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    • 3. 发明申请
    • NEW PEPTIDES
    • 新胶囊
    • WO1994015959A1
    • 1994-07-21
    • PCT/SE1993001090
    • 1993-12-20
    • AKTIEBOLAGET ASTRA
    • AKTIEBOLAGET ASTRASCHILLER, Peter
    • C07K05/10
    • C07K7/06A61K38/00C07K5/0207C07K5/06078C07K5/0812C07K5/1016
    • Compounds of formula (I) as well as methods for their preparation, their pharmaceutical preparations and their use. The compounds of formula (I) are useful in therapy, especially as analgesics and as immunosuppressive agents. R3, R4, R5, R6 are all H or R4 and R5 are both H and R3 and R6 are both lower alkyl groups or R3, R5, R6 are all H and R4 is F, Cl, Br, OH, NH2 or NO2; R7 is C = O or CH2; R8 is H or a lower alkyl group; R9 is (II), wherein m is 0-2 or (III) or (IV) or (V) or (VI) or (VII) or (VIII) wherein R10 is H, F, Cl, Br or I and m is 0-2; R11 is OH, NH2 or (IX) wherein R12 is H, NO2, F, Cl, Br or I, m is 0-2, R13 is COOH, CONH2, CH2OH, or any additional amino acid or peptide segment, or R11 is (X) wherein R14 is COOH, CONH2, CH2OH, or any additional amino acid or peptide segment; with the exceptions of the compounds wherein R1, R2, R3, R4, R5, R6 and R8 are all H, R7 is C = O and R9 is (XI) and R11 is Phe-OH, Phe-NH2, OH or NH2.
    • 式(I)化合物及其制备方法,其药物制剂及其用途。 式(I)化合物可用于治疗,特别是作为止痛剂和免疫抑制剂。 R3,R4,R5,R6全部为H或R4,R5均为H和R3,R6均为低级烷基或R3,R5,R6均为H,R4为F,Cl,Br,OH,NH2或NO2; R 7为C = O或CH 2; R8是H或低级烷基; R 9是(II),其中m是0-2或(III)或(IV)或(V)或(VI)或(VII)或(VIII)其中R 10是H,F,Cl,Br或I和m 是0-2; R 11是OH,NH 2或(IX)其中R 12是H,NO 2,F,Cl,Br或I,m是0-2,R 13是COOH,CONH 2,CH 2 OH或任何另外的氨基酸或肽片段,或者R 11是 (X)其中R14是COOH,CONH2,CH2OH或任何另外的氨基酸或肽段; 除了其中R 1,R 2,R 3,R 4,R 5,R 6和R 8都是H,R 7是C = O并且R 9是(Ⅺ),R 11是Phe-OH,Phe-NH 2,OH或NH 2的化合物之外。
    • 10. 发明申请
    • SUBSTITUTED BENZIMIDAZOLES, PROCESS FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
    • 替代苯西泮,其制备方法及其药物用途
    • WO1991019711A1
    • 1991-12-26
    • PCT/SE1991000415
    • 1991-06-11
    • AKTIEBOLAGET ASTRA
    • AKTIEBOLAGET ASTRABRÄNDSTRÖM, Arne, ElofLINDBERG, Per, LennartSUNDÉN, Gunnel, Elisabeth
    • C07D401/12
    • C07D401/12C07D405/14
    • The novel compounds of formula (I), wherein R and R , which are different, is each H, alkyl containing 1-4 carbon atoms or -C(O)-R ; one of R or R is always selected from the group -C(O)-R ; wherein R is alkyl containing 1-4 carbon atoms or alkoxy containing 1-4 carbon atoms, R is the group -CH2OCOOR , wherein R is alkyl containing 1-6 carbon atoms or benzyl; R and R are the same or different and selected from -CH3, -C2H5, (a), (b) and -CH2CH2OCH3, or R and R form together with the adjacent oxygen atoms attached to the pyridine ring and the carbon atoms in the pyridine ring a ring, wherein the part constituted by R and R is -CH2CH2CH2-, -CH2CH2- or -CH2- as well as pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
    • 式(I)的新化合物,其中不同的R 1和R 2各自为H,含有1-4个碳原子的烷基或-C(O)-R 6; R 1或R 2中的一个总是选自基团-C(O)-R 6; 其中R 6是含有1-4个碳原子的烷基或含有1-4个碳原子的烷氧基,R 3是基团-CH 2 COOOR 7,其中R 7是含有1-6个碳原子的烷基或苄基 ; R 4和R 5相同或不同,选自-CH 3,-C 2 H 5,(a),(b)和-CH 2 CH 2 OCH 3,或R 4和R 5与相邻的氧 连接到吡啶环上的原子和吡啶环中的碳原子是一个环,其中由R 4和R 5构成的部分是-CH 2 CH 2 CH 2 - , - CH 2 CH 2 - 或-CH 2 - 以及含有这样的药物组合物 化合物作为活性成分,以及该化合物在药物中的用途。