RU99106781A - 3-REPLACED PYRIDO DERIVATIVES [4 ', 3': 4,5] THIENO [2,3-ALPHA] PYRIMIDINE, THEIR RECEIVING AND APPLICATION - Google Patents

3-REPLACED PYRIDO DERIVATIVES [4 ', 3': 4,5] THIENO [2,3-ALPHA] PYRIMIDINE, THEIR RECEIVING AND APPLICATION

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Publication number
RU99106781A
RU99106781A RU99106781/04A RU99106781A RU99106781A RU 99106781 A RU99106781 A RU 99106781A RU 99106781/04 A RU99106781/04 A RU 99106781/04A RU 99106781 A RU99106781 A RU 99106781A RU 99106781 A RU99106781 A RU 99106781A
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Russia
Prior art keywords
group
carbon atoms
residue
alkyl
atom
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RU99106781/04A
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Russian (ru)
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RU2198888C2 (en
Inventor
Герд ШТАЙНЕР
Вильфрид БИШ
Альфред БАХ
Франц ЭМЛИНГ
Карстен ВИКЕ
Ханс-Юрген ТЕШЕНДОРФ
Бертольд БЕЛЬ
Франк Керриган
Шарон ЧИТХЕМ
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Басф Акциенгезелльшафт
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Priority claimed from DE19636769A external-priority patent/DE19636769A1/en
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Claims (6)

1. 3-Замещенные производные 3,4,5,6,7,8-гексагидропиридо[4', 3':4,5] тиено[2,3-d]-пиримидина формулы I
Figure 00000001

где R1 означает водород, алкил с 1 - 4 атомами углерода, ацетильную или бензоильную группу, фенилалкильный остаток с 1 - 4 атомами углерода в алкильном остатке, причем ароматический фрагмент при необходимости замещается галогеном, алкилом с 1 - 4 атомами углерода, трифторметилом, гидроксильной группой, алкоксигруппой с 1 - 4 атомами углерода, аминогруппой, циангруппой или нитрогруппой, нафтилалкильный остаток с 1 - 3 атомами углерода в алкиле, остаток фенилалканона с 2 - 3 атомами углерода в остатке алкана или фенилкарбамоилалкильный остаток с 2 атомами углерода в алкиле, причем фенильная группа может быть замещена галогеном,
R2 представляет собой при необходимости моно-, ди- или тризамещенную атомами галогена, алкилом с 1 - 4 атомами углерода, трифторметильными, трифторметоксильными, гидроксильными группами, алкоксигруппами с 1 - 4 атомами углерода, аминогруппами, монометиламиногруппами, диметиламино-, циан- или нитрогруппами фенильную, пиридильную, пиримидинильную или пиразинильную группу, которая при необходимости может быть анеллирована с шестичленным ароматическим ядром, которое при необходимости имеет один или два заместителя в виде атомов галогена, алкила с 1 - 4 атомами углерода, гидроксильной группы, трифторметильной группы, алкоксигруппы с 1 - 4 атомами углерода, аминогруппы, циангруппы или нитрогруппы и при необходимости может содержать один атом азота, или с 5- или 6-ти членным кольцом, которое может содержать 1 - 2 атома кислорода, или может быть замещена фенилалкильной группой или фенилалкоксигруппой с 1 - 2 атомами углерода в алкильном остатке, причем фенильный остаток может быть замещен галогеном, метильной группой, трифторметильной группой или метоксигруппой.1. 3-Substituted derivatives of 3,4,5,6,7,8-hexahydropyrido [4 ', 3': 4,5] thieno [2,3-d] pyrimidine of formula I
Figure 00000001

where R 1 means hydrogen, alkyl with 1-4 carbon atoms, acetyl or benzoyl group, phenylalkyl residue with 1-4 carbon atoms in the alkyl residue, and the aromatic fragment is replaced with halogen, alkyl with 1-4 carbon atoms, trifluoromethyl, hydroxyl, if necessary group, alkoxy group with 1-4 carbon atoms, amino group, cyano group or nitro group, naphthylalkyl residue with 1-3 carbon atoms in alkyl, the residue of phenylalkanone with 2-3 carbon atoms in the alkane residue or phenylcarbamoylalkyl residue with 2 atom amides of carbon in alkyl, wherein the phenyl group may be substituted with halogen,
R 2 represents, if necessary, mono-, di- or trisubstituted by halogen atoms, alkyl with 1-4 carbon atoms, trifluoromethyl, trifluoromethoxy, hydroxyl groups, alkoxy groups with 1-4 carbon atoms, amino groups, monomethylamino groups, dimethylamino, cyanorimer, or nitro groups phenyl, pyridyl, pyrimidinyl or pyrazinyl group, which if necessary can be anelated with a six-membered aromatic nucleus, which if necessary has one or two substituents in the form of halogen atoms, alky and with 1-4 carbon atoms, hydroxyl group, trifluoromethyl group, alkoxy group with 1-4 carbon atoms, amino group, cyano group or nitro group and, if necessary, may contain one nitrogen atom, or with 5- or 6-membered ring, which may contain 1 to 2 oxygen atoms, or it may be substituted by a phenylalkyl group or a phenylalkoxy group with 1 to 2 carbon atoms in the alkyl residue, and the phenyl residue may be replaced by a halogen, methyl group, trifluoromethyl group, or methoxy group. А означает иминогруппу или атом кислорода,
В означает водород или метил,
С означает водород, метил или гидроксильную группу,
Х означает атом азота,
Y означает СН2, СН2-СН2, СН2-СН2-СН2 или СН2-СН,
Z означает атом азота, атом углерода или СН, причем связь между Y и Z может быть также двойной,
n означает число 2, 3 или 4,
а также их физиологически приемлемые соли.And means imino group or oxygen atom,
B is hydrogen or methyl,
C means hydrogen, methyl or hydroxyl group,
X means a nitrogen atom
Y means CH 2 , CH 2 -CH 2 , CH 2 -CH 2 -CH 2 or CH 2 -CH,
Z means a nitrogen atom, a carbon atom or a CH, and the bond between Y and Z can also be double,
n means the number 2, 3 or 4,
and their physiologically acceptable salts. 2. Соединения по п. 1, отличающиеся тем, что R1 означает метил, этил, изопропил, бензил, замещенный бензил, фенэтил, замещенный фенэтил, R2 означает о-метоксифенил, 1-нафтил, пиримидин-2-ил, 2-метокси-1-нафтил, 2-метил-1-нафтил, А означает иминогруппу или атом кислорода, Х означает атом азота, Y означает СН2-СН2, СН2-СН, Z означает атом азота, атом углерода или СН и n является числом 2 и 3.2. Compounds according to claim 1, characterized in that R 1 is methyl, ethyl, isopropyl, benzyl, substituted benzyl, phenethyl, substituted phenethyl, R 2 is o-methoxyphenyl, 1-naphthyl, pyrimidin-2-yl, 2- methoxy-1-naphthyl, 2-methyl-1-naphthyl, A means imino group or oxygen atom, X means nitrogen atom, Y means CH 2 -CH 2 , CH 2 -CH, Z means nitrogen atom, carbon atom or CH and n is the number 2 and 3. 3. Применение соединений по пп.1 и 2 для приготовления лекарственных средств. 3. The use of compounds according to claims 1 and 2 for the preparation of medicines. 4. Применение по п.3 для лечения депрессий и родственных заболеваний. 4. The use according to claim 3 for the treatment of depression and related diseases. 5. Применение соединений по пп.1 и 2 в качестве селективных антагонистов 5-НТ1В и 5-НТ1А.5. The use of compounds according to claims 1 and 2 as selective antagonists of 5-HT 1B and 5-HT 1A . 6. Применение по п.5, причем, кроме селективного серотонинового антагонизма, добавляется ингибирование повторного использования серотонина. 6. The use of claim 5, wherein, in addition to selective serotonin antagonism, inhibition of serotonin reuse is added.
RU99106781/04A 1996-09-10 1997-08-22 3-substituted derivatives of 3,4,5,6,7,8-hexahydro-pyrido-[4',3':4,5]-thieno[2,3- d]-pyrimidine RU2198888C2 (en)

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DE19636769A DE19636769A1 (en) 1996-09-10 1996-09-10 3-Substituted pyrido [4 ', 3': 4,5] thieno [2,3-d] pyrimidine derivatives, their preparation and use
DE19636769.7 1996-09-10

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