利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

26 条记录 (耗时 0.029 秒)

    Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid amides
    2.
    发明授权
    Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid amides 失效
    使用新的噻吩并三唑-1,4-二氮杂-2-羧酸酰胺的方法

    公开(公告)号：US5155103A

    公开(公告)日：1992-10-13

    申请号：US774683

    申请日：1991-10-11

    申请人： Karl-Heinz Weber ,  Albrecht Harreus ,  Jorge Casals-Stenzel ,  Gojko Muacevic ,  Wolfgang Troger ,  Gerhard Walther

    发明人： Karl-Heinz Weber ,  Albrecht Harreus ,  Jorge Casals-Stenzel ,  Gojko Muacevic ,  Wolfgang Troger ,  Gerhard Walther

    IPC分类号： A61K31/55 ,  A61K31/5517 ,  A61P7/02 ,  A61P9/02 ,  A61P11/08 ,  A61P29/00 ,  A61P37/00 ,  A61P37/08 ,  C07C235/40 ,  C07D243/00 ,  C07D249/08 ,  C07D333/00 ,  C07D333/36 ,  C07D495/00 ,  C07D495/04 ,  C07D495/14

    CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D495/14

    摘要： The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.

    摘要翻译： 本发明涉及式I的新的噻吩并三唑并-1,4-二氮杂-2-羧酸酰胺其中R 1表示氢，可以任意被C 1 -C 4直链或支链烷基取代的C 1 -C 4直链或支链烷基 卤素，优选Cl或Br，或羟基，环丙基，C 1 -C 3烷氧基，优选甲氧基或卤素，优选氯或溴; R2和R3各自独立地代表氢，C1-C4直链或支链烷基，C1-C4羟基烷基或两个R2和R3与氮原子一起表示5-，6-或7-元环，其中 任选地含有氮，氧或硫原子作为另外的杂原子，第二氮原子任选被C 1 -C 4烷基，优选甲基取代; R4表示α-吡啶基或苯基，其中苯环优选在2-位上被甲基，卤素，优选氯或溴，硝基或三氟甲基取代; n表示数字0,1,2,3,4,5,6,7或8中的一个; 及其新型中间体。 式I化合物可用于治疗涉及血小板活化因子的病理状况和疾病。

    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents
    7.
    发明授权
    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents 失效
    3-OXA-5-FLOORO-CARBACYCLINS，其制备和用作药物代理

    公开(公告)号：US5157042A

    公开(公告)日：1992-10-20

    申请号：US713002

    申请日：1991-06-10

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    IPC分类号： C07C69/708 ,  A61K31/225 ,  A61K31/35 ,  A61K31/351 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  C07C51/00 ,  C07C51/367 ,  C07C59/125 ,  C07C59/62 ,  C07C67/00 ,  C07C67/31 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/88 ,  C07C405/00 ,  C07D309/12 ,  C07D317/72

    CPC分类号： C07D317/72 ,  C07C405/0083

    摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.5 is a free or functionally modified hydroxy group; andwhen R.sub.1 is OH, the salts thereof with physiologically compatible bases,are valuable pharmacological agents.

    摘要翻译： 式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，烷基，环烷基，芳基，杂芳基或杂环残基; 或R1是NHR3，其中R3是酸残基（酰基）或R2; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH基可以是α-或β-位; D是1-10个碳原子的直链饱和脂族基团; 或2-10个碳原子的支链，饱和或直链或支链的不饱和脂族基团; 所有这些都被氟原子取代; n为1,2或3; E是直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6是氢或1-5个碳原子的烷基，R 7是氢，卤素或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离或官能改性的羟基; 当R1是OH时，其与生理上相容的碱的盐是有价值的药剂。

    Carbacyclins, process for the preparation thereof, and use thereof as medicinal agents
    9.
    发明授权
    Carbacyclins, process for the preparation thereof, and use thereof as medicinal agents 失效
    卡巴菌素，其制备方法及其作为药剂的用途

    公开(公告)号：US5124343A

    公开(公告)日：1992-06-23

    申请号：US141233

    申请日：1988-01-06

    申请人： Helmut Vorbrueggen ,  Hernd Raduechel ,  Werner Skuballa ,  Norbert Schwarz ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    发明人： Helmut Vorbrueggen ,  Hernd Raduechel ,  Werner Skuballa ,  Norbert Schwarz ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    IPC分类号： C07C45/59 ,  C07C57/26 ,  C07C57/60 ,  C07C405/00 ,  C07D263/14 ,  C07D317/72 ,  C07F9/40

    CPC分类号： C07D317/72 ,  C07C405/0083 ,  C07C45/59 ,  C07C57/26 ,  C07C57/60 ,  C07D263/14 ,  C07F9/4018

    摘要： The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.4 is an alkyl, cycloalkyl, or optionally substituted arly group, or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group, andif R.sub.2 means a hydrogen atom, the salts thereof with physiologically compatible bases;to processes for the preparation thereof, and to the use thereof as blood-pressure-lowering agents.

    摘要翻译： 本发明涉及通式I的碳霉素，其中R 1是残基CH 2 OH或R 2，其中R 2表示氢原子，烷基，环烷基，芳基，芳基或杂环残基，或者R 1是 残基其中R3表示分别为1-10个碳原子的烷酰基或烷磺酰基残基或残基R2，或R1为残基，其中m为数1或2，X为氧原子或CH2- 基团，A是反式-CH = CH-或 - 3BOND C-基团，W是游离或官能改性的羟基亚甲基基团，其中OH-基团可以是α或β位置，n是数1，2 或3，D是1-5个碳原子的直链亚烷基，E是-C3OND C键或-CR6 = CR7-基团，其中R6和R7彼此不同，意指氢 原子或1-5个碳原子的烷基或氢原子或卤素原子，优选氯，R4是烷基，环烷基或任选取代的芳基或杂环基团 p，R5是游离或功能改性的羟基，如果R 2表示氢原子，则其与生理上相容的碱的盐; 其制备方法及其作为降血压剂的用途。