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    PROSTAGLANDIN I2 DERIVATIVE
    1.
    发明专利
    PROSTAGLANDIN I2 DERIVATIVE 失效

    公开(公告)号：JPS56120680A

    公开(公告)日：1981-09-22

    申请号：JP2227280

    申请日：1980-02-26

    Applicant: TORAY INDUSTRIES

    Inventor： OONO KIYOTAKA ,  NAGASE HIROSHI ,  NISHIO SHINTAROU

    IPC: C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61K31/557 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D405/12

    Abstract: NEW MATERIAL:A prostaglandin I2 derivative of formula I [R is group of formula II which may have a methyl group in the pyridine ring, group of formula III, formula IV, or -(CH2CH2O)2OR4; R1 is 1-3C alkylene; R3 is 1-29C alkyl; R4 is 1-12C alkyl]. EXAMPLE:Prostaglandin I2-2-pyridylmethyl ester. USE:Remedies such as antithrombic agent, antiulcer agent, antihypertension agent, etc., having improved stability under neutral or acidic conditions, keeping the strong pharmacological activity of the prostaglandin I2. It can be orally administered. PROCESS:The compound of formula I is prepared by (1) esterifying the compound of formula V, (2) reacting the product with a halogenating reagent thereby effecting intramolecular cyclization, and (3) reacting the resulting compound of formula VI (X is Br or I) with various bases to effect dehydrohalogenation reaction.

    PROSTAGLANDIN I2 DERIVATIVE
    7.
    发明专利
    PROSTAGLANDIN I2 DERIVATIVE 失效

    公开(公告)号：JPS5585578A

    公开(公告)日：1980-06-27

    申请号：JP15758978

    申请日：1978-12-22

    Applicant: TORAY INDUSTRIES

    Inventor： NISHIYAMA HISAO ,  OONO KIYOTAKA ,  NISHIO SHINTAROU

    IPC: C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/12 ,  C07D405/12

    Abstract: NEW MATERIAL:Prostaglandin I2 derivatives of formula VI[R is -OCH2COOC2H5, -OCH(CH3)COOC2H5, -OCH2CH2OCH3, -(OCH2CH2)3OH, phthalidoxy, -OC H2CH2N(CH2CH2OH)2, 2-(2-pyridyl)ethocy, 2-(6-hydroxypyridyl)methoxy, N- cyclohexylamide, N,N'-dicyclohexylureide]. EXAMPLE:PGI2 methoxyethyl ester. USE:Hypotensor and antithrombosis; the products sustain the equal or superior pharmaceutical activities to those of PGI2 and remove the structural instability under neutral and acidic conditions, thus permitting oral administration. PREPARATION:The compound of formula III is esterified or amidated and the resulting compound is cyclized intramolecularly. The product of formula V is subjected to dehydroiodization to give the objective compound of formula VI.

    PROSTAGLANDIN I2 DERIVATIVE
    9.
    发明专利
    PROSTAGLANDIN I2 DERIVATIVE 失效

    公开(公告)号：JPS56122372A

    公开(公告)日：1981-09-25

    申请号：JP2526580

    申请日：1980-03-03

    Applicant: TORAY INDUSTRIES

    Inventor： OONO KIYOTAKA ,  NAGASE HIROSHI ,  NISHIO SHINTAROU

    IPC: C07D307/935 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P43/00 ,  C07D405/06 ,  C07D405/12

    Abstract: NEW MATERIAL:A compound of formula I [R is H, alkali metal, alkaline earth metal, alkyl, cycloalkyl which may have alkyl group, aralkyl, phenyl which may have substituent groups, group of formula CH2COR1 (R1 is phenyl, p-bromophenyl, p-biphenyl, etc.), formulas II-V (R2 is alkylene), formula C2H2nOR3 (R3 is H or alkyl; n is an integer of 2-12) or formula (CH2CH2O)2OR3]. EXAMPLE:5,8,9,11,12,14,15-Heptadeutero-PGI2 methyl ester. USE:An intermediate of heptadeutero-6-oxo-PGF1alpha useful as an internal standard for the determination of the concentration of PGI2 in blood. It is also useful as a drug having a wide variety of physiolgical activities such as blood platelet coagulation inhibiting activity, vasodilating activity, gastric juice secretion suppressing activity, etc. PROCESS:The compound of formula I is prepared by the dehydrohalogenation of the compound of formula VI (X is Br or I) with a base.

    INDANE DERIVATIVE AND ANTIIINFLAMMATORY AGENT COMPRISING IT
    10.
    发明专利
    INDANE DERIVATIVE AND ANTIIINFLAMMATORY AGENT COMPRISING IT 失效

    公开(公告)号：JPS5587757A

    公开(公告)日：1980-07-02

    申请号：JP15931878

    申请日：1978-12-26

    Applicant: TORAY INDUSTRIES

    Inventor： SATOU HARUYO ,  IMAMURA SHINZOU ,  NISHIO SHINTAROU

    IPC: A61K31/15 ,  A61P29/00 ,  C07C67/00 ,  C07C239/00 ,  C07C251/44

    Abstract: NEW MATERIAL:An indane derivative of formula II (R is H or cyclohexyl group; R and R are H, straight, branched, or cyclic alkyl, aralkyl groups, etc.). EXAMPLE:1-N-Substituted amino-2-oxyiminoindane hydrochloride. USE:Medicines having an antiinflammatory and bacteriostatic actions, anmibistrable orally or parenterally. PROCESS:6-Cyclohexyl-indene or indene is chloronitrosated with a stoichiometric amount or less of nitrosyl chloride in the liquid state at -50 to -10 deg.C under normal pressure to give a nitroso compound of formula I, which is then aminated with a primary or secondary amine to form the indane derivative of formula II.

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