公开(公告)号：US5221606A

公开(公告)日：1993-06-22

申请号：US466425

申请日：1990-03-08

Applicant: Anthony C. Richardson ,  Brian V. Smith ,  Robert G. Price ,  Percy F. Praill

Inventor： Anthony C. Richardson ,  Brian V. Smith ,  Robert G. Price ,  Percy F. Praill

IPC: C07D213/30 ,  C07D215/14 ,  C07D231/26 ,  C07D239/66 ,  C07D277/20 ,  C07D277/36 ,  C07F9/6541 ,  C07H15/26 ,  C12Q1/00 ,  C12Q1/34 ,  C12Q1/42 ,  C12Q1/44

CPC classification number: C12Q1/34 ,  C12Q1/00 ,  C12Q2334/00 ,  Y10S435/975

Abstract: This invention relates to enzyme assays and substrates for use in such assays. The presence or absence of certain enzymes in vivo is a useful indicator of illness or deficiency in the organisms concerned. Enzymes are also useful in monitoring microbial growth in fermentors and in the food industry and are important in enzyme-linked immunosorbent assays (ELISA), and in the characterization of bacterial species in culture. Disclosed is a reagent for enzyme assay comprising a substrate consonant with a given enzyme to be assayed, labelled with a chromogenic group which, on action of the given enzyme, is liberated to give a colored product. Also disclosed is a kit for the assay of an enzyme comprising the reagent of the disclosed invention.

Abstract translation: PCT No.PCT / GB88 / 00737 Sec。 371 1990年3月8日第 102（e）1990年3月8日PCT PCT日期：1988年9月7日PCT公布。 第WO89 / 02473号公报 1989年3月23日。本发明涉及用于这种测定的酶测定和底物。 体内某些酶的存在或不存在是有关生物相关疾病或缺陷的有用指标。 酶还可用于监测发酵罐和食品工业中的微生物生长，并且在酶联免疫吸附测定（ELISA）和培养中细菌种类的表征中是重要的。 公开了用于酶测定的试剂，其包括与要测定的给定酶的底物辅音，用显色基团标记，所述显色基团在给定酶的作用下被释放以产生有色产物。 还公开了用于测定包含本发明的试剂的酶的试剂盒。

公开(公告)号：US5210312A

公开(公告)日：1993-05-11

申请号：US709874

申请日：1991-06-04

Applicant: Glynn Mitchell

Inventor： Glynn Mitchell

IPC: A01N35/06 ,  A01N37/08 ,  A01N43/08 ,  A01N43/10 ,  A01N43/30 ,  A01N43/32 ,  A01N43/36 ,  A01N43/38 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C45/51 ,  C07C45/54 ,  C07C45/60 ,  C07C45/67 ,  C07C45/72 ,  C07C49/403 ,  C07C49/713 ,  C07C49/792 ,  C07C49/813 ,  C07C49/835 ,  C07C49/84 ,  C07D207/32 ,  C07D207/333 ,  C07D207/36 ,  C07D209/12 ,  C07D215/14 ,  C07D215/36 ,  C07D231/12 ,  C07D231/16 ,  C07D233/84 ,  C07D237/12 ,  C07D241/12 ,  C07D241/16 ,  C07D241/42 ,  C07D261/08 ,  C07D263/56 ,  C07D277/24 ,  C07D277/32 ,  C07D277/36 ,  C07D307/70 ,  C07D307/71 ,  C07D317/52 ,  C07D317/62 ,  C07D319/08 ,  C07D319/18 ,  C07D333/22 ,  C07D333/28 ,  C07D333/62 ,  C07D409/04 ,  C07D417/04 ,  C07F9/6568

CPC classification number: C07D207/333 ,  A01N35/06 ,  A01N37/08 ,  A01N43/08 ,  A01N43/10 ,  A01N43/30 ,  A01N43/32 ,  A01N43/36 ,  A01N43/38 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C45/512 ,  C07C45/54 ,  C07C45/60 ,  C07C45/673 ,  C07C45/72 ,  C07C49/403 ,  C07C49/713 ,  C07C49/792 ,  C07C49/813 ,  C07C49/835 ,  C07D207/36 ,  C07D209/12 ,  C07D215/14 ,  C07D215/36 ,  C07D231/12 ,  C07D231/16 ,  C07D233/84 ,  C07D237/12 ,  C07D241/12 ,  C07D241/16 ,  C07D241/42 ,  C07D261/08 ,  C07D263/56 ,  C07D277/24 ,  C07D277/32 ,  C07D277/36 ,  C07D307/70 ,  C07D307/71 ,  C07D317/52 ,  C07D317/62 ,  C07D319/08 ,  C07D319/18 ,  C07D333/22 ,  C07D333/28 ,  C07D333/62 ,  C07D409/04 ,  C07D417/04 ,  C07F9/6568

Abstract: Process for the preparation of herbicidally active substituted cyclohexan-1,3,5-triones which comprises either(a) reacting a compound of formula (II) ##STR1## wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are, for example, hydrogen or C.sub.1 -C.sub.4 alkyl with a compound of formula (III):R.sup.1 COCN (III) wherein R.sup.1 is optionally substituted aryl in the presence of a base and a Lewis acid; or(b) reacting a compound of formula (VI) ##STR2## with a compound of formula (X) ##STR3## in the presence of a Lewis acid; or (c) where R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same, reacting a compound of formula (XI) ##STR4## with a compound of formula R.sup.3 X' in the presence of a base, wherein X' is a leaving group.

Abstract translation: 制备除草活性取代的环己烷-1,3,5-三酮的方法，其包括（a）使式（II）化合物其中R 2，R 3，R 4和R 5是例如， 氢或C 1 -C 4烷基与式（III）化合物反应：其中R 1为任选取代的芳基，在碱和路易斯酸存在下为R 1 COCN（III）; 或（b）在路易斯酸存在下使式（VI）化合物（VI）与式（X）化合物反应：（X） 或（c）其中R2，R3，R4和R5相同，在碱的存在下使式（XI）化合物（XI）与式R3X'化合物反应，其中X'为离去 组。

公开(公告)号：US5210093A

公开(公告)日：1993-05-11

申请号：US851926

申请日：1992-03-16

Applicant: Jean-Louis Brayer ,  Jean-Pierre Demoute ,  Gilles Mourioux

Inventor： Jean-Louis Brayer ,  Jean-Pierre Demoute ,  Gilles Mourioux

IPC: A01N43/78 ,  C07D277/20 ,  C07D277/22 ,  C07D277/30 ,  C07D277/32 ,  C07D277/34 ,  C07D277/36

CPC classification number: C07D277/32 ,  A01N43/78 ,  C07D277/30

Abstract: A compound of the formula ##STR1## wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenyl, phenoxy, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bonds independently have (E) or (Z) geometry having fungicidal activity and a process for their preparation.

Abstract translation: 式I的化合物，其中Ar是任选被至少一个由卤素，亚甲二氧基，苯基，苯氧基，-CF 3和1-6个碳原子的烷基，烷氧基和烷硫基取代的基团，Z是 选自氢，氯，-CF 3和具有1至6个碳原子的烷基，烷氧基和烷硫基，R 1和R 2分别是1至6个碳原子的烷基，并且环外双键独立地具有（E）或（Z ）几何具有杀真菌活性及其制备方法。

公开(公告)号：US5120755A

公开(公告)日：1992-06-09

申请号：US563178

申请日：1990-08-06

Applicant: Gerd Kleefeld ,  Alexander Klausener ,  Wolfgang Kramer ,  Wilhelm Brandes ,  Stefan Dutzmann ,  Gerd Hanssler

Inventor： Gerd Kleefeld ,  Alexander Klausener ,  Wolfgang Kramer ,  Wilhelm Brandes ,  Stefan Dutzmann ,  Gerd Hanssler

IPC: C07D277/20 ,  A01N43/50 ,  A01N43/74 ,  A01N43/78 ,  C07D263/38 ,  C07D263/46 ,  C07D263/48 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D277/42 ,  A01N43/50 ,  A01N43/74 ,  C07D263/48 ,  C07D277/34 ,  C07D277/36

Abstract: Fungicidal substituted acrylic acid esters of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each stand for hydrogen, alkyl, alkenyl or for in each case optionally substituted aralkyl, aralkenyl, aryl or heteroaryl,R.sup.3 stands for alkyl or for optionally substituted aralkyl,R.sup.4 stands for dialkylamino or for a radical --Z--R.sup.5,X stands for oxygen or sulphur andY stands for oxygen, sulphur or for a radical ##STR2## wherein R.sup.5 stands for alkyl or for optionally substituted aralkyl,R.sup.6 stands for hydrogen, alkyl, alkanoyl or for in each case optionally substituted aralkyl or aryl andZ stands for oxygen or sulphur.Some intermediates are also new.

公开(公告)号：US5116855A

公开(公告)日：1992-05-26

申请号：US521902

申请日：1990-05-11

Applicant: Hitoshi Inoue ,  Hiroki Kato ,  Noriyoshi Sueda ,  Yoshiyuki Tahara ,  Nobuhiro Kinoshita

Inventor： Hitoshi Inoue ,  Hiroki Kato ,  Noriyoshi Sueda ,  Yoshiyuki Tahara ,  Nobuhiro Kinoshita

IPC: C07D277/36 ,  C07D417/06 ,  C07D417/12

CPC classification number: C07D417/06 ,  C07D277/36 ,  C07D417/12

Abstract: Disclosed is a rhodanine derivative of formula (I).A rhodanine derivative of formula (I) ##STR1## wherein R.sup.1 is hdyrogen, C.sub.1 -C.sub.8 alkyl, carboxyl(C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxycarbonyl(C.sub.1 -C.sub.4)alkyl;R.sup.2 is --CH.sub.2 --CH.sub.2 --R.sup.3, CH.dbd.CH.sub.m R.sup.3 (m is 0 or 1), ##STR2## (R is C.sub.1 -C.sub.3 alkyl) or --CH.sub.2n CONHR.sup.4 (n is 0 or 1-4); R.sup.3 is a thienyl or furyl group which may be substituted by C.sub.1 -C.sub.3 alkyl or halogen; a pyrrolyl group which may be substituted by carboxy(C.sub.1 -C.sub.3)alkyl on the nitrogen atom; or a phenyl group which may be substituted by one or more substituents selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxyl, halogen, trifluoromethyl, carboxyl, (C.sub.1 -C.sub.3)alkoxycarbonyl, cyano, carboxy(C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.3)alkoxy, benzyloxycarbonyl(C.sub.1 -C.sub.3)alkoxy, piperidinylcarbonyl(C.sub.1 -C.sub.3)alkoxy, 2H-tetrazolyl, 2H-tetrazolyl-(C.sub.1 -C.sub.4)alkoxy, carboxy(C.sub.2 -C.sub.4)alkenyl, (C.sub.1 -C.sub.3)alkoxycarbonyl(C.sub.2 -C.sub.4)alkenyl, carboxy(C.sub.1 -C.sub.3)alkyl and (C.sub.1 -C.sub.3)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl; andR.sup.4 is a phenyl group which may be substituted by one or more of the same substituents as defined above, or a pharmaceutically acceptable salt thereof.The derivatives are of an inhibitory activity against aldose reductase and useful for the prevention or treatment of complications of diabetes.

公开(公告)号：US5112860A

公开(公告)日：1992-05-12

申请号：US608351

申请日：1990-11-02

Applicant: Horst Wingert ,  Hubert Sauter ,  Siegbert Brand ,  Bernd Wenderoth ,  Gisela Lorenz ,  Eberhard Ammermann

Inventor： Horst Wingert ,  Hubert Sauter ,  Siegbert Brand ,  Bernd Wenderoth ,  Gisela Lorenz ,  Eberhard Ammermann

IPC: C07D233/64 ,  A01N37/44 ,  A01N37/50 ,  A01N43/40 ,  C07C327/22 ,  C07C327/36 ,  C07D213/64 ,  C07D213/70 ,  C07D213/71 ,  C07D215/22 ,  C07D215/36 ,  C07D233/70 ,  C07D235/12 ,  C07D235/26 ,  C07D235/28 ,  C07D239/34 ,  C07D239/38 ,  C07D257/04 ,  C07D263/58 ,  C07D277/14 ,  C07D277/16 ,  C07D277/20 ,  C07D277/34 ,  C07D277/36 ,  C07D285/08 ,  C07D307/56 ,  C07D333/06 ,  C07D521/00

CPC classification number: C07D213/70 ,  A01N37/50 ,  A01N43/40 ,  C07C327/22 ,  C07C327/36

Abstract: Thiocarboxylic esters of the formula I ##STR1## where the substituents have the following meanings: X is oxygen, sulfur, oxymethylene, methyleneoxy, thiomethylene, methylenethio, ethylene, ethenylene or ethynylene,Y, Z are each sulfur or oxygen, but Y and Z are not simultaneously oxygen,R is alkyl, mononuclear, dinuclear or trinuclear aryl or hetaryl, where aryl and hetaryl may be substituted,and fungicidal agents containing these compounds.

Abstract translation: 式I的硫代羧酸酯其中取代基具有以下含义：X是氧，硫，甲醛，亚甲氧基，亚甲基，亚甲基，亚乙基，亚乙烯基或亚乙炔基，Y，Z各自为硫或氧，但Y和 Z不是同时氧，R是烷基，单核，双核或三核芳基或杂芳基，其中芳基和杂芳基可以被取代，和含有这些化合物的杀真菌剂。

公开(公告)号：US5104889A

公开(公告)日：1992-04-14

申请号：US529694

申请日：1990-05-29

Applicant: Kenichi Kanai ,  Kiyoto Goto ,  Kinji Hashimoto ,  Yoshiaki Tsuda

Inventor： Kenichi Kanai ,  Kiyoto Goto ,  Kinji Hashimoto ,  Yoshiaki Tsuda

IPC: A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P7/02 ,  A61P9/10 ,  A61P11/00 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  C07D277/20 ,  C07D277/22 ,  C07D277/24 ,  C07D277/30 ,  C07D277/32 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D277/54 ,  C07D277/56 ,  C07D277/58 ,  C10M105/32 ,  C10M111/04 ,  C10M169/04

CPC classification number: C07D277/56 ,  C07D277/24 ,  C07D277/30 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D277/54 ,  C07D277/58 ,  C10M105/32 ,  C10M111/04 ,  C10M169/04

Abstract: This invention provides thiazole derivative of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined above, and salts thereof. These compounds have particularly potent angiogenesis inhibiting activity.

公开(公告)号：US5091382A

公开(公告)日：1992-02-25

申请号：US552058

申请日：1990-07-13

Applicant: Friedhelm Adam ,  Walter Durckheimer ,  Karl-Heinz Scheunemann ,  Dieter Isert ,  Gerhard Seibert

Inventor： Friedhelm Adam ,  Walter Durckheimer ,  Karl-Heinz Scheunemann ,  Dieter Isert ,  Gerhard Seibert

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/36 ,  C07D277/56 ,  C07D501/00 ,  C07D501/36

CPC classification number: C07D277/56 ,  C07D277/36 ,  C07D501/00

Abstract: Cephalosporin derivatives of the general formula ##STR1## pharmaceutical preparations active against bacterial infections which contain such cephalosporin derivatives, processes for the preparation of the cephalosporin derivatives, use of the cephalosporin derivatives for the preparation of a pharmaceutical for combating bacterial infections, and starting products for the preparation of cephalosporin derivatives.

Abstract translation: 具有通式的头孢菌素衍生物，其含有这种头孢菌素衍生物的细菌感染活性的药物制剂，头孢菌素衍生物的制备方法，头孢菌素衍生物用于制备抗菌细菌感染药物，以及起始产品 头孢菌素衍生物的制备。

公开(公告)号：US5061794A

公开(公告)日：1991-10-29

申请号：US377086

申请日：1989-07-10

Applicant: Susumu Nakagawa ,  Koji Yamada ,  Fumio Nakano ,  Norikazu Otake ,  Akira Asai ,  Satoru Kuroyanagi ,  Yoshiharu Tanaka ,  Moriaki Ishikawa ,  Ryosuke Ushijima ,  Ryuji Mitomo

Inventor： Susumu Nakagawa ,  Koji Yamada ,  Fumio Nakano ,  Norikazu Otake ,  Akira Asai ,  Satoru Kuroyanagi ,  Yoshiharu Tanaka ,  Moriaki Ishikawa ,  Ryosuke Ushijima ,  Ryuji Mitomo

IPC: C07D235/28 ,  C07D263/46 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D277/20 ,  C07D277/36 ,  C07D277/56 ,  C07D285/12 ,  C07D285/125 ,  C07D501/36

CPC classification number: C07D263/58 ,  C07D235/28 ,  C07D263/46 ,  C07D271/113 ,  C07D277/36 ,  C07D277/56 ,  C07D277/587 ,  C07D285/125

Abstract: A compound having the formula: ##STR1## wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is ##STR2## (wherein R.sup.1 is a hydrogen atom or an acetyl group, R.sup.2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

Abstract translation: 具有下式的化合物：其中R是直链或支链的低级烷基，环状低级烷基，低级烯基（1-羧基-1-乙烯基），低级炔基，芳烷基，苯基或2 可以被取代的吡咯烷酮-3-基，Q是氢原子或乙酰基，R2是氢原子，羧基或羧甲基， Y是硫原子或氧原子，Z是硫原子，氧原子或可被低级烷基取代的亚氨基）; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。

公开(公告)号：US5057538A

公开(公告)日：1991-10-15

申请号：US587147

申请日：1990-09-24

Applicant: Tadayoshi Shiraishi ,  Keiji Kameyama ,  Takeshi Domoto ,  Naohiro Imai ,  Yoshio Shimada ,  Yutaka Ariki ,  Kazunoro Hosoe ,  Masaji Kawatsu ,  Ikuo Katsumi ,  Takayoshi Hidaka ,  Kiyoshi Watanabe

Inventor： Tadayoshi Shiraishi ,  Keiji Kameyama ,  Takeshi Domoto ,  Naohiro Imai ,  Yoshio Shimada ,  Yutaka Ariki ,  Kazunoro Hosoe ,  Masaji Kawatsu ,  Ikuo Katsumi ,  Takayoshi Hidaka ,  Kiyoshi Watanabe

IPC: B21B31/16 ,  A61K31/26 ,  A61K31/27 ,  A61K31/275 ,  A61K31/34 ,  A61K31/425 ,  B21B31/02 ,  B21B31/20 ,  B21B33/00 ,  B21B37/18 ,  B21B37/72 ,  C07C253/30 ,  C07C255/34 ,  C07C255/41 ,  C07C255/44 ,  C07C255/53 ,  C07D207/38 ,  C07D209/34 ,  C07D231/36 ,  C07D277/20 ,  C07D277/36 ,  C07D277/54 ,  C07D279/16 ,  C07D307/32 ,  C07D307/33 ,  C07D307/52 ,  C07D307/58 ,  C07D417/12 ,  C09K3/00 ,  C07C121/75

CPC classification number: C07D277/20 ,  B21B31/02 ,  B21B31/203 ,  C07C255/00 ,  C07C255/34 ,  C07D207/38 ,  C07D209/34 ,  C07D231/36 ,  C07D277/36 ,  C07D277/54 ,  C07D279/16 ,  C07D307/58 ,  C07D417/12

Abstract: A hydroxystyrene derivative represented by the formula (I): ##STR1## Wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O--(R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sub.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O--(R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O--(R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 --(Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxybenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.