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COMPOSITIONS AND METHODS OF STIMULATION OF THE MOTOR FUNCTION OF THE GASTROINTESTINAL TRACT
专利权人:
ИПСЕН ФАРМА С.А.С. (FR)
发明人:
ДАТТА Ракеш (US),ДОНГ Чжен Ксин (US)
申请号:
RU2011103062/15
公开号:
RU2011103062A
申请日:
2011.01.27
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A method of stimulating the motor function of the gastrointestinal tract in a patient, comprising administering a peptidic analog of ghrelin, a prodrug thereof or a pharmaceutically acceptable salt of said analogue or said prodrug. ! 2. The method according to claim 1, where the specified patient suffers from postoperative intestinal obstruction after surgery on the gastrointestinal tract. ! 3. The method according to claim 1, where the specified patient is simultaneously or pre-administered opioid painkillers. ! 4. The method according to claim 2, where the indicated patient is simultaneously or previously administered opioid painkillers. ! 5. The method according to claim 3, wherein said peptidyl analog of ghrelin comprises a compound of formula (I):! ! (I)! where A1 is Gly, Aib, Ala, ß-Ala or Acc; ! A2 is Ser, Aib, Act, Ala, Acc, Abu, Ava, Thr or Val; ! A3 is Ser, Ser (C (O) -R4), Asp (O-R8), Asp (NH-R9), Cys (S-R14), Dap (S (O) 2-R10), Dab (S ( O) 2-R11), Glu (O-R6), Glu (NH-R7), Thr, Thr (C (O) -R5) or HN-CH ((CH2) nN (R12R13)) - C (O) ; ! A4 stands for Phe, Acc, Aic, Cha, 2-Fua, 1-Nal, 2-Nal, 2-Pal, 3-Pal, 4-Pal, hPhe, (X1, X2, X3, X4, X5) Phe, Taz , 2-Thi, 3-Thi, Trp or Tyr; ! A5 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle or Val; ! A6 is Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr or Val; ! A7 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic or is excluded; ! A8 is Glu, Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN-CH ((CH2) n-N (R12R13)) - C (O) or is excluded; ! A9 stands for His, Apc, Aib, Acc, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi, (X1, X2, X3, X4, X5) Phe or is excluded ; ! A10 is Gln, Acc, Aib, Asn, Asp, Glu or is excluded; ! A11 is Arg, Apc, hArg, Dab, Dap, Lys, Orn, HN-CH ((CH2) n-N (R12R13)) - C (O) or is excluded; ! A12 is Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, Ile, Leu, Nle, Tle or is excluded; ! A13 is Gln, Acc, Aib, Asn, Asp, Glu or is excluded; ! A14 is Gln, Acc, Aib, Asn, Asp, Glu or is excluded; !
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