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Heterocyclic Compound For Inducing Degradation Of Mutant Kras Protein

Abstract: Provided is a compound useful as an active ingredient in a pharmaceutical composition for treating pancreatic cancer. The present inventors carried out investigations with regard to compounds useful as an active ingredient in a pharmaceutical composition for treating pancreatic cancer and have found that a heterocyclic compound represented by formula (I) has an excellent action with regard to inducing the degradation of mutant KRAS protein and particularly with regard to inducing the degradation of G12V mutant, G12D mutant, and G12C mutant KRAS proteins, and has a mutant KRAS inhibitory activity and particularly G12V mutant, G12D mutant, and G12C mutant KRAS inhibitory activities. The present invention was achieved on the basis of these findings. The heterocyclic compound according to the present invention or a salt thereof can be used as a therapeutic agent for pancreatic cancer.

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Patent Information

Application #
Filing Date
25 February 2025
Publication Number
10/2025
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

ASTELLAS PHARMA INC.
5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411

Inventors

1. MORIKAWA, Takahiro
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
2. IMADA, Sunao
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
3. HAMAGUCHI, Hisao
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
4. OKUMURA, Mitsuaki
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
5. IMAIZUMI, Tomoyoshi
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
6. KOGANEMARU, Yohei
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
7. HONJO, Eriko
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
8. FUJIWARA, Yuta
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
9. KAWAMINAMI, Eiji
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
10. YOSHINARI, Tomohiro
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
11. ISHIOKA, Hiroki
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
12. KURAMOTO, Kazuyuki
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411
13. NISHIZONO, Yoshihiro
c/o Astellas Pharma Inc., 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411

Specification

Documents

Application Documents

# Name Date
1 202547016301-TRANSLATIOIN OF PRIOIRTY DOCUMENTS ETC. [25-02-2025(online)].pdf 2025-02-25
2 202547016301-STATEMENT OF UNDERTAKING (FORM 3) [25-02-2025(online)].pdf 2025-02-25
3 202547016301-REQUEST FOR EXAMINATION (FORM-18) [25-02-2025(online)].pdf 2025-02-25
4 202547016301-PROOF OF RIGHT [25-02-2025(online)].pdf 2025-02-25
5 202547016301-PRIORITY DOCUMENTS [25-02-2025(online)].pdf 2025-02-25
6 202547016301-FORM 18 [25-02-2025(online)].pdf 2025-02-25
7 202547016301-FORM 1 [25-02-2025(online)].pdf 2025-02-25
8 202547016301-DECLARATION OF INVENTORSHIP (FORM 5) [25-02-2025(online)].pdf 2025-02-25
9 202547016301-COMPLETE SPECIFICATION [25-02-2025(online)].pdf 2025-02-25
10 202547016301-CLAIMS UNDER RULE 1 (PROVISIO) OF RULE 20 [25-02-2025(online)].pdf 2025-02-25
11 202547016301-FORM-26 [26-02-2025(online)].pdf 2025-02-26
12 202547016301-FORM 3 [04-08-2025(online)].pdf 2025-08-04