IP Library Granted Patent US 12,465,603
Granted Patent B2
US 12,465,603 · App. 18/770,015 · Granted Nov 11, 2025

Phthalazinone based modulators for the treatment of disease

Inventors: Nadia Mamoona Ahmad (Essex, GB); Christopher Charles Rennie (Essex, GB); William Rameshchandra Krishna Esmieu (Saffron Walden, GB); Mark Chambers (Saffron Walden, GB); Toby Jonathan Blench (Essex, GB); Susan Mary Cramp (Essex, GB); Toby Matthew Grover Mullins (Essex, GB); Terry Aaron Panchal (Essex, GB); Joseph Leo Mckenna (Essex, GB)
Assignee: SOLEY THERAPEUTICS, INC.
A61K31/5025A61K31/502A61K31/506C07D237/32C07D401/06C07D401/12C07D403/12C07D405/04C07D413/12C07D471/04
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Quick Facts
Patent No.
US 12,465,603
App. No.
18/770,015
Granted
Nov 11, 2025
Kind
B2
Abstract

The disclosure herein provides compounds and pharmaceutical compositions of Formula (II) for killing a cancer cell or inhibiting cancer cell proliferation. Further, the compounds and pharmaceutical compositions of Formula (II) are useful in methods for the inhibition of cancer cell proliferation.

Claims (35)

1. A compound represented by the structure of Formula (II):

or a pharmaceutically acceptable salt thereof wherein:

X 1 is N;

R 4 is independently selected at each occurrence from (a), (b), and (c):

(a) halogen, —OR 20 , —SR 20 , —N(R 20 ) 2 , —C(O)R 20 , —C(O)OR 20 , —OC(O)R 20 , —OC(O)N(R 20 ) 2 , —C(O)N(R 20 ) 2 , —N(R 20 )C(O)R 20 , —N(R 20 )C(O)OR 20 , —N(R 20 )C(O)N(R 20 ) 2 , —N(R 20 )S(O) 2 (R 20 ), —S(O)R 20 , —S(O) 2 R 20 , —S(O) 2 N(R 20 ) 2 , —NO 2 , and —CN;

(b) C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OR 20 , —SR 20 , —N(R 20 ) 2 , —C(O)R 20 , —C(O)OR 20 , —OC(O)R 20 , —OC(O)N(R 20 ) 2 , —C(O)N(R 20 ) 2 , —N(R 20 )C(O)R 20 , —N(R 20 )C(O)OR 20 , —N(R 20 )C(O)N(R 20 ) 2 , —N(R 20 )S(O) 2 (R 20 ), —S(O)R 20 , —S(O) 2 R 20 , —S(O) 2 N(R 20 ) 2 , —NO 2 , ═S, ═O, and —CN; and

(c) C 3-10 carbocycle and 3- to 10-membered heterocycle, any of which is optionally substituted with one or more substituents independently selected from halogen, —OR 20 , —SR 20 , —N(R 20 ) 2 , —C(O)R 20 , —C(O)OR 20 , —OC(O)R 20 , —OC(O)N(R 20 ) 2 , —C(O)N(R 20 ) 2 , —N(R 20 )C(O)R 20 , —N(R 20 )C(O)OR 20 , —N(R 20 )C(O)N(R 20 ) 2 , —N(R 20 )S(O) 2 (R 20 ), —S(O)R 20 , —S(O) 2 R 20 , —S(O) 2 N(R 20 ) 2 , —NO 2 , ═S, ═O, and —CN;

R 5 is C 1-6 alkyl optionally substituted with one or more substituents independently selected from: halogen, —OR 21 , —SR 21 , —N(R 21 ) 2 , —C(O)R 21 , —C(O)OR 21 , —OC(O)R 21 , —OC(O)N(R 21 ) 2 , —C(O)N(R 21 ) 2 , —N(R 21 )C(O)R 21 , —N(R 21 )C(O)OR 21 , —N(R 21 )C(O)N(R 21 ) 2 , —N(R 21 )S(O) 2 (R 21 ), —S(O)R 21 , —S(O) 2 R 21 , —S(O) 2 N(R 21 ) 2 , —NO 2 , ═S, ═O, and —CN;

R 6 is independently selected at each occurrence from:

C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OR 22 , —SR 22 , —N(R 22 ) 2 , —C(O)R 22 ,—C(O)OR 22 , —OC(O)R 22 , —OC(O)N(R 22 ) 2 , —C(O)N(R 22 ) 2 , —N(R 22 )C(O)R 22 , —N(R 22 )C(O)OR 22 , —N(R 22 )C(O)N(R 22 ) 2 , —N(R 22 )S(O) 2 (R 22 ), —S(O)R 22 , —S(O) 2 R 22 , —S(O) 2 N(R 22 ) 2 , —NO 2 , ═S, ═O, and —CN;

Ring B is selected from C 3-10 carbocycle and 3- to 10-membered heterocycle;

R 7 is independently selected at each occurrence from:

halogen, —OR 23 , —SR 23 , —N(R 23 ) 2 , —C(O)R 23 , —OC(O)R 23 , —OC(O)N(R 23 ) 2 , —C(O)N(R 23 ) 2 , —N(R 23 )C(O)R 23 , —N(R 23 )C(O)OR 23 , —N(R 23 )C(O)N(R 23 ) 2 , —N(R 23 )S(O) 2 (R 23 ), —S(O)R 23 , —S(O) 2 R 23 , —S(O) 2 N(R 23 ) 2 , —NO 2 , and —CN; and C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OR 23 , —SR 23 , —N(R 23 ) 2 , —C(O)R 23 , —C(O)OR 23 , —OC(O)R 23 , —OC(O)N(R 23 ) 2 , —C(O)N(R 23 ) 2 , —N(R 23 )C(O)R 23 , —N(R 23 )C(O)OR 23 , —N(R 23 )C(O)N(R 23 ) 2 , —N(R 23 )S(O) 2 (R 23 ), —S(O)R 23 , —S(O) 2 R 23 , —S(O) 2 N(R 23 ) 2 , —NO 2 , ═S, ═O, and —CN;

R 20 , R 21 , R 22 , and R 23 , are each independently selected at each occurrence from (d), (e), and (f):

(d) hydrogen;

(e) C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —O—C 1-6 alkyl, —O—C 1-6 haloalkyl, —NH 2 , —NO 2 , ═O, —CN, C 3-10 carbocycle and 3- to 10-membered heterocycle, wherein each C 3-10 carbocycle and 3- to 10-membered heterocycle are optionally substituted with one or more substituents independently selected from: halogen, —OH, —O—C 1-6 alkyl, —O—C 1-6 haloalkyl, —NH 2 , —NO 2 , ═O, and —CN; and

(f) C 3-10 carbocycle and 3- to 10-membered heterocycle optionally substituted with one or more substituents independently selected from: halogen, —OH, —O—C 1-6 alkyl, —O—C 1-6 haloalkyl, —NH 2 , —NO 2 , ═O, and —CN;

x is selected from 0, 1, 2, 3, and 4;

y is selected from 0, 1, 2, 3, and 4; and

z is selected from 0, 1, 2, 3, 4 and 5; wherein

at least one of x or y is selected from 1, 2, 3, and 4.

2. The compound or salt of claim 1 , wherein x is selected from 0 and 1.

3. The compound or salt of claim 1 , wherein R 4 is selected from:

halogen, —OR 20 , —N(R 20 ) 2 , —C(O)R 20 , —NO 2 , and —CN; and

C 1-3 alkyl, C 3-6 carbocycle, and 3- to 6-membered heterocycle, any of which is optionally substituted with one or more substituents independently selected from: halogen, —OR 20 , —N(R 20 ) 2 , —C(O)R 20 , —NO 2 , and —CN; and

each R 20 is independently selected from hydrogen, C 1-4 alkyl, and C 1-4 haloalkyl.

4. The compound or salt of claim 1 , wherein each R 4 is independently selected from: fluoro, chloro, bromo, —O—C 1-6 alkyl, —N(CH 3 ) 2 , —CN,

5. The compound or salt of claim 1 , wherein y is selected from 0 and 1.

6. The compound or salt of claim 1 , wherein R 5 is C 1-3 alkyl optionally substituted with one or more substituents independently selected from halogen, —OR 21 , —N(R 21 ) 2 , —C(O)R 21 , —NO 2 , ═S, ═O, and —CN; and R 21 is selected from hydrogen and C 1-3 alkyl.

7. The compound or salt of claim 1 , wherein z is selected from 0, 1, and 2.

8. The compound or salt of claim 1 , wherein R 7 is selected from halogen, —OR 23 , —N(R 23 ) 2 , —C(O)R 23 , —NO 2 , —CN; and C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OR 23 , —N(R 23 ) 2 , —C(O)R 23 , —NO 2 , and —CN; and R 23 is selected from hydrogen and C 1-3 alkyl.

9. The compound or salt of claim 1 , wherein

is selected from:

10. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt of any one thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 25, 2024
From: AHMAD, NADIA MAMOONA; RENNIE, CHRISTOPHER CHARLES; ESMIEU, WILLIAM RAMESHCHANDRA KRISHNA; CHAMBERS, MARK; BLENCH, TOBY JONATHAN; CRAMP, SUSAN MARY; MULLINS, TOBY MATTHEW GROVER; PANCHAL, TERRY AARON; MCKENNA, JOSEPH LEO
To: CHARLES RIVER DISCOVERY RESEARCH SERVICES UK LIMITED
Reel/Frame 069024/0475 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 25, 2024
From: CHARLES RIVER DISCOVERY RESEARCH SERVICES UK LIMITED
To: CHARLES RIVER LABORATORIES, INC.
Reel/Frame 069024/0710 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 25, 2024
From: CHARLES RIVER LABORATORIES, INC.
To: SOLEY THERAPEUTICS, INC.
Reel/Frame 069270/0787 →
Continuity (3)
Continuation PCTUS2023080304 · Nov 17, 2023
Provisional Application 63426670 · Nov 18, 2022
Related Publication 20240374589A1 · Nov 14, 2024
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