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1. 发明专利

JPH10158249A QUINAZOLINONE DERIVATIVE 失效
公开(公告)号：JPH10158249A
公开(公告)日：1998-06-16
申请号：JP31634796
申请日：1996-11-27
申请人： OTSUKA PHARMA FACTORY INC
发明人： KAWAMURA KENICHI , KUROKI YASUHISA
IPC分类号： C07D239/90 , A61K31/505 , A61K31/517 , A61K31/535 , A61P3/08 , A61P3/10
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound useful as medicines, especially a hypoglycemic agent for preventing and treating diabetes. SOLUTION: A compound of formula I (R is a lower alkyl; R is a halogen; R is a lower alkyl, a lower alkoxy, etc.; X is a lower alkylene; Y is S, sulfinyl, etc.,), e.g. 3-[7-chloro-3-methyl-4(3H)-quinazolinon-2-yl]propionic acid. The compound of formula I is produced by reacting a compound of formula II with a compound of formula III (R is a lower alkoxy; Z is a halogen) in an amount of the same mole or larger mole at or than that of the compound of formula II in the presence of an excessive amount of an acidremoving agent such as pyridine at 0 deg.C to a room temperature for approximately 0.5-50hr and subsequently subjecting the obtained compound of formula IV to a cyclization reaction with a trialkylsilane halide in the presence of a base in an inert solvent. The base and the trialkylsilane halide are used in amounts of generally 1 equivalent to excessive equivalent, preferably approximately 3-20 equivalent, respectively. The reaction is carried out usually at 0-100 deg.C for approximately 0.5-20hr.

2. 发明专利

JPH11302291A PHOSPHONIC DIESTER DERIVATIVE 失效
公开(公告)号：JPH11302291A
公开(公告)日：1999-11-02
申请号：JP11553698
申请日：1998-04-24
申请人： OTSUKA PHARMA FACTORY INC
发明人： SAKAI YASUHIRO , MIYATA KAZUYOSHI , KAWAMURA KENICHI , TSUDA YOSHIHIKO , INOUE YASUHIDE
IPC分类号： A61K31/66 , A61K31/675 , A61P3/08 , A61P3/10 , A61P31/10 , C07F9/40 , C07F9/58 , C07F9/6509
摘要： PROBLEM TO BE SOLVED: To obtain a specific new phosphonic diester derivative bearing substituted phenyl or substituted nitrogen-contg. heterocyclic group, having hypoglycemic action, therefore useful as e.g. an antidiabetic agent. SOLUTION: This new phosphonic diester derivative is shown by formula I [R is amino, an N-lower alkylamino, N-(substituted) phenylamino or the like; R and R are each H, a lower alkyl, halogen, lower alkoxy, nitro amino or the like; R is H, a lower alkyl or the like; R and R are each a lower alkyl; X, Y and Z are such that all of them are carbon atoms, or one of them is nitrogen atom and the other two are carbon atoms; Q is a single bond or an alkylene] and useful as e.g. an antidiabetic agent. This compound of formula I is obtained by reaction between an amine compound of formula II and an acid chloride of formula III (W is a halogen; Q' is an alkylene) in an inert solvent in the presence of a deacidifying agent.

3. 发明专利

JPH10167964A COUMARIN DERIVATIVE-CONTAINING MEDICINAL COMPOSITION 失效
公开(公告)号：JPH10167964A
公开(公告)日：1998-06-23
申请号：JP32550396
申请日：1996-12-05
申请人： OTSUKA PHARMA FACTORY INC
发明人： SHIBUYA NAOMASA , KAWAMURA KENICHI , HASHIMOTO KINJI , INOUE YASUHIDE , SATO KEIGO , MIKI SHINYA
IPC分类号： C07D311/56 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/385 , A61K31/40 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/54 , A61P3/08 , A61P3/10 , C07D409/04 , C07D411/04 , C07D417/04
摘要： PROBLEM TO BE SOLVED: To obtain the subject composition that contains a novel coumarin derivative as an active ingredient and is useful for treatment or prevention of diabetes as a hypoglycemic. SOLUTION: The objective composition contains, as an active ingredient, about 1-70wt.% of a coumarin derivative of formula I (R is a hydrogen atom, an alkyl, an alkoxy; R is an alkyl, a phenylalkyl, a carboxyalkyl, an alkoxycarbonylalkyl), typically 3-[methyl(diethyl-phosphoromethyl) sulfonio]coumarin-4-olate. The coumarin derivative of formula I is prepared, for example, by allowing a compound of formula II to react with iodobenzene diacetate in the presence of an alkali, for example, sodium carbonate in a solvent (water), then allowing the resultant compound of formula III to react with a thioether derivative of the formula: R -S-R in the presence of an acidic catalyst (acetic acid) in a solvent (methanol).

4. 发明专利

JPH09124615A QUINAZOLINONE DERIVATIVE 失效
公开(公告)号：JPH09124615A
公开(公告)日：1997-05-13
申请号：JP28522795
申请日：1995-11-01
申请人： OTSUKA PHARMA FACTORY INC
发明人： KUROKI YASUHISA , KAWAMURA KENICHI , SAKAI YASUHIRO , HASHIMOTO KINJI , MIYATA KAZUYOSHI , SHIBUYA NAOMASA , INOUE YASUHIDE , SATO KEIGO , MIKI SHINYA
IPC分类号： C07D239/91 , A61K31/505 , A61K31/517 , A61P3/08 , A61P3/10 , C07D401/10 , C07D403/10 , C07D409/10 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To obtain a new equinazolinone derivative as a therapeutic agent for diabetic, having hypoglycemic action. SOLUTION: A compound is shown by formula I [R is H or a halogen; R is a lower alkyl; (m) is 0 or 1; R is a bis(lower alkoxycarbonyl)methyl, etc., when m=0 and R is a group of the formula S-(O)1 -R (R is a lower alkyl, etc.; (1) is 0, 1 or 2)] such as 7-chloro-2-(4-ethylthiomethylphenyl)-3-methyl-4(3H)- quinazolinone. The compound of formula II is halogenated and reacted with a compound of the formula R -H (R is SR ) to obtain a compound of formula I, in which, for example, (m) is 1 and (1) is 0.

5. 发明专利

JPH09286792A PHOSPHONIC DIESTER DERIVATIVE 失效
公开(公告)号：JPH09286792A
公开(公告)日：1997-11-04
申请号：JP3361697
申请日：1997-02-18
申请人： OTSUKA PHARMA FACTORY INC
发明人： SAKAI YASUHIRO , KUROKI YASUHISA , MIYATA KAZUYOSHI , TSUDA YOSHIHIKO , SHIBUYA NAOMASA , KAWAMURA KENICHI , INOUE YASUHIDE , SATO KEIGO , MIKI SHINYA
IPC分类号： A61K31/66 , A61P3/08 , A61P3/10 , C07F9/6512 , C07F9/6558
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound derivative, which is a specific phosphonic diester derivative having the quinazolinone skeleton, having hypoglycemic actions and capable of manifesting excellent efficacies with a low dose and useful as an active ingredient, etc., of a medicine such as a therapeutic agent for diabetes. SOLUTION: This new phosphonic diester derivative is represented by formula I (R to R are each H, a halogen, a lower alkyl, a lower alkoxy, amino, nitro, etc.; R is a lower alkyl, a lower alkenyl, phenyl, etc.; R and R are each a lower alkyl; A is a thiophene ring, a pyrazine ring, a lower alkylene or a single bond) and is capable of manifesting hypoglycemic actions and excellent efficacies with a low dose and useful as a therapeutic agent, etc., for diabetes. This compound is obtained by reacting 2-amino-N-substituted benzamides represented by formula II with a dialkoxyphosphorylcarboxylic acid halide represented by formula III (X is a halogen) in the presence of a deacidifying agent in a solvent and then carrying out the cyclizing reaction of the reactional product.

6. 发明专利

JPH0952891A COUMARIN DERIVATIVE 失效
公开(公告)号：JPH0952891A
公开(公告)日：1997-02-25
申请号：JP12549896
申请日：1996-05-21
申请人： OTSUKA PHARMA FACTORY INC
发明人： SHIBUYA NAOMASA , KAWAMURA KENICHI , HASHIMOTO KINJI
IPC分类号： C07D311/56 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/395 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/54 , A61K31/665 , A61P3/08 , A61P3/10 , C07D407/04 , C07D417/04 , C07F9/655
摘要： PROBLEM TO BE SOLVED: To obtain the subject new derivative having excellent hypoglycemic action and useful for treating and preventing, etc., of diabetes mellitus as a hypoglycemic agent, etc., which is a specific coumarin derivative having an intrasulfonium salt. SOLUTION: This new coumarin derivative is expressed by formula I [R is H, a lower alkyl, a lower alkoxy or a halogen; R is a (substituted) lower alkyl, a cycloalkyl or a (substituted) phenyl, etc.; R is a di-lower alkylphosphoro lower alkyl, a carboxy lower alkyl, a (substituted) lower alkyl, a (substituted) phenyl, etc.; R and R may mutually bond to form 2H-1,4-benzothiazin-3(4H)-one ring, etc., together with S bonded to them]. The compound has excellent hypoglycemic action and is useful for treatment and prevention of diabetes, etc., as a hypoglycemic agent. The compound is obtained by reacting 4- hydroxycoumarin of formula II with iodobenzene diacetate and reacting the product with thioethers of the formula: R -S-R .

7. 发明专利

JPH07304775A NAPHTHYRIDINE AND PYRIDOPYRAZINE DERIVATIVE 失效
公开(公告)号：JPH07304775A
公开(公告)日：1995-11-21
申请号：JP16220894
申请日：1994-07-14
申请人： OTSUKA PHARMA FACTORY INC
发明人： SHIBUYA NAOMASA , KAWAMURA KENICHI , HASHIMOTO KINJI
IPC分类号： C07D471/04 , A61K31/395 , A61K31/435 , A61K31/495 , A61P1/16 , A61P11/00 , A61P11/08 , A61P13/02 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08
摘要： PURPOSE:To provide a new compound having anti-inflammatory action, immunomodulating action, analgesic action, antipyretic action, antiallergic action, antidepressive action, etc. CONSTITUTION:This naphthyridine and pyridopyrazine derivative is a compound of formula I [R is H, a lower alkyl or a (substituted)phenyl; R is H, a lower alkanoyl or an electron pair '-'; R is S(O)nR (R is a lower alkyl, or phenyl,; (n) is 0 or 1) when R is H or a lower alkanoyl and R is group of formula II (Ph is phenyl), etc., when R is electron pair '-'; X is CH or N], e.g. 1-(3- chlorophenyl)-4-hydroxy-3-methylthio-1,8-naphthyridin-2(1H)one. The compound of formula I can be produced by reacting a compound of formula III with an alkyl-thioacetic acid ester derivative of formula R -S-CH2COOR' (R and R' each is a lower alkyl) in a solvent such as benzene in the presence of a base (e.g. potassium t-butoxide).

8. 发明专利

JPH07126268A 1,8-NAPHTHYRIDINE DERIVATIVE 失效
公开(公告)号：JPH07126268A
公开(公告)日：1995-05-16
申请号：JP27250793
申请日：1993-10-29
申请人： OTSUKA PHARMA FACTORY INC
发明人： SHIBUYA NAOMASA , INOUE MAKOTO , KAWAMURA KENICHI , HASHIMOTO KINJI , SUGIMOTO YUKIO , HAGI AKIFUMI , KAMISAKO TAKUJI
IPC分类号： C07D471/04 , A61K31/435 , A61K31/44 , A61K31/535 , A61P25/04 , A61P29/00 , A61P37/00
摘要： PURPOSE:To obtain a new compound, having excellent antiinflammatory, immunomodulating, analgesic, antipyretic actions, etc., and useful for treating and preventing chronic articular rheumatism, nephritis, psoriasis, systemic lupus erythematosus, lumbago, etc. CONSTITUTION:This compound is expressed by formula I [R is piperidino, morpholino, etc.; R is expressed by formula II or III (R is H or hydroxy; R is H, pyridyl, etc.; R is a lower alkyl, phenyl-lower alkyl, etc.); R is a lower alkyl or phenyl; R is H or a lower alkyl], e.g. 1-(3-chlorophenyl)-4-(N,N- dimethylamino)-3-(1-hydroxyethyl)-1,8-naphthyridin-2(1H)-one. The compound is obtained by carrying out the Vilsmeier reaction of, e.g. a compound expressed by formula TV with an N,N-disubstituted formamide and an oxyhalide, then reacting the resultant compound with a compound expressed by the formula R -H (R is amino, morpholino, etc.) and subsequently reacting the resultant product with a Grignard reagent expressed by the formula R -MgBr (R is pyridyl, phenyl, etc.).

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