JP6655075B2 - オナプリストン持続放出組成物および方法 - Google Patents
オナプリストン持続放出組成物および方法 Download PDFInfo
- Publication number
- JP6655075B2 JP6655075B2 JP2017520520A JP2017520520A JP6655075B2 JP 6655075 B2 JP6655075 B2 JP 6655075B2 JP 2017520520 A JP2017520520 A JP 2017520520A JP 2017520520 A JP2017520520 A JP 2017520520A JP 6655075 B2 JP6655075 B2 JP 6655075B2
- Authority
- JP
- Japan
- Prior art keywords
- onapristone
- cancer
- formulation
- sustained release
- dose
- 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 - Fee Related
Links
- IEXUMDBQLIVNHZ-YOUGDJEHSA-N (8s,11r,13r,14s,17s)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(3-hydroxypropyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(O)CCCO)[C@@]2(C)C1 IEXUMDBQLIVNHZ-YOUGDJEHSA-N 0.000 title claims description 143
- 229950011093 onapristone Drugs 0.000 title claims description 141
- 238000013268 sustained release Methods 0.000 title claims description 28
- 239000012730 sustained-release form Substances 0.000 title claims description 28
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- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 3
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- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 3
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- 239000000044 progesterone antagonist Substances 0.000 description 2
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- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
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- 238000012360 testing method Methods 0.000 description 2
- CIUICCYYGROKEM-UHFFFAOYSA-N 2h-phenanthren-3-one Chemical compound C1=CC=C2C3=CC(=O)CC=C3C=CC2=C1 CIUICCYYGROKEM-UHFFFAOYSA-N 0.000 description 1
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 description 1
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- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
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- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462080868P | 2014-11-17 | 2014-11-17 | |
| US62/080,868 | 2014-11-17 | ||
| PCT/US2015/060940 WO2016081383A1 (en) | 2014-11-17 | 2015-11-16 | Onapristone extended-release compositions and methods |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537883A JP2017537883A (ja) | 2017-12-21 |
| JP2017537883A5 JP2017537883A5 (enExample) | 2018-12-27 |
| JP6655075B2 true JP6655075B2 (ja) | 2020-02-26 |
Family
ID=56014429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017520520A Expired - Fee Related JP6655075B2 (ja) | 2014-11-17 | 2015-11-16 | オナプリストン持続放出組成物および方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US10786461B2 (enExample) |
| EP (1) | EP3247362A4 (enExample) |
| JP (1) | JP6655075B2 (enExample) |
| KR (1) | KR20170084086A (enExample) |
| CN (2) | CN106999501B (enExample) |
| AU (2) | AU2015350241B2 (enExample) |
| CA (1) | CA2966753A1 (enExample) |
| HK (1) | HK1246653A1 (enExample) |
| MX (1) | MX391191B (enExample) |
| RU (1) | RU2017112748A (enExample) |
| WO (1) | WO2016081383A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2017112748A (ru) | 2014-11-17 | 2018-12-19 | Арно Терапьютикс, Инк. | Композиции онапристона пролонгированного действия и способы |
| CA2998924A1 (en) | 2015-09-25 | 2017-03-30 | Context Biopharma Inc. | Methods of making onapristone intermediates |
| CA3008422A1 (en) | 2015-12-15 | 2017-06-22 | Context Biopharma Inc. | Amorphous onapristone compositions and methods of making the same |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES533260A0 (es) | 1983-06-15 | 1985-02-01 | Schering Ag | Procedimiento para la preparacion de 13a-alquilgonanos |
| DE3321826A1 (de) | 1983-06-15 | 1984-12-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
| US4742000A (en) | 1986-05-02 | 1988-05-03 | University Of Chicago | Antibody to human progesterone receptor and diagnostic materials and methods |
| DE3630030A1 (de) | 1986-09-01 | 1988-03-03 | Schering Ag | 13(alpha)-alkylgonan-(delta)(pfeil hoch)9(pfeil hoch)(pfeil hoch)((pfeil hoch)(pfeil hoch)1(pfeil hoch)1(pfeil hoch))(pfeil hoch)-5,10-epoxide |
| US4774236A (en) | 1986-09-17 | 1988-09-27 | Research Triangle Institute | 17α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and pharmaceutical compositions containing them |
| IE60780B1 (en) | 1987-01-23 | 1994-08-10 | Akzo Nv | New 11-aryl steroid derivatives |
| DE3822770A1 (de) | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| US5283190A (en) | 1989-07-31 | 1994-02-01 | Traish Adbulmaged M | Specific monoclonal antibodies against a defined epitope of progesterone receptor and methods for their use |
| DE4008584A1 (de) | 1990-03-15 | 1991-09-26 | Schering Ag | Verfahren zur herstellung von zwischenprodukten fuer die antigestagensynthese (onapristonsynthese) |
| US5141961A (en) | 1991-06-27 | 1992-08-25 | Richrdson-Vicks Inc. | Process for solubilizing difficulty soluble pharmaceutical actives |
| MX9301121A (es) | 1992-03-02 | 1993-09-01 | Schering Ag | Metodo y equipo para la contracepcion oral y regulacion de la menstruacion con estrogeno/progestina/aniprogestina. |
| CN1053450C (zh) | 1992-11-19 | 2000-06-14 | 北京第三制药厂 | 17位取代11β－取代芳香基－4,9－雌甾二烯类化合物的全合成法 |
| DE4332283A1 (de) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| CA2203541A1 (en) | 1994-10-24 | 1996-05-02 | Kristof Chwalisz | Competitive progesterone antagonists for demand-oriented female birth control |
| US5759577A (en) | 1995-01-17 | 1998-06-02 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
| US6900193B1 (en) | 1996-05-01 | 2005-05-31 | The United States Of America As Represented By The Department Of Health And Human Services | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
| IL122740A (en) | 1997-01-15 | 2003-09-17 | Akzo Nobel Nv | 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them |
| US5962444A (en) | 1998-05-29 | 1999-10-05 | Research Triangle Institute | 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6537584B1 (en) | 1999-11-12 | 2003-03-25 | Macromed, Inc. | Polymer blends that swell in an acidic environment and deswell in a basic environment |
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| AU2015350241A1 (en) | 2017-05-04 |
| CN113559075A (zh) | 2021-10-29 |
| AU2015350241B2 (en) | 2021-05-20 |
| EP3247362A4 (en) | 2018-10-10 |
| MX391191B (es) | 2025-03-21 |
| CN106999501B (zh) | 2021-08-13 |
| CN106999501A (zh) | 2017-08-01 |
| US20230157960A1 (en) | 2023-05-25 |
| JP2017537883A (ja) | 2017-12-21 |
| KR20170084086A (ko) | 2017-07-19 |
| US11672762B2 (en) | 2023-06-13 |
| US20160166583A1 (en) | 2016-06-16 |
| HK1246653A1 (zh) | 2018-09-14 |
| CA2966753A1 (en) | 2016-05-26 |
| WO2016081383A1 (en) | 2016-05-26 |
| US20210220279A1 (en) | 2021-07-22 |
| AU2021218093A1 (en) | 2021-09-09 |
| RU2017112748A (ru) | 2018-12-19 |
| EP3247362A1 (en) | 2017-11-29 |
| MX2017005163A (es) | 2018-01-18 |
| RU2017112748A3 (enExample) | 2019-06-26 |
| US10786461B2 (en) | 2020-09-29 |
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