TW202309027A - Compound as a parp inhibitor - Google Patents

Abstract

PARP inhibitors, pharmaceutical composition, and methods of use thereof are provided in the present disclosure.

Description

Compounds as PARP Inhibitors

The present invention relates to a class of compounds or pharmaceutically acceptable salts capable of inhibiting the activity of poly ADP ribose polymerase (poly(ADP-ribose) polymerase, PARP), and as a drug for treating PARP-mediated diseases, such as proliferative diseases such as cancer and immune disease.

Proliferative diseases such as cancer and inflammation attract the academic community to provide effective treatment methods. And in this regard, efforts have been made to identify and target specific mechanisms that play a role in proliferative diseases.

The occurrence and development of tumors are closely related to genetic mutations and dysregulation of poly ADP-ribose polymerase (PARP) and its regulators, which suggests that inhibition of PARP may be an effective anti-tumor therapy.

PARPs belong to a protein family characterized by the PARP catalytic domain, and currently there are about 18 family members. PARP can be activated by damaged DNA fragments and catalyze the binding of poly ADP-ribose residues to target proteins, thereby regulating enzyme catalytic activity and protein interaction. PARP is closely related to many physiological processes, including DNA damage repair, gene transcription, cell cycle development (including proliferation and differentiation), apoptosis, chromatin function, maintenance of genome (eg, chromosome) stability, and telomere length.

DNA strand breaks produced by exposure of cells to chemotherapy, ionizing radiation, oxygen free radicals, or nitric oxide (NO) will cause PARP activation and poly ADP-ribose formation. This poly ADP-ribose conjugation process will induce DNA damage repair after radiotherapy or chemotherapy and lead to resistance to various tumor treatments. Therefore, inhibition of PARP is expected to delay intracellular DNA repair and enhance the antitumor effect of cancer therapy.

In tumor models, PARP inhibitors have been proven to enhance the efficacy of radiotherapy and chemotherapy, promote tumor cell apoptosis, limit tumor growth, reduce metastasis, and prolong the survival of tumor-bearing animals.

Therefore, compounds having PARP inhibitory activity are of great significance for the prevention and treatment of cancer. Although many PARP inhibitors are disclosed, such as: WO 2004080976 and WO 2009050469, many have short half-lives or are toxic. Therefore, there is still a need for novel PARP inhibitors that are useful in the treatment of hyperproliferative diseases in terms of solubility, drug interactions, efficacy, stability, selectivity, toxicity, drug resistance, pharmacokinetics and pharmacodynamics. Traits have at least one advantage. The present invention relates to a new class of PARP inhibitors.

This application claims the benefit of US Provisional Applications 63/180,058, 63/218,222, 63/248,264, 63/278,953, 63/320,162, and 63/331,810, the entire contents of which are hereby incorporated by reference in their entirety.

The invention discloses a new class of compound, its pharmaceutically acceptable salt and its pharmaceutical composition, and its application as medicine.

(I) 或其藥學上可接受的鹽，其中： X ¹選自N和CR ⁶； X ²選自N和CR ⁷； X ³選自N和CR ⁸； X ⁴選自N和CR ⁹； Q ¹選自C _3-10環烷基、雜環基和雜芳基； Q ²選自雜環基、芳基和雜芳基； L選自化學鍵、-(CR ^C0R ^D0) _u-、-(CR ^C0R ^D0) _uO(CR ^C0R ^D0) _t-、-(CR ^C0R ^D0) _uNR ^A0(CR ^C0R ^D0) _t-和-(CR ^C0R ^D0) _uS(CR ^C0R ^D0) _t-； 每個R ¹獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A1R ^B1、-OR ^A1、-C(O)R ^A1、-C(=NR ^E1)R ^A1、-C(=N-OR ^B1)R ^A1、-C(O)OR ^A1、-OC(O)R ^A1、-C(O)NR ^A1R ^B1、-C(O)NR ^A1S(O) _rR ^A1、-C(O)NR ^A1S(O) ₂OR ^A1、-C(O)NR ^A1S(O) _rNR ^A1R ^B1、-C(O)NR ^A1S(O)(=NR ^E1)R ^B1、-C(O)NR ^A1S(O)(=NR ^E1)NR ^A1R ^B1、-NR ^A1C(O)R ^B1、-C(=NR ^E1)NR ^A1R ^B1、-NR ^A1C(=NR ^E1)R ^B1、-OC(O)NR ^A1R ^B1、-NR ^A1C(O)OR ^B1、-NR ^A1C(O)NR ^A1R ^B1、-NR ^A1C(S)NR ^A1R ^B1、-NR ^A1C(=NR ^E1)NR ^A1R ^B1、-S(O) _rR ^A1、-S(O)(=NR ^E1)R ^B1、-N=S(O)R ^A1R ^B1、-S(O) ₂OR ^A1、-OS(O) ₂R ^A1、-NR ^A1S(O) _rR ^B1、-NR ^A1S(O)(=NR ^E1)R ^B1、-S(O) _rNR ^A1R ^B1、-S(O)(=NR ^E1)NR ^A1R ^B1、-NR ^A1S(O) ₂NR ^A1R ^B1、-NR ^A1S(O)(=NR ^E1)NR ^A1R ^B1、-P(O)R ^A1R ^B1和-P(O)(OR ^A1)(OR ^B1)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X1的取代基取代； 每個R ²獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A2R ^B2、-OR ^A2、-C(O)R ^A2、-C(=NR ^E2)R ^A2、-C(=N-OR ^B2)R ^A2、-C(O)OR ^A2、-OC(O)R ^A2、-C(O)NR ^A2R ^B2、-NR ^A2C(O)R ^B2、-C(=NR ^E2)NR ^A2R ^B2、-NR ^A2C(=NR ^E2)R ^B2、-OC(O)NR ^A2R ^B2、-NR ^A2C(O)OR ^B2、-NR ^A2C(O)NR ^A2R ^B2、-NR ^A2C(S)NR ^A2R ^B2、-NR ^A2C(=NR ^E2)NR ^A2R ^B2、-S(O) _rR ^A2、-S(O)(=NR ^E2)R ^B2、-N=S(O)R ^A2R ^B2、-S(O) ₂OR ^A2、-OS(O) ₂R ^A2、-NR ^A2S(O) _rR ^B2、-NR ^A2S(O)(=NR ^E2)R ^B2、-S(O) _rNR ^A2R ^B2、-S(O)(=NR ^E2)NR ^A2R ^B2、-NR ^A2S(O) ₂NR ^A2R ^B2、-NR ^A2S(O)(=NR ^E2)NR ^A2R ^B2、-P(O)R ^A2R ^B2和-P(O)(OR ^A2)(OR ^B2)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X2的取代基取代； R ³選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、CN、NO ₂、-NR ^A3R ^B3、-OR ^A3和-C(O)R ^A3，其中每個烷基、烯基、炔基、環烷基和雜環基是未被取代的或被至少一個獨立選自R ^X3的取代基取代； R ⁴選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、CN、NO ₂、-NR ^A4R ^B4、-OR ^A4和-C(O)R ^A4，其中每個烷基、烯基、炔基、環烷基和雜環基是未被取代的或被至少一個獨立選自R ^X4的取代基取代； 或R ³和R ⁴連同與它們相連的原子一起形成一個C _3-10環烷基或含1、2或3個雜原子的4-12元雜環基，其中雜原子獨立選自氧、硫、氮和磷，該環未被取代或由1、2或3個R ^X3取代基取代； R ⁵選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A5R ^B5、-OR ^A5、-C(O)R ^A5、-C(=NR ^E5)R ^A5、-C(=N-OR ^B5)R ^A5、-C(O)OR ^A5、-OC(O)R ^A5、-C(O)NR ^A5R ^B5、-NR ^A5C(O)R ^B5、-C(=NR ^E5)NR ^A5R ^B5、-NR ^A5C(=NR ^E5)R ^B5、-OC(O)NR ^A5R ^B5、-NR ^A5C(O)OR ^B5、-NR ^A5C(O)NR ^A5R ^B5、-NR ^A5C(S)NR ^A5R ^B5、-NR ^A5C(=NR ^E5)NR ^A5R ^B5、-S(O) _rR ^A5、-S(O)(=NR ^E5)R ^B5、-N=S(O)R ^A5R ^B5、-S(O) ₂OR ^A5、-OS(O) ₂R ^A5、-NR ^A5S(O) _rR ^B5、-NR ^A5S(O)(=NR ^E5)R ^B5、-S(O) _rNR ^A5R ^B5、-S(O)(=NR ^E5)NR ^A5R ^B5、-NR ^A5S(O) ₂NR ^A5R ^B5、-NR ^A5S(O)(=NR ^E5)NR ^A5R ^B5、-P(O)R ^A5R ^B5和-P(O)(OR ^A5)(OR ^B5)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X5的取代基取代； R ⁶選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A6R ^B6、-OR ^A6、-C(O)R ^A6、-C(=NR ^E6)R ^A6、-C(=N-OR ^B6)R ^A6、-C(O)OR ^A6、-OC(O)R ^A6、-C(O)NR ^A6R ^B6、-NR ^A6C(O)R ^B6、-C(=NR ^E6)NR ^A6R ^B6、-NR ^A6C(=NR ^E6)R ^B6、-OC(O)NR ^A6R ^B6、-NR ^A6C(O)OR ^B6、-NR ^A6C(O)NR ^A6R ^B6、-NR ^A6C(S)NR ^A6R ^B6、-NR ^A6C(=NR ^E6)NR ^A6R ^B6、-S(O) _rR ^A6、-S(O)(=NR ^E6)R ^B6、-N=S(O)R ^A6R ^B6、-S(O) ₂OR ^A6、-OS(O) ₂R ^A6、-NR ^A6S(O) _rR ^B6、-NR ^A6S(O)(=NR ^E6)R ^B6、-S(O) _rNR ^A6R ^B6、-S(O)(=NR ^E6)NR ^A6R ^B6、-NR ^A6S(O) ₂NR ^A6R ^B6、-NR ^A6S(O)(=NR ^E6)NR ^A6R ^B6、-P(O)R ^A6R ^B6和-P(O)(OR ^A6)(OR ^B6)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X6的取代基取代； R ⁷選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A7R ^B7、-OR ^A7、-C(O)R ^A7、-C(=NR ^E7)R ^A7、-C(=N-OR ^B7)R ^A7、-C(O)OR ^A7、-OC(O)R ^A7、-C(O)NR ^A7R ^B7、-NR ^A7C(O)R ^B7、-C(=NR ^E7)NR ^A7R ^B7、-NR ^A7C(=NR ^E7)R ^B7、-OC(O)NR ^A7R ^B7、-NR ^A7C(O)OR ^B7、-NR ^A7C(O)NR ^A7R ^B7、-NR ^A7C(S)NR ^A7R ^B7、-NR ^A7C(=NR ^E7)NR ^A7R ^B7、-S(O) _rR ^A7、-S(O)(=NR ^E7)R ^B7、-N=S(O)R ^A7R ^B7、-S(O) ₂OR ^A7、-OS(O) ₂R ^A7、-NR ^A7S(O) _rR ^B7、-NR ^A7S(O)(=NR ^E7)R ^B7、-S(O) _rNR ^A7R ^B7、-S(O)(=NR ^E7)NR ^A7R ^B7、-NR ^A7S(O) ₂NR ^A7R ^B7、-NR ^A7S(O)(=NR ^E7)NR ^A7R ^B7、-P(O)R ^A7R ^B7和-P(O)(OR ^A7)(OR ^B7)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X7的取代基取代； R ⁸選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A8R ^B8、-OR ^A8、-C(O)R ^A8、-C(=NR ^E8)R ^A8、-C(=N-OR ^B8)R ^A8、-C(O)OR ^A8、-OC(O)R ^A8、-C(O)NR ^A8R ^B8、-NR ^A8C(O)R ^B8、-C(=NR ^E8)NR ^A8R ^B8、-NR ^A8C(=NR ^E8)R ^B8、-OC(O)NR ^A8R ^B8、-NR ^A8C(O)OR ^B8、-NR ^A8C(O)NR ^A8R ^B8、-NR ^A8C(S)NR ^A8R ^B8、-NR ^A8C(=NR ^E8)NR ^A8R ^B8、-S(O) _rR ^A8、-S(O)(=NR ^E8)R ^B8、-N=S(O)R ^A8R ^B8、-S(O) ₂OR ^A8、-OS(O) ₂R ^A8、-NR ^A8S(O) _rR ^B8、-NR ^A8S(O)(=NR ^E8)R ^B8、-S(O) _rNR ^A8R ^B8、-S(O)(=NR ^E8)NR ^A8R ^B8、-NR ^A8S(O) ₂NR ^A8R ^B8、-NR ^A8S(O)(=NR ^E8)NR ^A8R ^B8、-P(O)R ^A8R ^B8和-P(O)(OR ^A8)(OR ^B8)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X8的取代基取代； R ⁹選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A9R ^B9、-OR ^A9、-C(O)R ^A9、-C(=NR ^E9)R ^A9、-C(=N-OR ^B9)R ^A9、-C(O)OR ^A9、-OC(O)R ^A9、-C(O)NR ^A9R ^B9、-NR ^A9C(O)R ^B9、-C(=NR ^E9)NR ^A9R ^B9、-NR ^A9C(=NR ^E9)R ^B9、-OC(O)NR ^A9R ^B9、-NR ^A9C(O)OR ^B9、-NR ^A9C(O)NR ^A9R ^B9、-NR ^A9C(S)NR ^A9R ^B9、-NR ^A9C(=NR ^E9)NR ^A9R ^B9、-S(O) _rR ^A9、-S(O)(=NR ^E9)R ^B9、-N=S(O)R ^A9R ^B9、-S(O) ₂OR ^A9、-OS(O) ₂R ^A9、-NR ^A9S(O) _rR ^B9、-NR ^A9S(O)(=NR ^E9)R ^B9、-S(O) _rNR ^A9R ^B9、-S(O)(=NR ^E9)NR ^A9R ^B9、-NR ^A9S(O) ₂NR ^A9R ^B9、-NR ^A9S(O)(=NR ^E9)NR ^A9R ^B9、-P(O)R ^A9R ^B9和-P(O)(OR ^A9)(OR ^B9)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X9的取代基取代； 其中， 當X ¹是CH，X ²選自N、CH和CF，X ³和X ⁴獨立選自N或CH，式(I)的

部分的結構是

，R ^B1選自氫和C _1-4烷基時，式(I)的

部分的結構不是

，其中L、Q ¹、Q ²、R ¹、R ²、R ³、R ⁴、m和n的定義與式(I)相同； 每個R ^A0獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X0的取代基取代； 每個R ^A1和R ^B1獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X1的取代基取代； 或「R ^A1和R ^B1」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X1的取代基取代； 每個R ^A2和R ^B2獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X2的取代基取代； 或「R ^A2和R ^B2」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X2的取代基取代； 每個R ^A3和R ^B3獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X3的取代基取代； 或「R ^A3和R ^B3」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X3的取代基取代； 每個R ^A4和R ^B4獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X4的取代基取代； 或「R ^A4和R ^B4」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X4的取代基取代； 每個R ^A5和R ^B5獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X5的取代基取代； 或「R ^A5和R ^B5」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X5的取代基取代； 每個R ^A6和R ^B6獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X6的取代基取代； 或「R ^A6和R ^B6」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X6的取代基取代； 每個R ^A7和R ^B7獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X7的取代基取代； 或「R ^A7和R ^B7」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X7的取代基取代； 每個R ^A8和R ^B8獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X8的取代基取代； 或「R ^A8和R ^B8」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X8的取代基取代； 每個R ^A9和R ^B9獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X9的取代基取代； 或「R ^A9和R ^B9」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X9的取代基取代； 每個R ^C0和R ^D0獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X0的取代基取代； 或者「R ^C0和R ^D0」一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可以是未被取代的或被1、2或3個R ^X0基團取代； 每個R ^E1、R ^E2、R ^E5、R ^E6、R ^E7、R ^E8和R ^E9獨立選自氫、C _1-10烷基、CN、NO ₂、-OR ^a1、-SR ^a1、-S(O) _rR ^a1、-C(O)R ^a1、C(O)OR ^a1、-C(O)NR ^a1R ^b1和-S(O) _rNR ^a1R ^b1； 每個R ^X0、R ^X1、R ^X2、R ^X3、R ^X4、R ^X5、R ^X6、R ^X7、R ^X8和R ^X9獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、鹵素、CN、-NO ₂、-(CR ^c1R ^d1) _tNR ^a1R ^b1、-(CR ^c1R ^d1) _tOR ^b1、-(CR ^c1R ^d1) _tC(O)R ^a1、-(CR ^c1R ^d1) _tC(=NR ^e1)R ^a1、-(CR ^c1R ^d1) _tC(=N-OR ^b1)R ^a1、-(CR ^c1R ^d1) _tC(O)OR ^b1、-(CR ^c1R ^d1) _tOC(O)R ^b1、-(CR ^c1R ^d1) _tC(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)R ^b1、-(CR ^c1R ^d1) _tC(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tOC(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)OR ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(S)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tS(O) _rR ^b1、-(CR ^c1R ^d1) _tS(O)(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tN=S(O)R ^a1R ^b1、-(CR ^c1R ^d1) _tS(O) ₂OR ^b1、-(CR ^c1R ^d1) _tOS(O) ₂R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O) _rR ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O)(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tS(O) _rNR ^a1R ^b1、-(CR ^c1R ^d1) _tS(O)(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O) ₂NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O)(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tP(O)R ^a1R ^b1和-(CR ^c1R ^d1) _tP(O)(OR ^a1)(OR ^b1)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 每個R ^a1和R ^b1獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 或R ^a1和R ^b1一起連同與它們相連的單個或多個原子構成含有0、1或2個額外的獨立選自氧、硫、氮和磷的雜原子的4-12元雜環，該環可任選地被1、2或3個R ^Y基團取代； 每個R ^c1和R ^d1獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 或R ^c1和R ^d1一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可任選地被1、2或3個R ^Y基團取代； 每個R ^e1獨立選自氫、C _1-10烷基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、CN、NO ₂、-OR ^a2、-SR ^a2、-S(O) _rR ^a2、-C(O)R ^a2、-C(O)OR ^a2、-S(O) _rNR ^a2R ^b2和-C(O)NR ^a2R ^b2； 每個R ^Y獨立地選自C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、鹵素、CN、-NO ₂、-NR ^a2R ^b2、-OR ^a2、-SR ^a2、-S(O) _rR ^a2、-S(O) ₂OR ^a2、-OS(O) ₂R ^b2、-S(O) _rNR ^a2R ^b2、-P(O)R ^a2R ^b2、-P(O)(OR ^a2)(OR ^b2)、-(CR ^c2R ^d2) _tNR ^a2R ^b2、-(CR ^c2R ^d2) _tOR ^b2、-(CR ^c2R ^d2) _tSR ^b2、-(CR ^c2R ^d2) _tS(O) _rR ^b2、-(CR ^c2R ^d2) _tP(O)R ^a2R ^b2、-(CR ^c2R ^d2) _tP(O)(OR ^a2)(OR ^b2)、  -(CR ^c2R ^d2) _tCO ₂R ^b2、-(CR ^c2R ^d2) _tC(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2C(O)R ^b2、-(CR ^c2R ^d2) _tNR ^a2CO ₂R ^b2、-(CR ^c2R ^d2) _tOC(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2C(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2SO ₂NR ^a2R ^b2、-NR ^a2(CR ^c2R ^d2) _tNR ^a2R ^b2、-O(CR ^c2R ^d2) _tNR ^a2R ^b2、-S(CR ^c2R ^d2) _tNR ^a2R ^b2、-S(O) _r(CR ^c2R ^d2) _tNR ^a2R ^b2、-C(O)R ^a2、-C(O)(CR ^c2R ^d2) _tOR ^b2、-C(O)(CR ^c2R ^d2) _tNR ^a2R ^b2、-C(O)(CR ^c2R ^d2) _tSR ^b2、-C(O)(CR ^c2R ^d2) _tS(O) _rR ^b2、-CO ₂R ^b2、-CO ₂(CR ^c2R ^d2) _tC(O)NR ^a2R ^b2、-OC(O)R ^a2、-CN、-C(O)NR ^a2R ^b2、-NR ^a2C(O)R ^b2、-OC(O)NR ^a2R ^b2、-NR ^a2C(O)OR ^b2、-NR ^a2C(O)NR ^a2R ^b2、-NR ^a2S(O) _rR ^b2、-CR ^a2(=N-OR ^b2)、-C(=NR ^e2)R ^a2、-C(=NR ^e2)NR ^a2R ^b2、-NR ^a2C(=NR ^e2)NR ^a2R ^b2、-CHF ₂、-CF ₃、-OCHF ₂和-OCF ₃，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自羥基、CN、氨基、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^a2和R ^b2獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基、二(C _1-10烷基)氨基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、環烷氧基、烷硫基、環烷硫基、烷氨基、環烷氨基、雜環基、芳基和雜芳基是未被取代的或被至少一個，獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 或R ^a2和R ^b2一起連同與它們相連的單個或多個原子構成含有0、1或2個額外的獨立選自氧、硫、氮和磷的雜原子的4-12元雜環，該環可任選地被1或2個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^c2和R ^d2獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基、二(C _1-10烷基)氨基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、環烷氧基、烷硫基、環烷硫基、烷氨基、環烷氨基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 或R ^c2和R ^d2一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可任選地被1或2個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^e2獨立選自氫、CN、NO ₂、C _1-10烷基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、-C(O)C _1-4烷基、-C(O)C _3-10環烷基、-C(O)OC _1-4烷基、-C(O)OC _3-10環烷基、-C(O)N(C _1-4烷基) ₂、-C(O)N(C _3-10環烷基) ₂、-S(O) ₂C _1-4烷基、-S(O) ₂C _3-10環烷基、-S(O) ₂N(C _1-4烷基) ₂和-S(O) ₂N(C _3-10環烷基) ₂； m選自0、1、2、3和4； n選自0、1、2、3和4； 每個r獨立選自0、1和2； 每個t獨立選自0、1、2、3和4； 每個u獨立選自0、1、2、3和4。 In one aspect, the present invention provides compounds represented by formula (I),

(I) or a pharmaceutically acceptable salt thereof, wherein: X ¹ is selected from N and CR ⁶ ; X ² is selected from N and CR ⁷ ; X ³ is selected from N and CR ⁸ ; X ⁴ is selected from N and CR ⁹ ; Q ¹ is selected from C _3-10 cycloalkyl, heterocyclic and heteroaryl; Q ² is selected from heterocyclic, aryl and heteroaryl; L is selected from chemical bonds, -(CR ^C0 R ^D0 ) _u -, -(CR ^C0 R ^D0 ) _u O(CR ^C0 R ^D0 ) _t -, -(CR ^C0 R ^D0 ) _u NR ^A0 (CR ^C0 R ^D0 ) _t -and-(CR ^C0 R ^D0 ) _u S(CR ^C0 R ^D0 ) _t -; each R ¹ is independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 ring Alkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 Alkyl, CN, NO ₂ , -NR ^A1 R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(=NR ^E1 )R ^A1 , -C(=N-OR ^B1 )R ^A1 , -C (O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) ₂ OR ^A1 、-C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 、-C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 、-C(O)NR ^A1 S(O )(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(O)R ^B1 , -C(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )R ^B1 , -OC(O) NR ^A1 R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -NR ^A1 C(S)NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )NR ^A1 R ^B1 , -S(O) _r R ^A1 , -S(O)(=NR ^E1 )R ^B1 , -N=S(O)R ^A1 R ^B1 , -S(O) ₂ OR ^A1 , -OS(O ) ₂ R ^A1 , -NR ^A1 S(O) _r R ^B1 , -NR ^A1 S(O)(=NR ^E1 )R ^B1 , -S(O) _r NR ^A1 R ^B1 , -S(O)(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 S(O) ₂ NR ^A1 R ^B1 , -NR ^A1 S(O)(=NR ^E1 )NR ^A1 R ^B1 , -P(O)R ^A1 R ^B1 and -P( O) (OR ^A1 ) (OR ^B1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X1 is replaced by a substituent; each R is ^{independently} selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 Cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _{1- 4} Alkyl, CN, NO ₂ , -NR ^A2 R ^B2 , -OR ^A2 , -C(O)R ^A2 , -C(=NR ^E2 )R ^A2 , -C(=N-OR ^B2 )R ^A2 , - C(O)OR ^A2 , -OC(O)R ^A2 , -C(O)NR ^A2 R ^B2 , -NR ^A2 C(O)R ^B2 , -C(=NR ^E2 )NR ^A2 R ^B2 , -NR ^A2 C(=NR ^E2 )R ^B2 , -OC(O)NR ^A2 R ^B2 , -NR ^A2 C(O)OR ^B2 , -NR ^A2 C(O)NR ^A2 R ^B2 , -NR ^A2 C(S)NR ^A2 R ^B2 、-NR ^A2 C(=NR ^E2 )NR ^A2 R ^B2 、-S(O) _r R ^A2 、-S(O)(=NR ^E2 )R ^B2 、-N=S(O)R ^A2 R ^B2 , -S(O) ₂ OR ^A2 , -OS(O) ₂ R ^A2 , -NR ^A2 S(O) _r R ^B2 , -NR ^A2 S(O)(=NR ^E2 )R ^B2 , -S(O) _r NR ^A2 R ^B2 、-S(O)(=NR ^E2 )NR ^A2 R ^B2 、-NR ^A2 S(O) ₂ NR ^A2 R ^B2 、-NR ^A2 S(O)(=NR ^E2 )NR ^A2 R ^B2 , -P(O)R ^A2 R ^B2 and -P(O)(OR ^A2 )(OR ^B2 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl R is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A3 R ^B3 , -OR ^A3 and -C(O)R ^A3 , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl and heterocyclyl is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; R ⁴ selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, Heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A4 R ^B4 , -OR ^A4 and -C(O)R ^A4 , wherein each alkyl, alkenyl, alkynyl, Cycloalkyl and heterocyclyl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or R ³ and R ⁴ together with their connected atoms form a C _3-10 cycloalkyl or containing 1, 2 or 3 heteroatoms of 4-12 membered heterocyclic groups, wherein the heteroatoms are independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring is unsubstituted or substituted by 1, 2 or 3 R ^X3 substituents; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkane radical, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A5 R ^B5 , -OR ^A5 , -C(O)R ^A5 , -C(=NR ^E5 )R ^A5 , -C(=N-OR ^B5 )R ^A5 , -C(O)OR ^A5 , -OC (O)R ^A5 , -C(O)NR ^A5 R ^B5 , -NR ^A5 C(O)R ^B5 , -C(=NR ^E5 )NR ^A5 R ^B5 , -NR ^A5 C(=NR ^E5 )R ^B5 , -OC(O)NR ^A5 R ^B5 , -NR ^A5 C(O)OR ^B5 , -NR ^A5 C(O)NR ^A5 R ^B5 , -NR ^A5 C(S)NR ^A5 R ^B5 , -NR ^A5 C(= NR ^E5 )NR ^A5 R ^B5 , -S(O) _r R ^A5 , -S(O)(=NR ^E5 )R ^B5 , -N=S(O)R ^{A5 R B5 ,} -S(O) ₂ OR ^A5 , -OS(O) ₂ R ^A5 , -NR ^A5 S(O) _r R ^B5 , -NR ^A5 S(O)(=NR ^E5 )R ^B5 , -S(O) _r NR ^A5 R ^B5 , -S( O)(=NR ^E5 )NR ^A5 R ^B5 、-NR ^A5 S(O) ₂ NR ^A5 R ^B5 、-NR ^A5 S(O)(=NR ^E5 )NR ^A5 R ^B5 、-P(O)R ^A5 R ^B5 and -P (O) (OR ^A5 ) (OR ^B5 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least A substituent independently selected from R ^X5 is substituted; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A6 R ^B6 , -OR ^A6 , -C(O)R ^A6 , -C(=NR ^E6 )R ^A6 , -C(=N-OR ^B6 )R ^A6 、-C(O)OR ^A6 、-OC(O)R ^A6 、-C(O)NR ^A6 R ^B6 、-NR ^A6 C(O)R ^B6 、-C(=NR ^E6 )NR ^A6 R ^B6 、- NR ^A6 C(=NR ^E6 )R ^B6 、-OC(O)NR ^A6 R ^B6 、-NR ^A6 C(O)OR ^B6 、-NR ^A6 C(O)NR ^A6 R ^B6 、-NR ^A6 C(S) NR ^A6 R ^B6 , -NR ^A6 C(=NR ^E6 )NR ^A6 R ^B6 , -S(O) _r R ^A6 , -S(O)(=NR ^E6 )R ^B6 , -N=S(O)R ^A6 R ^B6 、-S(O) ₂ OR ^A6 、-OS(O) ₂ R ^A6 、-NR ^A6 S(O) _r R ^B6 、-NR ^A6 S(O)(=NR ^E6 )R ^B6 、-S( O) _r NR ^A6 R ^B6 、-S(O)(=NR ^E6 )NR ^A6 R ^B6 、-NR ^A6 S(O) ₂ NR ^A6 R ^B6 、-NR ^A6 S(O)(=NR ^E6 )NR ^A6 R ^B6 , -P(O)R ^A6 R ^B6 and -P(O)(OR ^A6 )(OR ^B6 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and Heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl , C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkane base, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A7 R ^B7 , -OR ^A7 , -C(O)R ^A7 , -C(=NR ^E7 )R ^A7 , -C(=N-OR ^B7 )R ^A7 , -C(O)OR ^A7 , -OC(O)R ^A7 , -C(O)NR ^A7 R ^B7 , -NR ^A7 C(O)R ^B7 , -C (=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )R ^B7 , -OC(O)NR ^A7 R ^B7 , -NR ^A7 C(O)OR ^B7 , -NR ^A7 C(O)NR ^A7 R ^B7 , -NR ^A7 C(S)NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )NR ^A7 R ^B7 , -S(O) _r R ^A7 , -S(O)(=NR ^E7 )R ^B7 、-N=S(O)R ^A7 R ^B7 、-S(O) ₂ OR ^A7 、-OS(O) ₂ R ^A7 、-NR ^A7 S(O) _r R ^B7 、-NR ^A7 S(O) (=NR ^E7 )R ^B7 , -S(O) _r NR ^A7 R ^B7 , -S(O)(=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 S(O) ₂ NR ^A7 R ^B7 , -NR ^A7 S(O)(=NR ^E7 )NR ^A7 R ^B7 , -P(O)R ^A7 R ^B7 and -P(O)(OR ^A7 )(OR ^B7 ), wherein each of alkyl, alkenyl, alkynyl, Cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _{2 -10} alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, Aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A8 R ^B8 , -OR ^A8 , -C(O)R ^A8 、-C(=NR ^E8 )R ^A8 、-C(=N-OR ^B8 )R ^A8 、-C(O)OR ^A8 、-OC(O)R ^A8 、-C(O)NR ^A8 R ^B8 、- NR ^A8 C(O)R ^B8 、-C(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 C(=NR ^E8 )R ^B8 、-OC(O)NR ^A8 R ^B8 、-NR ^A8 C(O) OR ^B8 , -NR ^A8 C(O)NR ^A8 R ^B8 , -NR ^A8 C(S)NR ^A8 R ^B8 , -NR ^A8 C(=NR ^E8 )NR ^A8 R ^B8 , -S(O) _r R ^A8 , -S(O)(=NR ^E8 )R ^B8 , -N=S(O)R ^A8 R ^B8 , -S(O) ₂ OR ^A8 , -OS(O) ₂ R ^A8 , -NR ^A8 S(O) _r R ^B8 、-NR ^A8 S(O)(=NR ^E8 )R ^B8 、-S(O) _r NR ^A8 R ^B8 、-S(O)(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 S( O) ₂ NR ^A8 R ^B8 , -NR ^A8 S(O)(=NR ^E8 )NR ^A8 R ^B8 , -P(O)R ^A8 R ^B8 and -P(O)(OR ^A8 )(OR ^B8 ), where Each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^{X 8} ; R is selected from hydrogen, Halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, Heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A9 R ^B9 , -OR ^A9 , -C(O)R ^A9 , -C(=NR ^E9 )R ^A9 , -C(=N-OR ^B9 )R ^A9 , -C(O)OR ^A9 , -OC(O)R ^A9 , -C(O)NR ^A9 R ^B9 , -NR ^A9 C(O)R ^B9 , -C(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )R ^B9 , -OC(O)NR ^A9 R ^B9 , -NR ^A9 C(O)OR ^B9 , -NR ^A9 C(O)NR ^A9 R ^B9 , -NR ^A9 C(S)NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )NR ^A9 R ^B9 , -S(O) _r R ^A9 , -S(O)(=NR ^E9 )R ^B9 , -N=S(O)R ^A9 R ^B9 , -S(O) ₂ OR ^A9 , -OS(O) ₂ R ^A9 , -NR ^A9 S(O) _r R ^B9 , -NR ^A9 S(O)(=NR ^E9 )R ^B9 , -S(O) _r NR A9 R ^B9 , ^-S (O)(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 S(O) ₂ NR ^A9 R ^B9 , -NR ^A9 S(O)(=NR ^E9 )NR ^A9 R ^B9 , -P(O)R ^A9 R ^B9 and -P(O )(OR ^A9 )(OR ^B9 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X9 The substituent replaces; Wherein, when X ¹ is CH, X ² is selected from N, CH and CF, X ³ and X ⁴ are independently selected from N or CH, formula (I)

Part of the structure is

, R ^B1 is selected from hydrogen and C _1-4 alkyl, the formula (I)

Part of the structure is not

, wherein L, Q ¹ , Q ² , R ¹ , R ² , R ³ , R ⁴ , m and n are as defined in formula (I); each R ^A0 is independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl _- C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, Aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; each R ^A1 and R ^B1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl , _{C 2-10} alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _{1- 4} Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy Group, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X1 ; or " ^RA1 and R ^B1 " together with single or multiple atoms connected to them together form a 4-12 membered heterocycle containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 Substituents from R ^X1 are substituted; each R ^A2 and R ^B2 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, Heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; or " ^RA2 and R ^B2 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional independently selected from oxygen, A 4-12 membered heterocyclic ring of heteroatoms of sulfur, nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X2 ; each R ^A3 and R ^B3 independently selected From hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _{1- 10} alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Each of the alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl, and heteroaryl groups is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; or "R ^A3 and R ^B3 "together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the The ring can be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X3 ; each R ^A4 and R ^B4 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or " ^RA4 and R ^B4 " together together with the single or multiple atoms to which they are attached Consists of a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X4 is replaced by a substituent; each R ^A5 and R ^B5 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, hetero Aryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or Substituted by at least one substituent independently selected from R ^X5 ; or " ^RA5 and R ^B5 " together with single or multiple atoms connected to them form a substituent containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X5 ; each R ^A6 and R ^B6 are independently selected from Hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 Alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; or "R ^A6 and R ^B6 ”together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X6 ; each R ^A7 and R ^B7 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, Heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; or " ^RA7 and R ^B7 " together together form a single or multiple atoms connected to them A 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X7 is replaced by a substituent; each R ^A8 and R ^B8 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3- 10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by At least one substituent independently selected from R ^X8 is substituted; or " ^RA8 and R ^B8 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur, A 4-12 membered heterocyclic ring of nitrogen and phosphorus heteroatoms, the ring may be unsubstituted or substituted with 1, 2 or 3 substituents selected from R ^X8 ; each R ^A9 and R ^B9 are independently selected from hydrogen , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkane Oxygen, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl R, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X9 ; or "R ^A9 and R ^B9 ”together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring can be is unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X9 ; each R ^C0 and R ^D0 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl -C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is Unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; or "R ^C0 and R ^D0 "together together with the single or multiple carbon atoms to which they are attached contain 0, 1 or 2 substituents independently selected from oxygen , a 3-12 membered ring of heteroatoms of sulfur and nitrogen, which ring may be unsubstituted or substituted by 1, 2 or 3 R ^X0 groups; each of R ^E1 , R ^E2 , R ^E5 , R ^E6 , R ^E7 , R ^E8 and R ^E9 are independently selected from hydrogen, C _1-10 alkyl, CN, NO ₂ , -OR ^a1 , -SR ^a1 , -S(O) _rR ^a1 , -C(O)R ^a1 , C(O)OR ^a1 , -C(O)NR ^a1 R ^b1 , and -S(O) _r NR ^a1 R ^b1 ; each of R ^X0 , R ^X1 , R ^X2 , R ^X3 , R ^X4 , R ^X5 , R ^X6 , R ^X7 , R ^X8 and R ^X9 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl -C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl , Halogen, CN, -NO ₂ , -(CR ^c1 R ^d1 ) _t NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t OR ^b1 , -(CR ^c1 R ^d1 ) _t C(O)R ^a1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(=N-OR ^b1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(O)OR ^b1 ,- (CR ^c1 R ^d1 ) _t OC(O)R ^b1 , -(CR ^c1 R ^d1 ) _t C(O)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)R ^b1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t OC(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)OR ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C (S)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t N=S(O)R ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) ₂ OR ^b1 , -(CR ^c1 R ^d1 ) _t OS(O) ₂ R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(= NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) ₂ NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t P( O)R ^a1 R ^b1 and -(CR ^c1 R ^d1 ) _t P(O)(OR ^a1 )(OR ^b1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; each R ^a1 and R ^b1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl- C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or substituted by at least one substituent independently selected from ^RY ; or R ^a1 and R ^b1 together with the single or multiple atoms connected to them constitute 0, 1 or 2 additional independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be optionally substituted by 1, 2 or 3 ^RY groups; each R ^c1 and R ^d1 are independently selected from hydrogen, halogen, C _{1 -10} alkyl, C _2-10 alkenyl, C 2-10 alkynyl _, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl- C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; or R ^c1 and R ^d1 together, together with the single or multiple carbon atoms attached to them, constitute a 0, 1 or 2 3-12 membered rings of heteroatoms independently selected from oxygen, sulfur and nitrogen, which rings may be optionally substituted with 1, 2 or 3 ^RY groups; each R ^e1 is independently selected from Hydrogen, C _1-10 alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, CN, NO ₂ , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -C(O)R ^a2 , -C(O)OR ^a2 , -S(O) _rNR ^a2 R ^b2 and -C(O)NR ^a2 R ^b2 ; each ^RY is independently selected from C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl -C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, halogen, CN, -NO ₂ , -NR ^a2 R ^b2 , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -S(O) ₂ OR ^a2 , -OS(O) ₂ R ^b2 , -S(O) _r NR ^a2 R ^b2 , -P(O )R ^a2 R ^b2 , -P(O)(OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t OR ^b2 , -(CR ^c2 R ^d2 ) _t SR ^b2 , -(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -(CR ^c2 R ^d2 ) _t P(O)R ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t P(O) (OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C (O)R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t OC(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C( O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 SO ₂ NR ^a2 R ^b2 , -NR ^a2 (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -O(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(O) _r (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)R ^a2 , -C(O)(CR ^c2 R ^d2 ) _t OR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)(CR ^c2 R ^d2 ) _t SR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -CO ₂ R ^b2 , -CO ₂ (CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -OC(O)R ^a2 , -CN, -C(O )NR ^a2 R ^b2 , -NR ^a2 C(O)R ^b2 , -OC(O)NR ^a2 R ^b2 , -NR ^a2 C(O)OR ^b2 , -NR ^a2 C(O)NR ^a2 R ^b2 , -NR ^a2 S(O) _r R ^b2 , -CR ^a2 (=N-OR ^b2 ), -C(=NR ^e2 )R ^a2 , -C(=NR ^e2 )NR ^a2 R ^b2 , -NR ^a2 C(=NR ^e2 )NR ^a2 R ^b2 , -CHF ₂ , -CF ₃ , -OCHF ₂ and -OCF ₃ , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or by at least one member independently selected from hydroxyl, CN, amino, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{1- 10} alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _{1 -10} alkyl) amino substituent substitution; each R ^a2 and R ^b2 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkane Group, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio , C _1-10 alkylamino, C _3-10 cycloalkylamino, di(C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _{1 -4} alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, ring Alkylthio, alkylamino, cycloalkylamino, heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one, independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl radical, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkane Thio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^a2 and R ^b2 together together with the single or multiple atoms constitute a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may optionally be replaced by 1 or 2 heteroatoms independently selected from halogen, CN , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C Substituents of _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl) amino; each R ^c2 and R ^d2 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _{3- 10} cycloalkylamino, two (C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl Group-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, cycloalkylthio, alkylamino, cycloalkylamino, Heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one member independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _{3- 10} cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^c2 and R ^d2 together, together with the single or multiple carbon atoms connected to them, constitute 0, 1 or 2 independent A 3-12 membered ring of heteroatoms selected from oxygen, sulfur and nitrogen, which may optionally be replaced by 1 or 2 members independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, Amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl)amino are substituted by substituents; each R ^e2 is independently selected from hydrogen, CN, NO ₂ , C _1-10 Alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, -C(O)C _{1 -4} alkyl, -C(O)C _3-10 cycloalkyl, -C(O)OC _1-4 alkyl, -C(O)OC _3-10 cycloalkyl, -C(O)N( C _1-4 alkyl) ₂ , -C(O)N(C _3-10 cycloalkyl) ₂ , -S(O) ₂ C _1-4 alkyl, -S(O) ₂ C _3-10 ring Alkyl, -S (O) ₂ N (C _1-4 alkyl) ₂ and -S (O) ₂ N (C _3-10 cycloalkyl) ₂ ; m is selected from 0, 1, 2, 3 and 4 n is selected from 0, 1, 2, 3 and 4; each r is independently selected from 0, 1 and 2; each t is independently selected from 0, 1, 2, 3 and 4; each u is independently selected from 0, 1, 2, 3 and 4.

In another aspect, the present invention provides a pharmaceutical composition, which comprises a compound of formula (I) or at least one pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

In another aspect, the present invention provides a method for regulating PARP1, the method comprising administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or a pharmaceutical composition thereof to a system or individual in need, thereby regulating PARP1 .

The present invention also provides a method for treating, improving or preventing a disorder responding to inhibition of PARP1, comprising administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof to a system or individual in need, and Optionally in combination with a second therapeutic agent, to treat the conditions described above.

Alternatively, the present invention provides the use of the compound of formula (I) or a pharmaceutically acceptable salt thereof in the preparation of a medicament for treating PARP1-mediated disorders. In certain embodiments, the compounds are used alone or in combination with a second therapeutic agent to treat a PARP1 -mediated condition.

Alternatively, the present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof for use in the treatment of PARP1-mediated disorders.

Specifically, wherein the disorder includes, but is not limited to, autoimmune disease, transplant disease, infectious disease or abnormal cell proliferation.

In addition, the present invention provides a method for treating abnormal cell proliferation, which comprises administering an effective amount of the compound of formula (I) or its pharmaceutically acceptable salt or pharmaceutical composition to a system or individual in need, and optionally combined with The second therapeutic agent is used in combination to treat the conditions described above.

Alternatively, the present invention provides the use of the compound of formula (I) or a pharmaceutically acceptable salt in the manufacture of a medicament for treating abnormal cell proliferation. In certain embodiments, the compounds are used alone or in combination with chemotherapeutic agents to treat abnormal cell proliferation.

Specifically, wherein said abnormal cell proliferation includes, but is not limited to, lymphoma, osteosarcoma, melanoma, or tumors of the breast, kidney, prostate, colorectum, thyroid, ovary, pancreas, neurons, lung, uterus, or gastrointestinal tract.

In the above methods of using the compounds of the present invention, the compound of formula (I) or a pharmaceutically acceptable salt thereof may be administered to a system comprising cells or tissues, or to an individual comprising a mammalian individual, such as a human or an animal individual . [ term ]

Unless otherwise defined, all technical and scientific terms used in this patent have the same meaning as commonly understood by a person skilled in the art. Unless otherwise stated, all patents, patent applications, publicly disclosed materials, etc. referred to in this patent are fully incorporated by reference. If there are multiple definitions of the same term in this patent, the definition in this section shall prevail.

It is to be understood that both the foregoing general description and the following detailed description are explanatory only and are not restrictive of any claims. In this patent application, the use of the singular includes the plural unless otherwise stated. It should be noted that in the description and the appended claims, singular referents such as "a", "an", and "this" include plural referents, unless otherwise specified in the context. Also note that "or" means "and/or" unless stated otherwise. Furthermore, terms like "comprises", "comprises" and the like are not limiting.

Unless otherwise stated, conventional techniques of mass spectrometry, nuclear magnetic resonance, high performance liquid chromatography, infrared and ultraviolet/visible spectroscopy and pharmacology used in this patent are state of the art. Unless otherwise defined, nomenclature, experimental methods and techniques involved in analytical chemistry, organic synthetic chemistry, pharmaceutical and pharmaceutical chemistry in this patent are known. Standard techniques can be used for chemical syntheses, chemical analyses, preparation, formulation and administration of pharmaceuticals, and treatment of patients. Reaction and purification techniques can be carried out with reference to the manufacturer's instructions, or with reference to known common techniques, or with reference to the methods described in this patent. The techniques and operations described above can be carried out using known conventional methods and methods cited in the literature in this specification. In the specification, groups and substituents can be selected by those skilled in the art to form stable structures and compounds.

When a chemical formula is used to refer to a substituent, writing the substituent in the chemical formula from left to right is the same as writing from right to left. For example, _CH2O is the same as _OCH2 .

"Substitution" means that a hydrogen atom is replaced by a substituent. Note that the substituents on a particular atom are restricted by its valence.

As used herein, the term "C _ij " or "ij element" means that the moiety has ij carbon atoms or ij atoms. For example, "C _1-6 alkyl" means that the alkyl group has 1-6 carbon atoms. Likewise, C _3-10 cycloalkyl means that the cycloalkyl has 3-10 carbon atoms.

When any variable (such as R) occurs more than once in the structure of a compound, it is defined independently for each occurrence. Thus, for example, if a group is substituted with 0-2 R, that group may optionally be substituted with up to two R, with R being an independent choice in each case. Also, combinations of substituents and/or variations thereof are permissible only if such combinations would result in stable compounds.

"One or more" or "at least one" means one, two, three, four, five, six, seven, eight, nine or more.

Unless otherwise indicated, the term "hetero" refers to a heteroatom or group of heteroatoms (ie, a group containing heteroatoms), ie, atoms other than carbon and hydrogen atoms or a group containing these atoms. Preferably, the heteroatoms are independently selected from O, N, S, P and the like. In embodiments involving two or more heteroatoms, the two or more heteroatoms may be the same, or the two or more heteroatoms may be different in part or in total.

"Alkyl", whether used alone or in combination with other terms, refers to a branched or straight-chain saturated aliphatic hydrocarbon group with a specified number of carbon atoms. Unless otherwise specified, "alkyl" refers to C _{1 -10} alkyl. For example, "C _1-6 " in "C _1-6 alkyl" refers to a group having 1, 2, 3 _, 4, ₅ or 6 carbon atoms in a linear or branched arrangement. For example, "C _1-8 alkyl" includes, but is not limited to _, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, isobutyl, pentyl, hexyl, heptyl, and octyl .

"Cycloalkyl", whether used alone or in combination with other terms, refers to a saturated monocyclic or polycyclic (eg, bicyclic or tricyclic) hydrocarbon ring system, usually having 3 to 16 ring atoms. The ring atoms of a cycloalkyl group are all carbon, and the cycloalkyl group contains zero heteroatoms and zero double bonds. In a multicyclic cycloalkyl group, two or more rings may be fused or bridged or spliced together. Examples of single ring systems include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. Bridged cycloalkyl is a polycyclic ring system containing 3-10 carbon atoms, which contains one or two alkylene bridges, each consisting of 1, 2 or 3 carbon atoms, which are connected to the ring system Two non-adjacent carbon atoms. Cycloalkyl groups can be fused with aryl or heteroaryl groups. In some embodiments, the cycloalkyl group is benzo-fused. Representative examples of bridged cycloalkane systems include, but are not limited to, bicyclo[1.1.1]pentane, bicyclo[3.1.1]heptane, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octane, Bicyclo[3.2.2]nonane, bicyclo[3.3.1]nonane, bicyclo[4.2.1]nonane, tricyclo[3.3.1.03,7]nonane, and tricyclo[3.3.1.13,7]decane Alkane (adamantane). The cycloalkyl group can be attached to the parent molecular moiety through any substitutable atom in the ring system.

"Alkenyl", whether used alone or in combination with other terms, refers to a non-aromatic straight-chain, branched or cyclic hydrocarbon group containing 2-10 carbon atoms and having at least one carbon-carbon double bond. In some embodiments, cyclic refers to monocyclic or polycyclic. In a polycycloalkenyl, two or more rings may be joined by fusion, bridging or spiroring. In some embodiments, 1 carbon-carbon double bond is present, and up to 4 non-aromatic carbon-carbon double bonds may be present. _{Thus, "C 2-6 alkenyl} " refers to an alkenyl group _containing 2-6 carbon atoms. Alkenyl groups include, but are not limited to, vinyl, propenyl, butenyl, 2-methylbutenyl, cyclopentenyl, and cyclohexenyl. Straight chain, branched or cyclic moieties in alkenyl may contain double bonds, and if substituted alkenyl is indicated, it may be substituted.

"Alkynyl", whether used alone or in combination with other terms, refers to a straight-chain, branched or cyclic hydrocarbon group containing 2-10 carbon atoms and at least one carbon-carbon triple bond. In some embodiments, up to 3 carbon-carbon triple bonds may be present. Thus, " _C2-6alkynyl " refers to an alkynyl group _containing 2-6 carbon atoms. Alkynyl groups include, but are not limited to, ethynyl, propynyl, butynyl, 3-methylbutynyl, and the like. Straight-chain, branched or cyclic moieties in alkynyl groups may contain triple bonds, and a substituted alkynyl group indicates that it may be substituted.

"Halogen" means fluorine, chlorine, bromine, iodine.

"Alkoxy", used alone or in combination with other terms, refers to an alkyl group as defined above attached to an oxygen atom by a single bond. Alkoxy is attached to the molecule through an oxygen atom. Alkoxy may be represented as -O-alkyl. "C _1-10 alkoxy" refers to an alkoxy group containing 1-10 carbon atoms, which can be straight chain or branched. Alkoxy includes, but is not limited to, methoxy, ethoxy, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy, and the like.

"Cycloalkoxy", used alone or in combination with other terms, refers to a cycloalkyl group as defined above attached to an oxygen atom by a single bond. Cycloalkoxy is attached to the molecule through an oxygen atom. Cycloalkoxy may be represented as -O-cycloalkyl. "C _3-10 cycloalkoxy" refers to a cycloalkoxy group containing 3-10 carbon atoms. Cycloalkoxy groups can be fused with aryl or heteroaryl groups. In some embodiments, cycloalkoxy is benzo-fused. Cycloalkoxy includes, but is not limited to, cyclopropoxy, cyclobutoxy, cyclopentyloxy, cyclohexyloxy, and the like.

"Alkylthio", used alone or in combination with other terms, refers to an alkyl group as defined above attached to a sulfur atom by a single bond. The alkylthio group is attached to the molecule through the sulfur atom. Alkylthio can be represented as -S-alkyl. "C _1-10 alkylthio" refers to an alkylthio group containing 1-10 carbon atoms, which can be straight chain or branched. Alkylthio includes, but is not limited to, methylthio, ethylthio, propylthio, isopropylthio, butylthio, hexylthio and the like.

"Cycloalkylthio", used alone or in combination with other terms, refers to a cycloalkyl group as defined above linked to a sulfur atom by a single bond. The cycloalkylthio group is attached to the molecule through a sulfur atom. Cycloalkylthio can be represented as -S-cycloalkyl. "C _3-10 cycloalkylthio" refers to a cycloalkylthio group containing 3-10 carbon atoms. Cycloalkylthio can be fused with aryl or heteroaryl. In some embodiments, cycloalkylthio is benzo-fused. Cycloalkylthio includes, but is not limited to, cyclopropylthio, cyclobutylthio, cyclohexylthio and the like.

"Alkylamino", used alone or in combination with other terms, refers to an alkyl group as defined above attached to a nitrogen atom by a single bond. Alkylamino is linked to another molecule through a nitrogen atom. Alkylamino can be represented as -NH(alkyl). "C _1-10 alkylamino" refers to an alkylamino group containing 1-10 carbon atoms, which can be straight chain or branched. Alkylamino groups include, but are not limited to, methylamino, ethylamino, propylamino, isopropylamino, butylamino, hexylamino, and the like.

"Cycloalkylamino", used alone or in combination with other terms, refers to a cycloalkyl group as defined above attached to a nitrogen atom by a single bond. A cycloalkylamino group is linked to another molecule through a nitrogen atom. Cycloalkylamino can be represented as -NH(cycloalkyl). "C _3-10 cycloalkylamino" refers to a cycloalkylamino group containing 3-10 carbon atoms. Cycloalkylamino groups can be fused with aryl or heteroaryl groups. In some embodiments, the cycloalkylamino group is benzo-fused. Cycloalkylamino includes, but is not limited to, cyclopropylamino, cyclobutylamino, cyclohexylamino, and the like.

"Di(alkyl)amino", used alone or in combination with other terms, refers to two alkyl groups as defined above linked by a single bond to a nitrogen atom. The di(alkyl)amino group is attached to the molecule through a nitrogen atom. A di(alkyl)amino group can be represented as -N(alkyl) ₂ . "Di(C _1-10 alkyl)amino" refers to a di(C _1-10 alkyl)amino whose two alkyl moieties respectively contain 1-10 carbon atoms, which can be straight chain or branched.

"Aryl", used alone or in combination with other terms, means a group having 6, 7, 8, 9, 10, 11, 12, 13 or 14 carbon atoms (" _C6-14aryl " group) Monovalent, monocyclic, bicyclic or tricyclic aromatic hydrocarbon ring systems, especially rings having 6 carbon atoms (“C ₆ aryl” group), for example phenyl; or rings having 10 carbon atoms (“C ₁₀ aryl" group), such as naphthyl; or a ring having 14 carbon atoms ("C ₁₄ aryl" group), such as anthracenyl. Aryl groups can be fused with cycloalkyl or heterocyclyl groups.

The divalent groups formed by substituted benzene derivatives and having free valence electrons on the ring atoms are named substituted phenylene groups. A divalent group derived from a monovalent polycyclic hydrocarbon group whose name ends in "-yl", which is obtained by removing a hydrogen atom from a carbon atom containing free valence electrons, and its name is in the monovalent group Adding "-idene" to the name, for example, a naphthyl group with two attachment points is called a naphthylene group.

"Heteroaryl", used alone or in combination with other terms, means a group having 5, 6, 7, 8, 9, 10, 11, 12, 13 or 14 ring atoms ("5 to 14 membered heteroaryl" A monovalent, monocyclic, bicyclic or tricyclic aromatic ring system, especially 5 or 6 or 9 or 10 atoms, and containing at least one heteroatom, which may be the same or different, selected from N, O and S. A heteroaryl can be fused with a cycloalkyl or heterocyclyl. In some embodiments, "heteroaryl" refers to a 5- to 8-membered aromatic monocyclic ring containing 1 to 4 members selected from N, O and S, in some embodiments 1 to 3 heteroatoms, the rest being carbon atoms; and 8- to 12-membered bicyclic rings containing 1 to 6, in certain embodiments 1 to 4, selected from N, O and S heteroatoms, or in certain embodiments from 1 to 3 heteroatoms, the remainder being carbon atoms, at least one of which is present in the aromatic ring; and 11- to 14-membered tricyclic rings, the The ring contains N, O and S, in a number of 1 to 8, in certain embodiments, in a number of 1 to 6, or in certain embodiments, in a number of 1 to 4, or in certain embodiments In some embodiments, there are 1 to 3 heteroatoms, and the rest are carbon atoms.

When the total number of S and O in the heteroaryl group is greater than 1, the heteroatoms are not adjacent to each other. In some embodiments, the total number of S and O in the heteroaryl is no greater than 2. In some embodiments, the total number of S and O in the heteroaryl is no greater than one.

Examples of heteroaryl include, but are not limited to, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 3-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl , 6-pyrimidinyl, 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 1-imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl, Pyridazinyl, triazinyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, triazolyl, tetrazolyl, thienyl, furyl.

Further, heteroaryl includes, but is not limited to, indolyl, benzothienyl, benzofuryl, benzimidazolyl, benzotriazolyl, quinoxalinyl, quinolinyl and isoquinolyl. "Heteroaryl" includes the N-oxide derivative of any nitrogen-containing heteroaryl.

The name of the monovalent heteroaryl group ends with "-group", and the derived divalent group is obtained by removing a hydrogen atom from the carbon atom containing free valence electrons. The divalent group The nomenclature is based on adding "-idene" to the name of the monovalent group, for example: a pyridyl group with two linking sites is called a pyridyl group.

"Heterocycle" (and derivatives thereof such as "heterocyclic" or "heterocyclyl") generally refers to saturated or unsaturated, monocyclic or polycyclic (e.g. bicyclic or tricyclic) cyclic aliphatic hydrocarbon systems, Usually 3 to 16 ring atoms, containing at least 1 (eg: 2, 3 or 4) heteroatoms (preferably oxygen, sulfur, nitrogen) independently selected from oxygen, sulfur, nitrogen and phosphorus. In polycyclic ring systems two or more rings may be joined by fused, bridged or spiro rings, and heterocycles may be fused to aryl or heteroaryl groups. In some embodiments, the heterocycle is benzo-fused. Heterocycles also include ring systems substituted with one or more oxo or imino moieties. In some embodiments, the C, N, S and P atoms in the heterocycle are optionally substituted with oxo. In some embodiments, the C, S and P atoms in the heterocycle are optionally substituted with imino groups, and the imino groups may be unsubstituted or substituted. Either a carbon atom or a heteroatom on the heterocycle can be the linking site, provided a stable structure is formed. When there is a substituent on the heterocyclic ring, the substituent can be connected to any heteroatom or carbon atom on the heterocyclic ring, provided that a stable chemical structure is formed.

,

,

,

,

,

,

,

,

和

。 Suitable heterocycles include, for example, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 1-imidazolidinyl, 2-imidazolidinyl, 3-imidazolidinyl, 4-imidazolidinyl, 5 - imidazolidinyl, 1-pyrazolidinyl, 2-pyrazolidinyl, 3-pyrazolidinyl, 4-pyrazolidinyl, 5-pyrazolidinyl, 1-piperidinyl, 2-piperidine Base, 3-piperidinyl, 4-piperidinyl, 1-piperazinyl, 2-piperazinyl, 3-piperazinyl, 1-hexahydropyridazinyl, 3-hexahydropyridazinyl, 4- Hexahydropyridazinyl and tetrahydropyridyl. Also included are morpholinyl groups such as 1-morpholinyl, 2-morpholinyl, 3-morpholinyl and 4-morpholinyl. Examples of heterocycles with one or more oxo moieties include, but are not limited to, piperidinyl-N-oxide, morpholinyl-N-oxide, 1-oxo-thiomorpholinyl and 1,1- Dioxo-thiomorpholinyl. Bicyclic heterocycles include, but are not limited to:

,

,

,

,

,

,

,

,

and

.

"Aryl-alkyl" as used herein refers to an alkyl group as defined above substituted with an aryl group as defined above. Exemplary aralkyl groups include, but are not limited to, benzyl, phenethyl, naphthylmethyl, and the like. In some implementations, the aralkyl group contains 7-20 or 7-11 carbon atoms. When "arylC _1-4 alkyl" is used, wherein "C _1-4 " means the number of carbon atoms in the alkyl moiety instead of the aryl moiety.

As used herein, "heterocyclyl-alkyl" refers to a heterocyclyl as defined above substituted for an alkyl as defined above. When "heterocyclylC _1-4 alkyl" is used, "C _1-4 " means the number of carbon atoms in the alkyl moiety other than the heterocyclyl moiety.

"Cycloalkyl-alkyl" as used herein refers to an alkyl group as defined above substituted with a cycloalkyl group as defined above. When "C _3-10 cycloalkyl-C _1-4 alkyl" is used, "C _3-10 " means the number of carbon atoms in the cycloalkyl moiety other than the alkyl moiety. Wherein "C _1-4 " refers to the number of carbon atoms in the alkyl moiety other than the cycloalkyl moiety.

As used herein, "heteroaryl-alkyl" refers to an alkyl group as defined above substituted with a heteroaryl group as defined above. When "heteroaryl-C _1-4 alkyl" is used, wherein "C _1-4 " means the number of carbon atoms in the alkyl moiety other than the heteroaryl moiety.

For the avoidance of ambiguity, for example: when referring to alkyl, cycloalkyl, heterocyclylalkyl, aryl, and/or heteroaryl substitutions thereof, it is meant that each of these groups is individually substituted, or It means that these groups are mixed and substituted. That is: if R is aryl-C _1-4 alkyl, and may be unsubstituted or substituted by at least one substituent, such as 1, 2, 3 or 4 substituents independently selected from R ^X , It will be appreciated that the aryl moiety may be unsubstituted or substituted by at least one, such as 1, 2, 3 or 4 substituents independently selected from ^R , and the alkyl moiety may also be unsubstituted or substituted by at least one, Such as 1, 2, 3 or 4 substituents independently selected from R ^X are substituted.

"Pharmaceutically acceptable salt" refers to salts made with pharmaceutically acceptable non-toxic bases or acids, including inorganic or organic bases and inorganic or organic acids. Salts of inorganic bases may be selected from, for example: aluminum, ammonium, calcium, copper, ferric, ferrous, lithium, magnesium, manganese, manganous, potassium, sodium, zinc salts. Further, the salts of pharmaceutically acceptable inorganic bases can be selected from ammonium, calcium, magnesium, potassium, and sodium salts. A solid salt may exist in one or more crystalline forms, or polymorphs, and may also exist in the form of solvates, such as hydrates. Pharmaceutically acceptable salts of organic non-toxic bases may be selected from, for example: primary, secondary and tertiary amine salts, substituted amines including naturally occurring substituted amines, cyclic amines, basic ion exchange resins such as arginine, beet Alkaline, caffeine, choline, N,N' -dibenzylethylenediamine, diethylamine, 2-diethylaminoethanol, 2-dimethylaminoethanol, ethanolamine, ethylenediamine, N -ethylmorpholine, N -ethylpiperidine, glucosamine, glucosamine, histidine, hypamine, isopropylamine, lysine, methylglucosamine, morpholine, piperazine, piperidine, polyamine resin, procarb Because, purine, cocoaline, triethylamine, trimethylamine, tripropylamine, tromethamine.

When the compound referred to in this patent is alkali, its salt needs to be prepared with at least one pharmaceutically acceptable non-toxic acid, and these acids are selected from inorganic acids and organic acids. For example, selected from acetic acid, benzenesulfonic acid, benzoic acid, camphorsulfonic acid, citric acid, ethanesulfonic acid, fumaric acid, gluconic acid, glutamic acid, hydrobromic acid, hydrochloric acid, isethionic acid, lactic acid, horse Lactic acid, malic acid, mandelic acid, methanesulfonic acid, mucic acid, nitric acid, pamoic acid, pantothenic acid, phosphoric acid, succinic acid, sulfuric acid, tartaric acid, p-toluenesulfonic acid. In some embodiments, acids such as citric acid, hydrobromic acid, hydrochloric acid, maleic acid, phosphoric acid, sulfuric acid, fumaric acid, tartaric acid may be selected.

"Administering" or "administering" a compound or a pharmaceutically acceptable salt thereof means providing a compound of the present invention or a pharmaceutically acceptable salt thereof to an individual in need of treatment.

"Effective amount" refers to a dose of a compound or a pharmaceutically acceptable salt thereof capable of causing biological or medical responses in tissues, systems, animals or humans that can be observed by researchers, veterinarians, clinicians or other clinical personnel.

"Composition" includes: a product containing specified ingredients in specified amounts, and any product resulting from the direct or indirect combination of these specified ingredients in specified amounts. Pharmaceutical compositions, including: products containing active ingredients and inert ingredients as carriers, and products made by combining, compounding or aggregating any two or more ingredients directly or indirectly, or through one or more products resulting from the decomposition of its components, or through other types of reactions or interactions of one or more components.

"Pharmaceutically acceptable" means compatible with the other ingredients in the formulation and not unacceptably toxic to the user.

"Individual" means an individual suffering from a disease, condition or the like, including mammals and non-mammals. Mammals include, but are not limited to, any member of the class Mammalia: humans, non-human primates such as chimpanzees, and other apes and monkeys; farm animals such as cows, horses, sheep, goats, pigs; domestic animals such as rabbits, dogs and cats; experimental animals include rodents such as rats, mice and guinea pigs. Non-mammalian animals include, but are not limited to, birds, fish, etc. In one embodiment of the invention, the mammal is a human.

"Treatment" includes relieving, alleviating or ameliorating a disease or a symptom, preventing other symptoms, ameliorating or preventing underlying metabolic factors of a symptom, inhibiting a disease or a symptom, for example, arresting the development of a disease or a symptom, alleviating a disease or a symptom, promoting remission of a disease or a symptom, Or to cause the symptoms of a disease or condition to cease, and extends to include prophylaxis. "Treatment" also includes achieving therapeutic benefit and/or prophylactic benefit. Therapeutic benefit refers to eradication or amelioration of the condition being treated. In addition, therapeutic benefit is achieved by eradicating or ameliorating one or more physiological symptoms associated with the underlying disease, whereby improvement in the patient's disease is observed although the patient may still suffer from the underlying disease. Prophylactic benefit means that the composition is used by the patient to prevent the risk of a certain disease, or when the patient has one or more physiological symptoms of the disease, although the disease has not yet been diagnosed.

"Protecting group" (Pg) refers to a class of substituents used to block or protect a specific functional group by reacting with other functional groups on a compound. For example, "amino-protecting group" refers to a substituent attached to an amino group to block or protect the amino functional group on a compound. Suitable amino protecting groups include acetyl, trifluoroacetyl, tert-butoxycarbonyl (BOC), benzyloxycarbonyl (CBZ) and 9-fluorenylmethoxycarbonyl protecting group (Fmoc). Likewise, "hydroxyl protecting group" refers to a class of hydroxy substituents effective to block or protect the hydroxy function. Suitable protecting groups include, but are not limited to, acetyl and silyl groups. "Carboxyl protecting group" refers to a class of carboxyl substituents that can effectively block or protect the carboxyl group. Common carboxyl protecting groups include -CH ₂ CH ₂ SO ₂ Ph, cyanoethyl, 2-(trimethylsilyl)ethyl, 2-(trimethylsilyl)ethoxymethyl, 2-(p-toluenesulfonyl) Ethyl, 2-(p-nitrophenylsulfinyl)ethyl, 2-(diphenylphosphine)-ethyl, nitroethyl, etc. For a general description and instructions for protecting groups, see references: TW Greene, Protective Groups in Organic Synthesis, John Wiley & Sons , New York , 1991 .

"NH protecting group" includes, but is not limited to, trichloroethoxycarbonyl, tribromoethoxycarbonyl, benzyloxycarbonyl, p-nitrobenzylcarboyl, o-bromobenzyloxycarbonyl, chloroacetyl, dichloroacetyl base, trichloroacetyl, trifluoroacetyl, phenylacetyl, formyl, acetyl, benzoyl, tert-amyloxycarbonyl, tert-butoxycarbonyl, p-methoxybenzyloxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl, 4-(phenylazo)benzyloxycarbonyl, 2-furfuryloxycarbonyl, diphenylmethoxycarbonyl, 1,1-dimethylpropoxycarbonyl, Isopropoxycarbonyl, phthaloyl, succinyl, alanyl, leucyl, 1-adamantyloxycarbonyl, 8-quinolyloxycarbonyl, benzyl, benzhydryl, three Benzyl, 2-nitrophenylthio, methylsulfonyl, p-toluenesulfonyl, N,N -dimethylaminomethylene, benzylidene, 2-hydroxybenzylidene, 2- Hydroxy-5-chlorobenzylidene, 2-hydroxy-l-naphthylmethylene, 3-hydroxy-4-pyridylmethylene, cyclohexylene, 2-ethoxycarbonylcyclohexylene, 2- Ethoxycarbonylcyclopentylene, 2-acetylcyclohexylene, 3,3-dimethyl-5-oxycyclohexylene, diphenylphosphoryl, dibenzylphosphoryl, 5-methyl yl-2-oxyl- 2H -l,3-dioxol-4-yl-methyl, trimethylsilyl, triethylsilyl and triphenylsilyl.

"C(O)OH" protecting groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, 1,1-dimethylpropyl, n-butyl, tert-butyl, phenyl, Naphthyl, benzyl, benzhydryl, trityl, p-nitrobenzyl, p-methoxybenzyl, bis(p-methoxyphenyl)methyl, acetylmethyl, benzoylmethyl , p-nitrobenzoyl, p-bromobenzoyl, p-methylsulfonylbenzoyl, 2-tetrahydropyranyl, 2-tetrahydrofuranyl, 2,2,2-trichloroethyl 2-(trimethylsilyl)ethyl, acetyloxymethyl, propionyloxymethyl, pivalyloxymethyl, phthalimidemethyl, succinimide Methyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, methoxymethyl, methoxyethoxymethyl, 2-(trimethylsilyl)ethoxymethyl, benzyl Oxymethyl, methylthiomethyl, 2-methylthioethyl, phenylthiomethyl, 1,1-dimethyl-2-propenyl, 3-methyl-3-butene group, allyl group, trimethylsilyl group, triethylsilyl group, triisopropylsilyl group, diethylisopropylsilyl group, tert-butyldimethylsilyl group, tert-butyldiphenylsilane group group, diphenylmethylsilyl group and tert-butylmethoxyphenylsilyl group.

"OH or SH" protecting groups include, but are not limited to, benzyloxycarbonyl, 4-nitrobenzyloxycarbonyl, 4-bromobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl Oxycarbonyl, methoxycarbonyl, ethoxycarbonyl, tert-butoxycarbonyl, 1,1-dimethylpropoxycarbonyl, isopropoxycarbonyl, isobutoxycarbonyl, diphenylmethoxycarbonyl, 2, 2,2-trichloroethoxycarbonyl, 2,2,2-tribromoethoxycarbonyl, 2-(trimethylsilane)ethoxycarbonyl, 2-(benzenesulfonyl)ethoxycarbonyl, 2-(triphenylphosphonium)ethoxycarbonyl, 2-furfuryloxycarbonyl, 1-adamantyloxycarbonyl, vinyloxycarbonyl, allyloxycarbonyl, 4-ethoxy- 1-naphthyloxycarbonyl, 8-quinolyloxycarbonyl, acetyl, formate, chloroacetyl, dichloroacetyl, trichloroacetyl, trifluoroacetyl, methoxy Acetyl, phenoxyacetyl, popentyl, benzoyl, methyl, tert-butyl, 2,2,2-trichloroethyl, 2-trimethylsilylethyl, 1 ,1-Dimethyl-2-propenyl, 3-methyl-3-butenyl, allyl, benzyl (phenylmethyl), p-methoxybenzyl, 3,4-dimethoxy benzyl, diphenylmethyl, triphenylmethyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiopyranyl, methoxymethyl, methylthiomethyl, benzyloxymethyl , 2-methoxyethoxymethyl, 2,2,2-trichloro-ethoxymethyl, 2-(trimethylsilyl)ethoxymethyl, 1-ethoxyethyl, Methylsulfonyl, p-toluenesulfonyl, trimethylsilyl, triethylsilyl, triisopropylsilyl, diethylisopropylsilyl, tert-butyldimethylsilyl, tert-butyl Diphenylsilyl, diphenylmethylsilyl and tert-butylmethoxyphenylsilyl.

Geometric isomers may exist in the compounds of the present invention. The compounds of the present invention may have a carbon-carbon double bond or a carbon-nitrogen double bond in E or Z configuration, wherein "E" represents that according to the Cahn-Ingold-Prelog priority rule, the preferred substituent is at the carbon-carbon double bond or carbon -different sides of the nitrogen double bond, and "Z" represents a preferred substituent on the same side of the carbon-carbon double bond or carbon-nitrogen double bond. The compounds of the present invention may also be "E" and "Z" isomers exists in the form of a mixture. Substituents around a cycloalkyl or heterocyclyl group can be configured in cis or trans configuration. In addition, the present invention includes different isomers formed by different arrangements of substituents around the adamantane ring system and mixtures thereof. The two substituents around a single ring in the adamantane ring system are assigned the Z or E relative configuration. See, eg, C. D. Jones, M. Kaselj, R. N. Salvatore, W. J. le Noble J. Org. Chem. 1998, 63, 2758-2760.

The compounds of the present invention may contain asymmetrically substituted carbon atoms in the R or S configuration. For the definitions of "R" and "S", see IUPAC 1974 Recommendations for Section E, Fundamental Stereochemistry, Pure Appl. Chem. (1976) 45, 13- 10. Compounds containing asymmetrically substituted carbon atoms are racemates if the amounts of R and S configurations are the same. If one of the configurations is more abundant than the other, the configuration of the chiral carbon atom is expressed as the configuration with a greater amount, preferably in an enantiomeric excess of about 85-90%, more preferably about 95-99%, Further about 99% or more. Accordingly, the present invention includes racemic mixtures, relative and absolute stereoisomers, and mixtures of relative and absolute stereoisomers.

[ Isotopically enriched or labeled compounds ]

The compounds of the present invention may exist in isotopically labeled or enriched forms containing one or more atoms having an atomic mass and mass number different from the most common atomic mass and mass number found in nature. Isotopes can be radioactive or non-radioactive isotopes. Isotopes of atoms such as hydrogen, carbon, nitrogen, oxygen, phosphorus, sulfur, fluorine, chlorine, and iodine include, but are not limited to, ² H, ³ H, ¹³ C ^{, 14 C, 15 N, 18 O , 32} P, ³⁵ S , ¹⁸ F, ³⁶ Cl and ¹²⁵ I. Other isotopes and/or other atoms containing these atoms are also within the scope of the invention.

In another embodiment, the isotopically labeled compound contains deuterium ( ² H), tritium ( ³ H) or ¹⁴ C isotopes. Isotopically labeled compounds of the invention can be obtained using methods well known to those skilled in the art. These isotope-labeled compounds can be obtained by referring to the examples and reaction diagrams of the present invention and replacing non-labeled reagents with isotope-labeled reagents. In some instances, compounds can be treated with isotopically labeled reagents to replace atoms with isotopic atoms, for example, replacement of hydrogen with _deuterium can be exchanged by the action of a deuterated acid such as _D2SO4 / _D2O .

The isotope-labeled compound of the present invention can be used as a standard for a PARP1 inhibitor drug effect binding test. Isotope-containing compounds can be used in pharmaceutical research to evaluate the mechanism of action and metabolic pathways of non-isotope-labeled parent compounds, and to study the in vivo metabolic fate of compounds (Blake et al. J. Pharm. Sci. 64, 3, 367-391 (1975) ). This type of metabolism study is important for the design of safe and effective therapeutics, and it can be determined whether the active compound in the patient's body or the metabolite of the parent compound is toxic or carcinogenic (Foster et al., Advances in Drug Research Vol. 14, pp 2-36, Academic press, London, 1985; Kato et al, J. Labeled Compounds. Radiopharmaceuticals., 36(10), 927-932 (1995); Kushner et al., Can. J. Physiol. Pharmacology, 77 , 79-88 (1999).

In addition, drugs containing non-reflective active isotopes, such as deuterated drugs, known as "heavy drugs", can be used to treat diseases and conditions related to PARP1 activity. The ratio of a certain isotope in a compound exceeds its natural abundance is called enrichment. Enriched amounts include, but are not limited to, for example, from about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37, 42 , 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96 to about 100 mol %.

Isotopic labeling of stable drugs can alter their physicochemical properties, such as pKa and liquid solubility. If isotopic substitutions affect regions involved in ligand-receptor interactions, these effects and changes may affect the pharmacodynamic response of drug molecules. Stable isotope-labeled molecules have certain physical properties that differ from unlabeled molecules, while chemical and biological properties are the same, with one important difference: Due to the increased mass of the heavy isotope, any chemical bond that includes a heavy isotope and another atom is stronger than a light isotope. powerful. Accordingly, the presence of an isotope at a site of metabolism or enzymatic conversion slows down this reaction, thereby potentially altering its pharmacokinetic profile or potency compared to a non-isotopically labeled compound.

(I) 或其藥學上可接受的鹽，其中： X ¹選自N和CR ⁶； X ²選自N和CR ⁷； X ³選自N和CR ⁸； X ⁴選自N和CR ⁹； Q ¹選自C _3-10環烷基、雜環基和雜芳基； Q ²選自雜環基、芳基和雜芳基； L選自化學鍵、-(CR ^C0R ^D0) _u-、-(CR ^C0R ^D0) _uO(CR ^C0R ^D0) _t-、-(CR ^C0R ^D0) _uNR ^A0(CR ^C0R ^D0) _t-和-(CR ^C0R ^D0) _uS(CR ^C0R ^D0) _t-； 每個R ¹獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A1R ^B1、-OR ^A1、-C(O)R ^A1、-C(=NR ^E1)R ^A1、-C(=N-OR ^B1)R ^A1、-C(O)OR ^A1、-OC(O)R ^A1、-C(O)NR ^A1R ^B1、-C(O)NR ^A1S(O) _rR ^A1、-C(O)NR ^A1S(O) ₂OR ^A1、-C(O)NR ^A1S(O) _rNR ^A1R ^B1、-C(O)NR ^A1S(O)(=NR ^E1)R ^B1、-C(O)NR ^A1S(O)(=NR ^E1)NR ^A1R ^B1、-NR ^A1C(O)R ^B1、-C(=NR ^E1)NR ^A1R ^B1、-NR ^A1C(=NR ^E1)R ^B1、-OC(O)NR ^A1R ^B1、-NR ^A1C(O)OR ^B1、-NR ^A1C(O)NR ^A1R ^B1、-NR ^A1C(S)NR ^A1R ^B1、-NR ^A1C(=NR ^E1)NR ^A1R ^B1、-S(O) _rR ^A1、-S(O)(=NR ^E1)R ^B1、-N=S(O)R ^A1R ^B1、-S(O) ₂OR ^A1、-OS(O) ₂R ^A1、-NR ^A1S(O) _rR ^B1、-NR ^A1S(O)(=NR ^E1)R ^B1、-S(O) _rNR ^A1R ^B1、-S(O)(=NR ^E1)NR ^A1R ^B1、-NR ^A1S(O) ₂NR ^A1R ^B1、-NR ^A1S(O)(=NR ^E1)NR ^A1R ^B1、-P(O)R ^A1R ^B1和-P(O)(OR ^A1)(OR ^B1)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X1的取代基取代； 每個R ²獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A2R ^B2、-OR ^A2、-C(O)R ^A2、-C(=NR ^E2)R ^A2、-C(=N-OR ^B2)R ^A2、-C(O)OR ^A2、-OC(O)R ^A2、-C(O)NR ^A2R ^B2、-NR ^A2C(O)R ^B2、-C(=NR ^E2)NR ^A2R ^B2、-NR ^A2C(=NR ^E2)R ^B2、-OC(O)NR ^A2R ^B2、-NR ^A2C(O)OR ^B2、-NR ^A2C(O)NR ^A2R ^B2、-NR ^A2C(S)NR ^A2R ^B2、-NR ^A2C(=NR ^E2)NR ^A2R ^B2、-S(O) _rR ^A2、-S(O)(=NR ^E2)R ^B2、-N=S(O)R ^A2R ^B2、-S(O) ₂OR ^A2、-OS(O) ₂R ^A2、-NR ^A2S(O) _rR ^B2、-NR ^A2S(O)(=NR ^E2)R ^B2、-S(O) _rNR ^A2R ^B2、-S(O)(=NR ^E2)NR ^A2R ^B2、-NR ^A2S(O) ₂NR ^A2R ^B2、-NR ^A2S(O)(=NR ^E2)NR ^A2R ^B2、-P(O)R ^A2R ^B2和-P(O)(OR ^A2)(OR ^B2)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X2的取代基取代； R ³選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、CN、NO ₂、-NR ^A3R ^B3、-OR ^A3和-C(O)R ^A3，其中每個烷基、烯基、炔基、環烷基和雜環基是未被取代的或被至少一個獨立選自R ^X3的取代基取代； R ⁴選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、CN、NO ₂、-NR ^A4R ^B4、-OR ^A4和-C(O)R ^A4，其中每個烷基、烯基、炔基、環烷基和雜環基是未被取代的或被至少一個獨立選自R ^X4的取代基取代； 或R ³和R ⁴連同與它們相連的原子一起形成一個C _3-10環烷基或含1、2或3個雜原子的4-12元雜環基，其中雜原子獨立選自氧、硫、氮和磷，該環未被取代或由1、2或3個R ^X3取代基取代； R ⁵選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A5R ^B5、-OR ^A5、-C(O)R ^A5、-C(=NR ^E5)R ^A5、-C(=N-OR ^B5)R ^A5、-C(O)OR ^A5、-OC(O)R ^A5、-C(O)NR ^A5R ^B5、-NR ^A5C(O)R ^B5、-C(=NR ^E5)NR ^A5R ^B5、-NR ^A5C(=NR ^E5)R ^B5、-OC(O)NR ^A5R ^B5、-NR ^A5C(O)OR ^B5、-NR ^A5C(O)NR ^A5R ^B5、-NR ^A5C(S)NR ^A5R ^B5、-NR ^A5C(=NR ^E5)NR ^A5R ^B5、-S(O) _rR ^A5、-S(O)(=NR ^E5)R ^B5、-N=S(O)R ^A5R ^B5、-S(O) ₂OR ^A5、-OS(O) ₂R ^A5、-NR ^A5S(O) _rR ^B5、-NR ^A5S(O)(=NR ^E5)R ^B5、-S(O) _rNR ^A5R ^B5、-S(O)(=NR ^E5)NR ^A5R ^B5、-NR ^A5S(O) ₂NR ^A5R ^B5、-NR ^A5S(O)(=NR ^E5)NR ^A5R ^B5、-P(O)R ^A5R ^B5和-P(O)(OR ^A5)(OR ^B5)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X5的取代基取代； R ⁶選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A6R ^B6、-OR ^A6、-C(O)R ^A6、-C(=NR ^E6)R ^A6、-C(=N-OR ^B6)R ^A6、-C(O)OR ^A6、-OC(O)R ^A6、-C(O)NR ^A6R ^B6、-NR ^A6C(O)R ^B6、-C(=NR ^E6)NR ^A6R ^B6、-NR ^A6C(=NR ^E6)R ^B6、-OC(O)NR ^A6R ^B6、-NR ^A6C(O)OR ^B6、-NR ^A6C(O)NR ^A6R ^B6、-NR ^A6C(S)NR ^A6R ^B6、-NR ^A6C(=NR ^E6)NR ^A6R ^B6、-S(O) _rR ^A6、-S(O)(=NR ^E6)R ^B6、-N=S(O)R ^A6R ^B6、-S(O) ₂OR ^A6、-OS(O) ₂R ^A6、-NR ^A6S(O) _rR ^B6、-NR ^A6S(O)(=NR ^E6)R ^B6、-S(O) _rNR ^A6R ^B6、-S(O)(=NR ^E6)NR ^A6R ^B6、-NR ^A6S(O) ₂NR ^A6R ^B6、-NR ^A6S(O)(=NR ^E6)NR ^A6R ^B6、-P(O)R ^A6R ^B6和-P(O)(OR ^A6)(OR ^B6)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X6的取代基取代； R ⁷選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A7R ^B7、-OR ^A7、-C(O)R ^A7、-C(=NR ^E7)R ^A7、-C(=N-OR ^B7)R ^A7、-C(O)OR ^A7、-OC(O)R ^A7、-C(O)NR ^A7R ^B7、-NR ^A7C(O)R ^B7、-C(=NR ^E7)NR ^A7R ^B7、-NR ^A7C(=NR ^E7)R ^B7、-OC(O)NR ^A7R ^B7、-NR ^A7C(O)OR ^B7、-NR ^A7C(O)NR ^A7R ^B7、-NR ^A7C(S)NR ^A7R ^B7、-NR ^A7C(=NR ^E7)NR ^A7R ^B7、-S(O) _rR ^A7、-S(O)(=NR ^E7)R ^B7、-N=S(O)R ^A7R ^B7、-S(O) ₂OR ^A7、-OS(O) ₂R ^A7、-NR ^A7S(O) _rR ^B7、-NR ^A7S(O)(=NR ^E7)R ^B7、-S(O) _rNR ^A7R ^B7、-S(O)(=NR ^E7)NR ^A7R ^B7、-NR ^A7S(O) ₂NR ^A7R ^B7、-NR ^A7S(O)(=NR ^E7)NR ^A7R ^B7、-P(O)R ^A7R ^B7和-P(O)(OR ^A7)(OR ^B7)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X7的取代基取代； R ⁸選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A8R ^B8、-OR ^A8、-C(O)R ^A8、-C(=NR ^E8)R ^A8、-C(=N-OR ^B8)R ^A8、-C(O)OR ^A8、-OC(O)R ^A8、-C(O)NR ^A8R ^B8、-NR ^A8C(O)R ^B8、-C(=NR ^E8)NR ^A8R ^B8、-NR ^A8C(=NR ^E8)R ^B8、-OC(O)NR ^A8R ^B8、-NR ^A8C(O)OR ^B8、-NR ^A8C(O)NR ^A8R ^B8、-NR ^A8C(S)NR ^A8R ^B8、-NR ^A8C(=NR ^E8)NR ^A8R ^B8、-S(O) _rR ^A8、-S(O)(=NR ^E8)R ^B8、-N=S(O)R ^A8R ^B8、-S(O) ₂OR ^A8、-OS(O) ₂R ^A8、-NR ^A8S(O) _rR ^B8、-NR ^A8S(O)(=NR ^E8)R ^B8、-S(O) _rNR ^A8R ^B8、-S(O)(=NR ^E8)NR ^A8R ^B8、-NR ^A8S(O) ₂NR ^A8R ^B8、-NR ^A8S(O)(=NR ^E8)NR ^A8R ^B8、-P(O)R ^A8R ^B8和-P(O)(OR ^A8)(OR ^B8)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X8的取代基取代； R ⁹選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、CN、NO ₂、-NR ^A9R ^B9、-OR ^A9、-C(O)R ^A9、-C(=NR ^E9)R ^A9、-C(=N-OR ^B9)R ^A9、-C(O)OR ^A9、-OC(O)R ^A9、-C(O)NR ^A9R ^B9、-NR ^A9C(O)R ^B9、-C(=NR ^E9)NR ^A9R ^B9、-NR ^A9C(=NR ^E9)R ^B9、-OC(O)NR ^A9R ^B9、-NR ^A9C(O)OR ^B9、-NR ^A9C(O)NR ^A9R ^B9、-NR ^A9C(S)NR ^A9R ^B9、-NR ^A9C(=NR ^E9)NR ^A9R ^B9、-S(O) _rR ^A9、-S(O)(=NR ^E9)R ^B9、-N=S(O)R ^A9R ^B9、-S(O) ₂OR ^A9、-OS(O) ₂R ^A9、-NR ^A9S(O) _rR ^B9、-NR ^A9S(O)(=NR ^E9)R ^B9、-S(O) _rNR ^A9R ^B9、-S(O)(=NR ^E9)NR ^A9R ^B9、-NR ^A9S(O) ₂NR ^A9R ^B9、-NR ^A9S(O)(=NR ^E9)NR ^A9R ^B9、-P(O)R ^A9R ^B9和-P(O)(OR ^A9)(OR ^B9)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X9的取代基取代； 其中， 當X ¹是CH，X ²選自N、CH和CF，X ³和X ⁴獨立選自N或CH，式(I)的

部分的結構是

，R ^B1選自氫和C _1-4烷基時，式(I)的

部分的結構不是

，其中L、Q ¹、Q ²、R ¹、R ²、R ³、R ⁴、m和n的定義與式(I)相同； 每個R ^A0獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X0的取代基取代； 每個R ^A1和R ^B1獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X1的取代基取代； 或「R ^A1和R ^B1」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X1的取代基取代； 每個R ^A2和R ^B2獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X2的取代基取代； 或「R ^A2和R ^B2」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X2的取代基取代； 每個R ^A3和R ^B3獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X3的取代基取代； 或「R ^A3和R ^B3」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X3的取代基取代； 每個R ^A4和R ^B4獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X4的取代基取代； 或「R ^A4和R ^B4」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X4的取代基取代； 每個R ^A5和R ^B5獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X5的取代基取代； 或「R ^A5和R ^B5」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X5的取代基取代； 每個R ^A6和R ^B6獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X6的取代基取代； 或「R ^A6和R ^B6」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X6的取代基取代； 每個R ^A7和R ^B7獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X7的取代基取代； 或「R ^A7和R ^B7」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X7的取代基取代； 每個R ^A8和R ^B8獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X8的取代基取代； 或「R ^A8和R ^B8」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X8的取代基取代； 每個R ^A9和R ^B9獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X9的取代基取代； 或「R ^A9和R ^B9」一起連同與它們相連的單個或多個原子共同構成一個含有0、1或2個額外的獨立選自氧，硫、氮和磷的雜原子的4-12元雜環，該環可以是未被取代的或被1、2或3個選自R ^X9的取代基取代； 每個R ^C0和R ^D0獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^X0的取代基取代； 或者「R ^C0和R ^D0」一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可以是未被取代的或被1、2或3個R ^X0基團取代； 每個R ^E1、R ^E2、R ^E5、R ^E6、R ^E7、R ^E8和R ^E9獨立選自氫、C _1-10烷基、CN、NO ₂、-OR ^a1、-SR ^a1、-S(O) _rR ^a1、-C(O)R ^a1、C(O)OR ^a1、-C(O)NR ^a1R ^b1和-S(O) _rNR ^a1R ^b1； 每個R ^X0、R ^X1、R ^X2、R ^X3、R ^X4、R ^X5、R ^X6、R ^X7、R ^X8和R ^X9獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、鹵素、CN、-NO ₂、-(CR ^c1R ^d1) _tNR ^a1R ^b1、-(CR ^c1R ^d1) _tOR ^b1、-(CR ^c1R ^d1) _tC(O)R ^a1、-(CR ^c1R ^d1) _tC(=NR ^e1)R ^a1、-(CR ^c1R ^d1) _tC(=N-OR ^b1)R ^a1、-(CR ^c1R ^d1) _tC(O)OR ^b1、-(CR ^c1R ^d1) _tOC(O)R ^b1、-(CR ^c1R ^d1) _tC(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)R ^b1、-(CR ^c1R ^d1) _tC(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tOC(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)OR ^b1、-(CR ^c1R ^d1) _tNR ^a1C(O)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(S)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1C(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tS(O) _rR ^b1、-(CR ^c1R ^d1) _tS(O)(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tN=S(O)R ^a1R ^b1、-(CR ^c1R ^d1) _tS(O) ₂OR ^b1、-(CR ^c1R ^d1) _tOS(O) ₂R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O) _rR ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O)(=NR ^e1)R ^b1、-(CR ^c1R ^d1) _tS(O) _rNR ^a1R ^b1、-(CR ^c1R ^d1) _tS(O)(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O) ₂NR ^a1R ^b1、-(CR ^c1R ^d1) _tNR ^a1S(O)(=NR ^e1)NR ^a1R ^b1、-(CR ^c1R ^d1) _tP(O)R ^a1R ^b1和-(CR ^c1R ^d1) _tP(O)(OR ^a1)(OR ^b1)，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 每個R ^a1和R ^b1獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 或R ^a1和R ^b1一起連同與它們相連的單個或多個原子構成含有0、1或2個額外的獨立選自氧、硫、氮和磷的雜原子的4-12元雜環，該環可任選地被1、2或3個R ^Y基團取代； 每個R ^c1和R ^d1獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自R ^Y的取代基取代； 或R ^c1和R ^d1一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可任選地被1、2或3個R ^Y基團取代； 每個R ^e1獨立選自氫、C _1-10烷基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、CN、NO ₂、-OR ^a2、-SR ^a2、-S(O) _rR ^a2、-C(O)R ^a2、-C(O)OR ^a2、-S(O) _rNR ^a2R ^b2和-C(O)NR ^a2R ^b2； 每個R ^Y獨立地選自C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基、雜芳基-C _1-4烷基、鹵素、CN、-NO ₂、-NR ^a2R ^b2、-OR ^a2、-SR ^a2、-S(O) _rR ^a2、-S(O) ₂OR ^a2、-OS(O) ₂R ^b2、-S(O) _rNR ^a2R ^b2、-P(O)R ^a2R ^b2、-P(O)(OR ^a2)(OR ^b2)、-(CR ^c2R ^d2) _tNR ^a2R ^b2、-(CR ^c2R ^d2) _tOR ^b2、-(CR ^c2R ^d2) _tSR ^b2、-(CR ^c2R ^d2) _tS(O) _rR ^b2、-(CR ^c2R ^d2) _tP(O)R ^a2R ^b2、-(CR ^c2R ^d2) _tP(O)(OR ^a2)(OR ^b2)、  -(CR ^c2R ^d2) _tCO ₂R ^b2、-(CR ^c2R ^d2) _tC(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2C(O)R ^b2、-(CR ^c2R ^d2) _tNR ^a2CO ₂R ^b2、-(CR ^c2R ^d2) _tOC(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2C(O)NR ^a2R ^b2、-(CR ^c2R ^d2) _tNR ^a2SO ₂NR ^a2R ^b2、-NR ^a2(CR ^c2R ^d2) _tNR ^a2R ^b2、-O(CR ^c2R ^d2) _tNR ^a2R ^b2、-S(CR ^c2R ^d2) _tNR ^a2R ^b2、-S(O) _r(CR ^c2R ^d2) _tNR ^a2R ^b2、-C(O)R ^a2、-C(O)(CR ^c2R ^d2) _tOR ^b2、-C(O)(CR ^c2R ^d2) _tNR ^a2R ^b2、-C(O)(CR ^c2R ^d2) _tSR ^b2、-C(O)(CR ^c2R ^d2) _tS(O) _rR ^b2、-CO ₂R ^b2、-CO ₂(CR ^c2R ^d2) _tC(O)NR ^a2R ^b2、-OC(O)R ^a2、-CN、-C(O)NR ^a2R ^b2、-NR ^a2C(O)R ^b2、-OC(O)NR ^a2R ^b2、-NR ^a2C(O)OR ^b2、-NR ^a2C(O)NR ^a2R ^b2、-NR ^a2S(O) _rR ^b2、-CR ^a2(=N-OR ^b2)、-C(=NR ^e2)R ^a2、-C(=NR ^e2)NR ^a2R ^b2、-NR ^a2C(=NR ^e2)NR ^a2R ^b2、-CHF ₂、-CF ₃、-OCHF ₂和-OCF ₃，其中每個烷基、烯基、炔基、環烷基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自羥基、CN、氨基、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^a2和R ^b2獨立選自氫、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基、二(C _1-10烷基)氨基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、環烷氧基、烷硫基、環烷硫基、烷氨基、環烷氨基、雜環基、芳基和雜芳基是未被取代的或被至少一個，獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 或R ^a2和R ^b2一起連同與它們相連的單個或多個原子構成含有0、1或2個額外的獨立選自氧、硫、氮和磷的雜原子的4-12元雜環，該環可任選地被1或2個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^c2和R ^d2獨立選自氫、鹵素、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、C _1-10烷氨基、C _3-10環烷氨基、二(C _1-10烷基)氨基、雜環基、雜環基-C _1-4烷基、芳基、芳基-C _1-4烷基、雜芳基和雜芳基-C _1-4烷基，其中每個烷基、烯基、炔基、環烷基、烷氧基、環烷氧基、烷硫基、環烷硫基、烷氨基、環烷氨基、雜環基、芳基和雜芳基是未被取代的或被至少一個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 或R ^c2和R ^d2一起連同與它們相連的單個或多個碳原子構成含有0、1或2個獨立選自氧、硫和氮的雜原子的3-12元環，該環可任選地被1或2個獨立選自鹵素、CN、C _1-10烷基、C _2-10烯基、C _2-10炔基、C _3-10環烷基、羥基、C _1-10烷氧基、C _3-10環烷氧基、C _1-10烷硫基、C _3-10環烷硫基、氨基、C _1-10烷氨基、C _3-10環烷氨基和二(C _1-10烷基)氨基的取代基取代； 每個R ^e2獨立選自氫、CN、NO ₂、C _1-10烷基、C _3-10環烷基、C _3-10環烷基-C _1-4烷基、C _1-10烷氧基、C _3-10環烷氧基、-C(O)C _1-4烷基、-C(O)C _3-10環烷基、-C(O)OC _1-4烷基、-C(O)OC _3-10環烷基、-C(O)N(C _1-4烷基) ₂、-C(O)N(C _3-10環烷基) ₂、-S(O) ₂C _1-4烷基、-S(O) ₂C _3-10環烷基、-S(O) ₂N(C _1-4烷基) ₂和-S(O) ₂N(C _3-10環烷基) ₂； m選自0、1、2、3和4； n選自0、1、2、3和4； 每個r獨立選自0、1和2； 每個t獨立選自0、1、2、3和4； 每個u獨立選自0、1、2、3和4。 In embodiment (1), the present invention provides a compound represented by formula (I),

(I) or a pharmaceutically acceptable salt thereof, wherein: X ¹ is selected from N and CR ⁶ ; X ² is selected from N and CR ⁷ ; X ³ is selected from N and CR ⁸ ; X ⁴ is selected from N and CR ⁹ ; Q ¹ is selected from C _3-10 cycloalkyl, heterocyclic and heteroaryl; Q ² is selected from heterocyclic, aryl and heteroaryl; L is selected from chemical bonds, -(CR ^C0 R ^D0 ) _u -, -(CR ^C0 R ^D0 ) _u O(CR ^C0 R ^D0 ) _t -, -(CR ^C0 R ^D0 ) _u NR ^A0 (CR ^C0 R ^D0 ) _t -and-(CR ^C0 R ^D0 ) _u S(CR ^C0 R ^D0 ) _t -; each R ¹ is independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 ring Alkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 Alkyl, CN, NO ₂ , -NR ^A1 R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(=NR ^E1 )R ^A1 , -C(=N-OR ^B1 )R ^A1 , -C (O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) ₂ OR ^A1 、-C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 、-C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 、-C(O)NR ^A1 S(O )(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(O)R ^B1 , -C(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )R ^B1 , -OC(O) NR ^A1 R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -NR ^A1 C(S)NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )NR ^A1 R ^B1 , -S(O) _r R ^A1 , -S(O)(=NR ^E1 )R ^B1 , -N=S(O)R ^A1 R ^B1 , -S(O) ₂ OR ^A1 , -OS(O ) ₂ R ^A1 , -NR ^A1 S(O) _r R ^B1 , -NR ^A1 S(O)(=NR ^E1 )R ^B1 , -S(O) _r NR ^A1 R ^B1 , -S(O)(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 S(O) ₂ NR ^A1 R ^B1 , -NR ^A1 S(O)(=NR ^E1 )NR ^A1 R ^B1 , -P(O)R ^A1 R ^B1 and -P( O) (OR ^A1 ) (OR ^B1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X1 is replaced by a substituent; each R is ^{independently} selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 Cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _{1- 4} Alkyl, CN, NO ₂ , -NR ^A2 R ^B2 , -OR ^A2 , -C(O)R ^A2 , -C(=NR ^E2 )R ^A2 , -C(=N-OR ^B2 )R ^A2 , - C(O)OR ^A2 , -OC(O)R ^A2 , -C(O)NR ^A2 R ^B2 , -NR ^A2 C(O)R ^B2 , -C(=NR ^E2 )NR ^A2 R ^B2 , -NR ^A2 C(=NR ^E2 )R ^B2 , -OC(O)NR ^A2 R ^B2 , -NR ^A2 C(O)OR ^B2 , -NR ^A2 C(O)NR ^A2 R ^B2 , -NR ^A2 C(S)NR ^A2 R ^B2 、-NR ^A2 C(=NR ^E2 )NR ^A2 R ^B2 、-S(O) _r R ^A2 、-S(O)(=NR ^E2 )R ^B2 、-N=S(O)R ^A2 R ^B2 , -S(O) ₂ OR ^A2 , -OS(O) ₂ R ^A2 , -NR ^A2 S(O) _r R ^B2 , -NR ^A2 S(O)(=NR ^E2 )R ^B2 , -S(O) _r NR ^A2 R ^B2 、-S(O)(=NR ^E2 )NR ^A2 R ^B2 、-NR ^A2 S(O) ₂ NR ^A2 R ^B2 、-NR ^A2 S(O)(=NR ^E2 )NR ^A2 R ^B2 , -P(O)R ^A2 R ^B2 and -P(O)(OR ^A2 )(OR ^B2 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl R is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A3 R ^B3 , -OR ^A3 and -C(O)R ^A3 , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl and heterocyclyl is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; R ⁴ selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, Heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A4 R ^B4 , -OR ^A4 and -C(O)R ^A4 , wherein each alkyl, alkenyl, alkynyl, Cycloalkyl and heterocyclyl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or R ³ and R ⁴ together with their connected atoms form a C _3-10 cycloalkyl or containing 1, 2 or 3 heteroatoms of 4-12 membered heterocyclic groups, wherein the heteroatoms are independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring is unsubstituted or substituted by 1, 2 or 3 R ^X3 substituents; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkane radical, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A5 R ^B5 , -OR ^A5 , -C(O)R ^A5 , -C(=NR ^E5 )R ^A5 , -C(=N-OR ^B5 )R ^A5 , -C(O)OR ^A5 , -OC (O)R ^A5 , -C(O)NR ^A5 R ^B5 , -NR ^A5 C(O)R ^B5 , -C(=NR ^E5 )NR ^A5 R ^B5 , -NR ^A5 C(=NR ^E5 )R ^B5 , -OC(O)NR ^A5 R ^B5 , -NR ^A5 C(O)OR ^B5 , -NR ^A5 C(O)NR ^A5 R ^B5 , -NR ^A5 C(S)NR ^A5 R ^B5 , -NR ^A5 C(= NR ^E5 )NR ^A5 R ^B5 , -S(O) _r R ^A5 , -S(O)(=NR ^E5 )R ^B5 , -N=S(O)R ^{A5 R B5 ,} -S(O) ₂ OR ^A5 , -OS(O) ₂ R ^A5 , -NR ^A5 S(O) _r R ^B5 , -NR ^A5 S(O)(=NR ^E5 )R ^B5 , -S(O) _r NR ^A5 R ^B5 , -S( O)(=NR ^E5 )NR ^A5 R ^B5 、-NR ^A5 S(O) ₂ NR ^A5 R ^B5 、-NR ^A5 S(O)(=NR ^E5 )NR ^A5 R ^B5 、-P(O)R ^A5 R ^B5 and -P (O) (OR ^A5 ) (OR ^B5 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least A substituent independently selected from R ^X5 is substituted; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A6 R ^B6 , -OR ^A6 , -C(O)R ^A6 , -C(=NR ^E6 )R ^A6 , -C(=N-OR ^B6 )R ^A6 、-C(O)OR ^A6 、-OC(O)R ^A6 、-C(O)NR ^A6 R ^B6 、-NR ^A6 C(O)R ^B6 、-C(=NR ^E6 )NR ^A6 R ^B6 、- NR ^A6 C(=NR ^E6 )R ^B6 、-OC(O)NR ^A6 R ^B6 、-NR ^A6 C(O)OR ^B6 、-NR ^A6 C(O)NR ^A6 R ^B6 、-NR ^A6 C(S) NR ^A6 R ^B6 , -NR ^A6 C(=NR ^E6 )NR ^A6 R ^B6 , -S(O) _r R ^A6 , -S(O)(=NR ^E6 )R ^B6 , -N=S(O)R ^A6 R ^B6 、-S(O) ₂ OR ^A6 、-OS(O) ₂ R ^A6 、-NR ^A6 S(O) _r R ^B6 、-NR ^A6 S(O)(=NR ^E6 )R ^B6 、-S( O) _r NR ^A6 R ^B6 、-S(O)(=NR ^E6 )NR ^A6 R ^B6 、-NR ^A6 S(O) ₂ NR ^A6 R ^B6 、-NR ^A6 S(O)(=NR ^E6 )NR ^A6 R ^B6 , -P(O)R ^A6 R ^B6 and -P(O)(OR ^A6 )(OR ^B6 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and Heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl , C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkane base, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A7 R ^B7 , -OR ^A7 , -C(O)R ^A7 , -C(=NR ^E7 )R ^A7 , -C(=N-OR ^B7 )R ^A7 , -C(O)OR ^A7 , -OC(O)R ^A7 , -C(O)NR ^A7 R ^B7 , -NR ^A7 C(O)R ^B7 , -C (=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )R ^B7 , -OC(O)NR ^A7 R ^B7 , -NR ^A7 C(O)OR ^B7 , -NR ^A7 C(O)NR ^A7 R ^B7 , -NR ^A7 C(S)NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )NR ^A7 R ^B7 , -S(O) _r R ^A7 , -S(O)(=NR ^E7 )R ^B7 、-N=S(O)R ^A7 R ^B7 、-S(O) ₂ OR ^A7 、-OS(O) ₂ R ^A7 、-NR ^A7 S(O) _r R ^B7 、-NR ^A7 S(O) (=NR ^E7 )R ^B7 , -S(O) _r NR ^A7 R ^B7 , -S(O)(=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 S(O) ₂ NR ^A7 R ^B7 , -NR ^A7 S(O)(=NR ^E7 )NR ^A7 R ^B7 , -P(O)R ^A7 R ^B7 and -P(O)(OR ^A7 )(OR ^B7 ), wherein each of alkyl, alkenyl, alkynyl, Cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _{2 -10} alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, Aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A8 R ^B8 , -OR ^A8 , -C(O)R ^A8 、-C(=NR ^E8 )R ^A8 、-C(=N-OR ^B8 )R ^A8 、-C(O)OR ^A8 、-OC(O)R ^A8 、-C(O)NR ^A8 R ^B8 、- NR ^A8 C(O)R ^B8 、-C(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 C(=NR ^E8 )R ^B8 、-OC(O)NR ^A8 R ^B8 、-NR ^A8 C(O) OR ^B8 , -NR ^A8 C(O)NR ^A8 R ^B8 , -NR ^A8 C(S)NR ^A8 R ^B8 , -NR ^A8 C(=NR ^E8 )NR ^A8 R ^B8 , -S(O) _r R ^A8 , -S(O)(=NR ^E8 )R ^B8 , -N=S(O)R ^A8 R ^B8 , -S(O) ₂ OR ^A8 , -OS(O) ₂ R ^A8 , -NR ^A8 S(O) _r R ^B8 、-NR ^A8 S(O)(=NR ^E8 )R ^B8 、-S(O) _r NR ^A8 R ^B8 、-S(O)(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 S( O) ₂ NR ^A8 R ^B8 , -NR ^A8 S(O)(=NR ^E8 )NR ^A8 R ^B8 , -P(O)R ^A8 R ^B8 and -P(O)(OR ^A8 )(OR ^B8 ), where Each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^{X 8} ; R is selected from hydrogen, Halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, Heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A9 R ^B9 , -OR ^A9 , -C(O)R ^A9 , -C(=NR ^E9 )R ^A9 , -C(=N-OR ^B9 )R ^A9 , -C(O)OR ^A9 , -OC(O)R ^A9 , -C(O)NR ^A9 R ^B9 , -NR ^A9 C(O)R ^B9 , -C(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )R ^B9 , -OC(O)NR ^A9 R ^B9 , -NR ^A9 C(O)OR ^B9 , -NR ^A9 C(O)NR ^A9 R ^B9 , -NR ^A9 C(S)NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )NR ^A9 R ^B9 , -S(O) _r R ^A9 , -S(O)(=NR ^E9 )R ^B9 , -N=S(O)R ^A9 R ^B9 , -S(O) ₂ OR ^A9 , -OS(O) ₂ R ^A9 , -NR ^A9 S(O) _r R ^B9 , -NR ^A9 S(O)(=NR ^E9 )R ^B9 , -S(O) _r NR A9 R ^B9 , ^-S (O)(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 S(O) ₂ NR ^A9 R ^B9 , -NR ^A9 S(O)(=NR ^E9 )NR ^A9 R ^B9 , -P(O)R ^A9 R ^B9 and -P(O )(OR ^A9 )(OR ^B9 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X9 The substituent replaces; Wherein, when X ¹ is CH, X ² is selected from N, CH and CF, X ³ and X ⁴ are independently selected from N or CH, formula (I)

Part of the structure is

, R ^B1 is selected from hydrogen and C _1-4 alkyl, the formula (I)

Part of the structure is not

, wherein L, Q ¹ , Q ² , R ¹ , R ² , R ³ , R ⁴ , m and n are as defined in formula (I); each R ^A0 is independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl _- C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, Aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; each R ^A1 and R ^B1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl , _{C 2-10} alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _{1- 4} Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy Group, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X1 ; or " ^RA1 and R ^B1 " together with single or multiple atoms connected to them together form a 4-12 membered heterocycle containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 Substituents from R ^X1 are substituted; each R ^A2 and R ^B2 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, Heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; or " ^RA2 and R ^B2 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional independently selected from oxygen, A 4-12 membered heterocyclic ring of heteroatoms of sulfur, nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X2 ; each R ^A3 and R ^B3 independently selected From hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _{1- 10} alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Each of the alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl, and heteroaryl groups is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; or "R ^A3 and R ^B3 "together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the The ring can be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X3 ; each R ^A4 and R ^B4 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or " ^RA4 and R ^B4 " together together with the single or multiple atoms to which they are attached Consists of a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X4 is replaced by a substituent; each R ^A5 and R ^B5 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, hetero Aryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or Substituted by at least one substituent independently selected from R ^X5 ; or " ^RA5 and R ^B5 " together with single or multiple atoms connected to them form a substituent containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X5 ; each R ^A6 and R ^B6 are independently selected from Hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 Alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; or "R ^A6 and R ^B6 ”together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X6 ; each R ^A7 and R ^B7 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, Heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; or " ^RA7 and R ^B7 " together together form a single or multiple atoms connected to them A 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X7 is replaced by a substituent; each R ^A8 and R ^B8 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3- 10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by At least one substituent independently selected from R ^X8 is substituted; or " ^RA8 and R ^B8 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur, A 4-12 membered heterocyclic ring of nitrogen and phosphorus heteroatoms, the ring may be unsubstituted or substituted with 1, 2 or 3 substituents selected from R ^X8 ; each R ^A9 and R ^B9 are independently selected from hydrogen , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkane Oxygen, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl R, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X9 ; or "R ^A9 and R ^B9 ”together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring can be is unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X9 ; each R ^C0 and R ^D0 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl -C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is Unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; or "R ^C0 and R ^D0 "together together with the single or multiple carbon atoms to which they are attached contain 0, 1 or 2 substituents independently selected from oxygen , a 3-12 membered ring of heteroatoms of sulfur and nitrogen, which ring may be unsubstituted or substituted by 1, 2 or 3 R ^X0 groups; each of R ^E1 , R ^E2 , R ^E5 , R ^E6 , R ^E7 , R ^E8 and R ^E9 are independently selected from hydrogen, C _1-10 alkyl, CN, NO ₂ , -OR ^a1 , -SR ^a1 , -S(O) _rR ^a1 , -C(O)R ^a1 , C(O)OR ^a1 , -C(O)NR ^a1 R ^b1 , and -S(O) _r NR ^a1 R ^b1 ; each of R ^X0 , R ^X1 , R ^X2 , R ^X3 , R ^X4 , R ^X5 , R ^X6 , R ^X7 , R ^X8 and R ^X9 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl -C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl , Halogen, CN, -NO ₂ , -(CR ^c1 R ^d1 ) _t NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t OR ^b1 , -(CR ^c1 R ^d1 ) _t C(O)R ^a1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(=N-OR ^b1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(O)OR ^b1 ,- (CR ^c1 R ^d1 ) _t OC(O)R ^b1 , -(CR ^c1 R ^d1 ) _t C(O)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)R ^b1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t OC(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)OR ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C (S)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t N=S(O)R ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) ₂ OR ^b1 , -(CR ^c1 R ^d1 ) _t OS(O) ₂ R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(= NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) ₂ NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t P( O)R ^a1 R ^b1 and -(CR ^c1 R ^d1 ) _t P(O)(OR ^a1 )(OR ^b1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; each R ^a1 and R ^b1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl- C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or substituted by at least one substituent independently selected from ^RY ; or R ^a1 and R ^b1 together with the single or multiple atoms connected to them constitute 0, 1 or 2 additional independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be optionally substituted by 1, 2 or 3 ^RY groups; each R ^c1 and R ^d1 are independently selected from hydrogen, halogen, C _{1 -10} alkyl, C _2-10 alkenyl, C 2-10 alkynyl _, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl- C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; or R ^c1 and R ^d1 together, together with the single or multiple carbon atoms attached to them, constitute a 0, 1 or 2 3-12 membered rings of heteroatoms independently selected from oxygen, sulfur and nitrogen, which rings may be optionally substituted with 1, 2 or 3 ^RY groups; each R ^e1 is independently selected from Hydrogen, C _1-10 alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, CN, NO ₂ , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -C(O)R ^a2 , -C(O)OR ^a2 , -S(O) _rNR ^a2 R ^b2 and -C(O)NR ^a2 R ^b2 ; each ^RY is independently selected from C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl -C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, halogen, CN, -NO ₂ , -NR ^a2 R ^b2 , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -S(O) ₂ OR ^a2 , -OS(O) ₂ R ^b2 , -S(O) _r NR ^a2 R ^b2 , -P(O )R ^a2 R ^b2 , -P(O)(OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t OR ^b2 , -(CR ^c2 R ^d2 ) _t SR ^b2 , -(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -(CR ^c2 R ^d2 ) _t P(O)R ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t P(O) (OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C (O)R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t OC(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C( O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 SO ₂ NR ^a2 R ^b2 , -NR ^a2 (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -O(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(O) _r (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)R ^a2 , -C(O)(CR ^c2 R ^d2 ) _t OR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)(CR ^c2 R ^d2 ) _t SR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -CO ₂ R ^b2 , -CO ₂ (CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -OC(O)R ^a2 , -CN, -C(O )NR ^a2 R ^b2 , -NR ^a2 C(O)R ^b2 , -OC(O)NR ^a2 R ^b2 , -NR ^a2 C(O)OR ^b2 , -NR ^a2 C(O)NR ^a2 R ^b2 , -NR ^a2 S(O) _r R ^b2 , -CR ^a2 (=N-OR ^b2 ), -C(=NR ^e2 )R ^a2 , -C(=NR ^e2 )NR ^a2 R ^b2 , -NR ^a2 C(=NR ^e2 )NR ^a2 R ^b2 , -CHF ₂ , -CF ₃ , -OCHF ₂ and -OCF ₃ , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or by at least one member independently selected from hydroxyl, CN, amino, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{1- 10} alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _{1 -10} alkyl) amino substituent substitution; each R ^a2 and R ^b2 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkane Group, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio , C _1-10 alkylamino, C _3-10 cycloalkylamino, di(C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _{1 -4} alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, ring Alkylthio, alkylamino, cycloalkylamino, heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one, independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl radical, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkane Thio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^a2 and R ^b2 together together with the single or multiple atoms constitute a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may optionally be replaced by 1 or 2 heteroatoms independently selected from halogen, CN , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C Substituents of _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl) amino; each R ^c2 and R ^d2 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _{3- 10} cycloalkylamino, two (C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl Group-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, cycloalkylthio, alkylamino, cycloalkylamino, Heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one member independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _{3- 10} cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^c2 and R ^d2 together, together with the single or multiple carbon atoms connected to them, constitute 0, 1 or 2 independent A 3-12 membered ring of heteroatoms selected from oxygen, sulfur and nitrogen, which may optionally be replaced by 1 or 2 members independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, Amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl)amino are substituted by substituents; each R ^e2 is independently selected from hydrogen, CN, NO ₂ , C _1-10 Alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, -C(O)C _{1 -4} alkyl, -C(O)C _3-10 cycloalkyl, -C(O)OC _1-4 alkyl, -C(O)OC _3-10 cycloalkyl, -C(O)N( C _1-4 alkyl) ₂ , -C(O)N(C _3-10 cycloalkyl) ₂ , -S(O) ₂ C _1-4 alkyl, -S(O) ₂ C _3-10 ring Alkyl, -S (O) ₂ N (C _1-4 alkyl) ₂ and -S (O) ₂ N (C _3-10 cycloalkyl) ₂ ; m is selected from 0, 1, 2, 3 and 4 n is selected from 0, 1, 2, 3 and 4; each r is independently selected from 0, 1 and 2; each t is independently selected from 0, 1, 2, 3 and 4; each u is independently selected from 0, 1, 2, 3 and 4.

In another embodiment (2), the present invention provides the compound of embodiment (1), or a pharmaceutically acceptable salt thereof, wherein X ¹ is N.

In another embodiment (3), the present invention provides the compound of embodiment (1) or a pharmaceutically acceptable salt thereof, wherein X ¹ is CR ⁶ .

In another embodiment (4), the present invention provides a compound of any one of embodiments (1)-(3), or a pharmaceutically acceptable salt thereof, wherein X ² is N.

In another embodiment (5), the present invention provides the compound of any one of embodiments (1)-(3), or a pharmaceutically acceptable salt thereof, wherein X ² is CR ⁷ .

In another embodiment (6), the present invention provides the compound of any one of embodiments (1)-(5), or a pharmaceutically acceptable salt thereof, wherein X ³ is N.

In another embodiment (7), the present invention provides the compound of any one of embodiments (1)-(5), or a pharmaceutically acceptable salt thereof, wherein X ³ is CR ⁸ .

In another embodiment (8), the present invention provides the compound of any one of embodiments (1)-(7), or a pharmaceutically acceptable salt thereof, wherein X ⁴ is N.

In another embodiment (9), the present invention provides the compound of any one of embodiments (1)-(7), or a pharmaceutically acceptable salt thereof, wherein X ⁴ is CR ⁹ .

In another embodiment (10), the present invention provides a compound or a pharmaceutically acceptable salt thereof according to any one of embodiments ( ¹ ) and (3)-(9), wherein R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A6 R ^B6 , -OR ^A6 , -C(O)R ^A6 , -C(O) OR ^A6 , -OC(O)R ^A6 , -C(O)NR ^A6 R ^B6 , -NR ^A6 C(O)R ^B6 , -OC(O)NR ^A6 R ^B6 , -NR ^A6 C(O)OR ^B6 、-NR ^A6 C(O)NR ^A6 R ^B6 、-NR ^A6 C(S)NR ^A6 R ^B6 、-S(O) ₂ OR ^A6 、-OS(O) ₂ R ^A6 、-NR ^A6 S(O) _r R ^B6 , -S(O) _r NR ^A6 R ^B6 and -NR ^A6 S(O) ₂ NR ^A6 R ^B6 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or replaced by at least one independent Substituents selected from R ^X6 are substituted. In another embodiment, R ^is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy , F, Cl, Br, -CN, -NO ₂ , -OH and -NH ₂ . In another embodiment, ^R6 is selected from hydrogen, F, Cl and methyl.

In another embodiment (11), the present invention provides a compound of any one of embodiments (1)-(3) and (5)-(10), or a pharmaceutically acceptable salt thereof, wherein R ^is selected from Hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A7 R ^B7 , -OR ^A7 , -C(O)R ^A7 , - C(O)OR ^A7 , -OC(O)R ^A7 , -C(O)NR ^A7 R ^B7 , -NR ^A7 C(O)R ^B7 , -OC(O)NR ^A7 R ^B7 , -NR ^A7 C( O)OR ^B7 , -NR ^A7 C(O)NR ^A7 R ^B7 , -NR ^A7 C(S)NR ^A7 R ^B7 , -S(O) ₂ OR ^A7 , -OS(O) ₂ R ^A7 , -NR ^A7 S(O) _r R ^B7 , -S(O) _r NR ^A7 R ^B7 , and -NR ^A7 S(O) ₂ NR ^A7 R ^B7 , wherein each alkyl, alkenyl, and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X7 .

In another embodiment (12), the present invention provides the compound of embodiment (11) or a pharmaceutically acceptable salt thereof, wherein R ⁷ is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkene group, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A7 R ^B7 and -OR ^A7 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or is independently selected from R by at least one ^X7 is substituted with a substituent. In another embodiment, R ^is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy , F, Cl, Br, -CN, -NO ₂ , -OH and -NH ₂ . In another embodiment, ^R7 is hydrogen.

In another embodiment (13), the present invention provides a compound or a pharmaceutically acceptable salt thereof according to any one of embodiments (1)-(5) and (7)-(12), wherein R ^is selected from Hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A8 R ^B8 , -OR ^A8 , -C(O)R ^A8 , - C(O)OR ^A8 , -OC(O)R ^A8 , -C(O)NR ^A8 R ^B8 , -NR ^A8 C(O)R ^B8 , -OC(O)NR ^A8 R ^B8 , -NR ^A8 C( O)OR ^B8 , -NR ^A8 C(O)NR ^A8 R ^B8 , -NR ^A8 C(S)NR ^A8 R ^B8 , -S(O) ₂ OR ^A8 , -OS(O) ₂ R ^A8 , -NR ^A8 S(O) _r R ^B8 , -S(O) _r NR ^A8 R ^B8 , and -NR ^A8 S(O) ₂ NR ^A8 R ^B8 , wherein each of the alkyl, alkenyl and cycloalkyl groups is unsubstituted or Substituted by at least one substituent independently selected from R ^X8 .

In another embodiment (14), the present invention provides the compound of embodiment (13) or a pharmaceutically acceptable salt thereof, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkene group, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A8 R ^B8 and -OR ^A8 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or is independently selected from R by at least one The substituent of ^X8 is substituted. In another embodiment, R ^is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy , F, Cl, Br, -CN, -NO ₂ , -OH and -NH ₂ . In another embodiment, ^R8 is hydrogen.

In another embodiment (15), the present invention provides a compound or a pharmaceutically acceptable salt thereof according to any one of embodiments (1)-(7) and (9)-(14), wherein R ^is selected from Hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A9 R ^B9 , -OR ^A9 , -C(O)R ^A9 , - C(O)OR ^A9 , -OC(O)R ^A9 , -C(O)NR ^A9 R ^B9 , -NR ^A9 C(O)R ^B9 , -OC(O)NR ^A9 R ^B9 , -NR ^A9 C( O)OR ^B9 , -NR ^A9 C(O)NR ^A9 R ^B9 , -NR ^A9 C(S)NR ^A9 R ^B9 , -S(O) ₂ OR ^A9 , -OS(O) ₂ R ^A9 , -NR ^A9 S(O) _r R ^B9 , -S(O) _r NR ^A9 R ^B9 and -NR ^A9 S(O) ₂ NR ^A9 R ^B9 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or Substituted by at least one substituent independently selected from R ^X9 .

In another embodiment (16), the present invention provides the compound of embodiment (15) or a pharmaceutically acceptable salt thereof, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkene group, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A9 R ^B9 and -OR ^A9 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or is independently selected from R by at least one The substituent of ^X9 is substituted. In another embodiment, ^R is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy , F, Cl, Br, -CN, -NO ₂ , -OH and -NH ₂ . In another embodiment, ^R9 is hydrogen.

部分的結構選自

、

、

和

。 In another embodiment (17), the present invention provides the compound of any one of the embodiments (1)-(16) or a pharmaceutically acceptable salt thereof, wherein the compound of formula (I)

Some structures are selected from

,

,

and

.

部分的結構是

或

。 In another embodiment, wherein the formula (I)

Part of the structure is

or

.

In another embodiment (18), the present invention provides the compound of any one of embodiments (1)-(17) or a pharmaceutically acceptable salt thereof, wherein ^R is selected from hydrogen, halogen, C _1-10 Alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl , aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A5 R ^B5 , -OR ^A5 , -C(O)R ^A5 , - C(O)OR ^A5 , -OC(O)R ^A5 , -C(O)NR ^A5 R ^B5 , -NR ^A5 C(O)R ^B5 , -OC(O)NR ^A5 R ^B5 , -NR ^A5 C( O)OR ^B5 , -NR ^A5 C(O)NR ^A5 R ^B5 , -NR ^A5 C(S)NR ^A5 R ^B5 , -S(O) _r R ^A5 , -S(O) ₂ OR ^A5 , -OS( O) ₂ R ^A5 , -NR ^A5 S(O) _r R ^B5 and -S(O) _r NR ^A5 R ^B5 , wherein each of alkyl, alkenyl, cycloalkyl, heterocyclyl, aryl and heteroaryl The group is unsubstituted or substituted with at least one substituent independently selected from R ^X5 .

In another embodiment (19), the present invention provides the compound of embodiment (18) or a pharmaceutically acceptable salt thereof, wherein ^R is selected from hydrogen, halogen, methyl, ethyl, methoxy, ethoxy base, isopropyl, cyclopropyl, phenyl, CN, NO ₂ , -NH ₂ and -OH, wherein each of methyl, ethyl, isopropyl, cyclopropyl and phenyl is unsubstituted or Substituted by at least one substituent independently selected from R ^X5 . In another embodiment, wherein ^R is selected from hydrogen, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, ethyl, fluoroethyl, difluoroethyl, trifluoroethyl methoxy, ethoxy, isopropyl, methoxymethyl, cyclopropyl and phenyl.

In another embodiment (20), the present invention provides a compound of any one of embodiments (1)-(19), or a pharmaceutically acceptable salt thereof, wherein Q ¹ is heterocyclyl.

、

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、

、

、

、

、

、

、

、

、

、

、

和

。在另一個實施方案中，Q ¹選自

和

。 In another embodiment (21), the present invention provides the compound of embodiment (20) or a pharmaceutically acceptable salt thereof, wherein ^Q is selected from

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

and

. In another embodiment, ^Q is selected from

and

.

In another embodiment (22), the present invention provides a compound of any one of embodiments (1)-(21), or a pharmaceutically acceptable salt thereof, wherein ^each R is independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl- _{C 1-4} alkyl , aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A2 R ^B2 , -OR ^A2 , -C(O)R ^A2 、-C(O)OR ^A2 、-OC(O)R ^A2 、-C(O)NR ^A2 R ^B2 、-NR ^A2 C(O)R ^B2 、-OC(O)NR ^A2 R ^B2 、-NR ^A2 C(O)OR ^B2 , -NR ^A2 C(O)NR ^A2 R ^B2 , -NR ^A2 C(S)NR ^A2 R ^B2 , -S(O) _r R ^A2 , -S(O)(=NR ^E2 )R ^B2 , -S(O) ₂ OR ^A2 , -OS(O) ₂ R ^A2 , -NR ^A2 S(O) _r R ^B2 , -S(O) _r NR ^A2 R ^B2 and -NR ^A2 S(O ) ₂ ^NRA2 R ^B2 , wherein each alkyl, alkenyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or substituted with at least one substituent independently selected from R ^X2 .

In another embodiment (23), the present invention provides a compound of embodiment (22) or a pharmaceutically acceptable salt thereof, wherein each ^R is independently selected from hydrogen, F, Cl, Br, methyl, ethyl , isopropyl, cyclopropyl, methoxy, ethoxy, -OC(O)CH ₃ , CN, NO ₂ , -NH ₂ and -OH, wherein each of methyl, ethyl, isopropyl and Cyclopropyl is unsubstituted or substituted with at least one substituent independently selected from R ^X2 . In another embodiment, wherein each ^R is independently selected from hydrogen, F, Cl, Br, methyl, ethyl, isopropyl, cyclopropyl, methoxy, ethoxy, -OC(O) CH ₃ , CN, NO ₂ , -NH ₂ and -OH, wherein each of methyl, ethyl, isopropyl and cyclopropyl is unsubstituted or replaced by at least one independently selected from methoxy, ethoxy , F, Cl, Br, -CN, -NO ₂ , -NH ₂ and -OH substituents.

、-OC(O)CH ₃、CN、NO ₂、-NH ₂和-OH。 In another embodiment, wherein each ^R is independently selected from hydrogen, F, Cl, Br, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, ethyl, difluoroethyl group, trifluoroethyl, isopropyl, cyclopropyl, methoxy, ethoxy, methoxymethyl,

, -OC(O) _CH3 , CN, _NO2 , _-NH2 and -OH.

部分的結構選自

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、

、

、

、

、

、

、

、

、

、

、

、

、

、

、

、

、

、

和

。 In another embodiment (24), the present invention provides a compound of any one of embodiments (1)-(23) or a pharmaceutically acceptable salt thereof, wherein the compound of formula (I)

Some structures are selected from

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

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,

,

,

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,

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,

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,

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,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

and

.

In another embodiment (25), the present invention provides the compound of any one of embodiments (1)-(24) or a pharmaceutically acceptable salt thereof, wherein L is selected from a chemical bond, -CR ^CO R ^D0 -, -(CR ^C0 R ^D0 ) _u O(CR ^C0 R ^D0 ) _t -, (CR ^C0 R ^D0 ) _u NR ^A0 (CR ^C0 R ^D0 ) _t -and-(CR ^C0 R ^D0 ) _u S(CR ^C0 R ^D0 ) _t -.

In another embodiment (26), the present invention provides the compound of embodiment (25) or a pharmaceutically acceptable salt thereof, wherein L is selected from a chemical bond, -CH ₂ -, -O-, -NH- and -S -. In another embodiment, L is selected from a bond, -O- and -NH-.

In another embodiment (27), the present invention provides the compound of any one of embodiments (1)-(26) or a pharmaceutically acceptable salt thereof, wherein ^Q is selected from 5-12 membered heterocyclyl, Aryl and heteroaryl.

、

、

、

、

、

、

、

和

。在另一個實施方案中，其中Q ²選自

、

、

、

、

、

和

。 In another embodiment (28), the present invention provides the compound of embodiment (27) or a pharmaceutically acceptable salt thereof, wherein ^Q is selected from

,

,

,

,

,

,

,

and

. In another embodiment, wherein Q ² is selected from

,

,

,

,

,

and

.

In another embodiment (29), the present invention provides a compound of any one of embodiments (1)-(28), or a pharmaceutically acceptable salt thereof, wherein ^each R is independently selected from hydrogen, halogen, C _1-10 alkyl, C _3-10 cycloalkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, heteroaryl, CN, NO ₂ , -NR ^A1 R ^B1 , -OR ^A1 , -C (O)R ^A1 , -C(O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C( O)NR ^A1 S(O) _r NR ^A1 R ^B1 , -C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 , -NR ^A1 C(O)R ^B1 , OC(O)NR ^A1 R ^B1 、-NR ^A1 C(O)OR ^B1 、-NR ^A1 C(O)NR ^A1 R ^B1 、-S(O) _r NR ^A1 R ^B1 、-NR ^A1 S(O) _r R ^B1 、-NR ^A1 S (O) ₂ NR ^A1 R ^B1 and -NR ^A1 C(S)NR ^A1 R ^B1 , wherein each alkyl, cycloalkyl, heterocyclyl and heteroaryl is unsubstituted or replaced by at least one independently selected Substituents from R ^X1 are substituted.

、

、

、

、

、

、

、

、

、

、

、CN、NO ₂、-NR ^A1R ^B1、-NR ^A1C(O)R ^B1、-NR ^A1C(O)OR ^B1、-NR ^A1C(O)NR ^A1R ^B1、-NR ^A1S(O) _rR ^B1、-OR ^A1、-C(O)R ^A1、-C(O)OR ^A1、-OC(O)R ^A1、-C(O)NR ^A1R ^B1、-C(O)NR ^A1S(O) _rR ^A1、-C(O)NR ^A1S(O) _rNR ^A1R ^B1、-C(O)NR ^A1S(O)(=NR ^E1)R ^B1和-S(O) _rNR ^A1R ^B1，其中每個甲基、乙基、異丙基、環丙基、

、

、

、

、

、

、

、

、

、

和

是未被取代的或被至少一個獨立選自R ^X1的取代基取代。 In another embodiment (30), the present invention provides a compound of embodiment (29) or a pharmaceutically acceptable salt thereof, wherein in another embodiment, ^each R is independently selected from methyl, ethyl, Isopropyl, Cyclopropyl, F, Cl,

,

,

,

,

,

,

,

,

,

,

, CN, NO ₂ , -NR ^A1 R ^B1 , -NR ^A1 C(O)R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -NR ^A1 S(O ) _r R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 , -C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 and -S(O) _r NR ^A1 R ^B1 , where each of methyl, ethyl, isopropyl, cyclopropyl,

,

,

,

,

,

,

,

,

,

and

is unsubstituted or substituted with at least one substituent independently selected from ^RX1 .

In another embodiment (31), the present invention provides the compound of embodiment (30) or a pharmaceutically acceptable salt thereof, wherein each R ^A1 and R ^B1 are independently selected from hydrogen, deuterium, C _1-10 alkyl , C _3-10 cycloalkyl, heterocyclyl and C _1-10 alkoxy, wherein each alkyl, cycloalkyl, heterocyclyl and alkoxy are respectively unsubstituted or replaced by at least one independently selected Substituents from R ^X1 are substituted. In another embodiment, each of R ^A1 and R ^B1 is independently selected from hydrogen, deuterium, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, methoxy, and ethoxy, wherein each Methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, methoxy and ethoxy are unsubstituted or substituted with at least one substituent independently selected from ^RX1 .

In another embodiment (32), the present invention provides the compound of embodiment (30) or a pharmaceutically acceptable salt thereof, wherein each " ^RA1 and R ^B1 " together with single or multiple atoms connected to them together form a 4-8 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 selected Substituents from R ^X1 are substituted.

In another embodiment (33), the present invention provides a compound of any one of embodiments (1)-(32), or a pharmaceutically acceptable salt thereof, wherein each R ^X1 is independently selected from C _1-10 alkane group, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, halogen, CN, NO ₂ , -(CR ^c1 R ^d1 ) _t NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t OR ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)OR ^b1 and -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) _rRb1 , wherein each alkyl and cycloalkyl is unsubstituted or substituted with ^at least one substituent independently selected from ^RY .

、

、

、

和

，其中每個甲基、乙基、異丙基、叔丁基、環丙基、甲氧基和乙氧基是未被取代的或被至少一個獨立選自R ^Y的取代基取代。在另一個實施方案中，每個R ^X1獨立選自甲基、二氟甲基、三氟甲基、乙基、二氟乙基、三氟乙基、異丙基、叔丁基、環丙基、甲氧基、乙氧基、F、-CN、-NH ₂、-NHCH ₃、-NHCH ₂CH ₃、-NHC(O)CH ₃、-NHC(O)OCH ₃、

、

、

、

和

。 In another embodiment (34), the present invention provides the compound of embodiment (33) or a pharmaceutically acceptable salt thereof, wherein each R ^X1 is independently selected from methyl, ethyl, isopropyl, tert-butyl , cyclopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -OH, -NO ₂ , -NH ₂ , -NHCH ₃ , -NHCH ₂ CH ₃ , -NHC(O)CH ₃ , -NHC(O)OCH ₃ ,

,

,

,

and

, wherein each of methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, methoxy and ethoxy is unsubstituted or substituted with at least one substituent independently selected from ^RY . In another embodiment, each R ^X1 is independently selected from methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, isopropyl, tert-butyl, cyclopropyl radical, methoxy, ethoxy, F, -CN, -NH ₂ , -NHCH ₃ , -NHCH ₂ CH ₃ , -NHC(O)CH ₃ , -NHC(O)OCH ₃ ,

,

,

,

and

.

部分的結構選自

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、

、

、

、

、

、

、

、

和

。 In another embodiment (35), the present invention provides a compound of any one of embodiments (1)-(34) or a pharmaceutically acceptable salt thereof, wherein the compound of formula (I)

Some structures are selected from

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

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,

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,

,

,

,

,

,

,

,

,

and

.

In another embodiment (36), the present invention provides a compound of any one of embodiments (1)-(35) or a pharmaceutically acceptable salt thereof, wherein R ³ is selected from hydrogen, halogen, C _1-10 Alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, -NH ₂ and -OH, wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or is independently selected by at least one Substituents from R ^X3 . In another embodiment, wherein R ³ is selected from hydrogen and methyl, wherein methyl is unsubstituted or substituted with at least one substituent independently selected from R ^{X 3} .

In another embodiment (37), the present invention provides a compound of embodiment (36), or a pharmaceutically acceptable salt thereof, wherein R ³ is selected from hydrogen and methyl.

In another embodiment (38), the present invention provides a compound of any one of embodiments (1)-(37), or a pharmaceutically acceptable salt thereof, wherein ^R is selected from hydrogen, halogen, C _1-10 Alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, -NH ₂ and -OH, wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or is independently selected by at least one Substituents from R ^X4 . In another embodiment, wherein ^R4 is selected from hydrogen and methyl, it is unsubstituted or substituted with at least one substituent independently selected from ^RX4 .

In another embodiment (39), the present invention provides a compound of embodiment (38), or a pharmaceutically acceptable salt thereof, wherein R ⁴ is selected from hydrogen and methyl.

In another embodiment (40), the present invention provides a compound according to any one of embodiments (1)-(39), or a pharmaceutically acceptable salt thereof, wherein R ^{and R} together with the atoms connected to them Form a C _3-10 cycloalkyl group or a 4-8 membered heterocyclic group containing 1, 2 or 3 heteroatoms, wherein the heteroatoms are independently selected from oxygen, sulfur, nitrogen and phosphorus, and the ring is unsubstituted or composed of 1 , 2 or 3 R ^X3 substituents are substituted.

In another embodiment (41), the present invention provides the compound of embodiment (40) or a pharmaceutically acceptable salt thereof, wherein R ³ and R ⁴ form a cycloalkyl group together with the atoms connected to them, the ring Unsubstituted or substituted with 1, 2 or 3 R ^X3 substituents. In another embodiment, wherein ^R3 and ^R4 , together with the atoms to which they are attached, form a cycloalkyl group.

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， 和其藥學上可接受的鹽。 In another embodiment (42), the compound provided by the invention is selected from:

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, and pharmaceutically acceptable salts thereof.

、

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， 和其藥學上可接受的鹽。 In another embodiment, the compound provided by the invention is selected from:

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, and pharmaceutically acceptable salts thereof.

In another embodiment (43), the present invention provides a pharmaceutical composition comprising the compound of any one of embodiments (1)-(42) or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier.

In another embodiment (44), the present invention provides a method of treating, ameliorating or preventing a condition responsive to inhibition of PARP1 comprising administering to an individual in need thereof an effective amount of any one of embodiments (1)-(42) The compound of Item or a pharmaceutically acceptable salt thereof, or at least one pharmaceutical composition thereof, and optionally used in combination with a second therapeutic agent.

In another embodiment (45), the present invention provides the use of the compound of any one of the embodiments (1)-(42) or a pharmaceutically acceptable salt thereof in the preparation for treating abnormal cell proliferation diseases.

In another embodiment (46), the present invention provides the use of the compound of embodiment (45) or a pharmaceutically acceptable salt thereof, wherein abnormal cell proliferation diseases include but not limited to, breast cancer, ovarian cancer, bladder cancer , uterine cancer, prostate cancer, testicular cancer, lung cancer (including NSCLC, SCLC, squamous cell carcinoma or adenocarcinoma), esophageal cancer, head and neck cancer, colorectal cancer, kidney cancer (including RCC), liver cancer (including HCC), pancreatic cancer Carcinoma, gastric (i.e., of stomach) cancer, thyroid cancer, chronic lymphocytic leukemia (CLL), lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T- or B-cell origin, melanoma, bone marrow leukemia and myeloma.

In another aspect, the present invention provides a pharmaceutical composition comprising a compound disclosed in the present invention or a pharmaceutically acceptable salt thereof.

In another aspect, the invention provides a kit comprising a compound disclosed herein, or a pharmaceutically acceptable salt thereof; and instructions comprising one or more of the following information: the disease state for which the ingredient is used, storage information for the ingredient, Dosage information and instructions on how to use the ingredients. In a particular variant, the kit comprises the compound in multiple dosage form.

In another aspect, the invention provides an article of manufacture comprising a compound disclosed herein, or a pharmaceutically acceptable salt thereof; and packaging material. In one variation, the packaging material includes a container. In a particular variation, the container includes a label indicating one or more of the following: the disease state for which the compound is used, storage information, dosage information and/or instructions on how to use the compound. In another variation, the article of manufacture includes the compound in multiple dosage form.

In another aspect, the invention provides a method of treatment comprising administering to a subject a compound disclosed herein, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention provides a method of inhibiting PARP1 by contacting a compound disclosed herein, or a pharmaceutically acceptable salt thereof, with PARP1.

In another aspect, the present invention provides a method of inhibiting PARP1, comprising allowing a compound disclosed herein, or a pharmaceutically acceptable salt thereof, to be present in a subject to inhibit PARP1 activity in vivo.

In another aspect, the present invention provides a method of inhibiting PARP1, comprising administering to an individual a first compound that is converted in vivo to a second compound, wherein the second compound inhibits PARP1 activity in vivo, and the second compound is the above embodiment Compounds and variants of any of the schemes.

In another aspect, the present invention provides a method of treating a disease state in which PARP1 activity is responsible for the pathology and/or symptoms of the disease state, the method comprising administering a therapeutically effective amount of a compound disclosed herein or a pharmaceutically effective amount thereof to the disease state. acceptable salts, as they occur in the individual.

In another aspect, the invention provides a method of treating a disease state in which PARP1 activity is responsible for the pathology and/or symptoms of the disease state, the method comprising administering to an individual a first compound that is converted in vivo to a second compound , wherein the second compound inhibits PARP1 activity in vivo. It is worth noting that the compounds of the present invention may be pre-transformed or post-transformed compounds.

In variations on each of the above methods, the disease state is selected from the group consisting of: cancerous proliferative disease (e.g., brain, lung, squamous cell, bladder, stomach, pancreas, breast, head, neck, renal, kidney, ovarian, Prostate, colorectal, epidermal, esophageal, testicular, gynecologic, or thyroid cancer); noncancerous proliferative disorders (eg, benign skin hyperplasia (eg, psoriasis), restenosis, and benign prostatic hypertrophy (BPH)); pancreatitis; renal disease; pain; prevention of blastocyst implantation; treatment of angiogenesis or angiogenesis-related diseases (e.g. tumor angiogenesis, acute and chronic inflammatory diseases such as rheumatoid arthritis, atherosclerosis, inflammatory bowel disease, skin disease Such as psoriasis, eczema and scleroderma, diabetes mellitus, diabetic retinopathy, retinopathy of prematurity, age-related macular degeneration, hemangioma, glioma, melanoma, Kaposi's sarcoma and ovarian cancer, breast cancer , lung, pancreatic, prostate, colon, and epidermoid); asthma; neutrophil chemotaxis (eg, reperfusion injury and inflammatory arthritis in myocardial infarction and stroke); septic shock; T cell mediated diseases in which immunosuppression is valuable (eg, prevention of organ transplant rejection, graft-versus-host disease, lupus, multiple sclerosis, and rheumatoid arthritis); atherosclerosis; inhibition of keratin response to growth factor cocktails cells; chronic obstructive pulmonary disease (COPD) and other diseases.

In another aspect, the present invention provides a method of treating disease states in which mutations in the PARP1 gene cause pathology and/or symptoms, such as melanoma, lung cancer, colon cancer, and other types of tumors. .

In another aspect, the invention relates to the use of compounds and variants of any one of the above embodiments as medicaments. In another aspect, the present invention relates to the use of the compounds and variants of any one of the above embodiments for the manufacture of a medicament for inhibiting PARP1.

In another aspect, the present invention relates to the use of the compounds and variants of any one of the above embodiments for the manufacture of a medicament for the treatment of a disease state of pathology and/or symptoms caused by PARP1 activity.

[ Administration and pharmaceutical composition ]

Generally, the compounds of the present invention will be administered in a therapeutically effective amount by any common and acceptable means known in the art, alone or in combination with one or more therapeutic agents. A therapeutically effective amount can vary widely, depending on the severity of the disease, age and relative health of the subject, the potency of the compound used and other factors known in the art. For example, for the treatment of neoplastic diseases and diseases of the immune system, the required dosage will vary according to the mode of administration, the particular condition to be treated and the effect desired.

In general, satisfactory results are achieved at daily doses of 0.001 to 100 mg/kg body weight, specifically, from about 0.03 to 2.5 mg/kg body weight. The daily dosage for larger mammals, such as humans, may be from about 0.5 mg to about 2000 mg, or more specifically, from 0.5 mg to 1000 mg, administered in a convenient form, for example, in divided doses up to four times daily. times or in sustained-release form. Suitable unit dosage forms for oral administration contain from about 1 to 50 mg of active ingredient.

The compounds of the present invention can be administered in the form of pharmaceutical compositions by any conventional route; for example enterally, for example orally, for example in the form of tablets or capsules, parenterally, for example in the form of injectable solutions or suspensions; Or topically, for example as a lotion, gel, ointment or cream, or in nasal or suppository form.

The pharmaceutical composition containing the compound of the present invention in the form of free base or pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent can be mixed, granulated, coated, dissolved or freeze-dried in a conventional manner. to manufacture. For example, a pharmaceutical composition comprising a compound of the present invention in combination with at least one pharmaceutically acceptable carrier or diluent can be prepared by mixing with a pharmaceutically acceptable carrier or diluent in a conventional manner. Unit dosage forms for oral administration contain, for example, from about 0.1 mg to about 500 mg of active substance.

In one embodiment, the pharmaceutical composition is a solution, including suspension or dispersion, of the active ingredient, such as an isotonic aqueous solution. In the case of lyophilized compositions containing the active ingredient alone or in admixture with a carrier such as mannitol, dispersions or suspensions can be prepared before use. The pharmaceutical compositions can be sterilized and/or contain adjuvants, such as preservatives, stabilizers, wetting or emulsifying agents, dissolution accelerators, salts for adjusting the osmotic pressure and/or buffers. Suitable preservatives include, but are not limited to, antioxidants such as ascorbic acid, microbicides such as sorbic acid or benzoic acid. The solution or suspension may also contain a thickening agent, including but not limited to sodium carboxymethylcellulose, carboxymethylcellulose, dextran, polyvinylpyrrolidone, gelatin, or a solubilizing agent, such as Tween 80 (polyoxyethylene (20) Sorbitan monooleate).

Suspensions in oil may contain, as the oily component, vegetable, synthetic or semi-synthetic oils and are commonly used for injectable purposes. Examples include liquid fatty acid esters containing, as the acid component, long chain fatty acids having from 8 to 22 carbon atoms, or in some embodiments, from 12 to 22 carbon atoms. Suitable liquid fatty acid esters include but are not limited to lauric acid, tridecanoic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, stearic acid, arachidic acid, behenic acid or corresponding unsaturated Acids such as oleic acid, elaidic acid, erucic acid, brassenoic acid and linoleic acid and, if desired, antioxidants such as vitamin E, 3-carotene or 3,5-di-tert-butyl-hydroxytoluene . The alcohol component of these fatty acid esters may have six carbon atoms and may be monovalent or polyvalent, eg mono-, di- or trivalent alcohols. Suitable alcohol components include, but are not limited to, methanol, ethanol, propanol, butanol or pentanol or isomers thereof, ethylene glycol and glycerol.

Other suitable fatty acid esters include, but are not limited to, ethyl oleate, isopropyl myristate, isopropyl palmitate, LABRAFIL® M2375 (polyoxyethylene glycerol), LABRAFIL® M1944 CS (prepared by alcoholysis of almond oil Unsaturated PEGylated Glycerides, containing Glycerides and Polyethylene Glycol Esters), LABRASOL ^TM (saturated PEGylated Glycerides, containing Glycerides and Polyethylene Glycol Esters, prepared by alcoholysis of TCM; both available from French GaKefosse Company), and/or MIGLYOL® 812 (saturated fatty acid triglycerides with a chain length of C8 to C12 from Hüls AG, Germany), and vegetable oils such as cottonseed oil, almond oil, olive oil, castor oil, sesame oil, soybean oil or peanut oil.

Pharmaceutical compositions for oral administration can be obtained, for example, by mixing the active ingredient with one or more solid carriers, granulating the resulting mixture, and processing the mixture or granules by adding further excipients, In the form of tablets or cores.

Suitable carriers include, but are not limited to, fillers such as sugars such as lactose, sucrose, mannitol or sorbitol, cellulose preparations and/or calcium phosphates such as tricalcium phosphate or calcium hydrogen phosphate, and binders such as starches such as Corn, wheat, rice or potato starch, methylcellulose, hydroxypropylmethylcellulose, sodium carboxymethylcellulose and/or polyvinylpyrrolidone, and/or, if desired, a disintegrant, such as the starches above , carboxymethyl starch, cross-linked polyvinylpyrrolidone, alginic acid or its salts, such as sodium alginate. Additional excipients include flow regulators and lubricants, such as silicic acid, talc, stearic acid or its salts, such as magnesium stearate or calcium stearate, and/or polyethylene glycol, or its derivatives .

Tablet cores may be provided with a suitable, optionally enteric coating, by using, inter alia, concentrated sugar solutions, which may include gum arabic, talc, polyvinylpyrrolidone, polyethylene glycol and/or titanium dioxide, or dissolved in Coating solutions in suitable organic solvents or solvent mixtures or, for enteric coatings, solutions of suitable cellulose preparations, such as cellulose acetate phthalate or hydroxypropylmethylcellulose phthalate solutions. Dyestuffs or pigments may be added to the tablets or tablet coatings, eg for identification purposes or to indicate different doses of the active ingredient.

Pharmaceutical compositions for oral administration may also comprise hard capsules, including gelatin or soft, sealed capsules containing gelatin and a plasticizer, such as glycerol or sorbitol. Hard capsules may contain the active ingredients in granule form, for example in admixture with fillers such as corn starch, binders and/or glidants such as talc or magnesium stearate, and, optionally, stabilizers. In soft capsules, the active ingredients can be dissolved or suspended in suitable liquid excipients such as fatty oils, paraffin oil or liquid polyethylene glycol or fatty acid esters of ethylene glycol or propylene glycol, to which stabilizers and Detergents, such as fatty acid esters of polyoxyethylene sorbitol, may also be added.

Pharmaceutical compositions adapted for rectal administration, such as suppositories, comprise the active ingredient in combination with a suppository base. Suitable suppository bases are, for example, natural or synthetic triglycerides, paraffin hydrocarbons, polyethylene glycols or higher alkanols.

Pharmaceutical compositions suitable for parenteral administration may contain the active ingredients in water-soluble form, such as water-soluble salts or aqueous injection suspensions containing substances that increase viscosity, such as sodium carboxymethylcellulose, aqueous solutions of sorbitol and/or or dextran, and, if desired, stabilizers. The active ingredient, optionally with excipients, can also be in a freeze-dried form, and can be prepared in solution by adding a suitable solvent before parenteral administration. Solutions used, for example, for parenteral administration can also be used as infusion solutions. Preparations for injection are usually prepared under sterile conditions, filled into, for example, ampoules or vials, and sealed containers.

The present invention also provides a pharmaceutical combination, such as a kit, which comprises (a) the compound disclosed in the present invention in free form or in a pharmaceutically acceptable salt form, and (b) at least one auxiliary agent. The kit may contain instructions for its use.

[ combination therapy ]

The compounds or pharmaceutically acceptable salts described in this patent can be used alone or in combination with other therapeutic agents.

For example, the use of an adjuvant (adjuvant) can enhance the therapeutic effect of the compound of the present invention (for example, the therapeutic benefit of the adjuvant drug alone is minimal, but when combined with another drug, the therapeutic benefit of the individual can be enhanced), Alternatively, for example, a compound of the invention may be administered in combination with another equally therapeutic therapeutic agent to enhance the individual's therapeutic benefit. For example, in the treatment of gout, when the compound of the present invention is used in combination with another drug for the treatment of gout, the clinical benefit may be enhanced. Alternatively, for example, if nausea is the adverse effect of administration of the compounds of the invention, anti-nausea drugs may be administered in combination. Alternatively, therapies that may also be combined include, but are not limited to, physical therapy, psychotherapy, radiation therapy, compression therapy of the diseased area, rest, dietary modification, and the like. Regardless of the disease, disorder or condition, there should be an additive or synergistic effect of the two therapies to benefit the individual's treatment.

When the compound of this patent is used in combination with other therapeutic agents, the route of administration of the pharmaceutical composition of the compound of this patent may be the same as that of other drugs, or the route of administration may be different due to different physical and chemical properties. For example, oral administration of a patented compound may produce and maintain good blood levels, while another therapeutic agent may require intravenous administration. Thus the patented compound and another therapeutic agent may be administered simultaneously, sequentially or separately.

[ Example ]

There are many methods for synthesizing the compound of formula (I) or a pharmaceutically acceptable salt thereof, and the representative methods are listed in this example. However, it should be pointed out that the compound of formula (I) or a pharmaceutically acceptable salt thereof may also be synthesized by other synthetic schemes.

In a compound of formula (I), linkages between atoms and other atoms may result in the existence of particular stereoisomers (eg chiral centers). Synthesis of compounds of formula (I) or pharmaceutically acceptable salts thereof may result in mixtures of different isomers (enantiomers, diastereomers). Unless a specific stereoconfiguration is specified, the listed compounds include their possible different stereoisomers.

Compounds of formula (I) can also be prepared as pharmaceutically acceptable acid addition salts, for example, by reacting the free base form of a compound of the invention with a pharmaceutically acceptable inorganic or organic acid. Or react a compound of formula (I) in the form of free acid with a pharmaceutically acceptable inorganic or organic base to prepare a pharmaceutically acceptable base addition salt. Inorganic and organic acids and bases which are suitable for the preparation of pharmaceutically acceptable salts of compounds of formula (I) are described in the definitions section of this application. Furthermore, salt forms of compounds of formula (I) can also be prepared by using salts of starting materials or intermediates.

The free acid or free base of the compound of formula (I) can be prepared by its corresponding base addition salt or acid addition salt. Acid addition salt forms of compounds of formula (I) can be converted into the corresponding free base, for example by treatment with a suitable base (eg ammonium hydroxide solution, sodium hydroxide, etc.). A base addition salt form of a compound of formula (I) can be converted into the corresponding free acid, for example by treatment with a suitable acid (eg hydrochloric acid etc.).

An N-oxide of a compound of formula (I) or a pharmaceutically acceptable salt thereof may be prepared by methods known in the art. For example, the N-oxide compound can be obtained by reacting the non-oxidized form of the compound of formula (I) with an oxidizing agent (such as trifluoroperoxyacetic acid, permaleic acid (permaleic acid), peroxybenzene) under the condition of 0 ~ 80 ° C. Formic acid, peracetic acid and m-chloroperoxybenzoic acid, etc.) are obtained by reacting in an inert organic solvent (such as halogenated hydrocarbons such as dichloromethane). Alternatively, N-oxides of compounds of formula (I) can also be prepared from N-oxides of starting materials.

The non-oxidized form of the compound of formula (I) can be obtained by reacting its N-oxide with a reducing agent (such as sulfur, sulfur dioxide, triphenylphosphine, lithium borohydride, sodium borohydride, phosphorus trichloride and phosphorus tribromide, etc.) Prepared by reacting in corresponding inert organic solvents (such as acetonitrile, ethanol and dioxane aqueous solution, etc.) at 0 ~ 80 ° C.

Protected derivatives of compounds of formula (I) can be prepared by methods well known to those skilled in the art. For a detailed technical description of the addition and removal of protecting groups see: T.W. Greene, Protecting Groups in Organic Synthesis, 3rd edition, John Wiley & Sons, Inc. 1999.

The methods, routes and symbols used in the examples and common sense are consistent with current scientific literature, eg, Journal of the American Chemical Society or Journal of Biochemistry. Standard one-letter or three-letter abbreviations generally refer to L-form amino acid residues, unless otherwise indicated. Unless otherwise stated, all starting materials used were purchased from commercial suppliers and used without further purification. For example, the following abbreviations are used in the examples and throughout the specification: g (gram), mg (milligram), L (liter), mL (milliliter), μL (microliter), psi (pounds per square inch), M ( Mole), mM (millimole), iv (intravenous injection), Hz (hertz), MHz (megahertz), mol (mole), mmol (millimole), RT (ambient temperature), min (minute), h (hours), mp (melting point), TLC (thin layer chromatography), Rt (retention time), RP (reverse phase), MeOH (methanol), i-PrOH (isopropanol), TEA (triethylamine), TFA (trifluoroacetic acid), TFAA (trifluoroacetic anhydride), THF (tetrahydrofuran), DMSO (dimethylsulfene), EtOAc (ethyl acetate), DME (1,2-dimethoxyethane), DCM (dichloromethane), DCE (dichloroethane), DMF ( N , N -dimethylformamide), DMPU ( N , N' -dimethylpropenyl urea), CDI (1,1- carbonyldiimidazole), IBCF (isobutyl chloroformate), HOAc (acetic acid), HOSu (N-hydroxysuccinimide), HOBT (1-hydroxybenzotriazole), Et ₂ O (ether), EDCI (1-(3-Dimethylaminopropyl) 3-ethylcarbodiimide hydrochloride), BOC (tert-butoxycarbonyl), FMOC (9-fluorenylmethoxycarbonyl), DCC (dicyclohexyl Carbodiimide), CBZ (benzyloxycarbonyl), Ac (acetyl), atm (atmospheric pressure), TMSE (2-(trimethylsilyl) ethyl), TMS (trimethylsilyl), TIPS (triisopropyl Silyl), TBS (tert-butyldimethylsilyl), DMAP (4-dimethylaminopyridine), Me (methyl), OMe (methoxy), Et (ethyl), tBu (tert-butyl base), HPLC (high performance liquid chromatography), BOP (bis(2-oxo-3-oxazolidinyl)phosphinyl chloride), TBAF (tetra-n-butylammonium fluoride), mCPBA (m-chloroper oxybenzoic acid).

Ether or Et ₂ O refers to diethyl ether; brine refers to saturated NaCl aqueous solution. Unless otherwise stated, all temperatures are in °C (Celsius), and all reactions are at room temperature under an inert atmosphere.

¹ H NMR spectra were recorded using a Varian Mercury Plus 400 nuclear magnetic resonance spectrometer. Chemical shifts are expressed in ppm. Coupling constants are in Hertz (Hz). Apparent diversity was described in terms of segmentation patterns and designated as s (singlet), d (doublet), t (triplet), q (quartet), m (multiplet), and br (broad).

Low-resolution mass spectrometry (MS) and compound purity data were obtained from a Shimadzu LC/MS single quadrupole system equipped with an electrospray ionization detector (ESI), UV detectors (220 and 254nm) and an evaporative light scattering detector (ELSD) . TLC uses 0.25mm Asahi Kasei silica gel plate (60F-254), 5% ethanol solution of phosphomolybdic acid, ninhydrin or p-methoxybenzaldehyde solution and observes under ultraviolet light. The flash column chromatography used silica gel (200-300 mesh, Qingdao Ocean Chemical Co., Ltd.).

[ Synthetic scheme ]

Synthetic schemes for all compounds of the invention are illustrated by the following Schemes and Examples. The starting materials used are commercially available or can be prepared according to existing techniques or methods exemplified here.

The intermediates listed in the following schemes are known in the literature, or can be prepared by those skilled in the art according to similar methods.

合成方案1 As an illustration, Scheme 1 discloses two synthetic methods of the compound of formula I disclosed in the present invention. As shown in the scheme, the compound of formula I can be split into intermediates III and II, which can be obtained through alkylation coupling. Alternatively, compounds of formula I can be prepared by cross-coupling intermediates IV and V.

Synthetic scheme 1

合成方案2 As an illustration of the preparation of intermediates of formula II, one synthesis of compound IIa is shown in Scheme 2. Amino esters IIa-C can be prepared by Wittig-Horner reaction of IIa-A with IIa-B starting from commercially available or literature-reported aldehyde IIa-A. Intramolecular cyclization of IIa-C to prepare lactam IIa-D, reduction of the ester group of IIa-D to alcohol IIa-E, and conversion to IIa by chlorination agent such as _SOCl2 .

Synthetic scheme 2

合成方案3 As a further illustration of the preparation method of the intermediate of formula II, a synthesis method of compound IIb is shown in scheme 3. IIb-C was prepared by cross-coupling IIb-A with IIb-B via a nucleophilic substitution reaction. Reduction of the nitro group and intramolecular cyclization give lactam IIb-D, which can be converted to IIb-E by oxidative aromatization. After reduction/chlorination transformation as described in Scheme 2, lib-E can be converted to intermediate formula lib.

Synthetic scheme 3

合成方案4 As an illustration of the preparation method of the intermediate of formula IV, a synthetic method of compound IV is shown in scheme 4. Starting from the readily available ketone or aldehyde IV-A, the chiral amine IV-D is prepared by successive condensation of IV-A with Elman's reagent, addition of Grignard reagent, and acid hydrolysis. Amines IV-D are converted to intermediates of formula IV by art-known cyclization reactions.

Synthetic Scheme 4

In some cases, in order to promote the reaction or avoid unnecessary reaction products, the above synthetic schemes can be adjusted according to the order. In order that the present invention may be more fully understood, the following examples are provided. These examples are only examples and should not be construed as limiting the present invention. Example 1

5-(4-((6- Ethyl -7- oxo - 7,8- dihydro -1,8- naphthyridin -2- yl ) methyl ) piperazin -1- yl )-N- methyl Pyridinamide (1)

tert-butyl (6- chlorine -3- Formylpyridine -2- base ) Urethane (1a)

The title compound tert-butyl (6-chloro-3-formylpyridin-2-yl)carbamate (1a) was prepared according to the literature Journal of Medicinal Chemistry, 2000, 43, 3134-3147 . MS-ESI (m/z): 257 [M + 1] ⁺ .

2-Amino-6-chloronicotinaldehyde (1b)

To a solution of tert-butyl (6-chloro-3-formylpyridin-2-yl)carbamate ( 1a ) (0.53 g, 2.0 mmol) in DCM (5 mL) was added TFA (5 mL) and incubated at room temperature Stir for 1 h. The mixture was concentrated in vacuo. The residue was added water (25 mL) and neutralized with solid NaHCO ₃ until no gas evolved. The mixture was extracted with ethyl acetate (50 mL × 2), and the organic layer was dried over Na ₂ SO ₄ and concentrated to give 2-amino-6-chloronicotinaldehyde ( 1b ) as a yellow solid. MS-ESI (m/z): 157 [M + 1] ⁺ .

7- chlorine -3- Ethyl -1,8- naphthyridine -2(1H)- ketone ( 1c )

To a solution of 2-amino-6-chloronicotinaldehyde ( 1b ) (0.25 g, 1.6 mmol) in ethyl butyrate (8 mL) was added t -BuOK (0.5 g, 4.5 mmol), and heated at 120 ^° Stir at C for 1 h. The reaction mixture was cooled to RT, quenched with water (25 mL) and extracted with EtOAc (25 ml x 2), the organic layer was dried over Na ₂ SO ₄ and concentrated. The residue was purified by silica gel column chromatography, eluting with PE/EtOAc=4:1 to give 7-chloro-3-ethyl-1,8-naphthyridin-2(1 H )-one ( 1c ) as a white solid. MS-ESI (m/z): 209 [M + 1] ⁺ .

3- Ethyl -7- vinyl -1,8- naphthyridine -2(1H)- ketone ( 1d )

To the 1 , Add water (0.5 mL), K ₃ PO ₄ (0.5 g, 1.65 mmol) and PdCl ₂ (dppf) (48 mg, 0.06 mmol) to the suspension of 4-dioxane (5 mL), under nitrogen atmosphere at Stir at 90 ^o C for 1 h. Water (30 mL) was added to the reaction mixture and extracted with EtOAc (50 mL x 3), the organic layer was washed with brine, dried over Na ₂ SO ₄ and concentrated. The residue was purified by silica gel column chromatography, eluting with PE/EtOAc=10:1 to 4:1 to give white solid 3-ethyl-7-vinyl-1,8-naphthyridine-2(1 H )- Ketones ( 1d ). MS-ESI (m/z): 201 [M + 1] ⁺ .

6- Ethyl -7- Oxo -7,8- Dihydro -1,8- naphthyridine -2- formaldehyde ( 1f )

To 3-ethyl-7-vinyl-1,8-naphthyridin-2( 1H )-one ( 1d ) (20 mg, 0.1 mol) in 1,4-dioxane (2 mL) and water (0.5 mL) NaIO ₄ (85 mg, 0.4 mmol) and K ₂ OsO ₄ .2H ₂ O (5 mg, 0.01 mmol) were added to the solution, and stirred at room temperature for 24 h. Water (10 mL) was added to the reaction mixture and extracted with EtOAc (10 mL × 3 ₎ , the organic layer was washed with saturated _Na2SO3 solution, brine, dried _{over Na2SO4} and concentrated to give white solid 6-ethyl-7- Oxo-7,8-dihydro-1,8-naphthyridine-2-carbaldehyde ( 1f ). MS-ESI (m/z): 203 [M + 1] ⁺ .

N- methyl -5- Piperazine -1 - base - pyridine -2- Formamide , 2HCl ( 1e )

The title compound N -methyl-5-piperazin-1-yl-pyridine-2-carboxamide, 2HCl ( 1e ) was prepared according to patent WO 2021/013735 . MS-ESI (m/z): 221 [M + 1] ⁺ .

5-(4-((6- Ethyl -7- Oxo -7,8- Dihydro -1,8- naphthyridine -2- base ) methyl ) Piperazine -1- base )-N- Pyridinamide ( 1 )

To 6-ethyl-7-oxo-7,8-dihydro-1,8-naphthyridine-2-carbaldehyde ( 1f ) (5 mg, 0.025 mmol) and N -methyl-5-piperazine-1 -Yl-pyridine-2-carboxamide, 2HCl ( 1e ) (8 mg, 0.027mmol) in DCE (3 mL) was added TEA (5.5 mg, 0.055mmol) and NaBH(OAc) ₃ (32 mg, 0.15 mmol), the reaction was stirred overnight at room temperature. The reaction was quenched with saturated NaHCO ₃ solution, stirred for 0.5 h, extracted with DCM (10 mL × 3), and the organic layer was dried over Na ₂ SO ₄ and concentrated. The residue was purified by preparative TLC plate, eluting with DCM/MeOH=10:1 to give 5-(4-((6-ethyl-7-oxo-7,8-dihydro-1, 8-naphthyridin-2-yl)methyl)piperazin-1-yl) -N -methylpyridinamide ( 1 ). MS-ESI (m/z): 407 [M + 1] ⁺ . Example 2

1'-((7- Ethyl -6- oxo- 5,6- dihydro - 1,5- naphthyridin - 3- yl ) methyl )-N- methyl - 1',2',3',6'- Tetrahydro- [3,4'- bipyridyl ]-6- formamide ( 2 )

7-( Chloromethyl )-3- Ethyl -1,5- naphthyridine -2(1H)- ketone ( 2a )

7-(Chloromethyl)-3-ethyl-1,5-naphthyridin-2( 1H )-one ( 2a ) was prepared according to patent WO2021/013735 .

tert-butyl 6-( Methylcarbamoyl )-3',6'- Dihydro -[3,4'- Bipyridine ]-1'(2'H)- Formate ( 2b )

5-Bromo- N -methylpyridinamide ( WO2021/013735) (160 mg, 0.744 mmol), tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-di Oxaboran-2-yl)-3,6-dihydropyridine-1(2 H )-carboxylate (230 mg, 0.744 mmol), K ₂ CO ₃ (205 mg, 1.49 mmol) and PdCl ₂ ( dppf) (55 mg, 0.074 mmol) in DMF (3 mL) was stirred at 95 °C for 1.5 h under nitrogen. The mixture was cooled to room temperature and concentrated. The residue was purified by silica gel column chromatography, eluting with DCM/EtOAc (5:1 ~ 1:1) to obtain the title compound tert-butyl 6-(methylcarbamoyl)-3',6'-dihydro-[ 3,4'-bipyridine]-1'( 2'H )-carboxylate ( 2b ). MS-ESI (m/z): 318 [M + 1] ⁺ .

N- methyl -1',2',3',6'- Tetrahydro -[3,4'- Bipyridine ]-6- Formamide ( 2c )

tert-Butyl 6-(methylcarbamoyl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2' H )-carboxylate ( 2b ) (24 mg, 0.076 mmol) and TFA (1.0 mL, 10 mmol) in DCM (1 mL) was stirred at room temperature for 20 min. The mixture was evaporated to dryness to obtain the crude product of N -methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridine]-6-formamide ( 2c ), which was directly used in the next step reaction. MS-ESI (m/z): 218 [M + 1] ⁺ .

1'-((7- Ethyl -6- Oxo -5,6- Dihydro -1,5- naphthyridine -3- base ) methyl )-N- methyl -1',2',3',6'- Tetrahydro -[3,4'- Bipyridine ]-6- Formamide ( 2 )

7-(chloromethyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one ( 2a ) (17.0 mg, 0.076 mmol), N -methyl-1',2', A mixture of 3',6'-tetrahydro-[3,4'-bipyridine]-6-formamide ( 2c ) (16.6 mg, 0.076 mmol) and DIPEA (4 drops) in ACN (1.5 mL) was added to Stir at 80°C for 2 h. The mixture was cooled to room temperature and concentrated. The residue was purified by preparative thin layer chromatography to afford the title compound 1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridine]-6-formamide ( 2 ). MS-ESI (m/z): 404 [M + 1] ⁺ . Example 3

3- Ethyl -7-((4-(6- methyl -5- oxo - 6,7- dihydro -5H- pyrrolo [3,4-b] pyridin -2- yl ) piperazine -1 -yl ) methyl )-1,5- naphthyridin - 2 (1H) -one ( 3 )

methyl 2-( Chloromethyl ) Niacinate ( 3a )

A mixture of methyl 2-methylnicotinate (1.9 g, 0.013 mmol) and TCCA (3.7 g, 0.015 mmol) in DCM (50 mL) was stirred at room temperature for 16 h. The reaction product was concentrated, and the residue was purified by silica gel column chromatography, eluting with PE/EtOAc = 50:1-20:1 to obtain methyl 2-(chloromethyl)nicotinate ( 3a ). MS-ESI (m/z): 186 [M + 1] ⁺ .

2-( Chloromethyl )-3-( Methoxycarbonyl ) pyridine 1- Oxide ( 3b )

To a solution of methyl 2-(chloromethyl)nicotinate ( 3a ) (1.5 g, 8.1 mmol) in DCM (40 ml) was added m-CPBA (1.7 g, 9.7 mmol) at room temperature. and stirred overnight at room temperature. The mixture was evaporated to dryness to obtain the crude product of 2-(chloromethyl)-3-(methoxycarbonyl)pyridine 1-oxide ( 3b ), which was directly used in the next reaction. MS-ESI (m/z): 202 [M + 1] ⁺ .

methyl 6- chlorine -2-( Chloromethyl ) Niacinate ( 3c )

A mixture of 2-(chloromethyl)-3-(methoxycarbonyl)pyridine 1-oxide ( 3b ) (500 mg, 2.49 mmol) in POCl ₃ (2 mL) was stirred at 110° C. for 15 h . The mixture was poured into ice water, adjusted to pH 8~9 with saturated aqueous NaHCO ₃ , extracted with DCM, washed with brine, dried over Na ₂ SO ₄ , and concentrated. The residue was purified by silica gel column chromatography, eluting with PE/EtOAc = 30:1-20:1 to give methyl 6-chloro-2-(chloromethyl)nicotinate ( 3c ). MS-ESI (m/z): 220 [M + 1] ⁺ .

2- chlorine -6- methyl -6,7- Dihydro -5H- pyrrolo [3,4-b] pyridine -5- ketone ( 3d )

A mixture of methyl 6-chloro-2-(chloromethyl)nicotinate ( 3c ) (280 mg, 1.278 mmol) in NH ₂ Me (30% CH ₃ OH solution, 2 mL) was incubated at room temperature Stir for 20 min. The mixture was evaporated to dryness to obtain a crude product of 2-chloro-6-methyl-6,7-dihydro- 5H -pyrrolo[3,4- b ]pyridin-5-one ( 3d ), which was directly used in the next reaction. MS-ESI (m/z): 183 [M + 1] ⁺ .

tert-butyl 4-(6- methyl -5- Oxo -6,7- Dihydro -5H- pyrrolo [3,4-b] pyridine -2- base ) Piperazine -1- Formate ( 3e )

2-Chloro-6-methyl-6,7-dihydro- 5H -pyrrolo[3,4- b ]pyridin-5-one ( 3d ) (36 mg, 0.2 mmol), tert-butylpiperazine -1-Carboxylate (55 mg, 0.3 mmol), Pd ₂ (dba) ₃ (18 mg, 0.02 mmol), S-phos (16 mg, 0.028 mmol) and K ₃ PO ₄ (85 mg, 0.4 mmol) The mixture in DMF (1 mL) was stirred overnight at 130°C. The mixture was cooled to room temperature, quenched with water and extracted with EtOAc. The extract was washed with saturated brine, dried over Na ₂ SO ₄ and concentrated, and the residue was purified by silica gel column chromatography, eluted with PE/EtOAc = 5:1 - 3:1 to obtain tert-butyl 4-(6-methyl-5 -Oxo-6,7-dihydro- 5H -pyrrolo[3,4- b ]pyridin-2-yl)piperazine-1-carboxylate ( 3e ). MS-ESI (m/z): 333 [M + 1] ⁺ .

3- Ethyl -7-((4-(6- methyl -5- Oxo -6,7- Dihydro -5H- pyrrolo [3,4-b] pyridine -2- base ) Piperazine -1- base ) methyl )-1,5- naphthyridine -2(1H)- ketone ( 3 )

The title compound 3-ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro- 5H -pyrrolo[3,4- b ]pyridin-2-yl)piper Azin-1-yl)methyl)-1,5-naphthyridin-2( 1H )-one ( 3 ) was prepared according to the synthesis method of 2 , and tert-butyl 6-(methylaminoformyl )-3',6'-dihydro-[3,4'-bipyridine]-1'(2' H )-carboxylate ( 2b ) was replaced by tert-butyl 4-(6-methyl-5- Oxo-6,7-dihydro- 5H -pyrrolo[3,4- b ]pyridin-2-yl)piperazine-1-carboxylate ( 3e ). MS-ESI (m/z): 419 [M + 1] ⁺ . Reference compound 1

5-(4-((7- Ethyl -6- Oxo -5,6- Dihydro -1,5- naphthyridine -3- base ) methyl ) Piperazine -1- base )-N- Pyridinamide ( reference compound 1 )

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -methyl Pyridinamide ( reference compound 1 ) was prepared according to patent WO 2021013735 . MS-ESI (m/z): 407 [M + 1] ⁺ .

Examples 4-514 listed in Table 1 were basically followed the same method as Examples 1-3, and the starting materials used were commercially available or prepared according to literature methods. Table 1 shows the names and structures of Examples 4-514.

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 5

5-(5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)六氫吡咯並[3,4-c]吡咯-2(1H)-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 6

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 7

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)氮雜環丁烷-3-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 393 [M + 1] ⁺ 8

5-(7-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,7-二氮雜螺[3.5]壬烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 9

5-(6-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 10

5-((1R,4R)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.1]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 11

5-((1S,4S)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.1]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 12

5-(8-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 13

(R)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 14

(S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 15

5-(7-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4,7-二氮雜螺[2.5]辛烷-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 16

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,2-二甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 17

5-((2S,6R)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,6-二甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 18

5-((2R,6R)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,6-二甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 19

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,8-二氮雜雙環[3.2.1]辛烷-8-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 20

5-((1R,4R)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.2]辛烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 21

5-((1S,4S)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.2]辛烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 22

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 23

5-((1R,4R)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.1]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 24

5-((1S,4S)-5-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,5-二氮雜雙環[2.2.1]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 25

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-甲基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 26

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氟哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 439 [M + 1] ⁺ 27

5-((3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 28

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-羥基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 437 [M + 1] ⁺ 29

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-甲氧基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 451 [M + 1] ⁺ 30

5-((4-乙氧基-1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 465 [M + 1] ⁺ 31

5-((4-氰基-1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 32

1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-((6-(甲基氨基甲醯基)吡啶-3-基)氨基)哌啶-4-基 乙酸酯 MS-ESI (m/z): 479 [M + 1] ⁺ 33

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-(羥基甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 451 [M + 1] ⁺ 34

5-(9-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,9-二氮雜螺[5.5]十一烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 475 [M + 1] ⁺ 35

5-(8-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,8-二氮雜螺[4.5]癸烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 36

5-(2-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,8-二氮雜螺[4.5]癸烷-8-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 37

5-(2-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,7-二氮雜螺[3.5]壬烷-7-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 38

5-(2-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,6-二氮雜螺[3.4]辛烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 39

5-(6-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,6-二氮雜螺[3.4]辛烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 40

5-(6-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,6-二氮雜螺[3.3]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 41

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)吡咯烷-3-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 407 [M + 1] ⁺ 42

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)吡咯烷-3-基)氧)-N-甲基吡啶醯胺 MS-ESI (m/z): 408 [M + 1] ⁺ 43

5-((1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)氮雜環丁烷-3-基)氧)-N-甲基吡啶醯胺 MS-ESI (m/z): 394 [M + 1] ⁺ 44

1'-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 404 [M + 1]+ 45

1'-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 404 [M + 1]+ 46

5-(6-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-3,6-二氮雜雙環[3.1.1]庚烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 47

5-(5-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)六氫吡咯並[3,4-c]吡咯-2(1H)-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 48

5-(7-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-2,7-二氮雜螺[3.5]壬烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 49

5-(6-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-2,6-二氮雜螺[3.3]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 50

5-((7-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-7-氮雜螺[3.5]壬烷-2-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 51

5-(1-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 52

5-((1-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 53

5-((1-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-4-甲基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 54

5-((1-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)氮雜環丁烷-3-基)氧)-N-甲基吡啶醯胺 MS-ESI (m/z): 394 [M + 1] ⁺ 55

5-(3-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-3,8-二氮雜雙環[3.2.1]辛烷-8-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 56

5-(3-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-3,6-二氮雜雙環[3.1.1]庚烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 57

5-(9-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-3,9-二氮雜螺[5.5]十一烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 475 [M + 1] ⁺ 58

5-(7-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-2,7-二氮雜螺[3.5]壬烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 59

5-(6-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-2,6-二氮雜螺[3.3]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 60

5-((7-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-7-氮雜螺[3.5]壬烷-2-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 61

5-(1-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 62

5-((1-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 63

5-((1-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)-4-甲基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 64

5-((1-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)氮雜環丁烷-3-基)氧)-N-甲基吡啶醯胺 MS-ESI (m/z): 394 [M + 1] ⁺ 65

5-(3-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-3,8-二氮雜雙環[3.2.1]辛烷-8-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 66

5-(3-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-3,6-二氮雜雙環[3.1.1]庚烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 67

5-(9-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-3,9-二氮雜螺[5.5]十一烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 475 [M + 1] ⁺ 68

5-(7-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2,7-二氮雜螺[3.5]壬烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 69

5-(6-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2,6-二氮雜螺[3.3]庚烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 70

5-((7-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-7-氮雜螺[3.5]壬烷-2-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 71

5-(1-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 72

5-((1-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 73

5-((1-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-4-甲基哌啶-4-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 74

5-((1-((2-乙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)氮雜環丁烷-3-基)氧)-N-甲基吡啶醯胺 MS-ESI (m/z): 394 [M + 1] ⁺ 75

3-乙基-7-((4-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 76

3-乙基-7-((4-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 77

3-乙基-7-((4-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 78

3-乙基-7-((8-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 79

3-乙基-7-((2-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-2,7-二氮雜螺[3.5]壬烷-7-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 80

3-乙基-7-((4-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氨基)哌啶-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 81

3-乙基-7-((3-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氧)吡咯烷-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 82

3-乙基-7-((8-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 83

3-乙基-7-((2-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-2,7-二氮雜螺[3.5]壬烷-7-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 84

3-乙基-7-((4-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氨基)哌啶-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 85

3-乙基-7-((3-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氧)吡咯烷-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 86

3-乙基-7-((8-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 87

3-乙基-7-((2-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-2,7-二氮雜螺[3.5]壬烷-7-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 88

3-乙基-7-((4-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氨基)哌啶-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 89

3-乙基-7-((3-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氧)吡咯烷-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 90

3-乙基-7-((8-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 91

3-乙基-7-((2-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-2,7-二氮雜螺[3.5]壬烷-7-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 92

3-乙基-7-((4-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氨基)哌啶-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 93

3-乙基-7-((3-((6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)氧)吡咯烷-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 94

3-乙基-7-((8-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)-3,8-二氮雜雙環[3.2.1]辛烷-3-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 95

3-乙基-7-((2-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)-2,7-二氮雜螺[3.5]壬烷-7-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 96

3-乙基-7-((4-((6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)氨基)哌啶-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 97

3-乙基-7-((3-((6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)氧)吡咯烷-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 98

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 99

5-(3-((6-乙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)-3,8-二氮雜雙環[3.2.1]辛烷-8-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 100

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)哌嗪-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 101

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-2-基)哌嗪-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 102

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡嗪-2-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 103

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡嗪-2-基)哌嗪-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 104

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡嗪-2-基)哌嗪-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 105

3-乙基-7-((4-(6-甲基-5-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡嗪-2-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 420 [M + 1] ⁺ 106

3-乙基-7-((4-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 419 [M + 1] ⁺ 107

3-乙基-7-((4-(2-甲基-1-氧代異吲哚啉-5-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 418 [M + 1] ⁺ 108

3-乙基-7-((4-(2-甲基-1-氧代異吲哚啉-5-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 418 [M + 1] ⁺ 109

5-(4-((6-環丙基-7-氧代-7,8-二氫-1,8-萘啶-2-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 110

3-環丙基-7-((4-(6-甲基-7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 431 [M + 1] ⁺ 111

3-環丙基-7-((4-(2-甲基-1-氧代異吲哚啉-5-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 430 [M + 1] ⁺ 112

5-(9-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,9-二氮雜螺[5.5]十一烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 487 [M + 1] ⁺ 113

5-(7-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2,7-二氮雜螺[3.5]壬烷-2-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 459 [M + 1] ⁺ 114

5-((7-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-7-氮雜螺[3.5]壬烷-2-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 473 [M + 1] ⁺ 115

5-((7-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-7-氮雜螺[3.5]壬烷-2-基)氨基)-N-甲基吡啶醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 116

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,6-二氮雜雙環[3.2.0]庚烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 117

5-(6-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,6-二氮雜雙環[3.2.0]庚烷-3-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 118

6-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 407 [M + 1] ⁺ 119

6-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 405 [M + 1] ⁺ 120

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基嘧啶-2-甲醯胺 MS-ESI (m/z): 407 [M + 1] ⁺ 121

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基嘧啶-2-甲醯胺 MS-ESI (m/z): 405 [M + 1] ⁺ 122

N-甲基-6-(1-((6-氧代-7-苯基-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)噠嗪-3-甲醯胺 MS-ESI (m/z): 453 [M + 1] ⁺ 123

5-(2-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2-噁嗪-5-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 408 [M + 1] ⁺ 124

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲氧基吡啶醯胺 MS-ESI (m/z): 423 [M + 1] ⁺ 125

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-3-氟-N-甲基吡啶醯胺 MS-ESI (m/z): 424 [M + 1] ⁺ 126

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-5-氟-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 127

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-羥基哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 128

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-甲氧基哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 436 [M + 1] ⁺ 129

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氟哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 424 [M + 1] ⁺ 130

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-氟哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 424 [M + 1] ⁺ 131

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 404 [M + 1] ⁺ 132

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[4.1.0]庚烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 133

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-羥基哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 134

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4-甲氧基哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 436 [M + 1] ⁺ 135

5-(4-乙氧基-1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 450 [M + 1] ⁺ 136

5-(4-氰基-1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 431 [M + 1] ⁺ 137

N-甲基-5-(1-((6-氧代-7-苯基-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)吡啶醯胺 MS-ESI (m/z): 454 [M + 1] ⁺ 138

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲氧基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 420 [M + 1] ⁺ 139

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3,3-二氟哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 140

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3',3'-二氟-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 141

5-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 404 [M + 1] ⁺ 142

5-(1-((7-異丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 420 [M + 1] ⁺ 143

5-(1-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 144

N-甲基-5-(1-((6-氧代-7-(2,2,2-三氟乙基)-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)吡啶醯胺 MS-ESI (m/z): 460 [M + 1] ⁺ 145

5-(1-((7-(2,2-二氟乙基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 146

5-(1-((7-(二氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 428 [M + 1] ⁺ 147

N-甲基-5-(1-((6-氧代-7-(三氟甲基)-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)吡啶醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 148

1'-((7-異丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 149

1'-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 416 [M + 1] ⁺ 150

N-甲基-1'-((6-氧代-7-(2,2,2-三氟乙基)-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 151

1'-((7-(2,2-二氟乙基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 152

1'-((7-(二氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 426 [M + 1] ⁺ 153

N-甲基-1'-((6-氧代-7-(三氟甲基)-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 444 [M + 1] ⁺ 154

6-(1-((7-異丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 155

6-(1-((7-異丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 419 [M + 1] ⁺ 156

6-(1-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 419 [M + 1]+ 157

6-(1-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 417 [M + 1] ⁺ 158

N-甲基-6-(1-((6-氧代-7-(2,2,2-三氟乙基)-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)噠嗪-3-甲醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 159

N-甲基-6-(1-((6-氧代-7-(2,2,2-三氟乙基)-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)噠嗪-3-甲醯胺 MS-ESI (m/z): 459 [M + 1] ⁺ 160

6-(1-((7-(2,2-二氟乙基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 443 [M + 1] ⁺ 161

6-(1-((7-(2,2-二氟乙基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 441 [M + 1] ⁺ 162

6-(1-((7-(二氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 427 [M + 1] ⁺ 163

6-(1-((7-(二氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 429 [M + 1] ⁺ 164

N-甲基-6-(1-((6-氧代-7-(三氟甲基)-5,6-二氫-1,5-萘啶-3-基)甲基)-1,2,3,6-四氫吡啶-4-基)噠嗪-3-甲醯胺 MS-ESI (m/z): 445 [M + 1] ⁺ 165

N-甲基-6-(1-((6-氧代-7-(三氟甲基)-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)噠嗪-3-甲醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 166

6-(3-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基噠嗪-3-甲醯胺 MS-ESI (m/z): 405 [M + 1] ⁺ 167

5-(3-((7-異丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 168

5-(3-((7-環丙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 416 [M + 1] ⁺ 169

N-甲基-5-(3-((6-氧代-7-(2,2,2-三氟乙基)-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)吡啶醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 170

5-(3-((7-(2,2-二氟乙基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 171

5-(3-((7-(二氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 426 [M + 1] ⁺ 172

N-甲基-5-(3-((6-氧代-7-(三氟甲基)-5,6-二氫-1,5-萘啶-3-基)甲基)-3-氮雜雙環[3.1.0]己烷-6-基)吡啶醯胺 MS-ESI (m/z): 444 [M + 1] ⁺ 173

6-(二氟甲基)-5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 456 [M + 1] ⁺ 174

2-(二氟甲基)-1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 454 [M + 1] ⁺ 175

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-6-氟-N-甲基吡啶醯胺 MS-ESI (m/z): 424 [M + 1] ⁺ 176

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-氟-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 177

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-甲氧基吡啶醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 178

N-甲基-1'-((7-甲基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 390 [M + 1] ⁺ 179

(R)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 180

(S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-甲基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 181a

( S)-5-(3-乙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 181b

( R)-5-(3-乙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 182a

( S)-5-(2-乙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 182b

( R)-5-(2-乙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 183a

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-異丙基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 449 [M + 1] ⁺ 183b

( R)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-異丙基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 449 [M + 1] ⁺ 184

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-異丙基哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 449 [M + 1] ⁺ 185

5-(2-環丙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 186

5-(3-環丙基-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 187

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-(三氟甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 475 [M + 1] ⁺ 188

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-(甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 475 [M + 1] ⁺ 189a

( R)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-(羥基甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 437 [M + 1] ⁺ 189b

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-(羥基甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 437 [M + 1] ⁺ 190a

( R)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-(羥基甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 437 [M + 1] ⁺ 190b

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-(羥基甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 437 [M + 1] ⁺ 191

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-(甲氧基甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 451 [M + 1] ⁺ 192

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-(甲氧基甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 451 [M + 1]+ 193

( R)-5-(3-(氰基甲基)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 194a

( S)-5-(2-(氰基甲基)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 194b

( R)-5-(2-(氰基甲基)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 195

( S)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-3-(氟甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 439 [M + 1] ⁺ 196

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-2-(氟甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 439 [M + 1] ⁺ 197

5-(3-(二氟甲基)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 467 [M + 1] ⁺ 198

5-(2-(二氟甲基)-4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 467 [M + 1] ⁺ 199

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-4,7-二氮雜螺[2.5]辛-7-基)-N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 200

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 405 [M + 1] ⁺ 201

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌啶-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 404 [M + 1] ⁺ 202

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)-3,6-二氫吡啶-1(2H)-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 402 [M + 1] ⁺ 203

3-乙基-7-((4-(1-氧代異吲哚啉-5-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 404 [M + 1] ⁺ 204

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,8-萘啶-2(1H)-酮 MS-ESI (m/z): 405 [M + 1] ⁺ 205

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)-1,6-萘啶-2(1H)-酮 MS-ESI (m/z): 405 [M + 1] ⁺ 206

3-乙基-7-((4-(7-氧代-6,7-二氫-5H-吡咯並[3,4-b]吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1H)-酮 MS-ESI (m/z): 405 [M + 1] ⁺ 207

N-乙氧基-1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 434 [M + 1] ⁺ 208

1'-((7-(羥基甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 209

1'-((7-(氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 408 [M + 1] ⁺ 210

1'-((7-(甲氧基甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 420 [M + 1] ⁺ 211

N-(甲基-d3)-1'-((7-甲基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 393 [M + 1] ⁺ 212

N-(甲基-d3)-5-(1-((7-甲基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)吡啶醯胺 MS-ESI (m/z): 395 [M + 1] ⁺ 213

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-(甲基-d3)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 407 [M + 1] ⁺ 214

5-(1-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌啶-4-基)-N-(甲基-d3)吡啶醯胺 MS-ESI (m/z): 409 [M + 1] ⁺ 215

1'-((7-(氟甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-N-(甲基-d3)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 411 [M + 1] ⁺ 216

5-(4-((3-乙基-2-氧代-1,2-二氫-1,6-萘啶-7-基)甲基)哌嗪-1-基)-N-(甲基-d3)吡啶醯胺 MS-ESI (m/z): 410 [M + 1] ⁺ 217

5-(4-((7-(甲氧基甲基)-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 423 [M + 1] ⁺ 218

5-(4-((7-甲氧基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 409 [M + 1] ⁺ 219

5-(4-((7-乙氧基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 423 [M + 1] ⁺ 220

( S)-5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 221

( R)-5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 222

5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)環丙基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 223

3-乙基-7-((4-(6-(5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 224

7-((4-(6-(4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 417 [M + 1] ⁺ 225

3-乙基-7-((4-(6-(5-甲基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 431 [M + 1] ⁺ 226

3-乙基-7-((4-(6-(5-乙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 227

3-乙基-7-((4-(6-(5-甲氧基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 228

7-((4-(6-(5-乙氧基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 461 [M + 1] ⁺ 229

7-((4-(6-(5-氨基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 432 [M + 1] ⁺ 230

7-((4-(6-(5-(二甲基氨基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 460 [M + 1] ⁺ 231

7-((4-(6-(5-(二乙基氨基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 488 [M + 1] ⁺ 232

1'-((7-甲氧基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 406 [M + 1] ⁺ 233

1'-((7-乙氧基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 420 [M + 1] ⁺ 234

( S)-1'-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 235

( R)-1'-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 236

1'-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)環丙基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 430 [M + 1] ⁺ 237

3-乙基-7-((6-(5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 430 [M + 1] ⁺ 238

7-((6-(4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 414 [M + 1] ⁺ 239

3-乙基-7-((6-(5-甲基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 428 [M + 1] ⁺ 240

3-乙基-7-((6-(5-乙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 442 [M + 1] ⁺ 241

3-乙基-7-((6-(5-甲氧基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 242

7-((6-(5-乙氧基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 458 [M + 1] ⁺ 243

7-((6-(5-氨基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 429 [M + 1] ⁺ 244

7-((6-(5-(二甲基氨基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 457 [M + 1] ⁺ 245

7-((6-(5-(二乙基氨基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 485 [M + 1] ⁺ 246

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-(甲基-d ₃ )吡啶甲醯胺 MS-ESI (m/z): 410 [M + 1] ⁺ 247

3-乙基-7-((4-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 248

7-((4-(6-(5-環丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 457 [M + 1] ⁺ 249

3-乙基-7-((4-(6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 485 [M + 1] ⁺ 250

7-((4-(6-(5-(二氟甲基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 467 [M + 1] ⁺ 251

7-((4-(6-(5-(1,1-二氟乙基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 481 [M + 1] ⁺ 252

3-乙基-7-((6-(5-異丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 456 [M + 1] ⁺ 253

7-((6-(5-環丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 454 [M + 1] ⁺ 254

3-乙基-7-((6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 482 [M + 1] ⁺ 255

7-((6-(5-(二氟甲基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 464 [M + 1] ⁺ 256

7-((6-(5-(1,1-二氟乙基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 478 [M + 1] ⁺ 257

3-乙基-7-((4-(6-(5-甲基-1,3,4-噁二唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 432 [M + 1] ⁺ 258

5-(4-(2-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)丙烷-2-基)哌嗪-1-基)- N-甲基吡啶甲醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 259

1'-(2-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)丙烷-2-基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 432 [M + 1] ⁺ 260

5-(4-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-羰基)哌嗪-1-基)- N-甲基吡啶甲醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 261

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 390 [M + 1] ⁺ 262

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)乙醯胺 MS-ESI (m/z): 407 [M + 1] ⁺ 263

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)丙醯胺 MS-ESI (m/z): 421 [M + 1] ⁺ 264

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)異丁醯胺 MS-ESI (m/z): 435 [M + 1] ⁺ 265

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)環丙醯胺 MS-ESI (m/z): 433 [M + 1] ⁺ 266

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-2,2,2-三氟乙醯胺 MS-ESI (m/z): 461 [M + 1] ⁺ 267

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)新戊醯胺 MS-ESI (m/z): 449 [M + 1] ⁺ 268

7-((4-(6-(5-(叔丁基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 473 [M + 1] ⁺ 269

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-2,2-二氟丙醯胺 MS-ESI (m/z): 457 [M + 1] ⁺ 270

N-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-2,2-二氟乙醯胺 MS-ESI (m/z): 443 [M + 1] ⁺ 271

甲基 (5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 423 [M + 1] ⁺ 272

乙基 (5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 437 [M + 1] ⁺ 273

環丙基 (5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 449 [M + 1] ⁺ 274

異丙基 (5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 451 [M + 1] ⁺ 275

1-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-3-甲基脲 MS-ESI (m/z): 422 [M + 1] ⁺ 276

1-乙基-3-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)脲 MS-ESI (m/z): 436 [M + 1] ⁺ 277

1-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-3-異丙基脲 MS-ESI (m/z): 450 [M + 1] ⁺ 278

1-( 叔丁基)-3-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)脲 MS-ESI (m/z): 464 [M + 1] ⁺ 279

1-(1,1-二氟乙基)-3-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)脲 MS-ESI (m/z): 472 [M + 1] ⁺ 280

1-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-3-(三氟甲基)脲 MS-ESI (m/z): 476 [M + 1] ⁺ 281

3-乙基-7-((4-(6-(3-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 282

3-乙基-7-((4-(6-(3-乙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 461 [M + 1] ⁺ 283

3-乙基-7-((4-(6-(5-氧代-3-(三氟甲基)-2,5-二氫-1 H-1,2,4-三唑-1-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 501 [M + 1] ⁺ 284

3-乙基-7-((4-(6-(3-異丙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 475 [M + 1] ⁺ 285

3-乙基-7-((4-(6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 286

3-乙基-7-((4-(6-(1-乙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 461 [M + 1] ⁺ 287

甲基 (5-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-1,2,4-三唑-3-基)氨基甲酸酯 MS-ESI (m/z): 490 [M + 1] ⁺ 288

N-(5-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-1,2,4-三唑-3-基)乙醯胺 MS-ESI (m/z): 474 [M + 1] ⁺ 289

3-乙基-7-((4-(6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 448 [M + 1] ⁺ 290

3-乙基-7-((4-(6-(5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 430 [M + 1] ⁺ 291

2-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-甲腈 MS-ESI (m/z): 455 [M + 1] ⁺ 292

3-乙基-7-((4-(6-(5-乙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 462 [M + 1] ⁺ 293

3-乙基-7-((4-(6-(5-乙基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 294

5-乙基-2-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-甲腈 MS-ESI (m/z): 469 [M + 1] ⁺ 295

3-乙基-7-((4-(6-(5-(甲基氨基)-1,2,4-噁二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 296

3-乙基-7-((4-(6-(5-(乙基氨基)-1,2,4-噁二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 461 [M + 1] ⁺ 297

7-((4-(6-(5-(環丙基氨基)-1,2,4-噁二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 473 [M + 1] ⁺ 298

3-乙基-7-((4-(6-(5-(異丙基氨基)-1,2,4-噁二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 475 [M + 1] ⁺ 299

3-乙基-7-((4-(6-(5-(甲基氨基)-1,2,4-噻二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 463 [M + 1] ⁺ 300

3-乙基-7-((4-(6-(5-(乙基氨基)-1,2,4-噻二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 477 [M + 1] ⁺ 301

7-((4-(6-(5-(環丙基氨基)-1,2,4-噻二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 489 [M + 1] ⁺ 302

3-乙基-7-((4-(6-(5-(異丙基氨基)-1,2,4-噻二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 491 [M + 1] ⁺ 303

N-(3-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1,2,4-噁二唑-5-基)甲基磺醯胺 MS-ESI (m/z): 511 [M + 1] ⁺ 304

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-氨基磺醯基吡啶甲醯胺 MS-ESI (m/z): 472 [M + 1] ⁺ 305

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-( N-甲基氨基磺醯基)吡啶甲醯胺 MS-ESI (m/z): 486 [M + 1] ⁺ 306

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-( N-乙基氨基磺醯基)吡啶甲醯胺 MS-ESI (m/z): 500 [M + 1] ⁺ 307

N-( N, N-二甲基氨基磺醯基)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶甲醯胺 MS-ESI (m/z): 500 [M + 1] ⁺ 308

N-( N, N-二乙基氨基磺醯基)-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶甲醯胺 MS-ESI (m/z): 528 [M + 1] ⁺ 309

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-(甲基磺醯基)吡啶甲醯胺 MS-ESI (m/z): 471 [M + 1] ⁺ 310

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-(S-甲基磺醯亞胺基)吡啶甲醯胺 MS-ESI (m/z): 470 [M + 1] ⁺ 311

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)乙醯胺 MS-ESI (m/z): 404 [M + 1] ⁺ 312

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)丙醯胺 MS-ESI (m/z): 418 [M + 1] ⁺ 313

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)異丁醯胺 MS-ESI (m/z): 432 [M + 1] ⁺ 314

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)環丙醯胺 MS-ESI (m/z): 430 [M + 1] ⁺ 315

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-2,2,2-三氟乙醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 316

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)新戊醯胺 MS-ESI (m/z): 446 [M + 1] ⁺ 317

7-((6-(5-(叔丁基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 470 [M + 1] ⁺ 318

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-2,2-二氟丙醯胺 MS-ESI (m/z): 454 [M + 1] ⁺ 319

N-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-2,2-二氟乙醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 320

甲基 (1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 420 [M + 1] ⁺ 321

乙基 (1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 434 [M + 1] ⁺ 322

環丙基 (1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 446 [M + 1] ⁺ 323

異丙基 (1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 448 [M + 1] ⁺ 324

1-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-3-甲基脲 MS-ESI (m/z): 419 [M + 1] ⁺ 325

1-乙基-3-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)脲 MS-ESI (m/z): 433 [M + 1] ⁺ 326

1-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-3-異丙基脲 MS-ESI (m/z): 447 [M + 1] ⁺ 327

1-( 叔丁基)-3-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)脲 MS-ESI (m/z): 461 [M + 1] ⁺ 328

1-(1,1-二氟乙基)-3-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)脲 MS-ESI (m/z): 469 [M + 1] ⁺ 329

1-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-3-(三氟甲基)脲 MS-ESI (m/z): 473 [M + 1] ⁺ 330

3-乙基-7-((6-(3-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 331

3-乙基-7-((6-(3-乙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 458 [M + 1] ⁺ 332

3-乙基-7-((6-(5-氧代-3-(三氟甲基)-2,5-二氫-1 H-1,2,4-三唑-1-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2'H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 498 [M + 1] ⁺ 333

3-乙基-7-((6-(3-異丙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-1-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 472 [M + 1] ⁺ 334

3-乙基-7-((6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 335

3-乙基-7-((6-(1-乙基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 458 [M + 1] ⁺ 336

甲基 (5-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-1,2,4-三唑-3-基)氨基甲酸酯 MS-ESI (m/z): 487 [M + 1] ⁺ 337

N-(5-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-1,2,4-三唑-3-基)乙醯胺 MS-ESI (m/z): 471 [M + 1] ⁺ 338

3-乙基-7-((6-(4-氟-5-甲基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 445 [M + 1] ⁺ 339

3-乙基-7-((6-(5-甲基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2'H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 427 [M + 1] ⁺ 340

2-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-甲基-1 H-咪唑-4-甲腈 MS-ESI (m/z): 452 [M + 1] ⁺ 341

3-乙基-7-((6-(5-乙基-4-氟-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 342

3-乙基-7-((6-(5-乙基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 441 [M + 1] ⁺ 343

5-乙基-2-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-咪唑-4-甲腈 MS-ESI (m/z): 466 [M + 1] ⁺ 344

3-乙基-7-((6-(5-(甲基氨基)-1,2,4-噁二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 345

3-乙基-7-((6-(5-(乙基氨基)-1,2,4-噁二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 458 [M + 1] ⁺ 346

7-((6-(5-(環丙基氨基)-1,2,4-噁二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 470 [M + 1] ⁺ 347

3-乙基-7-((6-(5-(異丙基氨基)-1,2,4-噁二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 472 [M + 1] ⁺ 348

3-乙基-7-((6-(5-(甲基氨基)-1,2,4-噻二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 460 [M + 1] ⁺ 349

3-乙基-7-((6-(5-(乙基氨基)-1,2,4-噻二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 474 [M + 1] ⁺ 350

7-((6-(5-(環丙基氨基)-1,2,4-噻二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 486 [M + 1] ⁺ 351

3-乙基-7-((6-(5-(異丙基氨基)-1,2,4-噻二唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 488 [M + 1] ⁺ 352

N-(3-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1,2,4-噁二唑-5-基)甲基磺醯胺 MS-ESI (m/z): 508 [M + 1] ⁺ 353

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-氨基磺醯基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 469 [M + 1] ⁺ 354

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-( N-甲基氨基磺醯基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 483 [M + 1] ⁺ 355

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-( N-乙基氨基磺醯基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 497 [M + 1] ⁺ 356

N-( N, N-二甲基氨基磺醯基)-1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 497 [M + 1] ⁺ 357

N-( N, N-二乙基氨基磺醯基)-1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 525 [M + 1] ⁺ 358

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-(甲基磺醯基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 468 [M + 1] ⁺ 359

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-( S-甲基磺醯亞胺基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 467 [M + 1] ⁺ 360

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-磺醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 361

N-乙基-1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-磺醯胺 MS-ESI (m/z): 454 [M + 1] ⁺ 362

1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)- N-異丙基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-磺醯胺 MS-ESI (m/z): 468 [M + 1] ⁺ 363

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-甲基吡啶-2-磺醯胺 MS-ESI (m/z): 443 [M + 1] ⁺ 364

N-乙基-5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-磺醯胺 MS-ESI (m/z): 457 [M + 1] ⁺ 365

5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)- N-異丙基吡啶-2-磺醯胺 MS-ESI (m/z): 471 [M + 1] ⁺ 366

( S)-3-乙基-7-(1-(4-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 473 [M + 1] ⁺ 367

( S)-3-乙基-7-(1-(4-(6-(5-乙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 368

( S)-3-乙基-7-(1-(4-(6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 499 [M + 1] ⁺ 369

( R)-3-乙基-7-(1-(4-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 473 [M + 1] ⁺ 370

( R)-3-乙基-7-(1-(4-(6-(5-乙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 459 [M + 1] ⁺ 371

( R)-3-乙基-7-(1-(4-(6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 499 [M + 1] ⁺ 372

( S)-3-乙基-7-(1-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 470 [M + 1] ⁺ 373

( S)-3-乙基-7-(1-(6-(5-乙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 456 [M + 1] ⁺ 374

( S)-3-乙基-7-(1-(6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 496 [M + 1] ⁺ 375

( R)-3-乙基-7-(1-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 470 [M + 1] ⁺ 376

( R)-3-乙基-7-(1-(6-(5-乙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 456 [M + 1] ⁺ 377

( R)-3-乙基-7-(1-(6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 496 [M + 1] ⁺ 378

1'-((2-乙基-5-氟-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 379

2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 426 [M + 1] ⁺ 380

5-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 426 [M + 1] ⁺ 381

2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲氧基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 382

2-氟-1'-((5-氟-2-甲氧基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 383

2-氟-1'-((5-氟-2-異丙基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 454 [M + 1] ⁺ 384

1'-((2-(二氟甲基)-5-氟-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 462 [M + 1] ⁺ 385

2-氟-1'-((5-氟-3-氧代-2-(三氟甲基)-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 480 [M + 1] ⁺ 386

2-氟-1'-((5-氟-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 412 [M + 1] ⁺ 387

1'-((2-環丙基-5-氟-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 452 [M + 1] ⁺ 388

( S)-2-氟-1'-((5-氟-2-(1-氟乙基)-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 389

( R)-2-氟-1'-((5-氟-2-(1-氟乙基)-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 390

1'-((2-(1,1-二氟乙基)-5-氟-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 476 [M + 1] ⁺ 391

1'-((2,5-二甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 392

1'-((5-氯-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-2-氟- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 393

1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 408 [M + 1] ⁺ 394

2-氯-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 442 [M + 1] ⁺ 395

1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N,2-二甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 422 [M + 1] ⁺ 396

2-(二氟甲基)-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 458 [M + 1] ⁺ 397

8-氟-7-((4-(2-氟-6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 470 [M + 1] ⁺ 398

2-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 477 [M + 1] ⁺ 399

8-氟-7-((4-(2-氟-6-(5-甲基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 453 [M + 1] ⁺ 400

8-氟-7-((4-(2-氟-6-(4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 439 [M + 1] ⁺ 401

7-((4-(6-(5-乙基-4 H-1,2,4-三唑-3-基)-2-氟吡啶-3-基)哌嗪-1-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 467 [M + 1] ⁺ 402

8-氟-7-((4-(2-氟-6-(5-異丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 481 [M + 1] ⁺ 403

7-((4-(6-(5-環丙基-4 H-1,2,4-三唑-3-基)-2-氟吡啶-3-基)哌嗪-1-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 479 [M + 1] ⁺ 404

8-氟-7-((4-(2-氟-6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 507 [M + 1] ⁺ 405

8-氟-7-((4-(2-氟-6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 469 [M + 1] ⁺ 406

5-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-1,3,4-噁二唑-2(3 H)-酮 MS-ESI (m/z): 456 [M + 1] ⁺ 407

3-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-1,2,4-噁二唑-5(4 H)-酮 MS-ESI (m/z): 456 [M + 1] ⁺ 408

甲基 (6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 445 [M + 1] ⁺ 409

乙基 (6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)氨基甲酸酯 MS-ESI (m/z): 459 [M + 1] ⁺ 410

N-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)甲基磺醯胺 MS-ESI (m/z): 465 [M + 1] ⁺ 411

6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)- N-(甲基磺醯基)吡啶醯胺 MS-ESI (m/z): 493 [M + 1] ⁺ 412

( R)-5-(3-(氰基甲基)-4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)-6-氟- N-甲基吡啶醯胺 MS-ESI (m/z): 468 [M + 1] ⁺ 413

( S)-6-氟-5-(4-(1-(5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)乙基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 443 [M + 1] ⁺ 414

( R)-6-氟-5-(4-(1-(5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)乙基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 443 [M + 1] ⁺ 415

8-氟-7-((2-氟-6-(4-氟-5-甲基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 467 [M + 1] ⁺ 416

2-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 474 [M + 1] ⁺ 417

8-氟-7-((2-氟-6-(5-甲基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 450 [M + 1] ⁺ 418

8-氟-7-((2-氟-6-(4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 436 [M + 1] ⁺ 419

7-((6-(5-乙基-4 H-1,2,4-三唑-3-基)-2-氟-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 464 [M + 1] ⁺ 420

8-氟-7-((2-氟-6-(5-異丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 478 [M + 1] ⁺ 421

7-((6-(5-環丙基-4 H-1,2,4-三唑-3-基)-2-氟-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 476 [M + 1] ⁺ 422

8-氟-7-((2-氟-6-(5-(三氟甲基)-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 504 [M + 1] ⁺ 423

8-氟-7-((2-氟-6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 466 [M + 1] ⁺ 424

5-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1,3,4-噁二唑-2(3 H)-酮 MS-ESI (m/z): 453 [M + 1] ⁺ 425

3-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1,2,4-噁二唑-5(4 H)-酮 MS-ESI (m/z): 453 [M + 1] ⁺ 426

甲基 (2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 442 [M + 1] ⁺ 427

乙基 (2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)氨基甲酸酯 MS-ESI (m/z): 456 [M + 1] ⁺ 428

N-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)甲基磺醯胺 MS-ESI (m/z): 462 [M + 1] ⁺ 429

2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-(甲基磺醯基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 490 [M + 1] ⁺ 430

( S)-2'-(氰基甲基)-2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 465 [M + 1] ⁺ 431

( S)-2-氟-1'-(1-(5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)乙基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 432

( R)-2-氟-1'-(1-(5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)乙基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 440 [M + 1] ⁺ 433

3,6-二氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)- N-甲基吡啶醯胺 MS-ESI (m/z): 447 [M + 1] ⁺ 434

2,5-二氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 444 [M + 1] ⁺ 435

7-((4-(6-(5-氨基-1,2,4-噁二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 433 [M + 1] ⁺ 436

7-((4-(6-(5-氨基-1,2,4-噻二唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 449 [M + 1] ⁺ 437

5-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1,3,4-噁二唑-2(3 H)-酮 MS-ESI (m/z): 434 [M + 1] ⁺ 438

3-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1,2,4-噁二唑-5(4 H)-酮 MS-ESI (m/z): 434 [M + 1] ⁺ 439

1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-甲基-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 408 [M + 1] ⁺ 440

8-氟-7-((6-(5-異丙基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 460 [M + 1] ⁺ 441

8-氟-3-甲基-7-((6-(5-甲基-4 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 432 [M + 1] ⁺ 442

8-氟-3-甲基-7-((6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 448 [M + 1] ⁺ 443

8-氟-7-((6-(4-氟-5-甲基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 449 [M + 1] ⁺ 444

2-(1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 456 [M + 1] ⁺ 445

8-氟-7-((4-(6-(5-異丙基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 463 [M + 1] ⁺ 446

8-氟-3-甲基-7-((4-(6-(5-甲基-4 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 435 [M + 1] ⁺ 447

8-氟-3-甲基-7-((4-(6-(1-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 451 [M + 1] ⁺ 448

8-氟-7-((4-(6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 452 [M + 1] ⁺ 449

2-(5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 459 [M + 1] ⁺ 450

2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)- N-(甲基- d ₃ )-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-甲醯胺 MS-ESI (m/z): 429 [M + 1] ⁺ 451

2-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 531 [M + 1] ⁺ 452

8-氟-7-((4-(2-氟-6-(4-氟-5-(三氟甲基)-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 524 [M + 1] ⁺ 453

8-氟-7-((4-(2-氟-6-(5-(三氟甲基)-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 506 [M + 1] ⁺ 454

2-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 528 [M + 1] ⁺ 455

8-氟-7-((2-氟-6-(4-氟-5-(三氟甲基)-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 521 [M + 1] ⁺ 456

8-氟-7-((2-氟-6-(5-(三氟甲基)-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 503 [M + 1] ⁺ 457

3-乙基-7-((4-(6-(5-(三氟甲基)-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 484 [M + 1] ⁺ 458

3-乙基-7-((4-(6-(4-氟-5-(三氟甲基)-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 502 [M + 1] ⁺ 459

2-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 509 [M + 1] ⁺ 460

3-乙基-7-((6-(5-(三氟甲基)-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 481 [M + 1] ⁺ 461

3-乙基-7-((6-(4-氟-5-(三氟甲基)-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 499 [M + 1] ⁺ 462

2-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 506 [M + 1] ⁺ 463

8-氟-7-((4-(2-氟-6-(5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 455 [M + 1] ⁺ 464

8-氟-7-((2-氟-6-(5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 452 [M + 1] ⁺ 465

7-((4-(6-(5-乙基-4-氟-1 H-咪唑-2-基)-2-氟吡啶-3-基)哌嗪-1-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 484 [M + 1] ⁺ 466

5-乙基-2-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 491 [M + 1] ⁺ 467

7-((6-(5-乙基-4-氟-1 H-咪唑-2-基)-2-氟-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 481 [M + 1] ⁺ 468

5-乙基-2-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 488 [M + 1] ⁺ 469

3-乙基-7-((6-(4-氟-5-異丙基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 473 [M + 1] ⁺ 470

2-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 480 [M + 1] ⁺ 471

8-氟-7-((2-氟-6-(4-氟-5-異丙基-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 495 [M + 1] ⁺ 472

2-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 502 [M + 1] ⁺ 473

7-((6-(5-環丙基-4-氟-1 H-咪唑-2-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 471 [M + 1] ⁺ 474

5-環丙基-2-(1'-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 478 [M + 1] ⁺ 475

7-((6-(5-環丙基-4-氟-1 H-咪唑-2-基)-2-氟-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 493 [M + 1] ⁺ 476

5-環丙基-2-(2-氟-1'-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)-1',2',3',6'-四氫-[3,4'-聯吡啶]-6-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 500 [M + 1] ⁺ 477

3-乙基-7-((4-(6-(4-氟-5-異丙基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 476 [M + 1] ⁺ 478

2-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 483 [M + 1] ⁺ 479

8-氟-7-((4-(2-氟-6-(4-氟-5-異丙基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 498 [M + 1] ⁺ 480

2-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 505 [M + 1] ⁺ 481

7-((4-(6-(5-環丙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)甲基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 474 [M + 1] ⁺ 482

5-環丙基-2-(5-(4-((7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 481 [M + 1] ⁺ 483

7-((4-(6-(5-環丙基-4-氟-1 H-咪唑-2-基)-2-氟吡啶-3-基)哌嗪-1-基)甲基)-8-氟-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 496 [M + 1] ⁺ 484

5-環丙基-2-(6-氟-5-(4-((5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)甲基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 503 [M + 1] ⁺ 485

( S)-3-乙基-7-(1-(4-(6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 462 [M + 1] ⁺ 486

( R)-3-乙基-7-(1-(4-(6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 462 [M + 1] ⁺ 487

( S)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 469 [M + 1] ⁺ 488

( R)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 469 [M + 1] ⁺ 489

( S)-3-乙基-7-(1-(4-(6-(4-氟-5-(三氟甲基)-1H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 516 [M + 1] ⁺ 490

( R)-3-乙基-7-(1-(4-(6-(4-氟-5-(三氟甲基)-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 516 [M + 1] ⁺ 491

( S)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 523 [M + 1] ⁺ 492

( R)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-(三氟甲基)-1 H-咪唑-4-腈 MS-ESI (m/z): 523 [M + 1] ⁺ 493

( S)-3-乙基-7-(1-(4-(6-(5-乙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 476 [M + 1] ⁺ 494

( R)-3-乙基-7-(1-(4-(6-(5-乙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 476 [M + 1] ⁺ 495

( S)-5-乙基-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 483 [M + 1] ⁺ 496

( R)-5-乙基-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 483 [M + 1] ⁺ 497

( S)-3-乙基-7-(1-(4-(6-(4-氟-5-異丙基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 490 [M + 1] ⁺ 498

( R)-3-乙基-7-(1-(4-(6-(4-氟-5-異丙基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 490 [M + 1] ⁺ 499

( S)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 497 [M + 1] ⁺ 500

( R)-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-5-異丙基-1 H-咪唑-4-腈 MS-ESI (m/z): 497 [M + 1] ⁺ 501

( S)-7-(1-(4-(6-(5-環丙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 488 [M + 1] ⁺ 502

( R)-7-(1-(4-(6-(5-環丙基-4-氟-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-3-乙基-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 488 [M + 1] ⁺ 503

( S)-5-環丙基-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 495 [M + 1] ⁺ 504

( R)-5-環丙基-2-(5-(4-(1-(7-乙基-6-氧代-5,6-二氫-1,5-萘啶-3-基)乙基)哌嗪-1-基)吡啶-2-基)-1 H-咪唑-4-腈 MS-ESI (m/z): 495 [M + 1] ⁺ 505

( S)-8-氟-7-(1-(4-(2-氟-6-(4-氟-5-甲基-1 H-咪唑-2-基)吡啶-3-基)哌嗪-1-基)乙基)-3-甲基喹喔啉-2(1 H)-酮 MS-ESI (m/z): 484 [M + 1] ⁺ 506

( R)-2-(6-氟-5-(4-(1-(5-氟-2-甲基-3-氧代-3,4-二氫喹喔啉-6-基)乙基)哌嗪-1-基)吡啶-2-基)-5-甲基-1 H-咪唑-4-腈 MS-ESI (m/z): 491 [M + 1] ⁺ 507

3-乙基-7-((4-(6-(2-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 508

3-乙基-7-((4-(6-(4-甲基-5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 447 [M + 1] ⁺ 509

3-乙基-8-氟-7-((4-(2-氟-6-(2-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 483 [M + 1] ⁺ 510

3-乙基-8-氟-7-((4-(2-氟-6-(4-甲基-5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)吡啶-3-基)哌嗪-1-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 483 [M + 1] ⁺ 511

3-乙基-7-((6-(2-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 512

3-乙基-7-((6-(4-甲基-5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)-1,5-萘啶-2(1 H)-酮 MS-ESI (m/z): 444 [M + 1] ⁺ 513

3-乙基-8-氟-7-((2-氟-6-(2-甲基-5-氧代-2,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 480 [M + 1] ⁺ 514

3-乙基-8-氟-7-((2-氟-6-(4-甲基-5-氧代-4,5-二氫-1 H-1,2,4-三唑-3-基)-3',6'-二氫-[3,4'-聯吡啶]-1'(2' H)-基)甲基)喹喔啉-2(1 H)-酮 MS-ESI (m/z): 480 [M + 1] ⁺ Table 1 Example structure name data 4

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl Pyridinamide MS-ESI (m/z): 406 [M + 1] ⁺ 5

5-(5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)hexahydropyrrolo[3,4-c]pyrrole -2(1H)-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 6

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)amino)-N -Methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 7

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)azetidin-3-yl)amino )-N-Methylpyridinamide MS-ESI (m/z): 393 [M + 1] ⁺ 8

5-(7-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,7-diazaspiro[3.5] Nonan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 9

5-(6-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,6-diazabicyclo[3.1. 1] Heptane-3-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 10

5-((1R,4R)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.1]heptan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 11

5-((1S,4S)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.1]heptan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 12

5-(8-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,8-diazabicyclo[3.2. 1] Octane-3-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 13

(R)-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-methylpiperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 14

(S)-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-methylpiperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 15

5-(7-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4,7-diazaspiro[2.5] Octane-4-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 16

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,2-dimethylpiperazine-1 -yl)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 17

5-((2S,6R)-4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,6-di Methylpiperazin-1-yl)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 18

5-((2R,6R)-4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,6-di Methylpiperazin-1-yl)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 19

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,8-diazabicyclo[3.2. 1] Octane-8-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 20

5-((1R,4R)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.2]octane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ twenty one

5-((1S,4S)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.2]octane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ twenty two

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,6-diazabicyclo[3.1. 1] Heptane-6-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ twenty three

5-((1R,4R)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.1]heptan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ twenty four

5-((1S,4S)-5-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,5-di Azabicyclo[2.2.1]heptan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 25

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-methylpiperidin-4-yl )amino)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 26

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-fluoropiperidin-4-yl) Amino)-N-Methylpyridinamide MS-ESI (m/z): 439 [M + 1] ⁺ 27

5-((3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0] Hexan-6-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 28

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-hydroxypiperidin-4-yl) Amino)-N-Methylpyridinamide MS-ESI (m/z): 437 [M + 1] ⁺ 29

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-methoxypiperidine-4- Base) amino) -N-methylpyridinamide MS-ESI (m/z): 451 [M + 1] ⁺ 30

5-((4-ethoxy-1-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine-4- Base) amino) -N-methylpyridinamide MS-ESI (m/z): 465 [M + 1] ⁺ 31

5-((4-cyano-1-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl )amino)-N-methylpyridinamide MS-ESI (m/z): 446 [M + 1] ⁺ 32

1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-((6-(methylcarbamoyl) Pyridin-3-yl)amino)piperidin-4-yl acetate MS-ESI (m/z): 479 [M + 1] ⁺ 33

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-(hydroxymethyl)piperidine- 4-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 451 [M + 1] ⁺ 34

5-(9-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,9-diazaspiro[5.5] Undecyl-3-yl)-N-methylpyridinamide MS-ESI (m/z): 475 [M + 1] ⁺ 35

5-(8-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,8-diazaspiro[4.5] Decane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 36

5-(2-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,8-diazaspiro[4.5] Decane-8-yl)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 37

5-(2-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,7-diazaspiro[3.5] Nonan-7-yl)-N-methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 38

5-(2-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,6-diazaspiro[3.4] Octane-6-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 39

5-(6-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,6-diazaspiro[3.4] Octane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 40

5-(6-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,6-diazaspiro[3.3] Heptane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 41

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)pyrrolidin-3-yl)amino)-N -Methylpyridinamide MS-ESI (m/z): 407 [M + 1] ⁺ 42

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)pyrrolidin-3-yl)oxy)-N -Methylpyridinamide MS-ESI (m/z): 408 [M + 1] ⁺ 43

5-((1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)azetidin-3-yl)oxy )-N-Methylpyridinamide MS-ESI (m/z): 394 [M + 1] ⁺ 44

1'-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-N-methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 404 [M+1]+ 45

1'-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-N-methyl-1',2',3',6'- Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 404 [M+1]+ 46

5-(6-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-3,6-diazabicyclo[3.1. 1] Heptane-3-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 47

5-(5-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)hexahydropyrrolo[3,4-c]pyrrole -2(1H)-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 48

5-(7-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-2,7-diazaspiro[3.5] Nonan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 49

5-(6-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-2,6-diazaspiro[3.3] Heptane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 50

5-((7-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-7-azaspiro[3.5]nonane -2-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 51

5-(1-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)piperidin-4-yl)-N-methyl Pyridinamide MS-ESI (m/z): 406 [M + 1] ⁺ 52

5-((1-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)piperidin-4-yl)amino)-N -Methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 53

5-((1-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-4-methylpiperidin-4-yl )amino)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 54

5-((1-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)azetidin-3-yl)oxy )-N-Methylpyridinamide MS-ESI (m/z): 394 [M + 1] ⁺ 55

5-(3-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-3,8-diazabicyclo[3.2. 1] Octane-8-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 56

5-(3-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-3,6-diazabicyclo[3.1. 1] Heptane-6-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 57

5-(9-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-3,9-diazaspiro[5.5] Undecyl-3-yl)-N-methylpyridinamide MS-ESI (m/z): 475 [M + 1] ⁺ 58

5-(7-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-2,7-diazaspiro[3.5] Nonan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 59

5-(6-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-2,6-diazaspiro[3.3] Heptane-2-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 60

5-((7-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-7-azaspiro[3.5]nonane -2-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 61

5-(1-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)piperidin-4-yl)-N-methyl Pyridinamide MS-ESI (m/z): 406 [M + 1] ⁺ 62

5-((1-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)piperidin-4-yl)amino)-N -Methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 63

5-((1-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)-4-methylpiperidin-4-yl )amino)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 64

5-((1-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)azetidin-3-yl)oxy )-N-Methylpyridinamide MS-ESI (m/z): 394 [M + 1] ⁺ 65

5-(3-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-3,8-diazabicyclo[3.2.1]octane -8-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 66

5-(3-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-3,6-diazabicyclo[3.1.1]heptane -6-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 67

5-(9-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-3,9-diazaspiro[5.5]undecane- 3-yl)-N-methylpyridinamide MS-ESI (m/z): 475 [M + 1] ⁺ 68

5-(7-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2,7-diazaspiro[3.5]nonane-2 -yl)-N-methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 69

5-(6-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2,6-diazaspiro[3.3]heptane-2 -yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 70

5-((7-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-7-azaspiro[3.5]nonan-2-yl )amino)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 71

5-(1-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperidin-4-yl)-N-methylpyridinamide MS-ESI (m/z): 406 [M + 1] ⁺ 72

5-((1-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperidin-4-yl)amino)-N-methylpyridine Amide MS-ESI (m/z): 421 [M + 1] ⁺ 73

5-((1-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-4-methylpiperidin-4-yl)amino)- N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 74

5-((1-((2-Ethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)azetidin-3-yl)oxy)-N- Pyridinamide MS-ESI (m/z): 394 [M + 1] ⁺ 75

3-Ethyl-7-((4-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazine-1 -yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 76

3-Ethyl-7-((4-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazine-1 -yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 77

3-Ethyl-7-((4-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazine-1 -yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 78

3-Ethyl-7-((8-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3,8 -Diazabicyclo[3.2.1]octane-3-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 445 [M + 1] ⁺ 79

3-ethyl-7-((2-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-2,7 -Diazaspiro[3.5]nonan-7-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 459 [M + 1] ⁺ 80

3-ethyl-7-((4-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)amino)piper Pyridin-1-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 433 [M + 1] ⁺ 81

3-Ethyl-7-((3-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)oxy)pyrrole Alk-1-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 82

3-Ethyl-7-((8-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3,8 -Diazabicyclo[3.2.1]octane-3-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 445 [M + 1] ⁺ 83

3-ethyl-7-((2-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-2,7 -Diazaspiro[3.5]nonan-7-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 459 [M + 1] ⁺ 84

3-ethyl-7-((4-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)amino)piper Pyridin-1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 433 [M + 1] ⁺ 85

3-Ethyl-7-((3-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)oxy)pyrrole Alk-1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 86

3-Ethyl-7-((8-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3,8 -Diazabicyclo[3.2.1]octane-3-yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 445 [M + 1] ⁺ 87

3-ethyl-7-((2-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-2,7 -Diazaspiro[3.5]nonan-7-yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 459 [M + 1] ⁺ 88

3-ethyl-7-((4-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)amino)piper Pyridin-1-yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 433 [M + 1] ⁺ 89

3-Ethyl-7-((3-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)oxy)pyrrole Alk-1-yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 90

3-Ethyl-7-((8-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3,8 -Diazabicyclo[3.2.1]octane-3-yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 445 [M + 1] ⁺ 91

3-ethyl-7-((2-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-2,7 -Diazaspiro[3.5]nonan-7-yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 459 [M + 1] ⁺ 92

3-ethyl-7-((4-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)amino)piper Pyridin-1-yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 433 [M + 1] ⁺ 93

3-Ethyl-7-((3-((6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)oxy)pyrrole Alk-1-yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 94

3-Ethyl-7-((8-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)-3,8 -Diazabicyclo[3.2.1]octane-3-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 445 [M + 1] ⁺ 95

3-Ethyl-7-((2-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)-2,7 -Diazaspiro[3.5]nonan-7-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 459 [M + 1] ⁺ 96

3-ethyl-7-((4-((6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)amino)piper Pyridin-1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 433 [M + 1] ⁺ 97

3-Ethyl-7-((3-((6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)oxy)pyrrole Alk-1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 98

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)piperazine-1 -yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 99

5-(3-((6-Ethyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)-3,8-diazabicyclo[3.2. 1] Octane-8-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 100

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)piperazine-1 -yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 101

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-2-yl)piperazine-1 -yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 102

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-2-yl)piperazine- 1-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 103

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-2-yl)piperazine- 1-yl)methyl)-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 104

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-2-yl)piperazine- 1-yl)methyl)quinoxalin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 105

3-Ethyl-7-((4-(6-methyl-5-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-2-yl)piperazine- 1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 420 [M + 1] ⁺ 106

3-Ethyl-7-((4-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazine-1 -yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 419 [M + 1] ⁺ 107

3-Ethyl-7-((4-(2-methyl-1-oxoisoindoline-5-yl)piperazin-1-yl)methyl)-1,8-naphthyridine-2( 1H)-ketone MS-ESI (m/z): 418 [M + 1] ⁺ 108

3-Ethyl-7-((4-(2-methyl-1-oxoisoindoline-5-yl)piperazin-1-yl)methyl)-1,5-naphthyridine-2( 1H)-ketone MS-ESI (m/z): 418 [M + 1] ⁺ 109

5-(4-((6-cyclopropyl-7-oxo-7,8-dihydro-1,8-naphthyridin-2-yl)methyl)piperazin-1-yl)-N-methyl Pyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 110

3-cyclopropyl-7-((4-(6-methyl-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazine- 1-yl)methyl)-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 431 [M + 1] ⁺ 111

3-cyclopropyl-7-((4-(2-methyl-1-oxoisoindolin-5-yl)piperazin-1-yl)methyl)-1,8-naphthyridine-2 (1H)-Kone MS-ESI (m/z): 430 [M + 1] ⁺ 112

5-(9-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,9-diazaspiro[5.5 ]Undecyl-3-yl)-N-methylpyridinamide MS-ESI (m/z): 487 [M + 1] ⁺ 113

5-(7-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2,7-diazaspiro[3.5 ]nonan-2-yl)-N-methylpyridinamide MS-ESI (m/z): 459 [M + 1] ⁺ 114

5-((7-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-7-azaspiro[3.5]nonyl Alk-2-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 473 [M + 1] ⁺ 115

5-((7-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-7-azaspiro[3.5]nonane -2-yl)amino)-N-methylpyridinamide MS-ESI (m/z): 461 [M + 1] ⁺ 116

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,6-diazabicyclo[3.2. 0]heptane-6-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 117

5-(6-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,6-diazabicyclo[3.2. 0] Heptane-3-yl)-N-methylpyridinamide MS-ESI (m/z): 419 [M + 1] ⁺ 118

6-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl pyridazine-3-carboxamide MS-ESI (m/z): 407 [M + 1] ⁺ 119

6-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3,6-tetrahydropyridine -4-yl)-N-methylpyridazine-3-formamide MS-ESI (m/z): 405 [M + 1] ⁺ 120

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl pyrimidine-2-carboxamide MS-ESI (m/z): 407 [M + 1] ⁺ 121

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3,6-tetrahydropyridine -4-yl)-N-methylpyrimidine-2-formamide MS-ESI (m/z): 405 [M + 1] ⁺ 122

N-methyl-6-(1-((6-oxo-7-phenyl-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3, 6-tetrahydropyridin-4-yl)pyridazine-3-carboxamide MS-ESI (m/z): 453 [M + 1] ⁺ 123

5-(2-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2-oxazin-5-yl) -N-Methylpyridinamide MS-ESI (m/z): 408 [M + 1] ⁺ 124

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)-N-methoxy Pyridinamide MS-ESI (m/z): 423 [M + 1] ⁺ 125

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-3-fluoro- N-methylpyridinamide MS-ESI (m/z): 424 [M + 1] ⁺ 126

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-5-fluoro-N-methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 422 [M + 1] ⁺ 127

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-hydroxypiperidin-4-yl)- N-methylpyridinamide MS-ESI (m/z): 422 [M + 1] ⁺ 128

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-methoxypiperidin-4-yl )-N-Methylpyridinamide MS-ESI (m/z): 436 [M + 1] ⁺ 129

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-fluoropiperidin-4-yl)- N-methylpyridinamide MS-ESI (m/z): 424 [M + 1] ⁺ 130

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-fluoropiperidin-4-yl)- N-methylpyridinamide MS-ESI (m/z): 424 [M + 1] ⁺ 131

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0]hexyl Alkyl-1-yl)-N-methylpyridinamide MS-ESI (m/z): 404 [M + 1] ⁺ 132

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[4.1.0]heptane Alk-6-yl)-N-methylpyridinamide MS-ESI (m/z): 418 [M + 1] ⁺ 133

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-hydroxypiperidin-4-yl)- N-methylpyridinamide MS-ESI (m/z): 422 [M + 1] ⁺ 134

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4-methoxypiperidin-4-yl )-N-Methylpyridinamide MS-ESI (m/z): 436 [M + 1] ⁺ 135

5-(4-ethoxy-1-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl )-N-Methylpyridinamide MS-ESI (m/z): 450 [M + 1] ⁺ 136

5-(4-cyano-1-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl) -N-Methylpyridinamide MS-ESI (m/z): 431 [M + 1] ⁺ 137

N-methyl-5-(1-((6-oxo-7-phenyl-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl) Pyridinamide MS-ESI (m/z): 454 [M + 1] ⁺ 138

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methoxy-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 420 [M + 1] ⁺ 139

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3,3-difluoropiperidine-4- base) -N-methylpyridinamide MS-ESI (m/z): 442 [M + 1] ⁺ 140

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3',3'-difluoro-N-methyl -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 440 [M + 1] ⁺ 141

5-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0]hexyl Alk-6-yl)-N-methylpyridinamide MS-ESI (m/z): 404 [M + 1] ⁺ 142

5-(1-((7-isopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl Pyridinamide MS-ESI (m/z): 420 [M + 1] ⁺ 143

5-(1-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl Pyridinamide MS-ESI (m/z): 418 [M + 1] ⁺ 144

N-methyl-5-(1-((6-oxo-7-(2,2,2-trifluoroethyl)-5,6-dihydro-1,5-naphthyridin-3-yl) Methyl)piperidin-4-yl)pyridinamide MS-ESI (m/z): 460 [M + 1] ⁺ 145

5-(1-((7-(2,2-difluoroethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine-4 -yl)-N-methylpyridinamide MS-ESI (m/z): 442 [M + 1] ⁺ 146

5-(1-((7-(Difluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)- N-methylpyridinamide MS-ESI (m/z): 428 [M + 1] ⁺ 147

N-methyl-5-(1-((6-oxo-7-(trifluoromethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine- 4-yl)pyridinamide MS-ESI (m/z): 446 [M + 1] ⁺ 148

1'-((7-isopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 418 [M + 1] ⁺ 149

1'-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 416 [M + 1] ⁺ 150

N-methyl-1'-((6-oxo-7-(2,2,2-trifluoroethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl )-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 458 [M + 1] ⁺ 151

1'-((7-(2,2-difluoroethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl- 1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 440 [M + 1] ⁺ 152

1'-((7-(difluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 426 [M + 1] ⁺ 153

N-methyl-1'-((6-oxo-7-(trifluoromethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 444 [M + 1] ⁺ 154

6-(1-((7-isopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl Pyridazine-3-carboxamide MS-ESI (m/z): 421 [M + 1] ⁺ 155

6-(1-((7-isopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3,6-tetrahydro Pyridin-4-yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 419 [M + 1] ⁺ 156

6-(1-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methyl Pyridazine-3-carboxamide MS-ESI (m/z): 419 [M+1]+ 157

6-(1-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3,6-tetrahydro Pyridin-4-yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 417 [M + 1] ⁺ 158

N-methyl-6-(1-((6-oxo-7-(2,2,2-trifluoroethyl)-5,6-dihydro-1,5-naphthyridin-3-yl) Methyl)piperidin-4-yl)pyridazine-3-carboxamide MS-ESI (m/z): 461 [M + 1] ⁺ 159

N-methyl-6-(1-((6-oxo-7-(2,2,2-trifluoroethyl)-5,6-dihydro-1,5-naphthyridin-3-yl) Methyl)-1,2,3,6-tetrahydropyridin-4-yl)pyridazine-3-carboxamide MS-ESI (m/z): 459 [M + 1] ⁺ 160

6-(1-((7-(2,2-difluoroethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine-4 -yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 443 [M + 1] ⁺ 161

6-(1-((7-(2,2-difluoroethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2 ,3,6-tetrahydropyridin-4-yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 441 [M + 1] ⁺ 162

6-(1-((7-(Difluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1,2,3,6 -Tetrahydropyridin-4-yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 427 [M + 1] ⁺ 163

6-(1-((7-(Difluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)- N-methylpyridazine-3-carboxamide MS-ESI (m/z): 429 [M + 1] ⁺ 164

N-methyl-6-(1-((6-oxo-7-(trifluoromethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1, 2,3,6-tetrahydropyridin-4-yl)pyridazine-3-carboxamide MS-ESI (m/z): 445 [M + 1] ⁺ 165

N-methyl-6-(1-((6-oxo-7-(trifluoromethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine- 4-yl)pyridazine-3-carboxamide MS-ESI (m/z): 447 [M + 1] ⁺ 166

6-(3-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0]hexyl Alkyl-6-yl)-N-methylpyridazine-3-carboxamide MS-ESI (m/z): 405 [M + 1] ⁺ 167

5-(3-((7-isopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0] Hexan-6-yl)-N-methylpyridinamide MS-ESI (m/z): 418 [M + 1] ⁺ 168

5-(3-((7-cyclopropyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1.0] Hexan-6-yl)-N-methylpyridinamide MS-ESI (m/z): 416 [M + 1] ⁺ 169

N-methyl-5-(3-((6-oxo-7-(2,2,2-trifluoroethyl)-5,6-dihydro-1,5-naphthyridin-3-yl) Methyl)-3-azabicyclo[3.1.0]hexan-6-yl)pyridinamide MS-ESI (m/z): 458 [M + 1] ⁺ 170

5-(3-((7-(2,2-difluoroethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-nitrogen Heterobicyclo[3.1.0]hexan-6-yl)-N-methylpyridinamide MS-ESI (m/z): 440 [M + 1] ⁺ 171

5-(3-((7-(Difluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-azabicyclo[3.1 .0] Hexan-6-yl)-N-methylpyridinamide MS-ESI (m/z): 426 [M + 1] ⁺ 172

N-methyl-5-(3-((6-oxo-7-(trifluoromethyl)-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3- Azabicyclo[3.1.0]hexan-6-yl)pyridinamide MS-ESI (m/z): 444 [M + 1] ⁺ 173

6-(Difluoromethyl)-5-(1-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine- 4-yl)-N-methylpyridinamide MS-ESI (m/z): 456 [M + 1] ⁺ 174

2-(Difluoromethyl)-1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 454 [M + 1] ⁺ 175

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-6-fluoro- N-methylpyridinamide MS-ESI (m/z): 424 [M + 1] ⁺ 176

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-fluoro-N-methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 422 [M + 1] ⁺ 177

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-methoxy Pyridinamide MS-ESI (m/z): 422 [M + 1] ⁺ 178

N-methyl-1'-((7-methyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 390 [M + 1] ⁺ 179

(R)-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-methylpiperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 180

(S)-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-methylpiperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 181a

( S )-5-(3-ethyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl) -N -methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 181b

( R )-5-(3-ethyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl) -N -methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 182a

( S )-5-(2-ethyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 182b

( R )-5-(2-ethyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 435 [M + 1] ⁺ 183a

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-isopropylpiperazine -1-yl)-N-methylpyridinamide MS-ESI (m/z): 449 [M + 1] ⁺ 183b

( R )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-isopropylpiperazine -1-yl)-N-methylpyridinamide MS-ESI (m/z): 449 [M + 1] ⁺ 184

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-isopropylpiperazin-1-yl )-N-Methylpyridinamide MS-ESI (m/z): 449 [M + 1] ⁺ 185

5-(2-cyclopropyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl )-N-Methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 186

5-(3-cyclopropyl-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl )-N-Methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 187

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-(trifluoromethyl)piperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 475 [M + 1] ⁺ 188

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-(methyl)piperazine-1- base) -N -methylpyridinamide MS-ESI (m/z): 475 [M + 1] ⁺ 189a

( R )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-(hydroxymethyl) Piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 437 [M + 1] ⁺ 189b

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-(hydroxymethyl) Piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 437 [M + 1] ⁺ 190a

( R )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-(hydroxymethyl) Piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 437 [M + 1] ⁺ 190b

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-(hydroxymethyl) Piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 437 [M + 1] ⁺ 191

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-(methoxymethyl Base) piperazin-1-yl) -N-methylpyridinamide MS-ESI (m/z): 451 [M + 1] ⁺ 192

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-(methoxymethyl Base) piperazin-1-yl) -N-methylpyridinamide MS-ESI (m/z): 451 [M+1]+ 193

( R )-5-(3-(cyanomethyl)-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl )piperazin-1-yl)-N-methylpyridinamide MS-ESI (m/z): 446 [M + 1] ⁺ 194a

( S )-5-(2-(cyanomethyl)-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl )piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 446 [M + 1] ⁺ 194b

( R )-5-(2-(cyanomethyl)-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl )piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 446 [M + 1] ⁺ 195

( S )-5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-3-(fluoromethyl) Piperazin-1-yl) -N -methylpyridinamide MS-ESI (m/z): 439 [M + 1] ⁺ 196

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-2-(fluoromethyl)piperazine-1 -yl) -N -methylpyridinamide MS-ESI (m/z): 439 [M + 1] ⁺ 197

5-(3-(difluoromethyl)-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 467 [M + 1] ⁺ 198

5-(2-(difluoromethyl)-4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl)-N-methylpyridinamide MS-ESI (m/z): 467 [M + 1] ⁺ 199

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-4,7-diazaspiro[2.5] Oct-7-yl)-N-methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 200

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazin-1-yl)methyl )-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 405 [M + 1] ⁺ 201

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperidin-1-yl)methyl )-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 404 [M + 1] ⁺ 202

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3,6-dihydropyridine- 1(2H)-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 402 [M + 1] ⁺ 203

3-Ethyl-7-((4-(1-oxoisoindolin-5-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1H)-one MS-ESI (m/z): 404 [M + 1] ⁺ 204

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazin-1-yl)methyl )-1,8-naphthyridin-2(1H)-one MS-ESI (m/z): 405 [M + 1] ⁺ 205

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazin-1-yl)methyl )-1,6-naphthyridin-2(1H)-one MS-ESI (m/z): 405 [M + 1] ⁺ 206

3-Ethyl-7-((4-(7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)piperazin-1-yl)methyl )quinoxaline-2(1H)-one MS-ESI (m/z): 405 [M + 1] ⁺ 207

N-ethoxy-1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 434 [M + 1] ⁺ 208

1'-((7-(hydroxymethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 406 [M + 1] ⁺ 209

1'-((7-(fluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 408 [M + 1] ⁺ 210

1'-((7-(methoxymethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-methyl-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 420 [M + 1] ⁺ 211

N-(methyl-d3)-1'-((7-methyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 393 [M + 1] ⁺ 212

N-(methyl-d3)-5-(1-((7-methyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidine- 4-yl)pyridinamide MS-ESI (m/z): 395 [M + 1] ⁺ 213

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-(methyl-d3)-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 407 [M + 1] ⁺ 214

5-(1-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperidin-4-yl)-N-(methyl base-d3) pyridinamide MS-ESI (m/z): 409 [M + 1] ⁺ 215

1'-((7-(fluoromethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-N-(methyl-d3)-1 ',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 411 [M + 1] ⁺ 216

5-(4-((3-Ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)methyl)piperazin-1-yl)-N-(methyl base-d3) pyridinamide MS-ESI (m/z): 410 [M + 1] ⁺ 217

5-(4-((7-(methoxymethyl)-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) - N -Methylpyridinamide MS-ESI (m/z): 423 [M + 1] ⁺ 218

5-(4-((7-methoxy-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -methyl Pyridinamide MS-ESI (m/z): 409 [M + 1] ⁺ 219

5-(4-((7-ethoxy-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -methyl Pyridinamide MS-ESI (m/z): 423 [M + 1] ⁺ 220

( S )-5-(4-(1-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazin-1-yl )- N -methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 221

( R )-5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazin-1-yl )- N -methylpyridinamide MS-ESI (m/z): 421 [M + 1] ⁺ 222

5-(4-(1-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)cyclopropyl)piperazin-1-yl) -N -Methylpyridinamide MS-ESI (m/z): 433 [M + 1] ⁺ 223

3-Ethyl-7-((4-(6-(5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridin-3-yl)piper Azin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 433 [M + 1] ⁺ 224

7-((4-(6-( 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3-ethyl-1, 5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 417 [M + 1] ⁺ 225

3-Ethyl-7-((4-(6-(5-methyl- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl base)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 431 [M + 1] ⁺ 226

3-Ethyl-7-((4-(6-(5-ethyl- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl base)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 445 [M + 1] ⁺ 227

3-Ethyl-7-((4-(6-(5-methoxy- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 228

7-((4-(6-(5-ethoxy-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3 -Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 461 [M + 1] ⁺ 229

7-((4-(6-(5-Amino- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3-ethane yl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 432 [M + 1] ⁺ 230

7-((4-(6-(5-(dimethylamino)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl )-3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 460 [M + 1] ⁺ 231

7-((4-(6-(5-(diethylamino)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl )-3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 488 [M + 1] ⁺ 232

1'-((7-methoxy-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -methyl-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 406 [M + 1] ⁺ 233

1'-((7-ethoxy-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -methyl-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 420 [M + 1] ⁺ 234

( S )-1'-(1-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 418 [M + 1] ⁺ 235

( R )-1'-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 418 [M + 1] ⁺ 236

1'-(1-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)cyclopropyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 430 [M + 1] ⁺ 237

3-Ethyl-7-((6-(5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6'-dihydro- [3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 430 [M + 1] ⁺ 238

7-((6-(4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2' H ) -yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 414 [M + 1] ⁺ 239

3-Ethyl-7-((6-(5-methyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'- Pyridine]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 428 [M + 1] ⁺ 240

3-ethyl-7-((6-(5-ethyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'- Pyridine]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 442 [M + 1] ⁺ 241

3-Ethyl-7-((6-(5-methoxy-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 242

7-((6-(5-ethoxy-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]-1 '(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 458 [M + 1] ⁺ 243

7-((6-(5-amino-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]-1'( 2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 429 [M + 1] ⁺ 244

7-((6-(5-(dimethylamino)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine ]-1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 457 [M + 1] ⁺ 245

7-((6-(5-(diethylamino)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine ]-1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 485 [M + 1] ⁺ 246

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N- (methyl base-d ₃ ) pyridinecarboxamide MS-ESI (m/z): 410 [M + 1] ⁺ 247

3-Ethyl-7-((4-(6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 459 [M + 1] ⁺ 248

7-((4-(6-(5-cyclopropyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3 -Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 457 [M + 1] ⁺ 249

3-Ethyl-7-((4-(6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine-1 -yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 485 [M + 1] ⁺ 250

7-((4-(6-(5-(difluoromethyl)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl )-3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 467 [M + 1] ⁺ 251

7-((4-(6-(5-(1,1-difluoroethyl)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine-1- Base) methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 481 [M + 1] ⁺ 252

3-Ethyl-7-((6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 456 [M + 1] ⁺ 253

7-((6-(5-cyclopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]-1 '(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 454 [M + 1] ⁺ 254

3-Ethyl-7-((6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3, 4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 482 [M + 1] ⁺ 255

7-((6-(5-(difluoromethyl)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine ]-1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 464 [M + 1] ⁺ 256

7-((6-(5-(1,1-difluoroethyl)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4 '-bipyridyl]-1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 478 [M + 1] ⁺ 257

3-Ethyl-7-((4-(6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl) -1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 432 [M + 1] ⁺ 258

5-(4-(2-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)propan-2-yl)piperazin-1-yl) - N -Picolinamide MS-ESI (m/z): 435 [M + 1] ⁺ 259

1'-(2-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)propan-2-yl) -N -methyl-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 432 [M + 1] ⁺ 260

5-(4-(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridine-3-carbonyl)piperazin-1-yl) -N -methylpyridinecarboxamide MS-ESI (m/z): 421 [M + 1] ⁺ 261

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-tetra Hydrogen-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 390 [M + 1] ⁺ 262

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)acetamide MS-ESI (m/z): 407 [M + 1] ⁺ 263

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)acrylamide MS-ESI (m/z): 421 [M + 1] ⁺ 264

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)isobutyramide MS-ESI (m/z): 435 [M + 1] ⁺ 265

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl) cyclopropanamide MS-ESI (m/z): 433 [M + 1] ⁺ 266

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-2,2,2-trifluoroacetamide MS-ESI (m/z): 461 [M + 1] ⁺ 267

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl) pivalamide MS-ESI (m/z): 449 [M + 1] ⁺ 268

7-((4-(6-(5-(tert-butyl) -4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl) -3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 473 [M + 1] ⁺ 269

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-2,2-difluoropropanamide MS-ESI (m/z): 457 [M + 1] ⁺ 270

N -(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-2,2-difluoroacetamide MS-ESI (m/z): 443 [M + 1] ⁺ 271

Methyl(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl) carbamate MS-ESI (m/z): 423 [M + 1] ⁺ 272

Ethyl(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl) carbamate MS-ESI (m/z): 437 [M + 1] ⁺ 273

Cyclopropyl(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine -2-yl) carbamate MS-ESI (m/z): 449 [M + 1] ⁺ 274

Isopropyl(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine -2-yl) carbamate MS-ESI (m/z): 451 [M + 1] ⁺ 275

1-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-3-methylurea MS-ESI (m/z): 422 [M + 1] ⁺ 276

1-ethyl-3-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine-1 -yl)pyridin-2-yl)urea MS-ESI (m/z): 436 [M + 1] ⁺ 277

1-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-3-isopropylurea MS-ESI (m/z): 450 [M + 1] ⁺ 278

1-( tert-butyl )-3-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piper (oxazin-1-yl)pyridin-2-yl)urea MS-ESI (m/z): 464 [M + 1] ⁺ 279

1-(1,1-difluoroethyl)-3-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl )methyl)piperazin-1-yl)pyridin-2-yl)urea MS-ESI (m/z): 472 [M + 1] ⁺ 280

1-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-3-(trifluoromethyl)urea MS-ESI (m/z): 476 [M + 1] ⁺ 281

3-Ethyl-7-((4-(6-(3-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 282

3-ethyl-7-((4-(6-(3-ethyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 461 [M + 1] ⁺ 283

3-Ethyl-7-((4-(6-(5-oxo-3-(trifluoromethyl)-2,5-dihydro-1 H -1,2,4-triazole-1- Base) pyridin-3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 501 [M + 1] ⁺ 284

3-Ethyl-7-((4-(6-(3-isopropyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)pyridine -3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 475 [M + 1] ⁺ 285

3-Ethyl-7-((4-(6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 286

3-Ethyl-7-((4-(6-(1-ethyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 461 [M + 1] ⁺ 287

Methyl(5-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl )pyridin-2-yl) -1H -1,2,4-triazol-3-yl)carbamate MS-ESI (m/z): 490 [M + 1] ⁺ 288

N -(5-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl )pyridin-2-yl) -1H -1,2,4-triazol-3-yl)acetamide MS-ESI (m/z): 474 [M + 1] ⁺ 289

3-Ethyl-7-((4-(6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)- 1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 448 [M + 1] ⁺ 290

3-Ethyl-7-((4-(6-(5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)-1,5- Naphthyridin-2(1 H )-one MS-ESI (m/z): 430 [M + 1] ⁺ 291

2-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 455 [M + 1] ⁺ 292

3-Ethyl-7-((4-(6-(5-ethyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)- 1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 462 [M + 1] ⁺ 293

3-Ethyl-7-((4-(6-(5-ethyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)-1,5- Naphthyridin-2(1H)-one MS-ESI (m/z): 444 [M + 1] ⁺ 294

5-Ethyl-2-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine-1 -yl)pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 469 [M + 1] ⁺ 295

3-Ethyl-7-((4-(6-(5-(methylamino)-1,2,4-oxadiazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 296

3-Ethyl-7-((4-(6-(5-(ethylamino)-1,2,4-oxadiazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 461 [M + 1] ⁺ 297

7-((4-(6-(5-(cyclopropylamino)-1,2,4-oxadiazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)- 3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 473 [M + 1] ⁺ 298

3-Ethyl-7-((4-(6-(5-(isopropylamino)-1,2,4-oxadiazol-3-yl)pyridin-3-yl)piperazin-1-yl )methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 475 [M + 1] ⁺ 299

3-Ethyl-7-((4-(6-(5-(methylamino)-1,2,4-thiadiazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 463 [M + 1] ⁺ 300

3-Ethyl-7-((4-(6-(5-(ethylamino)-1,2,4-thiadiazol-3-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 477 [M + 1] ⁺ 301

7-((4-(6-(5-(cyclopropylamino)-1,2,4-thiadiazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)- 3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 489 [M + 1] ⁺ 302

3-Ethyl-7-((4-(6-(5-(isopropylamino)-1,2,4-thiadiazol-3-yl)pyridin-3-yl)piperazin-1-yl )methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 491 [M + 1] ⁺ 303

N -(3-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl )pyridin-2-yl)-1,2,4-oxadiazol-5-yl)methylsulfonamide MS-ESI (m/z): 511 [M + 1] ⁺ 304

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -sulfamic acid Acylpyridinecarboxamide MS-ESI (m/z): 472 [M + 1] ⁺ 305

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N- ( N -Methylaminosulfonyl)pyridinecarboxamide MS-ESI (m/z): 486 [M + 1] ⁺ 306

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N- ( N -Ethylsulfamoyl)pyridinamide MS-ESI (m/z): 500 [M + 1] ⁺ 307

N -( N , N -dimethylaminosulfonyl)-5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl ) methyl) piperazin-1-yl) pyridine carboxamide MS-ESI (m/z): 500 [M + 1] ⁺ 308

N -( N , N -diethylsulfamoyl)-5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl ) methyl) piperazin-1-yl) pyridine carboxamide MS-ESI (m/z): 528 [M + 1] ⁺ 309

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N- (methyl Sulfonyl)pyridine carboxamide MS-ESI (m/z): 471 [M + 1] ⁺ 310

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N- (S -Methylsulfonyl imido)pyridine carboxamide MS-ESI (m/z): 470 [M + 1] ⁺ 311

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)acetamide MS-ESI (m/z): 404 [M + 1] ⁺ 312

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)propionamide MS-ESI (m/z): 418 [M + 1] ⁺ 313

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)isobutyramide MS-ESI (m/z): 432 [M + 1] ⁺ 314

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)cyclopropamide MS-ESI (m/z): 430 [M + 1] ⁺ 315

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-2,2,2-trifluoroacetamide MS-ESI (m/z): 458 [M + 1] ⁺ 316

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)pivalamide MS-ESI (m/z): 446 [M + 1] ⁺ 317

7-((6-(5-(tert-butyl)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine] -1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 470 [M + 1] ⁺ 318

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-2,2-difluoropropanamide MS-ESI (m/z): 454 [M + 1] ⁺ 319

N -(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-2,2-difluoroacetamide MS-ESI (m/z): 440 [M + 1] ⁺ 320

Methyl(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 420 [M + 1] ⁺ 321

Ethyl(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 434 [M + 1] ⁺ 322

Cyclopropyl(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3', 6'-tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 446 [M + 1] ⁺ 323

Isopropyl(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3', 6'-tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 448 [M + 1] ⁺ 324

1-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-3-methylurea MS-ESI (m/z): 419 [M + 1] ⁺ 325

1-ethyl-3-(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)urea MS-ESI (m/z): 433 [M + 1] ⁺ 326

1-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-3-isopropylurea MS-ESI (m/z): 447 [M + 1] ⁺ 327

1-( tert-butyl )-3-(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)urea MS-ESI (m/z): 461 [M + 1] ⁺ 328

1-(1,1-difluoroethyl)-3-(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methanol base)-1',2',3',6'-tetrahydro-[3,4'-bipyridine]-6-yl)urea MS-ESI (m/z): 469 [M + 1] ⁺ 329

1-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-3-(trifluoromethyl)urea MS-ESI (m/z): 473 [M + 1] ⁺ 330

3-ethyl-7-((6-(3-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 331

3-ethyl-7-((6-(3-ethyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 458 [M + 1] ⁺ 332

3-Ethyl-7-((6-(5-oxo-3-(trifluoromethyl)-2,5-dihydro-1 H -1,2,4-triazol-1-yl)- 3',6'-Dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 498 [M + 1] ⁺ 333

3-Ethyl-7-((6-(3-isopropyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-1-yl)-3', 6'-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 472 [M + 1] ⁺ 334

3-Ethyl-7-((6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 335

3-ethyl-7-((6-(1-ethyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 458 [M + 1] ⁺ 336

Methyl(5-(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3 ',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -1,2,4-triazol-3-yl)carbamate MS-ESI (m/z): 487 [M + 1] ⁺ 337

N -(5-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3 ',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -1,2,4-triazol-3-yl)acetamide MS-ESI (m/z): 471 [M + 1] ⁺ 338

3-Ethyl-7-((6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 445 [M + 1] ⁺ 339

3-Ethyl-7-((6-(5-methyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2 'H)-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 427 [M + 1] ⁺ 340

2-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 452 [M + 1] ⁺ 341

3-Ethyl-7-((6-(5-ethyl-4-fluoro- 1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 459 [M + 1] ⁺ 342

3-ethyl-7-((6-(5-ethyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2 ' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 441 [M + 1] ⁺ 343

5-Ethyl-2-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 466 [M + 1] ⁺ 344

3-Ethyl-7-((6-(5-(methylamino)-1,2,4-oxadiazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 345

3-Ethyl-7-((6-(5-(ethylamino)-1,2,4-oxadiazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 458 [M + 1] ⁺ 346

7-((6-(5-(cyclopropylamino)-1,2,4-oxadiazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 470 [M + 1] ⁺ 347

3-Ethyl-7-((6-(5-(isopropylamino)-1,2,4-oxadiazol-3-yl)-3',6'-dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 472 [M + 1] ⁺ 348

3-Ethyl-7-((6-(5-(methylamino)-1,2,4-thiadiazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 460 [M + 1] ⁺ 349

3-Ethyl-7-((6-(5-(ethylamino)-1,2,4-thiadiazol-3-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 474 [M + 1] ⁺ 350

7-((6-(5-(cyclopropylamino)-1,2,4-thiadiazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 486 [M + 1] ⁺ 351

3-Ethyl-7-((6-(5-(isopropylamino)-1,2,4-thiadiazol-3-yl)-3',6'-dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 488 [M + 1] ⁺ 352

N -(3-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3 ',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1,2,4-oxadiazol-5-yl)methylsulfonamide MS-ESI (m/z): 508 [M + 1] ⁺ 353

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -aminosulfonyl-1',2', 3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 469 [M + 1] ⁺ 354

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N- ( N -methylsulfamoyl)- 1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 483 [M + 1] ⁺ 355

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N- ( N -ethylaminosulfonyl)- 1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 497 [M + 1] ⁺ 356

N -( N , N -dimethylaminosulfonyl)-1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methanol base)-1',2',3',6'-tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 497 [M + 1] ⁺ 357

N -( N , N -diethylsulfamoyl)-1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methanol base)-1',2',3',6'-tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 525 [M + 1] ⁺ 358

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N- (methylsulfonyl)-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 468 [M + 1] ⁺ 359

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N- ( S -methylsulfonimido) -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 467 [M + 1] ⁺ 360

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-sulfonamide MS-ESI (m/z): 440 [M + 1] ⁺ 361

N -Ethyl-1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-sulfonamide MS-ESI (m/z): 454 [M + 1] ⁺ 362

1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl) -N -isopropyl-1',2',3 ',6'-Tetrahydro-[3,4'-bipyridyl]-6-sulfonamide MS-ESI (m/z): 468 [M + 1] ⁺ 363

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -methyl Pyridine-2-sulfonamide MS-ESI (m/z): 443 [M + 1] ⁺ 364

N -ethyl-5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) Pyridine-2-sulfonamide MS-ESI (m/z): 457 [M + 1] ⁺ 365

5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl) -N -isopropyl Pyridine-2-sulfonamide MS-ESI (m/z): 471 [M + 1] ⁺ 366

( S )-3-Ethyl-7-(1-(4-(6-(5-isopropyl- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piper Azin-1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 473 [M + 1] ⁺ 367

( S )-3-ethyl-7-(1-(4-(6-(5-ethyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine -1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 459 [M + 1] ⁺ 368

( S )-3-Ethyl-7-(1-(4-(6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)pyridine-3- Base) piperazin-1-yl) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 499 [M + 1] ⁺ 369

( R )-3-Ethyl-7-(1-(4-(6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piper Azin-1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 473 [M + 1] ⁺ 370

( R )-3-ethyl-7-(1-(4-(6-(5-ethyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine -1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 459 [M + 1] ⁺ 371

( R )-3-ethyl-7-(1-(4-(6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)pyridine-3- Base) piperazin-1-yl) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 499 [M + 1] ⁺ 372

( S )-3-Ethyl-7-(1-(6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro- [3,4'-bipyridyl]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 470 [M + 1] ⁺ 373

( S )-3-ethyl-7-(1-(6-(5-ethyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[ 3,4'-bipyridyl]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 456 [M + 1] ⁺ 374

( S )-3-Ethyl-7-(1-(6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)-3',6'- Dihydro-[3,4'-bipyridine]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 496 [M + 1] ⁺ 375

( R )-3-Ethyl-7-(1-(6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro- [3,4'-bipyridyl]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 470 [M + 1] ⁺ 376

( R )-3-ethyl-7-(1-(6-(5-ethyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[ 3,4'-bipyridyl]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 456 [M + 1] ⁺ 377

( R )-3-Ethyl-7-(1-(6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)-3',6'- Dihydro-[3,4'-bipyridine]-1'(2' H )-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 496 [M + 1] ⁺ 378

1'-((2-Ethyl-5-fluoro-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 440 [M + 1] ⁺ 379

2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 426 [M + 1] ⁺ 380

5-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 426 [M + 1] ⁺ 381

2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methoxy-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 442 [M + 1] ⁺ 382

2-fluoro-1'-((5-fluoro-2-methoxy-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 442 [M + 1] ⁺ 383

2-fluoro-1'-((5-fluoro-2-isopropyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 454 [M + 1] ⁺ 384

1'-((2-(Difluoromethyl)-5-fluoro-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -methyl- 1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 462 [M + 1] ⁺ 385

2-fluoro-1'-((5-fluoro-3-oxo-2-(trifluoromethyl)-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl- 1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 480 [M + 1] ⁺ 386

2-fluoro-1'-((5-fluoro-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2',3', 6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 412 [M + 1] ⁺ 387

1'-((2-cyclopropyl-5-fluoro-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -methyl-1', 2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 452 [M + 1] ⁺ 388

( S )-2-fluoro-1'-((5-fluoro-2-(1-fluoroethyl)-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)- N -Methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 458 [M + 1] ⁺ 389

( R )-2-fluoro-1'-((5-fluoro-2-(1-fluoroethyl)-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)- N -Methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 458 [M + 1] ⁺ 390

1'-((2-(1,1-difluoroethyl)-5-fluoro-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -Methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 476 [M + 1] ⁺ 391

1'-((2,5-Dimethyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 422 [M + 1] ⁺ 392

1'-((5-chloro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-2-fluoro- N -methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 442 [M + 1] ⁺ 393

1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 408 [M + 1] ⁺ 394

2-Chloro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2 ',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 442 [M + 1] ⁺ 395

1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N ,2-dimethyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 422 [M + 1] ⁺ 396

2-(Difluoromethyl)-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 458 [M + 1] ⁺ 397

8-fluoro-7-((4-(2-fluoro-6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl Base)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 470 [M + 1] ⁺ 398

2-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 477 [M + 1] ⁺ 399

8-fluoro-7-((4-(2-fluoro-6-(5-methyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine-1- Base) methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 453 [M + 1] ⁺ 400

8-fluoro-7-((4-(2-fluoro-6-(4H - 1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl) -3-Methylquinoxalin-2(1 H )-one MS-ESI (m/z): 439 [M + 1] ⁺ 401

7-((4-(6-(5-Ethyl- 4H -1,2,4-triazol-3-yl)-2-fluoropyridin-3-yl)piperazin-1-yl)methyl )-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 467 [M + 1] ⁺ 402

8-fluoro-7-((4-(2-fluoro-6-(5-isopropyl- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine-1 -yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 481 [M + 1] ⁺ 403

7-((4-(6-(5-cyclopropyl- 4H -1,2,4-triazol-3-yl)-2-fluoropyridin-3-yl)piperazin-1-yl)methyl Base)-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 479 [M + 1] ⁺ 404

8-fluoro-7-((4-(2-fluoro-6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piper Azin-1-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 507 [M + 1] ⁺ 405

8-fluoro-7-((4-(2-fluoro-6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl )pyridin-3-yl)piperazin-1-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 469 [M + 1] ⁺ 406

5-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl)-1,3,4-oxadiazol-2(3 H )-one MS-ESI (m/z): 456 [M + 1] ⁺ 407

3-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl)-1,2,4-oxadiazol-5(4 H )-one MS-ESI (m/z): 456 [M + 1] ⁺ 408

Methyl(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- yl)pyridin-2-yl)carbamate MS-ESI (m/z): 445 [M + 1] ⁺ 409

Ethyl(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- yl)pyridin-2-yl)carbamate MS-ESI (m/z): 459 [M + 1] ⁺ 410

N -(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl) methylsulfonamide MS-ESI (m/z): 465 [M + 1] ⁺ 411

6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazin-1-yl)- N -(Methylsulfonyl)pyridinamide MS-ESI (m/z): 493 [M + 1] ⁺ 412

( R )-5-(3-(cyanomethyl)-4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl )piperazin-1-yl)-6-fluoro- N -methylpyridinamide MS-ESI (m/z): 468 [M + 1] ⁺ 413

( S )-6-fluoro-5-(4-(1-(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)ethyl)piperazine -1-yl) -N -methylpyridinamide MS-ESI (m/z): 443 [M + 1] ⁺ 414

( R )-6-fluoro-5-(4-(1-(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)ethyl)piperazine -1-yl) -N -methylpyridinamide MS-ESI (m/z): 443 [M + 1] ⁺ 415

8-fluoro-7-((2-fluoro-6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'- Pyridine]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 467 [M + 1] ⁺ 416

2-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 474 [M + 1] ⁺ 417

8-fluoro-7-((2-fluoro-6-(5-methyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4 '-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 450 [M + 1] ⁺ 418

8-fluoro-7-((2-fluoro-6-(4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'-bipyridine] -1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 436 [M + 1] ⁺ 419

7-((6-(5-Ethyl- 4H -1,2,4-triazol-3-yl)-2-fluoro-3',6'-dihydro-[3,4'-bipyridine ]-1'(2' H )-yl)methyl)-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 464 [M + 1] ⁺ 420

8-fluoro-7-((2-fluoro-6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3, 4'-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 478 [M + 1] ⁺ 421

7-((6-(5-cyclopropyl-4 H -1,2,4-triazol-3-yl)-2-fluoro-3',6'-dihydro-[3,4'-bi Pyridine]-1'(2' H )-yl)methyl)-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 476 [M + 1] ⁺ 422

8-fluoro-7-((2-fluoro-6-(5-(trifluoromethyl)-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro- [3,4'-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 504 [M + 1] ⁺ 423

8-fluoro-7-((2-fluoro-6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)-3 ',6'-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 466 [M + 1] ⁺ 424

5-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1,3,4-oxadiazol-2(3 H )-one MS-ESI (m/z): 453 [M + 1] ⁺ 425

3-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1,2,4-oxadiazol-5(4 H )-one MS-ESI (m/z): 453 [M + 1] ⁺ 426

Methyl(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 442 [M + 1] ⁺ 427

Ethyl(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)carbamate MS-ESI (m/z): 456 [M + 1] ⁺ 428

N -(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)methylsulfonamide MS-ESI (m/z): 462 [M + 1] ⁺ 429

2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N- (methylsulfonyl) -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 490 [M + 1] ⁺ 430

( S )-2'-(cyanomethyl)-2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl )methyl) -N -methyl-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 465 [M + 1] ⁺ 431

( S )-2-fluoro-1'-(1-(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)ethyl) -N -methyl Base-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 440 [M + 1] ⁺ 432

( R )-2-fluoro-1'-(1-(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)ethyl) -N -methyl Base-1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 440 [M + 1] ⁺ 433

3,6-Difluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- base) -N -methylpyridinamide MS-ESI (m/z): 447 [M + 1] ⁺ 434

2,5-Difluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1 ',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 444 [M + 1] ⁺ 435

7-((4-(6-(5-amino-1,2,4-oxadiazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3-ethyl- 1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 433 [M + 1] ⁺ 436

7-((4-(6-(5-amino-1,2,4-thiadiazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3-ethyl- 1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 449 [M + 1] ⁺ 437

5-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-1,3,4-oxadiazol-2(3 H )-one MS-ESI (m/z): 434 [M + 1] ⁺ 438

3-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-1,2,4-oxadiazol-5(4 H )-one MS-ESI (m/z): 434 [M + 1] ⁺ 439

1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N -methyl-1',2',3',6'-Tetrahydro-[3,4'-bipyridine]-6-formamide MS-ESI (m/z): 408 [M + 1] ⁺ 440

8-fluoro-7-((6-(5-isopropyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3,4'- Pyridine]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 460 [M + 1] ⁺ 441

8-fluoro-3-methyl-7-((6-(5-methyl-4 H -1,2,4-triazol-3-yl)-3',6'-dihydro-[3, 4'-bipyridyl]-1'(2' H )-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 432 [M + 1] ⁺ 442

8-fluoro-3-methyl-7-((6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)- 3',6'-Dihydro-[3,4'-bipyridine]-1'(2' H )-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 448 [M + 1] ⁺ 443

8-fluoro-7-((6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]-1 '(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 449 [M + 1] ⁺ 444

2-(1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2',3',6 '-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 456 [M + 1] ⁺ 445

8-fluoro-7-((4-(6-(5-isopropyl- 4H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl Base)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 463 [M + 1] ⁺ 446

8-fluoro-3-methyl-7-((4-(6-(5-methyl-4 H -1,2,4-triazol-3-yl)pyridin-3-yl)piperazine-1 -yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 435 [M + 1] ⁺ 447

8-fluoro-3-methyl-7-((4-(6-(1-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazole-3- Base) pyridin-3-yl) piperazin-1-yl) methyl) quinoxalin-2 (1 H )-one MS-ESI (m/z): 451 [M + 1] ⁺ 448

8-fluoro-7-((4-(6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3 -Methylquinoxalin-2(1 H )-one MS-ESI (m/z): 452 [M + 1] ⁺ 449

2-(5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 459 [M + 1] ⁺ 450

2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) -N- (methyl- d ₃ ) -1',2',3',6'-Tetrahydro-[3,4'-bipyridyl]-6-formamide MS-ESI (m/z): 429 [M + 1] ⁺ 451

2-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 531 [M + 1] ⁺ 452

8-fluoro-7-((4-(2-fluoro-6-(4-fluoro-5-(trifluoromethyl)-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1 -yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 524 [M + 1] ⁺ 453

8-fluoro-7-((4-(2-fluoro-6-(5-(trifluoromethyl)-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl Base)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 506 [M + 1] ⁺ 454

2-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 528 [M + 1] ⁺ 455

8-fluoro-7-((2-fluoro-6-(4-fluoro-5-(trifluoromethyl)-1 H -imidazol-2-yl)-3',6'-dihydro-[3, 4'-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 521 [M + 1] ⁺ 456

8-fluoro-7-((2-fluoro-6-(5-(trifluoromethyl)-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'- Pyridine]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 503 [M + 1] ⁺ 457

3-Ethyl-7-((4-(6-(5-(trifluoromethyl)-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)- 1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 484 [M + 1] ⁺ 458

3-Ethyl-7-((4-(6-(4-fluoro-5-(trifluoromethyl)-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 502 [M + 1] ⁺ 459

2-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 509 [M + 1] ⁺ 460

3-Ethyl-7-((6-(5-(trifluoromethyl)-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 481 [M + 1] ⁺ 461

3-Ethyl-7-((6-(4-fluoro-5-(trifluoromethyl)-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 499 [M + 1] ⁺ 462

2-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-Tetrahydro-[3,4'-bipyridyl]-6-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 506 [M + 1] ⁺ 463

8-fluoro-7-((4-(2-fluoro-6-(5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridine-3- Base) piperazin-1-yl) methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 455 [M + 1] ⁺ 464

8-fluoro-7-((2-fluoro-6-(5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6'- Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 452 [M + 1] ⁺ 465

7-((4-(6-(5-ethyl-4-fluoro-1 H -imidazol-2-yl)-2-fluoropyridin-3-yl)piperazin-1-yl)methyl)-8 -Fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 484 [M + 1] ⁺ 466

5-Ethyl-2-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl) Piperazin-1-yl)pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 491 [M + 1] ⁺ 467

7-((6-(5-Ethyl-4-fluoro-1 H -imidazol-2-yl)-2-fluoro-3',6'-dihydro-[3,4'-bipyridine]-1 '(2' H )-yl)methyl)-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 481 [M + 1] ⁺ 468

5-Ethyl-2-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1 ',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 488 [M + 1] ⁺ 469

3-Ethyl-7-((6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine] -1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 473 [M + 1] ⁺ 470

2-(1'-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2',3',6 '-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 480 [M + 1] ⁺ 471

8-fluoro-7-((2-fluoro-6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'- Bipyridyl]-1'(2' H )-yl)methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 495 [M + 1] ⁺ 472

2-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)-1',2', 3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 502 [M + 1] ⁺ 473

7-((6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2 ' H )-yl)methyl)-3-ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 471 [M + 1] ⁺ 474

5-cyclopropyl-2-(1'-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)-1',2 ',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 478 [M + 1] ⁺ 475

7-((6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)-2-fluoro-3',6'-dihydro-[3,4'-bipyridine]- 1'(2' H )-yl)methyl)-8-fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 493 [M + 1] ⁺ 476

5-cyclopropyl-2-(2-fluoro-1'-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)- 1',2',3',6'-tetrahydro-[3,4'-bipyridyl]-6-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 500 [M + 1] ⁺ 477

3-Ethyl-7-((4-(6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl) -1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 476 [M + 1] ⁺ 478

2-(5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine- 2-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 483 [M + 1] ⁺ 479

8-fluoro-7-((4-(2-fluoro-6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl) Methyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 498 [M + 1] ⁺ 480

2-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazine-1- Base) pyridin-2-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 505 [M + 1] ⁺ 481

7-((4-(6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)methyl)-3-ethyl -1,5-Naphthyridin-2(1 H )-one MS-ESI (m/z): 474 [M + 1] ⁺ 482

5-cyclopropyl-2-(5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazine- 1-yl)pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 481 [M + 1] ⁺ 483

7-((4-(6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)-2-fluoropyridin-3-yl)piperazin-1-yl)methyl)- 8-Fluoro-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 496 [M + 1] ⁺ 484

5-cyclopropyl-2-(6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl )piperazin-1-yl)pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 503 [M + 1] ⁺ 485

( S )-3-ethyl-7-(1-(4-(6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1- Base) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 462 [M + 1] ⁺ 486

( R )-3-ethyl-7-(1-(4-(6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1- Base) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 462 [M + 1] ⁺ 487

( S )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 469 [M + 1] ⁺ 488

( R )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 469 [M + 1] ⁺ 489

( S )-3-Ethyl-7-(1-(4-(6-(4-fluoro-5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-3-yl)piperazine -1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 516 [M + 1] ⁺ 490

( R )-3-ethyl-7-(1-(4-(6-(4-fluoro-5-(trifluoromethyl)-1 H -imidazol-2-yl)pyridin-3-yl)piper Azin-1-yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 516 [M + 1] ⁺ 491

( S )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 523 [M + 1] ⁺ 492

( R )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-(trifluoromethyl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 523 [M + 1] ⁺ 493

( S )-3-ethyl-7-(1-(4-(6-(5-ethyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1- Base) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 476 [M + 1] ⁺ 494

( R )-3-ethyl-7-(1-(4-(6-(5-ethyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1- Base) ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 476 [M + 1] ⁺ 495

( S )-5-ethyl-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl Base) piperazin-1-yl) pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 483 [M + 1] ⁺ 496

( R )-5-ethyl-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl) ethyl Base) piperazin-1-yl) pyridin-2-yl)-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 483 [M + 1] ⁺ 497

( S )-3-ethyl-7-(1-(4-(6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1 -yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 490 [M + 1] ⁺ 498

( R )-3-ethyl-7-(1-(4-(6-(4-fluoro-5-isopropyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazine-1 -yl)ethyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 490 [M + 1] ⁺ 499

( S )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 497 [M + 1] ⁺ 500

( R )-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)ethyl)piperazine- 1-yl)pyridin-2-yl)-5-isopropyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 497 [M + 1] ⁺ 501

( S )-7-(1-(4-(6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)ethyl )-3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 488 [M + 1] ⁺ 502

( R )-7-(1-(4-(6-(5-cyclopropyl-4-fluoro-1 H -imidazol-2-yl)pyridin-3-yl)piperazin-1-yl)ethyl )-3-Ethyl-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 488 [M + 1] ⁺ 503

( S )-5-cyclopropyl-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl) Ethyl)piperazin-1-yl)pyridin-2-yl) -1H -imidazole-4-carbonitrile MS-ESI (m/z): 495 [M + 1] ⁺ 504

( R )-5-cyclopropyl-2-(5-(4-(1-(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl) Ethyl)piperazin-1-yl)pyridin-2-yl) -1H -imidazole-4-carbonitrile MS-ESI (m/z): 495 [M + 1] ⁺ 505

( S )-8-fluoro-7-(1-(4-(2-fluoro-6-(4-fluoro-5-methyl-1 H -imidazol-2-yl)pyridin-3-yl)piperazine -1-yl)ethyl)-3-methylquinoxalin-2(1 H )-one MS-ESI (m/z): 484 [M + 1] ⁺ 506

( R )-2-(6-fluoro-5-(4-(1-(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)ethyl) )piperazin-1-yl)pyridin-2-yl)-5-methyl-1 H -imidazole-4-carbonitrile MS-ESI (m/z): 491 [M + 1] ⁺ 507

3-Ethyl-7-((4-(6-(2-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 508

3-Ethyl-7-((4-(6-(4-methyl-5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)pyridine- 3-yl)piperazin-1-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 447 [M + 1] ⁺ 509

3-Ethyl-8-fluoro-7-((4-(2-fluoro-6-(2-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-tri Azol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 483 [M + 1] ⁺ 510

3-Ethyl-8-fluoro-7-((4-(2-fluoro-6-(4-methyl-5-oxo-4,5-dihydro-1 H -1,2,4-tri Azol-3-yl)pyridin-3-yl)piperazin-1-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 483 [M + 1] ⁺ 511

3-ethyl-7-((6-(2-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 512

3-ethyl-7-((6-(4-methyl-5-oxo-4,5-dihydro-1 H -1,2,4-triazol-3-yl)-3',6 '-Dihydro-[3,4'-bipyridyl]-1'(2' H )-yl)methyl)-1,5-naphthyridin-2(1 H )-one MS-ESI (m/z): 444 [M + 1] ⁺ 513

3-Ethyl-8-fluoro-7-((2-fluoro-6-(2-methyl-5-oxo-2,5-dihydro-1 H -1,2,4-triazole-3 -yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2' H )-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 480 [M + 1] ⁺ 514

3-Ethyl-8-fluoro-7-((2-fluoro-6-(4-methyl-5-oxo-4,5-dihydro-1 H -1,2,4-triazole-3 -yl)-3',6'-dihydro-[3,4'-bipyridine]-1'(2' H )-yl)methyl)quinoxalin-2(1 H )-one MS-ESI (m/z): 480 [M + 1] ⁺

[ Cell Proliferation Assay ]

MTS detection kit was purchased from Promega (Madison, WI, USA). RPMI-1640 medium, fetal bovine serum and penicillin-streptomycin were purchased from BI (Biological Industries, Beit Haemek, Israel). Fetal bovine serum was purchased from GIBCO (Grand Island, NY, USA). Dimethylsulfone (DMSO) was purchased from Sigma (St. Louis., MO, USA). MDA-MB-436 (CAS, Cat. No: TCHu184) cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum and 100 U/mL penicillin-streptomycin.

The inhibitory effect of the compound on PARP1 was detected by measuring the inhibitory effect of the compound on the proliferation of MDA-MB-436 (BRCA1-deficient) cells. The cells were digested and collected, and the cells were seeded in a 96-well plate at a concentration of 2000 cells/well of MDA-MB-436, and incubated at 37°C, 5% CO ₂ for 4 hours. Compounds with different concentrations (final concentrations 10000, 3333.3, 1111.1, 370.4, 123.5, 41.2, 13.7, 4.6 and 1.5 nM) were added to 3 parallel wells of a 96-well cell culture plate, and incubated at 37°C, 5% CO ₂ for 120 h. Add 20 µL of MTS to each well, incubate at 37°C, 5% CO ₂ for 2 h, and measure the absorbance at 490 nm with a microplate reader. _IC50 values were calculated with GraphPad Prism 8.0.

Selected compounds prepared above were tested according to the biological methods described herein. The results are shown in Table 2.

Table 2 Example IC ₅₀ (nM) Example IC ₅₀ (nM) 2 1 192 1 4 5 195 1 13 1 193 1 44 1 194b 3 61 1 220 1 71 1 221 1 118 1 224 1 119 1 226 1 121 1 246 1 126 1 247 1 141 1 249 1 149 1 252 1 150 1 271 1 178 1 285 1 179 1 289 3 213 1 290 1 181b 1 291 2 191 1 / /

MTS detection kit was purchased from Promega (Madison, WI, USA). RPMI-1640 medium, IMDM medium, trypsin and penicillin-streptomycin were purchased from BI (Biological Industries, Beit Haemek, Israel). Fetal bovine serum was purchased from GIBCO (Grand Island, NY, USA). Dimethylsulfone (DMSO) was purchased from Sigma (St. Louis., MO, USA). Capan-1 (ATCC, Cat. No: HTB-79) and MX-1 (Cobioer, Cat. No: CBP60640) cells were cultured in IMDM containing 20% fetal bovine serum and RPMI-1640 containing 10% fetal bovine serum, respectively medium.

The inhibitory effect of the compound on PARP1 was detected by measuring the inhibitory effect of the compound on the proliferation of Capan-1 (BRCA2-deficient) and MX-1 (BRCA1-deficient) cells. The cells were digested, and the cells were seeded in 96-well plates at the optimal cell density (Capan-1: 10000 cells/well; MX-1: 5000 cells/well), and incubated at 37°C, 5% CO ₂ for 24 h. Compounds with different concentrations (final concentrations 10000, 3333.3, 1111.1, 370.4, 123.5, 41.2, 13.7, 4.6 and 1.5nM) were added to 3 parallel wells of a 96-well cell culture plate, and incubated at 37°C, 5% CO ₂ for 7 days. Add 20 µL of MTS to each well, incubate at 37°C, 5% CO ₂ for 2 h, and measure the absorbance at 490 nm with a microplate reader. _IC50 values were calculated with GraphPad Prism 8.0.

Selected compounds prepared above were tested according to the biological methods described herein. The results are shown in Table 3.

table 3 Example MX-1 IC ₅₀ (nM) Example MX-1 IC ₅₀ (nM) 2 1 221 2 4 1 246 1 13 3 247 2 194b 3 285 3 213 1 289 1 220 2 291 2

[ Pharmacokinetic experiment ]

The purpose of this experiment is to study the pharmacokinetic properties of Compound 2 in male Beagle dogs (provided by Beijing Masi Biotechnology Co., Ltd.). Including (1) 1mg/kg single intravenous bolus administration study; (2) 3mg/kg single gavage administration study.

Animals in group 1 were given 1 mg/kg, 1 mg/mL compound 2 solution by intravenous injection once, and animals in group 2 were given 3 mg/kg, 1 mg/mL compound 2 solution by intragastric administration. The vehicle for the two groups of drug preparations was 10% dimethylsulfoxide (Sigma, batch number: BCCG0331): 60% polyethylene glycol 400 (Sigma, batch number: MKCN6245): 30% water. The concentration of compound 2 in plasma samples was determined by LC/MS/MS method. (Liquid phase: Waters UPLC; Mass spectrometry: Triple Quad 6500 plus).

Selected compounds prepared above were tested according to the biological methods described herein. The results are shown in Table 4.

Table 4 compound Route of administration dose T _1/2 C _max /C ₀ (ng/mL) AUC _last (mg/kg) (h) (h.ng/mL) 2 po 3 6.97 17933 155312 iv 1 9.66 7861 50140 Reference compound 1 po 3 8.59 8753 88097 iv 1 13.1 2927 18833

Claims (23)

Compound shown in formula (I):

(I) or a pharmaceutically acceptable salt thereof, wherein: X ¹ is selected from N and CR ⁶ ; X ² is selected from N and CR ⁷ ; X ³ is selected from N and CR ⁸ ; X ⁴ is selected from N and CR ⁹ ; Q ¹ is selected from C _3-10 cycloalkyl, heterocyclic and heteroaryl; Q ² is selected from heterocyclic, aryl and heteroaryl; L is selected from chemical bonds, -(CR ^C0 R ^D0 ) _u -, -(CR ^C0 R ^D0 ) _u O(CR ^C0 R ^D0 ) _t -, -(CR ^C0 R ^D0 ) _u NR ^A0 (CR ^C0 R ^D0 ) _t -and-(CR ^C0 R ^D0 ) _u S(CR ^C0 R ^D0 ) _t -; each R ¹ is independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 ring Alkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 Alkyl, CN, NO ₂ , -NR ^A1 R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(=NR ^E1 )R ^A1 , -C(=N-OR ^B1 )R ^A1 , -C (O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) ₂ OR ^A1 、-C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 、-C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 、-C(O)NR ^A1 S(O )(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(O)R ^B1 , -C(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )R ^B1 , -OC(O) NR ^A1 R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -NR ^A1 C(S)NR ^A1 R ^B1 , -NR ^A1 C(=NR ^E1 )NR ^A1 R ^B1 , -S(O) _r R ^A1 , -S(O)(=NR ^E1 )R ^B1 , -N=S(O)R ^A1 R ^B1 , -S(O) ₂ OR ^A1 , -OS(O ) ₂ R ^A1 , -NR ^A1 S(O) _r R ^B1 , -NR ^A1 S(O)(=NR ^E1 )R ^B1 , -S(O) _r NR ^A1 R ^B1 , -S(O)(=NR ^E1 )NR ^A1 R ^B1 , -NR ^A1 S(O) ₂ NR ^A1 R ^B1 , -NR ^A1 S(O)(=NR ^E1 )NR ^A1 R ^B1 , -P(O)R ^A1 R ^B1 and -P( O) (OR ^A1 ) (OR ^B1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X1 is replaced by a substituent; each R is ^{independently} selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 Cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _{1- 4} Alkyl, CN, NO ₂ , -NR ^A2 R ^B2 , -OR ^A2 , -C(O)R ^A2 , -C(=NR ^E2 )R ^A2 , -C(=N-OR ^B2 )R ^A2 , - C(O)OR ^A2 , -OC(O)R ^A2 , -C(O)NR ^A2 R ^B2 , -NR ^A2 C(O)R ^B2 , -C(=NR ^E2 )NR ^A2 R ^B2 , -NR ^A2 C(=NR ^E2 )R ^B2 , -OC(O)NR ^A2 R ^B2 , -NR ^A2 C(O)OR ^B2 , -NR ^A2 C(O)NR ^A2 R ^B2 , -NR ^A2 C(S)NR ^A2 R ^B2 、-NR ^A2 C(=NR ^E2 )NR ^A2 R ^B2 、-S(O) _r R ^A2 、-S(O)(=NR ^E2 )R ^B2 、-N=S(O)R ^A2 R ^B2 , -S(O) ₂ OR ^A2 , -OS(O) ₂ R ^A2 , -NR ^A2 S(O) _r R ^B2 , -NR ^A2 S(O)(=NR ^E2 )R ^B2 , -S(O) _r NR ^A2 R ^B2 、-S(O)(=NR ^E2 )NR ^A2 R ^B2 、-NR ^A2 S(O) ₂ NR ^A2 R ^B2 、-NR ^A2 S(O)(=NR ^E2 )NR ^A2 R ^B2 , -P(O)R ^A2 R ^B2 and -P(O)(OR ^A2 )(OR ^B2 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl R is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A3 R ^B3 , -OR ^A3 and -C(O)R ^A3 , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl and heterocyclyl is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; R ⁴ selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, Heterocyclyl, heterocyclyl-C _1-4 alkyl, CN, NO ₂ , -NR ^A4 R ^B4 , -OR ^A4 and -C(O)R ^A4 , wherein each alkyl, alkenyl, alkynyl, Cycloalkyl and heterocyclyl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or R ³ and R ⁴ together with their connected atoms form a C _3-10 cycloalkyl or containing 1, 2 or 3 heteroatoms of 4-12 membered heterocyclic groups, wherein the heteroatoms are independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring is unsubstituted or substituted by 1, 2 or 3 R ^X3 substituents; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkane radical, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A5 R ^B5 , -OR ^A5 , -C(O)R ^A5 , -C(=NR ^E5 )R ^A5 , -C(=N-OR ^B5 )R ^A5 , -C(O)OR ^A5 , -OC (O)R ^A5 , -C(O)NR ^A5 R ^B5 , -NR ^A5 C(O)R ^B5 , -C(=NR ^E5 )NR ^A5 R ^B5 , -NR ^A5 C(=NR ^E5 )R ^B5 , -OC(O)NR ^A5 R ^B5 , -NR ^A5 C(O)OR ^B5 , -NR ^A5 C(O)NR ^A5 R ^B5 , -NR ^A5 C(S)NR ^A5 R ^B5 , -NR ^A5 C(= NR ^E5 )NR ^A5 R ^B5 , -S(O) _r R ^A5 , -S(O)(=NR ^E5 )R ^B5 , -N=S(O)R ^{A5 R B5 ,} -S(O) ₂ OR ^A5 , -OS(O) ₂ R ^A5 , -NR ^A5 S(O) _r R ^B5 , -NR ^A5 S(O)(=NR ^E5 )R ^B5 , -S(O) _r NR ^A5 R ^B5 , -S( O)(=NR ^E5 )NR ^A5 R ^B5 、-NR ^A5 S(O) ₂ NR ^A5 R ^B5 、-NR ^A5 S(O)(=NR ^E5 )NR ^A5 R ^B5 、-P(O)R ^A5 R ^B5 and -P (O) (OR ^A5 ) (OR ^B5 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or replaced by at least A substituent independently selected from R ^X5 is substituted; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A6 R ^B6 , -OR ^A6 , -C(O)R ^A6 , -C(=NR ^E6 )R ^A6 , -C(=N-OR ^B6 )R ^A6 、-C(O)OR ^A6 、-OC(O)R ^A6 、-C(O)NR ^A6 R ^B6 、-NR ^A6 C(O)R ^B6 、-C(=NR ^E6 )NR ^A6 R ^B6 、- NR ^A6 C(=NR ^E6 )R ^B6 、-OC(O)NR ^A6 R ^B6 、-NR ^A6 C(O)OR ^B6 、-NR ^A6 C(O)NR ^A6 R ^B6 、-NR ^A6 C(S) NR ^A6 R ^B6 , -NR ^A6 C(=NR ^E6 )NR ^A6 R ^B6 , -S(O) _r R ^A6 , -S(O)(=NR ^E6 )R ^B6 , -N=S(O)R ^A6 R ^B6 、-S(O) ₂ OR ^A6 、-OS(O) ₂ R ^A6 、-NR ^A6 S(O) _r R ^B6 、-NR ^A6 S(O)(=NR ^E6 )R ^B6 、-S( O) _r NR ^A6 R ^B6 、-S(O)(=NR ^E6 )NR ^A6 R ^B6 、-NR ^A6 S(O) ₂ NR ^A6 R ^B6 、-NR ^A6 S(O)(=NR ^E6 )NR ^A6 R ^B6 , -P(O)R ^A6 R ^B6 and -P(O)(OR ^A6 )(OR ^B6 ), wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and Heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl , C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkane base, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A7 R ^B7 , -OR ^A7 , -C(O)R ^A7 , -C(=NR ^E7 )R ^A7 , -C(=N-OR ^B7 )R ^A7 , -C(O)OR ^A7 , -OC(O)R ^A7 , -C(O)NR ^A7 R ^B7 , -NR ^A7 C(O)R ^B7 , -C (=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )R ^B7 , -OC(O)NR ^A7 R ^B7 , -NR ^A7 C(O)OR ^B7 , -NR ^A7 C(O)NR ^A7 R ^B7 , -NR ^A7 C(S)NR ^A7 R ^B7 , -NR ^A7 C(=NR ^E7 )NR ^A7 R ^B7 , -S(O) _r R ^A7 , -S(O)(=NR ^E7 )R ^B7 、-N=S(O)R ^A7 R ^B7 、-S(O) ₂ OR ^A7 、-OS(O) ₂ R ^A7 、-NR ^A7 S(O) _r R ^B7 、-NR ^A7 S(O) (=NR ^E7 )R ^B7 , -S(O) _r NR ^A7 R ^B7 , -S(O)(=NR ^E7 )NR ^A7 R ^B7 , -NR ^A7 S(O) ₂ NR ^A7 R ^B7 , -NR ^A7 S(O)(=NR ^E7 )NR ^A7 R ^B7 , -P(O)R ^A7 R ^B7 and -P(O)(OR ^A7 )(OR ^B7 ), wherein each of alkyl, alkenyl, alkynyl, Cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _{2 -10} alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, Aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A8 R ^B8 , -OR ^A8 , -C(O)R ^A8 、-C(=NR ^E8 )R ^A8 、-C(=N-OR ^B8 )R ^A8 、-C(O)OR ^A8 、-OC(O)R ^A8 、-C(O)NR ^A8 R ^B8 、- NR ^A8 C(O)R ^B8 、-C(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 C(=NR ^E8 )R ^B8 、-OC(O)NR ^A8 R ^B8 、-NR ^A8 C(O) OR ^B8 , -NR ^A8 C(O)NR ^A8 R ^B8 , -NR ^A8 C(S)NR ^A8 R ^B8 , -NR ^A8 C(=NR ^E8 )NR ^A8 R ^B8 , -S(O) _r R ^A8 , -S(O)(=NR ^E8 )R ^B8 , -N=S(O)R ^A8 R ^B8 , -S(O) ₂ OR ^A8 , -OS(O) ₂ R ^A8 , -NR ^A8 S(O) _r R ^B8 、-NR ^A8 S(O)(=NR ^E8 )R ^B8 、-S(O) _r NR ^A8 R ^B8 、-S(O)(=NR ^E8 )NR ^A8 R ^B8 、-NR ^A8 S( O) ₂ NR ^A8 R ^B8 , -NR ^A8 S(O)(=NR ^E8 )NR ^A8 R ^B8 , -P(O)R ^A8 R ^B8 and -P(O)(OR ^A8 )(OR ^B8 ), where Each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^{X 8} ; R is selected from hydrogen, Halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, Heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A9 R ^B9 , -OR ^A9 , -C(O)R ^A9 , -C(=NR ^E9 )R ^A9 , -C(=N-OR ^B9 )R ^A9 , -C(O)OR ^A9 , -OC(O)R ^A9 , -C(O)NR ^A9 R ^B9 , -NR ^A9 C(O)R ^B9 , -C(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )R ^B9 , -OC(O)NR ^A9 R ^B9 , -NR ^A9 C(O)OR ^B9 , -NR ^A9 C(O)NR ^A9 R ^B9 , -NR ^A9 C(S)NR ^A9 R ^B9 , -NR ^A9 C(=NR ^E9 )NR ^A9 R ^B9 , -S(O) _r R ^A9 , -S(O)(=NR ^E9 )R ^B9 , -N=S(O)R ^A9 R ^B9 , -S(O) ₂ OR ^A9 , -OS(O) ₂ R ^A9 , -NR ^A9 S(O) _r R ^B9 , -NR ^A9 S(O)(=NR ^E9 )R ^B9 , -S(O) _r NR A9 R ^B9 , ^-S (O)(=NR ^E9 )NR ^A9 R ^B9 , -NR ^A9 S(O) ₂ NR ^A9 R ^B9 , -NR ^A9 S(O)(=NR ^E9 )NR ^A9 R ^B9 , -P(O)R ^A9 R ^B9 and -P(O )(OR ^A9 )(OR ^B9 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by at least one independently selected from R ^X9 The substituent replaces; Wherein, when X ¹ is CH, X ² is selected from N, CH and CF, X ³ and X ⁴ are independently selected from N or CH, formula (I)

Part of the structure is

, R ^B1 is selected from hydrogen and C _1-4 alkyl, the formula (I)

Part of the structure is not

, wherein L, Q ¹ , Q ² , R ¹ , R ² , R ³ , R ⁴ , m and n are as defined in formula (I); each R ^A0 is independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl _- C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, Aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; each R ^A1 and R ^B1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl , _{C 2-10} alkynyl, C 3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _{1- 4} Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy Group, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X1 ; or " ^RA1 and R ^B1 " together with single or multiple atoms connected to them together form a 4-12 membered heterocycle containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 Substituents from R ^X1 are substituted; each R ^A2 and R ^B2 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, Heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X2 ; or " ^RA2 and R ^B2 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional independently selected from oxygen, A 4-12 membered heterocyclic ring of heteroatoms of sulfur, nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X2 ; each R ^A3 and R ^B3 independently selected From hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _{1- 10} alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Each of the alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl, and heteroaryl groups is unsubstituted or substituted by at least one substituent independently selected from R ^X3 ; or "R ^A3 and R ^B3 "together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the The ring can be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X3 ; each R ^A4 and R ^B4 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 Alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X4 ; or " ^RA4 and R ^B4 " together together with the single or multiple atoms to which they are attached Consists of a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X4 is replaced by a substituent; each R ^A5 and R ^B5 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3 -10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, hetero Aryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or Substituted by at least one substituent independently selected from R ^X5 ; or " ^RA5 and R ^B5 " together with single or multiple atoms connected to them form a substituent containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X5 ; each R ^A6 and R ^B6 are independently selected from Hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 Alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each Alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X6 ; or "R ^A6 and R ^B6 ”together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring may be unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X6 ; each R ^A7 and R ^B7 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkane Base, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, Heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X7 ; or " ^RA7 and R ^B7 " together together form a single or multiple atoms connected to them A 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may be unsubstituted or replaced by 1, 2 or 3 heteroatoms selected from R ^X7 is replaced by a substituent; each R ^A8 and R ^B8 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{3- 10} cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl is unsubstituted or replaced by At least one substituent independently selected from R ^X8 is substituted; or " ^RA8 and R ^B8 " together with single or multiple atoms connected to them form a group containing 0, 1 or 2 additional substituents independently selected from oxygen, sulfur, A 4-12 membered heterocyclic ring of nitrogen and phosphorus heteroatoms, the ring may be unsubstituted or substituted with 1, 2 or 3 substituents selected from R ^X8 ; each R ^A9 and R ^B9 are independently selected from hydrogen , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkane Oxygen, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl R, alkenyl, alkynyl, cycloalkyl, alkoxy, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X9 ; or "R ^A9 and R ^B9 ”together together with the single or multiple atoms connected to them form a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, the ring can be is unsubstituted or substituted by 1, 2 or 3 substituents selected from R ^X9 ; each R ^C0 and R ^D0 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl -C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is Unsubstituted or substituted by at least one substituent independently selected from R ^X0 ; or "R ^C0 and R ^D0 "together together with the single or multiple carbon atoms to which they are attached contain 0, 1 or 2 substituents independently selected from oxygen , a 3-12 membered ring of heteroatoms of sulfur and nitrogen, which ring may be unsubstituted or substituted by 1, 2 or 3 R ^X0 groups; each of R ^E1 , R ^E2 , R ^E5 , R ^E6 , R ^E7 , R ^E8 and R ^E9 are independently selected from hydrogen, C _1-10 alkyl, CN, NO ₂ , -OR ^a1 , -SR ^a1 , -S(O) _rR ^a1 , -C(O)R ^a1 , C(O)OR ^a1 , -C(O)NR ^a1 R ^b1 , and -S(O) _r NR ^a1 R ^b1 ; each of R ^X0 , R ^X1 , R ^X2 , R ^X3 , R ^X4 , R ^X5 , R ^X6 , R ^X7 , R ^X8 and R ^X9 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl -C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl , Halogen, CN, -NO ₂ , -(CR ^c1 R ^d1 ) _t NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t OR ^b1 , -(CR ^c1 R ^d1 ) _t C(O)R ^a1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(=N-OR ^b1 )R ^a1 , -(CR ^c1 R ^d1 ) _t C(O)OR ^b1 ,- (CR ^c1 R ^d1 ) _t OC(O)R ^b1 , -(CR ^c1 R ^d1 ) _t C(O)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)R ^b1 , -( CR ^c1 R ^d1 ) _t C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t OC(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)OR ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C(O)NR ^a1 R ^b1 、-(CR ^c1 R ^d1 ) _t NR ^a1 C (S)NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t N=S(O)R ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) ₂ OR ^b1 , -(CR ^c1 R ^d1 ) _t OS(O) ₂ R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) _r R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(= NR ^e1 )R ^b1 , -(CR ^c1 R ^d1 ) _t S(O) _r NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) ₂ NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 S(O)(=NR ^e1 )NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t P( O)R ^a1 R ^b1 and -(CR ^c1 R ^d1 ) _t P(O)(OR ^a1 )(OR ^b1 ), wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; each R ^a1 and R ^b1 are independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl- C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or substituted by at least one substituent independently selected from ^RY ; or R ^a1 and R ^b1 together with the single or multiple atoms connected to them constitute 0, 1 or 2 additional independently selected from oxygen, sulfur , a 4-12 membered heterocyclic ring of heteroatoms of nitrogen and phosphorus, which ring may be optionally substituted by 1, 2 or 3 ^RY groups; each R ^c1 and R ^d1 are independently selected from hydrogen, halogen, C _{1 -10} alkyl, C _2-10 alkenyl, C 2-10 alkynyl _, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl- C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl , heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from ^RY ; or R ^c1 and R ^d1 together, together with the single or multiple carbon atoms attached to them, constitute a 0, 1 or 2 3-12 membered rings of heteroatoms independently selected from oxygen, sulfur and nitrogen, which rings may be optionally substituted with 1, 2 or 3 ^RY groups; each R ^e1 is independently selected from Hydrogen, C _1-10 alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, CN, NO ₂ , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -C(O)R ^a2 , -C(O)OR ^a2 , -S(O) _rNR ^a2 R ^b2 and -C(O)NR ^a2 R ^b2 ; each ^RY is independently selected from C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl -C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl, heteroaryl-C _1-4 alkyl, halogen, CN, -NO ₂ , -NR ^a2 R ^b2 , -OR ^a2 , -SR ^a2 , -S(O) _r R ^a2 , -S(O) ₂ OR ^a2 , -OS(O) ₂ R ^b2 , -S(O) _r NR ^a2 R ^b2 , -P(O )R ^a2 R ^b2 , -P(O)(OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t OR ^b2 , -(CR ^c2 R ^d2 ) _t SR ^b2 , -(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -(CR ^c2 R ^d2 ) _t P(O)R ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t P(O) (OR ^a2 )(OR ^b2 ), -(CR ^c2 R ^d2 ) _t CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C (O)R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 CO ₂ R ^b2 , -(CR ^c2 R ^d2 ) _t OC(O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 C( O)NR ^a2 R ^b2 , -(CR ^c2 R ^d2 ) _t NR ^a2 SO ₂ NR ^a2 R ^b2 , -NR ^a2 (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -O(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -S(O) _r (CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)R ^a2 , -C(O)(CR ^c2 R ^d2 ) _t OR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t NR ^a2 R ^b2 , -C(O)(CR ^c2 R ^d2 ) _t SR ^b2 , -C(O)(CR ^c2 R ^d2 ) _t S(O) _r R ^b2 , -CO ₂ R ^b2 , -CO ₂ (CR ^c2 R ^d2 ) _t C(O)NR ^a2 R ^b2 , -OC(O)R ^a2 , -CN, -C(O )NR ^a2 R ^b2 , -NR ^a2 C(O)R ^b2 , -OC(O)NR ^a2 R ^b2 , -NR ^a2 C(O)OR ^b2 , -NR ^a2 C(O)NR ^a2 R ^b2 , -NR ^a2 S(O) _r R ^b2 , -CR ^a2 (=N-OR ^b2 ), -C(=NR ^e2 )R ^a2 , -C(=NR ^e2 )NR ^a2 R ^b2 , -NR ^a2 C(=NR ^e2 )NR ^a2 R ^b2 , -CHF ₂ , -CF ₃ , -OCHF ₂ and -OCF ₃ , wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is not Substituted or by at least one member independently selected from hydroxyl, CN, amino, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _{1- 10} alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _{1 -10} alkyl) amino substituent substitution; each R ^a2 and R ^b2 independently selected from hydrogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkane Group, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio , C _1-10 alkylamino, C _3-10 cycloalkylamino, di(C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _{1 -4} alkyl, heteroaryl and heteroaryl-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, ring Alkylthio, alkylamino, cycloalkylamino, heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one, independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl radical, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkane Sulfuryl, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^a2 and R ^b2 together together with single or multiple atoms constitute a 4-12 membered heterocyclic ring containing 0, 1 or 2 additional heteroatoms independently selected from oxygen, sulfur, nitrogen and phosphorus, which ring may optionally be replaced by 1 or 2 heteroatoms independently selected from halogen, CN , C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C Substituents of _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl) amino; each R ^c2 and R ^d2 are independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, C _1-10 alkylamino, C _{3- 10} cycloalkylamino, two (C _1-10 alkyl) amino, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl and heteroaryl Group-C _1-4 alkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, cycloalkoxy, alkylthio, cycloalkylthio, alkylamino, cycloalkylamino, Heterocyclyl, aryl and heteroaryl are unsubstituted or replaced by at least one member independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _{3- 10} cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and two (C _1-10 alkyl) amino substituents are substituted; or R ^c2 and R ^d2 together with the single or multiple carbon atoms connected to them constitute 0, 1 or 2 independent A 3-12 membered ring of heteroatoms selected from oxygen, sulfur and nitrogen, which may optionally be replaced by 1 or 2 members independently selected from halogen, CN, C _1-10 alkyl, C _2-10 alkenyl, C _2-10 alkynyl, C _3-10 cycloalkyl, hydroxyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, C _1-10 alkylthio, C _3-10 cycloalkylthio, Amino, C _1-10 alkylamino, C _3-10 cycloalkylamino and di(C _1-10 alkyl)amino are substituted by substituents; each R ^e2 is independently selected from hydrogen, CN, NO ₂ , C _1-10 Alkyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, C _1-10 alkoxy, C _3-10 cycloalkoxy, -C(O)C _{1 -4} alkyl, -C(O)C _3-10 cycloalkyl, -C(O)OC _1-4 alkyl, -C(O)OC _3-10 cycloalkyl, -C(O)N( C _1-4 alkyl) ₂ , -C(O)N(C _3-10 cycloalkyl) ₂ , -S(O) ₂ C _1-4 alkyl, -S(O) ₂ C _3-10 ring Alkyl, -S (O) ₂ N (C _1-4 alkyl) ₂ and -S (O) ₂ N (C _3-10 cycloalkyl) ₂ ; m is selected from 0, 1, 2, 3 and 4 n is selected from 0, 1, 2, 3 and 4; each r is independently selected from 0, 1 and 2; each t is independently selected from 0, 1, 2, 3 and 4; and each u is independently selected from 0 , 1, 2, 3 and 4. The compound or pharmaceutically acceptable salt ^thereof as claimed in item 1, wherein R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, CN, NO ₂ , -NR ^A6 R ^B6 and -OR ^A6 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X6 , preferably, R ⁶ is selected from Hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy, F, Cl, Br, -CN, - _NO2 , -OH and _-NH2 . The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-2, wherein R ⁷ is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, CN, NO ₂ , -NR ^A7 R ^B7 and -OR ^A7 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X7 , Preferably, R ^is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy, F, Cl, Br, -CN, _-NO2 , -OH and _-NH2 . The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-3, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, CN, NO ₂ , -NR ^A8 R ^B8 and -OR ^A8 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X8 , Preferably, R ^is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy, F, Cl, Br, -CN, _-NO2 , -OH and _-NH2 . The compound or pharmaceutically acceptable salt thereof as claimed in any one of items 1-4, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, CN, NO ₂ , -NR ^A9 R ^B9 and -OR ^A9 , wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X9 , Preferably, ^R is selected from hydrogen, methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl, trifluoroethyl, cyclopropyl, methoxy, ethoxy, F, Cl, Br, -CN, _-NO2 , -OH and _-NH2 . The compound or pharmaceutically acceptable salt thereof as described in any one of claim items 1-5, wherein formula (I)

Some structures are selected from

,

,

,

,

,

,

,

,

and

. The compound or pharmaceutically acceptable salt thereof as claimed in any one of items 1-6, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, heteroaryl , heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A5 R ^B5 , -OR ^A5 , -C(O)R ^A5 , -C(O)OR ^A5 , -OC(O)R ^A5 、-C(O)NR ^A5 R ^B5 、-NR ^A5 C(O)R ^B5 、-OC(O)NR ^A5 R ^B5 、-NR ^A5 C(O)OR ^B5 、-NR ^A5 C(O)NR ^A5 R ^B5 , -NR ^A5 C(S)NR ^A5 R ^B5 , -S(O) _r R ^A5 , -S(O) ₂ OR ^A5 , -OS(O) ₂ R ^A5 , -NR ^A5 S(O) _r R ^B5 and -S(O) _r NR ^A5 R ^B5 , wherein each alkyl, alkenyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is unsubstituted or is independently selected from R by at least one ^X5 is substituted by a substituent, preferably, ^R is selected from hydrogen, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, ethyl, fluoroethyl, difluoroethyl, trifluoroethyl methoxy, ethoxy, isopropyl, methoxymethyl, cyclopropyl and phenyl. The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-7, wherein Q ¹ is heterocyclyl, preferably, Q ¹ is selected from

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

and

. The compound or pharmaceutically acceptable salt thereof as claimed in any one of items 1-8, wherein each R ² is independently selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 cycloalkyl, C _3-10 cycloalkyl-C _1-4 alkyl, heterocyclyl, heterocyclyl-C _1-4 alkyl, aryl, aryl-C _1-4 alkyl, Heteroaryl, heteroaryl-C _1-4 alkyl, CN, NO ₂ , -NR ^A2 R ^B2 , -OR ^A2 , -C(O)R ^A2 , -C(O)OR ^A2 , -OC(O )R ^A2 , -C(O)NR ^A2 R ^B2 , -NR ^A2 C(O)R ^B2 , -OC(O)NR ^A2 R ^B2 , -NR ^A2 C(O)OR ^B2 , -NR ^A2 C(O )NR ^A2 R ^B2 , -NR ^A2 C(S)NR ^A2 R ^B2 , -S(O) _r R ^A2 , -S(O)(=NR ^E2 )R ^B2 , -S(O) ₂ OR ^A2 , - OS(O) ₂ R ^A2 , -NR ^A2 S(O) _r R ^B2 , -S(O) _r NR ^A2 R ^B2 and -NR ^A2 S(O) ₂ NR ^A2 R ^B2 , where each alkyl, alkene R, cycloalkyl, heterocyclyl, aryl and heteroaryl are unsubstituted or substituted by at least one substituent independently selected from R ^X2 , preferably, each ^R2 is independently selected from hydrogen, F, Cl, Br, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, ethyl, difluoroethyl, trifluoroethyl, isopropyl, cyclopropyl, methoxy, ethoxy base, methoxymethyl,

, -OC(O) _CH3 , CN, _NO2 , _-NH2 and -OH. The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-9, wherein the compound of formula (I)

Some structures are selected from

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

,

and

. The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-10, wherein L is selected from chemical bond, -CR ^C0 R ^D0 -, -(CR ^C0 R ^D0 ) _u O(CR ^C0 R ^D0 ) _t -, (CR ^C0 R ^D0 ) _u NR ^A0 (CR ^C0 R ^D0 ) _t - and -(CR ^C0 R ^D0 ) _u S(CR ^C0 R ^D0 ) _t -, preferably, L is selected from chemical bonds, -CH ₂ -, -O-, -NH-, and -S-. The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-11, wherein Q ² is selected from 5-12 membered heterocyclyl, aryl and heteroaryl, preferably, Q ² is selected from

,

,

,

,

,

,

,

and

. The compound or pharmaceutically acceptable salt thereof as claimed in any one of items 1-12, wherein each R ¹ is independently selected from hydrogen, halogen, C _1-10 alkyl, C _3-10 cycloalkyl, Heterocyclyl, heterocyclyl-C _1-4 alkyl, heteroaryl, CN, NO ₂ , -NR ^A1 R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 , -C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 , -NR ^A1 C(O)R ^B1 , OC(O)NR ^A1 R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -S(O) _r NR ^A1 R ^B1 , -NR ^A1 S(O) _r R ^B1 , -NR ^A1 S(O) ₂ NR ^A1 R ^B1 and -NR ^A1 C( S) NR ^A1 R ^B1 , wherein each alkyl, cycloalkyl, heterocyclyl and heteroaryl is unsubstituted or substituted by at least one substituent independently selected from R ^X1 , preferably, each R ¹ independently selected from methyl, ethyl, isopropyl, cyclopropyl, F, Cl,

,

,

,

,

,

,

,

,

,

,

, CN, NO ₂ , -NR ^A1 R ^B1 , -NR ^A1 C(O)R ^B1 , -NR ^A1 C(O)OR ^B1 , -NR ^A1 C(O)NR ^A1 R ^B1 , -NR ^A1 S(O ) _r R ^B1 , -OR ^A1 , -C(O)R ^A1 , -C(O)OR ^A1 , -OC(O)R ^A1 , -C(O)NR ^A1 R ^B1 , -C(O)NR ^A1 S(O) _r R ^A1 , -C(O)NR ^A1 S(O) _r NR ^A1 R ^B1 , -C(O)NR ^A1 S(O)(=NR ^E1 )R ^B1 and -S(O) _r NR ^A1 R ^B1 , where each of methyl, ethyl, isopropyl, cyclopropyl,

,

,

,

,

,

,

,

,

,

and

is unsubstituted or substituted with at least one substituent independently selected from ^RX1 . The compound or pharmaceutically acceptable salt thereof as claimed in any one of items 1-13, wherein each R ^X1 is independently selected from C _1-10 alkyl, C _3-10 cycloalkyl, C _3-10 Cycloalkyl-C _1-4 alkyl, halogen, CN, NO ₂ , -(CR ^c1 R ^d1 ) _t NR ^a1 R ^b1 , -(CR ^c1 R ^d1 ) _t OR ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)R ^b1 , -(CR ^c1 R ^d1 ) _t NR ^a1 C(O)OR ^b1 and -(CR ^c1 R ^d1 ) _t NR ^a1 S(O) _r R ^b1 , where each alkyl and Cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^Y , preferably, each R ^X1 is independently selected from methyl, difluoromethyl, trifluoromethyl, ethyl, difluoroethyl radical, trifluoroethyl, isopropyl, tert-butyl, cyclopropyl, methoxy, ethoxy, F, -CN, -NH ₂ , -NHCH ₃ , -NHCH ₂ CH ₃ , -NHC(O )CH ₃ , -NHC(O)OCH ₃ ,

,

,

,

and

. The compound or pharmaceutically acceptable salt thereof as described in any one of claim items 1-14, wherein formula (I)

Some structures are selected from

,

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and

. The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-15, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, CN, _-NH and -OH, wherein each of alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^X3 , preferably, ^R3 is selected from hydrogen and methyl, wherein methyl is unsubstituted or substituted with at least one substituent independently selected from R ^X3 . The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-16, wherein ^R is selected from hydrogen, halogen, C _1-10 alkyl, C _2-10 alkenyl, C _3-10 Cycloalkyl, CN, -NH ₂ and -OH, wherein each alkyl, alkenyl and cycloalkyl is unsubstituted or substituted by at least one substituent independently selected from R ^{X 4} , preferably, wherein R ⁴ is selected from selected from hydrogen and methyl, which is unsubstituted or substituted with at least one substituent independently selected from R ^X4 . The compound or pharmaceutically acceptable salt thereof as described in any one of claims 1-17, wherein R ³ and R ⁴ form a C _3-10 cycloalkyl group together with the atoms connected to them or contain 1, 2 Or a 4-8 membered heterocyclic group with 3 heteroatoms, wherein the heteroatoms are independently selected from oxygen, sulfur, nitrogen and phosphorus, and the ring is unsubstituted or substituted by 1, 2 or 3 R ^X3 substituents, preferably, wherein ^R3 and ^R4 together with the atoms to which they are attached form a cycloalkyl ring which is unsubstituted or substituted with 1, 2 or 3 ^RX3 substituents. A compound selected from:

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, and pharmaceutically acceptable salts thereof. A pharmaceutical composition, comprising the compound or a pharmaceutically acceptable salt thereof according to any one of claims 1-19, and at least one pharmaceutically acceptable carrier. A method for treating, improving or preventing a condition in response to inhibiting PARP1, comprising administering an effective amount of the compound or a pharmaceutically acceptable salt thereof as described in any one of claims 1-19 to an individual in need thereof, or at least A pharmaceutical composition thereof, and optionally in combination with a second therapeutic agent. Use of the compound as described in any one of claims 1-19 or a pharmaceutically acceptable salt thereof in the preparation for treating abnormal cell proliferation diseases. Use of the compound or a pharmaceutically acceptable salt thereof as claimed in item 22, wherein abnormal cell proliferation diseases include but not limited to, breast cancer, ovarian cancer, bladder cancer, uterine cancer, prostate cancer, testicular cancer, lung cancer (including NSCLC, SCLC, squamous cell carcinoma or adenocarcinoma), esophageal cancer, head and neck cancer, colorectal cancer, renal cancer (including RCC), liver cancer (including HCC), pancreatic cancer, gastric (i.e. gastric) cancer, thyroid cancer, Chronic lymphocytic leukemia (CLL), lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myelogenous leukemia and myeloma.