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    • 5. 发明申请
    • NOVEL 1,3-DIALKYLUREA DERIVATIVE HAVING HYDROXYL GROUP
    • 具有羟基的新型1,3-二氨基脲衍生物
    • WO1996014293A1
    • 1996-05-17
    • PCT/JP1995002236
    • 1995-11-01
    • SANTEN PHARMACEUTICAL CO., LTD.KAWASHIMA, YoichiFUJIMURA, Ken-ichiSUHARA, HiroshiMIYAWAKI, NobuakiFUJITA, Yuko
    • SANTEN PHARMACEUTICAL CO., LTD.
    • C07C275/10
    • C07C275/24C07C2601/14
    • A compound represented by general formula (I) and salts thereof, wherein R and R represent carboxyl optionally converted into an ester, amide or hydroxamate group; R represents lower alkyl or phenyl lower alkyl; and R represents hydrogen, lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, hydroxy lower alkyl, mercapto lower alkyl, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, imidazolyl lower alkyl, indolyl lower alkyl, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted naphthyl or optionally substituted naphthyl lower alkyl. The compound has an inhibitory effect on endopeptidase 24.11 and being useful as a remedy for cardiovascular diseases such as cardiac insufficiency and hypertension, kidney diseases such as renal insufficiency, gastrointestinal disorders such as diarrhea and gastric hyperacidity, endocrine/metabolic diseases such as obesity, and autoimmune diseases such as rheumatism, and as an analgesic agent for muscular pain, hemicrania, etc.
    • 由通式(I)表示的化合物及其盐,其中R 1和R 4表示任选转化为酯,酰胺或异羟肟基的羧基; R 2表示低级烷基或苯基低级烷基; R 3表示氢,低级烷基,氨基低级烷基,低级烷基氨基低级烷基,羟基低级烷基,巯基低级烷基,羧基低级烷基,低级烷氧基羰基低级烷基,咪唑基低级烷基,吲哚基低级烷基,任意取代的苯基, 取代的苯基低级烷基,任选取代的萘基或任选取代的萘基低级烷基。 该化合物对内肽酶24.11具有抑制作用,可用作心血管疾病如心功能不全和高血压,肾脏疾病如肾功能不全,胃肠疾病如腹泻和胃酸过多,内分泌/代谢疾病如肥胖症的补救措施,以及 自身免疫性疾病如风湿病,以及作为肌肉疼痛,血红素等的镇痛剂。
    • 8. 发明申请
    • BENZOTHIAZOLINE COMPOUNDS
    • 苯并噻唑化合物
    • WO1983000865A1
    • 1983-03-17
    • PCT/JP1982000363
    • 1982-09-10
    • SANTEN PHARMACEUTICAL CO., LTD.IWAO, Jun-ichiOYA, MasayukiISO, Tadashi
    • SANTEN PHARMACEUTICAL CO., LTD.
    • C07D277/66
    • C07D277/66
    • Benzothiazoline derivatives represented by the general formula (I): wherein R represents a lower alkanoyl group, R represents one or more groups selected from among a hydrogen atom, a lower alkyl group, a lower alkoxy group, a hydroxy group, a halogen atom, a nitro group, a halogen-substituted lower alkyl group, and a sulfamoyl group, R represents or -COR , R and R each represents a hydrogen atom, a lower alkyl group, a cyclohexyl group or a substituted lower alkyl group, R represents a hydrogen atom, an alkyl group, a substituted alkyl group, an alkanoyl group, a substituted alkanoyl group, an alkenoyl group, a substituted alkenoyl group or a furylcarbonyl group, R represents a hydrogen atom, a hydroxy group, a phenyl-lower alkyl group or a benzoyl group, R represents a hydroxy group, a lower alkoxy group, represents a straight or branched alkylene group containing 1 to 6 carbon atoms, m represents 0 or 1, n represents 0 or 1, and p represents 4 or 5, and salts thereof, useful for treating cardiovascular diseases, and a process for their preparation.
    • 由通式(I)表示的苯并噻唑啉衍生物:其中R 1表示低级烷酰基,R 2表示选自氢原子,低级烷基,低级烷氧基中的一个或多个基团 ,羟基,卤素原子,硝基,卤素取代的低级烷基和氨磺酰基,R 3表示“或”或“-COR”,R 4和R 5均为H. 各自表示氢原子,低级烷基,环己基或取代的低级烷基,R 6表示氢原子,烷基,取代的烷基,烷酰基,取代的烷酰基,烯酰基 基团,取代的烯酰基或呋喃基羰基,R 7表示氢原子,羟基,苯基 - 低级烷基或苯甲酰基,R 8表示羟基,低级烷氧基, IMAGE>表示含有1至6个碳原子的直链或支链亚烷基,m表示0或1,n表示0或1,p 呈现4或5及其盐,可用于治疗心血管疾病,及其制备方法。