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    • 3. 发明授权
    • Pharmaceutically active 9-chloroprostaglandins
    • 药用活性9-氯前列腺素
    • US5204371A
    • 1993-04-20
    • US792574
    • 1991-11-15
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenWalter ElgerOlaf LogeEkkehard Schillinger
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenWalter ElgerOlaf LogeEkkehard Schillinger
    • C07C405/00
    • C07C405/0041C07C405/00
    • Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2,--, trans--CH.dbd.CH--, or --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.
    • 其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物,A为-CH 2 -CH 2 - 或顺式-CH = CH-,B为-CH 2 -CH 2, - , CH = CH-或-CH 3 B - ,W是羟基亚甲基或D和E一起代表直接键,或D是1-10个碳原子的直链或支链亚烷基,任选被氟取代,E是 氧或硫或直接键,并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基,对上述R2定义的取代芳基或卤素; 或环烷基,取代的环烷基,芳基,取代的芳基或芳族杂环,全部如上述R2所定义; 或其生理上可接受的盐,当R1为OH时,具有有价值的药理学性质。
    • 4. 发明授权
    • Pharmaceutically active 9-chloroprostaglandins
    • 药用活性9-氯前列腺素
    • US4444788A
    • 1984-04-24
    • US387140
    • 1982-06-10
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenWalter ElgerOlaf LogeEkkehard Schillinger
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenWalter ElgerOlaf LogeEkkehard Schillinger
    • A61K31/557A61K31/5575A61P43/00C07C67/00C07C401/00C07C405/00C07C177/00
    • C07C405/00C07C405/0041
    • Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.- or .beta.-position,R.sub.1 is OR.sub.2, or NHR.sub.3 wherein R.sub.3 is H or the acyl group ofa C.sub.1-15 hydrocarbon carboxylic or sulfonic acid;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --,trans--CH.dbd.CH--, or --C.tbd.C--, ##STR2## wherein the OH-group in each case can be in the .alpha.- or .beta.-position, and can be etherified or esterified by tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, trimethylsilyl dimethyl, tert-butylsilyl, tribenzylsilyl, acetyl, propionyl, butyryl or benzoyl;D and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon, aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacological properties.
    • 其中9-氯原子可以是α-或β-位,R1是OR2或NHR3,其中R3是H或C1-15烃羧酸或磺酸的酰基; A是-CH 2 -CH 2 - 或顺式-CH = CH-,B是-CH 2 -CH 2 - ,反式-CH = CH-或-C 3位C,,其中每种情况下的OH-基团可以是 四氢呋喃基,α-乙氧基乙基,三甲基甲硅烷基二甲基,叔丁基甲硅烷基,三苄基甲硅烷基,乙酰基,丙酰基,丁酰基或苯甲酰基可以醚化或酯化。 D和E一起代表直接键或D是1-10个碳原子的直链或支链亚烷基,任选被氟取代,E是氧或硫或直接键,并且R 4是羟基或羟基醚化或 酯化如上述W所定义; R5是C1-10烃脂族基团; C1-10烃基,被芳基取代的脂族基团,对上述R2定义的取代芳基或卤素; 或环烷基,取代的环烷基,芳基,取代的芳基或芳族杂环,全部如上述R2所定义; 或其生理上可接受的盐,当R1为OH时,具有有价值的药理学性质。
    • 10. 发明授权
    • 1,2-Biguanides
    • 1,2双胍
    • US3960949A
    • 1976-06-01
    • US486758
    • 1974-07-09
    • Hanns AhrensClemens RuferHelmut BiereEberhard SchroderWolfgang LosertOlaf LogeEkkehard Schillinger
    • Hanns AhrensClemens RuferHelmut BiereEberhard SchroderWolfgang LosertOlaf LogeEkkehard Schillinger
    • C07C279/26C07C129/16
    • C07C279/26
    • 1,2-Substituted biguanides of the formula ##EQU1## wherein R.sub.1 is saturated or unsaturated, straight-chain or branched hydrocarbon of 1-12 carbon atoms which is unsubstituted or substituted by one or more fluorine atoms; a cycloalkyl group of 3-6 carbon atoms; or an aryl or aralkyl group of the formula ##SPC1##With n being the integer 0, 1 or 2 and X being hydrogen or halogen; and R'.sub.1 is a hydrogen atom or a saturated or unsaturated, straight-chain or branched hydrocarbon group of 1-12 carbon atoms; or R.sub.1 and R'.sub.1 collectively with the nitrogen atom to which they are attached are a heterocyclic ring containing one or more hetero atoms; and R.sub.2 is saturated or unsaturated, straight-chain or branched hydrocarbon of 1-12 carbon atoms which is unsubstituted or substituted by one or more fluorine atoms; or cycloalkyl of 3-6 carbon atoms, alkoxyalkyl containing a total of 2-12 carbon atoms, or alkoxy of 1-6 atoms; mixtures thereof, and pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of diabetes mellitus.
    • 1,2-取代的式R'1 | R1-NC-NH-C-NH2的平行二亚胺平行平行NNH | R2其中R1是1-12个碳原子的饱和或不饱和的直链或支链烃,未取代或未取代的 被一个或多个氟原子取代; 3-6个碳原子的环烷基; 或下式的芳基或芳烷基:其中N为整数0,1或2且X为氢或卤素; 并且R'1是1-12个碳原子的氢原子或饱和或不饱和的直链或支链烃基; 或者R1和R'1与它们所连接的氮原子一起是含有一个或多个杂原子的杂环; R2是未被取代或被一个或多个氟原子取代的1-12个碳原子的饱和或不饱和的直链或支链烃基; 或3-6个碳原子的环烷基,总共2-12个碳原子的烷氧基烷基或1-6个原子的烷氧基; 其混合物及其药学上可接受的酸加成盐可用于治疗糖尿病。