JP2011511011A5 - - Google Patents
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- Publication number
- JP2011511011A5 JP2011511011A5 JP2010545285A JP2010545285A JP2011511011A5 JP 2011511011 A5 JP2011511011 A5 JP 2011511011A5 JP 2010545285 A JP2010545285 A JP 2010545285A JP 2010545285 A JP2010545285 A JP 2010545285A JP 2011511011 A5 JP2011511011 A5 JP 2011511011A5
- Authority
- JP
- Japan
- Prior art keywords
- ethynyl
- androstane
- diol
- crystalline
- optionally
- 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.)
- Pending
Links
- 229960005546 17α-ethynyl-3α-androstanediol Drugs 0.000 claims description 76
- 239000000203 mixture Substances 0.000 claims description 29
- 238000001757 thermogravimetry curve Methods 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 17
- 230000004580 weight loss Effects 0.000 claims description 16
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 150000008064 anhydrides Chemical class 0.000 claims description 13
- 238000009472 formulation Methods 0.000 claims description 13
- 201000011510 cancer Diseases 0.000 claims description 12
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 10
- 239000012453 solvate Substances 0.000 claims description 8
- 238000001228 spectrum Methods 0.000 claims description 8
- 238000001069 Raman spectroscopy Methods 0.000 claims description 6
- 238000002844 melting Methods 0.000 claims description 6
- 230000008018 melting Effects 0.000 claims description 6
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 5
- 208000026310 Breast neoplasm Diseases 0.000 claims description 5
- 206010014733 Endometrial cancer Diseases 0.000 claims description 5
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 5
- 206010033128 Ovarian cancer Diseases 0.000 claims description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 5
- 206010060862 Prostate cancer Diseases 0.000 claims description 5
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 5
- 238000004455 differential thermal analysis Methods 0.000 claims description 5
- 239000002775 capsule Substances 0.000 claims description 4
- 239000013078 crystal Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 239000007787 solid Substances 0.000 claims description 4
- 239000007858 starting material Substances 0.000 claims description 4
- 239000003826 tablet Substances 0.000 claims description 4
- 238000002411 thermogravimetry Methods 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 238000005160 1H NMR spectroscopy Methods 0.000 claims description 2
- 206010008263 Cervical dysplasia Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 208000006402 Ductal Carcinoma Diseases 0.000 claims description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 238000002441 X-ray diffraction Methods 0.000 claims description 2
- 239000007894 caplet Substances 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 239000000463 material Substances 0.000 claims description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 2
- 229940068968 polysorbate 80 Drugs 0.000 claims description 2
- 229920000053 polysorbate 80 Polymers 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 239000004094 surface-active agent Substances 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 2
- 238000004442 gravimetric analysis Methods 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2647208P | 2008-02-05 | 2008-02-05 | |
| US9369408P | 2008-09-02 | 2008-09-02 | |
| PCT/US2009/033280 WO2009100258A1 (en) | 2008-02-05 | 2009-02-05 | Pharmaceutical solid state forms |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011511011A JP2011511011A (ja) | 2011-04-07 |
| JP2011511011A5 true JP2011511011A5 (https=) | 2012-06-21 |
Family
ID=40952461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010545285A Pending JP2011511011A (ja) | 2008-02-05 | 2009-02-05 | 医薬的固体状態形態 |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US8518922B2 (https=) |
| EP (1) | EP2249838A4 (https=) |
| JP (1) | JP2011511011A (https=) |
| KR (1) | KR20100113602A (https=) |
| CN (2) | CN103467554A (https=) |
| AU (1) | AU2009212314C1 (https=) |
| CA (1) | CA2712005C (https=) |
| EA (1) | EA018974B9 (https=) |
| IL (1) | IL207378A0 (https=) |
| WO (1) | WO2009100258A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3683218B1 (en) | 2007-12-07 | 2024-09-18 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
| DK2273994T3 (en) * | 2008-04-03 | 2016-02-01 | Neurmedix Inc | PHARMACEUTICAL FORMS OF A MEDICINE |
| WO2011109440A1 (en) | 2010-03-01 | 2011-09-09 | Caris Life Sciences Luxembourg Holdings | Biomarkers for theranostics |
| EP2506855A4 (en) * | 2009-11-30 | 2014-07-30 | Harbor Biosciences Inc | ANTICARCINOMA COMPOUNDS AND SCREENING METHODS |
| US20140148348A1 (en) | 2010-01-13 | 2014-05-29 | Christine Kuslich | Dectection of gastrointestinal disorders |
| WO2011127219A1 (en) | 2010-04-06 | 2011-10-13 | Caris Life Sciences Luxembourg Holdings | Circulating biomarkers for disease |
| US20120220560A1 (en) * | 2010-12-17 | 2012-08-30 | White Steven K | Steroid tetrol solid state forms |
| NZ727015A (en) | 2012-01-25 | 2017-12-22 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| CN104173353B (zh) * | 2013-05-22 | 2018-08-21 | 中国医药工业研究总院 | 不含表面活性剂的固体制剂及其制备方法 |
| AU2014349010C1 (en) * | 2013-11-12 | 2020-08-06 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases |
| CN105434444B (zh) * | 2014-09-29 | 2021-02-05 | 上海奥奇医药科技有限公司 | 一种A-失碳-5α雄甾烷化合物的口服制剂 |
| CN113559075A (zh) | 2014-11-17 | 2021-10-29 | 康泰科思特生物制药公司 | 奥那司酮延长释放组合物和方法 |
| AU2016326657B2 (en) | 2015-09-25 | 2019-10-24 | Context Biopharma, Inc. | Methods of making onapristone intermediates |
| EP3389632A4 (en) | 2015-12-15 | 2019-11-06 | Context Biopharma Inc. | AMORPHIC ONAPRISTON COMPOSITIONS AND METHOD FOR THE PRODUCTION THEREOF |
| WO2018102369A1 (en) | 2016-11-30 | 2018-06-07 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
| MX394899B (es) * | 2017-03-30 | 2025-03-24 | Merck Patent Gmbh | Forma solida de (s)-[2-cloro-4-fluoro-5-(7-morfolin-4-il-quinazolin-4-il)fenil]-(6-metoxi-piridazin-3-il)-metanol. |
| RU2668526C1 (ru) * | 2017-08-18 | 2018-10-01 | Федеральное государственное бюджетное учреждение "Информационно-методический центр по экспертизе, учету и анализу обращения средств медицинского применения" Федеральной службы по надзору в сфере здравоохранения | Способ идентификации и последующего количественного определения основных компонентов в инъекционных лекарственных средствах |
| JP7462632B2 (ja) | 2018-11-30 | 2024-04-05 | カリス エムピーアイ インコーポレイテッド | 次世代分子プロファイリング |
| CN111773388B (zh) * | 2019-04-04 | 2023-07-18 | 上海奥奇医药科技有限公司 | A-失碳-5α雄甾烷化合物类药物与抗癌药物的联合应用 |
| WO2021112918A1 (en) | 2019-12-02 | 2021-06-10 | Caris Mpi, Inc. | Pan-cancer platinum response predictor |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE681869C (de) * | 1935-11-22 | 1939-10-03 | Schering Ag | Verfahren zur Darstellung von tertiaeren Alkoholen der Cyclopentanopolyhydrophenanthrenreihe |
| CH202847A (de) * | 1937-06-26 | 1939-02-15 | Chem Ind Basel | Verfahren zur Darstellung von Acetylen-Derivaten der Cyclopentanopolyhydrophenanthren-Reihe. |
| EP0614456B1 (en) * | 1992-08-28 | 1999-06-09 | Bone Care International, Inc. | 1alpha,24(s)-dihydroxy vitamin d2, its formation and use |
| US5567830A (en) * | 1994-02-14 | 1996-10-22 | Cocensys, Inc. | Process for synthesis of acetylenic carbinols |
| DE69736704T2 (de) | 1996-03-29 | 2007-09-13 | Duphar International Research B.V. | Piperazin- und piperidin- derivate |
| ZA986614B (en) * | 1997-07-25 | 1999-01-27 | Gilead Sciences | Nucleotide analog composition |
| US7045513B1 (en) * | 1999-03-18 | 2006-05-16 | Genelabs Technologies, Inc. | DHEA composition and method |
| PT1955700E (pt) | 1999-09-30 | 2011-05-04 | Harbor Biosciences Inc | Tratamento terap?utico de doen?as associadas ao receptor de androg?nios |
| US6777399B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US7867990B2 (en) * | 2000-12-14 | 2011-01-11 | Ortho-Mcneil Pharmaceutical, Inc. | Steroid hormone products and methods for preparing them |
| AR034206A1 (es) | 2001-02-16 | 2004-02-04 | Solvay Pharm Bv | Un procedimiento para la preparacion de mesilatos de derivados de piperazina y dichos mesilatos |
| DE10314610A1 (de) * | 2003-04-01 | 2004-11-04 | Aventis Pharma Deutschland Gmbh | Neues Diphenylazetidinon mit verbesserten physiologischen Eigenschaften, Verfahren zu dessen Herstellung, diese Verbindungen enthaltende Arzneimittel und dessen Verwendung |
| US7540016B2 (en) * | 2004-07-21 | 2009-05-26 | Beachhead Solutions, Inc. | System and method for lost data destruction of electronic data stored on a portable electronic device which communicates with servers that are inside of and outside of a firewall |
| US7964604B2 (en) * | 2005-02-18 | 2011-06-21 | Solvay Pharmaceuticals B.V. | Bifeprunox mesylate maintenance dose compositions and methods for using the same |
| TW200730505A (en) * | 2005-12-07 | 2007-08-16 | Merck & Co Inc | Polymorphs of an androgen receptor modulator |
| TWI305979B (en) * | 2006-03-24 | 2009-02-01 | Hon Hai Prec Ind Co Ltd | Wireless transceiving system |
| WO2008039566A2 (en) * | 2006-04-22 | 2008-04-03 | Hollis-Eden Pharmaceuticals, Inc. | Drugs and uses |
| DE102007054497B3 (de) * | 2007-11-13 | 2009-07-23 | Sanofi-Aventis Deutschland Gmbh | Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung |
-
2009
- 2009-02-05 EA EA201070713A patent/EA018974B9/ru not_active IP Right Cessation
- 2009-02-05 CN CN2013102558234A patent/CN103467554A/zh active Pending
- 2009-02-05 CA CA2712005A patent/CA2712005C/en not_active Expired - Fee Related
- 2009-02-05 AU AU2009212314A patent/AU2009212314C1/en not_active Ceased
- 2009-02-05 JP JP2010545285A patent/JP2011511011A/ja active Pending
- 2009-02-05 KR KR1020107019161A patent/KR20100113602A/ko not_active Ceased
- 2009-02-05 WO PCT/US2009/033280 patent/WO2009100258A1/en not_active Ceased
- 2009-02-05 CN CN200980104255XA patent/CN101939009B/zh not_active Expired - Fee Related
- 2009-02-05 EP EP09709386A patent/EP2249838A4/en not_active Withdrawn
- 2009-02-12 US US12/370,510 patent/US8518922B2/en active Active
-
2010
- 2010-08-03 IL IL207378A patent/IL207378A0/en unknown
-
2013
- 2013-06-17 US US13/919,593 patent/US9314471B2/en active Active - Reinstated
- 2013-06-17 US US13/919,386 patent/US20130345184A1/en not_active Abandoned
- 2013-06-17 US US13/919,728 patent/US20130338125A1/en not_active Abandoned
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