公开(公告)号：US3686181A

公开(公告)日：1972-08-22

申请号：US3686181D

申请日：1969-10-29

Applicant: BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  SENG FLORIN

IPC: C07D241/52 ,  C07D491/04 ,  C07D51/78

CPC classification number: C07D241/52 ,  C07D491/04

Abstract: NEW QUINOXALINE-DI - N - OXIDE-LACTONES HAVING ANTIFUNGAL ACTIVITY ARE PROVIDED WHICH ARE PREPARED FROM A 2 - ACYLOXY-METHYL-3-CARBOXAMIDO-QUINOXALINE - DI - NOXIDE-(1,4) STARTING MATERIAL BY REACTION WITH AN INORGANIC OR ORGANIC ACID AT A TEMPERATURE OF 0* TO 100*C. IN A DILUENT.

公开(公告)号：US3682902A

公开(公告)日：1972-08-08

申请号：US3682902D

申请日：1970-06-08

Applicant: BAYER AG

Inventor： OERTEL HARALD ,  EHOLZER ULRICH ,  ROSENDAHL FRIEDRICH-KARL

IPC: C07D295/28 ,  C08F2/38 ,  C10L1/14 ,  C10L1/22 ,  C10L1/24 ,  C07D93/10 ,  C07D51/70 ,  C07D87/38

CPC classification number: C07D295/32 ,  C08F2/40 ,  C10L1/14 ,  C10L1/226 ,  C10L1/231 ,  C10L1/232 ,  C10L1/2412 ,  C10L1/2456

Abstract: A SEMICARBAZIDE HAVING THE FORMULA

(3-R,HO,((R2)3-C-)PHENYL)-CH2-(CH2)N-NH-CO-NH-N
CH2-X-(CH2)2-)

WHEREIN

R IS ALKYL WITH 1 TO 12 CARBON ATOMS, PREFERABLY ALKYL WITH 1 TO 4 CARBON ATOMS SUCH AS METHYL OR TERTIARY BUTYL; R2 IS ALKYL WITH 1 TO 8 CARBON ATOMS; THE -OH GROUP IS IN THE 2 OR 4 POSITION; N IS AN INTEGER FROM 0 TO 12, PREFERABLY 3 OR 2; R'' IS HYDROGEN OR ALKYL WITH 1 TO 4 CARBON ATOMS AND PREFERABLY METHYL; AND X IS A DEVALENT INORGANIC RADICAL, PREFERABLY>N-NH2, -O-, OR >SO2. SUCH COMPOUNDS ARE USEFUL TO STABILIZE ISOCYANATES AGAINST DISCOLORATION DURING STORAGE.

公开(公告)号：US3660398A

公开(公告)日：1972-05-02

申请号：US3660398D

申请日：1970-04-07

Applicant: BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  SENG FLORIN ,  NAST ROLAND

IPC: C07D241/52 ,  C07D51/78

CPC classification number: C07D241/52

Abstract: QUINOXALINE-DI-N-OXIDES, HAVING PHARMACOLOGICAL PROPERTIES AND USABLE AS INTERMEDIATES FOR PRODUCTING PLANT PROTECTING AGENTS, PRODUCED BY REACTING IN AN ORGANIC DILUENT (E.G. AT 20-100*C.) BENZOFURAZANE-N-OXIDE (OPTIONALLY SUBSTITUTED WITH HALO, ALKYL, ALKOXY, ACYL, SUBSTITUTED ACYL, AMIDO, SUBSTITUTED AMIDO, SULFONAMIDO, AND/ OR SUBSTITUTED SULFONAMIDO)WITH A REAGENT COMPOSED OF EITHER (A) AT LEAST AN EQUIVALENT QUANTITY OF BOTH AN ORGANIC CARBONYL COMPOUND (E.G. LINERR OR CYLCLO ALIPHATIC, ARYL, OR HETEROCYCLIC CARBONYL COMPOUND) WITH IS OPTIONALLY SUBSTITUTED AND WHICH CONTAINS THE LINKAGE

-CH2-CO-

AND A PRIMARY ALIPHATIC AMINE OR AMMONIA; OR (B) AT LEAST AN EQUIVALENT QUANTITY OF THE CORRESPONDING SCHIFF''S BASE TO THE REAGENT UNDER (A).

公开(公告)号：US3660391A

公开(公告)日：1972-05-02

申请号：US3660391D

申请日：1968-10-02

Applicant: BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  NAST ROLAND ,  METZGER KARL GEORG ,  FRITSCHE DIETER

IPC: C07D241/52 ,  C07D51/78

CPC classification number: C07D241/52

Abstract: 2-METHYL-3-CARBOXYLIC ACID-AMIDO-QUINOXALINE - 1,4-DIN-OXIDES OF THE FORMULA:

1,4-DI(O=),2-CH3,3-(R2-N(-R3)-OC-),R1-QUINOXALINE

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, CARBALKOXY, MONOALKYLAMINO OR DIALKYLAMINO, AND R3 IS HYDROGEN, STRAIGHT OR BRANCHED CHAIN ALKYL, STRAIGHT OR BRANCHED CHAIN ALKYL SUBSTITUTED BY HYDROXY, LOWER ALKOXY, CARBALKOXY, MONOALKYLAMINO OR DIALKYLAMINO, OR WHEN R2 IS IS HYDROGEN, CYCLOHEXYL, OR R2 AND R3 TOGETHER WITH THE AMIDE NITROGEN ATOM FORM PART OF A 5OR 6-MEMBERED HETEROCYCLIC RING, ARE USEFUL FOR THEIR ANTIBACTERIAL EFFECT. THESE COMPOUNDS MAY BE PRODUCED, INTER ALIA, BY REACTING A BENZOFUROXAN OF THE FORMULA:

1-(O=),R1-BENZOFURAZAN

WITH AN ACETOACETIC ACID AMIDE OF THE FORMULA:

CH3-CO-CH2-CO-N(-R2)-R3

WHEREIN R1, R2 AND R3 ARE AS ABOVE DEFINED.

公开(公告)号：US3651229A

公开(公告)日：1972-03-21

申请号：US3651229D

申请日：1969-11-12

Applicant: BAYER AG ,  DIETER FRITSCHE

Inventor： LEY KURT ,  EHOLZER ULRICH ,  METZGER KARL GEORG

IPC: C07D241/52 ,  A61K27/00

CPC classification number: C07D241/52

Abstract: PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHYL-3AMIDINO-QUINOXALINE-1,4-DI-N-OXIDES OF THE FORMULA:

1,4-DI(O=),2-(R2-NH-C(=NH)-),3-(CH3-),R1-QUINOXALINE

WHEREIN:

R1 IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY OR CHLORINE, AND R2 IS HYDROXY OR AMINO,

IN COMBINATION WITH A PHARMACEUTICALLY ACCEPTABLE INSERT CARRIER ARE USEFUL AS ANTIBACTERIAL AGENTS.

1,4-DI(O=),2-(NC-),3-(CH3-),R1-BENZENE

THESE COMPOSITIONS OR THE ACTIVE COMPOUND CAN BE ADMINISTERED SUBCUTANEOUSLY OR ORALLY TO HUMANS AND ANIMALS.

公开(公告)号：US3639400A

公开(公告)日：1972-02-01

申请号：US3639400D

申请日：1969-08-25

Applicant: BAYER AG

Inventor： NAST ROLAND ,  LEY KURT ,  EHOLZER ULRICH ,  METZGER KARL-GEORG ,  FRITSCHE DIETER

IPC: C07D241/52 ,  C07D51/78

CPC classification number: C07D241/52

Abstract: 3-CARBOXYLIC ACID-AMIDO-QUINOXALINE-DI-N-OXIDES-(1,4) OF THE FORMULA:

1,4-DI(O=),2-(R4-CH(-OH)-COO-CH2-),3-(R2-N(-R3)-CO-),R1-

QUINOXALINE

WHEREIN: R1 IS HYDROGEN, LOWER ALKYL, LOWER ALKOXYL, HYDROXY OR AN ACLOXY MOIETY OF A LOWER ALIPHATIC CARBOXYLIC ACID AND WHEREIN R1 IS FROM 1 TO 5 SUCH MOIETIES, R2 IS HYDROGEN, AND ALIPHATIC MOIETY OR AN ALIPHATIC MOIETY SUBSTITUTED BY HYDROXY, LOWER ALKOXY, CARBALKOXY, MONOALKYLAMINO OR DIALKYLAMINO, R3 IS HYDROGEN AND ALIPHATIC MOIETY OR LAN ALIPHATIC MOIETY SUBSTITUTED BY HYDROXYL, LOWR ALKOXY, CARBALKOXY, MONOALKYLAMINO OR DIALKYLAMINO, OR R2 AND R3 ARE EACH LOWER ALKYL LINKED TOGETHER WITH THE AMIDE NITROGEN TO FROM A 5-,6- OR 7-MEMBERED HETEROCYCLIC RING OR R2 AND R3 ARE EACH LOWER ALKYL LINKED TOGETHER WITH AN AMIDE NITROGEN TO FORM A 5-, 6- RO 7-MEMBERED HETEROCYCLIC RING HAVING N OR O AS A SECOND HETEROATOM, AND R4 IS HYDROGEN, LOWER ALKYL OR SUBSITURED OR UNSUBSTITUTED PHENYL, ARE USEFUL FOR THEIR ANTIBACTERIAL ACITVITY.

公开(公告)号：US3538046A

公开(公告)日：1970-11-03

申请号：US3538046D

申请日：1967-11-30

Applicant: BAYER AG

Inventor： OERTEL HARALD ,  ROSENDAHL FRIEDRICH-KARL ,  EHOLZER ULRICH

IPC: C07C59/52 ,  C07C243/32 ,  C08K5/25 ,  C08K5/26 ,  C08G51/60

CPC classification number: C08K5/25 ,  C07C59/52 ,  C07C243/32 ,  C08K5/26 ,  C08L75/04

公开(公告)号：US3694555A

公开(公告)日：1972-09-26

申请号：US3694555D

申请日：1970-02-16

Applicant: KURT LEY ,  ULRICH EHOLZER ,  ROLAND NAST ,  KARL GEORG METZGER ,  DIETER FRITSCHE ,  BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  NAST ROLAND ,  METZGER KARL GEORG ,  FRITSCHE DIETER

IPC: C07D241/52 ,  A61K27/00

CPC classification number: C07D241/52

Abstract: Pharmaceutical compositions are provided for controlling bacterial infections caused by gram-positive and gram-negative bacteria containing a 3-carboxylic acid amido-quinoxaline-1,4-diN-oxide as active ingredient, as exemplified by 2-acetoxymethyl3-carboxylic acid ethylamidoquinoxaline-di-N-oxide and its congeners. The dosage ranges from 5 mg/kg to 150 mg/kg daily orally or parenterally.

公开(公告)号：US3558624A

公开(公告)日：1971-01-26

申请号：US3558624D

申请日：1968-10-02

Applicant: BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  NAST ROLAND ,  METZGER KARL GEORG ,  FRITSCHE DIETER

IPC: C07D241/52 ,  C07D51/78

CPC classification number: C07D241/52

Abstract: COMPOUNDS, AND COMPOSITIONS CONTAINING THEM, ARE PROVIDED FOR CONTROLLING BACTERIAL INFECTIONS CAUSED BY GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA. THE COMPOUNDS ARE 3-CARBOXYLIC ACID AMIDO-QUINOXALINE-1,4-DI-N-OXIDES EXEMPLIED BY 2-ACETOXYMETHYL-3-CARBOXYLIC ACID ETHYLAMIDOQUINOXALINE-DI-N-OXIDE AND ITS CONGENERS PREPARED BY REACTING A 2-HALOMETHYL-3-CARBOXYLIC ACID AMIDO-QUINOXALINE,1,4-DI-N-OXIDE, WHEREIN HALO IS CHLORO OR BROMO, WITH A MONOCARBOXYLIC ACID ALKALI SALT IN AN ORGANIC SOLVENT WITH OR WITHOUT WATER PRESENT AT 40-160*C. THE SALT IS OF THE TYPE

ALKYL-CO-X-M OR PHENYL-CO-X-M

WHERE X IS S OR O AND M IS NA, K OR NH4. THE ALKYL GROUP CAN BE HALOGENATED AND THE PHENYL GROUP CAN BE SUBSTITUTED BY HYDROXY, METHYOXY OR ACETOXY. THE DOSAGE RANGES FROM 5 MG./KG. TO 150 MG./KG. DAILY ORALLY OR PARENTERALLY.

Abstract translation: 提供药物组合物用于控制由含有3-羧酸酰氨基 - 喹喔啉-1,4-二-N-氧化物的革兰氏阳性和革兰氏阴性菌作为活性成分引起的细菌感染，例如2-乙酰氧基甲基-3- 羧酸乙酰氨基喹喔啉二-N-氧化物及其同系物。 每日口服或非肠道给药的剂量范围为5mg / kg至150mg / kg。

公开(公告)号：US3557109A

公开(公告)日：1971-01-19

申请号：US3557109D

申请日：1968-10-02

Applicant: BAYER AG

Inventor： LEY KURT ,  EHOLZER ULRICH ,  NAST ROLAND ,  METZGER KARL-GEORG ,  FRITSCHE DIETER

IPC: C07D241/52 ,  C07D51/78

CPC classification number: C07D241/52

Abstract: 2-HALOMETHYL-3-CARBOXYLIC ACID-AMIDO-QUINOXALINE-1,4DI-N-OXIDES OF THE FORMULA:

2-(R2-N(-R3)-CO-),3-(HAL-CH2-),R1-QUINOXALINE 1,4-DIOXIDE

WHEREIN R1, R2 AND R3 ARE AS ABOVE DEFINED.

2-(R2-N(-R3)-CO-),3-CH3,R1-QUINOXALINE 1,4-DIOXIDE

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, MONALKYLAMINO 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-MEMBERED HETEROCYCLIC RING, AND HAL IS CHLORINE OR BROMINE, ARE USEFUL FOR THEIR ANTIBACTERIAL EFFECT. THESE COMPOUNDS MAY PRODUCED, INTER ALIA, BY CHORINATING OR BROMINATING A 2-METHYL-O-CARBOXYLIC ACID AMIDO-QUINOXALINE-1,4-DI-NOXIDE OF THE FORMULA: