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    • 4. 发明授权
    • Oxazolidine dione derivatives
    • 恶唑烷二酮衍生物
    • US5391565A
    • 1995-02-21
    • US978706
    • 1993-02-03
    • Richard M. Hindley
    • Richard M. Hindley
    • A61K31/42A61K31/421A61K31/425A61K31/44A61K31/496A61K31/505A61P3/06A61P3/08A61P9/00C07D263/44C07D263/58C07D413/12C07D417/12
    • C07D263/44C07D263/58C07D413/10
    • Compounds of the formula: ##STR1## or tautomeric forms and a pharmaceutically acceptable salt, and pharmaceutically acceptable solvates thereof, wherein:A.sup.1 is a substituted or unsubstituted oxazole substituted by up to 4 substituents selected from the group consisting of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, phenyl, and halogen or any two substituents on adjacent carbon atoms, together with the carbon atoms to which they are attached, form a benzene ring, and wherein the carbon atoms of the benzene ring represented by the said two substituents are unsubstituted or substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-5 -alkylcarbonyl;R.sup.l is a hydrogen atom, a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkylcarbonyloxy group, a phenyl-C.sub.1-6 -alkyl group, wherein the phenyl moiety may be substituted or unsubstituted, or a substituted or unsubstituted phenyl group, wherein the said phenyl groups may be substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-6 -alkylcarbonyl;A.sup.2 is a benzene ring having in total up to five substituents wherein three optional substituents are selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl. C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-6 -alkylcarbonyl; and n is an integer from 2 to 6, are disclosed as hypoglycemics, hypolipidemics and antihypertensives.
    • PCT No.PCT / GB91 / 01337 Sec。 371日期:1993年2月3日 102(e)日期1993年2月3日PCT 1991年8月5日PCT PCT。 出版物WO92 / 02520 日期:1992年2月20日,下列化合物:或互变异构形式及其药学上可接受的盐及其药学上可接受的溶剂化物,其中:A1是被至多4个取代基取代的取代或未取代的恶唑, C 1-6 - 烷基,C 1-6 - 烷氧基,苯基和卤素或相邻碳原子上的任何两个取代基与它们所连接的碳原子一起形成苯环,并且其中苯的碳原子 由所述两个取代基表示的环是未取代的或被至多三个选自卤素,C 1-6 - 烷基,苯基,C 1-6 - 烷氧基,卤代-C 1-6 - 烷基,羟基,氨基,硝基,羧基, C 1-6 - 烷氧基羰基,C 1-6 - 烷氧基羰基-C 1-6 - 烷基,C 1-6 - 烷基羰基氧基和C 1-5 - 烷基羰基; R1是氢原子,C1-6烷基,C1-6烷基羰基氧基,苯基-C1-6烷基,其中苯基部分可以是取代或未取代的,或取代或未取代的苯基, 其中所述苯基可以被最多三个选自卤素,C 1-6 - 烷基,苯基,C 1-6 - 烷氧基,卤代-C 1-6 - 烷基,羟基,氨基,硝基,羧基,C 1-6 - 烷氧基羰基-C 1-6 - 烷基,C 1-6 - 烷基羰基氧基和C 1-6 - 烷基羰基; A2是总共具有五个取代基的苯环,其中三个任选的取代基选自卤素,C 1-6 - 烷基,苯基,C 1-6 - 烷氧基,卤代-C 1-6 - 烷基,羟基,氨基,硝基,羧基 ,C 1-6 - 烷氧基羰基。 C 1-6 - 烷氧基羰基-C 1-6 - 烷基,C 1-6 - 烷基羰基氧基和C 1-6 - 烷基羰基; 并且n是2至6的整数,被公开为低血糖症,降血脂药和抗高血压药。
    • 7. 发明授权
    • Compounds
    • 化合物
    • US5194443A
    • 1993-03-16
    • US645092
    • 1991-01-24
    • Richard M. Hindley
    • Richard M. Hindley
    • C07D277/20C07D277/42C07D277/82C07D417/12
    • C07D277/20C07D277/42C07D277/82C07D417/12
    • Compounds of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A.sup.2 represents a benzene ring having in total up to five substituents; andn represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    • 式(I)的化合物:其中:A1表示取代或未取代的芳族杂环基;或其药学上可接受的盐, R1表示氢原子,烷基,酰基,芳烷基,其中芳基部分可以是取代或未取代的,或取代或未取代的芳基; R2和R3各自表示氢,或R2和R3一起表示键; A2代表总共有五个取代基的苯环; n表示2〜6的整数, 含有这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。