Abstract:
Described are glycosylated, partially glycosylated or unglycosylated polypeptides with the amino-acid sequence given in the sequence protocol and in which up to 10 amino acid groups can be replaced by other, naturally occurring, amino acids. The peptides are suitable for use in treating illnesses.
Abstract:
3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.
Abstract:
The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3': 4,5]-thieno [2,3-d] pyrimidine derivatives can be used as medicamentous forms for diseases where there is redud serotonin concentration and where, within the therapy, the activity of the presnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blocked without seriously affecting any other receptors. Depression is an example for such morbid state. The compounds have formula in which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl, phenylalkyl-C1-C4-residue where the aromatic residue is optionally substituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-, C1-C4-alkoxy-, amino-, cyano- or nitrogroups or is naphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue or phenylcarbamoylalkyl-C2-residue where the phenyl group can be substituted by halogen; R2 optionally is mono-, di- or trisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-, diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinyl or pyrasinyl reside which can optionally be ringed by one benzene ring which optionally can be mono- or disubstituted with halogen atom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-, cyano- or nitrogroup, and optionally can contain one nitrogen atom or be ringed by 5- or 6-member ring which can contain one to two oxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, or alkoxygroup, respectively, where the phenyl residue can be substituted with halogen, methyl, trifluormethyl or methoxygroup. A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where the bond between Y and Z can be double, n has the value of 2, 3 or 4. The invention also relates to physiologically acceptable salts of the above compounds. 6 claims
Abstract:
3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.
Abstract:
A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 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, andn 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.
Abstract:
A 3-substituted 3,4,5,7-tetrahhydropyrrolo[3',4':4,5]-thieno[2,3-d]pyrimidine derivative of the formula I, wherein, R1is a hydrogen atom, a C1-C4 alkyl group, an acetyl group, a phenylalkyl c1-c4 radical where the aromatic ring is unsubstituted or substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxyl, C1-C4 alkoxy, amino, cyano or nitro groups, or is a C1-C3 alkyl carboxylate radical, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4 alkoxy, amino, monoethylamino, dimethylamino, cyano or nitro groups, and may be fused to a benzene nucleus which may be mono or disubstituted by halogen atoms, C1-C4 alkyl, hydroxyl, trifluoromethyl, C1-C4 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 CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, where the linkage between Y and Z may also be a double bond, and n is 2,3 or 4, or a physiologically tolerated salt thereof. These compounds are useful as selective 5HT1B and/or 5HT1A antagonists.
Abstract:
Derivados de tetrahidropiridopirimidinona 3-sustituidos de la fórmula (I)caracterizados porque uno de los radicales X, Y significa CH2 y el otro significa NR1 , R1 significa hidrógeno, (C1-6 ) alquilo ramificado o sin ramificar, CO-(C1-4 )-ALQUILO, CO2 -tBu, CO-arilo y un radical fenilalquilo C1-4 , que a su vez puede estar sustituido en el aromático por F, Cl, Br, Y, C1 -C4 alquilo, C1 -C4 alcoxi, trifluorometilo, hidroxi, amino, ciano o nitro. A Significa (C1 -10 )-alquiteno ramificado o sin ramificar, (C2 -10 )-alquileno lineal o ramificado, que comprende al menos un grupo 2, seleccionado de entre 0, S. NR2 ciclopropilo, CHOH, un enlace doble o triple, R2 significa hidrógeno y C1 -C4 alquilo B significa 4-piperidina, 4-tetrahidro- 1,2,3,6 piridina, 4-piperacina y los compuestos anulares correspondientes, amplios por un grupo metileno, realizándose el enlace entre A y B por vía de un átomo de N, y Ar significa fenilo, que eventualmente está sustituido por (C1-6 )alquilo ramificado o sin ramificar, O-(C1-6 )-alquilo ramificado o sin ramificar, OH, F, Cl, Br, I, trifluorometilo, NR2 2 , CO2 R2 , ciano o fenilo, tetralina, indano, aromáticos de alto grado de condensación como p. ej. naftalina, que eventualmente está sustituida por (C1-4 )-alquilo o O(C1-4 )-alquilo, entraceno o heterociclos aromáticos de 5 ó 6 miembros con 1 a 2 heteroátomos, heteroátomos seleccionados independientemente de entre O y N, y que pueden estar aún fusionados con otros radicales aromáticos, así como sus sales con ácidos fisiológicamente tolerados.
Abstract:
PCT No. PCT/EP98/03230 Sec. 371 Date Dec. 6, 1999 Sec. 102(e) Date Dec. 6, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56792 PCT Pub. Date Dec. 17, 19983-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I where R1 and R2 are a hydrogen atom or a C1-C4-alkyl group, R3 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-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, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-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 CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it being possible for the linkage between Y and Z also to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.
Abstract:
PCT No. PCT/EP98/03231 Sec. 371 Date Dec. 8, 1999 Sec. 102(e) Date Dec. 8, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56793 PCT Pub. Date Dec. 17, 19983-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I where R1 is a hydrogen atom, a C1-C4-alkyl group, an acetyl group, a phenylalkyl C1-C4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-C4-alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-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, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-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 CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.