EA200100826A1 - 16-галогенопроизводные эпотилона, способ их получения и их применение в фармацевтике - Google Patents
16-галогенопроизводные эпотилона, способ их получения и их применение в фармацевтикеInfo
- Publication number
- EA200100826A1 EA200100826A1 EA200100826A EA200100826A EA200100826A1 EA 200100826 A1 EA200100826 A1 EA 200100826A1 EA 200100826 A EA200100826 A EA 200100826A EA 200100826 A EA200100826 A EA 200100826A EA 200100826 A1 EA200100826 A1 EA 200100826A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- epothilon
- pharmaceutics
- production
- application
- halogen derivatives
- Prior art date
Links
- 229910052736 halogen Inorganic materials 0.000 title 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 229930013356 epothilone Natural products 0.000 abstract 1
- 150000003883 epothilone derivatives Chemical class 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D493/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
В заявке описываются новые производные эпотилона общей формулы (I)в которой Rобозначает атом галогена, прежде всего атом фтора или хлора, а остальные заместители имеют значения, указанные в описании. Новые соединения могут применяться для получения соответствующих лекарственных средств.Отчет о международном поиске был опубликован 2000.12.28.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19908765A DE19908765A1 (de) | 1999-02-18 | 1999-02-18 | 16-Halogen-Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
DE19954230A DE19954230A1 (de) | 1999-11-04 | 1999-11-04 | 16-Halogen-Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
PCT/EP2000/001333 WO2000049021A2 (de) | 1999-02-18 | 2000-02-18 | 16-halogen-epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200100826A1 true EA200100826A1 (ru) | 2002-02-28 |
EA009206B1 EA009206B1 (ru) | 2007-12-28 |
Family
ID=26052117
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200100826A EA009206B1 (ru) | 1999-02-18 | 2000-02-18 | Производные 16-галогенэпотилона и их фармацевтическое использование |
Country Status (28)
Country | Link |
---|---|
US (3) | US6610736B1 (ru) |
EP (1) | EP1150980B1 (ru) |
JP (1) | JP2002537301A (ru) |
KR (1) | KR100718616B1 (ru) |
CN (1) | CN1209360C (ru) |
AR (1) | AR022636A1 (ru) |
AT (1) | ATE370946T1 (ru) |
AU (1) | AU3156700A (ru) |
BG (1) | BG105802A (ru) |
BR (1) | BR0008331A (ru) |
CA (1) | CA2361278A1 (ru) |
CZ (1) | CZ20012951A3 (ru) |
DE (1) | DE50014587D1 (ru) |
EA (1) | EA009206B1 (ru) |
EE (1) | EE200100431A (ru) |
ES (1) | ES2291194T3 (ru) |
HK (1) | HK1044945A1 (ru) |
HR (1) | HRP20010677A2 (ru) |
HU (1) | HUP0105478A3 (ru) |
IL (1) | IL144519A0 (ru) |
MX (1) | MXPA01008328A (ru) |
NO (1) | NO20014013L (ru) |
NZ (1) | NZ513268A (ru) |
PL (1) | PL349863A1 (ru) |
SK (1) | SK11852001A3 (ru) |
TW (1) | TWI285645B (ru) |
WO (1) | WO2000049021A2 (ru) |
YU (1) | YU59001A (ru) |
Families Citing this family (52)
Publication number | Priority date | Publication date | Assignee | Title |
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CN100344627C (zh) | 1996-11-18 | 2007-10-24 | 生物技术研究有限公司(Gbf) | 埃坡霉素c、其制备方法以及作为细胞抑制剂和植物保护剂的应用 |
US20050043376A1 (en) * | 1996-12-03 | 2005-02-24 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
WO1999001124A1 (en) | 1996-12-03 | 1999-01-14 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
US6204388B1 (en) * | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
US6605599B1 (en) | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
AU9340998A (en) * | 1997-08-09 | 1999-03-01 | Schering Aktiengesellschaft | New epothilone derivatives, method for producing same and their pharmaceutical use |
US6365749B1 (en) | 1997-12-04 | 2002-04-02 | Bristol-Myers Squibb Company | Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs |
US6498257B1 (en) | 1998-04-21 | 2002-12-24 | Bristol-Myers Squibb Company | 2,3-olefinic epothilone derivatives |
US6399638B1 (en) | 1998-04-21 | 2002-06-04 | Bristol-Myers Squibb Company | 12,13-modified epothilone derivatives |
US6518421B1 (en) | 2000-03-20 | 2003-02-11 | Bristol-Myers Squibb Company | Process for the preparation of epothilone analogs |
DE10020899A1 (de) * | 2000-04-20 | 2001-10-25 | Schering Ag | 9-Oxa-Epothilon-Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten |
HU229349B1 (en) | 2001-01-25 | 2013-11-28 | Bristol Myers Squibb Co | Methods for preparation of pharmaceutical composition containing epothilone analogs useful for treatment of cancer |
WO2002058699A1 (en) | 2001-01-25 | 2002-08-01 | Bristol-Myers Squibb Company | Pharmaceutical forms of epothilones for oral administration |
AU2002245296B2 (en) * | 2001-01-25 | 2006-12-21 | Bristol-Myers Squibb Company | Methods of administering epothilone analogs for the treatment of cancer |
EP1353667A1 (en) | 2001-01-25 | 2003-10-22 | Bristol-Myers Squibb Company | Parenteral formulations containing epothilone analogs |
EE200300397A (et) | 2001-02-20 | 2003-12-15 | Bristol-Myers Squibb Company | Epotilooni derivaadid refraktaarsete kasvajate raviks |
CN1774253A (zh) | 2001-02-20 | 2006-05-17 | 布里斯托尔-迈尔斯斯奎布公司 | 用环氧丙酯酮衍生物治疗顽固性肿瘤 |
US7312237B2 (en) | 2001-03-14 | 2007-12-25 | Bristol-Myers Squibb Co. | Combination of epothilone analogs and chemotherapeutic agents for the treatment of prolilferative diseases |
WO2002098868A1 (en) | 2001-06-01 | 2002-12-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
WO2003026744A1 (en) * | 2001-09-25 | 2003-04-03 | Alcon, Inc. | The use of epothilones and analogs in conjunction with ophthalmic surgery |
EP1340498A1 (en) * | 2002-03-01 | 2003-09-03 | Schering Aktiengesellschaft | Use of epothilones in the treatment of brain diseases associated with proliferative processes |
ES2337134T3 (es) | 2002-03-12 | 2010-04-21 | Bristol-Myers Squibb Company | Derivados de c3-ciano-epotilona. |
AU2003218107A1 (en) | 2002-03-12 | 2003-09-29 | Bristol-Myers Squibb Company | C12-cyano epothilone derivatives |
TW200403994A (en) | 2002-04-04 | 2004-03-16 | Bristol Myers Squibb Co | Oral administration of EPOTHILONES |
TW200400191A (en) | 2002-05-15 | 2004-01-01 | Bristol Myers Squibb Co | Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives |
AU2003243561A1 (en) | 2002-06-14 | 2003-12-31 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
RU2462463C2 (ru) * | 2002-08-23 | 2012-09-27 | Слоан-Кеттеринг Инститьют Фор Кэнсер Рисерч | Синтез эпотилонов, их промежуточных продуктов, аналогов и их применения |
PT1767535E (pt) | 2002-08-23 | 2010-02-24 | Sloan Kettering Inst Cancer | Síntese de epotilonas, respectivos intermediários, análogos e suas utilizações |
EP1542998A4 (en) | 2002-09-23 | 2007-01-31 | Bristol Myers Squibb Co | PROCESS FOR THE PREPARATION, ISOLATION AND PURIFICATION OF EPOTHILON B, AND RINSE CRYSTAL STRUCTURES OF EPOTHILON B |
EP1559447A1 (en) | 2004-01-30 | 2005-08-03 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism |
KR20070084325A (ko) * | 2004-11-18 | 2007-08-24 | 브리스톨-마이어스 스큅 컴퍼니 | 익사베필론을 포함하는 장용성 코팅된 비드 및 그의 제조방법 |
WO2006055742A1 (en) * | 2004-11-18 | 2006-05-26 | Bristol-Myers Squibb Company | Enteric coated bead comprising epothilone or epothilone analog, and preparation and administration thereof |
EP1674098A1 (en) | 2004-12-23 | 2006-06-28 | Schering Aktiengesellschaft | Stable and tolerable parental formulations of highly reactive organic drug substances with low or no solubility in water |
AU2006336468B2 (en) | 2005-02-11 | 2012-04-12 | University Of Southern California | Method of expressing proteins with disulfide bridges |
EP1883627B1 (en) | 2005-05-18 | 2018-04-18 | Pharmascience Inc. | Bir domain binding compounds |
US20070014978A1 (en) * | 2005-07-18 | 2007-01-18 | Anthony Poloso | Method of flame blocking and articles made therefrom |
US8008256B2 (en) * | 2006-05-01 | 2011-08-30 | University Of Southern California | Combination therapy for treatment of cancer |
CN101535300B (zh) | 2006-05-16 | 2014-05-28 | 埃格拉医疗公司 | Iap bir域结合化合物 |
EP2065054A1 (en) * | 2007-11-29 | 2009-06-03 | Bayer Schering Pharma Aktiengesellschaft | Combinations comprising a prostaglandin and uses thereof |
DE102007059752A1 (de) | 2007-12-10 | 2009-06-18 | Bayer Schering Pharma Aktiengesellschaft | Funktionalisierte, feste Polymernanopartikel enthaltend Epothilone |
EP2070521A1 (en) | 2007-12-10 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Surface-modified nanoparticles |
US8802394B2 (en) | 2008-11-13 | 2014-08-12 | Radu O. Minea | Method of expressing proteins with disulfide bridges with enhanced yields and activity |
EP2210584A1 (en) | 2009-01-27 | 2010-07-28 | Bayer Schering Pharma Aktiengesellschaft | Stable polymeric composition comprising an epothilone and an amphiphilic block copolymer |
NZ602368A (en) | 2010-02-12 | 2014-10-31 | Pharmascience Inc | Iap bir domain binding compounds |
WO2013092998A1 (en) | 2011-12-23 | 2013-06-27 | Innate Pharma | Enzymatic conjugation of antibodies |
US10132799B2 (en) | 2012-07-13 | 2018-11-20 | Innate Pharma | Screening of conjugated antibodies |
WO2014072482A1 (en) | 2012-11-09 | 2014-05-15 | Innate Pharma | Recognition tags for tgase-mediated conjugation |
US10611824B2 (en) | 2013-03-15 | 2020-04-07 | Innate Pharma | Solid phase TGase-mediated conjugation of antibodies |
EP3010547B1 (en) | 2013-06-20 | 2021-04-21 | Innate Pharma | Enzymatic conjugation of polypeptides |
KR20160042871A (ko) | 2013-06-21 | 2016-04-20 | 이나뜨 파르마, 에스.아. | 폴리펩티드의 효소적 콘쥬게이션 |
WO2019092148A1 (en) | 2017-11-10 | 2019-05-16 | Innate Pharma | Antibodies with functionalized glutamine residues |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2685521B2 (ja) | 1988-08-05 | 1997-12-03 | 株式会社日立製作所 | 車両用換気装置 |
EP0353732A3 (de) * | 1988-08-05 | 1991-11-06 | Ciba-Geigy Ag | Neue Fluorolefine, Verfahren zu deren Herstellung und deren Verwendung |
OA09338A (fr) * | 1989-12-27 | 1992-09-15 | Monsanto Co | "Pyridines substituées". |
US6441186B1 (en) * | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
AU9340998A (en) * | 1997-08-09 | 1999-03-01 | Schering Aktiengesellschaft | New epothilone derivatives, method for producing same and their pharmaceutical use |
WO2000000485A1 (de) * | 1998-06-30 | 2000-01-06 | Schering Aktiengesellschaft | Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung |
DE10020517A1 (de) * | 2000-04-19 | 2001-10-25 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
-
2000
- 2000-02-18 KR KR1020017010455A patent/KR100718616B1/ko not_active IP Right Cessation
- 2000-02-18 US US09/913,495 patent/US6610736B1/en not_active Expired - Fee Related
- 2000-02-18 DE DE50014587T patent/DE50014587D1/de not_active Expired - Fee Related
- 2000-02-18 CN CNB008039763A patent/CN1209360C/zh not_active Expired - Fee Related
- 2000-02-18 AU AU31567/00A patent/AU3156700A/en not_active Abandoned
- 2000-02-18 IL IL14451900A patent/IL144519A0/xx unknown
- 2000-02-18 WO PCT/EP2000/001333 patent/WO2000049021A2/de not_active Application Discontinuation
- 2000-02-18 CZ CZ20012951A patent/CZ20012951A3/cs unknown
- 2000-02-18 YU YU59001A patent/YU59001A/sh unknown
- 2000-02-18 CA CA002361278A patent/CA2361278A1/en not_active Abandoned
- 2000-02-18 BR BR0008331-3A patent/BR0008331A/pt not_active Application Discontinuation
- 2000-02-18 EP EP00909205A patent/EP1150980B1/de not_active Expired - Lifetime
- 2000-02-18 HU HU0105478A patent/HUP0105478A3/hu unknown
- 2000-02-18 ES ES00909205T patent/ES2291194T3/es not_active Expired - Lifetime
- 2000-02-18 AT AT00909205T patent/ATE370946T1/de not_active IP Right Cessation
- 2000-02-18 EE EEP200100431A patent/EE200100431A/xx unknown
- 2000-02-18 MX MXPA01008328A patent/MXPA01008328A/es active IP Right Grant
- 2000-02-18 JP JP2000599760A patent/JP2002537301A/ja active Pending
- 2000-02-18 PL PL00349863A patent/PL349863A1/xx not_active Application Discontinuation
- 2000-02-18 EA EA200100826A patent/EA009206B1/ru unknown
- 2000-02-18 NZ NZ513268A patent/NZ513268A/en unknown
- 2000-02-18 SK SK1185-2001A patent/SK11852001A3/sk unknown
- 2000-02-21 AR ARP000100714A patent/AR022636A1/es unknown
- 2000-04-19 TW TW089102834A patent/TWI285645B/zh not_active IP Right Cessation
-
2001
- 2001-08-09 BG BG105802A patent/BG105802A/bg unknown
- 2001-08-17 NO NO20014013A patent/NO20014013L/no not_active Application Discontinuation
- 2001-09-14 HR HR20010677A patent/HRP20010677A2/hr not_active Application Discontinuation
-
2002
- 2002-09-03 HK HK02106485A patent/HK1044945A1/xx not_active IP Right Cessation
-
2003
- 2003-02-12 US US10/364,337 patent/US6930102B2/en not_active Expired - Fee Related
-
2005
- 2005-03-25 US US11/090,841 patent/US20050187270A1/en not_active Abandoned
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