KR900006347A - 살균성 플루오로퀴놀로닐 세펨 - Google Patents

살균성 플루오로퀴놀로닐 세펨 Download PDF

Info

Publication number
KR900006347A
KR900006347A KR1019890015236A KR890015236A KR900006347A KR 900006347 A KR900006347 A KR 900006347A KR 1019890015236 A KR1019890015236 A KR 1019890015236A KR 890015236 A KR890015236 A KR 890015236A KR 900006347 A KR900006347 A KR 900006347A
Authority
KR
South Korea
Prior art keywords
hydrogen
alkyl
heterocyclic ring
alkenyl
ring
Prior art date
Application number
KR1019890015236A
Other languages
English (en)
Other versions
KR0139638B1 (ko
Inventor
주니어 토마스 프로서 데무스
유겐 화이트 로날드
Original Assignee
노르위치 이튼 파마슈티칼즈, 인코포레이티드
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 노르위치 이튼 파마슈티칼즈, 인코포레이티드 filed Critical 노르위치 이튼 파마슈티칼즈, 인코포레이티드
Publication of KR900006347A publication Critical patent/KR900006347A/ko
Application granted granted Critical
Publication of KR0139638B1 publication Critical patent/KR0139638B1/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C07D501/34—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group

Abstract

내용 없음

Description

살균성 플루오로퀴놀로닐 세펨
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 하기 일반식(I)의 화합물 및 이의 약제학적으로 허용되는 염, 생가수분해성 에스테르 및 수화물.
    상기식에서, R1은 수소, 할로겐, 알킬, 알케닐, 헤테로알킬, 카보사이클릭환, 헤테로사이클릭환, R10a-C-, R10aCH=N-, (R10)(R11)N-, R12-C(=CHR15)-C(=O)NH-, R12-C(=NO-R14)-C(=O)NH-, 또는 R13-(CH2)m-C(=O)NH-이며, 바람직하게는 알킬, 알케닐, R12-C(=NO-R14)-C(=O)NH-, 또는 R13-(CH2)m-C(=O)NH-이고, m은 0 내지 9, 바람직하게는 0 내지 3의 정수이며, R10및 R11은 각각 R10a이거나, R10및 R11이 함께는 이들이 결합된 질소를 함유한 헤테로사이클릭환을 포함하고, R10a는 수소, 알킬, 알케닐, 카보사이클릭환, 또는 헤테로사이클릭환 치환체이며, R12는 수소, 알킬, 알케닐, 헤테로알킬, 헤테로알케닐, 카보사이클릭환, 또는 헤테로사이클릭환이며, 바람직하게는 알킬, 카보사이클릭환 또는 헤테로사이클릭환이고, R13은 R12, -Z1또는 -CH(Z2)(R12)이며, R14는 R12아릴알킬, 헤테로아릴알킬, -C(=R17)(R18)COOH, -C(=O)O-R12, 또는 -C(=O)NH-R12이고, 바람직하게는 R12또는 -C(R17)(R18)COOH이며, R17및 R18은 각각 R12이거나, R17및 R18이 함께는 이들이 결합된 탄소원자를 함유한 카보사이클릭환 또는 헤테로사이클릭환을 포함하고, R15는 R14, 할로겐, -Z1, 또는 -CH(Z2)(R12)이며, 바람직하게는 R14또는 할로겐이고, Z1은 -C(=O)OR16, -C(=O)(R16), -N(R19)R16, -S(O)pR24, 또는 -OR24이며, Z2는 Z1, 또는 OH, -SH 또는 -SO3H이고, p는 0 내지 2의 정수이며, 바람직하게는 0이고, R19는 수소, 알킬, 알케닐, 헤테로알킬, 헤테로알케닐, 카보사이클릭환, 헤테로사이클릭환, -SO3H 또는 -C(=O)R20이거나, R13이 -CH(Z2)(R12)이고, Z2가 -N(R19)R16인 경우에 R19는 R16과 결합하여 헤테로사이클릭환을 형성하는 잔기를 포함할 수 있으며, R20은 R12, NH(R12), N(R12)(R21), O(R21), 또는 S(R21)이고, 바람직하게는 R12, NH(R12), 또는 N(R12)(R21)이며, R21은 알킬, 알케닐, 카보사이클릭환, 또는 헤테로사이클릭환이거나, R20이 N(R12)(R21)인 경우에 R21은 R12와 결합하여 헤테로사이클릭환을 형성하는 잔기일 수 있고, R16은 R24또는 수소이며, 바람직하게는 수소, 알킬, 카보사이클릭환 또는 헤테로사이클릭환이고, R24는 알킬, 알케닐, 아릴알킬, 헤테로알킬, 헤테로알케닐, 헤테로아릴알킬, 카보사이클릭환 또는 헤테로사이클릭환기어나, Z1이 N(R19)R16이고 R16이 R24인 경우에 R16및 R19는 함께 R19가 결합된 질소원자를 함유한 헤테로사이클릭환을 포함할 수 있으며, R2는 수소, 할로겐, 알콕시, 또는 R22(=O)NH-이고, 바람직하게는 수소 또는 알콕시이며, R22는 수소 또는 알킬이고, R3은 질소-함유 헤테로사이클릭환이며, C4는 수소, 하이드록시, 알콕시, 디트로, 시아노, 할로겐, 알킬 또는 N(R10)(R11)이다.
  2. 제1항에 있어서, R2가 수소 또는 알콕시인 화합물.
  3. 제1항에 있어서, R4가 수소 또는 할로이며, 바람직하게는 염소 또는 불소인 화합물.
  4. 제3항에 있어서, R3이 피페라진, 3-메틸피페라진, 3-아미노피롤리딘, 3-아미노메틸피롤리딘, N,N-디메틸이미노메틸피롤리딘, N-메틸이미노메틸피롤리딘, N-에틸아미노메틸피롤리딘, 피리딘, N-메틸피페라진, 또는 3,5-디메틸피페라진이며, 바람직하게는 피페라진인 화합물.
  5. 안전하고 유효한 양의 제1,2,3 또는 4항에 따른 화합물 및 약제학적으로 허용되는 담체를 함유함을 특징으로 하여, 인간 또는 다른 동물환자의 감연성 질환을 예방 또는 치료하기 위한 조성물.
  6. 제5항에 있어서, 비경구 투여에 적합한, 인간 또는 다른 동물환자의 감염성 질환을 예방 또는 치료하기 위한 조성물.
  7. 제5항에 있어서, 경구 투여에 적합한, 인간 또는 다른 동물환자의 감염성 질환을 예방 또는 치료하기 위한 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890015236A 1988-10-24 1989-10-24 살균성 플루오로퀴놀닐 세펨 KR0139638B1 (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US26194988A 1988-10-24 1988-10-24
US261,949 1988-10-24
US?261,949? 1988-10-24
US41802589A 1989-10-12 1989-10-12
US?418,025? 1989-10-12
US418,025 1989-10-12

Publications (2)

Publication Number Publication Date
KR900006347A true KR900006347A (ko) 1990-05-08
KR0139638B1 KR0139638B1 (ko) 1998-06-01

Family

ID=26948930

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019890015236A KR0139638B1 (ko) 1988-10-24 1989-10-24 살균성 플루오로퀴놀닐 세펨

Country Status (14)

Country Link
EP (1) EP0366640B1 (ko)
JP (1) JPH03503421A (ko)
KR (1) KR0139638B1 (ko)
AT (1) ATE176473T1 (ko)
AU (1) AU620651B2 (ko)
CA (1) CA2001204A1 (ko)
DE (1) DE68928925T2 (ko)
DK (1) DK527389A (ko)
ES (1) ES2129388T3 (ko)
GR (1) GR3030052T3 (ko)
NZ (1) NZ231113A (ko)
PH (1) PH26519A (ko)
SG (1) SG54293A1 (ko)
WO (1) WO1990004595A1 (ko)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5147871A (en) * 1986-07-03 1992-09-15 Hoffmann La-Roche, Inc. Anti-bacterial cephalosporin compounds
US5336768A (en) * 1988-05-24 1994-08-09 Hoffmann-La Roche Inc. Antibacterial cephalosporin compounds
CS273349B2 (en) * 1988-03-31 1991-03-12 Hoffmann La Roche Method of cephalosporin's new derivatives production
US5491139A (en) * 1988-10-24 1996-02-13 The Procter & Gamble Company Antimicrobial quinolonyl lactams
US5273973A (en) * 1988-10-24 1993-12-28 Norwich Eaton Pharmaceuticals, Inc. Antimicrobial quinolonyl esters
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones
CA2001203C (en) * 1988-10-24 2001-02-13 Thomas P. Demuth, Jr. Novel antimicrobial dithiocarbamoyl quinolones
US5180719A (en) * 1988-10-24 1993-01-19 Norwich Eaton Pharmaceuticals, Inc. Antimicrobial quinolonyl lactam esters
US5328908A (en) * 1988-10-24 1994-07-12 Procter & Gamble Pharmaceuticals, Inc. Antimicrobial quinolone thioureas
US5162523A (en) * 1989-07-21 1992-11-10 Hoffmann-La Roche Inc. Cephalosporin antibacterial compounds
US5159077A (en) * 1989-07-21 1992-10-27 Hoffmann-La Roche Inc. Penam antibacterial compounds
EP0525057B1 (en) * 1990-04-18 2000-06-14 Procter & Gamble Pharmaceuticals, Inc. Antimicrobial quinolonyl lactams
US5066800A (en) * 1990-04-27 1991-11-19 Hoffmann-La Roche Inc. Qunoline intermediates useful therein for synthesizing antibacterial compounds
DE69218445T2 (de) * 1991-10-01 1997-08-07 Procter & Gamble Pharma Verfahren zur herstellung von antimikrobiellen quinolonyl-lactamen
DE4234330A1 (de) * 1992-10-12 1994-04-14 Bayer Ag Chinoloncarbonsäuren
FR2873695A1 (fr) * 2004-07-30 2006-02-03 Palumed Sa Molecules hybrides qa ou q est une aminoquinoleine et a est un antibiotique ou un inhibiteur de resistance), leur synthese et leurs utilisations en tant qu'agent antibacterien
GB201818410D0 (en) * 2018-11-12 2018-12-26 Imperial Innovations Ltd Compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS565484A (en) * 1979-06-27 1981-01-20 Dainippon Pharmaceut Co Ltd Cephalosporin derivative and its salt
JPS565485A (en) * 1979-06-27 1981-01-20 Dainippon Pharmaceut Co Ltd Cephalosporin derivative and its salt
ZA874696B (en) * 1986-07-03 1988-01-04 F. Hoffmann-La Roche & Co. Aktiengesellschaft Acyl derivatives
JP2676082B2 (ja) * 1987-12-25 1997-11-12 住友化学工業株式会社 ゴキブリ防除用マイクロカプセル剤
NZ227470A (en) * 1987-12-28 1991-06-25 Hoffmann La Roche Acyl derivatives of substituted cephem compounds; pharmaceutical compositions and methods for preparation and treatment
EP0366193A3 (en) * 1988-10-24 1992-01-08 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial quinolonyl lactams
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones
CA2001203C (en) * 1988-10-24 2001-02-13 Thomas P. Demuth, Jr. Novel antimicrobial dithiocarbamoyl quinolones

Also Published As

Publication number Publication date
JPH03503421A (ja) 1991-08-01
DK527389A (da) 1990-04-25
CA2001204A1 (en) 1990-04-24
AU620651B2 (en) 1992-02-20
GR3030052T3 (en) 1999-07-30
DE68928925D1 (de) 1999-03-18
EP0366640B1 (en) 1999-02-03
NZ231113A (en) 1992-06-25
AU4369789A (en) 1990-04-26
DK527389D0 (da) 1989-10-24
EP0366640A3 (en) 1992-01-02
PH26519A (en) 1992-08-07
EP0366640A2 (en) 1990-05-02
KR0139638B1 (ko) 1998-06-01
ATE176473T1 (de) 1999-02-15
SG54293A1 (en) 1998-11-16
ES2129388T3 (es) 1999-06-16
DE68928925T2 (de) 1999-08-26
WO1990004595A1 (en) 1990-05-03

Similar Documents

Publication Publication Date Title
KR900006347A (ko) 살균성 플루오로퀴놀로닐 세펨
KR930701434A (ko) 옥사졸리딘 디온 유도체
NO931317L (no) Et terapeutisk middel for parkinson's sykdom
KR960007592A (ko) 신규한 피롤로카바졸
KR930700514A (ko) 항미생물성 퀴놀로닐 락탐
KR890011596A (ko) 불면증 치료용 의약품의 제조에 있어서 1,4-이치환-피페리디닐 화합물의 용도
KR930016402A (ko) 항-hiv 활성을 갖는 이미다졸 유도체
AU7379187A (en) Substituted 2-thiazolyl-imidazo{1,2-a}pyrimidine derivatives
ZA889023B (en) 2-(piperazinyl)-2-oxoethylene substituted flavonoid derivatives,processes for preparing them and pharmaceutical compositions containing them
NZ221699A (en) Pyridazinone derivatives; pharmaceutical compositions and intermediates
KR920007995A (ko) 벤즈아미드 유도체
KR900016178A (ko) 2-치환 n,n'-디트리메톡시벤조일 피페라진, 그의 제조 방법 및 그를 함유하는 치료 조성물
SE8304071L (sv) Nya piperazinderivat
KR890008148A (ko) 새로운 세파로스포린 화합물 및 항균제
KR900009640A (ko) 벤족 사제핀 유도체
DE3866292D1 (de) Piperazinylalkylpiperazindion-derivate, ihre verfahren zur herstellung und diese enthaltende pharmazeutische zusammenstellungen.
ATE49761T1 (de) 8-thiotetrahydrochinoleinderivate und deren salze.
DE3889993D1 (de) 2'-Deoxy-5-fluorouridin-Derivate.
DE68919869T2 (de) Cephalosporinderivate.
HUP0000275A2 (hu) Fenantridiniumszármazékok, valamint ezeket a vegyületeket tartalmazó gyógyászati készítmények
ES2045514T3 (es) Utilizacion de derivados del cromano para el tratamiento de los estados depresivos.
ES519530A0 (es) Procedimiento para la preparacion de tienobenzodiazepinonas sustituidas.
ATE56442T1 (de) 2,6-piperazin-dion-derivate, ihre verfahren zur herstellung und sie enthaltende pharmazeutische zusammensetzungen.
PT77466B (de) Neue 4-hydroxy-2h-1,2-benzothiazin-3-carboxamid-1,1-dioxide verfahren zu ihrer herstellung ihre verwendung und diese verbindungen enthaltende arzneimittel
ATE28192T1 (de) 4-alkylimidazol-derivate, ihre herstellung und verwendung.

Legal Events

Date Code Title Description
A201 Request for examination
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
LAPS Lapse due to unpaid annual fee