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1.发明公开VERFAHREN FÜR DIE HERSTELLUNG VON C1-C15-FRAGMENTEN VON EPOTHILONEN UND DEREN DERIVATEN 审中-公开用于生产C1-C15破片埃博霉素及其衍生物
公开(公告)号：EP1641734A1
公开(公告)日：2006-04-05
申请号：EP04740122.9
申请日：2004-06-19
IPC分类号： C07C49/17 , C07D417/06 , C07D493/04
CPC分类号： C07D417/06 , C07C45/673 , C07C49/17 , C07D493/04
摘要： The invention relates to a method for producing C1-C15 fragments of epothilones and the derivatives thereof, whereby a C1-C6 fragment is bonded to a C7-C12 fragment to form a C1-C12 fragment which is then converted with a C13-C15 fragment to form the C1-C15 epothilone intermediate product to be produced. The thus produced C1-C15 epothilone intermediate products can be converted into the intrinsic active ingredients according to known methods. The invention also relates to the corresponding C1-C12 fragments.
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2.发明公开NEUE EPOTHILON-DERIVATE, VERFAHREN ZU DEREN HERSTELLUNG UND IHRE PHARMAZEUTISCHE VERWENDUNG 审中-公开新的埃博霉素衍生物，PROCESS FOR THEIR和制药用
公开(公告)号：EP1276740A2
公开(公告)日：2003-01-22
申请号：EP01936262.3
申请日：2001-04-19
发明人： BUCHMANN, Bernd , KLAR, Ulrich , SKUBALLA, Werner , SCHWEDE, Wolfgang , LICHTNER, Rosemarie , HOFFMANN, Jens
IPC分类号： C07D419/06 , C07D413/06 , A61K31/44 , A61K31/42 , A61K31/425 , A61P35/00
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 R5 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.
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3.发明公开6-ALKENYL-, 6-ALKINYL- AND 6-EPOXY-EPOTHILONE DERIVATIVES, PROCESS FOR THEIR PRODUCTION, AND THEIR USE IN PHARMACEUTICAL PREPARATIONS 有权6链烯基，炔基和6-6-EPOXY埃坡霉素衍生物。 用于生产及其在药物组合物
公开(公告)号：EP1173441A1
公开(公告)日：2002-01-23
申请号：EP00922826.3
申请日：2000-05-01
发明人： KLAR, Ulrich , SCHWEDE, Wolfgang , SKUBALLA, Werner , BUCHMANN, Bernd , HOFFMANN, Jens , LICHTNER, Rosemarie
IPC分类号： C07D493/04 , C07D405/06 , C07D417/06 , C07D405/14 , C07D413/06 , A61K31/335
CPC分类号： C07D405/06 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D493/04 , Y02P20/55
摘要： This invention describes the new 6-alkenyl- and 6-alkinyl- epothilone derivatives of general formula (I) in which R , R , R , R , R , R , R , R , R , A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating 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 suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
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公开(公告)号：EP0716648A1
公开(公告)日：1996-06-19
申请号：EP94927509.0
申请日：1994-08-29
发明人： BUCHMANN, Bernd , SKUBALLA, Werner
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, R1 stands for hydrogen or straight or branched chain alkyl with 1-6 C atoms and A stands for trans-CH=CH- or -CH¿2?-CH2-, are disclosed, as well as their salts with physiologically neutral bases, when R?1¿ stands for hydrogen, their clathrates with α-, β- or η-cyclodextrin, a process for preparing the same and their pharmaceutical use.
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5.发明公开NEUE LEUKOTRIEN-B 4?-ANTAGONISTEN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 失效新白三烯B 4？拮抗剂，生产与应用，药物的方法。
公开(公告)号：EP0656896A1
公开(公告)日：1995-06-14
申请号：EP93919109.0
申请日：1993-08-19
发明人： BUCHMANN, Bernd , SKUBALLA, Werner , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
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.
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6.发明公开NEUE LEUKOTRIEN-B 4?-ANTAGONISTEN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 失效新白三烯B 4？拮抗剂，生产与应用，药物的方法。
公开(公告)号：EP0597968A1
公开(公告)日：1994-05-25
申请号：EP92916905.0
申请日：1992-08-06
发明人： SKUBALLA, Werner , BUCHMANN, Bernd , HEINDL, Josef , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
CPC分类号： C07D409/06 , C07D333/32
摘要： Il est décrit des antagonistes des leucotriènes-B4 ayant la formule (I) dans laquelle X désigne un alkoxy en C1-C4 ou un -S(O)p-(C1-C4)-alkyle, P est égal à 0, 1 ou 2, Y désigne un atome d'hydrogène ou le reste COACOR2 où A est un groupe alkylène de 1 à 6 atomes de carbone dans la chaîne ou un reste (a), (b) ou (c), R1 et R2 désignent le reste OH, -O-(C1-C4)-alkyle, -O-(C3-C6)-cycloalkyle, -O-(C7-C12)-aralkyle ou le reste NR3R4 où R3 et R4 désignent un hydrogène, un alkyle en C1-C4, un cycloalkyle en C3-C6, un aryle en C6-C10 ou un aralkyle en C7-C12, ainsi que leurs sels obtenus avec des bases physiologiquement tolérables et leurs cyclodextrine-clathrates, leur procédé de fabrication et leur utilisation comme médicaments.
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7.发明授权NEUE LEUKOTRIEN-B 4 -DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 失效新的六氟乙烯B 4衍生物，其制备方法及其作为药物使用
公开(公告)号：EP0416069B1
公开(公告)日：1993-07-28
申请号：EP90904600.5
申请日：1990-03-16
IPC分类号： C07C69/736 , C07C67/343 , A61K31/215 , C07C59/68 , C07C43/23 , C07C59/70 , C07D207/16
CPC分类号： C07D295/185 , C07C43/23 , C07C59/68
摘要： The invention concerns leucotriene B4 derivatives of the formula (I) in which: n = 1-10, R1 is the CH2OH, COOR4, CONHR5 or CONR6R7 residue, A is a cis/trans or trans/trans -CH=CH-CH=CH- group or a tetramethylene group, B is an alkylene group with up to 10 C-atoms, D is a direct link, oxygen, sulphur, a -C=C- group or a -CH=CR8- group, B and D together form a direct link, R2 is a hydrogen atom or an acid residue of an organic acid with 1-15 C-atoms, R3 is a hydrogen atom, an alkyl residue (which may be substituted ) with 1-10 C-atoms, a cycloalkyl residue with 3-10 C-atoms, an aryl residue (which may be substituted ) with 6-10 C-atoms or a 5- or 6-membered heterocyclic residue plus, if R4 is a hydrogen atom, their salts with physiologically compatiblel bases and their cyclodextrinclathrates, as well as a method for their preparation and their pharmaceutical use.
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8.发明公开NEUE LEUKOTRIEN-B 4?-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 失效新白三烯B 4？的衍生物，生产与应用，药物的方法。
公开(公告)号：EP0477311A1
公开(公告)日：1992-04-01
申请号：EP91905964.0
申请日：1991-03-19
发明人： HEINDL, Josef , SKUBALLA, Werner , BUCHMANN, Bernd , FRÖHLICH, Wolfgang , EKERDT, Roland , GIESEN, Claudia
CPC分类号： C07D213/30 , C07C59/48 , C07C69/732 , C07D213/50 , C07D213/55 , C07D213/64 , C07D213/73 , C07D213/81
摘要： Analogues de leucotriène B4 de la formule (I), dans laquelle R1 est le résidu COOR2, R2 représentant un atome d'hydrogène ou un groupe alkyle (C1-C4), ou bien R1 est le résidu CH2OH, B est un groupe alkylène avec 1 à 3 atomes de C dans la chaîne, un résidu (a) ou un résidu (b), R3 étant un atome d'hydrogène, un groupe carboxyle ou méthoxycarbonyle, A est le groupe (c), -O-, (d), -NH-CO-, -CO-NH-, -OCH2-, -CH=CH-, (e), -COCH2- ou -CHOH-CH2-, X est N ou CH, D est le groupe (f) ou (g) et (h) est une liaison simple ou double, ainsi que leurs sels avec des bases physiologiquement neutres, procédés de fabrication de ces dérivés et leur utilisation pharmaceutique.
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9.发明公开
公开(公告)号：EP1501794A1
公开(公告)日：2005-02-02
申请号：EP03718796.0
申请日：2003-04-29
发明人： SCHWEDE, Wolfgang , SCHULZE, Volker , EIS, Knut , BUCHMANN, Bernd , BRIEM, Hans , SIEMEISTER, Gerhard , BÖMER, Ulf , PARCZYK, Karsten
IPC分类号： C07D201/00
CPC分类号： C07D277/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/34 , C07D277/82 , C07D417/12 , C07D451/06 , C07D487/04
摘要： The invention relates to thiazolidones of general formula (I), in which R1, R2, R3, X and Y have the meanings as cited in the description and wherein represents an E or Z double bond. The invention also relates to the production of these compounds, to their use as inhibitors of the polo-like kinase (PLK) for treating different diseases, and to intermediate products for producing thiazolidones.
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10.发明授权LEUKOTRIEN-B4 DERIVATE, INSBESONDERE OXIMO-LTB4 ANTAGONISTEN 失效雷诺铂B4衍生物，INSBESONDERE OXIMO-LTB4 ANTAGONISTEN
公开(公告)号：EP0983235B1
公开(公告)日：2002-07-03
申请号：EP98930743.4
申请日：1998-05-22
发明人： BUCHMANN, Bernd , FRÖHLICH, Wolfgang , GIESEN, Claudia , HENNEKES, Hartwig , JAROCH, Stefan , SKUBALLA, Werner
IPC分类号： C07C405/00
CPC分类号： C07D277/56 , C07C403/08 , C07C2601/04 , C07C2601/14 , C07D257/06 , C07D277/24
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