IP Library Granted Patent US 11,364,241
Granted Patent B2
US 11,364,241 · App. 17/000,271 · Granted Jun 21, 2022

Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)

Inventors: Bing Wang (San Jose, CA); Daniel Chu (Santa Clara, CA)
Assignee: MEDIVATION TECHNOLOGIES LLC
A61K31/5025A61K31/282A61K31/4745A61K31/495A61K31/5377A61K33/243A61N5/10C07D471/06A61N2005/1098
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Quick Facts
Patent No.
US 11,364,241
App. No.
17/000,271
Granted
Jun 21, 2022
Kind
B2
Abstract

A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

Claims (16)

1. A method of treating lung cancer in a subject, comprising administering to the subject a therapeutically effective amount of 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one, or a pharmaceutically acceptable salt or solvate thereof.

2. The method of claim 1 , wherein said administration is in combination with ionizing radiation, one or more chemotherapeutic agents, or a combination thereof.

3. The method of claim 2 , wherein the compound is used in combination with one or more chemotherapeutic agents, wherein each chemotherapeutic agent is independently methyl methanesulfonate, temozolomide, dacarbazine (DTIC), a topoisomerase-1 inhibitor, Topotecan, Irinotecan, Rubitecan, Exatecan, Lurtotecan, Gimetecan, Diflomotecan, a homocamptothecin, Doxorubicin, a platinum based antineoplastic agent, a 7-substituted non-silatecan, a 7-silyl camptothecin, paclitaxel, cetuximab, daunorubicin, methotrexate, a hormone, an antiestrogen, an antiandrogen, a gonadotropin releasing hormone analog, an interferon, alpha interferon, a tyrosine kinase inhibitor, gefitinib, imatinib, gemtuzumab, or BNP 1350.

4. The method of claim 2 , wherein the compound is used in combination with one or more chemotherapeutic agents, wherein each chemotherapeutic agent is independently irinotecan, cisplatin, carboplatin, paclitaxel, or temozolomide.

5. The method of claim 1 , wherein the subject is a human.

6. The method of claim 2 , wherein the subject is a human.

7. The method of claim 3 , wherein the subject is a human.

8. The method of claim 4 , wherein the subject is a human.

9. A method of treating lung cancer in a subject, comprising administering to the subject a therapeutically effective amount of (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one, or a pharmaceutically acceptable salt or solvate thereof.

10. The method of claim 9 , wherein said administration is in combination with ionizing radiation, one or more chemotherapeutic agents, or a combination thereof.

11. The method of claim 10 , wherein the compound is used in combination with one or more chemotherapeutic agents, wherein each chemotherapeutic agent is independently methyl methanesulfonate, temozolomide, dacarbazine (DTIC), a topoisomerase-1 inhibitor, Topotecan, Irinotecan, Rubitecan, Exatecan, Lurtotecan, Gimetecan, Diflomotecan, a homocamptothecin, Doxorubicin, a platinum based antineoplastic agent, a 7-substituted non-silatecan, a 7-silyl camptothecin, paclitaxel, cetuximab, daunorubicin, methotrexate, a hormone, an antiestrogen, an antiandrogen, a gonadotropin releasing hormone analog, an interferon, alpha interferon, a tyrosine kinase inhibitor, gefitinib, imatinib, gemtuzumab, or BNP 1350.

12. The method of claim 10 , wherein the compound is used in combination with one or more chemotherapeutic agents, wherein each chemotherapeutic agent is independently irinotecan, cisplatin, carboplatin, paclitaxel, or temozolomide.

13. The method of claim 9 , wherein the subject is a human.

14. The method of claim 10 , wherein the subject is a human.

15. The method of claim 11 , wherein the subject is a human.

16. The method of claim 12 , wherein the subject is a human.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: MEDIVATION TECHNOLOGIES LLC
To: MEDIVATION TECHNOLOGIES LLC
Reel/Frame 063117/0642 →