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JPWO2020028608A5
JPWO2020028608A5 JP2021505800A JP2021505800A JPWO2020028608A5 JP WO2020028608 A5 JPWO2020028608 A5 JP WO2020028608A5 JP 2021505800 A JP2021505800 A JP 2021505800A JP 2021505800 A JP2021505800 A JP 2021505800A JP WO2020028608 A5 JPWO2020028608 A5 JP WO2020028608A5
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pharmaceutically acceptable
acceptable salt
cancer
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Claims (17)

式Ｉ：
Figure 2020028608000001
 [式中、
各Ｘ１は、独立して、ＮまたはＣＲ２であり；
Ｘ２は、Ｏ、ＣＨ２、ＮＨ、ＳまたはＮ(Ｃ１－Ｃ３アルキル)であり；
Ｒ１は、Ｈ、ＣＨ３(ＣＨ２)１－３、ＣＨ３(ＣＨ２)０－１Ｏ(ＣＨ２)２－３、ＣＨ３(ＣＨ２)０－３Ｃ(＝Ｏ)、ＣＨ３(ＣＨ２)０－１Ｏ(ＣＨ２)２－３Ｃ(＝Ｏ)、
Figure 2020028608000002
 であり；
Ｒ２は、Ｈ、Ｏ(Ｃ１－Ｃ３アルキル)、Ｃ１－Ｃ３アルキル、Ｃｌ、ＦまたはＣＮであり；
Ｒ３は、Ｈ、ハロ、ＯＨ、ＣＮ、ＮＨ２、ＮＨ(Ｃ１－Ｃ５アルキル)、Ｎ(Ｃ１－Ｃ５アルキル)２、ＮＨ(ＣＨ２)０－１(Ｃ３－Ｃ６シクロアルキル)、ＮＨ(Ｃ４－Ｃ８ビシクロアルキル)、ＮＨ(Ｃ６－Ｃ１０スピロシクロアルキル)、Ｎ(Ｃ３－Ｃ６シクロアルキル)２、ＮＨ(ＣＨ２)１－３(アリール)、Ｎ((ＣＨ２)１－３(アリール))２、構造：
Figure 2020028608000003
 を有する環状アミン基、６員環の芳香族基またはヘテロ芳香族基、あるいは５員環のヘテロ芳香族基であって；
ここで、アルキル、シクロアルキル、ビシクロアルキル、スピロシクロアルキル、環状アミン、６員環の芳香族基またはヘテロ芳香族基、あるいは５員環のヘテロ芳香族基は、所望により、ＯＨ、ハロ、ＣＮ、(Ｃ１－Ｃ３アルキル)、Ｏ(Ｃ１－Ｃ３アルキル)、Ｃ(＝Ｏ)(Ｍｅ)、ＳＯ２(Ｃ１－Ｃ３アルキル)、Ｃ(＝Ｏ)(Ｅｔ)、ＮＨ２、ＮＨ(Ｍｅ)、Ｎ(Ｍｅ)２、ＮＨ(Ｅｔ)、Ｎ(Ｅｔ)２およびＮ(Ｃ１－Ｃ３アルキル)、(ＣＨ２)１－２ＯＨ、(ＣＨ２)１－２ＯＭｅから選択される１以上の置換基で置換されていてもよく；および
シクロアルキル、ビシクロアルキル、スピロシクロアルキルまたは環状アミン基は、Ｏ、Ｓ、ＮＨ、Ｎ(Ｃ１－Ｃ３アルキル)またはＮ(Ｂｏｃ)により置換されたＣＨ２基を有してもよく；
ｍは、０または１であり；および
ｎは、１、２または３である]
の構造を有する、化合物またはその医薬的に許容される塩。 Formula I:
Figure 2020028608000001
 [In the formula,
each X 1 is independently N or CR 2 ;
X 2 is O, CH 2 , NH, S or N(C 1 -C 3 alkyl);
R 1 is H, CH 3 (CH 2 ) 1-3 , CH 3 (CH 2 ) 0-1 O(CH 2 ) 2-3 , CH 3 (CH 2 ) 0-3 C(=O), CH 3 (CH 2 ) 0-1 O(CH 2 ) 2-3 C(=O),
Figure 2020028608000002
 is;
R 2 is H, O(C 1 -C 3 alkyl), C 1 -C 3 alkyl, Cl, F or CN;
R 3 is H, halo, OH, CN, NH 2 , NH(C 1 -C 5 alkyl), N(C 1 -C 5 alkyl) 2 , NH(CH 2 ) 0-1 (C 3 -C 6 cycloalkyl), NH(C 4 -C 8 bicycloalkyl), NH(C 6 -C 10 spirocycloalkyl), N(C 3 -C 6 cycloalkyl) 2 , NH(CH 2 ) 1-3 (aryl) , N((CH 2 ) 1-3 (aryl)) 2 , structure:
Figure 2020028608000003
 A cyclic amine group, a 6-membered ring aromatic or heteroaromatic group, or a 5-membered ring heteroaromatic group having
wherein alkyl, cycloalkyl, bicycloalkyl, spirocycloalkyl, cyclic amine, 6-membered aromatic or heteroaromatic group, or 5-membered heteroaromatic group is optionally OH, halo, CN , (C 1 -C 3 alkyl), O(C 1 -C 3 alkyl), C(=O)(Me), SO 2 (C 1 -C 3 alkyl), C(=O)(Et), NH 2 , NH(Me), N(Me) 2 , NH(Et), N(Et) 2 and N(C 1 -C 3 alkyl), (CH 2 ) 1-2 OH, (CH 2 ) 1-2 optionally substituted with one or more substituents selected from OMe; and the cycloalkyl, bicycloalkyl, spirocycloalkyl or cyclic amine groups are O, S, NH, N(C 1 -C 3 alkyl) or may have a CH2 group substituted by N(Boc);
m is 0 or 1; and n is 1, 2 or 3]
or a pharmaceutically acceptable salt thereof, having the structure Ｒ１が、
Figure 2020028608000004
 からなる群から選択される、請求項１記載の化合物またはその医薬的に許容される塩。 R 1 is
Figure 2020028608000004
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof , selected from the group consisting of: Ｒ１が、
Figure 2020028608000005
 である、請求項１記載の化合物またはその医薬的に許容される塩。 R 1 is
Figure 2020028608000005
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, which is 基：
Figure 2020028608000006
 が、
Figure 2020028608000007
 からなる群から選択される、請求項１記載の化合物またはその医薬的に許容される塩。 Base:
Figure 2020028608000006
 but,
Figure 2020028608000007
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof , selected from the group consisting of: 基：
Figure 2020028608000008
 が、
Figure 2020028608000009
 である、請求項１記載の化合物またはその医薬的に許容される塩。 Base:
Figure 2020028608000008
 but,
Figure 2020028608000009
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, which is Ｒ３が、Ｃｌ、Ｈ、
Figure 2020028608000010
Figure 2020028608000011
 からなる群から選択される、請求項１記載の化合物またはその医薬的に許容される塩。 R 3 is Cl, H,
Figure 2020028608000010
Figure 2020028608000011
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof , selected from the group consisting of: Ｒ３が、
Figure 2020028608000012
 からなる群から選択される基：
Figure 2020028608000013
 である、請求項１記載の化合物またはその医薬的に許容される塩。 R3 is
Figure 2020028608000012
 A group selected from the group consisting of:
Figure 2020028608000013
 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, which is 式（Ｉ’）：
Figure 2020028608000014
 の構造を有する、請求項１記載の化合物またはその医薬的に許容される塩。 Formula (I'):
Figure 2020028608000014
 or a pharmaceutically acceptable salt thereof, according to claim 1, having the structure: 式Ｉａ：
Figure 2020028608000015
 の構造を有する、請求項１記載の化合物またはその医薬的に許容される塩。 Formula Ia:
Figure 2020028608000015
 or a pharmaceutically acceptable salt thereof, according to claim 1, having the structure: Ｒ１が、
Figure 2020028608000016
である、請求項９記載の化合物またはその医薬的に許容される塩。 R 1 is
Figure 2020028608000016
10. The compound of claim 9, or a pharmaceutically acceptable salt thereof, which is 式Ｉｂ：
Figure 2020028608000017
 の構造を有する、請求項１記載の化合物またはその医薬的に許容される塩。 Formula Ib:
Figure 2020028608000017
 or a pharmaceutically acceptable salt thereof, according to claim 1, having the structure:
Figure 2020028608000018
 が、
Figure 2020028608000019
 である、請求項１１記載の化合物またはその医薬的に許容される塩。
Figure 2020028608000018
 but,
Figure 2020028608000019
 12. The compound of claim 11, or a pharmaceutically acceptable salt thereof, which is ２ｋＤａ～４０ｋＤａの大きさであるポリ(エチレングリコール)基に共有結合されている、請求項１記載の化合物またはその医薬的に許容される塩。 2. The compound of claim 1, or a pharmaceutically acceptable salt thereof , covalently attached to a poly(ethylene glycol) group that is between 2 kDa and 40 kDa in size. がんを治療するための、抗がん免疫療法剤および請求項１記載の化合物またはその医薬的に許容される塩を含む、医薬組成物。 A pharmaceutical composition comprising an anticancer immunotherapeutic agent and a compound of claim 1 or a pharmaceutically acceptable salt thereof for treating cancer . 抗がん免疫療法剤が、アンタゴニスト性抗ＣＴＬＡ－４、抗ＰＤ－１または抗ＰＤ－Ｌ１抗体である、請求項１４記載の医薬組成物。 15. The pharmaceutical composition according to claim 14, wherein the anti-cancer immunotherapeutic agent is an antagonistic anti-CTLA-4, anti-PD-1 or anti-PD-L1 antibody. 抗がん免疫療法剤が、イピリムマブ、ニボルマブまたはペンブロリズマブである、請求項１４記載の医薬組成物。 15. The pharmaceutical composition according to claim 14 , wherein the anticancer immunotherapeutic agent is ipilimumab, nivolumab or pembrolizumab. がんが、肺がん(非小細胞肺がんを含む)、膵臓がん、腎臓がん、頭頸部がん、リンパ腫(ホジキンリンパ腫を含む)、皮膚がん(メラノーマおよびメルケル皮膚がんを含む)、尿路上皮がん(膀胱がんを含む)、胃がん、肝細胞がんまたは大腸がんである、請求項１４～１６のいずれか一項に記載の医薬組成物。 Cancer is lung cancer (including non-small cell lung cancer), pancreatic cancer, kidney cancer, head and neck cancer, lymphoma (including Hodgkin's lymphoma), skin cancer (including melanoma and Merkel skin cancer), urine The pharmaceutical composition according to any one of claims 14 to 16 , which is tract epithelial cancer (including bladder cancer), gastric cancer, hepatocellular carcinoma or colon cancer.
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