NZ771719B2 - Selective estrogen receptor degraders - Google Patents
Selective estrogen receptor degraders Download PDFInfo
- Publication number
- NZ771719B2 NZ771719B2 NZ771719A NZ77171919A NZ771719B2 NZ 771719 B2 NZ771719 B2 NZ 771719B2 NZ 771719 A NZ771719 A NZ 771719A NZ 77171919 A NZ77171919 A NZ 77171919A NZ 771719 B2 NZ771719 B2 NZ 771719B2
- Authority
- NZ
- New Zealand
- Prior art keywords
- cancer
- compound
- acceptable salt
- pharmaceutically acceptable
- use according
- Prior art date
Links
- 229940125641 estrogen receptor degrader Drugs 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 238000000034 method Methods 0.000 claims abstract 3
- 150000001875 compounds Chemical class 0.000 claims 14
- 206010006187 Breast cancer Diseases 0.000 claims 6
- 208000026310 Breast neoplasm Diseases 0.000 claims 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 6
- 206010017758 gastric cancer Diseases 0.000 claims 6
- 201000011549 stomach cancer Diseases 0.000 claims 6
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 5
- 201000005202 lung cancer Diseases 0.000 claims 5
- 208000020816 lung neoplasm Diseases 0.000 claims 5
- -1 5-(4-{2-[3-(Fluoromethyl)azetidinyl]ethoxy}phenyl) (trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolinol Chemical compound 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Abstract
Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts, pharmaceutical compositions, uses, and methods of use thereof are provided.
Claims (21)
1. A compound of the formula or a pharmaceutically acceptable salt thereof.
2. The compound according to Claim 1, wherein the compound is
3. A pharmaceutical composition comprising a compound of Claim 1 or Claim 2, or a pharmaceutically acceptable salt thereof, in combination with one or more pharmaceutically 20 acceptable excipients, carriers, or diluents.
4. The pharmaceutical composition according to claim 3, further comprising one or more additional therapeutic agents.
5. A compound of Claim 1 or Claim 2, or a pharmaceutically acceptable salt thereof, for use in therapy. 25
6. A compound of Claim 1 or Claim 2, or a pharmaceutically acceptable salt thereof, for use in the treatment of breast cancer, ovarian cancer, endometrial cancer, prostate cancer, uterine cancer, gastric cancer, or lung cancer.
7. The compound, or a pharmaceutically acceptable salt thereof, for use according to Claim 6, wherein the compound is to be administered orally.
8. The compound for use according to Claim 7, or a pharmaceutically acceptable salt thereof, wherein the breast cancer is ER positive breast cancer. 5
9. The compound for use according to Claim 7, or a pharmaceutically acceptable salt thereof, wherein the gastric cancer is ER positive gastric cancer.
10. The compound for use according to Claim 7, or a pharmaceutically acceptable salt thereof, wherein the lung cancer is ER positive lung cancer.
11. Use of a compound according to Claim 1 or Claim 2, or a pharmaceutically 10 acceptable salt thereof, for the manufacture of a medicament for treating breast cancer, ovarian cancer, endometrial cancer, prostate cancer, uterine cancer, gastric cancer, or lung cancer.
12. The use according to claim 11, wherein the compound, or a pharmaceutically acceptable salt thereof, is to be administered orally. 15
13. The use according to Claim 11 or 12, wherein the breast cancer is ER positive breast cancer.
14. The use according to Claim 11 or 12, wherein the gastric cancer is ER positive gastric cancer.
15. The use according to Claim 11 or 12, wherein the lung cancer is ER positive lung 20 cancer.
16. A method for preparing 5-(4-{2-[3-(Fluoromethyl)azetidinyl]ethoxy}phenyl) (trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolinol, comprising cooling a solution of (4-{2-[3-(fluoromethyl)azetidinyl]ethoxy}phenyl){3-[2-fluoro(trifluoromethyl)phenyl]- 7-hydroxyquinolinyl}methanone in 1,4-dioxane to about 5 °C then adding lithium triethylborohydride.
17. The pharmaceutical composition according to claim 4, wherein the additional therapeutic agent is 5-(4-{2-[3-(fluoromethyl)azetidinyl]ethoxy}phenyl) 5 (trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolinol.
18. A compound according to any one of Claims 1, 2 and 5 to 10 substantially as herein described with reference to any example thereof.
19. A pharmaceutical composition according to any one of Claims 3, 4 and 17 substantially as herein described with reference to any example thereof. 10
20. Use according to any one of Claims 11 to 15 substantially as herein described with reference to any example thereof.
21. A method according to claim 16 substantially as herein described with reference to any example thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862697100P | 2018-07-12 | 2018-07-12 | |
| US201962825172P | 2019-03-28 | 2019-03-28 | |
| PCT/US2019/041342 WO2020014440A1 (en) | 2018-07-12 | 2019-07-11 | Selective estrogen receptor degraders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NZ771719A NZ771719A (en) | 2024-02-23 |
| NZ771719B2 true NZ771719B2 (en) | 2024-05-24 |
Family
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