专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

61. 发明授权

US4783537A .alpha.-(aminoalkyl)-arylacetic acid derivatives 失效
标题翻译： α-（氨基烷基） - 芳基乙酸衍生物
公开(公告)号：US4783537A
公开(公告)日：1988-11-08
申请号：US797590
申请日：1985-11-13
申请人： Robert J. Murray
发明人： Robert J. Murray
IPC分类号： A61K31/165 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61P9/06 , A61P43/00 , C07C67/00 , C07C227/00 , C07C227/16 , C07C227/18 , C07C229/34 , C07C231/00 , C07C231/12 , C07C233/00 , C07C233/12 , C07C237/20 , C07C253/00 , C07C255/43 , C07C255/53 , C07D213/54 , C07D213/55 , C07D213/56 , C07D213/57 , C07D295/10 , C07D295/14 , C07D295/145 , C07D295/18 , C07D295/185
CPC分类号： C07D295/185 , C07C255/00 , C07D213/55 , C07D213/56 , C07D213/57 , C07D295/145
摘要： Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide, useful in the treatment of cardiovascular disease.
摘要翻译：新型α-芳基-α-（ω-氨基烷基）-α-[羟基（芳烷基和环烷基）]乙酸衍生物和α-芳基-α-（ω-氨基烷基）-α[烷酰氧基（芳烷基和环烷基）]乙酸衍生物，如N，N-二甲基-2-（羟基苯基甲基）-4-二甲基氨基-2-苯基丁酰胺，2-（羟基苯基甲基）-5-二甲基氨基-2-苯基戊腈，2-（羟苯基甲基）-5-二甲基氨基-2 - 苯基戊酸酯和N，N-二甲基-2 [（乙酰氧基）苯基甲基] -4-二甲基氨基-2-苯基丁酰胺，可用于治疗心血管疾病。

62. 发明授权

US4562258A 6-[3-Amino-1-(4-tolyl)prop-1E-enyl]pyridine-2-carboxylic acid derivatives having antihistaminic activity 失效
标题翻译：具有抗组胺活性的6- [3-氨基-1-（4-甲苯基）丙-1-烯基]吡啶-2-羧酸衍生物
公开(公告)号：US4562258A
公开(公告)日：1985-12-31
申请号：US462874
申请日：1983-02-01
申请人： John W. A. Findlay , Geoffrey G. Coker
发明人： John W. A. Findlay , Geoffrey G. Coker
IPC分类号： A61K31/215 , A61K31/165 , A61K31/195 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4439 , A61K31/455 , A61K31/485 , A61P11/00 , A61P37/08 , A61P43/00 , C07C17/00 , C07C25/02 , C07C45/00 , C07C47/575 , C07C49/76 , C07C51/00 , C07C63/04 , C07C65/32 , C07C67/00 , C07C69/025 , C07C209/00 , C07C211/27 , C07C213/00 , C07C215/32 , C07C217/62 , C07C223/02 , C07C229/34 , C07C229/38 , C07D213/38 , C07D213/54 , C07D213/55 , C07D213/56 , C07D213/61 , C07D213/79 , C07D295/155 , C07D401/10 , C07D405/04 , C07F9/38 , C07F9/40 , C07D401/06
CPC分类号： C07D213/79 , A61K31/44 , A61K31/485 , C07D213/55 , C07D213/56 , C07D213/61 , C07D295/155 , C07D405/04
摘要： This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects.
摘要翻译：本公开内容描述了具有基本上没有镇静作用的有效的抗组胺活性的式I化合物。（包括其药学上可接受的盐和酯）。

63. 发明授权

US4310670A Low-temperature, aqueous conversion of 4-picoline derivative to 5-cyano-[3,4'-bipyridin]-6(1H)-one 失效
标题翻译： 4-甲基吡啶衍生物低温水溶液转化为5-氰基 - [3,4'-联吡啶] -6（1H） - 酮
公开(公告)号：US4310670A
公开(公告)日：1982-01-12
申请号：US124807
申请日：1980-02-26
申请人： Karl O. Gelotte , Edward D. Parady
发明人： Karl O. Gelotte , Edward D. Parady
IPC分类号： C07D213/53 , C07D213/38 , C07D213/84 , C07D213/85 , C07D213/22 , C07D213/54
CPC分类号： C07D213/84 , C07D213/38
摘要： The process which comprises reacting 4-picoline below about 30.degree. C. with at least three mole equivalents of an inorganic acid halide, preferably phosphorus oxychloride, per mole of 4-picoline and excess dimethylformamide, reacting in solution the unisolated resulting N-[3-dimethylamino-2-(4-pyridinyl)-2-propenylidene]-N-methylmethaniminium salt (after adding the reaction mixture to cold water, adjusting the pH to about 8.0 and filtering off the precipitated inorganic cationic salts) with excess .alpha.-cyanoacetamide and at least three mole equivalents of base, and then isolating 5-cyano-[3,4'-bipyridin]-6(1H)-one in free base form (after neutralization) or in the form of its inorganic cationic salt. Said 5-cyano-[3,4'-bipyridin]-6(1H)-one is an intermediate for preparing the cardiotonic amrinone.
摘要翻译：该方法包括使低于约30℃的4-甲基吡啶与每摩尔4-甲基吡啶和过量的二甲基甲酰胺与至少三摩尔当量的无机酰卤，优选三氯氧化磷反应，在溶液中使未分离的所得N- [3 - 二甲基氨基-2-（4-吡啶基）-2-亚丙烯基] -N-甲基亚胺鎓盐（将反应混合物加入到冷水中，调节pH至约8.0，过滤沉淀的无机阳离子盐）与过量的α-氰基乙酰胺和至少三摩尔当量的碱，然后分离游离碱形式（中和后）的5-氰基 - [3,4'-联吡啶] -6（1H） - 酮或其无机阳离子盐的形式。所述5-氰基 - [3,4'-联吡啶] -6（1H） - 酮是制备强心型氨力农的中间体。

64. 发明授权

US4283541A Pyridylacyl-hydroxamates 失效
标题翻译：吡啶基酰基 - 异羟肟酸酯
公开(公告)号：US4283541A
公开(公告)日：1981-08-11
申请号：US153480
申请日：1980-05-27
申请人： James R. Shroff , Rohit Desai
发明人： James R. Shroff , Rohit Desai
IPC分类号： C07D213/54 , C07D213/56
CPC分类号： C07D213/54
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl, phenyl or phenyl-lower alkyl,n is an integer from 1 to 5, andm is an integer from 2 to 5 have antiarrhythmic activity.
摘要翻译：其中R 1，R 2和R 3独立地为氢，低级烷基，苯基或苯基 - 低级烷基，n为1至5的整数，m为2至5的整数，具有抗心律失常活性。

65. 发明授权

US4276288A Dehydrooligopeptides, their production and their medicinal use 失效
标题翻译：脱氢寡肽，其生产和药用
公开(公告)号：US4276288A
公开(公告)日：1981-06-30
申请号：US82451
申请日：1979-10-09
申请人： Eugen Etschenberg , Wolfgang Opitz , Siegfried Raddatz
发明人： Eugen Etschenberg , Wolfgang Opitz , Siegfried Raddatz
IPC分类号： C07D263/42 , A61K38/00 , A61P35/00 , C07D213/54 , C07D307/54 , C07D333/24 , C07D333/38 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/087 , C07K5/097 , A61K37/00 , C07C103/52
CPC分类号： C07K5/06034 , C07D213/54 , C07D307/54 , C07D333/24 , C07D333/38 , C07K5/06078 , C07K5/06139 , C07K5/0812 , C07K5/0821
摘要： New dehydrooligopepetides which bear, as one terminal substituent, an optionally substituted alkyl or alkenyl, optionally substituted aryl, optionally substituted heterocyclic radical, optionally substituted aralkyl or aralkenyl or a carbamoyl group and as the other terminal substituent a hydroxyl or amino, an optionally substituted alkylamino, optionally substituted arylamino, optionally substituted aralkylamino, an optionally substituted nitrogen-containing heterocyclic radical with five or six ring members optionally containing a further heteroatom, optionally substituted aralkoxy, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkylthio group or optionally substituted hydrazine demonstrate histolytic and tumor-resolving activity. The compounds are prepared by either hydrolyzing or aminolyzing the corresponding 2,4-disubstituted 5(4H)-oxazolones.
摘要翻译：作为一个末端取代基，任选取代的烷基或烯基，任选取代的芳基，任选取代的杂环基，任选取代的芳烷基或芳烯基或氨基甲酰基并且作为另一个末端取代基的羟基或氨基，任选取代的烷基氨基任选取代的芳基氨基，任选取代的芳烷基氨基，任选取代的含氮杂环基与五或六个环成员任选地含有另外的杂原子，任选取代的芳烷氧基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷硫基或任选取代的肼表明组织溶解和肿瘤分解活性。通过水解或氨基化相应的2,4-二取代的5（4H） - 恶唑酮来制备化合物。

66. 发明授权

US4098792A Substituted pyridine carboxylic acids and derivatives 失效
标题翻译：取代的吡啶羧酸及其衍生物
公开(公告)号：US4098792A
公开(公告)日：1978-07-04
申请号：US817330
申请日：1977-07-20
申请人： Lennon H. McKendry
发明人： Lennon H. McKendry
IPC分类号： C07D213/80 , C07D213/54
CPC分类号： C07D213/80
摘要： Disclosed are pyridinecarboxylic acids and derivatives thereof which are useful as intermediates for the preparation of 1H-pyrido(2,3-c or 4,3-c)(1,2,6)thiadiazin-4(3H)-one-2,2-dioxide compounds and derivatives thereof which are useful as herbicides.
摘要翻译：公开了可用作制备1H-吡啶并（2,3-c或4,3-c）（1,2,6）噻二嗪-4（3H） - 酮-2的中间体的吡啶羧酸及其衍生物，可用作除草剂的二氧化物化合物及其衍生物。

67. 发明授权

US3952101A .alpha.-Amino methyl-5-hydroxy-2-pyridinemethanols 失效
标题翻译： {60-氨基甲基-5-羟基-2-吡啶甲醇
公开(公告)号：US3952101A
公开(公告)日：1976-04-20
申请号：US568079
申请日：1975-04-14
申请人： Timothy Yu-Wen Jen , Carl Kaiser
发明人： Timothy Yu-Wen Jen , Carl Kaiser
IPC分类号： C07D213/65 , C07D213/38 , C07D213/48 , C07D213/54 , C07D405/12 , A61K31/44
CPC分类号： C07D213/54 , C07D213/38 , C07D213/48 , Y02P20/55
摘要： .alpha.-Aminomethyl-5-hydroxy-2-pyridinemethanols having .beta.-adrenergic stimulant activity, particularly as selective bronchodilators, are prepared generally from a 2-pyridine-carboxaldehyde by reaction with an appropriate isocyanide, via an amide intermediate followed by reduction to an amine and finally catalytic hydrogenation to remove benzyl protective groups.
摘要翻译：具有β-肾上腺素能兴奋剂活性的α-氨基甲基-5-羟基-2-吡啶甲醇，特别是作为选择性支气管扩张药通常由2-吡啶 - 甲醛通过与适当的靛蓝反应，经酰胺中间体然后还原成胺最后进行催化氢化除去苄基保护基。

68. 发明授权

US3914239A Certain 5-lower-alkyl-pyridine-2-carboxylates 失效
标题翻译：某些5-低级烷基 - 吡啶-2-羧酸盐
公开(公告)号：US3914239A
公开(公告)日：1975-10-21
申请号：US33114773
申请日：1973-02-09
申请人： CIBA GEIGY CORP
发明人： KUHNIS HANS , EGLI CHRISTIAN , EICHENBERGER KURT , HEDWALL PHYLLIS ROBERTA
IPC分类号： C07D213/64 , A61K20060101 , A61K31/44 , C07D20060101 , C07D211/00 , C07D213/00 , C07D213/54 , C07D213/55 , C07D213/61 , C07D213/63 , C07D213/68 , C07D213/79 , C07D213/81 , C07D213/83 , C07D213/89 , C07D401/04
CPC分类号： C07D213/89 , C07D213/61 , C07D213/63 , C07D213/79 , C07D213/81 , C07D213/83
摘要： Pyridines of the formula I

wherein R1 is free hydroxyl, lower alkoxy, cycloalkoxy, aminolower alkoxy or lower alkoxy-lower alkoxy, free amino, hydroxyamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino or mono- or di-lower alkylamino, R2 is oxygen or sulphur, R3 and R4 are each alkoxy, free amino, mono- or di-lower alkylamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino, halogen or free hydroxyl, and either R3 or R4 can be hydrogen, and alk is an alkyl group with 3-10 carbon atoms, and their N-oxides, and salts are useful as dopamine- Beta hydroxylase inhibitors.
摘要翻译：式I的吡啶，其中R1是游离羟基，低级烷氧基，环烷氧基，氨基 - 低级烷氧基或低级烷氧基 - 低级烷氧基，游离氨基，羟基氨基，低级亚烷基氨基，氧杂 - ，氮杂 - 或硫代 - 低级亚烷基氨基或单或二低级烷基氨基，R2是氧或硫，R3和R4分别是烷氧基，游离氨基，一或二低级烷基氨基，低级亚烷基氨基，氧杂 - ，氮杂 - 或硫代 - 低级亚烷基氨基，卤素或游离羟基，R3 或R4可以是氢，alk是具有3-10个碳原子的烷基，它们的N-氧化物和盐可用作多巴胺-β-羟化酶抑制剂。

69. 发明申请

US20220162197A1 MYST FAMILY HISTONE ACETYLTRANSFERASE INHIBITORS 有权
公开(公告)号：US20220162197A1
公开(公告)日：2022-05-26
申请号：US16766890
申请日：2018-11-29
申请人： Epizyme, Inc.
发明人： Darren Martin Harvey , John Emmerson Campbell , Kenneth William Duncan
IPC分类号： C07D405/12 , C07D401/12 , C07D405/14 , C07D417/12 , C07D403/12 , C07D413/12 , C07D403/14 , C07D401/14 , C07D205/04 , C07D207/08 , C07D211/24 , C07D213/54 , C07D223/04 , C07D231/12 , C07D233/64 , C07D241/04 , C07D257/04 , C07D265/30 , C07C311/49
摘要： The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

70. 发明申请

US20210371383A1 PYRIDIN-2-YL ALKYLAMINO SUBSTITUTED HYDROXAMIC ACID AND USES THEREOF 有权
公开(公告)号：US20210371383A1
公开(公告)日：2021-12-02
申请号：US16979503
申请日：2019-03-12
申请人： HAWAII BIOTECH, INC.
发明人： Guan-Sheng JIAO , Seong Jin KIM , Alan T. JOHNSON
IPC分类号： C07D213/65 , C07D213/61 , C07D213/54
摘要： Compounds of formula I are provided: wherein X is NH, or CH2, Y is a single bond, or —CHR5—, R1 is H, C1-C4 alkyl, or C1-C4 hydroxyalkyl, R2 and R2′ are each independently H, C1-C4 alkyl, or C1-C4 hydroxyalkyl, each R3 is independently H, halo, —CF3, C1-C4 alkyl, or C1-C4 alkoxy, C3 perhaloalkyl, each R4 is independently H, halo, or C1-C4 alkyl, R5 is C1-C4 alkoxy, r is integer from 0 to 3; and p is integer from 0 to 3.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式