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    • 4. 发明申请
    • ENDOPEPTIDASE 24.15 INHIBITOR
    • 内毒素24.15抑制剂
    • WO1995019356A1
    • 1995-07-20
    • PCT/JP1995000020
    • 1995-01-11
    • SANTEN PHARMACEUTICAL CO., LTD.MITA, ShiroRI, KyurinFUJITA, YukoITO, Susumu
    • SANTEN PHARMACEUTICAL CO., LTD.
    • C07D277/06
    • C07D277/06
    • An endopeptidase 24.15 inhibitor containing a compound represented by the general formula (I) or a salt thereof as the active ingredient, wherein R represents hydrogen, lower alkyl, hydroxy or lower alkanoyloxy; R represents hydrogen, lower alkanoyl or benzoyl; R represents hydrogen and R represents hydrogen, lower alkyl or phenylated lower alkyl, provided that R and R may be combined with each other to form a pyrrolidine ring, that the lower alkyl may be substituted by hydroxy, carboxy, mercapto, lower alkylthio, imidazolyl or indolyl, and that the phenyl of the phenylated lower alkyl may be substituted by hydroxy or lower alkoxy; R represents carboxyl which may be in the form of ester or amide; and A represents C1-C3 linear or branched alkylene. The compound has an excellent endopeptidase 24.15 inhibitory activity and is promising as an analgesic, antirheumatic, osteoporosis remedy, and dementia remedy.
    • 含有由通式(I)表示的化合物或其盐作为活性成分的内肽酶24.15抑制剂,其中R 1表示氢,低级烷基,羟基或低级烷酰氧基; R 2表示氢,低级烷酰基或苯甲酰基; R 3表示氢,R 4表示氢,低级烷基或苯基低级烷基,条件是R 3和R 4可以彼此结合形成吡咯烷环,低级烷基可以是 被羟基,羧基,巯基,低级烷硫基,咪唑基或吲哚基取代,苯基低级烷基的苯基可以被羟基或低级烷氧基取代; R 5表示可以是酯或酰胺形式的羧基; A表示C1-C3直链或支链亚烷基。 该化合物具有优异的内肽酶24.15抑制活性,并且有希望作为止痛,抗风湿,骨质疏松症和痴呆症。
    • 6. 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。