JP2019524846A5 - - Google Patents
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- Publication number
- JP2019524846A5 JP2019524846A5 JP2019509559A JP2019509559A JP2019524846A5 JP 2019524846 A5 JP2019524846 A5 JP 2019524846A5 JP 2019509559 A JP2019509559 A JP 2019509559A JP 2019509559 A JP2019509559 A JP 2019509559A JP 2019524846 A5 JP2019524846 A5 JP 2019524846A5
- Authority
- JP
- Japan
- Prior art keywords
- day
- fluoro
- methylene
- administered
- treatment
- 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
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 29
- PEUPUKDBCPLDIH-UHFFFAOYSA-N 1,2,4-triazole Chemical group C1=NC=N[N]1 PEUPUKDBCPLDIH-UHFFFAOYSA-N 0.000 claims description 24
- 229940127234 oral contraceptive Drugs 0.000 claims description 12
- 239000003539 oral contraceptive agent Substances 0.000 claims description 12
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims description 9
- 229960004400 levonorgestrel Drugs 0.000 claims description 9
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 7
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 7
- 229960002568 ethinylestradiol Drugs 0.000 claims description 7
- 239000003433 contraceptive agent Substances 0.000 claims description 6
- 239000000262 estrogen Substances 0.000 claims description 6
- 229940011871 estrogen Drugs 0.000 claims description 6
- 238000009472 formulation Methods 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 201000009273 Endometriosis Diseases 0.000 claims description 4
- 238000012423 maintenance Methods 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 3
- 229940124558 contraceptive agent Drugs 0.000 claims description 3
- 230000002254 contraceptive effect Effects 0.000 claims description 3
- 239000000583 progesterone congener Substances 0.000 claims description 3
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 claims description 2
- 229940022663 acetate Drugs 0.000 claims description 2
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims description 2
- 229960000978 cyproterone acetate Drugs 0.000 claims description 2
- 229960004976 desogestrel Drugs 0.000 claims description 2
- RPLCPCMSCLEKRS-BPIQYHPVSA-N desogestrel Chemical compound C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 RPLCPCMSCLEKRS-BPIQYHPVSA-N 0.000 claims description 2
- AZFLJNIPTRTECV-FUMNGEBKSA-N dienogest Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@](CC3)(O)CC#N)CC3)C3=C21 AZFLJNIPTRTECV-FUMNGEBKSA-N 0.000 claims description 2
- 229960003309 dienogest Drugs 0.000 claims description 2
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 claims description 2
- 229960004845 drospirenone Drugs 0.000 claims description 2
- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 claims description 2
- ONKUMRGIYFNPJW-KIEAKMPYSA-N ethynodiol diacetate Chemical compound C1C[C@]2(C)[C@@](C#C)(OC(C)=O)CC[C@H]2[C@@H]2CCC3=C[C@@H](OC(=O)C)CC[C@@H]3[C@H]21 ONKUMRGIYFNPJW-KIEAKMPYSA-N 0.000 claims description 2
- -1 guestden Chemical compound 0.000 claims description 2
- IMSSROKUHAOUJS-MJCUULBUSA-N mestranol Chemical compound C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(OC)=CC=C3[C@H]21 IMSSROKUHAOUJS-MJCUULBUSA-N 0.000 claims description 2
- 229960001390 mestranol Drugs 0.000 claims description 2
- 229940053934 norethindrone Drugs 0.000 claims description 2
- 229960001652 norethindrone acetate Drugs 0.000 claims description 2
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 claims description 2
- 229950011191 norgesterone Drugs 0.000 claims description 2
- YPVUHOBTCWJYNQ-SLHNCBLASA-N norgesterone Chemical compound C1CC(=O)CC2=C1[C@H]1CC[C@](C)([C@](CC3)(O)C=C)[C@@H]3[C@@H]1CC2 YPVUHOBTCWJYNQ-SLHNCBLASA-N 0.000 claims description 2
- 230000036470 plasma concentration Effects 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 230000003442 weekly effect Effects 0.000 claims description 2
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 9
- 230000002354 daily effect Effects 0.000 claims 4
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 239000003217 oral combined contraceptive Substances 0.000 claims 3
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000003203 everyday effect Effects 0.000 claims 1
- 229920000089 Cyclic olefin copolymer Polymers 0.000 description 2
- ORKBYCQJWQBPFG-WOMZHKBXSA-N (8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 ORKBYCQJWQBPFG-WOMZHKBXSA-N 0.000 description 1
- PZDLRBUQYWMNBR-UHFFFAOYSA-N 4-[(4-cyanophenyl)-fluoro-(1,2,4-triazol-1-yl)methyl]benzonitrile Chemical compound C=1C=C(C#N)C=CC=1C(N1N=CN=C1)(F)C1=CC=C(C#N)C=C1 PZDLRBUQYWMNBR-UHFFFAOYSA-N 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960004190 nomegestrol acetate Drugs 0.000 description 1
- IIVBFTNIGYRNQY-YQLZSBIMSA-N nomegestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 IIVBFTNIGYRNQY-YQLZSBIMSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1614179.8A GB201614179D0 (en) | 2016-08-19 | 2016-08-19 | Dosage regimen for the treatment of endometriosis |
| GB1614179.8 | 2016-08-19 | ||
| PCT/GB2017/052466 WO2018033759A1 (en) | 2016-08-19 | 2017-08-21 | Dosage regimen for the treatment of endometriosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019524846A JP2019524846A (ja) | 2019-09-05 |
| JP2019524846A5 true JP2019524846A5 (https=) | 2020-10-01 |
Family
ID=57045488
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019509559A Pending JP2019524846A (ja) | 2016-08-19 | 2017-08-21 | 子宮内膜症の治療のための投与レジメン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20190192485A1 (https=) |
| EP (1) | EP3500305A1 (https=) |
| JP (1) | JP2019524846A (https=) |
| CN (1) | CN109641057A (https=) |
| GB (1) | GB201614179D0 (https=) |
| WO (1) | WO2018033759A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12552754B1 (en) | 2025-06-11 | 2026-02-17 | ReproNovo SA | Leflutrozole compositions of matter and processes for preparation |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4749713A (en) | 1986-03-07 | 1988-06-07 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| TW210334B (https=) | 1990-12-12 | 1993-08-01 | Ciba Geigy Ag | |
| GB0302572D0 (en) * | 2003-02-05 | 2003-03-12 | Astrazeneca Ab | Method of treatment |
| US20070111975A1 (en) * | 2004-10-07 | 2007-05-17 | Duramed Pharmaceuticals, Inc. | Methods of Hormonal Treatment Utilizing Ascending-Dose Extended Cycle Regimens |
| DE102010003494A1 (de) * | 2010-03-31 | 2011-10-06 | Bayer Schering Pharma Aktiengesellschaft | Parenterales Abgabesystem, das Aromatasehemmer und Gestagene freisetzt, für die Behandlung von Endometriose |
| PT2753312T (pt) * | 2011-09-08 | 2017-02-03 | Mereo Biopharma 2 Ltd | Utilização de um inibidor da aromatase para o tratamento de hipogonadismo e doenças relacionadas |
-
2016
- 2016-08-19 GB GBGB1614179.8A patent/GB201614179D0/en not_active Ceased
-
2017
- 2017-08-21 US US16/325,872 patent/US20190192485A1/en not_active Abandoned
- 2017-08-21 CN CN201780050282.8A patent/CN109641057A/zh active Pending
- 2017-08-21 EP EP17757858.0A patent/EP3500305A1/en not_active Withdrawn
- 2017-08-21 JP JP2019509559A patent/JP2019524846A/ja active Pending
- 2017-08-21 WO PCT/GB2017/052466 patent/WO2018033759A1/en not_active Ceased
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