摘要:
Compounds of formula (I) ##STR1## wherein R represents a ##STR2## group in which R.sub.2 is a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxylic group, a sodium carboxylate group, a --CH.sub.2 OR.sub.4 group R.sub.4 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group or a (C.sub.1 -C.sub.4)acyl group, an amide group of the formula --CONR.sub.5 R.sub.6, or a --CN.sub.4 R.sub.5 group, R.sub.5 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 being a hydrogen atom, a (C.sub.1 -C.sub.4)alkyl group, a hydroxy group or a (C.sub.1 -C.sub.4)alkoxy group, and R.sub.3 is a (C.sub.1 -C.sub.4)alkyl group,R.sub.1 represents either a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group,X represents either a sulphur atom, an oxygen atom or a methylene group, n=1 or 2 andAr represents either a naphthalen-1-yl group substituted by a di(C.sub.1 -C.sub.4)alkylamino group, or a 6,7-di(C.sub.1 -C.sub.4)alkoxynaphthalen-1-yl group, or a quinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl group, or a 1,2,3,4-tetrahydroquinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl, or a 1H-indazol-7-yl group and pharmaceutically acceptable organic or inorganic salts thereof.Application in therapy.
摘要:
Compounds of formula (I) ##STR1## wherein R.sub.1 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group,X represents either a sulphur atom, an oxygen atom or a methylene group,Z.sub.1 represents either a hydrogen atom, or a 1,1-dimethylethyl group,Z.sub.2 represents either a hydrogen atom, a triphenylmethyl group, or a phenylmethoxycarbonyl group, andn=1 or 2,and addition salts to inorganic or organic acids thereof as synthetic intermediates.
摘要:
Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxyl group, a sodium carboxylate group, a group --CH.sub.2 OR.sub.4, where R.sub.4 is a hydrogen atom or R.sub.4 is a (C.sub.1 -C.sub.4) alkyl or (C.sub.1 -C.sub.4) acyl group, a group --CONR.sub.5 R.sub.6, or a group --CN.sub.4 R.sub.5, where R.sub.5 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, hydroxyl or (C.sub.1 -C.sub.4) alkoxy or (C.sub.1 -C.sub.3) alkoxyphenyl group and R.sub.3 represents a (C.sub.1 -C.sub.4)alkyl group, and their acid addition salts are useful as synthetic intermediates.
摘要翻译:下式的化合物:其中R 1表示氢原子或(C 1 -C 4)烷基,R 2表示氢原子,(C 1 -C 4)烷氧基羰基,羧基,羧酸钠 基团,-CH 2 OR 4,其中R 4是氢原子或R 4是(C 1 -C 4)烷基或(C 1 -C 4)酰基,基团-CONR 5 R 6或基团-CN 4 R 5,其中R 5是氢原子或 (C1-C4)烷基,R6是氢原子或(C1-C4)烷基,羟基或(C1-C4)烷氧基或(C1-C3)烷氧基苯基,R3表示(C1-C4)烷基 ,其酸加成盐可用作合成中间体。
摘要:
The invention concerns compounds of formula (I) in which: R is —NO2 or —NHR3, R3 being hydrogen, —COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, —COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), —CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), —SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a —CH2—, —SO2 or —NR1— group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.
摘要:
Compounds of the formula: ##STR1## in which R represents a chlorine atom or a hydroxyl group and R.sub.4 represents a (C.sub.1 -C.sub.4)alkyl group in the R or S form are useful as synthetic intermediates.
摘要:
Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.
摘要:
The present invention is directed to compounds of the general formula: as well as pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
摘要:
A method of treating a patient susceptible to thrombosis is provided which comprises treating the said patient with a compound of the formula ##STR1## wherein R' is H or CH.sub.3R is a ##STR2## radical in which Z is 0, S, SO, SO.sub.2 or NR.sub.1, R.sub.1 being H, C.sub.6 H.sub.5, CH.sub.3, CONR.sub.2 R.sub.3, COOR.sub.2, COR.sub.2 or SO.sub.2 R.sub.2, where R.sub.2 and R.sub.3 are, independently, H, C.sub.1-4 alkyl, C.sub.6 H.sub.5 or CF.sub.3.
摘要翻译:提供一种治疗易患血栓形成的患者的方法,其包括用下式化合物治疗所述患者:其中R'为H或CH 3 R为其中Z为0,S,SO, SO 2或NR 1,R 1是H,C 6 H 5,CH 3,CONR 2 R 3,COOR 2,COR 2或SO 2 R 2,其中R 2和R 3独立地是H,C 1-4烷基,C 6 H 5或CF 3。
摘要:
The present invention is directed to compounds of the general formula: as defined herein, and pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
摘要:
The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.