AR002756A1 - Derivado de fosfonooximetilcarbamato de paclitaxel soluble en agua que tiene efecto antineoplasico y composicion farmaceutica que lo contiene - Google Patents
Derivado de fosfonooximetilcarbamato de paclitaxel soluble en agua que tiene efecto antineoplasico y composicion farmaceutica que lo contieneInfo
- Publication number
- AR002756A1 AR002756A1 ARP960102865A AR10286596A AR002756A1 AR 002756 A1 AR002756 A1 AR 002756A1 AR P960102865 A ARP960102865 A AR P960102865A AR 10286596 A AR10286596 A AR 10286596A AR 002756 A1 AR002756 A1 AR 002756A1
- Authority
- AR
- Argentina
- Prior art keywords
- orx
- alkyl
- alkenyl
- phosphonoximetilcarbamato
- derived
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229930012538 Paclitaxel Natural products 0.000 title 1
- 230000000118 anti-neoplastic effect Effects 0.000 title 1
- 229960001592 paclitaxel Drugs 0.000 title 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 230000000259 anti-tumor effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000000466 oxiranyl group Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/6551—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a four-membered ring
- C07F9/65512—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a four-membered ring condensed with carbocyclic rings or carbocyclic ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epoxy Compounds (AREA)
Abstract
Este invención a los nuevos compuestos antitumorales de fórmula (I), o las sales farmacéuticamente aceptables de los mismos,en donde: R1 es OH, -OC(O)Rxó -OC(O)ORx, R2 es -H,-OH-,OC(O)Rx ó -OC(O)ORx, Res H,-OH ó fluoro, R6es -H o -OH,R6 es H,ó R2 yR6 conjuntamente pueden formar el anillo de oxirano o unenlace, R3 es H, OH, alcoxi, -OCONR11R12, -OC(O)Rx ó -OC(O)ORx, R8 es metilo o hidroximetilo,ó R8 y R2 conjuntamente puede formar ciclopropano,R9 es -OH ó --OC(O)Rx,con la condición de quecuan do R8 y R2 formen ciclopropano,R2 sea -H, cuando R2 y R6 formen el anillo de oxirano o el doble enlace, R2 y R6sean -H,cuando R2 es -OH, -OC(O)Rx ó OC(O)ORx, R2 sea -H, cuando R2 es fluoro, R2 sea H,uno de R7 o R7 sea -H y el otro sea H,-OC(O)Rx ó - OC(O)ORx, ó R7 y R7conjuntamente pueden formar un grupo oxo, R11 y R12 son alquilo, -H, arilo sustituido o nó,R4 y R5 son alquilo, alquenilo, alquinilo, ó -Z-R10, Z es un esun enlace directo, alquilo o alquenilo, R10 es arilosustituido o nó, cicloalquilo o heteroarilo,p es 0 ó 1,Rd y Re son -H,alquilo,arilo sustituido onó o el grupo protector de fosfono, Rf es -H ó -OH,Rx es cicloalquilo,alquenilo o alquilo. Otro aspecto más de la presente invención proporcionaunaformulación far macéutica que comprende una cantidad antitumoral efectiva del compuesto de la fórmula (I).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46924795A | 1995-06-06 | 1995-06-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR002756A1 true AR002756A1 (es) | 1998-04-29 |
Family
ID=23863053
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP960102865A AR002756A1 (es) | 1995-06-06 | 1996-06-03 | Derivado de fosfonooximetilcarbamato de paclitaxel soluble en agua que tiene efecto antineoplasico y composicion farmaceutica que lo contiene |
Country Status (23)
| Country | Link |
|---|---|
| EP (1) | EP0747385B1 (es) |
| JP (1) | JPH08337589A (es) |
| KR (1) | KR100375956B1 (es) |
| CN (1) | CN1066151C (es) |
| AR (1) | AR002756A1 (es) |
| AT (1) | ATE222259T1 (es) |
| AU (1) | AU695959B2 (es) |
| CA (1) | CA2176191A1 (es) |
| CZ (1) | CZ291516B6 (es) |
| DE (1) | DE69622933T2 (es) |
| DK (1) | DK0747385T3 (es) |
| ES (1) | ES2181824T3 (es) |
| HU (1) | HUP9601524A3 (es) |
| IL (1) | IL118526A (es) |
| MX (1) | MX9601994A (es) |
| NO (1) | NO315233B1 (es) |
| NZ (1) | NZ286723A (es) |
| PL (1) | PL187883B1 (es) |
| PT (1) | PT747385E (es) |
| RU (1) | RU2162082C2 (es) |
| SG (1) | SG72692A1 (es) |
| TW (1) | TW354293B (es) |
| ZA (1) | ZA964261B (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6395770B1 (en) * | 1995-10-26 | 2002-05-28 | Baker Norton Pharmaceuticals, Inc. | Method and compositions for administering taxanes orally to human patients |
| US6495579B1 (en) | 1996-12-02 | 2002-12-17 | Angiotech Pharmaceuticals, Inc. | Method for treating multiple sclerosis |
| US6515016B2 (en) | 1996-12-02 | 2003-02-04 | Angiotech Pharmaceuticals, Inc. | Composition and methods of paclitaxel for treating psoriasis |
| DE69832173T2 (de) * | 1997-05-27 | 2006-08-03 | IVAX RESEARCH, INC., Miami | Zusammensetzungen zur oralen verabreichung von taxanen und deren verwendung |
| US6204257B1 (en) | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
| WO2000048606A1 (en) * | 1999-02-18 | 2000-08-24 | Oxigene, Inc. | Compositions and methods for use in targeting vascular destruction |
| US6362172B2 (en) * | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
| AR030188A1 (es) | 2000-02-02 | 2003-08-13 | Univ Florida State Res Found | Compuestos de taxano sustituidos con esteres en el c7; composiciones farmaceuticas que los contienen y proceso para tratar un sujeto mamifero que sufre de una condicion que responde a los taxanos |
| CZ20013429A3 (cs) | 2000-02-02 | 2002-04-17 | Florida State University Research Foundation, Inc. | Taxany substituované v poloze C7 karbonátem jako protinádorová činidla |
| US6750246B1 (en) | 2000-02-03 | 2004-06-15 | Bristol-Myers Squibb Company | C-4 carbonate taxanes |
| US6916942B2 (en) | 2000-02-03 | 2005-07-12 | Bristol-Myers Squibb Company | Process for the preparation of C-4 carbonate taxanes |
| US7063977B2 (en) | 2001-08-21 | 2006-06-20 | Bristol-Myers Squibb Company | Enzymatic resolution of t-butyl taxane derivatives |
| KR20030049023A (ko) * | 2001-12-13 | 2003-06-25 | 주식회사 코오롱 | 방사선 감작제용 파클리탁셀 유도체 |
| US7229978B2 (en) * | 2001-12-21 | 2007-06-12 | Mgi Gp, Inc. | Process for preparing water soluble phosphonooxymethyl derivatives of alcohol and phenol |
| TW200540164A (en) | 2004-03-05 | 2005-12-16 | Univ Florida State Res Found | C7 lactyloxy-substituted taxanes |
| ES2663495T3 (es) * | 2005-02-18 | 2018-04-13 | Abraxis Bioscience, Llc | Fármacos con hidrofobicidad mejorada para incorporación en dispositivos médicos |
| ITMI20050614A1 (it) * | 2005-04-12 | 2006-10-13 | Indena Spa | Processo per la purificazione della 10-deacetilbaccatina iii dalla 10-deacetil-2-debenzoil-2-pentenoilbaccatina iii |
| RU2420239C1 (ru) * | 2009-10-21 | 2011-06-10 | Федеральное государственное учреждение "Ростовский научно-исследовательский онкологический институт Федерального агентства по высокотехнологичной медицинской помощи" | Способ лечения злокачественных забрюшинных опухолей у детей и подростков |
| EA201892726A1 (ru) | 2013-03-15 | 2019-04-30 | Консерт Фармасьютикалс, Инк. | Дейтерированный палбоциклиб |
| WO2015009889A1 (en) | 2013-07-18 | 2015-01-22 | Concert Pharmaceuticals, Inc. | Deuterated intedanib derivatives and their use for the treatment of proliferative disorders |
| ES2969792T3 (es) * | 2015-11-19 | 2024-05-22 | Biohaven Therapeutics Ltd | Profármacos de amina de compuestos farmacéuticos |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2017724C1 (ru) * | 1990-07-12 | 1994-08-15 | Дзе Юниверсити оф Канзас | Способ получения производных таксола |
| MX9308012A (es) * | 1992-12-24 | 1994-08-31 | Bristol Myers Squibb Co | Eteres fosfonooximetilicos de derivados de taxano, solubles en agua y composiciones farmaceuticas que los incluyen. |
| CA2129288C (en) * | 1993-08-17 | 2000-05-16 | Jerzy Golik | Phosphonooxymethyl esters of taxane derivatives |
-
1996
- 1996-04-27 TW TW085105043A patent/TW354293B/zh active
- 1996-05-09 CA CA002176191A patent/CA2176191A1/en not_active Abandoned
- 1996-05-27 MX MX9601994A patent/MX9601994A/es not_active IP Right Cessation
- 1996-05-27 ZA ZA9604261A patent/ZA964261B/xx unknown
- 1996-05-29 CZ CZ19961563A patent/CZ291516B6/cs not_active IP Right Cessation
- 1996-05-31 NO NO19962231A patent/NO315233B1/no not_active Application Discontinuation
- 1996-06-02 IL IL11852696A patent/IL118526A/en not_active IP Right Cessation
- 1996-06-03 JP JP8139795A patent/JPH08337589A/ja active Pending
- 1996-06-03 AR ARP960102865A patent/AR002756A1/es active IP Right Grant
- 1996-06-04 KR KR1019960019825A patent/KR100375956B1/ko not_active Expired - Fee Related
- 1996-06-04 NZ NZ286723A patent/NZ286723A/en unknown
- 1996-06-05 PT PT96109044T patent/PT747385E/pt unknown
- 1996-06-05 EP EP96109044A patent/EP0747385B1/en not_active Expired - Lifetime
- 1996-06-05 AU AU54718/96A patent/AU695959B2/en not_active Ceased
- 1996-06-05 DK DK96109044T patent/DK0747385T3/da active
- 1996-06-05 HU HU9601524A patent/HUP9601524A3/hu unknown
- 1996-06-05 ES ES96109044T patent/ES2181824T3/es not_active Expired - Lifetime
- 1996-06-05 AT AT96109044T patent/ATE222259T1/de not_active IP Right Cessation
- 1996-06-05 RU RU96111012/04A patent/RU2162082C2/ru not_active IP Right Cessation
- 1996-06-05 PL PL31463796A patent/PL187883B1/pl not_active IP Right Cessation
- 1996-06-05 DE DE69622933T patent/DE69622933T2/de not_active Expired - Fee Related
- 1996-06-06 SG SG1996009989A patent/SG72692A1/en unknown
- 1996-06-06 CN CN96106851A patent/CN1066151C/zh not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| PL187883B1 (pl) | 2004-10-29 |
| EP0747385A1 (en) | 1996-12-11 |
| NO962231D0 (no) | 1996-05-31 |
| IL118526A (en) | 2001-05-20 |
| NO315233B1 (no) | 2003-08-04 |
| ES2181824T3 (es) | 2003-03-01 |
| TW354293B (en) | 1999-03-11 |
| CN1144805A (zh) | 1997-03-12 |
| AU5471896A (en) | 1996-12-19 |
| KR100375956B1 (ko) | 2003-04-21 |
| EP0747385B1 (en) | 2002-08-14 |
| DK0747385T3 (da) | 2002-12-16 |
| CN1066151C (zh) | 2001-05-23 |
| KR970000222A (ko) | 1997-01-21 |
| NO962231L (no) | 1996-12-09 |
| RU2162082C2 (ru) | 2001-01-20 |
| CA2176191A1 (en) | 1996-12-07 |
| PL314637A1 (en) | 1996-12-09 |
| NZ286723A (en) | 1998-03-25 |
| JPH08337589A (ja) | 1996-12-24 |
| DE69622933T2 (de) | 2003-04-24 |
| DE69622933D1 (de) | 2002-09-19 |
| MX9601994A (es) | 1997-08-30 |
| AU695959B2 (en) | 1998-08-27 |
| ZA964261B (en) | 1997-11-27 |
| HU9601524D0 (en) | 1996-07-29 |
| CZ291516B6 (cs) | 2003-03-12 |
| PT747385E (pt) | 2002-11-29 |
| ATE222259T1 (de) | 2002-08-15 |
| SG72692A1 (en) | 2000-05-23 |
| CZ156396A3 (en) | 1996-12-11 |
| HUP9601524A3 (en) | 2000-03-28 |
| IL118526A0 (en) | 1996-10-16 |
| HUP9601524A2 (en) | 1997-05-28 |
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant, registration |