公开(公告)号：JPS5965076A

公开(公告)日：1984-04-13

申请号：JP17395082

申请日：1982-10-05

Applicant: Kowa Co

Inventor： SHIRATO SHIYOUZOU ,  ONOKI KAZUHIRO ,  SATOU SEIICHI ,  ISHIHAMA HIROSHI

IPC: A61K31/47 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D215/20 ,  C07D215/26 ,  C07D215/32 ,  C07D215/48 ,  C07D215/56 ,  C07D407/12

CPC classification number: C07D407/12 ,  C07D215/20 ,  C07D215/26 ,  C07D215/32 ,  C07D215/48 ,  C07D215/56

Abstract: NEW MATERIAL:A quinoline derivative shown by the formula I [ring Q is group shown by the formula II, or formula III (R' is H, or lower alkoxycarbonyl); A is direct bond, or CONH; n is integer of 1W4; R is H, or CF
3 ].
EXAMPLE: 4-[ ( 2-Hydroxy-3-isopropylamino )propyloxy ]-N-( nitroxypropyl )quin- oline-2-carboxamide.
USE: A drug useful as an anti-angina pectoris, hypotensive, improver for cerebral circulation, and antiarrhythmic agent having hypotensive action, vasodilating action, β-blocking action, and blood flow increasing action.
PROCESS: A compound shown by the formula IV is reacted with isopropylamine, or a compound shown by the formula V is esterified with nitric acid to give a compound shown by the formula I . When the ring Q is tetrahydroxycarbonyl group, etc., a nucleus nitrogen atom is preferably protected with a lower alkoxycarbonyl group or benzyloxycarbonyl group.
COPYRIGHT: (C)1984,JPO&Japio

Abstract translation: 新物质：由式I表示的喹啉衍生物[环Q为式II所示的基团或式III（R'为H或低级烷氧羰基）; A是直接债券，或CONH; n为1-4的整数; R为H或CF 3]。 实施例：4 - [（2-羟基-3-异丙基氨基）丙氧基] -N-（硝基丙基）喹啉-2-甲酰胺。 用途：可用作抗心绞痛，低血压，脑循环改善剂和具有降血压作用的抗心律失常药物，血管扩张作用，β-阻断作用和血流增加作用的药物。 方法：将式IV化合物与异丙胺反应，或将式V化合物用硝酸酯化，得到式I所示的化合物。 当环Q为四羟基羰基等时，核氮原子优选用低级烷氧羰基或苄氧羰基保护。

公开(公告)号：JPS53141275A

公开(公告)日：1978-12-08

申请号：JP5597477

申请日：1977-05-17

Applicant: KOWA CO

Inventor： SATOU SEIICHI ,  NAGAKURA MASAHIKO

IPC: C07D213/80 ,  A61K31/4418 ,  A61K31/455 ,  A61P29/00 ,  A61P37/08 ,  C07D213/02

公开(公告)号：JPS5295659A

公开(公告)日：1977-08-11

申请号：JP1087376

申请日：1976-02-05

Applicant: KOWA CO

Inventor： NAKAMURA KOUJI ,  OOTAKI HARUO ,  SHIMIZU NOBORU ,  YAMAMOTO YUTAKA ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI

IPC: C07D209/44 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P9/00 ,  A61P43/00 ,  C07D405/06

公开(公告)号：JPS577481A

公开(公告)日：1982-01-14

申请号：JP8084180

申请日：1980-06-17

Applicant: KOWA CO

Inventor： SHIRATO SHIYOUZOU ,  SHIMIZU NOBORU ,  SHIGIYOU HIROTAKA ,  KIYOUTANI YOSHINORI ,  KUNIEDA HISASHI ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI ,  AKASHI TOSHIHIRO ,  NAGAKURA MASAHIKO ,  SAWADA HISATOSHI ,  UCHIDA YASUYOSHI

IPC: C07D311/20 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61P9/00 ,  C07D311/04 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64

Abstract: NEW MATERIAL:A compound of formula I (P is 3,4-dihydro-2H-1-benzopyran ring; A is direct bond or -O-CH2; B is direct bond, alkylene, etc.; R is H, halogen, lower alkyl,alkoxyl,alkyleneoxy, etc.; R1 and R2 are H, alkyl, hydroxyalkyl, etc.; R3 is H or nitro; m and n are 1 or 2). EXAMPLE:3,4-Dihydro-8-[ (2-hydroxy-3-isopropylamino)propoxy ]-3-nitratomethyl- 2H-1-benzopyran. USE:An antistenocaridiac agent, hypotensive agent, ameliorant of cerebral circulation and antiarrhythmic agent. PROCESS:A compound of formula II (Q is OH, ethoxycarbonyloxy, acetoxy, etc.) is nitrated and converted into an aminoalkanol derivative thereof to give a compound of formula III. The resultant compound is then nitrated at room temperature to 90 deg.C to afford the compound of formula I.

公开(公告)号：JPS56113748A

公开(公告)日：1981-09-07

申请号：JP1543380

申请日：1980-02-13

Applicant: KOWA CO

Inventor： SHIRATO SHIYOUZOU ,  SHIMIZU NOBORU ,  SHIGIYOU HIROTAKA ,  KIYOUTANI YOSHINORI ,  KUNIEDA HISASHI ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI ,  AKASHI TOSHIHIRO ,  NAGAKURA MASAHIKO ,  SAWADA HISATOSHI ,  UCHIDA YASUYOSHI

IPC: A61K31/21 ,  A61K31/135 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/12 ,  A61P25/02 ,  A61P25/28 ,  C07C67/00 ,  C07C203/04 ,  C07C213/00 ,  C07C217/32 ,  C07C217/70 ,  C07C219/16 ,  C07C219/34 ,  C07C225/16 ,  C07C231/00 ,  C07C231/12 ,  C07C235/42 ,  C07C235/46 ,  C07C237/30 ,  C07C301/00 ,  C07C303/40 ,  C07C311/17 ,  C07C311/29 ,  C07C313/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C319/20 ,  C07C323/25 ,  C07D213/30 ,  C07D213/60 ,  C07D213/64 ,  C07D213/69 ,  C07D303/24 ,  C07D303/26 ,  C07D309/12

Abstract: NEW MATERIAL:An aminoethanol derivative of formula I [A is direct bond or -O-CH2-; B is alkylene which is bonded with an aromatic ring through O, S, SO, etc.; Q is C or N; R1 is H or residue of formula II; R2 is (hydroxy)alkyl, halogen, OH, lower acyl, nitro, etc.; (m) is 1 or 2; (n) is 1-3]. EXAMPLE:1-Isopropylamino- 3-[ 3-( 2-nitratoethoxy )phenoxy ]-2- propanol of formula III. USE:Antistenocardia, hypotensor, cerebral circulation improver, and antiarrythmia. PROCESS:The compound of formula I is prepared, e.g. by (1) converting the compound of formula IV (P is OH, acetyl, halogen, etc.) to the aminoalkanol derivative of formula V, and (2) nitrating the compound with fuming nitric acid, etc. pref. at -40 deg.C- room temperture for several minutes to 1hr.

公开(公告)号：JPS5452060A

公开(公告)日：1979-04-24

申请号：JP11515377

申请日：1977-09-27

Applicant: MICROBIAL CHEM RES FOUND ,  KOWA CO

Inventor： KIYOUTANI YOSHINORI ,  YAMAGUCHI TAKASHI ,  SATOU SEIICHI ,  NAGAKURA MASAHIKO ,  MORI TOSHITO ,  UMEZAWA HAMAO ,  UMEZAWA SUMIO

IPC: C07H15/234 ,  C07H1/00 ,  C07H15/22

Abstract: PURPOSE:To prepare tobramycin by condensing a lividamine deeivative having a sulfoxy group at 6' position with a hexopyranose derivative, converting the sulfonyloxy group to azide group, reducing the azide group to amino group, and eliminating the protecting group. CONSTITUTION:Tobramycin III is prepared by (1) condensing a lividamine derivative I [R is sulfonyloxy of formula -OSO2R (R is alkyl, aralkyl, aryl); Y' is an OH-protecting group; A, B are H or amino-protecting group; or A and B together form a divalent amino-protectng group] with a hexopyranose derivative II (X is halogen; Y, A', B' are same to the definitions of Y' A, B), (2) converting the sulfonyloxy group at 6' positin to azide group, and (3) reducing the azide group to amino group. The compound III can be also derived from a lividamine derivative having azidized 6' positin. Both of the compounds of I and II are novel.

公开(公告)号：JPS52105138A

公开(公告)日：1977-09-03

申请号：JP2002876

申请日：1976-02-27

Applicant: KOWA CO

Inventor： SAWADA NAOTOSHI ,  OOTA TOMIO ,  KIYOUTANI YOSHINORI ,  KUNIEDA EI ,  SATOU SEIICHI ,  NAGAKURA MASAHIKO

IPC: A61K31/135 ,  A61K31/17 ,  A61K31/18 ,  A61P9/00 ,  A61P11/00 ,  A61P11/08 ,  A61P25/02 ,  C07C67/00 ,  C07C213/00 ,  C07C215/30 ,  C07C215/60 ,  C07C301/00 ,  C07C311/08

公开(公告)号：JPS5233608A

公开(公告)日：1977-03-14

申请号：JP10945075

申请日：1975-09-11

Applicant: KOWA CO

Inventor： NAKAMURA KOUJI ,  YAMAMOTO YUTAKA ,  SHIMIZU NOBORU ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI

IPC: C07D295/08 ,  A61K31/13 ,  A61K31/215 ,  A61K31/22 ,  A61K31/235 ,  A61K31/245 ,  A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/455 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P25/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/10 ,  C07C219/04 ,  C07D209/44 ,  C07D213/79 ,  C07D215/14 ,  C07D217/02 ,  C07D317/28 ,  C07D401/14

Abstract: PURPOSE:Central nervous system pharmceuticals having the actions of anticataplexis and acclimatization.

公开(公告)号：JPS57167981A

公开(公告)日：1982-10-16

申请号：JP5167481

申请日：1981-04-08

Applicant: KOWA CO

Inventor： SHIRATO SHIYOUZOU ,  SHIMIZU NOBORU ,  SHIGIYOU HIROTAKA ,  KIYOUTANI YOSHINORI ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI ,  AKASHI TOSHIHIRO

IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D311/04 ,  C07D407/12

Abstract: NEW MATERIAL:A benzopyran derivative shown by the formulaI(R is H, halogen, OH, NO2, lower alkyl or lower alkoxy which may have a substitutent group, lower acyl, carbamoyl, aryloxy, lower alkoxycarbonyloxy, lower acyloxy, haloacyloxy, etc.; R is H, lower alkyl, lower alkoxy, OH, lower acyl; A is direct bond, 1-7C alkylene, 1-7C alkylene which is linked to benzopyran ring thrugh O or CONH; m, n, and p are 1 or 2). EXAMPLE:3,4-Dihydro-8-ethoxycarbonyloxy-3-nitratomethyl-2H-1-benzopyran. USE:An antihypertensive and vasodilator(anti-angina pectoris, improver for peripheral circulation). PROCESS:The substituent group Q of a compound shown by the formula II (Q is OH, halogen) is esterified with nitric acid, to give a compound shown by the formulaI.

公开(公告)号：JPS52133913A

公开(公告)日：1977-11-09

申请号：JP4845976

申请日：1976-04-30

Applicant: KOWA CO

Inventor： NAKAMURA KOUJI ,  YAMAMOTO YUTAKA ,  SHIMIZU NOBORU ,  KAWAMURA KIYOSHI ,  SATOU SEIICHI

IPC: A61K31/13 ,  A61K31/135 ,  A61K31/215 ,  A61K31/22 ,  A61K31/235 ,  A61K31/245 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/445 ,  A61K31/47 ,  A61K31/472 ,  A61K31/535 ,  A61K31/55 ,  A61P21/02 ,  A61P25/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/10 ,  C07C219/02 ,  C07C219/28 ,  C07D209/44 ,  C07D217/02 ,  C07D295/08