JPWO2022051198A5 - - Google Patents

Info

Publication number

JPWO2022051198A5

JPWO2022051198A5 JP2023514081A JP2023514081A JPWO2022051198A5 JP WO2022051198 A5 JPWO2022051198 A5 JP WO2022051198A5 JP 2023514081 A JP2023514081 A JP 2023514081A JP 2023514081 A JP2023514081 A JP 2023514081A JP WO2022051198 A5 JPWO2022051198 A5 JP WO2022051198A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

contraceptive

levonorgestrel

formula

pharmaceutical

Prior art date

2024-09-06

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

• Espacenet
• Global Dossier
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• 239000008194 pharmaceutical composition Substances 0.000 claims 21
• 239000003433 contraceptive agent Substances 0.000 claims 16
• 230000002254 contraceptive effect Effects 0.000 claims 16
• 150000001875 compounds Chemical class 0.000 claims 9
• 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 8
• 229960004400 levonorgestrel Drugs 0.000 claims 8
• PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 claims 8
• 230000002265 prevention Effects 0.000 claims 5
• 150000003839 salts Chemical class 0.000 claims 5
• 239000002202 Polyethylene glycol Substances 0.000 claims 4
• 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 4
• GPKLGCALNRZIDS-AYEDEZQKSA-N [(8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-3-oxo-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] butanoate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)CCC)[C@@]1(CC)CC2 GPKLGCALNRZIDS-AYEDEZQKSA-N 0.000 claims 4
• 229960002985 medroxyprogesterone acetate Drugs 0.000 claims 4
• 239000002245 particle Substances 0.000 claims 4
• 229920001223 polyethylene glycol Polymers 0.000 claims 4
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
• 229930195725 Mannitol Natural products 0.000 claims 2
• RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 2
• WWGTWFPUIPEHNX-UKNJCJGYSA-N [(8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-3-oxo-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] cyclobutanecarboxylate Chemical compound O([C@]1(CC[C@H]2[C@H]3[C@@H]([C@H]4CCC(=O)C=C4CC3)CC[C@@]21CC)C#C)C(=O)C1CCC1 WWGTWFPUIPEHNX-UKNJCJGYSA-N 0.000 claims 2
• 229960004976 desogestrel Drugs 0.000 claims 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 2
• 229960003309 dienogest Drugs 0.000 claims 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 2
• METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 claims 2
• 229960004845 drospirenone Drugs 0.000 claims 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 2
• 229960002941 etonogestrel Drugs 0.000 claims 2
• GCKFUYQCUCGESZ-BPIQYHPVSA-N etonogestrel Chemical compound O=C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 GCKFUYQCUCGESZ-BPIQYHPVSA-N 0.000 claims 2
• 229960005352 gestodene Drugs 0.000 claims 2
• SIGSPDASOTUPFS-XUDSTZEESA-N gestodene Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](C=C4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 SIGSPDASOTUPFS-XUDSTZEESA-N 0.000 claims 2
• 239000000594 mannitol Substances 0.000 claims 2
• 235000010355 mannitol Nutrition 0.000 claims 2
• 229960004616 medroxyprogesterone Drugs 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 229940053934 norethindrone Drugs 0.000 claims 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 2
• 229960000417 norgestimate Drugs 0.000 claims 2
• 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 claims 2
• 229920001983 poloxamer Polymers 0.000 claims 2
• 229960000502 poloxamer Drugs 0.000 claims 2
• 229940050929 polyethylene glycol 3350 Drugs 0.000 claims 2
• 229920000136 polysorbate Polymers 0.000 claims 2
• 229950008882 polysorbate Drugs 0.000 claims 2
• 230000035935 pregnancy Effects 0.000 claims 2
• 229960003387 progesterone Drugs 0.000 claims 2
• 239000000186 progesterone Substances 0.000 claims 2
• 229920002517 Poloxamer 338 Polymers 0.000 claims 1
• 229920001213 Polysorbate 20 Polymers 0.000 claims 1
• 239000002253 acid Substances 0.000 claims 1
• 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 1
• 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 1
• 229940068977 polysorbate 20 Drugs 0.000 claims 1
• 159000000000 sodium salts Chemical class 0.000 claims 1