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    • 5. 发明授权
    • Trioxopteridine derivatives suitable as medicament
    • 适合作为药物的三氟opter啶衍生物
    • US4046893A
    • 1977-09-06
    • US650749
    • 1976-01-20
    • Masuichi TakinoTeikichi KurosakiMunehiko Odaka
    • Masuichi TakinoTeikichi KurosakiMunehiko Odaka
    • A61K31/505
    • Trioxopteridine derivatives of the formula ##STR1## , wherein R.sub.1 is a normal alkyl group having 0 to 6 hydroxyl groups and R.sub.2 is hydrogen or a normal lower alkyl group having 0 to 5 hydroxyl groups, are prepared by catalytically hydrogenating a 6-substituted-5-nitro-2,4-dioxopyrimidine to give a 6-substituted-5-amino-2,4-dioxopyrimidine, and then reacting the latter compound with a compound of the formula R.sub.2 --A--COOR.sub.3, wherein R.sub.3 is hydrogen, lower alkyl, an alkali metal or an alkaline earth metal and A is carbonyl or a group of the formula ##STR2## wherein R.sub.4 is lower alkyl. The resulting trioxopteridine derivatives have analgesic and antiphlogistic properties and are therefore useful as pharmaceutical medicaments.
    • 其中R1是具有0至6个羟基并且R2是氢的正烷基或具有0至5个羟基的正常低级烷基,其通过催化氢化6-取代-5 - 硝基-2,4-二氧代嘧啶,得到6-取代-5-氨基-2,4-二氧代嘧啶,然后使后一化合物与式R2-A-COOR3的化合物反应,其中R3是氢,低级烷基 碱金属或碱土金属,A为羰基或式为“IMAGE”的基团,其中R4为低级烷基。 所得的三氟opter啶衍生物具有止痛和消炎性质,因此可用作药物药物。
    • 6. 发明授权
    • 1,2 Dihydro- and 1,2,3,4-tetrahydro quinolylacetic acids and analgesic
use thereof
    • 1,2二氢 - 和1,2,3,4-四氢喹啉基乙酸及其止痛用途
    • US4555513A
    • 1985-11-26
    • US452146
    • 1982-12-22
    • Masaaki HamadaKaoru OkamaotoTeikichi Kurosaki
    • Masaaki HamadaKaoru OkamaotoTeikichi Kurosaki
    • C07D215/14A61K31/47A61P25/04A61P29/00C07D215/06C07D215/08C07D215/12C07D215/18C07D215/22C07D215/233
    • C07D215/233C07D215/06C07D215/08C07D215/12C07D215/18
    • Novel quinolylacetic acid compounds of the formula (I): ##STR1## wherein R.sub.1 is a member selected from the group consisting of hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, and a lower alkyl group having 1 to 4 carbon atoms substituted with an aromatic group having a substituent;R.sub.2 is a member selected from the group consisting of hydrogen atom and a lower alkyl group having 1 to 4 carbon atoms;R.sub.3 is a member selected from the group consisting of hydrogen, a halogen atom, an alkyl group having 1 to 8 carbon atoms, and an alkenyl group having 2 to 8 carbon atoms;R.sub.4 and R.sub.5, carpable of cyclization, are each a member selected from the group consisting of hydrogen atom and a lower alkyl group having 1 to 4 carbon atoms;R.sub.6 is a member selected from the group consisting of hydrogen atom an alkyl group having 1 to 8 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, an alkynyl group having 3 to 8 carbon atoms, an aralkyl group, a substituted aralkyl group, an aliphatic or aromatic acyl group, and a substituted aliphatic or aromatic acyl group; andA is a member selected from the group consisting of hydrogen atom and an oxo group;the broken line denoting a second bond or no bond when A is a hydrogen atom and denoting no bond when A is an oxo group, and pharmaceutically acceptable salts thereof.
    • 式(I)的新型喹啉基乙酸化合物:其中R 1是选自氢原子,具有1至4个碳原子的低级烷基和具有1至4个碳原子的低级烷基的成员 4个碳原子被具有取代基的芳基取代; R2为选自氢原子和碳原子数为1〜4的低级烷基的成员; R3为选自氢,卤素原子,碳原子数为1〜8的烷基和碳原子数为2〜8的烯基的成员; 可环化的R 4和R 5各自是选自氢原子和具有1至4个碳原子的低级烷基的成员; R6为选自氢原子,碳原子数1〜8的烷基,碳原子数2〜5的烯基,碳原子数3〜8的炔基,芳烷基,取代芳烷基 脂族或芳族酰基,和取代的脂族或芳族酰基; A为选自氢原子和氧代基的成员; 当A是氢原子并且当A是氧代基时不表示键时,表示第二个键或无键的虚线及其药学上可接受的盐。