61K49/00
CPC分类号： A61K49/124 , A61K49/085 , A61K49/146
摘要： Conjugates consist of an amino-group-containing polymer, signal-generating group(s) which contain metal ion(s), and mono- or oligosaccharides, and optionally of cations of inorganic and/or organic bases, amino acids or amino acid amides. These conjugates are valuable compounds for diagnosis and therapy.
摘要翻译：由含氨基的聚合物的缀合物，含有信令组（一个或多个）和单糖或寡糖，以及无机和/或有机碱，氨基酸或氨基酸酰胺任选阳离子金属离子（S）是用于诊断和治疗价值的化合物。

39. 发明申请

WO1998024803A1 STEROID ESTERS, METHOD FOR THE MANUFACTURE THEREOF AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：甾族酯，PROCESS FOR THEIR和制药用
公开(公告)号：WO1998024803A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006829
申请日：1997-12-08
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , CLEVE, Arwed , SCHWEDE, Wolfgang , NEEF, Günter , OTTOW, Eckhard , CHWALISZ, Kristof , SCHNEIDER, Martin
IPC分类号： C07J53/00
CPC分类号： C07J53/002 , Y10S514/843
摘要： Disclosed are novel steroid esters of formula (I), wherein m means 1 or 2, n is 0 or 1, X is F or CN and the line drawn between carbon atoms 15 and 16 symbolizes the possible presence of a dual bond, excluding compound (Z)-6'-(4-cyanphenyl)-9,11 alpha -dihydro-17 beta -hydroxy-17 alpha -[3-(1-oxo-2-methylpropoxy)-1-propenyl]-4'H-naphto[3',2',1';10,9,11] ester-4-en-3-on. Derivatization occurs with a carboxylic acid. The novel compounds are characterized by a significantly enhanced solubility in comparison with the basic hydroxy compounds, and by enhanced biological effectiveness and selectivity. Said novel compounds are suitable for the production of medicaments.
摘要翻译：它描述了式（I）其中m是1或2的新的类固醇酯，n为0或1，X为F或CN和碳原子数为15和16之间的虚线，双键的符号，但不包括化合物（Z）的任选存在 - 6 ' - （4-氰基苯基）-9,11二氢-α17的β - 羟基17α - [3-（1-氧代-2-甲基丙氧基）-1-丙烯基] -4'H - 萘并[3' ，2”，1' ：10,9,11]雌-4-烯-3-酮。衍生化用的羧酸中进行。新化合物由显着改进的溶解度以及通过增加的生物活性和选择性是从基础羟基化合物区别开来。这些新化合物是适用于生产药品。

40. 发明申请

WO1998024801A1 OXYIMINOPREGNANCARBOLACTONE 审中-公开
公开(公告)号：WO1998024801A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006657
申请日：1997-12-01
申请人： SCHERING AKTIENGESELLSCHAFT , LAURENT, Henry , LIPP, Ralph , ESPERLING, Peter , TACK, Johannes-Wilhelm
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016
摘要： Disclosed are 3-oxyiminopregnan-21-carbolactone, (E,Z) mixtures and isomerically pure (E) and (Z) compounds, the production and use thereof as medicaments.
摘要翻译： 3- Oxyiminopregnan -21-内酯，（E，Z）-mixtures，和异构体纯的（E） - 和（Z）的化合物，它们的制备和在药物组合物使用进行了描述。

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