ES2184307T3 - Derivados de tiazol, procedimiento para su preparacion y su utilizacion. - Google Patents
Derivados de tiazol, procedimiento para su preparacion y su utilizacion.Info
- Publication number
- ES2184307T3 ES2184307T3 ES98936430T ES98936430T ES2184307T3 ES 2184307 T3 ES2184307 T3 ES 2184307T3 ES 98936430 T ES98936430 T ES 98936430T ES 98936430 T ES98936430 T ES 98936430T ES 2184307 T3 ES2184307 T3 ES 2184307T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- derivatives
- stands
- tiazol
- procedure
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
Classifications
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/24—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
- C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
La invención se refiere a derivados de tiazol de fórmula (II), en la que R1 es un alquilo C1-4, R2 es cualquier grupo protector con capacidad de quelación, R3 es hidrógeno o un alquilo C1-4 e Y es CO2R4, CHO, CH=CH2 o CH2R5, en la que R4 representa un alquilo C1-4 y un grupo bencilo opcionalmente sustituido, R5 es halógeno, hidroxi, p-toluenosulfonato y -OSO2B, y B representa un alquilo C1-4 o perfluoroalquilo C1-4. Estos derivados se producen sin diasterómeros y se utilizan en la producción de epotilón A y epotilón B y sus derivados.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19731316 | 1997-07-16 |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2184307T3 true ES2184307T3 (es) | 2003-04-01 |
Family
ID=7836432
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES98936430T Expired - Lifetime ES2184307T3 (es) | 1997-07-16 | 1998-07-16 | Derivados de tiazol, procedimiento para su preparacion y su utilizacion. |
Country Status (10)
Country | Link |
---|---|
US (1) | US6384230B1 (es) |
EP (1) | EP1001951B1 (es) |
JP (1) | JP2001510189A (es) |
AT (1) | ATE224882T1 (es) |
AU (1) | AU8542898A (es) |
DE (2) | DE19833750A1 (es) |
DK (1) | DK1001951T3 (es) |
ES (1) | ES2184307T3 (es) |
PT (1) | PT1001951E (es) |
WO (1) | WO1999003848A1 (es) |
Families Citing this family (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1440973A3 (de) | 1995-11-17 | 2004-10-20 | Gesellschaft für biotechnologische Forschung mbH (GBF) | Epothilonderivate, Herstellung und Mittel |
HU229833B1 (en) | 1996-11-18 | 2014-09-29 | Biotechnolog Forschung Gmbh | Epothilone d production process, and its use as cytostatic as well as phytosanitary agents |
DE69734362T2 (de) * | 1996-12-03 | 2006-07-20 | Sloan-Kettering Institute For Cancer Research | Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon |
US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
US20050043376A1 (en) * | 1996-12-03 | 2005-02-24 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
US6605599B1 (en) | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
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 |
US6320045B1 (en) | 1997-12-04 | 2001-11-20 | Bristol-Myers Squibb Company | Process for the reduction of oxiranyl epothilones to olefinic epothilones |
US6399638B1 (en) | 1998-04-21 | 2002-06-04 | Bristol-Myers Squibb Company | 12,13-modified epothilone derivatives |
US6498257B1 (en) | 1998-04-21 | 2002-12-24 | Bristol-Myers Squibb Company | 2,3-olefinic epothilone derivatives |
US6780620B1 (en) | 1998-12-23 | 2004-08-24 | Bristol-Myers Squibb Company | Microbial transformation method for the preparation of an epothilone |
CA2360452C (en) * | 1999-02-22 | 2011-07-26 | Gerhard Hoefle | C-21 modified epothilones |
US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
EP1169311A4 (en) * | 1999-03-22 | 2004-09-15 | Rhode Island Education | COMBINATORIAL OXAZOLE AND THIAZOLE BANKS |
US6291684B1 (en) | 1999-03-29 | 2001-09-18 | Bristol-Myers Squibb Company | Process for the preparation of aziridinyl epothilones from oxiranyl epothilones |
WO2000062778A1 (en) | 1999-04-15 | 2000-10-26 | Bristol-Myers Squibb Co. | Cyclic protein tyrosine kinase inhibitors |
US7125875B2 (en) | 1999-04-15 | 2006-10-24 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
CA2385528C (en) | 1999-10-01 | 2013-12-10 | Immunogen, Inc. | Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents |
AU2508201A (en) * | 1999-11-24 | 2001-06-04 | Basf Aktiengesellschaft | Fungicidal melithiazole derivatives |
US6518421B1 (en) * | 2000-03-20 | 2003-02-11 | Bristol-Myers Squibb Company | Process for the preparation of epothilone analogs |
US6593115B2 (en) | 2000-03-24 | 2003-07-15 | Bristol-Myers Squibb Co. | Preparation of epothilone intermediates |
UA75365C2 (en) * | 2000-08-16 | 2006-04-17 | Bristol Myers Squibb Co | Epothilone analog polymorph modifications, a method for obtaining thereof (variants), a pharmaceutical composition based thereon |
GB0029895D0 (en) * | 2000-12-07 | 2001-01-24 | Novartis Ag | Organic compounds |
SK8552003A3 (en) | 2001-01-25 | 2004-06-08 | Bristol Myers Squibb Co | Parenteral formulation containing epothilone analogs |
NZ526870A (en) | 2001-01-25 | 2005-11-25 | Bristol Myers Squibb Co | Methods of administering epothilone analogs for the treatment of cancer |
WO2002058699A1 (en) | 2001-01-25 | 2002-08-01 | Bristol-Myers Squibb Company | Pharmaceutical forms of epothilones for oral administration |
HUP0400041A2 (hu) | 2001-02-20 | 2004-04-28 | Bristol-Myers Squibb Co. | Epotilonszármazékok alkalmazása makacs tumorok kezelésére szolgáló gyógyszerkészítmények előállítására |
HUP0303175A2 (hu) | 2001-02-20 | 2003-12-29 | Bristol-Myers Squibb Co. | Epotilonszármazékok alkalmazása makacs tumorok kezelésére alkalmas gyógyszerkészítmény előállítására |
CA2440555A1 (en) | 2001-03-14 | 2002-09-19 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
JP2004532888A (ja) | 2001-06-01 | 2004-10-28 | ブリストル−マイヤーズ スクイブ カンパニー | エポチロン誘導体 |
DK1483251T3 (da) | 2002-03-12 | 2010-04-12 | Bristol Myers Squibb Co | C3-cyano-epothilon-derivater |
WO2003077903A1 (en) | 2002-03-12 | 2003-09-25 | 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 |
US7405234B2 (en) | 2002-05-17 | 2008-07-29 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
WO2003105828A1 (en) | 2002-06-14 | 2003-12-24 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
ES2281692T3 (es) | 2002-08-23 | 2007-10-01 | Sloan-Kettering Institute For Cancer Research | Sintesis de epotilones, sus intermediarios, sus analogos y sus usos. |
US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
TWI291464B (en) | 2002-09-23 | 2007-12-21 | Bristol Myers Squibb Co | Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B |
EP1567487A4 (en) | 2002-11-15 | 2005-11-16 | Bristol Myers Squibb Co | OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION |
US7820702B2 (en) | 2004-02-04 | 2010-10-26 | Bristol-Myers Squibb Company | Sulfonylpyrrolidine modulators of androgen receptor function and method |
US7378426B2 (en) | 2004-03-01 | 2008-05-27 | Bristol-Myers Squibb Company | Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3 |
US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
US7625923B2 (en) | 2004-03-04 | 2009-12-01 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
BRPI0718360A2 (pt) | 2006-12-04 | 2013-11-12 | Univ Illinois | "composições e métodos para o tratamento do câncer com cupredoxinas e dna rico em cpg" |
AU2012207142B2 (en) | 2011-01-20 | 2017-04-27 | Board Of Regents, The University Of Texas System | MRI markers, delivery and extraction systems, and methods of manufacture and use thereof |
JP5926374B2 (ja) | 2011-06-10 | 2016-05-25 | メルサナ セラピューティクス,インコーポレイティド | タンパク質−高分子−薬剤コンジュゲート |
CN102863474A (zh) | 2011-07-09 | 2013-01-09 | 陈小平 | 一类治疗细胞增殖性疾病的铂化合物、其制备方法和应用 |
CN102993239A (zh) | 2011-09-19 | 2013-03-27 | 陈小平 | 离去基团含氨基或烷胺基的丁二酸衍生物的铂类化合物 |
CN104768962B (zh) | 2012-11-17 | 2017-04-05 | 北京市丰硕维康技术开发有限责任公司 | 离去基团是含氨基或烷氨基的丙二酸衍生物的铂类化合物 |
JP6334553B2 (ja) | 2012-12-10 | 2018-05-30 | メルサナ セラピューティクス,インコーポレイティド | タンパク質−高分子−薬剤コンジュゲート |
EP2931316B1 (en) | 2012-12-12 | 2019-02-20 | Mersana Therapeutics, Inc. | Hydroxyl-polymer-drug-protein conjugates |
EP3007692A1 (en) | 2013-06-11 | 2016-04-20 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer comprising a mps-1 kinase inhibitor and a mitotic inhibitor |
US10316080B2 (en) | 2013-10-11 | 2019-06-11 | Asana Biosciences, Llc | Protein-polymer-drug conjugates |
EP3054991B1 (en) | 2013-10-11 | 2019-04-03 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
WO2018004338A1 (en) | 2016-06-27 | 2018-01-04 | Tagworks Pharmaceuticals B.V. | Cleavable tetrazine used in bio-orthogonal drug activation |
US11135307B2 (en) | 2016-11-23 | 2021-10-05 | Mersana Therapeutics, Inc. | Peptide-containing linkers for antibody-drug conjugates |
US10772971B2 (en) | 2017-06-22 | 2020-09-15 | Mersana Therpeutics, Inc. | Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates |
CA3099419A1 (en) | 2018-05-04 | 2019-11-07 | Tagworks Pharmaceuticals B.V. | Tetrazines for high click conjugation yield in vivo and high click release yield |
EP3788032B1 (en) | 2018-05-04 | 2024-01-24 | Tagworks Pharmaceuticals B.V. | Compounds comprising a linker for increasing transcyclooctene stability |
JP2022513400A (ja) | 2018-10-29 | 2022-02-07 | メルサナ セラピューティクス インコーポレイテッド | ペプチド含有リンカーを有するシステイン操作抗体-薬物コンジュゲート |
IL289094A (en) | 2019-06-17 | 2022-02-01 | Tagworks Pharmaceuticals B V | Tetrazines for increasing the speed and yield of the "click release" reaction |
JP2022537543A (ja) | 2019-06-17 | 2022-08-26 | タグワークス ファーマシューティカルス ビー.ブイ. | 高速で且つ効率的なクリック放出の為の化合物 |
CA3146023A1 (en) | 2019-07-05 | 2021-01-14 | Iomx Therapeutics Ag | Antibodies binding igc2 of igsf11 (vsig3) and uses thereof |
WO2022008027A1 (en) | 2020-07-06 | 2022-01-13 | Iomx Therapeutics Ag | Antibodies binding igv of igsf11 (vsig3) and uses thereof |
EP4399283A2 (en) | 2021-09-06 | 2024-07-17 | Veraxa Biotech GmbH | Novel aminoacyl-trna synthetase variants for genetic code expansion in eukaryotes |
EP4186529A1 (en) | 2021-11-25 | 2023-05-31 | Veraxa Biotech GmbH | Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion |
WO2023094525A1 (en) | 2021-11-25 | 2023-06-01 | Veraxa Biotech Gmbh | Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion |
WO2023104941A1 (en) | 2021-12-08 | 2023-06-15 | European Molecular Biology Laboratory | Hydrophilic tetrazine-functionalized payloads for preparation of targeting conjugates |
EP4314031B1 (en) | 2022-02-15 | 2024-03-13 | Tagworks Pharmaceuticals B.V. | Masked il12 protein |
WO2024013724A1 (en) | 2022-07-15 | 2024-01-18 | Pheon Therapeutics Ltd | Antibody-drug conjugates |
WO2024080872A1 (en) | 2022-10-12 | 2024-04-18 | Tagworks Pharmaceuticals B.V. | Strained bicyclononenes |
WO2024153789A1 (en) | 2023-01-20 | 2024-07-25 | Basf Se | Stabilized biopolymer composition, their manufacture and use |
WO2024191293A1 (en) | 2023-03-10 | 2024-09-19 | Tagworks Pharmaceuticals B.V. | Trans-cyclooctene with improved t-linker |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19542986A1 (de) | 1995-11-17 | 1997-05-22 | Biotechnolog Forschung Gmbh | Epothilon-Derivate und deren Verwendung |
-
1998
- 1998-07-16 JP JP2000503072A patent/JP2001510189A/ja active Pending
- 1998-07-16 US US09/462,882 patent/US6384230B1/en not_active Expired - Fee Related
- 1998-07-16 EP EP98936430A patent/EP1001951B1/de not_active Expired - Lifetime
- 1998-07-16 ES ES98936430T patent/ES2184307T3/es not_active Expired - Lifetime
- 1998-07-16 AU AU85428/98A patent/AU8542898A/en not_active Abandoned
- 1998-07-16 DE DE19833750A patent/DE19833750A1/de not_active Withdrawn
- 1998-07-16 DE DE59805727T patent/DE59805727D1/de not_active Expired - Lifetime
- 1998-07-16 PT PT98936430T patent/PT1001951E/pt unknown
- 1998-07-16 AT AT98936430T patent/ATE224882T1/de not_active IP Right Cessation
- 1998-07-16 WO PCT/EP1998/004462 patent/WO1999003848A1/de active IP Right Grant
- 1998-07-16 DK DK98936430T patent/DK1001951T3/da active
Also Published As
Publication number | Publication date |
---|---|
JP2001510189A (ja) | 2001-07-31 |
US6384230B1 (en) | 2002-05-07 |
EP1001951A1 (de) | 2000-05-24 |
DE59805727D1 (de) | 2002-10-31 |
PT1001951E (pt) | 2003-02-28 |
WO1999003848A1 (de) | 1999-01-28 |
DK1001951T3 (da) | 2002-12-23 |
DE19833750A1 (de) | 1999-02-25 |
EP1001951B1 (de) | 2002-09-25 |
ATE224882T1 (de) | 2002-10-15 |
AU8542898A (en) | 1999-02-10 |
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