CN101506217B - 埃坡霉素b的晶型及在药物组合物中的用途 - Google Patents
埃坡霉素b的晶型及在药物组合物中的用途 Download PDFInfo
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- CN101506217B CN101506217B CN2007800304132A CN200780030413A CN101506217B CN 101506217 B CN101506217 B CN 101506217B CN 2007800304132 A CN2007800304132 A CN 2007800304132A CN 200780030413 A CN200780030413 A CN 200780030413A CN 101506217 B CN101506217 B CN 101506217B
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- BEFZAMRWPCMWFJ-UHFFFAOYSA-N desoxyepothilone A Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC=CCC1C(C)=CC1=CSC(C)=N1 BEFZAMRWPCMWFJ-UHFFFAOYSA-N 0.000 description 1
- XOZIUKBZLSUILX-UHFFFAOYSA-N desoxyepothilone B Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC(C)=CCC1C(C)=CC1=CSC(C)=N1 XOZIUKBZLSUILX-UHFFFAOYSA-N 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- BEFZAMRWPCMWFJ-QJKGZULSSA-N epothilone C Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C=C/C[C@H]1C(\C)=C\C1=CSC(C)=N1 BEFZAMRWPCMWFJ-QJKGZULSSA-N 0.000 description 1
- XOZIUKBZLSUILX-GIQCAXHBSA-N epothilone D Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C(C)=C/C[C@H]1C(\C)=C\C1=CSC(C)=N1 XOZIUKBZLSUILX-GIQCAXHBSA-N 0.000 description 1
- FCCNKYGSMOSYPV-UHFFFAOYSA-N epothilone E Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC2OC2CC1C(C)=CC1=CSC(CO)=N1 FCCNKYGSMOSYPV-UHFFFAOYSA-N 0.000 description 1
- FCCNKYGSMOSYPV-OKOHHBBGSA-N epothilone e Chemical compound C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(CO)=N1 FCCNKYGSMOSYPV-OKOHHBBGSA-N 0.000 description 1
- DPUOLQHDNGRHBS-KTKRTIGZSA-N erucic acid Chemical compound CCCCCCCC\C=C/CCCCCCCCCCCC(O)=O DPUOLQHDNGRHBS-KTKRTIGZSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 229920000591 gum Polymers 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 1
- 231100000086 high toxicity Toxicity 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000000976 ink Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
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- 238000001990 intravenous administration Methods 0.000 description 1
- YAQXGBBDJYBXKL-UHFFFAOYSA-N iron(2+);1,10-phenanthroline;dicyanide Chemical compound [Fe+2].N#[C-].N#[C-].C1=CN=C2C3=NC=CC=C3C=CC2=C1.C1=CN=C2C3=NC=CC=C3C=CC2=C1 YAQXGBBDJYBXKL-UHFFFAOYSA-N 0.000 description 1
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 1
- 229960004232 linoleic acid Drugs 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 229940026778 other chemotherapeutics in atc Drugs 0.000 description 1
- 238000010525 oxidative degradation reaction Methods 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000001814 pectin Substances 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 238000004094 preconcentration Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- DPBVJRXPSXTHOL-UHFFFAOYSA-N propyl tetradecanoate Chemical compound CCCCCCCCCCCCCC(=O)OCCC DPBVJRXPSXTHOL-UHFFFAOYSA-N 0.000 description 1
- 208000023958 prostate neoplasm Diseases 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000008261 resistance mechanism Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 238000004904 shortening Methods 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 230000003068 static effect Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000005728 strengthening Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229920001169 thermoplastic Polymers 0.000 description 1
- 239000004416 thermosoftening plastic Substances 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- DPUOLQHDNGRHBS-MDZDMXLPSA-N trans-Brassidic acid Chemical compound CCCCCCCC\C=C\CCCCCCCCCCCC(O)=O DPUOLQHDNGRHBS-MDZDMXLPSA-N 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 description 1
- 229940117972 triolein Drugs 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06119043 | 2006-08-16 | ||
| EP06119043.5 | 2006-08-16 | ||
| PCT/EP2007/007173 WO2008019820A2 (en) | 2006-08-16 | 2007-08-14 | Crystal form of epothilone b and use in pharmaceutical compositions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101506217A CN101506217A (zh) | 2009-08-12 |
| CN101506217B true CN101506217B (zh) | 2012-09-05 |
Family
ID=37685905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800304132A Expired - Fee Related CN101506217B (zh) | 2006-08-16 | 2007-08-14 | 埃坡霉素b的晶型及在药物组合物中的用途 |
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| US (1) | US8178566B2 (enExample) |
| EP (1) | EP2064216A2 (enExample) |
| JP (1) | JP2010500387A (enExample) |
| KR (1) | KR20090038902A (enExample) |
| CN (1) | CN101506217B (enExample) |
| AR (1) | AR062375A1 (enExample) |
| AU (1) | AU2007286454A1 (enExample) |
| BR (1) | BRPI0715963A2 (enExample) |
| CA (1) | CA2658475A1 (enExample) |
| CL (1) | CL2007002362A1 (enExample) |
| IL (1) | IL196558A0 (enExample) |
| MA (1) | MA30656B1 (enExample) |
| MX (1) | MX2009001635A (enExample) |
| MY (1) | MY148355A (enExample) |
| NO (1) | NO20091081L (enExample) |
| NZ (1) | NZ574194A (enExample) |
| PE (1) | PE20081317A1 (enExample) |
| RU (1) | RU2009109352A (enExample) |
| TN (1) | TN2009000044A1 (enExample) |
| TW (1) | TW200815455A (enExample) |
| WO (1) | WO2008019820A2 (enExample) |
| ZA (1) | ZA200900227B (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011146638A1 (en) | 2010-05-18 | 2011-11-24 | Cerulean Pharma Inc. | Compositions and methods for treatment of autoimmune and other diseases |
| CN103910742B (zh) * | 2013-01-07 | 2016-07-13 | 浙江海正药业股份有限公司 | 一种制备埃博霉素b无定形粉末的方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1468243A (zh) * | 2000-08-16 | 2004-01-14 | ����˹�ж�-����˹˹������˾ | epothilone类似物的多晶型物 |
| CN1535971A (zh) * | 1998-02-19 | 2004-10-13 | ��˹��ŵ�� | 细胞抑制剂及其晶形的发酵制备方法 |
| CN1705662A (zh) * | 2002-09-23 | 2005-12-07 | 布里斯托尔-迈尔斯斯奎布公司 | 埃坡霉素b的制备、分离和纯化的方法,及埃坡霉素b的x－射线晶体结构 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1052974B1 (en) | 1998-02-05 | 2009-05-20 | Novartis AG | Pharmaceutical formulation containing epothilone |
| GB0029895D0 (en) | 2000-12-07 | 2001-01-24 | Novartis Ag | Organic compounds |
-
2007
- 2007-08-14 BR BRPI0715963-3A patent/BRPI0715963A2/pt not_active IP Right Cessation
- 2007-08-14 JP JP2009524113A patent/JP2010500387A/ja active Pending
- 2007-08-14 RU RU2009109352/04A patent/RU2009109352A/ru not_active Application Discontinuation
- 2007-08-14 AU AU2007286454A patent/AU2007286454A1/en not_active Abandoned
- 2007-08-14 CA CA002658475A patent/CA2658475A1/en not_active Abandoned
- 2007-08-14 CN CN2007800304132A patent/CN101506217B/zh not_active Expired - Fee Related
- 2007-08-14 US US12/376,973 patent/US8178566B2/en not_active Expired - Fee Related
- 2007-08-14 MY MYPI20090415A patent/MY148355A/en unknown
- 2007-08-14 KR KR1020097002958A patent/KR20090038902A/ko not_active Ceased
- 2007-08-14 NZ NZ574194A patent/NZ574194A/en not_active IP Right Cessation
- 2007-08-14 AR ARP070103603A patent/AR062375A1/es not_active Application Discontinuation
- 2007-08-14 EP EP07801648A patent/EP2064216A2/en not_active Withdrawn
- 2007-08-14 WO PCT/EP2007/007173 patent/WO2008019820A2/en not_active Ceased
- 2007-08-14 CL CL200702362A patent/CL2007002362A1/es unknown
- 2007-08-14 PE PE2007001090A patent/PE20081317A1/es not_active Application Discontinuation
- 2007-08-14 MX MX2009001635A patent/MX2009001635A/es not_active Application Discontinuation
- 2007-08-15 TW TW096130206A patent/TW200815455A/zh unknown
-
2009
- 2009-01-12 ZA ZA2009/00227A patent/ZA200900227B/en unknown
- 2009-01-15 IL IL196558A patent/IL196558A0/en unknown
- 2009-02-13 TN TN2009000044A patent/TN2009000044A1/fr unknown
- 2009-02-20 MA MA31654A patent/MA30656B1/fr unknown
- 2009-03-11 NO NO20091081A patent/NO20091081L/no not_active Application Discontinuation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1535971A (zh) * | 1998-02-19 | 2004-10-13 | ��˹��ŵ�� | 细胞抑制剂及其晶形的发酵制备方法 |
| CN1468243A (zh) * | 2000-08-16 | 2004-01-14 | ����˹�ж�-����˹˹������˾ | epothilone类似物的多晶型物 |
| CN1705662A (zh) * | 2002-09-23 | 2005-12-07 | 布里斯托尔-迈尔斯斯奎布公司 | 埃坡霉素b的制备、分离和纯化的方法,及埃坡霉素b的x－射线晶体结构 |
Also Published As
| Publication number | Publication date |
|---|---|
| CL2007002362A1 (es) | 2008-08-08 |
| AU2007286454A1 (en) | 2008-02-21 |
| MY148355A (en) | 2013-03-29 |
| WO2008019820A3 (en) | 2008-04-17 |
| IL196558A0 (en) | 2009-11-18 |
| TN2009000044A1 (en) | 2010-08-19 |
| US8178566B2 (en) | 2012-05-15 |
| WO2008019820A2 (en) | 2008-02-21 |
| NO20091081L (no) | 2009-03-16 |
| AR062375A1 (es) | 2008-11-05 |
| BRPI0715963A2 (pt) | 2013-08-06 |
| KR20090038902A (ko) | 2009-04-21 |
| JP2010500387A (ja) | 2010-01-07 |
| CN101506217A (zh) | 2009-08-12 |
| NZ574194A (en) | 2011-12-22 |
| PE20081317A1 (es) | 2008-10-28 |
| TW200815455A (en) | 2008-04-01 |
| MA30656B1 (fr) | 2009-08-03 |
| CA2658475A1 (en) | 2008-02-21 |
| RU2009109352A (ru) | 2010-09-27 |
| US20100160393A1 (en) | 2010-06-24 |
| EP2064216A2 (en) | 2009-06-03 |
| ZA200900227B (en) | 2009-12-30 |
| MX2009001635A (es) | 2009-02-23 |
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