TWI222445B - Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade - Google Patents

Abstract

The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Description

A7

1222445 V. Description of the invention (1) Scope of the invention The present invention is in the field of anticoagulant therapy, and specifically, it relates to compounds, compositions and methods for preventing and treating thrombotic symptoms, such as coronary arteries and Cerebrovascular disease. More specifically, the present invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds, which inhibit serine proteases of the clotting step reaction. BACKGROUND OF THE INVENTION The physiological system is to control the flow of blood in mammals. 1 > W et al .: Anticoagulant, thrombolytic and platelet destroying drugs, edited by Hardman, J.G. and Limbird, L.E. Goodman & Gilman, Pharmacological Basis of Therapeutics, 9th Edition, New York, McGraw -Hill Books, 1996, p. 1341_m3]. The blood must remain fluid within the vascular system, and it must be able to stop bleeding quickly and stop the loss of blood from the injured blood vessel. When platelets initially adhere to macromolecules in the endothelial area beneath damaged and / or injured blood vessels, they stop bleeding or clot. These platelets will agglomerate to form a main tampon, and stimulate local activation of plasma coagulation factors, resulting in the production of fibrin clots to strengthen the platelets that have been aggregated. Plasma coagulation factors include factors 11, 乂 ¥ 11, ^ 11, 1 ^, and ^ 1 and: 501; it is also called protease zymogen. These agglutination factors or protease zymogens are activated by serine proteases, leading to agglomeration in a so-called "coagulation step reaction" or chain reaction [Handin, R · L: bleeding and thrombosis, edited by Wilson J. et al. Harrison Internal Medicine Principles, 12th ed., New York, McGraw-Hill Books, Inc .: 1991, p. 350]. Agglomeration or clot occurs in two ways and through different paths. An internal or contact route that will lead from XII to Xlla to XIa to -4-This paper rule applies to China National Standard (CNS) A4 (210 X 297 mm) -------- ^ --- ------ (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 Printed by the Employee Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5- A7 _____ B7 V. Description of the invention ( 2) IXa 'and cause X to be converted into Xa. Xa with factor va will convert thrombin (π) to thrombin (na), resulting in the conversion of fibrinogen to fibrin. Polymerization of fibrin can cause fibrin clots. An external pathway is initiated by Xa, which is converted into vna by the condensation factor γπ. The presence of tissue factor and Vila ’will accelerate Xa formation in the presence of calcium ions and phospholipids. The formation of Xa causes thrombin, fibrin, and fibrin clots as described above. The presence of one or more of these many different agglomeration factors, and the two different clotting pathways enable effective selective control and a better understanding of part of the agglomeration or clotting process. Although the clot caused by the damage to blood vessels is an important physiological process for mammals (such as humans), the clot may also cause illness. When platelets aggregate and / or fibrin clots block (ie, occlude) blood vessels, they cause a pathological process called thrombosis. Arterial thrombosis may cause hemorrhagic necrosis of the tissue supplied by the arteries. When thrombosis occurs in the coronary arteries, it can cause myocardial infarction or heart attack. Thrombosis that occurs in veins can cause edema and inflammation in tissues drained from the vein. Deep vein thrombosis can be complicated by pulmonary vascular embolism. Preventing or treating blood clots can be therapeutically useful by inhibiting platelet aggregation, inhibiting fibrin formation, inhibiting thrombosis, inhibiting plug formation, and treating or preventing restless colic, Colic angina, myocardial infarction, transient hemorrhagic invasion, anterior atrial fibrillation, thrombotic stroke, plug stroke, deep vein thrombosis, disseminated intravascular agglomeration, clear accumulation of fibrin, and reocclusion of blood vessels Or restenosis. Private Paper Standard Turning Standard (CNS) A4 Specification ⑽χ 297 Public Love) -------- Order --------- Line · (Please read the precautions on the back before filling this page) Economy Printed by the Consumer Cooperatives of the Ministry of Intellectual Property Bureau 1222445 A7 __ B7 V. Description of the Invention (3) There have been several reports about non-peptidic and peptidyl pyrimidinone compounds, which are presumed to exist in the coagulation step reaction or clotting process Inhibitor of coagulation factors. In PCT Patent Application WO / 47876 by Van Boeckel et al., Peptide 6-alkylpyridone and 2-alkylpyrimidone are described as antithrombotic compounds. In Zhu and Scarborough, PCT Patent Application WO 98/16547, 3- (N-heterocyclylamino) -4,5,6_-substituted pyridone acetoacetamide, and 2,4-substituted 5- (N-heterocyclylamino) -pyrimidinone acetoamide, which contains amidamine substituents, and has activity against mammalian factor Xa. In U.S. Patent No. 5,656,645 to Tamura et al., 4,5-, 6-substituted 3-aminopyridone-acetamidamine, 1,6-substituted 5-aminouracilylacetamidamine, and 2,4-substituted 5-aminopyrimidinone-acetamidamine, which contains amidamine substituents, has a formamidine functional group, and has thrombin activity. In U.S. Pat. No. 5,658,930 to Tamura et al., 4,5,6-substituted 3-aminopyridone-acetamidamine, 1,6-substituted 5-aminouracilylacetamidamine are described once again, And 2,4-substituted 5-aminopyrimidinone-acetamidamine, which contains amidamine substituent, has a formamidine functional group, and has activity on thrombin. In PCT patent applications 96/18644 and 97/46207 to Tamura et al., 4,5,6-substituted 3-aminopyridone acetofluorenylamine and 1,6-substituted 5-amino groups are further described. Uracilyl-acetamidine, and 2,4-substituted 5-amino-pyrimidinone acetamidine, which contains amidoamine substituents, has a formic acid functional group, and has thrombin activity. In PCT patent application WO 98/09949 by Suzuki et al., A 2-heterocyclylacetamido derivative of 1,2-diketone is described and it is reported that it inhibits proteases, especially chymotrypsin inhibitors. Summary of the Invention--6 Fine paper size applicable to China National Standard (CNS) A4 specification (210 X 297 public love) -------- Order --------- line (please first (Read the notes on the back and fill out this page) U22445 A7

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

One of the items of the present invention is to provide anti-coagulation therapy, and it has a general structure;

Formula (I). Another aspect of the present invention is to provide a method for preventing and treating thrombotic symptoms, such as coronary artery disease, cerebrovascular disease, and other coagulation-related disorders. Such thrombotic symptoms are prevented and treated by administering an effective amount of a compound of formula (I) to a patient in need of treatment. Various other objects and advantages of the present invention will become apparent from the following description of the present invention. DESCRIPTION OF THE INVENTION The present invention relates to the type of compounds containing substituted polycyclic aryl and heteroaryl pyrimidines, which are beneficial to anticoagulant therapy for the treatment and prevention of various symptoms of thrombosis, including coronary and cerebrovascular diseases, such as As shown in formula ①: .R2 (I) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ---- l · --- Order --------- line # (Please read the seven notes on the back? Matters before filling this page) 1222445 A7 B7 V. Description of the invention (5) or its pharmaceutically acceptable salt, where: J is selected from the group consisting of 0 and S; U, ^ ^. CH.R ^ n.r6, r6 ^ ^ ^ ^ ^…, has a chain length of ... atoms, and is connected to a bond of a substituent ... The substituent is selected from the group consisting of R4a, R4bR39, R40, R5, Ri ^ Ri5 , A ^ forms a heterocyclic ring having 5 to 8 contiguous members;, j is optionally selected from the group consisting of coffee 6 and wealth 6, where r6 is a linear part and has! A chain length of 4 to 4 atoms, connected to the bond point of ya and the two to form a heterocyclyl ring with 5 to 8 adjacent members; J is selected from the group consisting of CH_R6 and Choi 6, where r6 is linear Shao Fen, having a chain length of 1 to 4 atoms, is connected to both ruler ^ and ruler ^: two nodes to form a heterocyclic ring having 5 to 8 adjacent members; B is formula (V) ··

R 34, 33 R ″ 1 p 3 〇j- Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economy (V) where D1, D2, J1, J2 and K1 are independently selected from the group consisting of c, N, 0, s and covalent The bond is subject to the condition that no more than one can be a covalent bond, and no more than one of D1, D2, jl, j2, and magic is 0, 1) 1, 1) 2, 1, 1, 2 and] ^ 1 More than one is 8, when 〇1, 02, ^ 2 and two of them are 〇 and 8, 〇1, 〇2, 11,】 2 and magic one -8-This paper standard applies Chinese national standard ( CNS) A4 specification (21 × X 297 printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Public Economics and Economics 1224245 A7 ___ B7 V. Description of the invention (6) must be a covalent bond, and D1, D2, J1, J2 and K1 More than four are N, with the proviso that 1132, 1133, 1134, 1135, and 1-36 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the second oxygen Valence properties; R36 is independently selected from the group consisting of hydrogen, acetamido, self-acetylacetamido, methylamido, guanidino, dialkylfluorene, trialkylrust, dialkylphosphonium alkyl, carboxyl, Heteroaralkylthio, Heteroaralkyloxy Alkyl, cycloalkylamino, fluorenylalkyl, fluorenylalkoxy, arylfluorenylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, arkenyl, aralkynyl, hetero Cyclic group, perfluorinated aralkyl group, aralkylsulfonyl group, arylene group, fluorenyl group, arylene group, fluorenylene group, arylene group, fluorenylene group, #cycloalkyl group, self ring Alkenyl, cycloalkylsulfinamidinyl, cycloalkylsulfinamidinylalkyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, heteroarylamino, N-heteroarylamino -N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkoxy, alkoxy, alkoxyalkyl, autoalkoxyalkyl, heteroarylalkoxy, cycloalkane Oxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, hypocycloalkyldioxy, autocycloalkoxy, and cyclocycloalkoxy Alkyl, alkenyloxy, alkenyloxy, hydroxy, amine, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthio Alkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroarylalkoxyalkyl, Alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfinylalkyl, heteroarylsulfinylalkyl, heteroarylsulfinylalkyl Base, alkylsulfonyl, sulfonylsulfanylalkyl, self-alkylsulfinylsulfanylalkyl, i-alkylsulfonylalkyl ___- 9- This paper size applies to China National Standard (CNS) A4 Specifications (210 X 297 mm) -------------------- Order --------- Line (Please read the phonetic on the back? Matters before filling in (This page) 1222445

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the Invention (7), Alkylsulfonamido, Alkylsulfosulfanyl, Alkylsulfonamido, Monoalkylammoniumsulfosulfanyl, Alkyl sulfonium sulfonyl, monoaryl sulfonyl sulfonyl, aryl sulfonyl sulfonyl, diaryl sulfonyl sulfonyl, monoalkyl monoaryl sulfonyl sulfonyl, aromatic Sulfenylsulfenyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkylsulfanyl, Alkenyl, arylfluorenyl, heteroarylfluorenyl, aralkylfluorenyl, heteroaralkylfluorenyl, alkylene, alkyl, alkenyl, alkynyl, alkenyl, alkenyloxy, alkylene Dioxy, alkylidene dioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower carbocycloalkylalkyl, lower carbocycloalkenylalkyl, halo, south alkyl, halo Fluorenyl, alkynyl, aryl, alkynyl, aryl, aryl, phenyl, phenyl, fe, phenyl, amine, peraryl, aryl, aryl, aryl, aryl, aromatic Alkyl, aryloxy, aryloxy, aryloxy, saturated heterocycle , Partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, aralkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl , Alkoxycarbonyl, alkoxycarboxyamido, alkylamidoamino, amino, amino, amino, etc., alkoxyalkyl, alkoxycarbonyl, carboxyl, Aryloxycarbonyl, benzylamino, carboxyamido, cyano, #oxyalkyl, phosphono, phosphono, diaryloxyphosphonic acid, and diarylalkoxyphosphine Acid-based alkyl groups; feet 16,1119, "2, feet 3 ^ 34,] 135 and feet 36 are independent furnaces as the case may be, with the proviso that no more than one of R16 and R19 is Qb at the same time, and the furnace is Qbe R32 and RD 'and R34, ruler "and" ^ and r35 and r36, are independently selected as appropriate to form spacer pairs, wherein the spacer pairs are used together to form a linear part with 3 to 6 adjacent atoms Copies, connect the spacer to the -------------------- order --------- line (Please read the precautions on the back before filling this page ) -10- 1222445 A7 B7 V. Description of the invention (8 key nodes of members, Form a ring, occupy 6 ke trench coat, selected from heteroaryl rings including 5 to 8 adjacent cardiocyclic alkenyl rings, partially saturated heterocyclic rings having 5 to 8 members, and 5 to 6 adjacent members , And aryl groups, with the proviso that they do not use more than one group containing spacer pairs 32 and 33, R34 and R35, and R35 and R36; ^ '㈣ ...' heart and ... and ^ and ... It is selected with the case of series to form a spacer pair ... The pair of spacers is used to form a linear part with 3 to 6 adjacent atoms, and the pair of spacers is connected to form a read node to form a ring. Selected from the group consisting of a cycloalkenyl ring having 5 to 8 adjacent members, a partially saturated heterocyclic ring having 5 to 8 members, an aryl ring having 5 to 6 adjacent members, and an aryl group, The condition is not to use more than one group containing spacers R9 and R10, ruler ... and R &D;, R11 and R12, and R12 and R13; "", B as the formula (VI) · R33 V .34 • R,

R 32. • D— I ---------------- ^ ---- Order --------- line (please read the t-note on the back first? (This page) Printed 'r35 (VI) printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, where D3, D4, j3 and J4 are independently selected from the group consisting of CN0 and s, a d4 j3 and π. Not more than one is 0, D3, And no more than -4 in j4 are s, and no more than three in J2 are N, with the proviso that each of r32, r3'r34 and R3 5 is independently selected to maintain the tetravalent nature of carbon and the trivalent nature of nitrogen Sex-11-1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (9)%, the monovalent nature of sulfur and the divalent nature of oxygen; B is selected from the group consisting of hydrogen and trioxane, as appropriate. Silyl, C2_C8 alkyl, C3-C8 alkenyl, C3-C8 alkenyl, C3_C8 alkynyl, C2_C8 haloalkyl, and C3_C8 haloalkenyl, where each member of group 3 is at a distance of 3 pairs depending on the situation Any point where the eight junctions are high and contain 6 atoms is replaced by one or more groups including Hua 32, Hua 33, ¥ 4, Hua 35 and Hua 36; B is optionally selected from the group consisting of C3-C15 rings Alkyl, C5-C10 cycloalkenyl, C4-C12 saturated heterocyclyl, and C4-C9 Saturated heterocyclic groups, where each ring carbon is optionally substituted by R33, one ring carbon, not the ring carbon at the point of attachment of B to A, is replaced by a fluorenyl group depending on the condition of k, the condition is that no more than one ring carbon at the same time Substituted by a fluorenyl group, the ring carbon and nitrogen atom of the carbon atom adjacent to the connection point are optionally replaced by R9 or R13, and the ring carbon or nitrogen atom adjacent to the position of R9 and two atoms from the connection point are optionally replaced by R1 0 Substitute, a ring carbon or nitrogen atom that is adjacent to the position of Rl 3 and two atoms away from the connection point is replaced by Rl 2 as appropriate, and a ring carbon or nitrogen atom that is three atoms away from the connection point and is adjacent to R10 position is optionally R11 substitution, a ring carbon or nitrogen atom that is three atoms away from the connection point and adjacent to R12 position, is replaced by R3 3 as appropriate, and a ring carbon or nitrogen atom that is four atoms away from the connection point and is adjacent to R11 and R33 positions, depending on the system Case is replaced by R34; A is selected from the group consisting of covalent single bonds, (W7) rr_ (CH (R15)) pa & (CH (R15)) pa- (W7) rr, where rr is an integer selected from 0 to 1 , Pa is an integer selected from 0 to 6, and W7 is selected from the group consisting of 0, s, C (O), C (S), C (0) S, C⑸0, C (0) N (R7), C (S) N (R7), (R7) NC (0), (R7) NC (S), S (0), S (0) 2, S (0) 2N (R7), (R7) NS (0 ) 2, Se⑼,

Se (0) 2, Se (0) 2 N (R7), (R7) NSe (0) 2, P (0) (R8), N (R7) P (0) (R8), p (〇) ( r8) N_ (R7), C (NR7) N (R7), (R7) NC (NR7), (R7) NC (NR7) NR7 and N (R7), which are attached with -12- This paper size applies to Chinese national standards (CNS) A4 specification (210 x 297 mm) --------------------- Order --------- line (please read the first Note: Please fill out this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1224245 A7 ______ B7 V. Description of the invention (10) The condition is that rr and pa are not more than one at the same time. , Hydroxy, alkyl, alkenyl, aryl, aralkyl, aryloxy, alkoxy, alkenyl, alkylthio, alkylamino, arylthio, arylamino, fluorenyl, arylfluorene Radical, heteroarylfluorenyl, aralkyloxy radical, heteroarylsulfanyl radical, aryloxylanthyl radical, oxygen radical, fluorenyl radical, sulfur radical, arylthio radical Aryl, aryl oxalyl, heteroarylalkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, heteroaryl, heteroaryloxy, heteroarylamino, Heteroaralkyl, heteroaralkyloxy, Aralkylamino and heteroaryloxyalkyl; 1114, 1115, 1137, 1138, 1139, 114 (), 1141, and 1142 are independently selected from the group consisting of methylamido, hydroxylamino, hydrogen, hydroxyl, and fluorenyl , Cyano, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, aminoalkyl, fluorenyl, arylfluorenyl, heteroarylfluorenyl, heteroaryloxyalkyl, hydrogen Thio, amidino, amido, alkoxy, thiothio, arylthio, pit, fluorenyl, block, aryl, aryl, aryloxyalkyl, aralkoxyalkane Alkylalkoxy, alkylsulfinamidoalkyl, alkylsulfoamidoalkyl, aralkylthioalkyl, heteroarylalkoxythioalkyl, alkoxyalkyl, heteroaryloxy Alkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylfluorenyl, cycloalkenyl, cycloalkenylalkyl, dentane Alkyl, haloalkenyl, _cycloalkyl, halocycloalkenyl, 1¾alkoxy, from alkoxyalkyl, _alkenyloxyalkyl, halocycloalkoxy, #cycloalkoxyalkyl, Functional cycloalkenyloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl , Heteroarylalkyl, heteroarylthioalkyl, heteroarylthioalkyl, monoalkyloxyalkyl, dialkyloxycarboxyalkyl, monocyanoalkyl, dicyanoalkyl, Alkoxycarbonyl cyanoalkyl, -13- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------------— l · —order --- ------ Line φ- (Please read the phonetic on the back? Matters before filling out this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 V. Invention Description (! 1) , Alkynyl acid, alkynyl sulfenyl, alkynyl sulfonyl, aryl sulfinyl, arylsulfinylalkyl, arylsulfonyl, arylsulfinyl Aryl, aralkylsulfinyl, aralkylsulfinyl, cycloalkylene, cycloalkyl, sulfofluorenyl, cycloalkylsulfinyl, alkylene , Heteroarylsulfonylalkyl, Heteroarylsulfinyl, Heteroarylsulfonyl, Heteroarylsulfinylalkyl, Aralkylsulfinylalkyl, Arylene Alkyl, carboxyl, carboxyalkyl, alkoxycarbonyl, carboxamido, carboxamido Alkyl, aralkoxycarbonyl, trialkylsilyl, dialkoxyphosphonic acid, diarkoxyphosphonic acid, dialkoxyphosphonic acid alkyl, and diarthoxyphosphonic acid alkyl Group, with the proviso that Y and Hua 3 are independently selected from the group consisting of methylamidyl and 2 · ketomethyl; R and R 'when combined with different carbons, are used together as appropriate to form a base A group selected from the group consisting of a covalent bond, an alkylene group, a self-alkylene group, and a linear partial spacer, selected to form a ring, selected from a group including a cycloalkyl ring having 5 to 8 adjacent members, having 5 A cycloalkenyl ring of up to 8 adjacent members, and a heterocyclic group of 5 to 8 adjacent members; R and R 'when combined to different carbons are used together as appropriate to form a group selected from the group consisting of A covalent bond, an alkylene group, an alkylene group, and a linear spacer, selected to form a ring, selected from a cycloalkyl ring including 5 to 8 adjacent members, and 5 to 8 adjacent members A cycloalkenyl ring, and a heterocyclic group having 5 to 8 adjacent members; R and R15 'are used together when combined to different carbons, as appropriate To form a group selected from the group consisting of covalent bonds, alkylene groups, self-alkylene groups, and a linear spacer, selected to form a ring, selected from the group including 5 ________14_ Standard (CNS) A4 specification (21G χ 297 public love) ----------------- ^ ---- Order --------- line (Please read first Note on the back, please fill out this page again) 1222445 A7 B7 Printed by the Consumers' Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the Invention (12) Cycloalkyl ring with 8 to 8 adjacent members, cycloolefin with 5 to 8 adjacent members A base ring, and a heterocyclic group having 5 to 8 adjacent members; selected from the group consisting of NR5, 0, C (0), C (S), S, S (0), S (0) 2, 0N ( R5), P (; 0) (R8) and CR39R40; R5 is selected from the group consisting of hydrogen, hydroxyl, amine, alkyl, alkenyl, bulk, aryl, aromatic, + oxy, aromatic Alkyl, aryloxy, alkenyloxy, thiothio, arylthio, aralkyloxyalkyl, heteroaralkyloxyalkyl, aryloxyalkyl, alkoxyalkyl, alkenyloxy , Alkylthioalkyl, arylthioalkyl, arylalkoxyalkyl, heteroarylalkoxyalkyl, alkyl Sulfenylalkyl, alkylsulfoalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, alkynyl, _alkenyl, _ Cycloalkyl, halocycloalkenyl, self-alkoxyalkyl, alkenyloxyalkyl, self-cycloalkoxyalkyl, 1¾cycloalkenyloxyalkyl, heteroaryl, heteroarylalkyl , Monoalkoxymethyl group, monoclonal antibody ^ group,-* ^ fe oxo ^ group; fe group, early reading ^ amino group, monocyano group, dicyano group, and oxycarboxycyano group Base group, acid group, aryl group, heteroaryl group, heteroaryloxyalkyl group and dialkoxyphosphonoalkyl group; R39 and R40, when combined to the same carbon, are used together as appropriate To form a group selected from the group consisting of keto, thiocarbonyl, R5-N, alkylene, haloalkylene, and a linear partial spacer with 2 to 7 adjacent atoms to form a ring, Is selected from the group consisting of a cycloalkyl ring having 3 to 8 adjacent members, a cycloalkenyl ring having 3 to 8 adjacent members, and a heterocyclic ring having 3 to 8 adjacent members; M is selected from the group consisting of N and R1 -C; R2 and R1 are independently selected from ZG_Q Fluorenyl, alkyl, alkenyl and halo; -15- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---------------- -^ ---- Order --------- line (please read the phonetic on the back first? Please fill out this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1224245 A7 ---- —_____ B7____ V. Description of the invention (13) R1 is optionally selected from the group consisting of amine, aminoalkyl, alkylamino, Formamidine, guanidyl, hydroxyl, hydroxylamino, alkoxy, hydroxyalkyl, alkoxyamine, thiol, alkylthio, dialkylfluorene, trialkylphosphonium, dialkylphosphonium alkyl , Heteroarylamino, nitro, arylamino, aralkylamino, alkylfluorenyl, alkenyl, arylfluorenyl, heteroarylfluorenyl, arylsulfonyl, heteroarylsulfonyl, _Tiger Group, hydroxy S alkyl group, cyano group, and phosphonic acid group; R2 is optionally selected from the group consisting of methyl amidino, guanidino, dialkyl amidino, trialkyl scale, dialkyl amidino, heteroarylamino , Amine, nitro, alkylamino, arylamino, arylalkylamino, alkylfluorenyl, alkenyl, arylfluorenyl, heteroarylfluorenyl, arylsulfonyl, heteroarylsulfonic acid, dentate Alkali group, self-burning group, cyano group and phosphonate group; R2 and R4a, R2 and R4b, R2 and R14, and R2 and r15 are independently selected to form spacer pairs, where the spacer pairs are together Take shape A linear part having 2 to 5 adjacent atoms, connecting the bonding points of the members of the spacer pair to form a heterocyclic ring having 5 to 8 adjacent members, with the proviso that not more than one spacer pair is used at the same time , Including R2 and Rh, R2 and R4b, R2 and R14, and R2 and R15; R2 is independently selected as appropriate to form a linear part with 2 to 5 adjacent atoms, and is connected to the bond between 1143 and R4b Point to form a heterocyclyl ring having 5 to 8 adjacent members; ZG is selected from the group consisting of covalent single bonds, (CR41R42) q, where q is an integer selected from 1 to 6, (CH (R41)) g_W0_ (CH (R42)) p, wherein g and p are integers independently selected from 0 to 3, and wG is selected from the group consisting of 0, s, c (o), c (s), cc〇) o, c⑼0, C (S) S, C (0) N (R41), (R41) NC (0), C (S) N (R41), (R41) NC (S), 0C (0) N (R41), 16- M's scale is applicable to China National Standard (CNS) A4 specification (210 x 297 mm) ---- κ ---- Order --------- line (Please read the note on the back first? Matters Refill this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 __ B7 V. Description of the Invention (14) (R41) NC⑼0, SC (S) N (R41), (R41) NC⑻S, SC (0) N (R41), (R41) NC⑼S, OC (S) N (R41), (R41) NCCD0, N (R4 2) C ( 0) N (R41 \ N (R4 2) C (S) N (R41), (R41) NC (S) N (R4 2), S (0)? S (0) 2, S (0) 2 N (R41 \ N (R41) S (0) 2? Se? Se (O), Se (0) 2? Se (0) 2N (R41), N (R41) Se (0) 2? P (0) ( R8)? N (R7) P ⑼ (R8), P (0) (R8) N (R7), N (R41), 0N (R41) and SiR2 8 R2 9, and (CH (R41)) e -W22 -(CH (R42)) h, where e and h are integers independently selected from 0 to 2, and W22 is selected from the group consisting of CR41 = CR42, CR41R42 = C (vinylene), and ethynylene (C ^ C; 1,2-ethynyl), 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3_ Cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6 · morpholinyl, 3,4 · morpholinyl, 3,5-morpholinyl, 1 , 2- ττ hydrogen plutonium ratio p well foundation, 1,3_hexahydro p ratio plutonium base, 2,3-hexahydro p ratio plutonium base, 2,6-hexahydropyridine base, 1,2-hexa Hydropyridyl, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2,4-hexahydropyridyl, 2,6-hexahydropyridyl, 3,4-hexahydropyridyl, 1 , 2_tetrahydropyrrolyl, 1,3_tetrahydro Pyryl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4 · tetrahydrop-pyrrolyl, 2,3-tetrahydro Sulfanyl, 2,4-tetrahydrocranyl, 2,5-tetrahydrocranyl, and 3,4-tetrahydrocranyl, with the proviso that when R41 and R42 are directly bound to N, they are selected From the other than halo and cyano, and Z0 is directly bound to the pyrimidinone ring; R28 and R29 are independently selected from the group consisting of hydrogen, hydroxyalkyl, alkyl, alkenyl, alkynyl, aryl, aralkyl, Aryloxyalkyl, fluorenyl, arylfluorenyl, aralkylfluorenyl, heteroarylfluorenyl, aralkyloxyalkyl, alkylsulfinylfluorenylalkyl, alkylsulfonylalkyl, aralkyl Thioalkyl, heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxy, alkylthioalkyl, arylthioalkyl, cycloalkyl, Cycloalkylalkyl, cycloalkylfluorenyl, cycloalkenyl ________ -17- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------- ----- K ---- Order --------- line (please read the notes on the back before filling this page) 1222445 A7 B7 V. Description of Invention (15) (Please read first Note on the back, fill in this page again), cycloalkenylalkyl, fluorenyl, #alkenyl, dentate cycloalkyl, fluorenyl alkenyl, haloalkoxyalkyl, self-alkenyloxyalkyl, Cycloalkoxy, _cycloalkoxyalkyl, #cycloalkenyloxyalkyl, all-functional aryl, all-aralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkane Alkyl, heteroarylthioalkyl, heteroarylalkylthioalkyl, cyanoalkyl, dicyanoalkyl, carboxyamidoalkyl, dicarboxyamidoalkyl, cyanoalkoxycarbonyl Alkyl, alkoxycarbonylalkyl, dialkoxycarbonylalkyl, cyanocycloalkyl, dicyanocycloalkyl, carboxyamidocycloalkyl, dicarboxyamidocycloalkyl, alkoxycarbonylcyano Cycloalkyl, alkoxycarbonylcycloalkyl, dialkoxycarbonylcycloalkyl, methylalkyl, fluorenylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, aralkyl Sulfinyl sulfenyl, cycloalkyl sulfinyl sulfinyl alkyl, cycloalkyl sulfinyl sulfinyl alkyl, heteroarylsulfonyl sulfinyl alkyl, heteroaryl sulfinyl sulfinyl alkyl, aralkyl sulfinyl sulfinyl Alkyl, aralkylsulfonylalkyl, carboxyl, dialkoxyphosphonic acid , Diarylalkoxyphosphine 8 ^ yl, dipitoxyoxytanoate: and diarylalkoxyphosphonic acid tiger group: R28 and R29 are used together as appropriate to form a group with 2 to 7 adjacent atoms A linear partial spacer, and forming a ring, selected from the group consisting of a cycloalkyl ring having 3 to 8 adjacent members, a cyclofluorenyl ring having 3 to 8 adjacent members, and a heterocyclic ring having 3 to 8 adjacent members Ring base ring; printed by the consumer co-operatives of the Intellectual Property Bureau of the Ministry of Economic Affairs (Π): R 丄

(II) -18- This paper uses Chinese National Standard (CNS) A4 specifications (21 × 297 mm) U22445 A7

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, where D1, D2, Ji, J2 and K1 are independently selected from the group consisting of c, N, 0, s and covalent bonds, with the condition that no more than one can be a covalent bond Not more than one of D1, D2, j2 and 0 may be 0, 01, 02 卩 1, and not more than one of D ^ 1 may be 8, when two of D, D2, Ji, J2 and K1 are 0 and s, one of did2,] 1, J2, and K1 must be covalent bonds, and 1) no more than four of 1, D2, J1, J2, and K1 can be N, with the condition that #, & 10, Chi 11 ice 12 and Y 13 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; Q is selected from formula (m) as appropriate:

/ (HI) where D3, D4, J3 and J4 are independently selected from the group consisting of C, N, 0 and S, D3, D4, J3 and J4. More than one is 3, and no more than three of D1, D2, Jl, and j2 are n, with the proviso that R9, R1 0, R11, and R1 2 are each independently selected to maintain the tetravalent nature of carbon and three of nitrogen Valence, divalent nature of sulfur, and divalent nature of oxygen; Q is optionally selected from the group consisting of hydrogen, alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, alkenyl, alkynyl , Saturated heterocyclic group, partially saturated heterocyclic group, donkey group, aromatic group, heteroaromatic group, cycloalkyl group, cycloalkyl group, cycloalkenyl group, cycloalkenylalkyl group, cycloalkylalkenyl group , Alkyl, alkoxy, -19- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------------- l · --- Order --------- line (please read the seven notes on the back before filling out this page) 1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs , Cyclic group, cyclic group, alkoxy group, # alkoxy group, self Cycloalkoxyalkyl and self-cycloalkenyloxyalkyl, with the condition that when Q is a hydrogen group, Z0 is selected from a group other than a covalent single bond; K is (CR4aR4b) n, where η is selected from An integer of 1 to 4; R and R4b are independently selected from the group consisting of halo, hydrogen, ethyl, cyano, lean, alkynyl, alkenyl, aryl, aralkyl, aralkoxyalkyl, Aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxy, alkylthio: alkyl, alkylthio, arylthioalkyl, cycloalkyl , Cycloalkenylalkyl, self-alkyl, self-alkenyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, cyanoalkyl, alkylene Sulfofluorenyl fei group :: fe-based SS-based group, halogen-based fluorenyl group, aryl fluorenyl group, aryl fluorenyl group, heteroaryl fluorenyl group, hetero Aryl fluorenylene alkyl, aralkyl fluorenylene alkyl, and aralkyl fluorenyl alkyl groups, with the proviso that when _ group, hydroxyl group and cyano group are bound to different carbons when they exist at the same time 'JL When R a and R 4 b are bonded to carbon and directly to p dense lake nitrogen, Not hydroxy or cyano; when combined with R4b to the same carbon, it is used together to form a group, selected from keto, thiocarboxy, and a linear group with 2 to 7 adjacent atoms Spacer portion, connected to form a ring, selected from a cycloalkyl ring having 3 to 8 adjacent members, a cycloalkenyl ring having 5 to 8 adjacent members, and a heterocyclic ring having 5 to 8 adjacent members Basic ring, with the proviso that when R4a and R4b are used together, when the common carbon is directly bound to the pyrimidone nitrogen, it is not a keto or thiocarbonyl group; when K is (CR4aR4b) n, E0 is E1, where E1 It is selected from the line including covalent single bond ---------------- K ---- order --------- line (please read the notes on the back before filling (This page) -20-1222445 A7 B7 V. Description of the invention (18) 0, S, C (0), C (S), C (0) 0, C⑶0, C (0) S, C (S) S, C (0) N (R, (Please read the phonetic on the back? Please fill in this page again for matters) N (R7), (R7) NC⑶, 0C (0) N (R7), (R7) NC (0) 0, SC (S) N SC (0) N (R7 \ (R7 ) NC (0) S? 0C (S) N (R7)? (R7) NC (S) 0, N (R8) C (0) N (R7)? (R7) NC (0) N (R8 XN ( R8) C (S) N (R7 \ (R7) NC (S) N (R8)? S (0)? S (0) 2? S (0) 2N- (R7), N (R7) S (0 ) 2, S (0) 2N (R7) C (0), C (0) N (R7) S (0) 2, Se, Se (0), Se (0) 2, Se (0) 2N (R7 ), N (R7) Se (0) 2, P (0) (R8), N (R7) P (0) (R8), P (〇) (R8) N (R7), N (R7), ON (R7), SiR28R29, CR4a = CR4b, ethynylene (CeC; 1,2-ethenyl), and C = CR4aR4b; K is optionally selected as (CH (R14)) jT, where j is selected from An integer of 0 to 3, and T is selected from the group consisting of a covalent single bond, 0, S, and N (R7), with the proviso that when j is 1, R14 is not a hydroxyl group, a cyano group, a fluorenyl group, an amine group, Alkylamino, dialkylamino and hydrogenthio groups, and (CH (R14)) j is bound to the pyrimidinone ring; when K is (CH (R14)) j_T, E0 is E2 as appropriate, of which E2 is Selected from the group consisting of covalent single bonds, (0), 0 (8), 0 (0) 0,0 (8) 0,0 (0) 8,0 (8) 8, €: (0 lectures (117), (Ruler 7)) ^ C (0 \ C (S) N (R71 (R7) NC (S)? (R7) NC (0) 0? (R7) NC (S) S? (R7) NC (0) S? (R7) NC (S) 0? N (R8) C (0) N (R7)? (R7) NC (0) N (R8)? N (R8) C (S) N (R7 \ (R7) NC (S) n (r8), s (o), s (o) 2, s (o) 2n (r7), n (r7) s (o) 2, s (o) 2n (h) c (o), c (o) n (h) s · Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs and Consumer Cooperatives (0) 2, Se (0), Se (0) 2, Se (0) 2 N (R7), N (R7) Se (0) 2, P ( 0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7) and N (R7); K is selected as G- (CH (R15)) k, where k is an integer selected from 1 to 3, and G is selected from the group consisting of 0, S, and N (R7), with the proviso that when k is 1, R15 is not a cyano group, a cyano group, a fluorenyl group, Amine group, amine group, diamine group and hydrogen thio group; when K is G- (CH (R15)) k, EG is optionally E3, where E3 is selected from the package ____- 21 _ Ben 1 Zhang scale is applicable to China National Standard (CNS) A4 specification (210 X 297 mm). Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. (0), C (S), c (o) o, c (s) o, C (0) S, C (S) S, C (0) N (R7), (R7) NC (0), C (S) N (R7), (R7) NC⑸, 0C (0) N (R7), (R7) NC (0) 0, SC (S) N (R7), (R7) NC⑸S, SC (0) N (R7), (R7) NC (0) S, 0C (S) N (R7), (R7) NC (S) 0, N (R8) C (O) N (R7), (R7) NC (0) N (R8) 5 N (R8) C (S) N (R7), (R7) NC (S) N (R8), S (0), S (〇) 2, S (0) 2 N (R7), N (R7) S (0) 2? Se, Se (0)? Se (0) 2, Se (0) 2 N (R7 \ N (R7) -Se (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), N (R7) , 0N (R7)? SiR28R29, CR4a = CR4b, ethynylene (CeC; 1,2-ethynyl), and C = CR4aR4b; is the formula (IV):

Qs

r16 / D ^ ° Xr19

Qb (IV) where D5, D6, J5, and J6 are independently selected from the group consisting of C, N, 0, S, and covalent bonds, with the proviso that no more than one is a covalent bond, and K2 is independently selected from the group including c and # , No more than one of d5, d6, j5 and J6 is 0, no more than one of D5, D6, j5 and J6 is S, when two of D5, D6, J5 and J6 are 0 and S, D5, D6 One of J5 and J6 must be a covalent bond. When K2 is ore, no more than three of D5, D6, J5, and J6 are N, and when K2 is carbon, no more than D5, D6, J5, and J6. Four are > ^, with the conditions being & 10,: ^ 17, H18, and F19, each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and oxygen One-price nature; ----------------- ^ ---- Order --------- line (please read the note on the back I? (This page) -22-

1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (20, used independently as appropriate to form a linear partial spacer with 3 to: atoms, connected to form a ring, including and = Ring ring with 8 adjacent members, K-saturated heterorubber ring with ... adjacent members, heteroaryl groups with 5 to 6 adjacent members, and aryl groups; R18 and R19 are used independently as appropriate To form a linear partial spacer with ... contiguous atoms, connected to form a ring, selected from cycloalkenyl rings including and having 5 to 8 contiguous members, with 5 to 8 contiguous members ^ Cyclocyclyl ring, a heteroaryl group having 5 to 6 adjacent members, and a radical;

Qb is selected from the group consisting of NR20R21, + NR20R21R22, oxy, alkyl, aminoalkylalkenyl, alkylamino, dialkylamino, dialkylfluorenyl, fluorenylamino, and Q, where Qbe Is a hydrogen group, and R20, R21 and r22 are independently selected from the group consisting of a hydrogen group, an amino group, an alkyl group, a hydroxyl group, an alkoxy group, an amino alkenyl group, an alkylamino group, a monoamino group, and a calcined group. The condition is that more than one of R2 0, R2 1 and R2 2 are not hydroxyl, alkoxy, alkylamino, amine and dialkylamino groups, and when K2 is a mineral, R20, R21 and R22 must be Not hydroxy, alkoxy, amine, amine and diamine; R20 and R21, R20 and R22, and 1 ^ 1 and 1122 are independently selected as appropriate to form a spacer pair, where the spacer The base pairs are used together to form a linear part having 4 to 7 adjacent atoms, and the bond points connecting the members of the spacer pair are formed to form a heterocyclic ring having 5 to 8 adjacent members. The conditions are different When using more than one spacer base pair, including R20 and R21, r20 and R22, and R21 and R22; 23 This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ---------------- K ---- order --------- line (please read the phonetic note on the back before filling this page) ) 1222445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (21)

Qb is optionally selected from the group consisting of N (R26) S02N (R23) (R24), N (R26) C (0) 0R5, n (r26) c (o) sr5, n (r26) c (s) or5 and n (r26) c (s) sr5, with the proviso that when two systems including R23, R24, and R26 are bonded to the same atom, no more than one of R23, R24, and R26 may be a hydroxyl, alkoxy, or hypoxane Amine, alkylamino, amine or dialkylamino;

Qb is optionally selected from the group consisting of dialkylfluorene, trialkylfluorene, C (NR25) NR23R24, N (R26) C (NR25) N (R23) (R24), N (R26) C (0) N (R23 ) (R24), N (R26) C (S) N- (R2 3) (R2 4), C (NR2 5) 0R5, C (0) N (R2 6) C (NR2 5) N (R2 3) (R2 4), C (S) N (R2 6) C (NR25) N (R23XR24) N (R26) N (R26) c (NR25) N (R23) (R24) 〇N (R26) C-

(NR2 5) N (R2 3) (R2 4), N (R2 6) N (R2 6) S02 (R2 3) (R2 4), C (NR2 5) SR5, C (0) N R23R24 and C ( 0) NR23R24, with the proviso that when any two of R23, R24 & r26 are bonded to the same atom, no more than one of R23, R24 and R26 may be hydroxyl, alkoxy, alkylamino, amine or di Alkylamino group, and the Qb group is directly bonded to a carbon atom; 3,1124, 1125 and 1126 are independently selected from the group consisting of hydrogen, alkyl, hydroxyl, fluorenyl, alkenylamino, amine, Burned amine group, diamine group and stilbene group; R23 and R24 are used together as appropriate to form a linear spacer portion with 4 to 7 adjacent atoms, and connect the bond points to form 5 to 8 adjacencies Heterocyclyl ring of members;

R23 and R25, R24 and R25, R25 and R26, R24 and R26, and ^^ and ^^ are independently selected to form spacer pairs, where the spacer pair is a bond between members of the selected spacer pair Points are used together to form a LUV group, where L, U, and V are independently selected from the group consisting of 0, S, C (0), C⑸, c (jh) 2s (c0, S02, 0P (0R3 1), r3 0 , P (〇) R3 0, p (S) R3 0, c (r3 〇) r3 1, 〇C (R3 0) r3 i, ⑼2 P _ -24- This paper has been oversized in accordance with Chinese National Standard (CNS) A4 Specifications (210 x 297 mm) ---------------- K ---- Order ---- I ---- Line ^ r (Please read the note on the back first 咅? Please fill out this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 ---------- B7 V. Description of the invention (22) 0P (0) 2? R3 0 (0) P0P ( 0) R3 〇? Si (R2 9) R2 8 si (R2 9) R2 8 Si (R2 9) R2 8 Si Si (R2 9) R28OSi (R29) r28, (R28) r29c〇c (r28) r29, (r28) r29csc (r28) r29, c (〇) C (R3 °) = C (R3 1), C (S) C (R3 G) = C (R3 1), s is like post 3.) < ^ 31), 802 and 30) = €-(R3 1), PR3 0 C (R3 0) = C (R3 1), P (〇) R3 〇 (r3 o) = c (r3 i), p ( s) r3 o C (R3 o) = c_ (R3 1) DC (R3 〇) (R3 1) D, OP (OR3 1) R3 G, p (〇) R3 G, p (s) R3 G, Si (R2 8) R2 9 and N (R3 〇) 'and covalent A bond, with the proviso that no more than two of l, u, and V are covalent bonds at the same time, and the heterocyclic group contained by L, U, and V has 5 to 10 adjacent members; D is selected from the group consisting of Oxygen, C = 0, 〇S, S (0) m, where m is an integer selected from 0 to 2; JH is independently selected from the group consisting of OR27, SR27 and N (R20) R21; , Alkynyl, fluorenyl, block, aryl tiger, aryloxy, square oxonyl, alkynyl, alkynyl, alkynyl, alkyl, aralkylthioalkyl , Heteroaralkylthioalkyl, Alkoxyalkyl, Hetero square lactyl pit group, Benzyloxy group, pitthio group, arylthio group, cycloalkyl, cycloalkylalkane Alkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, fluorenyl, i-alkenyl, self-cycloalkyl, cycloalkenyl, alkoxyalkyl, and alkenyloxyalkyl , Self-cycloalkoxyalkyl, self-cycloalkenyloxyalkyl, full-painted aryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaryl Alkylthioalkyl, arylsulfinylalkyl, arylsulfinylalkyl, cycloalkylsulfinylalkyl, cycloalkylsulfinylalkyl, heteroarylsulfinylalkyl R3G and R31 are independently selected from hydrogen, hydroxy, thiol, and aryloxy Base-25- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---- r ---- Order --------- line (Please read the note on the back first Huh? Please fill in this page again for details) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 __B7__ V. Description of the Invention (23), Amine, Alkylamino, Dialkylamino, Hydroxyalkyl, Heteroaryloxyalkyl , Methyloxy, thiothio, arylthio, thio, fluorenyl, block, aryl, aralkyl, aryloxyalkyl, aralkyloxyalkyl, alkylsulfinyl sulfanyl Alkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroarylalkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxy, alkylthio Alkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, _alkyl, _alkenyl, _aralkylsulfinyl Fluorenylalkyl, aralkylsulfonylalkyl, cyanoalkyl, dicyanoalkyl, amidoaminoalkyl, dicarboxyamidoalkyl, cyanoalkoxycarbonylalkyl, alkoxy Carbonylalkyl, dialkoxycarbonylalkyl, cyanocycloalkyl, dicyanocycloalkyl, carboxyamidocycloalkyl, dicarboxyamidocycloalkyl, alkoxycarbonylcyanocycloalkyl, Alkoxycarbonylcycloalkyl, dialkoxycarbonyl ring Alkyl, methylamidoalkyl, fluorenylalkyl, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, phosphonoalkyl, dialkoxyphosphonoalkoxy Group, diarylalkoxyphosphonic acid alkoxy, phosphonic acid alkoxy, dialkoxyphosphonic acid alkylamino, diarylalkoxyphosphonic acid amine, phosphonic acid tigeramine , Bis-alkyloxyphosphonic acid group, pentyloxypentanoic acid pentyl group, continyl fluorenyl group, alkoxy sulfonyl group, aralkyloxysulfonylalkyl group, alkoxysulfonyl group Alkyl alkoxy, aralkyloxy, fluorenyl alkoxy, sulfonyl alkoxy, alkoxy sulfonyl amine, aralkyloxy sulfonyl alkylamino, and sulfonyl alkylamino ; R30 and R31 are used as appropriate to form a linear partial spacer with 2 to 7 adjacent atoms to form a ring, which is selected from the group consisting of a ring having 3 to 8 adjacent members. Member's cycloalkenyl ring, and heterocyclic ring with 3 to 8 adjacent members; -26- this standard is suitable for financial standards (CNS) A4 (210 X 297 mm------ I丨 丨 丨! 丨 h 丨! Order ·----- 11 (Please read first (Notes on the back then fill out this page) A7

The Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs printed R and R25 ', instead of redundancies, r24 and r26, and r23 and Yu 6, are independently selected to form spacer pairs, where the spacer pairs are from their own The bonding points of the members of the spacer pair are selected to be used together to form the LUV group, where L, U and V are independently selected from the group L2-disubstituted, including the ring ... group, and the 晞 group. The group is substituted by one or more groups selected from R30 and R31, an aryl group, a heteroaryl group, a saturated heterocyclic group and a saturated saturated heterocyclic group, wherein the substituent is independently selected from 0. , C = S, C (R2 8) R3 2, S (〇), S (〇) 2, 〇p (〇R3 1) R3. , P (0) R3 Q, p (s) r3 〇 and Si (R ^) R29. R23 and R25, R24 and R25, 1125 and 1126, 1124 and 1126, and anti 23 and anti 26 'are independent as the case may be. Selected to form a spacer pair, wherein the spacer pair is used together from the bonding node of the selected spacer pair member to form a LUV group, wherein L, U, and V are independently selected from the group consisting of 1,2-disubstituted An alkylene group and a 1,2-disubstituted hypoalkenyl group, wherein the L2-substituent is independently selected from C = 0, C = s, C (R2 8) R2 9, S (0), s (0) 2, OP (OR3 1) R3 0, P (0) R3 0, P (S) R3 0 and

Si (R28) R29, and the alkylene group and the alkenylene group are substituted by one or more H30 or Rsi substituents; QHi, selected from the group consisting of covalent single bonds, (CR37R38) b- (WG) az, Where az is an integer selected from 0 to 1, b is an integer selected from 1 to 4, and WG is selected from the group consisting of 0, S, C (0), C (S), C (0) 0, C (S ) 0, C (0) s, C (S) S, CCC ^ ISKR14), (R1 4) nc (o), C (S) N (RX 4 \ (R14) NC (S)? 00 (0) Ν (Κχ 4 \ SC (S) N (R14)? SC ^ NCR14 \ 0C (S) N- (R141 NCR15) C (0) N (R141 (R14) NC (0) N (R15), NCR15) C (S) N (Kl 4)? (R14) NC (S) N (R15), S (0), S⑼2, S (0) 2N (R14), N (R14) S⑼2, Se, S Se (0) 2N (Ri7), N (B; 4) Se (0) 2, P (0) (R8), N (R7) P ⑼ (R8), P (〇) (R8) N (R7), -27- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------------- ^ ---- Order -------- -Line (Please read the notes on the back before filling this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ____B7 __ V. Description of the invention (25) N (R14), ON (R14) and SiR28R29, ( CE ^ RH ^ -WyCI ^ R15: ^, where c and d are independently integers selected from 1 to 4, and W1 is selected from the group consisting of S, C (0), C (S)? C (0) 0? C (S) 0? C (0) S? C (S) S? C (0) N (R14)? (R14) NC ( 0)? C (S) N (R14)? (R14) NC (S)? OC ^ NCR14% (R14) NC (0) 0? SC (S) N (R14)? (R14) NC (S) S ? SC (0) N (R14% (R14) NC (0) S? OC (S) N (R14)? (R14) NC (S) 09 NCR15) C (0) N- (R14% (R14) NC (0) N (R15% N (RX 5) C (S) N (R14 \ (R14) NC (S) N (R15)? S (0)? S (0) 2, SPhNR14), N (E; 4) S⑼2, Se, Se (0), S < 0) 2, SKC ^ l ^ R14), N (β; 4) Se (0) 2, P (0) (R8), N (R7) P ( 0) (R8), P (0) (R8) N (R7), N (K; 4), ON- (R14), SiR28R29, and (CH (R14)) e-W22- (CH (R15)) h, where e and h are integers independently selected from 0 to 2, and W22 is selected from the group consisting of CR41 = CR42, CR41R42 = C (vinylidene), ethylene block (Ce C; 1, 2_ ethyl block) ), 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2, 3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4_morpholinyl, 3,5_morpholinyl, 1,2-hexahydrop Than p well base, ι, 3_hexahydropyridyl, 2,3 · hexahydropyridyl, 2,6 · hexahydropyridyl, ι, 2_hexahydropyridyl, 1,3-hexa Hydropy , 2,3-hexahydropyridyl, 2,4-hexahydropyridyl, 2,6-hexahydropyridyl, 3,4 · hexahydropyridyl, 1,2-tetrahydropyrrolyl, i, 3_tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4-tetrahydropyrrolyl, 2,3 -Tetrahydrofuranyl, 2,4-tetrahydrocranyl, 2,5 · tetrahydroocanyl, and 3,4 · tetrahydrocranyl, the conditions of which are R1 4 and R15 when directly bound to N, Is selected from the group other than halo and cyano, and (CRnR3%, (CH (R14)) c, (CH (R14)) e is bound to the sand; R37 and R37, when bound to different carbons, depending on the situation Used together to form a linear partial spacer with 1 to 7 adjacent atoms to form a ring, ----------------- ^ ---- Order ----- ---- Line (Please read the precautions on the back before filling this page) -28-Printed by the Consumer Consumption Cooperative of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 ^ ~ ------- B7_____ V. Description of Invention (26) — ^ Since a cycloalkyl ring having 3 to 8 adjacent members, a base ring having 3 to 8 adjacent members, and a heterocyclic ring having 3 to 8 adjacent members, R and R, when Combine to not When carbon is used, it is used together to form a linear partial spacer with j to 7 adjacent atoms to form a ring. It is selected from the group consisting of a cycloalkyl ring with 3 to 8 adjacent members and 3 to 8 adjacent members. A cycloalkenyl ring, and a heterocyclic ring having 3 to 8 adjacent members; R and R, when bonded to different carbons, are used together to form a linear partial spacer with 1 to 7 adjacent atoms, To form a ring selected from the group consisting of a cycloalkyl ring having 3 to 8 adjacent members, a cycloalkenyl ring having 3 to 8 adjacent members, and a heterocyclic ring having 3 to 8 adjacent members; R and R 'When bound to the same carbon, are used together to form a group selected from the group consisting of keto, thiocarbonyl, alkylidene, self-alkylidene, and a linear partial spacer with 2 to 7 adjacencies Atoms to form a ring, selected from the group consisting of a cyclomorphic ring having 3 to 8 adjacent members, a cycloalkenyl ring having 3 to 8 adjacent members, and a heterocyclyl ring having 3 to 8 adjacent members; Y0 Qb-Qss as appropriate, where QW is selected from the group consisting of (CR37R38) f, where f is an integer selected from 1 to 6, Where c and d are integers independently selected from 1 to 4, and W1 is selected from the group consisting of 0, S, C (O), C (S), C (0) 0, C (S) 0, C (0) S, C (S) S, CXOMR14), (R14) NC (0), (XSMR14), (R14) NC (S)? OC ^ NCR14 \ (R14) NC (0) 0, SC (S) N ( R14 \ (R14) NC (S) S? SC (O) -N (RX 41 (R14) NC (0) S? OC (S) N (R14 \ (R14) NC (S) 0? N (RX 5 ) C (0) N (R14)? (R14) NC (0) N (R151 NCR15) C (S) N (R14)? (R14) NC (S) N (R15)? S (0)? S ( 0) 2? S (0) 2N (R14), N (R14) S (0) 2, Se, Se (0), Se (0) 2, Se (0) 2N (R14), N (R14) · Se (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), l ^ R14), OIS ^ R14), -29 -This paper size is applicable to China National Standard (CNS) A4 (210 x 297 mm) ---- l · --- ^ --------- (Please read the precautions on the back before filling in this (Page) 1222445 A7

V. Description of the invention (27) (Please read the note on the back? Matters before filling out this page)

SiR R29 'and (CH (Ri4)) e_w2_ (CH (Rl5)) h, where e and h are integers independently selected from 0 to 2, and W2 is selected from the group consisting of CR4a = CR4b, acetylene: group (C Ξ C; 1,2-ethynyl) and C = CR4aR4b, with the proviso that when Rl4 and Rl5 are directly bonded to N, they are selected from the group other than halo and cyano. When qSS is (CR37R38) f ', where f is not When it is an integer ^, (CR37R38) f, (CH (R15) 乂, and (CI ^ R15)) e are bound to E0, and Qb is selected from n (R2 6) N (R2 6) C (NR2 5) Other than N (R2 3) (R2 4) or ON (R26) C (NR25) (R23) (R24); printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs as Qb_Qsss, where QSSS is (CH ( R38)) r_w3, r is an integer selected from i to 3, W3 is selected from the group consisting of i, i-cyclopropyl, i, 2-cyclopropyl, ι, ΐ-cyclobutyl, 1,2-cyclobutane Base, 1,2 · cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2 · cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2, 4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2 · hexahydropyridine Plow-based, 1,3-hexahydropyridine, 1,4-hexahydropyridine, 2,3 -Hexahydropyridyl, 2,5-hexahydropyridyl, 2,6-hexahydropyridyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, 1,4-hexa Hydropyridyl, 2,3 · Hexahydropyridyl, 2,4-Hexahydropyridyl, 2,5 · Hydroxy p-pyridyl, 2,6 · Hydroxy p-pyridyl, 3,4-hexa Hydrogen tonyl, 3,5-hexahydro ρ than Dianji, 3,6-hexahydro; Dianji, 1,2_tetrahydroxyl, 1,3-tetrahydroerokyl, 2 ,, 3 · tetrahydropyrrolyl, 2,4-tetrahydrop-pyrrolyl, 2,5 · tetrahydropyrrolyl, 3,4-tetrahydropyrrolyl, 2Η · 2,3-piperanyl, 2H- 2,4-piperanyl, 2Η-2,5-piperanyl, 4Η-2,3-piperanyl, 4Η-2,4-piperanyl, 4Η-2,5-piperanyl, 2Η- Piperan-2-one_3,4_yl, 2'-piperan-2_one-4,5-yl, 4'-pyrrolidine-4-'2,3,3-yl, 2,3 · tetrakis p-furyl, 2,4-tetrahydropyranyl, 2,5-tetrahydrofuryl, 3,4-tetrahydrofuryl, 2,3-tetrahydropiperanyl, 2,4-tetrahydropiperanyl, 2,5-tetrahydropiperanyl, 2,6 · tetrahydropiperanyl, 3,4-tetrahydropiperanyl-30- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ----- B7 V. Description of the invention (28) and 3,5 · tetrahydropiperanyl group, and each carbon and hydrogen group containing the nitrogen member of the W3 ring instead of the connection point, is one or more depending on the situation Each group including R9, R10, R11 and R12 is substituted with the condition that (CH (R38)) r is bound to E0 and Qb is bound to the lowest number of substituent positions of each W3; Y0 as the case may be Qb-Qsssr, where Q_r is (αί (Ιι38 ^ · | 4, r is an integer selected from 1 to 3, W4 is selected from the group consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3 · Cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3 · morpholinyl, 2,4-morpholinyl, 2,5-morphol 4-based, 2,6_morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, M · hexahydropyridyl, 2,3-hexahydropyridyl, 2,5 · hexahydropyridyl, 2,6-hexahydro? Twelve well base, 1,2-Hexahydro-rhodium base, 1,3-Hexahydro-rhodium base, 1,4-Hexahydro-rhodium base, 2,3-Hexahydro-rhodium base, 2 , 4_Hexahydrobium base, 2,5-Hexahydrolate base, 2,6_Hydrogen p ratio, 3,4-Hexa p ratio, 3,5-Hexahydro Base, 3,6-hexahydrocarbyl, 1,2-tetrahydropyrrolyl, 1,3-tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydro p ratio Rocky, 2,5-tetrahydropyrolyl, 3,4-tetrahydropyroyl, 2H-2,3-piperanyl, 2H_2,4-piperanyl, 2H_2,5-piperanyl, 4Η -2,3 · piperanyl, 4Η-2,4_ananyl, 4Η · 2,5 · ananyl, 211_youran-2-one-3,4 · an, 2Η-anan-2 -S is -4,5 · yl, 4Η-Travelan-4-S is · 2,3-yl, 2,3-tetraazathiorane, 2,4_tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydroquinanyl, 2,4_tetrahydrofuranyl, 2,5_tetrachloroρuranyl, 2,6_tetranitrofuranyl, 3 , 4-tetrahydropiperanyl and 3,5-tetrahydropiperanyl, and each carbon and hydrogen group containing a nitrogen member of the W4 ring instead of the point of attachment are optionally one or more including R9, R10 , R11 and R12 group substitution, with the condition that (CH (R38)) r Bonded to EG, and @ is bound to the highest number of substituent positions of each W4; -31-This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ---------- ------ K ---- Order --------- line (please read the precautions on the back before filling this page) A7 B7, invention description (29 (please read the precautions on the back first) Fill out this page again) Y〇 Qb_Q_S as appropriate, where QSSS% (CH (R38)) r_w5, r is selected from 1 to 3 < integer, W5 is selected from the group consisting of indenyl, y • indenyl, J, 6 Indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5- Indenyl, indenyl, 3,7-indenyl, 2,4-benzofluorenylfuranyl, 2,5-benzobenzofuranyl, 2,6-phenylfluorenylfuranyl, 2,7-benzofluorenylfuranyl, 3 , 4-benzofuranyl, 3,5-benzofluorenylfuranyl, 3,6-benzofluorenylfuranyl, 3,7-benzofluorenylfuranyl, 2,4-benzofluorenylthio, 2,5-benzene Benzenethio, 2,6-Benzenethiophenyl, 2,7-Benzenethiophenyl, 3,4-Benzenephenylthio, 3,5-Benzenethio, 3,6-benzene Acenethio, 3,7-benzenesulfenylthio, 2,4-imidazoliumpyridyl, 2,5-imidazolium (l, 2-a) pyridyl, 2 Bumidazolium (1,2 pyridyl, πimidazolium (1 »pyridyl, 3,4-imidazolium (1,24 pyridyl, 3,5-imidazolium (1,2-a) pyridyl, Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, 3,6-Mi bite (1,2-a) p ratio Yodo base, 3,7_Mi Jun 幷 (i, 2-a) p ratio Yodo base, 2, 4_ 啕 基 Base, 2,5- 啕 啕 Base, 2,6- 啕 啕 Base, 2,7-indole, 3,4- 啕 啕 Base, 3,5_ 啕 p 木 基, 3,6 -Clever base, 3,7_ Θ 丨 base, 1,4-isoK 丨 base, ι, 5_iso < p-doyl, 1,6-iso4 丨 indolyl, 2,4-isoΘ丨 Horyl, 2,5-isoΘ 丨 Horyl, 2,6_isoport 5 丨 Horyl, 2,7-isopyridyl, U · isopyridyl, 3,4-oxazolyl, 3 , 5_ < oxazolyl, 3,6-oxazolyl, 3,7_indazolyl, 2,4-benzoxazolyl, 2,5_benzopyridyl, 2,6-phenylhydrazone Oxazolyl, 2,7_benzoxazolyl, 3,4_benzoxazolyl, 3,5-benzoxazolyl, 3,6_benzoxazolyl, 3,7 • Phenylisocyanate, 1,4-naphthyl, ι, 5 · fluorenyl, 1,6-pentyl, ι, 7-naphthyl, azyl, 2.4-fluorenyl, 2,5_fluorenyl, 2,6 fluorenyl, 2,7-fluorenyl, 2,8-naphthyl, 2 4_quinyl 4 wood , 2,5_jun τ »forest base, 2,6-jun p forest base, 2,7-junon base, 2,8-π quinolinyl, 3.4-quinolinyl, 3,5-quinolinyl , 3,6-quinolinyl, 3,7-quinolinyl, 3,8-p-quinolinyl, 4,5--4 4 xylan, 4,6-p quinolinyl, 4,7_ 4 4 quinyl, 4,8 · Kouquiji, ^ 4- -32 This paper size is applicable to the Chinese National Standard (CNS) A4 specification (21 × 297 mm) ^ 22445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 --- --B7 _____ V. Description of the invention (30) Isoquinolinyl, i, 5-isoquinolinyl, i, 6-isoquinolinyl, 17_isofluorinyl, 1,8_isojunyl 3,4_isolympholyl, 3,5_isomorpholinyl, ^ isoquinolinyl, 3J-isoquinolinyl, 3,8_isoquinolinyl, 4 > isoquinolinyl, 4,6 _Isoquinolinyl, 4,7-isoquinolinyl, 4,8_isofluorinyl, 3,4-fluorinyl, 3,5-fluorinyl, 3,6-fluorinyl, 3, 7-fluorenyl, 3 8-fluorinyl, 45-fluorinyl, 46-fluorenyl, 4,7_ and linyl, and 4,8_ and linyl, and contain a ring nitrogen member without Each carbon and hydrogen group is the connection point, which is optionally replaced by one or more groups including R9, R10, R11 and R12, with the condition that the furnace system is combined To the lowest number of substituent positions for each W5, and (CH (R38)) r is bound to e0; Y0 is Qb_QSSSSr as appropriate, where QSSSSr is (CH (R38)) r_w6, and Γ is selected from 1 to 3 Integer, W6 is selected from the group consisting of M · indenyl, M · indenyl, indenyl, i, 7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2, 4_mandarinyl, 3,4_india, 3,5_burden, 3,6_burden, 3,7-manganyl, 2,4_phenylbenzyl, 2,5-benzyl Sulfanyl, 2,6-phenylsulfanyl, 2,7-phenylsulfanyl, 3,4-phenylfluoranyl, 3,5-phenylfluoranyl, 3,6-phenylfluoranyl, 3,7-Benzamidinefuranyl, 2,4-Benzamidinephenylthio, 2,5-Benzamidinephenylthio, 2,6-Benzamidinephenylthio, 2,7-Benzamidinephenylthio, 3 , 4-Benzamidinephenylsulfanyl, 3,5-Benzamidinephenylsulfanyl, 3,6-benzylidenesulfanyl, 3,7-benzenesulfonylbenzenesulfanyl, 2,4-Weijungang (l, 2 -a) Eodoyl, 2,5-imidazolium (l, 2-a) pyridyl, 2,6-imidazolo (l, 2-a) pyridyl, 2,7-imidazolium (1,2, a) Pyridyl, 3,4-imidazolium (1,2-a) pyridyl, 3,5-imidazolium (1,2, a) pyridyl, 3,6-imidazolium (1,2-a) pyridyl , 3,7-imidazolium (l, 2-a) pyridyl, 2,4-oxindole , 2,5 · indolyl, 2,6-indolyl, 2,7-indolyl, 3,4 · indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-pyridyl, 1,4-isopyridyl, 1,5-isopyridyl, 1,6-isopyridyl, 2,4-isopyridyl, 2,5-isopyridyl Indyl, 2,6-iso ___- 33 -___ This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------------- ^ ---- Order --------- line (Please read the note on the back first? Please fill in this page again for details) 1222445 Α7 Β7 V. Description of the invention (31) Qiaoshen group, 2,7_isoindolinyl group, 1,3-isoindolinyl group, 3,4-chrysyl group, 3,5- Oxazolyl, 3,6-indazolyl, 3,7-oxazolyl, 2,4-benzozazolyl, 2,5-benzophenazolyl, 2,6 · benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzoxazine, 3,5-benzoxazine, 3,6-benzoxazine, 3,7_benzoxyl % Junyl, 1,4-naphthyl, ι, 5-fluorenyl, 1,6 · fluorenyl, ι, 7-fluorenyl, 1,8_fluorenyl, 2,4_fluorenyl, 2,5-fluorenyl Group, 2,6-fluorenyl, 2,7-fluorenyl, 2,8-g: group, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2, 7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5quinolinyl, 3,6quinolinyl, 3,7quinolinyl, 3,8 -Quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5_ Isoquinolinyl, ι, 6-isoquinolinyl,!, 7-isoquinolinyl, 1,8-isoquinolyl, 3,4-isoquinolinyl, 3,5_isoquinolinyl , 3,6 • isoquinolyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6_isoquinolinyl, 4,7 -Isoquinolinyl, 4,8-isoquinolinyl, 3,4-fluorinyl, 3,5-fluorinyl, 3,6-fluorinyl, 3,7 · fluorinyl, 3,8 -Fluorinyl, 4,5_fluorinyl, 4,6_fluorinyl, 4,7_fluorinyl, and 4,8-fluorinyl, each of which contains a nitrogen member of the w6 ring and is not a point of attachment Carbon and hydrogen groups are optionally substituted by one or more groups including W, R10, R11, and Ri2, with the proviso that the furnace system is bound to the highest number of substituent positions of each W6, and ((: 11 takes 38 Is bound to £. In a specific embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is selected from the group consisting of 0 and S; J is optionally selected from the group consisting of CH_R6 and N_R6, where R6 is a linear spacer Part, having a chain length of 1 to 4 atoms, the bond to a substituent =: the substituent is selected from the group consisting of R4a, R4b, R39, R40, R5, Rl4 & r15, and has 5 to 8 Heterocyclyl ring of adjacent members; ---- K ---- Order --------- line (please read the precautions on the back before filling this page) System-34- 1222445 A7 V. Description of the invention (32 B is formula (V): 34 R33,

R 32〆

D .D "

R 36 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (V) where D1, D2, J1, J2 and K1 are independently selected from the group consisting of c, N, 0, s and covalent bonds, with the condition that no more than one is Covalent bonds, no more than one of which is 0,1) 1, 〇2 "and no more than one of ruler 1 is 8, when two of D ^ D2, J1, J2 and K1 are 0 and s, d1 , d2, j !, and households — must be covalent bonds, and no more than four of 〇1, 〇2, < 11, < 12 and Min1! ^, 萁 The conditions are that the feet 32, feet 33, 1134, feet 35 and Han 36 are independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen. : — R9, R1 0, R1 1, R1 2, R1 3, Rl 6, Rl 7, R1 8, Rl 9, r3 2, R3 3, R3 4, r3 5 and R3 6 are independently selected from the group consisting of hydrogen , Acetamido, haloacetamido, hydradinyl, guanidino, dialkylphosphonium, trialkylphosphonium, dialkylphosphonium, carboxyl, 4-arylthio, heteroarylalkoxy , Cycloalkylamino, fluorenylalkyl, fluorenylalkoxy, arylfluorenylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, arkenyl, aralkynyl, heterocyclic Base, all_aralkyl, aralkylsulfonyl, arsenyl, alkynyl, aryl, alkynyl, aryl: aryl, aryl, phenyl, alkynyl, alkyl, alkyl Alkenyl, cycloalkylsulfinylene, cycloalkyl

------------------ ^ ---- Order --------- line (please read 1 note on the back? Matters before filling out this page) Economy Printed by the Consumer Cooperatives of the Ministry of Intellectual Property Bureau 1222445 A7-B7 V. Description of the invention (33) Subcontinuous si-based alkynyl, cyclic alkynyl-based acyl group, cyclic pit-based continuous brewing pit-based, hetero- square amine-based, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, fluorenyloxy, alkoxy, alkoxyalkyl, self-oxyalkoxy, hetero Aralkyloxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkyloxy, cyclofluorenyloxyalkyl, hypocycloalkyldioxy, self-cyclic feoxy , Self-Cycloalkyloxyalkyl, _Cycloalkyloxy, Cycloalkyloxyalkyl, Hydroxyl, Amine, Alkoxyamino, Thio, Nitro, Low-Carbonylamino, Alkyl Thio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinyl Arylalkyl, arylsulfinylalkyl, arylsulfinylalkyl, heteroarylalkylidene, heteroarylalkyl, alkyl Acid group, alkylsulfonylalkyl, alkylsulfinylalkyl, sulfinylsulfanylalkyl, alkylsulfonamido, alkylaminosulfonyl, sulfonamidosulfonyl , Monoalkylammonium amine base, diammonium amine base, monoaryl amine base continuous group, aryl sulfonyl amine, diaryl sulfonyl sulfonyl, mono Alkyl monoarylsulfonylsulfonyl, arylsulfinylsulfonyl, arylsulfinyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfinyl, heterocyclic Fluorenyl, heterocyclylthio, sulfonyl, fluorenyl, aryl, aryl, aryl, aryl, aryl, alkynyl, haloalkyl, alkyl, alkenyl, alkynyl Radical, alkenyloxy, alkoxyalkyl, alkanedioxy, alkanedioxy, cycloalkyl, cycloalkylalkylfluorenyl, cycloalkenyl, low-carbon cycloalkylalkyl, low-carbon Cyclofluorenylalkyl, halo, alkynyl, sulfonyl, self-oxyl, alkynyl, alkynyl, aralkyl, hydroxyalkyl, alkylalkenylamino, hydroxyheteroaralkyl , _Alkoxyalkyl, aryl, arylalkyl, aryloxy, aryloxy, aryloxyalkyl, ☆ -3 6- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---------------- K ---- Order ------- --Line (please read the precautions on the back before filling this page) 1222445 Printed by A7, Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs, Invention Description (34) Saturated heterocyclic group, partially saturated heterocyclic group, heteroaryl group, Heteroaryloxy, heteroaryloxyalkyl, aralkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, alkoxycarbonyl, alkoxycarboxyamido Alkylaminoalkylcarbonylamino, arylaminoaminocarbonylamino, alkoxycarbonylamino, alkoxycarbonylalkenyl, carboxyl, aralkyloxycarbonyl, carboxyamidoamino, carboxyamidoalkyl Group, cyano group, alkoxycarbonyl group, phosphonic acid group, phosphonic acid alkyl group, diarylalkoxyphosphonic acid group, and diarylalkoxyphosphonic acid alkyl group; and / 夂: ^ 气 炉 ': ^夂 ^^ and the mind are independent depending on the situation. The proviso is that no more than one of R16 and R19 is Qb at the same time, and ⑦ is Qbe; R32 and R33, & 33 and anti-34, r34 and r35, and r35 and r36, selected independently to form intervals Base pairs, where spacer pairs are used together to form a linear portion with 3 to 6 adjacent atoms, and the bond points connecting the members of the spacer pair form a ring, selected from the group consisting of 5 to 8 adjacent members & lt Cycloalkenyl ring, partially saturated heterocyclic ring with 5 to 8 adjacent members, heteroaryl ring with 5 to 6 adjacent members, and aryl groups, with the proviso that not more than one containing spacer can be used simultaneously The bases are groups of ruler and and 33, anti-33 and ruler 34, R34 and R35, and R35.R36; ', envy and Rio, R10 and R11, "丨 and"], and ruler 12 and ruler 13, Independently, as appropriate, selected to form a spacer pair, wherein the spacer pairs are used together to form a linear portion having 3 to 6 adjacent atoms, and the bond nodes connecting the members of the spacer pair are formed to form a ring, selected from Including cycloalkenyl rings having 5 to 8 adjacent members, partially saturated heterocyclic rings having 5 to 8 adjacent members, heteroaryl rings having 5 to 6 adjacent members, and aryl groups, subject to conditions It is not possible to use more than one pair of spacers including "和 化", ruler, and " Peachiness is timely_Home Standard (CNS) A4 Specification (210: -37-297 mm) ----- ^ ---- Order --------- Line (Please read the Note? Please fill out this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 ------- B7 V. Description of Invention (35) Groups of R11 and R12, and R12 and R13; Including hydrogen, trialkylsilyl, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 fluorenyl, C3-C8 alkynyl, C2-C8_alkyl, and C3-C8 haloalkenyl, where group b Each member may be replaced by one or more groups including R32, R33, R34, R35 & R36 at any carbon containing 6 atoms up to the junction point b to A, as appropriate; B is selected from C3-C15 cycloalkyl, C5-C10 cyclofluorenyl, C4-C12 saturated heterocyclyl and C4-C9 partially saturated heterocyclyl, in which each ring carbon is substituted by R33 as appropriate, one ring carbon, not B to A The ring carbon at the point of connection is optionally substituted by a keto group, provided that no more than one ring carbon is simultaneously substituted by the keto group, and the ring carbon and nitrogen atom of the carbon atom adjacent to the point of connection are replaced by R9 or R13, as the case may be. A ring carbon or nitrogen atom adjacent to R9 and two atoms away from the connection point is replaced by R1G as appropriate, and adjacent to R13 and two atoms away from the connection point A ring carbon or nitrogen atom, which is replaced by R12 as the case may be, a ring carbon or nitrogen atom that is two atoms away from the connection point and is adjacent to the R1 G position, and a ring that is three atoms away from the connection point and adjacent to the Ri2 position, as the case may be. A carbon or nitrogen atom, which is optionally substituted by R3 3, and a ring carbon or nitrogen atom that is four atoms away from the junction and is adjacent to R11 and R33, is optionally substituted by R34; A is selected from the group consisting of covalent single bonds, (W7KCH (R15)) pa & (CH (R15)) pa- (W7) rr, where rr is an integer selected from 0 to 1, pa is an integer selected from 0 to 6, and W7 is selected from the group including 0, S, CX0), C (S), CX0) S, CXS) 0, C (0) NCR7), C (S) N (R7)? (R7) NC (0)? (R7) NC (S)? S (O), S (0) 2? S (0) 2N (R7)? (R7) NS (0) 2? P (0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), C (NR7) N (R7), (R7) NC (NR7), (R7) NC (NR7) NR7 and N (R7), the conditions are that rr and pa cannot be At the same time exceeding -38-This paper size applies the Chinese National Standard (CNS) A4 specification (210 χ 297 mm) ----------------- ^ ---- Order --- ------ line (please read the precautions on the back before filling this page) 1222445 Employee Consumption of Intellectual Property Bureau, Ministry of Economic Affairs A7 B7 printed by Sakusha 5. Description of the invention (36) One is 0; R7 and R8 are independently selected from the group consisting of hydrogen, light, alkynyl, fluorenyl, arylfluorenyl, heteroarylfluorenyl and alkoxyalkyl R14, R15, R37 and R3 8 are independently selected from the group consisting of fluorenyl, hydroxyl, halo, cyano, hydroxyalkyl, alkoxy, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl , Cycloalkenyl, cycloalkenylalkyl, _alkyl, i alkenyl, alkoxy, alkoxyalkyl, self-alkenyloxyalkyl, self-cycloalkoxy, halocycloalkoxy Alkyl, S-cyclomethyloxyalkyl, carboxyl, carboxyalkyl, alkoxy, amine and lean amino groups; R14 and R38 can be independently selected from fluorenyl and arylfluorenyl groups And heteroarylfluorenyl groups, with the proviso that the base group is selected from the group consisting of methyl group and 2-keto acid group; the city group is selected from the group including NR5, 0, C (0), C (S), S, S (0), S (0) 2, ON (R5), P (0) (R8) and CR39R40; R5 is selected from the group consisting of hydrogen, hydroxyl, amine, alkyl, alkoxy, alkoxy, fluorene Pit group, fermenting group, aromatic acid group and heteroaromatic group; R39 and R4G are independently selected from the group consisting of hydrogen group, hydroxyl group, halogen group, Base, hydroxyalkyl, fluorenyl, arylfluorenyl, heteroarylfluorenyl, fluorenylfluorenyl, alkoxy, alkyl, alkoxyalkyl, alkanyl, self-alkoxy, self-alkoxyalkane Group, alkylsulfonyl, alkylsulfonyl, carboxyl, carboxyalkyl, alkoxycarbonyl, carboxyamido, and carboxyamidoalkyl; M is selected from the group consisting of N and R1-C; R2 and R1 is independently selected from the group consisting of ZG-Q, hydrogen, alkyl, alkenyl, and halo; R1 is optionally selected from the group consisting of amino, aminoalkyl, alkylamino, formamyl, guanidyl, hydroxyl, Hydroxylamino, alkoxy, hydroxyalkyl, alkoxyamino, -39- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) One ---------- ------- ^ ---- Order --------- line (Please read the phonetic on the back first? Please fill out this page again for details) 1222445 A7 B7 V. Description of the invention (37) (Please read the precautions on the back before filling this page) Thiol group, sulphur group, second group lens, three pit base scale, two pit base Sulfanyl, heteroarylamino, nitro, arylamino, aralkylamino, alkylfluorenyl, alkenyl, arylfluorenyl, heteroarylfluorenyl, arylfluorenyl, heteroarylsulfonyl, Self-baking group, hydroxy S alkyl group, cyano group and phosphonic acid group; Z0 is selected from the group consisting of covalent single bond, (CR41R42) q, where q is an integer selected from 1 to 6, (CH (; R41X) g -W0 < CH (R42X) p, where g and P are independently integers selected from 0 to 3, and W0 is selected from the group consisting of 0, S, C (0), C (S), C (0) 0, C (S) 0, C (0) S, C (S) S, C (0) N (R41), (R41) NC (0), C (S) N (R41), (R41) NC (S ), 0C (0) N (R41)? (R41) NC (0) 0, SC (S) N (R41)? (R41) NC (S) S? SC (0) N (R41), (R41) -NC (0) S, OC (S) N (R41), (R41) NC (S) 0, N (R4 2), C (0) N (R41), (R41) NC (0) N- (R4 2 XN (R4 2) C (S) N (R41), (R41) NC (S) N (R4 2 \ S (0 \ S (0) 2? S (0) 2N (R41 \ N (R41 _2, Se, Se (0), Se (0) 2, Se (0) 2N (R41), N (R4% Employee Consumer Cooperatives, Bureau of Intellectual Property, Ministry of Economic Affairs N (R7) P (0) (R8), P (0) (R8) N (R7), N (R41), ON (R41) and SiR2 8 R2 9, and (CH (R41)) e-W22 -(CH (R42)) h, where e and h are integers independently selected from 0 to 2, and W22 is selected from the group consisting of CR41 = CR42, CR41R42 = C (vinylidene), and ethylene block (C e C 1,2 ethyl block), 1,2 cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1, 3-Cyclopentyl, 2,3_Morphine 4-Mulyl, 2,4-Morphyrinyl, 2,6-Morphyrinyl, 3,4-Morpheline, 3,5-Morphine Base, 1, 2 · hexahydropyracyl, 1,3 · hexahydropyracyl, 2,3 · hexahydropyracyl, 2,6-hexahydropeptyl, 1,2 · hexahydropyridine Yodo, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2,4-hexamethylpyridyl, 2,6-hexahydropyridyl, 3,4-hexahydropyridyl, 1 2,2-tetrahydropyrrolyl, 1,3-tetrahydropyrrolyl, 2,3_tetrahydropyrrolyl, 2,4_tetrahydropyrrolyl, 2,5_tetrahydropyrrolyl, 3,4_tetrahydro Pyrrolyl, 2,3_tetrahydropyranyl, 2,4 · tetrahydrofuranyl, 2,5_tetrahydrofuranyl and 3,4 · -40- This paper size applies to Chinese National Standards (CNS) A4 size (210 X 297 mm) 1222 445

R A7 ^ __ B7___ 5. Description of the invention (38) Tetrahydrofuranyl, with the proviso that when R4 1 and R42 are directly bound to N, they are selected from the group other than halo and cyano, and Z0 is directly bound to the pyrimidinone ring; R41 and R42 are independently selected from the group consisting of methylamino, hydroxylamino, hydrogen, hydroxyl, amine, fluorenyl, cyano, aryloxy, carbofluorenyl, fluorenyl, arylfluorenyl, heteroarylfluorenyl, heteroaryl Aryloxyalkyl, alkoxy, alkyl, aryl, aralkyl, aryloxyalkyl, aryloxyalkyl, oxo, oxo, aryloxyalkyl, Cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, fluorenyl, pinenyl, cycloalkyl, cycloalkenyl, halooxy, halo Oxyalkenyl, fluorenyloxyhexyl, 1¾cycloalkoxy, halocycloalkoxyalkyl, _cycloalkenyloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl Base, heteroarylalkyl, heteroarylthioalkyl, heteroaryl thiosulfanyl, pit base continuation group, _fe group base group, aryl group base group, aryl group S & group Base, aromatic entertainment * base performance 8¾ base, environmental resistance base continued 醯: Base, cycloalkylsulfonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfonyl and arylalkyl; Q is formula (Π) ·· 11 ---- ------------- ^ ---- Order --------- line (please read the notes on the back before filling out this page) Employee Cooperatives of Intellectual Property Bureau, Ministry of Economic Affairs Print

R 9〆WRl2 D " 13 (II) where D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, 0, S and covalent bond -41-This paper size applies to Chinese National Standard (CNS) A4 Specifications (210 χ 297 mm) 1222445 A7 B7 Five acts, invention description (39 with the condition that no more than one is a covalent bond, D1, p2, J 'more than one is 0, D, D2, Ji, # And κι, when two of Dl, D2, J1, j2, and κ1 are 0 and S; D1 ,, J 'is n, which must be a covalent bond, and 1) 1, D2, Jl, In J2 and κ1, Zhao Shi 4 and 4 were kept in order to remain broken. The condition is that each of 9, 9, 10, 11, 12, and 13 is independent and can be selected from a distance. Trivalent nature, divalent nature and quality of sulfur; Q is selected from formula (m) as appropriate. Please read the notice on the back before filling this page Λ〇

(III), d'd4, J3 and j4

Among them, D3, D4, J3, and J4 are independently selected from the group consisting of C, N, 〇, and S, and no more than one is 〇, and no more than one of D3, D4, J3, and J4 is S i0, RA1. Valency II Order The Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Online Economy printed no more than three of D1, D2, J1 and J2 as N, with the proviso that each of R and R1 2 was independently selected to maintain the four-valent nature of carbon. ; The divalent nature of mass, sulfur and the divalent nature of oxygen; Q is optionally selected from the group consisting of hydrogen, alkyl, alkoxy, alkylaminothio, _alkylthio, alkenyl, alkynyl, saturated Heterocyclyl, partially saturated ring-opening group, fluorenyl, arylfluorenyl, heteroarylfluorenyl, cycloalkyl, cycloalkylpyridylcycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl, Alkyl, halooxyhalogeno, halocycloalkyl, autocycloalkenyl ,! | Alkoxyalkyl, haloalkenyloxyalkane 42- reference paper size applicable to Chinese National Standard (CNS) A4 (210 X 297 public love) 1222445 A7 B7_ V. Description of the invention (40) (Please read the note on the back first Please fill in this page again) for alkyl group, cycloalkoxyalkyl group and self-cycloalkenyloxyalkyl group, with the proviso that when Q is a hydrogen group, 'zG is selected from the covalent single bond; K Is (CR4aR4b) n, where η is an integer selected from 1 to 2; R4a and R4b are independently selected from the group consisting of halo, hydrogen, hydroxy, cyano, hydroxy, phenyl, >, KI, aryl aryl, heteroaryl, thioalkyl, i-alkyl, i-alkenyl, and cyano-alkyl; when K is (CR4aR4b) n, EG is E1, where E1 is selected from the group consisting of Valence single bond, 〇, S, C (0), C (S), C (0) 0, C⑸0, c (o) s, C (S) S, C (0) N (R7), (R7) NC⑼, C⑸ N (R71 (R7) NC (S)? 0C (0) N (R7)? (R7) NC (0) 0? SC (S) N (R7)? (R7) NC (S) S? SC (0) N (R7)? (R7) NC (0) S? 0C (S) N (R7)? (R7) NC (S) 0? N (R8) C (0) N (R7% (R7 ) NC (0) N (R8), N (R8), C (S) N (R7), (R7) NC (S) N (R8), S (0), S (0) 2, S (0) 2N- (R7), N (R7) S (0) 2, S (0) 2 N (R7) C (0), C (0) N (R7) S (0) 2, P (〇) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), N (R7), ON (R7), CR4a = CR4b, ethynylene (C; 1,2-ethynyl), and C = CR4aR4b; K is (CH (R14)) jT as appropriate , Where j is an integer selected from 0 to 2, and T is selected from the group consisting of covalent single bonds, 0, S, and N (R7), with the condition that (01 (1114)) j is bound to the pyrimidinone ring; Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs when K is (CH (R14)) j_T, E0 is optionally E2, where E2 is selected from the group consisting of covalent single bonds, C (0), CXS), c ( o) o, c (s) o, C (0) S, C's 8,0 (0)] ^ (117), (117) 1 ^ C (0), C (S) N (R7), ( R7) NC (S), (R7) NC⑼0, (R7) NC (S) S, (R7) NC (0) S, (R7) NC⑻0, N (R8) C (0) N (R7), (R7 ) NC (0) N (R8), N (R8), C (S) N (R7), (R7) NCXS) _N (R8), S (0), S (0) 2, S (0) 2N (R7), N (R7) S⑼2, S (0) 2N (H) C (0), C (0) N (H) -S (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R8), N (R7), and N (R7); K is optionally G- (CH (R15)) k, where k is an integer selected from 1 to 2 , And -43- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (41) G is selected from the group consisting of 0, S, and N (R7), with the proviso that when k is 1, R15 is not a hydroxyl group, a cyano group, an amino group, an amino group, an alkylamino group, or two Alkylamino and hydrogenthio groups; when K is G- (CH (R15)) k, EG is optionally E3, where E3 is selected from the group consisting of covalent single bonds, 0, S, C (0), C (S), C (0) 0, c (s) 0, C (0) S, C (S) S, C (0) N (R7), (R7) NC (0), C (S) N (R7), (R7) NC (S), 0C (0) N (R7), (R7) NC (0) 0, SC (S) N (R7), (R7) NC (S) S, SC ( 0) N (R7), (R7) NC (0) S, 0C (S) N (R7), (R7) NC but 0 small (to 8) -C (0) N (R7), (R7) NC (0) N (R8), N (R8), C (S) N (R7), (R7) NC (S) N (R8), S (0), S (0) 2, S (0) 2 N (R7), N (R7) S (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), N (R7) , ON (R7), CR4a = CR4b, ethylene block (CeC; C = CR4aR4b; is the formula (IV): 1,2-ethynyl), and 0s

R 17 18

R 19 ----------------- K ---- order --------- line (please read the back ^ / note 咅 first? Matters before filling out this page ) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs ^ (IV) where D5, D6, J5 and J6 are independently selected from C, N, Q, s and covalent bonds, with the condition that no more than one is covalent Bond, K2 is independently selected from the group consisting of C and B, no more than one of D5, D6, J5 and J6 is 0, no more than one of D'D6, J5 and j6 is S 'when D5, D6, J5 and J6 When two are 0 and s, one of J5 and J6 must be a covalent bond. When K2 is N4 ·, d6 j5 and J6 are not history. 44 1222445 A7 V. Description of invention (42) After three are N , And when K2 is carbon, d5 D6 has 5 its τ6 丄 ^^. , 13 ,: [and no more than four in Shanghai are N, with the proviso that Rl 6 Rl 7 8 is ρ 1 9々yu, K, R, and each are independently selected to maintain the tetravalent nature of carbon, Qi Xi's Secret Fat Qixin 1 > [Beijing Health Department, the divalent nature of sulfur and the divalent nature of oxygen; R and R are used independently as the case may be to form a linear with 3 to 6 adjacent atoms Partial spacer, connected to form a ring, selected from the group consisting of a base ring having 5 to 8 adjacent members, a partially saturated heterocyclic ring having | adjacent members, | a heterocyclic ring having 5 to 6 adjacent members Aryl, and aryl;

Qb is selected from the group consisting of nr20r21, + nr20r21r22, oxy, alkyl, aminoalkylalkenyl, alkylamino, dialkylamino, dialkylfluorenyl, fluorenylamino, and Qbe, where Qbe Is a hydrogen group, and R20, R2i & R22 are independently selected from the group consisting of a hydrogen group, an amino group, an alkyl group, a hydroxyl group, an alkoxy group, an aminoalkylenyl group, an alkylamino group, a dialkylamino group, and a hydroxyalkyl group, The condition is that more than one of R20, R2 1 and R22 are not hydroxyl, alkoxy, alkylamino, amine, and dialkylamino groups at the same time. When K2 is a mineral, R20, R2 1 and R22 must not be Hydroxyl, alkoxy, amine, amine and diamine; R20 and R21, R20 and R22, and r21 and R22 are independently selected to form spacer pairs, where the spacer pairs are together Adopted to form a linear part with 4 to 7 adjacent atoms and connect the bonding points of the members of the spacer pair to form a heterocyclyl ring with 5 to 8 adjacent members, with the proviso that not more than one is used at the same time Spacer pair, including R2G and R21, R20 and R22, and R21 and R22;

Qb is selected from N (R26) S02N (R23) (R24), N (R26) C⑼0R5, -45- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) (please first) (Please read the notes on the back and fill in this page again.) Packing ---- l · --- Order ί s'. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445

V. Description of the invention (43) N (R26) c⑼SR5, N (R26) C⑻OR5 and N (R2 6) C⑼SR5, with the condition that (Please read the note on the back? Matters before filling out this page> When including R23, When two of R24 and R26 are bonded to the same atom, no more than one of R23, R24 and R26 is a hydroxyl group, an alkoxy group, an alkylamino group, an amine group and a dialkylamine group;

Qb is optionally selected from the group consisting of dialkylfluorene, trialkyl scale, C ^ NR25) ^^ 23 ^ 4, N (R2 6) C (NR2 5) N (R2 3) (R2 4), N (R2 6) c (〇) n (r2 3) (r2 4), n (r2 6) cCDN_ (R2 3) (R2 4), C (NR2 5) 〇R5, C (〇) n (r2 6) C ( nr2 5) n (r2 3) (r2 4), c (s) n (r2 6) C (NR25) N (R23) (R24), N (R26) N (R26) C (NR25) N (R23) (R24), ON (R26) -C (NR2 5) N (R2 3) (R2 4), N (R2 6) N (R2 6) S02 (R2 3) (R2 4), C (NR2 5) SR5, C (0) NR23R24 and C (0) NR23R24, with the proviso that when two systems including R23, R24 and R26 are bonded to the same atom, no more than one of R23, r24 & r26 may be a hydroxyl or alkane Oxygen, alkylamino, amino or dialkylamino, and the Qb group is directly bonded to a carbon atom; H23, H24, H25, and H26 are independently selected from the group consisting of hydrogen, alkyl, and hydroxy , Feoxy, amine-based amine, amine, amine, diamine, and amine; R23 and R24 are used together as appropriate to form a linear spacer with 4 to 7 adjacent atoms Part, connecting the bond points to form a heterocyclic ring with 5 to 8 adjacent members; employees of the Intellectual Property Bureau of the Ministry of Economic Affairs Cooperatives printed QMf, selected from covalent single bonds, (CR37R38) b- (W〇) az, where az is an integer selected from 0 to 1, b is an integer selected from 1 to 4, and WG is selected Since including 0, S, C (0), C (S), C (0) 0, C (S) 0, C⑼S, C (S) S, CXOMR14), (R1 4) nc (o), c ( s) N (RX 4)? (R14) NC (S)? OC ^ NCR14) 5 SC (S) N (R14% SC (0) N (Rl 4% OC (S) N- (R14 \ N (RX 5) C (0) N (R14 \ (R14) NC (0) N (R15 \ N (RX 5) C (S) N (R14), (Rl 4) NC (S) N (R15), S ( 0), S (0) 2, S (0) 2N (R14), N (R14) S (0) 2, P⑼ (R8), N (R7) P (-46- This paper size applies to Chinese national standards ( CNS) A4 size (210 x 297 mm) " Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 _______ B7 V. Description of the invention (44) 〇) (R8 \ P (0) (R8) N (R71 N (RX 4)? ONCR14) ^ (CHCR14)) c -W1-(CHCR15)) d, where c and d are integers independently selected from 1 to 4, and W1 is selected from the group consisting of 0, S, C (0) , C (S), C (0) 0, C⑶0, C (0) s, C (S) S, CXOMR14), (R1 4) nc (o), C (S) N (R141 (R14) NC ( S)? OC ^^ R14 \ (R14) NC (0) 0, SqS) ^^ 4)? (R14) NCCDS, SCCCOl ^ R14), (R14) NC (0) S, OCXSKR14), (R14) NC⑶0 , N (Ri5) C (0) N (Ri4), (R14 WqOjNCR15), NCR15 4), (R14) NC⑻- N (R; 5), S (0), S (0) 2, S (0) 2 NCR14 ), N (Ri4) S (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R8) N (R7), N (Ι ^ 4) ONCR14), and (CI ^ R14)) e _W2 2-(CI ^ R15)) h, where e and h are integers independently selected from 0 to 2, and W22 is selected from CR41 = CR42, CR41R42 = C (Vinylidene), ethynylene (Ce C; 1,2-ethynyl), 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl , 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morphol Phenyl, 3,5-morpholinyl, 1,2-hexahydropyridyl, 1,3 · hexahydropyridyl, 2,3_hexahydropyridyl, 2,6-hexahydropyridine Calliyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2,4-hexahydropyridyl, 2,6-hexahydrop-pyridyl , 3,4 · Hexahydrop-pyridyl, 1,2-tetrahydropyridine, 1,3-tetrahydropyroyl, 2,3-tetrahydroeryl, 2,4 · tetrahydro p-blocyl, 2,5-tetrahydro-p-blocyl, 3,4-tetrahydro-p-blocyl, 2,3-tetrahydrocranyl, 2,4_tetrahydro Cranyl, 2,5-tetrahydrocranyl, and 3,4-tetrahydrocranyl, with the proviso that when R14 and R15 are directly bonded to N, they are selected from the group other than phenyl and cyano, and (CRHr3 ,, (CH (R14)) c, (CH (R14)) Jf, bound to E0; Y0 is optionally Qb-Qss, where Qss is selected from the group consisting of (CR37R38) f, where f is selected from An integer from 1 to 6, (CI ^ RH ^ -Wyci ^ R15 ^, where c and d are integers independently selected from 1 to 4, and W1 is selected from the group consisting of 0, S, C⑼, C⑻, -47- The standard is applicable to the Chinese National Standard (CNS) A4 specification (21 × X 297 mm) -----------------..---- Order -------- -Line (Please read the note on the back first? Please fill in this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 _______ B7 V. Description of the invention (45) c (0) 0, C (s) 0, C (0) S, C (S) S , CXOMR14), (R14) NC (0), CXS)! ^ 14), (R14) NC (S), OCpMR14), (R14) NC⑼0, SCXSMR14), (R14) NCCDS, SC (0) N_ (R14 ), (R14) NC (0) S, 4), (R14) NC⑸0, N (R; 5) 0 (0) 1 ^ (1114), (R14) N0 (0) N (E ^ 5), N (Ri5 ^ SMR14), (R14 jNCXS ^ R15), S (0), s (0) 2, 8 Jan 2 > ^ 14), N (E; 4) S (0) 2, P⑼ (R8), N (R7) P (0) (R8), P (R8) N (R7), N (R14), ON (R14), and (CH (R14)) e-W2- (CH (R15)) h, Where e and h are integers independently selected from 0 to 2, and W2 is selected from the group consisting of CR4a = CR4b, ethynylene (Cec; 1,2-ethynyl), and C = CR4aR4b, with the conditions of R14 and R15 When it is directly bonded to N, it is selected from the group other than halo and cyano, and (CR37R38) f, (0:11 (1114)). And ((^ (1114)) 6 is bound to E0; Y0 is optionally Qb-Qsss, where Qsss is (CH (R38)) r-W3, Γ is an integer selected from 1 to 3, and W3 is selected from Including 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4 _Cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6 -Morphine, 3,4-Morphyl, 3,5-Morphyl, 1,2-Hydrogen; p-well, 1,3-hexahydro p-well, 1, 4 Hexahydropyridine, 2,3_hexahydropyridine, 2,5 · hexahydropyridine, 2,6_hexahydropyridine, 1,2_hexahydropyridine, 1, 3-Hexahydro p ratio base, 1,4-Hexahydroe-based base, 2,3-Hexahydro p-based base, 2,4 · hexamethane p-based base, 2,5-Hexahydro p-based base Base, 2,6_hexahydro p ratio base, 3,4 · hexahydro p ratio base, 3,5_hexa hydrogen p ratio base, 3,6-hexahydro p ratio base, 1, 2- Tetrahydropyrrolyl, 1,3 · tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4_tetrahydropyrrolyl Hydrogen p-pyrrolyl, 2Η-2,3 · yranyl, 2Η_2,4-piperanyl, 2Η_2,5-piperan Base, 4Η_2,3-piperanyl, 4Η · 2,4 · piperanyl, 4Η-2,5 · piperanyl, 2Η · piperan-2-one-3,4 · yl, 2Η-piperanyl · 2 · Keto-4,5-based-48-This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ------- 1—I Pack ----- ^- --Order --------- (Please read the notes on the back before filling this page) 1222445 Α7 --- 一 -_ Β7 V. Description of the invention (46) (Please read the notes on the back before (Fill in this page), 4H-Culan-4_one-2,3, 3, 2,3-tetrahydrocranyl, 2,4-tetrahydrocranyl, 2,5_tetrahydrofuranyl, 3, 4_tetrahydrofuranyl, 2,3_tetrahydropiperanyl, 2,4_tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 2,6_tetrahydrofuranyl, 3,4_tetrahydrofuranyl Hydrocarbyl and 3,5_tetrahydropiperanyl, and each carbon and hydrogen group containing a nitrogen member of the W3 ring instead of a connection point are optionally one or more of R9, R10, R11 and The group substitution of R12 is subject to the condition that (CH (R38 is bound to E0, and Qb is bound to the lowest number of substituent positions of each W3; Y0 is Qb-QSSSr, where Qsssr is (CH ( R38)) r-w4, r is the Intellectual Property Bureau of the Ministry of Economic Affairs Industrial and consumer cooperatives printed from integers 1 to 3, W4 is selected from the group consisting of hi cyclobutyl, L2 · cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2 · cyclopentyl, ι , 3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholin , 3,5-morpholinyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, M-hexahydropyridyl, 2,3_hexahydropyridyl, 2 , 5-hexamethylpyridyl, 2,6-hexahydropyridyl, 1,2-hexahydropyridyl, ι, 3-hexaargyridyl, 1,4-hexahydropyridyl, 2,3- Hexahydropyridyl, 2,4-hexahydropyridyl, 2,5-hexahydropyridyl, 2,6-hexahydropyridyl, 3,4-hexahydropyridyl, 3,5-hexahydropyridyl, 3,6_hexahydro p-pyridyl, 1,2-tetrahydro p-pyrrolyl, 1,3_tetrahydro p-pyrrolyl, 2,3_tetrahydropyrrolyl, 2,4_tetrahydro Rotyl, 2,5-tetrahydroerrolyl, 3,4-tetrahydroerrolyl, 2H-2,3-p citranyl, 2H-2,4-hydroxyanyl, 2H-2,5- Travelanyl, 4H-2,3-Hyranyl, 4H.2,4-peakanyl, 4H-2,5-Hyranyl, 2H_longan-2-one_3,4-yl, ZH -Shouting -2- left, 4,5 base, 4 Ηρ guanan-4 嗣 2,3-base, 2, 3 · 4 Sulfanyl, 2,4-tetrahydrocarbyl, 2,5-tetrahydrofuryl, 3,4-tetrahydrodecanyl, 2,3__tetrahydro-0 citranyl, 2,4-tetrahydrobranyl , 2,5 · tetrahydropeakanyl, 2,6-tetrahydroanuranyl, 3,4-tetrahydroanurinyl and 3,5_tetrahydroanurinyl 'and containing the W4 ring -49- This paper size applies Chinese National Standard (CNS) A4 specification (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (47) Nitrogen members other than the carbon and hydrogen groups of the connection point are subject to one or more Group substitutions including R9, R10, R11 and RU, with the condition that (CH (R38)) 〆 !, be bound to eg, and Qb be bound to the highest number of substituent positions of each w4; Y0 as Qb as the case may be -Qssss, where Qsss $ (CH (R38)) r_W5, r is an integer selected from 1 to 3 'W5 is selected from the group consisting of 1,4_manganyl, 1,5-manganyl, 1,6_manganyl, 1,7-Indenyl, 2,7-Indenyl, 2,6-Indenyl, 2,5-Indenyl, 2,4-Indenyl, 3,4-Isyl, 3,5-Thinyl, 3 , 6-Indenyl, 3,7-Indenyl, 2,4-Benzenanyl, 2,5-Benzenesulfanyl, 2,6-Benzinyl, 2,7-Benzene Ranyl, 3,4-benzopyranyl, 3,5-benzopyranyl, 3,6-benzopyranyl Base, 3,7-benzocranyl, 2,4-benzofluorenylthio, 2,5 · benzobenzosulfanyl, 2,6-benzobenzosulfanyl, 2,7-benzofluorenylbenzene Base, 3,4-benzenesulfenylthio, 3,5-benzenesulfenylthio, 3,6-benzophenylsulfanyl, 3,7-benzenesulfenylthio, 2,7-imidazolium ( i, 2-a) #bYendyl, 3,4-imidazo (l, 2-a) pyridyl, 3,5-imidazolium (l, 2-a) pyridyl, 3,6-imidazolium (L, 2-a) Edoyl, 3,7-Mijun (l, 2_a) Edoyl, 2,4_pyridyl, 2,5-ΘΘ, and 2,6-pyridine , 2,7 · Indolyl, 3,4 · Adolyl, 3,5_Adolyl, 3,6_Aradyl, 3,7-Anadol, 1,4-Isoamyl, 1 , 5_isoindolyl, i, 6_isoindolyl, 2,4-isoquinolyl, 2,5-isofluorinyl, 2,6-isofluorinyl, 2,7_iso < Thymidyl, 1,3 · heteroquinyl, 3,4 · amidazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-oxazolyl, 2,4 · benzene Benzozolyl, 2,5-benzoxazolyl, 2,6 • benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzoxazolyl, 3,5- Benzamidine isoxazolyl, 3,6-Benzamidine isoxazolyl, 3,7-benzamide isoxazolyl, M_naphthyl, 1,5-amyl, 1,6-fluorenyl, 1, 7- 荇1-8-naphthyl, 2,4-fluorenyl, 2,5-fluorenyl, 2,6-fluorenyl, 2,7-fluorenyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5_quinoline ----------------- ^ ---- order --------- line (please read the note on the back first? (Please fill in this page for matters) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445

V. Description of the invention (48) It (please read the precautions on the back before filling out this page) soil, 2,60 quinolyl, 2,1 quinolinyl, 2,8-quinolinyl, 3,4- Quinolinyl, 3,5-earth 3'6 quinolinyl, 3,7 · junlinyl, 3,8_quinnyl, 4,5-quinolinyl, lindenyl, 4,7 _Quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, M-isoquinolinyl, 1,7-isoquinolinyl, 1,8 -Isoquinolinyl, '-iso4-linyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl glycyrrhizin, 4,8 · iso4-linyl, 3, 'fluorinyl, 3,5 · fluorinyl Group, 3,6 cockolinyl, 3,7-fluorenyl, 3,8-fluorinyl, 4,5_fluorinyl, 4,6_fluorinyl, 4,7_fluorinyl I and 4 ,8- #. Linji ', which contains the nitrogen member of the w5 ring and not the hydrogen point of the connection point, is optionally replaced by one or more groups including R9, R10, Rll, and R12, with the proviso that the furnace system It is bound to the lowest number of substituent positions of each W5, and (CH (R38)) ^ is bound to E〇; printed by the consumer consumer cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is Qb-QSsssr, where QSSSSr is (CH ( R38 is from #, r is an integer selected from 1 to 3, W6 is selected from the group consisting of M_indenyl, u • indenyl, ι, 6_indenyl, 1,7_indenyl, 2,7_indenyl, 2 , 6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2, 4-Benzamidinefuranyl, 2,5-Benzamidinefuranyl, 2,6-Benzamidinefuranyl, 2,7-Benzamidinefuranyl, 3,4-Benzamidinefuranyl, 3,5-benzene Fluorenylfuranyl, 3,6-phenylfluorenylfuranyl, 3,7-phenylfluorenylfuranyl, 2,4-phenylfluorenylphenylthio, 2,5_phenylfluorenylphenylthio, 2,6_phenylfluorenylbenzenesulfanyl Group, 2,7-phenylfluorenylbenzenethio, 3,4-phenylfluorenylbenzenethio, 3,5-phenylfluorenylbenzenethio, 3,6_benzophenylsulfanyl, 3,7-benzenefluorenylbenzenethio , 2,7 · imidazolium (i, 2_a) pyridyl, 3,4_imidazine (1 »pyridinyl, 3, 5_imidazo (i, 2_a) edlide, 3,6_imidazo (^ 2-a) pyridyl, 3,7-imidazolium (i, 2-a) pyridyl, 2,4_ind Indolyl, 2,5-pyridyl, 2,6-pyridyl, 2,7-pyridyl, 3,4 · indolyl, 3,5-pyridyl, 3,6-indole-51 -This paper uses the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 1222445 A7. 5. Description of the invention (of) t-based, 3,7_ < indolyl, 1,4_isofluorinyl,丨, 5_isoindolyl, i, ^ iso < wood-based, 2,4 · isoΘbmuyl, 2,5-isoΘ 丨 hexyl, 2,6-isog 丨 hexyl, 2,7- Heterogeneous base, 1, 3 · different Θ 丨 Duoji, 3,4 · the 5 丨 Junji, 3,5 · 4 丨 Junji, 3,6-port 5 丨 Junji, 3,7- 啕Yenyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzoxazolyl Oxazolyl, 3,5-benzidine isoxazolyl, 3,6_benzisoisonoxazolyl, 3,7_benzidine isoxazolyl, i, each hydrazone, 1,5-naphthyl, 1,6_ ^: group, 1,7_fluorenyl, ι, 8_fluorenyl, 2,4-fluorenyl, 2,5-naphthyl, 2,6 · fluorenyl, 2,7-fluorenyl, 2 , 8-fluorenyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7- Quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3, quinolinyl, 4,5-quinolinyl, 4,6.4 lysyl, 4,7-4 lysyl, 4,8. Lylinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl , 1,6_isoquinolinyl, 1,7_isoquinolinyl, ι, 8_isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6 -Isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl , 4,8-isoquinolinyl, 3,4-fluorinyl, 3,5 · fluorinyl, 3,6-fluorinyl, 3,7-fluorinyl, 3,8-fluorinyl, 4,5-fluorinyl, 4,6-fluorinyl, 4,7-fluorinyl, and 4,8-fluorinyl, and each carbon and hydrogen group containing a nitrogen member of the W6 ring instead of the point of attachment , Is optionally substituted by one or more groups including R9, R10, R1, and R12, with the proviso that Qb is bound to the highest number of substituent positions of each w6, and (CH (R3 8)) r System bound to E0. In another specific embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is selected from the group consisting of 0 and S; B is formula (V): —--------- 4 ^ —l · —Order --------- line, (Please read the note on the back? Matters before filling out this page) Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs-52-1222445 Printed by the Consumer ’s Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs System A7 B7 V. Description of the invention (50) r3 4 r3VkL, II f r32 / D \ ^ D2 \ r36 (V) where D, D2, J'J2 and K1 are independently selected from the group consisting of c, N, 0, s and Covalent bonds, with the proviso that no more than one is a covalent bond, no more than one of D1, D2, J1, J2, and K1 is 0, and no more than one of D1, D2, J1, J2, and K1 is S. When D1 When two of D2, J1, J2, and K1 are 0 and s, one of D, D2, J1, J2, and K1 must be a covalent bond, and no more than four of D1, D2, J1, J2, and κ1 Is N; R9, R10, R ", R12, R13, R16, r17, r18, r19, r32, r33, r34, r35, and R3 6 are independently selected from the group consisting of hydrogen, acetamido, and haloacetamido Base, formamyl, guanidyl, dialkylfluorenyl, trialkylphosphonium, dialkylphosphoranyl, carboxyl, Heteroaralkylthio, heteroarylalkoxy, cycloalkylamino, fluorenylalkyl, fluorenylalkoxy, arylfluorenylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl , Arylalkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, sulfonyl group, sulfonyl group, alkynyl, aryl group Transalkylene alkyl, halocycloalkyl, self-cycloalkenyl, cycloalkylsulfinamidinyl, cycloalkylsulfinamidinylalkyl, cycloalkylsulfinamido, cycloalkylsulfinamidoalkyl , Heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkoxy, alkoxy, alkoxyalkyl, fluorene Alkoxyalkyl, heteroarylalkoxy, cycloalkoxy, cyclofluorenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkyldi Oxygen and halocycloalkanes-53- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ------------------ Order --- ------ line, (Please read the precautions on the back before filling this page) A7

V. Description of the invention (5!) (Please read the notes on the back before filling out this page) Printed oxygen, _cycloalkenyloxy, self-cycloalkenyloxy, 卣Cyclopentyloxyalkyl, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, arylalkylamino , Arylthio'arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfinyl Alkyl, heteroarylsulfinylalkyl, heteroarylsulfinylalkyl, alkylsulfinyl, alkylsulfinylalkyl, alkylsulfinylalkyl, || alkane Sulfosulfanyl alkyl, alkylsulfonamido, alkylaminosulfonamido, sulfonamidosulfonyl, monoalkylsulfonamidosulfonyl, dialkylsulfonamidosulfonyl, monoaryl Alkylsulfonamido, arylsulfonamido, diarylsulfonamidosulfonyl, monoalkylmonoarylsulfonamidosulfonyl, arylsulfinamido, arylsulfonamido , Heteroarylthio, heteroarylsulfinamilide, heteroarylsulfonyl Base, heterocyclylsulfonyl, heterocyclylthio, alkenyl, alkenyl, arylfluorenyl, heteroarylfluorenyl, arylfluorenyl, heteroarylfluorenyl, fluorenyl, sulfonyl , Fluorenyl, block, alkoxy, alkoxyalkyl, alkanedioxy, i-alkylenedioxy, cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower carbocycloalkyl Alkyl, low-carbon cycloalkenylalkyl, halo, fluorenyl, alkynyl, oxo, oxo, alkynyl, aralkyl, hydroxyalkyl, alkylalkenylamino, Hydroxyheteroaralkyl, arylalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl , Heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylfluorenyl, heteroarylalkenyl, carboxyalkyl, alkoxycarbonyl, alkoxycarboxamide Alkyl, alkyl, amido, carbonyl, amido, aryl, amido, carbonyl, amido, alkoxy, carbonyl, alkyl, alkenyl, carboxy, aryl, oxo, carboxylic, amido, and amido • 54-I paper size applies to China National Standard (CNS) A4 specifications (210 X 297 mm) '1222445 A7 -------- B7 V. Description of the invention (52) (Please read the notes on the back before filling this page) Alkyl, cyano, self-alkoxycarbonyl, Phosphonic acid group, phosphonic acid alkyl group, diarylalkoxyphosphonic acid group and diarylalkoxyphosphonic acid alkyl group; and 16,1119,1132,1133,1134,113 5 and 113 6 are independent as the case may be (^, With the proviso that no more than one R10 and R19 are Qb at the same time, and Qb is Qbe; B is optionally selected from the group consisting of hydrogen, trialkylsilyl, C2-C8 alkyl, and C3_C8 alkene , C3-C8 alkenyl, C3-C8 alkynyl, C2-C8 haloalkyl, and C3_C8 haloalkenyl, where each member of the group b is, as the case may be, the highest from the point of attachment of B to A and contains 6 atoms Any carbon site is replaced by one or more groups including Hua 32, Hua 33, Hua 34, Hua 35, and Rule 36; printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. Cycloalkyl, C5-C10 cycloalkenyl, and C4-C9 saturated heterocyclyl, where each ring carbon is optionally substituted by R33, and one ring carbon, not the ring carbon at the point of B to λ attachment, is optionally ketone Radical substitution, Provided that no more than one ring carbon is substituted by a ketone group at the same time, the ring carbon and nitrogen atom of the carbon atom adjacent to the connection point are optionally substituted by R9 or Rl3, and the ring carbon or nitrogen adjacent to the position of R9 and two atoms away from the connection point Atom, which is replaced by R10 as appropriate, a ring carbon or nitrogen atom adjacent to R13 and two atoms away from the connection point, and is replaced by R12, which is a ring carbon or nitrogen atom that is three atoms away from the connection point and adjacent to R10, It is replaced by 1 depending on the situation. The ring carbon or nitrogen atom two positions away from the junction point JL Zheng near Ri2 is replaced by R3 3 as appropriate, and the ring is located four atoms away from the junction point and adjacent to r1 1 and R3 3. A carbon or nitrogen atom, optionally substituted by R34; A is selected from the group consisting of covalent single bonds, (W7) rr_ (CH (R15)) pe (CH (Rl5)) pr (W7) rr 'where rr is selected from Integer from 0 to 1, pa is an integer selected from 0 to 6, and W7 is selected from the group consisting of _ -55- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445 A7

V. Description of the invention (53) (R) NC (S) and N (R7) 'The additional condition is that the order and pa cannot be more than one at the same time as 0; (Please read the notes on the back before filling this page) R7 and R8 Is independently selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxyalkyl; R14, R15, R37 and R38 are independently selected from the group consisting of hydrogen, hydroxy, self-based, alkyl, alkoxyalkyl, alkyl, From alkoxy and alkoxyalkyl; R14 and R38 can be independently selected from arylfluorenyl and heteroarylfluorenyl; less selected from NR5, c (〇) and S (〇) 2; R5 selected Including hydrogen, hydroxyl, alkyl, and alkoxy; R39 and R4G are independently selected from the group consisting of hydrogen, hydroxyl, halo, hydroxyalkyl, alkyl, alkoxyalkyl, ialkyl, and alkoxy And i alkoxyalkyl; M is selected from the group consisting of n and R1-C; R1 is selected from the group consisting of hydrogen, alkynyl, alkenyl, cyano, halo, self-calcined, haloalkoxy, and alkane Thio, amine, aminoalkyl, alkylamino, formamidine, guanidyl, trisyl, ceramide, thiol, trisyl, thiol, thiol, alkylthio And phosphonic acid group; R2 is Z0_Q; Member of Intellectual Property Bureau, Ministry of Economic Affairs Z0 printed by the consumer cooperative is selected from the group consisting of covalent single bonds, (CR41R42) q, where q is an integer selected from 1 to 3, (CH (R41)) g-W0- (CH (R42)) p, where g And P is an integer independently selected from 0 to 3, and W0 is selected from the group consisting of 0, s, c (o), s (o), s (o) 2, n (r41), and ON (R41), and ( CHCRO ^ -WnKCH ^ R42): ^, where e and h are integers independently selected from 0 to 2, and W22 is selected from the group consisting of CR41 = CR42, 1, 2 · cyclopropyl, 1, 2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2, 6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridine-56-Applicable to this paper standard China National Standard (CNS) A4 Specification (210 X 297 mm) 1222445

R 12 R 13 A7 V. Description of the invention (54) group, 2,3-hexahydropyridyl, 2,6-hexahydropyridyl, 丨, 2-hexahydropyridyl, i, 3-hexapyridine Radical, 2,3-hexahydropyridyl, 2,4-hexahydropyridyl, 2, cardiodihydropyridyl, 3,4-hexahydropyridyl, 1,2-tetrahydropyrrolyl, Airpyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5 · tetrahydropyrrolyl, 3,4-tetrahydropyrrolyl, 2,3-tetrahydrofuryl, 2, private Tetrahydrofuranyl, 2 i tetrahydrofuranyl and 3,4-tetrahydrofuranyl, with the proviso that they are directly bonded to the pyrimidinone ring; R41 and R42 are independently selected from the group consisting of methylamido, hydroxylamine, hydrogen, and hydroxyl , Amine and alkyl; Q is selected from the group consisting of hydrogen, with the proviso that 20 is not a covalent single bond: formula (11): (II) where D1, D2, J1, J2 and K1 are independently selected Including c, N, 〇, s and covalent bonds, with the additional condition that no more than one is a covalent bond, 〇1, 〇2, '^ 2 and the super 1 to 0 is 0, so, 1) 2 ,: ^ When 2 and [1 do not exceed 'one is 〆, when two of D1, D2, J1, J2, and Kl are 0 and s, then, β p and r1 must be Valence bond, and ^, jealousy / and no more than four are ^^, with the conditions that ..., ..., ..., ^ and ... ^ each independently selected 'to maintain the nature of tetravalent, trivalent of nitrogen Nature, divalent nature of sulfur and divalent nature of oxygen »_______ -57- This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 χ 297)

1222445 Alkyl R- A7 B7 V. Description of the invention (55) Quality; K is (CR4aR4b) n, where η is an integer selected from 1 to 2; and "" and R4b are independently selected from the group consisting of halogen, hydrogen, and hydroxyl Alkylalkoxyalkyl, alkylthioalkyl and alkanyl; EG is selected from the group consisting of covalent single bonds, C (0), C (S), C (0) N (R7), (R7) NC (0), S (〇) 2, (R7) NS (0) 2 & S (0) 2N (R7); is formula (IV):

Qs 18

J (Please read the notes on the back before filling this page) R. 6〆 -Dc

• R 19 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (IV) where D5, D6, J5 and J0 are independently selected from the group consisting of C, N, 0, S and covalent bonds. Price key, K2 is C, no more than one of D5, D6, J5 and J6 is 0, no more than one of D5, D6, J5 and J6 is S, when two of D5, D6, J5 and J6 are 0 and At S, one of D5, D6, J5, and J6 must be a covalent bond, and when K2 is carbon, no more than four of D5, D6, J5, and J6 are n, and the conditions are R10, R17, and R18. And R19 are independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Qb is selected from the group consisting of NR20R21, + NR20R2lR22, aminoalkylalkenyl, and Qbe, where Qbe is hydrogen, and R20, R21, and RU are independently selected from the group consisting of hydrogen, alkyl, hydroxyl, amino, and aminoalkane Alkenyl, dialkylamino, alkylamino-58- This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) 1222445 Printed by A7 B7, Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs (56) and meridian: the fe group is subject to the condition that at least one of R20 and R21 is not meridian, amine, amine, or diamine;

Qb is optionally selected from the group consisting of C (NR2 5) NR2 3 R24, N (R2 6) C (NR2 5) N (; R2 "(R24), C (0) N (R2 6) C (NR2 5) N (R2 3) (R2 4)? N (R2 6) N (R2 6) C (NR2 5) N (R2 3) (R2 4) and ON (R26) C (NR25) N (R23) (R24), The condition is that when two systems including R23, R24 and R26 are bonded to the same atom, no more than one of R23, R24, and & 26 is a hydroxy, alkylamine, amine or dialkylamino group; R23 R24, R25 and R26 are independently selected from the group consisting of hydrogen, alkyl, hydroxyl, amino, alkenylamino, dialkylamino, alkylamino and hydroxyalkyl;

Qs # is selected from the group consisting of covalent single bonds, (CR37R38) b_ (W0) az, where az is an integer selected from 0 to 1, b is an integer selected from 1 to 5, and W0 is selected from the group consisting of 0, C ( 0), S (0) A0) 2, S (0) 2N (R14), N (R14) S (0) 2 & N (R14), (CH (R14)) c- WMCI ^ R15), where C and d are integers independently selected from 1 to 4, and W1 is selected from the group consisting of 0, S, C (0), C (S), C (0) 0, CXS) 0, C (0) S, ( XS) S, C (0) N (R14), (R14) NC (0), CXSMR14), (R14) NC (S), OCXO ^ R14), (R14) NC (0) 0, SC⑶N (E 4), (R14) NC asked 8,8 <: (0)] ^ (1114), (1114)] ^ (0) 8,0 (:( 8)] ^ (1114), (1114) -NC (S) 0, NCR15) C (0) N (R14% (R14) NC (0) N (R15)? NCR15) C (S) N (R14)? (R14) N0 × 8) N (Κ; 5), S (O), S (0) 2, 8 (0) 2N (B; 4), N (R; 4) S (0) 2, P (0) (R8), N (R7) P (0) (R8), P (0) (R84), ON (R14), and (01 (1114)) e-W22- (CH (R15)) h, where e and h are integers independently selected from 0 to 2, And W22 is selected from the group consisting of CR41 = CR42, CR41R42 = C (vinylidene), ethyleneidene (C ^ c; 1,2-ethynyl), 1,2-cyclopropyl, 1,2-cyclobutane Group, 1,2-cyclohexyl, n-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3- Fluorolinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2_hexa-59- Standards are applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) ---------------- K ---- Order --------- Line ( Please read the notes on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7-B7 V. Description of the invention (57) Hydropyridine, 1,3-hexahydropyridine, 2, 3-hexahydropyridyl, 2,6-hexahydropyridyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2,4-hexa Hydropyridyl, 2,6-hexahydropyridyl, 3,4-hexahydropyridyl, 1,2-tetrahydropyrrolyl, 1,3-tetrahydropyryl, 2,3 · tetrahydropyryl Group, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4 · tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydrocranyl and 3,4-tetrahydrocranyl, with the proviso that when R14 and R15 are directly bonded to N, they are selected from the group other than halo and cyano, and (CR37R38) b , (CH (R14)) c & (CH (R14)) ^, combined to E °; Y0 depends on the situation as Qb_Qss, where Q ss is selected from the group consisting of (CR37R38) f, where f is an integer selected from 1 to 4, wherein 0 and d are integers independently selected from 1 to 2, and w1 is selected from the group consisting of 0, s, q0), q0 ) _N (Ri4), (R ") NC⑼, IsKR15 XXOMR14), (R14 ^ CXOMR15), N (Ri4), ON (R14), and (CH (R14)) e-W2_ (CH (R15)) h, where 6 and 11 are independently selected from integers of 0 to 2, and W2 is selected from the group consisting of CR4a = CR4b, ethynylene (CeC; 1,2-ethynyl), and C = CR4aR4b, with the condition that Rl4. When Rl5 is directly bound to N, it is selected from the group other than halo, and (CR37R38) f, (CI ^ R14)) c and (CI ^ R14)) e are bound to E0; Υ0 is Qb_Qsss, where Qsss is (CH (R38)) r_w3, r is an integer selected from 1 to 2, W3 is selected from the group consisting of 1,1-cyclopropyl, i, fluorene cyclopropyl, 1,1-cyclobutyl, 1, 2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, i 4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl 2,4_morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5_morpholinyl, 1, 2 · Hydroxypyridyl, 1,3 · Hydroxypyridyl, M_Hydroxypyridyl 、 _____- 60 -___ This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm 1-* ---- ----------------- ^ ---- Order --------- line (please read the notes on the back before filling this page) 1222445 A7 B7 V. Description of the invention (58) * · (Please read the phonetic on the back? Please fill in this page again for details) 2,3_hexahydro p ratio p well foundation, 2,5-hexahydro p well foundation, 2,6-hexahydro outer b π well foundation, 1,2-hexaoxedrine base , 1,3-hexahydrop-pyridyl, 1,4-hexahydrop-pyridyl, 2,3- 7T hydrogen; pyridyl, 2,4-hexahydropyridyl, 2,5-hexahydropyridine Radical, 2,6-hexahydropyridyl, 3,4 · hexahydropyridyl, 3,5 · hexahydropyridyl, 3,6-hexahydropyridyl, 1,2-tetrahydropyrrolyl, 1, 3 _Tetrahydropyrrolyl, 2,3 · tetrahydropyrrolyl, 2,4 · tetrahydropyridyl, 2,5-tetrahydrop-pyridyl, 3,4_tetrahydroerrolyl, 2H- 2,3_Xyranyl, 2Η2,4-piperanyl, 2Η2,5_piperanyl, 4H-2,3-piperanyl, 4H-2,4-piperanyl, 4H_2, 5_Travelanyl, 2H-anan_2 · 嗣 -3,4_yl, 2H-Travelan-2- 嗣 -4,5-yl, 4H · anan-4-¾ _2,3_yl, 2,3_tetrahydrolan, 2,4 · tetrahydrolan, 2,5 · tetrahydrolan, 3,4-tetrahydrolan, 2,3-tetrahydrolan, 2,4_tetrahydrosulfanyl, 2,5 · tetrahydrosulfanyl, 2,6-tetrahydrosulfanyl, 3,4 · tetrahydroguananyl, and 3,5_tetrahydropiperanyl And each carbon and hydrogen group containing a nitrogen member of the W3 ring instead of a connection point is optionally one or more Including R9, R10, Ri 1 and R12 of the groups, with the proviso that (〇1 (line 1138 from binding to E0, and

Qb is the minimum number of substituent positions bound to each W3; Y0 is Qb-Qsssr as appropriate, where Qsssr is (CH (R38 ^ _W4, r is printed from 1 to 2 by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs) Integer, w4 is selected from the group consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, and 1,3-cyclopentyl Group, 2,3 · morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5 Morpholine, 1,2-Hydroxypyridyl, ι, 3-Hydroxypyridyl, 1,4-Hydroxypyridyl, 2,3 · Hydroxypyridyl, 2,5- Hexahydropyridyl, 2,6-hexahydropyridyl, 1,2-hexahydropyridyl, ι, 3-hexahydropyridyl, 1,4-hexahydropyridyl, 2,3-hexahydropyridine , 2,4-hexahydropyridyl, 2,5-hexahydropyridyl, 2,6-hexahydropyridyl, 3,4-hexamethylpyridyl, 3,5-hexahydropyridyl, _ -61 -This paper is used in the national standard (CNS) A4 specification (210 X 297 public love) 1222445 A7 B7 of the paper standard. V. Description of the invention (59) (Please read the note on the back? Matters before filling out this page) 3, 6-hexahydropyridyl, ι, 2-tetrahydropyrrolyl , Ι, 3 · tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4-tetrahydropyrrolyl, 2H-2, 3-piperanyl, 2H_2,4-piperanyl, 2H-2,5-piperanyl, 4Η-2,3 · piperanyl, 4Η-2,4-piperanyl, 4Η-2,5 · Piperanyl, 2Η-piperan-2-one-3,4-yl, 2Ηpiperan-2-one-4,5-yl, 4Ηpiperan-4-one-2,3-yl, 2, 3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5 · tetrahydrofuranyl, 3,4 · tetrahydrofuranyl, 2,3_tetrahydropiperanyl, 2,4-tetrahydropiperanyl, 2,5_tetrahydrofuranyl Hydropiperanyl, 2,6-tetrahydrothyranyl, 3,4 · tetrahydrobranyl, and 3,5_tetrahydrocarbyl, and containing the nitrogen member of the W4 ring instead of the carbons at the point of attachment With hydrogen, it is optionally substituted by one or more groups including R9, R10, RU, and R12, with the condition that (CH (R3 8)) r is bound to EG, and Qb is bound to each of W4 The highest number replaces the base position; Y0 printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is Qb-Qssss, where (^ ... is (CH (R38)) r_W5, r is an integer selected from 1 to 2, W5 is selected Self-included 1,4_thruyl, ι, 5-manganyl, ι, 6.heteroyl, 1,7- Base, 2,7 · mangan, 2,6-carbo, 2,5_mangan, 2,4-mangan, 3,4-anchi, 3,5_mangan, 3,6_mangan , 3,7 · Pingyl, 2,4-Benzenesulfanyl, 2,5-Benzenesulfanyl, 2,6-Benzenesulfanyl, 2,7-Benzanyl, 3, 4-Benzenesulfanyl, 3,5-Benzenesulfanyl, 3,6-Benzenesulfanyl, 3,7-Benzenesulfanyl, 2,4-benzophenylthio, 2, 5-benzofluorenylthio, 2,6-benzobenzosulfanyl, 2,7-benzofluorenylthio, 3,4-benzofluorenylthio, 3,5-benzophenylsulfanyl, 3, 6-benzophenylthio, 3,7-phenylfluorenylphenylthio, 2,7-imidazolium (i, 2-a) pyridyl, 3,4-imidazolium (1,2-a) pyridyl, 3,5 · imidazolium (l, 2-a) pyridyl, 3,6-imidazolium (l, 2-a) pyridyl, 3,7-imidazolium (l, 2-a) pyridyl, 2, 4-indolyl, 2,5-pyridyl, 2,6-ΘΘ indolyl, 2,7 · ardolyl, 3,4-ardolyl, 3,5-pyridyl, 3X indolyl- 62- This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 mm) Α7 Β7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (60), 3,7- 啕 0 wood , M_isoindolyl, isoxinyl, isoxinyl, 2 4_iso ♦ yl, 2,5_isopyridinyl, 2,6_isopyridyl, 2,7_isopyridyl, 1,3 · eccentric, 3, " oxazolyl, 3, 5-Indazolyl, 3,6 · Indazolyl, 3,7-Axazolyl, 2,4-Benzazolyl, 2,5-Benzazolyl, 2, Benzene: , 2,7 · Benzoline 4 groups, 3,4 Benzo group, 3,5 Benzo group, 3,6-Benzo group, 3,7_Benzo group, Lingyl, μ-fluorenyl, 1,5-fluorenyl, 1,6-fluorenyl, vulcanyl, M. naphthyl, 2,4-fluorenyl, 2 > fluorenyl, 2,6-phenyl, 2J_fluorenyl, 2, cardiacyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6 such as linyl, 2,7_cardiyl, 2,8_linyl , 3,4-heptadyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4 , 6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, M-isoquinolinyl, 0 isoquinolinyl, 1,6-isoquinolinyl, Quinolinyl, y-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8 · Isoquinolinyl, 4,5 · isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4_fluorinyl, 3,5-fluorinyl, 3,6 · fluorinyl, 3,7-fluorinyl, 3,8-fluorinyl, 4,5-fluorinyl, 4,6-fluorinyl, 4 , 7-fluorenyl group and 4,8 · fluorinyl group, and each carbon and hydrogen group containing a nitrogen member of the W5 ring instead of the connection point, is optionally one or more including R9, Ri0, Rii and The group substitution of r12 is subject to the condition that Qb is bound to the lowest number of substituent positions of each W5, and (CH (R38)) is bound to E0; Y0 is Qb_Qssssr, where Qssssr is (CH (R38 )) r-W6, r is an integer selected from 1 to 2, W6 is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2, 7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7 -Indenyl, 2,4_phenylsulfanyl, ____- 63- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------------- ---- ^ --- Order --------- Line (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ------ ---- B7______ V. Description of the Invention (ei) 2 > Benzofuranyl, 2,6_benzopyranylfuran , 2,7-phenylfluorenylfuranyl, 3,4-phenylfluorenylfuranyl, 3,5-phenylfluorenylfuranyl, 3,6_phenylfluorenylfuranyl, 3,7_phenylfluorenylfuranyl, 2,4- Phenylphenylthio, 2,5-phenylphenylthio, 2,6-phenylphenylthio, 2,7-phenylphenylthio, 3, 'phenylphenylthio, 3,5 • benzene Stilbenethio, 3,6_benzobenzothio, 3,7-phenylstilbenethio, 2,7_imidazolium (1,2-a) pyridyl, 3,4_ Weisha 弁 (l, 2_a > Spectidinyl, 3,5 · imidazolium (1,2-a) pyridyl, 3,6-imidazolo (1,2-ahl: bityl, 3,7 · imidazolium (1 »pyridyl, 2 , 4 ^ 5 丨 indolyl, "indolyl, 2,6-fluorinyl, 2,7-indolyl, 3,4-indolyl, 3,5_indolyl, 3,6 Group, 3,7-andolyl, M_isoamyl, 1,5-isoamyl, isoamyl, 2,4-isoamyl, 2,5-isoamyl , 2,6 · isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5 · indazolyl, 3,6-indazole Group, 3,7-oxazolyl group, 2,4 · benzoxazolyl group, 2,5-benzoxazolyl group, 2,6-benzoxazolyl group, 2,7_benzoxazolyl group, 3,4-Benzamidine isoxazolyl, 3,5-Benzamidine isoxazolyl, 3,6-Benzamidine isoxazolyl, 3,7-benzene Isoxazolyl, ι, 4-fluorenyl, 1,5-fluorenyl, 1,6-fluorenyl, 1,7-fluorenyl, 1,8-fluorenyl, 2,4-fluorenyl, 2, 5.Qin Ji, 2,6_Teaji, 2,7 · Fanji, 2,8_Fanji, 2,4_Xialin, 2,5-Quinyl, 2,6-4Linyl, 2,7-junlin, 2,8-4 linden, 3,4-junn, 3,5--4, 3,6--4, 3,7 8_ guolinyl, 4,5- 4 lysin, 4,6- p lysin, 4,7- 4 4 lysin, 4,8- p lysin, ι, 4-isop quine τ » Linyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, ι, 8-isoquinolinyl, 3,4-isoquinolinyl, 3, 5-Isoquinolinyl, 3,6-Isoquinolinyl, 3,7-Isoquinolinyl, 3,8 · Iso-4, 4-yl, 4,5-Iso-4linyl, 4,6-Iso JunLin base, 4,7_Isoprenalin, 4,8_Isunlin base, 3,4-Glypholyn base, 3,5-Peak Lyl base, 3,6-Peak 117 forest base, 3, 7-peak lymphatic base, 3,8-peak lymphatic base, 4,5-colinyl, 4,6- _ plinyl, 4,7- -64- ------------ ---- K ---- Order --------- Line (Please read the phonetic on the back first? Please fill in this page again for this matter) This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) '' 1222445 A7

R V. Description of the Invention (62) The perylene and 4,8-4 phosphono groups, each of which contains a nitrogen member of the W6 ring and is not a carbon and hydrogen group at the connection point, are optionally included by one or more of R9, The group substitution of Ri 0, Ri 1 and R12 is subject to the condition that Qb is bound to the highest number of substituent positions of each W6, and (CH (R38)) f is bound to E0. In a preferred embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is the following formula: 34 (Please read the notes on the back before filling this page)

R 33

R 35

R 3 6 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 119, 1110, 1111, 1112, 1113, 1132, Chem 33, 1134, & 35 and 1136 are independently selected from the group consisting of hydrogen, acetamido, and dentate Ethylamino, methyl, guanidyl, sub-pit dioxy, IS alkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, halooxyalkyl, meridyl, amine , Oxoamino, nitro, low-carbon phenylamino, alkylthio, alkylthioalkyl, alkylsulfinyl, alkylsulfenyl, alkylsulfonylalkyl, aromatic Base, aralkyl, cycloalkyl, cycloalkyl, alkylsulfonamido, alkylaminosulfonamido, fluorenylamino, monoalkylsulfonylsulfonyl, dialkyl Sulfonylaminosulfonyl, oxyl, oxanyl, oxanyl, alkenyl, yl, fluorenyl, sulfonyl, alkynyl, haloalkyl, hydroxyalkyl, amine Alkyl, self-alkoxy tiger-based, thin-based pit base 65 This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ---- ------ V. Description of invention (6 3), oxygen carboxyl group, I group, carboxyfluorenyl group, amidofluorenyl group, and cyano group; Yu Xin ^ and 'are optionally selected from the group consisting of heteroaryl and heterocyclic groups, and the conditions are ^^^, ^ And ^ is a substituent to the extra-heart; ^, "^, ... ',: ^' and the heart are independent as the case may be ^ with the condition that no more than one of R16 and R19 at the same time is ⑦, and ⑦ is Qbe; B is optionally selected from the group consisting of hydrogen, trialkylsilyl, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8_alkyl, where group B Each member may be replaced by one or more groups including R3 2, R3 3 R3 4 R3 5 and R36 at any carbon containing 6 atoms up to the junction of b to a, as the case may be; B is selected as the case may be Including C3_C12 ring alkyl group and C4-heterocyclyl group, where each ring carbon may be substituted by R3 3, a ring carbon, not the ring carbon of B to A junction point, may be substituted by keto group, the condition is not More than one ring is replaced by a ketone group at the same time. The ring carbon and nitrogen atom of the carbon atom adjacent to the connection point may be replaced by R9 or R13 as appropriate. It is adjacent to the position of R9 and two atoms away from the connection point. A ring carbon or nitrogen atom may be replaced by Ri 0 as appropriate, a ring carbon or nitrogen atom adjacent to the position of r1 3 and two atoms away from the connection point may be replaced by Rl 2 as appropriate, three atoms away from the connection point and adjacent to the position of R10 Ring carbon or nitrogen atom, optionally substituted by R11, ring carbon or nitrogen atom that is three atoms away from the connection point and adjacent to r1 2 position, may be replaced by R3 3, and four atoms away from the connection point and adjacent to Rl 1 and R33 The ring carbon or nitrogen atom at the position is optionally substituted by R34; A is selected from the group consisting of covalent single bonds, (W7) rr- (CH (R15)) pa & (CH (R15)) pa- _ _-66 -This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ---- K ---- Order --------- Line (Please read the precautions on the back before filling (This page)

Description of the invention (64) (W) rr printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, where rr is an integer selected from 0 to 1, pa is an integer selected from ο to 6, and W is selected from the group consisting of 0, S, C (0), (R7) NC (0), (R7) NC (S) and N (R7), with the proviso that if it is different from Pa, more than one is 0; R7 is selected from the group consisting of hydrogen, hydroxyl and alkyl;

R15 is selected from the group consisting of hydrogen, hydroxy, _, alkyl, and alkyl; city is selected from the group consisting of NH and NOH; M is selected from the group consisting of N and R1-C;

R1 is selected from the group consisting of hydrogen, alkyl, alkenyl, cyano, self-based, self-alkyl, 12-alkoxy, self-alkylthio, amino, aminoalkyl, alkylamino, formamyl, Ryl, hydroxylamino, alkoxy, hydroxyalkyl, alkoxyamine, thiol and alkylthio; R2 is Z0_Q; Z0 is selected from the group consisting of covalent single bonds, (CR41R42) q, where q is An integer selected from 1 to 3, (CH (R41)) g-W0- (CH (R42)) p, where g and p are integers independently selected from 0 to 3, and WG is selected from the group consisting of o, s, c (o), s (o), n (r41) & on (r41), and (CH (R41)) e-W22- (CH (R42)) h, where e and h are independently selected from 0 to The integer of 1 and W22 are selected from the group consisting of CR41 = CR42, 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, and 1,2-cyclopentyl. Base, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4 · morpholinyl, 3,5- Morpho p Linji, 1,2-Hexahydro-Ekinji, 1,3-Hexahydro-p-well foundation, 2,3-Hexahydrogen tocopherol, 2,6-Hexahydro-ratio phenyl 2-Hexahydro p ratio base, 1,3-Hexahydrooutside base, 2,3-Hexahydrooutside base, 2,4-Hexahydroside, 2,6_ Hexahydro p-pyridyl, 3,4-hexapyridyl, 1,2-tetrahydropyrrolyl, 1,3-tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrole Base, 2,5_tetrahydropyrrolyl, 3,4-tetra-67- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) '----------- -K-order --------- line (please read the precautions on the back before filling this page) 1222445 R11

A7 _____ — B7 _ V. Description of the Invention (65) Hydropyridyl, 2,3-tetrahydrocranyl, 2,4-tetrahydrocranyl, 2,5-tetrahydrocranyl, and 3, 4-tetrahydrocranyl, with the proviso that Z0 is directly bonded to the gluconanone ring; R4 1 and R42 are independently selected from the group consisting of methylamido, hydroxylamino, hydrogen, hydroxyl, amine, and alkyl; Q Is selected from the group consisting of hydrogen, with the proviso that Z0 is not a covalent single bond; and formula (Π): (II) where D ^ D ^ ji'J2 and K1 are independently selected from the group consisting of c, N, 0, s And covalent bonds, with the proviso that no more than one is a covalent bond, no more than one of Di, d2, J1, J2, and K1 is 0, and no more than one of D, D2, Ji, J2, and κ1 is S, when When two of D1, D2, J1, J2, and K1 are 0 and s, one of d1, D2, J1, J2, and K1 must be a covalent bond, and no more than four of K1 are N, with conditions attached R9, R1 〇, RU, Ri 2 and 3 are each independently selected to maintain the completed tetravalent property, nitrogen trivalent property, sulfur divalent property and oxygen divalent property; 'K is (CR4aR4b) n Where η is an integer selected from 1 to 2; R4a and R4b are independently selected from the group consisting of halo, hydrogen, Alkyl, alkyl, winter paper-like slaves 0 _Fresh (CNS) A4 miscellaneous coffee χ 2ϋ) — ~ ————- ------------ pack ----- ^- --Order --------- ^^^ 1 (Please read the phonetic on the back? Matters before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 B7 V. Description of Invention (66) Oxyalkyl, alkylthioalkyl, and fluorenyl; when K is (CR4aR4b) n, E0 is E1, where E1 is selected from the group consisting of covalent single bonds, c (0), C (s), C (0) N (R7), (R7) NC (0), S (〇) 2, (R7) NS (0) 2 and S (0) 2N (R7); is the formula (IV): 0s

R

J 18

R 16 / D5 \ K2 ^ 'R- (IV) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, where D5, D6, J5 and J6 are independently selected from the group consisting of C, N, 0, s and covalent bonds. Provided that no more than one is a covalent bond, no more than one of K2 is C, D5, D6, J5, and J0 is 0, no more than one of D5, D6, J5, and J6 is S. When D5, D6, J5, and J6 are When two of them are 0 and S, one of D5, D0, J5, and j6 must be a covalent bond, and no more than four of D5, D0, J5, and J6 are N. The conditions are R16, R17, and R18. And R19 are independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; R1 ^ R1 7, feet 1 8 and R1 9 are independently selected from the group including hydrogen Base, formamyl, guanidyl, carboxyl, haloalkylthio, alkoxy, hydroxyl, amino, nitro, alkoxyamino, low-carbon amine, thiosulfan, feyl Base, alkenyl, alkenyl, alkanoyl, alkyl, alkenyl, halo, fluorenyl, haloalkoxy, hydroxyalkyl, alkylalkenylamino, alkanoyl Alkyl, alkoxycarbonyl and cyano: -69- Applicable to this paper size China National Standard (CNS) A4 Specification (210 X 297 mm) ----------------- ^ ---- Order --------- line (please First read the phonetic on the back? Matters and then fill out this page)

1222445 V. Description of the invention (67) Q is selected from the group consisting of NR2 0R21, aminoalkyl, and Qbe, where Qbe is hydrogen, N (R26) C (NR25) N (R23) (R24), and C (NR25 ) NR23R24, with the proviso that more than one of R20 and R21 is hydroxyl, amine, alkylamino, or dialkylamine, and more than one of R23 and R24 is not hydroxyl, amine, alkylamine, or dialkylamine R2 (), R21, R23, R24, R25 & R26 are independently selected from the group consisting of hydrogen, alkyl, warpyl, aminophenenyl, amine, diamine, amine, and meso ; QMf, selected from the group consisting of covalent single bonds, (CrWr38, where b is an integer selected from 1 to 4, and (CI ^ RH ^ -Wyci ^ R15) ^, where c and d are independently selected from 1 to 3 The integer and w1 are selected from the group consisting of C (0) N (R14), (R14) NCX〇), S⑼, S (〇) 2, S (0) 2 Ν (Ι ^ 4), Ν (Κ ^ 4 ) S (; 0) 2 and N (Ri4), with the proviso that when R14 is directly bonded to N, it is selected from the group other than halo, and (〇? 371138) 1) and (CH ^ R14)). Is bound to e0; R14 is selected from the group consisting of hydrogen, fluorenyl, alkynyl, and automorph; R37 and R3 are independently selected from the group consisting of hydrogen, alkyl, and alkyl; R3 and 8 are optionally selected from the group including Arylpyridyl and heteroarylpyridyl; Y0 is optionally Qb_QW, where Qss is (CH (Rl4)) e-W2_ (CH (Rl5)) h, where e and h are integers independently selected from 1 to 2 And W2 is CR4a = CR4b, with the condition that (CH (R14)) "$ binds to E0; γ〇 is selected from the group consisting of Qb_Qssss and Qb_Qsssssr, where (^ ― is (CH (R38)) r_W5, and Qssssr is (CH (R3 8)) r_W6, Γ is an integer selected from 1 to 2, and W5 and w6 are independently selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl , 1,7_indenyl, 2,7_indenyl, 2,6_indenyl, 2,5_indenyl, 2,4-indenyl, 3,4-indenyl, 3,5_imidyl, 3,6-segment-based, 3,7-Θ-based, 2,4_benzopyranyl, _-70- Applicable to this paper size _ Home Standard (CNS) A4 Specification ⑽ x 297 mm) ---- -------- Installation —: — Order --------- (Please read the note on the back? Matters before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7

V. Description of the invention (68) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, 2,5-Benzosulfanyl, 2,6-phenylbenzofuranyl, 2,7_phenylbenzofuranyl, 3, 'benzo Cranyl, 3,5-benzofluorenyl, 3,6-benzobenzofuranyl, 3,7-benzofluorenyl furanyl, 2,4-benzobenzosulfanyl, 2,5_benzofluorenylphenylthio , 2,6-Benzamidinephenylthio, 2,7-Benzamidinephenylthio, 3,4-Benzamidinephenylthio, 3,5-Benzamidinebenzenethio, 3,6_Benzamidinebenzenethio, 3,7-benzophenylthio, 2,7-imidazolium (i, 2-a) pyridyl, 3,4-imidazolium (l, 2-a) pyridyl, 3,5-imidazolium ( l, 2-a) pyridyl, 3,6-imidazolium (1,2-pyridyl, 3,7-imidazolium (i, 2-a) pyridyl, 2,4-indolyl, 2,5-fluorene Indolyl, 2,6-fluorinyl, 2,7-indolyl, 3,4_ < indolyl, 3,5-indolyl, 3,6_indolyl, 3,7-indolyl, 1,4-Isoindolyl, 1,5-Isoindolyl, ι, 6-Isoindolyl, 2,4-Isoindolyl, 2,5-Isoindolyl, 2,6-Isopropyl Sulfonyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-oxazolyl, 3,5-indazolyl, 3,6- < oxazolyl, 3,7 -Indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2, 6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzoisoxazolyl, 3,5-benzoxazosilyl, 3,6-benzoxazoslyl , 3,7-benzyl isoxazolyl, ι, 4-fluorenyl, 1,5-fluorenyl, 1,6 · fluorenyl, 1,7-fluorenyl, 1,8-fluorenyl, 2,4 Fluorenyl, 2,5-fluorenyl, 2,6-naphthyl, 2,7-fluorenyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2, 6-quinolyl, 2,7-quinolyl, 2,8-quinolyl, 3,4-quinolyl, 3,5-quinolyl, 3,6_quinolyl, 3,7- p-queliny, 3,8 · xylenyl, 4,5--4 lysine, 4,6_ p-lynyl, 4,7-4 lysine, 4,8_ lysine, 1,4-isopropyl p-quinuclyl, 1,5-iso "quinyl, 1,6-iso4-yl, 1,7_isojunyl, ι, 8-iso-p-quinyl, 3,4 · iso-p-quinyl Lymphyl, 3,5-iso4-lyl, 3,6-isojunyl, 3,7-iso4-phosphonyl, 3,8-isoquinolinyl, 4,5-isoquinolyl, 4, 6-Isoquinolyl, 4,7-Isopropylquinyl, 4,8-Iso "quinyl, 3,4_Phenyl, 3,5_Phenyl, 3,6_Phenyl , 3,7-cocklinyl, 3,8-fluorinyl, 4,5-fluorinyl, 4,6_fluorolinyl, 4,7 · -71-This paper standard applies to Chinese National Standards (CNS) A4 size (210 X 297 mm ^ ---- ----------------- --------- set (please read the back of the phonetic? Please fill in this page again for details) A7 V. Description of the invention (69 B7 琳 基 基 基 基 and 4,8-Ceki, and contains nitrogen members of the jealous ring and _ ring instead of the carbon and hydrogen groups at the junction of W and _, It is optionally replaced by a plurality of groups including R9, W, R " and ^, with the proviso that it is the lowest number of substituent positions bound to each W5, and Qb is substituted to the highest number of each And ((: 11: 38 binds to E0 from the system. In a more specific embodiment of the compound of Formula I or a pharmaceutically acceptable salt thereof, J is 0; B is the following formula:

R 34

R 33

R 35 R3 6 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs R3 2, R33, R3 4, R35 & R36 are independently selected from the group consisting of hydrogen, acetamido, haloacetamido, formamidine, guanidine Alkyl, alkanedioxy, haloalkylthio, alkoxy, alkoxy, hydroxyl, amine, alkoxyamino, alkyl, halo, nitro, low-carbon, j : Endylamino, sulfanyl, aryl, arylphenyl, cycloalkyl, cycloalkylalkyl, alkylsulfonamido, sulfonamidosulfonyl, monoalkylamino , Dihexylaminoamine, fluorenyl, fluorenyl, fluorenyl, fluorenyl, alkyl, fluorenyl, alkoxy, hydroxyalkyl, alkylfluorenylamino, alkoxycarbonyl, carboxyl, carboxyl醯 Amine, cyano, and Qb; B is selected from the group consisting of hydrogen, trialkylsilyl, C2-C8 alkyl, -72- This paper is applicable to Chinese National Standard (CNS) A4 (210 X 297) (Mm) ------------ install -------- order --------- ^ A_wi (Please read the precautions on the back before filling in this page> Intellectual Property of the Ministry of Economic Affairs Printed by the Bureau's Consumer Cooperatives 1222445 A7 ----- ~~ ^ _____ V. Description of Invention (7 ) C3_C8 alkyl, C3_C8 fluorenyl, C3_C8 alkynyl, and C2_C8 _ alkyl, where each member of group B is optionally at any carbon that is at a distance from the junction of B to A and contains 6 atoms, or Multiple group substitutions including r32, r33, r34, r35 &R36; B is selected from the group consisting of C3-C12 cycloalkyl and C4-heterocyclyl, wherein each ring carbon system is optionally substituted by R3 3, one ring carbon , Is not the ring carbon of the junction of B to a, is optionally substituted by keto, the condition is that no more than one ring carbon is simultaneously substituted by keto's ring carbon and nitrogen atom of the carbon atom adjacent to the junction, depending on the situation Replaced by R9 or R13 'ring carbon or nitrogen atom adjacent to the position of r9 and two atoms away from the connection point, is replaced as appropriate, and ring carbon or nitrogen atom adjacent to the position of R13 and two atoms from the connection point is optionally Ri2 substitution, a ring carbon or nitrogen atom that is three atoms away from the junction and adjacent to R10, is replaced by R11 as appropriate, and a ring carbon or nitrogen atom that is three atoms away from the junction and adjacent to Ri2, is optionally used by R33 Substitute, and four atoms away from the junction and adjacent to R11 and R3 3 positions Ring carbon or nitrogen atom, which is optionally substituted by r3 4; 119,111 (), 1111, 1112, and 1113 are independently selected from the group consisting of hydrogen, acetamido, haloacetamido, and alkoxyamine , Alkylamino, alkylamino, methylamidino, guanidino, alkylenedioxy, alkylthio, alkoxy, hydroxyl, amino, lower alkylamino, alkylthio, alkyl Sulfinyl sulfenyl, alkylsulfonyl, alkylsulfonamido, sulfonamidosulfonyl, monoalkylsulfonamidosulfonyl, dialkylsulfonamidocontinyl, sulfonyl, Base, alkalyl, _ alkoxy, via alkyl, aminoalkyl, alkoxycarbonyl, carboxyalkyl, carboxyl, carboxyamido and gas groups; ____- 73 -___ This paper size applies to Chinese national standards (CNS) A4 specifications (210 X 297 male f " ----- ^ ---- ^ --------- Thread #-(Please read the phonetic notes on the back before filling this page) 1222445 A7 ------ 2Z__ V. Description of the invention (71) (Please read the precautions on the back before filling out this page) R, R10, R11, R12 and R13 are selected from the group consisting of heteroaryl and heterocyclic as appropriate Base, with the conditions of Hua 9, Ruler 10, Anti 11 on 12 and Ruler 13 are pair 3 A is selected from the group consisting of a covalent single bond and (CH (Ri5)) pa_ (w7) rr, where is an integer selected from 0 to 1, and pa is an integer selected from 0 to 3, and W7 is selected from the group consisting of 0, S, C⑼, (R7) NC (0), (R7) NC (S) and N (R7); R7 is selected from the group consisting of hydrogen, hydroxyl and alkyl; R15 is selected from the group consisting of Hydrogen, hydroxy, alkynyl, alkyl, and alkyi; Ψ is NH; M is selected from the group consisting of N and R1-C; R1 is selected from the group consisting of hydrogen, alkyl, cyano, fluorenyl, and self-alkyl , Halooxy, amine, aminoalkyl, alkylamino, formamyl, hydroxyl, hydroxylamino, alkoxy, hydroxyalkyl, alkoxyamine, thiol, and alkylthio; R2 Is Z0-Q; ZG is selected from the group consisting of covalent single bonds and (CR41R42) q, where q is an integer selected from 1 to 2, (CH (R41)) g_W0_ (CH (R42)) p, where g and p Is an integer independently selected from 0 to 3, and W0 is selected from the group consisting of 0, S, and N (R41), and (CH (R41)) e-W22_ (CH (R42)) h, where e and h are independently selected From 0 to 1, the number printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, and W22 is selected from the group consisting of CR41 = CR42, 1, 2 · cyclopropyl, 1, 2-cyclobutyl, and 1,2-cyclohexyl 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2 ,, 6-hexahydropyridyl, 1,2-hexahydropyridyl, 1,3-hexahydropyridyl, 2,3-hexahydropyridyl, 2,4-hexahydrop-pyridyl, 2, 6-Hydroxyhydroxyl, 3,4- ___- 74 -___ This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) 1222445, Description of the Invention (72) Hexahydropyridyl, 1, 2-tetrahydropyrrolyl, fluorene 53-tetrahydropyrrolyl, 2,3-tetrahydropyrrolyl, 2,4-tetrahydropyrrolyl, 2,5-tetrahydropyrrolyl, 3,4-tetrahydropyrrolyl, 2,3 · tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl and 3,4-tetrahydrofuranyl 'with the proviso that the ζ〇 system is directly bound to the pyrimidinone ring; R41 and R42 are independent Selected from the group consisting of hydrogen, hydroxyl and amine; Q is selected from the group consisting of hydrogen, with the proviso that Z0 is not a covalent single bond; aryl and heteroaryl, one of which is a carbon adjacent to the carbon of the attachment point, depending on Situation replaced by R9 Another carbon adjacent to the junction carbon is replaced as appropriate, a carbon adjacent to R9 and two atoms away from the junction carbon is replaced by Ri 〇 as appropriate, and a carbon adjacent to Ri 3 and two atoms away from the junction carbon is replaced. Carbon, which is optionally substituted by R12, and any carbon adjacent to both R10 and R12, which is optionally substituted by R11; K is CHR4 a 'where R4 a is selected from the group consisting of hydrogen, light lake, alkyl, and alkane Oxyalkyl, alkylthioalkyl, and ialkyl; E0 is selected from the group consisting of covalent single bonds, C (0) NH, (h) MC (〇), (R7) cis0) 2, and S (0) 2N (R7); Y13 is the formula (IV): ------------ install — ^ —— order --------- (Please read the precautions on the back I before filling in this Page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

Qs

-75- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) U22445 Printed by the Consumers ’Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs, Invention Description (73) Among which d5, d6, J5 and J6 are independently selected Since it includes c, N, 0, s and covalent bonds, the additional conditions are that no more than one is a covalent bond, K2 is C, ^, ^, and no more than one of Hu and Shanghai is 0, D5, D6, J5. And no more than one of J6 is S, when D5, D6? J5 ^ j6 ^ t vD5? D6? J5 ^ j6 ^ _ ^ ^ ^ common bond, and no more than four of D5, D6, J5 and J6 are N The conditions are that R10, R17, R1S, and R19 are each independently selected to maintain the tetravalent nature of carbon, the divalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; inverse 16, 1117, 1118, and 1119 is independently selected from the group consisting of hydrogen, methylamino, guanidino, carboxyl, alkylthio, alkoxy, hydroxyl, amino, alkoxyamino, lower alkylamino, alkylthio, and alkyl Sulfinyl sulfenyl, alkyl sulfonyl, alkyl sulfonyl, i alkynyl, alkyl, radical, alkyl, alkoxy, hydroxyalkyl, aminoalkyl, and cyano; R16 and R19 is Qb as the case may be. ^^ and Rl9 is not more than one at the same time as Qb, and Qb is Qbe, ·

Qb is selected from the group consisting of NR20R21 and Qbe, where Qbe is fluorenyl, N (R26) C (NR25) N (R23) (R24) and C (NR25) NR23R24, with the condition that R2G and R21 do not have more than one at the same time as a hydroxyl group , Amine, alkylamino or dialkylamino, and more than one of R23 and R24 is a hydroxyl, amine, alkylamino or amine group; R20, R2 1, R23, R24, R25 & R26 series Independently selected from the group consisting of hydrogen, alkyl, hydroxyl, amine, alkylamino, and dialkylamino; (^ is selected from the group consisting of covalent single bonds, (CR ^ R3%, where b is selected from 1 to 4) An integer, and (CH ^ Ic-WycI ^ R15: ^, where C and d are independently selected from integers 1 to 3, and W1 is selected from the group consisting of C (0) N (R14), (Ri4) NC (〇) , S (〇), -76- The paper size is applicable to China National Standard (CNS) A4 (210 x 297 mm) ---------------- K ---- Order --------- Cord (Please read the phonetic on the back? Matters before filling out this page) 1222445 A7

S (〇) 2, S (0) 2 N (Rl 4), N (R1 4) s (〇) 2 and N (Rl 4), with the proviso that when R14 is directly bound to N, it is selected from halogen Other than the base group, and (CR3 7 R3 8) b and (CH (R14)) ^ are bound to E0; R14 is selected from the group consisting of a hydrogen group, a self-based group, an alkyl group, and a pyrenyl group; R3 7 and R3 8 are independent It is selected from the group consisting of hydrogen, alkyl and functional alkyl; R3 8 is optionally selected from the group consisting of arylfluorenyl and heteroarylfluorenyl; Y0 is optionally Qb-Qss, where QSS is (CH (R14)) e_w2_ (CH (Rl5)) h, where e and h are integers independently selected from 1 to 2, and w2 is CR4a = CH, with the condition that (CH (R14)) ^ is bound to E0. " In a more preferred embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is the following formula:

R 34

R 33

R

R 35 3 3 6 ---------- I —install · ---- r I--order --------- ^ 9— CPlease read the back seven. Zhuyin? Please fill in this page again.) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 32, Y33, Y34, Y35, and Y36 are independently selected from the group consisting of hydrogen, acetamido, haloacetamido, Formamyl, guanidyl, alkoxy, mesityl, amino, alkoxyamino, lower alkylamino, alkylthio, sulfamoylsulfonyl, monoalkylsulfonylsulfonyl , Dialkylfluorenylsulfonyl, alkyl, self-supported, fluorenyl *, iS oxo, lightly burned, oxalyl, compound, compound, amine, -77- Paper size Applicable to China National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 V. Description of the invention (75) Cyano and Qb; (Please read the note on the back? Matters before filling out this page) Covalent single bond with (CH (R15)) pa- (W7) rr, where rr is an integer selected from 0 to 1, pa is an integer selected from 0 to 3, and W7 is selected from the group consisting of (R7) NC ( 〇) and n (R7); R7 is selected from the group consisting of hydrogen, hydroxy, and alkyl; R15 is selected from the group consisting of hydrogen, _, alkyl, and haloalkyl; 氺 is NH; M is selected from the group consisting of N and R1 -C;

R1 is selected from the group consisting of hydrogen, hydroxy, hydroxylamino, methylamido, amine, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, and alkoxy Amine, S-alkyl, self-alkoxy and self-group; R2 is Z0_Q; Z0 is selected from the group consisting of covalent single bonds, 0, s, NH and CH2; Department of Economics, Intellectual Property Bureau, Department of Consumer Cooperatives, Q Selected from aryl and heteroaryl groups, where one of the carbons adjacent to the point carbon is replaced by R9, the other of the carbons adjacent to the point carbon is replaced by R13, one is adjacent to R9 and is connected to the point carbon The carbon of two atoms is optionally replaced by R10, a carbon of two atoms adjacent to R13 and two carbons away from the connecting point is replaced by R12 as appropriate, and any carbon adjacent to both 10 and 12 is determined The case is replaced by Rl 1; R9, H11 and R13 are independently selected from the group consisting of hydrogen, hydroxyl, amine, formamyl, fox group, low-carbon alkyl, thio, thio, amine, and amine Alkylidene sulfenyl, alkylsulfonyl, sulfonylsulfonyl, monoalkylsulfonylsulfonyl, alkyl, alkoxy, radical, alkane , _ Alkoxy, hydroxyalkyl, carboxy, carboxyalkyl, acyl group and a cyano group;

297 mm) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (76) R10 and R12 are independently selected from the group consisting of hydrogen, acetamido, acetamido, methamidyl, Guanidine, alkyl, alkoxy, hydroxyl, amine, alkoxyamine, lower alkylamine, alkylsulfonamido, sulfonamidosulfonyl, monoalkylsulfonamido Group, dialkylfluorenylsulfofluorenyl, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, carboxyl, carboxyalkyl, fluorenylcarbonyl, phenyl, halo and cyano; K is CH2; E〇 is C (0) N (H); is formula (IV):

Qs R17, r18 ί 1 R16 / D5 \ k2 < D, R19

Qb (iv) where D5, D6, J5 and J0 are independently selected from the group consisting of C, N, 0, S and covalent bonds, with the proviso that no more than one is a covalent bond, and K2 is C, D5, D6, J5 And no more than one of J6 is 0, no more than one of D5, D6, J5 and J6 is S, when two of D5, D6, J5 and J6 are 0 and s, one of D5, D6, J5 and J6 Must be a covalent bond, and no more than four of D5, D6, J5, and J6 are N; R1 6, R1 7, R1 8 and R1 9 are independently selected from the group consisting of hydrogen, methyl, guanyl, guanidino, Alkyl, halogenated thio, alkoxy, mesityl, amine, low carbon oxenylamino, alkylthio, alkylidenefluorenyl, alkylfluorenyl, alkylsulfonyl, alkylsulfanyl-- --- -79- _ This paper size applies to China National Standard (CNS) A4 specifications (210 X 297 Public Love ------------------------------------) ------- ^ 9— (Please read the phonetic on the back? Matters before filling out this page) 1222445

、 Explanation of the invention (π eryl, phenyl, haloalkyl, 1¾ alkoxy, hydroxyalkyl, aminoalkyl, and cyano; (Please read the precautions on the back before filling this page > / and R19 The system is Qb, with the condition that the rule "is different from 9 when more than one is Qb, and Qb is Qbe; Q is selected from the group consisting of NR20R21, Qbe, where Qbe is chloro and. 25) View 23 feet 24 2 " With the condition that R20 and R21 are not more than one hydroxyl group at the same time, and R23 and R24 are not more than one hydroxyl group at the same time; R2Hw, r24 and r25 are independently selected from the group consisting of hydrogen, pit and several groups; Valence single bond, ch2 & CH2CH2. In another yet more specific embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is optionally selected from the group consisting of hydrogen, C2_C8 and C3_C8 Group, C3-C8 alkynyl group and C2-C8 haloalkyl group, where each member of the group B is optionally at any distance from the point of attachment of B to A to two and containing 6 atoms by one or more including 1132, 1133, 1134, 1135 and 1136 groups replaced; printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs with 2, ¥ 3, ¥ 4, ¥ 5 and Hua 36 is independently selected from the group consisting of hydrogen, acetamido, haloacetamido, methyl, oxo, alkoxy, meridyl, amine, lactyl amine, and low-carbon amine Base, sulfanyl group, amidoamino acid group, monoalkylamino group, dialkyl group, dialkyl group. Amido group, dialkyl group, alkyl group, alkyl group, alkyloxy group, hydroxyl group Alkyl, alkoxycarbonyl, carboxyl, carboxyamido, cyano, and Qb; A is selected from the group consisting of covalent single bonds and (CH (R15)) pa_ (W7) rr, where it is selected from 0 to 1 Integer, pa is an integer selected from 0 to 3, and w7 is selected from the group consisting of -80- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 --------- B7 V. Description of the invention (78) (R7) NC (0) and N (R7); R7 is selected from the group consisting of hydrogen, hydroxyl and alkyl; R15 is selected from the group consisting of基 is NH; M is selected from the group consisting of N and R1-C; R1 is selected from the group consisting of hydrogen, hydroxyl, hydroxylamine, methylamido, amine, cyano , Hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio , Alkoxyamine, self-alkyl, i-alkoxy, and i-group; R2 is Z0-Q; is selected from the group consisting of covalent single bonds, 0, s, NH and CH2; Q is selected from the group including aryl With heteroaryl, one of the carbons adjacent to the carbon of the junction is optionally replaced by R9, and the other carbon of the carbon adjacent to the junction is optionally replaced by R13, one of the carbons adjacent to R9 and two atoms away from the carbon of the junction , Which is replaced by R1G as appropriate, a carbon adjacent to R13 and two atoms away from the connecting point carbon, which is replaced by R12 as appropriate, and any carbon adjacent to both R1G and R12, which is replaced by R11 as appropriate; R9, R11 And R13 are independently selected from the group consisting of hydrogen, hydroxy, amine, formamidine, guanidino, lower alkylamino, alkylthio, alkylsulfonamido, alkylsulfinamido, alkylsulfonyl Fluorenyl, sulfonylsulfonyl, monoalkylsulfonylsulfonyl, alkyl, alkoxy, self-based, self-alkyl, i-alkoxy, hydroxyalkyl, carboxyl, carboxyfluorenyl, and Cyano; R10 and R12 are independently selected from the group consisting of hydrogen, acetamido, acetamido, methylamido, guanidino, alkyl, alkoxy, hydroxyl, amine, alkoxyamine Base, low-carbon alkylamino, alkylsulfonamido, sulfonamidosulfonyl, and monoalkane -81 -_ This paper size applies to China National Standard (CNS) A4 (210 X 297 public love)- -------------- r ---- Order --------- ^^ 1 (Please read the Zhuyin on the back? Please fill out this page again for details) 1222445 A7 R7 V. Description of the invention (79) Aminoylamino, dialkylamidosulfonyl, hydroxyalkyl, alkylalkenylamino, alkoxycarbonyl, carboxyl , Carboxyalkyl, amidocarbonyl, halo, halo, and cyano; K is CH2; E0 is C (0) N (H); YG is formula (IV):

Qs

R 17 18

R 19 (IV) (Please read the back ^ / Precautions before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, where D5, D6, j5 and J6 are independently selected from C, N, 0, s and Covalent bond, with the proviso that no more than one is a covalent bond, K2 is C, D5, D6, J5 and no more than one of the households is 09 D5, no more than one of D6, J5 and J6 is S, when D5 When two of D6, J5, and J6 are 0 and S, one of d5, D6, J5, and J6 must be a covalent bond ', and no more than four of D5, D6, J5, and J6 are N. The condition is that R1 6, R17, R1 8 and Ri 9 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; R1 6, R1 7, Ri 8 and Ri 9 is independently selected from the group consisting of hydrogen, methylamido, guanidino, carboxyl, self-alkylthio, alkoxy, hydroxyl, amine, lower alkylamino, thiothio, alkylsulfinyl , Alkylsulfonyl, alkylsulfonyl,! | Alkyl, alkyl, fluorenyl, haloalkyl, alkoxy, hydroxyalkyl, alkylalkenyl -82- as far as paper standards are applicable National Standards (CNS) A4 χ Norm) 1222445 A7

V. Description of the invention (80) Amino and cyano groups are printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs; R16 and R19 are Qb as the case may be. Qb is Qbe;

Qb is selected from the group consisting of NR20R21, Qbe, where Qbe is hydrogen, C (NRW) nr23r24an (r26) C (nr25) n (r23) (r24), and the attached soil is that R20 and R21 are not more than one when it is a hydroxyl group And more than one ruler 23 and 24 are not gift bases at the same time; ruler 20, ruler 21, ruler 23, ruler 24, ruler 25 and ruler 26 are independently selected from the group consisting of hydrogen, alkyl, and rosanyl; (^ is selected from Including covalent single bond, ch2 & ch2ch2. In yet another yet more specific embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is optionally selected from the group consisting of C3-C7 cycloalkyl With C4-heterocyclyl, where each ring carbon is optionally substituted by R3 3, a ring carbon, not a ring carbon that is the point of attachment of B to A, is optionally substituted by a keto group, provided that it does not exceed one ring carbon Simultaneously substituted by a keto group, the ring carbon and nitrogen atom of the carbon atom adjacent to the connection point are optionally replaced by R9 or R13, and the ring carbon or nitrogen atom adjacent to the R9 position and two atoms away from the connection point are optionally replaced by R1 0 substitution, adjacent to the position of Rl 3 and a ring carbon or nitrogen atom two atoms away from the connection point, which is optionally replaced by R1 2 and three atoms from the connection point And the ring carbon or nitrogen atom adjacent to the Ri 0 position is replaced by R11 as appropriate, three atoms away from the connection point and the soil carbon or nitrogen atom adjacent to the Ri2 position are replaced by R3 3 as appropriate, and four from the connection point A ring carbon or nitrogen atom that is adjacent to the positions of RH and R33, depending on the situation, is ____ -83- I Paper size applies the Zhongguanjia Standard (CNS) A4 specification (210 X 297 mm)----- K ------------- ^^ 1 (Please read the note on the back? Matters before filling out this page) Printed by the Consumer Consumption Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ---___ 1. Description of the invention (81) R34 substitution; R9, R11, and R13 are independently selected from the group consisting of hydrogen, hydroxyl, amine, methyl, guanidino, lower alkylamino, alkylthio, alkylsulfonamido, and A sulfenyl, alkylsulfonyl, sulfonylsulfonyl, monoalkyl amine, a continuation group, an alkyl group, an alkyl group, an alkyl group, an alkyl group, an alkyl group, an alkyl group, an alkyl group R10 and R12 are independently selected from the group consisting of hydrogen, ethylamino, ethylamino, methylamino, guanidyl, alkyl, alkoxy, hydroxyl, Amine, Burntoxy Group, low-carbon alkylamino group, alkylsulfonamido group, sulfonylsulfonyl group, monoalkylsulfonylaminosulfonyl group, dialkylfluorenylaminosulfonyl group, hydroxyalkyl group, alkylsulfonyl group R3 3 and R34 are independently selected from the group consisting of hydrogen, acetamido, and haloacetamido Base, formamyl, oxenyl, antioxidant, warpyl, amine, alkoxyamine, lower alkylamino, alkylthio, sulfamoylsulfonyl, monoalkylacidamino Fluorenyl, dialkylfluorenylsulfofluorenyl, alkyl, alkynyl, alkynyl, alkynyloxy, hydroxyalkyl, alkoxycarbonyl, carboxyl, carboxyamido, cyano, and Qb; A series Selected from the group consisting of a covalent single bond and (CH (Ri5)) pa- (W7) rr, where it is set to an integer selected from 0 to 1, pa is an integer selected from 0 to 3, and W7 is selected from the group consisting of (R7 ) NC (0) and N (R7); R7 is selected from the group consisting of hydrogen, meridian, and alkyl; R15 is selected from the group consisting of hydrogen, alkyl, alkyl, and alkyl; Ψ is NH; M is selected Including N and Ri-C; -84-This paper size is applicable to China National Standard (CNS) A4 (210 X 297 Mm) '---- ----------------- ^ ---- order --------- line (please read the notes on the back first (Fill in this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ----- B7 ____ V. Description of the Invention (82) R1 is selected from the group consisting of hydrogen, hydroxyl, hydroxylamine, formamidine, amine, Cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, self-alkyl, self-alkoxy, and radical; R2 is Z0- Q; ZG is selected from the group consisting of covalent single bonds, 0, s, NH and CH2; Q is selected from the group consisting of a square group and a hetero-square group 'one of which is adjacent to the carbon of the connecting point' is optionally substituted by R9 and the other The carbon adjacent to the connecting point carbon is replaced by R1 3 as appropriate, and a carbon adjacent to R9 is connected to the carbon of two atoms away from the connecting point carbon, which is replaced by R10 as appropriate, a carbon adjacent to R13 and two atoms away from the connecting point carbon, It is replaced by Ri2 as appropriate, and any carbon adjacent to Ri0 and RU is replaced by R1 1 as appropriate; K is ch2; EG is C (0) N (H); YQ is formula (IV):

Where D5, D6, J5 and J6 are independently selected from the group consisting of C, N, 0, s and covalent bonds, with the proviso that no more than one is a covalent bond, and K2 is c '1) 5,1) 6, No more than one of j5 and J6 is 0, no more than one of D5, D6, J5 and J6 is S, when D5, D6, _ ___________ This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------- Install ----- ^ ---- Order --------- (Please read the t-note on the back? Matters before filling out this page) 1222445 A7 V. Description of the Invention Bismuth) When two of J5 and J6 are 0 and S, one of D5, D6, J5 and J6 must be a covalent bond 'and not more than four of D5, D6, J5 and J6 are n. The conditions are that R16, R17, R18, and R19 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; The ruler 19 is independently selected from the group consisting of hydrogen, methylamino, guanidino, alkyl, i-alkylthio, alkoxy, hydroxyl, amine, lower alkylamino, sulfanyl, and sulfonyl. Base, base base, base base, haloalkoxy group, hydroxyalkyl group, alkyl alkenyl group Printed bases, alkyls, haloamines and cyano groups of the Consumer Cooperatives of the Ministry of Intellectual Property of the Ministry of Economic Affairs; R10 and R19 are Qb if more than one is Qb, and Qb is Qbe; Where Qbe is a hydrogen group and ¢ ^ (^ 25) ^ 23 ^ 'with the proviso that more than one R2 0 and R2 1 are warp groups, and more than one R2 3 and R24 are light groups; R2O, R2l R23, R24 & R25 are independently selected from the group consisting of hydrogen, alkyl and hydroxyl: Qs is selected from the group consisting of covalent single bonds, CH2 and CH2 CH2. In a preferred embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is the following formula: haloalkyl

R 34 (Please read the notes on the back before filling out this page) The condition is that R1 6 and R1 9 are different

R 33

R 35 r3 2 / ^^ Vr3 6 -86- The paper size is applicable to China National Standard (CNS) A4 (210 χ 297). U22445 A7

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (84) R 2, trans 33, 1134, 1135, and 1136 are independently selected from the group consisting of hydrogen, acetamido, acetaminophen, and formazan. Group, guanidino, alkoxy, hydroxyl, amine, alkoxyamine, lower alkylamine, alkylthio, sulfonamidosulfonyl, monoalkylsulfonylfluorenyl, dioxane Alkylamino, alkyl, alkyl, halo, alkoxy, hydroxyalkyl, alkoxycarbonyl, carboxyl, carboxyamido, cyano, and Qb; eight systems selected from covalent Single bond with (CH (R15)) pa- (W7) rr, where rr is an integer selected from 0 to 1, pa is an integer selected from 0 to 3, and W7 is N (R7); R7 is selected from the group consisting of Hydrogen and alkyl;

R15 is selected from the group consisting of hydrogen, self-based, alkyl, and self-alkyl; less is NH; M is selected from the group consisting of N and R1-C;

R1 is selected from the group consisting of hydrogen, hydroxy, hydroxylamino, methylamido, amine, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxy Amine, i-alkyl, self-alkoxy and self-group; R2 is Z〇_Q; z () is a covalent single bond; Q is selected from the group consisting of aryl and heteroaryl, one of which is adjacent to the carbon of the connection point Carbon, which is optionally replaced by R9, another carbon adjacent to the junction carbon, which is optionally replaced by R13, a carbon adjacent to 119, which is two atoms away from the junction carbon, is optionally replaced by R10, and one adjacent to R13, and The carbon two atoms away from the point of attachment is optionally replaced by R12, and any carbon adjacent to both R10 and r12 is optionally replaced by R11; R9, R11 and R13 are independently selected from the group consisting of hydrogen and hydroxyl , Amine, Formamidine-87- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---- K ---- Order --------- Line (Please Read the notes on the back before filling this page) 1222445 A7 ___ B7 V. Description of the Invention 垆) Group, guanidino, lower alkylamino, alkylthio, alkylsulfonyl, sulfonylsulfonyl Fluorenyl, alkyl, fluorenyl, self-alkyl, fluorenyl, alkoxy, and cyano; R10 and R12 are independently selected from the group consisting of hydrogen, methyl, methyl, guanidyl, alkyl, alkoxy,, Hydroxyl, amine, lower alkyl amine, alkyl sulfonyl, monoalkyl sulfonyl sulfonium, dialkyl, amine fe, functional group, self-burning group, :): end group, carboxyl group Amine group and cyano group; K is CH2; E0 is C (0) N (H); is formula (IV): oxo, oxo, succinyl, hydrazino, amine, and SS, hydroxyalkyl, Carboxyl, Carboxamidine, Ethylamine, Acetylamido, Alkoxyamino, Aminoalkyl, Continuous Amino, Amidino, SS, Amino, Lightly Oxycarbonyl, Lean Tetane Q3

R 17 18 ------------ ^ install ---- K ---- order --------- (Please read the back ^ / notes before filling in this page)

R

'R 19 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (IV) where D5, D6, J5 and J6 are independently selected from the group consisting of C, N, 0, s and covalent bonds. Valence bond, κ2 is c, no more than one of D5, D6, J5 and J6 is 0, no more than one of D5, D6, J5 and J6 is S, when two of D5, D6, J5 and J6 are 0 and When s, one of D5, D6, J5 and J6 must be -88- winter, A Zhang ruler! Weekly China National Standard (CNS) A4 (210 X 297 public reply) —

Description of the Invention (86 Covalent bonds printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, and no more than four of d5, d6, j5, and J6 are ^^; R, R, R18, and R19 are independently selected from the group consisting of hydrogen, Formamyl, guanidino carboxyl, S alkylthio, alkoxy, hydroxyl, amine, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylsulfonyl Alkyl, k-, s-, s-, s-, s-, s-, and s-oxyl, # tris-sulphonyl, amino-sulphonyl, and cyano; R and R 9 are Qb as the case may be, and the conditions are R16 and R1 9 Not more than one is Qb, and Qb is Qbe;

Qb is selected from the group consisting of NR2R2l, Qbe, where Qbe is hydrogen and C (NR25) NR23R24 and 2 (), 1121, 1123, 1124, and 25 are independently selected from the group consisting of fluorenyl and alkyl;

Qs is CH2. In another preferred embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is optionally selected from the group consisting of hydrogen, c: 2-C8 alkyl, and C3-C8 methyl. , C3-C8 alkynyl and C2-C8 self-alkyl, where each member of the group B is optionally one or more including 1132 at any carbon that is high from the point of attachment of B to A and contains 6 atoms, 1133, 1134, 1135, and 1136 group substitutions; Chemical 32, Chemical 33, 4, 5, and 6 are independently selected from the group consisting of hydrogen, acetamido, haloacetamido, formamidine, Guanidine, alkoxy, hydroxyl, amine, alkoxy amine, low-carbon thio amine, thio thio, sulfonyl amine, sulfonyl, sulfonyl Amino-based continuation, burn-in, self-based, alkynyl, alkoxy, hydroxyalkyl, alkoxycarbonyl, carboxyl, carboxamido, 89 μM scale applicable to Chinese National Standard (CNS) A4 Specifications (210 x 297 mm) ---------------- l · --- order --------- line Φ- (Please read the phonetic on the back? Please fill in this page for further information) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 V. Description of the invention (87) Cyano and Qb; Eight series are selected from the group consisting of covalent single bond and (CH (R15)) pa_ (W7) rr, where rr is an integer selected from 0 to 1, and pa is selected from An integer of 0 to 3, and W7 is N (R7); R7 is selected from the group consisting of hydrogen and alkyl;

R15 is selected from the group consisting of hydrogen, fluorenyl, alkyl, and ialkyl; 氺 is NH; M is selected from the group consisting of N and R1-C; R1 is selected from the group consisting of hydrogen, hydroxyl, hydroxylamine, and methylfluorenyl , Amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, self-alkyl, i-alkoxy, and i-group; R2 Is Z0-Q; is a covalent single bond; Q is selected from the group consisting of aryl and heteroaryl, one of which is adjacent to the carbon of the connecting point carbon, which is optionally substituted by R9, and the other of which is adjacent to the carbon of the connecting point carbon, which is The case is replaced by R13, a carbon adjacent to R9 and two atoms away from the connecting point carbon is replaced by R1G as the case, a carbon adjacent to R13 and two atoms away from the point carbon is replaced by R12, and the adjacent Any carbon of R10 and R12 is optionally substituted by Ri 1; R9, R11, and R13 are independently selected from the group consisting of hydrogen, hydroxyl, amine, formamidine, guanidyl, lower alkylamino, and alkyl Thio, alkoxy, alkylsulfinamidinyl, alkylsulfenyl, fluorenylamino, fluorenyl, monoalkylsulfinylfluorinyl, alkyl, alkyl, alkyl Hydroxyl Group, carboxyl group, carboxyamido group and cyano group; R10 and R12 are independently selected from the group consisting of hydrogen group, acetoamino group, and acetoamino group-90- This paper size applies to Chinese National Standard (CNS) A4 specifications (210 X 297 mm) ---------------- l · --- Order --------- line · (Please read the phonetic on the back? Matters before filling in this Page > 1222445

V. Invention Description (88)

Qs

, Formamidine, guanidyl, alkyl, alkoxy, alkoxyamino, aminoalkyl, warpyl, amine, lower alkylamino, alkylsulfonylamino, sulfonylamino Fluorenyl, monoalkylsulfonylsulfonyl, dialkylsulfonylsulfonyl, hydroxyalkyl, aminoalkyl, self-alkyl, alkoxycarbonyl, carboxyl, carboxyalkyl, carboxyamino, and Cyano; κ is ch2; E0 is C (0) N (H); is formula (IV): (IV) where D5, D6, J5 and J6 are independently selected from the group consisting of c, N, 〇, s and covalent The bond is subject to the condition that no more than one is a covalent bond, K2 is c, d5, D6, J5, and J6 are no more than one, and no more than one of D5, D6, J5, and j6 is s. When D5, D6 When two of J5 and J6 are 0 and s, one of d5, D6, J5 and J6 must be a covalent bond 'and no more than four of D5, D6, J5 and J6 are n, with the condition that R R, R18, and R19 are each independently selected to maintain the tetravalent nature of carbon, the trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen; R16, Hua17 ,! ^ 8 and Ri9 are independently selected from the group consisting of hydrogen, methylformyl, guanidyl, leptyl, sulfanyl, alkoxy, hydroxyl, amine, and lower alkyl amine groups -------- --91-The size of this paper applies Chinese National Standard (CNS) A ^^ 〇χ 297 male) -------------- ^ equipment ---- J ---- order-- ------- Hua (please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs ), Alkylthio, Alkylsulfinyl, Alkylsulfonyl, Alkyl, Alkyl, Alkyl, I, Alkyl, S Alkoxy, Hydroxyalkyl, Amine Alkyl And cyano groups; R16 and R19 series depending on the situation as a furnace, with the proviso that the rule ^ and "9 are not more than one when Qb, and the furnace is Qbe;

Qb is selected from the group consisting of NR20R21, Qbe, where Qbe is hydrogen, N (R26) C (NR25) N (R23) (R24) and C (NR25) nr23r24; ^, ... ^ '... and the heart system are independently selected Since including hydrogen and alkyl; q ^ ch2. In yet another preferred embodiment of the compound of formula I or a pharmaceutically acceptable salt thereof, J is 0; B is optionally selected from the group consisting of a C3-C7 ring alkyl group and a C4-heterocyclic group, wherein each ring carbon It is optionally substituted by R3 3, a ring carbon, not the ring carbon of the B to A connection point, and it is optionally replaced by a keto group, provided that no more than one ring carbon is simultaneously replaced by a keto group, and the carbon adjacent to the connection point The ring carbon and nitrogen atom of the atom are replaced by R9 or R13 as appropriate. The ring carbon or nitrogen atom adjacent to the position of R9 and two atoms away from the connection point are replaced by R10 as appropriate, two adjacent to the position 3 and two points away from the connection point. The ring carbon or nitrogen atom of the atom is replaced by r1 2 as appropriate, the ring carbon or nitrogen atom located three atoms away from the connection point and adjacent to Ri 〇, is replaced by R11 as the case may be, three atoms away from the connection point and adjacent to Ri2 The ring carbon or nitrogen atom at the position is replaced by R3 3 as appropriate, and the ring carbon or nitrogen atom that is four atoms away from the connection point and is adjacent to the positions of RH and R33 is replaced by R34 as the case may be; _ -92- Applicable to China National Standard (CNS) A4 specification (210 X 297 public love) --- --------------- ^ ---- Order --------- Line (Please read the note on the back? Matters before filling out this page) 1222445 A7

Printed by the Employees' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (90) R9, R11 and R13 are independently selected from the group consisting of hydrogen, hydroxyl, amine, formamidine, guanidyl, low-carbon alkylamine, Alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, alkylaminosulfonyl, monoalkylphosphonaminosulfonyl, alkyl, free radical, alkyl Oxy, hydroxyalkyl, carboxyl, carboxyamido, and cyano; R1G and R12 are independently selected from the group consisting of hydrogen, acetamido, autoacetamido, methylamido, guanidino, alkyl, and alkyl Oxy, alkoxyamino, aminoalkyl, hydroxy, amine, lower alkylamino, alkylsulfonamido, sulfonamidosulfonyl, monoalkylsulfonamidosulfonyl, Dialkylfluorenylaminosulfonyl, hydroxyalkyl, aminoalkyl, self-group, self-alkyl, alkoxycarbonyl, carboxyl, carboxyalkyl, carboxylamino and cyano; R3 3 and R3 4 series Independently selected from the group consisting of hydrogen, methylamino, guanidyl, alkoxy, hydroxyl, amine, alkoxyamino, lower alkylamino, alkylthio, sulfamoylsulfonyl, monoalkyl Sulfaminyl Sulfonylaminosulfonyl, sulfonyl, sulfonyl, sulfonyl, sulfonyl, sulfonyl, sulfonyl, sulfonyl, leptyl, aminoacid and diyl; R33 is Qb, as the case may be; A is selected from the group consisting of a covalent single bond and (CH (R15)) pa- (W7) rr, where rr is an integer selected from 0 to 1, pa is an integer selected from 0 to 3, and W7 is N (R7 "R7 is selected from the group consisting of hydrogen, alkoxy, and alkyl; R15 is selected from the group consisting of hydrogen, alkynyl, and alkyl; Ψ is NH; M is selected from the group consisting of N and R1 -C; R1 Selected from the group consisting of hydrogen, hydroxyl, hydroxylamine, methylamido, amine, cyanide ___-93 ~ __ This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) " ~ --- ---------- ^ 装 ---- J ---- Order --------- S— (Please read the precautions on the back before filling this page) 1222445 A7 B7 5 N Description of the invention (91 groups, free radicals, fluorenyl groups, pit groups, tiger amino groups, amine groups, fluorenylthio groups, alkoxyamine groups, haloalkyl groups, alkoxy groups and fluorenyl groups; R2 Is Z〇-Q; ZQ is a covalent single bond; Q is selected from the group consisting of an aryl group and a heterosquare group, 'after one of the Zheng Jin connection points is broken,' which is optionally replaced by R9 '; A carbon adjacent to the junction carbon is replaced by R13 as appropriate, a carbon adjacent to R9 and two atoms away from the junction carbon is replaced by R1 G as appropriate, a carbon adjacent to R13 and two atoms away from the junction carbon , Is optionally substituted by R1 2 and any carbon adjacent to both R10 and R12, is optionally substituted by R1 1; κ is ch2; E0 is C (0) N (H); W is formula (IV):

Qs

R 17

R 16〆 D, 18

'R 19 t ----- ^ ---- Order --------- (Please read the precautions on the back before completing this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs (IV) D5, D6, J5, and J6 are independently selected from the group consisting of c, N, 0, S, and covalent bonds, with the proviso that no more than one is a covalent bond, and κ2 is C, D5, D6, J5, and J0 More than one is 0, and not more than D5, D6, J5, and J6 are s. When two of D5, D6, J5, and J6 are 0 and S, one of d5, D6, J5, and j6 must be- 94-1222445 radicals, alkyls, alkyls, amidoalkylaminos and cyano groups; R10 and R19 are Qb if more than one is Qb, and Qb is Qb

R A7 V. Description of the invention (92) Covalent bond, and no more than four of D5, D6, J5 and J0 are N, with the proviso that each of Rl'Rl'RU and RW is independently selected to maintain the fourth carbon Valence properties, trivalent properties of nitrogen, divalent properties of sulfur, and divalent properties of oxygen; R16, R1'R18 and R19 are independently selected from the group consisting of hydrogen, formamyl, guanidyl, thio, halide , Oxo, hydroxy, amine, lower alkylamino, thiosulfanyl, sulfinylsulfenyl, alkylsulfonyl, alkylsulfonyl, alkylsulfonyloxy Alkylenyl with the additional condition that R1 6 and R1 9 are different

Qb is selected from the group consisting of NR20R21, Qbe, where Qbe is a hydrogen group and 112 (), and 21, 1123, 1124, and 1125 are independently selected from the group including hydrogen and alkyl;

Qs is CH2. In a preferred special embodiment of Formula I, the compound has the formula [_s: 2 (please read the precautions on the back before filling out this page)> ---- r ---- Order ------ --- Line ·· Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

Or a pharmaceutically acceptable salt thereof, wherein: B is the following formula: (I-S) -95- 34 A7 V. Description of the Invention 钿)

R 33

R

, R 35 R3 6 Read the back of the 'Note Han 32, 113: 3, 1134, 1135, and 1 ^ 6 are independently selected from the group consisting of hydrogen, methyl, guanidyl, carboxyl, methyl, ethyl, isopropyl Propyl, propyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amine, methoxyamino, ethoxyamino, ethoxylamine, trifluoroacetamido , Nitro, aminomethyl, iminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio Methyl, trifluoromethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy 1,1,2,2-tetrakiethoxy, oxo, oxo, oxo, glyoxanyl, yoxanyl, N-methylamidosulfonyl, n, N-di Methylsulfonylsulfonyl, ethylsulfonyl, propionyl, trifluoroethylsulfonyl, pentafluoropropionyl, methylol, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2 -Trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1-trifluoromethyl small hydroxyethyl, carboxymethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-formyl Sulfonylaminocarbonyl, N, N-dimethyl Amidocarbonyl, cyano and Qb: B is selected from the group consisting of hydrogen, trimethylsilyl, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2- Butyl, 3-butenyl, 2-butynyl, second-butyl, third-butyl, isobutyl, 2-methpropenyl, 1-pentyl, 2-pentenyl, 3- Pentamyl, 4-pentenyl, 2-pentynyl-96- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm). Refill this page Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, printed 1222445 A7 --------- B7______ V. Description of the Invention (94), 3-pentynyl, 2-pentyl, 1-methyl · 2_ Butenyl, 1-methyl-3-butenyl, 1-methyl · 2-butynyl, 3 · pentyl, 1-ethylpropenyl, 2 · methylbutyl, 2-methyl · 2 -Butenyl, 2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl- 3-butyridyl, 1-hexyl, 2-hexenyl, 3.hexenyl, 4.hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-form 2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl , 3-hexyl, 1-ethyl-2, butanyl, 1-ethyl-3, butanyl, 1-propyl_2-propanyl, 1-ethyl-2-butyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptyl, 5- Heptyl, 2-heptyl, 1-methyl-2-hexyl, 1-methyl_3-hexyl, 1-methyl-4-hexyl, 1-methyl_5-hexyl Alkyl, 1-methyl-2-hexyl, 1-methyl-3-hexyl, 1-methyl-4-hexyl, 3-heptyl, 1-ethyl-2-pentamidine 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl, 1-butyl-2-propenyl, 1-ethyl-2-pentyl, 1-ethyl 3-pentyl, 1-octyl, 2-octyl, 3-octenyl, 4-octenyl, 5-octenyl, 6-octenyl, 7-octyl, 2-octynyl: 3-octyl, 4-octyl, 5-octyl, 6-octyl, 2-octyl, 1-methyl-2-heptyl, 1-methyl-3-heptyl, 1-methyl-4-heptanyl, 1-methyl-5-heptanyl, 1-methyl-6-heptanyl, 1-methylheptyl Methyl, methyl-3-heptynyl, 1-methyl-4-heptenyl, 1-methyl-5 · heptenyl, 1_methyl-6_heptenyl, 1 · methyl-2 -Heptyl, 1-methyl-3_heptyl, 1-methylheptyl, 1-methyl · 5-heptyl, 3-octyl, 1-ethyl-2-hexenyl ,; Μethyl_3-hexyl, 1-ethyl-4_hexyl, 1_ethyl-2-hexyl, [_ethyl_3 «hexyl, 1_ethyl -4-Hexyl, 1_ethyl-5-hexyl, ι_pentyl_2_propanyl-97 · This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ''----- K ------------- ^^ 1 (Please read the precautions on the back before filling this page) A7

1222445 V. Description of the invention (95), 4-octyl, 1-propyl-2-pentenyl, 1-propyl-3-pentenyl, μpropyl 4-pentenyl, 1-butyl 2-butenyl, 1-propyl-2 · pentynyl, μpropyl · 3 · pentynyl 1-butyl-2-butdecyl, 1-butyl-3-butenyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl 5,5,5-trifluoropentyl, 4.trifluoromethylpentyl, 5,5, 6,6,6-pentafluorohexyl and 3,3,3-trifluoropropyl, where each member of the group B is optionally at any carbon containing 5 atoms from the point where the B-to-A connection is high, and One or more of the groups including "夂: ^ 夂 is substituted with hydrazone" and "H"; B is optionally selected from the group consisting of cyclopropyl, cyclobutyl, propylene oxide_2_yl, propylene oxide_3 _Yl, mononitrotetramethylpyridyl, mononitrotetramethylpyridine_2_yl, mononitrotetramethylpyridine · 3-yl, monothiotetramethylpyridine_2_yl, monothiotetramethylpyridine_yl, cyclopentyl, Cyclohexyl, gold steel pit base, n: f | group, 3-trifluoromethyl n-singyl group, bicyclofluorene [3; [〇] hexane-6-yl, cycloheptyl and cyclooctyl, wherein each ring carbon system Optionally replaced by R33, the ring carbon and nitrogen atom of the carbon atom adjacent to the connection point, It is replaced by R9 or R13 as appropriate, and the ring or nitrogen atom of two atoms adjacent to the position of R9 and two points away from the connection point is replaced by R10, and the ring carbon or nitrogen atom of two atoms adjacent to the position of Ri3 and two points away from the connection point, Is optionally substituted by Rl2; R9, R10, R11, R12 and R13 are independently selected from the group consisting of hydrogen, formyl, guanidino, carboxyl, carboxymethyl, methyl, ethyl, isopropyl, propyl, Methoxy, ethoxy, isopropoxy, propoxy, hydroxyl, amine, methoxyamine, ethoxyamine, ethylamine, trilactamamine, nitro, amine Methyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoro Methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2 · trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1 , 2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methyl tiger -98- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------ --------- l · — — —Order --------- line, (Please read the precautions on the back before (Write this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Consumer Cooperatives of the Ministry of Economic Affairs 1222445 A7 B7 V. Description of the invention (96) Sulfonamido, sulfonamidosulfonyl, N-methyl Sulfonylaminosulfonyl, N, N-dimethylsulfonylsulfonyl, ethynyl, propionyl, trifluoroethynyl, pentafluoropropionyl, hydroxymethyl, 1-hydroxyethyl , 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro · 1 · trifluoromethyl-1-hydroxyethyl, carboxymethyl, methoxy Carbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N, N-dimethylamino and fluorenyl; A is selected from the group consisting of covalent single bonds, 0, S, NH, N (CH3), N (OH), C (0), CH2, CH3 CH, CF3 CH, NHC (O), N (CH3) C (0), C (0) NH, C (0) N (CH3), CF3 CC (0), C (0) CCH3, C (0) CCF3, CH2 C (0), (0) CCH2, CH2 CH2, CH2 CH2 CH2, CH3 CHCH2, CF3 CHCH2, CH3 CC (0 ) CH2, CF3 CC (0) CH2, CH2 c (o) -CCH3, CH2 C (0) CCF3, CH2 CH2 C (0) and CH2 (o) cch2; A is selected from the group including CH2N (CH3), CH2N (CH2 CH3), CH2 CH2N (CH3) and CH2CH2N (CH2CH3). With the proviso that B is hydrogen; M is selected from the group consisting of N and R1 -C; R1 is selected from the group consisting of hydrogen, hydroxyl, amine, thiol, formamyl, hydroxylamine, aminomethyl, 1 · amine Ethyl, 2-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl, isopropyl, propyl, trifluoromethyl, pentafluoroethyl, 2, 2, 2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, methoxy, ethoxy, propoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, Methoxyamino, ethoxyamino, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro and bromo; R2 Is Z0-Q; ZG is selected from the group consisting of covalent single bonds, 0, S, NH, CH2, CH2 CH2, CH (OH), CH (NH2), CH2 CH (OH), CH2 CHNH2, CH (OH) CH2 And CH (NH2) CH2; -99- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) -----------------: --- -Order --------- line (please read the precautions on the back before filling this page) ^ 22445

Printed by the Employees' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the Invention (97) Q is selected from the group consisting of phenyl, 2-sphingyl, 3-side phenyl, 2-succino, 3-furanyl, and 2-pyrrole. , 3-pyrrolyl, 2-imidazolyl, each imidazolyl, 3-pyrazolyl, 4.pyrazolyl, 1,2,4.triazol-3-yl, 1,2,4_triazole_ 5_ki, maki-jun-3-ki, 1,2,4 'jijun-5-ki, 1,3,4_ginji_3_ji, [3,4-ginji- 5-yl, 3-isoxazolyl, 5-isopyrazolyl, 2.oxazolyl, 2-edgeoxazolyl, 3-isooxazolyl, 5-isooxazolyl, 2-pyridyl, 3- Pyridyl, 4-pyridyl, 2-p-pyridyl, 2-pyridyl, 4-pyridyl, 5-, pyridyl, 3-pyridyl, 4-pyridyl, 1, 3, 5 · triazine-2-yl, 1,2,4 · trinitrogen_3_base, 1,2,4 · trinitrogen well-5-based, 1,2,4_triazine_ -6 -Yl, 1,2,3-triazine_4_yl and ι, 2,3-triazine_-5- • yl, one of which is a carbon adjacent to the connecting point carbon, which is optionally replaced by R9, and the other A carbon adjacent to the junction carbon is replaced by R13 as appropriate, and a carbon adjacent to R9 and two atoms away from the junction carbon is replaced by R10 as appropriate. A carbon adjacent to R13 and two atoms away from the point of attachment is optionally replaced by R12, and any carbon adjacent to both R1 G and R12 is optionally replaced by R11; K is CHR4a, which is selected from the group consisting of A Methyl, ethyl, propyl, isopropyl, hydroxymethyl, 1, hydroxyethyl, methoxymethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoromethyl, methyl Thiomethyl and hydrogen; E0 is a covalent single bond, C (0) N (H), (H) NC (O) and S (0) 2N (H); Y0 is selected from the chemical formula including ： -100- 1 This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) ------------ K ---- Order -------- -(Please read the notes on the back before filling out this page) 1222445 A7 B7 V. Description of the invention (98)

Qs

R 17 18

R

Qb Qs 19

Qs

R 17

R 18

R N \ ^ \ r19 Qb Qsπ 丄 』Qb

R 16.

Qb 0s 18 N ^ Γ ΐ Ί, / Is 4 Ν r18

R 19 18 • R19 ---------------- K ---- Order --------- line (please read the note on the back? Matters before filling in this Page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

Qb -101-This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 B7 V. Description of the invention (")

Qs

R 17

Qb

R 18

R

Qb

N .R-

R 19

Qb R ''

R 19

Printed by Qb RJ Consumer Cooperatives, Intellectual Property Bureau, Ministry of Economic Affairs

R 19

Qb R "---------------- K ---- Order --------- line (Please read the back ^ / notes before filling in this page)

R 19

N -Qb -102 This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ____________ B7 V. Description of Invention (100)

Isopropyl, propyl, formamyl, guanidyl, carboxyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxyl, amino, methoxyamino, ethoxyamine, Aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, tris Fluoromethylthio, methylsulfenyl: methyl, ethylidene, methylphenyl, ethylsulfonyl SS, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoro Ethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, U, 2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amido Base, N-methyl acid amine group, hydroxy group, n, N-dimethyl SS amino group, si group, ethenyl group, propyl group, trifluoroethyl group, pentafluoropropionyl group, methylol Group, 1-hydroxyethyl group, 2-hydroxyethyl group, 2,2,2-trifluoro-1-hydroxyethyl group and cyano group; R10 and R19 are Qb as the case may be. When more than one is Qb, and Qb is Qbe;

Qb is selected from the group consisting of NR20R21, Qbe, where Qbe is hydrogen-based, -103-This paper is only 7 degrees applicable to China National Standard (CNS) A4 specifications (210 X 297 mm)---------- ------- K ---- Order --------- line (Please read the back ^ / Notes before filling out this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 0

A7 B7 V. Description of the invention (101) C (NR25) NR23R24 and N (R26) C (NR25) N (R23) (R24), with the proviso that more than one of R2G and R21 is not hydroxyl, N-methylamino And N, N-dimethylamino 'and R2 3 and R2 4 are not more than one per group, N-methylamino and N, N-dimethylamino; R2G, R21, R23, R24, R25 & R26 Is independently selected from the group consisting of hydrogen, methyl, ethyl, propyl, butyl, isopropyl, hydroxy, 2-aminoethyl, 2- (N-methylamino) ethyl, and 2- (N, N-dimethylamino) ethyl;

Qs is selected from the group consisting of covalent single bonds, CH2, CH2 CH2, CH3 CH, CF3 CH, CH3 CHCH2, CF3 CHCH2, CH2 (CH3) CH, CH = CH, CF = CH, C (CH3) = CH, CH = CHCH2, CF = CHCH2, C (CH3) = chch2, ch2 ch = ch, ch2 CF = CH, CH2 C (CH3) = CH, ch2 ch = chch2, ch2 cf = chch2, ch2 c (ch3) = chch2, ch2 CH = CH- CH2 CH2, CH2 CF = CHCH2 CH2 and CH2 C (CH3) = CHCH2 CH2. In a more preferred specific embodiment of Formula I, the compound has Formula I-MPS, where B is aromatic: o (I-MPS, where B is aromatic) or a pharmaceutically acceptable salt thereof, wherein: B is The following formula: -104- This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) ---- K ---- Order --------- Line (Please read the back first ^ / Notes, please fill out this page again) 1222445 A7 B7 V. Description of Invention (1〇2)

R 34, 33

R 35 r3 2 ^ \ ^ \ r36 Ruler 32, 1133, Chem 34, Ruler 35, and Rule 1136 printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs are independently selected from the group consisting of hydrogen, formamyl, guanidyl, carboxyl, and methoxy Group, ethoxy, isopropoxy, propoxy, hydroxyl, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, Dimethylamino, N · ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3 , 3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, fluoro, bromo, amidosulfonyl, N-methyl Amidosulfonyl, N, N-dimethylamidoamino, hydroxymethyl, μ light ethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl , Methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N, N-dimethylamidocarbonyl, cyano and Qb: A is selected from the group consisting of covalent single bonds, NH, n (CH3), N (OH), CH2, CH3 CH, CF3 CH, NHC (O), N (CH3) C (0), C (0) NH, C (0) N (CH3), CH2 CH2, CH2 CH2 CH2, CH3 CHCH2 CF3 CHCH2: Qb is selected from Including NR20R21, Qbe, where Qbe is hydrogen and C (NR25) NR23R24, with the proviso that r2o and R2i are different when more than one is a hydroxyl group, and R23 and R24 are not more than one is a hydroxyl group; R24 & R25 is independently selected from the group consisting of hydrogen, methyl, ethyl, propyl, butyl, isopropyl and light base; -105- This paper size is applicable to China National Standard (CNS) A4 (210 X 297) Li) ----- ^ ---- ^ --------- (Please read the precautions on the back before filling in this page> 1222445

V. Description of the invention (103)

Qs is selected from the group consisting of covalent single bonds, CH2 and CH2 CH2. In another more preferred specific embodiment of Formula 1, the compound has Formula I-MPS 'where B is a non-cyclic substituent: 2,

IV VR 0 Ή / 丫 0 〇 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (I-MPS 'where B is a non-cyclic substituent) or a pharmaceutically acceptable salt thereof, where: B is selected from the group consisting of hydrogen , Ethyl, 2-propenyl, 2-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, second-butyl, Tri-butyl, isobutyl, methacryl, μpentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2 -Pentyl, 1-methyl-2-butenyl, μmethyl_3-butenyl, μmethyl-2-butynyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 2-methyl-3 · butynyl, 3-methylbutyl, 3-methyl 2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 2-hexyl Bulk, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl_4-pentene Base, 1-methyl-2-pentyl, 1-methyl-3-pentyl, 3-hexyl, 1-ethyl-2-butenyl, 1-ethyl-3-but Base, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl, 2-heptanyl, 3-heptanyl, 4-heptanyl, 5-heptyl Base, 6 _______ -106- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) -------------:-order -------- -(Please read the phonetic on the back? Matters before filling out this page) 1222445 A7 _______ B7 V. Description of the invention (104) (Please read the notes on the back before filling out this page) Heptenyl, 2-heptynyl, 3 -Heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4 Hexenyl, 1 methyl 5-hexenyl, 1 methyl-2-hexynyl, 1-methyl_3_hexynyl, 1-methyl_4_hexynyl, 3 Heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4pentenyl, 1-butyl-2-propenyl, 1-ethyl 2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5 · Trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl and 3,3,3-trifluoropropyl, where each member of the group B is subject to the situation At distance B vs. A Any carbon where the connection point is high and contains 5 atoms is replaced by one or more groups including 1132, 1133, 1134, 1135, and 1136; printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs R3 2, R3 3, R3 4, R3 5 and R3 6 are independently selected from the group consisting of hydrogen, formamyl, guanidyl, methoxy, methoxy, ethoxy, isopropoxy, propoxy, chloro, amine, and methoxy Methylamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropyl Thio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2 , 2-tetrafluoroethoxy, fluoro, chloro, bromo, fluorenylsulfonyl, N-methylsulfonylsulfonyl, N, N-dimethylsulfonylsulfonyl, Hydroxymethyl, 1-hydroxyethyl, 2 · hydroxyethyl, 2,2,2 · trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidoamine Carbonyl, N, N-dimethylamidocarbonyl, cyano and Qb; A is selected from the group consisting of covalent single bonds, NH, N (CH3), N (OH), CH2, CH3 CH CF3 CH, NHC (O), N (CH3) C (0)? C (0) NH? C (0) N (CH3 \ CH2 CH2? CH2 CH2 CH2? CH3CHCH2 &CF3CHCH2; A is selected from the group including CH2N (CH3), CH2N (CH2 CH3), CH2 CH2N (CH3) -107- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 B7 V. Description of the invention (105) and CH; 2 CH2N (CH2 CHS) 'with the proviso that b is hydrogen. Qb is selected from the group consisting of NR20R2l, Qbe, where ^ C (NR25) NR23R24 and N (R26) C (NR25) N (R23) ( R24), the horse's gas group, R2 0 and R2 1 are not more than one hydroxyl group at the same time, and r2 3 blood, and the file with one of them are hydroxyl groups; no, more than R20, R21, R2W5 and heart system are independently selected Including hydrogen, methyl, ethyl, propyl, butyl, isopropyl and mesogen; Qs is selected from the group consisting of covalent single bonds, ch2 and ch2ch2. In yet another more preferred specific embodiment of Formula I, the compound has I-MPS, where B is a non-aromatic cyclic substituent: Formula V ^ '

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (I-MPS, where B is a non-aromatic cyclic substituent) or a pharmaceutically acceptable salt thereof, where: B is selected from cyclopropyl and cyclobutane Propylene oxide, propylene oxide monoazatetra-1-enylazatetramethyl-2-ylazatetramethyl-3-yl, monothiotetramethyl-3-yl, cyclopentyl, cyclohexyl, n-singyl, bicyclofluorene [31 · 〇] Hex-6-yl and cycloheptyl, wherein each ring carbon is substituted by R3 3 as appropriate, and the ring carbon and nitrogen atom of the carbon atom adjacent to the connection point are substituted by R9 or Ri 3 as appropriate, A ring carbon or nitrogen atom adjacent to R9 and two atoms away from the connection point, depending on the situation, is -108- This paper size applies the Chinese National Standard (CNS) A4 specification (21〇x 297 mm) ------ ------------ r --- order --------- line <read first read the seven notes on the back then fill out this page> 1222445 A7 Β7 V. Description of the invention (106 ) (Please read the notes on the back before filling out this page) R1G substitution, and the ring carbon or nitrogen atom adjacent to R13 and two atoms away from the connection point, are replaced by R12 as appropriate; A is selected from the group consisting of covalent orders Bond, NH, N (CH3 ), N (OH), CH2, CH3 CH, CF3 CH, NHC (0)? N (CH3) C (〇l C (0) NH? C (0) N (CH3% CH2 CH2, CH2 CH2 CH2? CH3CHCH2 & amp CF3CHCH2; R33 is independently selected from the group consisting of hydrogen, methylamino, guanidino, carboxyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxyl, amine, methoxyamino, and ethyl Oxyamino, acetylamino, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl Base, pentafluoroethyl, 2,2,2-difluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2, tetrafluoroethyl Oxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonamido, N, N-dimethylamidosulfamoamido, 1-methyl, 1- Hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N_methylamidocarbonyl, N, N_ Dimethylphosphoniumaminocarbonyl, cyano and Qb;

Qb is selected from the group consisting of NR20R2 !, Qbe, where Qbe is a hydrogen group and C (NR25) NR23R24, with the proviso that when more than one is not hydroxyl at the same time, and not more than one is hydroxyl at the same time Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 112 (), 1121, 1123, 1124 and 1 ^ 5 are independently selected from the group consisting of hydrogen, methyl, ethyl, propyl, butyl, isopropyl and hydroxyl;

Qs # is selected from the group consisting of a covalent single bond, O112, and CH2CH2. The compound of the present invention having the following formula is a more specific embodiment (I-MP8): 109 ^ 1 V 1 / r \ but-r 公 yy 1222445 A7 B7 gas group and brook group: 2-furanyl, 3-4 -Wei Junji, 3-V. Invention Description (107

Or a pharmaceutically acceptable salt thereof, having a common structural unit, wherein: M is selected from the group consisting of n and r1_c; R1 is selected from the group consisting of hydrogen, light, amine, formamidine, amido, amine Methyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2, trifluoroethyl, Methoxy, hydroxymethyl, 1-light ethyl, 2-hydroxyethyl, methoxyamino, methylthio, ethylthio, trifluoromethoxy, 1,: 1,2,2-tetramethyl Fluoroethoxy and fluoro group R2 are Z0-Q; Z0 is selected from the group consisting of covalent single bonds, s, nh, and ch2; Q is selected from the group consisting of phenyl, 2-pyrimyl, and 3-thienyl Ethyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl-pyridyl, 4-pyrazolyl, 2-pyrimazolyl, 3-isopyrazolyl, 5-isohumidyl, 2 -Pyridinyl, 3-pyridyl, 4-pyridyl, 2-pyridyl, 2-pyrimidinyl, 4-pyridyl, 5-pyridyl, 3-pyridyl, 4_ &amp; well-based, and three-kids-2 -Base, of which-a carbon adjacent to the carbon of the connection point is replaced by as appropriate, another carbon adjacent to the carbon of the connection point is replaced by RU as appropriate, one is adjacent to R9 and Two atoms away from the connection point are replaced by Ri0, depending on the situation,-a case of two atoms adjacent to W and two atoms away from the connection point ---- K- --- Order --------- line (Please read the back ^ / notes before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

1222445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ___B7___ V. The description of the invention (108) is replaced by R12, and any carbon adjacent to 1 () and R12 is replaced by R11 as appropriate; Is independently selected from the group consisting of hydrogen, methyl, guanidino, carboxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, meridyl, Amine, N-methylamino, n, N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2, 2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, Bromo, methylamine, sulfamoyl, N-methylsulfinomethylsulfonyl, N, N-dimethylamidosulfinomethyl, hydroxymethyl, 1-hydroxyethyl Group, 2-hydroxyethyl group, 2,2,2-trifluorosmall hydroxyethyl group, amino group, N-methyl group amino group, N, N-dimethyl group amino group R1G and R12 are independently selected from the group consisting of hydrogen, formamyl, guanidino, carboxyl, carboxymethyl, methyl, ethyl, propyl, isopropyl, Methoxy, ethoxy, isopropoxy, propoxy, hydroxyl, amine, methoxyamine, ethoxyamine, acetamido, trifluoroacetamido, aminomethyl , 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylamine, aminosulfonic acid, N-methyl Sulfonylaminosulfonyl, N, N-dimethylsulfonylsulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl Group, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N, N-dimethylamidocarbonyl, fluoro, chloro, bromo and gas groups; YG series It is selected from the following chemical formulas: -111-This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ----------------- ^ --- -Order --------- line (please read the notes on the back before filling this page) 1222445 A7 B7 V. Description of the invention (109) Q5

R 17

, R 18

R

Qb Qs 19 0s

R 17

, R 18

N \ ^^ r19

R

R 18 19

Qb Qs Q Qs b

R

R 18

R 18 19 ----------------: ---- Order --------- line (please read the phonetic on the back? Matters before filling out this page)

Qb

Qb Printed by the Consumer Property Cooperative of the Intellectual Property Bureau of the Ministry of Economy -112 This paper size applies to the Chinese National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 B7 V. Description of the invention (11) Employees ’consumption of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by a cooperative

HN \ / N

Qb (Please read the notes on the back before filling in this page> ----- ^ ---- Order --------- Line-This paper size is applicable to China National Standard (CNS) A4 specifications ( 210 X 297 mm) U22445 V. Description of the invention (111) V \ Q '

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs &amp; 16, 1117, 1118 and 19 are independently selected from the group consisting of hydrogen, methyl, ethyl, isopropyl, propyl, carboxyl, formamyl, guanidyl, Methoxy, ethoxy, isopropoxy, propoxy, hydroxyl, amine, amine fluorenyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamine Methyl, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylphenyl, ethyl Ceryl, trifluorofluorenyl, pentafluoroethyl, 2,2 &gt; trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2, 2. Tetrafluoroethoxy, fluoro, fluoro, bromo, acid amine, N-methyl sulfonyl sulfonyl, n, N-dimethyl sulfonyl sulfonyl, hydroxy Methyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl and cyano: R1 6 and R1 9 are Qb as the case may be, with the condition r1 6 When different from 9, more than one is Qb, and Qb is Qbe. In the best specific embodiment of Formula I, the compound has Formula I-EMP3, where B is aromatic: -114- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --- ------------- K ---- Order --------- (Please read the L Zhuyin on the back? Matters before filling out this page> 1222445

V. Description of the invention (112

V-R 2 〇 B human K · 〇 (I-EMPS, where B is aromatic) or a pharmaceutically acceptable salt thereof, wherein: B is the following formula:

R 34 Ή / 丫 0

R 33

R 35 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. R3 6 7 and 32, 33, 36, 36, 36 and 36 are independently selected from the group consisting of hydrogen, methyl, methyl, methyl, ethyl, Methoxy, ethoxy, mesityl, amine, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2 Gas ethyl, gas base, muryl, brook, amine based, &amp; methyl sulfonyl sulfonyl, hydroxymethyl, sulfonyl carbonyl, carboxyl, cyano and Qb: A series selection Since including covalent single bond, NH, n (CH3), CH2, CH3CH and CH2CH2: Qb is selected from the group consisting of NR20R21 and c (nr25) nr23r24, with the proviso that the Qb group is directly bound to a carbon atom; ____- 115- The size of this paper is applicable to China National Standard (CNS) A4 (210 X 297 mm) ------------------: ----- 丨 Order ----- ---- Line (please read the note on the back? Matters before filling out this page) 1222445 A7 B7 V. Description of the invention (113) Hua 20, Hua 21, &amp; 23, &amp; 24 and Hua25 are independently selected from the group consisting of Hydrogen, methyl, and ethyl; Qs is CH 2 〇 Another preferred specific embodiment of Formula I , The compound has the formula EMPS, where B is a non-cyclic substituent: 2 Μ Ο, k ', N, • ίί Ο Ή / γ 0 (I-EMPS, where B is Acyclic substituent) or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of hydrogen, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl'butyl, 2 -Butylfluorenyl, 2-butynyl, second-butyl, third-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2 · butenyl, 3-methylbutyl, 3-methyl 2-Butenyl, buhexyl, 2-hexenyl, 3-hexyl, 4-hexyl, 2-hexyl, 3-hexyl, 4-hexynyl, 2-hexyl , 1-methyl-2-pentenyl, p-methyl-3-fluorenyl, 1-methyl-2-pentyl, 1-methyl-3-pentyl, 3-hexyl, 1-ethyl 2-butanyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptanyl, 5-heptanyl, 2-heptyl, 3-heptyl, 4-heptyl Base, 5-heptyl, 2-heptyl, 1-methyl-2-hexyl, 1- Methyl-3-hexyl, 1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexyl Alkynyl, 3-heptyl-116- This paper 3 conforms to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) &quot; -----------------:- --- Order --------- line (please read the precautions on the back before filling out this page)> Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 ----- B7 V. Description of Invention (114), 1-ethyl-2-pentenyl, 1-ethyl_3-pentenyl, μethyl_2-pentyl, L ethyl-3-pentynyl, 2,2 , 2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5 · trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6, 6,6-pentafluorohexyl and 3,3,3_trifluoropropyl, where each member of group B is optionally one or more at any carbon that is up to the point of attachment of B to A and contains 5 atoms Each group includes Y 32, H 33, F 34, F 35, F 36 and F 36; and 弋: ^ ^ ^ and ^ are independently selected from the group consisting of a hydrogen group ~ a methyl group ~ a guanyl group, a Methyl, ethyl, methoxy, ethoxy, hydroxyl, amino, N • methylamino, dimethylamino Methylthio, Ethylthio, Trifluoromethyl, Pentafluoroethyl, 2,2,2-Dimuryl, Gas, Chloro, Aoyl, Aminopyranyl, &amp; Methylpyrene Aminosulfonyl, methylol, amidocarbonyl, carboxyl, cyano, and Qb; the eight series are selected from the group consisting of covalent single bonds: ^ 11, wind (: 113), (: 112,013 (: 11 and ( : 112 (: 112; A is selected from the group consisting of CH2N (CH3), CH2N (CH2 CH3), CH2 CH2N (CH3), and CH2CH2N (CH2CH3), with the condition that B is hydrogen;

Qb is selected from the group consisting of NR20R21, C (NR25) NR23r24 and ^^ 26) (3 (^ 25)% (R23) (R24), with the proviso that the Qb group is directly bound to a carbon atom; R20, R2 1 , R23, R24, R25 &amp; R26 are independently selected from the group consisting of hydrogen, methyl and ethyl;

Qs is CH2. In yet another preferred specific embodiment of Formula I, the compound has Formula I-EMPS, where B is a non-aromatic cyclic substituent ... -117- This paper size applies the Chinese National Standard (CNS) A4 specification ( 210 X 297 mm) ----------------- ^ ---- Order --------- line (Please read the precautions on the back before filling in this Page) 1222445 A7 B7 V. Description of the invention (115

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs (I-EMPS, where B is a non-aromatic cyclic substituent) or a pharmaceutically acceptable salt thereof, where: B is selected from the group consisting of cyclopropyl and cyclobutyl, as appropriate Radicals, propylene oxide radicals, monoazatetra-3--3-yl, monothiotetra-3--3-yl, cyclopentyl and cyclohexyl, wherein each ring carbon is optionally substituted by R33, and the carbon atom adjacent to the connection point The ring carbon and nitrogen atoms are optionally replaced by R9 or R13, and the ring carbon or nitrogen atoms adjacent to the position of R9 and two atoms away from the connection point are replaced by Ri 〇, which is adjacent to the position of R13 and two points away from the connection point The ring carbon or nitrogen atom of the atom is optionally substituted by R1 2; R3 3 is independently selected from the group consisting of hydrogen, formamyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxyl, and carboxyl , Amino, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2.2, 2-trifluoroethyl, fluoro, gas, bromo Sulfonylaminosulfonyl, N-methylsulfanylfluorenyl, hydroxymethyl, sulfonylaminocarbonyl, cyano, and Qb; A is selected from the group consisting of covalent single bonds, Li, n (ch3 ), CH2, CH3CH and CH2CH2: Qb is selected from the group consisting of nr20r21 and C (NR25) NR23R24, with the proviso that the Qb group is directly bound to the carbon atom; and 2 () ^ 21, Min 23, Anti 24 and " The 5 series is independently selected from the group consisting of hydrogen, methyl and ethyl; -118 This paper is a national standard (CNS) A4 specification (210 X 297 mm) ------------- --- ^ ---- Order --------- line (please read the note on the back? Matters before filling out this page> 1222445 A7 B7 V. Description of the invention (116 QS is CH2. It has the following formula tThe best specific embodiment of the present invention () μΕΜρβ compound: V / 1

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs or a pharmaceutically acceptable salt thereof, which have a common structural unit, where M is selected from the group consisting of N and Ri -c; R1 is selected from the group consisting of hydrogen, hydroxyl, and amine Methyl, methylamino, hydroxylamino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, methylol, methoxyamino, methylthio, trifluoromethyl R2 is Z0-Q; is a covalent single bond; Q is selected from the group consisting of phenyl, 2-pyrimyl, 2-furyl, 2-pyrrolyl, imimidazolyl, 2 -Pyrazolyl, 3-isopyrazolyl, 2-pyridyl, and 3-pyridyl, one of which is adjacent to the carbon of the connection point, which is optionally replaced by r9, and the other carbon adjacent to the connection point, which is The case is replaced by r1 3, a carbon adjacent to r9 and two atoms away from the junction carbon is replaced by R1 0 as the case, and a carbon adjacent to R13 and two atoms away from the junction carbon is replaced by R1 2 as the case ' And any carbon adjacent to R10 and R1 ▲ are optionally replaced by Rl 丨; R9, R11, and R1 3 are independently selected from the group consisting of hydrogen, methyl, ethyl, and methoxy Ethoxy, hydroxyl, amine, Qinmethylamino, N, N-dimethylamino, methyldi-119- This paper size applies to China National Standard (CNS) A4 (210 X 297 public love ----- ------------ ^ ---- Order --------- line (please read t note on the back? Matters before filling out this page) 1222445 A7 B7 V. Description of the invention ( 117) Thio, trifluoromethyl, pentafluoroethyl, 2,2,2 · trifluoroethyl, fluoro, chloro, bromo, amidosulfonamido, N-methylamidosulfenyl Fluorenyl, N, N-dimethylfluorenylaminosulfonyl, hydroxymethyl, 1-hydroxyethyl, fluorenylaminocarbonyl, N-methylaminoamino, leptyl and oxy; R1G and R12 is independently selected from the group consisting of fluorenyl, methylamidino, fluorenylaminocarbonyl, N-methylfluorenylaminocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxyl, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroethyl Fluorenylamino, aminomethyl, N-methylamino, dimethylamino, fluorenylsulfonylsulfonyl, N-methylsulfonylsulfonylsulfonyl, N, N-dimethylsulfonylsulfonylsulfonium base, Oxocarbonyl, fluoro, chloro, bromo and cyano; Y0 is selected from the chemical formulas including: ---------------- K ------------ ----- 线 # (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -120- This paper size applies to China National Standard (CNS) A4 (210 X 297) 1222445 A7 B7 V. Description of the invention (118) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

----------------- l · --- Order ---------% (Please read the precautions on the back before filling this page) This paper size applies China National Standard (CNS) A4 (210 X 297 mm) Α7

1222445

Qb a tick, methyl, ethyl, methyl ethyl, guanidino, methoxy, hydroxyl, amino, amino methyl, amino ethyl, 2-amino ethyl, N-methyl Amine, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethylpentafluoroethyl, 2,2,2 -Difluoroethyl, trifluoromethoxy, fluoro, fluoro, sulfamoyl, N-methylsulfamoyl, hydroxymethyl, carboxyl, and cyano. The compounds of the present invention are useful in anticoagulant therapy to treat and prevent a variety of thrombotic symptoms, including coronary and cerebrovascular diseases. The compounds of the present invention can be used to inhibit serine proteases associated with the coagulation step response and factors JJ, collar, K, K, x, or along. The compounds of the present invention can inhibit the formation of platelet aggregates 'in mammals, in blood, in blood products, and in mammalian organs', inhibit fibrin formation, inhibit thrombus formation, and inhibit plug formation. These compounds can also be used to treat or prevent restless colic, angina colic, myocardial infarction, transient hemorrhagic invasion, anterior atrial fibrillation, thrombotic stroke, plug stroke, deep silence in mammals- ------------- ^ ---- Order --------- line (please read the back ^ / notes? Matters before filling out this page) Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Employee Consumption Cooperative -122- 1222445 Printed by the Employee Consumption Cooperative of the Intellectual Property Bureau of the Ministry of Economy A7 B7 V. Description of the invention (12) Thrombosis, disseminated intravascular coagulation, accumulation of fibrin in the eyes, and re-occlusion of blood vessels Or restenosis. These compounds are also useful in the prevention and treatment of patients at risk of developing the condition. These compounds are used to reduce the risk of atherosclerosis. Compounds of formula (I) can also be used to prevent cerebrovascular accidents (CVA) or stroke. In addition to their use in human therapy, these compounds can also be used in veterinary treatment of companion animals, exotic animals, and farm animals, including mammals, lentils, and the like. Better animals include horses, dogs, and cats. In yet another embodiment of the present invention, these novel compounds are selected from the compounds set forth in Examples 1 to 19 and Table 1. The use of generic terms in the description of compounds is defined here for clarity. Standard single-letter element symbols are used to indicate specific atom types, unless otherwise defined. The symbol "C" represents a carbon atom. The symbol "0" represents an oxygen atom. The symbol "Nπ" represents a nitrogen atom. The symbol "p" represents a phosphorus atom. The symbol &quot; s "represents a sulfur atom. The symbol &quot; H "represents a hydrogen-based atom. The double letter element symbol is used as defined for a periodic table element (meaning, C1 represents chlorine, Se represents magnetic, etc.). As used herein," alkyl "- Words, whether alone or within other terms, such as "fluorinated alkyl" and, "alkylthio", mean acyclic alkyl groups, containing from 1 to about 10, preferably from 3 to about 8 Carbon atoms, and more preferably 3 to about 6 carbon atoms. This alkyl group may optionally be replaced by a group as defined below. Examples of such groups include methyl, ethyl, chloroethyl, hydroxyethyl, n-propyl, oxypropyl, isopropyl, n-butyl, cyanobutyl, isobutyl __- 123- The size of this paper applies to China National Standard (CNS) A4 (210 x 297 mm) -------------- Order --------- line · (Please read first (Notes on the back then fill out this page) 1222445

, Bis-butyl, tertiary-butyl, pentyl, aminopentyl, isopentyl, hexyl, octyl, and the like. "Amidino" refers to an unsaturated acyclic hydrocarbon group because it contains at least one double bond. Such an alkenyl group contains about 2 to about 10 carbon atoms, preferably about 3 to about 8 carbon atoms, and more It is preferably 3 to about 6 carbon atoms. The alkenyl group may be optionally substituted by a group defined below. Examples of suitable alkenyl groups include propenyl, 2-chloropropenyl, small butene, isobutenyl, pentene Small base, 2-methylbutenyl, 3-methylbutene-1 · yl, hexene small, 3-hydroxyhexene small, heptene_1-yl, and octene-1 · yl, etc. • The term “block group” refers to an unsaturated acyclic hydrocarbon group, which contains one to more than one reference bond. Such a group contains about 2 to about 10 carbon atoms, preferably about 3 to about 8 Carbon atoms, and more preferably from 3 to about 6 carbon atoms. The alkynyl group may optionally be substituted by a group as defined below. Examples of suitable alkynyl groups include ethynyl, propynyl, hydroxypropynyl, butyl Alkyne 4-yl, butyn-2-yl, pentyne · I, pentyne_2_yl, 4-methoxypentyne · 2-yl, 3-methylbutyne small group, hexyne small group , Hexyl_2_yl, Hexyl-3 · yl, 3,3-Dimethyl The term alkynyl group -μ. Hydrogen group "denotes a single hydrogen atom ([eta]). This hydrogen group can be attached to, for example, an oxygen atom to form a "hydroxyl", one hydrogen group can be attached to a carbon atom to form a &quot; Mechuan π group -CH =, or two hydrogen groups can be attached to a carbon atom to form "Methylene" (; · (: Η2 ·). The term "π carbon" group means a carbon atom that does not have any covalent bonds and can form four covalent bonds. The term "π cyano" refers to a carbon group Three of the four covalent bonds are shared by the nitrogen atom. (Please read the notes on the back before filling out this page). ¾ Order --------- line! -124- 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 ___ V. Description of the Invention (122), the term "hydroxyalkyl" includes any one or more alkyl carbon atoms whose hydroxyl group is as defined above. Substituted groups. Specifically, the included groups are monohydroxy, dihydroxy, and polyhydroxyalkyl. The term "pitting acid group" includes one or more terminal carbon atoms of which Or more carbonyl-substituted groups as defined below. To be clear, what is included One group: fe group. Examples of monoalkyl groups include formate, ethenyl, and pentamyl. Examples of dicarbonylalkyl include oxalyl, propylenediyl, and succinyl. The term '' means a linear or branched group having 1 to about 10 carbon atoms' and having points of attachment for two or more covalent bonds. Examples of such groups are methylene, Ethylene, methylethynyl, and isopropylidene. The term "π-fluorenyl" means a linear or branched group having 2 to about 10 carbon atoms, at least one double bond, and having Connection points for one or more covalent bonds. Examples of such groups are 1,1-vinylidene (CH2 = C), -vinylidene (_CH = CH-), and 1,4-butadiene The term π halo •• means halogen, such as fluorine, chlorine, bromine or a broken atom. • The term “haloalkyl” includes any one or more of the alkyl carbon atoms being replaced by a sufficient meaning as above. The radical 圑. Specifically, it includes monohaloalkyl, dialkyl, and polyalkyl. An example of a monohaloalkyl may have a bromo, chloro or fluoro group in the group Radicals. Di- radicals may have two or more of the same halogen atoms, or a combination of different halogen radicals, and polyhaloalkyls may have more than two identical self-atoms or a combination of different halide radicals. A more preferred alkyl radical is &quot; Low-carbon commercial carbon &quot;, which has one to about six carbon atoms. Examples of such self-carbonic radicals include fluoromethyl, monofluoromethyl, difluoromethyl, gas methyl, dimethyl (please read first Note on the back, please fill out this page again), ¾ Order --------- line- -125- 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, the invention description (123), dichloromethyl, Trifluoroethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, monochlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl and dichloropropyl. The term "anthenyl_alkyl" includes groups in which any one or more of the alkyl carbon atoms are substituted as above &lt; hydroxyl. &Quot;. Examples of hydroxyhaloalkyl, including hexafluoropropyl. The term haloalkylene &apos; &apos; denotes an alkylene group in which any one or more carbon atoms of the alkylene group are substituted with a fluorenyl group as defined above. A di-alkylene group may have two or more identical halogen atoms, or a combination of different halogen groups, and a polyhalogenated alkyl group may have more than two identical halogen atoms or a combination of different halogen groups. A more preferred haloalkylene group is "lower haloalkylene" having from one to about six carbon atoms. Examples of "halohaloalkyl" include difluoromethylene, tetrafluoroethyl, tetrachloro Ethyl, alkyl-substituted monofluoromethylene and aryl-substituted trifluoromethylene. Π 卣 alkenyl Π — to represents a linear or branched group, having 1 to about 10 carbon atoms, and having one or more double bonds, in which any one or more alkenyl carbon atoms are as described above Yoshinoki substituted. A difluorenyl group may have two or more of the same halogen atom, or a combination of different fluorenyl groups, and a polyfluorenyl group may have more than two of the same atom or a combination of different self groups. The terms &quot; alkoxy &quot; and &quot; alkoxyalkyl &quot; refer to a linear or branched oxygen-containing group 圑 ', each having one to about ten carbon atoms, such as a methoxy group. M pit oxygen radical π-the term also includes a alkynyl radical having one or more alkoxy radicals attached to the alkyl ', meaning that a monoalkoxyalkyl group and a dialkoxyalkyl group are formed. A more preferred oxygen-burning group is a low-breaking feioxy &quot; &apos; having one to six broken atoms. Examples of such groups include methoxy, ethoxy, propoxy, butoxy, isopropoxy, and 126-th paper sizes Applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) -------- Order --------- line (please read the precautions on the back before filling this page) 1222445 Printed by the Consumers' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description ( 124) tri-butoxyalkyl. The alkoxy group may be further substituted with one or more self-atoms, such as fluoro, chloro or bromo, to provide an alkoxy group, and "haloalkoxyalkyl". This type of pinane Examples of oxy include fluoromethoxy, chloromethoxy, trifluoromethoxy, difluoromethoxy, trifluoroethoxy, fluoroethoxy, tetrafluoroethoxy, pentafluoroethoxy And fluoropropoxy. Examples of such alkoxyalkyl include fluoromethoxymethyl, chloromethoxyethyl, trifluoromethoxymethyl, difluoromethoxyethyl, and trifluoro Ethoxymethyl. The terms "enenoxy" and "enoxyalkyl" refer to linear or branched oxygen-containing groups, each having an alkenyl moiety of two to about ten carbon atoms, such as ethylene Oxy or propionyloxy. The term "fluorenylalkyl" also includes a methyl group, having one or more alkenyloxy groups attached to the alkyl group, meaning a monoalkenyloxyalkyl group and a dialkenyloxyalkyl group. More preferred alkenyl groups are "lower alkenyl groups" having two to six carbon atoms. Examples of such groups include ethenyloxy, propionyloxy, butyryloxy, and isopropenyloxyalkyl. "Alkenyloxy" may be further substituted with one or more _ atoms, such as fluoro, chloro or bromo, to provide &quot; fluorenyloxy &quot;. Examples of such groups include trifluoroacetoxy, fluoroethyleneoxy, difluoroethyleneoxy, and fluoropropenyloxy. "• Haloalkoxyalkyl" also includes an alkyl group having one or more self-alkylated oxy groups attached to the alkyl group, meaning a mono-alkoxyalkyl group and a di-alkoxyalkyl group. " The term "alkenyloxy" also includes an oxy group, having one or more dioxy groups attached to this oxy group, meaning a mono-alkenyloxy group and a di-fluorenyl group. The group d also includes an alkyl group having one or more alkenyloxy groups attached to the alkyl group, meaning that a monohaloalkenyloxy group and a dialkenyl alkenyl group are formed. The term represents an alkylene group with at least two oxygen bonds -127-This paper size applies to China National Standard (CNS) A4 (210 X 297) ------ ------- order- ------- Line · (Please read the phonetic on the back? Matters before filling out this page) 1222445 Printed by the Consumers' Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (125) As early as: fe-based. Examples of "sub-pit monooxy" include methylenedioxy, ethylenedioxy, alkyl-substituted methylenedioxy and aryl-substituted methylenedioxy. "Means _ Has at least two oxygen groups bonded to a single alkyl group. Examples of "haloalkanedioxy" include difluoromethylenedioxy, tetrafluoroethylenedioxy, tetrachloroethylenedioxy, Alkenyl-substituted monofluoromethylenedioxy and aryl-substituted monofluoromethylenedioxy. · The term 'aryl', used alone or in combination, means a carbocyclic aromatic system containing one, two or three rings, wherein such rings can be linked together in a pendant manner, or can be fused. A series means that a second ring exists (meaning connected or formed) by having two adjacent atoms in common with the first ring (meaning shared). The word fused &quot; is equivalent to The word "condensed". The term "aryl" contains aromatic groups such as phenyl, naphthyl, tetrahydrofluorenyl, ammonium and biphenyl. &quot; Fully aryl "includes aromatic groups such as phenyl, fluorenyl, tetrafluorenyl, indene, and biphenyl, where the aryl group is substituted with 3 or more fluorenyl groups, as follows The term "heterocyclyl" includes saturated and partially saturated cyclic groups containing heteroatoms, having 4 to 15 ring members, referred to herein as "C4-Cl5 heterocyclyl," and is selected from Carbon, nitrogen, sulfur, and oxygen, at least one of which is a heteroatom. A heterocyclyl may contain one, two, or three rings, and such rings may be connected in a pendant manner: or may be fused. A saturated heterocyclic group Examples of groups include saturated 3 to 6-membered heteromonocyclic groups containing 丨 to 4 nitrogen atoms [for example, tetrahydropyrrolyl, imidodolide, hexahydro-4, hexahydro ^, etc.]; Saturated 3 to 1 heterocyclic monocyclic group, containing 1 to 2 oxygen atoms, and 1 to 3 nitrogen atoms τ 夂 夂 [for example? 128 This paper size applies the Zhongguanjia standard (⑽) A4 specification ( 21〇x 297 public shame "--------------------- Order --------- line · (Please read the precautions on the back before filling in (This page) 1222445 A7

1 Read the notes on the back and fill out this page

I *

1222445 A7 B7 V. Description of the invention (127, 1,3,4-fluoradiazolyl, 1A5_fluoradiazolyl, etc.); etc .; unsaturated condensed heterocyclic group containing 1 to 2 oxygen atoms, and Nitrogen atoms [e.g. benzopyrazolyl, benzoxadiazole, etc.]; unsaturated 5 to 6-membered heterocyclic monocyclic groups, containing 1 to 2 sulfur atoms, and 1 to 3 nitrogen atoms, such as Oxazolyl, oxadiazolyl [such as 1,2,4 · oxadiazolyl, 1,3 + pyrimadiazolyl, u, 5-pyrimadiazolyl, etc.], etc .; unsaturated condensed heterocyclic groups , Containing 1 to 2 sulfur atoms, and 1 to 3 nitrogen atoms [such as benzopyrazolyl, benzodiadizolyl, etc.], etc. This term also includes those in which heterocyclic groups are fused with aryl groups Examples of such fused bicyclic groups include benzofuran, benzopyrimine, etc. The hetero% group may have 1 to 3 substituents, as defined below. Preferred hetero Cyclic group groups include five to twelve member fused or unfused groups. Non-limiting examples of heteroaryl groups include pyrrolyl, pyridyl, pyridyloxy, ejunyl, dijunyl, Shout Yodoki, Tahuki, Saki Junki, p Saijunki, Mi Base, &lt; P-woodyl, phenylthio, sulfanyl, tetrabenzyl, 2.metulinyl, miridianyl, 2-dihydropyrazolyl, tetrahydropyrazolyl, isoxazolyl , Isoxazolyl, 1,2,3-oxadiazolyl, U3-triazolyl, 1,3,4-pyrimadiazolyl, pyrargyl, hexahydroetomyl, 1,3,5 · San Gengji, i, 3,5-trisulfuryl, phenylhydrazone (b) phenylsulfanyl, benzamidine, p-quelinyl, Sijunji, etc. Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs The term "continuous acid group", whether used alone or connected to other terms, such as alkylsulfonyl, individually represents the divalent group _S02_. "Alkylsulfonyl" includes an alkyl linkage To sulfonyl, wherein alkyl is as defined above. "Alkylsulfonylalkyl" includes an alkylsulfonyl group attached to an alkyl, wherein alkyl is as defined above. &Quot; alkylsulfonyl ", Including the connection from an alkyl group to a sulfofluorenyl group, in which the _alkyl group is as defined above." Amidinosulfonylalkyl ", including -130 This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445

Description of the invention (128 Printed by the Consumers' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, i-sulfanyl containing sulfonyl group is connected to the alkyl group, wherein the alkyl group is as defined above. &Quot; The term "sulfenyl", whether used alone or in conjunction with other terms, such as alkylidene, refers to the divalent group j (〇) _. &Quot; "Amidylene group" includes an alkyl group attached to a sulfinylene group, wherein the alkyl group is as defined above. "Alkylene sulfinylene group" includes an alkyl sulfinylene group attached to an alkyl group where The alkynyl group is as defined above. `` Self-alkynylidene, which contains a alkynyl group attached to a perylene group, where the haloalkylene group is as defined above. " Containing an alkyl sulfinyl group attached to an alkyl group, wherein the alkyl group is as defined above. The term πaralkyl &quot; includes an aryl-substituted alkyl group. A preferred aralkyl group is a "lower aralkyl group" ", Having an aryl group attached to an alkyl group having one to six carbon atoms. Examples of such groups include benzyl, dibenzoyl , Trityl, phenylethyl, and -pentylethyl. The terms fluorenyl and benzyl are interchangeable. &Quot; Heteroaryl group &quot; includes a heteroaryl substituted aryl group, of which heteroaryl The alkynyl group may be further substituted with three or more substituents as defined above for aralkyl. "The term" all-aryl alkynyl "includes aryl substituted alkynyl groups, where Or more aryl radicals as defined above. "Aralkylsulfinamilide π-The term includes an aralkyl group attached to a sulfinamilide group, wherein the aralkyl group is as defined above." Aralkylsulfinyl group "Amidinoalkyl" includes an aralkylsulfinylene group connected to an alkyl group, wherein the alkyl group is as defined above. The term "πaralkylsulfonyl group" includes an aralkyl group connected to a sulfonyl group in which the aralkyl group is It is as defined above. "Aralkylsulfonylalkyl" includes an aralkylsulfonyl group attached to an alkyl group, where the alkyl group is as defined above. -131-This paper size applies to Chinese National Standards (CNS) A4 specification (210 X 297 mm) ---------------- r ---- order --------- line (please read the precautions on the back first) (Fill in this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ________ B7 V. Description of the Invention (129) The term "pi ring pit group" includes a group with three to 15 carbon atoms. A better ring group is a low carbon soil. &Quot; has three to seven carbon atoms. Examples include groups such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl. The term cycloalkyl includes seven to five carbons An atom and a group having two to four rings. Examples include groups such as n-singyl (meaning bicyclofluorene [2.2.1] heptyl) and gold-steel alkyl. "Cycloalkylalkyl"- The word includes a cycloalkyl substituted alkyl group. A preferred cycloalkylalkyl group is "lower cycloalkylalkyl," having a cycloalkyl group attached to an alkyl group having one to six carbon atoms. Examples of such groups include cyclohexylhexyl. The term "cycloalkenyl" includes groups having three to ten carbon atoms and one or more carbon-carbon double bonds. Preferred cycloalkenyl is, "lower cycloalkenyl", having three to seven carbon atoms. Examples include groups such as cyclobutenyl, cyclopentyl, cyclohexyl, and cycloheptyl. " The term "cycloalkenyl" includes groups in which any one or more of the cycloalkyl carbon atoms is replaced by a radical as defined above. Specifically, the inclusions are monocycloalkyl, dicycloalkyl And polyhalocycloalkyl. An example of a mono-cycloalkyl group may have a bromo, chloro or fluoro group atom in the group. A diradical may have two or more of the same halogen atom or different halogen groups Combination, and the polyfluorinated cycloalkyl group may have more than two groups of the same atom or different self-groups. A more preferred self-cycloalkyl group is a "low-carbon self-cycloalkyl group" with three to about eight complete atoms. This Examples of such halocycloalkyl include fluorocyclopropyl, difluorocyclobutyl, trifluorocyclopentyl, tetrafluorocyclohexyl, and dichlorocyclopropyl. The term `` halocycloalkenyl '' includes any one or A group in which a plurality of cycloalkenyl carbon atoms is substituted with a halo group as defined above. Specifically, those included are mono-alkenyl, di-cycloalkenyl, and poly-cycloalkenyl. • The term 'cycloalkoxy group' includes a cycloalkyl group attached to an oxy group. The actual type of this group -132- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) I --- -^ ---- Order --------- line (please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 _____ B7 V. Description of the invention ( 13〇) Examples include cyclohexyloxy and cyclopentyloxy. The term "cycloalkoxyalkyl" also includes alkyl groups having one or more cycloalkoxy groups attached to the alkyl group, meaning a monocyclic ring Alkoxyalkyl and bicycloalkoxyalkyl. Examples of such groups include cyclohexyloxyethyl. `` Cycloalkoxy &quot; may be further substituted with one or more atoms, such as fluoro , Chloro or bromo to provide a π-functional cycloalkoxy &quot; and "halocycloalkoxyalkyl". The term "cycloalkylalkoxy" includes a cycloalkyl group attached to an alkoxy group. Examples of groups include cyclohexylmethoxy and cyclopentylmethoxy. The term `` cycloalkenyloxy '' includes a cycloalkenyl group attached to an oxy group. Examples of such groups include cyclohexyloxy and cyclopentenyloxy. The term "cycloalkenyloxyalkyl" also includes a aryl group having one or more oxalyloxy groups attached to the alkyl group, meaning a monocyclic alkenyloxyalkyl group and a bicycloalkenyloxy group. alkyl. Examples of such groups include cyclohexenyloxyethyl. "Cycloalkenyloxy" may be further substituted with one or more self-atoms, such as fluoro, chloro, or bromo, to provide &quot; cycloalkenyloxy &quot; and &quot; cycloalkenyloxyalkane "The term" subcyclic alkynyldioxy "means that the subazetidinyl group has at least two oxygens bound to a single primary cycloalkyl group." Examples of oxanedioxyπ include 1,2-di Oxycyclohexyl. The term &quot; cycloalkylene &quot; includes a cycloalkylene group attached to an oxyalkylene group, wherein cycloalkyl is as defined above. "Cycloalkylsulfinylalkyl" includes a cycloalkylsulfinamido group attached to an alkyl group, wherein alkyl is as defined above. The term "cycloalkylsulfonyl group" includes a cycloalkyl group attached to Continued fluorenyl, wherein the cycloalkyl group is as defined above. "Cycloalkylsulfonylalkyl'f contains a cycloalkylsulfonyl group attached to an alkyl group, where alkyl is as defined above. &Quot; Cycloalkylalkylsulfonyl" Word Package -133- Applicable to this paper standard China National Standard (CNS) A4 specification (210 x 297 mm) ---------------- K ---- Order --------- line (please first Read the phonetic on the back? Matters should be filled out on this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ______B7 V. Description of the invention (131) Containing one or more of the pit-based carbon atoms is defined by one or more of the following Talk about radical substitution. Specifically, those included are monocarbonylcycloalkyl and dicarbonylcycloalkyl. Examples of the monocarbonylcycloalkyl group include a cyclohexylcarbonyl group, a cyclohexylethylfluorenyl group, and a cyclopentylfluorenyl group. Examples of the tertiary cycloalkyl group include 1,2-dicarbonylcyclohexane. The term "pi-alkylthio" includes groups which are linear or branched alkyl groups containing one to ten carbon atoms and are connected to a divalent sulfur atom. A more preferred alkylthio group is &quot; low carbon thio group f ', having one to six carbon atoms. "Low-carbon thiol, 'An example is methylthio (CH3 -S-)." Pythio "may be further substituted with one or more atoms, such as fluoro, chloro or bromo, to provide "From the appearance of sulfur." Examples of such groups include fluoromethylthio, airmethylthio, trifluoromethylthio, difluoromethylthio, digasethanethio, gasethanethio, tetragasethanethio, pentagasethanethio And fluoropropylthio. The term "alkynylarylamino" includes a linear or branched alkyl group containing one to ten carbon atoms, and an aryl group attached to the amine group. Examples include N-methyl-4-methoxyaniline, N · ethyl-4-methoxyaniline and N-methyl-4-trifluoromethoxyaniline. The term alkylamino means "monoalkylamino" and "dialkylamino" and contains one or two alkyl groups, each of which is attached to an amine group. The term arylamino group means "monoarylamine" and "di "Arylamino", containing one or two aryl groups, each attached to an amine group. Examples of such groups include N-phenylamino and N-fluorenylamino. &Quot; aralkylaminoπ-the word contains The aralkyl group is connected to an amine group, wherein the aralkyl group is as defined above. The term aralkyl group means &quot; monoaryl amine group &quot; and πdiaryl group -134- This paper size applies to Chinese national standards (CNS ) A4 size (210 X 297 mm) ----------------- ^ ---- Order --------- line (Please read the note on the back first咅? Please fill in this page for matters)

1222445 V. Description of the invention (132) Amino group, which contains one or two aralkyl groups, is individually connected to the amine group. The term aralkylamino further refers to "a monoaralkylmonoalkylamino group, which contains an aralkyl group and a pit group, attached to the amine group. The term πarylarylenesulfenyl" includes a group of Contains an aryl group as defined above, which is attached to a divalent s (0) atom. &quot; Arylsulfinylalkyl "means an arylsulfinyl group, connected to a linear or branched alkyl group having one to ten carbon atoms. The term" arylsulfonyl "includes An aryl group is attached to a sulfofluorenyl group, wherein the aryl group is as defined above. &Quot; Arylsulfofluorenylalkyl &quot; includes an arylsulfonyl group connected to an alkyl group, wherein the alkyl group is as defined above. &quot; Heteroarylsulfinyl "includes a heteroaryl group, as defined above, attached to a divalent s (0) atom, a heterowanyl azinopyridyl resist group, which together denote a heteroaryl group Amidylene is a linear or branched alkyl group having one to ten carbon atoms. The term "heteroaryl" refers to a heteroaryl group attached to a fluorenyl group, where heteroaryl is as defined above. "Heteroarylsulfonylalkyl, which includes a heteroarylsulfonyl group attached to an alkyl group, wherein alkyl is as defined above. The term" aryloxy "includes an aryl group, as defined above, attached to oxygen atom. Examples of such groups include phenoxy, 4-chloro_3_ethylphenoxy, 4-chloro; methylphenoxy, 3-chloroethoxyphenoxy, 3,4_ Dichlorophenoxy, methylphenoxy, 3-trifluoromethoxyphenoxy, 3-trifluoromethylphenoxy, 4-fluorophenoxy, 3,4-dimethylphenoxy Methyl, 5-bromo-2-fluorophenoxy, 4-bromo-3-fluorophenoxy, 4-fluoro-3-methylphenoxy, 5,6,7,8_tetra Hydroxyloxy, 3-isopropylphenoxy, &gt; cyclopropylphenoxy, 1ethylphenoxy, 3-pentafluoroethylphenoxy, tetrafluoroethoxy) _benzene Oxygen and the standard of this paper are applicable to the Zhongguanjia Standard (CNS) A4 specification (21 () χ Norwegian public love) I --------------- Κ ---- Order --- ------ Line · (Please read the note on the back? Matters before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 122445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention ( 133) 4-Third-butylphenoxy. • The term “aryl acid group” includes an aryl group, as defined above, attached to a carbonyl group, as defined above. Examples of such groups include benzamyl and tolylmethyl. The word includes an aralkyl group, as defined herein, attached to a carbonyl group, as defined above. Examples of such groups include, for example, phenethylfluorenyl. The term "* aryl tigeroxy" includes oxygen-containing aralkyl groups, which are passed through oxygen Atoms are connected to other groups. More preferred aralkoxy is "lower aralkoxy" having a phenyl group attached to a lower alkoxy group as described above. Examples of such groups include fluorenyloxy, L-benzylethoxy, 3-difluoromethoxymethyloxy, 3 · trifluoromethylmethyloxy, 3,5-diazomethyloxy, 3-Bromoethoxy, 4-propylethoxy, 2-fluoro-3-trifluoromethylbenzyloxy and 2-phenylethoxy. The term "πaryloxy tigeryl" includes an aryloxy group, as defined above, attached to an alkyl group. Examples of such groups include phenoxymethyl. The term "haloaryloxyalkyl" includes as above An aryloxyalkyl group is defined in which one to five yl groups are attached to the aryloxy group. The term "πheteroaryl" includes a heteroaryl group, as defined above, attached to a carboxyl group, as defined above. Examples of such groups include succinylmethyl and thiol. "Heteroaryl" The term; includes a heteroaryl group as defined herein, attached to a carbonyl group as defined above. Examples of such groups include, for example, pyridylacetate and succinylbutanyl. The term "πheteroaralkoxy" includes oxygen-containing heteroaralkyl groups attached to other groups via an oxygen atom. A more preferred heteroaralkoxy group is "lower carbon heteroaralkoxy" with heteroaryl linkage To the low-carbon alkyloxy group as described above. The term "haloheteroaryloxyalkyl" includes heteroaryloxy as defined above. _ -136- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --- --------- K ---- Order -------- · Line (Please read the precautions on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ____B7 V. Description of the invention (134) Alkyl, in which one to four fluorenyl groups are connected to a heteroaryloxy group. The term "heteroarylamino" includes a heterocyclic group, as defined above, attached to an amine group. This Examples of such groups include pyridylamino. The term "heteroarylaminoalkyl" includes a heteroarylamino group, as defined above, attached to a fluorenyl group. Examples of such groups include pyridylmethylamino The term "πheteroaryloxy" includes a heterocyclyl group, as defined above, attached to an oxy group. Examples of such groups include 2-phenylthiooxy, 2-pyrimidinyloxy, 2-pyridyloxy, 3-pyridyloxy, and 4-pyridyloxy. The term "heteroaryloxyalkyl" includes a heteroaryloxy group, as defined above, attached to an alkyl group. Examples of such groups include 2 · ρ specific methyl, 3-π specific pyridine Oxyethyl and 4-pyridyloxymethyl. The term "arylthio" includes an aryl group, as defined above, attached to a sulfur atom. Examples of such groups include phenylthio. The term &quot; arylthioalkyl &quot; includes an arylthio group, as defined above, attached to a fluorenyl group. Examples of such groups include phenylthiomethyl. The term "thiothioalkyl" includes a thiothio group, as defined above, attached to a thio group. Examples of such groups include methylthiomethyl. The term "alkoxyalkyl," which includes an alkoxy group, as defined above, is attached to an alkyl group. Examples of such groups include methoxymethyl. The term "carboxy" means a carbon having four covalent bonds Group, two of which are in common with the oxygen atom. The term "π carboxyl" includes several groups as defined above, attached to one of the two unshared bonds in the fluorenyl group. &quot; Carboxamide "includes amine, monoalkylamino, dialkylamino, monocycloalkylamino, alkylcycloalkylamino, and bicycloalkylamino groups attached to two unshared bonds in the carbonyl group ___ -137- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------------------ ^ ---- Order -------- line (Please read the note on the back? Matters before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 --------- B7 V. Invention Note (135) The term "carboxylic acid aminoalkyl" includes a carboxyamido group as defined above, attached to a fe group. The term "carboxyl group" includes a carboxyl group as defined above, attached to a tiger group. "Alkane Oxycarbonyl π-The word includes an alkoxy group, as defined above, attached to one of two unshared bonds in the carboxyl group. The term &quot; aralkoxycarbonyl &quot; includes an aralkoxy group, as defined above, attached to one of two unshared bonds in the carboxyl group. The term "mono-oxyl carboxyfe group" includes an oxyalkyl group, as defined above, attached to the group. The "oxyalkyl" group includes two alkoxycarbonyl groups, as defined above, attached to an alkylene group. "The term" monocyanoalkyl "contains one cyano group, as defined above, attached to the alkyl group." The term dicyanoalkylene, "includes two cyano groups, as defined above, attached to the alkyl group." The term "alkoxycarbonylcyanoalkyl" includes a cyano group, as defined above, attached to an alkoxycarbonylalkyl group. The term "fluorenyl", alone or in combination, means carbonyl or thiocarbonyl, bound to A group selected from, for example, hydrogen, alkyl, fluorenyl, block, halo, alkoxy, alkoxy, alkoxy, aryl, heterocyclyl, heteroaryl, alkyl Sulfenylalkyl, alkylsulfoalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylthio, arylthio, amine, alkylamino, dioxane Amino, aralkyloxy and alkylthioalkyl. Examples of "fluorenyl" are methylamidino, ethylamido, benzamido, trifluoroethylamido, phthalofluorenyl, malonyl, and Test group, etc. The term "1¾ alkyl" includes one or more self-defined radicals as defined herein, attached to an alkyl radical as defined above. Examples of such radicals include, for example, chloroethyl The term "fluorenyl, trifluoroethylfluorenyl, bromopropylfluorenyl, and heptafluorobutylfluorenyl. F. Phosphonate" includes pentavalent phosphorus linked to oxygen by two covalent bonds. π -138- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ---------------- l · --- Order ----- ---- Line · (Please read the note on the back? Matters before filling out this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 _ B7 _ V. Description of the invention (136) Dioxalyl phosphonate The term means that two oxooxy groups as defined above are attached to the phosphonate group by two covalent bonds. The term "diarylalkoxyphosphono group" means two aryloxy groups as defined above to Two covalent bonds are attached to the tenthyl group. The term "• dialkoxyphosphonoalkyl" means a dialkoxyphosphonic acid group, as defined above, attached to the alkyl group. The term "diarylalkoxyphosphonoalkyl" refers to a diarylalkoxyphosphonic acid group, as defined above, attached to an alkyl group. The term "amino" means that the nitrogen atom contains two substituents, such as hydrogen, hydroxy, or alkyl, and has a covalent bond that can be used to bond to a single atom, such as broken. Examples of such amine groups include, for example, -NH2, -NΗΟΗ, and -NHOCH3. The term "imino" means that the nitrogen atom contains a substituent, such as hydrogen, hydroxy, or alkyl, and has two covalent bonds that can be used to bond to a single atom, such as carbon. Examples of such imino groups include, for example, = NCH3, = NOH, and = NOCH3. The term "iminocarbonyl" refers to a carbon group having four covalent bond positions, two of which are common to the imino group. Examples of such iminocarbonyl groups include, for example, C = NH, C = NCH3, C = NOH and C = NOCH3. The term "formamidine" includes substituted or unsubstituted amine groups, and one of the two bonded to the iminocarbonyl group may be used. Examples of such formamyl include, for example, nh2-c = nh, nh2-c = nch3, nh2_c = noch3, and ch3nh-c = noh. The term "guanidino" means that the methylformyl group is bound to an amine group as defined above, wherein the amine group can be bonded to a third group. Examples of such guanidino groups include, for example, NH2-C (NH) -NH- &gt; NH2_C (NCH3) _NH-, NH2_C (NOCH3) -NH- and CH3NH-C (NOH) -NH-. &quot; The term `` 锍 '' means a trivalent sulfur atom with a positive charge, in which the sulfur system is Carbon-based group substitution, such as alkyl, fluorenyl, aralkyl, or aryl. "Dioxane-139- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----- ----------- K ---- Order --------- line (Please read the precautions on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 _________ B7 V. Description of the invention (137) The term "basal rice" means a radical, in which the sulfur system is replaced by two alkyl radicals. Examples of such dialkylfluorene groups include, for example, (ch3) 2s +-. & Quot The term "dialkylfluorenyl" refers to a dialkylfluorenyl group in which the group is bonded to a bond of a secondary alkyl group as defined above. Examples of such dialkylfluorenyl groups include (ch3) 2s + -ch2ch2- 0 '· scale "means a tetravalent fluorene atom having a positive charge, in which the phosphorus system is substituted with a four-carbon group, such as an alkyl group , Fluorenyl, aralkyl, or aryl. The term "trialkylphosphonium" means a rust group in which the phosphorus system is substituted with three alkyl groups. Examples of such trialkylfluorenyl groups include, for example, (CH3) 3P +- "Alkyl", "alkynyl", "alkynyl", "alkylene", "alkylene", π-hydroxyalkyl "," _alkyl "as defined above "," Haloalkylene ", 丨 丨 Haloalkenyl 丨 丨, 丨 丨 alkoxy '丨 ,, 丨 alkenoxy &quot;, 丨 丨 alkoxyalkyl &quot;, and 丨 alkoxyalkyl &quot;, "Aryl", "All_aryl", "From alkoxy", "From alkoxyalkyl", "Phenenyloxy", "From alkenyloxy" &quot;, "Hydrylenedioxy", "Haloalkylenedioxy", "Heterocyclyl", "Heteroaryl", "Hydroxyalkylene", &quot; Alkylsulfonyl ", π from alkylsulfonyl ", &quot; alkylsulfonyl "," Haloalkylsulfonylalkylπ, "alkylsulfinylsulfonylπ", "alkylsulfinylsulfinylalkyl" &quot; fluorinylsulfinylalkyl "aralkyl", π heteroaralkyl perhaloaralkyl &quot;, "aralkylsulfonyl", "aralkylsulfonyl", "aralkylsulfinyl", "aralkylsulfinyl" "Cycloalkyl", "Cycloalkylalkyl", "Cycloalkylalkyl", "Cycloalkenyl" "Cycloalkylalkyl", "Halocycloalkenyl", "Cycloalkyl" Alkylsulfinyl "," Cycloalkylsulfinylalkyl "," Cycloalkylsulfinyl "," Cycloalkylsulfinylalkyl "," Cycloalkoxy "· , •• cycloalkoxyalkyl ”,“ cycloalkylalkoxyπ, ”“ cycloalkenyloxy ”,“ cyclo-140- ”This paper size applies to China National Standard (CNS) A4 (210 X 297 Mm) ------------------: ---- Order --------- line (Please read the precautions on the back before filling this page) 1222445 Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (138) Alkenyloxyalkyl", "Nycloalkane Dioxy "," from cycloalkoxy π, π halocycloalkoxyalkyl "," cyclocycloalkenyloxy &quot;, "cyclocycloalkenyloxyalkyl", "alkylthio" , "I alkylthio", "alkylsulfinyl π," amino "," oxy "," thio "," alkylamino ", &quot; arylamino", &quot; aryl Alkylamino π, &quot; arylsulfinamilide &quot;, &quot; arylsulfinamilide alkyl &quot;, &quot; arylsulfonamilide &quot; Sulfonyl π, "heteroarylsulfinylalkyl", "heteroarylsulfonyl", "heteroarylsulfonyl" &quot;, "heteroarylamino", "heteroaryl" Aminoalkyl ", &quot; heteroaryloxy &quot;, &quot; heteroaryloxyalkyl &quot;, πaryloxy &quot;," arylamido "," aralkylamido "," aralkoxy " "", "Aryloxyalkyl", "_aryloxyalkyl", 11 heteroarylfluorenyl ππheteroaralkylfluorenyl "," heteroaralkyloxy "," heteroaralkoxyalkyl " "", "Arylthio", "arylthioalkyl", "alkoxyalkyl", "fluorenyl", "formamyl" , "Guanidino", "dialkylfluorene", "trialkylrust" and "dialkylphosphonium", optionally with one or more non-hydrogen substituents, such as formamyl , Guanidino, dialkylfluorenyl, trialkylfluorenyl, dialkylfluorenyl, all-aralkyl, aralkylfluorenyl, arylsulfanylfluorenyl, sulfanylfluorenyl , Arylene sulfenylalkyl, i-cycloalkyl, _cycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfinyl, cycloalkylsulfonyl Fluorenylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, heteroaryloxy, heteroaryloxyalkyl, autoalkylthio Alkyl, alkoxy, alkoxy, alkoxyalkyl, i-alkoxyalkyl, heteroarylalkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkane Oxy, cycloalkenyloxy tigeryl, hypocycloalkyldioxy, self-cycloalkoxy, self-cycloalkoxyalkyl, halocyclofluorenyloxy, self-cycloalkenyloxyalkyl, hydroxyl , Amine, Sulfur, ------- 141-This paper size applies to China National Standard (CNS) A4 210 X 297 mm) ---------------- l · --- --------- Order Line (Read the back of the phonetic? Please fill in this page again for details) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (139) Nitro, low-carbon amine, thiosulfate, thiosulfate, arylamine, aromatic Amino, arylthio, arylthioalkyl, heteroaryloxyalkyl, alkynylsulfenyl, alkynylene, alkylene, arylphenylene, alkylene Alkylidene, heteroarylallylidene, alkylene, heteroarylallylidene, alkylene, alkynyl, phenylene, etc. Sulfofluorenylalkyl, alkylsulfonamido, alkylaminocontinyl, fluorenylaminocontinyl, monoalkylsulfonylfluorenyl, diamylsulfonylfluorinyl, monoaryl Sulfonyl sulfonyl, arylsulfonyl sulfonyl, diarylsulfonyl sulfonyl, succinyl sulfonyl, succinyl sulfonyl , Heteroarylthio, Heteroarylidene, Heteroarylidene, Heteroaryl, Sodium, Aromatic, Heteroaryl, Heteroaryl, Heteroaryl, Halogen Oxalyl, alkynyl, fluorenyl, block, fluorenyl, Alkoxyalkyl, secondary dioxy, self-alkylenedioxy, cycloalkyl, cycloalkylalkylfluorenyl, cycloalkenyl, low-carbon cyclopentyl-resistive group, low-carbon cyclofluorenylalkyl, Free radical, free radical, halomethyl, aryloxy, mesial self-grafted, triaryl, alkynyl, aminoalkyl, hydroxy heteroaralkyl, alkoxyalkyl, Aryl, aralkyl, aryloxy, aralkyloxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, Aryloxetyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carbonylalkoxy, alkoxycarbonyl, aralkyloxycarbonyl, carboxyamido, carboxyamidoalkyl, cyano Base, halo postprandial base, tentonate, tentonate, diaryl alkoxylate and diaralkoxyphosphonate alkyl. • The term 'spacer' can include a covalent bond and a linear portion of the backbone with 1 to 7 adjacent atoms. This spacer can have a single from 1 to 7 atoms ___ -142- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------------- --- ^ ---- Order --------- line (please read the notes on the back before filling out this page) Printed by the Consumer Consumption Cooperative of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 ____________ B7 V. Description of Invention (14) A valence or multivalent chain. The monovalent chain can be selected from = C (H)-, = C (R2a), -〇-, each, -S (0) 2-? -NH-? -N (R2a)-? -N =?- CH (OH)-? = C (OH)-? -CH (OR2a)-, = C (OR2a) _ and -C (0) ·, wherein R2a is selected from the group consisting of alkyl, fluorenyl, Alkynyl, aryl, heteroaryl, aralkyl, aryloxyalkyl, alkoxyalkyl, sulfanyl fe, arylthio, alkynyl, cycloalkyl, cyclopentyl , Self-fluorenyl, fluorenyloxyalkyl, all-arylalkyl, heteroarylalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, and heteroarylalkenyl. The multivalent chain may include a straight chain of 1 or 2 or 3 or 4 or 5 or 6 or 7 atoms or a straight chain of 1 or 2 or 3 or 4 or 5 or 6 atoms and a side chain. This chain may be composed of one or more groups selected from the group consisting of: lower alkylene, lower alkylene, -0-, -0-CH2-, each 012-, &lt; 112012_, vinyl, -(: 11 = €: 11 (011)-,-0 € 1120, -0 ((: 112) 20 ·, · NHCH2 _, _ OCH (R2 a) 0, -0 (CH2 CHR2 a) 0-, · ΟΟΤ2 0_, -〇 (CF2) 2 0_, -S-, S (0), -S (0) 2-, -N (H)-, · N (Η) 0 ·, -N (R2a) 0 · , -N (R2a)-, -C (0) ·, -C (0) NH-, -C (0) NR2a-9 -N = -OCH2-? -SCH2-? S (0) CH2-,- CH2C (0)-? -CH (OH &gt;? = C (OH)-, -CH (OR2a) ·, = C (OR2a) ·, S (0) 2CH2- and _NR2aCH2-, as defined above or Many other groups generally known or determined by those skilled in the art. The side chain may contain substituents, such as 1 or more non-hydrogen substituents, such as formamyl, guanidyl, dialkyl mirror, trialkyl Scale, dialkyl sulfoalkyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, Cycloalkyl, cycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, hetero Arylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, heteroaryloxy, heteroaryloxyalkyl, haloalkylthio, alkylalkoxy , Alkoxy, alkoxyalkyl, i-alkoxyalkyl, hetero ____- 143 -__ The paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) &quot; &quot; --- -------------- r ---- Order --------- line (Please read the note on the back? Matters before filling out this page) 1222445 Intellectual Property of the Ministry of Economic Affairs Printed by the Consumer Cooperative of the Bureau A7 B7 V. Description of the invention (141) Aromatic oxygen, cycloalkyloxy, cycloalkyloxy, cycloalkyloxy, cycloalkyloxy, cycloalkyloxyalkyl Base, cycloalkyldioxy, autocycloalkoxy, halocycloalkyl, halocycloalkyloxy, autocycloalkyloxy, phenyl, amino, thio, nitrate Base, low-carbon alkylamino, alkylthio, alkylthio, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroarylalkyl, sulfhydryl Fermenting base, pit base, base substrate, square sulfinyl sulfenylalkyl, arylsulfonyl alkyl, heteroarylsulfinyl sulfenyl Alkyl, heteroaryl, fluorenyl, alkyl, fluorenyl, sulfonyl, sulfonyl, sulfinyl, sulfinyl, alkyl, sulfonyl, alkyl , Alkylamine continuous base, Alkaline continuous base, Mono; Fe-based aminoamine continuous base, Dipitylsulfonylsulfonyl, Monoarylsulfonylsulfonyl, Arylsulfonyl Amine, diarylsulfonylsulfonyl, monoalkylmonoarylsulfonylsulfonyl, arylsulfinyl, arylsulfinyl, heteroarylthio, heteroarylsulfinyl Base, heteroaryl base, resistant base, fermenting base, aromatic base, heteroaryl base, aromatic acid base, heteroaralkylamido, haloalkyl, alkyl, alkenyl, alkynyl , Alkenyloxy, alkenyloxyalkyl, alkanedioxy, alkanedioxy, cycloalkyl, cycloalkenyl, lower carbocycloalkylalkyl, lower carbocycloalkenylalkyl, selfgroup , Alkyl, haloalkenyl, i-alkoxy, hydroxy-alkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl, hydroxyheteroalkyl, i-alkoxyalkyl, aryl, aromatic Alkyl, aryllactyl, arylfeoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated Cyclic, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylfluorenyl, carboxyalkyl, oxocarbonyl, Aralkyloxycarbonyl, carboxyamido, carboxyamidoalkyl, cyano, haloalkoxycarbonyl, phosphonic, phosphonoalkyl, diarylalkoxyphosphonic ------ 144- The scales of Zhang and Zhang are applicable to China National Standard (CNS) A4 (210 X 297 mm) II ---------- MW ---- l · --- order ------ --- line · (Please read the notes on the back before filling this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 '------------------_____ 5. Description of the invention (142) ^-and a diarylalkoxyphosphonoalkyl group. The compounds of the present invention may exist in tautomeric, geometric or stereoisomeric forms. The present invention intends to cover all the compounds included in the scope of the present invention, including cis · and trans_ geometric isomers, E- and 厶 geometry Isomers, S-palladium isomers, diastereomers, d isomers, isomers, racemic mixtures and other mixtures thereof. Such pharmaceutically acceptable salts of tautomeric, isomeric or stereoisomeric forms are also encompassed by the present invention. "Cis," and "trans" terms refer to geometrically isomeric forms in which two carbon atoms connected by a double bond each have a hydrogen atom on the same side of the double bond (&quot; cis &quot;) or On the opposite side of the double bond (&quot; trans "). Some of the compounds described contain alkenyl groups and are meant to include both cis and trans, or, Έ &quot; and, Z &apos;, geometric forms. Some of the compounds described contain one or more stereocenters and are meant to include each of the stereocenters in the form of R, S and a mixture of R and S forms. Some of the compounds described herein may contain one or more keto or aldehyde peptidyl groups or combinations thereof 'alone or as part of a heterocyclic system. Such fluorenyl groups may exist partially or mainly in the form of "keto", and partially or mainly in the form of one or more "enols" of each acid and keto group present. The compounds of the present invention are meant to include "keto", tautomeric forms with "enol". Some of the compounds described herein may contain one or more amidocarbonyl groups or combinations thereof 'alone or as part of a heterocyclic system. Such fluorenyl groups may exist partially or predominantly in the form of &apos; keto &apos; and partially or predominantly in the form of one or more enols of each fluorenylamino group present. The invention with amido carbonyl group _ -145- This paper size is applicable to China National Standard (CNS) A4 (21G X 297 mm)-&quot; ^ --------------- -K ---- Order --------- Line 4! ^ · (Please read the notes on the back before filling this page)

1222445 V. Description of the invention (143) Compounds are meant to include, &apos; keto &quot; and, enol &quot; tautomeric forms. The amino carbonyls can be keto (c = 0) and thiocarbonyl (c = s) based on type. Some of the compounds described herein may contain one or more imine or enamine groups, or a combination thereof. Such groups may exist partially or predominantly in the form of &quot; imines &quot;, and may exist in the form of one or more of the &quot; enamines &quot; in each of the existing groups. The compounds of the present invention are meant to include, tautomeric forms of imine π and "enamine". The present invention also includes treatment and prevention in anticoagulant therapy to treat and prevent various thrombotic symptoms in patients , Including coronary and cerebrovascular diseases, which include administering to a patient with such a condition a therapeutically effective amount of a compound of formula (I): J (I) or a pharmaceutically acceptable salt thereof, as defined above Another embodiment of the compound of formula (I) or a pharmaceutically acceptable salt thereof according to the present invention 9 is the treatment and prevention of coronary artery disease, cerebrovascular disease, and other coagulation step-related disorders in patients. A patient having such a condition may be administered a therapeutically effective amount of a compound of the formula (I) of the present invention or a pharmaceutically acceptable salt thereof. The compound of the formula (I) of the present invention or a pharmaceutically acceptable salt thereof may also be administered. Yu Tai ------------- 41 ^ ---- r ---- Order --------- line (please read the phonetic on the back? Matters before filling in this hundred, &gt; Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -146- izz ^ 445 A7 ------- V. Description of the invention (144) To inhibit the use of blood coagulation, ^ m, for example, to prevent the aggregation of stored whole blood and to prevent it from being used in other biological samples for testing or storage Coagulation. This inhibitory coagulation inhibitor can be added to or contacted stored whole blood and any medium containing or suspected of containing blood aggregation factors, and those who wish to inhibit blood coagulation, such as when the blood of mammals When in contact with materials selected from the group consisting of vascular grafts, Wengshi graft membranes, orthopedic reliefs, cardiac deficiencies and extracorporeal circulation system. Formula_ 合 能 _ can produce serine acid related to the coagulation step response Proteases (active, therefore useful in the manufacture of pharmaceuticals, for the prevention or treatment of Insera blood)-methods for serine protease-mediated diseases, such as in mammals, in blood, in blood products, and In mammalian g Agglomerate formation, inhibition of fibrin formation, inhibition of thrombus formation, and inhibition of emboli formation. These compounds can also be used to treat or prevent restless colic, angina, myocardial infarction, transient hemorrhagic invasion in mammals , Anterior atrial fibrillation, thrombotic stroke, plug stroke, wood vein thrombosis, disseminated intravascular agglomeration, fibrin deposits, and re-occlusion or narrowing of re-formed blood vessels. These compounds can also be used Investigate the mechanism of the coagulation step response serine protease, so that better inhibitors can be designed and better detection methods developed. Compounds of formula (I) can also be used to prevent cerebrovascular accidents (CVA) or stroke. Those included in the family of compounds of formula (I) are their pharmaceutically acceptable salts. The term "pharmaceutically acceptable salts" includes salts commonly used to form free acid or metallurgical salts and addition salts. The nature of this salt is not important, provided that it is pharmaceutically acceptable. Formula ① Compound —_ -147- This paper ruler, National Fresh (CNS) A4 specification (210 X 297 public love) One (Please read the precautions on the back before filling this page)

if——l · — — —Order --------- Line I Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 122445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the Invention (145) Suitable pharmaceutically acceptable acid addition salts can be prepared from inorganic or organic acids. Examples of such inorganic acids are hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, carbonic acid, sulfuric acid, and phosphoric acid. Suitable organic acids may be selected from the group consisting of aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic, polyacid and transverse acids of organic acids, examples of which are formic acid, acetic acid, propionic acid, succinic acid, glycolic acid, Gluconic acid, lactic acid, malic acid, tartaric acid, citric acid, ascorbic acid, glucoconic acid, maleic acid, fumaric acid, pyruvic acid, aspartic acid, bran; amino acids, benzoic acid, o- Aminobenzoic acid, formic acid, salicylic acid, p-acrylic acid, phenylacetic acid, phenylglycolic acid, ambonic acid (bishydroxylic acid), methanesulfonic acid, ethyl dipic acid, benzoic acid , P-aminobenzonic acid, stearic acid, cyclohexylamino acid, alginic acid, galacturonic acid. Suitable pharmaceutically acceptable addition salts of compounds of formula (I) include metal salts made from aluminum, calcium, flour, magnesium, magnesium, sodium, and zinc, or from N, N1-difluorethylene ethylenediamine , Choline, chloroprocaine, diethanolamine, ethylenediamine, meglumine (N-methylglucosamine) and organic salts of procaine. All such salts can be prepared from conventional compounds of formula ① by conventional methods by reacting, for example, a suitable acid or base with a compound of formula ①. The invention also includes a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I), accompanied by at least one pharmaceutically acceptable carrier, adjuvant or diluent. The pharmaceutical composition of the present invention may comprise an active compound of formula (1) accompanied by one or more non-toxic pharmaceutically acceptable carriers and / or diluents and / or adjuvants (collectively referred to herein as "carriers") ), And other active ingredients if needed. The active compound of the present invention may be administered by any appropriate route, preferably in the form of a pharmaceutical composition suitable for such a route, and administered in a dose effective for the desired treatment. Paper size and standard (CNS) A4 specifications (21._ -148- x 297) (Please read the note on the back? Matters before filling out this page) ------ ^ ---- Order --- ------ Xiangtai 1222445 This active compound and composition can be administered, for example, orally, subcutaneously, intramuscularly, with clear eyes, or topically, to the accumulation of white eyes. 'These compounds can be administered orally or parenterally. Medication. A7 __------ ~ 5. Description of the invention (146), intravascular and peritoneal cavity. For the treatment of fibrous eggs in the eye or topically, and these compounds can be stored injectable glycosides, and also can be administered in the form of implants or implants, and can be formulated in a manner that allows delayed release of the active ingredient. This active ingredient can be compressed into pellets or small cylinders and made into a storage injection or implant for implantation subcutaneously or intramuscularly. Implants can be made of inert materials, such as biodegradable polymers or synthetic silicones, such as Slastle, silicone rubber, or other silicon-containing polymers. These compounds can also be administered in the form of liposome delivery systems, such as small monolayer vesicles, large monolayer vesicles, and multilayer vesicles. Liposomes can be made from a variety of phospholipids, such as cholesterol, stearylamine, or phospholipids choline. These compounds can also be delivered using individual antibodies as individual carriers to which the compound molecules are bound. The compound can also be combined with a soluble polymer &apos; to become a target pharmaceutical carrier. Such polymers may include polytetrahydropyrrolidone, piperan copolymer, polyhydroxynaphthyl-methylpropanamine-phenol, polyhydroxyethyl-asparagine-amine, or polyepoxy Ethane_Polylysine substituted with palmitoyl residues. Furthermore, these compounds can be combined with biodegradable polymer species, which can be used to achieve drug production and release, such as polylactic acid, polyglycolic acid, copolymers of polylactic acid and polyglycolic acid, polyε-caprolactone, Cross-linked or amphoteric block copolymers of polyhydroxybutyric acid, polyorthoesters, polyacetals, polydihydropiperans, polycyanopropanoic acid, and hydrogels. For oral administration, the pharmaceutical composition can be, for example, tablets, capsules (____ -149- This paper "uses 1P National Standard (CNS) A4 specification (21G X 2W mm) '---- --- -^ ---- Order --------- line (please read the notes on the back before filling this page) Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Preparation A7 B7 V. Description of the invention (147) The parent material includes the forms of delayed release or timed release), pills, powders, granules, agents, ST agents, suspensions, liquids (including syrups) and emulsions. The pharmaceutical composition is preferably made in the form of a dosage unit containing a specific amount of the active ingredient. Examples of such dosage units are tablets or capsules. The active ingredient can also be formulated into a composition for administration by injection, of which, for example, Saline, dextran, or water as appropriate carriers. The amount of therapeutically active compound administered and the dosage regimen of the compound and / or composition of the present invention for the treatment of disease symptoms depend on a variety of factors, including the patient Age, weight, gender and Therapeutic state, severity of the disease, the route and frequency of administration, and the particular compounds used, and therefore can be widely varied. These pharmaceutical compositions may contain the active ingredient in the range of about 0.1 to 2000 milligrams, and are preferably In the range of about 0.5 to 500 mg. The daily dose may suitably be about 0.01 to 100 mg / kg body weight, and preferably between about 0.05 and about 20 mg / kg body weight. The daily dose may be one to Four doses are administered. These compounds can be formulated in topical ointments or creams, or as suppositories, containing a total amount of active ingredients of, for example, 0.075 to 30% w / w, preferably 0.2 to 20% w / w 'and optimally 0.4 to 15% w / w. When formulated in an ointment, these active ingredients can be paraffin or water-miscible ointment bases. Alternatively, the active ingredients can be formulated with oil in water The cream base is formulated together in the cream. If necessary, the aqueous phase of the cream base may contain, for example, at least 30% w / w of a few alcohols, such as propylene glycol, butane-1,3-diol , Mannitol, anthocyanin, glycerin, polyethylene glycol and mixtures thereof. Topical formula Looking at the package -150- ------------------ ^ ---- order --------- line (please read the note on the back first? Please fill in this page again) ί 4 1 / b Nί 0 豕 ϋ if degree 1222445

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the Invention (148) Contains a compound that enhances the absorption or penetration of active ingredients through the skin or other infected areas. Examples of such skin penetration enhancers include dimethylformite and related analogs. The compounds of the invention can also be administered via a transdermal device. Local administration is preferably achieved using a patch, regardless of the type of reservoir and porous film, or the type of solid matrix. In either case, the active agent is continuously transported from the reservoir or microcapsule through the film to the adhesive through which the active agent passes, which is in contact with the skin or mucosa of the recipient. If the active agent is absorbed through the skin, a controlled and predetermined flow of active agent is administered to the recipient. In the case of microcapsules, the 'encapsulating agent can also be used as a film. The oil phase of the emulsion of the present invention can be formed from known ingredients in a known manner. Although this phase may contain only emulsifiers, it may contain at least one emulsifier and a fat or oil or a mixture of both fat and oil. It preferably contains a hydrophilic emulsifier, and is accompanied by a lipophilic emulsifier, which acts as a stabilizer. It is also better to include both oil and fat. Emulsifiers, with or without stabilizers, constitute the so-called emulsified waxes, which together with oils and fats constitute the so-called emulsified ointment bases, which form the oily dispersed phase of cream formulations. Emulsifiers and stabilizers suitable for the formulations of the present invention include, in particular, TWeen 60, Span 80, cetyl stearyl alcohol, myristyl alcohol, glyceryl monostearate, and sodium lauryl sulfate. The selection of the appropriate oil or fat for the formulation is based on achieving the desired aesthetic properties, because the solubility of the active compound in the large oils that may be used in pharmaceutical emulsion formulations is extremely low. Therefore, the cream should preferably be non-greasy, non-staining, and washable with a suitable consistency to avoid leakage from pipes or other containers. Straight chain or branch chain single _ or __ -151-This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---------------- -^ ---- Order --------- line fp · (Please read the notes on the back before filling in this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ------ -B7 V. Description of the invention (149) Dibasic alkyl esters, such as diisoadipate, isocetyl stearate, propylene glycol diester of coconut fatty acid, isopropyl myristate, decyl oleate Ester, isopropyl pivalate, butyl stearate, 2-ethylhexyl palmitate, or a blend of branched chain esters can be used. They can be used individually or in combination, depending on the nature required. Alternatively, high melting point lipids can be used, such as white soft rock and / or liquid rock or other mineral oil. For therapeutic purposes, the active compounds of the present invention are usually combined with one or more adjuvants suitable for the indicated route of administration. If administered orally, these compounds can be combined with lactose, sucrose, starch powder, cellulose esters of alkyl acids, cellulose alkyl esters, talc, stearic acid, magnesium stearate, magnesium oxide, phosphoric acid and sulfuric acid. Sodium is mixed with calcium salt, gelatin, acacia gum, sodium alginate, polyethylenetetrahydropyrrolidone, and / or polyvinyl alcohol, and then tabletted or encapsulated to facilitate drug administration. Such capsules or tablets may contain a formulation which may be provided as a dispersion of activated panthenol per propyl methylcellulose. Formulations for parenteral administration can be in the form of aqueous or non-aqueous isotonic sterile injection solutions or suspensions. These solutions and suspensions can be prepared from sterile powders or granules with one or more of the carriers or diluents mentioned in the oral dosage formulation. These compounds are soluble in water, polyethylene glycol, propylene glycol, ethanol, corn oil, cottonseed oil, peanut oil, sesame oil, benzyl alcohol, sodium chloride, and / or various buffering agents. Other adjuvants and modes of administration are well and widely known in the medical arts. In the practice of the method of the present invention to treat and prevent various thrombotic symptoms, including coronary artery and cerebrovascular diseases, the compound of the present invention and the medicinal group of the pharmaceutical group are used alone or in combination with each other, or in combination with other therapeutic agents or in vivo diagnosis- -------------- K ---- Order --------- Line (Please read the precautions on the back before filling this page)

1222445 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (15) Dosage. The coagulation step response inhibitor of the present invention may also be co-administered with an appropriate agglutinating agent that destroys platelets, including but not limited to ticlopidine or clopidogrel, a fibrinogen receptor antagonist ( For example, to treat or prevent restless colic, or to prevent re-occlusion and restenosis after angioplasty), anti-agglomerating agents, such as aspirin, kawaii, or heparin, solubilizing thrombolytic agents, such as fibrinolytic Zymogen activator or streptokinase to achieve synergistic effects in various pathological treatments, lipid-lowering agents' include antihyperlipidemic drugs (such as HMGCoA reductase inhibitors such as mevastatin, lovastatin ( lovastatin), simvastatin, pravastatin and fluvastatin, HMG CoA synthetase inhibitors, etc., antidiabetic drugs, or other cardiovascular agents (circulating diuretics) , Thiazide-type diuretics, nitrates, aldosterone antagonists (meaning, stronongolide and epoxy melistanone), angiotensin-converting enzyme (such as ACE) inhibitors, vascular collection Π hormone receptor antagonist, a blocker 'antiarrhythmic agents, antihypertensive agents and calcium channel blockers) to treat or prevent arteriosclerosis. For example, patients with coronary artery disease and patients undergoing angioplasty procedures will benefit from co-administration of fibrinogen receptor antagonists and the coagulation step response inhibitors of the present invention. Coagulation step response inhibitors can also enhance the efficiency of tissue plasminogen activator-mediated hemolysis and reperfusion. The typical doses of the coagulation step response inhibitor of the present invention and other appropriate platelet-destroying agents, anticoagulants, cardiac and vascular therapeutic agents or thrombolytic agents may be co-administered with other platelet-destroying agents, anticoagulants, heart and blood vessels. Dosage phase of coagulation cascade inhibitors for therapeutic agents or thrombolytic agents ---- K ---- ^ --------- (Please read the precautions on the back before filling this page )

1222445 Still A7 V. Description of the invention (151) ^ or may be lower than the dose of the blood coagulation cascade inhibitor &lt; administered without co-administration of other platelet-destroying agents, anticoagulant = II; According to the needs of the patient's treatment, all the reference materials mentioned are in the form of references ^ in general written in this article. Although the invention has been described in terms of specific embodiments, the details of these specific embodiments are not intended to be construed as limiting. The following ㈣w is provided to illustrate the present invention and is not intended to limit its scope. I believe that the artist needs to further scrutinize the artist, so that he can use the foregoing description to utilize the present invention to its fullest extent. Therefore, the following preferred special embodiments are intended to be interpreted as merely illustrative examples, and not to limit the rest of the disclosure in any way. Compounds containing multiple modifications of the structural modification shown in the scheme or the examples below are also intended to be included. Those skilled in the art will readily understand the known variations of the conditions and methods of the preparation procedures described below, which can be used to prepare these compounds. Those skilled in the art can use these general methods to prepare the following specific examples, which have been or can be properly identified by 1HNMR, mass spectrometry, elemental composition, and similar procedures. These compounds can also be formed in vivo. The following examples contain detailed descriptions of the methods for preparing compounds of formula (I). These detailed descriptions are within their scope and are presented for illustrative purposes only and are not intended as a limitation on the scope of the invention. All parts are by weight and temperatures are in degrees Celsius unless otherwise noted. The general synthesis sequence described below can be used to practice the invention. Abbreviations used in drawings and tables, including: &quot; AA &quot; for amino acids, &quot; AcCN, for acetonitrile, -154 (Please read the precautions on the back before filling out this page);-order --- ------ Line · Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs ^ The paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 Α7 Β7 5 Explanation of the invention (152) • 'AcOH "means acetic acid, nBINAF' means 2,2 '· bis (diphenylphosphino) -1, Γ-bifluorene, &quot;: ΒηΟΗ', which means benzyl alcohol, &quot; BnCHO &quot; Represents 2-phenylacetaldehyde, ·· Βη802α ··· represents benzylsulfonium chloride, ', Bocn represents the third-butoxycarbonyl group, and "ΒΟΡ" represents benzotriazol-1-yl-oxy parameter- (Dimethylamino), nbu "means butyl, ndba &quot; means diphenylmethyleneacetone, nDCC" means 1,3-dicyclohexylcarbodiimide, •• DCM 'means dichloromethane, "" "DIBAH" or "DIBAL" stands for diisobutylaluminum hydride, "DMFn stands for dimethylformamide," DMSOn stands for dimethylformamide, " "DPPA" means diphenylphosphonium azide, &quot; EDC &quot; means 1 · [3 · (dimethylamino) propyl] -3-ethylcarbodiimide hydrochloride, "Ex. No. &quot; Represents the instance number, "Fmoc" represents 9-fluorenylmethoxycarbonyl, "HOBt" represents hydroxybenzotriazole, •, LDAff represents lithium diisopropylamine, "MW" represents molecular weight, and "NMMM" represents Ν -Methylmorpholine, "Ph" means phenyl or aryl, "ΤΗΤΗ" means phthalofluorenyl, "pnZ" means 4-nitrobenzyloxycarbonyl, "TTC" means phase transfer catalyst, and "pyn" Pyridine, "RNH2 '" means primary organic amine, "SEM" means 2- (trimethylsilyl) ethoxymethane chloride, "p-TsOH" means p-toluenesulfonic acid, and "TBAF" means fluorinated Tetrabutylammonium, ffTBTUn means tetrafluoroborate 2- (1Η · phenylhydrazine-1-yl) _1,1,3,3_tetramethylphosphonium, &quot; TEA &quot; means triethylamine, &quot; TFA &quot; For trifluoroacetic acid, "THFf for tetrahydrofuran," TMS "for trimethylsilyl," TMSCN "for trimethylsilyl cyanide, and" Cbz "or ΠZ" for 芊Oxycarbonyl. General Synthesis Procedures and Special Examples The compounds of the present invention can be synthesized, for example, according to the following procedures and the schemes given below. The general synthetic pathways to achieve a wide variety of R2-substituted pyrimidinones are shown in Schemes 1 to below In Equation 5. Aminoacetaldehyde dimethyl acetal for the treatment of phenylarylene -155- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ----------- • equipment ---- l · --- Order --------- Line Dance (Please read the notes on the back before filling this page) 1222445 A7 -------------- ------ 5. Description of the invention (153) A solution of ethyl acetate hydrochloride in methanol to provide substituted benzamidine. The cyclization of benzamidine with methoxymethylene-dimethylmalonate will cause the formation of a heterocyclic nucleus of ketone ketone, which has the required functional groups for further processing. This ester is demethylated by lithium iodide, followed by the Curtius rearrangement of the acid formed, by placing a decisive nitrogen at C-5 to form a protected urethane. The dimethyl acetal is hydrolyzed and the aldehyde formed is oxidized with sodium chlorite to obtain glycine units at N_3. The protection of this acid becomes ditributyric acid 'followed by the deprotection of the carbamate by hydrogenation to obtain free amidine, at C-5. This amine is treated with chloramidine or acid under reductive amination conditions to obtain sulfonamide or secondary amine individually. The protected acid was then exposed with HC1. These acids are then coupled to various amines under standard peptide coupling conditions. These amines are typically polyfunctional and are used in some protected form. Remove these protecting groups and provide the compounds for evaluation. These synthetic schemes and procedures are exemplified below. ----------- • installation ---- l · --- order --------- line_ (Please read the phonetic on the back? Matters before filling out this page) Ministry of Economy Printed by the Intellectual Property Bureau, Consumer Cooperative

1222445 A7 B7 V. Description of the invention (154)

Scheme 1: General pyrimidone synthesis-I Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

4b 1. 1N HCI, 2. NaCI〇2 -157- This paper size is applicable to China National Standard (CNS) A4 specification (210 x 297 mm) ----------- · installation ---- l · --- Order --------- line Φ- (Please read the precautions on the back of the L before filling this page) 1222445 A7 B7 V. Description of the invention (155) Scheme 2:-general call Synthesis-I (continued)

γ 〇 YA OH

〇 R 4b (ClC〇) 2, t-BuOH, Eo, N,

4b H2, Pd / C

R, ◦ dog

2 N,,. Too ----------- · install ---- K ---- order --------- line (please read the precautions on the back before filling this page &gt;

〇R 4b Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs-158- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 B7 V. Description of the invention (156) Schema 3: General shouting_Synthesis-I (continued) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-159- ----------- · Install ---- l · --- Order --------- (Please read the precautions on the back before filling this page) This paper Standards are applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) 1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (157 Scheme 4: General pyrimone synthesis-I (End) , 2 where

B-HIST

B-HN

HCI ▼

〇 R 4 b BC (〇) -HN, 2

0 R 4b EDC H〇BT, Cbz-Y ° -NH2 BC (0) -HN ^ ▼

B-HNT

Pd / C, H2

Where / FT

O R 4b BC (〇) guest

1 / FT

A

R 4b

HCI ΌΗ JM,

FT 〇 ΌΗ R4b EDC H〇BT, Cbz-Y ° -NH2 Pd / C, H2-R2

〇R 4b · Shang · Order · ^ • 1 (Please read the Cautions on the back before filling in this page> • ϊί -160 This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs V. Invention Description (158)

巳 S〇2-HfsT 巳 s〇2-hn Scheme 5:-General synthesis of ketolide_1 (end)

HCI

R 〇 4b, n, BCH2-HI \ r

Where yFT

R 4b

Y

R 4b EDC HOBT, Cbz-Y ° -NH2 BCH2-HN ^ ▼

Pd / C, H2

Where / FT

JNL ΌΗ

HCI 〇 ΌΗ BS02-HNy

R 4b BCH2-HN Scheme 1 to Scheme 5 are exemplified in the following examples -161 R4b EDC HOBT, Cbz-Y ° -NH2 Pd / C, H2

FT

* O 'ίί I ---------- · 装 ---- l · --- order --------- ^ φ— (Please read the precautions on the back before filling in this Page &gt;

〇 R 4b This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) B7 V. Description of the invention (159 Example 1

(Please read the note on the back? Matters before filling out this page) X_1A) A solution of ethyl benzimidate hydrochloride (92.25 g, 496.9 mmol) in 300 · mL of anhydrous methanol ( 1.68 M), cooled to about (TC, and amine acetaldehyde dimethyl acetal (73 10 ml, 6709 mmol) was added dropwise to methanol (75.0 ml, 9.0 M). The solution was kept at a temperature lower than 5 at this rate. (: The solution was stirred for 3 days and kept at a temperature lower than 5 ° C. The reaction mixture was then concentrated under reduced pressure to obtain Yellow oil. The residue was dissolved in iNNaOH (750 ml) and extracted with methane gas (4 X 250 ml). The organic solutions were combined, dried (MgS04), and concentrated. Staff of Intellectual Property Office, Ministry of Economic Affairs The consumer cooperative printed 108.13 grams of crude team (2,2-dimethoxyethyl) benzamidine as a yellow oil. Here, crude N- (2,2-dimethoxyethyl) benzamidine ( 108.13 g, 519.2 mmol) in anhydrous methanol (125.0 ml, 4.2 M) at room temperature, add dimethyl methoxymethylenemalonate (94.13 g, 540) .5 mmol). The resulting mixture was heated to about 100 ° C while slowly distilling off the solvent over a period of two hours. The resulting dark brown solution was cooled to room temperature and ethyl acetate was added. (1 liter) diluted. The organic solution was washed with saturated NH4C1 (2 X 500 ml) and brine (1 X 500 ml). The organic solution was dried (MgS04), filtered and concentrated. Borrow MPLC (25% ethyl acetate / hexane Alkane) purify the crude product to obtain pure -162- This paper size is applicable to the Chinese National Standard (CNS) A4 specification (21〇x 297 public love ^ &quot; &quot; &quot; &quot; 1222445 A7 _______ B7 V. Description of the invention (16〇 ) (Please read the notes on the back before filling this page) 1_ (2,2_Dimethoxyethyl-2-phenylpyrimidine 6 (1H) -one-5-carboxylic acid methyl ester (EX-1A) , 73% yield, yellow brown oil: 1hnMR (300MHz, CDC13) β 8.73 (s, 1H), 7.59-7.49 (m, 5Η), 4.86 (t, J = 5.5 Ηζ, 1Η), 4.16 (d, J = 5.4 Ηζ, 2Η), 3.95 (s, 3Η), 3.32 (s, 6H); 13 C NMR (75 MHz, CDC13) ά 165.9, 164.6, 159.3, 158.2, 134.6, 130.9, 128.93, 128.78, 114.9, 101.4, 56.0, 55.1, 52. 7, 49.1; Calculate HRMS (ES) for C16H19N205 294 319.1294, measured 値 319.1288. (EX-IB) in 1- (2,2-dimethoxyethyl-2 · phenylpyrimidine-6 (1Η) · keto-5-carboxylic acid methyl ester (93.00 g, 292.2 mmol) In a solution of 420.0 ml of anhydrous pyridine (0.70 M), lithium iodide (98.00 ml, 732.2 mmol) was added in one portion and stirred at room temperature, at which time an exotherm occurred. The pale brown suspension formed was suspended The liquid was heated to reflux for 2 hours. The dark brown reaction was cooled to room temperature and the volatiles were removed under reduced pressure. The resulting oil was diluted with 1 NHC1 (500 ml). The aqueous solution was diluted with dichloromethane / Methanol (4: 1, 4 X 250 ml) extraction. The combined organic solutions were washed with 6 NHC1 (2 X 250 ml), dried (MgS04), filtered and concentrated. The crude product was crystallized (ethyl acetate / Ministry of Economy) Intellectual Property Bureau employee consumer cooperative printed hexane) purified to obtain pure 1- (2,2-dimethoxyethyl-2-phenylpyrimidine 6 (1Η) -one · 5-carboxylic acid ester (EX_1B) "% Yield, as a white solid: iHNMR (300 MHz, CDC13) d 12.99 (s, 1H), 8.97 (s, 1H), 7.63_7.51 (m, 5H), 4.78 (dd, J = 4.3, 5.5 Hz, 1H), 4.28 (d, J = 5.4 Hz, 2H) 3 · 30 (s, 6H); 13 C NMR (75 MHz, CDCI3) d 165.8, 165.1, 164.1, 159.1, 133.6, 131.5, 129.1, 129.0, 112.6, 101.0, 55.8, 49.2; Calculate for C15H17N205iHRMS (ES) 値305.1137, measured 値 305.1113. In 1_ (2,2_ —methyllactylethyl_2 · phenylanodo-6 (1H) _ 嗣 -5-metanoic acid · (65.93 g, 216.67 mmol) in 800 ml 1,4_ of Dioxin (0.27 M) _ -163- This paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7- ----------- B7 fi 9 1 uj ϋ d 5 V. Description of the invention (161) Triethylamine (50_0 ml, 358.7 mmol) was added to the suspension, and then at room temperature ' Diazide diphenyl phosphate (51.40 ml, 238.5 mol) was added in one portion. The resulting solution was slowly heated to reflux for 2 hours. Then, benzyl alcohol (45.00 liter, 434.8 mol) and kept at reflux for about 14 hours. The black solution was allowed to cool to room temperature and the volatiles were removed under air. The resulting residue was diluted with ethyl acetate (G5 liter). The organic solution was washed with saturated NH4C1 (2 x 500 mL), iNNaOH (1 X 500 mL), and brine (1 X 500 mL). The organic solution was dried (1080), filtered and concentrated to obtain the crude product. By] ^ 1 ^ purification (15% -30% ethyl acetate / hexane), pure [5-[(fluorenyloxycarbonyl) amino] -2 · phenyl-6-keto · 1,6-di Hydro-1-pyrimidinyl] acetaldehyde dimethyl acetal (EX-1C) as a light brown solid, 46% Yield: 1111 ^ [11 (400) ^ 1112, 0 (: 13) (^ 8.72) 8, 111), 7.53-7.32 (m, 11Η), 5.20 (s, 2Η), 4.68 (t, J = 5.6 Ηζ, 1Η), 4.12 (d, J = 5.6 Ηζ, 2Η), 3.22 (s, 6H ); 13 C NMR (100 MHz, CDC13) β 158.3, 153.7, 153.2, 135.9, 134.9, 134.7, 130.1, 129.1, 128.9, 128.8, 128.71, 128.66, 128.4, 125.1, 101.3, 67.7, 55 · 4, 48 · 6; Calculate 値 410.1716 for C22H24N305iHRMS (EI), find 値 410.1741 〇 (EX-1D) in [5 · [(benzyloxycarbonyl) amino] _2_phenyl_6_keto-1 , 6-Dihydro_1 · pyrimidinyl] acetaldehyde dimethyl acetal (17.24 g, 42.11 mmol) in 103.0 ml of tetrahydrofuran · 35.0 ml of 1 NHC1 was added. The two-phase mixture formed Heat to reflux over 12 hours. Allow the reaction mixture to cool to room temperature and remove the volatiles under air. Dilute the resulting residue with water (200 mL) And by adding solid NaHC03, the pH was adjusted to 7. The resulting emulsion was extracted with dichloromethane (4 x 150 ml). Combined 164- This paper is in accordance with China National Standards (CNS) ) A4 specification (210 X 297 public love) ------------ • Installation ---- l · — (Please read the phonetic on the back? Matters before filling out this page) 4 1222445 Ministry of Economic Affairs wisdom Printed by A7 B7, Consumer Cooperative of the Property Bureau. 5. The organic solution of the invention description (162) was washed with water (1 X 200 liters), dried (MgS04), filtered and concentrated to obtain 15.74 g of crude [5-[(benzyl Oxycarbonyl) amino] 2-phenyl-6-keto · 1,5-dihydro-1-pyrimidinyl] acetaldehyde. The crude [5-[(benzyloxycarbonyl) amino 1-2-benzene -6-keto-1,6-dihydropyrimidinyl] acetaldehyde (15.30 g, 42.11 mmol) in 198.0 ml of tetrahydrofuran, tertiary-butyl alcohol, and 2-methyl · 2-butene (1 : 1: 13, 0.21 M), the solution was cooled to 0 ° C. Then, sodium chlorite (29.94 g, 331.1 mmol) and sodium dihydrogen phosphate monohydrate (35.42 g) were slowly added to the solution. , 256.7 millimoles) in 102.0 ml of water (3.2 M, based on sodium chlorite). The formed gold two-phase solution was stirred for 10 minutes and the cold bath was removed. The reaction was stirred at room temperature for 1 hour. The volatiles were removed under reduced pressure. The resulting solution was diluted with water (200 ml) and the pH was adjusted to 3 by adding saturated NaHC03 and 1 NHC1. The aqueous solution was extracted with tetrahydromethylene chloride (1: 2, 4 x 180 ml). The combined organic solutions were dried (MgS04), filtered and concentrated to give the crude product. Diethyl ether was used for purification through trituration to obtain [5 _ [(fluorenyl) amino] -2-phenyl-6-fluorenyl-1,6_dichloro-1_p denselyl] acetic acid, As a white solid: iHNMR (300 MHz, Dd-DMSO) d 13.34 (brs, 1H), 9.03 (s, 1H), 7.57-7.34 (m, 10H), 5.23 (s, 2H), 4.56 (s, 2H) ; 13 C NMR (75 MHz, d-DMSO) d 169.4, 158.0, 154.6, 154.3, 137.1, 134.8, 130.9, 129.4, 129.1, 128.78, 128.72, 128.50, 125.5, 67.0, 48 · 8; to C20H18N3〇5 HRMS (El) calculated 値 380.1246, found 値 380.1246. (EX-IE) make [5-[(fluorenyl) amino] -2-phenyl-6-fluorenyl-1,6-dihydro-1-p denselyl] acetic acid (5.2503 g, A suspension of 13.84 mmol in 70.0 ml of chloroform (0.2 M) was cooled in an ice bath to about 0 ° C. Then, in this cold suspension -165- This paper size is applicable to China National Standard (CNS) A4 (21〇X 297mm) ----------- • Packing ---- K- --- Order --------- ^ 9— (Please read the notes on the back before filling this page) 1222445 A7

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the Invention (163), Chloroprolamide (6.0 liters, 78 millimoles) was added dropwise via a syringe. After intense gas release, a golden uniform solution was formed. After stirring for 5 minutes, the cold bath was removed and the solution was stirred for another 2 hours at room temperature. The solvents were removed under reduced pressure and placed in a high-altitude air system to remove residual solvents over a period of 10 minutes. The resulting yellow solid was diluted with 70.0 ml of air-form (02 M), and pyridine (1.70 ml, 21.02 mmol) and 2-methyl-2-propanol (3.50 ml, 36.60 mmol) were added. . The resulting yellow-brown solution was stirred at room temperature for 1 hour, and then heated to reflux for 12 hours. The reaction mixture was allowed to cool to room temperature 'and diluted with chloroform (3 ml). The organic solution was washed with water (1 X 100 ml), saturated NaHC03 (1 X 100 ml) and brine (1 x 100 ml). The organic cereal was dried (MgSO4), filtered and concentrated. The crude reaction was purified by MPLC (25% ethyl acetate / hexane) to give a product in a 49/0 yield: 1H NMR (300 MHz, CDC13) d 8.81 (br s, 1H), 7.57 · 7 · 38 (m, 11H), 5.27 (s, 2H), 4.57 (s, 2H), 1.47 (s, 9H); 13 C NMR (75 MHz, CDC13) d 166.4, 158.0, 153.2, 135.9, 135.0, 134.4, 130.6, 129.1, 128.9, 128.7, 128.5, 128.4, 125.4, 83.4, 67.7, 49.1, 28.2 'Calculate the HRMS (El) of C24H26N3O5 値 436.1872, measured 値 436.1876. (EX_1F) in [5-Amino · 2-phenyl-6 · keto · 1,6_dihydro_lu denselyl] tert-butyl acid (1.8647 g, 4.282 mmol) at 21.0 To a solution in ml of methanol (0.2 M), 211.3 mg of 10% Pd / C was added in one portion. The resulting mixture was stirred at room temperature under an atmosphere of hydrogen (cylinder) for about 16 hours. The crude reaction mixture was filtered through a pad of celite 545 and the solvent was removed under reduced pressure. This crude product was triturated from diethyl ether to obtain the pure product [5-amino-2-phenyl-6-keto-I, 6-dihydro-1_pyrimidinyl] tributyl acetate (EX_1F), 99% Yield: -166- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ----------- install -----: ---- order-- ------- (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ------- B7 V. Description of the invention (164) 1HNMR (400MHz5 CDC13) cy 7.41-7.39 (m, 6H), 4.48 (s, 2H), 4.06 (br s, 2H), 1.39 (s, 9H); 13CNMR (100MHz? CDC13) d 166.8, 158.6, 149.3, 134.9 , 132.9, 130.0, 128.9, 128.5, 127.7, 82.9, 48.7, 28.1; Calculate HRMS (EI) for C16H20N3O33302.1505, measured 实 302.1491. (EX_1G) tert-Butyl acetate (1.0300 g, 3.418 mmol) in [5_amino_2_phenyl-6-keto · 1,6_dihydro_1-pyrimidinyl] in 5.5 ml To a solution of tetrahydrofuran and 2.0 liters of dimethylformamide (0.45 M), N-methylmorpholin (1.20 liters, 10.91 mmol) was added in one portion. This solution was allowed to cool to 0 ° C in an ice bath. After stirring for 10 minutes, a solution of 718.2 mg of p-toluenesulfonium chloride (3.767 mmol) in 5.5 ml of tetrahydrofuran (0.68 M) was added dropwise over a period of 5 minutes. The reaction mixture was stirred at 0 ° C for 2 hours. The reaction mixture was diluted with ethyl acetate (150 ml). The organic solution was washed with 1NHC1C2X25 ml), saturated NaHC03 (2 X 25 ml) and brine (1 X 50 ml). The organic solution was dried (MgS04), filtered and concentrated under reduced pressure. The formed yellow solid was triturated with diethyl ether, filtered and dried under vacuum to give the pure product (EX-1G) as a white solid, 74% yield: iHNMRGOOMHz, d-DMSO) ^ 9.34 (s, 1H), 7.76 (s, 1H), 7.55-7.28 (m, 10H), 4.59 (s, 2H), 4.49 (s, 2H), 1.32 (s, 9Η); 13 C NMR (100 MHz, d-DMSO) d 167.0, 158.8, 156.5, 142.1, 134.5, 131.7, 131.0, 130.1, 129.4, 129.0, 128.94, 128.58, 124.8, 83.0, 59.6, 49 · 2, 28 · 1; .C23H26N305S HRMS (EI) calculation 値 456.1593, Found 値 456.1597. (EX-1H) A solution of (EX-1G) (1.0643 g, 2.336 mmol) in 9.0 ml of 4MHC1 in dioxolane (0.1M) was stirred at room temperature for 12 hours. The crude reaction was concentrated under reduced pressure. The formed residue is ground with ether-167- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) &quot; &quot; ----------- pack --- -^ ---- Order --------- ^ 9— (Please read the notes on the back before filling this page) 1222445 A7 B7 V. Invention Description (165) (Please read the notes on the back first Please fill in this page again) to obtain pure product (EX-1H), 87% yield, white solid: IhNMR (400 MHz, d-DMSO) δ 9.32 (s, 1Η), 7.74 (s, 1Η), 7.51-7.30 (m, 10Η), 4.58 (s, 2H), 4.48 (s, 2H); 13 C NMR (100 MHz, d-DMSO) d 169.2, 158.7, 156.6, 141.9, 134.5, 131.7, 131.0, 130.1, 129.4, 129.0, 128.90, 128.56, 124.8, 59.6, 48.9; Calculate 値 400.0967 for HRMS (El) of 8N305S, Measured 値 400.0959. (EX-11) To a solution of acid (EX-1 酸) (40. 8 mg, 1.08 mmol) in lo.o ml of dimethylformamide (0.10 M), add N , N-diisopropylethylamine (0.900 ml, 5.167 mmol), N-hydroxybenzotriazole (167.7 mg, 1.241 mmol) and 1- [3- (dimethylamino) propyl] 3-Ethylcarbodiimide hydrochloride (236.1 mg, 1.232 mmol). The resulting mixture was stirred at room temperature for 30 minutes, and the mixture became homogeneous. To the reaction mixture was then added '(at main temperature)' in one portion of 4- (Cbz-methylmethyl) ethanamine (324.6 mg, 1.126 mmol). The resulting mixture was then stirred for 18 hours. The reaction mixture was diluted with ethyl acetate (50 ml). The organic solution was washed with 50/0 citric acid (1 X 25 mL), saturated NaHC03 (1 X 25 mL), and brine (1 X 25 mL). The organic solution was dried (MgS04), filtered and concentrated. The crude reaction mixture was triturated with diethyl ether to obtain the pure product (EX-1I), which was printed as a solid by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs: 4 NMR (300 MHz, Dd-DMSO) d 9.36-9.18 (brm, 3H), 8.82-8.78 (m, 1H), 7.98 (d, J = 8.3 Hz, 2H), 7.84, (s, 1H), 7.56-7.32 (m, 16H), 5.15 (s, 2H), 4.65 (s, 2H), 4.58 (s, 2H), 4.40 (d, J = 5.4 Hz, 2H); Calculate HRMS (El) for C3 5 H3 3 N6 06 S2 値665.2182, measured 665.2177. In a solution of Cbz-fluorene (EX-11) (237.7 mg, 357.6 mmol) in 3.5 ml of methanol and 4 MHC1 (in dioxolane) (4: 1, 0_i M), Copies _ -168- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 1222445 Printed by A7 B7, Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (166) Add 42.1 mg 10% Pd / C. The resulting mixture was stirred under an atmosphere of hydrogen (gas bottle) 'at room temperature for about 16 hours. The crude reaction mixture was filtered through a pad of Celite 545 and the solvent was removed under reduced pressure. The crude product was purified by HPLC (gradient 5%-95% acetonitrile / water with 0.1% trifluoroacetic acid) to obtain the pure product as a white solid: iHNMR (300MHz, d-DMSO) 9.31-9.28 (m, 4H )? 8.88 (br s, 1H)? 7.81-7.77 (m, 3H), 7.60-7.54 (m? 5H)? 7.43-

7.37 (m, 7H), 4.65 (s, 2H), 4.58 (s, 2H), 4.42-4.41 (m, 2H); for C2 7 H2 7 04 S 101] ^ (£ 1) Calculate 値 531.1815, measured値 531.1794. Example 2

The title compound was prepared according to the method of Example 1: 1 H NMR (300 MHz, d-DMSO) β 9.40-9.33 (m, 4H), 8.86 (s, 1H), 7.82 (s, 2H), 7.72-737 (m , 15H), 4.65-4.59 (m, 4H), 4.41-4.40 (m, 2H); Calculate El531.1815 for HRMS (El) of C2 7H2 7N6 04 S, Measured 値 531.1794. Example 3

NH -169- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) · Packing ---- K ---- Order --------- (Please read the back t Please fill in this page for precautions> 1222445 A7 B7___ 5. Description of the invention (167) (Please read the precautions on the back before filling in this page) (EX-3A) in [5-Amino-2-phenyl-6- Keto · 1,6-dihydro-1-oxoyl] tert-butyl acetate (EX-1F) (613.7 mg, 2.037 mmol) in 7.0 ml tetrahydrofuran and dichloromethane (1: 1: 03 M) To the solution in 2), add 25.0 ml of acetic acid and phenylacetic acid (0.475 ml '4.060 mmol). Allow the solution to cool to 0 ° C in an ice bath and add sodium triethoxylate borohydride in one portion. (1.9131 g, 9.027 mmol). 撗: After dropping for 5 minutes, remove the ice bath and stir the reaction mixture at room temperature for 2 hours. The reaction was quenched by adding INNaOH (5 ml), and the mixture was quenched. Stir for 5 minutes. Dilute the reaction mixture with 0.5 NNaOH (100 mL). Extract the aqueous solution with ethyl acetate (3 X 25 mL). Combine the organic solutions with 0.5 N NaOH (1 x 25 mL) and brine (1 x 25 mL) The solution was dried (MgS04), filtered and concentrated under reduced pressure. Purified by MPLC (25% ethyl acetate / hexane) to obtain EX-3A as a yellow oil, 74% yield: 1H NMR (400 MHz CDC13) ^ 7.43-7.40 (m, 4H), 7.31-7.26 (m, 2H), 7.23 · 7.16 (m, 5H), 4.70 (br s, 1H), 4.49 (s, 2H), 3.38- 3.34 (m, 2H), 2.96-2.92 (m, 2H), 1.40 (s, 9H); HRMS (El) calculated for C24H28N303: 406.2131, measured: 406-2125. Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs A solution (0.1 M) of EX-3A (521 · 3 mg, 1.286 mmol) in 13.0 ml of 4MHC1 (in dioxolane) was stirred at room temperature for 12 hours. The crude reaction was Concentrated under reduced pressure. The resulting residue was triturated with diethyl ether to obtain the pure product EX-3B in quantitative yield as a yellow solid: iHNMR (300 MHz, d-DMSO). 7.66-7.57 (m, 5H), 7.33-7.23 (m, 6H), 4.57 (s, 2H), 3.44-3.35 (m, 2H), 2.97-2.92 (m, 2H); 13 C NMR (75 MHz? D-DMSO) ά 168.8, 157.0, 148.0, 139.9, 135.0, 132.2, 129.69, 129.48, 129.07, 126.9, 48.8, 44.5, 34.5; for C20H20N3 The 3 HRMS (El) Calcd 350.1505, found 350.1520 Zhi. -170- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economy 1222445 A7 _ B7 V. Description of the invention (168)

To a solution of EX-3B (497 · 8 mg, 1.290 mmol) in ΐ3.0 ml of dimethylformamide (0.10M), Ν, Ν · diisopropylethylamine (υοοml, 1033 mmol), N-hydroxybenzotriazole (212.8 mg, 1.575 mmol) and 1- [3- (dimethylamino) propyl] _3-ethylcarbodiimide hydrochloride (302.5 Mg, 1.578 millimoles). The resulting mixture was stirred at room temperature for 30 minutes, and the mixture became homogeneous. Then, 4- (Cbz-formamyl) benzylamine (410.9 mg, 1.425 mmol) was added to the reaction mixture in one portion at room temperature. Then, the resulting mixture was dropped for 18 hours. The reaction mixture was diluted with ethyl acetate (50 ml). The organic solution was washed with 5% citric acid (1 x 25 ml), saturated NaHC03 (l x 25 ml) and brine (1 x 25 ml). The organic solution was dried (MgS04), filtered and concentrated. Trituration with ether and purification of the crude reaction mixture gave the pure product EX-3C as a white solid: iHNMR (400 MHz, d-DMSO) d 9 · 08 (br s, 2H), 8.62 (t, J = 5.8 Hz , 1H), 7.90 (d, J = 8.3 Hz, 2H), 7.44-7.15 (m, 17H), 5.35 (t, J = 5.9 Hz, 1H), 5.07 (s, 2H), 4.44 (s, 2H) , 4.29 (d, J = 5.4 Hz, 2H), 3.31-3.26 (m, 2H), 2.88-2.85 (m, 2H); Calculate HRMS (El) for C3 6H3 5N604 値 615-2720, measured 値 615.2688. In a solution of EX-3C (222.6 mg, 362.1 mmol) in 4.0 ml of methanol and 4 MHC1 (in dioxolane) (3: 1, 0 · 1 M), 53.0 mg of 10 was added in one portion. % Pd / C. The resulting mixture was stirred under a hydrogen (gas cylinder) atmosphere at room temperature for about 16 hours. The crude reaction mixture was filtered through a pad of celite 545 and the solvent was removed under reduced pressure. Trituration from ether to purify the crude product to obtain the pure product as a yellow solid: 111 ^ 111 (30〇) ^ 1112, (1-DMSO) ά 9.62-9.30 (br m? 5H), 7.88 (br m? 2H) 7.58-6.86 (br m? 15H), 4.59 (br s, 2H), 4.36 (br s, 2H), 3.38 (br s, 2H), 2.91 (br s, 2H); For C28H29N602 -171-this paper The scale applies to China National Standard (CNS) A4 specification (210 x 297 mm) ------------ quake ----- ^ ---- order --------- Line ^ 1- (Please read the note on the back? Matters before filling out this page) 1222445 A7 V. Selection of invention description (169) · Calculation of hunger rule, actual measured value 481 2348.: For example, a direct combination of 2 · Aryl, 2 · heteroaryl or 2-heteroatom, and w-bonded organic group passes through the heteroatom to the fluorenone of the fluorenone ring, uf is prepared by the following schemes 6 and 7. The heteroatoms are The above is sulfur, nitrogen, lice or another suitable heteroatom. The general procedure of Scheme 6 is used to prepare a special foot heteroatom-substituted pyrimidinone, which is disclosed in Examples 4 and 5. · Installation ----- ^ ---- Order --------- line (Please read the notes on the back before filling this page) Printed by Sakusho-172- X 297 mm) The Weiwei scale turned over Jiaxuan (CNS) A4 specifications (210 1222445 A7 B7 V. Description of the invention (17. Figure 6. 2-Substituted pyrimidinone preparation SEM steps A1 · K2C03 SEMC1

〇2N η2ν

Step ^ Η2, Pd / C MeOH • co2ch3 Step B 2. K2C〇3 CICH2-CO2CH3

CO2CH3

1. PhCH2CH〇 Step D \ 2. NaBH (〇Ac) 3 THF, CH2a2, AcOH Printed by Consumer Consumption Cooperative of Intellectual Property Bureau of Ministry of Economic Affairs Step E: 1. LiOH, MeOH H2〇 Step R 2. EDC, H〇Bt, DIEA, DMF, R -NH2 H Step I: 1. R-SH, R-〇H, or R-NH2 dioxolane, base t or, X Step J: '2. ArB (〇H) 2, Pd (PPh〇) 4 / / N, / Na2C03

Nv ^ xjC〇2CH3

H EM

CONH-R Step K (deprotection) • CONH-R -173-

Step G: 1.TBAF, THF Step H: CONH-R \ 2. PhNMe2 POCI3 t XI ----------- Lu Chang ------------- Order ----- ---- (Please read the back ^ / notes before filling out this page) This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) 1222445 A7 B7 V. Description of the invention (171 Example 4

Ph, / \

2 HCI

NH 2

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs (EX-4A) in a solution of 5-nitro-2,4 (1H, 3H) pyrimidinedione in the dimethyl subordinated job. Add 1.1 equivalents of potassium carbonate in one portion and stir. After about minutes, 1 equivalent of a solution of gasified 2- (trimethylsilyl) ethoxymethane in dimethylsulfene was added dropwise. The reaction mixture was then heated to 40 r and stirred for 18 hours. Treatment of a typical aqueous solution followed by chromatographic purification provided the pure product EX-4A. EX_4B) In a solution of 5-nitro_1-SEM-2,4 (1H, 3H) pyrimidinedione (EX-4A) in dimethylsulfite (0.2 M), I was added in one portion. · Equivalent carbonic acid, and stir. After about 10 minutes, a solution of methyl bromoacetate in dimethylarsine was added dropwise. The reaction mixture was then heated to 40 ° C and stirred for 18 hours. Treatment with a typical aqueous solution followed by chromatographic purification provided the pure product Ex-4B OEX-4C) with hydrogen to make 5-nitro-i-SEM-3-methoxycarbonylmethyl 2,4 (1Η, 3Η) pyrimine A solution of dioxin (EX-4B) in methanol is degassed. Then, 5% Pd / C 'was added to the solution, and the solution was stirred at room temperature for 24 hours under a hydrogen atmosphere. The crude reaction was filtered through a pad of celite 545 and concentrated under reduced pressure. Purification by column chromatography ’to obtain pure 5-amino-1-SEM-3-methoxycarbonylmethyl · 2,4 (1Η, 3Η)

Packing ----- ^ ---- Order --------- line (Please read the precautions on the back before filling out this page> 1222445 Printed by A7 of the Intellectual Property Bureau Staff Consumer Cooperatives of the Ministry of Economic Affairs ~- --------—— V. Description of the invention (172) Pyrimidinedione EX-4C. EX_4D) in% amine small SEM-3_methoxycarbonylmethyl 2,4 (m, 3H) pyrimidine di In a solution of ketone (EX-4C) in tetrahydrofuran and dichloromethane (1: 1, 0.3M), a catalytic amount of acetic acid and i equivalent of phenylacetaldehyde were added. The solution was allowed to cool to 0 ° C. in an ice bath, and an equivalent of sodium triethoxylate borohydride was added in one portion. After stirring for 5 minutes, the ice bath was removed and the reaction mixture was stirred at room temperature for 2 hours. The reaction was quenched by the addition of INNaOH, and the mixture was stirred for 5 minutes. Typical water falling treatment followed by chromatographic purification provided the pure product EX_4D. EX-4E) at 1-SEM-3 · methoxycarbonylmethyl_5 · (2 · Phenylethyl) amino_ 2,4 (1Η, 3 嘧) pyrimidinedione (EX-4D) in a solution of tetrahydrofuran and methanol (丨: 1, 02), add 1 A solution of equivalent lithium hydroxide in water. After the reaction is completed, the volatiles are removed under reduced pressure. The residual aqueous solution is cooled in an ice bath and acidified with 1.0NHC1 to a pH of 1. Extracted with an organic solvent, and The solvent was removed under reduced pressure to obtain the pure product EV_4E. EX-4F) at 1-SEM-3-methylenecarboxy-5- (2-phenylethyl) amino-2,4 (1H, 3H) A solution of pyrimedione in dimethylformamide (01 M ^, 5 equivalents of N, N-diisopropylethylamine, 1 equivalent of hydroxybenzotriazole and 1 equivalent of ι_ [3_ (dimethylformate) Amino) propyl] -3-ethyl carbon Diimine hydrochloride. Stir the resulting mixture for 30 minutes. Then, treat the reaction mixture with 1 equivalent of the appropriate amine and stir it overnight. Treat with a typical aqueous solution followed by purification by chromatography to obtain the pure product EX-4F EX-4G) in 1-SEM-3 · Methylene urea-5- (2-phenylethyl) amino-2,4 (1Η, 3Η) pyrimidinedione in tetrahydrofuran (0.3 M) Then, a solution of 2 equivalents of tetrabutylammonium fluoride in tetrahydrofuran was added. The resulting solution was refluxed for several hours. -175- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) Packing ----- ^ ---- Order --------- Line (Please read the (Please fill in this page for attention) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

A7 B7 V. Description of the invention (173) After treatment with a typical aqueous solution, followed by chromatographic purification, a pure product EX-4G was obtained. EX-4H) in 3-methylenecarboxamide-5_ (2-phenylethyl) amino-2,4 (1H, 3H) pyrimidinedione (EX-4G) To the solution (0.3 M), add 1 mole of Mole to the scales. The resulting solution was refluxed for several hours. After treatment with a typical aqueous solution, followed by chromatographic purification, pure product AX-4Η was obtained. Εχ · 4Ι) in 2-chloroyl methylenechiamine-5 (2 · phenylethyl) amino-2,4 (1Η, 3Η) pyrimidinedione (ΕAX-4Η) in dioxolane To the solution (0.3 M), 2 equivalents of phenyl mercaptan was added. The resulting solution was refluxed for several hours. After treatment with a typical aqueous solution, followed by chromatographic purification, pure product AX-4I was obtained. With tritium gas, make 2-phenylthio-3-methylene chloramine-5- (2-phenylethyl) amino-2,4 (111,311 &gt; dense lake dione (^ (-41 ) Degassing the solution in methanol and 4] ^ 1 ^ 1 dioxolane (3: 1, 0.1 M). Then, 5% P (j / c) was added to the solution, and it was placed under a hydrogen atmosphere at Stir for 24 hours at room temperature. Filter the crude reaction through a pad of celite and concentrate under reduced pressure. Purify by column chromatography to obtain pure product. Example 5

Ph &gt; EX-5A) in the 2-chloro-3-methylene group S &amp; amine-5- (2-phenylethyl) amino group--176- ----------- pack ----- ： ---- Order --------- line (please read the L note on the back? Matters before filling out this page) 1222445 Α7 Β7 V. Description of the invention (174) 2,4 (m 3H) Pyrimidinedione and 1 equivalent of 3-pyridinedihydroxyborane in a degassed solution (0.5 M) in 1-propanol, 1.2 equivalents of 2.0 M sodium carbonate were added, followed by 1 mole. /. (Triphenylphosphine) palladium. The resulting mixture was heated to reflux for several hours. After cooling to room temperature, a typical aqueous solution was processed, followed by chromatographic purification to obtain pure product EX-5A. Under nitrogen, make 2- (3-0 than yodoyl) -3_methylene amines 5- (2-phenylethyl) amino-2,4 (1H, 3H) pyrimidinedione (EX -5A) Degassing in a solution of methanol and 4MHC1 dioxolane (3: i, 0.1 M). To this solution, 50 / was added. pwc, and this grain solution was left in the rat's atmosphere at room temperature for 24 hours. The crude reaction was filtered through a pad of celite 545 and concentrated under reduced pressure. Purify by column chromatography to obtain pure product. Pyrimidolones having, for example, a directly bonded 2-aryl, 2-heteroaryl, or 2-heteroatom linking / bonding organic group through the heteroatom to the pyrimidinone ring can also be prepared using Figure 7 below. In this reaction scheme, an aryl group is introduced by forming a carbon-carbon bond. Heteroatoms suitable for forming hetero-linked arylpyrimidone include sulfur, nitrogen, oxygen, or another suitable heteroatom. The general procedure of Scheme 7 to prepare specific heteroatom-substituted pyrimidinones is disclosed in Examples 6 and 7. ----------- install ----- ^ ---- order --------- line (please read the precautions on the back before filling this page) Bureau of Consumer Cooperatives Prints Moderate Rule Sheet Paper Rule 4 A IS) § quasi-standard home country 21 t 77 public 97 1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of invention (175) Figure 7 : Scream of Substitution_Synthesis

-178- (Please read the precautions on the back before filling in this page'_installation ---- l · --- order --------- line * This paper size applies to Chinese National Standard (CNS) A4 Specifications (210 X 297 mm) 1222445 A7

Example 6

(EX-6A) 2-thiouracil (66.7 g, 52.5 mmol) was dissolved in a sodium hydroxide solution (41.6 g of solid NaOH in 365 ml of water). Then, the mixture was treated with methyl iodide (37 ml, 583 mmol), and the resulting reaction mixture was stirred at room temperature for 16 hours. Then, the solution was acidified with glacial acetic acid (30 ml). The white precipitate was collected by suction filtration, and the solid was washed several times with cold water and dried to obtain 74 g of ex_6A in a quantitative yield as a white crystalline solid. (EX-6B) A solution of EX-6A (74.0 g, 520.5 mmol) in glacial acetic acid (2275 ml) was cooled to 0 ° C in an ice bath and treated with Br2. The reaction mixture was allowed to warm to room temperature and stirred for 16 hours. A yellow precipitate formed, which was filtered and washed three times with ether. Take 62. . Yield, 97.2 g of EX-6B was isolated. (EX-6C) The mixture of calcium hydride in THF was cooled to zero. (:, And treated with pure EX-6B, followed by pure tert-butyl bromoacetate. The reaction mixture was stirred at 0 ° C. for 1 hour. Then, after the mixture was allowed to warm to room temperature, the reaction mixture was stirred 2 Hours. The reaction mixture was heated to reflux temperature, after __- 179- This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 public love) ----------- pack --- ----- Order --------- line (please read the t note on the back? Matters before filling out this page) Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 Preparation of A7 B7 V. Description of the invention (177) 16 hours. After cooling the reaction mixture to room temperature, slowly pour the mixture into a 1 liter ice-water slurry. The quenched mixture was extracted with dichloromethane (3 X 500 ml). The organic layers were combined and washed with water and brine. After drying and filtering the organic layer with MgS04, the volatile components were removed in the air, and 28.81 g (90%) of EX-6C was obtained as an off-white solid. , Is a mixture of N-regularized and 0-fluorinated isomers (9: 1). N-alkylated isomers: 1H NMR (30 0 MHz, CDC13) β 8.07 (s, 1Η), 4.75 (s, 2Η), 2.57 (s, 3Η), 1.47 (s, 9Η); 13CNMR (75MHz, CDC13) (ί 165.1, 162.7, 158.4, 152.5, 108.3, 83.7, 46.8, 28 · 2 (3C), 15.5; HRMS (E1) calculated for C! IHuBrNsC ^ S: 335.0065, measured: 335.0077. (EX-6D) In an argon-filled glove box containing magnetic In a 12-ounce Fischer-Porter bottle of the stir bar, add EX-6C (5.00 g, 15.0 mmol), Pd (OAc) 2 (168 mg, 0.75 mmol, 5 Mol.), Racemic -ΒΝΝΑΡ (654 mg, 1.05 mmol, 7 mole%), Cs2C03 (6.84 g, 21.0 mmol) and anhydrous and degassed toluene (65.0 ml). To this mixture was added isopropylamine (3.00 ml , 35.2 millimoles). The bottle was capped with a pressure head equipped with a pressure gauge and removed from the glove box. The closed system was heated in an oil bath of 118_12 (rc, and then magnetically stirred for 16 hours. A headspace pressure of ~ 10 psi developed during the reaction. Remove the Fischer_Porter bottle containing the reaction mixture from the oil bath, allow it to cool for 30 minutes, and vent to argon flow System, and by sampling syringe .LCMS analysis showed 35% product and 65% starting substance residue. Under argon, the pressure head was removed, and the reaction mixture was treated with Pd (OAc) 2 (337 mg, u mM, 10 mol%), racemic · ΒΙΝΑρ ^ 〇〇 克 '1.6 halo Mohr's 11 Mohr 0 / 〇), Cs2c〇3 (i.00 grams, 30.7 millimoles) Pack ----- ^ ---- Order --------- line (please First read the note on the back? Matters and then fill out this page) This paper size is applicable to China -180- * public 97 2 X 1ϋ u ¾ c / · * 1222445 Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Instructions (178) and isopropylamine (6.00 ml, 70.4 mmol). Cap the bottle with a pressure head, heat it again to 118-120 ° C, and magnetically stir for 16 hours. The sampling procedure was repeated and LCMS showed that the reaction was complete. The reaction mixture was cooled to room temperature and filtered through a medium frit glass frit funnel. The solid was washed thoroughly with toluene and discarded. The filtrate was concentrated and purified by flash chromatography (Merck 230-400 mesh Si02, 10% ethyl acetate in hexane) to give 380 g (81% yield) (EX_6D) as yellow Brown solid: iHNMR (300 MHz, CDCI3) d 7.05 (s, 1H), 4.74 (s, ZH), 3.44 (seventh peak, J = 6.3 Hz, 1H), 2.53 (s, 3H) , 1.47 (s, 9H), 1.21 (d, J = 6.3 Hz, 6H); 13 C NMR (75 MHz, CDC13) d 165.7 (s), 158.7 (s), 147.4 (s), 130.5 (s ), 123.6 (d), 82.9 (s), 45.9 (t), 44.1 (d), 28.0 (q), 22.1 (q), 14.8 (q); Calculate HRMS (ESI) of C14H24N3S0303 [M + H] + = 314.1538, measured 値 314.1539. (EX-6E) In an argon-filled glove box, in a 3-ounce Fischer-Porter bottle containing a magnetic stir bar, add EX-6D (1.00 g, 3.20 mmol), 3-nitrophenyldihydroxy Borane (634 g, 3.80 mmol), Cu (I) -2-tetraphenocarboxylate (1.21 g, 6.37 mmol) and Pd (PPh3) 4 (100 mg, 0.86 mmol, 2.7 Mole%). THF (25 ml) was added and the bottle was capped with a pressure head equipped with a pressure gauge and removed from the glove box. This closed system was heated in an oil bath at 70 ° C, and then magnetically stirred for 16 hours. The reaction mixture was allowed to cool to room temperature 'aerated and diluted with acid (200 liters). The mixture was filtered through a medium frit frit glass funnel. The green solid was washed with ether (100 ml) and discarded. The filtrate was concentrated and purified by flash chromatography (Merck 230-400 mesh Si02, 10% ethyl acetate in hexane to 30/0) to give 961 mg (78% yield) EX_6E, yellow Foam: iHNMR (300MHz CDCl3) d839 (s, ___ -181- This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 public love) ---------- -# 装 ---- l · --- Order --------- line t (Please read the phonetic on the back? Matters before filling out this page) Printed by the Intellectual Property Bureau Staff Consumer Cooperatives of the Ministry of Economic Affairs 1222445 A7 _ B7 V. Description of the invention (179) 1H), 8.31 (d, J-8.1 Hz, 1H), 7.86 (d = 7.8 Hz, 1H), 7.64 (t, J = 8.1 Hz, 1H) 7 15 (bs, 1H), 4.51 (s, 2H), 3.58 (seventh peak, j = 6 0 to m), i gene &amp; 9H), i knife ("J = 6.3Hz, 6H); calculated for C19H25N40〆HRMS (ESI)値 ρν [+ Η] + = 389.1815, measured 値 389.1825. (EX-6F) In a 250-ml round-bottomed flask equipped with a magnetic stir bar, EV-6E (755 mg '1.9 ¾ mole) and difluoroacetic acid (30 ml) were added. The mixture was dried in a wind flowing atmosphere and at room temperature; dropped for 30 minutes, and concentrated on a rotary evaporator. The residue was triturated with ether (50 ml) and co-evaporated with heptamate (2 x 50 ml) to obtain 801 mg (95% yield) of EX-6F as a transparent yellow glass material: 1H NMR (300 MHz , DMSO_d6) d 8 · 34_8 · 26 (m, 2Η), 7.89 (d, J = 7.8 Hz, 1H), 7.76 (t, J = 7.9 Hz, 1H), 7.20 (s, 1H), 4.51 ( s, 2H), 3.57 (seventh peak, J = 6.6 Hz, 1H), 1.17 (d, J = 6.6 Hz, 6H); Calculate HRMS (ESI) for q 51 ^ 7N4 05 free state base 値 [M + H] — = 333.1223, measured 値 333.1199. Prepared from EX-6F according to the procedure described for the precursor of CBZ-protection: 1H NMR (300 MHz, CDC13) d 9.34 (bs, 1H), 8.32 (s, 1H), 8.14 (d, J = 8.0 Hz, 1H), 7.81 (t, J = 7.8 Hz, 2H), 7.53 (d, J = 7.8 Hz, 2H), 7.47 (t, J = 7.8 Hz, 1H), 7.39-7.25 (m, 5H), 7.08 (s, 1H), 7.00 (d, J = 7.8 Hz, 2H), 5.12 (s, 2H), 4.61 (d, J = 7.8 Hz, 1H), 4.35 (s, 2H), 4.21 ( m, 1H), 3.50 (seven peaks of d, 8 lines, J = 6.3 Hz, 1H), 1.22 (d, J = 6.3 Hz, 6H); 13 C NMR (75 MHz, CDC13) d 168.5 (s), 167.4 (s), 164.0 (s), 158.6 (s), 148.2 (s), 143.8 (s), 142.6 (s), 136.6 (s), 136.2 (s), 135.0 (d), 133.4 (s), 133.2 (s), 129.9 (d), 128.7 (d), 128.3 (d), 127.8 (d), 127.5 (d), 124.4 (d), 124.1 (d), 121.8 (d), 67.4 (t), 49.9 (t), 44.1 (d), 43.2 (t), 22.4 (q); Calculate HRMS (ESI) of C3 i H3 2N7 06 値 [M + H] +: 598.2463, found 値 598.2414. _-182-_ This paper size applies to China National Standard (CNS) A4 specification (210 χ 297 mm) ----------- installed -----: ---- order --- ------ Line ^ ΙΓ (Please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7 ___—______ B7 V. Description of Invention (18〇) According to SC- The method described in 81703, produced from EX-6G: 1H NMR (300 MHz, CD3 OD) d 9.25 (bs, 1H), 8.97 (m, 1H), 8.78 (bs, 1H), 7. 93- 7.14 (complex m, 9H), 4.77 (s, 2H), 4.51 (s, 3H), 3.66 (m, 1H), 1.30 (d, 6.3 Hz, 6H); HRMS for C2 3 H2 8N7 02 ( ESI) calculated 値 [M + Hf = (598 free state base) 434.2304, measured ， 434.2318. Example 7

NH (EX-7A) uses the same procedure described for EX-6E and is made from EX-6D, with the exception of the Cs2C03 base. Therefore, EX_6D (213 mg, 0.68 mmol), pyridine-3-dihydroxyborane, 1,3-propanediol cyclic ester (166 mg, 1.02 mmol) and Cs2C03 (771 mg '2.37 mmol) 'After flash chromatography (Merck 230-400 mesh Si02, 2% MeOH in CHC13), 143 mg of EX-7A (61% yield) was obtained as a slightly yellow glass material: dNMRpOOMHACDClJ d 8.79-8.66 (m, 2H ), 7.90-7.26 (complex m, 3H), 7.16 (s, 1H), 4.53 (s, 2H), 3.57 (seventh peak, J = 6.3Hz, 1H), 1.44 (s, 9H), 1.27 ( d, J = 6.3Hz, 6H); Calculate HRMS (ESI) of C18H25N403 値 [Μ + Η] + = 345 · 1927, measured 値 345.1928 〇 (ΕΧ-7Β) using the same procedure described in EX-6F, Manufactured from Εχ-7Α (143m-183- This paper size applies to China National Standard (CNS) A4 specifications (210 X 297 public love) ------------ installation ---- r-- --Order -------Line (Please read the phonetic on the back? Matters before filling out this page) 1222445 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ------ B7__ _ V. Description of the invention. 81) grams, 0.41 millimoles) to give 212 mg (100% yield) of EX-7B as a yellow foam : 1H NMR (300 MHz, CDC13) d 8.72-8.64 (m, 2H), 7.95-7.89 (m, 1H), 7.62-7.52 (complex m, 2H), 7.42-737 (m, 1H), 7.20 (s, 1H), 4.52 (s, 2H), 3.57 (seventh peak J = 6.3Hz, 1H), 1.18 (d, J = 6.3Hz, 6H) ;, H14 (ESI) calculation of C14H17N403 値 [M + H ] +289.1301, found 289.1296. (EX-7C) Using the same procedure as described for CBZ-protected substances, made from EX-7B to obtain EX-7C; for C30H32N7O4i HRMS (ESI), calculate [M + H] + = 554.2516, measured 554.2523 . Using the same procedure described in Example 6, from EX-7C, the product was obtained. Example 8

NH2 According to the method of Example 6, the title compound was prepared: Calculate [M + H] + 446.2304 for HRMS (ESI) of C24H27n70.2 and find 値 446.2309. Methylene analog of pyrimidinone, in which methylene is present, as an alternative to the acetamidocarbonyl group at the position of the ketone N-3, can be used as shown in the following detailed description accompanied by special example 9 8 M-general methylene pyrimidinone preparation method. -184-This paper size applies to China National Standard (CNS) A4 specification (210 X 297 mm) ------------ φpack ---- l · --- order ---- ----- Line φ. (Please read the back ^ / notes? Matters before filling out this page> 1222445 A7 B7 V. Description of the invention (182) Scheme 8: —General methylene pyrimidinone synthesis Ministry of Economy wisdom Printed by the Property Agency Staff Consumer Cooperative

------------ φ installed ---- l · --- order --------- line Φ- (please read the t-voice on the back? Matters before filling out this page) This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 mm) 1222445 Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, Invention Description (183

ΝΗ Εχ-9Α) in [[5-[(Eryloxycarbonyl) amino] 1phenyl each keto group;!, 6_dichloro] _ranyl group) Ethyl tetrahydrofuran and dichloromethane (1: 1, 0 · 3 M), add a catalytic amount of acetic acid and 1 equivalent of an appropriate amine. The solution was allowed to cool to 0 in an ice bath. (: And 1 equivalent of sodium triethoxylate borohydride was added in one portion. After stirring for 5 minutes, the ice bath was removed, and the reaction mixture was stirred at room temperature for 2 hours. The reaction was made by adding 1 NNaOH Quench and stir the mixture for 5 minutes. After treatment with a typical aqueous solution, followed by chromatographic purification, the pure product Εχ_9Α〇Εχ-9B) was provided in [5-[(fluorenylamino) amino] · 2 · phenyl To a solution of -6-fluorenyl-1,6-dihydropyranoyl] acetamidine (E × -9A) in methanol (0.2 M), 10% Pd / C was added in one portion. The resulting mixture was stirred under an atmosphere of hydrogen (cylinder) at room temperature; stirred for about 16 hours. The crude reaction mixture was passed through celite 545 as a whole and the solvent was removed under reduced pressure. The residue was triturated from diethyl ether to obtain pure product EX-9B. EX-9C) in [5-amino · 2-benzyl-6-alanyl-1,6-diazine-1-ranyl] acetamidine (EX-9B) in tetrahydrofuran and dichloromethane (1 : In a solution of 1, 0.3 M), a catalytic amount of acetic acid and 1 equivalent of phenylacetaldehyde were added. Allow the solution to cool in an ice bath. 186- This paper is sized to the Chinese National Standard (CNS) A4 (21〇X 297 mm). ---- K ---- Order --------- Line _ (Please read the precautions on the back before filling this page> 1222445 A7 V. Description of the invention (彳 84) to 0 ° C, and add 1 equivalent of sodium triethoxylate borohydride in one portion. After stirring for 5 minutes , The ice bath was removed, and the reaction mixture was stirred at room temperature for 2 hours. The reaction was quenched by the addition of 1 N NaOH, and the mixture was stirred for 5 minutes. After a typical aqueous solution treatment, it was then purified by chromatography to provide pure Product EX_9C. [5_ (2-Phenylethyl) amino_2_phenyl-6-g isopropyl-1,6-dihydro-1-pyridyl] acetamidine at 4 MHC1 The solution in mash (0.2 M) was stirred for several hours. After the reaction was completed, the volatile materials were removed under reduced pressure. Trituration with ether and purification of the residue gave pure product 5. Pyrimidone sulfonyl group was similar The sulfonyl group is present as an alternative to the ethylaminoamine carbonyl group at the N-3 position of the pyrimidinone, which can be made using procedures generally based on those disclosed in Figures 1-5, Qi Fang It is N-Boc-formamyl-propane amine methylammonium diamine, which replaces the aminoformamidine of Li dimethoxyethylamine. For example, N- (4-formamyl Fluorenyl) -2-aminomethylcarbamidine. Using this route, the sulfo analogue of Example 10 can be prepared. Example 10 Packing ---- K ---- Order ------- -(Please read the notes on the back before filling this page)

1222445 A7 B7 V. Description of the Invention (185) Example 11

. Mi Dian § The same as the three p-one ketone analogs, in which nitrogen is present, as a substitute for the carbon at the 4-position of 17 Mi Dianone, which can be used as shown in Figure 9 detailed below with special example 12 " 4-Aminopyrimidone preparation method ". (Please read the precautions on the back before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -188- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the Invention (186) Scheme 9: General 4_azapyrimidone synthesis

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

----------- • Install ---- j ---- Order --------- ^ • 1 (Please read the precautions on the back before filling this page) This paper Standards are applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) 1222445 A7 V. Description of the invention (187) &gt;%

Example 12

NH NH '

CH3PhS03H EX-12A) a solution of glycine tert-butyl ester hydrochloride (1 mmol) in methane gas to vaporize benzamidine (1 mmol) and triethylamine (2 mmol Moore) processing. The reaction mixture was stirred at room temperature for 6 hours. The mixture was washed with water and extracted with methane gas. The combined organic layers were dried over MgS04. After the volatiles were removed in the air, the pure product Ex_12A was isolated. EX-12B) A mixture of N-benzylpyridine glycine tertiary-butyl ester Q mmol; ε 12-12), Lawesson's reagent (0.5 mmol) and toluene was heated to ⑽ 乇 for 16 hours. The reaction mixture was concentrated under reduced pressure. Purified on silica gel by column chromatography to obtain pure product EX-12B. EX-12C) a mixture of N-thiobenzidine glycine tertiary-butyl ester (1 millimolar: ε × 12B) in one gas, and trimethylphosphonium tetrafluoroborate (1.1 millimol Mohr), treated at -78 ° C. After the reaction mixture was stirred for 2 hours, the mixture was washed with NaHC03 (aqueous solution) and extracted with dichloromethane. The combined organic layers were dried over MgS04 and filtered. After the volatile organic components are concentrated, the desired product EX-12C is isolated. EX-12D) A solution of N-thiomethylamidinyl glycine tert-butyl ester (1 mmol; Ex-12C) in methanol was treated with europium (1 mmol). Remove in the air ----------- • install ----- ^ ---- order --------- (Please read the back ^ / Zhuyin? Matters before filling in (This page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1222445 A7

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the Invention (188) Volatile substances, and the desired compound EX-12D was isolated without further purification. EX-12E) A mixture of the compound EX-12D (1 millimolar) and ethyl thioamidate acetate (1 hamol) in methanol was heated to reflux temperature for 4 hours. Precipitation of colorless crystals occurred, and the desired product Ex_12E was isolated by suction filtration. A solution of the compound EX-12E (1 mmol) and pyridine (5 mmol) in acetonitrile was treated with a solution of p-toluenesulfonium chloride (3 mmol) in acetonitrile. The reaction mixture was stirred at -10 ° C to 0 ° C for 3 hours. After completion of the reaction, a white precipitate was formed. Crystals of the desired product EX_12F were isolated by suction filtration. EX-12G) Trifluoroacetic acid was added to a mixture of compound EX-12F (1 mmol) in toluene ether at 0 ° C. The reaction mixture was at 0. (Stir at 3 hours for 1 hour. Extract the reaction mixture with an organic solvent. Remove the organic solvent under reduced pressure to obtain the pure product EX-12G. EX-12H) The compound EX-12G (1 mmol), EDC (1.3 Millimoles) and HOBT (1.3 millimoles) were mixed in DMF, and the mixture was stirred at 20 ° C for 15 minutes. To this mixture, [[(4-aminomethylphenyl) iminomethyl] amino] carbamic acid benzyl hydrogen chloride (1.3 mmol) and DIEA (1.3 mmol) Solution in DMF. After treatment with a typical aqueous solution, it is then purified by chromatography to provide the desired product, EV-12Η. The compound EX-12Η (1 mmol), p-toluenesulfonic acid monohydrate (1 亳 Mol), and 10% Pd / activated carbon (0.1 mmol) were mixed with methanol. The mixture was stirred for 2 hours under a hydrogen atmosphere, which was introduced and maintained through a rubber balloon. __ -191-This paper size is applicable to China National Fresh (CNS) A4 (21G X 297mm) — ^ (Please read the precautions on the back before filling this page) -Packing ----- ^ ---- Order --------- line one 1222445 A7 B7 V. Description of the invention (189) After filtering off the catalyst and removing methanol, the desired product is separated. (Please read the notes on the back before filling out this page) The Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs has printed compounds of the formula (I) of the present invention with a base, a sulfur Sf · and an amino group, which can be converted into many derivative. Alternatively, the derivatized compound of formula (I) can be obtained by first derivatizing one or more intermediates during the preparation process before further converting the derivatized intermediate into a compound of formula (I). The side groups in alcohol or various forms can be easily converted into esters of carboxylic acid, sulfonic acid, aminomethyl acid, phosphonic acid and squatting acid. Tritiation to form a carboxylic acid ester can be easily accomplished using a suitable tritiated reagent, such as a fatty acid anhydride or phosphonium chloride. Corresponding aryl and heteroaryl acid livers and phosphonium chlorides can also be used. This reaction is usually carried out using an amine catalyst, such as leaf b lake, in an inert solvent. Similarly, aminomethyl esters (urethanes) can be obtained by reacting a hydroxyl group with an isocyanate and carbamic acid chloride. Sulfonates, phosphonates and phosphates can be made using their corresponding rhenium chloride and similar reagents. The compound of formula (I) 'having at least one thiol group can be classified similarly to alcohols and g, using the same reagents and equivalent reaction conditions, and converted into its corresponding thioester derivative. Compounds of formula (I) with the presence of at least one primary or secondary amine can be converted into their corresponding amidine derivatives. The amidines of carboxylic acids can be made using appropriate ammonium chlorides or anhydrides under similar reaction conditions to those used for alcohols and phenols. The ureas of the corresponding primary or secondary amines can be made directly using isocyanate and amine formamidine in the presence of an acid scavenger such as triethylamine or pyridine. Sulfonamides can be prepared from their corresponding sulfonium chloride in the presence of aqueous sodium hydroxide or tertiary amines. Appropriate procedures and methods for the preparation of these derivatives can be found in House's Modern Synthetic Reaction (w A Benjamin), Systematic Review of Organic Compounds by Shriner, Fuson and Curtin, 5th Edition (John Wiley &amp; Sons), and Organic synthesis reagents of Fieser and Fieser, -——__ -192- The standard of Chinese, National, and National Standards (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (19〇) 1 (John Wiley &amp; Sons). A wide variety of reagents that can be used to derivate the hydroxyl groups of compounds of formula (I), (please read the notes on the back before filling out this page) thiols and amines can be obtained from commercial sources or the references cited above. For reference. The compound of formula (I) of the present invention, which has hydroxyl, thiol and amine functional groups, is printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, and can be sintered to form a wide variety of derivatives. Alternatively, the alkylated compound of formula (I) can be obtained by first alkylating one or more intermediates during the preparation process before further converting this alkylated intermediate to a compound of formula (I). The hydroxyl group of the compound of formula (I) can be easily converted into ethers. Alkylation to form ethers can be easily accomplished using suitable alkylating agents, such as alkyl bromides, alkyl iodides, or alkyl sulfonates. The corresponding aralkyl, heteroaralkyl, alkoxyalkyl, aralkoxyalkyl and heteroaralkoxyalkyl bromides, iodides and sulfonates can also be used. This reaction usually uses reagents that can form alkoxides, such as sodium hydride, potassium tert-butoxide, sodium amine, lithium amine, and n-butyl bell, and uses inert polar solvents such as DMF, DMSO, THF, and the like An amine catalyst equivalent to a solvent, such as P ratio, is performed in an inert solvent. Compounds of formula (I) having at least one thiol group can be converted into their corresponding thioether derivatives similarly to alcohols and amidines, using the same reagents and equivalent reaction conditions. A compound of formula (I) 'having at least one primary, secondary or tertiary amine group present can be converted into its corresponding secondary, tertiary or quaternary ammonium derivative. The quaternary ammonium derivatives can be made using suitable bromides, decomposers, and esters similar to those used in alcohols and tests. The conditions involve the reaction of the amine by preheating it with the calcining reagent, using the stoichiometry of the amine (meaning using a tertiary amine as one equivalent, using a secondary amine as two equivalents, and using a primary Amine is three equivalents). When using primary and secondary amines, both ___ -193- scale is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (191) (Please read the back first Note of note? Please fill in this page again.) Use two and one equivalent of acid scavenger individually. Secondary or tertiary amines can be produced from their corresponding primary or secondary amines. Primary amines can use aldehydes, such as formaldehyde and sodium cyanoborohydride, which are dialkylated by reductive amination in the presence of glacial acetic acid. The primary amine can be monoalkylated by protecting the amine immediately, such as trifluoroacetamidine, by first protecting the amine. Alkylating agents, such as dimethylsulfate, in the presence of non-nucleophilic tests, such as Barton's test (2-third-butyl-1,1,3,3-tetramethylguanidine), will obtain Monomethylated protected amine. Removal of the protecting group with an aqueous potassium hydroxide solution will give the desired monoalkylated amine. Other suitable procedures and methods for preparing these derivatives can be found in House's Modern Synthetic Reaction (WA Benjamin), Systematic Identification of Organic Compounds by Shriner, Fuson and Curtin, 5th Edition (John Wiley &amp; Sons), and Fieser Organic Synthesis Reagent with Fieser (published by John Wiley &amp; Sons). Perfluoroalkyl derivatives can be prepared as described by DesMarteau in J. Chem. Soc. Chem. Cornnmn. 2241 (1998). A wide variety of reagents are available for derivatizing the hydroxyl, thiol, and amines of compounds of formula (I), which are available from commercial sources or the references cited above, which are incorporated herein by reference. The results of the aforementioned synthetic pathways for the preparation of pyrimidone by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, which are derived from nucleophilic substituents (such as those that can exist in B, ΕΛίΙ2 and YG), are shown in Table 1. For special examples 13 to 19. The special examples listed below should be regarded as just a wide variety of possible illustrative examples for a person skilled in the art, and not as a limitation. -194- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (192) Table 1. Pyrimidone structure made by general derivatization procedures, N, B ' Η, Ν, kN Η General Structure Example No. 13 R2 Phenyl BA-methoxyethylfluorenyl γΟ 14 Phenyl 4-methylbenzyl 15 Phenyl 4-nitrobenzyl 16 Phenyl isobutyl Alkyl 17 18 19 Phenylphenylphenyl 2,4,6-trimethylbenzyl Benzylfluorenylethylfluorenyl 4-fluorenylfluorenyl 4-fluorenylfluorenyl 4-methylfluorenyl Fluorenyl 4-methylfluorenylbenzyl 4-methylfluorenylbenzyl 4-methylfluorenylbenzyl 4-fluorenylaminofluorenyl

TF-VIIa test printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs in this cooperative test, 100 nM recombinant soluble tissue factor virtual 1 ^-nJVi recombinant human Vila factor was added to the 96-well test plate, Its phi human ..., s has 0.4 mM substrate N-methacryl-D-phe-gly-arg-p-acylaniline, and inhibitors or buffers (5 mM CaCl2, 50 mM Tris-HCl , PH 8.0, 100 mM NaCl (100 / BSA). This reactant 'was measured in a volume of 100 microliters immediately at 4 micrometers to measure the background absorbance. The plate was incubated at room temperature for 60 minutes. At this time, p-nitroaniline was released at 405 nm by monitoring the reaction to measure the hydrolysis rate of the substrate. The percentage inhibition of TF-VIIa activity was calculated from the OD4Q5nm 値 of experimental and control samples. 1222445 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

Xa detection: 0.3nM human Xa factor and 0.15mMN -... benzyloxycarbonyl-D-sperminefluorenyl-L-glycinamine spermine-p-nitroaniline-dihydrochloride (S-2765) , Added to a 96-well assay plate, which contains an inhibitor or buffer (5010 ^ 11118-HC1, pH 8.0, 100 mM NaCl, 0.1% BSA). This reaction, in a final volume of 100 microliters, was measured immediately at 405 nm to determine the background absorbance. The plate was incubated at room temperature for 60 minutes. At this time, p-nitroaniline was released at 405 nm by monitoring the reaction to measure the hydrolysis rate of the substrate. The percentage inhibition of Xa activity was calculated from OD4Q5nm 値 of experimental and control samples. Thrombin test Add 0.28 nM human thrombin and 0.06 mMH-D-amphetamine hexahydropyridine hydrazine cardioline-p-nitroaniline dihydrochloride to 96-well test The plate contains an inhibitor or buffer (50 mM Tris-HCl, pH 8.0, 100 mM NaCl, 0.1% BSA). This reaction was measured in a final volume of 100 microliters at 405 nanometers to determine the background absorbance. The plate was incubated at room temperature for 60 minutes. At this time, by monitoring the reaction, p-nitroaniline was released at 40 μm, and the hydrolysis rate of the substrate was measured. The percentage inhibition of thrombin activity was calculated from the 0d405 of the experimental and control samples. Trypsin Assay Add 5 μg / ml trypsin (obtained from porcine pancreas) and 0.375 g of N-benzylidene cardiac arginine-p-succinylphenylaniline (L_BApNA) to 96 -Well detection plate 'which contains an inhibitor or buffer (5〇 ^ 丁 也------------- ^ 装 ----- ^ ---- Order ----- ---- Line (Please read the notes on the back before filling in this page)

1222445 A7 _B7 _ 5. Description of the invention (194) HC1, pH 8.0, 100 mM NaCl, 0.1% BSA). This reaction, in a final volume of 100 microliters, was measured immediately at 405 nm to determine the background absorbance. The plate was incubated at room temperature for 60 minutes. At this time, p-nitroaniline was released at 405 nm by monitoring the reaction to measure the hydrolysis rate of the substrate. The percentage inhibition of trypsin activity was calculated from the OD405nm 値 of experimental and control samples. Recombinant soluble TF, consisting of amino acids 1-219 of the mature protein sequence, was expressed in E. coli and purified using Mono Q Sepharose FPLC. Recombinant human Vila was purchased from US Diagnostica (Greenwich CT), and the chromogen receptor N-methylsulfonyl_D-phe-gly-arg-p-nitroaniline was prepared by American Peptide Company (Sunnyvale, CA). Factor Xa was obtained from the Enzyme Research Laboratory (South Bend IN), thrombin was obtained from Calbiochem (La, Jolla, CA), and trypsin and L-BAPNA were obtained from Sigma (St. Louis MO). The chromogen receptors S-2765 and S-2238 were purchased from Chromogenix (Sweden). The bioactivity of the compounds of Examples 1 to 19 was determined in Table 2 when measured using a bioassay procedure. (Please read the precautions on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -197- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 1222445 A7 B7 V. Description of the invention (195) Table 2. Inhibitory activity of pyrimidinone on factor Xa, TF-VIIA, thrombin Π and trypsin Π (Please read the precautions on the back before filling this page) Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs -198- Example No. TF-VIIA IC50 (αM) Thrombin II IC50 (uM) Factor Xa IC50 (uM) Trypsin II IC50 (uM) 1 15.4 22.4 — 0.5 2 &gt; 30 &gt; 30 — &gt; 30 3 1.0 1.0 — 0.6 4 1 — — — 5 — — — — 6 0.05 43% @ 30 uM 33% @ 30 uM &lt; 0.04 7 0.7 11.3 33% @ 30 uM 0.04 8 0.08 42% @ 30 uM 15% @ 30 uM 0.04 9 — — — One 10 One — One — 11 — — One — 12 One — One — 13 — One — One 14 — — One — 15 — One — — 16 — — One One 17 — — — — 18 — — — — 19 — — — — This paper size applies to China National Standard (CNS) A4 Grid (210 χ 297 mm)

Claims (1)

1222445 Patent Application No. 089109595 Chinese Patent Application Replacement (July 1993) A8 B8 C8 D8 K, Application by Chunli Wei ~~ 1 · A compound having the formula Or a pharmaceutically acceptable salt thereof, wherein: B is an unsubstituted or substituted phenyl, CrCs alkyl, alkoxy, or C3-C6 cycloalkyl, wherein the substituent is selected from the group consisting of alkyl and nitrate Group consisting of bases; A is a covalent bond,-(CH2) r-,-(CH2) r _S02 ·, -C (O)-, or -C (0)-(CH2) r-, where r is selected An integer from 1 to 4; R is phenyl, thiophenyl, or pyridyl, unsubstituted or one or more selected from amine, alkoxycarbonyl, carboxy, and (: 1- &lt;: 6 alkylamine Substituted with a carbonyl group; K is-(CH2) n-, where η is an integer selected from 1 to 4; E0 is -C (0) -NH-, -NΗ-, or -S02-NH-; Q is -C (NH) NH2 or -C (0) NH2. 2_ The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of ethyl, propyl, isopropyl, trimethylene, tetramethylene Base, butyl, second-butyl, third_butyl and this paper size are applicable to Chinese National Standard (CNS) A4 specification (210 X 297 public love) 1222445 A8 B8 C8 D8 6. Apply for patent Fanyuan isobutyl A is a single covalent single bond; R2 is phenyl, 2-p specific fluorenyl, 3-ρ specific fluorenyl or 4-p specific fluorenyl, unsubstituted or selected from one or more carboxyl and amine groups , Methoxycarbonyl, and ethoxycarbonyl; and K is C Η 2 and EG is -C (0) N Η. 3. The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of 3-methylphenyl, 4-methylphenyl, and phenyl; A is selected from the group consisting of CH2, CH2CH2 &amp;CH2CH2CH2K; R2 is thiophenyl, 5-amino-3 -methoxycarbonylphenyl, 3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5 -Aminophenyl, 3-methoxycarbonylphenyl, phenyl, 3- ° specific phenyl or 4-methylamino. 4. The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is phenyl, unsubstituted or substituted with one or more groups selected from methyl and ethyl A is selected from the group consisting of a single covalent single bond, CH2 and CH2CH2; R2 is selected from the group consisting of: phenyl, 2-pyridyl, and 3-esigma, unsubstituted or via one or Substituted by a plurality of groups selected from the group consisting of an amine group, a carboxyl group, and an oxocarbonyl group. 5. The compound according to item 4 of the scope of patent application, or a pharmaceutically acceptable salt thereof, of which-·-2-This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) 1222445 A8 B8 C8 'Scope of patent application B is selected from the group consisting of 3-methylphenyl, 4-methylphenyl and phenyl; A is selected from the group consisting of CH2, CH2CH2 and CH2CH2CH2A; R2 is selected from the group consisting of 5-amino-3-methoxycarbonylphenyl, 3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-methyl Oxyl phenyl, phenyl, 3-eryl and 4-p-pyridyl. 6. The compound according to item 5 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of 4-methylphenyl and phenyl; A is selected from the group consisting of CH2, CH2CH2 and CH2CH2CH2K The group consisting of: R2 is selected from the group consisting of 3-aminophenyl and phenyl; Y0 is 4-fluorenylbenzyl. 7. The compound according to item 1 of the scope of the patent application, or a pharmaceutically acceptable salt thereof, wherein #K is CH2 and E0 is-(:( 0) · ΝΗ; and R2 is a 3-aminophenyl group, B is a phenyl group, A is CH2, and γ0 is a 4-imidyl group; or R2 is a phenyl group, Bphenyl, A is CH2, and Y0 is a 4-fluorenylbenzyl group. The compound according to item 1, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of ethyl, propyl, isopropyl, butyl, second-butyl, and third-butyl , Isobutyl, 丨 -pentyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 3-fluorenylbutyl, 1-hexyl, 2-hex-3- This paper standard applies to China Standard (CNS) A4 specification (210X297 public director) 1222445 Group, 3-hexyl, 1-heptyl, 2-heptyl and 3-heptyl; R2 is selected from the group consisting of phenyl, thiophenyl, 2-ringyl, 3-pyridyl and 4 -Pyridyl, unsubstituted or substituted with one or more groups selected from the group consisting of acyl, amine, methoxycarbonyl and ethoxycarbonyl; K is CH2; and E0 is -C (0) -NH. 9. The compound according to item 8 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of ethyl, propyl, isopropyl, butyl, 2-butyl, (R) -2-butyl, (S) -2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 4-methyl- 2-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methylbutyl, 2-methylbutyl, (s) -2-methylbutyl and 2-Hexyl; A is selected from the group consisting of a single valence single bond, CH2, CH2CH2 &amp; CH2CH2CHy / ^ a; R2 is selected from the group consisting of: 5-amino-3 -methoxyisopropylphenyl, 3 -Aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-methoxyepiphenyl, thiophenyl, phenyl, 3-p-pyridyl, and 4-mer alpha Fixed base. 10. The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of ethyl, propyl, isopropyl, butyl, and second butyl Base, tert-butyl, isobutyl, 1-pentyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 3-methylbutyl, 1.hexyl, 2-hexyl and 3 -Hexyl, unsubstituted or substituted with one or more groups selected from fluorenyl and ethyl; -4- This paper size applies to China National Standard (CNS) A4 specifications (210X 297 mm) Binding # 1222445 A8 B8 C8 ------ ____D8 6. The scope of patent application A is selected from the group consisting of a single covalent bond, cH2 and ch2CH2; R2 is selected from the group consisting of: phenyl, 2-pyridine And pyridyl, unsubstituted or substituted with one or more groups selected from the group consisting of amine, carboxy, and fluorenyl. 11. The compound according to item 0 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: B is selected from the group consisting of ethyl, propyl, isopropyl, butyl, 2- Butyl, (R) -2-butyl, (s) _2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2 · methylbutyl, 2-methyl · 2-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methylbutyl, 2-methylbutyl, (s) _2-methylbutyl and hexyl; A Is selected from the group consisting of a single covalent bond, ^ and CH2CH2; R2 is selected from the group consisting of: 5_amino_3 -methoxycarbonylphenyl, 3-aminophenyl, carboxyphenyl , 3-carboxy-5-aminophenyl, 3-methoxycarbonylphenyl, phenyl, 3-pyridyl, and 4-pyridyl. 12. A compound according to item 11 of the scope of patent application, or a pharmaceutically acceptable compound thereof Accepted salts, where: B is selected from the group consisting of ethyl, propyl, isopropyl, butyl, 2-butyl, (R) _2 · butyl, (s) _2 -butyl, Tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 4-methyl-2- Methyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methylbutyl, 2-methylbutyl, (S) _2methylbutyl and 2-hexyl; A It is selected from the group consisting of a single covalent bond, ch2 and CH2CH2; -5- This paper size is applicable to SB family standard (CNS) A4 specification (21GX 297 mm)-&quot; Binding # 1222445 Α8 Β8 C8 D8 6. The scope of the patent application R is selected from the group consisting of 3-aminophenyl, 3-carboxyphenyl, 3-methoxy-chimephenyl, phenyl, and 3-ethynyl; Y0 is 4-fluorenyl Benzyl. 13. Compound according to item 1 of the scope of patent application, or complex / acceptable salt, wherein: K is CH2 and EG is -C (0) -NH; and R2 is 3. aminophenyl, B is (S) -2-butyl, A is a single bond, and γ0 is 4-fluorenylbenzyl; R2 is 3-aminophenyl, B is ethyl, A is a single bond, and one is 4 -Fluorenyl group; ~ R2 is 3-aminophenyl group, B is isopropyl group, A is a single bond, and γ0 is April methionyl group; '' 'R is 3-amine basic group' Β Is 2-butyl ', A is a single bond, and γ0 is 4-methylpyridyl;' 'R2 is 3-aminophenyl, B is (R) -2-butyl, a is a single bond, and γ0 is 4-fluorenylfluorenyl, and M is CH; R2 is 3-aminophenyl, B is 3-pentyl, A is a single bond, and γ0 is 4.adenosyl; R2 is 3-amine Phenyl, B is ethyl, AgCH2, and γ is 4-fluorenylfluorenyl; R2 is 3-aminophenyl, B is 2-methylpropyl, A is a single bond, and γ is 4-fluorenylfluorenyl; R2 is 3-aminophenyl, B is tertiary-butyl, A is a single bond, and γ0 is 4-fluorenylfluorenyl; R2 is 3-aminophenyl, B Is butyl, a is a single bond, and γ〇 is each 脒 ______- 6 -The size of this paper applies to China National Standard (CNS) A4 specification (210X 297 public directors) '-------- _ 1222445 A8 B8 C8 ---__ D8 VI. Application scope of patents; R is 3-endylbenzene Group, B is a 2-propyl group, A is a single bond, and γ is a cyclamyl group; R2 is a 3-aminophenyl group, B is a (S) -2-butyl group, and A is a single bond, and γ0 is a 4-fluorenylfluorenyl group; or R is a 3-aminophenyl group, B is an ethyl group, A is a single bond, and γ0 is 4 · Myridyl. 14. The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, Unsubstituted or substituted with one or more groups selected from methyl, ethyl, propyl, and isopropyl; A is selected from the group consisting of a single covalent bond, CH2, CH2CH2, and CH2CH2CH2. R 2 is sulfur. Phenyl, phenyl, 2_bitenyl, 3_pbitenyl or 4-ρbitenyl; K-based CH2; and E0-based &lt;: (0) _ΝΗ 〇1 5 According to the scope of the patent application 14 of the compounds, or a pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, and A is selected from the group consisting of a single covalent bond, A group consisting of CH2, CH2CH2 and CH2CH2CH2; R2 is thiophenyl, 5-amino-3-methoxycarbonylphenyl, 3.aminobenzine. -7- This paper size applies to China National Standard (CNS) A4 specifications (210 X 297 mm) 1 ~~ 1222445 A8 B8 C8 D8 Group, 3-carboxyphenyl group, 3-carboxy group; aminophenyl group, 3-methoxycarbonylphenyl group, 3-p-pyridyl or 4-p-bityl. 16. The compound according to item 1 of the scope of patent application, or a pharmaceutically acceptable salt thereof, wherein: K is CH2 &amp; EG is -C (0) _NH; and R2 is 3-aminophenyl, and B is ring Propyladenosyl group; B is cyclobutyl, A is a single bond, and γ0 is 4 R2 is 3-aminophenyladenosyl group; R2 is 3-aminophenyladenosyl group; R2 is 3-Aminophenylmethylenegiyl; R is 3-aminophenyl is 4-adenosyl; or R2 is phenyl, B is cyclobutyl, A is a single bond, and γ is 4 -脒 基 芊 基. 17. A pharmaceutical composition for inhibiting the symptoms of thrombosis in the blood, comprising the compound according to any one of claims 8, 13, and 16 of the scope of the patent application, and a pharmaceutically acceptable carrier. 18. A pharmaceutical composition for inhibiting the symptoms of thrombosis in the blood, which comprises a compound according to any one of claims 1 to 7, 9 to 12, and 14 to 15 and a pharmaceutically acceptable carrier. 19. A pharmaceutical composition for inhibiting the formation of platelet aggregation in the blood, comprising a therapeutically effective amount according to the scope of the patent application No. 8, 1 A is a single bond, and Y0 is 4_B is cyclopentyl, A Is a single bond, and γ0 is 4_ B is cyclopropyl, A is CH2, and Y0 is 4-B is cyclohexyl, A is CH2CH2, and Y0 -8- This paper size applies to China National Standard (CNS) A4 specifications ( 210X 297 mm) Binding 1222445 A8 B8 C8 ------ £ f., Patent application park and any one of 16 compounds. 20. A pharmaceutical composition for inhibiting the formation of platelet aggregates in blood, comprising a therapeutically effective amount of a compound according to any one of claims 1 to 7, 9 to 12, and 14 to 15 . 21. A pharmaceutical composition for inhibiting thrombosis in blood, comprising a therapeutically effective amount of a compound according to any one of claims 8, 3, and 6 of the scope of patent application. 22. A pharmaceutical composition for inhibiting thrombosis in blood, which comprises a therapeutically effective amount of a compound according to any one of claims i to 7, 9 to 12, and 14 to 15 of the scope of patent application. 23 · —A pharmaceutical composition for treating or preventing venous thromboembolism and pulmonary vascular embolism in mammals, which comprises a therapeutically effective amount according to any one of claims 8, 13 and 16 of the scope of patent application Of compounds. 24.-A pharmaceutical composition for treating or preventing venous thromboembolism and pulmonary thromboembolism in mammals, comprising a therapeutically effective amount according to the scope of application patents 1 to 7, 9 to 12 and 14 to A compound according to any one of 15 items. 25. A medicinal composition for treating or preventing deep vein thrombosis in a mammal, comprising a therapeutically effective amount of a compound according to any one of claims 8, 13 and 16 of the scope of patent application. 26 · —A pharmaceutical composition for treating or preventing deep vein thrombosis in mammals, comprising a therapeutically effective amount of any one of items 1 to 7, 9 to 12, and 14 to 15 Compounds. 27. —A pharmaceutical composition for treating or preventing cardiac thromboembolism in mammals, comprising a therapeutically effective amount according to patent application range -9-This paper standard is applicable to Chinese National Standard (CNS) A4 specifications (210X 297 public -------- 6. Apply for a compound in any one of Fanyuanwei Items 8, 13 and 16. 28. One, for the treatment or prevention of cardiac thrombosis in mammals Said composition 'comprising a therapeutically effective amount of a compound according to any one of claims 1 to 7, 9 to 12 and 14 to 15 of the scope of the patent application. A species for treating or preventing humans and other mammals A thrombotic thrombolytic medicinal composition 'comprising a therapeutically effective amount of a compound according to any one of claims 8, 13 and 16 of the stated patent scope. 30.-A species for treating or preventing humans and other mammals A medicinal composition for a blood test plug for stroke, comprising a therapeutically effective amount of a compound according to the scope of patent applications 1 to 7, 9 to 12, and 14 to 15. 31.-A kind for treating or preventing human and Cancer and cancer chemotherapy linked in other mammals A pharmaceutical composition for the formation of a gold suppository, comprising a therapeutically effective amount of a compound according to any one of claims 8, 13 and 16 of the scope of the patent application. 32.-for treating or preventing humans and other mammals A pharmaceutical composition for thrombosis associated with cancer and cancer chemotherapy, comprising a therapeutically effective amount of a compound according to any one of claims 1 to 7, 9 to i 2 and 14 to 15. 33. -A pharmaceutical composition for treating or preventing restless colic in humans and other mammals, comprising a therapeutically effective amount of a compound according to any one of claims 8, 13 and 16 of the scope of the patent application. 34 -A pharmaceutical composition for treating or preventing restless colic in humans and other mammals, comprising a therapeutically effective amount of items 1 to 7, 9 to 12 and 14 to 15 according to the scope of patent application The combination of any one of -10 · This paper size applies to Chinese National Standard (CNS) A4 specifications (210X297 public directors) 1222445 A8 B8 C8 D8, the scope of patent applications. 35. According to the scope of patent applications No. 1 to 16 Transformation of either Compound, or a pharmaceutically acceptable salt thereof, which is used to inhibit the formation of blood clots in the blood. 36. A compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof , Which is used to manufacture a pharmaceutical used in mammals to inhibit thrombosis, treat thrombosis or prevent thrombosis. 0 -11-This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)