Piperidines, processes of preparation and medications containing them
    2.
    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。

    4(3H)-pteridinones, preparation processes and drugs containing them
    4.
    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。

    2-Amino-5-phenyl-1,3-benzodiazepines
    5.
    发明授权
    2-Amino-5-phenyl-1,3-benzodiazepines 失效
    2-氨基-5-苯基-1,3-苯并二氮杂卓

    公开(公告)号:US4554273A

    公开(公告)日:1985-11-19

    申请号:US578046

    申请日:1984-02-07

    摘要: Disclosed are 2-amino-5-phenyl-1,3-benzodiazepines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, halogen, alkyl, or alkoxy; R.sub.2 being able to occupy any of the possible positions on the aromatic ring; R.sub.3 is hydrogen or alkyl; and R.sub.4 is hydrogen, alkyl, cycloalkyl, arylalkyl, heteroarylalkyl, dialkylaminoethyl, dialkylaminopropyl, (1-ethyl-2-pyrrolidino) methyl, dialkylamino, alkoxycarbonyl or cyano; or R.sub.3 and R.sub.4 form, with the adjacent nitrogen atom, a heterocycle having 5 to 7 side chains, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen, this latter being able to be substituted by an alkyl group. The majority of the compounds are obtained by condensation of the corresponding 2-methylthio benzodiazepine hydroiodide with an appropriate amine. The compounds are useful as antidepressants.

    摘要翻译: 公开了下式的2-氨基-5-苯基-1,3-苯并二氮杂其中R 1和R 2是氢,卤素,烷基或烷氧基; R2能够占据芳香环上任何可能的位置; R3是氢或烷基; 并且R 4是氢,烷基,环烷基,芳基烷基,杂芳基烷基,二烷基氨基乙基,二烷基氨基丙基,(1-乙基-2-吡咯烷子基)甲基,二烷基氨基,烷氧基羰基或氰基; 或R3和R4与相邻的氮原子形成具有5至7个侧链的杂环,任选地含有选自氧,硫或氮的另外的杂原子,后者可被烷基取代。 大部分化合物通过相应的2-甲硫基苯并二氮杂环丁烷与合适的胺的缩合得到。 这些化合物可用作抗抑郁药。

    4(3H)-pteridinone compounds
    6.
    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。

    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。

    5-Substituted indan-2 carboxylic acid and functional derivatives
    8.
    发明授权
    5-Substituted indan-2 carboxylic acid and functional derivatives 失效
    5-取代的茚满-2-羧酸和官能衍生物

    公开(公告)号:US4224341A

    公开(公告)日:1980-09-23

    申请号:US860466

    申请日:1977-12-14

    摘要: 5-Substituted indan-2-carboxylic acids and functional derivatives thereof having inflammation-reducing properties have the general formula ##STR1## in which R is a phenyl, phenyl-lower alkenyl, phenyl-lower alkyl, phenyl substituted by at least one of the halogens, lower alkyl, lower alkoxy, acetamido, amino, lower dialkylamino, nitro, phenyl, lower alkylsulfonyl, lower dialkylaminosulfonyl and sulfamido, cyclohexyl, furyl, lower alkylfuryl, thienyl, halothienyl, lower alkylthienyl, or pyridyl group and R' is a hydroxyl, lower alkoxy, lower dialkylaminoalkoxy, cinnamoylamido lower alkoxy, 2-hydroxyethylamino, amino or lower dialkylaminoalkyl amino group. Besides the esters and amides, the functional derivatives of the acids include the pharmacologically acceptable salts of the above compounds. The compounds are also of low toxicity, have analgesic activity and exert an antipyretic effect.

    摘要翻译: 5-取代的茚满-2-羧酸及其具有炎症降低性质的功能衍生物具有通式“IMAGE”,其中R是苯基,苯基 - 低级烯基,苯基 - 低级烷基,被至少一个 卤素,低级烷基,低级烷氧基,乙酰氨基,氨基,低级二烷基氨基,硝基,苯基,低级烷基磺酰基,低级二烷基氨基磺酰基和磺酰氨基,环己基,呋喃基,低级烷基呋喃基,噻吩基,卤代噻吩基,低级烷基噻吩基或吡啶基,R' 低级烷氧基,低级二烷基氨基烷氧基,肉桂酰氨基低级烷氧基,2-羟基乙基氨基,氨基或低级二烷基氨基烷基氨基。 除了酯和酰胺之外,酸的官能衍生物包括上述化合物的药理学上可接受的盐。 该化合物也具有低毒性,具有镇痛作用,并具有解热作用。