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61. 发明授权

US5773284A Phenylserine amides and the preparation of phenylserines/phenylserine amides 失效
标题翻译：苯基丝氨酸酰胺和苯基丝氨酸/苯基丝氨酸酰胺的制备
公开(公告)号：US5773284A
公开(公告)日：1998-06-30
申请号：US662797
申请日：1996-06-12
申请人： Bernardus Kaptein
发明人： Bernardus Kaptein
IPC分类号： A61K31/165 , C07C315/04 , C07C317/46 , C07C317/48 , C07C319/20 , C07C323/41 , C07C323/45 , C07C323/63 , C12P13/04 , C12P41/00 , C12P13/06 , C07B55/00 , C12N9/78 , C12P7/40
CPC分类号： C12P41/006 , C07C315/04 , C07C317/48 , C07C319/20 , C07C323/41 , C07C323/63 , C12P13/04
摘要： Process for the preparation of a threo-phenylserine amide of the general formula 2 in which glycine amide is contacted with the corresponding substituted benzaldehyde of formula 3 in an excess relative to the amount of glycine amide, this taking place at a pH between 9 and 14 in the presence of a suitable solvent. The resulting phenylserine amide can subsequently be hydrolyzed to a phenylserine amide of the general formula 1, which is subsequently hydrolyzed to a phenylserine amide of the general formula 1, which is subsequently subjected to a stereoselective enzymatic hydrolysis yielding a (2S,3R) phenylserine. The non-hydrolyzed (2R,3S) phenylserine amide can be isolated as a Schiff base and be recirculated and simply racemized. The (2S,3R) phenylserine obtained can be used in the preparation of thiamphenicol or florfenicol. The threo-phenylserine amides of the general formula 1 or 2 are new intermediates in this commercially attractive process for the preparation of thiamphenicol and florfenicol.
摘要翻译：制备通式2的苏氨基丝氨酸酰胺的方法，其中甘氨酰胺与相应的取代的式3的取代的苯甲醛相对于甘氨酸酰胺的量相对过量，其发生在9-14之间的pH 在合适的溶剂存在下。随后将所得苯基丝氨酰胺水解成通式1的苯基丝氨酰胺，随后将其水解成通式1的苯基丝氨酰胺，随后将其进行立体选择性酶水解，得到（2S，3R）苯基丝氨酸。非水解的（2R，3S）苯基丝氨酸酰胺可以作为希夫碱分离并进行再循环并简单地外消旋化。获得的（2S，3R）苯基丝氨酸可用于制备甲砜霉素或氟苯尼考。通式1或2的苏氨基丝氨酸酰胺是制备硫代吗啉和氟苯尼考的商业上有吸引力的方法的新中间体。

62. 发明授权

US5629441A 2-(arylimino-methyl)-3-dialkylaminoacrylonitriles, a process for their preparation and their use 失效
标题翻译： 2-（芳基亚氨基 - 甲基）-3-二烷基氨基丙烯腈，其制备方法及其应用
公开(公告)号：US5629441A
公开(公告)日：1997-05-13
申请号：US514277
申请日：1995-08-11
申请人： Helmut Kraus , Horst Behre , Helmut Fiege
发明人： Helmut Kraus , Horst Behre , Helmut Fiege
IPC分类号： C07D213/74 , C07C253/30 , C07C255/61 , C07C319/20 , C07C323/45 , C07D239/28 , C07C255/00
CPC分类号： C07D239/28 , C07C255/61
摘要： 2-(Arylimino-methyl)-3-dialkylaminoacrylonitriles can be obtained by reaction of .beta.-anilino-acrylonitriles with ortho-formamides. They are suitable as starting substances for the preparation of 4-amino-5-iminiummethylene-2-pyrimidines or 4-amino-5-formyl-2-pyrimidines.
摘要翻译： 2-（芳基亚氨基 - 甲基）-3-二烷基氨基丙烯腈可以通过β-苯胺基丙烯腈与邻甲酰胺的反应获得。它们适用于制备4-氨基-5-亚氨基亚甲基-2-嘧啶或4-氨基-5-甲酰基-2-嘧啶的起始物质。

63. 发明授权

US5583249A Pesticides 失效
标题翻译：农药
公开(公告)号：US5583249A
公开(公告)日：1996-12-10
申请号：US460175
申请日：1995-06-02
申请人： Albert Pfifner , Stephen Trah
发明人： Albert Pfifner , Stephen Trah
IPC分类号： C07D295/14 , A01N37/36 , A01N37/50 , A01N37/52 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/30 , A01N43/42 , A01N43/52 , A01N43/54 , A01N43/60 , A01N43/78 , A01N43/84 , A01N55/00 , C07C69/734 , C07C251/60 , C07C255/61 , C07C311/16 , C07C317/26 , C07C323/45 , C07C327/42 , C07C327/48 , C07D207/335 , C07D213/53 , C07D213/61 , C07D213/84 , C07D215/12 , C07D217/02 , C07D235/14 , C07D265/30 , C07D271/12 , C07D277/20 , C07D277/50 , C07D279/12 , C07D285/10 , C07D307/52 , C07D307/79 , C07D307/81 , C07D311/68 , C07D317/58 , C07D317/60 , C07D319/18 , C07D333/22 , C07D333/28 , C07D333/38 , C07D333/58 , C07D521/00 , C07F7/12 , C07C229/36 , C07C69/76
CPC分类号： A01N37/50 , A01N37/36 , C07C251/60 , C07C69/734 , C07D317/58 , C07C2101/02
摘要： Compounds of formula I are suitable for controlling and preventing infestation by microorganisms, insects and acarina on plants ##STR1## and their possible isomers and mixtures of isomers, whereina) X is CH.sub.2 F or CHF.sub.2, Y is CH and Z is OCH.sub.3, orb) X is CH.sub.2 F or CHF.sub.2, Y is a nitrogen atom and Z is OCH.sub.3 or NHCH.sub.3,and wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen, cyano, C.sub.1 -C.sub.12 alkyl, halo-C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, cyclopropylmethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.12 alkoxyalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylthio, C.sub.2 -C.sub.5 alkylthioalkyl; or an unsubstituted or mono- to tri-substituted ring having not more than 15 ring carbon atoms that may be multi-membered and that contains from 0 to 3 hetero atoms N, O or S, it being possible for that ring to be bonded via an aliphatic bridge having not more than 4 carbon atoms and/or via CO, oxygen or sulfur, as desired; orwherein R.sub.1 and R.sub.2 together with their common carbon atom form an unsubstituted or mono- to tri-substituted ring having not more than 15 ring carbon atoms that may be multi-membered and that contains from 0 to 3 hetero atoms N, O or S.They can be used in the form of commercially customary formulated compositions.
摘要翻译：式I化合物适用于控制和防止植物上的微生物，昆虫和螨虫侵染及其可能的异构体和异构体混合物，其中a）X是CH 2 F或CHF 2，Y是CH，Z是OCH 3 ，或b）X是CH 2 F或CHF 2，Y是氮原子，Z是OCH 3或NHCH 3，并且其中R 1和R 2各自独立地是氢，氰基，C 1 -C 12烷基，卤代-C 1 -C 12烷基，C 2 -C 12链烯基，C 2 -C 12炔基，C 3 -C 6环烷基，环丙基甲基，C 1 -C 4烷氧基，C 2 -C 12烷氧基烷基，C 1 -C 4烷氧基羰基，C 1 -C 4烷硫基，C 2 -C 5烷硫基烷基; 或具有不多于15个环碳原子的未取代或单 - 三取代的环，其可以是多元的并且含有0-3个杂原子N，O或S，该环可能通过根据需要具有不超过4个碳原子和/或通过CO，氧或硫的脂肪族桥; 或其中R 1和R 2与它们的共同碳原子一起形成未被取代的或一至三取代的环，其具有不多于15个可以是多元环的碳原子并且含有0-3个杂原子的N，O或S 它们可以以商业习惯配制的组合物的形式使用。

64. 发明授权

US5288727A Hydrazone compounds, processes for their production, intermediates useful for their production and pesticidal compositions containing them 失效
标题翻译：腙化合物，其制备方法，可用于其生产的中间体和含有它们的杀虫组合物
公开(公告)号：US5288727A
公开(公告)日：1994-02-22
申请号：US834835
申请日：1992-02-13
申请人： Tadaaki Toki , Toru Koyanagi , Kiyomitsu Yoshida , Hiroshi Sasaki , Masayuki Morita , Tetsuo Yoneda
发明人： Tadaaki Toki , Toru Koyanagi , Kiyomitsu Yoshida , Hiroshi Sasaki , Masayuki Morita , Tetsuo Yoneda
IPC分类号： H01L21/02 , A01N33/00 , A01N35/10 , A01N37/52 , A01N47/06 , A01N47/24 , A01N47/34 , A01N55/00 , C07C45/00 , C07C45/27 , C07C49/215 , C07C49/233 , C07C49/782 , C07C49/813 , C07C249/16 , C07C251/08 , C07C251/72 , C07C251/86 , C07C251/88 , C07C257/02 , C07C257/06 , C07C257/22 , C07C281/04 , C07C281/14 , C07C303/30 , C07C303/40 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/49 , C07C317/32 , C07C319/20 , C07C323/45 , C07C323/48 , C07C323/65 , C07F7/18 , C07F9/09 , H01L21/677 , H01L21/68 , C07C251/80 , A01N47/40
CPC分类号： C07C323/65 , A01N35/10 , A01N37/52 , A01N47/06 , A01N47/24 , A01N47/34 , A01N55/00 , C07C251/86 , C07C251/88 , C07C257/06 , C07C257/22 , C07C281/04 , C07C281/14 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/49 , C07C317/32 , C07C323/45 , C07C45/004 , C07C45/27 , C07C49/782 , C07C49/813
摘要： The present invention relates to a hydrazone compound of the formula (I) or its salt, a process for its preparation, an intermediate of the formula (II-5), a pesticidal composition containing said hydrazone compound or its salt as the active ingredient, and a pesticidal method of applying an effective amount thereof: ##STR1##
摘要翻译：本发明涉及式（I）的腙化合物或其盐，其制备方法，式（II-5）的中间体，含有所述腙化合物或其盐作为活性成分的杀虫组合物，（*化学结构*）（I）（*化学结构*）（II-5）的有效量的杀虫剂法

65. 发明授权

US4699919A Lipoxygenase and cyclogenase inhibiting thiachromen and thiepan derivatives and pharmaceutical compositions therefor 失效
标题翻译：脂氧合酶和环化酶抑制thiromromen和thiepan衍生物及其药物组合物
公开(公告)号：US4699919A
公开(公告)日：1987-10-13
申请号：US908407
申请日：1986-09-16
申请人： Michel Follet , Marc Bonato
发明人： Michel Follet , Marc Bonato
IPC分类号： C12N9/99 , A61K31/095 , A61K31/10 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/235 , A61K31/38 , A61K31/382 , A61K45/06 , A61P7/02 , A61P7/06 , A61P9/08 , A61P9/10 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/20 , C07C323/45 , C07C323/62 , C07D335/04 , C07D335/06 , C07D337/08 , C07D337/12 , C07D521/00
CPC分类号： C07D335/06 , A61K31/10 , C07C323/00 , C07D337/08
摘要： This invention relates to bicyclic catechol derivatives having the general formulae I and II ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and Z represent various substituents, to a preparation process of the same comprising reacting a compound of formula III ##STR2## wherein R.sub.1 and R.sub.2 have the meanings given above with an appropriately substituted propionic or butyric acid (or an ester or a salt of the same) of formula IV ##STR3## wherein R.sub.3 has the meaning given above, and to therapeutical compositions wherein the active ingredient is one of these compounds.
摘要翻译：本发明涉及具有通式I和II的双环类邻苯二酚衍生物，其中R1，R2，R3和Z代表各种取代基，涉及其制备方法，包括使式III化合物

66. 发明授权

US4250092A Derivatives of N-cyano-azomethines and process for their preparation 失效
标题翻译： N-氰基偶氮甲碱的衍生物及其制备方法
公开(公告)号：US4250092A
公开(公告)日：1981-02-10
申请号：US38838
申请日：1979-05-14
申请人： Franjo Kajfez
发明人： Franjo Kajfez
IPC分类号： C07C261/04 , C07C20060101 , C07C67/00 , C07C239/00 , C07C253/30 , C07C255/61 , C07C313/00 , C07C323/25 , C07C323/45 , C07D203/12 , C07D203/20 , C07D233/64 , C07C125/08
CPC分类号： C07D203/12
摘要： N-Cyano-azomethines, useful as intermediates for the production of antihistamines are described. They are produced by reaction of ##STR1## where R.sub.3 is a thiomethyl group, an alkylamino group or N-1-amino-.omega.-alkylthiomethyl group, with primary or secondary alkyl- or hydroxyalkyl-amines or with ethylenimine.
摘要翻译：描述了可用作生产抗组胺剂的中间体的N-氰基 - 偶氮甲碱。它们通过＆lt; IMAGE＆gt;其中R3是硫代甲基，烷基氨基或N-1-氨基-ω-烷基硫代甲基与伯或仲烷基 - 或羟基烷基 - 胺或与亚乙基亚胺反应制备。

67. 发明授权

US4191776A Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US4191776A
公开(公告)日：1980-03-04
申请号：US852714
申请日：1977-11-18
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C147/107 , A61K31/235 , A61K31/44 , C07C147/14
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, methyl, methoxy, methylthio or cyano;R.sub.2 is hydrogen or fluorine;R.sub.3 is carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl or pyridyl-methoxy-carbonyl,A is (alkyl of 1 to 3 carbon atoms)-methylene,m is 1 or 2; andn is 0, 1, 2 or 3;and, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：其中R 1是氢，氟，氯，溴，甲基，甲氧基，甲硫基或氰基的式 R2是氢或氟; R 3为羧基，（碳原子数1〜6的烷氧基） - 羰基，甲氧基 - （1〜6个碳原子的烷氧基） - 羰基，（2〜6个碳原子的烯氧基） - 羰基，（碳原子数为7〜12）） - 羰基，苯氧基 - 羰基或吡啶基 - 甲氧基 - 羰基，A是（1至3个碳原子的烷基） - 亚甲基，m是1或2; 并且n为0,1,2或3; 并且当R 3为羧基时，其无毒盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

68. 发明授权

US3993683A Biphenylyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US3993683A
公开(公告)日：1976-11-23
申请号：US577169
申请日：1975-05-14
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C149/40
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, fluorine, bromine, methyl, methoxy, methylthio, nitro, cyano or, when A is other than methylene, R.sub.2 is hydrogen, R.sub.3 is carboxyl, m is 2 and n is 0, also chlorine;R.sub.2 is hydrogen or fluorine;R.sub.3 is hydrogen, methyl, hydroxymethyl, carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl, pyridylmethoxy-carbonyl, amino-carbonyl, (alkyl of 1 to 3 carbon atoms-amino)-carbonyl, (dialkyl of 1 to 3 carbon atoms-amino)-carbonyl, phenylamino-carbonyl, morpholino-carbonyl, piperidino-carbonyl, thiomorpholino-carbonyl, (1-oxidothiomorpholino)-carbonyl or (1,1-dioxido-thiomorpholino)-carbonyl;A is methylene, (alkyl of 1 to 3 carbon atoms)-methylene, di-(alkyl of 1 to 3 carbon atoms)-methylene, hydroxymethyl-methylene, hydroxymethylene or carbonyl;m is 1 or 2; andn is 0, 1, 2 or 3;And, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：式A的化合物是氢，氟，溴，甲基，甲氧基，甲硫基，硝基，氰基，或当A不是亚甲基时，R 2是氢，R 3是羧基，m是2，n是0，也是氯; R2是氢或氟; R 3是氢，甲基，羟甲基，羧基，（1至6个碳原子的烷氧基） - 羰基，甲氧基 - （1至6个碳原子的烷氧基） - 羰基，（2至6个碳原子的链烯氧基） - 羰基 7至12个碳原子的羰基，苯氧基 - 羰基，吡啶基甲氧羰基，氨基 - 羰基，（1至3个碳原子的烷基 - 氨基） - 羰基，（1至3个碳原子的二烷基 - 氨基） - 羰基，苯基氨基羰基，吗啉代羰基，哌啶子基 - 羰基，硫代吗啉代羰基，（1-氧硫基吗啉代）羰基或（1,1-二氧化硫代吗啉代）羰基。 A是亚甲基，（1至3个碳原子的烷基） - 亚甲基，二（1至3个碳原子的烷基） - 亚甲基，羟甲基 - 亚甲基，羟基亚甲基或羰基; M IS 1 OR 2; 和N是0,1,2或3; 当R 3为羧基时，其无机盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

69. 发明授权

US3901945A 1,1a,6,10b-tetrahydrodibenzo (a,e) cyclopropa (c) cyclohepten-6-imines 失效
标题翻译： 1,1A,6,10B-四氢苯并噻唑（A，E）环丙基（C）环己基-6-氨基
公开(公告)号：US3901945A
公开(公告)日：1975-08-26
申请号：US38962973
申请日：1973-08-21
申请人： DU PONT
发明人： UYEDA ROY TERUYUKI
IPC分类号： C08K5/00 , C07C67/00 , C07C209/00 , C07C211/44 , C07C241/00 , C07C251/22 , C07C301/00 , C07C303/40 , C07C311/37 , C07C313/00 , C07C315/04 , C07C317/32 , C07C323/45 , C07C323/65 , C07C323/67 , C08K5/29 , C08L1/00 , C08L27/00 , C07C119/00
CPC分类号： C08K5/29 , C08L27/06
摘要： 6-(Substituted imino)-1,1a,6,10b-tetrahydrodibenzo(a, e)cyclopropa(c)cycloheptenes are plasticizers for polyvinyl chloride polymers. Some of the compounds also have activity in the central nervous system of warm-blooded animals.

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