MCL-1 inhibitors and methods of use thereof
US-9840518-B2 · Dec 12, 2017 · US
MCL-1 inhibitors and methods of use thereof
US10889594B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10889594-B2 |
| Application number | US-201816223538-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 18, 2018 |
| Priority date | Apr 22, 2016 |
| Publication date | Jan 12, 2021 |
| Grant date | Jan 12, 2021 |
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- Title
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- Abstract
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- Assignees and inventors
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- First independent claim
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- CPC / IPC classifications
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Abstract
Official abstract text for this publication.
Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 4,7 .0 11,15 ,0 16,21 .0 20,24 .0 30,35 ]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 4,7 .0 11,15 .0 16,21 .0 20,24 .0 30,35 ]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound which is Form A (R a )-17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 4,7 .0 11,15 .0 16,21 .0 20,24 .0 30,35 ]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid monohydrate. 2. The compound of claim 1 , wherein said compound has an XRPD pattern comprising at least one peak expressed as 2θ (±0.2°) at about 7.0°. 3. The compound of claim 1 , wherein said compound has an XRPD pattern comprising at least one peak expressed as 2θ (±0.2°) at about 8.4°. 4. The compound of claim 1 , wherein said compound has an XRPD pattern comprising at least one peak expressed as 2θ (±0.2°) at about 12.5°. 5. The compound of claim 1 , wherein said compound has an XRPD pattern comprising at least one peak expressed as 2θ (±0.2°) selected from about 7.0°, 8.4° and 12.5°. 6. The compound of claim 1 , wherein said compound has an XRPD pattern comprising at least one peak expressed as 2θ (±0.2°) selected from about 5.4°, 7.0°, 8.4°, 10.7°, 12.5°, 13.1°, 14.4°, 15.1°, 15.6°, 17.1° and 18.2°. 7. The compound of claim 1 , wherein the compound has a DSC thermogram comprising an endotherm with a desolvation onset at about 121° C. and a peak at about 152° C. 8. The compound of claim 1 , wherein the compound has a DSC thermogram comprising an endotherm with a melting/decomposition onset at about 181° C. and a peak at about 194° C. 9. The compound of claim 1 , wherein the compound has a TGA thermogram exhibiting a mass loss of about 4.0% upon heating from about 25° C. to about 160° C. 10. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier, excipient or diluent.
Assignees
Inventors
Classifications
- C07D515/22Primary
in which the condensed system contains four or more hetero rings · CPC title
- C07D497/22Primary
in which the condensed system contains four or more hetero rings · CPC title
having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins · CPC title
Antineoplastic agents · CPC title
specific for leukemia · CPC title
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- What does patent US10889594B2 cover?
- Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 4,7 .0 11,15 ,0 16,21 .0 20,24 .0 30,35 ]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical composi…
- Who is the assignee on this patent?
- Astrazeneca Ab
- What technology area does this patent fall under?
- Primary CPC classification C07D515/22. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jan 12 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 2 related publications on this page (citations in our corpus or others sharing the same primary CPC).