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1. (WO1991005549) BENZOHETEROCYCLIC COMPOUNDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/005549 International Application No.: PCT/JP1990/001340
Publication Date: 02.05.1991 International Filing Date: 18.10.1990
IPC:
C07D 215/08 (2006.01) ,C07D 215/12 (2006.01) ,C07D 215/14 (2006.01) ,C07D 215/20 (2006.01) ,C07D 215/233 (2006.01) ,C07D 215/38 (2006.01) ,C07D 215/42 (2006.01) ,C07D 215/54 (2006.01) ,C07D 223/16 (2006.01) ,C07D 225/06 (2006.01) ,C07D 241/42 (2006.01) ,C07D 243/12 (2006.01) ,C07D 243/14 (2006.01) ,C07D 265/36 (2006.01) ,C07D 267/14 (2006.01) ,C07D 279/16 (2006.01) ,C07D 281/10 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 409/12 (2006.01) ,C07D 417/12 (2006.01) ,C07D 491/04 (2006.01) ,C07D 491/10 (2006.01) ,C07D 498/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
04
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
08
with acylated ring nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12
with substituted hydrocarbon radicals attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12
with substituted hydrocarbon radicals attached to ring carbon atoms
14
Radicals substituted by oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Oxygen atoms
22
attached in position 2 or 4
233
only one oxygen atom which is attached in position 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
42
attached in position 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
54
attached in position 3
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
223
Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
14
condensed with carbocyclic rings or ring systems
16
Benzazepines; Hydrogenated benzazepines
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
225
Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
04
condensed with carbocyclic rings or ring systems
06
condensed with one six-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
36
condensed with carbocyclic rings or ring systems
38
with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
40
Benzopyrazines
42
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
243
Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06
having the nitrogen atoms in positions 1 and 4
10
condensed with carbocyclic rings or ring systems
12
1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
243
Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06
having the nitrogen atoms in positions 1 and 4
10
condensed with carbocyclic rings or ring systems
14
1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
34
condensed with carbocyclic rings
36
condensed with one six-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
267
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
02
Seven-membered rings
08
having the hetero atoms in positions 1 and 4
12
condensed with carbocyclic rings or ring systems
14
condensed with one six-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
279
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
10
1,4-Thiazines; Hydrogenated 1,4-thiazines
14
condensed with carbocyclic rings or ring systems
16
condensed with one six-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
281
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
02
Seven-membered rings
04
having the hetero atoms in positions 1 and 4
08
condensed with carbocyclic rings or ring systems
10
condensed with one six-membered ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
OTSUKA PHARMACEUTICAL CO., LTD. [JP/JP]; 9, Kandatsukasa-cho 2-chome Chiyoda-ku Tokyo 101, JP (AllExceptUS)
OGAWA, Hidenori [JP/JP]; JP (UsOnly)
MIYAMOTO, Hisashi [JP/JP]; JP (UsOnly)
KONDO, Kazumi [JP/JP]; JP (UsOnly)
YAMASHITA, Hiroshi [JP/JP]; JP (UsOnly)
NAKAYA, Kenji [JP/JP]; JP (UsOnly)
KOMATSU, Hajime [JP/JP]; JP (UsOnly)
TANAKA, Michinori [JP/JP]; JP (UsOnly)
KORA, Shinya [JP/JP]; JP (UsOnly)
TOMINAGA, Michiaki [JP/JP]; JP (UsOnly)
YABUUCHI, Yoichi [JP/JP]; JP (UsOnly)
Inventors:
OGAWA, Hidenori; JP
MIYAMOTO, Hisashi; JP
KONDO, Kazumi; JP
YAMASHITA, Hiroshi; JP
NAKAYA, Kenji; JP
KOMATSU, Hajime; JP
TANAKA, Michinori; JP
KORA, Shinya; JP
TOMINAGA, Michiaki; JP
YABUUCHI, Yoichi; JP
Agent:
AOYAMA, Tamotsu; Aoyama & Partners IMP Building 3-7, Shiromi 1-chome Chuo-ku, Osaka-shi Osaka 540, JP
Priority Data:
1/27433820.10.1989JP
2/10558020.04.1990JP
2/18185809.07.1990JP
2/6606315.03.1990JP
Title (EN) BENZOHETEROCYCLIC COMPOUNDS
(FR) COMPOSES BENZOHETEROCYCLIQUES
Abstract:
(EN) Novel benzoheterocyclic compounds of formula (I), wherein R1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R3 is a group: -NR4R5 or -CO-NR11R12; R4 is H, optionally substituted benzoyl, alkyl; R5 is a group $g(a) [R16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: -O-A-NR6R7; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenyl-alkanoyl, etc.; R11 is H or alkyl; R12 is cycloalkyl or optionally substituted phenyl; and W is a group: -(CH2)p (p is 3 to 5) or -CH=CH-(CH2)q (q is 1 to 3), the carbon atom of these groups being optionally replaced by 0, S, SO, SO2 or a group: -N(R13)- and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., which have excellent vasopressin antagonistic activies and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
(FR) Nouveaux composés benzohétérocycliques de formule (I), dans laquelle R1 représente H, halogène, alkyle, amino éventuellement substitué, alcoxy; R2 représente H, halogène, alcoxy, phénylalcoxy, OH, alkyle, amino éventuellement substitué, carbamoyle-alcoxy, amino-alcoxy éventuellement substitué, benzoyloxy éventuellement substitué; R3 représente un groupe -NR4R5 ou -CO-NR11R12; R4 est H, benzoyle éventuellement substitué, alkyle; R5 est un groupe $g(a) [dans lequel R16 représente halogène, alkyle éventuellement substitué, OH, alcoxy, alcanoyloxy, alkylthio, alcanoyle, carboxy, alcoxycarbonyle, CN, NO2, amino éventuellement substitué, phényle, cycloalkyle, etc., ou un groupe -O-A-NR6R7; m est compris entre 0 et 3], phényl-alcoxycarbonyle, alcanoyle, phényl-alcanoyle, etc.; R11 représente H ou alkyle; R12 représente cycloalkyle ou phényle éventuellement substitué; et W est un groupe -CH2)p (p étant compris entre 3 et 5) ou -CH=CH-(CH2)q (q étant compris entre 1 et 3), l'atome de carbone de ces groupes étant éventuellement remplacé par 0, S, SO, SO2 ou un groupe -N(R13)-, ces groupes comportant éventuellement de 1 à 3 substituants d'alkyle, alcoxycarbonyle, carboxy, OH, O, alcanoyloxy, etc. Ces composés présentent d'excellentes activités antagonistes de la vasopressine et sont utiles en tant que vasodilateurs, agents hypotensifs, diurétiques et inhibiteurs d'agglutination de plaquettes. On décrit également une composition antagoniste de la vasopressine contenant ce composé en tant qu'ingrédient actif.
Designated States: KR, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0450097US5258510US5559230US5753677KR1019927001160