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1. 发明专利

JPH05201865A BENZOTHIAZEPINE DERIVATIVE 失效
公开(公告)号：JPH05201865A
公开(公告)日：1993-08-10
申请号：JP28287492
申请日：1992-10-21
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , HARADA HIROSHI , SAKAI KATSUNORI , MATSUNAGA KAZUKI , IWAKI KAZUMI
IPC分类号： A61K31/55 , A61K31/554 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D281/10 , C07D417/12
摘要： PURPOSE:To provide a new compound having a calcium-antagonizing action and useful for treating and preventing transient ischemic diseases, essential hypertension, etc. CONSTITUTION:A compound of formula I [X is >N-A-R , >C(R )R ; A is single bond, polymethylene, -CO-; R , R are H, 1-6C alkyl, phenyl, benzhydryl, etc.; Y is H, halogen, 1-6C alkyl, alkoxy, phenoxy, etc.; Z is H, acyl; n is 2-6], e.g. (2S-cis)-3-acetoxy-5-[3-(4-(2-methoxyphenyl)-1-piperazinyl)propyl]-2,3 -dihydro-2-(4- methoxyphenyl)-8-chloro-1,5-benzothiazepin-4(5H)-one. The compound of formula I is obtained by reacting a compound of formula II with a compound of formula Z2O in the presence of a base (e.g. triethylamine) in a solvent (e.g. dichloromethane).

2. 发明专利

JPH036151B2 失效
公开(公告)号：JPH036151B2
公开(公告)日：1991-01-29
申请号：JP17676382
申请日：1982-10-05
申请人： SHIONOGI & CO
发明人： ADACHI IKUO , YAMAMORI TERUO , UEDA MOTOHIKO , SATO HATSUO
IPC分类号： A61K31/435 , A61P3/00 , A61P7/04 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07C205/56 , C07D231/38 , C07D401/04 , C07D407/04 , C07D471/04

3. 发明专利

JPS59152386A 4,7-dihydroisoxazolo(5,4-b)pyridine derivative and its preparation 失效
标题翻译： 4,7-二氢异恶唑（5,4-B）吡啶衍生物及其制备
公开(公告)号：JPS59152386A
公开(公告)日：1984-08-31
申请号：JP2598183
申请日：1983-02-17
申请人： Shionogi & Co Ltd
发明人： ADACHI IKUO , YAMAMORI TERUO , UEDA MOTOHIKO , TAINAI MASAMI
IPC分类号： C07D498/04 , A61K31/535 , A61P3/00 , A61P3/14
摘要： NEW MATERIAL:The compound of formula I [R
1 is straight chain, branched chain or cyclic alkyl, cyclic alkoxyalkyl, (substituted) phenyl, etc.; R
2 is alkyl or (substituted) phenyl; R
3 is alkyl, straight or branched chain alkoxy, or alkoxyalkoxy; R
4 is methyl or phenyl].
EXAMPLE: Methyl 3-( n-butyl )-6-methyl-4-(3-nitrophenyl)-4, 7-dihydroxazolo-[5.4-b] pyridine-5-carboxylate.
USE: It has calcium antagonistic activity and is useful as a remedy for the diseases of circulatory system such as stenocardia, hypertension, arrhythmia, cerebral blood flow disorder, etc.
PREPARATION: The compound of formula I can be prepared by reacting the compound of formula II with the compound of formula III. The reaction is carried out in a solvent or in the absence of solvent, if necessary in the presence of a catalyst (e.g. sulfuric acid) at room temperature or under heating (at 20W100°C).
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新物质：式I化合物[R 1]为直链，支链或环状烷基，环烷氧基烷基，（取代）苯基等; R 2是烷基或（取代的）苯基; R 3是烷基，直链或支链烷氧基或烷氧基烷氧基; R 4是甲基或苯基]。实施例：3-（正丁基）-6-甲基-4-（3-硝基苯基）-4,7-二氢氮杂 - [5.4-b]吡啶-5-甲酸甲酯。用途：具有钙拮抗作用，可用作心律失常，高血压，心律失常，脑血流紊乱等循环系统疾病的治疗剂。制剂：式Ⅰ化合物可以通过使式 II与式III化合物反应。反应在溶剂中或在不存在溶剂的情况下进行，如果需要，在室温或加热（在20-100℃）下，在催化剂（如硫酸）存在下进行。

4. 发明专利

JP2001139550A NEW USE OF AMIDE COMPOUND 失效
公开(公告)号：JP2001139550A
公开(公告)日：2001-05-22
申请号：JP32641699
申请日：1999-11-17
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , NAGATA KIYOSHI , ISHIZUKA NATSUKI , SAKAI KATSUNORI
IPC分类号： C07D215/38 , A61K31/03 , A61K31/343 , A61K31/352 , A61K31/395 , A61K31/404 , A61K31/4184 , A61K31/421 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/433 , A61K31/436 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/538 , C07D213/56 , C07D213/81 , C07D215/48 , C07D235/30 , C07D241/44 , C07D263/58 , C07D277/82 , C07D285/06 , C07D307/85 , C07D311/58 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D491/052
摘要： PROBLEM TO BE SOLVED: To obtain a compound having excellent apo AI expression accelerating actions and useful as a medicine. SOLUTION: This apo AI expression accelerator comprises a compound represented by the formula (I) (wherein the ring A and Ar1 are each a monocyclic or a bicyclic aromatic hydrocarbon cyclic group or an aromatic heterocyclic group or the like which may respectively have a substituent group; R is hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are each hydrogen, a lower alkyl or the like; (n) is an integer of 0-2; the broken line indicates the presence or absence of a bond; and the wavy line indicates the cis- or trans- geometrical isomerism related to the double bond), its prodrug, a phemaceutically acceptable salt thereof and a hydrate thereof.

5. 发明专利

JPH08176131A PRODUCTION OF OPTICALLY ACTIVE 3-(PARAALKOXYPHENYL) GLYCIDIC ACID ESTER DERIVATIVE 失效
公开(公告)号：JPH08176131A
公开(公告)日：1996-07-09
申请号：JP32215294
申请日：1994-12-26
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , KIYOKAWA MITSUGI , SAKAI KATSUNORI , SHIODA TAKESHI
IPC分类号： C07D303/48 , C07B53/00
摘要： PURPOSE: To efficiently obtain the subject compound useful as a synthetic intermediate for medicines in high yield by reacting an optically active metallic salt of 3-(p-alkoxyphenyl)glycidic acid with alcohols in the presence of a chlorinating agent. CONSTITUTION: A compound of formula I (R is an alkoxy; M is an alkali metal) is reacted with a compound of the formula R OH (R is an alkyl or a substitutive phenyl) in the presence of a chlorinating agent (e.g. thionyl chloride) in a solvent (e.g. THF) in the coexistence of a base (e.g. pyridine) at -20 to +50 deg.C to afford the objective compound of formula II. The reaction is carried out by using 1.1-1.5 equiv. chlorinating agent, 1.5-3 equiv. base and >=1 equiv., preferably 5 equiv. alcohol based on 1 equiv. compound of formula I. The compound of formula II is useful for producing medicines useful in treatment, etc., of hypertension.

6. 发明专利

JPH08119956A PRODUCTION OF OPTICALLY ACTIVE 3-(PARA-ALKOXYPHENYL) GLYCIDIC ACID ESTER DERIVATIVE 失效
公开(公告)号：JPH08119956A
公开(公告)日：1996-05-14
申请号：JP26224294
申请日：1994-10-26
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , KIYOKAWA MITSUGI , SAKAI KATSUNORI , SHIODA TAKESHI
IPC分类号： C07D281/10 , C07B53/00 , C07B61/00 , C07D303/48
摘要： PURPOSE: To obtain an optically active 3-(p-alkoxyphenyl)glycidic acid ester derivative having vasodilator or myocardial protecting actions as an intermediate for synthesizing medicines in high yield. CONSTITUTION: This compound of formula I (R is an alkoxy group; R is an alkyl group, etc.) is obtained by reacting 1 equiv. metallic salt compound of formula II (R is an alkoxy group; M is an alkali metal) with 2 equiv. base such as triethylamine in an ethereal solvent such as tetrahydrofuran in the presence of 1.5 equiv. compound of the formula, R COX (R is a bulky alkyl group, etc., which may be substituted; X is a halogen) such as pivaloyl chloride, preferably at ambient temperature for 1hr and then reacting the resultant reactional product with 1 equiv. compound of the formula, R OH (R is an alkyl group, a cycloalkyl group, etc.), preferably at ambient temperature for 1hr.

7. 发明专利

JPH07112975A 2-AMINOAZOLE DERIVATIVE 失效
公开(公告)号：JPH07112975A
公开(公告)日：1995-05-02
申请号：JP16539294
申请日：1994-07-18
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , KAMATA SUSUMU , SHIODA TAKESHI , FUJIMOTO MASABUMI
IPC分类号： C07D233/88 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61P9/00 , A61P9/12 , A61P43/00 , C07D233/90 , C07D263/48 , C07D277/20 , C07D277/42 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： PURPOSE:To obtain the subject new compound useful for treatment of e.g. hypertension and congestive heart failure as an angiotensin II receptor antagonistic agent or hypotensive agent. CONSTITUTION:A compound of formula I (R is H, an alkyl, alkenyl, cyclic alkyl, aryl or heteroaryl; R and R are each H, a halogen, alkyl, alkenyl, cyclic alkyl, alkoxyl, hydroxycarbonyl, etc.; Y is hydroxycarbonyl or a heteroaryl), e.g. 4-methyl-2-[N-(n-propyl)-N-{[ 2'-(1H-tetrazol-5-yl)biphenyl-4- yl]methyl}amino]thiazole-5-carboxylic acid. The compound of formula I can be obtained by reaction between a compound of formula II (R ' and R ' are the same as R and R , respectively; Z is a halogen, etc.) and a biphenylmethyl- substituted amine of formula III to produce a compound of formula IV followed by substituting the substituted groups in the compound of formula IV.

8. 发明专利

JPH02311479A QUINOLINE DERIVATIVE 失效
公开(公告)号：JPH02311479A
公开(公告)日：1990-12-27
申请号：JP13120289
申请日：1989-05-24
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , SAKAI KATSUNORI , TSUTSUMIUCHI MASAMI , ARITA HITOSHI , MIZUI TAKUJI
IPC分类号： C07D491/052 , A61K31/435 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07D495/04
摘要： NEW MATERIAL:A quinoline derivative shown by formula I (Ar is phenyl or 5 or 6-membered heterocyclic containing N, O and/or S; R and R are H or alkyl or both are bonded to form alkylene; W is O or S; X is H, nitro, halogen or alkoxy; Y is ethylene or vinylene; (n) is 1 to 3 and broken line shown existence or absence of bond). EXAMPLE:2,2-Dimethyl-2H-5-(4-hydroxystyryl)pyrano[3,2-C]quinoline. USE:A drug for treating or preventing transient ischemic disease such as coronary blood vessel infarct or cerebral infarct and arteriosclerosis. PREPARATION:A compound shown by formula II is condensed with a compound shown by formula III to give a compound shown by formula I.

9. 发明专利

JP2001233767A APO AI EXPRESSION STHENIC AGENT 失效
公开(公告)号：JP2001233767A
公开(公告)日：2001-08-28
申请号：JP2000048509
申请日：2000-02-25
申请人： SHIONOGI & CO
发明人： ISHIZUKA NATSUKI , NAGATA KIYOSHI , YAMAMORI TERUO , SAKAI KATSUNORI
IPC分类号： C07D249/06 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4178 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/32 , C07D207/34 , C07D207/50 , C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D249/10 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/22 , C07D277/24 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/135 , C07D307/36 , C07D307/38 , C07D307/42 , C07D307/68 , C07D333/06 , C07D333/12 , C07D333/16 , C07D333/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide excellent apo AI expression sthenic agents since substances capable of activating apo AI are conceived to lead to the creation of entirely new medicaments for blood lipid. abnormalities, arteriosclerotic disorders and other various diseases involving HDL. SOLUTION: The apo AI expression sthenic agents include compounds each shown by the formula (I) (wherein, Y1 is O, S or NR1; Y2, Y3, Y4 and Y5 are CR2 or N, CR3 or N, CR4 or N, and CR5 or N, respectively; R1 is A1, Z-A2, H, a lower alkyl of the like; R2, R3, R4 and R5 are each A1, Z-A2, H, a halogen or the like; at least one arbitrarily selected from Y1, Y2, Y3, Y4 and Y5 has A1, either one of them has Z-A2; Z is a single bond, CR6=CR7 or the like; R6 and R7 are each H or a lower alkyl; and A1 and A2 are each an aryl, heterocyclic group or the like), prodrugs thereof, pharmaceutically acceptable salts thereof and solvates thereof.

10. 发明专利

JP2001131151A NEW USE OF OLEFIN DERIVATIVE 失效
公开(公告)号：JP2001131151A
公开(公告)日：2001-05-15
申请号：JP31231399
申请日：1999-11-02
申请人： SHIONOGI & CO
发明人： YAMAMORI TERUO , NAGATA KIYOSHI , ISHIZUKA NATSUKI , HAYASHI KUNIO
IPC分类号： C07D215/14 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/47 , A61K31/498 , A61P3/06 , A61P9/10 , A61P43/00 , C07D213/06 , C07D213/53 , C07D241/42 , C07D401/06 , C07D405/06 , C07D409/06 , C07D417/06
摘要： PROBLEM TO BE SOLVED: To provide a compound having an excellent apolipoprotein AI expression-promoting action. SOLUTION: This apoAI expression-promoting agent containing a compound represented by formula (I) [Ar1 and Ar2 are each phenyl, naphthyl, an aromatic heterocyclic group or the like which may have one or more substituents; X is N=CZ2, CY2=CZ2, CY2Y3-CHZ2, S, O or the like; Y1, Y2, Y3, Z1 and Z2 are each H, a halogen, a lower alkyl, phenyl or the like, provided that Z1 and Z2 may each independently a bonding group to form a condensed ring together with Ar1 or Ar2; (m) is 0 or 1; (n) is 0 to 2], a prodrug thereof, pharmaceutically acceptable salts thereof or hydrates thereof is provided.

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