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1. 发明授权

KR810001107B1 PROCESS FOR PREPARING CARBOSTYRIL DERIVATIVES 失效
公开(公告)号：KR810001107B1
公开(公告)日：1981-09-18
申请号：KR770000642
申请日：1977-03-17
申请人： OTSUKA PHARMA CO LTD
发明人： TONE HITOSHI , TOMINAGA MICHIAKI , NAKAKAWA KAZUYUKI
IPC分类号： C07D413/12
摘要： Carbostyril derivs. (I; R1 = H, alkyl, phenyl alkyl; R2 = H, alkyl, phenyl alkyl, alkenyl, alkoxyalkyl, hydroxyalkyl, R3,R4 = H, alkyl, cycloalkyl, alkenyl, phenylalkyl, phenoxyalkyl, heterocyclic alkyl; Y = IV, IV'; X = halogen), useful for tratment of bronchial asthma, were prepd. by reacting carbostyril compd. (II) with compd. (III) at 0- 100oC. Thus, 1-methyl-5-(2,3-epoxy propoxy)-8-benzyloxy-3,4-dihydro carbostyril 1.7 g was dissolved in the methanol 20 ml, benzylamine 1.6 ml was added, stirred for 4 hr at 40- 50oC and then evaporated. The residue was rfined and recrystallized to give compd.(I) (m.p. 155-157oC).

2. 发明公开

EP1114812A4 PROCESSES FOR THE PREPARATION OF FLUORINATED BENZOIC ACIDS 有权
标题翻译：用于生产氟化苯甲酸
公开(公告)号：EP1114812A4
公开(公告)日：2005-05-04
申请号：EP99943255
申请日：1999-09-09
申请人： OTSUKA PHARMA CO LTD
发明人： HASHIMOTO AKIHIRO , MATSUDA SATOSHI , TAI KUNINORI , TONE HITOSHI , NISHI TAKAO , MINAMIKAWA JUN-ICHI , TOMINAGA MICHIAKI
IPC分类号： C07C51/353 , C07C51/377 , C07C51/347 , C07C63/10 , C07C63/70
CPC分类号： C07C51/353 , C07C51/377 , C07C63/70
摘要： Industrially advantageous processes for the preparation of fluorinated benzoic acids represented by general formula (2): (wherein R1 is halogeno; and R2 is lower alkyl) which comprise alkylating a fluorinated benzoic acid represented by general formula (3) (wherein R1 is as defined above), or reducing a fluorinated benzoic acid represented by general formula (4): (wherein R?1 and R2¿ are each as defined above).

3. 发明专利

JP2523092B2 失效
公开(公告)号：JP2523092B2
公开(公告)日：1996-08-07
申请号：JP23886594
申请日：1994-10-03
申请人： OTSUKA PHARMA CO LTD
发明人： UEDA TAKASHI , MYAMOTO HISASHI , YAMASHITA HIROSHI , TONE HITOSHI
IPC分类号： C07D215/56 , A01N37/10 , A01N43/32 , C07C25/02 , C07C69/76 , C07C211/52 , C07C251/16 , C07C323/29

4. 发明专利

JPH0643419B2 失效
公开(公告)号：JPH0643419B2
公开(公告)日：1994-06-08
申请号：JP2193790
申请日：1990-01-30
申请人： OTSUKA PHARMA CO LTD
发明人： KITA YASUYUKI , AKAI SHUJI , FUJIOKA HIROMICHI , TAMURA YASUMITSU , TONE HITOSHI
IPC分类号： C07D403/06

5. 发明专利

JPH06135946A PYRAZINE DERIVATIVE 失效
公开(公告)号：JPH06135946A
公开(公告)日：1994-05-17
申请号：JP33342892
申请日：1992-10-30
申请人： OTSUKA PHARMA CO LTD
发明人： TONE HITOSHI , TAMURA KATSUMI , SATO HIDEAKI , MORISUE MASATOSHI , MIYAZAKI TOSHIKI , NAKANO YOSHIMASA
IPC分类号： A61K31/495 , A61P1/16 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P29/00 , C07D241/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： PURPOSE:To obtain a new compound useful for preventing and treating autoimmune disease such as rheumatism, etc., arteriosclerosis, ischemic heart disease, cerebral disorder, nephritis, etc., having inhibitory action superoxide and anti- proteinuria action. CONSTITUTION:A compound of formula I (R is lower alkoxy; B is N O, N; R is lower alkyl ; A is lower alkylene; R is N-containing 5to 13-membered ring monocyclic or heterocyclic residue, X-R', amino, etc.; X is O or S(O)m: (m) is 0-2; R is lower alkyl, phenyl, etc.) such as 3-isobutyl-5-methoxy-6-(1,2,4- triazol-3-yl)thiomethyl-1,2-dihydropyrazin-2-on-4-oxide. The compound of formula I is obtained by reacting a compound of formula II (Y is halogen, lower alkanesulfonyloxy, etc.; R is phenyl lower alkoxy) with a compound of the formula R H (R is phthalimide, etc.) and reducing the reaction product.

6. 发明专利

JPH03135930A BENZENE DERIVATIVE 失效
公开(公告)号：JPH03135930A
公开(公告)日：1991-06-10
申请号：JP21738590
申请日：1990-08-17
申请人： OTSUKA PHARMA CO LTD
发明人： UEDA TAKASHI , MIYAMOTO HISASHI , YAMASHITA HIROSHI , TONE HITOSHI
IPC分类号： C07D295/04 , A61K31/47 , A61K31/535 , A61K31/5375 , A61P31/04 , C07B61/00 , C07C17/00 , C07C25/13 , C07C63/70 , C07C69/738 , C07C69/76 , C07C205/11 , C07C211/52 , C07C227/08 , C07C227/16 , C07C229/34 , C07C229/60 , C07C233/15 , C07C255/50 , C07D215/56 , C07D295/12 , C07D295/14 , C07D295/22 , C07D409/04 , C07D498/06
摘要： PURPOSE:To obtain various intermediates for synthesizing benzoheterocyclic compounds, capable of widely exhibiting excellent antibacterial activity against Gram-positive and Gram-negative bacterial and useful as a remedy for diseases caused by various pathogenic bacteria. CONSTITUTION:Ten kinds of intermediate compounds expressed by formula I [R is cyclopropyl, phenyl, alkyl, etc.; R is H, alkyl or halogen; R is alkyl or halogen; X and X are halogen; R is H, alkyl or formula II (R and R are alkyl)], formula III {R ' is halogen or 5- to 9-membered heterocyclic residue; X is halogen; R is formula IV or V [R is COR or COOR (R is lower alkyl; R is alkyl); R is alkyl; R is alkoxy, etc.]}, formula VI[X is halogen; R is alkyl; R is H or CH2R (R is H or alkyl)], formula VII (X is halo gen; R is halogen or CH2R ; R is H or NO2), etc.

7. 发明专利

JPH0399078A PRODUCTION OF SUBSTANCE NF-1616-904 失效
公开(公告)号：JPH0399078A
公开(公告)日：1991-04-24
申请号：JP2193790
申请日：1990-01-30
申请人： OTSUKA PHARMA CO LTD
发明人： KITA YASUYUKI , AKAI SHUJI , FUJIOKA HIROMICHI , TAMURA YASUMITSU , TONE HITOSHI
IPC分类号： C07D403/06
摘要： PURPOSE:To industrially and advantageously obtain the subject compound useful for preventing and treating renal, hepatic insufficiencies, etc., by cyclizing an indole derivative, then protecting oxo group, subsequently methylating the resultant compound and removing protecting groups in the aforementioned methylated derivative. CONSTITUTION:A compound expressed by formula I (R is H, lower alkoxycarbonyl, lower alkanoyl or benzoyl) is cyclized, preferably in the presence of a condensing agent, such as trimethylsilylethoxyacetylene, to provide an indole derivative expressed by formula II, which is then reacted with a compound expressed by formula III (R is lower alkoxycarbonyl, etc.) in an inert solvent to protect the oxo group. The resultant compound is further reacted with diazomethane is the presence of a catalyst, such as boron tribromide, in a solvent, such as methanol, and methylated. The protecting groups in the methylated indole derivative are subsequently removed by hydrolytic and reduction treatment, etc., and the resultant compound is isolated and purified to afford the objective compound expressed by formula IV.

8. 发明专利

JPS609501B2 失效
公开(公告)号：JPS609501B2
公开(公告)日：1985-03-11
申请号：JP5249876
申请日：1976-05-07
申请人： OTSUKA PHARMA CO LTD
发明人： TOMINAGA MICHIAKI , TONE HITOSHI , NAKAGAWA KAZUYUKI
IPC分类号： C07D215/26 , A61K31/47 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D215/22 , C07D215/32

9. 发明专利

JPS53108978A CARBOSTYRIL DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS53108978A
公开(公告)日：1978-09-22
申请号：JP2404177
申请日：1977-03-04
申请人： OTSUKA PHARMA CO LTD
发明人： TOMINAGA MICHIAKI , TONE HITOSHI , NAKAGAWA KAZUYUKI
IPC分类号： C07D215/26 , A61K31/47 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D215/22
摘要： PURPOSE:Carbostyril derivatives I (R1 is lower alkyl, hydroxyalkyl, carbamoylalkyl, etc.; R2,3 are H, lower alkyl, cycloalkyl, alkoxyalkyl, etc.; the 3-4 bond of carbostyril skelton is single or double bond), or their acid addition salts; e.g. 8-(2-propynyloxy)-5-[3-(t-butylamino)-2-hydroxypropoxy]3,4-dihydrocarb ostyril hydrochloric acid salt.

10. 发明专利

JP2523383B2 失效
公开(公告)号：JP2523383B2
公开(公告)日：1996-08-07
申请号：JP1455190
申请日：1990-01-23
申请人： OTSUKA PHARMA CO LTD
发明人： MATOBA KATSUHIDE , TANIGUCHI YOICHI , NISHITANI SHINJI , HAYAKAWA SATOSHI , KANEYASU TOSHINORI , TONE HITOSHI , SATO SEIJI , SATO HIDEAKI , TAMURA KATSUMI , NAKANO YOSHIMASA
IPC分类号： C12P17/16 , C07D403/06 , C12R1/645

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