Prodrugs of the selective progesterone receptor modulator (sprm) (11.beta.,17.beta.)-17-hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one
US-2019367555-A1 · Dec 5, 2019 · US
Prodrugs of the selective progesterone receptor modulator (SPRM) (11.beta.,17.beta.)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl] -17-(pentafluoroethyl)estra-4,9-dien-3-one
US10894805B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10894805-B2 |
| Application number | US-201716082025-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 1, 2017 |
| Priority date | Mar 4, 2016 |
| Publication date | Jan 19, 2021 |
| Grant date | Jan 19, 2021 |
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Abstract
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This invention concerns Selective Progesterone Receptor Modulators (SPRM) in a prodrug form as well as their application in therapy. (3α, 11β,17β)-1 1-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-diene-3,17-diol (Compound 1) is one of the invention prodrugs.
First claim
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The invention claimed is: 1. A prodrug of a Selective Progesterone Receptor Modulator (SPRM), wherein the SPRM is (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one and wherein the prodrug is (3α,11β, 17β)-11-[4-(methyl sulfonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-diene-3,17-diol (Compound 1) or a pharmaceutically acceptable salt thereof. 2. A pharmaceutical composition comprising the prodrug according to claim 1 , optionally admixed with a pharmaceutically acceptable excipient or carrier. 3. A method for fertility control and emergency contraception comprising administering to a patient an effective amount of a prodrug according to claim 1 . 4. A method for the treatment of a gynaecological disease, or a symptom thereof, comprising administering to a patient an effective amount of a prodrug according to claim 1 . 5. The method according to claim 4 wherein the gynaecological disease is selected from the group consisting of Uterine Fibroids, Endometriosis, and symptoms thereof. 6. A method for producing the prodrug according to claim 1 , which method comprises reacting (11β,17β)-17-hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 2) in the presence of a reducing agent. 7. The method according to claim 6 wherein the prodrug is produced by a reaction that is catalyzed by an isolated Aldo-Keto Reductase (AKR) enzyme. 8. A pharmaceutical composition comprising an isolated Cytochrome P450, a prodrug according to claim 1 , and a pharmaceutically acceptable excipient or carrier. 9. An ex vivo method for activating the prodrug according to claim 1 , which method comprises contacting the prodrug with an activating agent, wherein the activating agent is an isolated Cytochrome P450. 10. The method according to claim 6 wherein the reducing agent is sodium borohydride. 11. The pharmaceutical composition according to claim 8 , wherein the isolated Cytochrome P450 is CYP3A4. 12. The method of claim 9 , wherein the isolated cytochrome P450 is CYP3A4.
Assignees
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Classifications
- C07J31/006Primary
not covered by C07J31/003 · CPC title
Antigestagens · CPC title
Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Feminine contraceptives · CPC title
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Frequently asked questions
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- What does patent US10894805B2 cover?
- This invention concerns Selective Progesterone Receptor Modulators (SPRM) in a prodrug form as well as their application in therapy. (3α, 11β,17β)-1 1-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-diene-3,17-diol (Compound 1) is one of the invention prodrugs.
- Who is the assignee on this patent?
- Bayer Pharma AG
- What technology area does this patent fall under?
- Primary CPC classification C07J31/006. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jan 19 2021 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 6 related publications on this page (citations in our corpus or others sharing the same primary CPC).