4(3H)-pteridinones, preparation processes and drugs containing them
    6.
    发明授权
    4(3H)-pteridinones, preparation processes and drugs containing them 失效
    4(3H) - 哌啶酮,制备方法和含有它们的药物

    公开(公告)号:US5167949A

    公开(公告)日:1992-12-01

    申请号:US501104

    申请日:1990-03-29

    CPC分类号: C07D475/02

    摘要: The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical. Application of these compounds as anti-allergic drugs.

    摘要翻译: 本发明涉及由下式表示的4(3H) - 蝶啶酮:其中X是氧原子或硫原子,Y是氢原子,低级烷基,特别是甲基,在6 位置或羟基,R1是氢原子,低级烷基,取代或未取代的苯基,苄基,甲氧基甲基,乙酰基,2-乙酰氧基乙基或2 ,2,2-三氟乙基,R 2为氢原子或低级烷基,特别是甲基。 这些化合物作为抗过敏药物的应用。

    Benzo- and thieno-triazine-1,2,3 ones-4
    7.
    发明授权
    Benzo- and thieno-triazine-1,2,3 ones-4 失效
    苯并 - 噻吩并三嗪-1,2,3,4-四酮

    公开(公告)号:US4552878A

    公开(公告)日:1985-11-12

    申请号:US534173

    申请日:1983-09-19

    CPC分类号: C07D253/08 C07D495/04

    摘要: This invention relates to benzo- and thieno-triazine-1,2,3 ones-4 represented by the formula ##STR1## in which m is 2, 3 or 4, X is the vinylene group --CH.dbd.CH-- or a sulfur atom; R.sub.1 and R.sub.2 can be alike or different and are hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or trifluoromethyl radical; when X is --CH--CH-- n is 0, 1 or 2 and R is hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or nitro group; when X is a sulfur atom, R is hydrogen or constitutes a --CH.sub.2 --.sub.4 chain between the two open positions of the thiophenic ring. The compounds are useful as antidepressant drugs.

    摘要翻译: 本发明涉及由式“IMAGE”表示的苯并 - 噻吩并三嗪-1,2,3,4-四烷基,其中m为2,3或4,X为亚乙烯基-CH = CH-或硫原子 ; R 1和R 2可以相同或不同,为氢,卤素,低级烷基,低级烷氧基或三氟甲基; 当X是-CH-CH- n是0,1或2且R是氢时,卤素,低级烷基,低级烷氧基或硝基; 当X是硫原子时,R是氢或在噻吩环的两个开放位置之间构成-CH2-4链。 该化合物可用作抗抑郁药物。

    4(3H)-pteridinone compounds
    8.
    发明授权
    4(3H)-pteridinone compounds 失效
    4(3H) - 蝶啶酮化合物

    公开(公告)号:US5270465A

    公开(公告)日:1993-12-14

    申请号:US970839

    申请日:1992-11-03

    IPC分类号: C07D475/02 A61K31/505

    CPC分类号: C07D475/02

    摘要: The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical.Application of these compounds as anti-allergic drugs.

    摘要翻译: 本发明涉及由下式表示的4(3H) - 蝶啶酮:其中X是氧原子或硫原子,Y是氢原子,低级烷基,特别是甲基,在6 位置或羟基,R1是氢原子,低级烷基,取代或未取代的苯基,苄基,甲氧基甲基,乙酰基,2-乙酰氧基乙基或2 ,2,2-三氟乙基,R 2为氢原子或低级烷基,特别是甲基。 这些化合物作为抗过敏药物的应用。

    Piperidines, processes of preparation and medications containing them
    9.
    发明授权
    Piperidines, processes of preparation and medications containing them 失效
    哌啶类,制剂过程和含有它们的药物

    公开(公告)号:US5001134A

    公开(公告)日:1991-03-19

    申请号:US461515

    申请日:1990-01-05

    摘要: The present invention relates to piperidines denoted by the formula: ##STR1## in which X is the 4-fluorobenzoyl, 2-(4-fluorophenyl)-1,3-dioxolan-2-yl or 6-fluoro-1,2-benzisoxazol-3-yl group, Y is a hydrogen atom or the hydroxyl group, m is an integer between 0 and 4 inclusive, n is 0 or 1, Q is a nitrogen atom or the methine group; when Q is a nitrogen atom, R is the cyano group or the carbamoyl group; when Q is the methine group, R is the nitro group; R.sup.1 and R.sup.2 may be identical or different and are hydrogen, a lower alkyl radical, the phenyl radical, the 2,2,2-trifluoroethyl group or the 2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl group; or the NR.sup.1 R.sup.2 structural unit is the piperidino radical or the 4-(4-fluorobenzoyl)-1-piperidinyl group.Application of these compounds as antihypertensive medications.

    摘要翻译: 本发明涉及由下式表示的哌啶:其中X是4-氟苯甲酰基,2-(4-氟苯基)-1,3-二氧戊环-2-基或6-氟-1,2-苯并异恶唑 3-基,Y为氢原子或羟基,m为0〜4的整数,n为0或1,Q为氮原子或次甲基。 当Q为氮原子时,R为氰基或氨基甲酰基; 当Q为次甲基时,R为硝基; R 1和R 2可以相同或不同,为氢,低级烷基,苯基,2,2,2-三氟乙基或2- [4-(4-氟苯甲酰基)-1-哌啶基]乙基; 或NR1R2结构单元是哌啶子基或4-(4-氟苯甲酰基)-1-哌啶基。 这些化合物作为抗高血压药物的应用。

    3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and
derivatives, their preparations and medicines containing them
    10.
    发明授权
    3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and derivatives, their preparations and medicines containing them 失效
    3,4-二氢-4-氧代-3-(2-丙烯基)-1-酞嗪乙酸及其衍生物,其制剂和含有它们的药物

    公开(公告)号:US5489592A

    公开(公告)日:1996-02-06

    申请号:US211427

    申请日:1994-06-20

    摘要: Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) ##STR1## in which R.sub.1 R.sub.2 and R.sub.3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R.sub.4 residue such as defined below, except when R.sub.4 is H; R.sub.4 and R.sub.5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R.sub.4 and R.sub.5 do not simultaneously denote H; R.sub.6 stands for hydroxy or alkoxy radical; R.sub.7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by analiphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R.sub.8 or a cyano group; n is equal to 0,1 or 2; R.sub.8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. This invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.

    摘要翻译: PCT No.PCT / FR92 / 00920 Sec。 371日期:1994年6月20日 102(e)日期1994年6月20日PCT提交1992年10月2日PCT公布。 公开号WO93 / 07109 日期1994年4月15日。新型3,4-二氢-4-氧代-3(丙-2-烯基)-1-对乙酰乙酸及式(I)的衍生物其中R1R2和R3相同 或不同的,代表H,卤素或直链或支链的脂肪族,饱和或不饱和基团,除非是R4是H,而是被至少一个卤素或R4残基取代或不被定义如下。 R 4和R 5相同或不同,代表H,直链或支链脂族基团,饱和或不饱和的芳基或杂芳基,所述基团被至少一个基团取代,例如氟,氯,溴,甲基 或三氟甲基,其中R 4和R 5不同时表示H; R6代表羟基或烷氧基; R7代表H,卤素,直链或支链脂族饱和或不饱和基团,烷氧基,所述基团被脂肪族或卤代基团取代,或不被取代或未取代的氨基取代或未取代的氨基S(O)n R8或氰基; n等于0,1或2; R 8是脂族,直链或支链基团,芳基或杂芳基,氨基,所述基团被脂肪族或卤代基取代。 本发明还涉及所述酸及其药学上可接受的碱加成盐的任选互变异构形式。 还描述了制备所述化合物和含有它们的药物的方法。