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1. 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.

2. 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.

3. 发明专利

JP2000226397A LIPID A INTERMEDIATE, ITS PRODUCTION AND PRODUCTION OF LIPID A AND ITS DERIVATIVE 失效
公开(公告)号：JP2000226397A
公开(公告)日：2000-08-15
申请号：JP21716699
申请日：1999-07-30
申请人： OTSUKA PHARMA FACTORY INC
发明人： SAKAI YASUHIRO , OIKAWA MASAHITO , KUSUMOTO SHOICHI , OGAWA TOMOHIKO
IPC分类号： C07H11/04 , A61K31/00 , A61K31/70 , A61K31/7024 , A61K31/7028 , A61P37/00 , A61P37/04 , C07H15/10 , C07H15/18
摘要： PROBLEM TO BE SOLVED: To produce a new compound useful as a chemical synthetic intermediate for mass-producing lipid A and its derivative in good yield on an industrial scale. SOLUTION: This compound is represented by formula I (R1 is allyl; R2 is a group reductively eliminable group; R3 is a hydrolyzable group), e.g. a compound represented by formula II (Bzl is benzyl; Troc is 2,2,2- trichloroethoxycarbonyl). The compound represented by formula I is produced by reacting a compound represented by formula III e.g. 1-imino-2,2,2- trichloroethyl 6-O-benzyloxymethyl-2-deoxy-3,4-di-O-benzyl-2-[2,2,2- trichloroethoxycarbonylamino]-D-glucopyranoside} with a compound represented by formula IV e.g. allyl 2-deoxy-3,4-di-O-benzyl-2-[(R)-3-(4- trifluoromethylbenzyloxy)octadecanoylamino]-α-D-glucopyranoside} in an inert solvent.

4. 发明专利

JPH11302177A MEDICINE FOR TREATING NEPHRITIS 失效
公开(公告)号：JPH11302177A
公开(公告)日：1999-11-02
申请号：JP11664598
申请日：1998-04-27
申请人： OTSUKA PHARMA FACTORY INC
发明人： MIYATA KAZUYOSHI , TSUDA YOSHIHIKO , SHOJI YASUO , KUROKI YASUHISA , SAKAI YASUHIRO , MUKAI KIYOSHI , HASHIMOTO KINJI , KORI HIDEAKI
IPC分类号： A61K31/66 , A61P13/02 , A61P15/00
摘要： PROBLEM TO BE SOLVED: To obtain a medicine for treating nephritis, having an action for inhibiting the excretion of urinary protein, scarcely accompanied with side effects such as a hemolytic action and excellent in safety, by compounding a specific phosphate derivative as an active ingredient. SOLUTION: This medicine for treating nephritis contains a phosphate derivative of the formula: R -(A)1 -(O)n -(CH)m -PO(Z1 )Z2 [A is phenylene, thiophenediyl or pyrazinediyl; (1) is 0-1; (m) is 1-4; (n) is 0-1; Z1 and Z2 are simultaneously each OR (R is a lower alkyl), or either of Z1 and Z2 is a lower alkoxy and the other is phenyl; R is a (substituted) lower alkylcarbonyl, a group of formula I (R is H or a halogen; D is O or S), a group of formula II (E is carbonyl or methylene), a group of formula III (R is a halogen, a lower alkoxy or the like), a (substituted) quinolyl, a (substituted) quinazolinyl or the like] as an active ingredient. The medicine is preferably administered at a daily dose of about 0.05-80 mg per kg of the body weight of an adult as the active ingredient compound.

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

AU6755496A Process for producing quinazolin-4-one derivatives 未知
公开(公告)号：AU6755496A
公开(公告)日：1997-03-19
申请号：AU6755496
申请日：1996-08-26
申请人： OTSUKA PHARMA FACTORY INC
发明人： MIYATA KAZUYOSHI , KUROGI YASUHISA , SAKAI YASUHIRO , TSUDA YOSHIHIKO
IPC分类号： C07D239/90 , C07D239/91 , C07F9/6512
摘要： PCT No. PCT/JP96/02388 Sec. 371 Date Feb. 25, 1998 Sec. 102(e) Date Feb. 25, 1998 PCT Filed Aug. 26, 1996 PCT Pub. No. WO97/08153 PCT Pub. Date Mar. 6, 1997The present invention provides a novel process for preparing a series of quinazolin-4-one derivatives in high yields with reduced amounts of byproducts, the process comprising reacting, in the presence of a base, a trialkylsilyl halide with a compound represented by the formula wherein; R5 is a phenyl group which may have 1 to 3 substituents each selected from a lower alkyl group, a lower alkoxy group or a halogen atom, a lower alkyl group, a phenyl-lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, a lower alkenyl group, a lower alkoxy-lower alkyl group or a lower alkynyl group; R6 is a lower alkyl group, a halogen-substituted lower alkyl group, a lower alkoxycarbonyl group or a phenyl group which may have, as a substituent, a lower alkyl group or a group of the formula wherein A is an oxygen atom or a single bond, Z is a lower alkylene group, R7 is a lower alkyl group and R8 is a lower alkoxy group, a phenyl group or a phenyl-lower alkoxy group which may have a halogen atom on the phenyl ring; to produce the quinazolin-4-one derivatives which is valuable as pharmaceuticals or intermediates for synthesis thereof and represented by the formula wherein R1,R2, R3, R4, R5, and R6 are as defined above.

7. 发明专利

AU1173497A Phosphonic acid diester derivatives 未知
公开(公告)号：AU1173497A
公开(公告)日：1997-07-28
申请号：AU1173497
申请日：1996-12-24
申请人： OTSUKA PHARMA FACTORY INC
发明人： MIYATA KAZUYOSHI , SAKAI YASUHIRO , SHOJI YASUO , TSUDA YOSHIHIKO , INOUE YASUHIDE , SATO KEIGO , MIKI SHINYA
IPC分类号： C07F9/6509 , C07F9/6539 , C07F9/6553 , C07F9/6558 , C07F9/6561 , A61K31/67 , A61K31/675
摘要： Phosphonic acid diester derivatives represented by general formula (1) which are useful as a remedy for hyperlipidemia and diabetes, an antitumour agent and a preventive or remedy for cataract, wherein R represents cycloalkyl, etc.; R represents hydrogen, phenyl or lower alkyl; R and R represent each lower alkyl; and A represents a heterocycle selected from among pyrazine, thiophene and phenyl-substituted thiazole rings.

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