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21. 发明授权

US5654468A Heteroacetic acid derivatives 失效
标题翻译：异丁酸衍生物
公开(公告)号：US5654468A
公开(公告)日：1997-08-05
申请号：US680731
申请日：1996-07-15
申请人： Naokata Yokoyama, deceased , Gordon Northrop Walker , Alan Joseph Main
发明人： Naokata Yokoyama, deceased , Gordon Northrop Walker , Alan Joseph Main
IPC分类号： A61K31/165 , A61P3/06 , C07C41/00 , C07C229/18 , C07C229/36 , C07C233/56 , C07C235/72 , C07C323/37 , C07C323/52 , C07J41/00 , C07C229/00
CPC分类号： C07C323/52 , C07C229/18 , C07C229/36 , C07C233/56 , C07J41/0055
摘要： Disclosed are compounds of formula ##STR1## wherein R is hydroxy, esterified hydroxy or etherified hydroxy;R.sub.1 is halogen, trifluoromethyl or lower alkyl;R.sub.2 is halogen, trifluoromethyl or lower alkyl;R.sub.1 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalokyl or cycloalkyl-lower alkyl; orR.sub.3 is the radical ##STR2## wherein R.sub.8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkil-lower alkyl; R.sub.9 is hydroxy or acyloxy; R.sub.10 represents hydrogen or lower alkyl; or R.sub.9 and R.sub.10 together represent oxo;R.sub.4 is hydrogen, halogen, trifluoromethyl or lower alkyl;X is --NR.sub.7, S or O;W is O or S;R.sub.5 represents hydrogen, lower alkyl or aryl-lower alkyl; andR.sub.6 represents hydrogen; orR.sub.5 and R.sub.6 together represent oxo provided that X represents --NR.sub.7 ;R.sub.7 represents hydrogen or lower alkyl;Z represents carboxyl, carboxyl derivatized as a pharmaceutically acceptable ester or as a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; which are useful as hypocholesteremic agents.
摘要翻译：公开了式（I）的化合物，其中R是羟基，酯化的羟基或醚化的羟基; R1是卤素，三氟甲基或低级烷基; R2是卤素，三氟甲基或低级烷基; R1是卤素，三氟甲基，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基 - 低级烷基; 或R3是基团，其中R8是氢，低级烷基，芳基，环烷基，芳基 - 低级烷基或环烷基 - 低级烷基; R9是羟基或酰氧基; R 10表示氢或低级烷基; 或R 9和R 10一起代表氧代; R4是氢，卤素，三氟甲基或低级烷基; X是-NR 7，S或O; W为O或S; R5代表氢，低级烷基或芳基 - 低级烷基; R6代表氢; 或者R 5和R 6一起代表氧代，条件是X代表-NR7; R7代表氢或低级烷基; Z表示羧基，羧基衍生化为药学上可接受的酯或作为药学上可接受的酰胺; 及其药学上可接受的盐; 其可用作低胆固醇剂。

22. 发明授权

US5488149A Substituted amic acid derivatives 失效
标题翻译：取代的酰胺酸衍生物
公开(公告)号：US5488149A
公开(公告)日：1996-01-30
申请号：US471081
申请日：1995-06-06
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07C235/72
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中每个取代基在本文中定义。

23. 发明授权

US5414122A Process for producing alpha-ketoamide derivative 失效
标题翻译：生产α-酮酰胺衍生物的方法
公开(公告)号：US5414122A
公开(公告)日：1995-05-09
申请号：US107032
申请日：1993-08-17
申请人： Akira Murabayashi , Hideyuki Takenaka , Hiroyuki Kai
发明人： Akira Murabayashi , Hideyuki Takenaka , Hiroyuki Kai
IPC分类号： C07C231/06 , C07C231/10 , C07C235/72 , C07C317/44 , C07C323/42
CPC分类号： C07C231/10
摘要： There is disclosed an efficient process for producing .alpha.-ketoacetamide of the formula: ##STR1## which is useful as an intermediate for the production of various alkoxyiminoacetamide compounds to be used for agricultural fungicides. In this process, a corresponding acid halide is condensed with isocyanide to produce the .alpha.-ketoacetamide.
摘要翻译：公开了一种制备下式的α-酮乙酰胺的有效方法：＆lt; IMAGE＆gt;其可用作制备用于农用杀真菌剂的各种烷氧基亚氨基乙酰胺化合物的中间体。在该方法中，将相应的酰卤与异氰化物缩合以产生α-酮乙酰胺。

24. 发明授权

US5387714A Process of producing intermediates for use in production of alkoxyiminoacetamides and intermediates to be used therein 失效
标题翻译：制备用于生产烷氧基亚氨基乙酰胺的中间体及其中使用的中间体的方法
公开(公告)号：US5387714A
公开(公告)日：1995-02-07
申请号：US953884
申请日：1992-09-30
申请人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
发明人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
IPC分类号： C07D215/12 , C07C51/58 , C07C59/84 , C07C59/88 , C07C59/90 , C07C227/02 , C07C229/42 , C07C231/02 , C07C233/56 , C07C235/72 , C07C235/78 , C07C237/20 , C07C249/08 , C07C319/12 , C07C319/20 , C07C323/62 , C07D215/20 , C07D215/36 , C07D239/26 , C07D239/34 , C07D239/38 , C07D239/42 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/14 , C07D263/32 , C07D263/36 , C07D263/46 , C07D263/48 , C07D263/56 , C07D263/58 , C07D277/62 , C07D303/38 , C07D413/04 , C07C55/38 , C07C59/21
CPC分类号： C07C59/84 , C07C231/02 , C07C249/08
摘要： There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.
摘要翻译：公开了一种制备用作生产可用作杀真菌剂的各种烷氧基亚氨基乙酰胺化合物的中间体的α-甲酰胺的方法。还公开了在该方法中使用的中间体。

25. 发明授权

US5204338A Oxalylamino acid derivatives and their use as medicaments for inhibiting proline hydroxylase 失效
标题翻译：氧亚氨基酸衍生物及其用作抑制甘氨酸羟化酶的药物
公开(公告)号：US5204338A
公开(公告)日：1993-04-20
申请号：US698097
申请日：1991-05-10
申请人： Ekkehard Baader , Harald Burghard , Volkmar Gunzler-Pukall
发明人： Ekkehard Baader , Harald Burghard , Volkmar Gunzler-Pukall
IPC分类号： A61K31/195 , A61K31/16 , A61K31/198 , A61K31/215 , A61K31/22 , A61K31/223 , A61K31/225 , A61K31/395 , A61K31/401 , A61P1/16 , A61P37/00 , A61P37/06 , A61P43/00 , C07C233/47 , C07C233/56 , C07C235/72 , C07C323/59 , C07D207/16 , C12N9/99
CPC分类号： C07C323/59 , C07C233/56
摘要： The invention relates to oxalylamino acid derivatives of the formula I ##STR1## in which R and R' are identical or different and are C.sub.1 -C.sub.6 -alkyl or hydrogen,R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.3 -alkoxy, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aryl, SH, NH.sub.2 or halogen, where the alkyl radicals are unsubstituted or substituted by aryl, OH, SH or NH.sub.2 orR.sup.1 and R.sup.2 together are a C.sub.2 -C.sub.4 -alkylene chain and the compounds in their predominantly pure D- and L-form and the physiologically tolerable salts.The compounds are distinguished as excellent inhibitors of prolyl hydroxylase and lysine hydroxylase.
摘要翻译：本发明涉及式Ⅰ的草酰氨基酸衍生物，其中R和R'相同或不同，为C1-C6-烷基或氢，R1为氢或C1-C4-烷基，R2为氢，C1- C 1 -C 6烷基，C 1 -C 3 - 烷氧基，羧基，C 1 -C 6 - 烷氧基羰基，芳基，SH，NH 2或卤素，其中烷基是未取代的或被芳基，OH，SH或NH 2取代或者R 1和R 2一起是C 2 -C4-亚烷基链和其主要为纯的D-和L-形式的化合物和生理上可耐受的盐。该化合物被认为是脯氨酰羟化酶和赖氨酸羟化酶的优异抑制剂。

26. 发明授权

US4564623A Aminoalkylbenzene derivatives 失效
标题翻译：氨基烷基苯衍生物
公开(公告)号：US4564623A
公开(公告)日：1986-01-14
申请号：US573685
申请日：1984-01-25
申请人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
发明人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
IPC分类号： C07D295/18 , A61K31/16 , A61K31/165 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/4245 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/455 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07C67/00 , C07C231/00 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/60 , C07C233/69 , C07C235/20 , C07C235/48 , C07C235/72 , C07C237/08 , C07C237/32 , C07C237/42 , C07C239/00 , C07C261/04 , C07C301/00 , C07C311/18 , C07C313/00 , C07C323/29 , C07C323/39 , C07C323/41 , C07C325/00 , C07C327/40 , C07C327/46 , C07C327/48 , C07C327/50 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D249/10 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/08 , C07D295/096 , C07D295/14 , C07D295/15 , C07D307/68 , C07D333/38 , C07D335/06 , C07D498/04 , C07D207/04
CPC分类号： C07D213/81 , C07C323/29 , C07D207/16 , C07D207/28 , C07D213/82 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/096 , C07D295/15 , C07D333/38 , C07D335/06 , Y10S514/927
摘要： An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;Y is oxo, thioxo, or cyanoimino;a is an integer of 1 to 3;b is an integer of 0 to 3;c is an integer of 1 to 4;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl; orR.sup.1 and R.sup.2 taken together represent pyrrolidinyl;R is hydrogen, cycloaklkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: ##STR2## (wherein R.sup.3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy;R.sup.4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; orR.sup.3 and R.sup.4 taken together represent alkylidene or aralkylidene);with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents] and its pharmaceutically acceptable acid addition salts being useful as histamine H.sub.2 blockers, especially peptic ulcer remedies, are provided via several routes.

27. 发明授权

US4559371A Photocurable colored compositions employing alpha-amino phenone initiator 失效
标题翻译：使用α-氨基苯酮引发剂的光固化着色组合物
公开(公告)号：US4559371A
公开(公告)日：1985-12-17
申请号：US579622
申请日：1984-02-13
申请人： Rinaldo Husler , Rudolf Kirchmayr , Werner Rutsch
发明人： Rinaldo Husler , Rudolf Kirchmayr , Werner Rutsch
IPC分类号： C07D319/24 , C07C45/46 , C07C45/63 , C07C49/84 , C07C67/00 , C07C225/16 , C07C225/18 , C07C229/38 , C07C235/72 , C07C255/13 , C07C301/00 , C07C309/63 , C07D217/20 , C07D265/30 , C07D295/10 , C07D295/108 , C07D303/48 , C07D307/91 , C07F7/18 , C08F2/00 , C08F2/50 , C09D11/10 , G03F7/031
CPC分类号： C07D295/108 , C07C45/46 , C07C45/63 , C07C49/84 , C07D303/48 , C07D307/91 , C08F2/50 , G03F7/031
摘要： Compounds of the formula I, II or III ##STR1## in which Ar and Ar' are an oxygen-containing aromatic radical, R.sup.1 and R.sup.2 are a monovalent hydrocarbon radical which is substituted or unsubstituted, or R.sup.1 and R.sup.2 together form alkylene, oxaalkylene or azaalkylene, R.sup.3 is a direct bond or a divalent hydrocarbon radical, X and X' are a monovalent amino group and Y is a divalent amino or diamino group, are excellent photoinitiators for the photocuring of colored, especially pigmented, compositions containing an olefinically unsaturated, photopolymerizable binder.
摘要翻译：其中Ar和Ar'是含氧芳族基团的式I，II或III化合物其中R 1和R 2是一价烃基，其中是取代或未取代的，或者R 1和R 2一起形成亚烷基，氧杂亚烷基或氮杂亚烷基，R 3是直接键或二价烃基，X和X'是一价氨基，Y是二价氨基或二氨基，是优异的光引发剂用于对含有烯属不饱和的可光聚合粘合剂的着色的，特别是着色的组合物的光固化。

28. 发明授权

US4370498A Preparation of .alpha.-ketocarboxylic acid N-acylamides 失效
标题翻译： α-酮羧酸N-酰基酰胺的制备
公开(公告)号：US4370498A
公开(公告)日：1983-01-25
申请号：US235497
申请日：1981-02-19
申请人： Gerhard Bonse , Heinz U. Blank
发明人： Gerhard Bonse , Heinz U. Blank
IPC分类号： C07D253/06 , B01J27/00 , B01J27/02 , C07B61/00 , C07C51/06 , C07C67/00 , C07C231/00 , C07C231/06 , C07C235/72 , C07C235/88 , C07D253/075 , C07C102/08 , C07C103/147 , C07C103/19 , C07C103/24
CPC分类号： C07D253/075 , C07C51/06
摘要： .alpha.-Ketocarboxylic acid N-acylamides of the formulaR.sup.1 --CO--CO--NH--CO--R.sup.2in whichR.sup.1 is an optionally substituted aliphatic radical with up to 12 carbon atoms, an optionally substituted cycloalkyl radical with 3 to 10 carbon atoms, an optionally substituted heterocyclic radical, andR.sup.2 is an optionally substituted aliphatic radical with up to 8 carbon atoms or an optionally substituted phenyl radical,are prepared by reacting an acyl cyanide of the formulaR.sup.1 --CO--CNwith a carboxylic acid anhydride of the formulaR.sup.2 --CO--O--CO--R.sup.2in the presence of a strong acid, and then adding water to the reaction mixture. The products can be used directly in the synthesis of known herbicides.
摘要翻译：式R1-CO-CO-NH-CO-R2的α-甲基羧酸N-酰基酰胺，其中R 1是具有至多12个碳原子的任选取代的脂族基，任选取代的具有3至10个碳原子的环烷基，任选取代的杂环基，并且R 2是具有至多8个碳原子的任选取代的脂族基团或任选取代的苯基，通过使式R 1 -CO-CN的酰基氰与式R 2的羧酸酐反应制备 -CO-O-CO-R 2，然后向反应混合物中加入水。该产品可直接用于合成已知除草剂。

29. 发明授权

US4228082A N-Substituted .alpha.-ketocarboxylic acid amides 失效
标题翻译： N-取代的α-酮羧酸酰胺
公开(公告)号：US4228082A
公开(公告)日：1980-10-14
申请号：US56084
申请日：1979-07-09
申请人： Axel Kleemann , Herbert Klenk , Heribert Offermanns , Paul Scherberich , Werner Schwarze
发明人： Axel Kleemann , Herbert Klenk , Heribert Offermanns , Paul Scherberich , Werner Schwarze
IPC分类号： A01N25/00 , A01P3/00 , A01P13/00 , C07C67/00 , C07C231/00 , C07C231/06 , C07C231/08 , C07C235/72 , C07D307/54 , C07C103/737 , C07C103/76
CPC分类号： C07D307/54
摘要： Compounds are prepared of the formula ##STR1## where R' is a t-alkyl group having 4 to 18 carbon atoms, preferably t-butyl, t-amyl or t-octyl and R is a straight or branched chain alkyl group with 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms or an alkyl group substituted with one or more phenyl group or a halogen atom, particularly a chlorine atom, or a cycloalkyl group with 3 to 8 carbon atoms, particularly cyclopropyl, which can be substituted by one or more 1 to 3 carbon atom alkyl groups or one or more halogen atoms, preferably chlorine, or phenyl or naphthyl or a five membered heterocyclic group or such phenyl, naphthyl or heterocyclic group substituted by halogen atoms, nitro groups, alkyl or alkoxy with 1 to 5 carbon atoms by condensing in acid medium an acyl cyanide of the formulaR--CO--CN (II)where R is as defined above with either(a) a tertiary alcohol of the formulaHO--R' (III) in which R' is as defined above, or preferably(b) an alkene of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are hydrogen or an alkyl group and wherein R.sub.3 and R.sub.4 are the same or different and wherein the alkyl groups in each case can be 1 to 15 carbon atoms. Some of the compounds are new. They are useful as intermediates for synthesizing herbicides and can be used directly as fungicides.
摘要翻译：化合物由式（I）制备，其中R'是具有4至18个碳原子的叔烷基，优选叔丁基，叔戊基或叔辛基，R是直链或支链烷基具有1至18个碳原子，优选1至10个碳原子的烷基或被一个或多个苯基或卤素原子，特别是氯原子或具有3至8个碳原子的环烷基特别是环丙基取代的烷基，其可以被一个或多个1至3个碳原子的烷基或一个或多个卤素原子，优选氯，或苯基或萘基或五元杂环基或被卤素原子取代的苯基，萘基或杂环基，硝基，烷基或具有1至5个碳原子的烷氧基，通过在酸性介质中缩合式R-CO-CN（II）的酰基氰，其中R如上定义，与（a）式HO-R'（III ），其中R'如上所定义，或优选（b）下式的烯烃（I） V）其中R 1和R 2相同或不同并且是氢或烷基，并且其中R 3和R 4相同或不同，并且其中每种情况下的烷基可以是1至15个碳原子。一些化合物是新的。它们可用作合成除草剂的中间体，可直接用作杀真菌剂。

30. 发明申请

US20090062284A1 Thio-Substituted Biarylmethanesulfinyl Derivatives 有权
标题翻译：硫取代的二芳基甲亚磺酰基衍生物
公开(公告)号：US20090062284A1
公开(公告)日：2009-03-05
申请号：US12199167
申请日：2008-08-27
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg A. Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg A. Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/381 , C07D333/24 , C07D307/54 , C07D409/12 , C07D405/12 , C07D401/12 , C07D413/12 , C07D209/44 , C07C235/72 , A61K31/496 , A61K31/40 , A61K31/4025 , A61K31/5377 , A61P25/00
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病阿尔茨海默氏病; 注意力缺陷障碍注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。

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