JP2013522361A5 - - Google Patents
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- Publication number
- JP2013522361A5 JP2013522361A5 JP2013501240A JP2013501240A JP2013522361A5 JP 2013522361 A5 JP2013522361 A5 JP 2013522361A5 JP 2013501240 A JP2013501240 A JP 2013501240A JP 2013501240 A JP2013501240 A JP 2013501240A JP 2013522361 A5 JP2013522361 A5 JP 2013522361A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- administered
- acetoxy
- norpregna
- diene
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 15
- 201000009273 Endometriosis Diseases 0.000 claims description 12
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims description 10
- 206010046798 Uterine leiomyoma Diseases 0.000 claims description 8
- 201000010260 leiomyoma Diseases 0.000 claims description 8
- 230000001419 dependent effect Effects 0.000 claims description 7
- 208000002193 Pain Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 210000004877 mucosa Anatomy 0.000 claims description 6
- 208000005641 Adenomyosis Diseases 0.000 claims description 5
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 5
- 208000005171 Dysmenorrhea Diseases 0.000 claims description 5
- 206010013935 Dysmenorrhoea Diseases 0.000 claims description 5
- 206010033128 Ovarian cancer Diseases 0.000 claims description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 201000009274 endometriosis of uterus Diseases 0.000 claims description 5
- 239000000186 progesterone Substances 0.000 claims description 5
- 229960003387 progesterone Drugs 0.000 claims description 5
- 230000002357 endometrial effect Effects 0.000 claims description 4
- 239000002674 ointment Substances 0.000 claims description 3
- 229940120293 vaginal suppository Drugs 0.000 claims description 3
- 239000006216 vaginal suppository Substances 0.000 claims description 3
- 239000002552 dosage form Substances 0.000 claims 7
- HKDLNTKNLJPAIY-WKWWZUSTSA-N Ulipristal 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)C(C)=O)[C@]2(C)C1 HKDLNTKNLJPAIY-WKWWZUSTSA-N 0.000 claims 3
- 239000002775 capsule Substances 0.000 claims 2
- 239000006071 cream Substances 0.000 claims 2
- 239000000499 gel Substances 0.000 claims 2
- 239000006187 pill Substances 0.000 claims 2
- 239000003826 tablet Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- -1 azilinyl Chemical group 0.000 description 19
- 238000000034 method Methods 0.000 description 16
- 150000003839 salts Chemical class 0.000 description 11
- 125000000217 alkyl group Chemical group 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 230000000708 anti-progestin effect Effects 0.000 description 5
- 229910052739 hydrogen Inorganic materials 0.000 description 5
- 239000001257 hydrogen Substances 0.000 description 5
- 125000002252 acyl group Chemical group 0.000 description 4
- 239000003418 antiprogestin Substances 0.000 description 4
- 125000004193 piperazinyl group Chemical group 0.000 description 4
- 125000004423 acyloxy group Chemical group 0.000 description 3
- 125000002393 azetidinyl group Chemical group 0.000 description 3
- 125000004069 aziridinyl group Chemical group 0.000 description 3
- 125000005331 diazinyl group Chemical group N1=NC(=CC=C1)* 0.000 description 3
- 229940088597 hormone Drugs 0.000 description 3
- 239000005556 hormone Substances 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 230000002611 ovarian Effects 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 125000005910 alkyl carbonate group Chemical group 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 229910052736 halogen Inorganic materials 0.000 description 2
- 150000002367 halogens Chemical class 0.000 description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 125000000392 cycloalkenyl group Chemical group 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000005906 menstruation Effects 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 125000005309 thioalkoxy group Chemical group 0.000 description 1
- 125000004001 thioalkyl group Chemical group 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229940042129 topical gel Drugs 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
- 229940044959 vaginal cream Drugs 0.000 description 1
- 239000000522 vaginal cream Substances 0.000 description 1
- 229940044950 vaginal gel Drugs 0.000 description 1
- 239000000029 vaginal gel Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31626310P | 2010-03-22 | 2010-03-22 | |
| US61/316,263 | 2010-03-22 | ||
| PCT/US2010/062068 WO2011119194A1 (en) | 2010-03-22 | 2010-12-23 | Compositions and methods for non-toxic delivery of antiprogestins |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015201752A Division JP2016029083A (ja) | 2010-03-22 | 2015-10-13 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013522361A JP2013522361A (ja) | 2013-06-13 |
| JP2013522361A5 true JP2013522361A5 (https=) | 2014-01-16 |
| JP5894143B2 JP5894143B2 (ja) | 2016-03-23 |
Family
ID=44343114
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013501240A Expired - Fee Related JP5894143B2 (ja) | 2010-03-22 | 2010-12-23 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
| JP2015201752A Withdrawn JP2016029083A (ja) | 2010-03-22 | 2015-10-13 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
| JP2017213755A Withdrawn JP2018016655A (ja) | 2010-03-22 | 2017-11-06 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
| JP2019088915A Withdrawn JP2019123756A (ja) | 2010-03-22 | 2019-05-09 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015201752A Withdrawn JP2016029083A (ja) | 2010-03-22 | 2015-10-13 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
| JP2017213755A Withdrawn JP2018016655A (ja) | 2010-03-22 | 2017-11-06 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
| JP2019088915A Withdrawn JP2019123756A (ja) | 2010-03-22 | 2019-05-09 | 抗黄体ホルモンの無毒送達のための組成物および方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US20130018027A1 (https=) |
| EP (2) | EP3865502A1 (https=) |
| JP (4) | JP5894143B2 (https=) |
| KR (2) | KR20130009990A (https=) |
| CN (3) | CN102906103A (https=) |
| AR (1) | AR080692A1 (https=) |
| AU (4) | AU2010348967C1 (https=) |
| BR (2) | BR112012023281A2 (https=) |
| CA (1) | CA2793712A1 (https=) |
| CL (1) | CL2012002544A1 (https=) |
| CO (1) | CO6602170A2 (https=) |
| CR (1) | CR20120514A (https=) |
| EA (1) | EA023743B1 (https=) |
| EC (1) | ECSP12012226A (https=) |
| IL (2) | IL221820B (https=) |
| MX (1) | MX2012010327A (https=) |
| MY (1) | MY164622A (https=) |
| NI (2) | NI201200142A (https=) |
| NZ (1) | NZ602525A (https=) |
| PH (2) | PH12012501812A1 (https=) |
| SG (3) | SG10201504913UA (https=) |
| TW (1) | TWI581797B (https=) |
| UA (1) | UA110030C2 (https=) |
| WO (1) | WO2011119194A1 (https=) |
| ZA (1) | ZA201207688B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3139908A4 (en) * | 2014-05-05 | 2018-05-16 | Repros Therapeutics Inc. | Formulations and methods for vaginal delivery of antiprogestins |
| 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 |
| JP2019506443A (ja) * | 2016-02-24 | 2019-03-07 | イースタン バージニア メディカル スクール | 改良された持効性注射用デポ型ブタン酸レボノルゲストレル懸濁製剤 |
| WO2018102369A1 (en) | 2016-11-30 | 2018-06-07 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2377418A1 (fr) * | 1977-01-13 | 1978-08-11 | Roussel Uclaf | Nouveaux derives steroides 4,9-dieniques 11b-substitues, leur procede de preparation et leur application comme medicaments |
| ZA8231B (en) | 1981-01-09 | 1982-11-24 | Roussel Uclaf | New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained |
| FR2521565B1 (fr) | 1982-02-17 | 1985-07-05 | Dior Sa Parfums Christian | Melange pulverulent de constituants lipidiques et de constituants hydrophobes, procede pour le preparer, phases lamellaires lipidiques hydratees et procede de fabrication, compositions pharmaceutiques ou cosmetiques comportant des phases lamellaires lipidiques hydratees |
| FR2522328B1 (fr) * | 1982-03-01 | 1986-02-14 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments |
| FR2534487B1 (fr) | 1982-10-15 | 1988-06-10 | Dior Christian Parfums | Procede d'homogeneisation de dispersions de phases lamellaires lipidiques hydratees, et suspensions obtenues par ce procede |
| EP0116974B1 (de) | 1983-02-18 | 1986-10-29 | Schering Aktiengesellschaft | 11-Beta-Aryl-Estradiene, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate |
| US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
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| DE3347126A1 (de) | 1983-12-22 | 1985-07-11 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3506785A1 (de) | 1985-02-22 | 1986-08-28 | Schering AG, Berlin und Bergkamen, 1000 Berlin | 11ss-n,n-dimethylaminophenyl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| FR2598421B1 (fr) * | 1986-05-06 | 1988-08-19 | Roussel Uclaf | Nouveaux produits 19-nor ou 19-nor d-homo steroides substitues en position 11b par un radical phenyle portant un radical alkynyle, leur procede de preparation, leur application comme medicaments et les compositions les renfermant |
| DE3625315A1 (de) | 1986-07-25 | 1988-01-28 | Schering Ag | 11ss-(4-isopropenylphenyl)-estra-4,9-diene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US5446178A (en) | 1987-03-18 | 1995-08-29 | Schering Aktiengesellschaft | Process for preparing 19,11β-bridged steroids |
| DE3708942A1 (de) | 1987-03-18 | 1988-09-29 | Schering Ag | 19,11ss-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
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| DE3820948A1 (de) | 1988-06-16 | 1989-12-21 | Schering Ag | 10ss, 11ss-ueberbrueckte steroide |
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| AU2805397A (en) * | 1996-08-30 | 1998-03-19 | Population Council, Center For Biomedical Research, The | Vaginal application mifepristone |
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| DE19652408C2 (de) | 1996-12-06 | 2002-04-18 | Schering Ag | Steroidester, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneimitteln |
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| UA74168C2 (uk) * | 1999-10-05 | 2005-11-15 | Коламбіа Леборетеріс (Бермуда) Лімітед | Лікування ендометріозу або безпліддя, або покращення плідності та застосування бета-адренергічного агоніста для виробництва лікарського засобу |
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| CN1210079C (zh) * | 2001-04-25 | 2005-07-13 | 上海市计划生育科学研究所 | 阴道环制剂及其应用 |
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| CN1846703A (zh) * | 2006-02-13 | 2006-10-18 | 程定超 | 米非司酮阴道给药制剂及其组成和制备方法 |
| SI2148681T1 (sl) * | 2007-04-20 | 2016-07-29 | Preglem S.A. | Selektivni modulatorji progesterona v zdravljenju maternične krvavitve |
| DK2197415T3 (da) * | 2007-09-20 | 2014-05-26 | Lapidot Medical Imp And Marketing Ltd | Sammensætninger og midler til at behandle uterusleiomyomer, leiomyom, myom, uterusfibroid, endometriose, adenomyose og beslægtede forstyrrelser med mifepriston |
| US8299050B2 (en) * | 2008-01-29 | 2012-10-30 | Laboratoire Hra-Pharma | Method for treating uterine fibroids |
-
2010
- 2010-12-23 EP EP21167932.9A patent/EP3865502A1/en not_active Withdrawn
- 2010-12-23 NZ NZ602525A patent/NZ602525A/en not_active IP Right Cessation
- 2010-12-23 US US13/636,119 patent/US20130018027A1/en not_active Abandoned
- 2010-12-23 EP EP10807575A patent/EP2550288A1/en not_active Ceased
- 2010-12-23 BR BR112012023281A patent/BR112012023281A2/pt not_active IP Right Cessation
- 2010-12-23 PH PH1/2012/501812A patent/PH12012501812A1/en unknown
- 2010-12-23 WO PCT/US2010/062068 patent/WO2011119194A1/en not_active Ceased
- 2010-12-23 SG SG10201504913UA patent/SG10201504913UA/en unknown
- 2010-12-23 SG SG2012065801A patent/SG183924A1/en unknown
- 2010-12-23 CN CN2010800669434A patent/CN102906103A/zh active Pending
- 2010-12-23 CN CN201710457367.XA patent/CN107260745A/zh active Pending
- 2010-12-23 CN CN201710457607.6A patent/CN107260746A/zh active Pending
- 2010-12-23 KR KR1020127027413A patent/KR20130009990A/ko not_active Ceased
- 2010-12-23 MY MYPI2012004016A patent/MY164622A/en unknown
- 2010-12-23 JP JP2013501240A patent/JP5894143B2/ja not_active Expired - Fee Related
- 2010-12-23 MX MX2012010327A patent/MX2012010327A/es unknown
- 2010-12-23 AU AU2010348967A patent/AU2010348967C1/en not_active Ceased
- 2010-12-23 UA UAA201212075A patent/UA110030C2/uk unknown
- 2010-12-23 CA CA2793712A patent/CA2793712A1/en not_active Abandoned
- 2010-12-23 KR KR1020187026211A patent/KR102166867B1/ko not_active Expired - Fee Related
-
2011
- 2011-03-11 TW TW100108248A patent/TWI581797B/zh not_active IP Right Cessation
- 2011-03-18 AR ARP110100899A patent/AR080692A1/es unknown
- 2011-09-08 BR BR112013015509A patent/BR112013015509A2/pt not_active IP Right Cessation
- 2011-09-08 PH PH1/2013/501176A patent/PH12013501176A1/en unknown
- 2011-09-08 SG SG10201510568WA patent/SG10201510568WA/en unknown
- 2011-09-08 EA EA201390959A patent/EA023743B1/ru not_active IP Right Cessation
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2012
- 2012-09-06 IL IL221820A patent/IL221820B/en active IP Right Grant
- 2012-09-13 CL CL2012002544A patent/CL2012002544A1/es unknown
- 2012-09-20 CO CO12163077A patent/CO6602170A2/es not_active Application Discontinuation
- 2012-09-20 NI NI201200142A patent/NI201200142A/es unknown
- 2012-10-05 EC ECSP12012226 patent/ECSP12012226A/es unknown
- 2012-10-11 CR CR20120514A patent/CR20120514A/es not_active Application Discontinuation
- 2012-10-12 ZA ZA2012/07688A patent/ZA201207688B/en unknown
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2013
- 2013-06-21 NI NI201300059A patent/NI201300059A/es unknown
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2015
- 2015-03-20 US US14/664,518 patent/US20150203526A1/en not_active Abandoned
- 2015-10-13 JP JP2015201752A patent/JP2016029083A/ja not_active Withdrawn
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2016
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2017
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2018
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2019
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2020
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