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US 2026/0098043 A1Published application
Polycyclic compound and use thereof
AssigneeHainan Simcere Zaiming Pharmeceutical Co., Ltd.
InventorsJinghai JIN, Yuewen LI, Yu SHI, Wei ZHU, Zhengtao LI
Life of this patent
Estimating the term…
Abstract
A compound represented by formula (I) CLM-L-PTM or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a use thereof, which are particularly suitable for preparing drugs for treating or preventing abnormal cell proliferation diseases.
Claims31
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof:
- wherein,
- CLM has the structure shown below:
- “” is selected from a single bond and a double bond;
- Z is selected from C(R3)2, NR3, and O;
- ring B is selected from 5- to 6-membered heteroaromatic ring, 5- to 8-membered heterocyclic ring, benzene ring, and C5-C8 saturated or partially saturated carbon ring;
- ring C is selected from 5- to 6-membered heteroaromatic ring, 5- to 8-membered heterocyclic ring, benzene ring, and C5-C8 saturated or partially saturated carbon ring;
- R1, R2, and R5 are each independently selected from halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each R3 is independently selected from H, halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- or R1 and R3, together with the atoms linked thereto, form C5-C8 saturated or partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring, wherein the C5-C8 saturated or partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring is optionally substituted with R5;
- each R4 is independently selected from halogen, CN, NO2, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each Ra is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rb is independently selected from H, halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rc is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rd;
- each Rd is independently selected from halogen, CN, OH, NH2, and C1-C6 alkyl;
- n is independently selected from 0, 1, 2, 3, and 4;
- m and p are independently selected from 0, 1, 2, 3, 4, 5, and 6;
- L represents a linking unit of CLM and PTM;
- PTM is selected from binding moieties of targeted proteins.
15 more elements
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A compound represented by formula (III) or a pharmaceutically acceptable salt thereof:
- wherein X1 and X2 are independently selected from N and CH, wherein the CH is optionally substituted with R2;
- Z is selected from C(R3)2, NR3, and O;
- R1, R2, and R5 are each independently selected from halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each R3 is independently selected from H, halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- or R1 and R3, together with the atoms linked thereto, form C5-C8 saturated or partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring, wherein the C5-C8 saturated or partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring is optionally substituted with R5;
- each R4 is independently selected from halogen, CN, NO2, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each Ra is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rb is independently selected from H, halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rc is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rd;
- each Rd is independently selected from halogen, CN, OH, NH2, and C1-C6 alkyl;
- n is independently selected from 0, 1, 2, 3, and 4;
- m and P are independently selected from 0, 1, 2, 3, 4, 5, and 6;
- L represents a linking unit;
- ring C is selected from 5- to 6-membered heteroaromatic ring and benzene ring;
- provided that the following compounds or pharmaceutically acceptable salts thereof are excluded:
12 more elements
A compound represented by formula (IV) or a pharmaceutically acceptable salt thereof:
- wherein X1 and X2 are independently selected from N and CH, wherein the CH is optionally substituted with R2;
- Z is selected from C(R3)2, NR3, and O;
- R1, R2, and R5 are each independently selected from halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each R3 is independently selected from H, halogen, ═O, CN, NO2, —ORb, —N(Rb)2, —S(O)Rb, —SO2Rb, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- or R1 and R3, together with the atoms linked thereto, form C5-C8 saturated or Partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring, wherein the C5-C8 saturated or partially saturated carbon ring, 5- to 6-membered heteroaromatic ring, or 5- to 8-membered heterocyclic ring is optionally substituted with R5;
- each R4 is independently selected from halogen, CN, NO2, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, 4- to 8-membered heterocyclyl, C6-C10 aryl, or 5- to 10-membered heteroaryl is optionally substituted with Ra;
- each Ra is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the 2- to 10-membered heteroalkyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rb is independently selected from H, halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rc;
- each Rc is independently selected from halogen, CN, OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, and 4- to 8-membered heterocyclyl, wherein the OH, NH2, 2- to 10-membered heteroalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, or 4- to 8-membered heterocyclyl is optionally substituted with Rd;
- each Rd is independently selected from halogen, CN, OH, NH2, and C1-C6 alkyl;
- n is independently selected from 0, 1, 2, 3, and 4;
- m and P are independently selected from 0, 1, 2, 3, 4, 5, and 6;
- ring C is selected from 5- to 6-membered heteroaromatic ring and benzene ring;
- provided that the following compounds or pharmaceutically acceptable salts thereof are excluded:
11 more elements
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Dependencies are inferred from the claim text.