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1. 发明授权

US3890319A (2-imidazolin-2-y(amino) substituted quinolines, -quinoxalines and -quinazolines as antihypertensive agents 失效
标题翻译：（2-IMIDAZOLIN-2-Y（AMINO）取代的喹啉， - 喹唑啉和等离子体作为抗菌剂
公开(公告)号：US3890319A
公开(公告)日：1975-06-17
申请号：US33248573
申请日：1973-02-14
申请人： PFIZER
发明人： DANIELEWICZ JOHN C , SNAREY MICHAEL , THOMAS GEOFFREY N
IPC分类号： A61K31/495 , A61K31/505 , A61P9/12 , B01J23/00 , C07B61/00 , C07D215/18 , C07D215/38 , C07D215/40 , C07D241/42 , C07D241/44 , C07D401/12 , C07D403/12 , C07D51/78
CPC分类号： C07D403/12 , A61K31/505 , C07D215/18 , C07D215/38 , C07D215/40 , C07D241/42
摘要： Novel (2-imidazolin-2-ylamino)substituted quinolines, quinoxalines and -quinazolines, their preparation and use as antihypertensive agents are described.

2. 发明授权

US3864336A Imines, their preparation and their pharmaceutical use 失效
标题翻译：辛胺，他们的制剂和药物用途
公开(公告)号：US3864336A
公开(公告)日：1975-02-04
申请号：US35930873
申请日：1973-05-11
申请人： BAYER AG
发明人： SENG FLORIN , LEY KURT , METZGER KARL GEORG
IPC分类号： A23K1/16 , C07D241/52 , C07D277/18 , C07D401/12 , C07D491/04 , C07D51/78
CPC分类号： C07D277/18 , A23K20/116 , A23K20/137 , C07D241/52 , C07D401/12 , C07D491/04
摘要： Imines of 2-formylquinoxaline-3-carboxylic acid-1,4-dioxides and their salts are obtained through treatment of the lactone or a salt of 2-dihydroxymethylquinoxaline-N,N-dioxide-3-carboxylic acid with a reactant bearing a free primary amino group. The resultant compounds and their non-toxic salts are antibacterial agents and can be incorporated in pharmaceutical compositions and feedstuffs for this use. A typical embodiment is 2(carbomethoxyhydrazonomethyl)-quinoxaline-3-carboxylic acid-1,4dioxide.
摘要翻译： 2-甲酰基喹喔啉-3-羧酸-1,4-二氧化物及其盐的亚胺通过用含有自由基的反应物处理内酯或2-二羟基甲基喹喔啉-N，N-二甲基-3-羧酸的盐得到伯氨基。所得化合物及其无毒盐是抗菌剂，可以并入用于该用途的药物组合物和饲料中。典型的实施方案是2-（甲酯基亚肼基甲基） - 喹喔啉-3-羧酸-1,4-二氧化物。

3. 发明授权

US3682906A Certain 2 - hydroxymethyl-3-carboxylic acid amidoquinoxaline-di-n-oxides (1,4) 失效
标题翻译：某些2-羟基甲基-3-羧酸酰胺氧基 - 二氧化氮（1,4）
公开(公告)号：US3682906A
公开(公告)日：1972-08-08
申请号：US3682906D
申请日：1969-11-28
申请人： BAYER AG
发明人： SENG FLORIN , LEY KURT , METZER KARL GEORG
IPC分类号： A61K20060101 , C07D20060101 , C07D241/52 , C07D491/04 , C07D51/78
CPC分类号： C07D241/52 , C07D491/04
摘要： CERTAIN 2-HYDROXYMETHYL-3-CARBOXYLIC ACID AMIDOQUINOXALINE-DI-N-OXIDES(1,4) ARE PROVIDED HAVING ANTIBACTERIAL ACTIVITY AGAINST BOTH GRAM-NEGATIVE AND GRAMPOSITIVE ORGANISMS. THE COMPOUNDS ARE USEFUL ALSO IN ANIMAL FEEDS AND DRINKING WATER AND ARE MADE BY REACTING THE CORRESPONDING LACTONE WITH AMMONIA OR AN AMINE IN A DILUENT AT 0* TO 80*C.

4. 发明授权

US3654275A Quinoxalinecarboxamide antiinflammatory agents 失效
标题翻译：喹喔啉甲酰胺抗炎药
公开(公告)号：US3654275A
公开(公告)日：1972-04-04
申请号：US3654275D
申请日：1969-10-15
申请人： PFIZER & CO C
发明人： MCMANUS JAMES M
IPC分类号： C07D241/44 , C07D51/78
CPC分类号： C07D241/44
摘要： 1,2,3,4-TETRAHYDRO - 1 - ACYL-3-OXO-2-QUINOXALINECARBOXAMIDES, A NOVEL CLASS OF HETERCYCLIC COMPOUNDS POSSESSING ANTINFLAMMATORY ACTIVITY.

5. 发明授权

US3647793A 2-piperidino-3-phenylquinoxaline compounds 失效
标题翻译： 2-哌啶-3-基苯基喹啉化合物
公开(公告)号：US3647793A
公开(公告)日：1972-03-07
申请号：US3647793D
申请日：1969-11-05
申请人： LILLY CO ELI
发明人： SOPER QUENTIN FRANCIS
IPC分类号： C07D241/42 , C07D51/78
CPC分类号： C07D241/42
摘要： AND ITS ACID ADDITION SALTS, WHEREIN R, AS ABOVE, REPRESENTS HALO OR METHYL, SAID R BEING LOCATED ON THE 6 OR 7 POSITION, ONLY, AND N REPRESENTS AN INTEGER OF FROM 0 TO 1, BOTH INCLUSIVE.
THE PRESENT INVENTION IS CONCERNED WITH METHODS AND COMPOSITIONS USEFUL IN INHIBITING THE GROWTH OF PLANTS, AND IS PARTICULARLY DIRECTED TO METHOD EMPLOYING AND COMPOSITIONS COMPRISING AN ACTIVE AGENT WHICH IS A COMPOUND OF THE FORMULA

2-R'',3-PHENYL,(R)N-QUINOXALINE

OR ITS ACID ADDITION SALTS, WHEREIN R REPRESENTS HALO OR METHYL, SAID R BEING LOCATED ON THE 6 OR 7 POSITION, ONLY; R'' REPRESENTS HALO, HYDROXY, LOWERALKOXY, AMINO, N-LOWERALKYLAMINO, DI-N-LOWERALKYLAMINO, OR PIPERIDINO; AND N REPRESENTS AN INTEGER OF FROM 0 TO 1, BOTH INCLUSIVE. THE PRESENT INVENTION IS ALSO DIRECTED TO THE NOVEL COMPOUND OF THE FORMULA

2-PIPERIDINO,3-PHENYL,(R)N-QUINOXALINE

6. 发明授权

US3644363A 1 4-dioxidoquinoxalinyl nitrones 失效
标题翻译： 1 4-DIOXIDOQUINOXALINYN NONRONES
公开(公告)号：US3644363A
公开(公告)日：1972-02-22
申请号：US3644363D
申请日：1969-09-02
申请人： RICHARDSON MERRELL INC
发明人： KIM HYUN KOO
IPC分类号： C07D241/52 , C07D51/78
CPC分类号： C07D241/52
摘要： 1,4-DIOICXIDOQUINOXALINYL NITRONES HAVING THE FORMULA

1,4-DI(O=),2-(R1-N(=O)=CH-),3-(R2-),R3,R4-QUINOXALINE

IN WHICH R1 IS AN ALKYL RADICAL OF 1 TO 10 CARBON ATOMS OF STRAIGH, BRANCHED OR CYCLIC CONFIGURATION WHICH MAY BE SUBSTITUTED WITH HYDROXY, DIHYDROXY, ALKOXY, ACLOXY, HALOGEN, OR TRIHALO GROUPS; OR R1 MAY BE A PHENYL RADICAL OR A PHENYL RADICAL SUBSTITUTED WITH A LOWER ALKYL GROUP OF 1 TO 4 GROUP CARBON ATOMS OR A HALOGEN; R2 IS HYDROGEN, LOWER ALKYL OF 1 TO 4 CARBON ATOMS, AND R3 AND R4 ARE CHOSEN FROM THE GROUP CONSISTING OF HYDROGEN, ALKOXY OR ALKYL OF 1 TO 4 CARBON ATOMS, HALOGEN, TRIHALOMETHYL, OR NITRO GROUPS. THESE NEW COMPOUNDS, WHICH ARE POTENT ANTIBACTERIAL AGENTS, ARE EFFECTIVE ORALLY, TOPICALLY AND PARENTERALLY IN LOW CONCENTRATIONS IN INHIBITING THE GROWTH OF BOTH GRAM-NEGATIVE AND GRAMPOSITIVE BACTERIA. THE COMPOUNDS MAY BE MADE BY REACTING AN APPROPRIATE 2-FORMYLQUINOXALINE 1,4-DIOXIDE WITH AN N-SUBSTITUTED HYDROXYLAMINE.

7. 发明授权

US3642796A Process for the preparation of quinoxaline-di-n-oxide-aldehyde 失效
标题翻译：制备喹喔啉二氧化物 - 二氧化锆的方法
公开(公告)号：US3642796A
公开(公告)日：1972-02-15
申请号：US3642796D
申请日：1970-06-16
申请人： BAYER AG
发明人： SENG FLORIN , LEY KURT
IPC分类号： C07D241/52 , C07D491/04 , C07D51/78
CPC分类号： C07D241/52 , C07D491/04
摘要： QUINOXALINE-DI-N-OXIDE-ALDEHYDE IS PRODUCTED BY HEATING QUINOXALINE-DI-N-XIDE-HYDROXY-LACTONE OF THE FORMULA:

1,4,9-TRI(O=),3-(HO-)-1,3-DIHYDROFURO(3,4-B)QUINOXALINE

IN AN AQUEOUS OR ORGANIC DILUENT OR IN A MIXTURE THEREOF TO A TEMPERATURE OF FROM ABOUT 50*C. TO ABOUT 150* C. UNTIL EVOLUTION OF CARBON DIOXIDE HAS SUBSTANTIALLY ENDED.

8. 发明授权

US3639397A 2-amino-3-amidino-quinoxaline-di-noxides and their production 失效
标题翻译： 2-氨基-3-氨基喹啉 - 二氧化氮及其生产
公开(公告)号：US3639397A
公开(公告)日：1972-02-01
申请号：US3639397D
申请日：1968-07-29
申请人： BAYER AG
发明人： SENG FLORIN , LEY KURT , METZGER KARL-GEORG , FRITSCHE DIETER
IPC分类号： C07D241/52 , C07D51/78
CPC分类号： C07D241/52
摘要： OR A COMPOUND IN WHICH THE BENZENE RING IS SUBSTITUTED BY LOWER ALKYL, LOWER ALKOXY OR HALOGEN. THE DIMETHYLAMINO GROUP CAN BE REPLACED BY VARIOUS HETEROCYCLIC RADICALS, BY HYDROXYALKYL, ETC. THE COMPOUNDS ARE ACTIVE AGAINST E, COLI, KLEBSIELLA, S AUREUS, DIPLOCOCCUS PNEUMONIAE, PROTEUS MIRABILIS, PSEUDOMONAS AERUGINOSA, ETC. AT A DOSAGE OF 25 TO 500 MG./KG. AND MAY BE COMBINED WITH USUAL CARRIERS OR VEHICLES.

1-(O=),2-(H3C-N(-CH3)-C(=NH)-),3,4-(-NH-H-O=)QUINOXALINE

NEW COMPOUNDS ARE PROVIDED HAVING ANTIBACTERIAL ACTIVITY AND WHICH ARE 2-AMINO-3-AMIDINO-QUINOXALINE-DINOXIDES PREPARED FROM 2-AMINO-3-CYANO-QUINOXALINE-DI-NOXIDES AS BY MEANS OF REACTION WITH PIPERIDINE. A TYPICAL COMPOUND IS:

9. 发明授权

US3598820A 2 - isothiouronium-methyl - 3 - carboxylic acid amido-quinoxaline - 1,4 - di-n-oxide halides and their production 失效
标题翻译： 2-异丙基-3-甲氧基亚氨基 - 喹喔啉-1,4-二氧化氮铪及其生产
公开(公告)号：US3598820A
公开(公告)日：1971-08-10
申请号：US3598820D
申请日：1968-10-02
申请人： BAYER AG
发明人： LEY KURT , EHOLZER ULRICH , NAST ROLAND , METZGER KARL-GEORG , FRITSCHE DIETER
IPC分类号： C07D241/52 , C07D51/78
CPC分类号： C07D241/52
摘要： 2-ISOTHIOURONIUM-METHYL-3-CARBOXYLIC ACID-AMIDO-QUINOXALINE-1,4-DI-N-OXIDE HALIDES OF THE FORMULA:

(R1-,1,4-DI-O-,2-R2-N(-R3)-CO-,3-H2N-C(=NH2(+))-S-CH2-

QUINAZOLINE)(+) HAL(-) (I)

WHEREIN

R1 IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY OR CHLORINE, R2 IS HYDROGEN, STRAIGHT OR BRANCHED CHAIN ALKYL OR STRAIGHT OR BRANCHED CHAIN ALKYL SUBSTITUTED BY HYDROXY LOWER ALKOXY, ACYLOXY, MONOALKYLAMINO OR DIALKYLAMINO, R3 IS HYDROGEN, STRAIGHT OR BRANCHED CHAIN ALKYL, STRAIGHT OR BRANCHED CHAIN ALKYL SUBSTITUTED BY HYDROXY, LOWER ALKOXY, ACYLOXY, MONOALKYLAMINO OR DIALKYLAMINO, OR WHEN R2 IS HYDROGEN, CYCLOHEXYL, OR R2 AND R3 TOGETHER WITH THE AMIDE NITROGEN ATOM FORM PART OF A 5- OR 6-MENBERED HETEROCYCLIC RING, AND HAL IS CHLORINE OR BROMINE,

ARE USEFUL FOR THEIR ANTIBACTERIAL EFFECT. THESE COMPOUNDS MAY BE PRODUCED, INTER ALIA, BY REACTING A 2-HALOMETHYL3-CARBOXYLIC ACID AMIDO-QUIOXALINE-1,4-DI-N-OXIDE OF THE FORMULA:

R1-,1,4-DI-O
WITH THIOUREA, WHEREIN R1, R2, R3 AND HAL ARE AS ABOVE DEFINED.
摘要翻译： 2-异硫脲鎓 - 甲基-3-羧酸 - 酰氨基喹喔啉-1,4-二-N-氧化物的下式：

10. 发明授权

US3598819A Quinoxaline derivatives and process for producing the same 失效
标题翻译：喹啉衍生物及其生产方法
公开(公告)号：US3598819A
公开(公告)日：1971-08-10
申请号：US3598819D
申请日：1968-09-26
申请人： MERCK & CO INC
发明人： STAPLEY EDWARD O , MATA JUSTO M , WOLF FRANK J , MILLER THOMAS W
IPC分类号： C07D241/52 , C07D51/78
CPC分类号： C07D241/52 , Y10S435/886
摘要： A NOVEL ANTIBIOTIC SUBSTANCE, IDENTIFIED AS 6-CHLORO-2QUINOXALINECARBOXYLIC ACID 1,4-DIOXIDE, HAS BEEN PRODUCED BY CULTIVATING STRAINS OF STREPTOMYCES AMBOFACIENS, VAR. NRRL 3455. THE SALTS, AS WELL AS DERIVATIVES SUCH AS ESTERS, AMIDES AND N-SUBSTITUTED AMIDES, LIKEWISE DEMONSTRATE ANTIBIOTIC ACTIVITY.

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