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
Patent number: 5334607
Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.
Type:
Grant
Filed:
May 28, 1992
Date of Patent:
August 2, 1994
Assignee:
BASF Aktiengesellschaft
Inventors:
Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich