KR890006631A - 퀴놀론카르복실산 화합물 및 이의 약학적 용도 - Google Patents
퀴놀론카르복실산 화합물 및 이의 약학적 용도 Download PDFInfo
- Publication number
- KR890006631A KR890006631A KR1019880012996A KR880012996A KR890006631A KR 890006631 A KR890006631 A KR 890006631A KR 1019880012996 A KR1019880012996 A KR 1019880012996A KR 880012996 A KR880012996 A KR 880012996A KR 890006631 A KR890006631 A KR 890006631A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- oxoquinoline
- difluoro
- morpholino
- cyclopropyl
- Prior art date
Links
- XOQQVKDBGLYPGH-UHFFFAOYSA-N 2-oxo-1h-quinoline-3-carboxylic acid Chemical class C1=CC=C2NC(=O)C(C(=O)O)=CC2=C1 XOQQVKDBGLYPGH-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- -1 Quinolonecarboxylic acid compound Chemical class 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000000845 anti-microbial effect Effects 0.000 claims 2
- 239000004599 antimicrobial Substances 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- NTBFOBUDTNNTGO-UHFFFAOYSA-N 1-cyclopropyl-6,8-difluoro-7-[2-(methylaminomethyl)morpholin-4-yl]-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CNC)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F NTBFOBUDTNNTGO-UHFFFAOYSA-N 0.000 claims 1
- GSBGPIMFZFPCOK-UHFFFAOYSA-N 1-cyclopropyl-6,8-difluoro-7-[2-(morpholin-4-ylmethyl)morpholin-4-yl]-4-oxoquinoline-3-carboxylic acid Chemical compound C12=C(F)C(N3CC(CN4CCOCC4)OCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 GSBGPIMFZFPCOK-UHFFFAOYSA-N 0.000 claims 1
- QGJVTUIQIULLMU-UHFFFAOYSA-N 1-cyclopropyl-7-[2-(diethylaminomethyl)morpholin-4-yl]-6,8-difluoro-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CN(CC)CC)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F QGJVTUIQIULLMU-UHFFFAOYSA-N 0.000 claims 1
- VZZZYESOQUATCO-UHFFFAOYSA-N 1-cyclopropyl-7-[2-(ethylaminomethyl)morpholin-4-yl]-6,8-difluoro-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CNCC)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F VZZZYESOQUATCO-UHFFFAOYSA-N 0.000 claims 1
- LWNJCRBOLZSQHL-UHFFFAOYSA-N 1-cyclopropyl-7-[2-[(dimethylamino)methyl]morpholin-4-yl]-6,8-difluoro-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CN(C)C)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F LWNJCRBOLZSQHL-UHFFFAOYSA-N 0.000 claims 1
- LDNQYBHILWUHMH-UHFFFAOYSA-N 7-[2-(acetamidomethyl)morpholin-4-yl]-1-cyclopropyl-6,8-difluoro-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CNC(=O)C)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F LDNQYBHILWUHMH-UHFFFAOYSA-N 0.000 claims 1
- MVKGRIHKSLEKTE-UHFFFAOYSA-N 7-[2-(aminomethyl)morpholin-4-yl]-1-cyclopropyl-6,8-difluoro-4-oxoquinoline-3-carboxylic acid Chemical compound C1COC(CN)CN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F MVKGRIHKSLEKTE-UHFFFAOYSA-N 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (5)
- 하기식(I)의 퀴놀론카르복실산 화합물 및 이의 염.상기식에서 R1은 알킬기, 시클로알킬기, 할로알킬기, 알케닐기, 모노- 또는 디-알킬아미노기, 페닐기, 또는 할로겐 원자, 알킬기, 알콕시기, 히드록시기, 니트로기 또는 아미노기로 구성된 군에서 선책되는 1~3 치환체에 희해 치환된 페닐기이고, R2는 수소원자, 알킬기 시클로알킬기, 아실기 또는 알콕시카르보닐기 이고, R3은 수소원자, 알킬기 또는 아르알킬기이며, 또는 R2및 R3는 인접한 질소원자와 함께 헤테로환 고리를 형성하며, R4는 수소원자 또는 알킬기이고, R5는 수소원자, 알킬기, 아르아킬기, 또는 생체내에서 용이하게 가수분해 가능한 에스테르 잔기이고, X는 수소원자, 할로겐원자 또는 알킬기이고, n은 1~3의 정수이다.
- 제1항에 있어서, 1-시클로프로필-6,8-디플루오로-1,4-디히드로-7[2-(메틸아미노메틸)모르폴리노]-4-옥소퀴놀린-3-카르복실산,1-시클로프로필-6,8-디플루오로-1,4-디히드로-7-[2-(디메틸아미노메틸)모르폴리노]-4-옥소퀴놀린-3-카르복실산, 7-[2-(아미노메틸)모르폴리노]-1-시클로프로필-6,8-디플루오로-1,4-디히드로-4-옥소퀴놀린-3-카르복실산, 1-시클로프로필-7-[2-(에틸아미노메틸)모르폴리노]-6,8-디플루오로-1,4-디히드로-4-옥소퀴놀린-3-카르복실산, 1-시클로프로필-7-[2-(디에틸아미노메틸)모르폴리노]-6,8-디플루오로-1,4-디히드로-4-옥소퀴놀린-3-카르복실산, 7-[2-(아세틸아미노메틸)모르폴리노]-1-시클로프로필-6,8-디플루오로-1,4-디히드로-4-옥소퀴놀린-3-카르복실산, 1-시클로프로필-6,8-디플루오로-7-[2-(포르밀아미노메틸)모르폴리노]-1,4-디히드로-4-옥소퀴놀린-3-카르복실산, 1-시클로프로필-6,8-디플루오로-1,4-디히드로-7-[2-(모르포리노메틸)모르폴리노]-4-옥소퀴놀린-3-카르복실산 및 1-시클로프로필-7-[2-(시클프로필아미노메틸)모르폴리노-6,8-디플루오로-1,4-디히드로-4-옥소퀴놀린-3-카르복실으로 구성된 군에서 선택되는 식(I)의 퀴놀린카르복실산 화합물.
- 제1항에 있어서, 1-시클로프로필-6,8-디플루오로-1,4-디히드로-7-2[-(메틸아미노메틸)모르폴리노]-4-옥소퀴놀린-3-카르복실산인 식(I)의 퀴놀론카르복실산 화합물.
- 제1항의 화합물의 항균적 유효량 및 약학적으로 허용 가능한 담체로 구성됨을 특징으로 하는 약학 조성물.
- 제1항의 화합물의 항균적 유효량을 투여함을 특징으로 하는 각종 전염병의 치료방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (10)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP25677987 | 1987-10-12 | ||
JP256779/1987 | 1987-10-12 | ||
JP29475987 | 1987-11-20 | ||
JP294759/1987 | 1987-11-20 | ||
JP1935288 | 1988-01-28 | ||
JP19352/1988 | 1988-01-28 | ||
JP137909/1988 | 1988-06-03 | ||
JP13790988 | 1988-06-03 | ||
JP20400488 | 1988-08-17 | ||
JP204004/1988 | 1988-08-17 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR890006631A true KR890006631A (ko) | 1989-06-14 |
KR900009024B1 KR900009024B1 (ko) | 1990-12-17 |
Family
ID=27520129
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880012996A KR900009024B1 (ko) | 1987-10-12 | 1988-10-05 | 퀴놀론카르복실산 화합물 및 이의 약학적 용도 |
Country Status (3)
Country | Link |
---|---|
US (1) | US4889857A (ko) |
EP (1) | EP0311948A3 (ko) |
KR (1) | KR900009024B1 (ko) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3906365A1 (de) * | 1988-07-15 | 1990-01-18 | Bayer Ag | 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe |
AU6408894A (en) * | 1993-03-26 | 1994-10-24 | Schering Corporation | 2-substituted morpholine and thiomorpholine derivatives as gaba-b antagonists |
DE19652239A1 (de) * | 1996-12-16 | 1998-06-18 | Bayer Ag | Verwendung von 7-(2-Oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-chinolon- und -naphthyridoncarbonsäure-Derivaten zur Therapie von Helicobacter-pylori-Infektionen und den damit assoziierten gastroduodenalen Erkrankungen |
TWI452044B (zh) * | 2007-06-15 | 2014-09-11 | Mitsubishi Tanabe Pharma Corp | 嗎啉衍生物 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5746986A (en) * | 1980-09-02 | 1982-03-17 | Dai Ichi Seiyaku Co Ltd | Pyrido(1,2,3-de)(1,4)benzoxazine derivative |
US4670444B1 (en) * | 1980-09-03 | 1999-02-09 | Bayer Ag | and-naphthyridine-3-carboxylic acids and antibacte7-amino-1-cyclopropyl-4-oxo-1,4-dihydro-quinoline-rial agents containing these compounds |
US4665079A (en) * | 1984-02-17 | 1987-05-12 | Warner-Lambert Company | Antibacterial agents |
DE3318145A1 (de) * | 1983-05-18 | 1984-11-22 | Bayer Ag, 5090 Leverkusen | 7-amino-1-cyclopropyl-6,8-difluor-1,4-dihydro-4-oxo-3-chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel |
DE3409922A1 (de) * | 1984-03-17 | 1985-09-26 | Bayer Ag, 5090 Leverkusen | 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie ihre verwendung bei der bekaempfung bakterieller erkrankungen |
DE3509546A1 (de) * | 1985-03-16 | 1986-09-25 | Bayer Ag, 5090 Leverkusen | 7-amino-1-(subst.cyclopropyl)-1,4-dihydro-4-oxo-3-chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel |
DE3525108A1 (de) * | 1985-06-07 | 1986-12-11 | Bayer Ag, 5090 Leverkusen | Antibakteriell wirksame chinoloncarbonsaeureester |
-
1988
- 1988-09-29 US US07/250,634 patent/US4889857A/en not_active Expired - Fee Related
- 1988-10-05 KR KR1019880012996A patent/KR900009024B1/ko not_active IP Right Cessation
- 1988-10-10 EP EP88116770A patent/EP0311948A3/en not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
US4889857A (en) | 1989-12-26 |
EP0311948A3 (en) | 1990-05-09 |
EP0311948A2 (en) | 1989-04-19 |
KR900009024B1 (ko) | 1990-12-17 |
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