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1. 发明授权

US3654272A X-ray contrast media 失效
标题翻译： X射线对比媒介
公开(公告)号：US3654272A
公开(公告)日：1972-04-04
申请号：US3654272D
申请日：1969-08-13
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07C59/305 , C07C59/315 , C07C103/32
CPC分类号： A61K49/0452 , C07C59/305 , C07C59/315
摘要： THE DI-(3-CARBOXY-2,4,6-TRIIODOANILIDES) OR 4,7,10-TRIOXATRIDECANE-1,13-DIOIC ACID AND 4,7,10,13-TETRAOXAHEXADECANE-1,16-DIOIC ACID AND THE NON-TOXIC WATER-SOLUBLE SALTS THEREOF WITH METALS AND AMINES ARE EFFECTIVE, WELLTOLERATED X-RAY CONTRAST MEDIA WHICH TEND TO ACCUMULATE IN THE GALL BLADER WHEN THEIR AQUEOUS SOLUTIONS ARE INJECTED INTRAVENOUSLY.

2. 发明授权

US3557197A Radiopaque compounds 失效
标题翻译：放射性化合物
公开(公告)号：US3557197A
公开(公告)日：1971-01-19
申请号：US3557197D
申请日：1969-04-07
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07C51/02 , C07C51/41 , C07C51/60 , C07C103/32
CPC分类号： C07C51/412 , A61K49/0433 , C07C51/02 , C07C51/60 , C07C59/305
摘要： RADIOPAQUE COMPOUNDS OF THE FORMULA

((2,4,6-TRI(I-),3-(R-CO-NH-CH2-),5-(HOOC-)PHENYL)-NH-

CO-)2-X

ARE READILY CONVERTED TO THEIR WATER-SOLUBLE SALTS WITH SODIUM, LITHIUM, CALCIUM, MAGNESIUM, AND THE ALKANOLAMINES GENERALLY USED IN GALENIC PHARMACY, AND THE SOLUTIONS ARE GOOD CONTRAST MEDIA FOR INTRAVENOUS INJECTION IN CHOLECYSTOGRAPHY, AND PARTLY ALSO IN ANGIOGRAPHY. IN THE FORMULA, X IS ALKYLENE OR OXA-ALKYLENE HAVING 4-10 CARBON ATOMS, AND R IS LOWER ALKYL.

3. 发明授权

US3576854A Method of optically resolving racemic bases and optically active n-(1-phenylethyl)-carbamyl carboxylic acids for use in said method 失效
标题翻译：光聚合基团和光学活性N-（1-苯乙烯基） - 羧甲基羧酸的方法，用于合成方法
公开(公告)号：US3576854A
公开(公告)日：1971-04-27
申请号：US3576854D
申请日：1969-02-25
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： C07C233/00 , C07C103/34
CPC分类号： C07C233/00
摘要： THE OPTICALLY ACTIVE FORMS OF ACIDS OF THE FORMULA

PHENYL-CH(-CH3)-NH-CO-A-COOH

WHEREIN A IS A SINGLE CARBON-TO-CARBON BOND, A RADICAL OF THE FORMULA -(CH2)N- (N BEING AN INTEGER BETWEEN 1 AND 4), THE RADICAL -CH=CH-, OR PHENYLENE ARE READILY AVAILABLE FROM INEXPENSIVE STARTING MATERIALS AND WELL SUITED FOR FORMING DISASTEREOISOMERS WITH RACEMIC BASES. THE DIASTEREOISOMERS MAY BE FRACTIONATED BY CRYSTALLIZATION IN A CONVENTIONAL MANNER AND DECOMPOSED TO ISOLATE THE OPTICALLY ACTIVE FORMS OF THE BASE. THE ACID IS RECOVERED IN GOOD YIELD.

4. 发明授权

US3910989A N-triiodobenzyl-carbamic acid derivatives 失效
标题翻译： N-三碘苄基 - 氨基甲酸衍生物
公开(公告)号：US3910989A
公开(公告)日：1975-10-07
申请号：US48266574
申请日：1974-06-24
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07C67/00 , C07C239/00 , C07C269/00 , C07C271/22 , C07C125/06
CPC分类号： A61K49/0452
摘要： Water-soluble salts of pharmaceutically acceptable bases with N(2,4,6-triiodo-3-acylamino-5-carboxy-benzyl)-carbamic acid esters of the formula

ARE RELATIVELY NON-TOXIC, QUICKLY EXCRETED X-ray contrast agents suitable for intravenous administration. The carboxylic acids of the formula are monoesters of alcohols R1OH having up to four carbon atoms which are alkanols, mono- and dihydroxyalkanols, or alkoxyalkanols, when n is 1, and diesters of alcohols HO-R1-R1OH having up to 10 carbon atoms which are alkanediols or ethyleneglycol ethers when n is 2. R2 has up to three carbon atoms and is alkyl, hydroxyalkyl, or alkoxyalkyl.
摘要翻译：药学上可接受的碱的水溶性盐与式COOH | R2-CO-NHCH2-NH-CO-OR1的N-（2,4,6-三碘-3-酰基氨基-5-羧基 - 苄基） - 氨基甲酸酯 n相对非毒性，快速成型适用于静脉给药的X射线造影剂。下式的羧酸是当具有至多10个碳原子的醇为HO-R1-R1OH的二烷基酯时，具有至多4个碳原子的具有至多4个碳原子的醇，即烷醇，单羟基烷醇和二羟基链烷醇或烷氧基烷醇的单酯，当n为2时，它们是烷二醇或乙二醇醚.R 2具有至多三个碳原子，并且是烷基，羟基烷基或烷氧基烷基。

5. 发明授权

US3886203A 3-Hydroxyacyl aminomethyl-5-acylamino-2,4,6-triiodobenzoic acid salts as x-ray contrast agents 失效
标题翻译： 3-羟基酰基氨基甲基-5-酰基氨基-2,4,6-三碘苯甲酸盐作为X射线造影剂
公开(公告)号：US3886203A
公开(公告)日：1975-05-27
申请号：US48266674
申请日：1974-06-24
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/54 , C07C235/12 , C07C235/16 , C07C103/32
CPC分类号： A61K49/0433
摘要： The water-soluble, physiologically tolerated sodium and alkanolamine salts of 3-hydroxyacylaminomethyl-5-acylamino-2,4,6triiodobenzoic acids of the formula
WHEREIN R and R'''' are hydrogen or methyl, R'' is hydrogen or hydroxy, R'' is hydroxyl when R is hydrogen, and R'''' is hydrogen when R'' is hydrogen, are X-ray contrast agents suitable for urography and vasography and well tolerated when their aqueous solutions are injected into a vein.
摘要翻译：式WHEREIN R和R“的3-羟基酰基氨基甲基-5-酰基氨基-2,4,6-三碘苯甲酸的水溶性生理耐受性钠和链烷醇胺盐是氢或甲基，R'是氢或羟基，R 当R为氢时为羟基，当R'为氢时，R“为氢，为适用于尿路造影术和血管成像术的X线造影剂，当其水溶液注入静脉时，耐受性良好。

6. 发明授权

US3825591A Orally applicable contrast agents for cholecystography 失效
标题翻译： ORALLY适用的对照代理选择
公开(公告)号：US3825591A
公开(公告)日：1974-07-23
申请号：US25877772
申请日：1972-06-01
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： C07C235/84 , A61K49/04 , C07D295/192 , C07C101/72
CPC分类号： C07D295/192 , A61K49/0495
摘要： COMPOUNDS OF THE FORMULA

-CO-)-BENZENE

WHEREIN R1 IS METHYL OR ETHYL WHEN R2 IS HYDROGEN, OR R1 AND R2 JOINTLY ARE ETHYLENEOXYETHYLENE, AND R3 IS METHYL OR ETHYL, AND THEIR PHYSIOLOGICALLY TOLERATED ALKALI METAL, ALKALINE EARTH METAL, AND ALKANOLAMINE SALTS PRODUCE SUPERIOR X-RAY IMAGES OF THE GALL BLADDER AND OF THE BILE DUCTS AFTER ORAL INGESTION AND ARE WELL TOLERATED AND QUICKLY ELIMINATED IN EFFECTIVE DOSES.
1,3,5-TRI(I-),2-(HOOC-CH(-R3)-CH2-O-CH2-CH2-),4-(R1-N(-R2)

7. 发明授权

US3883535A Radiopaque derivatives of triiodobenzoic acid with heterocyclic side chains 失效
标题翻译：三碘苯甲酸与杂环侧链的不透射线衍生物
公开(公告)号：US3883535A
公开(公告)日：1975-05-13
申请号：US81419369
申请日：1969-04-07
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07D207/26 , C07D207/27 , C07D211/76 , C07D265/32 , C07D29/28 , C07D29/30
CPC分类号： C07D207/27 , A61K49/0433 , C07D211/76 , C07D265/32
摘要： Compounds of the formula R - R'', wherein

R1 is alkylene or oxaalkylene having 2 or 3 carbon atoms; R2 is -(CH2)a- or -CO-; R3 is hydrogen or lower alkanoyl; R4 is hydrogen, lower alkyl, or R-NH-CO-R5-CO-, R3 being hydrogen when R4 is R-NH-CO-R5-CO; R5 is alkylene or polyoxaalkylene having 4 to 8 carbon atoms; A IS ZERO OR ONE, AND -(CH2)a is a single carbon-to-carbon bond when a is zero; and A is hydrogen or a non-toxic metal or amine, the compound being water-soluble when A is metal or amine; have been found to be well tolerated, effective contrast media for the X-ray investigation of blood vessels, the urinary tract, and the gall bladder when used parenterally.
摘要翻译：式R-R'的化合物，其中R 1是具有2或3个碳原子的亚烷基或氧杂亚烷基; R2是 - （CH2）a-或-CO-; R3是氢或低级烷酰基; R4是氢，低级烷基或R-NH-CO-R5-CO-，当R4是R-NH-CO-R5-CO时，R3是氢; R5是具有4-8个碳原子的亚烷基或聚氧亚烷基; A是零或一个，和 - （CH 2）a是当a为零时的单个碳 - 碳键; A是氢或无毒的金属或胺，当A是金属或胺时，该化合物是水溶性的; 已被发现是耐受性良好的有效的造影剂，用于胃肠外使用时血管，尿道和胆囊的X线检查。

8. 发明授权

US3867431A Contrast agent for angiography and urography 失效
标题翻译：血管造影和尿路造影的对比剂
公开(公告)号：US3867431A
公开(公告)日：1975-02-18
申请号：US27497372
申请日：1972-07-25
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE , ZUTTER HANS
IPC分类号： A61K49/04 , C07C67/00 , C07C231/00 , C07C231/08 , C07C233/54 , C07C233/56 , C07C103/32
CPC分类号： A61K49/0433
摘要： 3-(N- Beta , gamma -dihydroxypropyl-acetyl-amino)-5acetylaminomethyl-2,4,6-triiodobenzoic acid and its non-toxic, water-soluble salts with alkali metals and amines are better tolerated by the central nervous system for intracerebral and intracisternal application than X-ray contrast agents available heretofore for cerebral angiography. They are preferentially excreted from the blood by the kidney in a manner to make them useful for urography.
摘要翻译： 3-（N-β-，γ-二羟丙基 - 乙酰基 - 氨基）-5-乙酰氨基甲基-2,4,6-三碘苯甲酸及其与碱金属和胺类无毒的水溶性盐，较好地被中枢神经脑内和脑内应用的系统比目前可用于脑血管造影术的X射线造影剂。它们优先通过肾脏从血液中排出，以使其可用于尿路造影术。

9. 发明授权

US3644409A Radiopaque compounds and methods of preparing the same 失效
标题翻译：放射性化合物及其制备方法
公开(公告)号：US3644409A
公开(公告)日：1972-02-22
申请号：US3644409D
申请日：1970-05-28
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07D207/26 , C07D207/27 , C07D211/02 , C07D211/76 , C07D265/32 , C07D27/08 , C07D29/22 , C07D87/30
CPC分类号： C07D207/27 , A61K49/0495 , C07D211/02 , C07D211/76 , C07D265/32
摘要： COMPOUNDS OF THE FORMULA

1,3,5-TRI(I-),4-(HOOC-ALK-Y-),6-((-CO-X-CH2-)>N-)BENZENE

ARE RADIOPAQUE, TEND TO COLLECT IN THE GALL BLADDER WHEN INGESTED ORALLY, AND ARE WELL TOLERATED, IF X HAS 2-4 CARBON ATOMS AND IS ALKYLENE OR ALKYLENOXYALKYLENE, Y IS A SINGLE CARBON-TO-CARBON BOND OR OXYGEN, AND AKL IS LOWER ALKYLENE OR PHENYL-LOWER-ALKYLENE HAVING NOT MORE THAN FOUR CARBON ATOMS IN THE ALKYLENE GROUP. THE PHYSIOLOGICALLY TOLERATED SALTS OF THE ABOVE CARBOXYLIC ACIDS HAVE THE SAME EFFECTS. THE COMPOUNDS ARE PREPARED BY CLOSURE OF THE RING

-N
WHEN OTHERWISE SIMILAR COMPOUNDS HAVING THE GROUP

-NH-CO-X-CH2-Z

ARE EXPOSED TO ALKALI METAL HYDROXIDE IN A STRONGLY ALKALINE AQUEOUS MEDIUM AND ARE PRECIPITATED WHEN THE MEDIUM IS ACIDIFIED AFTER RING FORMATION.

10. 发明授权

US3553260A Radiopaque derivatives of alpha-phenoxy-phenylacetic acid 失效
标题翻译：阿魏酸 - 苯甲酸的放射性衍生物
公开(公告)号：US3553260A
公开(公告)日：1971-01-05
申请号：US3553260D
申请日：1968-05-14
申请人： BRACCO IND CHIMICA SPA
发明人： FELDER ERNST , PITRE DAVIDE
IPC分类号： A61K49/04 , C07C103/32
CPC分类号： A61K49/0433
摘要： A - (3 - N-ALKYL-N-ACETYLAMINO-2,4,6-TRIIODOPHENOXY)PHENYLACETIC ACID AND CLOSELY RELATED DERIVATIVES OF THE FORMULA

1,3,5-TRI(I-),2-((R3-PHENYL)-CH(-COOH)-O-),4-(R2-CO-

N(-R1)-)BENZENE

WHEREIN R1 IS LOWER ALKYL, R2 IS HYDROGEN OR LOWER ALKYL, AND R3 IS HYDROGEN, HALOGEN OR LOWER ALKYL, AND THE PHYSIOLOGICALLY TOLERATED, WATER SOLUBLE METAL OR AMINE SALTS THEREOF ARE RADIOPAQUE, TEND TO ACCUMULATE IN THE GALL BLADDER WHEN APPLIIED ORALLY, AND ARE NON-TOXIC IN EFFECTIVE AMOUNTS. THE CORRESPONDING LOWER ALKYL ESTERS ARE INTERMEDIATES IN THE SYNTHESIS OF THE ACIDS AND SALTS.

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