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1. (WO1997044326) ARYL PYRIMIDINE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/1997/044326 International Application No.: PCT/EP1997/002454
Publication Date: 27.11.1997 International Filing Date: 14.05.1997
Chapter 2 Demand Filed: 28.11.1997
IPC:
C07D 239/42 (2006.01) ,C07D 239/46 (2006.01) ,C07D 239/48 (2006.01) ,C07D 401/04 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/04 (2006.01) ,C07D 405/04 (2006.01) ,C07D 405/12 (2006.01) ,C07D 409/04 (2006.01) ,C07D 413/04 (2006.01) ,C07D 473/32 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
42
One nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
48
Two nitrogen atoms
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
04
directly linked by a ring-member-to-ring- member bond
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
04
directly linked by a ring-member-to-ring- member bond
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
04
directly linked by a ring-member-to-ring- member bond
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
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32
Nitrogen atom
Applicants:
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basle, CH
Inventors:
BERGER, Jacob; US
FLIPPIN, Lee, Allen; US
GREENHOUSE, Robert; US
JAIME-FIGUEROA, Saul; US
LIU, Yanzhou; US
MILLER, Aubry, Kern; US
PUTMAN, David, George; US
WEINHARDT, Klaus, Kurt; US
ZHAO, Shu-Hai; US
Agent:
BRAUN, Axel; Grenzacherstrasse 124 CH-4070 Basle, CH
Priority Data:
60/018,21823.05.1996US
60/040,37710.03.1997US
Title (EN) ARYL PYRIMIDINE DERIVATIVES
(FR) DERIVES D'ARYL PYRIMIDINE
Abstract:
(EN) The present invention is directed to pyrimidine derivatives, and pharmaceutically acceptable salts and $i(N)-oxides thereof, which exhibit useful pharmacological properties, in particular use as selective 5HT2B-antagonists, their preparation, pharmaceutical compositions comprising them and their use in the treatment of various diseases, especially migraine. The invention is also directed to formulations and methods for treatment.
(FR) Cette invention a trait à des dérivés d'aryl pyrimidine ainsi qu'à leurs sels et à leurs $i(N)-oxydes, acceptables d'un point de vue pharmaceutique. Ces substances, qui font montre d'utiles propriétés pharmacologiques, sont notamment efficaces comme antagonistes sélectifs de 5HT2B. L'invention a également trait à la préparation de ces substances, à des compositions pharmaceutiques les contenant, ainsi qu'à leur utilisation dans le traitement de troubles divers, de la migraine notamment. Elle concerne, de surcroît, des formulations et des méthodes thérapeutiques.
Designated States: AU, BR, CA, CN, CZ, HU, IL, JP, KR, MX, NO, NZ, PL, RU, SG, TR, YU
European Patent Office (EPO) (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)