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公开(公告)号：US4041030A
公开(公告)日：1977-08-09
申请号：US714473
申请日：1976-08-16
IPC分类号： C07D239/42 , C07D401/12 , C07D413/12
CPC分类号： C07D401/12 , C07D239/42 , Y10S514/869 , Y10S514/906 , Y10S514/927
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。
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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＆lt; IMAGE＆gt;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。
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3.发明授权Pyrimidin-6-yl acethydroxamic acids, their therapeutic application and their process of preparation 失效吡咯烷-6-YL乙酰氧基酸，其治疗应用及其制备方法
公开(公告)号：US4013768A
公开(公告)日：1977-03-22
申请号：US554532
申请日：1975-03-03
IPC分类号： C07D239/28 , A61K31/505 , C07D239/42 , C07D413/12 , C07D239/26
CPC分类号： C07D239/42 , C07D413/12
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 2-Ar-4-chloro-pyrimidin-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.
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公开(公告)号：US3978055A
公开(公告)日：1976-08-31
申请号：US502285
申请日：1974-09-03
IPC分类号： A61K31/505 , C07D239/42 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/10
CPC分类号： C07D239/42 , C07D401/12 , Y10S514/869 , Y10S514/906 , Y10S514/927 , Y10S514/929
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。
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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
CPC分类号： C07D413/12 , Y10S514/869 , Y10S514/925 , Y10S514/929
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。
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公开(公告)号：US4041072A
公开(公告)日：1977-08-09
申请号：US668061
申请日：1976-03-18
IPC分类号： A61K31/165 , A61K31/15 , C07C251/32 , C07C259/14 , C07C103/28 , C07C103/365 , C07C103/76
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。
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公开(公告)号：US3951968A
公开(公告)日：1976-04-20
申请号：US506825
申请日：1974-09-17
IPC分类号： C07D498/12 , C07D235/12 , C07D498/18 , C07D265/00 , C07D273/00 , C07D295/00
CPC分类号： C07D235/12 , Y10S148/067 , Y10S514/869 , Y10S514/87 , Y10S514/927
摘要： Compounds having the formula ##SPC1##Wherein Y is an aliphatic radical having up to 4 carbon atoms, phenyl, or phenyl substituted by one or more halogens, aliphatic radical having up to 4 carbon atoms, methoxy or trifluoromethyl.The compounds are prepared by reacting epichlorohydrin with benzimidazole substituted at the 2 position by ##EQU1## The compounds possess diuretic, sedative, antiulcerous, analgesic, antiinflammatory and cardiac analeptic properties.
摘要翻译： 具有式WHEREIN Y的化合物是具有至多4个碳原子的脂族基团，苯基或被一个或多个卤素取代的苯基，具有至多4个碳原子的脂族基团，甲氧基或三氟甲基。
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公开(公告)号：US3959270A
公开(公告)日：1976-05-25
申请号：US453425
申请日：1974-03-21
IPC分类号： C07D498/04 , C07D279/00 , C07D285/00 , C07D295/00
CPC分类号： C07D498/04
摘要： A compound of the formula ##SPC1##Wherein R.sub.1 is alkyl having one to 4 carbon atoms, and R.sub.2 is (a) alkyl having one to 4 carbon atoms, or (b) alkyl having one to 4 carbon atoms and substituted by (1) dialkylamino the latter alkyl having from one to 3 carbon atoms, (2) pyrrolidino or (3) morpholino, with the proviso that when R.sub.1 is ethyl, R.sub.2 is not ethyl, propyl, or diethylamino. The compounds are prepared by reacting 2-methyl-3-alkoxycarbonyl-5-hydroxyindole with a primary amine. The compounds possess diuretic, antihypertensive, antiulcerous, antiinflammatory, sedative and analgesic properties.
摘要翻译： 式WHERE R1的化合物是具有1至4个碳原子的烷基，R 2是（a）具有1至4个碳原子的（a）烷基，或（b）具有1至4个碳原子并由（1）二烷基氨基取代的烷基 具有1至3个碳原子的烷基，（2）吡咯烷子基或（3）吗啉代，条件是当R 1是乙基时，R 2不是乙基，丙基或二乙基氨基。 通过2-甲基-3-烷氧基羰基-5-羟基吲哚与伯胺反应来制备化合物。 该化合物具有利尿，抗高血压，抗溃疡，抗炎，镇静和镇痛等特点。
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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
申请人： Philippe L. Dostert , Colette A. Douzon , Guy R. Bourgery , Claude J. Gouret , Gisele C. Mocquet , Jean A. Coston
发明人： Philippe L. Dostert , Colette A. Douzon , Guy R. Bourgery , Claude J. Gouret , Gisele C. Mocquet , Jean A. Coston
IPC分类号： A61K31/42 , A61K31/421 , A61P25/24 , A61P25/26 , C07D263/24
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：
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10.发明授权
公开(公告)号：US5017723A
公开(公告)日：1991-05-21
申请号：US484493
申请日：1990-02-26
申请人： Gilbert G. Aubard , Alain P. Calvet , Claude J. Gouret , Agnes M. Grouhel , Henry L. Jacobelli , Jean-Louis Junien , Xavier B. Pascaud , Francois J. Roman , Claude D. Soulard , James P. Hudspeth , Yuan Lin
发明人： Gilbert G. Aubard , Alain P. Calvet , Claude J. Gouret , Agnes M. Grouhel , Henry L. Jacobelli , Jean-Louis Junien , Xavier B. Pascaud , Francois J. Roman , Claude D. Soulard , James P. Hudspeth , Yuan Lin
IPC分类号： C07C211/28 , C07C211/29 , C07C217/58 , C07C217/60 , C07C217/74 , C07C255/42 , C07C255/43 , C07C265/08 , C07D307/52 , C07D333/20 , C07D409/06
CPC分类号： C07D409/06 , C07C211/28 , C07C211/29 , C07C217/58 , C07C217/60 , C07C217/74 , C07C255/42 , C07C255/43 , C07C265/08 , C07D307/52 , C07D333/20 , C07C2101/02
摘要： Substituted ethylamines of the formula ##STR1## wherein R.sub.1 is phenyl optionally mono-, di- or trisubstituted by halogen, lower alkyl, lower haloalkyl or lower alkoxy, or is an aromatic heterocycle having 5 to 7 chains wherein the heteroatom is nitrogen, oxygen or sulfur,R.sub.2 is lower alkyl,R.sub.3 and R.sub.4, each independently, represent hydrogen, lower alkyl or lower alkenyl,R.sub.5 is phenyl optionally mono-, di- or trisubstituted by halogen or lower alkoxy or is an aromatic heterocycle having 5 to 7 chains wherein the heteroatom is nitrogen, oxygen or sulfur andQ represents a --CH.dbd.CH-- ethylene group or a 1,2-diyl ##STR2## propane group, their acid addition salts and their optically active forms. These substituted ethylamines have psycotropic properties and are useful as medicines.
摘要翻译： 下式的取代的乙胺（I）其中R1是任选被卤素，低级烷基，低级卤代烷基或低级烷氧基单取代，二取代或三取代的苯基，或是具有5至7个链的芳族杂环，其中杂原子是氮 ，氧或硫，R 2是低级烷基，R 3和R 4各自独立地代表氢，低级烷基或低级烯基，R 5是任选地被卤素或低级烷氧基单，二或三取代的苯基，或者是具有5至 7个链，其中杂原子是氮，氧或硫，Q表示-CH = CH-亚乙基或1,2-二基丙烷基，它们的酸加成盐及其光学活性形式。 这些取代的乙胺具有抗菌性，可用作药物。
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