Arylamino pyrimidinic derivatives
    1.
    发明授权
    Arylamino pyrimidinic derivatives 失效
    芳基嘧啶衍生物

    公开(公告)号:US4041030A

    公开(公告)日:1977-08-09

    申请号:US714473

    申请日:1976-08-16

    摘要: Compounds of the formula ##STR1## WHEREIN Ar is phenyl or phenyl substituted by one or more halogens, a trifluoromethyl, a methylenedioxy, one or more methoxy, an alkyl having one to 4 carbon atoms or a dimethylamino,And R is ##STR2## wherein R.sub.1 and R.sub.2 each are hydrogen or alkyl of 1 to 4 carbon atoms, or ##STR3## PYRROLIDINO, MORPHOLINO, PIPERIDINO OR PIPERAZINO N'-substituted by alkyl of 1 to 4 carbon atoms, or phenyl, or R is para-2-morpholino ethylamino carbonyl, and R.sub.3 is hydrogen or methyl.The compounds are obtained by reacting 2-Ar-2-chloro-6-methyl pyrimidine, with ##STR4## The compounds possess sedative, antiulcerous, antibronchoconstrictive, anticholinergic, diuretic, analgesic myorelaxant and antianoximia properties.

    摘要翻译: 下式的化合物Ar是苯基或被一个或多个卤素,三氟甲基,亚甲二氧基,一个或多个甲氧基,具有1至4个碳原子的烷基或二甲基氨基取代的苯基,AND R是其中 R 1和R 2各自为氢或1至4个碳原子的烷基,或由1-4个碳原子的烷基或苯基取代的吡咯烷基,吗啉,哌啶或哌嗪,或R为对位-2-吗啉代 乙氨基羰基,R 3为氢或甲基。

    Arylamino pyrimidinic derivatives
    2.
    发明授权
    Arylamino pyrimidinic derivatives 失效
    芳基嘧啶衍生物

    公开(公告)号:US4025514A

    公开(公告)日:1977-05-24

    申请号:US714472

    申请日:1976-08-16

    IPC分类号: C07D239/42 C07D401/12

    CPC分类号: C07D401/12 C07D239/42

    摘要: Compounds of the formula ##STR1## wherein Ar is phenyl or phenyl substituted by one or more halogens, a trifluoromethyl, a methylenedioxy, one or more methoxy, an alkyl having one to 4 carbon atoms or a dimethylamino,And R is ##STR2## and R.sub.5 is alkyl of 1 to 4 carbon atoms, 2,3-dihydroxypropyl or 2,2-dimethyl dioxolan-4-yl methyl or hydroxycarbonylmethyl.The compounds are obtained by reacting 2-Ar-4-chloro-6-methyl pyrimidine, with ##STR3## The compounds possess sedative, antiinflammatory, antiulcerous, and anti-anoxemia properties.

    摘要翻译: 其中Ar是苯基或被一个或多个卤素取代的苯基,三氟甲基,亚甲二氧基,一个或多个甲氧基,具有1-4个碳原子的烷基或二甲基氨基的化合物,和R是< IMAGE>和 R5是1-4个碳原子的烷基,2,3-二羟基丙基或2,2-二甲基二氧戊环-4-基甲基或羟基羰基甲基。

    Pyrimidin-6-yl acethydroxamic acids
    4.
    发明授权
    Pyrimidin-6-yl acethydroxamic acids 失效
    嘧啶-6-基乙酸异羟肟酸

    公开(公告)号:US4061855A

    公开(公告)日:1977-12-06

    申请号:US749221

    申请日:1976-12-10

    IPC分类号: C07D413/12 A61K31/535

    摘要: Compounds of the formula ##STR1## IN WHICH R is aminocarbonylphenyl in which amino is --NH.sub.2, pyrrolidino, piperidino or morpholino, and Ar is phenyl substituted with chloro, fluoro, trifluoromethyl, methylenedioxy or one or more methoxy. The compounds are prepared by reacting 2-Ar-4-chloropyrimidin-6-yl ethylacetate with ##STR2## and then reacting that reaction product with hydroxylamine hydrochloride. The compounds possess vasodilatatory, anti-ulcerous, respiratory analeptic, hypotensive, diuretic, anti-depressive, analgesic, anti-inflammatory and neurotropic properties.

    摘要翻译: 其中R为氨基羰基苯基的化合物,其中氨基为-NH 2,吡咯烷子基,哌啶子基或吗啉代,Ar为被氯,氟,三氟甲基,亚甲二氧基或一个或多个甲氧基取代的苯基。 该化合物通过使2-氨基-4-氯嘧啶-6-基乙酸乙酯与“IMAGE”反应,然后使该反应产物与盐酸羟胺反应制备。 该化合物具有血管舒张,抗溃疡,呼吸消炎,降血压,利尿,抗抑郁,镇痛,抗炎和神经营养特性。

    Acetamidoxime compounds
    5.
    发明授权
    Acetamidoxime compounds 失效
    乙酰肟化合物

    公开(公告)号:US4041072A

    公开(公告)日:1977-08-09

    申请号:US668061

    申请日:1976-03-18

    CPC分类号: C07C259/14

    摘要: Compounds having the formula ##STR1## wherein R is hydrogen, or chlorine, or alkyl having one to 4 carbons, or alkoxy having one to 3 carbons, and R.sub.1 is hydrogen, or ##STR2## or --CONH--R.sub.3, wherein R.sub.2 is hydrogen, or chlorine, or nitro, or alkoxy having no more than 3 carbons, or trifluoromethyl, and R.sub.3 is alkyl having one to 4 carbons, or cycloalkyl having no more than 6 carbons, or phenyl.The compounds are prepared by reacting R-substituted cyano-2 acetanilides with hydroxylamine to obtain compounds in which R.sub.1 is hydrogen, and then reacting with acid chlorides containing R.sub.2 or isocyanates containing R.sub.3. The compounds possess psychtropic properties.

    摘要翻译: 具有式“IMAGE”的化合物,其中R是氢或氯,具有1至4个碳的烷基或具有1至3个碳原子的烷氧基,R 1是氢,或者R 3是-CONH-R 3,其中R 2是氢 或氯或硝基,或不多于3个碳原子的烷氧基,或三氟甲基,R3是具有1-4个碳原子的烷基,或不多于6个碳的烷基或苯基。

    Arylamino pyrimidinic derivatives
    6.
    发明授权
    Arylamino pyrimidinic derivatives 失效
    芳基嘧啶衍生物

    公开(公告)号:US3978055A

    公开(公告)日:1976-08-31

    申请号:US502285

    申请日:1974-09-03

    摘要: Compounds of the formula ##SPC1##Wherein Ar is phenyl or phenyl substituted by one or more halogens, by a trifluoromethyl or a methylenedioxy, by one or more methoxy, by an alkyl having one to 4 carbon atoms or by a dimethylamino,And R is ##EQU1## or --O-- ##EQU2## or ##EQU3## wherein R.sub.1 and R.sub.2 each are hydrogen or alkyl of 1 to 4 carbon atoms, or ##EQU4## is pyrrolidino, morpholino, piperidino or piperazino N'-substituted by alkyl of 1 to 4 carbon atoms, or phenyl; R.sub.3 and R.sub.4 each are alkyl of 1 to 3 carbon atoms or ##EQU5## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, n is an integer of 1 to 5; and R.sub.5 is alkyl of 1 to 4 carbon atoms, 2,3-dihydroxypropyl or 2,2-dimethyl dioxolan-4-yl methyl or hydroxycarbonylmethyl.The compounds are obtained by reacting 2-Ar-2-chloro-6-methyl pyrimidine, with ##SPC2##The compounds possess sedative, antiinflammatory, antiulcerous, vasodilatatory, antibronchoconstrictive, anticholinergic, diuretic, spasmolytic, cardiac analeptic, analgesic and myorelaxant properties.

    摘要翻译: 式WHEREIN Ar的化合物是苯基或被一个或多个卤素,三氟甲基或亚甲二氧基,一个或多个甲氧基,具有1至4个碳原子的烷基或二甲基氨基取代的苯基,并且R 1是R 1 -CN ANGLE,PARALLEL OR2或-O- R3(CH2)nN ANGLE,R4或OC ANGLE OR5,其中R1和R2各自为氢或1-4个碳原子的烷基,或R1-ANGLE R2为吡咯烷子基,吗啉代,哌啶子基或哌嗪基 N'被1至4个碳原子的烷基取代,或苯基; R3和R4各自为1至3个碳原子的烷基或R3-ANGLE R4为吗啉代,吡咯烷子基,哌啶子基或六亚甲基亚氨基,n为1至5的整数; R5为1-4个碳原子的烷基,2,3-二羟基丙基或2,2-二甲基二氧戊环-4-基甲基或羟基羰基甲基。

    Furo (2,3d) pyrimidines
    7.
    发明授权
    Furo (2,3d) pyrimidines 失效
    呋喃(2,3d)嘧啶

    公开(公告)号:US4031089A

    公开(公告)日:1977-06-21

    申请号:US715377

    申请日:1976-08-18

    IPC分类号: C07D491/04 C07D491/048

    摘要: Compounds of the formula ##STR1## wherein R is alkyl of 1-4 carbon atoms, phenyl, or phenyl substituted by one or more halogen or trifluoromethyl, and Z is ##STR2## wherein R.sub.1 is hydrogen, alkyl of 1-4C, 2,2-dimethyldioxolan-4-yl methyl, or 2,3-dihydroxy prop-1-yl, R.sub.2 is ##STR3## wherein ##STR4## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, and n is an integer from 4 to 7.The compounds are prepared by reacting R-substituted 4-chloro-2-methyl furo (2,3d) pyrimidine with HZ. The compounds possess antiulcerous, antibronchoconstrictive and anticholinergic, analgesic, antihistamine, diuretic, cardiovascular analeptic, antiinflammatory and hypertensive properties.

    摘要翻译: 其中R是1-4个碳原子的烷基,苯基或被一个或多个卤素或三氟甲基取代的苯基,Z是下式的化合物,其中R 1是 氢,1-4C的烷基,2,2-二甲基二氧杂环戊烷-4-基甲基或2,3-二羟基丙-1-基,其中,作为吗啉,吡咯烷子基,哌啶子基或哌啶子基, 六亚甲基亚氨基,n为4〜7的整数。

    3-Aryl 2-oxazolidinones, their process of preparation and their
therapeutical application
    9.
    发明授权
    3-Aryl 2-oxazolidinones, their process of preparation and their therapeutical application 失效
    3-芳基2-恶唑烷酮,其制备方法及其治疗应用

    公开(公告)号:US4150029A

    公开(公告)日:1979-04-17

    申请号:US771814

    申请日:1977-02-23

    CPC分类号: C07D263/24

    摘要: Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or CONHR.sub.7 and R.sub.7 is methyl or isopropyl,And whereinWhen R.sub.1 is hydrogen: R is p-nitro, p-cyano; p-aldehydo; p-acetyl; m-ethyl; m-nitro; m-bromo; 3,4-dimethyl; m-NH.sub.2 ; p-methylamino; p-dimethylamino; p-diethylamino; p-methylbenzylamino; p-pyrrolidino; p-piperidino; SR.sub.4 in para position in which R.sub.4 is alkyl having 1 to 4 carbon atoms or cyclohexyl; OR.sub.5 is para position in which R.sub.5 is alkyl having 2 to 7 carbon atoms, cyclohexyl, cyclohexylmethyl, acetylmethyl; cyanomethyl, alkene-2 yl having 3 to 5 carbon atoms, butene-3 yl, cyclohexene-1 methyl, propargyl, butyne-2 yl, ##STR2## in which n is one or 2 and when n is one, R.sub.6 is hydrogen, o-fluoro, o-methyl, m-chloro, m-fluoro, m-methyl, m-trifluoromethyl, p-chloro, p-bromo-, p-fluoro, p-cyano, p-nitro or p-dimethylamino and when n is 2, R.sub.6 is hydrogen; and 3-methyl-4-benzyloxy:When R.sub.1 is CONHR.sub.7 and R.sub.7 is methyl: R is m-trifluoromethyl; m-bromo; p-chloro; p-fluoro; 3,4-dichloro; p-thiomethyl; p-acetyl; OR.sub.8 in para position wherein R.sub.8 is alkyl having 2 to 5 carbon atoms, cyanomethyl, acetylmethyl, propargyl or ##STR3## in which R.sub.9 is hydrogen, m-chloro, m-bromo, m-fluoro, p-fluoro, p-chloro or p-nitro;And when R.sub.1 is CONHR.sub.7 and R.sub.7 is isopropyl; R is m-trifluoromethyl or p-benzyloxy.The compounds are prepared by cyclizing 1-phenylamino-2,3-propandiol derivatives to form 5-hydroxymethyl-3 phenyl-2-oxozolidinone derivatives. The 5-hydroxymethyl group can be transformed to --CH.sub.2 OCONHR.sub.7 by reaction with methyl isocyanate or isopropyl isocyanate. The compounds possess psychotropic, particularly antidepressant, activity.

    摘要翻译: 具有式“IMAGE”的化合物,其中R1是氢或CONHR7,R7是甲基或异丙基,当R1是氢时,R是对硝基,对氰基; 对醛 对乙酰基; 甲基; 间硝基 溴代 3,4-二甲基 m-NH2; 对甲基氨基; 对二甲基氨基; 对二乙基氨基; 对甲基苄基氨基; 对 - 吡咯烷子; 对哌啶子 其中R4是具有1-4个碳原子的烷基的对位的SR4或环己基; OR5是R5是具有2至7个碳原子的烷基的对位,环己基,环己基甲基,乙酰基甲基; 氰基甲基,具有3至5个碳原子的烯-2,丁烯-3,环己烯-1甲基,炔丙基,丁炔-2基,其中n为1或2,当n为1时,R6为氢, 邻 - 甲基,间 - 氯,间氟,间甲基,间三氟甲基,对氯,对溴 - ,对氟,对氰基,对硝基或对二甲基氨基,当 n为2,R6为氢; 和3-甲基-4-苄氧基:

    Furo (2,3d) pyrimidines
    10.
    发明授权
    Furo (2,3d) pyrimidines 失效
    呋喃(2,3d)嘧啶

    公开(公告)号:US4007187A

    公开(公告)日:1977-02-08

    申请号:US506826

    申请日:1974-09-17

    CPC分类号: C07D491/04

    摘要: Compounds of the formula ##STR1## wherein R is alkyl of 1-4 carbon atoms, phenyl, or phenyl substituted by one or more halogen or trifluoromethyl, and Z is ##STR2## wherein R.sub.1 is hydrogen, alkyl of 1-4C, 2,2-dimethyldioxolan-4-yl methyl, or 2,3-dihydroxy prop-1-yl, R.sub.2 is ##STR3## wherein ##STR4## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, and n is an integer from 4 to 7. The compounds are prepared by reacting R-substituted 4-chloro-2-methyl furo (2,3d) pyrimidine with HZ. The compounds possess antiulcerous, antibronchoconstrictive and anticholinergic, analgesic, antihistamine, diuretic, cardiovascular analeptic, antiinflammatory and hypertensive properties.

    摘要翻译: 其中R是1-4个碳原子的烷基,苯基或被一个或多个卤素或三氟甲基取代的苯基,Z是下式的化合物,其中R 1是 氢,1-4C的烷基,2,2-二甲基二氧杂环戊烷-4-基甲基或2,3-二羟基丙-1-基,其中,作为吗啉,吡咯烷子基,哌啶子基或哌啶子基, 六亚甲基亚氨基,n为4〜7的整数。该化合物通过R-取代的4-氯-2-甲基呋喃(2,3d)嘧啶与HZ反应来制备。 该化合物具有抗溃疡,抗纤维蛋白胆固醇和抗胆碱能药,止痛药,抗组胺药,利尿剂,心血管镇痛药,抗炎和高血压药物。