AR066430A1 - Proceso para preparar inhibidores de aromatasa y forma cristalina de exemestano - Google Patents
Proceso para preparar inhibidores de aromatasa y forma cristalina de exemestanoInfo
- Publication number
- AR066430A1 AR066430A1 ARP080101880A ARP080101880A AR066430A1 AR 066430 A1 AR066430 A1 AR 066430A1 AR P080101880 A ARP080101880 A AR P080101880A AR P080101880 A ARP080101880 A AR P080101880A AR 066430 A1 AR066430 A1 AR 066430A1
- Authority
- AR
- Argentina
- Prior art keywords
- exemestane
- prepare
- crystal form
- aromatase inhibitors
- formula
- Prior art date
Links
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 title abstract 2
- 239000003886 aromatase inhibitor Substances 0.000 title abstract 2
- 229960000255 exemestane Drugs 0.000 title abstract 2
- 229940046844 aromatase inhibitors Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 229940122815 Aromatase inhibitor Drugs 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000002904 solvent Substances 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
-
- 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
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un proceso para preparar un inhibidor de aromatasa de la formula (1) en donde cada uno de R1, R2, R3, y R4 es de modo independiente hidrogeno, halogeno o alquilo C1-6, que comprende hacer reaccionar Un compuesto de la formula (2) con un ácido enpresencia de un solvente apropiado. También se describe una nueva forma cristalina de exemestano.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92762607P | 2007-05-04 | 2007-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR066430A1 true AR066430A1 (es) | 2009-08-19 |
Family
ID=39940021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101880A AR066430A1 (es) | 2007-05-04 | 2008-05-02 | Proceso para preparar inhibidores de aromatasa y forma cristalina de exemestano |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20080275259A1 (es) |
| EP (1) | EP2142561B9 (es) |
| JP (1) | JP5282084B2 (es) |
| KR (1) | KR101446825B1 (es) |
| CN (1) | CN101730705B (es) |
| AR (1) | AR066430A1 (es) |
| AU (1) | AU2008248222B2 (es) |
| CA (1) | CA2686312C (es) |
| DK (1) | DK2142561T3 (es) |
| ES (1) | ES2428166T3 (es) |
| NZ (1) | NZ580956A (es) |
| PL (1) | PL2142561T3 (es) |
| TW (1) | TWI354675B (es) |
| WO (1) | WO2008137048A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005070951A1 (en) | 2004-01-16 | 2005-08-04 | Cedarburg Pharmaceuticals, Inc. | Exemestane and its intermediates and methods of making the same |
| CN105061539A (zh) * | 2015-08-18 | 2015-11-18 | 齐鲁安替(临邑)制药有限公司 | 一种依西美坦的新晶型及其制备工艺 |
| CN106928303B (zh) * | 2017-03-30 | 2018-11-23 | 绍兴文理学院 | 一种螺环化合物及其制备方法和应用 |
| CN106928302B (zh) * | 2017-03-30 | 2019-02-22 | 浙江医药股份有限公司昌海生物分公司 | 一种雄烯二酮衍生物及其制备方法和应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3112305A (en) * | 1960-11-07 | 1963-11-26 | British Drug Houses Ltd | 6-methylene-3-oxo-delta4-steroids and process for their preparation |
| NL122154C (es) * | 1963-10-18 | |||
| JPS5614675B2 (es) * | 1973-06-16 | 1981-04-06 | ||
| GB8517360D0 (en) * | 1985-07-09 | 1985-08-14 | Erba Farmitalia | Substituted androsta-1,4-diene-3,17-diones |
| DD258820A1 (de) | 1986-06-13 | 1988-08-03 | Adw Ddr | Verfahren zur herstellung von 6beta-hydroxy-methyl-androsta-1,4-dien-3,17-dion |
| GB8617107D0 (en) * | 1986-07-14 | 1986-08-20 | Erba Farmitalia | 6-/7-methylenandrosta-1 4-diene-3 17-dione derivatives |
| GB8721383D0 (en) * | 1987-09-11 | 1987-10-21 | Erba Farmitalia | Preparation of methylene derivatives |
| DD264220A1 (de) * | 1987-09-23 | 1989-01-25 | Adw Ddr | Verfahren zur herstellung von 6-methylen-androsta-1,4-dien-3,17-dion |
| GB8801697D0 (en) * | 1988-01-26 | 1988-02-24 | Erba Farmitalia | Improvements in synthesis of 6-methylene derivatives of androsta-1 4-diene-3 17-dione |
| WO2001004342A1 (en) * | 1999-07-07 | 2001-01-18 | Pharmacia & Upjohn Company | Process to prepare exemestane |
| AU2002331916B2 (en) * | 2001-10-03 | 2008-07-24 | Merck Sharp & Dohme Corp. | Androstane 17-beta-carboxamides as androgen receptor modulators |
| CN1317293C (zh) * | 2002-10-24 | 2007-05-23 | 南京长澳医药科技有限公司 | 一种依西美坦的合成工艺 |
| JP4970932B2 (ja) * | 2003-03-11 | 2012-07-11 | トロフォ | コレスト−4−エン−3−オンの誘導体の医薬としての使用、これらを含む医薬組成物、新規誘導体及びそれらの製造方法 |
| WO2005070951A1 (en) * | 2004-01-16 | 2005-08-04 | Cedarburg Pharmaceuticals, Inc. | Exemestane and its intermediates and methods of making the same |
-
2008
- 2008-04-30 US US12/150,661 patent/US20080275259A1/en not_active Abandoned
- 2008-05-01 CA CA2686312A patent/CA2686312C/en not_active Expired - Fee Related
- 2008-05-01 CN CN2008800231422A patent/CN101730705B/zh not_active Expired - Fee Related
- 2008-05-01 DK DK08754185.0T patent/DK2142561T3/da active
- 2008-05-01 JP JP2010507413A patent/JP5282084B2/ja not_active Expired - Fee Related
- 2008-05-01 AU AU2008248222A patent/AU2008248222B2/en not_active Ceased
- 2008-05-01 EP EP08754185.0A patent/EP2142561B9/en not_active Not-in-force
- 2008-05-01 KR KR1020097025203A patent/KR101446825B1/ko not_active Expired - Fee Related
- 2008-05-01 PL PL08754185T patent/PL2142561T3/pl unknown
- 2008-05-01 WO PCT/US2008/005646 patent/WO2008137048A1/en not_active Ceased
- 2008-05-01 ES ES08754185T patent/ES2428166T3/es active Active
- 2008-05-01 NZ NZ580956A patent/NZ580956A/xx not_active IP Right Cessation
- 2008-05-02 AR ARP080101880A patent/AR066430A1/es unknown
- 2008-05-02 TW TW097116398A patent/TWI354675B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| TW200904823A (en) | 2009-02-01 |
| EP2142561A4 (en) | 2010-04-21 |
| EP2142561B9 (en) | 2014-02-19 |
| JP2010526141A (ja) | 2010-07-29 |
| EP2142561A1 (en) | 2010-01-13 |
| US20080275259A1 (en) | 2008-11-06 |
| TWI354675B (en) | 2011-12-21 |
| CA2686312A1 (en) | 2008-11-13 |
| WO2008137048A1 (en) | 2008-11-13 |
| AU2008248222A1 (en) | 2008-11-13 |
| CN101730705B (zh) | 2012-10-03 |
| NZ580956A (en) | 2012-08-31 |
| EP2142561B1 (en) | 2013-06-26 |
| CA2686312C (en) | 2013-06-25 |
| AU2008248222A8 (en) | 2009-12-24 |
| JP5282084B2 (ja) | 2013-09-04 |
| CN101730705A (zh) | 2010-06-09 |
| KR20100028543A (ko) | 2010-03-12 |
| AU2008248222B2 (en) | 2013-03-28 |
| PL2142561T3 (pl) | 2013-11-29 |
| DK2142561T3 (da) | 2013-09-02 |
| ES2428166T3 (es) | 2013-11-06 |
| KR101446825B1 (ko) | 2014-10-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |