Claims for Patent: 10,533,014
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Summary for Patent: 10,533,014
Title: | Immunoregulatory agents |
Abstract: | Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. |
Inventor(s): | Beck; Hilary Plake (Emerald Hills, CA), Jaen; Juan Carlos (Burlingame, CA), Osipov; Maksim (Redwood City, CA), Powers; Jay Patrick (Pacifica, CA), Reilly; Maureen Kay (Burlingame, CA), Shunatona; Hunter Paul (Oakland, CA), Walker; James Ross (Verona, WI), Zibinsky; Mikhail (Redwood City, CA), Balog; James Aaron (Lambertville, NJ), Williams; David K. (Delran, NJ), Markwalder; Jay A. (Lahaska, PA), Cherney; Emily Charlotte (Newtown, PA), Shan; Weifang (Princeton, NJ), Huang; Audris (New Hope, PA) |
Assignee: | FLEXUS BIOSCIENCES, INC. (Princeton, NJ) |
Application Number: | 16/123,912 |
Patent Claims: | 1. A compound having the formula (I): ##STR00284## or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein, the subscript n is 1; the subscript p is 1;
the ring designated as A is phenyl, 5- or 6-membered heteroaryl, or C.sub.5-7 cycloalkyl; Z is O; B is C(R.sup.3a); each X is independently, CHR.sup.5, C(O), or CH(OR.sup.5a); Q is N, C(CN), or CR.sup.6; D is a bond, O, C(R.sup.5).sub.2, or
NR.sup.5a; E is a 10-membered fused bicyclic heteroaryl, optionally substituted with halogen; R.sup.1 and R.sup.2 are independently hydrogen or halogen; R.sup.3, R.sup.3a and R.sup.4 are independently hydrogen or C.sub.1-C.sub.6 alkyl; each R.sup.5
is independently H, F, OH, or C.sub.1-C.sub.6 alkyl; each R.sup.5a is independently H, or C.sub.1-C.sub.6 alkyl; R.sup.6 is H, OH, F, C.sub.1-C.sub.6 alkyl, --O--C.sub.1-C.sub.6 alkyl, or --N(R.sub.5a).sub.2; and each m is independently 1, 2, or 3.
2. A combination comprising a compound of claim 1 or a pharmaceutically acceptable salt, hydrate or solvate thereof, and at least one additional therapeutic agent. 3. The combination of claim 2, wherein said additional therapeutic agent is an immuno-oncology agent. 4. The combination of claim 3, wherein said immuno-oncology agent is selected from a CTLA-4 antagonist, a PD-1 antagonist, a PD-L1 antagonist, a LAG-3 antagonist, a CD137 agonist, a GITR agonist, an OX40 agonist, an OX40L antagonist, a CD40 agonist or antagonist, a CD27 agonist, a BTLA antagonist, a TIM-3 antagonist, an A2aR antagonist, a Killer Inhibitor Receptor antagonist, or a B7H3 antibody. 5. The combination of claim 2, wherein said additional therapeutic agent is ipilimumab. 6. The combination of claim 2, wherein said additional therapeutic agent is nivolumab. 7. The combination of claim 5, in further combination with at least one chemotherapeutic agent. 8. The combination of claim 6, in further combination with at least one chemotherapeutic agent. 9. The combination of claim 2, wherein said additional therapeutic agent is BMS-986016, BMS-936559, urelumab, BMS-986153, or BMS-986156. 10. The combination of claim 2, wherein said additional therapeutic agent is tremelimumab, pembrolizumab, MEDI-0680, pidilizumab, MPDL3280A, durvalumab, MSB0010718C, IMP-731, IMP-321, PF-05082566, TRX-518, MK-4166, MEDI-6383, MEDI-6469, RG-7888, lucatumumab, dacetuzumab, varlilumab or MGA271. 11. A method of treating melanoma, lung cancer, head cancer, neck cancer, renal cell carcinoma, or bladder cancer in a human in need of such treatment, comprising administering to the human an effective amount of the compound of claim 1, or a pharmaceutically acceptable salt, hydrate or solvate thereof. 12. The method of claim 11, further comprising administering to said human at least one additional therapeutic agent. 13. The method of claim 12, wherein said at least one additional therapeutic agent is an immuno-oncology agent. 14. The method of claim 13, wherein said immuno-oncology agent is selected from a CTLA-4 antagonist, a PD-1 antagonist, a PD-L1 antagonist, a LAG-3 antagonist, a CD137 agonist, a GITR agonist, an OX40 agonist, and OX40L antagonist, a CD40 agonist or antagonist, a CD27 agonist, a BTLA antagonist, a TIM-3 antagonist, an A2aR antagonist, a Killer Inhibitor Receptor antagonist, or a B7H3 antibody. 15. The method of claim 12, wherein said additional therapeutic agent is ipilimumab. 16. The method of claim 12, wherein said additional therapeutic agent is nivolumab. 17. The method of claim 15, in further combination with at least one chemotherapeutic agent. 18. The method of claim 16, in further combination with at least one chemotherapeutic agent. 19. The method of claim 12, wherein said additional therapeutic agent is BMS-986016, BMS-936559, urelumab, BMS-986153, or BMS-986156. 20. The method of claim 12, wherein said additional therapeutic agent is tremelimumab, pembrolizumab, MEDI-0680, pidilizumab, MPDL3280A, durvalumab, MSB0010718C, IMP-731, IMP-321, PF-05082566, TRX-518, MK-4166, MEDI-6383, MEDI-6469, RG-7888, lucatumumab, dacetuzumab, varlilumab, or MGA271. |
Details for Patent 10,533,014
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Bristol-myers Squibb Company | YERVOY | ipilimumab | Injection | 125377 | 03/25/2011 | ⤷ Try a Trial | 2034-11-05 |
Merck Sharp & Dohme Corp. | KEYTRUDA | pembrolizumab | For Injection | 125514 | 09/04/2014 | ⤷ Try a Trial | 2034-11-05 |
Merck Sharp & Dohme Corp. | KEYTRUDA | pembrolizumab | Injection | 125514 | 01/15/2015 | ⤷ Try a Trial | 2034-11-05 |
Bristol-myers Squibb Company | OPDIVO | nivolumab | Injection | 125554 | 12/22/2014 | ⤷ Try a Trial | 2034-11-05 |
Bristol-myers Squibb Company | OPDIVO | nivolumab | Injection | 125554 | 10/04/2017 | ⤷ Try a Trial | 2034-11-05 |
Bristol-myers Squibb Company | OPDIVO | nivolumab | Injection | 125554 | 08/27/2021 | ⤷ Try a Trial | 2034-11-05 |
Astrazeneca Uk Ltd | IMFINZI | durvalumab | Injection | 761069 | 05/01/2017 | ⤷ Try a Trial | 2034-11-05 |
>Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
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