IP Library Granted Patent US 10,780,088
Granted Patent B2
US 10,780,088 · App. 16/714,474 · Granted Sep 22, 2020

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

Inventors: Bing Wang (San Jose, CA); Daniel Chu (Santa Clara, CA)
Assignee: MEDIVATION TECHNOLOGIES LLC
A61K31/5025
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Quick Facts
Patent No.
US 10,780,088
App. No.
16/714,474
Granted
Sep 22, 2020
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 prostate 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 prostate 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.

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 10 , 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 (5)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: MEDIVATION TECHNOLOGIES LLC
To: MEDIVATION TECHNOLOGIES LLC
Reel/Frame 063117/0642 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2020
From: WANG, BING; CHU, DANIEL
To: BIOMARIN PHARMACEUTICAL INC.
Reel/Frame 052714/0863 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2020
From: BIOMARIN PHARMACEUTICAL INC.
To: MEDIVATION, INC.
Reel/Frame 052714/0883 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2020
From: MEDIVATION, INC.
To: MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 052714/0908 →
CERTIFICATES OF FORMATION AND CONVERSION Recorded May 20, 2020
From: MEDIVATION TECHNOLOGIES, INC.
To: MEDIVATION TECHNOLOGIES LLC
Reel/Frame 052718/0844 →