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1. 发明授权

US4643990A N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof 失效
标题翻译： N-酰基肽，其制备方法及其药物组合物
公开(公告)号：US4643990A
公开(公告)日：1987-02-17
申请号：US452827
申请日：1982-12-23
申请人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , A61K37/43 , C07C67/02 , C07C69/52 , C07C101/26 , C07C101/30 , C07C143/12 , C07K5/08
CPC分类号： C07K5/06104 , C07K5/06052 , C07K5/06078 , C07K5/06086 , A61K38/00
摘要： N-acylpeptides are disclosed of the formula: ##STR1## wherein R.sup.1 is alkanoyloxy or alkenoyloxy; R.sup.2 is alkyl or alkenyl; R.sup.3 and R.sup.4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R.sup.5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R.sup.6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A.sup.1, A.sup.2 and A.sup.3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.
摘要翻译： N-酰基肽公开于下式：其中R 1是烷酰氧基或烯酰基氧基; R2是烷基或烯基; R 3和R 4各自为低级烷基，羟基（低级）烷基，芳（低级）烷基，酯化羧基（低级）烷基，羧基（低级）烷基，被保护的氨基（低级）烷基或氨基（低级） R5是氢，羟基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基或酯化羧基（低级）烷基; R6是羧基，酯化的羧基或磺基（低级）烷基; A1，A2和A3各自为键或低级亚烷基; m和n分别为0或1的整数; 或其药学上可接受的盐。这些化合物具有抗互补活性和纤维蛋白溶解活性，并且可用作免疫复合物疾病或自身免疫性疾病如肾炎，风湿性疾病，系统性红斑狼疮等的治疗剂，以及血栓形成如脑中风，冠状动脉功能不全，肺栓塞等等

2. 发明授权

US4594188A Use of diamino ketones as analgesic agents 失效
标题翻译：使用二氨基酮作为止痛剂
公开(公告)号：US4594188A
公开(公告)日：1986-06-10
申请号：US735924
申请日：1985-05-20
申请人： Norma G. Delaney , Eric M. Gordon
发明人： Norma G. Delaney , Eric M. Gordon
IPC分类号： A61K38/00 , C07K5/065 , C07K7/02 , C07K5/06 , C07C61/08 , C07C69/74 , C07C101/00 , C07C101/02 , C07C101/24 , C07C101/26 , C07C101/42 , C07C109/10 , C07C147/02 , C07C149/20 , C07C149/243 , C07C149/40 , C07C149/43
CPC分类号： C07K7/02 , C07K5/06078 , A61K38/00
摘要： An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.5 each is independently glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, or prolyl, norleucyl, or norvalyl; andn.sub.1, n.sub.2, n.sub.3, n.sub.4 and n.sub.5 each is independently 0 or 1.
摘要翻译：脑啡肽降解氨基肽酶被具有式（IMAGE）+ TR（A2）n2（A3）n3（A4）n4（A5）n5R3的化合物及其药学上可接受的盐抑制，其中R 1和R 2各自独立地为氢，烷基，羧基烷基，卤素取代的烷基，羟基烷基，氨基烷基，巯基烷基，烷硫基烷基，（环烷基）烷基，（杂芳基）烷基，芳基烷基，氨基甲酰基烷基，胍基烷基或杂芳基; R3是羟基，烷氧基，（取代的烷基）氧基，芳基烷氧基，（杂芳基）烷氧基或-NY1Y2，其中Y1和Y2各自独立地是氢，烷基，芳基或芳烷基或Y1是氢，Y2是取代的烷基或（杂芳基）烷基; A1是甘氨酰基，丙氨酰基，亮氨酰基，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺基，赖氨酰，谷氨酰，组氨酸，色氨酸，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰，脯氨酰，其中n6为2至15的整数; A2，A3，A4和A5各自独立地是甘氨酰，丙氨酰，亮氨酰，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺酰基，赖氨酰，谷氨酰，组氨酸，色氨酰，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰或脯氨酰，正亮酰基或诺瓦尔基; n1，n2，n3，n4和n5各自独立地为0或1。

3. 发明授权

US4359332A Amide and hydrazide derivatives of N-trifluoroacetyl-N-phosphonomethylglycine as herbicides 失效
标题翻译：作为除草剂的N-三氟乙酰基-N-膦酰基甲基甘氨酸的酰胺和酰肼衍生物
公开(公告)号：US4359332A
公开(公告)日：1982-11-16
申请号：US922923
申请日：1978-07-10
申请人： John E. Franz , Robert J. Kaufman
发明人： John E. Franz , Robert J. Kaufman
IPC分类号： A01N57/28 , A01N57/26 , A01N57/32 , A01P13/00 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/572 , C07F9/59 , C07F9/6533 , A01N57/00 , C07C101/00 , C07C101/26
CPC分类号： C07F9/6533 , A01N57/26 , C07F9/4407 , C07F9/4496 , C07F9/5721 , C07F9/591
摘要： This disclosure relates to alkyl N-trifluoroacetyl-N-phosphonomethylglycine amide and hydrazide derivatives, to herbicidal compositions containing same and to the herbicidal use thereof. These amide and hydrazide derivatives are useful as pre-emergent and/or post-emergent herbicides.
摘要翻译：本公开内容涉及N-三氟乙酰基-N-膦酰基甲基甘氨酸烷基酰胺和酰肼衍生物，含有其的除草组合物及其除草用途。这些酰胺和酰肼衍生物可用作芽前和/或芽后除草剂。

4. 发明授权

US4352751A Species-linked diamine triacetic acids and their chelates 失效
标题翻译：物种连接的二胺三乙酸及其螯合物
公开(公告)号：US4352751A
公开(公告)日：1982-10-05
申请号：US73728
申请日：1979-09-10
申请人： Irwin Wieder , Robert H. Wollenberg
发明人： Irwin Wieder , Robert H. Wollenberg
IPC分类号： C09K11/06 , C07C67/00 , C07C227/00 , C07C227/02 , C07C227/18 , C07C229/16 , C07C229/76 , C07C231/00 , C07C231/02 , C07C231/12 , C07C237/06 , C07C237/12 , C07C301/00 , C07C303/00 , C07C303/22 , C07C309/01 , C07C325/00 , C07C327/06 , C07C381/00 , C07D265/32 , C07D265/33 , C07F3/00 , C07F5/00 , C07J41/00 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/00 , C07K19/00 , G01N21/76 , G01N33/532 , G01N33/533 , C07C101/26 , C07C103/18 , C12Q1/06 , G01N33/48 , G01N33/50
CPC分类号： C07D265/33 , C07J41/0055 , C07K5/022 , G01N33/533 , Y10S435/968 , Y10S530/862 , Y10S530/868
摘要： Species-linked diamine triacetic acids of the formula ##STR1## wherein T is an organic species containing at least one amine, hydroxyl, or thiol functional group, L is the residue of at least one of those functional groups and R is a two or more atom long covalent bridge, are disclosed. Methods for their preparation, for the preparation of metal chelates from them and for the use of the chelates are also disclosed. In a preferred embodiment, the metal ions employed in the formation of the chelates are rare earth metal ions capable of forming fluorescent chelates which can in turn be employed in fluoroassay techniques.
摘要翻译：具有式的物种连接的二胺三乙酸，其中T是含有至少一个胺，羟基或硫醇官能团的有机物质，L是这些官能团中的至少一个的残基，R是两个或更多个原子长的共价桥。还公开了其制备方法，用于制备它们的金属螯合物和螯合物的用途。在优选的实施方案中，用于形成螯合物的金属离子是能够形成荧光螯合物的稀土金属离子，其可以用于氟化物分析技术。

5. 发明授权

US4136101A Process for preparing dialkyl (p-aminobenzoyl) glutamates 失效
标题翻译：制备二烷基（对氨基苯甲酰）谷氨酸的方法
公开(公告)号：US4136101A
公开(公告)日：1979-01-23
申请号：US875051
申请日：1978-02-03
申请人： John Kazan
发明人： John Kazan
IPC分类号： C07F3/06 , C07C20060101 , C07C237/36 , C07D475/08 , C07C101/26
CPC分类号： C07C2101/14
摘要： A process for the preparation of dialkyl (p-aminobenzoyl) glutamates is disclosed. Dialkyl (p-Aminobenzoyl) glutamates are useful as intermediates in the synthesis of N-{p-([(2,4-diamino-6-pteridinyl)-methyl]methylamino)benzoyl} glutamic acid, also known as 4-amino-N.sup.10 -methylpteroylglutamic acid. The compound zinc N-(p-methylaminobenzoyl)-L-(+)-glutamate, is also disclosed.

6. 发明授权

US3939200A Aliphatic acyl-containing amine hydrochlorides 失效
标题翻译：含脂肪酰基的胺盐酸盐
公开(公告)号：US3939200A
公开(公告)日：1976-02-17
申请号：US69965
申请日：1970-09-04
申请人： William D. Emmons , Jerome F. Levy
发明人： William D. Emmons , Jerome F. Levy
IPC分类号： C07C331/16 , C08G18/77 , C07C101/26
CPC分类号： C08G18/771 , C07C229/08 , C07C229/24 , C07C229/60
摘要： Novel acyl-containing amine hydrochlorides are produced by first converting the amino group or groups of an amino acid to an acid salt by reaction with hydrochloric acid and the resulting product is reacted with an alkanolamine or diol in an inert liquid medium while passing a stream of hydrogen chloride gas therethrough. The amine hydrochlorides produced in this manner may be converted to the corresponding isocyanates by reaction with phosgene or other carbonyl dihalide.
摘要翻译：新型含酰基的胺盐酸盐是通过首先通过与盐酸反应将氨基酸的氨基或氨基酸转化成酸性盐，并将所得产物与惰性液体介质中的链烷醇胺或二醇反应，同时通过氯化氢气体通过其中。以这种方式制备的胺盐酸盐可以通过与光气或其它羰基二卤化物反应转化成相应的异氰酸酯。

7. 发明授权

US3833590A Chelates for the control of metaldeficiency phenomena in biological systems 失效
标题翻译：用于控制生物系统中金属化学物质的化学物质
公开(公告)号：US3833590A
公开(公告)日：1974-09-03
申请号：US27437772
申请日：1972-07-24
申请人： CIBA GEIGY CORP
发明人： DAZZI J
IPC分类号： C07D215/38 , A01N37/44 , A01N43/40 , A01P15/00 , C02F5/12 , C05D9/02 , C07C67/00 , C07C237/00 , C07C237/04 , C07C237/30 , C07C237/42 , C07C239/00 , C07C261/04 , C07C301/00 , C07C303/22 , C07C309/49 , C07C309/51 , C07C309/63 , C07C309/76 , C07C311/00 , C07C311/16 , C07C311/21 , C07C311/46 , C07C313/00 , C07C315/04 , C07C317/40 , C07C323/41 , C07C331/14 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/86 , C07D213/87 , C07D215/40 , C07K5/02 , C07C101/26 , C07F15/02
CPC分类号： C07D213/75 , C02F5/12 , C05D9/02 , C07C255/00 , C07C309/51 , C07C309/76 , C07C311/16 , C07C311/21 , C07C317/40 , C07C323/41 , C07C331/14 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/40
摘要： HEAVY METAL CHELATES OF ETHYLENEDIAMINETETRAACETIC ACID DERIVATIVES

R-NH-CO-CH2-N(-CH2-COOH)-CH2-CH2-N(-CH2-COOH)-CH2-CO-NH-R

ARE USEFUL FOR THE CONTROL OF METAL-DEFICIENCY PHENOMENA IN BIOLOGICAL SYSTEMS. IN THE FORMULA R REPRESENTS THE PHENYL OR NAPHTHYL RADICAL WHICH CAN BE SUBSTITUTED BY HALOGEN, HYDROXY, MERCAPTO, NITRO, CYANO, THIOCYANO, ALKYL, ALKOXY, MERCAPTO, NITRO, CYAMINO ACYLIXY, CARBOXYL, ALKOXYCARBONYL, ACRBAMOYL, PYRIDOYLAMINO, N-CARBOXYALKYL-CAARBAMOYL, SULPHO, SULPHAMOYL, MONO- OR DIALKYLATED OR PHENYLATED SULPHAMOYL WHICH CAN ALSO CARRY ONE OF THE GROUPS

-CH2-CH2-SO3-H OR-CH2-COOH

ALKYLSULPHONYL, ALKOXYSULPHONYL, OR BY AN OPTIONALLY HYDROXY-CONTAINING PHENYLSULPHONY OR PHENOXYSULPHONYL; OR WHEREIN R REPRESENTS THE PYRIDINE OR QUINOLINE RADICAL WHICH CAN BE SUBSTITUTED BY HALOGEN, HYDROXY ALKYL, OR CARBAMOYL.

8. 发明授权

US3772374A Process for preparing alkali metal nitrilotriacetates 失效
标题翻译：制备碱性金属硝酸酯的方法
公开(公告)号：US3772374A
公开(公告)日：1973-11-13
申请号：US3772374D
申请日：1971-08-09
申请人： MONSANTO CO
发明人： SHEN C
IPC分类号： C07C101/26
CPC分类号： C11D3/33
摘要： A PROCESS IS DESCRIBED FOR PREPARING ALKALI METAL NITRILOTRIACETATE BY HYDROLYZING NITRILOTRIACETONITRILE DISSOLVED IN AN AQUEOUS SOLUTION CONTAING AN ALKALI METAL HYDROXIDE AT A TEMPERATURE OF FROM ABOUT 90*C. TO AOUT 150*C. WITH THE ALKALI METAL HYDROXIDE BEING IN AN EXCESS AMOUNT SUFFICIENT TO RAPIDLY CONVERT SAID NITRILE TO ALKALI METAL NITRILOTRIACETATE AND FORM AN AQUEOUS ALKALI METAL HYDROXIDE SOLUTION CONTAING ALKALI METAL NITRILOTRIACETATE CRYSTALS, AND RECOVERING THE ALKALI METAL NITRILOTRIACETATE CRYSTALS FROM THE SOLUTION.

9. 发明授权

US3642887A Preparation of amino-substituted carboxylic acids 失效
标题翻译：氨基取代的羧酸的制备
公开(公告)号：US3642887A
公开(公告)日：1972-02-15
申请号：US3642887D
申请日：1966-12-19
申请人： ETHYL CORP
发明人： JACKISCH PHILIP F
IPC分类号： C07C101/20 , C07C101/26
CPC分类号： C11D3/33
摘要： DIMETHYL SULFOXIDE CATALYZES THE REACTION BETWEEN AHALOSUBSITUTED CARBOXYLIC ACIDS AND NITROGEN COMPOUNDS SELECTED FROM AMMONIA, PRIMARY, AND SECONDARY AMINES. FOR EXAMPLE, HIGH YELDS OF NITRILOTRIACETIC ACID ARE OBTAINED WHEN AMMONIA IS REACTED WITH CHLOROACETIC ACID IN THE PRESENCE OF PROMOTER QUANTITIES OF DIMETHYL SULFOXIDE.

10. 发明授权

US3578708A Metal sequestrant 失效
标题翻译：金属序列
公开(公告)号：US3578708A
公开(公告)日：1971-05-11
申请号：US3578708D
申请日：1967-11-02
申请人： HOOKER CHEMICAL CORP
发明人： CARLSON RONALD H
IPC分类号： C01B15/037 , C02F5/14 , C07F9/30 , C07F9/38 , C07F9/50 , C07F9/53 , C11D3/36 , C23G1/00 , C07C101/26
CPC分类号： C23G1/00 , C01B15/037 , C02F5/14 , C07F9/30 , C07F9/38 , C07F9/50 , C07F9/53 , C07F9/5304 , C11D3/365 , Y10S210/912
摘要： THIS INVENTION RELATES TO NOVEL COMPOUNDS USEFUL AS A SEQUESTRANT, AND AS A STABILIZER FOR HYDROGEN PEROXIDE, AGAINST CONTAMINATING CATALYST IONS SUCH AS CUPRIC, FERRIC AND MANGANOUS IONS WHICH CAUSE DECOMPOSITION OF HYDROGEN PEROXIDE FOR EXAMPLE. ALTHOUGH THE NOVEL COMPOUNDS INCLUDED WITHIN THIS INVENTION ARE OF BROAD SCOPE, REPRESENTATIVE COMPOUNDS INCLUDE; HEXASODIUM TRIS(N,N-DIACETATOAMINOMETHYL)PHOSPHINE; TRISODIUM TRIS(N-ACETATOAMINOMETHYL)PHOSPHINE; TRIS(N,N - DIACETOAMINOMETHYL)PHOSPHINE; TETRASODIUM MONO(HYDROXYMETHYL)BIS(N,N - DIACETATOAMINOMETHYL) PHOSPHINE; AND DISODIUM BIS(HYDROXYMETHYL)N,N-DIACETATOAMINOMETHYL PHOSPHINE.
摘要翻译：通过使氨基羧酸膦螯合剂与含有过渡金属离子的水溶液接触，所述离子与氨基羧酸膦反应形成可溶性络合物。由于过氧化氢的分解是通过痕量金属离子（如Cu ++，MN ++）和Fe +++的存在催化的，因此将这些螯合剂加入到过氧化物溶液中可以失活从而降低其对过氧化物组成的催化作用。这样的试剂还用于控制水的硬度并且在织物加工和金属清洁和整理中使不令人反感的金属离子失活。

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