GPR119 AGONIST
    1.
    发明申请

    公开(公告)号:US20110137032A1

    公开(公告)日:2011-06-09

    申请号:US13056673

    申请日:2009-07-31

    摘要: A cyclic amine derivative represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes. wherein Ar0 is phenyl or phenyl having a substituent such as C1-8 alkylsulfonyl or the like, pyridyl, or pyridyl having a substituent such as C1-8 alkylsulfonyl;A0 is (CH2)p, O, or the like;B0 is (CH2)q, or the like, provided that B0 is neither O nor NR25 when A0 is O or NR24;one of U0 and V0 is N, and the other is N or CR26;each of X0 and Y0 is C1-3 alkylene or C1-3 alkylene having a substituent;R23 is a C1-8 alkyl group or the like;each of R21 and R22 is hydrogen, a halogen atom, or the like.

    摘要翻译: 由式(II)表示的环胺衍生物是GPR119激动剂,用作治疗糖尿病的药剂。 其中Ar 0是苯基或具有取代基的苯基,例如C1-8烷基磺酰基等,吡啶基或具有取代基的吡啶基,例如C1-8烷基磺酰基; A 0为(CH 2)p,O等; B0为(CH2)q等,条件是当A0为O或NR24时,B0既不为O也不为NR25; U0和V0之一是N,另一个是N或CR26; X0和Y0各自为C1-3亚烷基或具有取代基的C1-3亚烷基; R 23是C 1-8烷基等; R 21和R 22各自为氢,卤素原子等。

    Epoxysuccinic acid derivatives
    2.
    发明授权
    Epoxysuccinic acid derivatives 失效
    环氧琥珀酸衍生物

    公开(公告)号:US5843992A

    公开(公告)日:1998-12-01

    申请号:US930509

    申请日:1997-09-29

    IPC分类号: C07D303/48 A61K31/335

    CPC分类号: C07D303/48

    摘要: An epoxysuccinic acid derivative having the following formula: ##STR1## �wherein R.sup.1 is hydrogen, alkyl, aryl, or aralkyl; each of R.sup.2 and R.sup.3 independently is aryl, aralkyl or alkyl; X is --O-- or --NR.sup.4 --; and R.sup.4 is hydrogen, alkyl, or aralkyl! is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.

    摘要翻译: PCT No.PCT / JP96 / 00889 Sec。 371日期:1997年9月29日 102(e)日期1997年9月29日PCT提交1996年4月1日PCT公布。 出版物WO96 / 30354 日期:1996年10月3日具有下式的环氧琥珀酸衍生物:其中R 1是氢,烷基,芳基或芳烷基; R2和R3各自独立地为芳基,芳烷基或烷基; X是-O-或-NR4-; 和R4是氢,烷基或芳烷基]可用于预防和治疗骨质疏松症,恶性高钙血症和佩吉特综合征等骨疾病,并且还可用于治疗组织蛋白酶L活性异常增强的骨关节炎和类风湿性关节炎, 并且还可用作治疗组织蛋白酶B和L参与的疾病的药物,例如肌营养不良和肌肉萎缩。

    GPR119 agonist
    6.
    发明授权
    GPR119 agonist 失效
    GPR119激动剂

    公开(公告)号:US08536176B2

    公开(公告)日:2013-09-17

    申请号:US13056673

    申请日:2009-07-31

    IPC分类号: A61K31/50 A61K31/501

    摘要: A cyclic amine derivative represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes. wherein Ar0 is phenyl or phenyl having a substituent such as C1-8 alkylsulfonyl or the like, pyridyl, or pyridyl having a substituent such as C1-8 alkylsulfonyl; A0 is (CH2)p, O, or the like; B0 is (CH2)q, or the like, provided that B0 is neither O nor NR25 when A0 is O or NR24; one of U0 and V0 is N, and the other is N or CR26; each of X0 and Y0 is C1-3 alkylene or C1-3 alkylene having a substituent; R23 is a C1-8 alkyl group or the like; each of R21 and R22 is hydrogen, a halogen atom, or the like.

    摘要翻译: 由式(II)表示的环胺衍生物是GPR119激动剂,用作治疗糖尿病的药剂。 其中Ar 0是苯基或具有取代基的苯基,例如C1-8烷基磺酰基等,吡啶基或具有取代基的吡啶基,例如C1-8烷基磺酰基; A 0为(CH 2)p,O等; B0为(CH2)q等,条件是当A0为O或NR24时,B0既不为O也不为NR25; U0和V0之一是N,另一个是N或CR26; X0和Y0各自为C1-3亚烷基或具有取代基的C1-3亚烷基; R 23是C 1-8烷基等; R 21和R 22各自为氢,卤素原子等。