KR920701229A - 에리트로마이신 유도체 - Google Patents
에리트로마이신 유도체Info
- Publication number
- KR920701229A KR920701229A KR1019910701206A KR910701206A KR920701229A KR 920701229 A KR920701229 A KR 920701229A KR 1019910701206 A KR1019910701206 A KR 1019910701206A KR 910701206 A KR910701206 A KR 910701206A KR 920701229 A KR920701229 A KR 920701229A
- Authority
- KR
- South Korea
- Prior art keywords
- deoxo
- epoxy
- amino
- trideoxy
- oxoerythromycin
- Prior art date
Links
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical class O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 title claims 8
- 229960003276 erythromycin Drugs 0.000 claims 9
- 229930006677 Erythromycin A Natural products 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- YKAVHPRGGAUFDN-JTQLBUQXSA-N 24464-30-0 Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]2(C)O[C@]3([C@@H]([C@H]2O)C)[C@H](C)C[C@](O3)(C)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 YKAVHPRGGAUFDN-JTQLBUQXSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 230000001580 bacterial effect Effects 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 150000002576 ketones Chemical class 0.000 claims 2
- 230000000813 microbial effect Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- -1 phenylmethoxy Chemical group 0.000 claims 2
- SZZIJYBWFJCYOX-OWJHGTNRSA-N (2r,6s,7s,8r,11r,12r)-5-[(2s,3r,4s)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-11-ethyl-4-hydroxy-7-[(2r,4r,5s,6s)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-2,4,6,8,12,14-hexamethyl-10,15-dioxabicyclo[10.2.1]pentadec-1(14)-ene-9,13-dione Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@]2(C)C(=O)C(C)=C(O2)[C@H](C)CC(C)(O)C(O[C@H]2[C@@H]([C@H](CC(C)O2)N(C)C)O)[C@H]1C)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 SZZIJYBWFJCYOX-OWJHGTNRSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- FATAVLOOLIRUNA-UHFFFAOYSA-N formylmethyl Chemical group [CH2]C=O FATAVLOOLIRUNA-UHFFFAOYSA-N 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 150000002923 oximes Chemical class 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- 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)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (7)
- 하기 일반식의 화합물, 및 이의 약제학적으로 허용되는 염 및 에스테르.상기식에서, R1은 11위치의 옥소, 옥심, 하이드록시 또는 아미노 그룹이고, R2는 4"위치의 수소, 산소-함유 그룹 또는 질소-함유그룹이며, R3수소 또는 저급 알킬이다.
- 치료학적 유효량의 제1항에 따른 에리트로마이신 유도체를포함하는 약제학적 조성물.
- 세균성 및 기타 미생물성 감염의 치료 및 예방이 필요한 포유동물에게 치료학적 유효량의 제1항에 따른 에리트로마이신 유도체를 투여함을 특징으로 하여, 상기 포류동물의 세균성 및 기타 미생물성 감염을 예방 및 치료하는 방법.
- (9S,11S)-9-데옥소-12-데옥시-9,12-에폭시 에리트로마이신 A; (9S)-9-데옥소-11,12-디데옥시-9,12-에폭시-11-옥소-4"-〔〔(페닐메톡시)카보닐〕아미노〕에리트로마이신 A; (4"R,9S)-4"-아미노-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-11-옥소에리트로마이신 A; (4"'R, 9S)-4",11,12-트리데옥시-9,12-에폭시-4"-〔〔(디메틸아미노)메틸렌〕아미노〕-11-옥소에리트로마이신 A;(4"R,9S)-4"-아세틸아미노-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-11-옥소에리트로마이신 A; (4"R,9S)-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-4"-〔(메틸설포닐)아미노〕-11-옥소에리트로마이신 A;(4"R,9S)-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-11-옥소-4"-〔(페닐메틸)아미노〕에리트로마이신 A; (4"R,9S,11S)-4"-아미노-9-데옥소-4",11,12-데옥시-9,12-에폭시에리트로마이신 A;(4"S,9S)-4"-아미노-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-11-옥소에리트로마이신 A; (4"S,9S,11S)-4"-아미노-9-데옥소-4",12-디에옥시-9,12-에폭시에리트로마이신 A; (4"S,9S)-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-4"-(메틸설포닐)아미노-11-옥소에리트로마이신 A; (9S,11S)-4"-0-아미노카보닐-9-데옥소-12-데옥시-9,12-에폭시에리트로마이신 A;(9S)-9-데옥소-11,12-데옥시-9,12-에폭시-11-하이드록시 이미노에리트로마이신; (9S,11S)-11-아미노-9-데옥소-11,12-데옥시-에폭시-에리트로마이신 A; (9S,11S)-11-아미노-98-데옥소-4",11,12-트리데옥시-9,12-에폭시에리트로마이신 A; (4"R,9S,11S)-4"-디아미노-9-데옥소-4",11,12-트리데옥시-9,12-에폭시에리트로마이신 A; (4"R,9S)-9-데옥소-11,12-디데옥시-9,12-에폭시-11-옥소-에리트로마이신 A; (4"R,9S,11S)-4",11-디아미노-9-데옥소-4",11,12-트리데옥시-9,12-에폭시에리트로마이신 A; (9S,11S)-4"-O-아세틸-9-데옥소-12-9,12-에폭시-에리트로마이신 A; (9S)-4"-O-아미노카보닐-9-데옥소-11,12-디데옥시-9,12-에폭시-11-옥소에리트로마이신 A; 및 (4"R,9S)-4"-〔(아미노카보닐)아미노〕-9-데옥소-4",11,12-트리데옥시-9,12-에폭시-11-옥소에리트로마이신 A로 구성된 그룹중에서 선택된 화합물, 및 이의 염 및 에스테르.
- 9,10-디데하이드로-9-데옥소-11,12-디데옥시-9,12-에폭시-11-옥소-4"-O-〔(페닐메톡시)카보닐〕에리트로마이신 A; 2'-O-아세틸-11-데옥시-11-옥소안하이드로에리트로마이신 A; 9,10-디데하이드로-9-데옥소-11,12-디데옥시-9,12-에폭시-11-옥소에리트로마이신 A; (4"E)-9,10-디데하이드로-9-데옥소-4"11,12-트리데옥시-9,12-에폭시-4"-아이드록시이미노-11-옥소에리트로마이신 A;(9S,11S)-2'-O-(2-옥소에틸)에리트로마이신 A; 및 9,10-디데하이드로-9-데옥소-11,12-디데옥시-9,12-에폭시-6-O-메틸-11-옥소에리트로마이신A로 구성된 그룹중에서 선택된 화합물, 및 이의 염 및 에스테르.
- 하기 일반식의 화합물.상기식에서, R1은 옥소 또는 하이드록시이고, R2는 하이드록시이며, R3은 수소이다.
- (a)에리트로마이신 A를 산으로 처리하여 안하이드로에리트로마이신 A를 형성시키고; (b)2'위치를 보호그룹으로 보호시키며; (c)보호된 안하이드로에리트로마이신 A를 산화시켜 불포화된 케톤을 생성시키고; (d)불포화된 케톤을 에논으로 전환시키고 2'위치를 탈보호시킨 다음; (e)에논을 환원시킴을 특징으로하는, 제6항에 따른 화합물의 제조방법.※참고사항 : 최초출원 내용에 의하여 공개되는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32947389A | 1989-03-28 | 1989-03-28 | |
| US07/329473 | 1989-03-28 | ||
| PCT/US1990/001658 WO1990011288A1 (en) | 1989-03-28 | 1990-03-28 | Erythromycin derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR920701229A true KR920701229A (ko) | 1992-08-11 |
Family
ID=23285572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019910701206A KR920701229A (ko) | 1989-03-28 | 1990-03-28 | 에리트로마이신 유도체 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US5288709A (ko) |
| EP (1) | EP0465581B1 (ko) |
| JP (1) | JPH04504259A (ko) |
| KR (1) | KR920701229A (ko) |
| AT (1) | ATE128714T1 (ko) |
| AU (1) | AU623764B2 (ko) |
| CA (1) | CA2049359A1 (ko) |
| DE (1) | DE69022845T2 (ko) |
| DK (1) | DK0465581T3 (ko) |
| ES (1) | ES2080140T3 (ko) |
| GR (1) | GR1000519B (ko) |
| IL (1) | IL93936A (ko) |
| NZ (1) | NZ233117A (ko) |
| WO (1) | WO1990011288A1 (ko) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0549040A1 (en) * | 1991-12-20 | 1993-06-30 | Merck & Co. Inc. | Methods of making 4" derivatives of 9-deoxo-8a-aza-8a-alkyl-8a-homoerythromycin A |
| FR2713226B1 (fr) * | 1993-12-03 | 1996-01-05 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| EP1125935A3 (en) * | 1995-08-03 | 2001-12-12 | Dade Behring Inc. | Quinidine conjugates and their use in immunoassays |
| EP0895999A1 (en) * | 1997-08-06 | 1999-02-10 | Pfizer Products Inc. | C-4" substituted macrolide antibiotics |
| GB0127349D0 (en) | 2001-11-14 | 2002-01-02 | Glaxo Group Ltd | Macrolides |
| EP1579864A1 (en) * | 2002-04-25 | 2005-09-28 | Abbott Laboratories | Oxolide antibacterials |
| KR101051613B1 (ko) * | 2002-08-29 | 2011-07-25 | 화이자 인코포레이티드 | 모틸리드 화합물 |
| GB0310980D0 (en) * | 2003-05-13 | 2003-06-18 | Glaxo Group Ltd | Novel compounds |
| SI1628989T1 (sl) * | 2003-05-13 | 2007-06-30 | Glaxo Group Ltd | Nove cikliäśne spojine s 14 in 15 obroäśnimi äśleni |
| GB0310986D0 (en) * | 2003-05-13 | 2003-06-18 | Glaxo Group Ltd | Novel compounds |
| GB0310984D0 (en) * | 2003-05-13 | 2003-06-18 | Glaxo Group Ltd | Novel compounds |
| CN107365338B (zh) * | 2016-08-12 | 2021-03-19 | 西安世纪盛康药业有限公司 | 一类红霉素a-6,9-9,12-螺缩酮衍生物及其制备方法和应用 |
| CN114504585A (zh) * | 2020-11-16 | 2022-05-17 | 中国人民解放军海军军医大学 | 一种大环内酯类衍生物在制备减重降糖药物中的应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1451798A (en) * | 1973-08-02 | 1976-10-06 | Ici Ltd | Prostanoic acid derivatives |
| US3963696A (en) * | 1975-02-21 | 1976-06-15 | Abbott Laboratories | 6,6A-AND 6,7-Anhydroerythromycin B and derivatives thereof |
| EP0184921A3 (en) * | 1984-12-08 | 1986-10-29 | Beecham Group Plc | Erythromycin derivatives |
| US5008249A (en) * | 1985-08-31 | 1991-04-16 | Kitasato Kenkyusho | Therapeutic method of stimulating digestive tract contractile motion in mammals |
| SE519436C2 (sv) * | 2001-04-09 | 2003-02-25 | Anoto Ab | Penna med på pennan löstagbart anordnade medel för byte av i pennan anordnat bläckstift, samt förfarande för stiftbyte |
-
1990
- 1990-03-28 AT AT90906030T patent/ATE128714T1/de not_active IP Right Cessation
- 1990-03-28 IL IL9393690A patent/IL93936A/en not_active IP Right Cessation
- 1990-03-28 JP JP2505715A patent/JPH04504259A/ja active Pending
- 1990-03-28 GR GR900100232A patent/GR1000519B/el unknown
- 1990-03-28 DK DK90906030.3T patent/DK0465581T3/da active
- 1990-03-28 NZ NZ233117A patent/NZ233117A/en unknown
- 1990-03-28 AU AU54028/90A patent/AU623764B2/en not_active Ceased
- 1990-03-28 ES ES90906030T patent/ES2080140T3/es not_active Expired - Lifetime
- 1990-03-28 EP EP90906030A patent/EP0465581B1/en not_active Expired - Lifetime
- 1990-03-28 KR KR1019910701206A patent/KR920701229A/ko not_active Application Discontinuation
- 1990-03-28 DE DE69022845T patent/DE69022845T2/de not_active Expired - Fee Related
- 1990-03-28 WO PCT/US1990/001658 patent/WO1990011288A1/en active IP Right Grant
- 1990-03-28 CA CA002049359A patent/CA2049359A1/en not_active Abandoned
- 1990-03-28 US US07/743,424 patent/US5288709A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US5288709A (en) | 1994-02-22 |
| JPH04504259A (ja) | 1992-07-30 |
| IL93936A0 (en) | 1990-12-23 |
| EP0465581A4 (en) | 1992-05-13 |
| EP0465581B1 (en) | 1995-10-04 |
| AU623764B2 (en) | 1992-05-21 |
| GR900100232A (en) | 1990-07-31 |
| EP0465581A1 (en) | 1992-01-15 |
| ATE128714T1 (de) | 1995-10-15 |
| DE69022845D1 (en) | 1995-11-09 |
| GR1000519B (el) | 1992-08-25 |
| AU5402890A (en) | 1990-10-22 |
| NZ233117A (en) | 1991-05-28 |
| CA2049359A1 (en) | 1990-09-29 |
| IL93936A (en) | 1994-06-24 |
| WO1990011288A1 (en) | 1990-10-04 |
| ES2080140T3 (es) | 1996-02-01 |
| DK0465581T3 (da) | 1996-02-12 |
| DE69022845T2 (de) | 1996-06-13 |
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