AR015774A1 - Derivados de epotilona 12,13-modificados y sus sales - Google Patents
Derivados de epotilona 12,13-modificados y sus salesInfo
- Publication number
- AR015774A1 AR015774A1 ARP990101834A ARP990101834A AR015774A1 AR 015774 A1 AR015774 A1 AR 015774A1 AR P990101834 A ARP990101834 A AR P990101834A AR P990101834 A ARP990101834 A AR P990101834A AR 015774 A1 AR015774 A1 AR 015774A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- group
- aryl
- heterocycle
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 101100173726 Arabidopsis thaliana OR23 gene Proteins 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000003107 substituted aryl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 102200033028 rs587777512 Human genes 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 101100495913 Arabidopsis thaliana CHR17 gene Proteins 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 101150020251 NR13 gene Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 150000003883 epothilone derivatives Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 102200120416 rs150931842 Human genes 0.000 abstract 1
- 102220250649 rs369908377 Human genes 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N sulfur dioxide Inorganic materials O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se trata de derivados de epotilona modificados en la posicion 12.13. de formulas: (I) y (II); Q se elige entre los grupos (1); O es alquilo, alquilosustituido, arilo, arilo sustituido, heterociclo, del grupo (2) y L representa O, S, SO2 o NR13 o CR14R15; W es O, o NR16; X es O. S, CHR17 o H2R18; A es O;S; H R19 o R20, o R21; Y se elige entre O; H, H; H,OR22; OR23;OR23,NOR24; H, NOR25; H,NR26R27; NHNR28R29; H, NHNR30R31; O CHR32; en donde OR23, OR23 puedenformar un cetal cíclico; B1 y B2 es H o un grupo OR23, OCOR34, OCONR35R36, NR37R38 O NR39CONR40R41; D es un grupo de NR42R43 o heterociclo; y los demás sesleccionan a partir de carbono, R1, R2, R3 y R4 se seleccionan a partir de H, alquilo inferior; R5, R8, R9, R10 y R11 se seleccionan a partir del grupo queconsiste de H, alquilo, alquilo sustituido, arilo, arilo sustituido, cicloalquilo, heterociclo o heterociclo sustituido; R6 y R7 se seleccionan del grupo queconsiste de H, alquilo, halogeno, nitro ciano, OR47, NR48R49, R50C=O, R17,R18, R22 y R23 se seleccionan a partir del grupo que consiste de H, alquilo yalquilo sustituido; arilo, acilo o arilo sustituido. R20, R21, R24, R25, R26, R28, R30, R32, R33, R34, R35, R36, R37, R39, R40, R41, R42, R47, R48, R50, R51,R52, R53, R54, R56,, R57, R58, R59, y R61 se seleccionan a partir del grupo de H, alquilo, alquilo sustituido, arilo, o arilo sustituido; R12, R13, R16, R27,R31, R38, R43, R44,, R49, R55 y R60 se seleccionan a partir del grupo que consiste en H, alquilo, alquilo sustituido, arilo sustituido, cicloalquilo,heterociclo, R51C=O,R53SO2, hidroxi, O-alquilo o alquilo O sustituido; en donde X es O entonces R16 no es R51C=O, R52OC=O, y R53SO2; y en el cual R44 es ademásamino y formula (B); R14 y R15 se seleccionan a partir del grupo que consiste en H; halogeno, alquilo o alquilo sustituido; R19 se selecciona a partir delgrupo que consiste de H, alquilo, alquilo sustituido, O-alquilo, alquilo O-sustituido, NR54R55, R56C=O; cuando L es O,S, o NR3 entonces R19 no esO-alquilo,
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8256498P | 1998-04-21 | 1998-04-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR015774A1 true AR015774A1 (es) | 2001-05-16 |
Family
ID=22171978
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990101834A AR015774A1 (es) | 1998-04-21 | 1999-04-21 | Derivados de epotilona 12,13-modificados y sus sales |
| ARP990101833A AR015007A1 (es) | 1998-04-21 | 1999-04-21 | Compuestos de 12,13-ciclopropano epotilona y sales, solvatos e hidratos de los mismos |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990101833A AR015007A1 (es) | 1998-04-21 | 1999-04-21 | Compuestos de 12,13-ciclopropano epotilona y sales, solvatos e hidratos de los mismos |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US6380395B1 (es) |
| EP (3) | EP1073647B1 (es) |
| JP (2) | JP4476483B2 (es) |
| CN (1) | CN1142923C (es) |
| AR (2) | AR015774A1 (es) |
| AT (2) | ATE340177T1 (es) |
| AU (2) | AU748526B2 (es) |
| BR (1) | BR9909795A (es) |
| CA (2) | CA2329181C (es) |
| CY (2) | CY1105836T1 (es) |
| DE (2) | DE69941083D1 (es) |
| DK (3) | DK1073647T3 (es) |
| ES (3) | ES2273484T3 (es) |
| PE (1) | PE20000460A1 (es) |
| PT (3) | PT1073648E (es) |
| TR (1) | TR200003036T2 (es) |
| WO (2) | WO1999054318A1 (es) |
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| DE19826988A1 (de) * | 1998-06-18 | 1999-12-23 | Biotechnolog Forschung Gmbh | Epothilon-Nebenkomponenten |
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| BR9915940A (pt) * | 1998-12-02 | 2001-09-11 | Pfizer Prod Inc | Métodos e composições para restaurar a estabilidade conformacional de uma proteìna da famìlia p53 |
| US6780620B1 (en) * | 1998-12-23 | 2004-08-24 | Bristol-Myers Squibb Company | Microbial transformation method for the preparation of an epothilone |
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| IL155306A0 (en) | 2000-10-13 | 2003-11-23 | Univ Mississippi | Methods for producing epothilone derivatives and analogs and epothilone derivatives and analogs produced thereby |
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| BRPI0206509B8 (pt) * | 2001-01-25 | 2021-05-25 | R Pharm Us Operating Llc | processo para formular, para administração parenteral, um análogo de epotilona, preparação farmacêutica, processo para formar uma composição farmacêutica para administração parental, composição farmacêutica e uso de um análogo de epotilona na preparação de uma composição farmacêutica para o tratamento de câncer |
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|---|---|---|---|---|
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| CN1128803C (zh) | 1997-02-25 | 2003-11-26 | 生物技术研究有限公司(Gbf) | 环氧噻嗪酮b-n-氧化物及其制备方法 |
| DE19713970B4 (de) | 1997-04-04 | 2006-08-31 | R&D-Biopharmaceuticals Gmbh | Epothilone-Synthesebausteine II - Prenylderivate |
| EP0975622B1 (de) | 1997-04-18 | 2002-10-09 | Studiengesellschaft Kohle mbH | Selektive olefinmetathese von bi- oder polyfunktionellen substraten in komprimiertem kohlendioxid als reaktionsmedium |
| DE19720312A1 (de) | 1997-05-15 | 1998-11-19 | Hoechst Ag | Zubereitung mit erhöhter in vivo Verträglichkeit |
| DE19821954A1 (de) | 1997-05-15 | 1998-11-19 | Biotechnolog Forschung Gmbh | Verfahren zur Herstellung eines Epothilon-Derivats |
| DE19726627A1 (de) | 1997-06-17 | 1998-12-24 | Schering Ag | Zwischenprodukte, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Epothilon |
| US6605599B1 (en) * | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
| PT1001951E (pt) | 1997-07-16 | 2003-02-28 | Schering Ag | Derivados de tiazolo, processo para a sua preparacao e utilizacao |
| US7407975B2 (en) | 1997-08-09 | 2008-08-05 | Bayer Schering Pharma Ag | Epothilone derivatives, method for producing same and their pharmaceutical use |
| AU753519B2 (en) | 1998-02-05 | 2002-10-17 | Novartis Ag | Compositions containing organic compounds |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| FR2775187B1 (fr) | 1998-02-25 | 2003-02-21 | Novartis Ag | Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo |
| CA2322157C (en) | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| AU5036999A (en) | 1998-06-30 | 2000-01-17 | Schering Aktiengesellschaft | Epothilon derivatives, their preparation process, intermediate products and their pharmaceutical use |
| NZ511722A (en) | 1998-11-20 | 2004-05-28 | Kosan Biosciences Inc | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| BR9916833A (pt) | 1998-12-22 | 2001-09-25 | Novartis Ag | Derivados de epotilona e seu uso como agentes antitumor |
| DE50014587D1 (de) | 1999-02-18 | 2007-10-04 | Bayer Schering Pharma Ag | 16-halogen-epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung |
| US6211412B1 (en) | 1999-03-29 | 2001-04-03 | The University Of Kansas | Synthesis of epothilones |
| AR023792A1 (es) | 1999-04-30 | 2002-09-04 | Bayer Schering Pharma Ag | Derivados 6-alquenilo- y 6-alquinilo-epotilona, los procedimientos para prepararlos y su empleo en productos farmaceuticos |
-
1999
- 1999-03-29 US US09/280,192 patent/US6380395B1/en not_active Expired - Lifetime
- 1999-03-29 US US09/280,191 patent/US6399638B1/en not_active Expired - Lifetime
- 1999-04-05 PT PT99916383T patent/PT1073648E/pt unknown
- 1999-04-05 DK DK99915273T patent/DK1073647T3/da active
- 1999-04-05 DE DE69941083T patent/DE69941083D1/de not_active Expired - Lifetime
- 1999-04-05 DK DK05015236.2T patent/DK1589017T3/da active
- 1999-04-05 CA CA2329181A patent/CA2329181C/en not_active Expired - Fee Related
- 1999-04-05 ES ES99916383T patent/ES2273484T3/es not_active Expired - Lifetime
- 1999-04-05 AU AU34716/99A patent/AU748526B2/en not_active Ceased
- 1999-04-05 ES ES99915273T patent/ES2327803T3/es not_active Expired - Lifetime
- 1999-04-05 TR TR2000/03036T patent/TR200003036T2/xx unknown
- 1999-04-05 WO PCT/US1999/007448 patent/WO1999054318A1/en not_active Ceased
- 1999-04-05 WO PCT/US1999/007475 patent/WO1999054319A1/en not_active Ceased
- 1999-04-05 PT PT50152362T patent/PT1589017E/pt unknown
- 1999-04-05 AT AT99916383T patent/ATE340177T1/de active
- 1999-04-05 PT PT99915273T patent/PT1073647E/pt unknown
- 1999-04-05 JP JP2000544658A patent/JP4476483B2/ja not_active Expired - Fee Related
- 1999-04-05 BR BR9909795-8A patent/BR9909795A/pt not_active IP Right Cessation
- 1999-04-05 EP EP99915273A patent/EP1073647B1/en not_active Expired - Lifetime
- 1999-04-05 EP EP99916383A patent/EP1073648B1/en not_active Expired - Lifetime
- 1999-04-05 AU AU33827/99A patent/AU757733B2/en not_active Ceased
- 1999-04-05 CA CA002323609A patent/CA2323609A1/en not_active Abandoned
- 1999-04-05 ES ES05015236T patent/ES2400049T3/es not_active Expired - Lifetime
- 1999-04-05 EP EP05015236A patent/EP1589017B1/en not_active Expired - Lifetime
- 1999-04-05 DE DE69933287T patent/DE69933287T2/de not_active Expired - Lifetime
- 1999-04-05 DK DK99916383T patent/DK1073648T3/da active
- 1999-04-05 AT AT99915273T patent/ATE435861T1/de active
- 1999-04-05 CN CNB998052663A patent/CN1142923C/zh not_active Expired - Fee Related
- 1999-04-05 JP JP2000544657A patent/JP2002512238A/ja active Pending
- 1999-04-20 PE PE1999000331A patent/PE20000460A1/es not_active Application Discontinuation
- 1999-04-21 AR ARP990101834A patent/AR015774A1/es unknown
- 1999-04-21 AR ARP990101833A patent/AR015007A1/es unknown
-
2006
- 2006-12-08 CY CY20061101766T patent/CY1105836T1/el unknown
-
2009
- 2009-09-01 CY CY20091100911T patent/CY1109593T1/el unknown
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