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    • 4. 发明授权
    • 3-(1-Pyrazolyl)-pyridazine derivatives and hypotensive compositions
thereof
    • 3-(1-吡唑基) - 哒嗪衍生物及其低血压组合物
    • US4224325A
    • 1980-09-23
    • US923623
    • 1978-07-11
    • Geza SzilagyiEndre KasztreinerLaszlo TardosEdit KosaLaszlo JaszlitsGyorgy CsehIlona Kovacs, nee SzaboPal TolnaySandor ElekIstvan ElekesIstvan Polgari
    • Geza SzilagyiEndre KasztreinerLaszlo TardosEdit KosaLaszlo JaszlitsGyorgy CsehIlona Kovacs, nee SzaboPal TolnaySandor ElekIstvan ElekesIstvan Polgari
    • C07D403/04A61K31/50A61K31/501A61P9/12A61P43/00C07D403/14C07D521/00A61K31/535C07D413/14
    • C07D231/12C07D233/56C07D249/08
    • The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group,R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group,R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group,R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.10 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-5 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl, a phenyl or a benzyl group, or --NR.sup.9 R.sup.10 may represent a morpholine, piperidine or piperazine ring,and their pharmaceutically acceptable acid-addition salts. Furthermore, the invention relates to a process for preparing these compounds.The novel compounds of general formula I have valuable pharmacological properties. Thus they show a considerable hypotensive effect and are capable to inhibit enzymes regulating the catabolism of prostaglandins.
    • 本发明涉及通式为“IMAGE”的化合物,其中R1代表氢原子或C1-6烷基,C2-4羟基烷基,C3-6环烷基或苯基,R2代表氢,氟, 氯或溴原子或C 1-6烷基,C 2-4羟基烷基,硝基或-NR 5 R 6基团,其中R 5和R 6可以具有相同或不同的含义,并且各自代表氢原子或C 1-4烷基或 C2-4羟基烷基,R3代表氢原子或C1-6烷基,C2-4羟烷基,C3-6环烷基或苯基,氯原子或羟基,氨基或甲氧基,R4代表 对于氨基甲酰基,氰基或-NR 7 -NHR 8基团,其中R 7和R 8可以具有相同或不同的含义,各自代表氢原子或C 1-4烷基,C 2-4羟烷基,C 1-4烷氧基羰基 或-NR 9 R 10基团,其中R 9和R 10可以具有相同或不同的含义,并且各自表示氢原子或C 1-5烷基,C 2-4的羟基烷基,C 3-6环烷基,苯基或苯基 或-NR9R10可以表示吗啉,哌啶或哌嗪环及其药学上可接受的酸加成盐。 此外,本发明涉及一种制备这些化合物的方法。 通式Ⅰ的新化合物具有有价值的药理学性质。 因此,它们显示出相当的降血压作用,并且能够抑制调节前列腺素分解代谢的酶。
    • 8. 发明授权
    • Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    • 厌氧性4 - [(3,4-二烷氧基苯基)烷基] -2-咪唑烷酮衍生物
    • US4308278A
    • 1981-12-29
    • US90450
    • 1979-11-01
    • Geza SchneiderFerenc AndrasiPal BerzsenyiArpad LazarSandor ElekIstvan ElekesIstvan Polgari
    • Geza SchneiderFerenc AndrasiPal BerzsenyiArpad LazarSandor ElekIstvan ElekesIstvan Polgari
    • A61K31/415A61K31/4166A61P1/00A61P3/04C07C45/71C07D233/32C07D233/34C07D233/38C07D233/78
    • C07C255/00C07C45/71C07D233/32C07D233/38C07D233/78Y10S514/91
    • 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.
    • 4 - [(3,4-二烷氧基苯基)烷基] -2-咪唑啉酮衍生物,其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基,是通过以下步骤制备的:(a)将具有通式II的乙内酰脲衍生物(其中R 1和R 2如上定义)与中性的氢化铝锂 有机溶剂,或(b)催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物,其中R 1和R 3如上所定义,而R 4的含义是氢原子或烷基 含有1至4个碳原子的基团,或(c)使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义,而R6代表含有1至4个碳原子的烷基,与有机或无机 基础。 具有式I的化合物具有有价值的治疗性质,主要是厌食症活性。