Compound, use of a compound, and, method for treating a disease or condition associated with a kras mutation

Description

[001] This patent application claims priority to: CN202310290481.3, filed on March 23, 2023; CN202311634664.9, filed on November 30, 2023; and CN202410309827.4, filed on March 18, 2024. Technical field of the invention

[002] The present description refers to a class of piperazine ring-bridged substituted pyrimidopyran compounds and uses thereof and, specifically to a compound represented by formula (I”), formula (Γ) or formula (I), a stereoisomer thereof and a pharmaceutically acceptable salt thereof. Fundamentals of the invention

[003] KRAS is the most common oncogenic mutation gene. Mutations in the KRAS gene occur in approximately 1 in 7 cancers. KRAS mutation / KRAS gene amplification is most common in colorectal cancer (USA: ~45%, China: ~49%), pancreatic cancer (USA: ~90%, China: ~87%), and non-small cell lung cancer (USA: ~35%, China: ~13%). Among these, KRASG12D, KRASG12V, and KRASG12C are responsible for the largest proportion.

[004] KRAS is a murine sarcoma viral oncogene and an important member of the RAS proteins. KRAS acts as a molecular switch that regulates the cell growth pathway when its function is normal. After undergoing a mutation, the KRAS gene can independently transmit growth and proliferation signals to downstream pathways independent of upstream growth factor receptor signaling, resulting in uncontrolled cell growth and tumor progression. At the same time, whether or not the KRAS gene is mutated is an important indicator of tumor prognosis. Petition 870250110557, dated 02 / 12 / 2025, page 6 / 975 / 465

[005] Currently, small molecules targeting KRAS mutations are primarily concentrated in the KRASg12c field. Among these, Amgen's AMG510 and Mirati Therapeutics' MRTX849 have been approved for marketing, both demonstrating good therapeutic effects on patients with KRASg12c mutations. Additionally, MRTX1133, a small molecule drug targeting KRASg12d mutations, has entered Phase I clinical trials and demonstrated excellent antitumor properties in preclinical studies. However, this class of compounds still presents some challenges, and patients with KRASg12d mutations have not yet benefited from precision medicine, making the continued development of small molecule inhibitors targeting KRASg12d highly significant.

[006] The present description describes a series of small molecule inhibitors targeting KRASg12 and methods for preparing them. Summary of the invention

[007] In some respects, the present description provides a compound represented by formula (I”) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof: in which, Rné selected from H and the C1-3 alkyl, wherein the C1-3 alkyl. 3 is optionally replaced with 1, 2 or 3 F or Cl; Petition 870250110557, dated 02 / 12 / 2025, page 7 / 975 / 465 ring A is selected from aryl C6e heteroaryl of 5 to 6 members; ring B is selected from where ring B is optionally replaced with 1, 2, 3 or 4 R10; L is selected from -C(RliRl2)-, where Rli and Rl2 are each selected independently from H, D, and C1-3 alkyl; R1 and R2 are selected, each independently, from oxo, H, F, Cl, Br, I, and CN; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Each Ra is selected independently from among D, F, Cl, Br, and I; R4, R5, R6, R7, R6' and R7' are each selected independently from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =NO(C1-3 alkyl). Petition 870250110557, dated 02 / 12 / 2025, p. 8 / 975 / 465 in which C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently and optionally replaced with 1, 2, 3, 4 or 5 Rb; Alternatively, R6 and R7, together with the carbon atom to which they are attached, form a 3- to 5-membered heterocycloalkyl group; Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy, and -C(=O)-NRb1Rb2; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Alternatively, R8 and R8', together with the carbon atom to which they are attached, form a C3-5 cycloalkyl or a 3- to 5-membered heterocycloalkyl, wherein the C3-5 cycloalkyl and the 3- to 5-membered heterocycloalkyl are each independently and optionally substituted with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb3Rb4 and -CH2Rc; each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, -C(=O)-Rd, -S-Rd, -S(=O)-Rd, -S(=O)2-Rd, -NH-C(=O)-Rd, C6-10 aryl and 5- to 10-membered heteroaryl, wherein C1-3 alkyl is optionally substituted with 1, 2 or 3 OH or F and C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs1; Rb1 and Rb2 are each selected independently from H, C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C16 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2, 3 or 4 Re1; Alternatively, Rbi and Rb2, together with the atom of Petition 870250110557, dated 02 / 12 / 2025, p. 9 / 975 / 465 nitrogen to which they are attached, form a 3 to 6 membered heterocycloalkyl group, in which the 3 to 6 membered heterocycloalkyl group is optionally substituted with 1, 2, 3 or 4 Re1; Rb3 and Rb4 are each selected independently from H, C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C16 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2, 3 or 4 Re2; Alternatively, Rb3 and Rb4, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group, in which the 3- to 6-membered heterocycloalkyl group is optionally substituted with 1, 2, 3 or 4 Re2; Rc is selected from F, Cl, Br, I, OH, NH2, (C=O)NRc1Rc2, -O(C=O)NRc1Rc2, -NRc0(C=O)Rc1 and -NRc0(C=O)NRc1Rc2; RC0, RC1 and RC2 are each selected independently from H, C1-6 alkyl, C3-6 cycloalkyl and 3- to 6-membered heterocycloalkyl; Rd is C1-3 alkyl; Re1 is selected from the following: -(C=O)NH(C1-3 alkyl), (C=O)N(C1-3 alkyl)2, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl, and 5- to 10-membered heteroaryl; Re2 is selected from the following: -(C=O)NH(C1-3 alkyl), (C=O)N(C1-3 alkyl)2, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl, and 5- to 10-membered heteroaryl, wherein C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl, and 5- to 10-membered heteroaryl 10 Petition 870250110557, dated 02 / 12 / 2025, p. 10 / 975 6 / 465 members are replaced, each independently and optionally, with 1, 2, 3, 4 or 5 Rsi, and wherein the C1-3 alkyl and C1-3 alkoxy are replaced, each independently and optionally, with 1, 2, 3, 4 or 5 RS2; Alternatively, two or more Re2, together with the carbon atom(s) to which they are attached, form an aryl group Ce or a 5- or 6-membered heteroaryl group; Rsi is selected from oxo, F, Cl, Br, I, OH, NH2, NO2, C1-6 alkyl, C1-6 alkylamine, C1-6 dialkylamine, CN, C1-6 alkoxy, -S(=O)2(C1.3 alkyl), -(C=O)(C1.3 alkyl), -(C=O)O(C1.3 alkyl), -(C=O)NH(C1.3 alkyl) and -(C=O)N(C1.3 alkyl)2; RS2 is selected from F, Cl, Br, I, OH, NH2, C1-6 alkylamine, C1-6 dialkylamine, CN, C1-6 alkoxy, -S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) and -(C=O)N(C1-3 alkyl)2; em is selected from 0, 1, 2, 3, 4 and 5; on the condition that, 1) when ring B is is replaced with a Rio and Rio is F, at least one of Ri, R2, R4, R5, Ró, R7, Ró' and R7' is not H; / 5 / 5 2) when ring B is '—I , where the '—I is optionally replaced with 1, 2, 3 or 4 Rio, at least one of Ri, R2, R4, R5, Ró, R7, Ró' and R7' are not H; and 3) the compound is not Petition 870250110557, dated 02 / 12 / 2025, p. 11 / 975 / 465

[008] In some forms, Rn is H.

[009] In some embodiments, Rn is C1-3 alkyl optionally substituted with 1, 2 or 3 F or Cl.

[0010] The present description provides a compound represented by formula (I'), a stereoisomer thereof or a pharmaceutically acceptable salt thereof: (I'), wherein, ring A is selected from aryl C6 and heteroaryl of 5 to 6 members; ring B is selected from Ring B is optionally replaced with 1, 2, 3 or 4 R10; Petition 870250110557, dated 02 / 12 / 2025, p. 12 / 975 / 465 L is -CH2-, where the -CH2- is optionally replaced with 1 or 2 D; Ri and R2 are selected, each independently, from oxo, H, F, Cl, Br, I and CN; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Each Ra is selected independently from among D, F, Cl, Br, and I; R4, R5, R6, R7, R6' and R7' are each selected independently from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =NO(C1-3 alkyl), wherein the C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rb; Alternatively, R6 and R7, together with the carbon atoms to which they are attached, form a 3- to 5-membered heterocycloalkyl group; Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy, and -C(=O)-NRb1Rb2; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Alternatively, R8 and R8', together with the carbon atom to which they are attached, form a 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl, wherein the 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl is independently substituted and Petition 870250110557, dated 02 / 12 / 2025, p. 13 / 975 / 465 optionally, with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb1Rb2 and -CH2Rc; Each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, wherein the C1-3 alkyl is optionally substituted with 1, 2 or 3 OH; Rb1 and Rb2 are each selected independently from H, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2 or 3 Re; Alternatively, Rbi and Rb2, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group; Rc is selected from F, Cl, Br, I, OH, NH2, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=O)NRciRc2; RC0, RC1 and RC2 are each selected independently from H, C1-6 alkyl, C3-6 cycloalkyl and 3- to 6-membered heterocycloalkyl; Rd is C1-3 alkyl; Re is selected from F, Cl, Br, I, OH, NH2, C13 alkylamine, C1-3 dialkylamine, CN, C1-3 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl; m is selected from 0, 1, 2, 3, 4 and 5; on the condition that, 1) When ring B is , where is replaced with an R10 and R10 is F, at least one of R1, R2, R4, R5, Ró, R7, Ró' and R7' is not H; Petition 870250110557, dated 02 / 12 / 2025, p. 14 / 975 10 / 465 optionally replaced with 1, 2, 3 or 4 Rio, at least one of Ri, R2, R4, R5, Ró, R7, Ró' and R7' are not H; and 3) the compound is not

[0011] The present description also provides a compound represented by the formula (I'-l), a stereoisomer thereof or a pharmaceutically acceptable salt thereof: where, ring A is aril Cô; ring B is selected from 9 9 9 9 9 9 Petition 870250110557, dated 02 / 12 / 2025, p. 15 / 975 / 465 and, Ring B is optionally replaced with 1, 2, 3 or 4 R10; L is -CH2-, where the -CH2- is optionally replaced with 1 or 2 D; R1 and R2 are selected, each independently, from oxo, H, F, Cl, Br, I, and CN; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; each Ra is selected independently from among D, F, Cl, Br and I; R4, R5, R6, R7, R6' and R7' are each selected independently from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =NO(C1-3 alkyl), wherein the C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rb; Alternatively, R6 and R7, together with the carbon atoms to which they are attached, form a 3- to 5-membered heterocycloalkyl group; Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy, and -C(=O)-NRb1Rb2; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, alkyl Petition 870250110557, dated 02 / 12 / 2025, p. 16 / 975 / 465 C1-3 and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Alternatively, R8 and R8', together with the carbon atom to which they are attached, form a 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl, wherein the 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl is substituted, each independently and optionally, with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb1Rb2 and -CH2Rc; Each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, wherein the C1-3 alkyl is optionally substituted with 1, 2 or 3 OH; Rb1 and Rb2 are each selected independently from H, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2 or 3 Re; Alternatively, Rbi and Rb2, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group; Rc is selected from F, Cl, Br, I, OH, NH2, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=O)NRciRc2; RC0, RC1 and RC2 are each selected independently from H, C1-6 alkyl, C3-6 cycloalkyl and 3- to 6-membered heterocycloalkyl; Rd is C1-3 alkyl; Re is selected from F, Cl, Br, I, OH, NH2, C13 alkylamine, C1-3 dialkylamine, CN, C1-3 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl; Petition 870250110557, dated 02 / 12 / 2025, p. 17 / 975 13 / 465 m is selected from 0, 1, 2, 3, 4 and 5; on the condition that, Λ 1) When ring B is \, where V_J is replaced with a Rio and Rio is F, at least one of Ri, R2, R4, R5, Ró, R7, Ró' and R7' is not H; xo 2) when ring B is \, where the \ is optionally replaced with 1, 2, 3 or 4 RbR2, at least one of which is RbR2, R4, R5, Ró, R7, Ró' and R7' are not H; and 3) the compound is not or

[0012] The present description also provides a compound represented by the formula (I'-2), a stereoisomer thereof or a pharmaceutically acceptable salt thereof: wherein, ring A is a 5-membered heteroaryl ring; Petition 870250110557, dated 02 / 12 / 2025, p. 18 / 975 / 465, ring B is selected from Ring B is optionally replaced with 1, 2, 3 or 4 R10; L is -CH2-, where the -CH2- is optionally replaced with 1 or 2 D; R1 and R2 are selected, each independently, from oxo, H, F, Cl, Br, I, and CN; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Each Ra is selected independently from among D, F, Cl, Br, and I; R4, R5, R6, R7, R6' and R7' are each selected independently from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =NO(C1-3 alkyl), wherein the C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rb; Alternatively, R6 and R7, together with the atoms of Petition 870250110557, dated 02 / 12 / 2025, p. 19 / 975 / 465 carbon atoms to which they are attached, form a 3 to 5 membered heterocycloalkyl group; Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy, and -C(=O)-NRb1Rb2; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; Alternatively, R8 and R8', together with the carbon atom to which they are attached, form a 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl, wherein the 3- to 5-membered C3-5 cycloalkyl or heterocycloalkyl is substituted, each independently and optionally, with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb1Rb2 and -CH2Rc; Each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, wherein the C1-3 alkyl is optionally substituted with 1, 2 or 3 OH; Rb1 and Rb2 are each selected independently from H, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2 or 3 Re; Alternatively, Rbi and Rb2, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group; Rc is selected from F, Cl, Br, I, OH, NH2, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=O)NRciRc2; RC0, RC1, and RC2 are selected, each independently. Petition 870250110557, dated 02 / 12 / 2025, p. 20 / 975 16 / 465 among H, C1-6 alkyl, C3.0 cycloalkyl and 3- to 6-membered heterocycloalkyl; Rd is C1-3 alkyl; Reé selected from F, Cl, Br, I, OH, NH2, C1-3 alkylamine, C1-3 dialkylamine, CN, C1-3 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C1-10 aryl and 5- to 10-membered heteroaryl; m is selected from 0, 1, 2, 3, 4 and 5; on the condition that, 1) When ring B is \, where the \ is replaced with a Rio and Rio is F, at least one of Ri, R2, R4, R5, Ró, R7, Ró' and R7' is not H; 1 1 2) when ring B is \, where the \ is optionally replaced with 1, 2, 3 or 4 R1, at least one of R1, R2, R4, R5, R1, R7, R1' and R7' is not H; and 3) the compound is not

[0013] In some embodiments of the present description, ring B is replaced with 1, 2, 3 or 4 Rio. and said ring B is optionally

[0014] In some embodiments of the present description, ring B is Petition 870250110557, dated 02 / 12 / 2025, p. 21 / 975 / 465 , where ring B is optionally replaced with 1, 2, 3 or 4 R10. In some embodiments, ring B is not replaced. In some embodiments, ring B is replaced with 1 or 2 R10. In some embodiments, ring B is replaced with 1 R10. In some embodiments, ring B is replaced with 2 R10.

[0015] In some embodiments of the present description, the compound represented by formula (I'-1), a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from compounds of formula (I'-1-i) and (I'-2-i), stereoisomers thereof or pharmaceutically acceptable salts thereof, (I'-1-i) and

[0016] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-1-i), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0017] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-2-i), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0018] In some embodiments of the present description, ring B is , where ring B is optionally replaced with 1, 2, 3 or 4 Petition 870250110557, dated 02 / 12 / 2025, p. 22 / 975 / 465 Rio. In some events, ring B is not replaced. In some events, ring B is replaced with 1 or 2 Rio. In some events, ring B is replaced with 1 Rio. In some events, ring B is replaced with 2 R1o.

[0019] In some embodiments of the present description, the compound represented by formula (I'-1), a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from among the compounds of formulas (I'-1-ii) and (I'-2-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof, (I'-2-ii). [oo2o] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-1-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof. [oo21] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-2-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof. selected from [oo22] In some embodiments of the present description, ring B is Petition 870250110557, dated 02 / 12 / 2025, p. 23 / 975 / 465 said ring B is optionally replaced with 1, 2, 3 or 4 R10. In some embodiments, ring B is not replaced. In some embodiments, ring B is replaced with 1 or 2 R10. In some embodiments, ring B is replaced with 1 R10. In some embodiments, ring B is replaced with 2 R10.

[0023] In some embodiments of the present description, the compound of formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from compounds of formulas (I'-3), (I'-4), (I'-5), (I'-6), (I'-7), (I'-8), (I'-9), (I'-10), (I'-11), (I'-12) and (I'-13), stereoisomers thereof or pharmaceutically acceptable salts thereof, Petition 870250110557, dated 02 / 12 / 2025, p. 24 / 975 / 465 8), 10),

[0024] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from among the compounds represented by formulas (I'-14) and (I'-15), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0025] In some embodiments of the present description, ring A is phenyl, wherein the phenyl is substituted with at least one R3, and each R3 is independently selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are substituted, each independently and Petition 870250110557, dated 02 / 12 / 2025, p. 25 / 975 / 465 optionally, with 1, 2, 3, 4 or 5 Ra.

[0026] In some embodiments of the present description, ring A is phenyl, wherein the phenyl group is substituted with at least one R3, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, -a=····, , ., «Ξ·®., —., -nm, -BΞI·, - and cyclopropyl. In some embodiments of the present description, ring A is phenyl, wherein the phenyl group is substituted with two R3 groups, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, -“n, -, —=!, — ·μ,, — =, — =, — N· , — = and cyclopropyl. In some embodiments of the present description, ring A is phenyl, wherein the phenyl group is substituted with three R3 groups, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, M,, IMJ, -^β·,, , , , and cyclopropyl. In some embodiments of the present description, ring A is phenyl, wherein the phenyl is substituted with four R3s, and each R3 is selected independently from F, OH, NH2, CF3, OCH3,

[0027] is selected , and cyclopropyl. ,,, In some versions of the present description, Petition 870250110557, dated 02 / 12 / 2025, p. 26 / 975 / 465 , , , In some versions of the present description,,, In some versions of the present description,

[0029]

[0028] is selected from Petition 870250110557, dated 02 / 12 / 2025, p. 27 / 975 / 465

[0030] In some versions of the present description,

[0031] In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl group (e.g., pyridyl), wherein the 5- to 6-membered heteroaryl group is substituted with at least one R3, and each R3 is independently selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra.

[0032] In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl group (e.g., pyridyl), wherein the 5- to 6-membered heteroaryl group is substituted with at least one R3, and each R3 is selected independently from F, OH, NH2, CF3, OCH3,_·=, Petition 870250110557, dated 02 / 12 / 2025, p. 28 / 975 / 465, ., ·Ξ··., —-, -ram, - —, and cyclopropyl. In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl group (e.g., pyridyl), wherein the 5- to 6-membered heteroaryl group is substituted with two R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3,_·=, , ., «Ξ·®., —., -nm, -βξ·, - and cyclopropyl. In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl group (e.g., pyridyl), wherein the 5- to 6-membered heteroaryl group is substituted with three R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, -, -, -HE, -, -, -, -, Ξ, ΒΞ, - and cyclopropyl. In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl group (e.g., pyridyl), wherein the 5- to 6-membered heteroaryl group is substituted with four R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, -, -, -., ^-1., —., -B , -1 —, - and cyclopropyl.

[0033] In some embodiments of the present description, ring A is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group is substituted with at least one R3, and each R3 is independently selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl groups are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra.

[0034] In some embodiments of the present description, ring A is selected from a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group is replaced with at least one R3, and each R3 is selected independently from F, OH, NH2, CF3, OCH3,_·=, Petition 870250110557, dated 02 / 12 / 2025, p. 29 / 975 / 465 , —., ·Ξ··., ., =, ·ξ·, - and cyclopropyl. In some embodiments of the present description, ring A is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group is substituted with two R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, “, -«., -i^Oío., ooa,_·=O®ιι, =, — Γ·, — ·ξ· and cyclopropyl. In some embodiments of the present description, ring A is a 5-membered heteroaryl group, wherein the 5-membered heteroaryl group is substituted with three R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, —I, -=., -11=1^, OO., —., -·Ξϋ, —1=10, — = and cyclopropyl. The 5-membered heteroaryl group is substituted with 4 R3s, and each R3 is selected independently from F, OH, NH2, CF3, OCH3, “·. -·Ξ··.·, -^βίο., IM,,_0=0100111, — =, —ιξοί, — = and cyclopropyl.

[0035] In some embodiments of the present description, ring A is a 6-membered heteroaryl group, wherein the 6-membered heteroaryl group is substituted with at least one R3, and each R3 is independently selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra.

[0036] In some embodiments of the present description, ring A is a 6-membered heteroaryl group, wherein the 6-membered heteroaryl group is substituted with at least one R3, and each R3 is selected independently from F, OH, NH2, CF3, OCH3,_·=, —=,_, —=, -^=00,1, =, —IΞOI, — = and cyclopropyl. In some embodiments of the present description, ring A is a group. Petition 870250110557, dated 02 / 12 / 2025, p. 30 / 975 / 465 6-membered heteroaryl group, wherein the 6-membered heteroaryl group is replaced with two R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, “, -«., -MM··., M.,_“=“, =, — =, — ·ξ· and cyclopropyl. In some embodiments of the present description, ring A is a 6-membered heteroaryl group, wherein the 6-membered heteroaryl group is replaced with three R3s, and each R3 is independently selected from F, OH, NH2, CF3, OCH3, —1, ·Ξ··, -1=1^, M,, —., -nm, —, — = and cyclopropyl. R3 is independently selected from F, OH, NH2, CF3, OCH3,_^“n,_=, —=!, — bm,, —im,, — =, — Ν·, — ·ξ· and cyclopropyl.

[0037] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from among the compounds of formulas (I'-1'-i) and (I'-2'-i), stereoisomers thereof or pharmaceutically acceptable salts thereof, (I'-2'-i).

[0038] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-1'-i), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0039] In some embodiments of the present description, the compound Petition 870250110557, dated 02 / 12 / 2025, p. 31 / 975 / 465 represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-2'-i), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0040] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from among the compounds of formulas (I'-1'-ii) and (I'-2'-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof, (I'-1'-ii) and (I'-2'-ii).

[0041] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-1'-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0042] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof constitutes the compounds represented by formula (I'-2'-ii), stereoisomers thereof or pharmaceutically acceptable salts thereof.

[0043] In some embodiments of the present description, the compound of formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from compounds of formulas (I'-3'), (I'-4'), (I'-5'), (I'-6'), (I'-7'), (I'-8'), (I'-9'), (I'-10'), (I'-11'), (I'-12') and (I'-13'), stereoisomers thereof or salts Petition 870250110557, dated 02 / 12 / 2025, p. 32 / 975 / 465, pharmaceutically acceptable of the same. (I'-4'), (I'-6'), (I'-7'), (I'-8'), (I'-9'), (I'-10'), ill (I'-3'), (I'-5'), (I'-12') and Petition 870250110557, dated 02 / 12 / 2025, p. 33 / 975 / 465 (I'-13').

[0044] In some embodiments of the present description, the compound represented by formula (I'-1) of the present description, a stereoisomer thereof or a pharmaceutically acceptable salt thereof is selected from compounds of formulas (I'-14') and (I'-15'), stereoisomers thereof or pharmaceutically acceptable salts thereof, (I'-14') and (I'-15').

[0045] In some embodiments of the present description, ring A is selected from C6 aryl and 5- to 6-membered heteroaryl (for example, a heteroaryl that includes a ring containing 1-4 heteroatoms selected from O, N, and S), as described herein. In some embodiments of the present description, ring A is phenyl, as described herein. In some embodiments of the present description, ring A is a 5- to 6-membered heteroaryl, as described herein. In some embodiments of the present description, ring A is a 5-membered heteroaryl, as described herein. In some embodiments of the present description, ring A is a 6-membered heteroaryl, as described herein. In some embodiments of the present description, ring A is unsubstituted. In some embodiments of the present description, ring A is substituted, as described herein. In some embodiments of the present description, ring A is substituted with at least one R3 (for example, 2, 3, or 4 R3), as described herein. Petition 870250110557, dated 02 / 12 / 2025, p. 34 / 975 / 465 described.

[0046] In some embodiments of the present description, L is C(RliRl2)-, where Rli and Rl2 are selected, each independently, from H and D.

[0047] In some embodiments of the present description, L is C(RliRl2)-, where Rli and Rl2 are each independently H.

[0048] In some embodiments of the present description, L is C(R1iR12)-, where at least one of R1i and R12 is C1-3 alkyl.

[0049] In some embodiments of the present description, L is -CH2-, where the -CH2- is optionally replaced with 1 or 2 D.

[0050] In some embodiments of the present description, L is -CH2-. In some embodiments of the present description, L is -CD2-. In some embodiments of the present description, L is -CHD-.

[0051] In some embodiments of the present description, L is selected from -CH2- and -CD2-.

[0052] In some embodiments of the present description, Ri and R2 are selected, each independently, from oxo, H, F, Cl, Br, I and CN.

[0053] In some embodiments of the present description, Ri and R2 are H.

[0054] In some embodiments of the present description, Ri is selected from oxo, H, F, Cl, Br, I and CN. In some embodiments of the present description, R2 is selected from oxo, F, Cl and CN.

[0055] In some embodiments of the present description, R2 is selected from oxo, H, F, Cl, Br, I and CN. In some embodiments of the present description, Ri is selected from oxo, F, Cl and CN.

[0056] In some embodiments of the present description, each R3 is independently selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (e.g., methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), C1-3 alkylamine (e.g., methylamine, ethylamine, n-propylamine or Petition 870250110557, de 02 / 12 / 2025, pág. 35 / 975 / 465 isopropylamine), di-alkylamine C1-3 (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propylisopropylamine), alkenyl C2-4 (for example, ethenyl (C2), 1-propenyl (C3), 2propenyl (C3), 1-butenyl (C4), 2-butenyl (C4) or butadienyl (C4)), alkynyl C2-4 (for example, ethynyl (C2), 1-propenyl (C3), 2-propenyl (C3), 1-butynyl (C4) or 2-butynyl (C4)) and cycloalkyl C3-5 (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5)), in which the alquila C1-3, alcóxi C1-3, alquilamina C1-3, di-alquilamina C1-3, alquenila C2-4, alquinila C2.4e cicloalquila C3-5 são substitutosos, cada um independente e opcionalmente, com 1, 2, 3, 4 ou 5 Ra.

[0057] In some embodiments of the present description, each R3 is selected independently from F, OH, NH2, CF3, OCH3,—a=····, , , -1·^, —-, -=, - —, - and cyclopropyl.

[0058] In some embodiments of the present description, each Ra is selected independently from D, F, Cl, Br, and I. In some embodiments of the present description, each Ra is selected independently from D, F, and I.

[0059] In some embodiments of the present description, m is selected from 0, 1, 2, 3, 4 and 5. In some embodiments of the present description, m is 0. In some embodiments of the present description, m is 1. In some embodiments of the present description, m is 2. In some embodiments of the present description, m is 3. In some embodiments of the present description, m is 4. In some embodiments of the present description, m is 5.

[0060] In some embodiments of the present description, m is 4.

[0061] In some embodiments of the present description, R4, R5, R6, R7, R6' and R7' are each selected independently from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (e.g., methyl (C1), ethyl (C2), n Petition 870250110557, dated 02 / 12 / 2025, p. 36 / 975 / 465 propyl (C3) or isopropyl (C3)), C2-4 alkenyl (for example, vinyl (C2), 1-propenyl (C3), 2-propenyl (C3), 1-butenyl (C4), 2-butenyl (C4) or butadienyl (C4)), C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), -C(=O)-Rd, -C(=O)-NRb1Rb2 and =NO(C1-3 alkyl), wherein C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rb.

[0062] In some embodiments of the present description, R4, R5, R6, R7, R6' and R7' are H.

[0063] In some embodiments of the present description, at least one of R4, R5, R6, R7, Ró' and R7' is not H.

[0064] In some embodiments of the present description, Rho and R7, together with the carbon atoms to which they are attached, form a 3- to 5-membered heterocycloalkyl group (for example, a 3- to 5-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N, O, and S). In some embodiments of the present description, Rho and R7, together with the carbon atoms to which they are attached, form a 3-membered heterocycloalkyl group containing 1 heteroatom selected from N, O, and S. In some embodiments of the present description, Rho and R7, together with the carbon atoms to which they are attached, form a 3-membered heterocycloalkyl group containing 1 heteroatom selected from N, O, and S. In some embodiments of the present description, Rho and R7, together with the carbon atoms to which they are attached, form a 4-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N, O, and S.In some embodiments of the present description, R6 and R7, together with the carbon atoms to which they are attached, form a 4-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N and O. In some embodiments of the present description, R6 and R7, together with the carbon atoms to which they are attached, form a 4-membered heterocycloalkyl group containing 1. Petition 870250110557, dated 02 / 12 / 2025, p. 37 / 975 / 465 heteroatom selected from N and O. In some embodiments of the present description, R6 and R7, together with the carbon atoms to which they are attached, form a 5-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N, O and S. In some embodiments of the present description, R6 and R7, together with the carbon atoms to which they are attached, form a 5-membered heterocycloalkyl group containing 12 heteroatoms selected from N and O. In some embodiments of the present description, R6 and R7, together with the carbon atoms to which they are attached, form a 5-membered heterocycloalkyl group containing 1 heteroatom selected from N and O.

[0065] In some embodiments of the present description, each Rb is independently selected from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)) and -C(=O)-NRb1Rb2. In some embodiments of the present description, each Rb is independently selected from D, F, Cl, OH, NH2, CN, C1-3 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)) and C(=O)-NRb1Rb2.

[0066] In some embodiments of the present description, R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)) and C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra.

[0067] In some embodiments of the present description, R8 is H.

[0068] In some embodiments of the present description, R8 is selected from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)) and C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), wherein the C1-3 alkyl and C1-3 alkoxy are substituted, each independently and Petition 870250110557, dated 02 / 12 / 2025, p. 38 / 975 / 465 optionally, with 1, 2, 3, 4 or 5 Ra.

[0069] In some embodiments of the present description, R8 is selected from F, Cl, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)) and C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), wherein the C13 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra.

[0070] In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a C3-5 cycloalkyl group (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5)) or a 3- to 5-membered heterocycloalkyl group (for example, a heterocycloalkyl group that includes a ring containing 1 to 3 heteroatoms selected from O, N and S), wherein the C3-5 cycloalkyl group or the 3- to 5-membered heterocycloalkyl group are each independently and optionally substituted with 1, 2 or 3 R10.

[0071] In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a C3-5 cycloalkyl group (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5)), which is optionally substituted with 1, 2 or 3 R10.

[0072] In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 3- to 5-membered heterocycloalkyl group (for example, a 3- to 5-membered heterocycloalkyl group including a ring containing 1 to 2 heteroatoms selected from O, N, and S), wherein the 3- to 5-membered heterocycloalkyl group is substituted, each independently and optionally, with 1, 2, or 3 R10. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 3-membered heterocycloalkyl group containing 1 heteroatom selected from N, O, and S. In some embodiments of the present description, R8 and R8', together with the Petition 870250110557, dated 02 / 12 / 2025, page 39 / 975 / 465. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 3-membered heterocycloalkyl group containing 1 heteroatom selected from N and O. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 4-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N, O, and S. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 4-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N and O. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 4-membered heterocycloalkyl group containing 1 heteroatom selected from N and O.In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 5-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N, O, and S. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 5-membered heterocycloalkyl group containing 1-2 heteroatoms selected from N and O. In some embodiments of the present description, R8 and R8', together with the carbon atom to which they are attached, form a 5-membered heterocycloalkyl group containing 1 heteroatom selected from N and O.

[0073] In some embodiments of the present description, R9 is selected from -C(=O)-NRb3Rb4 and -CH2Rc. In some embodiments of the present description, R9 is selected from -C(=O)-NRb3Rb4. In some embodiments of the present description, R9 is selected from -CH2Rc.

[0074] In some embodiments of the present description, R9 is -C(=O)NRb1Rb2.

[0075] In some embodiments of the present description, each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl Petition 870250110557, dated 02 / 12 / 2025, page. 40 / 975 / 465 (C3)), C1-3 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), C1.3 alkylamine (e.g., methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (e.g., dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), -C(=O)-Rd, -S-Rd, -S(=O)Rd, -S(=O)2-Rd, -NH-C(=O)-Rd, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C1-3 alkyl is optionally substituted with 1, 2 or 3 OH or F, and the C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs1.

[0076] In some embodiments of the present description, at least one R10 is selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propylisopropylamine), -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, wherein the C1-3 alkyl group is optionally substituted with 1, 2 or 3 OH or F groups.

[0077] In some embodiments of the present description, at least one R10 is selected from oxo, D, F, Cl, OH, NH2, CN, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propylisopropylamine), -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, where o. Petition 870250110557, dated 02 / 12 / 2025, p. 41 / 975 / 465 the C1-3 alkyl group is optionally replaced with 1, 2 or 3 OH or F groups.

[0078] In some embodiments of the present description, at least one R10 is selected from oxo, F, Cl, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), wherein the C1-3 alkyl group is optionally substituted with 1, 2 or 3 OH or F groups.

[0079] In some embodiments of the present description, at least one R10 is selected from -C(=O)-Rd, -S-Rd, -S(=O)-Rd, -S(=O)2-Rd and -NHC(=O)-Rd.

[0080] In some embodiments of the present description, at least one R10 is selected from C6-10 aryl and 5 to 10 member heteroaryl, wherein the C6-10 aryl and 5 to 10 member heteroaryl are each replaced independently and optionally with 1, 2, 3, 4 or 5 Rs1.

[0081] In some embodiments of the present description, Rb1 and Rb2 are each independently selected from among C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), m-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), C3-10 cycloalkyl (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6)), C3-10 cycloalkyl (e.g. cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (Ce), cycloheptyl (C7), cyclooctyl (C8), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclodecyl (C10), octahydro-1Hindenyl (C9), decahydronaphthyl (C10) or spiro[4.5]decyl (C10)), Petition 870250110557, dated 02 / 12 / 2025, p. 42 / 975 / 465 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S), C1-10 aryl (for example, phenyl or naphthyl) and 5- to 10-membered heteroaryl (for example, a heteroaryl including one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently and optionally substituted with 1, 2, 3 or 4 Re1.

[0082] In some embodiments of the present description, at least one of Rb1 and Rb2 is selected from C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), m-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C3-6 cycloalkyl (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6)), C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropyl (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (Có)), C3-10 cycloalkyl (e.g., cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (Có), cycloheptyl (C7), cyclooctyl (Cs), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (Cs), cyclononyl (C9), cyclodecyl (C10), octahydro-1H-indenyl (C9), decahydronaphthyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, the heterocycloalkyl including one or two 3- to 8-membered rings and 1 to 5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as polycyclic spirocyclic, bridged or fused), C1-10 aryl (for example, phenyl or naphthyl) and 5- to 10-membered heteroaryl (for example, the heteroaryl including one or two 5- or 6-membered rings and 1 to 5 heteroatoms selected from N, O and S), wherein the C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C1-10 aryl and 5- to 10-membered heteroaryl are each substituted. Petition 870250110557, dated 02 / 12 / 2025, page 43 / 975 / 465 an independent and optionally, with 1, 2, 3 or 4 Kings.

[0083] In some embodiments of the present description, at least one of Rb1 and Rb2 is selected from C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), m-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C3-6 cycloalkyl (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6)) and C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropyl (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), in which the C1-6 alkyl and C1-6 alkoxy groups are each independently and optionally replaced with 1, 2, 3 or 4 RI groups.

[0084] In some embodiments of the present description, at least one of Rb1 and Rb2 is selected from C3-i0 cycloalkyl (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6), cycloheptyl (C7), cyclooctyl (C8), bicyclo[2.2.i]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclodecyl (C9), octahydro-iH-indenyl (C9), decahydronaphthyl (C10) or spiro[4.5]decyl (C10)), 3- to i0-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and i-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl group may be monocyclic or polycyclic, such as polycyclic spirocyclic, bridged or fused), C6-i0 aryl (e.g., phenyl or naphthyl) and 5- to i0 membered heteroaryl (e.g., a heteroaryl including one or two 5- or 6 membered rings and 5 heteroatoms selected from N, O and S), wherein the C3-i0 cycloalkyl, 3- to i0 membered heterocycloalkyl, C6 aryl.i0e heteroaryl groups of 5 to i0 members are replaced, each independently and optionally, with i, 2, 3, or 4 King.

[0085] In some embodiments of the present description, at least one of Rbi and Rb2 is selected from C3-6 cycloalkyl (for example, Petition 870250110557, dated 02 / 12 / 2025, p. 44 / 975 / 465 cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6)), 3- to 6-membered heterocycloalkyl, C6 aryl and 5- to 6-membered heteroaryl (for example, a heteroaryl that includes 1-3 heteroatoms selected from N, O and S), wherein the C3-6 cycloalkyl, 3- to 6-membered heterocycloalkyl, C6 aryl and 5- to 6-membered heteroaryl are each independently and optionally substituted with 1, 2, 3 or 4 Re1.

[0086] In some embodiments of the present description, Rb1 and Rb2, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group (for example, a heterocycloalkyl group including one or two 3- to 6-membered rings and 1-4 heteroatoms selected from N, O and S), wherein the 3- to 6-membered heterocycloalkyl group is optionally substituted with 1, 2, 3 or 4 Re1 groups.

[0087] In some embodiments of the present description, Rb3 and Rb4 are independently H, C1-6 alkyl, C1-6 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), C3-10 cycloalkyl (e.g., cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), bicyclo[2.2.1]heptanyl (C7), bicyclo[2.2.2]octanyl (Cs), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro- 1Hindenyl (C9), decalinyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl including one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the alkyl group, alkoxy,. Petition 870250110557, dated 02 / 12 / 2025, p. 45 / 975 / 465 cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally replaced with 1, 2, 3 or 4 Re2.

[0088] In some embodiments of the present description, at least one of Rb1 and Rb2 is C1-6 alkyl or C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), wherein alkyl or alkoxy is optionally substituted with 1, 2, 3 or 4 Re2.

[0089] In some embodiments of the present description, at least one of Rb1 and Rb2 is a C3-10 cycloalkyl group (for example, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decahydronaphthyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted with 1, 2, 3 or 4 Re2.

[0090] In some embodiments of the present description, at least one of Rb1 and Rb2 is a C3-6 cycloalkyl (for example, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6)), a 3- to 6-membered heterocycloalkyl (for example, a Petition 870250110557, dated 02 / 12 / 2025, p. 46 / 975 / 465 heterocycloalkyl containing 1-3 heteroatoms selected from N, O and S), C6 aryl, 5- to 6-membered heteroaryl (for example, a heteroaryl containing 1-4 heteroatoms selected from N, O and S), wherein the cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted with 1, 2, 3 or 4 Re2.

[0091] In some embodiments of the present description, Rb3 and Rb4, together with the nitrogen atom to which they are attached, form a 3- to 6-membered heterocycloalkyl group (for example, a heterocycloalkyl group containing 1-4 heteroatoms selected from N, O and S), wherein the 3- to 6-membered heterocycloalkyl group is optionally substituted with 1, 2, 3 or 4 Re2.

[0092] In some embodiments of the present description, Rc is selected from F, Cl, Br, I, OH, NH2, -(C=O)NRC1RC2, -O(C=O)NRC1RC2, -NRco(C=O)Rci and -NRco(C=O)NRciRc2. In some embodiments of the present description, Rc is selected from F, Cl, OH, NH2, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=0)NRciRc2. In some embodiments of the present description, Rc is selected from F, Cl, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=0)NRciRc2. In some embodiments of the present description, Rc is selected from F, Cl, OH and NH2. In some embodiments of the present description, Rc is selected from O(C=O)NRciRc2, -NRco(C=0)Rci and -NRco(C=0)NRciRc2.

[0093] In some embodiments of the present description, Rco, Rci and Rc2 are each selected independently from H, C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), m-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C3-6 cycloalkyl (for example, cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6)) and 3- to 6-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 6-membered rings and 1-4 heteroatoms selected from N, O and S). Petition 870250110557, dated 02 / 12 / 2025, p. 47 / 975 / 465

[0094] In some embodiments of the present description, Rd is selected from C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)).

[0095] In some embodiments of the present description, Re1 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), -S(=O)2(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl), -(C=O)N(C1-3 alkyl)2, C3-10 cycloalkyl (e.g., cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7),cyclooctyl (Cs), cyclooctenyl (Cs), bicyclo[2.2.1]heptaniyl (C7), bicyclo[2.2.2]octyl (Cs), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decanyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1 to 5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1 to 5 heteroatoms selected from N, O, and S).

[0096] In some embodiments of the present description, Re1 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (e.g., methyl (C1), ethyl (C2), n Petition 870250110557, dated 02 / 12 / 2025, page. 48 / 975 / 465 propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), dia-C1-3alkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, diisopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-3 alkoxy (e.g. methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), -S(=O)2(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(alkyl C1-3) or -(C=O)N(C1-3 alkyl)2.

[0097] In some embodiments of the present description, Re1 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN or C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)).

[0098] In some embodiments of the present description, Re1 is -S(=O)2(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or -(C=O)N(3-3 alkyl)2.

[0099] In some embodiments of the present description, Re1 is selected from F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), cycloalkyl C3-10 (e.g., cyclopropyl (C3), cyclobutyl (C4), cyclopentyl (C5), cyclohexyl (C6), cycloheptyl (C7), cyclooctyl (Cs), Petition 870250110557, dated 02 / 12 / 2025, p. 49 / 975 / 465 bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C5), cyclononyl (C9), cyclodecyl (C10), octahydro-1H-indenyl (C9), decahydronaphthyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl group may be monocyclic or polycyclic, for example, polycyclic spirocyclic, bridged or fused ring), C6-10 aryl (for example, phenyl or naphthyl) and 5- to 10-membered heteroaryl (for example, a heteroaryl including one or two 5- or 6-membered rings) and 1-5 heteroatoms selected from N, O, and S).

[00100] In some embodiments of the present description, Re1 is a C3-10 cycloalkyl group (for example, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C5), cyclooctenyl (C5), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decanyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl comprising one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S).

[00101] In some embodiments of the present description, Re2 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, Petition 870250110557, 02 / 12 / 2025, pág. 50 / 975 / 465 ethylamine, n-propylamine or isopropylamine), di-alquilamine C1-3 (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, alkóxi C1-3(for example, metóxi (C1), ethóxi (C2), propóxi (C3) or isopropóxi (C3)), -S(=O)2(alkyla C1-3), -(C=O)(alkyla C1-3), -(C=O)O(alkyla C1-3), -(C=O)NH(alkyl C1-3), -(C=O)N(alkyl C1-3)2, cycloalkyl C3-10 (for example, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexiyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (Cs), cyclooctenyl (Cs), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (Cs), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decanyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the Cycloalkyl, heterocycloalkyl, aryl and heteroaryl groups are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs1, and wherein the alkyl and alkoxy groups are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs2.

[00102] In some embodiments of the present description, Re2 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, Petition 870250110557, dated 02 / 12 / 2025, p. 51 / 975 / 465 methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), -S(=O)2(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3 alkyl)2, wherein the alkyl and alkoxy groups are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs2.

[00103] In some embodiments of the present description, Re2 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN or C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), wherein the alkyl groups and alkoxy are each replaced independently and optionally with 1, 2, 3, 4 or 5 Rs2.

[00104] In some embodiments of the present description, Re2 is -S(=O)2(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or -(C=O)N(3-3 alkyl)2.

[00105] In some embodiments of the present description, Re2 is F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3) or isopropyl (C3)), C1-3 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-3 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-3 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3) or isopropoxy (C3)), cycloalkyl C3-10 (e.g. cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), Petition 870250110557, of 02 / 12 / 2025, page 52 / 975 / 465 cyclo-hexyl (C6), cyclo-hexenyl (C6), cyclo-hexadienyl (C6), cyclo-heptyl (C7), cyclo-heptenyl (C7), cyclo-heptadienyl (C7), cyclo-heptatrienyl (C7), cyclo-octyl (Cs), cyclooctenyl (Cs), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (Cs), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3- to 8-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), 5- to 10-membered heteroaryl (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs1, wherein the alkyl and alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs2.

[00106] In some embodiments of the present description, Re2 is a C3-10 cycloalkyl group (for example, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C5), cyclooctenyl (C5), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decyl (C10)), 3- to 10-membered heterocycloalkyl (for example, a heterocycloalkyl including one or two 3-membered rings and 1-5 heteroatoms selected from N, O and S, wherein the heterocycloalkyl may be monocyclic or polycyclic, such as spiro polycyclic, bridged polycyclic or fused polycyclic), C6-10 aryl (for example, phenyl or naphthyl), heteroaryl Petition 870250110557, dated 02 / 12 / 2025, p. 53 / 975 / 465 of 5 to 10 members (for example, a heteroaryl comprising one or two 5- or 6-membered rings and 1-5 heteroatoms selected from N, O and S), wherein the cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rs1.

[00107] In some embodiments of the present description, two or more Re2 groups, together with the carbon atom(s) to which they are attached, form a C6 aryl group or a 5- or 6-membered heteroaryl group.

[00108] In some embodiments of the present description, Rs1 is oxo, F, Cl, Br, I, OH, NH2, NO2, C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), sec-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-6 alkoxy (e.g. methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), (C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3 alkyl)2.

[00109] In some embodiments of the present description, Rs1 is oxo, F, Cl, Br, I, OH, NH2, NO2, C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), sec-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN or C1-6 alkoxy (e.g., methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), Petition 870250110557, dated 02 / 12 / 2025, page 54 / 975 / 465 isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)).

[00110] In some embodiments of the present description, Rs1 is C1-6 alkyl (for example, methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), isobutyl (C4), sec-butyl (C4), tert-butyl (C4), pentyl (C5) or hexyl (C6)), C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4)), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), (C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3 alkyl)2.

[00111] In some embodiments of the present description, Rs1 is oxo, F, Cl, Br, I, OH, NH2, NO2, -S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), (C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3>2 alkyl.

[00112] In some embodiments of the present description, Rs1 is (C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or (C=O)N(C1-3 alkyl)2.

[00113] In some embodiments of the present description, Rs2 is F, Cl, Br, I, OH, NH2, C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN, C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)). S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), (C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3 alkyl)2. Petition 870250110557, dated 02 / 12 / 2025, page 55 / 975 / 465

[00114] In some embodiments of the present description, Rs2 is F, Cl, Br, I, OH, NH2, C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 di-alkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propyl-isopropylamine), CN or C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)).

[00115] In some embodiments of the present description, Rs2 is C1-6 alkylamine (for example, methylamine, ethylamine, n-propylamine or isopropylamine), C1-6 dialkylamine (for example, dimethylamine, diethylamine, di-n-propylamine, di-isopropylamine, methylethylamine, methyl-n-propylamine, methyl-isopropylamine, ethyl-n-propylamine, ethyl-isopropylamine or n-propylisopropylamine), CN, C1-6 alkoxy (for example, methoxy (C1), ethoxy (C2), propoxy (C3), isopropoxy (C3), butoxy (C4), isobutoxy (C4), sec-butoxy (C4), tert-butoxy (C4), pentoxy (C5), hexoxy (C6)), -S(=O)2-(C1-3 alkyl), (C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or (C=O)N(C1-3 alkyl)2.

[00116] In some embodiments of the present description, Rs2 is F, Cl, Br, I, OH, NH2, -S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or -(C=O)N(C1-3>2 alkyl.

[00117] In some embodiments of the present description, Rs2 is (C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) or (C=O)N(C1-3 alkyl)2.

[00118] The present description provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, Petition 870250110557, dated 02 / 12 / 2025, p. 56 / 975 / 465 ι·ι wherein, ring A is selected from C6-10 aryl and heteroaryl rings with 5 to 10 members; ring B is selected from in which the They are replaced, each independently and optionally, with 1, 2, 3 or 4 R10s; L is -CH2-, where the -CH2- is optionally replaced with 1 or 2 D; R1 and R2 are each selected independently from H, F, Cl, Br, I, C1-3 alkyl and C3-5 cycloalkyl, wherein the C1-3 alkyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2 or 3 Ra; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein the C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; R4, R5, R6, and R7 are selected, each independently. Petition 870250110557, dated 02 / 12 / 2025, p. 57 / 975 / 465 among H, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Rb; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; R9 is selected from -C(=O)-NRb1Rb2 and -CH2Rc; Each R10 is selected independently from D, F, Cl, Br, I, OH, NH2, C1-3 alkyl, C1-3 alkylamine, and -NH-C(=O)-Ra; Each Ra is selected independently from among D, F, Cl, Br, and I; Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, and -C(=O)-NRb1Rb2; Rb1 and Rb2 are each selected independently from H and C1-3 alkyl; Rc is selected from F, Cl, Br, I, OH, and NH2; Rd is C1-3 alkyl; m is selected from 0, 1, 2, 3, 4 and 5.

[00119] In some embodiments of the present description, the L above is selected from -CH2- and -CD2-, and other variables are as defined in the present description.

[00120] In some embodiments of the present description, each Ra mentioned above is selected independently from D, F, and Cl, and other variables are as defined in the present description.

[00121] In some embodiments of the present description, each Rb mentioned above is selected independently from OH, CN and C(=O)-NH2, and other variables are as defined in the present description.

[00122] In some embodiments of the present description, Rb1 and Rb2 mentioned above are selected, each independently, from H Petition 870250110557, dated 02 / 12 / 2025, page 58 / 975 / 465 and CH3, and other variables are as defined in this description.

[00123] In some embodiments of the present description, Rcacima is OH, and other variables are as defined in the present description.

[00124] In some embodiments of the present description, the Rd above is CH3, and other variables are as defined in the present description.

[00125] In some embodiments of the present description, the R1 above is H, and the other variables are as defined in the present description.

[00126] In some embodiments of the present description, the R2 above is H, and the other variables are as defined in the present description.

[00127] In some embodiments of the present description, each R3 mentioned above is selected independently from F, Cl, Br, I, OH, NH2, CN, CH3, CH2CH3, OCH3, OCH2CH3, NHCH3, N(CH3)2, -=,_·=, cyclopropyl and cyclobutyl, wherein CH3, CH2CH3, OCH3, OCH2CH3, NHCH3, N(CH3)2, —=,_=, cyclopropyl and cyclobutyl are each independently and optionally substituted with 1, 2, 3, 4 or 5 Ra; and other variables are as defined herein.

[00128] In some embodiments of the present description, the present description provides a compound represented by formula (Ia) or a pharmaceutically acceptable salt thereof, wherein, ring A is selected from among C6 aryl and 5-membered heteroaryl; Petition 870250110557, dated 02 / 12 / 2025, p. 59 / 975 / 465, ring B is other variables in formula (Ia) are as defined in formula (I).

[00129] In some embodiments of the present description, in the compound represented by formula (Ia) above, or a pharmaceutically acceptable salt thereof, ring A is aryl C6.

[00130] In some embodiments of the present description, in the compound represented by formula (Ia) above, or a pharmaceutically acceptable salt thereof, ring A is a 5-membered heteroaryl group.

[00131] In some embodiments of the present description, the present description provides a compound represented by formula (Ib) or a pharmaceutically acceptable salt thereof, wherein, ring A is selected from among C6 aryl and 5-membered heteroaryl; in which the ring B is selected from They are replaced, each independently and optionally, with 1, 2, 3 or 4 R10s; and Petition 870250110557, dated 02 / 12 / 2025, page 60 / 975 / 465 other variables in formula (Ib) are as defined in formula (I).

[00132] In some embodiments of the present description, in the compound represented by formula (Ib) above, or a pharmaceutically acceptable salt thereof, ring A is aryl C6.

[00133] In some embodiments of the present description, in the compound represented by formula (Ib) above, or a pharmaceutically acceptable salt thereof, ring A is a 5-membered heteroaryl group.

[00134] In some embodiments of the present description, each R3 is selected independently from F, OH, NH2, CF3, OCH3, -“n, , -, ), , , and cyclopropyl, and other variables are as defined in the present description.

[00135] In some embodiments of the present description, ring A above is phenyl, and other variables are as defined herein. In some versions of the present description, the fraction

[00136] selected from ,,,,structure above and Petition 870250110557, dated 02 / 12 / 2025, page 61 / 975 / 465 , and other variables are as defined in the present description.

[00137] In some embodiments of the present description, the R5 above is selected from H, OH, NH2, CN, CH3, CH2CH3, OCH3 and OCH2CH3, wherein CH3, CH2CH3, OCH3 and OCH2CH3 are each independently and optionally replaced with 1, 2, 3, 4 or 5 Rb, and other variables are as defined herein.

[00138] In some embodiments of the present description, R5 above is selected from H, CH3, CH2CN, CH2OH and CH2CONH2, and other variables are as defined in the present description.

[00139] In some embodiments of the present description, R6 above is selected from H and OH, and the other variables are as defined in the present description.

[00140] In some embodiments of the present description, the R4 above is H, and the other variables are as defined in the present description.

[00141] In some embodiments of the present description, the R7 above is H, and the other variables are as defined in the present description.

[00142] In some embodiments of the present description, the R8 above is selected from H and F, and the other variables are as defined in the present description.

[00143] In some embodiments of the present description, R9 is selected from -C(=O)-NH2, -C(=O)-NHCH3, -C(=O)-N(CH3)ie CH2OH, and other variables are as defined in the present description.

[00144] In some embodiments of the present description, each R10 is selected independently from D, F, NH2, CH3, -N(CH3)2 and -NHC(=O)-CH3, and other variables are as defined in the present description.

[00145] In some embodiments of the present description, ring B Petition 870250110557, dated 02 / 12 / 2025, page 62 / 975 / 465 , , in which the are replaced, each one, independently and optionally, with 1, 2, 3 or 4 Rio, and other variables are as defined in this description. ,,

[00146] In some embodiments of the present description, ring B and other variables are as defined in the present description.

[00147] The present description also includes some modalities derived from any combination of the above variables.

[00148] The present description provides the compounds shown in Table 1 or pharmaceutically acceptable salts thereof. Table 1 Petition 870250110557, dated 02 / 12 / 2025, p. 63 / 975 / 465 . $ Ç1·'· ·. ç·7· · ' · ' . $ ψ r^A· C\ xx^^Q -Uh . $xL·· . $ χ · . . : / ; '.'. .. : ι . Φ 1X? I . $ / A γυ V ' . $. £ Sjc^MX >4ϊχΛυ9 γ / γ ... $ Sjp·^ h . £ Petition 870250110557, dated 02 / 12 / 2025, p. 64 / 975 / 465 A γ A OTx B aXYQÍa xi? y· χ9 ^x χχ xi YX,i ò ... Φ . I Ã 1 B vàáIá h Xlj 11 H çC Χ9χ·Χ9 IX t;· X à 9 ·'· ·' . Φ.w . ϊγγ ^> YC- γι Y y 1 . χχ □Xo XB <ÍXXv>o xt· 1 aYx V. · Ύ γγ· γ Y . Ύ 1 Petition 870250110557, dated 02 / 12 / 2025, p. 65 / 975 / 465 7 1 ;· 7' '' XV A 1 A 1 Γ 7 . $ \L·· χχ^-χΧ . νΧ XX *' S|p^x / ... $ l . $ '?··'· ·· γΧ χ ·. ; vx - 1 χ|ιΧ.χ Petition 870250110557, dated 02 / 12 / 2025, p. 66 / 975 / 465 H H2N Petition 870250110557, dated 02 / 12 / 2025, p. 67 / 975 / 465 X / 1 Ί 'χ ! . X'! Φ <ύλ·· “X x^1-^ S^x5\!^ H N. FFF í ^χΧχ^ NH2 . $ ÇX-. ; H N. n' FX X , ; NH2 χΐϊά,ηΐ^ yx ΐ1·· ' Petition 870250110557, dated 02 / 12 / 2025, p. 68 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 69 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 70 / 975 / 465 . Φ .. Slyy^A ô aJIjCÒ. yx- -??1 - .,. A Λ '·-' Γ xW·^ γ / · x5x A ;y-.X Slyy^xy S^' xxs% γ / <by- S^xv-A <!----><?OX -nJA yy- χ5Α^ 0 Λ S^yçxxD A A·’· ^· •j;X...; SlyA^jX / A . $ -. 2 '' . ' ,·. X ·’· Ó ψ,ν. , '.^ Petition 870250110557, de 02 / 12 / 2025, pág. 71 / 975 / 465 ou sais pharmaceuticamente aceitáveis ​​dos mesmos. Table 2 Petition 870250110557, de 02 / 12 / 2025, pág. 72 / 975 / 465 . $ γ / 1 2 •F' γ / NFNO / ' o 'N'O NH2 XiXíLo^ -?9v xL· ô .?. -L ·z 2 '··· · · <Ecô. w <5h . .·. $ - S^^^C?V,AO· A T <Nl ? ΓΛ -'iV^'NEo 1 · · · Petição 870250110557, de 02 / 12 / 2025, pág. 73 / 975 / 465 . δ ': . XbcA^s^ > >Γ· ·7?1 δ δ χΧχχΧ Χχ^χχ1^ ψ' r^· “ χχ^Χ^δδ . δ τ Τ^ΙΙ ? ,_, / - / X . V Ψ J3 Λ. Á ,Λ \ 3 ' Ο ~υ δ δ φ ·χ| / · Β-^_Χ· :·. .; ^ΫγΛ „ .'1 χχ·' ·ΧΛΓ^ $ . / , XC. i χ^ςχ^ δ δ 2 :. .· ι Stcêr XX W ^χ^] δ ^Χχχχ χχ· ΧΛ<·. ^ΧΧΛ^γλΛΛ Χχ^ . Γ \ Λ1 β^Α· *~Χ Γ <δηΧ^:^ ™. Petition 870250110557, de 02 / 12 / 2025, pág. 74 / 975 / 465 ò •JC . Φ ^ÃJCXa ΓΥ i^·JX / ' “ co Λ. O w Ch CXT* -οΛ'Ο .......Ç Ο . Φ λΑ ^.rv γΑ' ΑΑ 1 CW^-nÁ CçC' W . $ Λ \ kJ 'Λ 1 V 7ν,..;· - :ç C··' . φ '\ SAA?õ Λ. nA \ \^ SlAcxA . Φ ò . ΆΧΧι : C / ' . $ ^Νλ~Χα ΓΛ . Φ C^AsÕ5 ·. $ •1- Ϊ. .. , ·; SA^NX-N <··. / a . Φ S|Ao.NA χχχΑ γ / 1 ·Χ·Χ^ Petition 870250110557, de 02 / 12 / 2025, pág. 75 / 975 / 465 Tabela 3 ou um sal pharmaceuticamente aceitável do mesmo, Petition 870250110557, de 02 / 12 / 2025, pág. 76 / 975 / 465 ·, ί . νΧά,ο,Ο $ 0 2 '·'·? ' ·. I . 2 2 ' · ' X γΧ' XX Γ -.XrX π ' XçX- XX. XXX γΧ- XX. ... ' 2 è χχ· w . $ / 21·· ' 0 Α^ΧΧ-^ 2'X·· γΧ-ΧΧ.^ 2 · ·:' -2 2,... . $ KL·· b'''NS|fXxX.r Χ^χΧγρ^Χ. χ^Χ^χχ'Χ Petition 870250110557, de 02 / 12 / 2025, pág. 77 / 975 / 465 L. A ХХ $ . T \ Л· ^Х- “ХЛ Х'7 Л__ГА ϊχ2 χχχ χ|οΧχΧ S^íXax 1 '3 '<·' S^XX “Xi ΓΛ 'xX^X· 'J. ' ' . φ S|X 3 ' ' ' XbcA χχ· -χ. ô ·. ψχΛ .χ $ ...; Λ Ά ·Ά^· χχΧΧ,·'© è 1 A1 ''X· sj^xx 7: ' :' ι _γ\ ϊΧ χΧ· . φ Sj^xxx i Η / ύ ^Γλ Χχ· X. Petition 870250110557, de 02 / 12 / 2025, pág. 78 / 975 / 465 Ου · ' · J ·· ·? Τ <·\ YboY~rvY γγ·γγ. Ο . ? ·γ YrjO^^YY φ . YWγγ ΥΥ Μ< . YloX^-^i γ. .7 Ybortt. I f O'. ' “ Cr^- ' - .§ fXf NI ίπ r\ NN OOYx>x'--x'^ n^o'O^· )— / Ο ΛN & - F '—' NH2 . £ Sj^VYfb i YYY.,nj^Xj v. YY à s^Oy / í Ύϊι..ηΙΛ'·' Y Ύ . Φ Y· SJ^Oy' . o?-'eyo XXE· xXCOwv V? 0 >>1Οηΐ rx SvS ψ Y- è X »Υ· ..- ,.-1 Y Ο··' Petition 870250110557, de 02 / 12 / 2025, pág. 79 / 975 / 465 Petition 870250110557, de 02 / 12 / 2025, pág. 80 / 975 / 465 Tabela 4 ou sais pharmaceuticalamente aceitáveis ​​dos mesmos. Petition 870250110557, de 02 / 12 / 2025, pág. 81 / 975 / 465

[00152] The present description provides the compounds shown in the Table or pharmaceutically acceptable salts thereof. Table 5 Petition 870250110557, dated 02 / 12 / 2025, p. 82 / 975 / 465 . £ Λ.~ . JL l7>· . sjc^-T? . $7 ···' . '7' - ?' / . ·. 0β <7· “ 7 ·'· ·' . $ ·. *' ... Φ.. A 71····· 1 1 :7··'·.· v Petition 870250110557, dated 02 / 12 / 2025, p. 83 / 975 / 465

[00153] The present description provides the following compounds or pharmaceutically acceptable salts thereof: Petition 870250110557, dated 02 / 12 / 2025, p. 84 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 85 / 975 / 465

[00154] In some embodiments of the present description, the compound or a pharmaceutically acceptable salt thereof is selected from: Petition 870250110557, dated 02 / 12 / 2025, p. 86 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 87 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 88 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 89 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 90 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 91 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 92 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 93 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 94 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 95 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 96 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 97 / 975 / 465 h2n h2n h2n CF3 CF3 tyX,N CF3 Petition 870250110557, dated 02 / 12 / 2025, p. 98 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 99 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 100 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 101 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 102 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 103 / 975 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 104 / 975 100 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 105 / 975 101 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 106 / 975 102 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 107 / 975 103 / 465 Petition 870250110557, dated 02 / 12 / 2025, p. 108 / 975 104 / 465 Petition 870250110557, dated 02 / 12 / 2025, page 109 / 975 105 / 465

[00155] The present description also provides for the use of the compound mentioned above, stereoisomers thereof or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of a disease or condition associated with a KRAS mutation.

[00156] The present description also provides for the use of the compound mentioned above, stereoisomers thereof or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of a disease or condition associated with a KRAS mutation.

[00157] The present description also provides for the use of the compound mentioned above, stereoisomers thereof or pharmaceutically acceptable salts thereof for the treatment of a disease or condition associated with a KRAS mutation.

[00158] The present description also provides the compound mentioned above, stereoisomers thereof or pharmaceutically acceptable salts thereof for use in the treatment of a disease or condition associated with a KRAS mutation.

[00159] The present description also provides a method for treating a disease or condition associated with a KRAS mutation, comprising administering the compound mentioned above, stereoisomers thereof, or pharmaceutically acceptable salts thereof to an individual in need thereof.

[00160] In some embodiments of the present description, the KRAS mutation is a KRASG12D mutation. Petition 870250110557, dated 02 / 12 / 2025, page 110 / 975 106 / 465

[00161] This description also provides the following biological test method: Test method 1. p-ERK inhibition test in GP2D cells 1. Objective

[00162] Using the HTRF method, compounds that can effectively inhibit p-ERK in GP2D cells with KRASG12D mutation were screened out. 2. Experimental procedure

[00163] 1). GP2D cells were inoculated into a transparent 96-well cell culture plate with 80 μL of cell suspension per well (containing 8,000 cells per well). The plate was placed in a CO2 incubator and incubated overnight at 37°C.

[00164] 2). 2 μL of compound were added to 78 μL of cell culture medium and mixed well; then, 20 μL of the compound solution were added to the corresponding wells in the cell plate. The cell plate was returned to the CO2 incubator and incubated for an additional 1 hour.

[00165] 3). After incubation, the cell supernatant was discarded and 1X μL of cell lysis buffer was added to each well. The plate was incubated at room temperature with shaking for 30 minutes.

[00166] 4). Anti-Phospho-ERK1 / 2 I Cryptate antibody and anti-Phospho-ERK1 / 2 d2 antibody were diluted 20 times with the detection buffer.

[00167] 5). 16 pL of cell lysate supernatant were transferred to each well in a new 384-well white microplate. An additional 2 pL of the anti-Phospho-ERK1 / 2 I Cryptate antibody dilution and 2 pL of the anti-Phospho-ERK1 / 2 d2 antibody dilution were added, and the plate was incubated at room temperature for at least 4 hours.

[00168] 6). After incubation, a Multilabel analyzer was used to read the HTRF with excitation: 320 nm, emission: 615 nm, 665 nm; Petition 870250110557, dated 02 / 12 / 2025, page 111 / 975 107 / 465

[00169] 7). The IC50 of the compound under test was calculated.

[00170] Test method 2. p-ERK inhibition test in AGS cells. Objective

[00171] Using the HTRF method, compounds that can effectively inhibit p-ERK in KRASG12D mutated AGS cells were filtered. Experimental procedure

[00172] 1). AGS cells were inoculated into a transparent 96-well cell culture plate, with 80 pL of cell suspension per well (containing 10,000 cells per well). The plate was placed in a CO2 incubator and incubated overnight at 37°C.

[00173] 2). After incubation, the cell supernatant was discarded and µL of culture medium containing 0.02% serum was added to each well. The cell plate was placed in a CO2 incubator and incubated overnight at 37°C.

[00174] 3). 2 pL of the compound were added to 78 pL of cell culture medium and mixed well; then, 20 pL of the compound solution were added to the corresponding well in the cell plate. The cell plate was returned to the CO2 incubator and incubated for another 3 hours.

[00175] 4). After incubation, the cell supernatant was discarded and 1X pL of cell lysis buffer was added to each well. The plate was incubated at room temperature with shaking for 30 minutes.

[00176] 5). Anti-Phospho-ERK1 / 2 I Cryptate antibody and anti-Phospho-ERK1 / 2 d2 antibody were diluted 20 times with the detection buffer.

[00177] 6). 16 pL of cell lysate supernatant were transferred to each well in a new 384-well white microplate. 2 pL of the anti-Phospho-ERK1 / 2 Cryptate antibody dilution and 2 pL of the anti-Phospho-ERK1 / 2 d2 antibody dilution were then added, and incubated at Petition 870250110557, dated 02 / 12 / 2025, page 112 / 975 108 / 465 room temperature for at least 4 hours.

[00178] 7). After incubation, a Multilabel analyzer was used to read the HTRF with excitation: 320 nm, emission: 615 nm, 665 nm;

[00179] 8). The IC50 of the compound under test was calculated.

[00180] Test method 3. Antiproliferative cellular effect of compounds on the AsPC-1 tumor cell line. Objective of the experiment.

[00181] In this study, the inhibitory effect of compounds on cell proliferation was investigated by detecting their effects on cellular activity in vitro in the KRASG12D mutated AsPC-1 tumor cell line. Experimental materials

[00182] Cell line: AsPC-1; tumor type: pancreatic cancer; growth characteristics: adherent growth; culture method: RPMI 1640 + FBS 10%

[00183] 96-well Ultra Low Cluster Plate (Corning-7007)

[00184] Greiner CELLSTAR 96-well plate (no655090)

[00185] Promega CellTiter-Glo 3D Luminescent Cell Viability Assay Kit (Promega-G9683)

[00186] PerkinElmer EnVision 2104-10 License Plate Reader

[00187] RPMI 1640, DMEM, PBS (phosphate-buffered saline), FBS (fetal bovine serum), antibiotic-antifungal drug, L-glutamine (L-Gln), DMSO (dimethyl sulfoxide) Experimental methods and steps Cell culture

[00188] Tumor cell lines were cultured in a 5% CO2 incubator at 37°C, according to the culture conditions indicated in the culture methods. The cells were regularly passaged and cells in the logarithmic growth phase were used. Petition 870250110557, dated 02 / 12 / 2025, page 113 / 975 109 / 465 for plating. Cell plating

[00189] The cells were stained with trypan blue and the viable cells were counted.

[00190] The cell concentration was adjusted to an appropriate level.

[00191] Cell line: AsPC-1; Density (per well): 7000 cells.

[00192] 135 μL of cell suspension were added to each well of a ULA culture plate, and the same volume of cell-free culture medium was added to the control blank well.

[00193] Immediately after plating, the ULA culture plate was centrifuged at room temperature for 10 minutes at 1000 rpm. Note: after centrifugation, care should be taken to avoid any unnecessary agitation during subsequent operations.

[00194] The culture plate was incubated overnight in an incubator at 37°C, 5% CO2 and 100% relative humidity.

[00195] Preparation of the 10X working solution of the compound and treatment of cells with the compound (Day 1)

[00196] After preparing the 10X working solution of the compound (10X DMSO working solution), 15 pL of the 10X working solution of the compound were added to each well of a ULA culture plate. 15 pL of a DMSO-cell culture medium mixture were added to the control vehicle and control blank.

[00197] The 96-well cell plate was returned to the incubator and cultured for 120 hours.

[00198] The formation of cellular spheres was observed every day until the end of the experiment.

[00199] CellTiter-Glo luminescent cell viability assay (Day 5) Petition 870250110557, dated 02 / 12 / 2025, page 114 / 975 110 / 465

[00200] The following steps were performed in accordance with the instructions of the Promega CellTiter-Glo 3D luminescent cell viability assay kit (Promega, noG9683).

[00201] 150 μL (equal to the volume of cell culture medium in each well) of CellTiter-Glo 3D reagent were added to each well. The cell plate was wrapped in aluminum foil to keep it in the dark.

[00202] The culture plate was shaken in an orbital shaker for 5 minutes.

[00203] The mixture in the well was carefully moved up and down 10 times with a pipette to mix evenly. It was ensured that the cellular spheroids were completely dissociated before proceeding to the next step.

[00204] The solution in the ULA culture plate was then transferred to a black background culture plate (no655090) and placed at room temperature for 25 minutes to stabilize the luminescent signal.

[00205] Luminescent signals were detected on an EnVision 2104 license plate reader. Data analysis

[00206] The inhibition rate (IR) of the compound under test was calculated using the following formula: IR (%) = (1 - (RLU compound - RLU control blank) / (RLU control vehicle - RLU control blank)) * 100%. The inhibition rate at different concentrations of the compound was calculated in Excel. GraphPad Prism software was then used to plot the inhibition curves and calculate relevant parameters, including minimum inhibition rate, maximum inhibition rate, and IC50.

[00207] Test Method 4. Pharmacokinetic study of test compounds in CD-1 mice after oral and intravenous administration. Objective of the experiment.

[00208] In vivo pharmacokinetics were tested in CD-1 mice Petition 870250110557, dated 02 / 12 / 2025, page 115 / 975 111 / 465 who received the compound orally and intravenously. Experimental procedures

[00209] The test compound was mixed with a 95% aqueous solution of DMSO 5% + (HP-e-CD 10%), vortexed, and sonicated to prepare a clear 0.5 mg / mL solution (intravenous) or a clear 3 mg / mL solution (oral). The solution was then passed through a microporous filter for later use. Male CD-1 mice aged 7 to 10 weeks were selected and received the candidate compound solution intravenously or orally. Whole blood was collected at defined intervals to prepare plasmas. Drug concentrations were analyzed by LC-MS / MS, and pharmacokinetic parameters were calculated using Phoenix WinNonlin software (Pharsight, USA). Technical effects

[00210] The compound described herein exhibits good inhibitory activity on cell proliferation in KRASG12D mutant cells and a significant inhibitory effect on p-ERK in KRASG12D mutant cells. Related definitions

[00211] Unless otherwise specified in this descriptive report, the following terms and phrases are intended to have the meanings set forth below. A specific term or phrase should not be considered undefined or unclear in the absence of a specific definition, but should be understood in its conventional sense. When a trade name appears herein, it is intended to refer to the corresponding product or active ingredient thereof.

[00212] The term “pharmaceutically acceptable”, in this descriptive report, is intended to refer to those compounds, materials, compositions and / or pharmaceutical forms that are, within the scope of reasoned medical judgment, suitable for use in contact with the tissues of humans and animals without excessive toxicity, irritation, allergic reaction or other problems or Petition 870250110557, dated 02 / 12 / 2025, page 116 / 975 112 / 465 complications, commensurate with a reasonable risk / benefit ratio.

[00213] The term “pharmaceutically acceptable salt” means a salt of compounds described herein that is prepared by reacting the compound having a specific substituent described herein with a relatively non-toxic acid or base. When compounds described herein contain a relatively acidic functional group, a base addition salt can be obtained by contacting the compound with a sufficient amount of base in a pure solution or a suitable inert solvent. When compounds described herein contain a relatively basic functional group, an acid addition salt can be obtained by contacting the compound with a sufficient amount of acid in a pure solution or a suitable inert solvent. Certain specific compounds described herein contain both basic and acidic functional groups and can be converted into either a base or acid addition salt.

[00214] The pharmaceutically acceptable salt described herein may be prepared from the parent compound containing an acidic or basic fraction by conventional chemical methods. In general, such a salt may be prepared by reacting the free acid or base form of the compound with a stoichiometric amount of an appropriate acid or base in water or an organic solvent or a mixture thereof.

[00215] The compounds described herein may be present in a specific geometric or stereoisomeric form. The present description covers all such compounds, including cis and trans isomers, (-) and (+) enantiomers, (R) and (S) enantiomers, diastereomers, (D) isomers, (L) isomers, and racemic mixtures and other mixtures, for example, a mixture enriched with an enantiomer or diastereomer, all of which are covered by the scope described herein. The substituent, such as alkyl, may have an asymmetric carbon atom. All such isomers and mixtures thereof are covered by the scope described herein. Petition 870250110557, dated 02 / 12 / 2025, page 117 / 975 113 / 465

[00216] The compounds described herein may contain an unnatural ratio of atomic isotopes in one or more of the atoms that make up the compounds. For example, a compound may be labeled with a radioisotope such as tritium (3H), iodine-125 (125I), or C-14 (14C). For another example, hydrogen may be replaced by heavy hydrogen to form a deuterated drug. The bond between deuterium and carbon is more robust than that between ordinary hydrogen and carbon. Compared to non-deuterated drugs, deuterated drugs have advantages such as reduced toxic effects, increased drug stability, enhanced efficacy, and prolonged biological half-life of drugs. All changes in the isotopic composition of compounds described herein, regardless of radioactivity, are included within the scope of this description.

[00217] The term “optional” or “optionally” means that the subsequent event or condition may occur, but is not mandatory; that the term includes the case where the event or condition occurs and the case where the event or condition does not occur.

[00218] The term “substituted” means that one or more hydrogen atoms are replaced by a substituent, including deuterium or hydrogen variants, provided that the valence of the specific atom is normal and the substituted compound is stable. When the substituent is oxo (i.e., =O), it means that two hydrogen atoms are substituted. The term “optionally substituted” means that an atom may or may not be substituted by a substituent unless otherwise specified, and that the species and number of substituents may be arbitrary as long as they are chemically attainable.

[00219] When any variable (such as R) occurs in the constitution or structure of the compound more than once, the definition of the variable in each occurrence is independent. Thus, for example, if a group is replaced by 0-2 R, the group can optionally be replaced by up to two R, where Petition 870250110557, dated 02 / 12 / 2025, page 118 / 975 114 / 465 The definition of R in each occurrence is independent. Furthermore, a combination of the substituent and / or its variant is permitted only when the combination results in a stable compound.

[00220] When the number of a linking group is 0, such as -(CRR)o-, this means that the linking group is a single bond.

[00221] When one of the variables is a single link, this means that the two groups joined by the single link are directly connected. For example, when L in ALZ represents a single link, the structure of ALZ is actually AZ.

[00222] When a numbered linking group does not indicate its linking direction, its linking direction is arbitrary. For example, when the C “ 7 \ “ 7 linking group L in is -MW-, the -MW- may be attached to ring A and ring B in the same direction as the reading order, from left to right, and constitute , or it may be attached to ring A and ring B in the reverse direction of the reading order, from left to right, and ( “ / M\1) constitute . A combination of linking groups, substituents and / or variants thereof is permitted only when such a combination can result in a stable compound.

[00223] Unless otherwise specified, when a group has one or more connectable sites, any one or more sites of the group may be connected to other groups by means of chemical bonds. When the position of the chemical bond connection is variable, and there are H atom(s) in one or more connectable sites, when the connectable site(s) having H atom(s) is / are connected to the chemical bond, the number of H atom(s) in that site will decrease correspondingly as the number of connected chemical bonds increases, and the group will become a corresponding valence group. The chemical bond between the site and other groups may Petition 870250110557, dated 02 / 12 / 2025, p. 119 / 975 115 / 465 can be represented by a straight solid link (X), a straight dashed link ) or a wavy line (^^). For example, the straight solid link in -OCH3 indicates that the group is connected to other groups through the oxygen atom in the group; the straight dashed link in indicates that the group is connected to other groups through the two ends of the nitrogen atom in the group; the wavy line in indicates that the group is connected to other groups through the 1st and 2nd carbon atoms in the phenyl group; This indicates that any connectable site on the piperidinyl group can be connected to other groups through a chemical bond, including at least four modes of connection. Even if a hydrogen atom is drawn in -N-, It also includes the connection mode; however, when a chemical bond is connected, the H in that site will be reduced by one, and the group will become the corresponding monovalent piperidinyl group.

[00224] Unless otherwise specified, a solid wedge line (>^) and a dashed wedge line (^) indicate the absolute configuration of a stereocenter; a solid straight line and a dashed straight line (^) indicate the relative configuration of a stereocenter; a wavy line (^) indicates a solid wedge line (-*^) or a dashed wedge line (^); or a wavy line indicates a solid straight line (X*) or a dashed straight line (^)

[00225] Unless otherwise specified, when a double-bonded structure exists in a compound, such as a carbon-carbon double bond, a carbon-nitrogen double bond, and a nitrogen-nitrogen double bond, and each atom in the double bond is connected to two Petition 870250110557, dated 02 / 12 / 2025, page 120 / 975 116 / 465 different substituents (in a double bond involving a nitrogen atom, a lone pair of electrons on the nitrogen atom is considered as a substituent attached to it), if the atom in the double bond and its substituent in the compound are represented by / , this represents a mixture of two isomers of the compound.

[00226] Unless otherwise specified, the term “tautomer” or “tautomeric form” means that, at room temperature, isomers with different functional groups are in dynamic equilibrium and can be rapidly converted into one another. If tautomerism is possible (as in solution), the chemical equilibrium of tautomerism can be achieved. For example, proton tautomers (also called prototropic tautomers) include interconversions via proton migration, such as keto-enol isomerization and imine-enamine isomerization. Valence isomers are tautomers that interconvert by rearranging some of the bonding electrons. A specific example of ketoenol isomerization is the interconversion between pentane-2,4-dione and 4-hydroxypent-3-en-2-one.

[00227] Unless otherwise indicated, the terms “enriched in an isomer”, “isomerically enriched”, “enantiomer-enriched” or “enantiomerically enriched” mean that the content of an isomer or enantiomer is less than 100%, and the content of that isomer or enantiomer is greater than or equal to 60%, greater than or equal to 70%, greater than or equal to 80%, greater than or equal to 90%, greater than or equal to 95%, greater than or equal to 96%, greater than or equal to 97%, greater than or equal to 98%, greater than or equal to 99%, greater than or equal to 99.5%, greater than or equal to 99.6%, greater than or equal to 99.7%, greater than or equal to 99.8% or greater than or equal to 99.9%.

[00228] Unless otherwise indicated, the term “isomer excess” or “enantiomeric excess” refers to the difference between the relative percentages of two isomers or two enantiomers. For example, Petition 870250110557, dated 02 / 12 / 2025, p. 121 / 975 117 / 465 if the content of one isomer or enantiomer is 90% and the content of the other isomer or enantiomer is 10%, the excess of isomer or enantiomer (ee value) is 80%.

[00229] Unless otherwise specified, Cn-n+m or Cn-Cn+m includes any specific case of na n+m carbons, for example, C1-12 includes C1, C2, C3, C4, C5, C6, C7, Cs, C9, C10, C11 and C12, and also includes any range of na n+m, for example, C1-12 includes C1-3, C1-6, C1-9, C3-6, C3-9, C3-12, C6-9, C6-12 and C9-12 etc.; Similarly, n members to n+m members indicates that the number of atoms in a ring is n+m, for example, a 3-12 membered ring includes a 3-membered ring, a 4-membered ring, a 5-membered ring, a 6-membered ring, a 7-membered ring, an 8-membered ring, a 9-membered ring, a 10-membered ring, an 11-membered ring, and a 12-membered ring, and also includes any range of n+m, for example, a 3-12 membered ring includes a 3-6 membered ring, a 3-9 membered ring, a 5-6 membered ring, a 5-7 membered ring, a 6-7 membered ring, a 6-8 membered ring, a 6-10 membered ring, and the like.

[00230] Unless otherwise specified, the term “halo” or “halogen”, by itself or as part of another substituent, means an atom of fluorine, chlorine, bromine or iodine.

[00231] Unless otherwise specified, the term “C13 alkyl” is used to represent a linear or branched saturated hydrocarbon group consisting of 1 to 3 carbon atoms. C1-3 alkyl includes C1-2 alkyl, C2-3 alkyl, etc. It can be monovalent (like methyl), divalent (like methylene), or multivalent (like methenyl). Examples of C1-3 alkyl include, but are not limited to, methyl (Me), ethyl (Et), propyl (including n-propyl and isopropyl), and the like.

[00232] Unless otherwise specified, the term “C16 alkyl” is used to refer to a linear or branched saturated hydrocarbon group consisting of 1 to 6 carbon atoms. The C1-6 alkyl group Petition 870250110557, dated 02 / 12 / 2025, p. 122 / 975 118 / 465 includes C1-5, C1-4, C1-3, C1-2, C2-6, C2-4, C6 and C5 alkyl groups, etc.; and can be monovalent (like methyl), divalent (like methylene) or polyvalent (like methyne). Examples of C1-6 groups include, among others, methyl (Me), ethyl (Et), propyl (including n-propyl and isopropyl), butyl (including n-butyl, isobutyl, 5-butyl and t-butyl), pentyl (including n-pentyl, isopentyl and neopentyl), hexyl, etc.

[00233] Unless otherwise specified, the term “C13 alkoxy” refers to an alkyl group containing 1 to 3 carbon atoms that is linked to the rest of a molecule via a hydrogen atom. The C1-3 alkoxy group includes C1-2, C2-3, C3 and C2 alkoxy groups, etc. Examples of C1-3 alkoxy groups include, but are not limited to, methoxy, ethoxy, propoxy (including npropoxy and isopropoxy) and the like.

[00234] Unless otherwise specified, the term “C1-3 alkylamine” refers to C1-3 -NH-alkyl, including C1-2, C3 and C2 alkylamines, etc. Examples of C1-3 alkylamines include, but are not limited to, -NHCH3, NHCH2CH3, -NHCH2CH2CH3, -NHCH2(CH3)2, etc.

[00235] Unless otherwise specified, the term “C1-3 dialkylamine” refers to -N(C1-3 alkyl)2, including C1-2 dialkylamine, C3 dialkylamine and C2 dialkylamine etc. Examples of C1-3 dialkylamine include, but are not limited to, -N(CH3)2 and -N(CH3)CH2CH3.

[00236] Unless otherwise specified, “C2-4 alkenyl” refers to a linear or branched hydrocarbon group consisting of 2 to 4 carbon atoms containing at least one carbon-carbon double bond, which may be located anywhere in the group. The C2-4 alkenyl group includes C2-3, C4, C3, and C2 alkenyl groups, etc., and the C2-4 alkenyl group may be monovalent, divalent, or polyvalent. Examples of C2-4 alkenyl groups include, but are not limited to, ethenyl, propenyl, butenyl, butadienyl, and the like. Unless otherwise specified, “C2-3 alkenyl” refers to a hydrocarbon group Petition 870250110557, dated 02 / 12 / 2025, p. 123 / 975 119 / 465 linear or branched, consisting of 2 to 3 carbon atoms containing at least one carbon-carbon double bond, which may be located in any position in the group. The C2-3 alkenyl group includes C3 and C2 alkenyl groups, and the C2-3 alkenyl group may be monovalent, divalent, or polyvalent. Examples of C2-3 alkenyl groups include, among others, ethenyl, propenyl, and the like.

[00237] Unless otherwise specified, “C2-4 alkynyl” refers to a linear or branched hydrocarbon group consisting of 2 to 4 carbon atoms containing at least one carbon-carbon triple bond, which may be located in any position within the group. Examples of C2-4 alkynyl groups include C2-3, C4, C3, and C2 alkynyl groups, etc. These groups may be monovalent, divalent, or polyvalent. Examples of C2-4 alkynyl groups include, but are not limited to, ethinyl, propynyl, butynyl, and the like.

[00238] Unless otherwise specified, “C3-5 cycloalkyl” refers to a saturated cyclic hydrocarbon group consisting of 3 to 5 carbon atoms that is a monocyclic ring system. Such C3-5 cycloalkyl groups include C3-4 and C4-5 cycloalkyl groups, etc., and may be monovalent, divalent, or polyvalent. Examples of C3-5 cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, etc.

[00239] Unless otherwise specified, “C3-10 cycloalkyl” refers to a saturated cyclic hydrocarbon group consisting of 3 to 10 carbon atoms, including monocyclic, bicyclic and tricyclic ring systems, wherein the bicyclic and tricyclic ring systems include spirocyclic, fused and bridging rings. The C3-10 cycloalkyl group includes C3-8, C3-6, C3-5, C4-10, C4-8, C4-6, C4-5, C5-8 or C5-6 etc.; and may be monovalent, divalent or polyvalent. Examples of C3-10 cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, norbornyl, [2.2.2]bicyclooctane and the like. Petition 870250110557, dated 02 / 12 / 2025, page 124 / 975 120 / 465

[00240] Unless otherwise specified, “C3-10 carbocyclyl” refers to a saturated or partially saturated cyclic hydrocarbon group consisting of 3 to 10 carbon atoms, including monocyclic, bicyclic and tricyclic ring systems, wherein the bicyclic and tricyclic ring systems include spirocyclic, fused and bridging rings. The C3-10 carbocyclyl includes C3-8, C3-6, C3-5, C4-10, C4-8, C4-6, C4-5, C5-8 or C5-6 etc.; and may be monovalent, divalent or polyvalent. Examples of C3-10 carbocyclyl groups include, but are not limited to, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), bicyclo[2.2.1]heptyl (C7), bicyclo[2.2.2]octyl (C8), cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decalinyl (C10) or spiro[4.5]decyl (C10).

[00241] Unless otherwise specified, the term “3- to 5-membered heterocycloalkyl”, by itself or in combination with other terms, refers to a saturated monocyclic group consisting of 3 to 5 atoms in the ring, of which 1, 2, 3 or 4 are heteroatoms independently selected from O, S and N, and the remainder consists of carbon atoms, wherein the carbon atoms are optionally oxidized (i.e., C(O)), the nitrogen atoms are optionally quaternized and the nitrogen and sulfur heteroatoms are optionally oxidized (i.e., NO and S(O)p, where p is 1 or 2). Furthermore, with respect to such a “3- to 5-membered heterocycloalkyl”, a heteroatom may occupy the position to which the heterocycloalkyl is attached to the rest of the molecule. These 3- to 5-membered heterocycloalkyl groups include 4- to 5-membered, 4-membered, 5-membered heteroalkyl groups, etc.Examples of 3- to 5-membered heterocycloalkyl groups include, among others, azetidinyl, oxetanyl, thietaninyl, pyrrolidinyl. Petition 870250110557, dated 02 / 12 / 2025, p. 125 / 975 121 / 465 pyrazolidinyl, imidazolidinyl, tetrahydrothiophenyl (including tetrahydrothiophen2-yl and tetrahydrothiophen-3-yl etc.) or tetrahydrofuranyl (including tetrahydrofuran-2-yl etc.) etc.

[00242] Unless otherwise specified, the term “3- to 6-membered heterocycloalkyl”, by itself or in combination with other terms, refers to a saturated cyclic group consisting of 3 to 6 atoms in the ring, of which 1, 2, 3 or 4 are heteroatoms independently selected from O, S and N, and the remainder consist of carbon atoms, wherein the carbon atoms are optionally oxidized (i.e., C(O)), the nitrogen atoms are optionally quaternized and the nitrogen and sulfur heteroatoms are optionally oxidized (i.e., NO and S(O)p, wherein p is 1 or 2). It includes monocyclic and bicyclic ring systems, wherein the bicyclic ring systems include spirocyclic, fused and bridging rings. Furthermore, with regard to the "3- to 6-membered heterocycloalkyl group," a heteroatom may occupy the position to which the heterocycloalkyl group is connected to the rest of the molecule.The 3- to 6-membered heterocycloalkyl group includes 4- to 6-membered, 5- to 6-membered, 4-membered, 5-membered, 6-membered, etc. heterocycloalkyl groups. Examples of 3- to 6-membered heterocycloalkyl groups include, but are not limited to, azetidinyl, oxetanyl, thietanyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, tetrahydrothiophenyl (including tetrahydrothiophen-2-yl and tetrahydrothiophen-3-yl etc.), tetrahydrofuranyl (including tetrahydrofuran-2-yl etc.), tetrahydropyranyl, piperidinyl (including 1-piperidinyl, 2-piperidinyl, 3-piperidinyl etc.), piperazinyl (including 1-piperazinyl, 2-piperazinyl etc.), morpholinyl (including 3-morpholinyl, 4-morpholinyl etc.), dioxanyl, ditianyl, isoxazolidinyl, isothiazolidinyl, 1,2-oxazinyl, 1,2-thiazinyl or hexahydropyridazinyl etc.

[00243] Unless otherwise specified, the term “3- to 10-membered heterocycloalkyl”, by itself or in combination with other terms, refers to a saturated cyclic group consisting of 3 to 10 Petition 870250110557, dated 02 / 12 / 2025, p. 126 / 975 122 / 465 atoms in the ring, wherein 1, 2, 3, or 4 of the atoms in the ring are heteroatoms independently selected from O, S, and N, and the remainder consists of carbon atoms, wherein the carbon atoms are optionally oxidized (i.e., C(O)), the nitrogen atoms are optionally quaternized, and the nitrogen and sulfur heteroatoms are optionally oxidized (i.e., NO and S(O)P, wherein p is 1 or 2). Includes monocyclic, bicyclic, and tricyclic ring systems, wherein the bicyclic and tricyclic ring systems include spirocyclic, fused, and bridging rings. Furthermore, with respect to the term “3- to 10-membered heterocycloalkyl,” a heteroatom may occupy the position to which the heterocycloalkyl group is attached to the rest of the molecule. The 3- to 10-membered heterocycloalkyl group includes heterocycloalkyl groups with 3- to 8 members, 3- to 6 members, 3- to 5 members, 4- to 6 members, 5- to 6 members, 4 members, 5 members, 6 members, etc.Examples of 3- to 10-membered heterocycloalkyl groups include, but are not limited to, azetidinyl, oxetanyl, thietanyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, tetrahydrothiophenyl (including tetrahydrothiophen-2-yl, tetrahydrothiophen-3-yl, etc.), tetrahydrofuranyl (including tetrahydrofuran-2-yl, etc.), tetrahydropyranyl, piperidinyl (including 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, etc.), piperazinyl (including 1-piperazinyl, 2-piperazinyl, etc.), morpholinyl (including 3-morpholinyl, 4-morpholinyl, etc.), dioxanyl, ditianyl, isoxazolidinyl, isothiazolidinyl, hexahydropyridazinyl, homopiperazinyl, homopiperidinyl or dioxepanil, etc.

[00244] Unless otherwise specified, the terms “C6-10 aromatic ring” and “C6-10 aryl” are used interchangeably in this document. The term “C6-10 aromatic ring” or “C6-10 aryl” refers to a cyclic hydrocarbon group composed of 6 to 10 carbon atoms and having a conjugated π electron system. It may be a monocyclic ring system, a fused bicyclic ring, or a fused tricyclic ring, where each ring is aromatic. It may be monovalent, divalent, or polyvalent. C6-10 aryl groups Petition 870250110557, dated 02 / 12 / 2025, p. 127 / 975 123 / 465 include C6-9, C9, C10 and C6 aryl groups. Examples of C6-10 aryl groups include, among others, phenyl and naphthyl (including 1-naphthyl, 2-naphthyl, etc.).

[00245] Unless otherwise specified, the terms “5- to 10-membered heteroaromatic ring” and “5- to 10-membered heteroaryl” may be used interchangeably. The term “5- to 10-membered heteroaryl” means a cyclic group having a conjugated pi electron system and consisting of 5 to 10 ring atoms, of which 1, 2, 3, or 4 ring atoms are heteroatoms independently selected from O, S, and N, and the remainder being carbon atoms. It may be a monocyclic, fused bicyclic, or fused tricyclic ring system, in which each ring is aromatic and in which the nitrogen atom is optionally quaternized and the nitrogen and sulfur heteroatoms are optionally oxidized (i.e., NO and S(O)p, p is 1 or 2). A 5- to 10-membered heteroaryl group can be linked to the rest of a molecule via a heteroatom or a carbon atom. The 5- to 10-membered heteroaryl group includes 5- to 8-membered, 5- to 7-membered, 5- to 6-membered, and 5-membered heteroaryl groups.6 members etc. Examples of 5- to 10-membered heteroaryl groups include, but are not limited to, pyrrolyl (including N-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl and the like), pyrazolyl (including 2-pyrazolyl, 3-pyrazolyl and the like), imidazolyl (including N-imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl and the like), oxazolyl (including 2-oxazolyl, 4-oxazolyl, 5-oxazolyl and the like), triazolyl (1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, 1H-1,2,4-triazolyl, 4H-1,2,4-triazolyl and the like), tetrazolyl, isoxazolyl (3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl and the like), thiazolyl (including 2-thiazolyl, 4-thiazolyl, 5-thiazolyl and similar), furyl (including 2-furyl, 3-furyl and similar), tienyl (including 2-thienyl, 3-thienyl and similar), pyridyl (including 2-pyridyl, 3-pyridyl, 4-pyridyl and similar), pyrazinyl, pyrimidinyl (including 2-pyrimidinyl, 4-pyrimidinyl and similar), benzothiazolyl (including 5-benzothiazolyl and similar), purinyl,benzimidazolyl (including 2, Petition 870250110557, dated 02 / 12 / 2025, p. 128 / 975 124 / 465 benzimidazolyl and the like), benzoxazolyl, indolyl (including 5-indolyl and the like), isoquinolyl (including 1-isoquinolyl, 5-isoquinolyl and the like), quinoxalinyl (including 2-quinoxalinyl, 5-quinoxalinyl and the like) or quinolyl (including 3-quinolyl, 6-quinolyl and the like).

[00246] Unless otherwise specified, the terms “5- to 6-membered heteroaromatic ring” and “5- to 6-membered heteroaryl” are used interchangeably in this document. The term “5- to 6-membered heteroaryl” refers to a monocyclic group consisting of 5 to 6 atoms in the ring with a conjugated π electron system, where 1, 2, 3, or 4 of the atoms in the ring are heteroatoms independently selected from O, S, and N, and the remainder are carbon atoms. The nitrogen atom is optionally quaternized, and the nitrogen and sulfur heteroatoms are optionally oxidized (i.e., NO and S(O)p, where p is 1 or 2).The 5- to 6-membered heteroaryl group can be linked to the rest of the molecule via a heteroatom or a carbon atom. The 5- to 6-membered heteroaryl group includes both 5-membered and 6-membered heteroaryl groups. Examples of the 5- to 6-membered heteroaryl group include, among others, pyrrolyl (including N-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl, etc.), pyrazolyl (including 2-pyrazolyl, 3-pyrazolyl, etc.), imidazolyl (including N-imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl, etc.), oxazolyl (including 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, etc.), triazolyl (1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, 1H-1,2,4-triazolyl, 4H-1,2,4-triazolyl, etc.), tetrazolyl, isoxazolyl (3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, etc.), thiazolyl (including 2-thiazolyl, 4-thiazolyl, 5thiazolyl etc.), furyl (including 2-furyl, 3-furyl etc.), thienyl (including 2thienyl, 3-thienyl etc.), pyridyl (including 2-pyridyl, 3-pyridyl, 4-pyridyl etc.), pyrazinyl or pyrimidinyl (including 2-pyrimidinyl, 4-pyrimidinyl, etc.).

[00247] The compounds of the present description can be prepared by a variety of synthetic methods well known to those skilled in the art, including the specific embodiments listed below, embodiments Petition 870250110557, dated 02 / 12 / 2025, page 129 / 975 125 / 465 formed by combining them with other chemical synthesis methods and equivalents well known to those skilled in the art. Alternative embodiments include, among others, the examples in the present description.

[00248] The structures of the compounds in the present description can be confirmed by conventional methods well known to those skilled in the art. If the present description refers to the absolute configuration of a compound, such absolute configuration can be confirmed using conventional techniques in the art. For example, single-crystal X-ray diffraction (SXRD) is performed by collecting diffraction intensity data from a grown single crystal using a Bruker D8 venture diffractometer, CuKa radiation as the light source and φ / ω scanning mode. After collecting relevant data, the crystal structure can be further analyzed by a direct method (Shelxs97) to confirm the absolute configuration.

[00249] The solvents used in this description are commercially available. This description uses the following abbreviations: NaOH represents sodium hydroxide; DMF represents N,N-dimethylformamide; THF represents tetrahydrofuran; 2-MeTHF represents 2-methyltetrahydrofuran; DCM represents dioxane; EA represents ethyl acetate; DIPEA represents N,N-diisopropylamine; DCM represents dichloromethane; m-CPBA represents m-chloroperbenzoic acid; Boc2O represents di-tert-butylcarbonic anhydride; LiAlH4 represents lithium aluminum tetrahydride; MNO2 represents manganese dioxide; NBS represents N-bromosuccinimide; TMP represents trimethylolpropane; n-BuLi represents n-butyllithium; TFA represents trifluoroacetic acid; Xphos Pd G4 representa: (SP-4-3)-[diciclo-hexil[2',4',6'tri(isopropil)[1,1'-bifenil]-2-il]fosfina](ácido metanossulfônico)[2'(metilamina)[1,1'-bifenil]-2-il]paládio; AgNO3 represents silver nitrate; NCS stands for N-chlorosuccinimide.

[00250] The compounds were named according to conventional nomenclature in the art or using ChemDraw® software. Compounds Petition 870250110557, dated 02 / 12 / 2025, p. 130 / 975 126 / 465 commercially available were named according to the supplier's catalog name. Detailed description of the invention

[00251] The present description is described in detail below by way of examples, but the examples are not intended to limit the present description in any way. Although the present description has been described here in detail, and specific embodiments thereof have been described, it will be evident to those skilled in the art that various alterations and modifications may be made to the specific embodiments of the present description without departing from the spirit and scope of the present description. Example 1 Petition 870250110557, dated 02 / 12 / 2025, p. 131 / 975 127 / 465 Step 1

[00252] Compound 1-1 was subjected to preparative supercritical liquid chromatography (SFC) (Chromatographic column: ChiralPak IH, 250*50 mm, 10 pm; mobile phase: A: supercritical carbon dioxide, B: [0.1% ammonia-ethanol]; B%: 20%-20%, run time 3.7 min) to obtain compound 1-1A. SFC analytical method (Chromatographic column: Chiralpak IH-3, 100*4.6 mm ID, 3 pm; mobile phase: A (supercritical carbon dioxide) and B (ethanol, containing 0.1% isopropylamine); gradient: B% = 10-50%, 4 min; flow rate: 3.4 mL / min; wavelength: 220 nm; pressure: 2000 psi (13.8 MPa)). Compound 1-1A: Rt = 1.489 min and ee value of 98.82%. 1H NMR (400 MHz, CDCl3) δ = 4.99 - 4.86 (m, 2H), 4.26 - 3.95 (m, 3H), 3.59 (m, 1H), 3.00 - 2.88 (m, 1H), 2.87 - 2.12 (m, 4H), 1.91 (s, 1H), 1.20 - 1.08 (m, 3H). Step 2

[00253] Lithium aluminum tetrahydride (1.55 g, 40.15 mmol) was dissolved in anhydrous tetrahydrofuran (30 mL). The mixture was cooled to 0°C. Under nitrogen, a solution of compound 1-1A (2.8 g, 13.38 mmol) in anhydrous tetrahydrofuran (20 mL) was added. The reaction took place at 70°C for 1 hour. At 0°C, 1.5 mL of water was added to the reaction, followed by 1.5 mL of 15% NaOH solution and 4.5 mL of water. The mixture was stirred for 20 minutes. The reaction mixture was filtered. The filtered cake was washed with 10 mL of tetrahydrofuran, and the filtrate was concentrated to obtain compound 12. 1H NMR (400 MHz, CDCl3) δ = 4.99 - 4.86 (m, 2H), 4.26 - 3.95 (m, 3H), 3.59 (m, 1H), 3.00 - 2.88 (m, 1H), 2.74 - 2.27 (m, 4H), 1.91 (s, 1H), 1.20 - 1.08 (m, 3H). Step 3

[00254] Compound 1-3 (480 g, 2.53 mol) was weighed and DMF (2500 mL) was added. 4-methoxybenzyl chloride (5.18 mol, 702.79 mL), potassium carbonate (872.82 g, 6.32 mol) and potassium iodide (419.35 g, Petition 870250110557, dated 02 / 12 / 2025, page 132 / 975 128 / 465 2.53 mol) were then added. The mixture was reacted at 65°C for 2 hours. Water (1000 mL) was added and the mixture was extracted with ethyl acetate (1000 mL x 3). The organic phase was concentrated under reduced pressure to obtain compound 1-4. MS m / z = 430.0 [M+H]+. Step 4

[00255] The compound 2,2,6,6-tetramethylpiperidine (220.59 g, 1.56 mol, 265.13 mL) was weighed and THF (3000 mL) was added. n-butyllithium (2.5 M, 499.73 mL) was added at -5°C and the mixture was stirred for 0.5 hours. The temperature was then reduced to -60°C and compound 1-4 (280 g, 624.67 mmol) was added. The mixture was stirred for 0.5 hours and finally DMF (228.28 g, 3.12 mol, 240.30 mL) was added. The mixture was reacted for an additional 0.5 hours. The reaction mixture was poured into water (1000 mL) and the pH was adjusted to 7 with 1N hydrochloric acid. The mixture was extracted with ethyl acetate (1000 mL x 3). The organic phase was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 10:1) to obtain compound 1-5. Step 5

[00256] Compound 1-5 (370 g, 807.30 mmol) was weighed. Toluene (1500 mL), dichlorobis(di-tert-butyl-(4-dimethylaminophenyl)phosphine)palladium (2.86 g, 4.04 mmol, 2.86 mL) and tributyl(1-propynyl)tin (265.69 g, 807.30 mmol) were added. The mixture was reacted at 120°C for 2 hours under nitrogen. The reaction solution was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 1-6. MS m / z = 418.1 [M+H]+. Step 6

[00257] Compound 1-6 (450 g, 970.13 mmol) was weighed and DMF (100 mL) was added. N-bromosuccinimide (189.93 g, 1.07 mol) was added and the mixture was reacted at 25°C for 2 hours. More N-bromosuccinimide (17.27 g, 97.01 mmol) was added and the mixture was reacted for 3 hours. Petition 870250110557, dated 02 / 12 / 2025, p. 133 / 975 129 / 465 additional. The reaction solution was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 1-7. MS m / z = 496.0 [M+H]+. Step 7

[00258] Compound 1-7 (55 g, 110.81 mmol) was weighed and DMF (300 mL) was added. Methyl fluoro-(fluorosulfonyl)-difluoroacetate (42.57 g, 221.61 mmol, 28.19 mL) and cuprous iodide (42.21 g, 221.61 mmol) were added and the reaction mixture was reacted at 110°C under nitrogen for 2 hours. The mixture was rapidly cooled by the addition of 500 mL of water and extracted with ethyl acetate (600 mL x 3). The extracted organic phases were combined and washed sequentially with water (800 mL x 2) and saturated brine (800 mL), dried with anhydrous sodium sulfate, filtered and concentrated. Compound 1-8 was obtained by column chromatography (petroleum ether:ethyl acetate = 10:1). MS m / z = 485.9 [M+H]+. Step 8

[00259] To a solution of sodium hydride (6.34 g, 158.61 mmol, 60% purity) in tetrahydrofuran (350 mL) at 0°C, methyl acetoacetate (158.61 mmol, 17.10 mL) was added dropwise. The mixture was allowed to react for 15 minutes. After cooling to -20°C, n-butyllithium (2.5 M, 63.44 mL) was added dropwise. After the addition was complete, the mixture was stirred for an additional 15 minutes. A solution of compound 1-8 (35 g, 72.10 mmol) in tetrahydrofuran (350 mL) was then added. The mixture was allowed to react for 0.5 hours. The reaction was rapidly cooled by the addition of 200 mL of saturated ammonium chloride solution. The mixture was extracted with ethyl acetate (300 mL x 2). The extracted organic phases were combined and washed with saturated brine (400 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Compound 1-9 was obtained by column chromatography (petroleum ether:ethyl acetate = 10:1 to 1:1). MS m / z = 624.2 [M+Na]+. Petition 870250110557, dated 02 / 12 / 2025, page 134 / 975 130 / 465 Step 9

[00260] Compound 1-9 (38 g, 63.17 mmol) was weighed and dichloromethane (300 mL) was added, followed by N,N-dimethylformamide dimethyl acetal (9.03 g, 75.80 mmol). The mixture was reacted at 25°C for 16 hours. The mixture was cooled to 0°C and boron trifluoride etherate (10.76 g, 75.80 mmol, 9.32 mL) was added. The system was stirred at 0°C for an additional 1 hour. 200 mL of saturated sodium bicarbonate solution were added to the mixture. The organic phase was separated. The aqueous phase was extracted with 200 mL of dichloromethane. The extracted organic phases were combined and washed with 250 mL of saturated brine, dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (petroleum ether:ethyl acetate = 10:1 to 1:1) yielded compound 1-10. MS m / z = 612.1 [M+H]+. Step 10

[00261] Compound 1-10 (30 g, 49.05 mmol) was weighed and tetrahydrofuran (300 mL) was added, followed by lithium tri-sec-butylborohydride (1 M, 53.96 mL) at -60°C. The mixture was reacted at -60°C for 1 hour, rapidly cooled with 200 mL of water, and extracted with ethyl acetate (300 mL x 2). The extracted organic phases were combined, washed with 300 mL of saturated brine, dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Compound 1-11 was obtained by column chromatography (petroleum ether:ethyl acetate = 10:1 to 5:1). MS m / z = 614.1 [M+H]+. Step 11

[00262] Compound 1-11 (20 g, 32.59 mmol) was weighed and ethanol (200 mL) was added. 2-Methyl-2-thioisourea sulfate (27.22 g, 97.78 mmol) and sodium carbonate (6.91 g, 65.19 mmol) were then added and reacted at 50°C for 13 hours. The reaction mixture was concentrated to dryness. 40 mL of water were added and the mixture was extracted with ethyl acetate (50 Petition 870250110557, dated 02 / 12 / 2025, page 135 / 975 131 / 465 mL x 2). The extracted organic phases were combined, washed with 60 mL of saturated brine, and dried with anhydrous sodium sulfate. The mixture was filtered and concentrated under reduced pressure to obtain compound 1-12, MS m / z = 654.3 [M+H]+. Step 12

[00263] Compound 1-12 (21 g, 32.13 mmol) was weighed and DMF (200 mL) was added. N,N-diisopropylamine (12.46 g, 96.38 mmol, 16.79 mL) and N-phenyl-bis(trifluoromethanesulfonyl)imide (13.77 g, 38.55 mmol) were then added. The mixture was reacted at 25°C for 1 hour. 300 mL of water were added to the mixture and the mixture was extracted with ethyl acetate (300 mL x 3). The mixture was washed sequentially with water (2 x 400 mL) and saturated brine (400 mL), dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure. Compound 1-13 was obtained by column chromatography (petroleum ether:ethyl acetate = 10:1). Preparative SFC separation (Chromatographic column: DAICEL CHIRALPAK IG (250 mm*50 mm, 10 μm); mobile phase: [supercritical carbon dioxide-ethanol (0.1% ammonia)]; ethanol (0.1% ammonia) percentage: 25%-25%) yielded compound 1-13B.Chiral SFC analysis (Chromatographic column: ChiralPak IG-3 (100 mm*4.6 mm, 3 pm); mobile phase: [supercritical carbon dioxide-ethanol (diethylamine 0.05%)]; ethanol (diethylamine 0.05%) percentage: 5%-40%) revealed compound 1-13B with an Rt of 3.055 minutes and an ee value of 99%. Step 13

[00264] Compound 1-13B (200 mg, 254.53 μmol) and compound 114A (174.74 mg) were added to N,N-dimethylformamide (2 mL), followed by N,N-diisopropylamine (131.58 mg, 1.02 mmol). The resulting reaction mixture was heated to 105°C under nitrogen and stirred for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 1-14. MS m / z = Petition 870250110557, dated 02 / 12 / 2025, page 136 / 975 132 / 465 906.3 [M+H]+. Step 14

[00265] Compound 1-14 (120 mg, 132.45 μmol) was dissolved in dichloromethane (2 mL), followed by the addition of m-chloroperbenzoic acid (29.58 mg, 145.70 μmol, 85% purity). The resulting reaction mixture was stirred at 20°C under nitrogen for 2 hours. The reaction mixture was diluted with 30 mL of dichloromethane and then washed with 5 mL of saturated sodium bicarbonate solution and 5 mL of saturated brine. The organic phase was dried and concentrated under reduced pressure to yield compound 1-15. MS m / z = 922.7 [M+H]+. Step 15

[00266] Sodium tert-butoxide (23.97 mg, 249.46 μmol) and compound 1-2 (38.22 mg, 249.46 μmol) were added to tetrahydrofuran (1.5 mL) and stirred at 20°C for 0.5 hours. The solution of compound 1-15 (115 mg, 124.73 μmol) in tetrahydrofuran (1 mL) was then added to the mixture and stirred for a further 1 hour. The reaction mixture was pH adjusted to 7 with 0.5M hydrochloric acid, followed by the addition of 20 mL of ethyl acetate and 10 mL of water. The mixture was dissolved with stirring. The aqueous layer was separated. The organic phase was washed with 2 mL of saturated brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to produce compound 1-16. MS m / z = 1011.5 [M+H]+. Step 16

[00267] Compound 1-16 (120.00 mg, 118.68 μmol) was dissolved in tetrahydrofuran (2 mL). The resulting solution was cooled to 0°C and lithium aluminum tetrahydride (1 M, 118.68 μL) was added dropwise. The reaction was stirred for 0.5 hours. The reaction solution was carefully and rapidly cooled with 0.2 mL of water, followed by the addition of 0.5 g of anhydrous sodium sulfate and stirring for 2 minutes. The mixture was filtered through a layer of Celite, and the filtered cake was rinsed with 20 mL of Petition 870250110557, dated 02 / 12 / 2025, page 137 / 975 133 / 465 tetrahydrofuran. The filtrate was collected and concentrated under reduced pressure to produce compound 1-17. MS (ESI) m / z = 983.4 [M+H]+. Step 17

[00268] Compound 1-17 (120 mg, 122.06 pmol) was added to trifluoroacetic acid (2 mL) and stirred at 20°C for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by high-performance liquid chromatography HPLC column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (0.05% hydrochloric acid)-acetonitrile]; (acetonitrile): 10%-40%) and concentrated under reduced pressure to obtain the hydrochloride salt of compound 1. MS m / z = 643.3 [M+H]+. Example 2 Step 1

[00269] Compound 2-1 (2.3 g, 4.77 mmol) was dissolved in dioxane (30 mL), followed by the addition of hydrochloric acid (1 M, 14.30 mL). The mixture Petition 870250110557, dated 02 / 12 / 2025, page 138 / 975 134 / 465 of the resulting reaction was stirred at 20°C under nitrogen for 1 hour. The reaction mixture was concentrated under reduced pressure, and 20 mL of water and 50 mL of ethyl acetate were added to the residue and stirred until completely dissolved. The aqueous phase was separated. The organic phase was washed with 10 mL of 0.5 M hydrochloric acid. The aqueous phases were combined, the pH was adjusted to 10 with 20% sodium carbonate solution, and then extracted with dichloromethane (20 mL x 2). The organic phases were combined and concentrated under reduced pressure to produce compound 2-2. Step 2

[00270] To compound 2-2 (1.2 g, 4.77 mmol), 20 mL of dichloromethane was added, followed by Boc2O (2.08 g, 9.53 mmol). The mixture was stirred at 20°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) to give compound 2-3. 1H NMR (400 MHz, CDCl3) δ: 9.55 - 9.47 (m, 1H), 4.40-4.00 (m, 2H), 3.95 - 3.55 (m, 1H), 3.30 - 2.90 (m, 2H), 2.25 - 1.91 (m, 2H), 1.78 (s, 2H), 1.47 (s, 18H). Step 3

[00271] Potassium tert-butoxide (830.68 mg, 7.40 mmol) was added to ethylene glycol dimethyl ether (25 mL). The resulting mixture was cooled to -78°C, followed by the addition of ptoluenesulfonylmethyl isocyanide (794.91 mg, 4.07 mmol). After the addition, the reaction was stirred for 30 minutes. The solution of compound 2-3 (1.26 g, 3.70 mmol) in ethylene glycol dimethyl ether (25 mL) was then added dropwise. After the addition, the mixture was stirred for 30 minutes. The cooling bath was removed. The mixture was heated to room temperature (20°C) and stirred for 30 minutes. Finally, 40 mL of methanol were added, and the resulting reaction mixture was heated to 90°C and stirred for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a product. Petition 870250110557, dated 02 / 12 / 2025, page 139 / 975 135 / 465 crude. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 3:1) to obtain compound 2-4. 1H NMR (400MHz, CDCl3) δ: 4.22 (s, 1H), 3.65 - 3.55 (m, 2H), 3.30-2.62 (m, 4H), 1.99 - 1.89 (m, 2H), 1.65 - 1.30 (m, 20H). Step 4

[00272] Compound 2-4 (375 mg, 1.07 mmol) was dissolved in dichloromethane (2 mL), followed by the addition of trifluoroacetic acid (1.22 g, 10.67 mmol). The resulting reaction mixture was stirred at 20°C under nitrogen for 1 hour. The reaction mixture was concentrated under reduced pressure, and 20 mL of ethyl acetate were added to the residue. Then, 1 mL of a 4M hydrogen chloride / ethyl acetate solution was added, and the mixture was concentrated under reduced pressure to obtain the hydrochloride salt of compound 2-5. Step 5

[00273] Compound 1-13B (350 mg, 445.44 μmol) and the hydrochloride salt of compound 2-5 (299.51 mg) were added to N,N-dimethylformamide (3 mL), followed by N,N-diisopropylamine (460.56 mg, 3.56 mmol). Under nitrogen, the mixture was heated to 105°C with stirring for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product, which was dissolved in 50 mL of ethyl acetate and washed with saturated brine (10 mL x 2). The organic phase was dried and concentrated under reduced pressure to obtain compound 2-6. MS m / z = 787.2 [M+H]+. Step 6

[00274] Compound 2-6 (368 mg, 467.67 μmol) and N,N-diisopropylamine (120.89 mg, 935.34 μmol) were added to dichloromethane (3 mL), followed by Boc2O (153.10 mg, 701.51 μmol). The resulting reaction mixture was stirred at 20°C under nitrogen for 3 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:acetate of Petition 870250110557, dated 02 / 12 / 2025, page 140 / 975 136 / 465 ethyl = 3:1) to obtain compound 2-7. MS m / z = 887.4 [M+H]+. Step 7

[00275] Compound 2-7 (220 mg, 248.03 pmol) was dissolved in dichloromethane (2 mL), followed by the addition of m-chloroperbenzoic acid (50.35 mg, 248.03 pmol, 85% purity). The resulting reaction mixture was stirred at 20°C under nitrogen for 2 hours. The reaction mixture was concentrated under reduced pressure to produce compound 2-8. MS m / z = 903.6 [M+H]+. Step 8

[00276] Compound 1-2 (75.68 mg, 493.91 pmol) was dissolved in THF (2 mL), followed by the addition of sodium tert-butoxide (47.47 mg, 493.91 pmol). Under nitrogen, the reaction was stirred at 20°C for 1 hour. The solution of compound 2-8 (223 mg, 246.96 pmol) in tetrahydrofuran (1 mL) was then added. After the addition, the reaction was stirred at 20°C for 0.5 hour. The reaction solution was dissolved in 10 mL of ethyl acetate and washed with 5 mL of saturated brine. The organic phase was dried and filtered. The filtrate was concentrated under reduced pressure to yield compound 2-9, MS m / z = 992.5 [M+H]+. Step 9

[00277] Trifluoroacetic acid (2 mL) was added to compound 2-9 (214 mg, 215.70 pmol) and the resulting reaction mixture was stirred at 20°C for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (0.05% hydrochloric acid)-acetonitrile]; (acetonitrile): 10%-40%) and concentrated under reduced pressure to obtain the hydrochloride salt of compound 2. MS m / z = 652.2 [M+H]+. Example 3 Petition 870250110557, dated 02 / 12 / 2025, page 141 / 975 137 / 465 3A or 3B (isolated compound or mixture) Step 1

[00278] A borane solution in tetrahydrofuran (1 M, 21 mL) was added slowly, dropwise, to a solution of compound 3-1 (1.7 g, 5.18 mmol) in anhydrous THF (20 mL) at 0°C under nitrogen. The mixture was then stirred at 25°C for 12 hours. A 5% NaOH solution (26.31 mmol, 21 mL) was then added dropwise at 0°C, followed by the dropwise addition of hydrogen peroxide (4.88 g, 43.04 mmol, 4.14 mL, 30% purity). A Petition 870250110557, dated 02 / 12 / 2025, page 142 / 975 The 138 / 465 mixture was reacted at 25°C for 2 hours. The reaction mixture was rapidly cooled by the slow addition of 50 mL of saturated sodium sulfite solution and extracted with 50 mL of ethyl acetate. The organic phase was washed with 50 mL of brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 3:1) to give compound 3-2. MS m / z = 347.2 [M+H]+. Step 2

[00279] To a solution of compound 3-2 (1 g, 2.89 mmol) in anhydrous dioxane (10 mL), a solution of hydrochloric acid / dioxane (4 M, 10 mL) was added and the mixture was reacted at 20°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain the hydrochloride salt of compound 3-3. Step 3

[00280] Compound 3-4A (750 mg, 3.04 mmol) was dissolved in anhydrous DCM (10 mL). Then, triethylamine (584 mg, 5.77 mmol) and the hydrochloride salt of compound 3-3 (921 mg) were added and the reaction was carried out at 20°C for 1 hour. The resulting solution of compound 3-4 in dichloromethane was used directly in the next step. MS m / z = 457.2 [M+1]+. Step 4

[00281] To 10 mL of the solution of compound 3-4 in dichloromethane obtained in step 3, triethylsilyl chloride (871 mg, 5.78 mmol) and imidazole (590 mg, 8.67 mmol) were added, respectively. The mixture was reacted at 25°C for 12 hours. The reaction solution was diluted with 10 mL of water and extracted with 10 mL of dichloromethane. The organic phase was washed with 10 mL of brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by column chromatography (petroleum ether:ethyl acetate = 50:1) to obtain compound 3-5. MS m / z = 571.3 Petition 870250110557, dated 02 / 12 / 2025, page 143 / 975 139 / 465 [M+1]+. Step 5

[00282] To a solution of compound 3-5 (1.43 g, 2.50 mmol) in THF (20 mL), a solution of lithium aluminum hydride (2.5 M, 2.00 mL) in tetrahydrofuran at 0°C was slowly added. The reaction was allowed to proceed at 25°C for 5 hours. Ethyl acetate (10 mL) was then added dropwise to rapidly cool the reaction. The resulting suspension was filtered and the filtrate concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 20:1) to yield compound 3-6. MS m / z = 529.3 [M+1]+. Step 6

[00283] The compound tetramethylpiperidine (460 mg, 3.26 mmol) was dissolved in anhydrous tetrahydrofuran (1.0 mL) and cooled to -40°C under nitrogen, then n-butyllithium (2.5 M, 1.3 mL) was added dropwise. The reaction was stirred for 0.5 hours. Compound 3-6 (430 mg, 813 pmol) was dissolved in anhydrous tetrahydrofuran (0.5 mL) and added dropwise to the reaction flask at -60°C. After the addition was complete, the reaction was stirred for 0.5 hours. Finally, a solution of compound 1-8 (486 mg, 1.00 mmol) in anhydrous tetrahydrofuran (0.5 mL) was added to the reaction at -60°C. The mixture was then heated to 20°C and stirred for 2.5 hours. The reaction was rapidly cooled by the addition of 20 mL of water and extracted with ethyl acetate (20 mL). The organic phase was washed with 20 mL of brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product.The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) and separated by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 3:1) to obtain compound 3-7. MS m / z = 1014.5 [M+H]+. Step 7 Petition 870250110557, dated 02 / 12 / 2025, page 144 / 975 140 / 465

[00284] Compound 3-7 (70 mg, 69.0 μmol) was dissolved in anhydrous toluene (1.5 mL) and cyanomethylenetri-n-butylphosphine (150 mg, 621.50 μmol) was added. After nitrogen substitution, the reaction was stirred at 110°C for 12 hours. The reaction solution was cooled and concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 5:1) to give compound 3-8. MS m / z = 996.5 [M+H]+. Step 8

[00285] Compound 3-8 (22.5 mg, 22.58 μmol) was dissolved in anhydrous dichloromethane (0.5 mL). Meta-chloroperbenzoic acid (5 mg, 24.63 μmol, 85% purity) was added and stirred at 25°C for 12 hours. The reaction mixture was rapidly cooled by the addition of 4 mL of saturated sodium sulfite solution and extracted with dichloromethane (20 mL x 3). The organic phase was washed with 20 mL of brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 3-9, MS m / z = 1012.6 [M+H]+. Step 9

[00286] Compound 3-9 (19 mg, 18.8 μmol) was dissolved in anhydrous toluene (0.5 mL). Sodium tert-butoxide (7.22 mg, 75.1 μmol), 4A molecular sieves (10 mg), and compound 3-10A (12 mg, 75.08 μmol) were added. The reaction was stirred at 100°C for 12 hours. The reaction solution was cooled and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (ethyl acetate:methanol = 10:1) to obtain compound 3-10. MS m / z = 1107.7 [M+H]+. Step 10

[00287] Compound 3-10 (17 mg, 15.35 μmol) was dissolved in acid Petition 870250110557, dated 02 / 12 / 2025, page 145 / 975 141 / 465 trifluoroacetic acid (5 mL) and reacted at 20°C for 12 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative high-performance liquid chromatography (Chromatographic column: Phenomenex luna C18 150*25 mm*10 µm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 18%48%) to obtain the trifluoroacetic acid salts of compounds 3A and 3B.

[00288] Trifluoroacetate salt of compound 3A (compound alone or mixture), MS m / z = 635.3 [M+H]+. 1H NMR (CD3OD, 400 MHz) δ 6.94 (d, J = 8.50 Hz, 1 H), 5.71 - 5.50 (m, 1 H), 5.17 (br dd, J = 10.94; 4.06 Hz, 1 H), 4.80 (br d, J = 13.63 Hz, 2 H), 4.62 - 4.48 (m, 3 H), 4.17 - 3.73 (m, 7 H), 3.54 - 3.36 (m, 3 H), 3.31 - 3.25 (m, 1 H), 2.93 (br dd, J = 18.01; 3.75 Hz, 1 H), 2.77 - 2.48 (m, 3 H), 2.46 - 2.28 (m, 3 H), 2.26 - 2.12 (m, 1 H), 2.04 (s, 3 H), 1.96 (dd, J = 14.01, 4.13 Hz, 1 H).

[00289] Trifluoroacetate salt of compound 3B (isolated compound or mixture), MS m / z = 635.2 [M+H]+. 1H NMR (CD3OD, 400 MHz) δ 6.93 (d, J = 8.50 Hz, 1 H), 5.69 - 5.49 (m, 1 H), 5.30 (d, J = 13.88 Hz, 1 H), 5.18 (br dd, J = 1.19), 1.16 Hz; 4.87 - 4.78 (m, 2 H), 4.69 - 4.50 (m, 3 H), 4.29 (br d, J = 13.26 Hz, 1 H), 4.20 - 3.87 (m, 6 H), 3.63 (br d, J = 14.51 Hz, 13.3 Hz), H), 3.35 (br s, 1 H), 2.93 (br dd, J = 17.70; 3.56 Hz, 1 H), 2.77 - 2.51 (m, 3 H), 2.47 - 2.28 (m, 3 H), 2.26 - 2.12 (m, 3 H), (dd, J = 13.88; 4.25 Hz, 1 H). Example 4 Petition 870250110557, of 02 / 12 / 2025, p. 146 / 975 142 / 465 4-5A or 4-5 B 4-4A or 4-4 B 4-4B or 4-4A 4-5B or 4-5A 4-6A or 4-6 B 4-6B or 4-6A 4A or 4B 4B or 4A Step 1

[00290] Compound 1-13B (240 mg, 305.44 μmol) and compound 4-1A (97.26 mg, 458.16 μmol) were dissolved in DMF (5 mL). DIPEA (916.33 μmol, 159.61 pL) was added and stirred at 100°C for 1 hour. The mixture was extracted with 30 mL of ethyl acetate. The organic phase was washed with 50 mL of brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 4-1. MS m / z = 848.5 [M+H]+. Step 2

[00291] Compound 4-1 (200 mg, 235.86 pmol) was dissolved in dichloromethane (5 mL). Meta-chloroperbenzoic acid (40.70 mg, 235.86 pmol, 85% purity) was added and stirred at 25°C for 1 hour. The reaction solution was extracted with 5 mL of dichloromethane. The organic phase was washed with 10 mL of saturated sodium bicarbonate and dried with sodium sulfate. Petition 870250110557, dated 02 / 12 / 2025, page 147 / 975 143 / 465 anhydrous and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative thin-layer chromatography (dichloromethane:methanol = 10:1) to obtain compound 4-2. MS m / z = 864.3 [M+H]+. Step 3

[00292] Compound 4-3 (610 mg, hydrochloride) was dissolved in acetonitrile (10 mL), and potassium carbonate (1.46 g, 10.6 mmol) and potassium iodide (35.1 mg, 212 μmol) were added. The reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) and then separated by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compounds 4-4A and 4-4B. Compound 4-4A (petroleum ether:ethyl acetate = 1:1, Rf = 0.21) showed an MS m / z of 216.0 [M+1]+ and compound 4-4B (petroleum ether:ethyl acetate = 1:1, Rf = 0.12) showed an MS m / z of 216.1 [M+1]+.

[00293] Compound 4-4A: 1H NMR (400 MHz, CDCl3) δ ppm 3.75 (s, 3H), 3.54 (dd, J = 6.5; 9.0 Hz, 1H), 3.33 (tt, J = 6.4; 10.6 Hz, 1H), 3.13 (td, J = 6.4; 10.8Hz, 1H), 2.86 - 2.75 (m, 2H), 2.52 (t, J = 9.6Hz, 1H), 2.30 - 2.18 (m, 1H), 2.15 (s, 3H), 1.99 - 1.81 (m, 3H), 1.61 (dd, J = 11.3; 12.6Hz, 1H); compound 4-4B: 1H NMR (400 MHz, CDCl3) δ ppm 3.67 (s, 3H), 3.28 - 3.08 (m, 2H), 3.06 - 2.92 (m, 2H), 2.56 (td, J = 7.4; 9.5 Hz, 1H), 2.37 - 2.17 (m, 2H), 2.09 (dd, J = 6.9; 13.2 Hz, 1H), 2.04 (s, 3H), 1.79 - 1.69 (m, 2H), 1.67 1.56 (m, 1H). Step 4

[00294] Compound 4-4A (102 mg, 474 μmol) was dissolved in THF (5.0 mL). Lithium aluminum tetrahydride (2.5 M, 0.3 mL) was added dropwise at 0°C. The reaction mixture was heated to 25°C and allowed to react for 1 hour. Water (0.03 mL), 15% aqueous sodium hydroxide (0.03 mL), and water (0.1 mL) were added. Petition 870250110557, dated 02 / 12 / 2025, page 148 / 975 144 / 465 mL) were then added dropwise at 0°C, followed by stirring for 0.5 hours. The mixture was filtered. The filtered cake was washed with 10 mL of ethyl acetate and the filtrate concentrated under reduced pressure to produce compound 4-5A. MS m / z = 188.1 [M+1]+. Step 5

[00295] Compound 4-2 (120 mg, 139 pmol), compound 4-5A (89 mg, 475 pmol), 4A molecular sieves (120 mg) and sodium tert-butoxide (80 mg, 832 pmol) were added to toluene (15 mL) and heated to 100°C for 6 hours. The reaction mixture was filtered. The filtered cake was washed with 10 mL of ethyl acetate and the filtrate concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (dichloromethane:methanol = 10:1) to obtain compound 4-6A, MS m / z = 987.4 [M+1]+. Step 6

[00296] Compound 4-6A (81 mg, 82.0 pmol) was dissolved in dichloromethane (10.0 mL) and trifluoroacetic acid (3.07 g, 26.9 mmol, 2 mL) was added. The reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 15%-45%) to obtain the trifluoroacetate salt of compound 4A. MS m / z = 647.3 [M+1]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.94 (d, J = 8.5 Hz, 1H), 5.21 (br dd, J = 3.9; 11.1 Hz, 1H), 4.79 - 4.49 (m, 4H), 4.47 - 4.32 (m, 1H), 4.24 - 4.02 (m, 3H), 3.86 (br d, J = 13.9 Hz, 1H), 3.76 - 3.65 (m, 2H), 3.65 - 3.55 (m, 1H), 3.54 - 3.46 (m, 1H), 3.41 - 3.35 (m, 1H), 3.20 - 3.08 (m, 1H), 3.01 - 2.89 (m, 1H), 2.71 (br dd, J = 6.5; 13.4 Hz, 1H), 2.41 - 2.19 (m, 8H), 2.19 - 1.90 (m, 8H). Step 7

[00297] Compound 4-4B (51 mg, 237 pmol) was dissolved in THF Petition 870250110557, dated 02 / 12 / 2025, page 149 / 975 145 / 465 (3.0 mL). Lithium aluminum tetrahydride (2.5 M, 0.15 mL) was added dropwise at 0°C. The reaction mixture was heated to 25°C and allowed to react for 1 hour. Water (0.02 mL), 15% aqueous NaOH (0.02 mL), and water (0.06 mL) were then added dropwise at 0°C, followed by stirring for 0.5 hours. The mixture was filtered. The filtered cake was washed with 10 mL of ethyl acetate, and the filtrate was concentrated under reduced pressure to yield compound 4-5B. MS m / z = 188.2 [M+1]+. Step 8

[00298] Compound 4-2 (100 mg, 116 μmol), compound 4-5B (41 mg, 219 pmol), molecular sieves of 4A (70 mg) and sodium tert-butoxide (80 mg, 832 pmol) were added to toluene (15 mL) and heated to 100°C for 6 hours. The reaction mixture was filtered. The filtered cake was washed with 10 mL of ethyl acetate and the filtrate concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (dichloromethane:methanol = 20:1) to obtain compound 4-6B, MS m / z = 987.4 [M+1]+. Step 9

[00299] Compound 4-6B (70 mg, 70.9 pmol) was dissolved in dichloromethane (10.0 mL) and trifluoroacetic acid (3.07 g, 26.9 mmol, 2 mL) was added. The reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 15%-45%) to obtain the trifluoroacetate salt of compound 4B. MS m / z = 647.3 [M+1]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.94 (d, J = 8.5 Hz, 1H), 5.21 (br dd, J = 4.1; 10.6 Hz, 1H), 4.78 - 4.64 (m, 4H), 4.54 (br d, J = 11.8 Hz, 1H), 4.42 - 4.32 (m, 1H), 4.21 - 4.11 (m, 2H), 3.88 - 3.54 (m, 6H), 3.40 - 3.34 (m, 2H), 2.96 (br dd, J = 4.0; 17.9 Hz, 1H), 2.55 - 2.37 (m, 2H), 2.36 - 1.89 (m, 14H). Petition 870250110557, dated 02 / 12 / 2025, page 150 / 975 146 / 465 Example 5 Step 1

[00300] Compound 5-1 (10.0 g, 43.5 mmol) was dissolved in DMF (4 mL), followed by the addition of potassium carbonate (15.0 g, 109 mmol) and p-methoxybenzyl chloride (16.3 g, 104 mmol, 14.2 mL). The reaction mixture was allowed to react at 80°C for 12 hours. After the reaction mixture had cooled to room temperature, 200 mL of ethyl acetate were added to the reaction mixture. The mixture was washed with 200 mL of water and 100 mL of saturated brine, dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate). Petition 870250110557, dated 02 / 12 / 2025, page 151 / 975 147 / 465 ethyl = 30:1) to obtain compound 5-2. 1H NMR (400 MHz, CDCI3) δ ppm 7.48 (t, J = 1.31 Hz, 1H), 7.41 (dd, J = 2.38; 1.13 Hz, 1H), 7.13 (d, J = 8.50 Hz, 4H), 7.06 - 7.02 (m, 1H), 6.92 - 6.83 (m, 4H), 4.56 (s, 4H), 3.86 (s, 3H) 3.81 (s, 6H). Step 2

[00301] Compound 5-2 (17.5 g, 37.2 mmol) was dissolved in anhydrous THF (200 mL). LiAlH4 (2.5 M, 30 mL) was then added at 0°C, followed by reaction at 25°C for 1 hour. The reaction mixture was cooled to room temperature, and 2.85 mL of H2O, 2.85 mL of 15% aqueous NaOH, and 8.6 mL of H2O were slowly added dropwise under a stream of nitrogen. The resulting solid was filtered, and the filtrate was concentrated under reduced pressure to produce compound 5-3. 1H NMR (400 MHz, CDCL) δ ppm 7.03 (d, J = 8.63 Hz, 4H), 6.82 - 6.67 (m, 6H), 6.57 (s, 1H), 4.44 (s, 6H), 3.71 (s, 6H). Step 3

[00302] Compound 5-3 (15.0 g, 33.9 mmol) was dissolved in THF (150 mL). The atmosphere was replaced with nitrogen three times and MnO2 (60.0 g, 690 mmol) was added. After reacting at 75°C for 12 hours, the reaction solution was cooled and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 20:1) to obtain compound 5-4. 1H NMR (400 MHz, CDCl3) δ ppm 9.79 (s, 1H), 7.16 - 7.09 (m, 6H), 6.92 - 6.86 (m, 5H), 4.59 (s, 4H), 3.81 (s, 6H). Step 4

[00303] Compound 5-4 (7.20 g, 16.4 mmol), 1-propynyltri-n-butyltin (5.38 g, 16.4 mmol) and dichlorobis(di-tert-butyl-(4-dimethylaminophenyl)phosphine)palladium(II) (57.9 mg, 81.8 pmol) were dissolved in anhydrous toluene (170 mL). The atmosphere was purged with nitrogen three times and the mixture reacted at 110°C for 12 hours. The reaction solution was Petition 870250110557, dated 02 / 12 / 2025, page 152 / 975 148 / 465 concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 10:1) to obtain compound 5-5. MS m / z = 400.3 [M+H]+, 1H NMR (400 MHz, CDCl3) δ ppm 9.82 (s, 1H), 7.21 (s, 1H), 7.18 - 7.15 (m, 1H), 7.12 (d, J = 8.63 Hz, 4H), 7.03 - 7.01 (m, 1H), 6.87 (d, J = 8.63 Hz, 4H), 4.58 (s, 4H), 3.81 (s, 6H), 2.02 (s, 3H). Step 5

[00304] Compound 5-5 (4.60 g, 11.5 mmol) was dissolved in anhydrous DMF (50 mL) and NBS (2.25 g, 12.7 mmol) was added. The mixture was allowed to react at room temperature for 0.5 hours. Water (150 mL) was added to the organic phase and the mixture was extracted three times with ethyl acetate (50 mL). The organic phase was washed three times with saturated brine (50 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 10:1) to obtain compound 5-6. MS m / z = 478.2 [M+H]+. 1H NMR (400 MHz, CDCl3) δ ppm 10.31 (s, 1H), 7.24 (d, J = 3.38 Hz, 1H), 7.10 (d, J = 8.63 Hz, 4H), 7.05 (d, J = 3.38 Hz, 1H), 6.89 - 6.83 (m, 4H), 4.55 (s, 4H), 3.80 (s, 6H), 2.09 (s, 3H). Step 6

[00305] Compound 5-6 (5.30 g, 11.1 mmol), cuprous iodide (4.22 g, 22.2 mmol), and methyl 2,2-difluoro-2-fluorosulfonylacetate (8.09 g, 42.1 mmol) were dissolved in DMF (50 mL). The atmosphere was purged with nitrogen three times, and the mixture was reacted at 110°C for 2.5 hours. The reaction solution was cooled, filtered through celite, and water (150 mL) was added to the organic phase. The mixture was extracted three times with 150 mL of ethyl acetate. The organic phase was washed three times with saturated brine (150 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified. Petition 870250110557, dated 02 / 12 / 2025, page 153 / 975 149 / 465 por chromatografia em column (petroleum ether: ethyl acetate = 20:1) to provide compound 5-7. MS m / z = 468.2 [M+H] + . 1H NMR (400 MHz, CDCl3) δ ppm 10.30 (q, J = 2.71 Hz, 1H), 7.25 (d, J = 2.75 Hz, 1H), 7.10 (d, J = 8.63 Hz, 4H), 7.00 (d, J = 2.88 Hz, 1H), 6.90 - 6.85 (m, 4H), 4.60 (s, 4H), 3.81 (s, 6H), 2.05 (d, J = 4.13 Hz, 3H). Stage 7

[00306] TMP (2.45 g, 17.4 mmol, 2.94 mL) was dissolved in THF (20 mL). The atmosphere was purged with nitrogen three times. The temperature was reduced to -40°C and n-BuLi (2.5 M, 6.71 mL) was added slowly, drop by drop. After the addition was complete, the mixture was allowed to react at -40°C for 30 minutes. The reaction system was then cooled to -60°C, and the 5-7A solution (2.20 g, 5.78 mmol) in THF (20 mL) was added slowly, drop by drop, to the reaction mixture. After reacting at -40°C for 15 minutes, compound 57 (3.94 g, 6.94 mmol) was added portion by portion to the reaction mixture, and the mixture was reacted at room temperature for 2 hours. The reaction mixture was rapidly cooled with saturated aqueous ammonium chloride (100 mL) and extracted twice with ethyl acetate (100 mL). The organic phase was washed twice with saturated brine (100 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product.The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 2:1) to obtain compound 5-8. MS m / z = 848.4 [M+H]+. 1H NMR (400 MHz, CDCf) δ ppm 7.15 - 6.99 (m, 5H), 6.79 (d, J = 8.63 Hz, 4H), 6.75 (br d, J = 2.38 Hz, 1H), 5.39 (br d, J = 8.63 Hz, 1H), 4.84 - 4.40 (m, 5H), 4.38 - 4.12 (m, 5H), 3.72 (s, 6H), 3.42 - 3.11 (m, 2H), 3.06 - 2.86 (m, 1H), 2.70 - 2.51 (m, 1H), 2.40 (s, 3H), 2.36 - 2.23 (m, 1H), 1.94 (s, 2H), 1.85 - 1.74 (m, 3H), 1.66 (br d, J = 9.13 Hz, 1H), 1.42 (s, 9H). Step 8

[00307] Compound 5-8 (324 mg, 390 μmol) was dissolved in toluene. Petition 870250110557, dated 02 / 12 / 2025, page 154 / 975 150 / 465 anhydrous (23 mL) and tributyl cyanomethylene phosphate (1.30 g, 5.40 mmol) was added. The atmosphere was then purged with nitrogen three times and the mixture reacted at 110°C for 12 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 10:1), separated by high-performance preparative liquid chromatography (Phenomenex luna C18 column 150*25 mm*10 μm; mobile phase: [water (0.05% hydrochloric acid)-acetonitrile]; (acetonitrile): 55%-85%) and concentrated under reduced pressure to obtain the hydrochloride salt of compound 5-9, MS m / z = 830.5 [M+H]+. Step 9

[00308] Compound 5-9 (324 mg, hydrochloride) was dissolved in anhydrous dichloromethane (3 mL) and m-chloroperbenzoic acid (83.2 mg, 410 pmol, 85% purity) was added. The mixture was allowed to react at room temperature for 0.5 hours. The reaction solution was concentrated under reduced pressure. Sodium bicarbonate (10 mL) and sodium sulfite (10 mL) were added for rapid cooling. The mixture was extracted twice with DCM (50 mL), washed with 50 mL of saturated brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure to obtain compound 5-10. MS m / z = 846.5 [M+H]+. Step 10

[00309] Compound 5-10 (280 mg, 331 μmol) was dissolved in anhydrous toluene (20 mL). Molecular sieves of 4A (150 mg, 2.34 mmol), compound 1-2 (203 mg, 1.32 mmol) and sodium tert-butoxide (127 mg, 1.32 mmol) were added and the mixture was reacted at 100°C for 12 hours. The reaction mixture was filtered and concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (dichloromethane:methanol = 20:1) and separated by preparative high-performance liquid chromatography (Phenomenex luna C18 150*30 mm*10 μm; Petition 870250110557, dated 02 / 12 / 2025, page 155 / 975 151 / 465 Mobile phase: [water (formic acid 0.225%)-acetonitrile]; (acetonitrile): 48%-78%). The mixture was then concentrated under reduced pressure to obtain the formate salt of compound 5-11. MS m / z = 935.7 [M+H]+. The residue was then subjected to preparative SFC separation (chiral column: DAICEL CHIRALCEL OD (250 mm*30 mm, 10 pm); mobile phase: [supercritical carbon dioxide-acetonitrile / isopropanol (ammonia 0.1%)]; acetonitrile / isopropanol (ammonia 0.1%): 45%-45%), and concentrated under reduced pressure to obtain compounds 5-11A and 5-11B. After analytical SFC (chiral column: DAICEL CHIRALCEL OD-3 (50 mm*4.6 mm, 3 pm); mobile phase: [supercritical carbon dioxide-methanol (diethylamine 0.05%)]; methanol (diethylamine 0.05%)%: 40%), compound 5-11A showed an Rt of 0.657 minutes and an ee value of 99%; MS m / z = 935.6[M+H]+; compound 5-11B showed an Rt of 1.848 minutes and an ee value of 99%, MS m / z = 935.5 [M+H]+. Step 11

[00310] Compound 5-11A (105 mg, 112 pmol) was dissolved in TFA (1 mL) and reacted at 50°C for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product, which was separated by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 12%-42%) and lyophilized to obtain the trifluoroacetate salt of compound 5A. MS m / z = 595.4 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.96 (d, J = 2.4 Hz, 1H), 6.75 (d, J = 2.4 Hz, 1H), 5.34 - 5.28 (m, 2H), 5.11 (dd, J = 2.8; 10.8 Hz, 1H), 4.99 - 4.92 (m, 1H), 4.82 - 4.75 (m, 1H), 4.57 (d, J = 1.6 Hz, 2H), 4.44 - 4.30 (m, 2H), 4.21 - 4.11 (m, 2H), 3.96 - 3.83 (m, 2H), 3.81 - 3.66 (m, 2H), 3.33 (br s, 1H), 3.24 (td, J = 7.2; 11.6 Hz, 1H), 3.05 (br s, 1H), 3.03 - 2.98 (m, 1H), 2.87 - 2.74 (m, 2H), 2.41 - 2.32 (m, 1H), 2.30 - 2.19 (m, 2H), 2.18 - 2.05 (m, 4H), 2.05 - 1.93 (m, 4H).

[00311] Compound 5-11B (110 mg, 118 pmol) was dissolved in TFA (1 mL) and reacted at 50°C for 2 hours. The reaction solution was concentrated under Petition 870250110557, dated 02 / 12 / 2025, p. 156 / 975 152 / 465 reduced pressure to obtain a crude product, which was separated by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 12%-42%) and lyophilized to obtain the trifluoroacetate salt of compound 5B. MS m / z = 595.4 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.97 (d, J = 2.4 Hz, 1H), 6.76 (d, J = 2.4 Hz, 1H), 5.30 (br d, J = 8.0 Hz, 2H), 5.11 (br dd, J = 10.8; 2.8 Hz, 1H), 4.98 - 4.94 (m, 1H), 4.84 - 4.77 (m, 1H), 4.66 - 4.55 (m, 2H), 4.46 (br d, J = 14.0 Hz, 1H), 4.34 (br d, J = 14.0 Hz, 1H), 4.17 (br d, J = 16.0 Hz, 2H), 3.96 - 3.85 (m, 2H), 3.82 - 3.68 (m, 2H), 3.37 (br d, J = 14.0 Hz, 1H), 3.23 (td, J = 7.2; 11.6 Hz, 1H), 3.03 (br d, J = 16.4 Hz, 2H), 2.89 - 2.75 (m, 2H), 2.42 - 2.33 (m, 1H), 2.28 - 2.20 (m, 2H), 2.20 - 2.09 (m, 4H), 2.06 - 1.93 (m, 4H). Example 7 Step 1

[00312] Compound 7-1 (1.20 g, 1.26 mmol) was dissolved in anhydrous toluene (12.0 mL), followed by the addition of tributyl(trimethylsilylethinyl)tin (2.94 g, 7.58 mmol) and dichlorobis[di-tert-butyl-(4-dimethylaminophenyl)phosphine]palladium(II) (537 mg, 758 pmol). The reaction was Petition 870250110557, dated 02 / 12 / 2025, page 157 / 975 153 / 465 allowed to proceed at 110°C for 20 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 2:1) to obtain compound 7-1. MS m / z = 1011.6 [M+1]+. Step 2

[00313] Compound 7-2 (1.00 g, 989 pmol) was dissolved in anhydrous tetrahydrofuran (10.0 mL), followed by the addition of tetrabutylammonium fluoride (1 M, 989 pL). The mixture was reacted at 25°C for 4 hours. 30.0 mL of water were added to the reaction solution and the mixture was extracted with ethyl acetate (150 mL). The organic phase was dried and concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 7-2. MS m / z = 939.6 [M+1]+. Step 3

[00314] Compound 7-2 (310 mg, 330.12 pmol) was dissolved in anhydrous acetone (5 mL), followed by the addition of AgNOs (350 mg, 2.06 mmol) and NCS (220.41 mg, 1.65 mmol). The reaction was allowed to proceed at 25°C for 10 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (dichloromethane:methanol = 10:1) to obtain compound 7-3. MS m / z = 973.4 [M+1]+. Step 4

[00315] Compound 7-3 (120 mg, 12.3 pmol) was dissolved in dichloromethane (1 mL) and trifluoroacetic acid (153 mg, 1.35 mmol, 0.1 mL) was added. The mixture was reacted at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 18%-48%) and lyophilized. Petição 870250110557, de 02 / 12 / 2025, pág. 158 / 975 154 / 465 para obter o sal trifluoroacetato do composto 7. MS m / z = 633,2[M+1]+. RMN 1H (400 MHz, CD3OD) δ ppm 7,00 (d, J = 8,5 Hz, 1H), 5,33 - 5,30 (m, 2H), 5,21 - 5,18 (m, 1H), 4,85 (s, 4H), 4,76 - 4,71 (m, 1H), 4,54 (s, 2H), 4,35 - 4,30 (m, 2H), 4,17 - 4,12 (m, 2H), 3,93 (d, J = 14,0 Hz, 1H), 3,86 - 3,70 (m, 2H), 3,68 - 3,64 (m, 1H), 3,07 - 2,88 (m, 2H), 2,82 - 2,73 (m, 1H), 2,37 - 2,29 (m, 1H), 2,28 - 2,18 (m, 2H), 2,17 - 2,05 (m, 4H), 2,01 - 1,92 (m, 1H). Exemplo 8 μ8A ou 8B8B ou 8A Etapa 1

[00316] Compound 1-13B (100 mg, 127 μmol), compound 8-1 (63.4 mg, 280 μmol), and triethylamine (509 μmol, 70.9 μL) were dissolved in DMF (1.00 mL). The atmosphere was purged with nitrogen three times, and the mixture was reacted at 50°C for 6 hours. 10.0 mL of water were added to the reaction solution, and the mixture was extracted three times with ethyl acetate (20.0 mL). The organic phase was washed with saturated brine (50.0 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 3:1) to obtain compound 8-2. MS m / z = 862.4 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, page 159 / 975 155 / 465 Step 2

[00317] Compound 8-2 (600 mg, 69.6 μmol) was dissolved in anhydrous dichloromethane (1.00 mL). Meta-chloroperbenzoic acid (15.5 mg, 76.6 μmol, 85.0% purity) was added portion by portion at 0°C. The mixture was allowed to react at room temperature for 1 hour. 10.0 mL of sodium bicarbonate solution and 10.0 mL of sodium sulfite solution were added to the reaction solution, and the mixture was extracted three times with dichloromethane (30.0 mL). The organic phase was washed with saturated brine (50.0 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (petroleum ether:ethyl acetate = 2:1) to obtain compound 8-3. MS m / z = 878.3 [M+H]+. Step 3

[00318] Compound 8-3 (350 mg, 39.9 μmol) was dissolved in anhydrous toluene (1.00 mL). Compound 1-2 (12.2 mg, 79.7 μmol), sodium tert-butoxide (15.3 mg, 159 μmol), and 4A molecular sieves (180 mg) were added. After the atmosphere was replaced with nitrogen, the mixture was reacted at 100°C for 6 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (pure ethyl acetate) to obtain compound 8-4. MS m / z = 967.4 [M+H]+. Step 4

[00319] Compound 8-4 (300 mg, 31.0 μmol) was dissolved in anhydrous dichloromethane (0.5 mL) and trifluoroacetic acid (1.35 mmol, 100 μL) was added. The mixture was allowed to react at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product, which was then separated by high-performance preparative liquid chromatography (Phenomenex luna C18 150*25 mm*10 μm column; mobile phase: [water (0.075% trifluoroacetic acid)-acetonitrile]; Petition 870250110557, dated 02 / 12 / 2025, page 160 / 975 156 / 465 acetonitrile: 16%-46%). After lyophilization, trifluoroacetic acid salts of compounds 8A and 8B were obtained.

[00320] Sal trifluoroacetato do composto 8A: MS m / z = 627,3 [M+H]+, RMN 1H (400 MHz, CD3OD) δ ppm 6,92 (d, J = 8,5 Hz, 1H), 5,31 (br d, J = 8,5 Hz, 2H), 5,19 (br dd, J = 3,6; 11,8 Hz, 1H), 4,97 - 4,93 (m, 1H), 4,73 (br d, J = 14,6 Hz, 1H), 4,65 - 4,45 (m, 2H), 4,34 (br d, J = 14,4 Hz, 1H), 4,14 (br d, J = 5,5 Hz, 1H), 4,03 - 3,89 (m, 3H), 3,81 - 3,70 (m, 1H), 3,42 - 3,34 (m, 1H), 3,29 - 3,23 (m, 1H), 3,22 - 3,15 (m, 1H), 3,07 - 2,91 (m, 3H), 2,81 (br d, J = 16,0 Hz, 1H), 2,36 (br dd, J = 5,9; 11,4 Hz, 2H), 2,31 - 2,10 (m, 5H), 2,06 - 1,93 (m, 4H), 1,15 (d, J = 6,0 Hz, 3H). 5.10 - 4.99 (m, 2H), 4.75 (s, 1H), 4.57 (s, 2H), 4.33 (br d, J = 14.3 Hz, 1H), 4.21 - 4.09 (m, 1H), 3.98 - 3.84 (m, 3H), 3.82 - 3.71 (m, 1H), 3.45 (br dd, J = 11.2, 17.7 Hz, 1H), 3.28 - 3.18 (m, 2H), 3.15 - 3.01 (m, 2H), 2.92 - 2.77 (m, 2H), 2.40 - 2.11 (m, 7H), 2.03 - 1.92 (m, 4H), 1.02 (d, J = 6.3 Hz, 3H). Example 9 Petition 870250110557, on 12 / 02 / 2025, page. 161 / 975 157 / 465 9-2A or 9-2B 9-4A or 9-4B 9-2B or 9-2A 9-3A or 9-3B 9A or 9B 9B or 9A Etapa 1

[00322] Compound 1-13B (49.0 mg, 62.4 pmol) and compound 9-1 (480 mg, 187 pmol) were dissolved in dichloromethane (1.00 mL). N,N-diisopropylamine (54.3 pL) was added and the reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 10:1) to obtain compound 9-2. MS m / z = 892.4 [M+1]+. Preparative SFC separation was then performed (chiral column: (s,s) WHELK-O1 (250 mm*30 mm, 10 pm); mobile phase: [supercritical carbon dioxide-acetonitrile / isopropanol (0.1% ammonia)]; acetonitrile / isopropanol (0.1% ammonia): 50%-50%). After concentration under reduced pressure, compounds 9-2A and 9-2B were obtained.SFC analytical: (chiral column: (s,s) WHELK-O1 (50 mm*4.6 mm, 3.5 pm); mobile phase: [supercritical carbon dioxide-isopropanol (diethylamine 0.05%)]; isopropanol (diethylamine 0.05%)%: 40%), compound 9-2A, Rt = 1.768 min, 99% ee; MS m / z = 892.4 [M+H]+; compound 9-2B, Rt = 2.286 min, 99% ee, MS m / z = 892.4 [M+H]+. Step 2

[00323] Compound 9-2A (300 mg, 33.6 pmol) was dissolved in dichloromethane (1.00 mL) and m-chloroperbenzoic acid (8.19 mg, Petition 870250110557, dated 02 / 12 / 2025, page 162 / 975 158 / 465 40.4 pmol. 85.0% purity). The reaction mixture was reacted at 25°C for 2 hours. The reaction mixture was rapidly cooled with a saturated sodium sulfite solution. The organic phase was collected and concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 9-3A. m / z = 908.4 [M+1]+.

[00324] Referring to step 2, compound 9-2B was used as the starting material instead of compound 9-2A to obtain compound 9-3B. m / z = 908.4 [M+1]+. Step 3

[00325] Compound 9-3A (120 mg, 13.2 μmol), compound 1-2 (6.07 mg, 39.7 pmol), sodium tert-butoxide (3.81 mg, 39.7 μmol) and 4A molecular sieves (120 mg) were added to toluene (1.00 mL). The reaction mixture was reacted at 110°C for 12 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 9-4A. MS m / z = 997.6 [M+1]+.

[00326] Referring to step 3, compound 9-3B was used as the starting material instead of compound 9-3A to obtain compound 9-4B. MS m / z = 997.6 [M+1]+. Step 4

[00327] Compound 9-4A (100 mg, 10.0 μmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was reacted at 25°C for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 μm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 15%-45%) to obtain the salt. Petition 870250110557, dated 02 / 12 / 2025, page 163 / 975 159 / 465 9A trifluoroacetate. MS m / z = 657.4 [M+1]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.97 - 6.92 (m, 1H), 5.33 (br d, J = 7.8 Hz, 2H), 5.28 - 5.17 (m, 1H), 4.76 - 4.72 (m, 1H), 4.56 (s, 2H), 4.41 - 4.28 (m, 2H), 4.22 - 4.15 (m, 1H), 3.99 - 3.91 (m, 1H), 3.79 - 3.63 (m, 5H), 3.52 - 3.48 (m, 3H), 3.35 (br d, J = 1.8 Hz, 1H), 3.31 - 3.23 (m, 3H), 3.09 - 2.79 (m, 3H), 2.40 - 2.10 (m, 6H), 2.04 (s, 3H), 2.01 - 1.88 (m, 2H).

[00328] Compound 9-4B (13.0 mg, 13.0 pmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was reacted at 25°C for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by preparative high-performance liquid chromatography (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 15%45%) to obtain the trifluoroacetate salt of 9B. MS m / z = 657.5 [M+1]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.94 (d, J = 8.5 Hz, 1H), 5.33 (br d, J = 7.6 Hz, 2H), 5.26 - 5.18 (m, 1H), 4.78 - 4.73 (m, 1H), 4.57 (s, 2H), 4.39 - 4.28 (m, 2H), 4.17 - 4.12 (m, 1H), 3.94 (br d, J = 14.4 Hz, 1H), 3.85 - 3.63 (m, 5H), 3.50 (s, 3H), 3.41 - 3.34 (m, 2H), 3.31 - 3.21 (m, 2H), 3.09 - 2.78 (m, 3H), 2.41 - 2.12 (m, 6H), 2.04 (s, 3H), 2.02 - 1.91 (m, 2H). Example 10 Petition 870250110557, dated 02 / 12 / 2025, page 164 / 975 160 / 465 Step 1

[00329] Compound 1-13B (49.0 mg, 62.4 μmol) and compound 10-1 (480 mg, 187 pmol) were dissolved in dichloromethane (1.00 mL). N,N-diisopropylamine (40.3 mg, 312 μmol, 54.3 μL) was added and the reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated directly to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 10-2. MS m / z = 894.4 [M+1]+. Step 2

[00330] Compound 10-2 (50.0 mg, 55.9 μmol) was dissolved in dichloromethane (1.00 mL) and m-chloroperbenzoic acid (13.6 mg, 67.1 μmol, 85.0% purity) was added. The reaction mixture was reacted at 25°C for 1 hour. The reaction mixture was rapidly cooled with a saturated sodium sulfite solution, and the aqueous phase was extracted with dichloromethane (10.0 mL x 2). The organic phase was collected and concentrated to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 10-3. m / z = 910.3 [M+1]+. Petition 870250110557, dated 02 / 12 / 2025, pages 165 / 975 161 / 465 Step 3

[00331] Compound 10-3 (300 mg, 32.9 pmol), compound 1-2 (15.2 mg, 98.9 pmol), sodium tert-butoxide (9.50 mg, 98.9 pmol) and 4A molecular sieves (300 mg) were added to toluene (1.00 mL). The reaction mixture was reacted at 110°C for 12 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 10-4. MS m / z = 999.6 [M+1]+. Step 4

[00332] Compound 10-4 (250 mg, 25.0 pmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was allowed to react at 25°C for 1 hour. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 12%-42%) to obtain the trifluoroacetate salt. MS m / z = 659.3 [M+1]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.92 (d, J = 8.5 Hz, 1H), 5.54 - 5.52 (m, 1H), 5.31 (br d, J = 7.6 Hz, 2H), 5.23 - 5.13 (m, 1H), 4.94 - 4.90 (m, 1H), 4.85 - 4.63 (m, 5H), 4.62 - 4.25 (m, 4H), 4.23 - 4.11 (m, 1H), 3.97 - 3.67 (m, 4H), 3.40 - 3.33 (m, 1H), 3.28 - 3.22 (m, 1H), 3.10 - 2.89 (m, 2H), 2.80 (br d, J = 15.9 Hz, 1H), 2.44 - 2.33 (m, 2H), 2.27 - 2.11 (m, 5H), 2.02 (s, 3H), 1.98 - 1.91 (m, 1H). Example 11 Petition 870250110557, on 12 / 02 / 2025, page. 166 / 975 162 / 465 11-1A or 11-1B 11-1B or 11-1A 11-2A or 11-2B 11-2B or 11-2A 11-3A or 11-3B 11-3B or 11-3A 11-4A or 11-4B 11-4B or 11-4A 11-5A or 11-5B 11-5B or 11-5A 11A or 11B 11B or 11A Etapa 1

[00333] Compound 11-1 was subjected to preparative SFC separation (chiral column: DAICEL CHIRALPAK AD (250 mm*30 mm, 10 pm; mobile phase: [supercritical carbon dioxide - acetonitrile / isopropanol (ammonia 0.1%)]; acetonitrile / isopropanol (ammonia 0.1%): 30%30%). After concentration under reduced pressure, compounds 11-1A and 11-1B were obtained. Analytical SFC: (chiral column: DAICEL CHIRALPAK AD (50 mm*4.6 mm, 3 pm); mobile phase: [supercritical carbon dioxide - isopropanol (diethylamine 0.05%)]; isopropanol (diethylamine 0.05%)%: 5%40%), compound 11-1A, Rt = 1.308 min, 99% ee; MS m / z = 503.2 [M+Na]+; compound 11-1B, Rt = 1.499 min, 99% ee, MS m / z = 503.2 [M+Na]+. Step 2 Petition 870250110557, dated 02 / 12 / 2025, page 167 / 975 163 / 465

[00334] Compound 11-1A (238 mg, 495 pmol) was dissolved in acetic acid (4.00 mL), reacted at 25°C for 12 hours, and then concentrated under reduced pressure to remove the acetic acid and obtain the acetate salt of compound 11-2A.

[00335] With reference to step 2, compound 11-1B was used as raw material in place of compound 11-1A to obtain the acetate salt of compound 11-2B. Step 3

[00336] Compound 1-13B (200 mg, 254 pmol) and compound 11-2A (182 mg, acetate salt) were dissolved in dichloromethane (3.00 mL). N,N-diisopropylamine (1.27 mmol, 222 pL) was added and the reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated directly to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 11-3A. MS m / z = 874.4 [M+1]+.

[00337] Referring to step 3, the acetate salt of compound 11-2B was used as starting material instead of the acetate salt of compound 11-2A to obtain compound 11-3B. MS m / z = 874.4 [M+1]+. Step 4

[00338] Compound 11-3A (180 mg, 206 pmol) was dissolved in dichloromethane (3.00 mL) and m-chloroperbenzoic acid (43.9 mg, 216 pmol, 85.0% purity) was added. The reaction mixture was reacted at 25°C for 2 hours. 10.0 mL of sodium bicarbonate solution and 10.0 mL of sodium sulfite solution were added to the reaction mixture. The aqueous phase was extracted with dichloromethane (30.0 mL x 2). The organic phase was collected and concentrated to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 11-4A.

[00339] With reference to step 4, compound 11-3B was Petition 870250110557, dated 02 / 12 / 2025, pp. 168 / 975 164 / 465 used as starting material in place of compound 11-3A to obtain compound 11-4B. Step 5

[00340] Compound 11-4A (140 mg, 157 μmol), compound 1-2 (48.2 mg, 315 μmol), sodium tert-butoxide (60.5 mg, 629 μmol) and 4A molecular sieves (700 mg) were added to toluene (3.00 mL). The reaction mixture was reacted at 110°C for 12 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 1:2) to obtain compound 11-5A. MS m / z = 979.5 [M+1]+.

[00341] Referring to step 4, compound 11-4B was used as the starting material instead of compound 11-4A to obtain compound 11-5B. MS m / z = 979.5 [M+1]+. Step 6

[00342] Compound 11-5A (720 mg, 73.5 μmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.20 mL) was added. The reaction mixture was allowed to react at 25°C for 2 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 16%-46%) to obtain the trifluoroacetate salt of 11A. MS m / z = 639.3 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.92 (d, J = 8.6 Hz, 1H), 6.15 (dd, J = 11.2; 17.7 Hz, 1H), 5.61 - 5.46 (m, 2H), 5.31 (br d, J = 7.5 Hz, 2H), 5.25 - 5.17 (m, 1H), 5.09 - 4.97 (m, 1H), 4.77 - 4.72 (m, 2H), 4.55 (s, 2H), 4.39 - 4.22 (m, 3H), 3.98 - 3.70 (m, 3H), 3.55 (d, J = 13.6 Hz, 1H), 3.28 - 3.21 (m, 2H), 3.09 - 2.90 (m, 2H), 2.79 (br d, J = 16.3 Hz, 1H), 2.40 - 2.05 (m, 8H), 2.02 (s, 3H).

[00343] Compound 11-5B (640 mg, 65.4 μmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, page 169 / 975 165 / 465 dichloromethane (1.00 mL) and trifluoroacetic acid (0.20 mL) was added. The reaction mixture was allowed to react at 25°C for 2 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 µm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 16%-46%) to obtain the 11B trifluoroacetate salt. MS m / z = 639.3 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.92 (d, J = 8.5 Hz, 1H), 6.18 (dd, J = 11.2; 17.7 Hz, 1H), 5.66 - 5.48 (m, 2H), 5.31 (br d, J = 7.4 Hz, 2H), 5.20 (br dd, J = 4.1; 10.9 Hz, 1H), 4.95 - 4.91 (m, 1H), 4.78 4.71 (m, 2H), 4.55 (s, 2H), 4.45 - 4.16 (m, 3H), 3.98 - 3.62 (m, 4H), 3.27 3.22 (m, 2H), 3.09 - 2.88 (m, 2H), 2.79 (br d, J = 16.3 Hz, 1H), 2.56 - 2.03 (m, 8H), 2.02 (s, 3H). Example 12 Step 1

[00344] Compound 4-2 (100 mg, 115 μmol), compound 12-1A (83.0 mg, 463 μmol), sodium tert-butoxide (44.5 mg, 463 μmol), and 4A molecular sieves (1000 mg) were added to toluene (5.00 mL). The reaction mixture was reacted at 110°C for 12 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 12-1. MS m / z = 979.5 [M+1]+. Step 2

[00345] Compound 12-1 (900 mg, 91.9 μmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, page 170 / 975 166 / 465 dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was allowed to react at 25°C for 2 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 16%-46%) to obtain the 12-trifluoroacetate salt, MS m / z = 639.4 [M+H]+, 1H NMR (400 MHz, D2O) δ ppm 7.12 (d, J = 8.5 Hz, 1H), 5.33 - 5.26 (m, 2H), 5.05 - 4.94 (m, 2H), 4.36 - 4.19 (m, 4H), 3.99 - 3.87 (m, 3H), 3.62 - 3.25 (m, 5H). 3.21 - 2.85 (m, 4H), 2.31 - 2.07 (m, 6H), 2.06 - 2.01 (m, 3H), 1.96 - 1.86 (m, 1H), 0.87 - 0.72 (m, 4H). Example 13 13-1A or 13-1B 13-1B or 13-1A 13A or 13B 13B or 13A Step 1

[00346] Compound 4-2 (50.0 mg, 57.9 pmol), compound 13-1A (26.6 mg, 174 pmol), sodium tert-butoxide (27.8 mg, 289 pmol), and 4 Å molecular sieves (50.0 mg) were added to toluene (2.00 mL). The reaction mixture was reacted at 110°C for 12 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 13-1. MS m / z = 953.5 [M+1]+. Compound 13-1 was subjected to separation by SFC. Petition 870250110557, dated 02 / 12 / 2025, page 171 / 975 167 / 465 preparative (chiral column: (s,s) WHELK-O1 (250 mm*30 mm, 10 μm); mobile phase: [supercritical carbon dioxide - acetonitrile / isopropanol (ammonia 0.1%)]; acetonitrile / isopropanol (ammonia 0.1%): 38%-38%) and concentrated under reduced pressure to obtain compounds 13-1A and 13-1B. SFC analytical: (chiral column: (s,s) WHELK-O1 (50 mm*4.6 mm, 3.5 μm); mobile phase: [supercritical carbon dioxide - isopropanol (diethylamine 0.05%)]; isopropanol (diethylamine 0.05%)%: 40%), compound 13-1A, Rt=1.495 min, 99% ee; MS m / z = 953.5 [M+H]+; compound 13-1B, Rt=1.716 min, ee value 95%, MS m / z = 953.5 [M+H]+. Step 2

[00347] Compound 13-1A (17.0 mg, 17.8 μmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was allowed to react at 25°C for 1 hour. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 10%-40%) to obtain the trifluoroacetate salt of 13A. MS m / z =613.4 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.92 (d, J = 8.5 Hz, 1H), 5.41 - 5.27 (m, 2H), 5.18 (br dd, J = 3.8; 10.8 Hz, 1H), 4.77 - 4.70 (m, 1H), 4.68 - 4.50 (m, 2H), 4.32 (br d, J = 14.4 Hz, 1H), 4.22 - 4.10 (m, 2H), 3.88 - 3.63 (m, 4H), 3.48 - 3.32 (m, 4H), 3.27 (br d, J = 12.1 Hz, 1H), 3.03 - 2.88 (m, 3H), 2.53 - 2.40 (m, 1H), 2.32 - 2.09 (m, 6H), 2.04 - 2.01 (m, 3H), 2.01 - 1.93 (m, 1H).

[00348] Compound 13-1B (200 mg, 21.0 μmol) was dissolved in dichloromethane (1.00 mL) and trifluoroacetic acid (0.30 mL) was added. The reaction mixture was allowed to react at 25°C for 1 hour. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 μm; mobile phase: [water (trifluoroacetic acid 0.075%)). Petition 870250110557, dated 02 / 12 / 2025, page 172 / 975 168 / 465 acetonitrile]; acetonitrile: 10%-40%) to obtain the 13B trifluoroacetate salt. MS m / z =613.5 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.94 (d, J = 8.5 Hz, 1H), 5.44 - 5.30 (m, 2H), 5.20 (dd, J = 3.8; 11.3 Hz, 1H), 4.79 - 4.73 (m, 1H), 4.70 - 4.56 (m, 2H), 4.39 (br d, J = 14.0 Hz, 1H), 4.22 - 4.13 (m, 2H), 3.88 - 3.69 (m, 4H), 3.47 - 3.34 (m, 4H), 3.32 - 3.27 (m, 1H), 3.01 - 2.94 (m, 3H), 2.53 - 2.40 (m, 1H), 2.32 - 2.12 (m, 6H), 2.04 (s, 3H), 2.02 - 1.94 (m, 1H). Example 14 14-8A or 14-8B 14-7A or 14-7B 14-7B or 14-7A 14-9A or 14-9B 14-9B or 14-9A 14-8B or 14-8A 14A or 14B 14B or 14A Step 1

[00349] Compound 14-1 (5.00 g, 20.6 mmol) was dissolved in DMF (50.0 mL), followed by the addition of triphenylphosphonium difluoroacetate (19.0 g, 53.4 mmol). The reaction mixture was reacted at 80°C for 2 hours. 300 mL of water were added to the reaction solution and the mixture was extracted three times with ethyl acetate (200 mL). The organic phase was washed with saturated brine (200 mL), dried with anhydrous sodium sulfate, filtered, and concentrated. Petition 870250110557, dated 02 / 12 / 2025, page 173 / 975 169 / 465 to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 100:1 to 3:1) to obtain compound 14-2. 1H NMR (400 MHz, CDCl3) 5.00 - 4.76 (m, 1H), 3.82 - 3.65 (m, 4H), 3.61 - 3.45 (m, 1H), 2.71 - 2.55 (m, 2H), 1.49 - 1.38 (m, 9H). Step 2

[00350] Compound 14-2 (2.80 g, 10.1 mmol) was dissolved in tetrahydrofuran (3.00 mL) and lithium diisopropylamide (2.00 M, 10.1 mL) was added. The mixture was reacted at -60°C for 1 hour. Then, 1-chloro-3-iodopropane (10.3 g, 50.5 mmol, 1.55 mL) was added and the mixture was reacted at 60°C for 1 hour, followed by 12 hours at 25°C. 50.0 mL of ammonium chloride solution was added to the reaction solution and the mixture was extracted three times with ethyl acetate (50.0 mL). The organic phase was washed with saturated brine (100 mL), dried with anhydrous sodium sulfate, filtered and concentrated to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 50:1-10:1) to obtain compound 14-3. MS m / z = 376.1 [M+Na]+. Step 3

[00351] Compound 14-3 (3.20 g, 9.04 mmol) was dissolved in acetonitrile (1.00 mL) and hydrochloric acid / dioxane (2.00 M, 5.00 mL) was added. The mixture was reacted at 25°C for 12 hours. The mixture was concentrated under reduced pressure to remove the solvent, obtaining the hydrochloride salt of compound 14-4. MS m / z = 254.1 [M+H]+. Step 4

[00352] Compound 14-4 (2.50 g, hydrochloride salt) was dissolved in acetonitrile (25.0 mL). Potassium carbonate (5.95 g, 43.1 mmol) and potassium iodide (143 mg, 862 μmol) were added. The mixture was reacted at 25°C for 12 hours. The mixture was filtered and concentrated to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 50:1-20:1) to obtain compound 14-5. MS m / z = Petition 870250110557, dated 02 / 12 / 2025, page 174 / 975 170 / 465 218 [M+H]+. Step 5

[00353] Compound 14-5 (300 mg, 1.38 mmol) was dissolved in THF (3.00 mL) and lithium aluminum tetrahydride (2.50 M, 1.10 mL) was added. The mixture was then reacted at 0°C for 1 hour. To the reaction solution, 0.11 mL of water, 0.11 mL of 15% sodium hydroxide solution, and 0.33 mL of water were added. The reaction solution was filtered and concentrated to obtain compound 14-6. MS m / z = 190.1 [M+H]+. Step 6

[00354] Compound 14-6 (300 mg, 1.59 mmol) was dissolved in anhydrous dichloromethane (3.00 mL). Imidazole (432 mg, 6.34 mmol), 4-dimethylaminopyridine (19.37 mg, 159 pmol), and tert-butyldiphenylsilyl chloride (872 mg, 3.17 mmol, 812 pL) were added and reacted at 25°C for 12 hours. The reaction solution was concentrated to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 25%-55%) to obtain compound 14-7. MS m / z = 428.3 [M+H]+. Compound 14-7 was subjected to preparative SFC separation (chiral column: DAICEL CHIRALCEL OX (250 mm*50 mm, 10 pm); mobile phase: [supercritical carbon dioxide methanol (ammonia 0.1%)]; methanol (ammonia 0.1%): 10%-10%) and concentrated under reduced pressure to obtain compounds 14-7A and 14-7B.SFC analytical: (chiral column: DAICEL CHIRALCEL OX (50 mm*4.6 mm, 3 pm); mobile phase: [supercritical carbon dioxide-methanol (diethylamine 0.05%)]; methanol (diethylamine 0.05%): 5%-40%), compound 14-7A, Rt=1.165 min, 99% ee; MS m / z = 428.2 [M+H]+; compound 14-7B, Rt=1.233 min, ee value 95%, MS m / z = 428.2 [M+H]+. Step 7

[00355] Compound 14-7A (126 mg, 295 pmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, pages 175 / 975 171 / 465 dioxane (2.00 mL) and hydrochloric acid (12 M, 0.50 mL) was added. The mixture was reacted at 95°C for 12 hours and then dissolved by adding 2 mL of water. The mixture was extracted with ethyl acetate (10 mL) and the aqueous phase was lyophilized to obtain the hydrochloride salt of compound 14-8A. MS m / z = 190.1 [M+H]+.

[00356] Referring to step 7, compound 14-7B was used as starting material instead of compound 14-7A to obtain the hydrochloride salt of compound 14-8B. MS m / z = 190.1 [M+H]+. Step 8

[00357] Compound 4-2 (120 mg, 139 μmol), compound 14-8A (62.7 mg, hydrochloride), sodium tert-butoxide (66.7 mg, 695 μmol) and 4A molecular sieves (300 mg) were added to toluene (3.00 mL). The reaction solution was reacted at 100°C for 6 hours. The reaction solution was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by thin-layer chromatography (pure ethyl acetate) to obtain compound 14-9A. MS m / z = 989.7 [M+1]+.

[00358] Referring to step 8, compound 14-8B was used as the starting material instead of compound 14-8A to obtain compound 14-9B. MS m / z = 989.6 [M+H]+. Step 9

[00359] Compound 14-9A (63.0 mg, 63.7 μmol) was dissolved in dichloromethane (4.00 mL) and trifluoroacetic acid (1.00 mL) was added. The reaction mixture was allowed to react at 25°C for 12 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 16%-46%) to obtain the trifluoroacetate salt of 14A. MS m / z = 649.2 [M+H]+, 1H NMR (400 MHz, MeOD) δ ppm 6.92 (d, J = 8.5 Petition 870250110557, dated 02 / 12 / 2025, page 176 / 975 172 / 465 Hz, 1H), 5.19 (br dd, J = 3.9; 11.1 Hz, 1H), 4.96 - 4.90 (m, 1H), 4.84 - 4.78 (m, 1H), 4.77 - 4.70 (m, 2H), 4.66 - 4.58 (m, 1H), 4.32 (br d, J = 14.0 Hz, 1H), 4.15 (br dd, J = 3.0; 13.6 Hz, 2H), 3.97 - 3.63 (m, 4H), 3.57 - 3.39 (m, 2H), 3.36 - 3.33 (m, 1H), 3.09 - 2.87 (m, 3H), 2.49 - 2.05 (m, 7H), 2.04 - 1.93 (m, 4H).

[00360] Compound 14-9B (880 mg, 89.0 pmol) was dissolved in dichloromethane (4.00 mL) and trifluoroacetic acid (1.00 mL) was added. The reaction mixture was allowed to react at 25°C for 12 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 16%-46%) to obtain the 14B trifluoroacetate salt. MS m / z = 649.2 [M+H]+, 1H NMR (400 MHz, MeOD) δ ppm 6.92 (d, J = 8.5 Hz, 1H), 5.19 (br dd, J = 4.1; 11.3 Hz, 1H), 4.93 - 4.88 (m, 2H), 4.80 - 4.70 (m, 2H), 4.59 (d, J = 12.4 Hz, 1H), 4.30 (br d, J = 14.1 Hz, 1H), 4.15 (br dd, J = 2.1; 14.3 Hz, 2H), 3.95 - 3.62 (m, 4H), 3.58 - 3.38 (m, 2H), 3.30 - 3.24 (m, 1H), 3.09 - 2.87 (m, 3H), 2.47 - 2.07 (m, 7H), 2.05 - 1.94 (m, 4H). Example 15 15-2-1 or 15-2-2 15-2-2 or 15-2-1 15-2A or 15-2B 15-3A or 15-3B Petition 870250110557, dated 02 / 12 / 2025, p. 177 / 975 173 / 465 15-4A or 15-4B 15A or 15B Stage 1

[00361] Compound 14-5 (500 mg, 2.30 mmol) was dissolved in 2MeTHF (5.00 mL) and sodium bis(2-methoxyethoxy)aluminum hydride (2.66 g, 9.21 mmol, 2.57 mL, 70% purity) was added. The mixture was reacted for 2.5 hours at 10°C and then at room temperature for 12 hours. 10.0 mL of water were added to the reaction mixture, which was concentrated to remove dimethyltetrahydrofuran and lyophilized to obtain compound 15-1. MS m / z = 172.1 [M+H]+. Step 2

[00362] Compound 15-1 (261 mg, 1.52 mmol) was dissolved in anhydrous dichloromethane (3.00 mL). Imidazole (415 mg, 6.10 mmol), 4-dimethylaminopyridine (18.6 mg, 152 pmol), and tert-butyldiphenylsilyl chloride (838 mg, 3.05 mmol, 780 pL) were added and reacted at 45°C for 12 hours. The reaction solution was concentrated to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)-acetonitrile]; acetonitrile: 35%-65%) to obtain compound 15-2. MS m / z = 410.3 [M+H]+. Compound 15-2 was subjected to preparative SFC separation (chiral column: DAICEL CHIRALPAK IG (250 mm*50 mm, 10 pm); mobile phase: [supercritical dichloromethane-methanol (0.1% ammonia)]; methanol (0.1% ammonia): 18%-18%) and concentrated under Petition 870250110557, dated 02 / 12 / 2025, page 178 / 975 174 / 465 reduced pressure to provide compounds 15-2-1 and 15-2-2. SFC analytical: (chiral column: Chiralcel OX-3 (50 mm*4.6 mm, 3 μm); mobile phase: [supercritical carbon dioxide-ethanol (diethylamine 0.05%)]; ethanol (diethylamine 0.05%)%: 5%-40%), compound 15-2-1, Rt=1.18 min, 99% ee; MS m / z = 410.2[M+H]+; compound 15-2-2, Rt=1.46 min, 97% ee, MS m / z = 410.2 [M+H]+.

[00363] Compound 15-2-1 was subjected to separation by chiral preparative HPLC (chiral column: DAICEL CHIRALCEL OX (250 mm*50 mm, 10μm); mobile phase: [n-hexane - ethanol (0.1% ammonia)]; ethanol (0.1% ammonia): 10%-10%) and concentrated under reduced pressure to give compounds 15-2A and 15-2B. Analytical SFC: (chiral column: Chiralcel OX-3 (50 mm*4.6 mm, 3 pm); mobile phase: [supercritical carbon dioxide-ethanol (0.05% diethylamine)]; ethanol (0.05% diethylamine): 5%-40%), compound 152A, Rt=1.18 min, 99% ee; MS m / z = 410.2[M+H]+; compound 15-2B, Rt=1.21 min, 99% ee, MS m / z = 410.2 [M+H]+. Step 3

[00364] Compound 15-2A (160 mg, 391 pmol) was dissolved in dioxane (4.00 mL) and hydrochloric acid (12 M, 1.00 mL) was added. The mixture was reacted at 95°C for 12 hours. The mixture was dissolved by adding 5 mL of water and extracted with ethyl acetate (3.0 mL). The aqueous phase was lyophilized to obtain the hydrochloride salt of compound 15-3A. MS m / z = 172.1 [M+H]+.

[00365] Referring to step 3, compound 15-2B was used as starting material instead of compound 15-2A to obtain the hydrochloride salt of compound 15-3B. MS m / z = 172.1 [M+H]+. Step 4

[00366] Compound 4-2 (100 mg, 116 pmol), compound 15-3A (48.1 mg, hydrochloride salt), sodium tert-butoxide (55.6 mg, 579 pmol), and molecular sieves of 4A (50.0 mg) were added to toluene (3.00 mL). A Petition 870250110557, dated 02 / 12 / 2025, page 179 / 975 The reaction solution 175 / 465 was reacted at 100°C for 6 hours. The reaction solution was cooled to room temperature and filtered. The filtrate was concentrated to obtain a crude product. The crude product was purified by preparative thin-layer chromatography (pure ethyl acetate) to obtain compound 154A. MS m / z = 971.4 [M+1]+.

[00367] Referring to step 4, the hydrochloride of compound 153B was used as starting material instead of the hydrochloride of compound 15-3A to obtain compound 15-4B. MS m / z = 971.4 [M+H]+. Step 5

[00368] Compound 15-4A (710 mg, 73.1 μmol) was dissolved in dichloromethane (5.00 mL) and trifluoroacetic acid (1.00 mL) was added. The reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated to obtain a crude product. The crude product was then purified by preparative HPLC (Chromatographic column: Waters Xbridge 150*25 mm*5 pm; mobile phase: [water (0.1% ammonia)-acetonitrile]; acetonitrile: 35%-65%) to obtain compound 15A. MS m / z = 631.3 [M+H]+, 1H NMR (400 MHz, MeOD) δ ppm 6.99 - 6.71 (m, 2H), 5.14 (br dd, J = 4.1; 11.5 Hz, 1H), 4.81 - 4.76 (m, 2H), 4.20 - 4.09 (m, 3H), 3.61 - 3.38 (m, 4H), 3.26 - 3.00 (m, 4H), 2.90 - 2.58 (m, 5H), 2.25 - 2.10 (m, 1H), 2.07 - 1.60 (m, 10H).

[00369] Compound 15-4B (610 mg, 62.8 pmol) was dissolved in dichloromethane (5.00 mL) and trifluoroacetic acid (1.00 mL) was added. The reaction mixture was reacted at 25°C for 12 hours. The reaction mixture was concentrated directly to obtain a crude product. The crude product was purified by preparative HPLC (Chromatographic column: Phenomenex luna C18 150*25 mm*10 pm; mobile phase: [water (trifluoroacetic acid 0.075%)acetonitrile]; acetonitrile: 10%-40%) to obtain the trifluoroacetate salt of compound 15B. MS m / z = 631.3 [M+H]+, 1H NMR (400 MHz, MeOD) δ ppm 7.27 - 6.84 (m, 2H), 5.19 (br dd, J = 3.5; 11.0 Hz, 1H), 4.79 - 4.50 (m, 4H), Petition 870250110557, dated 02 / 12 / 2025, page 180 / 975 176 / 465 4.34 (br d, J = 14.3 Hz, 1H), 4.15 (br dd, J = 2.9; 14.6 Hz, 2H), 3.91 - 3.61 (m, 4H), 3.49 - 3.33 (m, 3H), 3.30 - 3.24 (m, 1H), 3.17 - 2.87 (m, 3H), 2.54 2.05 (m, 7H), 2.04 - 1.92 (m, 4H). Example 16 you 16-4A or 16-4B. 16-5C or 16-5D you OH You 16-6C ou 16-6D \ JO\ P o A / —.o \ / r-\ _ OU_ XN^'yOH XN yOH O.O. 16-7C or 16-7D ZERO PMB N You I go. ZERO PMB No, I am. PMB 16-8C or 16-8D HO ZERO PMB No, I am. PMB I go. HO ZERO PMB N I am ZERO PMB In N 16-9C or 16-9D Petition 870250110557, dated 02 / 12 / 2025, page 181 / 975 177 / 465 16-10C or 16-10D 16C or 16D Step 1

[00370] Under nitrogen, a solution of lithium bis-trimethylsilylamide in tetrahydrofuran (569.72 mL, 569.72 mmol, 1M) was added slowly, dropwise, to a solution of compound 16-1 (100.00 g, 379.81 mmol) in tetrahydrofuran (1000 mL) at -70°C. The mixture was reacted at -70°C for 1 hour. 4-bromo-1-butene (128.19 g, 949.53 mmol) was added dropwise to the reaction mixture at -70°C and the mixture was heated to 20°C with stirring for 12 hours. The reaction was rapidly cooled by the addition of 1000 mL of saturated aqueous ammonium chloride. The mixture was extracted with ethyl acetate (700 mL x 3), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 9:1) to give compound 16-2, MS m / z = 318.0 [M+H]+. Step 2

[00371] Compound 16-2 (96.00 g, 302.48 mmol) was dissolved in dichloromethane (1000 mL) and m-chloroperbenzoic acid (135.10 g, 665.45 mmol, 85% purity) was added. The reaction was stirred at 20°C under nitrogen for 12 hours. The reaction was rapidly cooled by the addition of saturated aqueous sodium sulfite (1500 mL) and washed with saturated aqueous sodium bicarbonate (1000 mL). The organic phase was separated, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 6:1) to Petition 870250110557, dated 02 / 12 / 2025, page 182 / 975 178 / 465 obtain compound 16-3. MS m / z = 334.1 [M+H]+. Step 3

[00372] To a solution of compound 16-3 (79.00 g, 236.97 mmol) in methanol (1500 mL), palladium / carbon (16.64 g, 156.40 mmol, 10% purity) was added. The mixture was reacted at 20°C under a hydrogen atmosphere (15 psi (0.1 MPa)) for 16 hours. The filtrate was obtained, concentrated under reduced pressure, and separated by column chromatography (dichloromethane:methanol = 20:1 to 9:1) to give compounds 16-4A (developing solvent: dichloromethane:methanol = 15:1, Rf = 0.5) and 16-4B (developing solvent: dichloromethane:methanol = 15:1, Rf = 0.3), respectively. Compound 16-4A: MS m / z = 200.0 [M+H]+. 1H NMR (400 MHz, CDCl3) δ ppm 3.71 (s, 3H), 3.60 (dd, J = 12.0 Hz, 4.0 Hz,1H), 3.41 (dd, J = 12.0 Hz, 4.0 Hz,1H), 3.13 - 3.05 (m, 1H), 2.99 - 2.94 (m, 1H), 2.73 - 2.67 (m, 1H), 2.36 - 2.31 (m, 1H), 2.24 - 2.20 (m, 1H), 1.93 - 1.79 (m, 5H), 1.74 1.66 (m, 1H). Compound 16-4B: MS m / z = 200.0 [M+H]+.- 3.07 (m, 1H), 2.76 - 2.69 (m, 1H), 2.58 - 2.52 (m, 1H), 2.29 - 2.21 (m, 1H), 1.89 - 1.80 (m, 4H), 1.67 1.54 (m, 2H). Step 4

[00373] Compound 16-4B (21.00 g, 105.40 mmol) was dissolved in dichloromethane (200 mL). Imidazole (15.07 g, 221.33 mmol) was added at 0°C and stirred for 10 minutes. Then, tert-butyldiphenylsilyl chloride (37.66 g, 137.02 mmol) was added. The mixture was heated to 20°C and stirred for 7 hours. The mixture was filtered, concentrated under reduced pressure, and separated by column chromatography (petroleum ether:ethyl acetate = 8:1) to give compound 16-5, MS m / z = 438.0 [M+H]+. Subsequently, chiral preparative HPLC (Chromatographic column: Regis (S,S)Whelk-O 1, 25 x 250 mm 10 μm; mobile phase: A: n-hexane, B: ethanol; B%: 2%) provided the Petition 870250110557, dated 02 / 12 / 2025, page 183 / 975 179 / 465 compounds 16-5C and 16-5D. Analysis method by SFC (Chromatographic column: Regis (s,s) WHELK-01 (4.6 mm ID *150 mm, 5 μm); mobile phase: [supercritical carbon dioxide-methanol (diethylamine 0.05%)]; gradient: methanol (diethylamine 0.05%)%: 5%-40%, 4 min), compound 16-5C, Rt=3.640 minutes, ee value 97.06%, MS m / z = 438.0 [M+H]+; compound 165D, Rt=3.826 minutes, ee value 97.88%, MS m / z = 438.0 [M+H]+. Step 5

[00374] Compound 16-5C (12.00 g, 27.42 mmol) was dissolved in a hydrogen chloride / 1,4-dioxane solution (100 mL, 4 M) and stirred at 50°C for 16 hours. The reaction solution was concentrated under reduced pressure and separated by column chromatography (dichloromethane:methanol = 7:1) to give compound 16-6C. MS m / z = 200.0 [M+H]+.

[00375] Referring to step 5, compound 16-5D was used as the starting material instead of compound 16-5C to obtain compound 16-6D. MS m / z = 200.0 [M+H]+. Step 6

[00376] Compound 16-6C (1.00 g, 5.02 mmol) was dissolved in 10 mL of a mixed solvent (acetonitrile:water = 100:0.75). Chromium trioxide (150.56 mg, 1.51 mmol) and periodic acid (2.86 g, 12.55 mmol) were added at 0°C. The mixture was heated to 20°C and the reaction was stirred under nitrogen for 16 hours. The reaction solution was filtered, and the filtrate was concentrated under reduced pressure to obtain compound 16-7C. MS m / z = 214.0 [M+H]+.

[00377] Referring to step 6, compound 16-6D was used as the starting material instead of compound 16-6C to obtain compound 16-7D. MS m / z = 214.0 [M+H]+. Step 7

[00378] Compound 16-7C (0.20 g, 0.94 mmol) was dissolved in N,N-dimethylformamide (5 mL). N-ethyl-4-methoxybenzylamine (154.98 mg, 0.94 Petition 870250110557, dated 02 / 12 / 2025, page 184 / 975 180 / 465 mmol), N,N-diisopropylamine (606.12 mg, 4.69 mmol), 2-(7-azobenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate were added sequentially. The reaction mixture was stirred at room temperature for 1 hour. Water (50 mL) was added to the reaction solution and the mixture was extracted with ethyl acetate (20 mL x 3). The organic phases were combined, washed with saturated brine (50 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 2:1) to obtain compound 168C. ​​MS m / z = 361.0 [M+H]+.

[00379] Referring to step 7, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 16-8D. MS m / z = 361.0 [M+H]+. Step 8

[00380] Compound 16-8C (150 mg, 0.42 mmol) was dissolved in anhydrous methanol (3 mL). The mixture was cooled to 0°C and sodium borohydride (50 mg, 1.25 mmol) and sodium methoxide / methanol solution (7.49 mg, 41.62 μmol, 30% purity) were added sequentially. The reaction was stirred at room temperature for 8 hours. The reaction was rapidly cooled with a saturated aqueous ammonium chloride solution (10 mL) and extracted with ethyl acetate (20 mL x 3). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 16-9C. MS m / z = 333.3 [M+H]+.

[00381] Referring to step 8, compound 16-8D was used as the starting material instead of compound 16-8C to obtain compound 16-9D. MS m / z = 333.3 [M+H]+. Step 9

[00382] Compound 16-9C (0.10 g, 0.30 mmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, pages 185 / 975 181 / 465 anhydrous tetrahydrofuran (3 mL) was added and cooled to 0°C. Sodium hydride (60.16 mg, 1.50 mmol, 60% purity) was added. After stirring at 0°C for half an hour, compound 4-2 (264.70 mg, 0.30 mmol) was added and the reaction was stirred at room temperature for 1 hour. The mixture was rapidly cooled with a saturated aqueous solution of ammonium chloride (10 mL) and extracted with ethyl acetate (20 mL x 3). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 2:1) to obtain compound 16-10C. MS m / z = 1132.5 [M+H]+.

[00383] Referring to step 9, compound 16-9D was used as the starting material instead of compound 16-9C to obtain compound 16-10D. MS m / z = 1132.5 [M+H]+. Step 11

[00384] Compound 16-10C (0.20 g, 0.18 mmol) was added to trifluoroacetic acid (4 mL) and stirred at 60°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: [water (ammonia 0.1%)acetonitrile]; gradient: (acetonitrile): 55%-70%) and lyophilized to obtain compound 16C. MS m / z = 672.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.16 - 5.14 (m, 1H), 4.81 - 4.78 (m, 1H), 4.67 4.63 (m, 1H), 4.16 - 4.13 (m, 2H), 4.09 - 4.08 (m, 1H), 3.75 - 3.72 (m, 1H), 3.54 - 3.51 (m, 3H), 3.43 - 3.40 (m, 1H), 3.28 - 3.17 (m, 3H), 3.06 - 3.03 (m, 1H), 2.91 - 2.83 (m, 2H), 2.78 - 2.72 (m, 1H), 2.12 - 2.08 (m, 2H), 2.02 - 1.91 (m, 11H), 1.76 - 1.66 (m, 2H), 1.14 (t, J = 8.0 Hz, 3H).

[00385] Compound 16-10D (0.16 g, 0.14 mmol) was added to trifluoroacetic acid (4 mL) and stirred at 60°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The Petition 870250110557, dated 02 / 12 / 2025, page 186 / 975 182 / 465 crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: [water (ammonia 0.1%)acetonitrile]; gradient: (acetonitrile): 55%-70%) and lyophilized to obtain compound 16D. MS m / z = 672.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.17 - 5.12 (m, 1H), 4.84 - 4.78 (m, 1H), 4.66 4.63 (m, 1H), 4.18 - 4.12 (m, 2H), 4.05 - 4.03 (m, 1H), 3.74 - 3.71 (m, 1H), 3.53 - 3.50 (m, 3H), 3.43 - 3.40 (m, 1H), 3.28 - 3.17 (m, 3H), 3.05 - 3.02 (m, 1H), 2.92 - 2.82 (m, 2H), 2.78 - 2.71 (m, 1H), 2.13 - 2.07 (m, 2H), 2.01-1.82 (m, 11H), 1.76 - 1.66 (m, 2H), 1.14 (t, J = 8.0 Hz, 3H).

[00386] It was confirmed that the 16C and 16D structures were as follows: Example 17 17-1C or 17-1D 17-2C or 17-2D Petition 870250110557, dated 02 / 12 / 2025, page 187 / 975 183 / 465 17C or 17D Step 1

[00387] Compound 16-7C (0.90 g, 4.22 mmol) was dissolved in N,N-dimethylformamide (10 mL). N,N-diisopropylamine (2.73 g, 21.10 mmol), N,N,N',N'-tetramethyl-O-(7-azabenzotriazol-1yl)uronium hexafluorophosphate (3.21 g, 8.44 mmol) and morpholine (735.43 mg, 8.44 mmol) were added sequentially. The mixture was reacted at 25°C for 12 hours. Water (10 mL) was added to the reaction solution, which was then extracted with ethyl acetate (20 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (dichloromethane:methanol = 20:1) to give compound 17-1C. MS m / z = 283.2 [M+H]+.

[00388] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 17-1D. MS m / z = 283.2 [M+H]+. Step 2

[00389] Compound 17-1C (20.00 mg, 70.84 pmol) was dissolved in methanol (0.5 mL). Sodium methoxide (38.27 pg, 0.71 pmol) and sodium borohydride (8.04 mg, 212.51 pmol) were added at 0°C and reacted at 25°C for 16 hours. The reaction was rapidly cooled by the addition of saturated ammonium chloride (10 mL). The product was extracted with ethyl acetate (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to Petition 870250110557, dated 02 / 12 / 2025, page 188 / 975 184 / 465 obtain compound 17-2C. MS m / z = 255.3 [M+H]+.

[00390] Referring to step 2, compound 17-1D was used as the starting material instead of compound 17-1C to obtain compound 17-2D. MS m / z = 255.3 [M+H]+. Step 3

[00391] Compound 17-2C (66.00 mg, 259.51 pmol) was dissolved in tetrahydrofuran (10 mL). Sodium hydride (31.14 mg, 1.30 mmol, 60% purity) was added at 0°C and stirred for 0.5 hours. Finally, compound 4-2 (228.36 mg, 259.51 pmol) was added and reacted at 25°C for 2 hours. The reaction was rapidly cooled by the addition of water (10 mL), and the mixture was extracted with ethyl acetate (20 mL). The mixture was dried with anhydrous sodium sulfate and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 0:1) to give compound 17-3C. MS m / z = 1054.9 [M+H]+.

[00392] Referring to step 3, compound 17-2D was used as the starting material instead of compound 17-2C to obtain compound 17-3D. MS m / z = 1054.9 [M+H]+. Step 4

[00393] Compound 17-3C (0.20 g, 189.72 pmol) was dissolved in dichloromethane (4 mL) and trifluoroacetic acid (2 mL) was added. The mixture was reacted at 25°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250 x 19 mm, 5 pm; mobile phase: [water (formic acid 0.1%)-acetonitrile]; gradient: (acetonitrile): 40% - 75%) and lyophilized to obtain the formate salt of compound 17C. MS m / z = 714.6 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 8.29 (s, 1H), 6.91 (d, J = 8.0 Hz, 1H), 5.18 (dd, J = 8.0; 4.0 Hz, 1H), 4.82 (s, 1H), 4.71 (d, J = 16.0 Hz, 1H), 4.30 - 4.22 (m, 3H), 4.12 (d, J = 12.0 Hz, 2H), 4.04 (dd, J = 12.0; 4.0 Hz, 1H), 3.78 - 3.57 (m, 9H), 3.52 - 3.46 (m, 1H), 3.25 (d, J Petition 870250110557, dated 02 / 12 / 2025, p. 189 / 975 185 / 465 = 12.0 Hz, 2H), 2.94 - 2.87 (m, 2H), 2.76 - 2.70 (m, 1H), 2.31 - 2.24 (m, 2H), 2.12 - 2.09 (m, 3H), 2.02 (s, 3H), 1.99 - 1.83 (m, 6H), 1.74 - 1.66 (m, 1H).

[00394] Compound 17-3D (0.10 g, 94.86 μmol) was dissolved in dichloromethane (2 mL) and trifluoroacetic acid (1 mL) was added. The mixture was reacted at 25°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250*19 mm, 5 mm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 55%-70%) and lyophilized to obtain compound 17D. MS m / z = 714.6 [M+H]+.1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.14 (dd, J = 12.0; 4.0 Hz, 1H), 4.80 (d, J = 12.0 Hz, 1H), 4.65 (d, J = 12.0 Hz, 1H), 4.37 (d, J = 8.0 Hz, 1H), 4.11 - 4.05 (m, 2H), 3.80 - 3.76 (m, 1H), 3.74 - 3.60 (m, 4H), 3.58 - 3.48 (m, 6H), 3.42 - 3.39 (m, 2H), 3.21 (dd, J = 16.0; 12.0 Hz, 1H), 3.03 (d, J = 12 Hz, 1H), 2.87 - 2.76 (m, 2H), 2.58 - 2.52 (m, 1H), 2.22 - 2.11 (m, 1H), 2.01 - 1.98 (m, 5H), 1.94 - 1.88 (m, 1H), 1.85 1.80 (m, 4H), 1.79-1.66 (m, 3H), 1.61-1.54 (m, 1H).

[00395] It has been confirmed that the structures of compounds 17C and 17D Example 18 Petition 870250110557, dated 02 / 12 / 2025, p. 190 / 975 186 / 465 18-1C or 18-1D 18-2C or 18-2D or 18-3C or 18-3D Step 1

[00396] Compound 16-7C (0.15 g, 703.47 μmol) was dissolved in dichloromethane (10 mL). N,N-diisopropylamine (3.52 mmol, 612.65 pL), N(2,4-dimethoxybenzyl)-2-methoxyethylamine (316.96 mg, 1.41 mmol) and N,N,N',N'-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (534.96 mg, 1.41 mmol) were added. The mixture was reacted at 25°C for 1 hour. The organic phase was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 3:1) to obtain compound 18-1C. MS m / z = 421.4 [M+H]+.

[00397] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 18-1D. MS m / z = 421.4 [M+H]+. Step 2

[00398] Compound 18-1C (0.27 g, 642.10 pmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, page 191 / 975 187 / 465 tetrahydrofuran (3 mL), and sodium borohydride (485.84 mg, 12.84 mmol) and lithium chloride (27.22 mg, 642.10 μmol) were added. The mixture was reacted at 50°C for 16 hours. After cooling to room temperature, the reaction was rapidly cooled with water (3 mL). The mixture was extracted with ethyl acetate (5 mL x 3). The organic phases were combined and concentrated under reduced pressure to obtain compound 18-2C. MS m / z = 393.3 [M+H]+.

[00399] Referring to step 2, compound 18-1D was used as the starting material instead of compound 18-1C to obtain compound 18-2D. MS m / z = 393.3 [M+H]+. Step 3

[00400] Compound 18-2C (0.18 g, 321.03 μmol) was dissolved in tetrahydrofuran (5 mL) and cooled to 0°C. Sodium hydride (17.12 mg, 428.04 pmol, 60% purity) was added and reacted at 0°C for 0.5 hours. Compound 4-2 (188.33 mg, 214.02 μmol) was added and reacted at 25°C for 0.5 hours. The reaction was rapidly cooled with saturated aqueous ammonium chloride (15 mL) and extracted with ethyl acetate (5 mL x 3). The organic phases were combined, concentrated under reduced pressure, and separated by column chromatography (petroleum ether:ethyl acetate = 1:1) to give compound 18-3C. MS m / z = 1192.8 [M+H]+.

[00401] Referring to step 3, compound 18-2D was used as the starting material instead of compound 18-2C to obtain compound 18-3D. MS m / z = 1192.8 [M+H]+. Step 4

[00402] Compound 18-3C (0.20 g, 167.74 μmol) was dissolved in trifluoroacetic acid (10 mL) and reacted at 50°C for 0.5 hours. The organic phase was concentrated under reduced pressure to obtain a crude product, which was then separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: water (0.1% ammonia)-acetonitrile; Petition 870250110557, dated 02 / 12 / 2025, page 192 / 975 188 / 465 gradiente: acetonitrila: 55%-70%). Depois da liofilização, o composto 18C foi obtido. MS m / z = 702,6 [M+H]+. RMN 1H (400 MHz, CD3OD) δ ppm 6,90 (d, J = 8,0 Hz, 1H), 5,15 (dd, J = 12,0; 4,0 Hz, 1H), 4,78 (s, 1H), 4,65 (d, J = 12,0 Hz, 1H), 4,17 - 4,06 (m, 3H), 3,77 (dd, J = 8,0; 4,0 Hz, 1H), 3,53 (d, J = 12,0 Hz, 3H), 3,49 - 3,36 (m, 5H), 3,34 (s, 3H), 3,21 (dd, J = 16,0; 12,0 Hz, 1H), 3,04 (d, J = 12,0 Hz, 1H), 2,95 - 2,91 (m, 1H), 2,85 (dd, J = 16,0; 4,0 Hz, 1H), 2,78 - 2,69 (m, 1H), 2,13 - 2,06 (m, 2H), 2,04 - 1,96 (m, 5H), 1,94 1,89 (m, 4H), 1,85 - 1,82 (m, 2H), 1,76 - 1,66 (m, 2H).

[00403] Compound 18-3D (0.15 g, 125.80 μmol) was weighed. Dichloromethane (2.5 mL) and trifluoroacetic acid (2.5 mL) were added, and the mixture was reacted at 25°C for 0.5 hours. The organic phase was concentrated under reduced pressure, and the crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 55%-70%). After lyophilization, compound 18D was obtained. MS m / z = 702.6 [M+H]+.1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.15 (dd, J = 12.0; 4.0 Hz, 1H), 4.78 (s, 1H), 4.65 (d, J = 12.0 Hz, 1H), t 12.0 Hz, 2H), 4.05 (d, J = 12.0 Hz, 1H), 3.78 - 3.75 (m, 1H), 3.53 (d, J = 8.0 Hz, 3H), 3.49 - 3.36 (m, 5H), 3.34 (s, 3.2H), J 16.0; 12.0 Hz, 1H), 3.04 (d, J = 12.0 Hz, 1H), 2.95 - 2.90 (m, 1H), 2.84 (dd, J = 16.0; 4.0 Hz, 1H), 2H), 2.01 - 1.94 (m, 5H),1.95 - 1.87 (m, 4H), 1.86-1.80 (m, 2H), 1.76-1.66 (m, 2H).

[00404] It was confirmed that the structures of compounds 18C and 18D were as follows: Petition 870250110557, of 02 / 12 / 2025, p. 193 / 975 189 / 465 Example 19 19-1C or 19-1D 19-2C or 19-2D Step 1

[00405] Compound 16-7C (0.40 g, 1.86 mol) was weighed and dichloromethane (6 mL) was added. Isopropylamine (166.33 mg, 2.81 mmol), 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate (1.43 g, 3.75 mmol) and N,N-diisopropylamine (0.73 g, 5.63 mol) were also added. The mixture was reacted at 25°C for 3 hours. Water (10 Petition 870250110557, dated 02 / 12 / 2025, pp. 194 / 975 190 / 465 mL), and the mixture was extracted with dichloromethane (10 mL x 3). The organic phase was concentrated under reduced pressure to obtain compound 19-1C. MS m / z = 255.0 [M+H]+.

[00406] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 19-1D. MS m / z = 255.0 [M+H]+. Step 2

[00407] Compound 19-1C (0.10 g, 0.39 mmol) was weighed and anhydrous tetrahydrofuran (3 mL) was added under nitrogen. The mixture was cooled to 0°C and a lithium-aluminum tetrahydride solution in tetrahydrofuran (1.18 mmol, 0.47 mL, 2.5 M) was added. The mixture was reacted at 25°C for 15 minutes. At 0°C, 0.2 mL of water was added to the reaction solution and the reaction was rapidly cooled by the addition of 0.2 mL of 15% NaOH solution. The reaction was stirred for 10 minutes and filtered. The filtered cake was washed with 5 mL of tetrahydrofuran. The filtrate was concentrated to obtain compound 19-2C. MS m / z = 227.1 [M+H]+

[00408] With reference to step 2, compound 19-1D was used as starting material in place of compound 19-1C to obtain compound 19-2D. MS m / z = 227.1 [M+H]+. Step 3

[00409] Compound 19-2C (50.0 mg, 0.22 mmol) was weighed and anhydrous tetrahydrofuran (5 mL) was added. Sodium hydride (15.91 mg, 0.66 mmol, 60%) was added under an ice bath at 0°C. The mixture was stirred at 25°C for 30 minutes and compound 4-2 (0.20 g, 0.22 mmol) was added. The reaction mixture was allowed to react at 25°C for 1 hour. The reaction mixture was rapidly cooled with water (5 mL) and extracted with ethyl acetate (5 mL x 3). The organic phase was concentrated under reduced pressure and separated by column chromatography (dichloromethane:methanol = 20:1) to give compound 19-3C. MS m / z = 1026.8 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, pages 195 / 975 191 / 465

[00410] Referring to step 3, compound 19-2D was used as the starting material instead of compound 19-2C to obtain compound 19-3D. MS m / z = 1026.8 [M+H]+. Step 4

[00411] Compound 19-3C (50 mg, 0.05 mmol) was dissolved in dichloromethane (2 mL) and trifluoroacetic acid (1 mL) was added. The reaction mixture was allowed to react at 25°C for 0.5 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250 x 19 mm, 5 μm; mobile phase: [water (formic acid 0.05%)acetonitrile]; (acetonitrile): 45%-75%) and lyophilized to obtain the salt formate of compound 19C. MS m / z = 686.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 8.45 (s, 1.52 H), 6.91 (d, J = 8.4 Hz, 1 H), 5.20 - 5.16 (m, 1 H), 4.84 4.79 (m, 1 H), 4.70 (d, J = 13.7 Hz, 1 H), 4.33 (d, J = 11.2 Hz, 1 H), 4.26 4.10 (m, 2 H), 4.08 - 3.97 (m, 4 H), 3.76 - 3.73 (m, 1 H), 3.58 (d, J = 13.4 Hz, 1 H), 3.27 - 3.21 (m, 3 H), 3.03 - 3.01 (m, 1 H), 2.93 - 2.88 (m, 1 H), 2.26 2.06 (m, 8 H), 2.01 - 1.94 (m, 5 H), 1.92 - 1.87 (m, 2 H), 1.17 (dd, J = 6.6; 1.5 Hz, 6 H).

[00412] Compound 19-3D (50 mg, 0.05 mmol) was dissolved in dichloromethane (2 mL) and trifluoroacetic acid (1 mL) was added. The reaction mixture was reacted at 25°C for 0.5 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250 x 19 mm, 5 pm; mobile phase: [water (formic acid 0.05%)-acetonitrile]; (acetonitrile): 45%-75%) and lyophilized to obtain the salt formate of compound 19D. MS m / z = 686.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 8.36 (s, 1.59 H), 6.81 (d, J = 8.4 Hz, 1 H), 5.10 - 5.07 (m, 1 H), 4.81 - 4.78 (m, 1 H), 4.61 (d, J = 13.6 Hz, 1 H), 4.22 - 4.08 (m, 3 H), 3.94 - 3.88 (m, 4 H), 3.63 (d, J = 13.6 Hz, 1 H), 3.48 (d, J = 13.2 Hz, 1 H), 3.17 - 3.03 (m, 3 H), 2.91 - 2.78 Petition 870250110557, dated 02 / 12 / 2025, p. 196 / 975 192 / 465 (m, 2 H), 2.15 - 1.99 (m, 6 H), 1.98 - 1.92 (m, 6 H), 1.84 - 1.76 (m, 3 H), 1.07 (d, J = 6.6 Hz, 6 H).

[00413] It was confirmed that the structures of compounds 19C and 19D were as follows: Example 20 20-1C or 20-1D 20-3C or 20-3D 20C or 20D Step 1 20-2C or 20-2D

[00414] Compound 16-7C (100 mg, 468.98 μmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, pp. 197 / 975 193 / 465 N,N-dimethylformamide (2 mL), 2-chloro-1-methylpyridinium iodide (179.72 mg, 703.47 μmol), triethylamine (142.37 mg, 1.41 mmol), and tert-butylamine (51.45 mg, 703.47 μmol) were added and reacted at 25°C for 2 hours. Water (10 mL) was added, and the mixture was extracted with ethyl acetate (10 mL * 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (petroleum ether:ethyl acetate = 1:1) yielded compound 20-1C. MS m / z = 269.0 [M+H]+.

[00415] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 20-1D. MS m / z = 269.0 [M+H]+. Step 2

[00416] Compound 20-1C (300 mg, 1.12 mmol) was dissolved in anhydrous tetrahydrofuran (5 mL) and cooled to 0°C under nitrogen. A 2M lithium borohydride solution in tetrahydrofuran (1.12 mL) was added dropwise and the mixture was heated to 50°C with stirring for 8 hours. The reaction was rapidly cooled by the addition of 3 mL of water and filtered. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 20-2C. MS m / z = 241.1 [M+H]+.

[00417] Referring to step 2, compound 20-1D was used as the starting material instead of compound 20-1C to obtain compound 20-2D. MS m / z = 241.1 [M+H]+. Step 3

[00418] Compound 20-2C (81.90 mg, 340.93 μmol) was dissolved in anhydrous tetrahydrofuran (5 mL) and cooled to 0°C. Sodium hydride (20.50 mg, 853.75 μmol, 60% purity) was added slowly and the mixture was Petition 870250110557, dated 02 / 12 / 2025, pp. 198 / 975 194 / 465 was heated to 25°C with stirring for 0.5 hours. Compound 4-2 (200 mg, 227.28 μmol) was then added and allowed to react at 25°C for 2 hours. The reaction was rapidly cooled by the addition of 3 mL of water and extracted with ethyl acetate (5 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (petroleum ether:ethyl acetate = 1:1) yielded compound 203C. MS m / z = 1040.8 [M+H]+.

[00419] Referring to step 3, compound 20-2D was used as the starting material instead of compound 20-2C to obtain compound 20-3D. MS m / z = 1040.8 [M+H]+. Step 4

[00420] Compound 20-3C (100 mg, 96.14 μmol) was dissolved in anhydrous dichloromethane (3 mL) and trifluoroacetic acid (1 mL) was added. The reaction mixture was reacted at 25°C for 2 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 µm; mobile phase: [water (formic acid 0.05%)acetonitrile]; acetonitrile: 10%-40%) and lyophilized to obtain the formate salt of compound 20C. MS m / z = 700.6 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 8.51 (s, 1H), 6.91 (d, J = 8.4 Hz, 1H), 5.20 - 5.15 (m, 1H), 4.82 (d, J = 13.6 Hz, 1H), 4.69 (d, J = 13.6 Hz, 1H), 4.27 - 4.14 (m, 3H), 3.88 (s, 3H), 3.68 (d, J = 13.2 Hz, 1H), 3.54 (d, J = 13.2 Hz, 1H), 3.28 - 3.15 (m, 2H), 3.10 - 3.04 (m, 1H), 2.95 - 2.86 (m, 2H), 2.21 - 2.12 (m, 3H), 2.02 - 1.76 (m, 12H), 1.36 (s, 9H).

[00421] Compound 20-3D (150 mg, 144.21 μmol) was dissolved in dichloromethane (4.5 mL) and trifluoroacetic acid (1.5 mL) was added. The reaction mixture was allowed to react at 25°C for 2 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The product Petition 870250110557, dated 02 / 12 / 2025, page 199 / 975 195 / 465 crude was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 μm; mobile phase: [water (ammonium bicarbonate 0.1%)acetonitrile]; (acetonitrile): 35%-53%) and lyophilized to obtain compound 20D. MS m / z = 700.6 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.4 Hz, 1H), 5.17 - 5.12 (m, 1H), 4.80 (d, J = 13.6 Hz, 1H), 4.65 (d, J = 13.6 Hz, 1H), 4.18 - 4.12 (m, 2H), 4.05 (d, J = 16.0 Hz, 1H), 3.71 - 3.68 (m, 1H), 3.54 - 3.51 (m, 3H), 3.43 - 3.40 (m, 1H), 3.25 - 3.18 (m, 1H), 3.04 (d, J = 16.0 Hz, 1H), 2.93 - 2.71 (m, 3H), 2.14 - 2.09 (m, 2H), 2.06 - 2.01 (m, 4H), 1.92-1.83 (m, 7H), 1.74 - 1.96 (m, 2H), 1.35 (s, 9H).

[00422] It was confirmed that the structures of compounds 20C and 20D were as follows: Example 21 21-3C or 21-3D / or % 21-1C or 21-1D 21-2C or 21-2D $ or φ 21-3C or 21-3D or Petition 870250110557, dated 02 / 12 / 2025, page 200 / 975 196 / 465 Step 1

[00423] Compound 16-7C (150 mg, 703.47 μmol) was dissolved in N,N-dimethylformamide (2 mL). 4-aminotetrahydrofuran (106.73 mg, 1.06 mmol), N-methylimidazole (173.27 mg, 2.11 μmol), and tetramethylchlorouronic acid hexafluorophosphate (296.07 mg, 1.06 mmol) were added and reacted at 25°C for 3 hours. Water (10 mL) was added, and the mixture was extracted with ethyl acetate (10 mL * 3). The extracted organic phases were combined, washed with saturated brine (5 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 20:1) yielded compound 21-1C. MS m / z = 297.1 [M+H]+.

[00424] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 21-1D. MS m / z = 297.1 [M+H]+. Step 2

[00425] Compound 21-1C (300 mg, 1.01 mmol) was dissolved in anhydrous methanol (5 mL). Sodium methoxide (21.90 mg, 404.91 μmol) and sodium borohydride (191.50 mg, 5.06 mmol) were added and reacted at 50°C for 24 hours. The reaction was rapidly cooled by the addition of 3 mL of saturated aqueous ammonium chloride. The mixture was filtered, and the filtrate was concentrated under reduced pressure to obtain a crude product. Separation by column chromatography (dichloromethane:methanol = 10:1) yielded compound 21-2C. MS m / z = 269.2 268.5 [M+H]+.

[00426] Referring to step 2, compound 21-1D was used as the starting material instead of compound 21-1C to obtain compound 21-2D. MS m / z = 269.2 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, page 201 / 975 197 / 465 Step 3

[00427] Compound 21-2C (100 mg, 372.65 μmol) was dissolved in anhydrous tetrahydrofuran (5 mL) and cooled to 0°C. Sodium hydride (44.70 mg, 1.12 mmol, 60% purity) was added slowly. The mixture was heated to 25°C and stirred for 0.5 hours. Compound 4-2 (163.90 mg, 186.32 μmol) was then added and allowed to react at 25°C for 2 hours. The reaction was rapidly cooled by the addition of 3 mL of water and extracted with ethyl acetate (5 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 20:1) yielded compound 21-3C. MS m / z = 1068.5 [M+H]+.

[00428] Referring to step 3, compound 21-2D was used as the starting material instead of compound 21-2C to obtain compound 21-3D. MS m / z = 1068.5 [M+H]+. Step 4

[00429] Compound 21-3C (114 mg, 106.72 μmol) was dissolved in anhydrous dichloromethane (0.9 mL) and trifluoroacetic acid (0.3 mL) was added. The mixture was reacted at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 μm; mobile phase: [water (formic acid 0.05%)-acetonitrile]; (acetonitrile): 10%-60%) and lyophilized to obtain the formate salt of compound 21C. MS m / z = 728.5 [M+H]+, 1H NMR (400 MHz, DMSO-de) δ ppm 8.22 (s, 1.38H), 7.97 (d, J = 7.7 Hz, 1H), 6.88 (d, J = 8.4 Hz, 1H), 6.02 (s, 2H), 5.05 - 5.01 (m, 1H), 4.75 (d, J = 13.7 Hz, 1H), 4.57 (d, J = 13.7 Hz, 1H), 3.94 - 3.90 (m, 3H), 3.83 - 3.79 (m, 3H), 3.64 (s, 2H), 3.54 - 3.51 (m, 1H), 3.44 3.41 (m, 1H), 3.35 - 3.30 (m, 4H), 3.09 - 3.02 (m, 1H), 2.98 (d, J = 12.5 Hz, 1H), 2.82 - 2.77 (m, 1H), 2.75 - 2.70 (m, 1H), 2.66 - 2.59 (m, 1H), 2.03 (s, Petition 870250110557, dated 02 / 12 / 2025, page 202 / 975 198 / 465 3H), 1.97 - 1.80 (m, 6H), 1.80 - 1.52 (m, 8H), 1.47 - 1.37 (m, 2H).

[00430] Compound 21-3D (200 mg, 187.23 μmol) was dissolved in anhydrous dichloromethane (5 mL) and trifluoroacetic acid (5 mL) was added. The mixture was reacted at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 µm; mobile phase: [water (formic acid 0.05%)-acetonitrile]; (acetonitrile): 10%-60%) and lyophilized to obtain the formate salt of compound 21D. MS m / z = 728.5 [M+H]+, 1H NMR (400 MHz, DMSO-de) δ ppm 8.14 (s, 0.56H), 7.96 (d, J = 7.8 Hz, 1H), 6.88 (d, J = 8.3 Hz, 1H), 6.01 (s, 2H), 5.04 - 5.00 (m, 1H), 4.74 (d, J = 13.7 Hz, 1H), 4.54 (d, J = 13.7 Hz, 1H), 4.05 - 3.92 (m, 4H), 3.85 - 3.79 (m, 4H), 3.64 - 3.51 (m, 2H), 3.46 (d, J = 13.3 Hz, 1H), 3.40 - 3.35 (m, 3H), 3.14 - 3.06 (m, 2H), 2.87 - 2.68 (m, 2H), 2.67 - 2.52 (m, 1H), 2.03 (s, 3H), 1.91 - 1.53 (m, 14H), 1.46 - 1.38 (m, 2H).

[00431] It was confirmed that the structures of compounds 21C and 21D were as follows: Example 22 Petition 870250110557, dated 02 / 12 / 2025, page 203 / 975 199 / 465 22-2C or 22-2D 22-3C or 22-3D 22-4C or 22-4D Step 1

[00432] 2,4-Dimethoxybenzaldehyde (500 mg, 3.01 mmol) was added to anhydrous tetrahydrofuran (5 mL), followed by cyclopropylamine (6.02 mmol, 416.97 μL) and glacial acetic acid (18.00 mg, 300.89 pmol). The mixture was reacted at 25°C for 2 hours. Sodium borohydride (567.20 mg, 9.03 mmol) was added to the reaction system and the mixture was stirred at 25°C for 16 hours. The mixture was rapidly cooled with water (5 mL) and extracted with dichloromethane (10 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to yield compound 221C. MS m / z = 208.2 [M+H]+. Step 2

[00433] Compound 16-7C (140 mg, 656.56 pmol) was dissolved in anhydrous dichloromethane (6 mL). N,N-diisopropylamine (3.28 mmol, 571.80 pL), compound 22-1C (176.90 mg, 853.54 mmol), and N,N,N',N'-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (499.31 mg, 1313.14 pmol) were added. The reaction was allowed to proceed at 25°C for 16 Petition 870250110557, dated 02 / 12 / 2025, page 204 / 975 200 / 465 hours. The mixture was rapidly cooled by the addition of water (5 mL) and extracted with ethyl acetate (10 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 3:1) to give compound 22-2C. MS m / z = 403.2 [M+H]+.

[00434] Referring to step 2, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 22-2D. MS m / z = 403.2 [M+H]+. Step 3

[00435] Compound 22-2C (170 mg, 422.38 μmol) was dissolved in anhydrous tetrahydrofuran (3 mL) and anhydrous methanol (3 mL). Sodium borohydride (79.90 mg, 2.11 mmol) and lithium chloride (17.90 mg, 422.38 μmol) were added and reacted at 50°C for 2 hours. The mixture was rapidly cooled by the addition of water (0.5 mL) and filtered. The filtrate was concentrated under reduced pressure to obtain compound 22-3C. MS m / z = 375.2 [M+H]+.

[00436] Referring to step 3, compound 22-2D was used as the starting material instead of compound 22-2C to obtain compound 22-3D. MS m / z = 375.2 [M+H]+. Step 4

[00437] Compound 22-3C (104 mg, 277.72 μmol) was dissolved in anhydrous tetrahydrofuran (5 mL) and sodium hydride (33.30 mg, 833.17 pmol, 60% purity) was added. The mixture was reacted at 0°C for 0.5 hours. Compound 4-2 (150.00 mg, 170.46 pmol) was then added and the mixture was reacted at 25°C for 1 hour. The mixture was rapidly cooled by the addition of saturated aqueous ammonium chloride (10 mL) and extracted with ethyl acetate (10 mL x 3). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, and filtered. The Petition 870250110557, dated 02 / 12 / 2025, page 205 / 975 201 / 465 filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 1:1) to give compound 22-4C. MS m / z = 1174.5 [M+H]+.

[00438] Referring to step 4, compound 22-3D was used as the starting material instead of compound 22-3C to obtain compound 22-4D. MS m / z = 1174.5 [M+H]+. Step 5

[00439] Compound 22-4C (150.00 mg, 127.73 μmol) was dissolved in trifluoroacetic acid (5 mL) and reacted at 50°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product, which was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 35%-60%) and lyophilized to obtain compound 22C. MS m / z = 684.6 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.4 Hz, 1H), 5.14 (dd, J = 11.6 Hz, 4.8 Hz, 1H), 4.79 (d, J = 13.6 Hz, 1H), 4.64 (d, J = 13.6 Hz, 1H), 4.14 - 4.04 (m, 3H), 3.68 (dd, J = 8.0 Hz, 5.2 Hz, 1H), 3.52 - 3.49 (m, 3H), 3.42 - 3.38 (m, 1H), 3.21 (dd, J = 17.6 Hz, 11.2 Hz, 1H), 3.03 (d, J = 12.4 Hz, 1H), 2.88 - 2.84 (m, 2H), 2.73 - 2.65 (m, 2H), 2.11 - 2.05 (m, 2H), 2.01 - 1.97 (m, 5H), 1.94 - 1.81 (m, 6H), 1.76 - 1.64 (m, 2H), 0.75 - 0.71 (m, 2H), 0.53 - 0.48 (m, 2H).

[00440] Compound 22-4D (100.00 mg, 85.16 μmol) was dissolved in trifluoroacetic acid (3 mL) and reacted at 50°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product, which was separated by high-performance preparative liquid chromatography (Chromatographic column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 35%-70%) and lyophilized to obtain compound 22D. MS m / z = 684.5 [M+H]+. RMN1H (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.4 Hz, 1H), 5.14 (dd, J = 11.6; 4.8 Hz, 1H), 4.79 (d, J = 13.6 Hz, 1H), 4.64 (d, J = 13.6 Hz, 1H), 4.16 - 4.12 (m, 2H), 4.03 (d, J Petition 870250110557, dated 02 / 12 / 2025, page 206 / 975 202 / 465 = 10.4 Hz, 1H), 3.68 (dd, J = 8.0 Hz, 5.2 Hz, 1H), 3.53 - 3.50 (m, 3H), 3.42 3.39 (m, 1H), 3.21 (dd, J = 17.6 Hz, 11.2 Hz, 1H), 3.03 (d, J = 12.4 Hz, 1H), 2.88 - 2.81 (m, 2H), 2.78 - 2.66 (m, 2H), 2.12 - 2.06 (m, 2H), 2.01 - 1.97 (m, 5H), 1.95 - 1.81 (m, 6H), 1.77 - 1.66 (m, 2H), 0.76 - 0.72 (m, 2H), 0.52 - 0.48 (m, 2H).

[00441] It was confirmed that the structures of compounds 22C and 22D were as follows: Example 23 23-1C or 23-1D 23-2C or 23-2D Petition 870250110557, dated 02 / 12 / 2025, page 207 / 975 203 / 465 23C or 23D Step 1

[00442] Compound 16-7C (0.20 g, 937.96 μmol) was dissolved in dimethylformamide (2 mL). N,N-diisopropylamine (606.12 mg, 4.69 mmol), N,N,N',N'-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (713.28 mg, 1.88 mmol) and N-[(2,4-dimethoxyphenyl)methyl]cyclobutanamine (207.56 mg, 937.96 pmol) were added sequentially. The mixture was reacted at 25°C for 12 hours. Water (10 mL) was added to the reaction solution, which was extracted with ethyl acetate (20 mL x 3). The mixture was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 23-1C. MS m / z = 417.4 [M+H]+

[00443] Referring to step 1, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 23-1D. MS m / z = 417.4 [M+H]+. Step 2

[00444] Compound 23-1C (0.20 g, 480.18 pmol) was dissolved in methanol (2 mL). Sodium methoxide (2.59 mg, 48.02 pmol) and sodium borohydride (90.83 mg, 2.40 mmol) were added at 0°C and reacted at 25°C for 16 hours. The reaction was rapidly cooled by the addition of saturated ammonium chloride (10 mL) and the mixture was extracted with ethyl acetate (20 mL). The mixture was dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain compound 23-2C. MS m / z = 389.3 [M+H]+

[00445] Referring to step 2, compound 23-1D was used as the starting material instead of compound 23-1C to obtain compound 23-2D. MS m / z = 389.3 [M+H]+. Step 3 Petition 870250110557, dated 02 / 12 / 2025, page 208 / 975 204 / 465

[00446] Compound 23-2C (50.00 mg, 128.70 pmol) was dissolved in tetrahydrofuran (1 mL). Sodium hydride (51.48 mg, 1.29 mmol, 60% purity) was added at 0°C and stirred for 0.5 hours. Finally, compound 4-2 (113.25 mg, 128.70 pmol) was added and the mixture was reacted at 25°C for 2 hours. The reaction was rapidly cooled by the addition of water (10 mL), and the mixture was extracted with ethyl acetate (20 mL). The mixture was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 0:1) to obtain compound 23-3C. MS m / z = 1188.7 [M+H]+.

[00447] Referring to step 3, compound 23-2D was used as the starting material instead of compound 23-2C to obtain compound 23-3D. MS m / z = 1188.7 [M+H]+. Step 4

[00448] Compound 23-3C (17 mg, 14.31 pmol) was dissolved in dichloromethane (1 mL) and trifluoroacetic acid (0.3 mL) was added. The mixture was reacted at 25°C for 0.5 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 55%-70%) and lyophilized to obtain compound 23C. MS m / z = 698.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.15 (dd, J = 12.0; 4.0 Hz, 1H), 4.84 - 4.79 (m, 1H), 4.62 (d, J = 16.0 Hz, 1H), 4.34 - 4.26 (m, 1H), 4.16 - 4.06 (m, 3H), 3.74 - 3.70 (m, 1H), 3.51 - 3.48 (m, 3H), 3.44 - 3.41 (m, 1H), 3.25 - 3.13 (m, 1H), 3.04 (d, J = 12.0 Hz, 1H), 2.89 - 2.82 (m, 2H), 2.76 - 2.70 (m, 1H), 2.32 - 2.26 (m, 2H), 2.12 - 2.06 (m, 2H), 2.04 - 1.89 (m, 11H), 1.85 - 1.83 (m, 2H), 1.77 - 1.71 (m, 4H).

[00449] Compound 23-3D (40 mg, 33.66 pmol) was dissolved in dichloromethane (1 mL) and trifluoroacetic acid (1 mL) was added. The mixture was reacted at 25°C for 0.5 hours. The reaction solution was concentrated under Petition 870250110557, dated 02 / 12 / 2025, page 209 / 975 205 / 465 reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Waters Xbridge, 250 x 19 mm, 5 mm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 55%-70%) and lyophilized to obtain compound 23D. MS m / z = 698.5 [M+H]+. RMN1H (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.15 (dd, J = 12.0; 4.0 Hz, 1H), 4.83 - 4.78 (m, 1H), 4.65 (d, J = 16.0 Hz, 1H), 4.34 - 4.26 (m, 1H), 4.18 - 4.12 (m, 2H), 4.04 (d, J = 8.0 Hz, 1 H), 3.73 - 3.69 (m, 1H), 3.53 (d, J = 12.0 Hz, 3H), 3.43 - 3.41 (d, J = 8.0 Hz, 1H), 3.25 - 3.18 (m, 1H), 3.04 (d, J = 12.0 Hz, 1H), 2.91 - 2.82 (m, 2H), 2.76-2.70 (m, 1H), 2.33 - 2.26 (m, 2H), 2.11 - 2.07 (m, 2H), 2.01 - 1.90 (m, 11H), 1.85 - 1.83 (m, 2H), 1.78-1.68 (m, 4H).

[00450] It was confirmed that the structures of compounds 23C and 23D were as follows: Example 24 Petition 870250110557, dated 02 / 12 / 2025, page 210 / 975 206 / 465 24-4C or 24-4D or 24-5C or 24-5D 24-6C or 24-6D h2n 24C or 24D Step 1

[00451] Compound 4-1 (280 mg, 0.33 mmol) was dissolved in dichloromethane (3 mL) and trifluoroacetic acid (376 mg, 3.30 mmol) was added. The resulting reaction solution was stirred at 25°C under nitrogen for 3 hours. The reaction solution was concentrated under reduced pressure and 3 mL of ethyl acetate was added to the residue. Then, a hydrogen chloride / ethyl acetate solution (4 M, 1 mL) was added. The reaction was stirred at 25°C for 1 hour and the mixture was concentrated under reduced pressure to obtain the hydrochloride salt of compound 24-1. Step 2

[00452] The hydrochloride salt of compound 24-1 (160 mg) and triethylamine (159.50 mg, 1.58 mol) were added to dichloromethane (5 mL). Di-tert-butyl dicarbonate (1.38 g, 6.30 mmol) and 4-dimethylaminopyridine (38.51 mg, 0.33 mmol) were then added. The resulting reaction mixture was stirred at 25°C under nitrogen for 12 hours. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (petroleum ether:ethyl acetate = 5:1) to obtain compound 24-2. MS m / z = 808.6 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, page 211 / 975 207 / 465 Step 3

[00453] Compound 24-2 (240 mg, 0.30 mmol) was dissolved in tetrahydrofuran (5 mL) and m-chloroperbenzoic acid (61.52 mg, 0.35 mmol, 85% purity) was added. The resulting reaction mixture was stirred at 25°C under nitrogen for 0.5 hours. The reaction mixture was concentrated under reduced pressure to obtain compound 24-3. MS m / z = 824.5 [M+H]+. Step 4

[00454] Compound 16-7C (180 mg, 0.84 mmol) was dissolved in N,N-dimethylformamide (4 mL). Benzotriazole hexafluorophosphate N,N,N',N'-tetramethyluronium (641.95 mg, 1.69 mmol) and N,N-diisopropylamine (218.42 mg, 1.69 mmol) were added, and the reaction mixture was stirred at 25°C for 30 minutes. 3-Oxethanolamine hydrochloride (92.09 mg, 1.26 mmol) was added to the mixture, and the resulting mixture was stirred at 25°C for 16 hours. The reaction mixture was diluted with water (20 mL) and extracted with ethyl acetate (50 mL). The organic phase was washed with saturated brine, dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 20:1) yielded compound 24-4C. MS m / z = 269.18 [M+H]+.

[00455] Referring to step 4, compound 16-7D was used as the starting material instead of compound 16-7C to obtain compound 24-4D. MS m / z = 269.18 [M+H]+. Step 5

[00456] Compound 24-4C (100 mg, 0.37 mmol) was dissolved in tetrahydrofuran (5 mL), and sodium borohydride (69.98 mg, 1.85 mmol) and lithium chloride (78.42 mg, 1.85 mmol) were added. The mixture was reacted at 25°C under nitrogen for 12 hours. The reaction mixture was diluted with water (10 mL) and extracted with ethyl acetate (30 mL). The organic phase was washed with saturated brine, dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography was performed. Petition 870250110557, dated 02 / 12 / 2025, page 212 / 975 208 / 465 (dichloromethane:methanol = 10:1) provided compound 24-5C. MS m / z = 241.22 [M+H]+.

[00457] Referring to step 5, compound 24-4D was used as the starting material instead of compound 24-4C to obtain compound 24-5D. MS m / z = 241.22 [M+H]+. Step 6

[00458] Compound 24-5C (70 mg, 0.29 mmol) was dissolved in tetrahydrofuran (3 mL), followed by the addition of sodium hydride (12 mg, 0.29 mmol, 60% purity). Under nitrogen, the reaction was stirred at 25°C for 0.5 hours. Then, a solution of compound 24-3 (210 mg, 0.29 mmol) in tetrahydrofuran (1 mL) was added. After the addition, the reaction was stirred at 25°C for 2 hours. The reaction solution was dissolved in 10 mL of ethyl acetate and washed with saturated brine (5 mL). The organic phase was dried and filtered. The filtrate was concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 20:1) yielded compound 24-6C. MS m / z = 900.6 [M-100+1]+.

[00459] Referring to step 6, compound 24-5D was used as the starting material instead of compound 24-5C to obtain compound 24-6D. MS m / z = 900.6 [M-100+1]+. Step 7

[00460] Compound 24-6C (10 mg, 10.00 pmol) was dissolved in dichloromethane (3 mL), followed by the addition of zinc bromide (5 mg, 20.00 pmol). The mixture was stirred at 25°C under nitrogen for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250*19 mm, 5 µm; mobile phase: [water (formic acid 0.1%)acetonitrile]; (acetonitrile): 10%-40%) and lyophilized to obtain the formate salt of compound 24C. MS m / z = 700.4 [M+H]+, 1H NMR (400 MHz, CD3OD) δ ppm 8.39 (s, 2H), 6.92 (d, J = 8.4 Hz, 1H), 5.19 (dd, J = 11.2; 4.4 Hz, 1H), Petition 870250110557, dated 02 / 12 / 2025, page 213 / 975 209 / 465 4.94 (q, J = 6.4 Hz, 1H), 4.88 (d, J = 6.8 Hz, 3H), 4.72 (d, J = 13.8 Hz, 1H), 4.59 (q, J = 5.8 Hz, 2H), 4.41 (d, J = 6.8 Hz, 3H), 4.27 (d, J = 13.8 Hz, 1H), 4,11 (d, J = 12,8 Hz, 2H), 3,78 (d, J = 13,6 Hz, 1H), 3,65 (d, J = 13,2 Hz, 1H), 3,49 - 3,36 (m, 1H), 3,27 (d, J = 11,6 Hz, 2H), 3,13 (s, 1H), 2,93 (dd, J = 18,2; 4,4 Hz, 1H), 2,37 - 2,19 (m, 5H), 2,14 - 2,05 (m, 4H), 2,03 - 1,99 (m, 4H), 1,97 - 1,91 (m, 2H).

[00461] Compound 24-6D (30 mg, 30.00 pmol) was dissolved in dichloromethane (3 mL), followed by the addition of zinc bromide (14 mg, 30.00 pmol). Under nitrogen, the mixture was stirred at 25°C for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250*19 mm, 5 pm; mobile phase: [water (formic acid 0.1%)-acetonitrile]; (acetonitrile): 10%-40%) and lyophilized to obtain the formate salt of compound 24D. MS m / z = 700.5 [M+H]+.1H NMR (400 MHz, CD3OD) δ ppm 8.46 (s, 3H), 6.92 (d, J = 8.4 Hz, 1H), 5.19 (dd, J = 11.0; 4.0 Hz, 1H), 4.98 - 4.92 (m, 1H), 4.91 - 4.89 (m, 2H), 4.72 (d, J = 13.6 Hz, 2H), 4.60 - 4.57 (m, 2H), 4.37 - 4.23 (m, 3H), 4.21 - 4.15 (m, 1H), 4.07 (d, J = 12.6 Hz, 2H), 3.76 (d, J = 14.6 Hz, 1H), R (s, 3H), 1.99 - 1.85 (m, 3H).

[00462] It was confirmed that the structures of compounds 24C and 24D were as follows: Example 25 Petition 870250110557, dated 02 / 12 / 2025, p. 214 / 975 210 / 465 25-4A or 25-4B 25-4B or 25-4A 25A or 25B Step 1

[00463] Compound 16-3 (8.00 g, 24.00 mmol) was dissolved in methanol (30 mL) and 10% palladium on carbon (1.5 g) was added. The reaction mixture was stirred at 25°C for 24 hours under a hydrogen atmosphere. The reaction mixture was filtered and the filtrate was concentrated to obtain compound 25-1. MS m / z = 200.2 [M+H]+ Step 2

[00464] Periodic acid (12.30 g, 53.95 mmol) was dissolved in acetonitrile (0.075% water) (50.0 mL). Chromium trioxide (647.40 mg, 6.47 mmol) was added slowly at 0°C and stirred for 10 minutes. Compound 25-1 was dissolved in acetonitrile (50.0 mL) and added slowly to the mixed solution at 0°C. After the addition, the mixture was heated slowly to room temperature and stirred for 10 hours. The mixture was filtered and the filtrate concentrated under reduced pressure to obtain compound 25-2. MS m / z = 214.2 [M+H]+ Step 3

[00465] Compound 25-2 (0.90 g, 4.22 mmol) was dissolved in N,N-dimethylformamide (20 mL). Benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate (2.41 g, 6.33 mmol) and N,N-diisopropylamine (2.73 g, 21.10 mmol) were added, and the reaction mixture was stirred at room temperature for 30 minutes. Dimethylamine hydrochloride (1.72 g, 21.10 mmol) Petition 870250110557, dated 02 / 12 / 2025, page 215 / 975 211 / 465 was added to the above mixture, and the resulting mixture was stirred at room temperature for 16 hours. The reaction mixture was diluted with water (100 mL) and extracted with dichloromethane (35 mL). The organic phase was washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain a crude product. The crude product was subjected to separation by high-performance preparative liquid chromatography (Chromatographic column: Waters Xbridge, 250*19 mm, 5 mm; mobile phase: [water (0.1% ammonia-water)-acetonitrile]; gradient: (acetonitrile): 10%-40%) to obtain compound 25-3A and compound 25-3B.LCMS analytical method (Chromatographic column: Waters Xbridge C18, (50 mm*4.6 mm*3.5 μm); mobile phase: [A: water (0.1% ammonia) B: acetonitrile]; gradient: B%: 0-10%, 0.2 min; 20-95%, 1.8 min; 95-95%, 0.7 min; 95-10%, 0.1 min; 10-10%, 0.7 min) Rt = 1.780 min for compound 25-3A, MS m / z = 241.2 [M+H]+, and Rt = 1.833 min for compound 25-3B, MS m / z = 241.2 [M+H]+. Step 4.

[00466] Compound 25-3A (0.13 g, 540.99 μmol) was dissolved in methanol (5 mL). Sodium borohydride (61.40 mg, 1.62 mmol) and 30% sodium methoxide in methanol (2.92 mg, 54.10 μmol) were added at 0°C. The reaction mixture was stirred at 25°C for 16 hours. After completion, the reaction was rapidly cooled with saturated ammonium chloride solution (10 mL) and extracted with dichloromethane (10 mL). The organic phase was washed with saturated brine (5 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 10:1) yielded compound 25-4A. MS m / z = 213.1 [M+H]+.

[00467] Referring to step 4, compound 25-3B was used as the starting material instead of compound 25-3A to obtain compound 25-4B. MS m / z = 213.1 [M+H]+. Step 5 Petition 870250110557, dated 02 / 12 / 2025, page 216 / 975 212 / 465

[00468] Compound 25-4A (50.00 mg, 235.53 pmol) was dissolved in tetrahydrofuran (2 mL) and cooled to 0°C. NaH (16.96 mg, 706.59 pmol, 60% purity) was added and stirred for 1 hour. Compound 4-2 (50.00 mg, 235.53 pmol) was added to the above mixture and the resulting mixture was stirred at 25°C for 1 hour. The resulting mixture was diluted with water (5 mL) and extracted with ethyl acetate (20 mL). The organic phase was washed with saturated brine (2 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 10:1) yielded compound 25-5A. MS m / z = 1012.8 [M+H]+.

[00469] Referring to step 5, compound 25-4B was used as the starting material instead of compound 25-4A to obtain compound 25-5B. MS m / z = 1012.8 [M+H]+. Step 6

[00470] Compound 25-5A (0.14 g, 138.32 pmol) was dissolved in trifluoroacetic acid (2 mL) and stirred at 25°C for 1 hour. The reaction mixture was concentrated to remove TFA. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; [water (0.1% ammonia)-acetonitrile]; gradient: acetonitrile: 30%-70%). Mobile phases A: water (0.1% ammonia) and B: (acetonitrile); gradient: B% = 30%-70%). After lyophilization, compound 25A was obtained. MS m / z = 672.6 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.13 - 5.09 (m, 1H), 4.78 - 4.67 (m, 2H), 4.54 (d, J = 8.0 Hz, 1H), 4.35 - 4.28 (m, 1H), 4.26 - 4.23 (m, 1H), 4.13 - 4.09 (m, 1H), 3.91 - 3.88 (m, 1H), 3.27 3.19 (m, 2H), 3.16 - 3.10 (m, 4H), 2.94 - 2.88 (m, 4H), 2.79 - 2.66 (m, 4H), 2.22 - 2.15 (m, 2H), 2.11 - 1.89 (m, 11H), 1.78 - 1.75 (m, 1H), 1.72 - 1.66 (m, 1H).

[00471] Compound 25-5B (60.00 mg, 59.28 pmol) was dissolved in trifluoroacetic acid (1 mL) and stirred at 25°C for 1 hour. The mixture of Petition 870250110557, dated 02 / 12 / 2025, p. 217 / 975 213 / 465 reaction was concentrated to remove TFA. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 mm; [water (0.1% ammonia)-acetonitrile]; gradient: acetonitrile: 30%-70%). Mobile phases A: water (0.1% ammonia) and B: (acetonitrile); gradient: B% = 30%-70%). After lyophilization, compound 25B was obtained. MS m / z = 672.1 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.13 - 5.10 (m, 1H), 4.78 - 4.67 (m, 2H), 4.52 - 4.47 (m, 1H), 4.32 - 4.28 (m, 1H), 4.26 - 4.21 (m, 1H), 4.15 - 4.10 (m, 1H), 3.91 - 3.87 (m, 1H), 3.27 - 3.22 (m, 2H), 3.15 - 3.13 (m, 3H), 2.93 - 2.92 (m, 3H), 2.80 - 2.72 (m, 4H), 2.67 2.66 (m, 1H), 2.54 - 2.50 (m, 1H), 2.18 - 2.04 (m, 3H), 2.02 - 1.89 (m, 7H), 1.83 - 1.74 (m, 4H), 1.62 - 1.55 (m, 1H). Example 26 Step 1

[00472] Compound 25-2 (1.00 g, 4.69 mmol) was dissolved in N,N-dimethylformamide (20 mL). N,N-diisopropylamine (2.12 g, 16.41 mmol), N,N,N',N'-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (2.67 g, 7.03 mmol) and 2,4-dimethoxybenzylamine (1.02 g, 6.10 mmol) were added sequentially. The mixture was reacted at 25°C for 2 hours. Water (50 mL) was added to the reaction solution, which was then extracted with ethyl acetate (40 mL x 3). The mixture was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 2:3) to obtain compound 26-1. MS m / z = 363.5 [M+H]+. Step 2

[00473] Compound 26-1 (50.00 mg, 137.96 pmol) was dissolved in ethanol (1 mL), and tetrahydrofuran (0.6 mL), lithium chloride (11.70 mg, 275.92 pmol), and sodium borohydride (10.44 mg, 275.92 pmol) were added. Petition 870250110557, dated 02 / 12 / 2025, page 218 / 975 214 / 465 sequentially. The mixture was reacted at 50°C for 3 hours. The mixture was cooled to room temperature and DCM (20 mL) was added. The mixture was washed with saturated brine (3 mL x 3), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain compound 262. MS m / z = 335.3 [M+H]+. Step 3

[00474] Compound 26-2 (30.00 mg, 89.71 pmol) was dissolved in tetrahydrofuran (3 mL). Sodium tert-butoxide (43.11 mg, 44.85 pmol) was added and stirred for 0.5 hours, and finally compound 42 (77.51 mg, 89.71 pmol) was added. The reaction mixture was stirred at 25°C for 1 hour. Water (3 mL) was added to rapidly cool the reaction, and the mixture was extracted with ethyl acetate (20 mL). The mixture was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 1:4) to give compound 26-3. MS m / z = 1134.6 [M+H]+. Step 4

[00475] Compound 26-3 (50.00 mg, 44.08 pmol) was dissolved in trifluoroacetic acid (1 mL) and reacted at 70°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters SunFire, 250*19 mm, 5 pm; mobile phase: [water (formic acid 0.1%)acetonitrile]; gradient: (acetonitrile): 40%-75%) and lyophilized to obtain the salt formate of compound 26. MS m / z = 644.1 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 8.38 (brs, 1H), 6.91 (d, J = 8.5 Hz, 1H), 5.20 - 5.12 (m, 1H), 4.82 - 4.66 (m, 4H), 4.47 (d, J = 6.4 Hz, 1H), 4.27 (q, J = 10.8 Hz, 2H), 3.58 (d, J = 12.5 Hz, 1H), 3.52 - 3.41 (m, 1H), 3.26 - 3.15 (m, 4H), 2.91 - 2.77 (m, 2H), 2.38 - 2.28 (m, 2H), 2.20 - 2.09 (m, 2H), 2.07 - 1.93 (m, 9H), 1.86 - 1.71 (m, 2H). Example 27 Petition 870250110557, dated 02 / 12 / 2025, p. 219 / 975 215 / 465 16-4A 27-1A 16-4B 27-1B 4-2 77 7 D4 -----*“ 27-2A * 27-3A * Zf-4A A 4-2 ____77.70 -----► 77.70----► 27-4R----► 27B ZfZ“r 1 4-2 77 7 D7 * Zí-ZV * 273U * Z / -4U Z / V 4-2 ----► 27-2D----- 27-3D----- 27-4D----- 27D Zí·Ζ·ΓΖ The the 27-1A or 27-1Β 27-1Bou27-1A 27-2-P2 or 27-2-P1 27-2-P1 or 27-2-P2 27-3A or 27-3B 27-4A or 27-4B Petition 870250110557, de 02 / 12 / 2025, pág. 220 / 975 216 / 465 27-4C or 27-4D 27A or 27B 27C or 27D Stage 1

[00476] Periodic acid (1.71 g, 7.54 mmol) was dissolved in 15 mL of a mixed solvent (acetonitrile:water = 100:0.75). Chromium trioxide (89.54 mg, 0.90 mmol) was added at 0°C and stirred for 15 minutes. Compound 16-4A (0.60 g, 3.02 mmol) was dissolved in acetonitrile (15 mL) and slowly added to the above mixed solution at 0°C. After the addition, the mixture was slowly heated to room temperature and stirred for 16 hours. The reaction mixture is filtered and the filtrate is concentrated under reduced pressure to produce compound 27-1A. MS m / z = 214.0 [M+H]+.

[00477] Referring to step 1, compound 16-4B was used as the starting material instead of compound 16-4A to obtain compound 27-1B. MS m / z = 214.0 [M+H]+. Step 2

[00478] Compound 27-1A (0.20 g, 0.94 mmol) was dissolved in N,N-dimethylformamide (5 mL). 2,4-Dimethoxy-N-methylbenzylamine (254.92 mg 1.41 mmol), N,N-diisopropylamine (605.63 mg 4.69 mmol) and 2-(7-azobenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate (606.57 mg 1.60 mL) were added sequentially. The mixture was Petition 870250110557, dated 02 / 12 / 2025, page 221 / 975 217 / 465 reacted at room temperature for 1 hour. 25 mL of water were added to the reaction solution and the mixture was extracted with ethyl acetate (15 mL x 3). The organic phases were combined, washed sequentially with water (10 mL x 2) and saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered and concentrated. Separation by column chromatography (dichloromethane:methanol = 20:1) yielded compound 27-2-P1, MS m / z = 377.1 [M+H]+.

[00479] Compound 27-2-P1 was subjected to preparative SFC separation (Chromatographic column: DAICEL CHIRALPAK® AS-10, 25*250 mm 10 pm; mobile phase: A: supercritical carbon dioxide, B: [ammonia 0.05% - methanol-ethanol]; B%: 80%-20%) to obtain compound 272A and compound 27-2B. After analytical SFC (Chromatographic column: DAICEL CHIRALPAK®AS-10 (4.6 mm ID *150 mm, 5 pm); mobile phase: [A: supercritical carbon dioxide, B: ethanol (diethylamine 0.05%)]; gradient: B%: 5%-40%, 4 min), compound 27-2A showed an Rt of 2.824 min, ee value 99.05%, MS m / z = 377.1 [M+H]+; compound 27-2B showed an Rt of 3.327 min, ee value 99.10%, MS m / z = 377.1 [M+H]+.

[00480] With reference to step 2, compound 27-1B was used as starting material in place of compound 27-1A to obtain compound 27-2-P2. MS m / z = 377.1 [M+H]+.

[00481] Compound 27-2-P2 was subjected to preparative SFC separation (Chromatographic column: DAICEL CHIRALPAK® AS-10, 25*250 mm 10 pm; mobile phase: A: supercritical carbon dioxide, B: [ammonia 0.05% - methanol-ethanol]; B%: 80%-20%) to obtain compound 272C and compound 27-2D. Following analytical SFC (chromatographic column: DAICEL CHIRALPAK®AS-10 (4.6 mm ID*150 mm, 5 pm); mobile phase: [A: supercritical carbon dioxide, B: ethanol (diethylamine 0.05%)]; gradient: B%: 5%-40%, 4 min), compound 27-2C showed an Rt of 2.891 min, ee value 95.80%, MS m / z = 377.1 [M+H]+; compound 27-2D showed Petition 870250110557, dated 02 / 12 / 2025, page 222 / 975 218 / 465 Rt of 3.327 min, ee value 96.34%, MS m / z = 377.1 [M+H]+. Step 3

[00482] Compound 27-2A (80.00 mg, 0.21 mmol) was dissolved in methanol (5 mL). A solution of sodium methoxide-methanol (7.66 mg, 0.04 mmol, 30% purity) and sodium borohydride (24.2 mg, 0.63 mmol) were added, and the reaction was stirred at 25°C for 16 hours. The mixture was rapidly cooled by the addition of 3 mL of saturated ammonium chloride solution and extracted with dichloromethane (5 mL x 3). The extracted organic phases were combined, washed with 5 mL of saturated brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (dichloromethane:ethyl acetate = 20:1) to obtain compound 27-3A. MS m / z = 349.1 [M+H]+.

[00483] Referring to step 3, compound 27-2B was used as the starting material instead of compound 27-2A to obtain compound 27-3B. MS m / z = 349.1 [M+H]+.

[00484] Referring to step 3, compound 27-2C was used as the starting material instead of compound 27-2A to obtain compound 27-3C. MS m / z = 349.1 [M+H]+.

[00485] Referring to step 3, compound 27-2D was used as the starting material instead of compound 27-2A to obtain compound 27-3D. MS m / z = 349.1 [M+H]+. Step 4

[00486] Compound 27-3A (60.00 mg, 0.17 mmol) was dissolved in tetrahydrofuran (5 mL). Sodium hydride (34.48 mg, 0.85 mmol, 60% purity) was added at 0°C and stirred for 0.5 hours. Then, a solution of compound 4-2 (164.56 mg, 0.19 mmol) in tetrahydrofuran (1 mL) was added to the system, and the mixture was heated to 25°C and stirred for an additional 1 hour. The reaction was rapidly cooled by the addition of 6 mL of saturated aqueous ammonium chloride. The mixture was extracted with ethyl acetate (5 mL). Petition 870250110557, dated 02 / 12 / 2025, page 223 / 975 219 / 465 x 2). The extracted organic phases were combined, washed with 5 mL of saturated brine, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (dichloromethane:methanol = 20:1) to give compound 27-4A. MS m / z = 1148.5 [M+H]+.

[00487] Referring to step 4, compound 27-3B was used as the starting material instead of compound 27-3A to obtain compound 27-4B. MS m / z = 1148.5 [M+H]+.

[00488] Referring to step 4, compound 27-3C was used as the starting material instead of compound 27-3A to obtain compound 27-4C. MS m / z = 1148.5 [M+H]+.

[00489] Referring to step 4, compound 27-3D was used as the starting material instead of compound 27-3A to obtain compound 27-4D. MS m / z = 1148.5 [M+H]+. Step 5

[00490] Compound 27-4A (0.10 g, 87.15 μmol) was dissolved in trifluoroacetic acid (3 mL) and stirred at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250 x 19 mm, 5 μm; mobile phase: [water (0.1% ammonia) acetonitrile]; (acetonitrile): 50%-70%) and lyophilized to obtain compound 27A. MS m / z = 658.6 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.18 - 5.10 (m, 1H), 4.78 (s, 1H), 4.65 (d, J = 12.0 Hz, 1H), 4.23 (d, J = 12.0 Hz, 1H), 4.16 - 4.07 (m, 2H), 3.57 - 3.48 (m, 3H), 3.45 3.38 (m, 1H), 3.29 - 3.17 (m, 2H), 3.10 - 3.01 (m, 2H), 2.89 - 2.81 (m, 1H), 2.73 (s, 3H), 2.67 - 2.60 (m, 1H), 2.31 - 2.23 (m, 1H), 2.15 - 2.08 (m, 1H), 2.04 - 1.96 (m, 4H), 1.95 - 1.87 (m, 4H), 1.86 - 1.79 (m, 2H), 1.76 - 1.65 (m, 3H).

[00491] Compound 27-4B (80.00 mg, 69.71 μmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, page 224 / 975 220 / 465 trifluoroacetic acid (3 mL) and stirred at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250*19 mm, 5 µm; mobile phase: [water (ammonia 0.1%)acetonitrile]; (acetonitrile): 50%-70%) and lyophilized to obtain compound 27B. MS m / z = 658.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.21 - 5.09 (m, 1H), 4.80 (d, J = 12.0 Hz, 1H), 4.65 (d, J = 12.0 Hz, 1H), 4.25 (d, J = 9.0 Hz, 1H), 4.16 - 4.06 (m, 2H), 3.57 - 3.48 (m, 3H), 3.44 - 3.38 (m, 1H), 3.30 - 3.15 (m, 2H), 3.10 - 3.01 (m, 2H), 2.89 - 2.80 (m, 1H), 2.73 (s, 3H), 2.68 - 2.60 (m, 1H), 2.31 - 2.21 (m, 1H), 2.19 - 2.09 (m, 1H), 2.01 - 1.96 (m, 4H), 1.94 - 1.78 (m, 6H), 1.77 - 1.64 (m, 3H).

[00492] Compound 27-4C (90.00 mg, 78.36 pmol) was dissolved in trifluoroacetic acid (3 mL) and stirred at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250*19 mm, 5 pm; mobile phase: [water (ammonia 0.1%)acetonitrile]; (acetonitrile): 50%-70%) and lyophilized to obtain compound 27C. MS m / z = 658.3 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.19 - 5.10 (m, 1H), 4.79 (d, J = 12.0 Hz, 1H), 4.65 (d, J = 12.0 Hz, 1H), 4.18 - 4.10 (m, 2H), 4.10 - 4.05 (m, 1H), 3.76 - 3.71 (m, 1H), 3.57 - 3.48 (m, 3H), 3.45 - 3.38 (m, 1H), 3.26 - 3.16 (m, 1H), 3.04 (d, J = 12.7 Hz, 1H), 2.92 - 2.81 (m, 2H), 2.75 (s, 3H), 2.75 - 2.68 (m, 1H), 2.14 - 2.05 (m, 2H), 2.04 - 1.97 (m, 5H), 1.96 - 1.80 (m, 6H), 1.76 - 1.64 (m, 2H).

[00493] Compound 27-4D (95.00 mg, 82.28 pmol) was dissolved in trifluoroacetic acid (3 mL) and stirred at 25°C for 1 hour. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Waters Xbridge, 250*19 mm, 5 µm; mobile phase: [water (ammonia 0.1%) acetonitrile]; (acetonitrile): 50%-70%) and lyophilized to obtain the compound Petition 870250110557, dated 02 / 12 / 2025, page 225 / 975 221 / 465 27D. MS m / z = 658.4 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.18 - 5.11 (m, 1H), 4.79 (d, J = 12.0 Hz, 1H), 4.64 (d, J = 12.0 Hz, 1H), 4.19 - 4.10 (m, 2H), 4.07 - 4.01 (m, 1H), 3.76 - 3.71 (m, 1H), 3.56 - 3.48 (m, 3H), 3.45 - 3.38 (m, 1H), 3.26 - 3.17 (m, 1H), 3.03 (d, J = 12.6 Hz, 1H), 2.92 - 2.81 (m, 2H), 2.75 (s, 3H), 2.75 - 2.69 (m, 1H), 2.15 - 2.06 (m, 2H), 2.05 - 1.97 (m, 5H), 1.96 - 1.80 (m, 6H), 1.76 - 1.65 (m, 2H).

[00494] It has been confirmed that the structures of compounds 27C and 27D Example 28 28-7A or 28-7B 28-7B or 28-7A 28-8A or 28-8B 28-8B or 28-8A 28-9A or 28-9B 28-9B or 28-9A Petition 870250110557, dated 02 / 12 / 2025, page 226 / 975 222 / 465 28-10A or 28-10B 28-10B or 28-10A 28A or 28B Step 1

[00495] Compound 28-1 (1 g, 4.04 mmol) was weighed and anhydrous tetrahydrofuran (10 mL) was added under nitrogen. The mixture was cooled to 76°C in a dry ice bath and lithium bis(trimethylsilyl)amide (12.12 mL, 12.12 mmol, 1 M) was added slowly. The mixture was stirred at -76°C for 40 minutes. A solution of 4-bromobutene (654.48 mg, 4.84 mmol) in anhydrous tetrahydrofuran (5 mL) was added and stirred for a further 60 minutes. The reaction was rapidly cooled by the addition of saturated aqueous ammonium chloride (10 mL) and extracted with ethyl acetate (15 mL x 3). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (ethyl acetate:petroleum ether = 1:7) yielded compound 28-2. MS m / z = 302.2 [M+H]+ Step 2

[00496] Compound 28-2 (500 mg, 1.66 mmol) was weighed. Dichloromethane (3 mL) and a hydrochloric acid / 1,4-dioxane solution (3 mL) were added, and the mixture was reacted at room temperature for 30 minutes. The reaction solution was concentrated directly to obtain the hydrochloride salt of compound 28-3. MS m / z = 202.1 [M+H]+ Step 3

[00497] Compound 28-3 (500 mg, hydrochloride salt) was weighed and anhydrous tetrahydrofuran (10 mL) was added. Sodium hydride (148.80 mg, 3.72 mmol, 60% purity) was added under an ice bath at 0°C. The mixture was stirred at 0°C for 1 hour. Benzyl chloroformate (634.59 mg, 3.72 mmol) was added portion by portion and stirred at 40°C for 16 hours. Petition 870250110557, dated 02 / 12 / 2025, page 227 / 975 223 / 465 hours. The reaction was rapidly cooled with water (15 mL) and extracted with ethyl acetate (20 mL x 3). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Separation by column chromatography (ethyl acetate:petroleum ether = 1:8) yielded compound 28-4 with MS m / z = 336.2 [M+H]+. Step 4

[00498] Compound 28-4 (300 mg, 0.89 mmol) was weighed and dichloromethane (5 mL) was added. m-Chloroperbenzoic acid (307.17 mg, 1.78 mmol) was added and the mixture was stirred at room temperature for 2 hours. Saturated aqueous sodium sulfite solution (1 mL) was added to the reaction solution and stirred for 5 minutes. Water (10 mL) was added and the mixture was extracted with dichloromethane (15 mL * 3). The organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure. Separation by column chromatography (ethyl acetate:petroleum ether = 1:6) yielded compound 28-5. MS m / z = 352.2 [M+H]+. Step 5

[00499] Compound 28-5 (1 g, 2.85 mmol) was weighed and anhydrous methanol (10 mL) was added. 10% palladium in carbon (100 mg) was added and the atmosphere was replaced with hydrogen three times. The mixture was stirred at room temperature for 1 hour. The reaction solution was filtered directly, the filter cake was washed with methanol (10 mL) and the filtrate was concentrated under reduced pressure. Separation by column chromatography (dichloromethane:methanol = 50:1) yielded compound 28-6A (developing solvent: DCM / MeOH = 15:1, Rf = 0.5), MS m / z = 218.1 [M+H]+, and compound 28-6B (developing solvent: DCM / MeOH = 15:1, Rf = 0.3), MS m / z = 218.1 [M+H]+.

[00500] Compound 28-6A: 1H NMR (400 MHz, DMSO-de) δ ppm 5.39 Petition 870250110557, dated 02 / 12 / 2025, page 228 / 975 224 / 465 - 5,21 (m, 1 H), 4,37 (d, J = 8,0 Hz, 1H), 3,58 (s, 3H), 3,39 - 3,35 (m, 1H), 3,29 - 3,21 (m, 2H), 2,99 - 2,86 (m, 1H), 2,82 - 2,77 (m, 1H), 2,61 - 2,52 (m, 1H), 2,09 - 1,91 (m, 3H), 1,84 - 1,78 (m, 1H), 1,68 - 1,60 (m, 1H).

[00501] Composto 28-6B: RMN 1H (400 MHz, DMSO-de) δ ppm 5,27 - 5,10 (m, 1H), 4,64 (d, J = 8,0 Hz, 1H), 3,59 (s, 3H), 3,58 - 3,54 (m, 1H), 3,51 - 3,46 (m, 1H), 3,25 - 3,18 (m, 1H), 3,09 - 2,95 (m, 2H), 2,69 - 2,60 (m, 1H), 2,02 - 1,70 (m, 4H), 1,59 - 1,48 (m, 1H). Etapa 6

[00502] Compound 28-6A (200.00 mg, 920.65 mmol) was weighed. Acetonitrile (2 mL) and water (0.014 mL) were added. The mixture was cooled to 0°C and periodic acid (662.87 mg, 2.30 mmol) and chromium trioxide (27.62 mg, 1.84 mmol) were added. The reaction was allowed to proceed at room temperature for 4 hours. The reaction mixture was filtered. The filtered cake was washed with 10 mL of dichloromethane and the filtrate was concentrated to obtain compound 28-7A (MS m / z = 232.1 [M+H]+).

[00503] Referring to step 6, compound 28-6B was used as the starting material instead of compound 28-6A to obtain compound 28-7B. MS m / z = 232.1 [M+H]+. Step 7

[00504] Compound 28-7A (120 mg, 518.99 μmol) was dissolved in N,N-dimethylformamide (3 mL). N-methyl-3,4-dimethylbenzylamine (92.94 mg, 622.79 μmol), 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate (394.67 mg, 1.04 mmol) and N,N-diisopropylamine (201.22 mg, 1.56 mmol) were added and reacted at 25°C for 4 hours. The mixture was extracted with ethyl acetate (20 mL x 2). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Compound 28-8A was obtained by column chromatography (petroleum ether:ethyl acetate = 10:1 to 1:1). MS m / z = 395.2 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, page 229 / 975 225 / 465

[00505] Referring to step 7, compound 28-7B was used as the starting material instead of compound 28-7A to obtain compound 28-8B. MS m / z = 395.2 [M+H]+. Step 8

[00506] Compound 28-8A (20.00 mg, 55.18 pmol) was dissolved in methanol (0.5 mL) and sodium borohydride (4.18 mg, 110.36 pmol) and sodium methoxide (29.81 pg, 0.55 pmol) were added. The reaction was allowed to proceed at 25°C for 4 hours. The mixture was extracted with ethyl acetate (20 mL x 2). The extracted organic phases were combined, washed with saturated brine (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain compound 28-9A. MS m / z = 367.3 [M+H]+.

[00507] Referring to step 8, compound 28-8B was used as the starting material instead of compound 28-8A to obtain compound 28-9B. MS m / z = 367.3 [M+H]+. Step 9

[00508] Compound 28-9A (20 mg, 54.58 pmol) was dissolved in anhydrous tetrahydrofuran (0.5 mL) and cooled to 0°C. Sodium hydride (2.62 mg, 109.16 pmol, 60% purity) was added under nitrogen. The mixture was allowed to react at room temperature for 1 hour. The reaction was rapidly cooled by the addition of 5 mL of saturated ammonium chloride solution and extracted with ethyl acetate (10 mL x 2). The extracted organic phases were combined, washed with saturated brine (10 mL), dried with anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. Purification by preparative thin-layer chromatography (dichloromethane:methanol = 20:1) yielded compound 28-10A. MS m / z = 1166.5 [M+H]+.

[00509] Referring to step 9, compound 28-9B was used as the starting material instead of compound 28-9A to obtain compound 28-10B. MS m / z = 1166.5 [M+H]+. Petition 870250110557, dated 02 / 12 / 2025, page 230 / 975 226 / 465 Step 10

[00510] Compound 28-10A (20 mg, 17.63 pmol) was added to dichloromethane (1 mL) and trifluoroacetic acid (0.1 mL) and the reaction was stirred at 20°C for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (formic acid 0.05%)-acetonitrile]; gradient: (acetonitrile): 10%-40%) and lyophilized to obtain the formate salt of compound 28A. MS m / z = 676.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 8.52 (brs, 1H), 6.91 (d, J = 8.0 Hz, 1H), 5.49 - 5.27 (m, 1H), 5.17 (dd, J = 11.6, 4.5 Hz, 1H), 4.82 4.79 (m, 1H), 4.69 (d, J = 16.0 Hz, 1H), 4.39 (d, J = 12.0 Hz, 1H), 4.30 - 4.19 (m, 2H), 3.91 (s, 2H), 3.71 - 3.64 (m, 1H), 3.59 - 3.42 (m, 2H), 3.29 - 3.12 (m, 3H), 3.04 - 2.85 (m, 2H), 2.73 (s, 3H), 2.44 - 2.29 (m, 2H), 2.23 - 2.15 (m, 2H), 2.07 - 1.98 (m, 6H), 1.97 - 1.75 (m, 3H).

[00511] Compound 28-10B (20 mg, 17.63 pmol) was added to dichloromethane (1 mL) and trifluoroacetic acid (0.1 mL) and the reaction was stirred at 20°C for 2 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Chromatographic column: Xtimate C18 150*40 mm*5 pm; mobile phase: [water (0.05% hydrochloric acid)-acetonitrile]; gradient: (acetonitrile): 10%-40%) and lyophilized to obtain the hydrochloride salt of compound 28B. MS m / z = 676.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.90 (d, J = 8.0 Hz, 1H), 5.42 - 5.25 (m, 1H), 5.18 - 5.11 (m, 1H), 4.79 (d, J = 13.5 Hz, 1H), 4.64 (d, J = 16.0 Hz, 1H), 4.23 (d, J = 8.0Hz, 1H), 4.20 - 4.11 (m, 2H), 3.75 (t, J = 5.6Hz, 1H), 3.52 (d, J = 12.0Hz, 3H), 3.42 (d, J = 12.0Hz, 1H), 3.26 - 3.12 (m, 2H), 3.10 - 2.99 (m, 2H), 2.88 - 2.80 (m, 1H), 2.73 (s, 3H), 2.45 - 2.35 (m, 1H), 2.24 - 2.07 (m, 2H), 2.06 - 1.96 (m, 7H), 1.87 - 1.77 (m, 2H), 1.68 (t, J = 8.9 Hz, 1H). Example 29 Petition 870250110557, dated 02 / 12 / 2025, page 231 / 975 227 / 465 Step 1

[00512] To a solution of compound 1-2 (50.00 mg, 326.33 μmol) in methanol (2 mL), palladium / carbon (16.64 mg, 10% purity) was added and the mixture was reacted under a hydrogen atmosphere (15 psi (0.1 MPa)) at 20°C for 16 hours. The reaction mixture was filtered. The filtrate was concentrated to dryness by nitrogen blowing to obtain compound 29-1. MS m / z = 156.15 [M+H]+ Step 2

[00513] Potassium tert-butoxide (257.54 mg, 2.68 mmol) was added to a solution of compound 29-1 (52.00 mg, 334.97 μmol) in tetrahydrofuran (4 mL) at 0°C and stirred for 1 hour. Compound 4-2 (347.28 mg, 401.97 pmol) was added to the above mixture and the resulting mixture was stirred at 25°C for 1 hour. 5 mL of saturated aqueous ammonium chloride were added to rapidly cool the reaction. The mixture was extracted with ethyl acetate (2 mL*2), dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 3:1) to obtain compound 29-2. MS m / z = 955.2 [M+H]+ Step 3

[00514] Compound 29-2 (0.11 g, 115.17 pmol) was dissolved in trifluoroacetic acid (1 mL). The mixture was stirred at 25°C for 1 hour. The reaction mixture was concentrated under reduced pressure to obtain a crude product. The crude product was separated by high-performance preparative liquid chromatography (Chromatographic column: Waters Xbridge, 250*19 mm, 5 µm; mobile phase: [water (formic acid 0.1%)-acetonitrile]; gradient: (acetonitrile): Petition 870250110557, dated 02 / 12 / 2025, page 232 / 975 228 / 465 45%-75%) para obter o sal formato do composto 29, MS m / z = 615,2 [M+H]+. RMN 1H (400 MHz, CD3OD) δ ppm 8,53 (s, 0,71H), 6,93 (d, J = 12,0 Hz, 1H), 5,18 - 5,15 (m, 1H), 4,80 - 4,73 (m, 3H), 4,62 - 4,60 (m, 1H), 4,49 - 4,43 (m, 3H), 3,78 - 3,72 (m, 1H), 3,52 - 3,36 (m, 2H), 3,30 - 3,17 (m, 2H), 3,02 - 2,99 (m, 1H), 2,91- 2,87 (m, 2H), 2,83 - 2,75 (m, 2H), 2,62 - 2,42 (m, 1H), 2,35 - 2,26 (m, 1H), 2,21 - 2,18 (m, 3H), 2,10 - 2,06 (m, 2H), 2,04 (m, 5H), 1,90 - 1,70 (m, 1H), 1,20 - 1,15 (m, 3H). Exemplo 30 Etapa 1

[00515] Compound 30-1 (10 g, 40.44 mmol) was dissolved in tetrahydrofuran (100 mL) and cooled to -78°C. Lithium hexamethyldisylazide (1 M, 52.58 mmol, 52.58 mL) was then added and stirred at -78°C for 0.5 hours. Allyl bromide (5.87 g, 48.53 mmol) was added to the reaction mixture, which was then stirred at room temperature for 2 hours. Saturated ammonium chloride solution (100 mL) was added and the mixture was extracted with ethyl acetate (50 mL x 3). The organic phases were combined, concentrated under reduced pressure, and separated by column chromatography (petroleum ether:ethyl acetate = 10:1) to obtain compound 30-2. MS m / z = 288.2 [M+H]+ Step 2

[00516] Compound 30-2 (200 mg, 696.07 μmol) was dissolved in tetrahydrofuran (1 mL). Water (1 mL) was added and stirred well. N-bromosuccinimide (123.89 mg, 696.07 μmol) was added in three batches. Petition 870250110557, dated 02 / 12 / 2025, page 233 / 975 229 / 465 Saturated aqueous sodium bicarbonate solution (3 mL) was added and the mixture was extracted with ethyl acetate (5 mL x 3). The mixture was dried with sodium sulfate and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 4:1) to obtain compound 30-3. MS m / z = 384.2 [M+H]+ Step 3

[00517] Compound 30-3 (400 mg, 1.04 mmol) was dissolved in dichloromethane (3 mL) and cooled to 0°C. Trifluoroacetic acid (1 mL) was added and the mixture was reacted at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure to obtain compound 30-4. MS m / z = 284.2 [M+H]+ Step 4

[00518] Compound 30-4 (295.78 mg, 1.04 mmol) was dissolved in acetonitrile (4 mL). Potassium carbonate (719.38 mg, 5.21 mmol) was added, and the mixture was heated to 80°C and stirred for 3 hours. After cooling to room temperature, the mixture was filtered, concentrated, and separated by column chromatography (dichloromethane:methanol = 10:1) to obtain compound 30-5. MS m / z = 204.3 [M+H]+ Step 5

[00519] Compound 30-5 (500 mg, 2.46 mmol) was dissolved in chloromethane. Dess-Martin periodinane (3.13 g, 7.38 mmol) was added at 0°C and stirred at room temperature for 2 hours. Saturated aqueous sodium bicarbonate (10 mL) was added to rapidly cool the reaction, and the mixture was filtered and extracted with ethyl acetate (5 mL x 3). The mixture was dried with anhydrous sodium sulfate, concentrated under reduced pressure, and separated by column chromatography (dichloromethane:methanol = 10:1) to give compound 30-6. MS m / z = 202.1 [M+H]+ Step 6

[00520] Compound 30-6 (240 mg, 1.19 mmol) was dissolved in Petition 870250110557, dated 02 / 12 / 2025, page 234 / 975 230 / 465 toluene (5 mL) and ethylene glycol (0.37 g, 5.96 mmol) was added. Ptoluenesulfonic acid monohydrate (22.69 mg, 0.12 mmol) was added, heated to 90°C and stirred for 16 hours. After cooling to room temperature, a saturated aqueous solution of sodium bicarbonate (5 mL) was added. The mixture was extracted with ethyl acetate (5 mL * 3). The organic phases were combined, dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure to obtain compound 30-7. MS m / z = 246.1 [M+H]+. Step 7

[00521] Compound 30-7 (100 mg, 0.41 mmol) was dissolved in tetrahydrofuran (5 mL) and cooled to 0°C. Lithium aluminum tetrahydride (15.48 mg, 0.41 mmol) was added, and the mixture was slowly brought back to room temperature and stirred for 1 hour. Water (0.02 mL), 15% aqueous sodium hydroxide solution (0.02 mL), and water (0.06 mL) were added sequentially to rapidly cool the reaction. The mixture was stirred at room temperature for 0.5 hours, filtered, and concentrated under reduced pressure to obtain compound 30-8. MS m / z = 218.2 [M+H]+. Step 8

[00522] Compound 30-8 (60 mg, 0.28 mmol) was dissolved in anhydrous tetrahydrofuran (1 mL) and cooled to 0°C. Sodium hydride (55.23 mg, 1.38 mmol, 60% purity) was added. After stirring at 0°C for half an hour, compound 4-2 (264.70 mg, 0.30 mmol) was added and stirred at room temperature for 2 hours. The reaction was rapidly cooled with saturated aqueous ammonium chloride (5 mL) and extracted with ethyl acetate (5 mL x 3). The organic phases were combined, dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure and separated by column chromatography (petroleum ether:ethyl acetate = 1:1) to obtain compound 30-9, MS m / z = 1017.7 [M+H]+. Step 9 Petition 870250110557, dated 02 / 12 / 2025, page 235 / 975 231 / 465

[00523] Compound 30-9 (0.10 g, 0.098 mmol) was added to 10 mL of a mixed solvent (trifluoroacetic acid:dichloromethane = 1:3) at 0°C and stirred at room temperature for 4 hours. The reaction solution was concentrated under reduced pressure to obtain a crude product. The crude product was separated by preparative HPLC (Waters Xbridge, 250 x 19 mm, 5 μm; mobile phase: [water (0.1% ammonia)-acetonitrile]; gradient: (acetonitrile): 55%-70%) and concentrated under reduced pressure to obtain compound 30. MS m / z = 677.5 [M+H]+. 1H NMR (400 MHz, CD3OD) δ ppm 6.96 (d, J = 8.0 Hz, 1H), 5.42 - 5.28 (m, 1H), 5.20 - 5.17 (m, 1H), 4.85 - 4.47 (m, 2H), 4.62 4.60 (m, 1H), 4.46 - 4.41 (m, 1H), 4.35 - 4.27 (m, 2H), 4.03 - 3.92 (m, 4H), 3.55 - 3.38 (m, 3H), 3.31 - 3.18 (m, 3H), 3.08 - 2.99 (m, 1H), 2.92 - 2.84 (m, 3H), 2.59 - 2.49 (M, 1H), 2.43 - 2.35 (m, 1H), 2.31 - 2.16 (m, 2H), 2.12 - 2.01 (m, 7H). Example 31 Step 1

[00524] Compound 31-1 (20 mg, 57.87 μmol) was dissolved in anhydrous tetrahydrofuran (3 mL), cooled to 0°C, and sodium hydride (4.63 mg, 115.75...

Claims

1. Compound, characterized in that it is represented by formula (I”) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof: Rn is selected from H and C1-3 alkyl, wherein the C1-3 alkyl is optionally substituted by 1, 2 or 3 F or Cl; ring A is selected from C6 aryl and 5- to 6-membered heteroaryl; ring B is selected from wherein ring B is optionally substituted by 1, 2, 3 or 4 R10; L is selected from -C(RL1RL2)-, wherein RL1 and RL2 are each independently selected from H, D and C1-3 alkyl; R1 and R2 are each independently selected from oxo, Petition 870250110557, dated 02 / 12 / 2025, p. H, F, Cl, Br, I and CN;Each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl, and C3-5 cycloalkyl, where C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl, and C3-5 cycloalkyl are each independently optionally substituted with 1, 2, 3, 4, or 5 Ra; each Ra is selected independently from D, F, Cl, Br, and I; R4, R5, R6, R7, R6' and R7' are each independently selected from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =No(C1-3 alkyl), wherein the C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently optionally substituted with 1, 2, 3, 4 or 5 Rb; alternatively, R6 and R7 together with the carbon atoms to which they are attached form a 3- to 5-membered heterocycloalkyl group;Each Rb is selected independently from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy and -C(=O)-NRMRb2; R8 is selected from H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein the C1-3 alkyl and C1-3 alkoxy are each independently optionally substituted with 1, 2, 3, 4 or 5 Ra; alternatively, R8 and R8' together with the carbon atom to which they are attached form a C3-5 cycloalkyl or a 3- to 5-membered heterocycloalkyl, wherein the C3-5 cycloalkyl and the 3- to 5-membered heterocycloalkyl are each independently optionally substituted with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb3Rb4 and -CH2Rc;Each R10 is selected independently from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, dialkylamine. Petition 870250110557, dated 02 / 12 / 2025, p. 472 / 975 3 / 18 C1-3, -C(=O)-Rd, -SRd, -S(=O)-Rd, -S(=O)2-Rd, -NH-C(=O)-Rd, C6-10 aryl and 5- to 10-membered heteroaryl, wherein C1-3 alkyl is optionally substituted by 1, 2 or 3 OH or F, and C6-10 aryl and 5- to 10-membered heteroaryl are each independently optionally substituted with 1, 2, 3, 4 or 5 Rsi; Rb1 and Rb2 are each independently selected from H, C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently optionally substituted with 1, 2, 3 or 4 Re1;Alternatively, Rb1 and Rb2 together with the nitrogen atom to which they are attached form a 3- to 6-membered heterocycloalkyl group, in which the 3- to 6-membered heterocycloalkyl group is optionally substituted by 1, 2, 3 or 4 Re1 groups; Rb3 and Rb4 are each independently selected from H, C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, in which C1-6 alkyl, C1-6 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently optionally substituted with 1, 2, 3 or 4 Re2; Alternatively, Rb3 and Rb4 together with the nitrogen atom to which they are attached form a 3- to 6-membered heterocycloalkyl group, in which the 3- to 6-membered heterocycloalkyl group is optionally replaced by 1, 2, 3 or 4 Re2 groups;Rc is selected from F, Cl, Br, I, OH, NH2, -(C=O)NRC1RC2, O(C=O)NRciRc2, -NRco(C=O)Rci and -NRco(C=O)NRciRc2; RC0, RC1 and RC2 are each independently selected from H, C1-6 alkyl, C3-6 cycloalkyl and 3- to 6-membered heterocycloalkyl; Petition 870250110557, dated 02 / 12 / 2025, p. 473 / 975 4 / 18 Rd is selected from C1-3 alkyl; King is selected from F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl, Camino alkyl, C1-3 di-alkylamine, CN, C1-3 alkoxy, -S(=O)2-(C1-3 alkyl), (C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(alkyl C1-3), (C=O)N(C1-3 alkyl)2, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5 to 10-membered heteroaryl;Re2 is selected from F, Cl, Br, I, OH, NH2, NO2, C1-3 alkyl, C1-3 alkylamine, C1-3 dialkylamine, CN, C1-3 alkoxy, -S(=O)2-(C1-3 alkyl), (C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl), (C=O)N(C1-3 alkyl)2, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, wherein the C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently optionally substituted with 1, 2, 3, 4 or 5 Rs1, and wherein the C1-3 alkyl and C1-3 alkoxy are each independently optionally substituted with 1, 2, 3, 4 or 5 Rs2; alternatively, two or more Re2 together with the carbon atom(s) to which they are attached form a C6 aryl group or a 5- or 6-membered heteroaryl group;Rs1 is selected from oxo, F, Cl, Br, I, OH, NH2, NO2, C1-6 alkyl, C1-6 alkylamine, C1-6 di-alkylamine, CN, C1-6 alkoxy, -S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) and -(C=O)N(C1-3 alkyl)2; Rs2 is selected from F, Cl, Br, I, OH, NH2, C1-6 alkylamine, C1-6 dialkylamine, CN, C1-6 alkoxy, -S(=O)2-(C1-3 alkyl), -(C=O)(C1-3 alkyl), -(C=O)O(C1-3 alkyl), -(C=O)NH(C1-3 alkyl) and -(C=O)N(C13 alkyl)2; em is selected from 0, 1, 2, 3, 4 and 5; provided that, Petition 870250110557, dated 02 / 12 / 2025, page. 474 / 975 5 / 18 1) when ring B is , where is replaced by a Rio, and Rio is F, at least one among Ri, R2, R4, R5, Ró, R7, Ró- and R7 is not H; 2) when ring B is replaced by 1, 2, 3 or 4 R1, by R2 and R7 it is not H; and less, where it is optionally one of R1, R2, R4, R5, R2, R7, 3) the compound is not 2. Compound according to claim 1, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that the compound has one of the following definitions: i) wherein Rn is H; or ii) where Rn is a C1 alkyl group optionally substituted by 1, 2 or 3 F or Cl groups.

3. Compound, characterized in that it is represented by the formula (Γ) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof: Petition 870250110557, dated 02 / 12 / 2025, page 475 / 975 6 / 18 ring A is selected from 5 to 6 membered C6 aryl and heteroaryl; ring B is selected from wherein ring B is optionally substituted by 1, 2, 3 or 4 R10; L is selected from -CH2-, where the -CH2- is optionally replaced by 1 or 2 D; R1 and R2 are each selected independently from oxo, H, F, Cl, Br, I, and CN; each R3 is selected independently from F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine,C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl, wherein C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, C2-4 alkenyl, C2-4 alkynyl and C3-5 cycloalkyl are each independently optionally substituted with 1, 2, 3, 4 or 5 Ra; Petition 870250110557, dated 12 / 02 / 2025, p. 476 / 975 7 / 18 each Ra is selected independently from D, F, Cl, Br and I; R4, R5, R6, R7, R6' and R7' are each independently selected from oxo, H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C2-4 alkenyl, C1-3 alkoxy, -C(=O)-Rd, -C(=O)-NRb1Rb2 and =No(C1-3 alkyl), wherein the C1-3 alkyl, C2-4 alkenyl and C1-3 alkoxy are each independently optionally substituted with 1, 2, 3, 4 or 5 Rb; alternatively, R6 and R7 together with the carbon atoms to which they are attached form a 3- to 5-membered heterocycloalkyl group; each Rb is independently selected from D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkoxy and -C(=O)-NRMRb2; R8 is selected from H, F,Cl, Br, I, OH, NH2, CN, C1-3 alkyl and C1-3 alkoxy, wherein C1-3 alkyl and C1-3 alkoxy are each independently optionally substituted with 1, 2, 3, 4 or 5 Ra; alternatively, R8 and R8' together with the carbon atom to which they are attached form a C3-5 cycloalkyl or a 3- to 5-membered heterocycloalkyl, wherein the C3-5 cycloalkyl and the 3- to 5-membered heterocycloalkyl are each independently optionally substituted with 1, 2 or 3 R10; R9 is selected from -C(=O)-NRb1Rb2 and -CH2Rc; Each R10 is independently selected from oxo, D, F, Cl, Br, I, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylamine, C1-3 dialkylamine, -SRd, -S(=O)-Rd, -S(=O)2-Rd and -NH-C(=O)-Rd, wherein the C1-3 alkyl is optionally substituted with 1, 2 or 3 OH groups; Rb1 and Rb2 are each independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C10 aryl and 5- to 10-membered heteroaryl, wherein C1-6 alkyl, C3-10 cycloalkyl,3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are each independently optionally substituted with 1, Petition 870250110557, 02 / 12 / 2025, p. 477 / 975 8 / 18 2 or 3 Rei; alternatively, Rbi and Rb2 together with the nitrogen atom to which they are attached form a 3- to 6-membered heterocycloalkyl group; Rc is selected from F, Cl, Br, I, OH, NH2, -O(C=O)NRCiRC2, NRco(C=O)Rci and -NRCo(C=O)NRCiRc2; Rco, Rei and Rc2 are each independently selected from H, C1-6 alkyl, C3-6 cycloalkyl and 3- to 6-membered heterocycloalkyl; Rd is C1-3 alkyl; King is selected from F, Cl, Br, I, OH, NH2, C1-3-mino alkyl, C1-3-mino dialkyl, CN, C1-3 alkoxy, C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C1-10 aryl and 5- to 10-membered heteroaryl; in is selected from 0, 1, 2, 3, 4 and 5; with the condition that, 1) when ring B is '—', where is replaced by a R1, and R1 is F, at least one of Rb, R2, R4, R5, R6, R7,1) where R1 and R7 are not H; 2) when ring B is \, where \ is optionally replaced by 1, 2, 3 or 4 R1, at least one of R1, R2, R4, R5, R1, R7, R1 and R7 is not H; and 3) the compound is not Petition 870250110557, dated 02 / 12 / 2025, p. 478 / 975 9 / 18 4. Compound according to any one of claims 1 to 3, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that ring A is C6 aryl.

5. Compound according to any one of claims 1 to 3, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that ring A is a 5-membered heteroaryl group.

6. A compound according to any one of claims 1 to 5, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein the compound has one of the following definitions: i) wherein ring B is selected from each of which is optionally replaced by 1, 2,3 or 4 R10; ii) wherein ring B is optionally replaced by 1, 2, 3 or 4 R10; optionally wherein the compound is a compound of formula (I'-1-i), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, optionally, wherein the compound is a compound of Petition 870250110557, dated 02 / 12 / 2025, page 479 / 975 10 / 18 formula (I'-2-i), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, optionally replaced by 1, 2, 3 or 4 R10; optionally wherein the compound is a compound of formula (I'-1-ii), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, optionally wherein the compound is a compound of formula (I'-2-ii), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, 7. Compound according to any one of claims 1 to 5, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof,characterized by the fact that ring B is selected from Petition 870250110557, dated 02 / 12 / 2025, page 480 / 975 11 / 18, which are optionally replaced by 1, 2, 3 or 4 R10.

8. Compound according to claim 7, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that it is selected from a compound of formulas (I'-3), (I'-4), (I'-5), (I'-6), (I'-7), (I'-8), (I'-9), (I'-10), (I'-11), (I'-12) and (I'-13), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, H (R3)m (I'-3) (R3)m (Rlo)o-4 (I'-4) NHN / R5 r6 ^Re' (r1o)o-4 (I'-5), (I'-6), r4x r7 R7— (Rio)(m Petition 870250110557, dated 12 / 02 / 2025, p. 481 / 975 12 / 18 (I'-13).or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that it is selected from a compound of formulas (I'-14) and (I'-15), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, Petition 870250110557, dated 02 / 12 / 2025, p. 482 / 975 13 / 18 11. Compound according to any one of claims 1 to 4 and 6 to 10, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that the compound has one of the following definitions: i) wherein ring A is phenyl and is substituted by at least one R3, each R3 being selected independently from F, OH, NH2, CF3, —C=CCD3 —cech , , OCH3, -C^CCH3, -CECCH2F, -cecchf2? -c=ccf3 , Petition 870250110557, dated 02 / 12 / 2025, p. 483 / 975 14 / 18 or 12. Compound according to ii) of claim 11, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof,characterized by the fact that the compound has one of the following definitions: i) is a compound of formula (I'-1'-i), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, ii) is a compound of formula (Γ-Γ-ii), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, Petition 870250110557, dated 02 / 12 / 2025, page. 484 / 975 15 / 18 iii) is a compound of formula (I'-2'-i), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, iv) is a compound of formula (I'-2'-ii), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, v) is selected from a compound of formulas (I'-3'), (I'-4'), (I'-5'), (I'-6'), (I'-7'), (I'-8'), (I'-9'), (I'-10'), (I'-11'), (I'-12') and (I'-13'), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, Petition 870250110557, dated 02 / 12 / 2025,pg. 485 / 975 16 / 18 HNN / R5 R6 R' H2N R4X R7 Ry^ R4x Ry Ry— Ri r5 N^R6' (I'-m h2n ........ (Ri 0)0-4 Petition 870250110557, of 02 / 12 / 2025, p. 486 / 975 17 / 18 or optionally, where R4, R5, Ró, R7, Ró' and R7' are each H; or vi) is selected from a compound of formulas (I'-14') and (I'15'), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, (T-14') and (T-15').

13. A compound according to any one of claims 1 to 12, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that the compound has one or more of the following definitions: i) wherein L is -C(RL1RL2)-, wherein RL1 and RL2 are selected independently of H and D; or ii) wherein L is -C(RL1RL2)-, wherein RL1 and RL2 are independently H; or iii) wherein L is -C(RL1RL2)-, wherein at least one of RL1 and RL2 is C1-3 alkyl; and / or iv) wherein R1 and R2 are each H.

14. A compound according to claim 1, or a Petition 870250110557,From 02 / 12 / 2025, page 487 / 975 18 / 18 stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that the compound has one of the following definitions: i) it is selected from those in Table 1; or ii) it is selected from those in Table 2 and Table 3.

15. Use of a compound as defined in any of claims 1 to 14, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, characterized in that it is in the manufacture of a medicament, wherein the use has one of the following definitions: i) to treat a disease or condition associated with a KRAS mutation; or ii) to treat a disease or condition associated with a mutation in the KRAS gene, wherein the KRAS mutation is a KRASG12D mutation.

16. Invention of a product, process, system, kit or use, characterized in that one or more elements are described in the application.

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