AR070185A1 - Formas solidas de ortataxel - Google Patents
Formas solidas de ortataxelInfo
- Publication number
- AR070185A1 AR070185A1 ARP090100137A ARP090100137A AR070185A1 AR 070185 A1 AR070185 A1 AR 070185A1 AR P090100137 A ARP090100137 A AR P090100137A AR P090100137 A ARP090100137 A AR P090100137A AR 070185 A1 AR070185 A1 AR 070185A1
- Authority
- AR
- Argentina
- Prior art keywords
- ortataxel
- beta
- water
- isobutylserinyl
- boc
- Prior art date
Links
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
-
- 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
- C07D493/06—Peri-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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
-
- 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
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D305/06—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 the ring atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Epoxy Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
La presente invencion hace referencia a las formas solidas de Ortataxel [13-(N-Boc-beta-isobutilserinil)-14-beta-hidroxibacatina III 1,14-carbonato] (Ortataxel). Se divulgan la forma A amorfa; la forma B cristalina, las mezclas de las mismas; los procesos para prepararlas. Composiciones farmacéuticas que contienen la forma A o la forma B de Ortataxel y uso de las formas A o B para la preparacion de composiciones farmacéuticas. La forma A se transforma en la forma B cuando se suspende y se agita en una mezcla de etanol y agua por 4-8 horas. Si la suspension se agita por menos de 4 horas, se obtienen mezclas de la Forma A y la Forma B. Se puede obtener también la Forma B o mezclas de las Formas A y B mediante la disolucion de Ortataxel en un solvente orgánico protico seguido por la adicion de agua. Compuesto antitumoral activo en tumores de mamas, pulmon, ovario, prostata, colon, rinon y páncreas. Reivindicacion 1: Forma A amorfa de Ortataxel [13-(N-Boc-beta-isobutilserinil)-14-beta--hidroxibacatina III 1,14-carbonato] (formula 1). Reivindicacion 2: Proceso para preparar la Forma A amorfa de la reivindicacion 1 que comprende disolver Ortataxel en cetona o en un solvente orgánico dipolar aprotico, seguido por la adicion de agua con 0,001-0,003% p/v de un ácido orgánico. Reivindicacion 6: Forma cristalina de Ortataxel [13-(N-Boc-beta-isobutilserinil)-14-beta-hidroxibacatina III 1,14-carbonato] (formula 1) cuya XRPD se caracteriza por los siguientes picos 3,5, 6,8, 9,9, 10,1, 10,7, 12,1, 13,1, 14,8, 18,2, 19,7, 21,3, 29,3 grados 2-teta. Reivindicacion 7: Un proceso para la preparacion de la Forma B de Ortataxel de la reivindicacion 6, que comprende disolver Ortataxel en etanol que contiene trazas de un ácido orgánico, seguido por la adicion de agua y agitar a una temperatura que oscila de 0 a 60°C por un rango de tiempo que va de 4 a 8 horas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08000904A EP2080764B1 (en) | 2008-01-18 | 2008-01-18 | Solid forms of ortataxel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070185A1 true AR070185A1 (es) | 2010-03-17 |
Family
ID=39205210
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100137A AR070185A1 (es) | 2008-01-18 | 2009-01-16 | Formas solidas de ortataxel |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20110054015A1 (es) |
| EP (1) | EP2080764B1 (es) |
| JP (1) | JP2011509957A (es) |
| KR (1) | KR101583098B1 (es) |
| CN (1) | CN101952297A (es) |
| AR (1) | AR070185A1 (es) |
| AU (1) | AU2009204559B2 (es) |
| BR (1) | BRPI0906698A2 (es) |
| CA (1) | CA2711690C (es) |
| DK (1) | DK2080764T3 (es) |
| ES (1) | ES2389518T3 (es) |
| HK (1) | HK1131782A1 (es) |
| IL (1) | IL207045A (es) |
| MX (1) | MX2010007850A (es) |
| NO (1) | NO342387B1 (es) |
| RU (1) | RU2488586C2 (es) |
| TW (1) | TWI432437B (es) |
| WO (1) | WO2009090024A1 (es) |
| ZA (1) | ZA201004507B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2389518T3 (es) | 2008-01-18 | 2012-10-26 | Indena S.P.A. | Formas sólidas de ortataxel |
| CN104650109B (zh) * | 2013-11-22 | 2019-01-01 | 江苏天士力帝益药业有限公司 | 紫杉烷类化合物 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3938480A1 (de) | 1989-11-20 | 1991-05-23 | Hell Rudolf Dr Ing Gmbh | Vorrichtung zum aufspannen von blattfoermigem aufzeichnungsmaterial |
| US5380916A (en) | 1990-11-02 | 1995-01-10 | University Of Florida | Method for the isolation and purification of taxane derivatives |
| MX9102128A (es) | 1990-11-23 | 1992-07-08 | Rhone Poulenc Rorer Sa | Derivados de taxano,procedimiento para su preparacion y composicion farmaceutica que los contiene |
| IT1254517B (it) | 1992-03-06 | 1995-09-25 | Indena Spa | 14-beta idrossi-10-deacetil-baccatina iii, suoi derivati, loro prepazione ed impiego terapeutico |
| US5698712A (en) | 1992-03-06 | 1997-12-16 | Indena S.P.A. | Baccatine III derivatives |
| FR2688499B1 (fr) | 1992-03-10 | 1994-05-06 | Rhone Poulenc Rorer Sa | Procede de preparation de la beta-phenylisoserine et de ses analogues. |
| US5200534A (en) * | 1992-03-13 | 1993-04-06 | University Of Florida | Process for the preparation of taxol and 10-deacetyltaxol |
| US5319112A (en) * | 1992-08-18 | 1994-06-07 | Virgnia Tech Intellectual Properties, Inc. | Method for the conversion of cephalomannine to taxol and for the preparation of N-acyl analogs of taxol |
| FR2696460B1 (fr) | 1992-10-05 | 1994-11-25 | Rhone Poulenc Rorer Sa | Procédé de préparation de dérivés du taxane. |
| IL107950A (en) | 1992-12-15 | 2001-04-30 | Upjohn Co | b 7, b 8 - Matano - Taxols, their preparation and pharmaceutical preparations against malignant tumors containing them |
| CA2111527C (en) | 1992-12-24 | 2000-07-18 | Jerzy Golik | Phosphonooxymethyl ethers of taxane derivatives |
| US5475011A (en) | 1993-03-26 | 1995-12-12 | The Research Foundation Of State University Of New York | Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment |
| IT1261667B (it) | 1993-05-20 | 1996-05-29 | Tassano ad attivita' antitumorale. | |
| ES2145829T3 (es) | 1993-06-11 | 2000-07-16 | Upjohn Co | Uso antineoplasico de delta 6,7-taxoles y composiciones farmaceuticas que los contienen. |
| IL109926A (en) | 1993-06-15 | 2000-02-29 | Bristol Myers Squibb Co | Methods for the preparation of taxanes and microorganisms and enzymes utilized therein |
| FR2722191B1 (fr) * | 1994-07-08 | 1996-08-23 | Rhone Poulenc Rorer Sa | Procede de preparation du trihydrate du (2r,3s)-3-tertbutoxycarbonylamino-2-hydroxy-3-phenylpropionate de 4-acetoxy2alpha-benzoyloxy-5beta,20epoxy-1,7beta,10beta trihydroxy-9-oxo-tax-11-en-13alpha-yle |
| IT1275936B1 (it) | 1995-03-17 | 1997-10-24 | Indena Spa | Derivati della 10-deacetilbaccatina iii e della 10-deacetil-14b- idrossibaccatina iii loro metodo di preparazione e formulazioni |
| FR2732341A1 (fr) | 1995-03-27 | 1996-10-04 | Rhone Poulenc Rorer Sa | Nouveaux taxoides, leur preparation et les compositions pharmaceutiques qui les contiennent |
| IT1275435B (it) | 1995-05-19 | 1997-08-07 | Indena Spa | Derivati della 10-desacetil-14beta-idrossibaccatina iii,loro metodo di preparazione e formulazioni che li contengono |
| IT1283633B1 (it) | 1996-05-10 | 1998-04-23 | Indena Spa | Derivati tassanici loro sintesi e formulazioni che li contengono |
| US5811452A (en) | 1997-01-08 | 1998-09-22 | The Research Foundation Of State University Of New York | Taxoid reversal agents for drug-resistance in cancer chemotherapy and pharmaceutical compositions thereof |
| ITMI991483A1 (it) | 1999-07-06 | 2001-01-06 | Indena Spa | Derivati tassanici e procedimenti per la loro preparazione |
| IT1318678B1 (it) | 2000-08-10 | 2003-08-27 | Indena Spa | Procedimento per la preparazione di derivati della baccatina iii. |
| IT1320107B1 (it) * | 2000-11-28 | 2003-11-18 | Indena Spa | Procedimento per la preparazione di derivati tassanici. |
| ITMI20012185A1 (it) | 2001-10-19 | 2003-04-19 | Indena Spa | Procedimento per la preparazione della 14beta-idrossi-baccatina iii-1,14-carbonato |
| ITMI20012186A1 (it) | 2001-10-19 | 2003-04-19 | Indena Spa | Procedimento per la preparazione della 14-beta-idrossi-baccatina iii-1,14-carbonato |
| WO2005061474A1 (en) | 2003-12-12 | 2005-07-07 | Quiral Química Do Brasil | Process for the preparation of anhydrous and hydrated active pharmaceutical ingredients (apis); stable pharmaceutical compositions prepared from the same and uses of said compositions |
| WO2006058121A1 (en) | 2004-11-23 | 2006-06-01 | Bristol-Myers Squibb Company | Crystalline forms of 3'-tert-butyl-3'-n-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-n-debenzoyl-4-o-methoxycarbonyl-paclitaxel |
| KR100995390B1 (ko) * | 2006-01-02 | 2010-11-19 | 주식회사 삼양제넥스 | 무정형, 무수결정형 또는 수화 결정형 도세탁셀의 제조방법 |
| US7919108B2 (en) * | 2006-03-10 | 2011-04-05 | Cook Incorporated | Taxane coatings for implantable medical devices |
| US7232916B1 (en) | 2006-05-11 | 2007-06-19 | Indena S.P.A. | Process for the preparation of a taxane derivative |
| DK1854799T3 (da) | 2006-05-12 | 2011-07-18 | Indena Spa | Fremgangsmåde til fremstilling af et taxanderivat |
| ES2389518T3 (es) | 2008-01-18 | 2012-10-26 | Indena S.P.A. | Formas sólidas de ortataxel |
-
2008
- 2008-01-18 ES ES08000904T patent/ES2389518T3/es active Active
- 2008-01-18 DK DK08000904.6T patent/DK2080764T3/da active
- 2008-01-18 EP EP08000904A patent/EP2080764B1/en active Active
-
2009
- 2009-01-12 CN CN2009801025573A patent/CN101952297A/zh active Pending
- 2009-01-12 BR BRPI0906698-5A patent/BRPI0906698A2/pt not_active Application Discontinuation
- 2009-01-12 MX MX2010007850A patent/MX2010007850A/es active IP Right Grant
- 2009-01-12 AU AU2009204559A patent/AU2009204559B2/en not_active Ceased
- 2009-01-12 WO PCT/EP2009/000112 patent/WO2009090024A1/en active Application Filing
- 2009-01-12 CA CA2711690A patent/CA2711690C/en not_active Expired - Fee Related
- 2009-01-12 US US12/863,167 patent/US20110054015A1/en not_active Abandoned
- 2009-01-12 JP JP2010542566A patent/JP2011509957A/ja active Pending
- 2009-01-12 KR KR1020107015731A patent/KR101583098B1/ko active IP Right Grant
- 2009-01-12 RU RU2010134415/04A patent/RU2488586C2/ru not_active IP Right Cessation
- 2009-01-16 AR ARP090100137A patent/AR070185A1/es not_active Application Discontinuation
- 2009-01-16 TW TW098101503A patent/TWI432437B/zh not_active IP Right Cessation
- 2009-11-13 HK HK09110647.7A patent/HK1131782A1/xx not_active IP Right Cessation
-
2010
- 2010-06-25 ZA ZA2010/04507A patent/ZA201004507B/en unknown
- 2010-07-15 IL IL207045A patent/IL207045A/en active IP Right Grant
- 2010-08-12 NO NO20101144A patent/NO342387B1/no not_active IP Right Cessation
-
2013
- 2013-12-10 US US14/102,365 patent/US9127018B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| IL207045A0 (en) | 2010-12-30 |
| JP2011509957A (ja) | 2011-03-31 |
| WO2009090024A1 (en) | 2009-07-23 |
| EP2080764B1 (en) | 2012-08-22 |
| HK1131782A1 (en) | 2010-02-05 |
| DK2080764T3 (da) | 2012-09-24 |
| US9127018B2 (en) | 2015-09-08 |
| MX2010007850A (es) | 2010-11-09 |
| NO342387B1 (no) | 2018-05-14 |
| AU2009204559B2 (en) | 2013-09-26 |
| EP2080764A1 (en) | 2009-07-22 |
| AU2009204559A1 (en) | 2009-07-23 |
| RU2488586C2 (ru) | 2013-07-27 |
| ES2389518T3 (es) | 2012-10-26 |
| TWI432437B (zh) | 2014-04-01 |
| NO20101144L (no) | 2010-08-12 |
| US20140128459A1 (en) | 2014-05-08 |
| CA2711690C (en) | 2017-05-16 |
| TW200936594A (en) | 2009-09-01 |
| US20110054015A1 (en) | 2011-03-03 |
| ZA201004507B (en) | 2011-04-28 |
| IL207045A (en) | 2014-08-31 |
| BRPI0906698A2 (pt) | 2015-07-07 |
| CN101952297A (zh) | 2011-01-19 |
| KR20100102160A (ko) | 2010-09-20 |
| CA2711690A1 (en) | 2009-07-23 |
| RU2010134415A (ru) | 2012-02-27 |
| KR101583098B1 (ko) | 2016-01-07 |
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