JP2020522525A5 - - Google Patents
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- Publication number
- JP2020522525A5 JP2020522525A5 JP2019566909A JP2019566909A JP2020522525A5 JP 2020522525 A5 JP2020522525 A5 JP 2020522525A5 JP 2019566909 A JP2019566909 A JP 2019566909A JP 2019566909 A JP2019566909 A JP 2019566909A JP 2020522525 A5 JP2020522525 A5 JP 2020522525A5
- Authority
- JP
- Japan
- Prior art keywords
- human patient
- item
- pharmaceutical composition
- compound
- administered
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 146
- 229960005309 estradiol Drugs 0.000 claims description 51
- 239000008194 pharmaceutical composition Substances 0.000 claims description 49
- 238000002560 therapeutic procedure Methods 0.000 claims description 49
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class 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 48
- 150000003839 salts Chemical class 0.000 claims description 32
- 239000004381 Choline salt Substances 0.000 claims description 29
- 235000019417 choline salt Nutrition 0.000 claims description 29
- 206010046798 Uterine leiomyoma Diseases 0.000 claims description 18
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 17
- 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 17
- 229960001652 norethindrone acetate Drugs 0.000 claims description 17
- 239000000583 progesterone congener Substances 0.000 claims description 16
- 201000010260 leiomyoma Diseases 0.000 claims description 15
- 229940011871 estrogen Drugs 0.000 claims description 12
- 239000000262 estrogen Substances 0.000 claims description 12
- 230000002175 menstrual effect Effects 0.000 claims description 9
- -1 2,3-difluoro-6-methoxybenzyloxy Chemical group 0.000 claims 8
- IIVUJUOJERNGQX-UHFFFAOYSA-N pyrimidine-5-carboxylic acid Chemical compound OC(=O)C1=CN=CN=C1 IIVUJUOJERNGQX-UHFFFAOYSA-N 0.000 claims 8
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical group C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 claims 5
- 239000008280 blood Substances 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 229960003575 estradiol acetate Drugs 0.000 claims 3
- 239000002552 dosage form Substances 0.000 claims 2
- 238000000034 method Methods 0.000 description 251
- 210000002966 serum Anatomy 0.000 description 32
- 201000000736 Amenorrhea Diseases 0.000 description 24
- 206010001928 Amenorrhoea Diseases 0.000 description 24
- 231100000540 amenorrhea Toxicity 0.000 description 24
- 150000003248 quinolines Chemical class 0.000 description 24
- 229960003387 progesterone Drugs 0.000 description 16
- 239000000186 progesterone Substances 0.000 description 16
- 239000000126 substance Substances 0.000 description 14
- 229940035811 conjugated estrogen Drugs 0.000 description 10
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 description 10
- 229960004616 medroxyprogesterone Drugs 0.000 description 10
- FRQMUZJSZHZSGN-HBNHAYAOSA-N medroxyprogesterone Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FRQMUZJSZHZSGN-HBNHAYAOSA-N 0.000 description 10
- ZAHDXEIQWWLQQL-IHRRRGAJSA-N Deoxypyridinoline Chemical compound OC(=O)[C@@H](N)CCCC[N+]1=CC(O)=C(C[C@H](N)C([O-])=O)C(CC[C@H](N)C(O)=O)=C1 ZAHDXEIQWWLQQL-IHRRRGAJSA-N 0.000 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 description 8
- 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 description 8
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 description 8
- 229960004845 drospirenone Drugs 0.000 description 8
- 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 description 8
- 229960002568 ethinylestradiol Drugs 0.000 description 8
- 230000000740 bleeding effect Effects 0.000 description 6
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 description 6
- 229960000417 norgestimate Drugs 0.000 description 6
- 238000004319 19F solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 4
- 208000008035 Back Pain Diseases 0.000 description 4
- 208000015710 Iron-Deficiency Anemia Diseases 0.000 description 4
- 208000000450 Pelvic Pain Diseases 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 229940053934 norethindrone Drugs 0.000 description 4
- 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 description 4
- 238000000634 powder X-ray diffraction Methods 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 210000000689 upper leg Anatomy 0.000 description 4
- 238000004922 13C solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 3
- 238000005481 NMR spectroscopy Methods 0.000 description 2
- 210000000988 bone and bone Anatomy 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 1
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 1
- 0 CCc1c(*)ccc(OC)c1COc(cc(*(C(c1c(C(*)=O)[n]cc1*1)O)C1=O)c(*)c1)c1OC Chemical compound CCc1c(*)ccc(OC)c1COc(cc(*(C(c1c(C(*)=O)[n]cc1*1)O)C1=O)c(*)c1)c1OC 0.000 description 1
- 102000012422 Collagen Type I Human genes 0.000 description 1
- 108010022452 Collagen Type I Proteins 0.000 description 1
- 108010050808 Procollagen Proteins 0.000 description 1
- 210000004899 c-terminal region Anatomy 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023043718A JP7485815B2 (ja) | 2017-06-05 | 2023-03-20 | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762515232P | 2017-06-05 | 2017-06-05 | |
| US62/515,232 | 2017-06-05 | ||
| PCT/EP2018/064767 WO2018224497A1 (en) | 2017-06-05 | 2018-06-05 | Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023043718A Division JP7485815B2 (ja) | 2017-06-05 | 2023-03-20 | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020522525A JP2020522525A (ja) | 2020-07-30 |
| JP2020522525A5 true JP2020522525A5 (https=) | 2021-07-26 |
| JP7292566B2 JP7292566B2 (ja) | 2023-06-19 |
Family
ID=62636157
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019566909A Active JP7292566B2 (ja) | 2017-06-05 | 2018-06-05 | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
| JP2023043718A Active JP7485815B2 (ja) | 2017-06-05 | 2023-03-20 | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023043718A Active JP7485815B2 (ja) | 2017-06-05 | 2023-03-20 | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US11759464B2 (https=) |
| EP (2) | EP3634419B1 (https=) |
| JP (2) | JP7292566B2 (https=) |
| KR (1) | KR102884301B1 (https=) |
| CN (1) | CN110996957A (https=) |
| AU (2) | AU2018280741B2 (https=) |
| CA (1) | CA3066188A1 (https=) |
| DK (1) | DK3634419T3 (https=) |
| EA (1) | EA201992812A1 (https=) |
| ES (1) | ES3018358T3 (https=) |
| FI (1) | FI3634419T3 (https=) |
| HR (1) | HRP20250390T1 (https=) |
| HU (1) | HUE070907T2 (https=) |
| MX (2) | MX2019014482A (https=) |
| PL (1) | PL3634419T3 (https=) |
| PT (1) | PT3634419T (https=) |
| SG (1) | SG11201911599XA (https=) |
| WO (1) | WO2018224497A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10881659B2 (en) | 2013-03-15 | 2021-01-05 | Abbvie Inc. | Methods of treating heavy menstrual bleeding |
| KR102884301B1 (ko) | 2017-06-05 | 2025-11-11 | 깃세이 야쿠힌 고교 가부시키가이샤 | 자궁 근종을 치료하고 월경혈량을 감소시키기 위한 고나도트로핀 방출 호르몬 길항제 투약 요법 |
| EA201992612A1 (ru) | 2017-06-05 | 2020-05-20 | Обсева С.А. | Схемы применения антагониста гонадотропин-высвобождающего гормона для лечения эндометриоза |
| CN112261942A (zh) | 2018-04-19 | 2021-01-22 | 艾伯维公司 | 治疗重度月经出血的方法 |
| JP2021532160A (ja) * | 2018-08-01 | 2021-11-25 | アッヴィ・インコーポレイテッド | エラゴリックスに関する投与計画 |
| CA3117092A1 (en) | 2018-10-29 | 2020-05-07 | ObsEva S.A. | Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis |
| SG11202104053TA (en) * | 2018-11-07 | 2021-05-28 | ObsEva SA | Compositions and methods for the treatment of estrogen-dependent disorders |
| CN114466665A (zh) * | 2019-08-08 | 2022-05-10 | 奥布赛瓦股份公司 | 用于治疗雌激素依赖性病症的组合物和方法 |
| AU2020325721A1 (en) * | 2019-08-08 | 2022-03-03 | ObsEva S.A. | GnRH antagonists for the treatment of estrogen-dependent disorders |
| KR20210155350A (ko) | 2020-06-15 | 2021-12-22 | 한상왕 | 녹차 추출물 및 비타민 d3를 유효성분으로 포함하는 자궁근종 개선용 조성물 |
| CN115232144B (zh) * | 2021-04-22 | 2024-04-02 | 长春金赛药业有限责任公司 | 含氮稠环类衍生物、药物组合物及其制备方法和应用 |
| KR102738115B1 (ko) | 2024-03-25 | 2024-12-05 | 한상왕 | 자궁근종 예방, 개선 또는 치료용 약학 조성물 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7109171B2 (en) | 2000-02-28 | 2006-09-19 | Praecis Pharmaceuticals Inc. | Methods for treating FSH related conditions with GnRH antagonists |
| KR101384132B1 (ko) | 2005-10-19 | 2014-04-10 | 깃세이 야쿠힌 고교 가부시키가이샤 | 축합 복소환 유도체, 그것을 함유하는 의약 조성물 및 그의약 용도 |
| SG183243A1 (en) * | 2010-02-10 | 2012-09-27 | Kissei Pharmaceutical | Salt of fused heterocyclic derivative and crystal thereof |
| WO2014042176A1 (ja) | 2012-09-14 | 2014-03-20 | キッセイ薬品工業株式会社 | 縮合複素環誘導体の製造方法およびその製造中間体 |
| US10881659B2 (en) * | 2013-03-15 | 2021-01-05 | Abbvie Inc. | Methods of treating heavy menstrual bleeding |
| TWI746613B (zh) | 2016-08-08 | 2021-11-21 | 日商橘生藥品工業股份有限公司 | 子宮內膜病症治療劑之用法及用量 |
| ES2912929T5 (en) | 2016-09-30 | 2025-05-09 | Sumitomo Pharma Switzerland Gmbh | Methods of treating uterine fibroids and endometriosis |
| KR102884301B1 (ko) | 2017-06-05 | 2025-11-11 | 깃세이 야쿠힌 고교 가부시키가이샤 | 자궁 근종을 치료하고 월경혈량을 감소시키기 위한 고나도트로핀 방출 호르몬 길항제 투약 요법 |
| EA201992612A1 (ru) | 2017-06-05 | 2020-05-20 | Обсева С.А. | Схемы применения антагониста гонадотропин-высвобождающего гормона для лечения эндометриоза |
| SG11202104053TA (en) | 2018-11-07 | 2021-05-28 | ObsEva SA | Compositions and methods for the treatment of estrogen-dependent disorders |
-
2018
- 2018-06-05 KR KR1020197038980A patent/KR102884301B1/ko active Active
- 2018-06-05 EP EP18731976.9A patent/EP3634419B1/en active Active
- 2018-06-05 PT PT187319769T patent/PT3634419T/pt unknown
- 2018-06-05 AU AU2018280741A patent/AU2018280741B2/en active Active
- 2018-06-05 EP EP24221894.9A patent/EP4509173A3/en active Pending
- 2018-06-05 ES ES18731976T patent/ES3018358T3/es active Active
- 2018-06-05 CN CN201880050807.2A patent/CN110996957A/zh active Pending
- 2018-06-05 JP JP2019566909A patent/JP7292566B2/ja active Active
- 2018-06-05 DK DK18731976.9T patent/DK3634419T3/da active
- 2018-06-05 HR HRP20250390TT patent/HRP20250390T1/hr unknown
- 2018-06-05 FI FIEP18731976.9T patent/FI3634419T3/fi active
- 2018-06-05 HU HUE18731976A patent/HUE070907T2/hu unknown
- 2018-06-05 MX MX2019014482A patent/MX2019014482A/es unknown
- 2018-06-05 CA CA3066188A patent/CA3066188A1/en active Pending
- 2018-06-05 US US16/619,702 patent/US11759464B2/en active Active
- 2018-06-05 WO PCT/EP2018/064767 patent/WO2018224497A1/en not_active Ceased
- 2018-06-05 EA EA201992812A patent/EA201992812A1/ru unknown
- 2018-06-05 MX MX2023013582A patent/MX2023013582A/es unknown
- 2018-06-05 PL PL18731976.9T patent/PL3634419T3/pl unknown
- 2018-06-05 SG SG11201911599XA patent/SG11201911599XA/en unknown
-
2023
- 2023-03-20 JP JP2023043718A patent/JP7485815B2/ja active Active
- 2023-09-11 US US18/244,773 patent/US20240000785A1/en active Pending
-
2024
- 2024-03-14 AU AU2024201694A patent/AU2024201694A1/en not_active Abandoned
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