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1. 发明申请

WO0032584A3 NONSTEROIDAL ANTIINFLAMMATORIES 审中-公开
标题翻译：的NSAIDs
公开(公告)号：WO0032584A3
公开(公告)日：2000-11-09
申请号：PCT/EP9909754
申请日：1999-11-29
申请人： SCHERING AG , LEHMANN MANFRED , KROLIKIEWICZ KONRAD , SKUBALLA WERNER , STREHLKE PETER , KALKBRENNER FRANK , EKERDT ROLAND , GIESEN CLAUDIA
发明人： LEHMANN MANFRED , KROLIKIEWICZ KONRAD , SKUBALLA WERNER , STREHLKE PETER , KALKBRENNER FRANK , EKERDT ROLAND , GIESEN CLAUDIA
IPC分类号： C07D237/32 , A61K31/343 , A61K31/381 , A61K31/502 , A61K31/536 , A61K31/5365 , A61P1/00 , A61P1/08 , A61P1/16 , A61P7/00 , A61P9/00 , A61P11/00 , A61P17/00 , A61P19/02 , A61P23/00 , A61P25/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/00 , C07D265/02 , C07D307/88 , C07D333/72 , A61K31/16 , A61K31/165 , A61K31/365 , A61K31/38 , A61K31/50 , A61K31/535
CPC分类号： C07D265/02 , A61K31/502 , A61K31/5365 , C07D307/88
摘要： The invention relates to the use of compounds of general formula (I), wherein A, B, A, Ar, R , R and R have the meanings detailed more closely in the description, for producing medicaments with an antiinflammatory action. The compounds of general formula (I) show a clear dissociation between antiinflammatory and metabolic effects.
摘要翻译：本发明描述了使用通式（I），其中A，B，A中，Ar，R <1>，R <2>和R <3>是如在说明书中给出更详细定义的，用于与产生药物抗炎活性。通式（I）的化合物显示出抗炎和代谢作用之间有明显的解离。

2. 发明申请

WO9852915A3 LEUKOTRIENE B4 DERIVATIVES, IN PARTICULAR OXIMO-LTB4 ANTAGONISTS 审中-公开
标题翻译：低氧素B4衍生物，特别是OXIMO-LTB4拮抗剂
公开(公告)号：WO9852915A3
公开(公告)日：1999-02-25
申请号：PCT/EP9803139
申请日：1998-05-22
申请人： SCHERING AG , BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , JAROCH STEFAN , SKUBALLA WERNER
发明人： BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , JAROCH STEFAN , SKUBALLA WERNER
IPC分类号： A61K31/19 , A61K31/23 , A61K31/557 , A61K31/5575 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C403/08 , C07C405/00 , C07D251/44 , C07D251/50 , C07D251/54 , C07D251/60 , C07D257/04 , C07D257/06 , C07D277/24 , C07D277/28 , C07D277/56
CPC分类号： C07D277/56 , C07C403/08 , C07C2601/04 , C07C2601/14 , C07D257/06 , C07D277/24
摘要： The invention relates to leukotriene B4 derivatives of general formula (I) in which R1 stands for H, CF3, CH2OH; R2 stands for an organic acid radical; R3 stands for H, C1-C14-alkyl, C3-C10-cycloalkyl, or a 5-6-link aromatic heterocyclic ring with at least one heteroatom; R4 is hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl; A is a trans-, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group; B is a C1-C10 linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, -C C-, -CH=CR7, or a direct bonding with B; R5 and R6 are identical or different and are H or C1-C4-alkyl, or R6 stands for H and R5 stands for C1-C15-alkanoyl or R8 SO2-; R7 is H, C1-C5-alkyl, chlorine, bromine; R8 is the same as R3; m is 1-3; o is 0-5; p is 0-5; x is a direct bonding, oxygen, sulphur, an aromatic or heterocyclic compound; y is a C1-C8-alkyl, C3-C10-cycloalkyl; n is 2-5. When R4 is hydrogen, the invention also relates to their salts with physiologically compatible bases and their cyclodextrin clathrates. The leukotriene derivatives are used as dermatological products.

3. 发明申请

WO9852913A3 LEUKOTRIENE B4 ANTAGONISTS, IN PARTICULAR 3-OXA-TETRAHYDRONAPHTHALENE-LTB4 ANTAGONISTS 审中-公开
标题翻译：亮氨酸B4拮抗剂，特别是3-氧化四氢噻吩 - LTB4拮抗剂
公开(公告)号：WO9852913A3
公开(公告)日：1999-02-25
申请号：PCT/EP9803137
申请日：1998-05-22
申请人： SCHERING AG , BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , REHWINKEL HARTMUT , SKUBALLA WERNER , SCHNEIDER FRANK
发明人： BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , REHWINKEL HARTMUT , SKUBALLA WERNER , SCHNEIDER FRANK
IPC分类号： C07C59/72 , C07C69/712 , C07C69/92 , C07C405/00
CPC分类号： C07C69/712 , C07C59/72 , C07C69/92
摘要： The invention relates to leukotriene B4 antagonists of general formula (I) in which the contact of the chain O-(CH2)p-R1 can be situated at one of the free positions on the aromatic compound. R1 stands for CH2OH, COOR4, CONR5R6; R2 stands for H or an organic acid radical with 1-15 C atoms; R3 stands for H, C1-C14-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical or a 5-6-link aromatic heterocyclic ring; R4 is H, C1-C10-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical, CH2-CO-(C6-C10)aryl or a 5-6-link aromatic heterocyclic ring; A is a trans-, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group; B is a C1-C10-alkylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, -C C-, -CH=CR7, or a direct bonding together with B; Y is a C1-C8-alkyl, C3-C10-cycloalkyl; R5 and R6 are identical or different and are H; R7 is H, C1-C5-alkyl, chlorine, bromine; R8 is the same as R3; p is 1-6; m is 1-3, n is 2-5. When R4 is hydrogen. The invention also relates to their salts with physiologically compatible bases and their cyclodextrin clathrates. The leukotriene antagonists are effective dermatological products.

4. 发明申请

WO9852912A3 LEUKOTRIENE B4 ANTAGONISTS, IN PARTICULAR 3-CARBA-TETRAHYDRONAPHTHALENE-LTB4 ANTAGONISTS 审中-公开
标题翻译：亮氨酸B4拮抗剂，特别是3-CARBA-TETRAHYDRONAPHTHALENTHALENE-LTB4 ANTAGONISTS
公开(公告)号：WO9852912A3
公开(公告)日：1999-02-25
申请号：PCT/EP9803136
申请日：1998-05-22
申请人： SCHERING AG , BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , JAROCH STEFAN , SKUBALLA WERNER
发明人： BUCHMANN BERND , FROEHLICH WOLFGANG , GIESEN CLAUDIA , HENNEKES HARTWIG , JAROCH STEFAN , SKUBALLA WERNER
IPC分类号： C07C33/38 , C07C59/54 , C07C403/00 , C07C405/00
CPC分类号： C07C59/54 , C07C33/38 , C07C405/0066
摘要： The invention relates to leukotriene B4 antagonists of formula (I), a method for the production and the pharmaceutical use thereof.

5. 发明申请

WO0181342A2 NOVEL EPOTHILONE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0181342A2
公开(公告)日：2001-11-01
申请号：PCT/EP0104552
申请日：2001-04-19
申请人： SCHERING AG , BUCHMANN BERND , KLAR ULRICH , SKUBALLA WERNER , SCHWEDE WOLFGANG , LICHTNER ROSEMARIE , HOFFMANN JENS
发明人： BUCHMANN BERND , KLAR ULRICH , SKUBALLA WERNER , SCHWEDE WOLFGANG , LICHTNER ROSEMARIE , HOFFMANN JENS
IPC分类号： A61K31/427 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/06 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D491/04 , C07D493/04 , C07D493/10 , C07D498/04 , C07D419/06 , A61K31/42 , A61K31/425 , A61K31/44
CPC分类号： C07D401/06 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D491/04 , C07D493/04 , C07D493/10 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein R represents a halogen atom or a cyano group and the other substituents have the meanings as cited in the description. The novel compounds interact with tubulin by stabilizing formed microtubules. They are capable of influencing the cell division in a phase-specific manner and are well-suited for the treatment of malignant tumors, for example, ovarian, stomach, colon, adeno, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are well-suited for anti-angiogenesis therapy and for the treatment of chronic inflammable medical disorders (psoriasis, arthritis). In order to prevent uncontrolled cell growths as well as to improve the compatibility of medical implants, the inventive epothilone derivatives can be applied to or introduced into polymeric materials. The inventive compounds can be used alone or in order to obtain additive or synergistic effects, in conjunction with additional principles and substance classes that can be used in tumor therapy.
摘要翻译：本发明描述了通式I的埃坡霉素的新衍生物，其中R <5>表示卤原子或氰基，而另一取代基具有本说明书中给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

6. 发明申请

WO0049020A3 NOVEL EPOTHILON DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0049020A3
公开(公告)日：2000-12-28
申请号：PCT/EP0001332
申请日：2000-02-18
申请人： SCHERING AG , KLAR ULRICH , SCHWEDE WOLFGANG , BUCHMANN BERND , SKUBALLA WERNER , SCHIRNER MICHAEL , GRIMM MICHAEL
发明人： KLAR ULRICH , SCHWEDE WOLFGANG , BUCHMANN BERND , SKUBALLA WERNER , SCHIRNER MICHAEL , GRIMM MICHAEL
IPC分类号： C07D417/06 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D405/06 , C07D493/08
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, R , R , R , R , R , R , E, R , R , R , R , R 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）的新的埃坡霉素衍生物，其中取代基Y，Z，R <1A>，R <1B>，R <2A>，R <2B>，R <3A>，R < 图3b>，E，R <5> - [R <6> - [R <7> - [R <8>，R <14>和X具有说明书中更详细地给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

7. 发明申请

WO9967212A2 OXIDATION INHIBITORS FOR PROSTANE DERIVATIVES 审中-公开
标题翻译：氧化抑制剂prostane衍生品
公开(公告)号：WO9967212A2
公开(公告)日：1999-12-29
申请号：PCT/EP9904278
申请日：1999-06-22
申请人： SCHERING AG , WAGNER TORSTEN , WESSEL MARTIN , LIPP RALPH , IFFERT BERND , MICHEL HEINRICH , WESTERMANN JUERGEN , DAHL HELMUT , SKUBALLA WERNER
发明人： WAGNER TORSTEN , WESSEL MARTIN , LIPP RALPH , IFFERT BERND , MICHEL HEINRICH , WESTERMANN JUERGEN , DAHL HELMUT , SKUBALLA WERNER
IPC分类号： A61K31/557 , A61K9/16 , A61K31/5575 , A61K31/5578 , A61K31/5585 , C07C59/46 , C07C405/00 , C08B37/00
CPC分类号： A61K31/5585 , A61K9/1694 , A61K31/5575 , C08B37/0015
摘要： The invention relates to the use of an oxidation inhibitor, i.e. active carbon, for ambient air in industrial manufacturing, especially in the processing of prostane derivatives, whereby the oxidation inhibitor removes ozone from the process air before contact with said prostane derivatives. The concentration of decomposition products is reduced.
摘要翻译：即，本发明包括使用氧化抑制剂活性炭工业制造环境空气，特别是prostane衍生物的处理，由此从处理空气中的氧化抑制剂臭氧与prostane衍生物接触之前去除。分解产物的浓度被降低。

8. 发明申请

WO0049019A3 NOVEL EPOTHILONE DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0049019A3
公开(公告)日：2001-03-01
申请号：PCT/EP0001331
申请日：2000-02-18
申请人： SCHERING AG , KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL , MENRAD ANDREAS
发明人： KLAR ULRICH , SCHWEDE WOLFGANG , SKUBALLA WERNER , BUCHMANN BERND , SCHIRNER MICHAEL , MENRAD ANDREAS
IPC分类号： C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/14 , C07D493/20 , C07F7/18 , A61K31/427 , A61P35/00
CPC分类号： C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/14 , C07F7/1856 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein the substituents Y, Z, R , R , R , R , G'-G-E-E', R , R , R , R , R and X have the meanings specified in the description. The novel compounds interact with tubulin by stabilising the microtubuli which are formed. They are able to influence the cell division phase-specifically and are suitable for treating malignant tumours such as cancers of the ovaries, stomach, colon, glands, breasts, lungs and head and neck, malignant melanoma and acute lymphocytic and myelocytic leukaemia. The compounds are also suitable for anti-angiogenesis therapy and for treating chronic inflammatory diseases (psoriasis, arthritis) and can be deposited on or in polymer materials in order to prevent uncontrolled cell proliferations on medical implants and to improve the compatibility thereof. The inventive compounds can be used alone or in combination with other principles and classes of substances that can be used in the therapy of tumours in order to achieve additive or synergistic effects.
摘要翻译：本发明涉及通式（I），其中取代基Y，Z，R <1A>，R <1B>，R <2A>，R <2B>，G 'GE-E' 的新的埃坡霉素衍生物，R <5> - [R <6> - [R <7> - [R <8>，R <14>和X具有说明书中更详细地给出的含义。所述新的化合物通过稳定微管形成与微管蛋白相互作用。它们能够影响细胞分裂期特异性和适用于治疗恶性肿瘤，如卵巢癌，胃癌，结肠癌，腺，乳腺，肺，头和颈癌，恶性黑色素瘤，急性淋巴细胞和myelocytäre白血病。它们也适用于抗血管生成治疗和用于慢性炎症性疾病（银屑病关节炎）的治疗。为了避免上不受控制的细胞生长和医疗植入物的更好的相容性，它们可以向上移动到聚合物材料或贡献。新化合物可单独使用或以达到添加剂或与其它肿瘤治疗适用的原则和物质类组合的协同效应。

9. 发明申请

WO0049021A3 16-HALOGEN-EPOTHILONE DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译： 16个卤素埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0049021A3
公开(公告)日：2000-12-28
申请号：PCT/EP0001333
申请日：2000-02-18
申请人： SCHERING AG , KLAR ULRICH , SKUBALLA WERNER , BUCHMANN BERND , SCHWEDE WOLFGANG , SCHIRNER MICHAEL
发明人： KLAR ULRICH , SKUBALLA WERNER , BUCHMANN BERND , SCHWEDE WOLFGANG , SCHIRNER MICHAEL
IPC分类号： A61K31/336 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/18
CPC分类号： C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/1856 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein R means a halogen atom, especially a fluorine or chlorine atom, and the remaining substituents have the meanings given in the description. The novel compounds are suitable for producing medicaments.
摘要翻译：本发明描述了通式（I），其中R <8>是卤素原子，尤其是氟或氯原子的新的埃坡霉素衍生物，且其他取代基具有本说明书中给出的含义。这些新化合物是适用于生产药品。

10. 发明申请

WO0047584A3 EPOTHILON DERIVATIVES, METHOD FOR THE PRODUCTION AND THE USE THEREOF AS PHARMACEUTICALS 审中-公开
标题翻译：埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：WO0047584A3
公开(公告)日：2000-12-28
申请号：PCT/EP0001104
申请日：2000-02-11
申请人： SCHERING AG , KLAR ULRICH , SKUBALLA WERNER , BUCHMANN BERND , SCHWEDE WOLFGANG , SCHIRNER MICHAEL
发明人： KLAR ULRICH , SKUBALLA WERNER , BUCHMANN BERND , SCHWEDE WOLFGANG , SCHIRNER MICHAEL
IPC分类号： A61K31/422 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D493/04 , A61K31/425
CPC分类号： C07D405/06 , C07D413/06 , C07D417/06 , C07D493/04
摘要： The invention relates to the novel epothilon derivatives of general formula (I) wherein R is hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl, R is hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl, R , R are each a hydrogen atom, or together an additional bond or an oxygen atom, R is a methyl group or hydrogen, and simultaneously R and R together represent a trimethylene group and X is a 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl residue or simultaneously R and R together represent a trimethylene group, R is a methyl, ethyl or propyl group and X is a 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl residue or simultaneously R and R each represents a methyl group, R is a methyl, ethyl or propyl residue and X is a 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl residue, wherein the nitrogen and/or sulfur atom in X can be present in oxidized form and, if R and R each means a methyl residue, X can only be a 2-pyridyl residue which is optionally oxidized at the nitrogen atom, including all possible stereoisomers and their mixtures. The novel compounds are useful for producing medicaments.
摘要翻译：本发明描述了通式（I），其中R <4>为氢，C1-C10烷基，芳基，C7-C20芳烷基，R <5>为氢，C1-C10-烷基，芳基的新的埃坡霉素衍生物，C7-C20芳烷基，R <6> - [R <7>各自为氢原子，一起附加的键或氧原子，R <8>是甲基或氢，并且同时 - [R <1A>和R <1B> 一起代表三亚甲基且X为2-吡啶基，2-甲基-4-噻唑基或2-甲基-4-恶唑基团或在同一时间R <1A>和R <1B>一起代表三亚甲基，R <2>是甲基，乙基或丙基，X是2-吡啶基，2-甲基-4-噻唑基或2-甲基-4-恶唑基团或在同一时间R <1A>和R <1B>各自为甲基，R <2>表示甲基，乙基或丙基，X是2-吡啶基，2-甲基-4-噻唑基或2-甲基-4-恶唑基团，在X，由此氮和/或硫原子可被氧化的形式，并且其中，当R <2>和R <8>各自代表甲基基团，X可以是只有一个，任选地被氧化的氮原子，2-吡啶基，被提供，包括所有可能的立体异构和它们的混合物。这些新化合物是适用于生产药品。

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