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公开(公告)号:IN184759B
公开(公告)日:2000-09-23
申请号:IN1259CA1998
申请日:1998-07-20
Applicant: KANEKA CORP
Inventor: UEDA YASUYOSHI , KINOSHITA KOICHI , MOROSHIMA TADASHI , YANAGIDA YOSHIFUMI , FUSE YOSHIHIDE
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).
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22.
公开(公告)号:CA2302832A1
公开(公告)日:2000-02-03
申请号:CA2302832
申请日:1999-07-19
Applicant: KANEKA CORP
Inventor: KINOSHITA KOICHI , MOROSHIMA TADASHI , UEDA YASUYOSHI , FUSE YOSHIHIDE , YANAGIDA YOSHIFUMI
Abstract: A method for crystallizing the maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (Enalapril) from an aqueous liquid with ease in good yield, which comprises mixing an aqueous liquid containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, maleic acid and a base and having a pH of 4 or more with an acid in an amount of the acid sufficient to convert the base to a neutral salt, to thereby crystallize N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline in the form of a maleic acid salt.
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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
Inventor: YOKOTA SHINICHI , YAMAMOTO KOZO , MORIKAWA SOUICHI , FUSE YOSHIHIDE , KITAHARA MIKIO
IPC: C07D405/06 , A61K31/40 , A61K31/445
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.
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公开(公告)号:HU227816B1
公开(公告)日:2012-03-28
申请号:HU0001145
申请日:1998-07-21
Applicant: KANEKA CORP
Inventor: MOROSHIMA TADASHI , UEDA YASUYOSHI , KINOSHITA KOICHI , YANAGIDA YOSHIFUMI , FUSE YOSHIHIDE
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).
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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
Inventor: YOKOTA SHIN-ICHI , YAMAMOTO KOZO , MORIKAWA SOUICHI , FUSE YOSHIHIDE , KITAHARA MIKIO
IPC: A61K31/40 , A61K31/445 , C07D405/06
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.
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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
Inventor: UEDA YASUYOSHI , KINOSHITA KOICHI , MOROSHIMA TADASHI , YANAGIDA YOSHIFUMI , FUSE YOSHIHIDE
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).
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公开(公告)号:DE60008334D1
公开(公告)日:2004-03-25
申请号:DE60008334
申请日:2000-04-14
Applicant: KANEKA CORP
Inventor: KINOSHITA KOICHI , MOROSHIMA TADASHI , YANAGIDA YOSHIFUMI , NAGASHIMA NOBUO , SAKA YASUHIRO , HONDA TATSUYA , FUSE YOSHIHIDE , UEDA YASUYOSHI
IPC: C07C29/147 , C07C31/42 , C07D307/20
Abstract: The application is concerned with a process for producing a 3-hydroxytetrahydrofuran of the formula (3): by cyclizing a 4-halo-1,3-butanediol of the general formula (2): wherein X represents a halogen atom in an aqueous solution, which comprises carrying out the cyclization reaction under weakly acidic to neutral conditions. Furthermore several methods are disclosed for the isolution of highly pure 3-hydroxytetrahydrofuran.
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公开(公告)号:CZ20014121A3
公开(公告)日:2002-10-16
申请号:CZ20014121
申请日:2001-02-16
Applicant: KANEKA CORP
Inventor: SUGAWARA MASANOBU , FUJII AKIO , OKURO KAZUMI , SAKA YASUHIRO , NAGASHIMA NOBUO , INOUE KENJI , TAKEDA TOSHIHIRO , KINOSHITA KOICHI , MOROSHIMA TADASHI , FUSE YOSHIHIDE , UEDA YASUYOSHI
IPC: C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24 , C07C227/04 , C07C227/26 , C07B53/00
Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
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公开(公告)号:HU0201353A2
公开(公告)日:2002-08-28
申请号:HU0201353
申请日:2001-02-16
Applicant: KANEKA CORP
Inventor: FUJII AKIO , FUSE YOSHIHIDE , INOUE KENJI , KINOSHITA KOICHI , MOROSHIMA TADASHI , NAGASHIMA NOBUO , OKURO KAZUMI , SAKA YASUHIRO , SUGAWARA MASANOBU , TAKEDA TOSHIHIRO , UEDA YASUYOSHI
IPC: C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24
Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
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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
Inventor: MOROSHIMA TADASHI , YANAGIDA YOSHIFUMI , FUSE YOSHIHIDE , UEDA YASUYOSHI
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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