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    • 1. 发明授权
    • Process for preparing acetonin
    • 制备乙酰丙酮的方法
    • US3943134A
    • 1976-03-09
    • US515815
    • 1974-10-18
    • Shigeo KajiyamaTakamitsu KobayashiKeiro Yoshizue
    • Shigeo KajiyamaTakamitsu KobayashiKeiro Yoshizue
    • C07D239/06C07D239/04
    • C07D239/06
    • 2,2,4,4,6-Pentamethyl-2,3,4,5-tetrahydropyrimidine, called acetonin, is prepared by reacting acetone with ammonia in the presence of an ammonium halide catalyst and in the presence of from 0.01 to 0.5 mole % (based on acetone) of a promoter selected from the group consisting of: bromine; iodine; iodine trichloride; alkali metal iodides; lithium rhodanide, bromide, nitrate and cyanide; ammonium iodide, rhodanide, bromide, nitrate and sulfide; ammonium salts of carboxylic acids and of sulfonic acids; salts of nitrogen-containing organic bases with carboxylic acids and with sulfonic acids; aliphatic amine hydroiodides; carboxylic acids; and sulfonic acids.
    • 2,2,4,4,6-五甲基-2,3,4,5-四氢嘧啶,称为乙炔二酮,是通过丙酮与氨在卤化铵催化剂存在下反应制备的,并且在0.01至0.5摩尔 %(基于丙酮)的促进剂,其选自:溴; 碘; 三氯化碘; 碱金属碘化物; 硫氰酸锂,溴化物,硝酸根和氰化物; 碘化铵,硫化铑,溴化物,硝酸盐和硫化物; 羧酸和磺酸的铵盐; 含氮有机碱与羧酸和磺酸的盐; 脂肪胺氢碘酸盐; 羧酸; 和磺酸。
    • 2. 发明申请
    • SPIROKETAL DERIVATIVES AND USE THEREOF AS DIABETIC MEDICINE
    • SPIROKETAL衍生物及其作为糖尿病药物的用途
    • US20090030006A1
    • 2009-01-29
    • US11815074
    • 2006-01-27
    • Takamitsu KobayashiTsutomu SatoMasahiro Nishimoto
    • Takamitsu KobayashiTsutomu SatoMasahiro Nishimoto
    • A61K31/352A61P3/10C07D493/10A61K31/381A61K31/4433A61K31/498A61K31/404A61K31/4155C07D495/20C07D491/20
    • C07D311/96C07D491/153C07D493/10C07H19/01
    • The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(═O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.
    • 本发明提供式(I)的化合物:其中R 1,R 2,R 3和R 4各自独立地选自氢原子,任选取代的C 1 -C 6烷基,任选取代的C 7 -C 14芳烷基和-C( -O)Rx; Rx表示任选取代的C 1 -C 6烷基,任选取代的芳基,任选取代的杂芳基,任选取代的C 1 -C 6烷氧基或-NRrf; Ar 1表示任选取代的芳族碳环或任选单取代的芳族杂环; Q表示 - (CH 2)m - (L)p-或 - (L)p-(CH 2)m - ; m表示选自0至2的整数,n表示选自1和2的整数,p表示选自0和1的整数; L表示-O - , - S-或-NR5-; A表示任选取代的芳基或任选取代的杂芳基,其前药及其药学上可接受的盐,以及包含这种化合物的药物制剂或药物组合物。
    • 9. 发明授权
    • Spiroketal derivatives and use thereof as diabetic medicine
    • 螺缩酮衍生物及其作为糖尿病药物的用途
    • US07767651B2
    • 2010-08-03
    • US11815074
    • 2006-01-27
    • Takamitsu KobayashiTsutomu SatoMasahiro Nishimoto
    • Takamitsu KobayashiTsutomu SatoMasahiro Nishimoto
    • A01N43/04C07H1/00C07H3/00C08B37/00
    • C07D311/96C07D491/153C07D493/10C07H19/01
    • The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(═O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.
    • 本发明提供式(I)的化合物:其中R 1,R 2,R 3和R 4各自独立地选自氢原子,任选取代的C 1 -C 6烷基,任选取代的C 7 -C 14芳烷基和-C( ΟO)Rx; Rx表示任选取代的C 1 -C 6烷基,任选取代的芳基,任选取代的杂芳基,任选取代的C 1 -C 6烷氧基或-NRrf; Ar 1表示任选取代的芳族碳环或任选单取代的芳族杂环; Q表示 - (CH 2)m - (L)p-或 - (L)p-(CH 2)m - ; m表示选自0至2的整数,n表示选自1和2的整数,p表示选自0和1的整数; L表示-O - , - S-或-NR5-; A表示任选取代的芳基或任选取代的杂芳基,其前药及其药学上可接受的盐,以及包含这种化合物的药物制剂或药物组合物。