Granted Patent
B2
US 12,371,454 · App. 18/773,066 · Granted Jul 29, 2025
Cyclic peptide compound having Kras inhibitory action
Inventors:
Mikimasa Tanada (Gotemba, JP); Koji Takano (Kamakura, JP); Atsushi Matsuo (Kamakura, JP); Minoru Tamiya (Gotemba, JP); Aya Chiyoda (Gotemba, JP); Toshiya Ito (Gotemba, JP); Takeo Iida (Singapore, SG)
Assignee:
CHUGAI SEIYAKU KABUSHIKI KAISHA
C07K7/64C07C271/22C07C317/04C07C323/09C07D205/04C07D211/38C07D213/55C07D213/61C07D213/64C07D213/65C07D295/15C07D309/12C07D333/28C07D409/12C07F5/025A61K38/00C07C2601/02C07C2601/04C07C2601/08C07C2603/18
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Abstract
The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.
Claims (12)
1. A compound, which is (5S,8S,11S,15S,18S,23aS,29S,35S,37aS)-8-((S)-sec-butyl)-18-cyclopentyl-29-(3,5-difluoro-4-(trifluoromethyl) phenethyl)-36-ethyl-11-isobutyl-N,N,5,6,12,16,19,33-octamethyl-35-(4-methylbenzyl)-4,7,10,13,17,20,23,28,31,34,37-undecaoxotetratriacontahydro-2H,4H-spiro[azeto[2,1-u]pyrrolo[2,1-i][1,4,7,10,13,16,19,22,25,28,31]undecaazacyclotetratriacontine-21,1′-cyclopentane]-15-carboxamide.
2. A solvate of (5S,8S,11S,15S,18S,23aS,29S,35S,37aS)-8-((S)-sec-butyl)-18-cyclopentyl-29-(3,5-difluoro-4-(trifluoromethyl)phenethyl)-36-ethyl-11-isobutyl-N,N,5,6,12,16,19,33-octamethyl-35-(4-methylbenzyl)-4,7,10,13,17,20,23,28,31,34,37-undecaoxotetratriacontahydro-2H,4H-spiro[azeto[2,1-u]pyrrolo[2,1-i][1,4,7,10,13,16,19,22,25,28,31]undecaazacyclotetratriacontine-21,1′-cyclopentane]-15-carboxamide.
3. The solvate according to claim 2 , which is a hydrate.
4. A pharmaceutical composition comprising the compound of claim 1 .
5. A pharmaceutical composition comprising the solvate of claim 2 .
6. A pharmaceutical composition comprising the solvate of claim 3 .
7. A method of treating cancer in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of the compound of claim 1 , wherein the cancer is pancreatic cancer.
8. The method of claim 7 , wherein the subject is human.
9. A method of treating cancer in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of the solvate of claim 2 , wherein the cancer is pancreatic cancer.
10. The method of claim 9 , wherein the subject is human.
11. A method of treating cancer in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of the solvate of claim 3 , wherein the cancer is pancreatic cancer.
12. The method of claim 11 , wherein the subject is human.
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Mar 25, 2025
From: TANADA, MIKIMASA; TAKANO, KOJI; MATSUO, ATSUSHI; TAMIYA, MINORU; CHIYODA, AYA; ITO, TOSHIYA; IIDA, TAKEO
To: CHUGAI SEIYAKU KABUSHIKI KAISHA
Reel/Frame 070615/0501 →
Priority Claims (1)
JP 2019-202407
· Nov 7, 2019
· national
Continuity (2)
Continuation
17773733
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