Patent number: 6222034
Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine compound of formula I
wherein
R1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,
R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,
A is NH or oxygen,
B is hydrogen or methyl,
C is hydrogen, methyl or hydroxyl,
X is nitrogen,
Y is CH2, CH2—C2, CH2—C2—CH2 or CH2—CH,
Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, and
n is 2, 3 or 4,
or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.
Type:
Grant
Filed:
March 10, 1999
Date of Patent:
April 24, 2001
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerd Steiner, Wilfried Lubisch, Alfred Bach, Franz Emling, Karsten Wicke, Hans-Jürgen Teschendorf, Berthold Behl, Sharon Cheetham, Frank Kerrrigan
Patent number: 6159962
Abstract: 3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which may be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, and may contain 1 nitrogen atom, or to a 5- or 6-membered ring, which may contain 1-2 oxygen atoms,A is NH or an oxygen atom,Y is CH.sub.2, CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --CH.sub.2 or CH.sub.
Type:
Grant
Filed:
December 6, 1999
Date of Patent:
December 12, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerd Steiner, Uta Dullweber, Dorothea Starck, Alfred Bach, Karsten Wicke, Hans-Jurgen Teschendorf, Francisco-Javier Garcia-Ladona, Franz Emling
Patent number: 6159981
Abstract: 3-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl group, an acetyl group, a phenylalkyl C.sub.1 -C.sub.4 radical, the aromatic system being unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen,R.sup.2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
December 12, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerd Steiner, Uta Dullweber, Dorothea Starck, Alfred Bach, Karsten Wicke, Hans-Jurgen Teschendorf, Francisco-Javier Garcia-Ladona, Franz Emling