KR850001207A - 수용성 리팜피신 유도체의 제조방법 - Google Patents
수용성 리팜피신 유도체의 제조방법 Download PDFInfo
- Publication number
- KR850001207A KR850001207A KR1019840003836A KR840003836A KR850001207A KR 850001207 A KR850001207 A KR 850001207A KR 1019840003836 A KR1019840003836 A KR 1019840003836A KR 840003836 A KR840003836 A KR 840003836A KR 850001207 A KR850001207 A KR 850001207A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- hydrogen
- formula
- methyl
- general formula
- Prior art date
Links
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title claims 5
- 238000000034 method Methods 0.000 title claims 2
- JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical class O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 229960005070 ascorbic acid Drugs 0.000 claims 2
- 235000010323 ascorbic acid Nutrition 0.000 claims 2
- 239000011668 ascorbic acid Substances 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 150000005846 sugar alcohols Polymers 0.000 claims 2
- -1 4-methyl-1-piperazinyl Chemical group 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 229930189077 Rifamycin Natural products 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 238000005917 acylation reaction Methods 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 235000006708 antioxidants Nutrition 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 229960003292 rifamycin Drugs 0.000 claims 1
- HJYYPODYNSCCOU-ODRIEIDWSA-N rifamycin SV Chemical compound OC1=C(C(O)=C2C)C3=C(O)C=C1NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)\C=C\O[C@@]1(C)OC2=C3C1=O HJYYPODYNSCCOU-ODRIEIDWSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Pharmacology & Pharmacy (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cephalosporin Compounds (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- 하기 일반식(I)의 화합물 :식중, R은(C1-C3) 알킬 또는 (C1-C3) 알콕시기이고, R1은 수소 또는 2 내지 4개의 탄소원자를 갖는 지방족아실기이고, Me는 메틸기임.
- 제1항에 있어서, R이 메틸, 에틸 또는 에톡시이고, R1은 수소 또는 아세틸인 화합물.
- 제1항에 있어서, R이 메틸 또는 에틸이고, R1은 수소인 화합물.
- 하기 일반식(II)의 1.4-디데옥시-1,4-디히드로-3-[[(4-메틸-1-피페라지닐)이미노]메틸]-1,4-디옥소리파마이신을 할로겐화수소 수용체의 존재하에 일반식 RCOX의 화합물과 반응시켜서 일반식(III)의 화합물을 얻고, 이 일반식(III)의 화합물을 아스코르빈산으로 환원시켜서 R1이 수소인 일반식(I)의 화합물을 얻고, R1이 수소가 아닌 일반식(I)의 화합물이 필요한 경우에는 R1이 수소인 하기 일반식(I)의 대응하는 화합물을 할로겐화 수용체 존재하에 R1이 2 내지 4개의 탄소원자를 갖는 지방족아실이고 X1에 염소 또는 브롬인 R1X1의 화합물과 아실화 반응시킴을 특징으로 하는 일반식(I)로 표시되는 리파마이신의 제조방법.식중, R은 (C1-C3) 알킬 또는 (C1-C3) 알콕시기이고, R1은 수소 또는 2 내지 4개의 탄소원자를 갖는 지방족 아실기이고, X는 염소 또는 브롬임.
- 하기 일반식(III)의 화합물 :식중, R은(C1-C3) 알킬 또는 (C1-C3) 알콕시기임.
- 유효성분으로서 제1항의 화합물을 함유하는 근육내 투여용에 적합한 약물학적 조성물.
- 유효성분으로서 제1항의 화합물과, 약물학적으로 허용가능한 용매로서 물 또는 물과 지방족 다가 알코올의 혼합물을 함유하는 약물학적 액상 조성물.
- 유효성분으로서 제1항의 화합물과, 약물학적으로 허용가능한 용매로서 물 또는 물과 지방족 다가 알코올의 혼합물과 항 산화제를 함유하는 약물학적 액상 조성물.
- 제8항에 있어서, 황산화제로서 아스코트빈산을 사용하는 약물학적 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB838318072A GB8318072D0 (en) | 1983-07-04 | 1983-07-04 | Water-soluble rifampicin derivatives |
GB8318072 | 1983-07-04 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR850001207A true KR850001207A (ko) | 1985-03-16 |
KR910005847B1 KR910005847B1 (ko) | 1991-08-05 |
Family
ID=10545208
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019840003836A KR910005847B1 (ko) | 1983-07-04 | 1984-07-03 | 수용성 리팜피신 유도체의 제조방법 |
Country Status (17)
Country | Link |
---|---|
US (1) | US4585589A (ko) |
EP (1) | EP0133887B1 (ko) |
JP (1) | JPS6036490A (ko) |
KR (1) | KR910005847B1 (ko) |
AT (1) | ATE29136T1 (ko) |
AU (1) | AU558707B2 (ko) |
CA (1) | CA1212670A (ko) |
DE (1) | DE3465597D1 (ko) |
DK (1) | DK157875C (ko) |
ES (1) | ES8601949A1 (ko) |
GB (1) | GB8318072D0 (ko) |
HU (1) | HU190576B (ko) |
IE (1) | IE57930B1 (ko) |
IL (1) | IL72234A (ko) |
NZ (1) | NZ208757A (ko) |
PH (1) | PH20342A (ko) |
ZA (1) | ZA844661B (ko) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8408924D0 (en) * | 1984-04-06 | 1984-05-16 | Dobfar Spa | 3-azinomethyl rifamycins |
AU621811B2 (en) * | 1987-09-25 | 1992-03-26 | Ciba-Geigy Ag | Diacyl derivatives of 4-(trialkylbenzyl)-piperazinyl compounds |
US5180718A (en) * | 1989-03-02 | 1993-01-19 | Ciba-Geigy Corporation | Acyl derivatives of oxazolorifamycins |
JP2001504830A (ja) * | 1996-11-19 | 2001-04-10 | ジョージタウン ユニバーシティ | ヘレグリン拮抗因子及びその利用方法 |
WO2003045319A2 (en) * | 2001-11-21 | 2003-06-05 | Activbiotics, Inc. | Targeted therapeutics and uses thereof |
US7137963B2 (en) * | 2002-08-26 | 2006-11-21 | Flowcardia, Inc. | Ultrasound catheter for disrupting blood vessel obstructions |
US7820652B2 (en) * | 2003-09-24 | 2010-10-26 | Activbiotics Pharma, Llc | Regimen for the administration of rifamycin-class antibiotics |
US20170176475A1 (en) * | 2014-04-11 | 2017-06-22 | Drexel University | Novel methods and kits for detecting a rifamycin, or derivative or analogue thereof |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR208F (ko) * | 1964-07-31 | |||
GB1159267A (en) * | 1966-11-03 | 1969-07-23 | Lepetit Spa | Rifamycin Derivatives |
NL145554B (nl) * | 1967-06-07 | 1975-04-15 | Lepetit Spa | Werkwijze voor het bereiden van een 3-formylrifamycine sv-derivaat |
AR207762A1 (es) * | 1973-07-25 | 1976-10-29 | Archifar Ind Chim Trentino | Procedimiento para la preparacion de 3-((4-metil-1-piperazin-1-il)-imino)-metil-rifamicina sv o rifampicina |
GB1594134A (en) * | 1977-11-25 | 1981-07-30 | Holco Investment Inc | Rifamycins |
US4298692A (en) * | 1979-01-25 | 1981-11-03 | Ciba-Geigy Corporation | Fermentation process for producing a rifamycin derivative |
US4411896A (en) * | 1981-06-03 | 1983-10-25 | Ciba-Geigy Corporation | Rifamycins, their compositions and use as antibiotics |
-
1983
- 1983-07-04 GB GB838318072A patent/GB8318072D0/en active Pending
-
1984
- 1984-06-15 AU AU29411/84A patent/AU558707B2/en not_active Ceased
- 1984-06-17 AT AT84106938T patent/ATE29136T1/de not_active IP Right Cessation
- 1984-06-17 EP EP84106938A patent/EP0133887B1/en not_active Expired
- 1984-06-17 DE DE8484106938T patent/DE3465597D1/de not_active Expired
- 1984-06-20 ZA ZA844661A patent/ZA844661B/xx unknown
- 1984-06-26 DK DK311484A patent/DK157875C/da active
- 1984-06-27 IL IL72234A patent/IL72234A/xx unknown
- 1984-06-27 PH PH30892A patent/PH20342A/en unknown
- 1984-06-29 US US06/626,358 patent/US4585589A/en not_active Expired - Fee Related
- 1984-07-02 JP JP59135371A patent/JPS6036490A/ja active Granted
- 1984-07-03 CA CA000457960A patent/CA1212670A/en not_active Expired
- 1984-07-03 ES ES533957A patent/ES8601949A1/es not_active Expired
- 1984-07-03 NZ NZ208757A patent/NZ208757A/en unknown
- 1984-07-03 HU HU842575A patent/HU190576B/hu not_active IP Right Cessation
- 1984-07-03 IE IE1693/84A patent/IE57930B1/en not_active IP Right Cessation
- 1984-07-03 KR KR1019840003836A patent/KR910005847B1/ko not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
ZA844661B (en) | 1985-04-24 |
DK157875C (da) | 1990-08-20 |
GB8318072D0 (en) | 1983-08-03 |
IL72234A0 (en) | 1984-10-31 |
DK157875B (da) | 1990-02-26 |
PH20342A (en) | 1986-12-04 |
DK311484A (da) | 1985-01-05 |
KR910005847B1 (ko) | 1991-08-05 |
US4585589A (en) | 1986-04-29 |
AU2941184A (en) | 1985-01-10 |
HU190576B (en) | 1986-09-29 |
NZ208757A (en) | 1987-08-31 |
EP0133887A1 (en) | 1985-03-13 |
ES533957A0 (es) | 1985-11-01 |
ATE29136T1 (de) | 1987-09-15 |
DK311484D0 (da) | 1984-06-26 |
IE57930B1 (en) | 1993-05-19 |
CA1212670A (en) | 1986-10-14 |
DE3465597D1 (en) | 1987-10-01 |
ES8601949A1 (es) | 1985-11-01 |
JPH0544467B2 (ko) | 1993-07-06 |
HUT36128A (en) | 1985-08-28 |
IL72234A (en) | 1987-09-16 |
IE841693L (en) | 1985-01-04 |
EP0133887B1 (en) | 1987-08-26 |
JPS6036490A (ja) | 1985-02-25 |
AU558707B2 (en) | 1987-02-05 |
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E902 | Notification of reason for refusal | ||
G160 | Decision to publish patent application | ||
E701 | Decision to grant or registration of patent right | ||
GRNT | Written decision to grant | ||
LAPS | Lapse due to unpaid annual fee |