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21. 发明授权

US5342970A Hydrosoluble coumarin derivatives, their preparation and their use as an enzyme substrate or for the preparation of such substrates 失效
标题翻译：可溶性香豆素衍生物，它们的制备及其作为酶底物的用途或用于制备这些底物
公开(公告)号：US5342970A
公开(公告)日：1994-08-30
申请号：US887767
申请日：1992-05-22
申请人： Joseph Chalom , Christine Griffoul , Michel Tod , Stephane Reveilleau
发明人： Joseph Chalom , Christine Griffoul , Michel Tod , Stephane Reveilleau
IPC分类号： C07C69/716 , C07D311/06 , C07D311/16 , C07D311/20 , C07D311/58 , C07D405/12 , C07D491/16 , C12Q1/37 , G01N33/535 , C07D311/04
CPC分类号： C12Q1/37 , C07C69/716 , C07D311/16 , C07D311/20 , C07D311/58 , C12Q2337/20
摘要： The invention relates to hydrosoluble coumarin derivatives. These derivatives comply with the formula: ##STR1## in which R.sup.1 represents ##STR2## with m=1 to 30 and in which R.sup.7 can be a hydrogen atom or various groups, R.sup.2 to R.sup.6 can be different substituents, particularly substituents making it possible to introduce into the derivative an appropriate group as the enzyme substrate or for the synthesis of enzyme substrates.
摘要翻译：本发明涉及水溶性香豆素衍生物。这些衍生物符合下式：其中R1表示（OCH2CH2）mOCH2R7或（OCH（CH3）CH2）mOCH2R7，m = 1-30，其中R7可以是氢原子或各种基团，R2 到R6可以是不同的取代基，特别是取代基，使得可能将合适的基团引入衍生物作为酶底物或用于合成酶底物。

22. 发明授权

US5189183A Aromatic amine derivatives 失效
标题翻译：芳香族胺衍生物
公开(公告)号：US5189183A
公开(公告)日：1993-02-23
申请号：US598061
申请日：1990-10-16
申请人： Daisuke Fukuoka , Katsuya Takahashi , Isao Hashimoto
发明人： Daisuke Fukuoka , Katsuya Takahashi , Isao Hashimoto
IPC分类号： C07D307/79 , C07D307/83 , C07D307/86 , C07D307/91 , C07D311/20 , C07D311/22 , C07D311/58 , C07D311/64 , C07D311/78 , C07D311/96 , C07D317/46 , C07D317/64 , C07D317/72 , C07D405/12 , C07D493/10
CPC分类号： C07D307/79 , C07D307/83 , C07D307/86 , C07D307/91 , C07D311/20 , C07D311/22 , C07D311/58 , C07D311/64 , C07D311/78 , C07D311/96 , C07D317/46 , C07D317/64 , C07D317/72 , C07D405/12 , C07D493/10
摘要： Novel aromatic amine derivatives of specific structure are useful intermediates for herbicides. The aromatic amine compounds have the structure shown by formula [I]: ##STR1## wherein Ar and A are as defined herein.
摘要翻译：具有特殊结构的新型芳香胺衍生物是除草剂的有用中间体。芳族胺化合物具有式[I]所示的结构：其中Ar和A如本文所定义。

23. 发明授权

US5072007A Process for preparing polyalkyl-2-alkoxy-7-hydroxychroman derivatives 失效
标题翻译：制备聚烷基-2-羟基-7-羟基喹啉衍生物的方法
公开(公告)号：US5072007A
公开(公告)日：1991-12-10
申请号：US547132
申请日：1990-07-03
申请人： Daisuke Fukuoka , Takeshi Ishitoku , Katsuya Takahashi , Takashi Tashiro , Junichi Imuta , Hiroaki Tan , Masaharu Ishiguro , Noriaki Kihara , Teruaki Mukaiyama
发明人： Daisuke Fukuoka , Takeshi Ishitoku , Katsuya Takahashi , Takashi Tashiro , Junichi Imuta , Hiroaki Tan , Masaharu Ishiguro , Noriaki Kihara , Teruaki Mukaiyama
IPC分类号： C07D311/20
CPC分类号： C07D311/20
摘要： Process for preparing polyalkyl-2-alkoxy-7-hydroxychroman derivative of the general formula (V): ##STR1## wherein R.sup.1 denotes lower primary alkyl, R.sup.2 denotes hydrogen or lower primary alkyl and R.sup.3 denotes loweralkyl, by reacting resorcin with either an aliphatic ketone of the general formula (I): ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and an alcohol of the formula (II):R.sup.3 OH (II)wherein R.sup.3 is as defined above, in the presence of an acid catalyst, or an aliphatic ketone acetal of the general formula (III): ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, in the presence of an acid catalyst.

24. 发明授权

US4996332A Optical indicator coumarins and methods for their preparation and use 失效
标题翻译：光学指示剂香豆素及其制备和使用方法
公开(公告)号：US4996332A
公开(公告)日：1991-02-26
申请号：US205732
申请日：1988-06-13
申请人： Robert T. Buckler , Robert P. Hatch
发明人： Robert T. Buckler , Robert P. Hatch
IPC分类号： C07D215/54 , C07D311/20 , C12Q1/28
CPC分类号： C07D311/20 , C07D215/54 , C12Q1/28
摘要： Optical indicator chalcogen (selenide or sulfide) compounds responsive to oxidants, e.g., hydrogen peroxide, and methods for preparing and using such indicators. Upon oxidation the resulting intermediate undergoes spontaneous elimination of the chalcogen residue to yield a signal compound which provides an optical signal such as fluorescence. Preferred fluorogenic indicator compounds are 3-chalcogen-3,4-dihydrocoumarin derivatives and 3-chalcogen-3,4-dihydro-2-quinolone derivatives. Such indicator compounds provide highly fluorescent products upon oxidation by hydrogen peroxide and are useful in analytical systems which generate hydrogen peroxide in response to the analyte under determination.
摘要翻译：对氧化剂（例如过氧化氢）有响应的光学指示剂硫属化合物（硒化物或硫化物）以及制备和使用这些指示剂的方法。氧化后，得到的中间体自发消除硫族元素残余物，产生提供光信号如荧光的信号化合物。优选的荧光指示剂化合物是3-硫族原-3,4-二氢香豆素衍生物和3-硫族原-3,4-二氢-2-喹诺酮衍生物。这种指示剂化合物在通过过氧化氢氧化时提供高度荧光的产物，并且可用于响应于待测分析物产生过氧化氢的分析系统。

25. 发明授权

US4857643A Antitussive and mucus regulating 2-substituted thiazolidines 失效
标题翻译：镇静和粘液调节2-取代噻唑烷
公开(公告)号：US4857643A
公开(公告)日：1989-08-15
申请号：US266559
申请日：1988-11-03
申请人： Carmelo A. Gandolfi , Silvano Spinelli , Odoardo Tofanetti , Raimondo Russo , Sergio Tognella
发明人： Carmelo A. Gandolfi , Silvano Spinelli , Odoardo Tofanetti , Raimondo Russo , Sergio Tognella
IPC分类号： A61K31/425 , A61K31/426 , A61K31/44 , A61K31/495 , A61P11/00 , A61P11/10 , A61P11/14 , C07C43/23 , C07C45/29 , C07C49/255 , C07D277/04 , C07D277/06 , C07D311/20 , C07D319/20 , C07D417/06 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07C43/23 , C07C45/29 , C07C49/255 , C07D233/56 , C07D249/08 , C07D277/04 , C07D277/06 , C07D311/20 , C07D319/20 , C07D417/06
摘要： 2-Substituted thiazolidines compounds having formula I ##STR1## wherein X is a CH.sub.2, O or S, R is hydroxy or an acyloxy, alkyloxy, alkenyloxy or alkinyloxy group, R.sub.1 is hydrogen or a group of formula ##STR2## R.sub.2 is hydrogen or a free or esterified carboxy group, R.sub.a and R.sub.b are hydrogen or methyl, p is zero or 1, R.sub.3 is hydrogen, a C.sub.1 -C.sub.2 alkylsulphonyl group, a phenyl or p-Cl phenyl, p-methylsulphonyl group or an acyl group; are useful as mucus regulating, antitussive and antibronchospastic agents.
摘要翻译： 2-取代的具有式I的噻唑烷化合物（I）其中X是CH 2，O或S，R是羟基或酰氧基，烷氧基，烯氧基或烷氧基，R 1是氢或式是氢或游离或酯化的羧基，R a和R b是氢或甲基，p是0或1，R 3是氢，C 1 -C 2烷基磺酰基，苯基或对C 1 -C 6苯基，对甲基磺酰基或酰基组; 可用作粘液调节，镇咳药和抗骨质疏松剂。

26. 发明授权

US4680404A Benzopyrans 失效
标题翻译：苯并吡喃
公开(公告)号：US4680404A
公开(公告)日：1987-07-14
申请号：US639151
申请日：1984-08-09
申请人： James F. Eggler , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C37/055 , C07C39/08 , C07C43/23 , C07C61/39 , C07D311/22 , C07D311/58 , C07D405/12 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10 , C07D311/20 , C07D405/04
CPC分类号： C07D405/12 , C07C255/00 , C07C37/055 , C07C41/30 , C07C61/39 , C07D311/22 , C07D311/58 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
摘要： Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 and Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, Antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译：式（I'）的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐，其中M为O，CH 2或NR 6; R6是氢，甲酰基，苄氧羰基或某些烷氧基烷基，烷酰基，烷基，芳烷基或芳烷基羰基; A'为：（1）其中A和B之一为氢，使得当A为氢时，B为C（R2R3）（CH2）fQ且f为1或2; 当B为氢时，A为C（R2R3）（CH2）fQ，f为0或1，当A和OR1一起形成内酯或其某些衍生物时; （2）A'是（3）A'是Q3; Q是CO 2 R 7，COR 8，C（OH）R 8 R 9，CN，CONR 12 R 13，CH 2 NR 12 R 13，CH 2 NHCOR 14，CH 2 NHSO 2 R 17或5-四唑基; Q3是5-四唑基，CH 2 CONHCOR 7，COOH或其某些酯，酰胺，羧酰亚氨基或磺酰亚氨基衍生物，CONHOH，CONHCONH 2或COCH 2 Q 4和Q 4是CN或COOH或其某些酯; R1是氢，苄基或某些酰基; R4是氢，某些烷基或某些芳烷基; R5是氢或某些烷基; Z是（C 1 -C 9）亚烷基，任选地被O，S，SO或SO 2中断; W是氢，甲基，某些芳基或环烷基; 因此，在哺乳动物中作为止痛剂，镇静剂，止吐剂，利尿剂，抗惊厥药，止泻药，镇咳药，在治疗青光眼中有用。

27. 发明授权

US4511685A Chroman derivatives and stabilized polypropylene composition 失效
标题翻译：色甘烷衍生物和稳定的聚丙烯组合物
公开(公告)号：US4511685A
公开(公告)日：1985-04-16
申请号：US238593
申请日：1981-02-26
申请人： Axel Nissen , Michael Horner , Dieter Horn , Erik Lueddecke , Gernot Teege
发明人： Axel Nissen , Michael Horner , Dieter Horn , Erik Lueddecke , Gernot Teege
IPC分类号： C07D311/72 , C07D311/20 , C07D311/58 , C07D311/66 , C07D311/70 , C09K15/08 , C09K15/14 , C09K15/24 , C09K15/28 , C08K5/09
CPC分类号： C07D311/58 , C07D311/66 , C09K15/08
摘要： Chroman derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 -alkyl, R.sup.5 is C.sub.10 -C.sub.30 -alkyl or C.sub.10 -C.sub.30 -alkenyl, X and Y are each O, NH or S, m is 0, 1, 2 or 3 and n and r are each 0 or 1, the preparation of compounds I by various methods known per se, and the use of the compounds as stabilizers for organic materials.
摘要翻译：其中R 1，R 2，R 3和R 4各自为H或C 1 -C 4 - 烷基，R 5为C 10 -C 30 - 烷基或C 10 -C 30 - 烯基，通式I的色原衍生物，X和Y各自为O， NH或S，m为0,1,2或3，n和r各自为0或1，通过本身已知的各种方法制备化合物I，以及将化合物用作有机材料的稳定剂。

28. 发明授权

US4155916A Fluorescence method for enzyme analysis which couples aromatic amines with aromatic aldehydes 失效
标题翻译：芳香族胺与芳族醛结合的酶分析荧光法
公开(公告)号：US4155916A
公开(公告)日：1979-05-22
申请号：US828394
申请日：1977-08-29
申请人： Robert E. Smith , Frank A. Dolbeare
发明人： Robert E. Smith , Frank A. Dolbeare
IPC分类号： C07D311/20 , C12Q1/00 , C07C119/00
CPC分类号： C07D311/20 , C12Q1/00
摘要： Analysis of proteinases is accomplished using conventional amino acid containing aromatic amine substrates. Aromatic amines such as 4-methoxy-2-naphthylamine (4M2NA), 2-naphthylamine, aminoisophthalic acid dimethyl ester, p-nitroaniline, 5-methoxy-1-aminofluorene and coumarin derivatives resulting from enzymatic hydrolysis of the substrate couples with aromatic aldehydes such as 5-nitrosalicylaldehyde (5-NSA), benzaldehyde and p-nitrobenzaldehyde to produce Schiff-base complexes which are water insoluble. Certain Schiff-base complexes produce a shift from blue to orange-red (visible) fluorescence. Such complexes are useful in the assay of enzymes.
摘要翻译：使用常规含氨基酸的芳香族胺底物进行蛋白酶分析。芳基胺如4-甲氧基-2-萘胺（4M2NA），2-萘胺，氨基间苯二甲酸二甲酯，对硝基苯胺，5-甲氧基-1-氨基芴和由底物的酶水解产生的香豆素衍生物与芳族醛偶联作为5-硝基水杨醛（5-NSA），苯甲醛和对硝基苯甲醛以产生水不溶性的席夫碱配合物。某些席夫碱配合物产生从蓝色到橙红色（可见）荧光的转变。这样的复合物在酶的测定中是有用的。

29. 发明授权

US4080335A Anorexic chromans 失效
标题翻译：厌食染色剂
公开(公告)号：US4080335A
公开(公告)日：1978-03-21
申请号：US652041
申请日：1976-01-26
申请人： Derek Victor Gardner
发明人： Derek Victor Gardner
IPC分类号： C07D233/44 , A61K31/395 , A61K31/415 , A61K31/4168 , C07D20060101 , C07D231/06 , C07D233/48 , C07D311/16 , C07D311/20 , C07D311/58 , C07D317/58 , C07D317/60 , C07D405/12 , C07D311/02 , A61K31/35 , A61K31/40 , C07D207/04
CPC分类号： C07C255/00 , A61K31/415 , C07D231/06 , C07D233/44 , C07D311/16 , C07D311/20 , C07D311/58 , C07D317/58 , C07D317/60 , C07D405/12 , Y10S514/906
摘要： Compounds within formula ##STR1## and their salts wherein X is alkylene of 2 - 4 carbon atoms; R.sub.1 is hydrogen or alkyl of 1 - 6 carbon atoms; R.sub.2 is hydrogen, alkyl of 1 - 6 carbon atoms or benzyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5-, 6- or 7-membered saturated ring; R.sub.3 is aryl; R.sub.4 is hydrogen or alkyl of 1 - 4 carbon atoms; and R.sub.5 is hydrogen or alkyl of 1 - 4 carbon atoms; have been found to possess mood-modifying and anorexia inducing activity.
摘要翻译：式（II）中的化合物及其盐，其中X是2-4个碳原子的亚烷基; R1是氢或1-6个碳原子的烷基; R2是氢，1-6个碳原子的烷基或苄基，或R1和R2与它们所连接的氮原子一起形成5-，6-或7-元饱和环; R3是芳基; R4是氢或1-4个碳原子的烷基; R5为氢或1-4个碳原子的烷基; 已被发现具有心境改善和厌食诱导活性。

30. 发明授权

US3969369A Bruceantin 失效
标题翻译：布鲁斯坦丁
公开(公告)号：US3969369A
公开(公告)日：1976-07-13
申请号：US371634
申请日：1973-06-20
申请人： S. Morris Kupchan , Ronald W. Britton
发明人： S. Morris Kupchan , Ronald W. Britton
IPC分类号： C07D493/10 , C07D311/20
CPC分类号： C07D493/10 , Y10S514/908
摘要： There is provided a novel simaroubolide derived from Brucea antidysenterica which possesses high and surprising anti-leukemic activity at dosage levels of micrograms per kilogram body weight.
摘要翻译：提供了一种来源于布鲁斯抗散热药物的新西他宝钠，它以每公斤体重微克的剂量水平具有高而令人惊奇的抗白血病活性。

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