CN102614207A - 18元环大环化合物及其类似物 - Google Patents
18元环大环化合物及其类似物 Download PDFInfo
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- CN102614207A CN102614207A CN2012100323954A CN201210032395A CN102614207A CN 102614207 A CN102614207 A CN 102614207A CN 2012100323954 A CN2012100323954 A CN 2012100323954A CN 201210032395 A CN201210032395 A CN 201210032395A CN 102614207 A CN102614207 A CN 102614207A
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- 0 CC[C@]([C@@](*[C@@]([C@]([C@]1*C(C(C)C)=O)O)OC(C)(C)[C@]1O)C(C)=CC(C)=CC[C@@]([C@](C)O)O1)C=C(C)[C@@](*)CC=CC=C(CO[C@@]([C@@](C2O)OC)O[C@](C)[C@]2OC(c(c(CC)c(c(O)c2Cl)Cl)c2O)=O)C1=O Chemical compound CC[C@]([C@@](*[C@@]([C@]([C@]1*C(C(C)C)=O)O)OC(C)(C)[C@]1O)C(C)=CC(C)=CC[C@@]([C@](C)O)O1)C=C(C)[C@@](*)CC=CC=C(CO[C@@]([C@@](C2O)OC)O[C@](C)[C@]2OC(c(c(CC)c(c(O)c2Cl)Cl)c2O)=O)C1=O 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
- A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
- A01N43/22—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom rings with more than six members
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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- 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
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- 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
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- 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
- A61P31/10—Antimycotics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
化合物 | X | Y | Z |
R-Tiacumicin B | 乙基 | (R)-OH | 异丙基 |
S-Tiacumicin B | 乙基 | (S)-OH | 异丙基 |
闰年霉素A4 | 甲基 | (S)-OH | 异丙基 |
C-19酮 | 乙基 | =O | 异丙基 |
范围 | 几何平均数 | MIC50 | MIC90 | |
OPT-80 | 0.015-0.25 | 0.08 | 0.125 | 0.125 |
甲硝唑 | 0.025-0.5 | 0.15 | 0.125 | 0.25 |
万古霉素 | 0.06-4 | 0.8 | 1 | 1 |
生物编号 | OPT-80 | MTZ | VAN | 生物编号 | OPT-80 | MTZ | VAN |
A1 1535 | 0.125 | 0.25 | 1 | CO1 4652 | 0.25 | 0.125 | 1 |
B1 832 | 0.06 | 0.125 | 1 | CP1 5491 | 0.125 | 0.25 | 1 |
D1 1360 | 0.03 | 0.25 | 1 | 61 5930 | 0.03 | 0.25 | 1 |
E1 816 | 0.06 | 0.125 | 1 | 63 6029 | 0.25 | 0.25 | 0.06 |
F1 1015 | 0.125 | 0.125 | 1 | 64 5940 | 0.125 | 0.25 | 1 |
G1 1077 | 0.125 | 0.125 | 1 | 65 5967 | 0.06 | 0.25 | 0.5 |
I1 1389 | 0.125 | 0.125 | 1 | 66 6366 | 0.015 | 0.125 | 0.5 |
J1 5971 | 0.06 | 0.25 | 1 | 67 6367 | 0.125 | 0.25 | 1 |
J7 4224 | 0.03 | 0.125 | 1 | 68 6368 | 0.03 | 0.125 | 0.06 |
J9 4478 | 0.06 | 0.125 | 1 | 69 6370 | 0.25 | 0.25 | 0.5 |
K1 4305 | 0.125 | 0.25 | 0.5 | 70 6376 | 0.125 | 0.25 | 2 |
K14 5780 | 0.125 | 0.125 | 1 | 71 6379 | 0.125 | 0.25 | 1 |
L1 1423 | 0.125 | 0.125 | 0.5 | 72 6380 | 0.125 | 0.25 | 2 |
N1 471 | 0.125 | 0.125 | 0.5 | 73 6382 | 0.25 | 0.25 | 1 |
O1 1861 | 0.06 | 0.125 | 1 | 75 6388 | 0.125 | 0.125 | 0.5 |
生物编号 | OPT-80 | MTZ | VAN | 生物编号 | OPT-80 | MTZ | VAN |
R1 397 | 0.125 | 0.125 | 1 | 76 6389 | 0.125 | 0.25 | 0.5 |
R6 6015 | 0.015 | 0.25 | 2 | 77 6390 | 0.06 | 0.125 | 1 |
V1 1521 | 0.125 | 0.125 | 0.5 | 78 6392 | 0.015 | 0.03 | 0.5 |
W1 3931 | 0.125 | 0.5 | 1 | 80 6327 | 0.125 | 0.125 | 0.5 |
X1 1890 | 0.125 | 0.125 | 1 | 81 6328 | 0.125 | 0.125 | 0.5 |
Y1 5639 | 0.06 | 0.125 | 0.5 | 82 6329 | 0.06 | 0.03 | 0.5 |
Y2 1459 | 0.06 | 0.125 | 1 | 83 6330 | 0.06 | 0.125 | 0.5 |
Z1 3036 | 0.03 | 0.125 | 1 | 84 6331 | 0.125 | 0.25 | 0.5 |
AA2 4380 | 0.015 | 0.125 | 1 | 85 6332 | 0.06 | 0.125 | 1 |
AB2 1725 | 0.06 | 0.125 | 1 | 86 6333 | 0.03 | 0.125 | 0.5 |
AC1 1546 | 0.06 | 0.125 | 1 | 87 6334 | 0.125 | 0.125 | 0.5 |
AF1 1808 | 0.125 | 0.125 | 0.5 | 88 6335 | 0.125 | 0.25 | 0.5 |
AG1 3044 | 0.125 | 0.125 | 1 | 89 6336 | 0.25 | 0.5 | 1 |
AH1 3430 | 0.125 | 0.25 | 0.5 | 90 6338 | 0.125 | 0.125 | 1 |
AJ1 1557 | 0.06 | 0.125 | 1 | 91 6339 | 0.125 | 0.125 | 1 |
AL1 1753 | 0.06 | 0.125 | 0.5 | 93 6341 | 0.125 | 0.125 | 1 |
AN1 464 | 0.125 | 0.125 | 0.5 | 94 6343 | 0.015 | 0.06 | 0.5 |
AO1 287 | 0.125 | 0.125 | 1 | 95 6347 | 0.125 | 0.125 | 1 |
AS1 4099 | 0.125 | 0.125 | 1 | 96 6348 | 0.06 | 0.125 | 0.5 |
AT1 1216 | 0.125 | 0.125 | 1 | 97 6349 | 0.25 | 0.125 | 1 |
AV1 941 | 0.25 | 0.125 | 0.5 | 98 6350 | 0.125 | 0.5 | 1 |
CJ1 893 | 0.125 | 0.025 | 1 | 101 6354 | 0.015 | 0.06 | 1 |
AW1 4501 | 0.125 | 0.125 | 1 | 102 6355 | 0.016 | 0.125 | 1 |
BE1 4307 | 0.125 | 0.25 | 1 | 103 6068 | 0.06 | 0.125 | 1 |
BH1 4506 | 0.06 | 0.06 | 0.5 | 104 6060 | 0.03 | 0.25 | 1 |
BI1 1675 | 0.125 | 0.125 | 1 | 105 6071 | 0.03 | 0.125 | 0.5 |
BK1 4291 | 0.125 | 0.125 | 0.5 | 106 6078 | 0.03 | 0.25 | 0.5 |
BL1 716 | 0.125 | 0.125 | 1 | 107 6079 | 0.06 | 0.125 | 0.5 |
BM1 1453 | 0.06 | 0.125 | 1 | 109 6274 | 0.015 | 0.125 | 1 |
BN1 1322 | 0.125 | 0.25 | 1 | 111 6279 | 0.03 | 0.125 | 1 |
BR1 1321 | 0.06 | 0.125 | 1 | 112 6280 | 0.06 | 0.125 | 0.5 |
BT1 706 | 0.06 | 0.125 | 1 | 113 6304 | 0.06 | 0.125 | 1 |
BV1 1183 | 0.125 | 0.25 | 1 | 114 386 | 0.06 | 0.125 | 4 |
BW1 3130 | 0.125 | 0.125 | 1 | 115 5985 | 0.015 | 0.25 | 2 |
BX1 4271 | 0.125 | 0.25 | 1 | 116 5702 | 0.06 | 0.125 | 1 |
CN1 667 | 0.25 | 0.25 | 1 | 117 6026 | 0.06 | 0.125 | 2 |
CB1 1584 | 0.25 | 0.125 | 1 | 120 6057 | 0.03 | 0.25 | 1 |
CF1 5922 | 0.125 | 0.125 | 1 | 121 6072 | 0.06 | 0.25 | 0.5 |
CG1 1566 | 0.125 | 0.125 | 1 | 122 6111 | 0.25 | 0.25 | 0.5 |
CL1 3851 | 0.25 | 0.125 | 1 | 100 6353 | 0.125 | 0.25 | 1 |
Claims (10)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN201210032395.4A CN102614207B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
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Application Number | Priority Date | Filing Date | Title |
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CN201210032395.4A CN102614207B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
CN2005800487153A CN101128114B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
PCT/US2005/002887 WO2006085838A1 (en) | 2005-01-31 | 2005-01-31 | 18-membered macrocycles and analogs thereof |
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CN2005800487153A Division CN101128114B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
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CN102614207A true CN102614207A (zh) | 2012-08-01 |
CN102614207B CN102614207B (zh) | 2016-01-13 |
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Application Number | Title | Priority Date | Filing Date |
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CN2005800487153A Active CN101128114B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
CN201210032395.4A Active CN102614207B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
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CN2005800487153A Active CN101128114B (zh) | 2005-01-31 | 2005-01-31 | 18元环大环化合物及其类似物 |
Country Status (10)
Country | Link |
---|---|
EP (1) | EP1848273A4 (zh) |
JP (1) | JP5166040B2 (zh) |
KR (1) | KR101203118B1 (zh) |
CN (2) | CN101128114B (zh) |
AU (1) | AU2005327308B2 (zh) |
BR (1) | BRPI0519890A2 (zh) |
CA (1) | CA2596387C (zh) |
MX (2) | MX2007009196A (zh) |
TW (1) | TWI306097B (zh) |
WO (1) | WO2006085838A1 (zh) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103897003A (zh) * | 2014-03-28 | 2014-07-02 | 华北制药集团新药研究开发有限责任公司 | 非达霉素晶型ii及其制备方法 |
CN105237599A (zh) * | 2015-10-09 | 2016-01-13 | 华北制药集团新药研究开发有限责任公司 | 闰年霉素a4晶体及其制备方法 |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7906489B2 (en) | 2004-05-14 | 2011-03-15 | Optimer Pharmaceuticals, Inc. | 18-membered macrocycles and analogs thereof |
US7378508B2 (en) * | 2007-01-22 | 2008-05-27 | Optimer Pharmaceuticals, Inc. | Polymorphic crystalline forms of tiacumicin B |
EP1940417A4 (en) * | 2005-10-21 | 2010-07-07 | Optimer Pharmaceuticals Inc | METHOD FOR TREATING DIARRHOE IN CONNECTION WITH CLOSTRIDIUM DIFFICILE |
TWI482772B (zh) * | 2006-08-21 | 2015-05-01 | Astrazeneca Ab | 適合口服且包含三唑并[4,5-d]嘧啶衍生物之組合物 |
US20080176927A1 (en) * | 2007-01-19 | 2008-07-24 | Optimer Pharmaceuticals, Inc. | Compositions of stable tiacumicins |
ZA200905337B (en) * | 2007-01-22 | 2010-10-27 | Optimer Pharmaceuticals Inc | Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof |
AU2012244278C1 (en) * | 2007-01-22 | 2014-11-06 | Merck Sharp & Dohme Llc | Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof |
TWI523654B (zh) * | 2007-11-27 | 2016-03-01 | 默沙東藥廠 | 抗生素巨環化合物以及其製造及使用之方法 |
CA2826662A1 (en) * | 2011-02-04 | 2012-08-09 | Optimer Pharmaceuticals, Inc. | Treatment of bacterial infections |
WO2013170142A1 (en) * | 2012-05-10 | 2013-11-14 | Teva Pharmaceutical Works Ltd. | Solid state forms of fidaxomycin and processes for preparation thereof |
US8722863B2 (en) | 2012-05-10 | 2014-05-13 | Teva Pharmaceutical Works Ltd. | Solid state forms of fidaxomycin and processes for preparation thereof |
JO3464B1 (ar) | 2013-01-15 | 2020-07-05 | Astellas Pharma Europe Ltd | التركيبات الخاصة بمركبات التياكوميسين |
CN103275152B (zh) * | 2013-05-29 | 2015-11-18 | 华北制药集团新药研究开发有限责任公司 | 一种高纯度非达霉素的制备方法 |
PT3119793T (pt) * | 2014-03-18 | 2018-05-10 | Xellia Pharmaceuticals Aps | Polimorfos inovadores e estados sólidos inovadores de tiacumicina b |
TR201815891T4 (tr) | 2014-05-09 | 2018-11-21 | Astellas Pharma Europe Ltd | Tiakumisin bileşiği için tedavi rejimi. |
JP2018519344A (ja) | 2015-07-03 | 2018-07-19 | アステラス ファーマ ユーロープ リミテッド | チアクマイシン化合物の新規の投薬レジメン |
CN110183502A (zh) * | 2019-05-28 | 2019-08-30 | 杭州华东医药集团新药研究院有限公司 | 一种非达霉素杂质及其制备方法 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5583115A (en) * | 1995-05-09 | 1996-12-10 | Abbott Laboratories | Dialkyltiacumicin compounds |
US5767096A (en) * | 1996-07-12 | 1998-06-16 | Abbott Laboratories | Bromotiacumicin compounds |
WO2004014295A2 (en) * | 2002-07-29 | 2004-02-19 | Optimer Pharmaceuticals, Inc. | Tiacumicin production |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1458512A (en) * | 1973-11-22 | 1976-12-15 | Lepetit Spa | Antibiotic substance |
US4918174A (en) * | 1986-09-26 | 1990-04-17 | Abbott Laboratories | Tiacumicin compounds |
BRPI0511119A (pt) * | 2004-05-14 | 2007-11-27 | Optimer Pharmaceuticals Inc | tratamento de doenças associadas com o uso de antibióticos |
-
2005
- 2005-01-31 CN CN2005800487153A patent/CN101128114B/zh active Active
- 2005-01-31 MX MX2007009196A patent/MX2007009196A/es active IP Right Grant
- 2005-01-31 BR BRPI0519890-9A patent/BRPI0519890A2/pt not_active Application Discontinuation
- 2005-01-31 MX MX2012009525A patent/MX340742B/es unknown
- 2005-01-31 KR KR1020077019982A patent/KR101203118B1/ko active IP Right Grant
- 2005-01-31 CN CN201210032395.4A patent/CN102614207B/zh active Active
- 2005-01-31 CA CA2596387A patent/CA2596387C/en active Active
- 2005-01-31 AU AU2005327308A patent/AU2005327308B2/en active Active
- 2005-01-31 EP EP05712354A patent/EP1848273A4/en not_active Ceased
- 2005-01-31 JP JP2007553073A patent/JP5166040B2/ja active Active
- 2005-01-31 WO PCT/US2005/002887 patent/WO2006085838A1/en active Application Filing
- 2005-05-17 TW TW094115942A patent/TWI306097B/zh active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5583115A (en) * | 1995-05-09 | 1996-12-10 | Abbott Laboratories | Dialkyltiacumicin compounds |
US5767096A (en) * | 1996-07-12 | 1998-06-16 | Abbott Laboratories | Bromotiacumicin compounds |
WO2004014295A2 (en) * | 2002-07-29 | 2004-02-19 | Optimer Pharmaceuticals, Inc. | Tiacumicin production |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103897003A (zh) * | 2014-03-28 | 2014-07-02 | 华北制药集团新药研究开发有限责任公司 | 非达霉素晶型ii及其制备方法 |
CN103897003B (zh) * | 2014-03-28 | 2016-07-06 | 华北制药集团新药研究开发有限责任公司 | 非达霉素晶型ii及其制备方法 |
CN105237599A (zh) * | 2015-10-09 | 2016-01-13 | 华北制药集团新药研究开发有限责任公司 | 闰年霉素a4晶体及其制备方法 |
CN105237599B (zh) * | 2015-10-09 | 2018-10-02 | 华北制药集团新药研究开发有限责任公司 | 闰年霉素a4晶体及其制备方法 |
Also Published As
Publication number | Publication date |
---|---|
KR20070110504A (ko) | 2007-11-19 |
TWI306097B (en) | 2009-02-11 |
JP2008528582A (ja) | 2008-07-31 |
TW200626585A (en) | 2006-08-01 |
WO2006085838A1 (en) | 2006-08-17 |
MX2007009196A (es) | 2009-02-25 |
CN101128114A (zh) | 2008-02-20 |
EP1848273A4 (en) | 2010-02-24 |
BRPI0519890A2 (pt) | 2009-03-31 |
AU2005327308A1 (en) | 2006-08-17 |
AU2005327308B2 (en) | 2011-11-10 |
EP1848273A1 (en) | 2007-10-31 |
CN102614207B (zh) | 2016-01-13 |
CA2596387C (en) | 2012-11-20 |
JP5166040B2 (ja) | 2013-03-21 |
KR101203118B1 (ko) | 2012-11-20 |
MX340742B (es) | 2016-07-21 |
CN101128114B (zh) | 2012-03-28 |
CA2596387A1 (en) | 2006-08-17 |
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