Heat shock factor activity inhibitors

    公开(公告)号:AU7933298A

    公开(公告)日:1999-01-19

    申请号:AU7933298

    申请日:1998-06-25

    Applicant: KANEKA CORP

    Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    25.
    发明专利
    未知

    公开(公告)号:DE69831950D1

    公开(公告)日:2006-03-02

    申请号:DE69831950

    申请日:1998-06-25

    Applicant: KANEKA CORP

    Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    26.
    发明专利
    未知

    公开(公告)号:DE69830307D1

    公开(公告)日:2005-06-30

    申请号:DE69830307

    申请日:1998-07-21

    Applicant: KANEKA CORP

    Abstract: Preparation of salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acid derivatives of formula (R1)NH-CH(R2)-CO2H (I) comprises: (a) condensing an amino acid with N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxyanhydride of formula (II), under basic conditions; (b) decarboxylating the condensate under neutral to acidic conditions to give (I); and (c) and converting (I) to its salt. Steps (a), (b) and optionally (c) are carried out in aqueous liquid to inhibit the formation of by-products of formula (III): -N(R1)CH(R2)-C(O)- = e.g. group of formula (i).

    Process for preparing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline

    公开(公告)号:CZ20001897A3

    公开(公告)日:2000-10-11

    申请号:CZ20001897

    申请日:1999-09-22

    Applicant: KANEKA CORP

    Abstract: The process for producing N -(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline in a simple, efficient and industrially advantageous manner, which comprises: the first step of subjecting the N -(1(S)-alkoxycarbonyl-3-phenylpropyl)-N -trifluoroacetyl-L-lysyl -L-proline (1) to alkali hydrolysis in a mixed solution composed of water and a hydrophilic organic solvent using an inorganic base in an amount of n molar equivalents (n >/= 3) per mole of the above compound (1), the second step of neutralizing the hydrolysis product using an inorganic acid in an amount of (n - 1) to n molar equivalents (n >/= 3) and removing the inorganic salt formed by causing the same to precipitate out from a solvent system suited for decreasing the solubility of the inorganic salt, and the third step of causing the compound (2) existing in the mixture after removal of the inorganic salt to crystallize out at the isoelectric point thereof and thereby recovering the compound (2) in the form of crystals while retaining the salts comprising the trifluoroacetic acid-derived organic acid salt in a state dissolved in the mother liquor.

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