JP2020522571A5 - - Google Patents
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- JP2020522571A5 JP2020522571A5 JP2020516959A JP2020516959A JP2020522571A5 JP 2020522571 A5 JP2020522571 A5 JP 2020522571A5 JP 2020516959 A JP2020516959 A JP 2020516959A JP 2020516959 A JP2020516959 A JP 2020516959A JP 2020522571 A5 JP2020522571 A5 JP 2020522571A5
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- JP
- Japan
- Prior art keywords
- item
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- pharmaceutical composition
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- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 49
- 238000002560 therapeutic procedure Methods 0.000 claims description 42
- 239000008194 pharmaceutical composition Substances 0.000 claims description 26
- 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 23
- 201000009273 Endometriosis Diseases 0.000 claims description 20
- 229960005309 estradiol Drugs 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- 239000000583 progesterone congener Substances 0.000 claims description 15
- 229940011871 estrogen Drugs 0.000 claims description 13
- 239000000262 estrogen Substances 0.000 claims description 13
- -1 2,3-difluoro-6-methoxybenzyloxy Chemical group 0.000 claims description 10
- 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 9
- 229960001652 norethindrone acetate Drugs 0.000 claims description 9
- 102000012673 Follicle Stimulating Hormone Human genes 0.000 claims description 8
- 108010079345 Follicle Stimulating Hormone Proteins 0.000 claims description 8
- 102000009151 Luteinizing Hormone Human genes 0.000 claims description 8
- 108010073521 Luteinizing Hormone Proteins 0.000 claims description 8
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical group C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 claims description 8
- 229940028334 follicle stimulating hormone Drugs 0.000 claims description 8
- 229940040129 luteinizing hormone Drugs 0.000 claims description 8
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 7
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- IIVUJUOJERNGQX-UHFFFAOYSA-N pyrimidine-5-carboxylic acid Chemical compound OC(=O)C1=CN=CN=C1 IIVUJUOJERNGQX-UHFFFAOYSA-N 0.000 claims 4
- 239000004381 Choline salt Substances 0.000 claims 2
- 235000019417 choline salt Nutrition 0.000 claims 2
- 229960003575 estradiol acetate Drugs 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 201
- 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 description 108
- 239000002474 gonadorelin antagonist Substances 0.000 description 102
- 125000000217 alkyl group Chemical group 0.000 description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 8
- 239000000126 substance Substances 0.000 description 8
- MJBWDEQAUQTVKK-IAGOWNOFSA-N aflatoxin M1 Chemical compound C=1([C@]2(O)C=CO[C@@H]2OC=1C=C(C1=2)OC)C=2OC(=O)C2=C1CCC2=O MJBWDEQAUQTVKK-IAGOWNOFSA-N 0.000 description 6
- 125000003277 amino group Chemical group 0.000 description 6
- 229960001231 choline Drugs 0.000 description 6
- 125000004122 cyclic group Chemical group 0.000 description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 description 6
- 210000002966 serum Anatomy 0.000 description 6
- 208000000450 Pelvic Pain Diseases 0.000 description 5
- 229960004616 medroxyprogesterone Drugs 0.000 description 5
- 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 5
- QLLWADSMMMNRDJ-AFRFTAIISA-N (2R)-N'-[5-[(Z)-2-(1H-benzimidazol-2-yl)-3-(2,5-difluorophenyl)-1-hydroxy-3-oxoprop-1-enyl]-2-fluorophenyl]sulfonyl-2-hydroxypropanimidamide Chemical compound C[C@@H](O)C(\N)=N\S(=O)(=O)c1cc(ccc1F)C(\O)=C(\C(=O)c1cc(F)ccc1F)c1nc2ccccc2[nH]1 QLLWADSMMMNRDJ-AFRFTAIISA-N 0.000 description 4
- 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 4
- 208000004483 Dyspareunia Diseases 0.000 description 4
- HEAUOKZIVMZVQL-VWLOTQADSA-N Elagolix Chemical compound COC1=CC=CC(C=2C(N(C[C@H](NCCCC(O)=O)C=3C=CC=CC=3)C(=O)N(CC=3C(=CC=CC=3F)C(F)(F)F)C=2C)=O)=C1F HEAUOKZIVMZVQL-VWLOTQADSA-N 0.000 description 4
- 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 4
- 125000000304 alkynyl group Chemical group 0.000 description 4
- 125000004093 cyano group Chemical group *C#N 0.000 description 4
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 description 4
- 229960004845 drospirenone Drugs 0.000 description 4
- 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 4
- 229950004823 elagolix Drugs 0.000 description 4
- 229960002568 ethinylestradiol Drugs 0.000 description 4
- 125000005843 halogen group Chemical group 0.000 description 4
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 230000000977 initiatory effect Effects 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
- 239000000186 progesterone Substances 0.000 description 4
- 229960003387 progesterone Drugs 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 3
- 229940035811 conjugated estrogen Drugs 0.000 description 3
- 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 3
- 150000002148 esters Chemical class 0.000 description 3
- 229960000417 norgestimate Drugs 0.000 description 3
- 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 3
- PZGSYNNVPNLHQG-SANMLTNESA-N (2s)-n-[[3-chloro-5-(trifluoromethyl)pyridin-2-yl]methyl]-2-cyclopropyl-1-(4-fluorophenyl)sulfonyl-1',1'-dioxospiro[2h-indole-3,4'-thiane]-5-carboxamide Chemical compound C1=CC(F)=CC=C1S(=O)(=O)N1C2=CC=C(C(=O)NCC=3C(=CC(=CN=3)C(F)(F)F)Cl)C=C2C2(CCS(=O)(=O)CC2)[C@@H]1C1CC1 PZGSYNNVPNLHQG-SANMLTNESA-N 0.000 description 2
- 208000005171 Dysmenorrhea Diseases 0.000 description 2
- 206010013935 Dysmenorrhoea Diseases 0.000 description 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 2
- 125000003342 alkenyl group Chemical group 0.000 description 2
- 125000002947 alkylene group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 210000000988 bone and bone Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 230000013872 defecation Effects 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000009977 dual effect Effects 0.000 description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 238000000691 measurement method Methods 0.000 description 2
- 230000002175 menstrual effect Effects 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 125000002950 monocyclic group Chemical group 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 125000003107 substituted aryl group Chemical group 0.000 description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 2
- 125000003831 tetrazolyl group Chemical group 0.000 description 2
- 210000000689 upper leg Anatomy 0.000 description 2
- 238000004922 13C solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 1
- 238000004319 19F solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 1
- 208000008035 Back Pain Diseases 0.000 description 1
- BMAAMIIYNNPHAB-UHFFFAOYSA-N COc(cc1)c(COc(c(OC)c2)cc(N(C(c3c(C(O)=O)[s]cc3N3)=O)C3=O)c2F)c(F)c1F Chemical compound COc(cc1)c(COc(c(OC)c2)cc(N(C(c3c(C(O)=O)[s]cc3N3)=O)C3=O)c2F)c(F)c1F BMAAMIIYNNPHAB-UHFFFAOYSA-N 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 1
- 230000001755 vocal effect Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023084336A JP7657855B2 (ja) | 2017-06-05 | 2023-05-23 | 子宮内膜症の治療のための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 |
|---|---|---|---|
| US201762515268P | 2017-06-05 | 2017-06-05 | |
| US62/515,268 | 2017-06-05 | ||
| PCT/EP2018/064768 WO2018224498A1 (en) | 2017-06-05 | 2018-06-05 | Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023084336A Division JP7657855B2 (ja) | 2017-06-05 | 2023-05-23 | 子宮内膜症の治療のための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 |
|---|---|
| JP2020522571A JP2020522571A (ja) | 2020-07-30 |
| JP2020522571A5 true JP2020522571A5 (cg-RX-API-DMAC7.html) | 2021-07-26 |
| JP7348171B2 JP7348171B2 (ja) | 2023-09-20 |
Family
ID=62620835
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020516959A Active JP7348171B2 (ja) | 2017-06-05 | 2018-06-05 | 子宮内膜症の治療のためのゴナドトロピン放出ホルモンアンタゴニスト投与計画 |
| JP2023084336A Active JP7657855B2 (ja) | 2017-06-05 | 2023-05-23 | 子宮内膜症の治療のための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 |
|---|---|---|---|
| JP2023084336A Active JP7657855B2 (ja) | 2017-06-05 | 2023-05-23 | 子宮内膜症の治療のための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 (12)
| Country | Link |
|---|---|
| US (2) | US11980621B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3634418A1 (cg-RX-API-DMAC7.html) |
| JP (2) | JP7348171B2 (cg-RX-API-DMAC7.html) |
| KR (2) | KR20250117836A (cg-RX-API-DMAC7.html) |
| CN (1) | CN110996956A (cg-RX-API-DMAC7.html) |
| AU (2) | AU2018280742B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA3066190A1 (cg-RX-API-DMAC7.html) |
| EA (1) | EA201992612A1 (cg-RX-API-DMAC7.html) |
| MA (1) | MA49256A (cg-RX-API-DMAC7.html) |
| MX (1) | MX2019014483A (cg-RX-API-DMAC7.html) |
| SG (1) | SG11201911598WA (cg-RX-API-DMAC7.html) |
| WO (1) | WO2018224498A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3518933T4 (da) | 2016-09-30 | 2025-04-22 | Takeda Pharmaceuticals Co | Fremgangsmåder til behandling af uterusfibromer og endometriose |
| MX2019014482A (es) | 2017-06-05 | 2020-08-17 | ObsEva SA | Régimenes de dosificación de antagonistas de hormona liberadora de gonadotropina para tratar miomas uterinos y reducir la menstruación. |
| KR20250117836A (ko) | 2017-06-05 | 2025-08-05 | 깃세이 야쿠힌 고교 가부시키가이샤 | 자궁내막증의 치료를 위한 고나도트로핀 방출 호르몬 길항제 투약 요법 |
| EP3873465B1 (en) | 2018-10-29 | 2025-01-15 | Kissei Pharmaceutical Co., Ltd. | Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis |
| US20220305017A1 (en) * | 2019-08-08 | 2022-09-29 | ObsEva S.A. | Compositions and methods for the treatment of estrogen-dependent disorders |
| CN113384581B (zh) * | 2020-03-12 | 2023-11-14 | 成都倍特药业股份有限公司 | 一种包含促性腺激素释放激素拮抗剂的药物组合物 |
| WO2022101303A1 (en) * | 2020-11-11 | 2022-05-19 | Myovant Sciences Gmbh | Methods of administering relugolix |
| TWI796144B (zh) * | 2021-02-23 | 2023-03-11 | 大陸商南京明德新藥研發有限公司 | 噻吩並嘧啶二酮類化合物及其應用 |
| 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 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5342760A (en) | 1992-06-10 | 1994-08-30 | Abbott Laboratories | Determination of estradiol by competitive immunoassay |
| US5663054A (en) | 1995-03-03 | 1997-09-02 | Abbott Laboratories | Determination of steroids by competitive immunoassay |
| US7109171B2 (en) | 2000-02-28 | 2006-09-19 | Praecis Pharmaceuticals Inc. | Methods for treating FSH related conditions with GnRH antagonists |
| EP1300398B1 (en) | 2000-07-05 | 2006-04-05 | Astellas Pharma Inc. | Propane-1,3-dione derivatives |
| EP1591446B1 (en) | 2003-01-29 | 2013-03-06 | Takeda Pharmaceutical Company Limited | Thienopyrimidine compounds and use thereof |
| ATE407679T1 (de) | 2003-07-07 | 2008-09-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| BRPI0609625A2 (pt) | 2005-03-31 | 2010-04-20 | Astellas Pharma Inc | derivados de propano-1,3-diona ou sal destes |
| BRPI0617436B8 (pt) | 2005-10-19 | 2021-05-25 | Kissei Pharmaceutical | derivado heterocíclico fundido, composição farmacêutica compreendendo o mesmo e usos do dito derivado na prevenção ou tratamento de doença dependente de hormônio sexual e na regulação da reprodução, contracepção ou indução de ovulação |
| US8765948B2 (en) | 2007-11-07 | 2014-07-01 | Neurocrine Biosciences, Inc. | Processes for the preparation of uracil derivatives |
| BR112012020110B1 (pt) | 2010-02-10 | 2021-06-08 | Kissei Pharmaceutical Co., Ltd. | composto derivado heterocíclico fusionado, composição farmacêutica que compreende o mesmo e uso terapêutico do dito composto |
| HK1199878A1 (en) | 2012-01-16 | 2015-07-24 | Bayer Intellectual Property Gmbh | Spiroindoline derivatives as gonadotropin-releasing hormone receptor antagonists |
| EP2817621A4 (en) | 2012-02-21 | 2016-02-24 | Univ Northwestern | PROOF OF ANTI-MÜLLER-HORMON IN FULL BLOOD |
| CN104603114B (zh) | 2012-09-07 | 2017-06-20 | 安斯泰来制药株式会社 | 磺酰脒化合物的制造方法 |
| 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 |
| LT3415517T (lt) | 2012-09-28 | 2022-06-10 | Takeda Pharmaceutical Company Limited | Kristalinė 1-(4-(1-(2,6-difluorbenzil)-5-dimetilaminometil-3-(6-metoksipiridazin-3-il)-2,4-diokso-1,2,3,4- tetrahidrotieno(2,3-d)pirimidin-6-il)fenil)-3-metoksikarbamido forma |
| EP3384930A1 (en) | 2013-03-15 | 2018-10-10 | AbbVie Inc. | Compositions for use in treating heavy menstrual bleeding |
| AR095785A1 (es) | 2013-04-09 | 2015-11-11 | Bayer Pharma AG | Derivados de espiroindolina y composiciones farmacéutica de los mismos |
| WO2017040841A1 (en) | 2015-09-01 | 2017-03-09 | Abbvie Inc. | Methods of administering elagolix |
| CA3025760A1 (en) | 2016-08-08 | 2018-02-15 | Kissei Pharmaceutical Co., Ltd. | Usage and dosage of therapeutic agents for endometriosis |
| DK3518933T4 (da) | 2016-09-30 | 2025-04-22 | Takeda Pharmaceuticals Co | Fremgangsmåder til behandling af uterusfibromer og endometriose |
| KR20250117836A (ko) | 2017-06-05 | 2025-08-05 | 깃세이 야쿠힌 고교 가부시키가이샤 | 자궁내막증의 치료를 위한 고나도트로핀 방출 호르몬 길항제 투약 요법 |
| MX2019014482A (es) | 2017-06-05 | 2020-08-17 | ObsEva SA | Régimenes de dosificación de antagonistas de hormona liberadora de gonadotropina para tratar miomas uterinos y reducir la menstruación. |
| EP3876943A2 (en) | 2018-11-07 | 2021-09-15 | ObsEva S.A. | Compositions and methods for the treatment of estrogen-dependent disorders |
-
2018
- 2018-06-05 KR KR1020257024754A patent/KR20250117836A/ko active Pending
- 2018-06-05 KR KR1020197038977A patent/KR102839190B1/ko active Active
- 2018-06-05 EP EP18731378.8A patent/EP3634418A1/en active Pending
- 2018-06-05 US US16/619,776 patent/US11980621B2/en active Active
- 2018-06-05 JP JP2020516959A patent/JP7348171B2/ja active Active
- 2018-06-05 CN CN201880050650.3A patent/CN110996956A/zh active Pending
- 2018-06-05 WO PCT/EP2018/064768 patent/WO2018224498A1/en not_active Ceased
- 2018-06-05 AU AU2018280742A patent/AU2018280742B2/en active Active
- 2018-06-05 MX MX2019014483A patent/MX2019014483A/es unknown
- 2018-06-05 MA MA049256A patent/MA49256A/fr unknown
- 2018-06-05 CA CA3066190A patent/CA3066190A1/en active Pending
- 2018-06-05 EA EA201992612A patent/EA201992612A1/ru unknown
- 2018-06-05 SG SG11201911598WA patent/SG11201911598WA/en unknown
-
2023
- 2023-05-23 JP JP2023084336A patent/JP7657855B2/ja active Active
-
2024
- 2024-03-14 AU AU2024201701A patent/AU2024201701B2/en active Active
- 2024-04-12 US US18/634,241 patent/US20240293414A1/en active Pending
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