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61. 发明授权

US06930102B2 16-halogen-epothilone derivatives, process for their production, and their pharmaceutical use 失效
标题翻译： 16-卤素 - 埃坡霉素衍生物，其制备方法及其药物用途
公开(公告)号：US06930102B2
公开(公告)日：2005-08-16
申请号：US10364337
申请日：2003-02-12
申请人： Ulrich Klar , Werner Skuballa , Bernd Buchmann , Wolfgang Schwede , Michael Schirner
发明人： Ulrich Klar , Werner Skuballa , Bernd Buchmann , Wolfgang Schwede , Michael Schirner
IPC分类号： A61K31/336 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/18 , A61K31/395 , C07D269/00
CPC分类号： C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/1804 , Y02P20/55
摘要： A compund of formula I, an epothilone derivative, its method of preparation, and use as a pharmaceutical agent in treating malignant tumors
摘要翻译：式I化合物，埃坡霉素衍生物，其制备方法和用作治疗恶性肿瘤的药物的组合物

62. 发明授权

US06225347B1 9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z） - 前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US06225347B1
公开(公告)日：2001-05-01
申请号：US08313667
申请日：1994-09-27
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C40500
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a —CR6═CR7 group, and R6 and R7 are different and mean a hydrogen atom, a chlorine atom or a C1-C4 alkyl group, R4 resents a free or functionally modified hydroxy group, R5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group, and if R2 means a hydrogen atom, its salts with physiologically compatible bases or its cyclodextrin chlathrates, process for their production and their pharmaceutical use.
摘要翻译：本发明涉及式Iin的9-卤素 - （Z）前列腺衍生物，其中Z代表基团.Hal表示α或β位上的氯或氟原子，R 1表示R 2表示氢原子，烷基，环烷基，芳基或杂环基或R 1表示基团，其中R 3表示酸基或基团R 2且A表示-CH 2 -CH 2 - ，反式-CH = CH或-C = C基团，W表示游离或功能修饰基团， OH基可以是α或β位，D和E一起代表直接键或D表示具有1-10个C原子的直链亚烷基，具有2-10个C原子的支链亚烷基或环状亚烷基具有3-10个C原子的基团，其任选地可以被氟原子取代，E表示氧或硫原子，直接键合，C = C键或-CR 6 = CR 7基团，并且R 6和R 7不同，一个氢原子，一个氯原子或一个C 1 -C 4烷基，R 4是一个游离的或官能改性的羟基，R 5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱或其环糊精的盐 chlathrates，生产过程及其药物用途。

63. 发明授权

US5891910A 9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z）前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US5891910A
公开(公告)日：1999-04-06
申请号：US467888
申请日：1995-06-06
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I ##STR1## in which ##STR2## Z represents the radicals Hal represents a chlorine or fluorine atom,R.sub.1 represents ##STR3## A represents a --CH.sub.2 --CH.sub.2 --, a trans--CH=CH or --C.ident.C, W represents a free or a functionally modified ##STR4## group, D and E together represent a direct bond orD represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, andE represents an oxygen or sulfur atom, a direct bond, a C.ident.C bond or a --CR.sub.6 =CR.sub.7 group, and R.sub.6 and R.sub.7 are different and mean a hydrogen atom, a chlorine atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.4 represents a free or functionally modified hydroxy,R.sub.5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group.
摘要翻译：本发明涉及式I的9-卤代 - （Z）前列腺衍生物，其中，Z表示基团，Hal表示氯或氟原子，R1表示A表示 -CH 2 -CH 2 - ，反式-CH = CH或-C = C，W表示游离或官能改性的基团，D和E一起表示直接键或D表示直链亚烷基，其中1 -10个C原子，具有2-10个碳原子的支链亚烷基或具有3-10个C原子的环状亚烷基，其任选可以被氟原子取代，E表示氧或硫原子，直接键，C = C键或-CR6 = CR7基，R6和R7不同，表示氢原子，氯原子或C1-C4烷基，R4表示游离或官能改性的羟基，R5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基。

64. 发明授权

US5859054A Leukotriene B4 derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译：白三烯B4衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US5859054A
公开(公告)日：1999-01-12
申请号：US682724
申请日：1996-11-08
申请人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
发明人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
IPC分类号： C07D521/00 , A61K31/19 , A61K31/195 , A61K47/40 , A61P1/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07C43/115 , C07C59/13 , C07C59/58 , C07C59/62 , C07C59/72 , C07C67/31 , C07C67/343 , C07C69/708 , C07C69/734 , C07C235/04 , C07C235/08 , C07C311/00 , C07C323/14 , A61K31/215
CPC分类号： C07C59/72 , C07C235/08 , C07C59/62 , C07C69/708 , C07C2101/14
摘要： Pharmacologically active leukotriene-B.sub.4 derivatives of general formula I, ##STR1## are described, in whichR.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sub.4, CONR.sub.5 R.sub.6, orR.sub.2 represents H or an organic acid radical with 1-15 C atoms,R.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; C.sub.6 -C.sub.10 aryl radicals optionally substituted by 1-3 halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy; CH.sub.2 --CO--(C.sub.6 -C.sub.10) aryl or a 5- to 6-membered ring with at least 1 heteroatom,A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group,B symbolizes a C.sub.1 -C.sub.10 straight-chain or branched-chain alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D means a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond,R.sub.5 and R.sub.6 are the same or different, and represent H or C.sub.1 -C.sub.4 alkyl or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 SO.sub.2, and are optionally substituted with OH,R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine,R.sub.8 has the same meaning as R.sub.3,n is 2-5, and, if R.sub.4 means hydrogen, their salts with physiologically compatible bases and their cyclodextrin clathrates.
摘要翻译： PCT No.PCT / EP94 / 00216 Sec。 371日期：1996年11月8日 102（e）日期1996年11月8日PCT 1994年1月27日PCT公布。出版物WO95 / 20564 日期：1995年8月3日描述了通式I的化学活性白三烯-BB衍生物，其中R1表示CH 2 OH，CH 3，CF 3，COOR 4，CONR 5 R 6或R 2表示H或有机酸基团，其中1 -15 C原子，R3表示H; 任选取代的C 1 -C 14烷基，C 3 -C 10环烷基或多或多个; 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，羰基，羧基或羟基任意取代; C 6 -C 10芳基独立地彼此独立地被卤素，苯基，或具有至少1个杂原子的5至6元芳族杂环，R 4表示氢，C 1 -C 10烷基，C 3 -C 10环烷基; 任选被1-3个卤素，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，羧基或羟基取代的C 6 -C 10芳基; CH2-CO-（C6-C10）芳基或具有至少1个杂原子的5-至6-元环，A表示反式，反式-CH = CH-CH = CH，-CH 2 CH 2 -CH = CH-或四亚甲基，B表示C1-C10直链或支链亚烷基，其任选可以被氟取代，或者基团D表示直接键，氧，硫，-C 3位C，-CH = CR7或与B一起也可以表示直接键合，R5和R6相同或不同，表示H或C1-C4烷基或R6表示H，R5表示C1-C15烷酰基或R8SO2，并且任选被 OH，R7表示H，C1-C5烷基，氯，溴，R8具有与R3相同的含义，n为2-5，如果R 4表示氢，则其与生理上相容的碱和它们的环糊精包合物的盐。

65. 发明授权

US5541202A New leukotriene-B4 Antagonists and their use as pharmaceutical agents 失效
标题翻译：新白三烯-B4拮抗剂及其作为药剂的用途
公开(公告)号：US5541202A
公开(公告)日：1996-07-30
申请号：US193192
申请日：1994-06-28
申请人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
发明人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
IPC分类号： A61K31/38 , A61K31/381 , A61P1/00 , A61P11/08 , A61P17/00 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/00 , C07D333/32 , C07D409/04 , C07D409/06 , A61K31/44
CPC分类号： C07D409/06 , C07D333/32
摘要： 1. Leukotriene-B.sub.4 antagonists of formula I, ##STR1## are described, in whichX represents C.sub.1 -C.sub.4 -alkoxy or --S(O).sub.p --(C.sub.1 -C.sub.4)-alkyl,p represents 0, 1 or 2Y represents a hydrogen atom or the radical CO--A--COR.sub.2 with A meaning an alkylene group with 1-6 C atoms in the chain or a radical ##STR2## R.sub.1 and R.sub.2 represents the radical OH, --O--(C.sub.1 -C.sub.4)-alkyl, --O--(C.sub.3 -C.sub.6)-cycloalkyl, --O--(C.sub.7 -C.sub.12)-aralkyl or the radical NR.sub.3 R.sub.4 with R.sub.3 and R.sub.4 meaning hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.6 -C.sub.10)-aryl or (C.sub.7 -C.sub.12)-aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their use as pharmaceutical agents.
摘要翻译： PCT No.PCT / EP92 / 01816 Sec。 371日期：1994年6月28日 102（e）日期1994年6月28日PCT提交1992年8月6日PCT公布。出版物WO93 / 04056 1991年3月4日。式I的白三烯-B4拮抗剂，ts-C4-烷氧基或-S（O）p-（C1-C4） - 烷基，p代表0,1或2，Y表示氢原子或具有A的基团CO-A-COR2表示链中具有1-6个C原子的亚烷基或基团R 1和R 2表示基团OH，-O-（C 1 -C 4） - 烷基，（C 3 -C 6） - 环烷基，-O-（C 7 -C 12） - 芳烷基或R 3和R 4的基团NR 3 R 4表示氢，（C 1 -C 4） - 烷基，（C 3 -C 6） - 环烷基，（ C 6 -C 10） - 芳基或（C 7 -C 12） - 芳烷基以及它们与生理上相容的碱和它们的环糊精包合物的盐，它们的生产方法及其作为药剂的用途。

66. 发明授权

US5414016A New leukotriene-B.sub.4 derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译：新的白三烯-B4衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US5414016A
公开(公告)日：1995-05-09
申请号：US259111
申请日：1994-06-13
申请人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
发明人： Werner Skuballa , Bernd Buchmann , Josef Heindl , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
IPC分类号： C07C33/12 , C07C59/46 , C07C69/007 , C07C69/732 , C07C405/00 , A61K31/557
CPC分类号： C07C405/00 , C07C33/12 , C07C59/46 , C07C69/007 , C07C69/732
摘要： Leukotriene-B.sub.4 derivatives of formula I ##STR1## are described, in which R.sup.1 means CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5, CONR.sup.6 R.sup.7, orR.sup.1 together with R.sup.2 means a carbonyl group,R.sup.4 symbolizes H, C.sub.1 -C.sub.10 alkyl optionally substituted, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.10 aryl radical optionally substituted, or a 5-6-membered aromatic heterocyclic ring,A symbolizes a trans, trans-CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group,B symbolizes a C.sub.1 -C.sub.10 alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sup.6 or together withB can also mean a direct bond, their salts with physiologically compatible bases and their cyclodextrin clathrates.
摘要翻译：其中R 1表示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，R4表示H，任选取代的C 1 -C 10烷基，C 3 -C 10环烷基，任选取代的C 6 -C 10芳基或5-6元芳族杂环，A表示反式，反式-CH = CH-CH = CH，-CH 2 CH 2 -CH = CH-或四亚甲基，B表示C1-C10亚烷基，其任选可以被氟取代，或者基团D可以表示直接键，氧，硫，-C 3位C，-CH = CR 6或与B一起也可以指直接键合，它们与生理上相容的碱的盐和它们的环糊精包合物。

67. 发明授权

US5352701A Leukotriene-B.sub.4 antagonist compounds and their use as pharmaceutical agents 失效
标题翻译：白三烯B4拮抗剂化合物及其作为药剂的用途
公开(公告)号：US5352701A
公开(公告)日：1994-10-04
申请号：US50195
申请日：1993-05-05
申请人： Josef Heindl , Werner Skuballa , Bernd Buchmann , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
发明人： Josef Heindl , Werner Skuballa , Bernd Buchmann , Wolfgang Frohlich , Roland Ekerdt , Claudia Giesen
IPC分类号： A61K31/19 , A61K31/215 , A61K31/22 , A61K31/44 , A61K31/4402 , A61K31/557 , A61P1/04 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07C20060101 , C07C59/64 , C07C59/68 , C07C59/90 , C07C65/40 , C07C69/738 , C07C69/94 , C07C235/20 , C07C235/34 , C07C317/22 , C07C323/19 , C07D213/55 , C07D213/79 , C07D213/80
CPC分类号： C07D213/79 , A61K31/19 , A61K31/215 , A61K31/44 , A61K31/557 , C07C59/68 , C07C59/90 , C07C69/738 , C07C69/94
摘要： 1. Leukotriene-B.sub.4 antagonists of formula I ##STR1## are described, in which X is a CH.sub.2 group or an oxygen atom,Y is C.sub.1 -C.sub.4 -alkoxy or --S(O).sub.p --C.sub.1 -C.sub.4 -alkyl,p is 0, 1 or 2Z is a hydrogen atom or the radical A-B-COOH with A being a hydroxymethylene group or a carbonyl group and B being an alkylene group with 1-6 atoms in the chain or a radical ##STR2## with the exception that B cannot mean the radical ##STR3## if X is a CH.sub.2 group, R.sub.1 is the radical OH, --O--(C.sub.1 --C.sub.4) -alkyl, --O--(C.sub.3-C.sub.6) -cycloalkyl, --O--(C.sub.7-C.sub.12) -aralkyl or the radical NHR.sub.4 with R.sub.4 being hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, C.sub.6 -C.sub.10 -aryl or (C.sub.7 -C.sub.12)-aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their use as pharmaceutical agents.
摘要翻译：描述了式I的白三烯-B4拮抗剂（I），其中X是CH 2基或氧原子，Y是C 1 -C 4 - 烷氧基或-S（O）p -C 1 -C 4 - 烷基，p为0,1或2，Z为氢原子或基团AB-COOH，其中A为羟基亚甲基或羰基，B为链中为1-6个原子的亚烷基或基团，如果X是CH2基团，B不能表示基团的例外，R1是基团OH，-O-（C 1 -C 4） - 烷基，-O-（C 3 -C 6） - 环烷基，-O-（ C7-C12） - 芳烷基或具有R4为氢的基团NHR4，（C1-C4） - 烷基，（C3-C6） - 环烷基，C6-C10-芳基或（C7-C12） - 芳烷基，以及它们与生理相容的碱和它们的环糊精包合物，其制备方法及其作为药剂的用途。

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