TW473474B - Substituted benzo[de]isoquinoline-1,3-diones - Google Patents

Abstract

Novel compounds of the formula I, in which R, R1 and R2 have the meaning indicated, and their salts or solvates as glycoprotein IbIX antagonists.

Description

473474 A7 B7 V. Description of the Invention (i) This application is a continuation of Part No. 09 / 199,413, the entirety of which is incorporated herein by reference. The present invention relates to substituted phenylhydrazone [de] isojunlin-1,3-dione of formula I

Where R is Η or N02, R1 S-Het, -Het-S02-Ar, -Het-R5, -Het- (CH2) n-Ar, N02, -N = CH-Ar, NHAlk, NAAlk, NHA ' , NA'2 »(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 -YDH, -Y-Ar'-R3, -Y- (CH2) 0-R3, -Y- (CH2) n- (CHR4) -R5, -YC [(CH2 ) 〇-OH] 3, -Y- (CH2) m-NA2, -Y- (CH2) ra-NHA ', -Y- (CH2) 0-OH, -Y- (CH2) k-R6, -Y -(CH2) i-R8 ^ -Y- (CH2) n-Het, -Y- (CH2) n-Ar, -Y- (CH2) n-Ar '-(CH2) i-R6, -Y- ( CH2) nD- (CH2) i-R6 ^ -Y- (CH2) n-Het- (CH2) rR6, -Y- (CH2) n-NA- (CH2) rR6 ^ -Y- (CH2) n-NH -(CH2) i-R6, -Y- (CH2) nD- (CH2) rR8 »-Y- (CH2) n-Ar '-(CH2) i-R8, -Y- (CH2) n-NH- ( CH2) rR8 ^ 4- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474

A7 B7 V. Description of the invention (2) -Y- (CH2) n-NA- (CH2) rR8 -Υ- (〇Η2) η- -Y-tX-COt-tX ^ OK-X2-! ^ Or- Y-tX-NHVX'-OH, R2 is -Ar, -Ar'-DH-, -Het1, -He ^ -Ar, -Ar'-Het1, -Ar '-(CH2) n-R3, -Ar' -Y- (CH2) n-R3, -Ar'-YC (A) 2-R3, -Het1 』3, -Ar'-Het'R3, -Ar,-(CH2) n-R6, -Ar,- S02-Het, -Ar'-NH-S02-Het, -Ar'-S02-R7, -Ar '-(CH2) n- (CO-NH)-(CH2) i-R6, -Ar'-(CH2 ) n- (CO-NH)-(CH2) i-R11, -Ar '-(CH2) n-CO-Het, -Ar'-(CH2) „-(CO-NH)-(CH2) iDH,- Ar '-(CH2) n- (CO-NH)-(CH2) i-Ar, -Ar'-(CH2) n- (CO-NH)-(CH2) i-HetI, -Ar,-(CH2) „-(CH (CN))-(CH2) i-Ar, -Ar '-(CH2) n- (CO-NH)-(CH2) i-CH (Arl) -Ar2, -Ar'-S- ( CH2) n- (CO-NH)-(CH2) i-Ar, -Ar, -S- (CH2) n- (CO-NH)-(CH2) i-R11, -Ar'-S- (CH2) n- (C〇-NH)-(CH2) i-Het1, -Ar'-S- (CH2) n- (CO-NH)-(CH2) i-CH (Ar1) -Ar2 ^ -Ar, -S -(CH2) n- (CO-NHHCH2) iDH, R3 is C (0) A, CONH2, CONHA, CONA2, COOH or COOA, R4 is Ph or OH, R5 is XH3, CH2C1, CF3 or Ph, R6 is NH2 , NHA, NA2, NH (DH) or NH-C (0) A, R7 is NA (DH), NHA, NH (DH) or NA2, R8 is -NH- (C = NH) -NH2, -NH- (C = NH) -NHA, -NH- (C = NH) -NA2, -NA- (C = N H) -NH2, -NA- (ONH) -NHA or -NA- (C = NH) -NA2, R " Department -CH (A) -Ph, -5- This paper size applies to Chinese National Standard (CNS) A4 Specifications (210 X 297 mm) (Please read the notes on the back before filling this page)

Order --------- Line I Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the Invention (3)

Ar · is phenyl, phenyl, phenyl, or pyrazol-4-yl, which is unsubstituted or via A, OH, OA, OCF3, Hal, CN, NH2, NHA, NA2, N02. CF3, S02NH2, S02Ph, S02NAH, 802 ^ 2 single, double or triple substitution,

Ar 'Ar1 and Ar2 are each phenyl, biphenyl, fluorenyl, pyridyl, pyridyl, dolyl, 1-imidazolyl, pyrazolyl, hydroindenyl, and benzo [1,3] di Hexazol-5-yl, diphenylphosphofuranyl, 9-H-fluorenyl, 9-H-carbazolyl, [1, Γ, 4 ', 1 "] Third phenyl, anthracenyl, fluorene- 丨基, 荅 -2_, or 苐 -9-one-2-yl, which are unsubstituted or substituted with a, 〇Η, OA, OCF3, 〇, Ph, 0-Ph-CH3, CH2-Ph, 0- CH2-Ph, Hal, CN, NH2, NHA, NA2, N02, CF3, S02NH2, S02Ph, S02NAH, S02NA2 or R8 single, double or triple substitution,

Het is a saturated, partially or completely unsaturated mono-, bi- or tricyclic heterocyclic group, with 5 to 13 ring circles, of which 1 or 2 N and / or 1 or 2 Lu or 0 atoms may be present, and hetero The cyclic group may be mono- or double-substituted by CN, Hal, OH, 0A, CF3, A, NO, oxygen or R5, wherein the pyrazole is not bonded through N,

Het1 is an unsaturated mono-, bi- or tricyclic heterocyclic group having 5 to 13 ring members, of which 1 or 2 N and / or 1 or 2 S or 0 atoms may be present and / or may be Hal, A , OH, OA, oxygen or CF3 or hexachloro p-pyridine, morphine, p-pyridine or p-pyridin-2-one, single or double substitution, A is unbranched with 1 to 8 C atoms Or branched alkyl, A, is an unbranched or branched alkyl having 2 to 6 C atoms,

Aik is an unbranched alkyl group with 4 to 8 C atoms, D is a cycloalkylene or cyclohexene-1 radical with 4 to 7 C atoms, -6- This paper size applies Chinese national standards ( CNS) A4 size (210 X 297 mm) (please read the note P on the back before filling this page)

A7

473474 V. Description of the invention (4)

Hal is F, C 1, B r or I, and X ′ X1 ′ X2 is an alkylene group having i to 2 c atoms in each case, Y is 0, S, N Η or NA, and i is 0 , 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12, k is 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12, and m is 0 , 1 or 2, η is 0, I, 2, 3 or 4, 0 is 丨, 2, 3, 4, 5, 6, 7, 8, 9 or 10, t is 0, 1 or 2, and u is 1 Or 2, wherein if R2 is a 4-gas phenyl group, R1 is not _NH-CH2-CH2-OH and is pharmaceutically tolerant to salts and solvates. Similar compounds with the parent structure of phenylhydrazone [de] isoxoline-1,3-dione are disclosed in US 4,200,752, FR 2 272 215, FR 2 271 216 A, Chemical

Abstracts, Vol. 73, No. 2, 13 July 1970, Chemical Abstracts, Vol. 57, No. 13, 24 December 1962 and Chemical Abstracts, Vol. Ill, No. 20, 13 November 1989. The present invention is based on the discovery of novel compounds with valence properties, especially their use in the production of pharmaceuticals. It was found that the compounds of formula I and their salts or solvates have very valuable pharmacological and physical properties and are well tolerated. They are particularly useful as GPibIX inhibitors, and in particular, they inhibit the interaction of this incinerator with the ligand von Willebrand factor (vWF). This effect can be confirmed as described by S. Meyer et al. In J. Biol. Chem. 1993, 268, 2055-20562. In addition, the GPIbIX receptor can bind α- This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm). -------- Order --------- line (please first Read the notes on the back and fill in this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (5) Prothrombin (NJ Greco, Biochemistry 1996, 35, 915-921). Compounds block this effect. Many authors (such as Z. M. Ruggeri in Thromb. Hemost. 1997, 78 6 11 -6 1 6) have described the significance of GPIbIX as an adhesion receptor on platelets, which is bound to the expressed vWF mediator The initial interaction of platelets with arteriosclerotically-adjusted vessel walls. Following the GpibIX_vWF interaction, the activation of another platelet adhesion receptor, GPIIbllla, guides platelet aggregation and thus causes thrombotic vessel closure. Therefore, GPIbIX antagonists can prevent the initial effect of thrombosis, and also release active substances from the blood platelet, which, for example, promotes the growth of thrombus and has an additional nourishing effect on the vessel wall. This shows inhibitory peptides or antibodies in different experimental modes (such as H. Yamamoto et al., Thromb. Hemost. 1998, 79, 202-210). In the case of higher shear forces ’(such as J.J. Sixma et al. In Arteri〇scler〇sis,

Thrombosis and Vascular Biology 1996, 16, 64-71) The blocking effect of GPIbIX inhibitors exerts its maximum effect. According to the flow cell method used herein, the compound of formula I can be specialized to inhibit GPIbIX in whole blood. The inhibitory effect of GPIbIX inhibitors on thrombosis can be measured by a modified Born method (Nature 1962, 4832, 927-929), using bottrocetin or ristocetin as an aggregation stimulant. The compounds of formula I according to the invention are therefore useful as pharmaceutically active compounds for human and veterinary use. They can be used as adhesion receptor antagonists, especially as glycoprotein IbIX antagonists, and are suitable for the prevention and / or treatment of thrombotic disorders and their secondary complications. Anticipated best action is thrombosis in the arterial vasculature 'but -8-473474 A7 V. Description of the invention (6) GPIbIX inhibitors also play a role in thrombotic disorders in venous vascular beds. Illness Acute symptomatic arterial syndrome in horses, angina pectoris, myocardial infarction, peripheral circulation disease Ischemic attack during stroke i, arteriosclerosis, angioplasty / transplantation, and closure / restenosis after implantation. The compound may further act as an anti-adhesive substance, with the middle body in contact with foreign objects such as implants, catheters or heart rhythm devices. Comparable drugs are marketed as anti-resistance agents, especially ReOPrQ®. The compounds of formula 1 and their salts and solvates, and a method of preparing these compounds and their salts or solvents ′, servant Nan ^ mchu < million go, characterized by a) formula! Chemical compounds, which are released with a solvent solubilizer or a hydrolyzed functional group derivative, from either or b) a compound of formula 11 R9 I I ------ order ------ (please read the back first Please fill in this page again) Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 〇 Among them,' R9 is Br, N02 or r1, and R has the definition shown in the first scope of the patent application. III Compound Reaction

H2N—R2 III, where R2 has the definition shown in item 1 of the scope of patent applicationa

This paper size applies to China National Standard (CNS) A4 specifications (21 × X 297 public copy A7 B7 V. Description of the invention (7 and if necessary, R9 base is converted to R1 base, or (C) R base and / or R2 and / Or R9 is converted into another R group and / or R2 and / or R9, which are converted to guanidino group by-by the reaction of amidating agent, -I all use _ acid Suzuki coupling method to react aromatic Bromine or cleavage to produce the corresponding coupling product,-reduction of nitro, fluorenyl or thiooxy groups,-etherification of 0H groups or 0A groups for ether cleavage,-alkylation of first or second order amine groups,- Partial or complete hydrolysis of the CN group, cleavage of the g group or esterification of the acid group,-or nucleophilic or electrophilic substitution, and / or (d) conversion of formula I to any of its salts or solvents Compounds of formula VII may have a pair of palm centers and therefore have several stereoisomeric forms. All these forms (such as R and s forms) and mixtures thereof (such as RS forms) are included in formula I. This unknown compound also includes the so-called Prodrug derivatives, i.e. compounds of formula I modified with, for example, alkyl or fluorenyl, sugar or glutin, which can be rapidly cleaved in the body to produce the compounds of the invention In addition, the present invention relates to compounds of formula J, in which the free-form amine group is provided by HEXIX " amino protecting group " (Please read the precautions on the back before filling this page.) -------- Order --------- Printed by the Consumers' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs '10-473474 Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7_ printed by employee consumer cooperatives V. Description of the invention (8) Condensates formed due to their attractiveness. Solvates, such as mono- or dihydrates or alcoholates. The abbreviations used have the following definitions: BOC third Butoxycarbonyl CBZ fluorenyl carbonyl DCC dicyclohexylcarbodiimide DMF dimethylfluorenamine

Et ethyl

Fmoc methoxycarbonyl

Me 曱 基

Mtr 4-methoxy-2,3,6-trifluorenylphenyl OBut tertiary butyl ester OMe methoxy OEt ethoxy POA phenoxyethylfluorenyl

Ph phenyl tert-bu third butyl TFA trifluoroacetic acid In the above formula, A is an alkyl group and has 1 to 8, preferably 1, 2, 3, 4 or 5 carbon atoms. Alkyl is preferably fluorenyl, further ethyl, propyl, isopropyl, butyl, isobutyl, second-butyl or third-butyl, and also amyl, 1-, 2- Or 3-fluorenylbutyl, 1,1-, 1,2- or 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1-, 2-, 3-, or 4-methylpentyl, 1 , 1-, 1,2-, 1,3-, 2,2-, 2,3- or 3,3-dimethylbutyl, 1- or 2-ethylbutyl, 1-ethyl-1-methyl C-11- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ------------------- Order ------- --Line 0 ^ (please read the precautions on the back before filling this page) "474 A7 B7 Printed by the Consumers' Cooperative of the Intellectual Property Bureau of the Ministry of Economy (9) Base, 1-Ethyl-2-A Group, 1,1,2- or 1,2,2-trimethylpropyl, heptyl, 1-, 2-, 3-, 4-, 5-methylhexyl, 1,1-, 1,2-, 1 , 3-, 1, 4-, 2, 2-, 2, 3-, 2, 4- or 3, 3-dimethylpentyl, 1-, 2-, 3-, 4-ethylpentyl 'U, 2-, 1,1,3-, 1,1,4-, 1,2,2-, 1,2,3-, 1,2,4-, 1,3,3-, 1,3,4 -, 1,4,4- or 2,2,3-trimethylbutyl or octyl. A 'is an alkyl group and has 2 to 6 carbon atoms, preferably 2, 3 or 4 carbons Originally, A, preferably ethyl, propyl, isopropyl, butyl, isobutyl, second 'butyl or third-butyl. Aik is unbranched with 4 to 8 carbon atoms T; octyl, preferably n-butyl, n-pentyl, n-hexyl, n-heptyl or n-octyl. A r is preferably phenyl, preferably mono-substituted benzene as shown Group, more preferably phenyl, o-, m- or p-tolyl, o-, m- or p-ethylphenyl, o-, m- or p-propylphenyl, o-, m- or p-phenyl -Cumenyl, o-, m- or p-tert-butylphenyl, o-, m- or p-aminophenyl, o-, m- or p- (N, N-diamidoamino) ) Phenyl, o-, m-, or p-sulfasulfonylphenyl, o-'m- or p-nitrophenyl 'o-, m- or p-hydroxyphenyl, o-, m- or p-formyl Oxyphenyl, o-, m- or p-ethoxybenzyl, o-, m- or p-benzyloxyphenyl, o-, m- or p- (phenylfluorenyloxy) phenyl, o-m- Or p-trigasmethyl) phenyl 'o-, m- or p- (trifluoromethoxy) phenyl, hao-, m- or p-like phenyl, o-, m- or p-chlorobenzene , O-, m- or p-bromophenyl, o-, m- or p-iodine 4-phenylbenzenesulfonyl-phenyl, 4- (4-chloro-phenoxy) -phenyl, and more preferably 2,3., 2,4-, 2,5-, 2,6-, 3 , 4- or 3,5-xylyl, 2,3_, 2,4-, 2,5_, 2,6_, 3,4_ or 3,5_dimethoxyphenyl, 2,3-, 2 , 4-, 2,5-, 2,6_, 3,4_ or 3,5_ Erxianji, 2,3_, 12- This paper is suitable for the standard + National Standard (CNS) A4 (21G X 297) Meal Υ " (Please read the notes on the back before filling in this page) -------- Order ------- Line win 473474 A7 B7 V. Description of the invention (ίο) 2.4-, 2, 5-, 2,6-, 3,4- or 3,5-difluorophenyl, 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5 -Dichlorophenyl, 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or (Please read the notes on the back before filling this page) 3.5-dibromophenyl , 2-Gas-3-fluorenyl-, 2-chloro-4-fluorenyl-, 2-gas-5-methyl-, 2-chloro-6-methyl-, 3-chloro-2-methyl- , 4-chloro-2-methyl-, 5-chloro-2-fluorenyl-, 3-chloro-4-methyl-, 3-gas-5-methyl-, 4-gas-3-tolyl- Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, 2-bromo-3-fluorenyl-, 2-bromo-4-fluorenyl-, 2-bromo-5-methyl-, 2-bromo-6-fluorenyl- , 3-bromo-2-fluorenyl-, 4-bromo-2-methyl -, 5-bromo-2-fluorenyl-, 3-bromo-4-methyl-, 3-bromo-5-methyl-, 4-bromo-3-fluorenylphenyl, 2-iodo-3-fluorene Phenyl-, 2-trans-4-methyl-, 2-fluoro-methyl-5,2-ox-6-methyl-, 3-yloxy-2-fluorenyl-, 4-iodo-2 -Fluorenyl-, 5-iodo-2-methyl-, 3-iodo-4-methyl-, 3-iodo-5-amido-, 4-iodo-3-tolyl-, 2-chloro-3 -Methoxy-, 2-chloro-4-methoxy-, 2-gas-5-methoxy-, 2-gas-6-methoxy-, 3-chloro-2-methoxy-, 4-chloro-2-methoxy-, 5-chloro-2-methoxy-, 3-chloro-4-methoxy-, 3-gas-5-methoxy-, 4-chloro-3- Oxophenyl-, 2-chloro-3-hydroxy-, 2-qi-4-hydroxy, 2-chloro-5-hydroxy-, 2-qi-6-hydroxy-, 3-qi-2-hydroxy-, 4-chloro-2-hydroxy-, 5-chloro-2-hydroxy-, 3-chloro-4-hydroxy-, 3-gas-5-hydroxy-, 4-chloro-3-hydroxyphenyl, 3-fluoro- 4-methoxy, 4-fluoro-3-methyllactate '2 -mouse-3-rat-, 2-milk-4-rat-' 2 -qi-5-rat- '2 -nitro-6- Fluorine-, 3-gas-2-fluoro-, 4-gas-2-fluoro-, 5-gas-2-fluoro-, 3-chloro-4-fluoro-, 3-gas-5-fluoro-, 4- Chloro-3-fluorophenyl, 2-fluoro-3-fluorenyl-, 2-fluoro-4-fluorenyl-, 2-fluoro-5-methyl-, 2-fluoro-6-methyl-, 3- Fluoro-2-methyl-, 4-fluoro-2-fluorenyl-, 5-fluoro 2-methyl-, 3-fluoro-4-methyl-, 3-fluoro-5-methyl-, 4-fluoro-3-fluorenyl-, 2,5- or 3,4-dioxo Phenyl, 2-cyano-4,5-dioxophenyl, 5-gas-2,4-dioxo-phenyl, 2-cyano-3,4-dimethoxyphenyl or -13-benzyl Paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 4/3474 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention ("π) 3,4,5-Trimethoxy- Phenyl. In addition, it is also preferably an unsubstituted biphenyl group as shown or another monosubstituted biphenyl group, more preferably a biphenyl-4-yl group or a biphenyl-3-yl group, and a 2, -methylbiphenyl group. _4_ group, 3'-biphenyl_4_yl, 4, _methylbiphenyl_4_yl, methylbiphenyl_3-yl '3 · methylbiphenyl_3_yl, 4, • Methylbiphenyl_3_yl, 2 · methylbiphenyl-4_yl '3_methylbiphenyl_4 · yl' 2_methylbiphenyl_3_yl, 4 • methylbiphenyl_ 3 groups, 2_second-butybiphenyl-4-yl, 3'-third-butybiphenyl_4_yl, 4__second_butybiphenyl_4_yl, 2 '- Tertiary-butylbiphenyl_3,3, _tertiary-butylbiphenyl_3_, 4 | tertiary-butylbiphenyl_3_yl, 2_tertiary-butylbiphenyl 4-Alkyl-4-yl '3 -Second-butybiphenyl-4-yl, 2-Third-butybiphenyl-3-yl, 4-Third-butylbiphenyl-3-yl, 2, Cumene 4-yl, 3, cumene 4-yl, 4, cumene 4-yl, 2, cumene 3-yl, 3'-isopropylphenyl_3_yl, 4, _isopropylphenyl_3 • yl, cumene-4-yl, 3-isopropylphenyl_4yl, 2_ Isopropylbenzyl, 4-isopropylphenyl-3-yl, 2, -fluorobibenzyl_4-yl, 3, _fluorobiphenylyl, 4'-fluorobiphenyl-4-yl, 2, -fluorobiphenyl-3-yl, 3, _fluorobiphenyl-3-yl, 41-fluorobiphenyl _3_yl, 2-fluorobiphenyl_4_yl, 3-fluorobiphenyl_4_yl, 2-fluorobiphenyl_3_yl, 4-fluorobiphenyl_3_yl, 2, _Methoxybiphenyl-4-yl, 3′-methoxybiphenyl-4-yl, 4, _methoxybiphenyl-4-yl, 2, _methoxybiphenyl-3-yl, 3'-fluorenylbiphenyl_3yl, 4, _methoxybiphenyll_yl, 2-methoxybiphenyl_4_yl, 3_methoxybiphenyl_4_yl, octamethoxy Biphenyl-3-yl, 4-methoxybiphenylyl, 2, _nitrobiphenyl-4-yl, 3, _nitrobiphenyl-4-yl, 4'-nitrobiphenyl_4 _ Group, 2, _ biphenyl nitrobiphenyl- group, 4,-nitrobiphenyl _3_ group, 2 =; group 4_ ---------------- ---- Order --------- line (please read the notes on the back before filling this page) -14-A7 B7 V. Description of the invention (η) group, 3-nitrobiphenyl_4 _Yl, 2-nitrobiphenyl_3_yl, renylbiphenyl_3_yl, 2'-difluorofluorenylbiphenyl_4yl, 3, · trifluoromethylbiphenylyl, tri ^ Methylbiphenyl-4-yl, 2, -trifluoromethylbiphenyl-3-yl, 3, _trifluoromethylbiphenyl-3-yl '4- Fluoromethylbiphenyl_3_yl, 2-trifluoromethylphenyl_4_yl, 3-difluoromethylphenyl_4_yl, 2-trifluoromethylphenyl, trifluoromethyl Phenyl-3-yl, 2'-trifluoromethoxybiphenyl-4-yl, 3, _trifluoromethoxybiphenyl-4-yl, 4'_trifluoromethoxybiphenyl_4_ 2,3-trifluorofluorenyloxyphenyl 3-yl, 3-difluorofluorenyloxybiphenyl-3-yl, 4, trifluorofluorenoxybiphenyl-3-yl, 2-difluoromethoxy Biphenyl _4_, 3 _ trifluoromethoxybiphenyl _ Consumers' cooperation of Intellectual Property Bureau of the Ministry of Economic Affairs Du printed 4-based, 2-based, 2-based, 2-based, 3-based, 3-based, 4 Radical, 2 radical, 2 radical, 3 radical, 3 radical, 4, radical, 3 ′ 4-yl, 2-difluoromethoxybiphenyl_3_yl, 4_trifluorophosphobiphenyl_3_ Disubstituted biphenyls such as 2, -fluorenyl-3, -nitrobiphenyl_4-methyl-4'-nitrobiphenyl_4,2, _fluorenyl_5, _ Nitrobiphenyl_4__methyl-6'-nitrobiphenyl-4-yl-fluorenyl-4'-nitrobiphenyl_4_yl • methyl-6'-nitrobiphenyl-4- -Methyl-3'-nitrobiphenyl_4_yl-methyl_4'_nitrobiphenyl_3_yl-methyl-6'-nitrobiphenyl_3_yl-methyl_ 4'-Nitrobiphenyl_3-yl-methyl-6'-nitrobiphenyl-3- 3'-fluorenyl-2'-nitrobiphenyl_3methyl-5'-nitrobiphenyl_4_4'-fluorenyl-2'-nitrobiphenyl_4_2'-methyl -3'-nitrobiphenyl_3_ 2'-fluorenyl-5'-nitrobiphenyl_3_ 3'-methyl-2'-nitrobiphenyl_3_ 3 '-methyl-5'-nitro Biphenyl_3_4'-methyl-2'-nitrobiphenyl_3_-methylnitrobiphenyl-3-yl'2, -methoxy-2-methylbiphenyl_4-oxo Methyl-2-methylbibenzyl_4-yl, 4, _methoxy_2_methylbiphenyl _Fluorobiphenyl_4 group, 2'-chloro-4'-fluorobiphenyl_4_yl, 2, _chloro_5, _fluorobiphenyl_4_yl, -15- This paper size Applicable to Zhongguanjia Standard (CNS) A4 specification ⑵G X 297 Public Love ------------------- Order --------- Line (Please read the back first (Notes on this page, please fill in this page) 473474 V. Description of the Invention (η) ^ Chloropsinofluorobiphenyl. 4-yl, 3, chloro. 2, _fluorobiphenyl winteryl, 3, _chloro-rat Ki · 4 -ki, 3 丨-教 -5, # 妒 poorgan, ^, lice 5_qi such as phenyl-4-yl, 3, -chloro_6: fluoro-linked 4 ί_4_yl, 4, _qi · 2, _Fluorobiphenyl_4-yl, 4'-chloro-3 ,. Fluorobiphenyl. 2,3, -Gas 3'-fluorobiphenyl-3-yl, 2, 'Chloro Fluorine _3_yl, fluorenylbiphenyl-3-ylfluorobiphenyl_3yl, ν_gas · ^ biphenyl-3-yl, 3, chlorobiphenyl-3-yl, 3 | _Chloro_5, _Gasylbenzyl-3-yl, 3, _chloropyridine-fluorobibenzyl_3_yl, 4, _Gas_2, -fluorobiphenyl_yl, 41-Gas _3'_fluorobiphenyl_3_yl, (2,, 3, _dimethoxy) biphenyl_4_yl, (2,4methoxy) biphenyl_4_yl, (2 ,, 5, _dimethoxy) biphenyl-4-yl, (2 ', 6'_dimethoxy) biphenyl-4-yl, (3,, 4, _dimethoxy) Bibenzyl-4-yl, (3,, 5, _dimethoxy) bibenzyl-4-yl, (2,, 3, _dimethoxy) biphenyl-3-yl, (2 ,, 4, -dimethoxy) biphenyl-3-yl, (2,, 5, _dimethoxy) biphenyl-3-yl, (2,, 6'-dimethoxy) Biphenyl_3-yl, (3,, 4, _dimethoxy) biphenyl-3-yl, (3 ', 5'-dioxyl) biphenyl-3-yl, (2 ', 3'-bis (trifluoromethyl)) biphenyl-4-yl, (2,, 4'_bis (; tri | 1methyl)) biphenyl-4-yl, (2', 5'_bis (trifluorofluorenyl)) biphenyl-4-yl, (2 丨, 6, -bis (trifluoromethyl) ) Biphenyl-4-yl, (3 ·, 4 · -bis (trifluoromethyl)) biphenyl-4-yl, (31,5, bis (trifluoromethyl)) biphenyl_4 _Yl, (2 ', 3, -bis (trifluoromethyl)) biphenyl-3-yl, (2', 4'-bis (trifluoromethyl)) biphenyl-3-yl, ( 2 ', 5, -bis (trifluoromethyl)) biphenyl-3-yl, (2 ·, 6'_bis (trifluoromethyl)) biphenyl-3-yl, (3', 4 , Di (trifluorofluorenyl)) biphenyl-3-yl, (3,, 5, -bis (trifluorofluorenyl)) biphenyl-3-yl, (2,2'_difluorenyl) Biphenyl-4-yl, (2,3'-dimethyl) biphenyl-4-yl, (2,4 ^ (dimethyl) biphenyl-4-yl, (2,2'_ Dimethyl) bibenzyl-3-yl, (2,3 '_ (dimethyl) biphenyl-3-yl, (2,4 ^ dimethyl) biphenyl-16- This paper is for China National Standard (CNS) A4 Specification (210 X 297 mm) (Please read the precautions on the back before filling out this page) Order --------- Line Win Economy Intellectual Property Bureau Employee Consumption Cooperative Printed Economy Printed by the Consumer Cooperatives of the Ministry of Intellectual Property Bureau, 473474. A7 V. Description of Invention (14) Base-3-base. In addition, it is also preferable that the benzyl-2 sulfo-5-yl group, 9-H-carbazolyl group, quinolinyl group, diphenylfluorenylfuranyl group, 9_H_thyl group, 7_bromo_yang-wan-2-yl group , 9H-fluorene-9-one-1: yl, fluorene-9-one-2-yl, imidyl, fluorenyl, 1-imidazolyl, pyrazolyl, 9-11-carbazolyl, [1,1 ,, 4 ', 1 "] Third phenyl, anthracenyl'fluoren-1-yl'naphthalene-2: yl, 4-bromo-pyridin-1-yl, 4-cyano-1-yl' 4-gas Tea-1-yl, 4-nitrothenyl, 4-methoxynaphthyl-2 -yl, 6-isochloro-1-yl, 7-hydroxyfluoren-1-yl, 8-hydroxynaphthyl-1- or hydrazone base. In addition, Ar is preferably p to 唉 _2_ group, p to bite _ 3- group, leaf dagger-4-yl, leaf drazol-3-yl, pyrazol-4-yl, or pyrazole_ 5-yl, pyrimidin-2-yl, pyrimidine-cardiyl, .pyrimidin-5-yl, which is unsubstituted or substituted with a or Hal, and Ar is particularly preferably pyridin-2-yl, pyridin-3-yl, 4-chloro-p-pyridine_2-yl, 1-methyl p-pyridyl-4-yl or pyrimido-2-yl. AW is preferably phenylene, phenylene, phenylene or pyrazol-4-yl, which is unsubstituted or monosubstituted with A, 0H, 0A, CF3, 0CF3, or Hal. Unsubstituted phenylene or 1-naphthyl, 2-methoxyphenyl, 2-methylphenyl, 3-phenylene, 4-phenylene or methylpyrazole _ The base is very good.

Ar1 and Ar2 are eighth with better definition in each case !. Ar1 and Ar2 are particularly preferably phenyl. In -Ar'-D-H, 'Ar' is preferably an unsubstituted or substituted phenylene group, and d has the following preferable or particularly good definition.

-17- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) —I --------------- Order ·· -------- (Please read the note on the back before filling out this page)

473474 A7 _ ^ _ B7_ V. Description of the Invention (15) The best of -Ar'-D-H. In -Ar'-Het1, Ar 'is preferably unsubstituted or substituted phenylene. Het1 has any one of the preferable or particularly good definitions described below.

CH, • 18- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) ------.-------------- Order ---- ----- line (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

473474 Α7 Β7 V. Description of the invention (16)

The -Ar'-Het1 is particularly preferred. In -Ar'-Y-C (A) 2-R3, Ar 'is preferably an unsubstituted or substituted biphenyl group, wherein R3 is preferably an alkoxycarbonyl group and A has the above-mentioned preferred definition. ch ^ 0C2h5 is particularly good for -Ar'-Y-C (A) 2-R3. In -Ar '-(CH2) n-R3, Af is preferably unsubstituted or substituted phenylene, phenylene, phenylene, or pyrazol-4-yl, and R3 is preferably amidamine Group, fe acid amine group or dinoic acid amine group, alkyl group, oxoyl group, or fe compound group and η may be 0, 1, 2, 2, 3, or 4. (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

ΝΗ.

OCH / (CH2) 2- ^ rC3H7 p -〇 Η -19- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (17)

〇 (CH2) 2 — ^:

Ο—Ν -CH3 Η

N- (CH2) 2Η, ch3: CH ch3 3 -〇

CH 2 'o o 0 (Please read the notes on the back before filling this page) (ch2) 3-

NH 2 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

NH, O

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 _B7 V. Description of the invention (18) 0

Particularly preferred for Ar '-(CH2) n-R3. In Ar'-Y- (CH2) n-R3, Ar 'is preferably an unsubstituted or substituted phenylene group, γ in true is preferably S or ◦, and R3 is preferably amidino or alkylamino Or a dialkylamino, alkoxycarbonyl or alkoxy group and n may be 0, 1, 2, 3 or 4. -21- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---------- 1 -------- Order -------- -(Please read the notes on the back before filling this page) A7 V. Description of the invention (19 B7 g, CH2—c〇NH — (CH2) 2-C (CH3) 3

CH2 '~~ CONH—C3H7 nh2 or

ch2—i (o

NK to seven, -Y- (CH cut is particularly good. For -Ar'-HetLR3 ^ A # ^ T, A »" is preferably unsubstituted or substituted n where Het 丨 has the following Jiao_ 3 There is no preferred definition of the base J, and R3 is preferably a base.

or

(Please read the notes on the back before filling out this page.) Order. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. -Ai ^ HeP-R3 is an excellent person. In -Ar .- (CH2) n-R6, Ar is preferably an unsubstituted or substituted phenylene or a biphenylene, and R6 is preferably an amino group, an alkylamino group, a dialkylamino group, or Alkoxy number amine group and η may be 0, 1, 2, 3 or 4. -22 · This paper size is applicable to China National Standard (CNS) A4 specifications (^ 7297), 473474, A7 _B7_ V. Description of the invention (2)

-OQ b-Q

nh2 I

(Please read the precautions on the back before filling out this page.) For -Ar ’-(CH2) n-R6 is particularly good. In -Ar'-S02-Het, Ar 'is preferably an unsubstituted or substituted naphthyl group or a phenylene group, and Het has any of the preferred definitions shown below. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-23- The size of this paper is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (21) Right-Ar'-S02-Het is an excellent one. In -Ar'-NH-S02-Het, Ar 'is preferably an unsubstituted or substituted phenylene', and Het is particularly preferably a 5-methoxy-pyrimidin-2-yl group.

ρ · Η > \ Η3 The pair -Ar'-NH-S02-Het is particularly good. In -Ar'-SOyR7, Ar 'is preferably an unsubstituted or substituted fluorenyl group. Among them, R7 is preferably a amine group, a diamine group, a cyclic amine group, or a cyanide group. _

------------------- Order --------- line (please read the precautions on the back before filling this page) Staff Consumption of Intellectual Property Bureau of the Ministry of Economic Affairs The cooperative prints the best of -Ar'-S02-R7 series. In -ArMCHAJCONHHCHA-R6, Ar is preferably unsubstituted or substituted and substituted by phenyl. Among them, R6 is preferably an amino group, an alkylamino group, a dioxanyl group, or a cycloalkylamino group and η may be 0. , 1, 2, 3, or 4 and i can be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12. -24- This paper size applies to China National Standard (CNS) A4 (210 X 297 Public Love 473474 A7 B7

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

CONH- (CH2) 2 V. Description of the invention (22) / (CH2) 2-CONH- (CH2) 3-N (CH3) 2 (CH2) 2- CONH- (CH2) 4-NH2

-(CH2) 2- CONH- (CH2) 2-NH2 or -Ar'-CCHJn-iCONHHCHJi-R6 is particularly preferred. In which, Ar ′ is preferably unsubstituted or substituted phenylene, wherein D has any of the following preferred definitions and η may be 0, 1, 2, 3, or 4 and i may be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 120-d -25 · This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) ---- --------------- Order --------- ^ AVI (Please read the precautions on the back before filling this page) 473474, A7 B7 V. Description of the invention (23 )

(CH2) 2- CONH-CH. (CH2) 2- CONH- (CH2) 2 — or

-Ar '-(CH2) n- (CONH)-(CH2) rD-H is particularly preferred. In -Ar'-S- (CH2) n- (CONH)-(CH2) rD-H, Ar1 is preferably unsubstituted or substituted phenylene, wherein D has any of the following preferred definitions and η Can be 0, 1, 2, 3 or 4 and i can be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 °

S-CH〇-CONH or

S—CH2— CONH-(CH2) 2 -ο ———--------------- Order --------- ^ AWI (Please read the precautions on the back before (Fill in this page) To -Ar'-S- (CH2) n- (CONHHCH2) rD-H is particularly good. Printed in -Ar '-(CH2) n- (CONHHCH2) rRn by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, Ar' is preferably unsubstituted or substituted phenylene, of which R11 is -CH (A)- Ph, where A has any of the preferred definitions previously described, Ph is phenyl and η may be 0, 1, 2, 3, or 4 and i may be 0, 1, 2, 3, 4, 5, 6, 7 , 8, 9, 10, 11 or 12. -26- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474, Α7 Β7 V. Description of the Invention (24)

Right-Ar '^ CHdnJCONHHCHdrR11 is particularly good. In -Ar'-S-CCHdn-CCONHHCHJi-R11, Ar1 is preferably unsubstituted or substituted phenyl, wherein R11 is -CH (A) -Ph, where A has any of the foregoing preferred definitions, P h is phenyl and η may be 0, 1, 2, 3, or 4 and i may be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12.

To -Ar'-S-CCHzh-CCONHHCHJrR11 is particularly good. In -Ar '-(CH2) n- (CO) -Het, Ar · is preferably an unsubstituted or substituted phenyl group. Het has any of the following preferred definitions and η may be 0, 1 , 2, 3, or 4.

-27- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --------------------- Order --------- (Please read the notes on the back before filling out this page) 473474 A7 B7 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

V. Description of the invention (25) The -Ar '-(CH2) n- (CO) -Het is particularly good. In -Ar'-CCHDn-CCONHHCHJi-Ar, Ar 'is preferably unsubstituted or substituted phenylene, wherein Ar has any one of the above-mentioned preferred definitions and η may be 0, 1, 2, 3, or 4 And i can be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 1 1 or 12. CONH

Br

(CH2) 2-CONH Br CONH CN

-28- 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) 473474 A7 B7 V. Description of the invention (26) ~ < s

(CH2) 2-CONH

CN

(CH2) 2-CONH- (CH2) f— () —NO.

CONH- (CH2) FactoryNO:

(CH2) 2-CONH-CH2— (Jv

NO.

iONH-CH

NO,

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

/ = N (CH2) 2-CONH-CH2— /) (CH2) 2-CONH- (CH2) j

, (CH2) 2 -CONH-CH2 —N -29- ------- I ----------- Order -------- line (Please read the note on the back first Please fill in this page for more details) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7

N, (CH2) 2 -CONH

-c2h5 'c2h5

CONH -Or '-C2H5, c2h5 »<, (CH2) 2-C〇NH— ^

, CH, CH, 3

, (CH2) 2-C〇NH-CH2

.CH CH 3: ONH-CH,

.CH, CH,, (ch2) 2

-CONH

------------------- Order --------- line (please read the precautions on the back before filling this page) Staff Consumption of Intellectual Property Bureau of the Ministry of Economic Affairs Printed by a cooperative

-30- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (28

CH, (CH2) 2-CONH CH

3 -CH

CH 3 (Please read the notes on the back before filling this page)

3

CH CONH-

3 CH

CH 3

3 (CH2) 2-C〇NH- (CH2) 2

Cl Printed by Employee Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

(CH2) 2-CONH-CH2-

Cl

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (29)

, (ch2) 2-conh- (ch2) 2

-Q Cl

Cl

, (CH2) 2-CONH

/ ch2) 2-conh-ch2

Cl

CONH-CH-

Cl Printed by Employee Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

-32- ------------------- Order --------- Line (Please read the precautions on the back before filling this page) This paper size applies China National Standard (CNS) A4 specification (210 x 297 mm) 473474 A7 B7 V. Description of invention (30)

(CH2) 2-CONH- (CH2) 2 — (ch2) 2-conh-ch2-

CH2) 2-CONH-N > -CI

CH 3 CONH- (CH2) 2-7-CH ------------------- Order --------- line (Please read the precautions on the back first (Fill in this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

CH, This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7

V. Description of the invention (31) CONH I-

, (CH2) 2-CONH · (Please read the precautions on the back before filling this page)

, (CH2) 2-CONH-CH2

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

. (CH2) 2-CONH

Cl _och3

34- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 • B7 V. Description of Invention (32)

, (CH2) 2-CONH

, (CH2) 2- CONH

cf3 CF3 cf3 Cl

ONH

Cl CF, (Please read the notes on the back before filling this page)

CH2) 2-C〇NH_CH2

Cl

Cl CONH-CH2

Cl Printed by Employee Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

Cl (CH2) 2-C〇NH- (CH2)

Cl

Cl Cl r (CH2) 2_c〇NH " CH2

-35- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (33)

CI,

Cl, CI

CONH-CH,

CI

CONH- (CH2) 2— (7 X > -CI

Cl

(CH2) 2- conh ------------------- Order --------- line (Please read the precautions on the back before filling this page) Economy Ministry of Intellectual Property Bureau, printed clothing for consumer cooperative

CONH

Cl

Cl -0

Cl -36- The paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474. Α7 Β7 5. Description of the invention (34)

CH2) 2-CONH ^ VCI

CI

CI

ύτ conh — (/ ν · α

'CONH-CH ί_0

, (ch2) 2-conh- (ch2) 3- (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

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of Invention (35)

, (CH2) rCONH- (CH2) 4—

P〇NH- (CH2) 4

(CH2) 2-CONH- (CH2) 2— < N > —CH CONH- (CH2) r- \ CH3 (Please read the precautions on the back before filling this page)

(CH2) 2-CONH

CH, CH,

CONH

CH 3

Printed by CH Consumer Intellectual Property Bureau, Ministry of Economic Affairs

ch2) 2-conh 3

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474, A7 B7 V. Description of the invention (36)

c2h5 ch2) 2-conh—y / C2H5

CONH-

, (CH2) 2-CONH

CF,

(CH2) 2- conh-ch2

CF,

CONH-CH-

CF,

, CONH

1 /, CF, ------------------- Order --------- line (Please read the precautions on the back before filling this page) Ministry of Economic Affairs Printed by the Intellectual Property Bureau Staff Consumer Cooperative

(CH2) 2-C〇NH-CH2—

Cl

(CH2) 2- conh

Cl -39- This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of the invention (37)

.CONH-CH, " WF Cl CONH Vf

Cl

(CH2) 2- CONH-CH2 < BU Fcr

CONH-CH,

F Cl (Please read the notes on the back before filling this page)

, (ch2) 2- conh- (ch2) 2-

OCH 3

, (CH2) 2- CONH

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs OCH3

-40- This paper size applies to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (38) Printing of clothing by employees ’cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

ocf3

(CH2) 2-C〇NH-CH2— (_ / a · ocf3 (ch2) 2-con

och3

-d

CON

och3

.CONH-iCH ^ — \) 〇CH

(CH2) rCONH * (CH2) 2

F ------------------- Order --------- line (Please read the precautions on the back before filling this page) -41- This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 male f) 473474 A7 B7 V. Description of invention (39)

rC〇NH- (CH2) 2 ~ Qr

F (CH2) 2-CONH-CH2

F

F ------------------- Order --------- line (Please read the precautions on the back before filling this page) Employees of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by Consumer Cooperatives

oph This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 473474 ^ A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (40) -d, OPhp〇nh—

OPh -d

CONH — ([,) 一 〇 — (\ /) ~ CH,

-d

; CH2) 2-CONH

r (CH2) 2- CONH -〇OCH, Ph ------------------- Order --------- line (Please read the precautions on the back first (Fill in this page again)

CONH— O (ch2) 2-conh-ch2 -43 · -Ph This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 Α7 Β7 V. Description of the invention (41)

F, (CH2) 2-CONH

och3

CONH

F good OCH 3

F, (CH2) 2-C〇NH

CH 3, CONH-

CF,

, (CH2) 2- CONH

OCH, CF, ------------------- Order --------- line (Please read the precautions on the back before filling this page) Printed by the Property Agency Staff Consumer Cooperative

CONH

OCH, (CH2) 2-CONH

Tertiary-butyl Tertiary-butyl _44 · This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 'B7 V. Description of the invention (42

CONH

Tertiary-butyl tertiary-butyl CH, -d CONH- (CH2) 2

ch2) 2-conh

och3 ch3 OCH, (Please read the notes on the back before filling this page)

ONH

CH, OCH, OCH,

.CONH- (CH2) j

OCH, printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economy

CH2) 2- CONH- (CH2) 2 CH,

OCH, / (CH2) 2- CONH- (CH2) 2

CH, OCH, or pair -Ar '-(CH2) n- (CONH)-(CH2) i-Ar is a particularly good person-45- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ) 473474 A7 B7

S—CH2—C〇NH- (CH2) 2 S—CH2 C0NH-CH2 5. Description of the invention (43) In -Ar'-S- (CH2) n- (CONH)-(CH2) rAr, Ar 'is more It is preferably an unsubstituted or substituted phenylene group, wherein A r has any of the foregoing preferred definitions and η may be 0, 1, 2, 3, or 4 and i may be 0, 1, 2, 3, 4, 5 , 6, 7, 8, 9, 10, 11 or 12 °

s—CH2——CONH-Br ----------- Cloth -------- Order --------- (Please read the precautions on the back before filling this page ) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

s—ch2——conh-ch2 — // N: 3 3

-46-

.CH CH

-S—CH〇 CONH

CN 1

This paper size applies to China National Standard (CNS) A4 (210 X 297 male f)

473474. A7 B7 V. Description of the invention (44) S-CH2—CONH — ^

S——CH, —CONH

-< > 4-3CH,

S— CH2 ——CONH- (CH2) 2

Cl

S—CH, —CONH

Cl

s——ch2—conh-ch2 ----------- clothing -------- order --------- line (please read the precautions on the back before filling in this Page) Printing of clothing by employees' cooperatives in the Intellectual Property Bureau of the Ministry of Economic Affairs

Cl

Cl-47- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (45) S—CH2 —CONH- ( CH2) 2 -S—CH2—CONH- > • S— CH2 CONH-CH2

CH 3 3

~ ^ lT-〇

CH

S——CH2——CONH

s—CH, — CONH—〇CHl

Cl

s—CH, —c

S—CH, one — 《）-* s—CH2

Cl ----------- clothing -------- order --------- line (please read the precautions on the back before filling this page) 48_ This paper size is applicable Chinese National Standard (CNS) A4 specification (210 X 297 mm) 473474. A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs V. Invention Description (46)

CI

S- ^ CH5-CONH

S—CH, —CONH-CH,

S—CH2-CONH-

S—CH, —CONH

S_CH, — C〇NH- S_ch2—conh-ch2 —

S—CH, CONH

Cl

Cl

Cl Cl

Cl, o. S ch2 CONH- (CH accounts for o, s—CH2——CONH- (CH2) 4 S—CHo——CONH- (CH2) 2

S—CH〇 CONH

3 ----------- clothing -------- order --------- line (please read the precautions on the back before filling this page) -49- This paper Standards are applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (47

S—CHo—CONH

C2H5

S— CH〇 CONH

CF. 3 s—ch2—conh-ch2

-o s—ch2——conh-ch2

CF F 3

Cl (Please read the notes on the back before filling this page)

S— CH, CONH

• F

s—ch2—-conh-ch2

Cl

F Cl

S——CH2——CONH- (CH2) 2-

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs OCH 3

-50- This paper size applies Yin National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (48)

S—CH2—CON S— CH2 CONH- (CH2) 2 s— ch2—conh-ch2

och3

F

-Q. F -o-

S— CHo CONH

F

S— CH〇 CON

F (Please read the notes on the back before filling this page)

s—CH2—CONH S—CH? —CONH / ~ V_s— CH2—CONH -s—CH, — CONH

-Or yOPh -OPh -Qr ^ -Qr

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

S— CH〇-CONH-CHj

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474, A7 B7 V. Description of the invention (49)

S—CH, — CONH

S-CH2——CONH CH, CF,

S—-CH, — CONH

OCH,

OCH, ------------ clothing (please read the precautions on the back before filling in this page) Order --------- line one or

S— CH2——CONH- (CH2) t

OCH3 is printed in -ArXCHDn ^ CONHHCHdi-Het1 by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. 1, 2, 3, or 4 and i can be 0, 1, 2, 3, 4, 5, 6, 7'8, 9, 10, 11 or 12 ° -52- This paper size applies to Chinese National Standards (CNS) A4 specifications (210 X 297 mm) 473474 A7 B7 V. Description of the invention (50)-^ ddd

CONH- (CH2) 2-N

(CH2) 2-CONH- (CH2) Factory N (CH2) 2-CONH- (CH2) 2-N 0

O

(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

O

• 53- This paper size applies to China National Standard (CNS) A4 (210 x 297 public love) 473474 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (51)

S, conh-ch2

CH2) 2-CONH-CH2 1

Or CH2) 2-CONH-CH2—

0 CONH-CH2—Yes-Ari-CCHDn-CCONHMCHJi-Het1 is an excellent one. Among them, Ar1 is preferably unsubstituted or substituted phenylene, wherein Het1 has any of the preferred definitions described below and η may be 0, 1, 2, 3, or 4 and i may be 0 '1, 2 , 3, 4, 5, 6'7'8, 9, 10, 11 or 12 °

s—ch2—- conh- (ch2) 2——n ο

S- S—CH2 CONH-CH2

Or -54- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) (Please read the precautions on the back before filling this page)

Clothing -------- Order .-------- Line I 〇

473474, A7 B7 V. Description of the invention (52

S——CH, — CONH-CH2- vs. -Ar'-SJCHdnJCONHMCHdi-Het1 is an excellent one. In -Ar,-(CH2) n- (CH (CN))-(CH2) rAr, Ar1 is preferably an unsubstituted or substituted phenylene group, wherein A r has any of the foregoing preferred definitions and η Can be 0, 1, 2, 3 or 4 and i can be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 1 1 or 1 2 ° (Please read the (Please fill in this page for attention) -----

ch-ch2IIN

ΧΗCH 3

Order --------- Line < To -Ar ''-(CH2) n- (CH (CN) HCH2) rAr is particularly good. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs ^ t-Ar'-CCHJn-CCONHHCHJi-CHCAr ^ -Ar2, Ar 'is preferably unsubstituted or substituted phenylene, wherein Ar1 and Ar2 each have the aforementioned Any preferred definition and η can be 0, 1, 2, 3 or 4 and i can be 0, 1, 2'3'4, 5, 6, 7, 8'9, 10, 11412 ° -55- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (53

CONH- (CH2) 2-CH

2_v Ό Ό Ό Ό

Or (Please read the notes on the back before filling out this page) To -Ar '.- CCHA-CCONHXCHdi-Ci ^ Arb-Ar2 is particularly good. Printed in -Ar'-S ^ CHdn-CCONHHCHdrCHiArh-Ar2 by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, Ar 'is preferably unsubstituted or substituted phenylene, where Ar1 and Ar2 each have any of Well-defined and η ′ may be 0, 1, 2, 3, or 4 and i may be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12 ° -56- Paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (54)

s—CH2—CONH- (CH2) 2-CH or

s—CH2 —CONH-CHrCH X) Ό 印 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. -Ar'-S-CCHUCONHHCHdi-CHCArh-Ar2 is an excellent one. In the above formula, D is a cycloalkylene group and has 4 to 7, preferably 5 or 6 carbon atoms. The cycloalkylene group is preferably cyclobutyl'cyclopentyl, cyclohexyl, or cycloheptyl, and particularly preferably cyclopentyl or cyclohexyl. In addition, D is preferably a cyclohexyl group. Hal is preferably F, Cl, Br or magnetic. Het1 is preferably a substituted or unsubstituted squean-2-yl or squeak,, soil, mouth card 0 seat-9-based, soul spit-2-yl, remote spit-4-yl., P plug bite -5-yl, qg ρ sitting -2 -yl, l, 2-: iLp ratio ^ -3-8 is the same as -4-yl, 1,2-diamino, pyridazol-3-one_5_ Radical, pyrimidine_2 · yl, benzothiophene_3_yl, 3H-benzidinetrityl t 5 & benzothiazol-2-yl, benzofuran-2-yl, benzofuran_3_ Among them, A 丞, n-Mol-1, pyrrolidin_K-based furan-2-yl, carbazole_9_yl, 3-methylene-tertiary-butcarbazole-9-yl, and , Thiazol-3-yl, 5 _ φ M _ τ ^ [1,3,41 pyrimidazol-2-yl, 5-trifluoromethyl- [1,3,4] -fluorenediazol-2-yl ,] C, 1,5-dimethyl or benzo [1,3] dihumazol-5-yl or hexahydropyridin-1-yl, or pyrrolidin-2-one-1-yl. In addition, -57- wood paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --------------------- Order ----- ---- Line (Please read the phonetic on the back? Matters before filling out this page) 473474 A7 B7

V. Description of the invention (55) -1,2-dihydropyrazol-3-one-4-yl, benzofuran-2-yl, 6-methyl-benzothiazol-2-yl, 2,3 -Dihydro-1H-pyridin-6-yl, 3H-benzotriazol-5-yl, benzothiophen-2-yl, imidazole-1 -yl, or benzofluorene [1,3] dihumidazole-5 -Radical or hexahydro p ratio -1 -radical, is it plin-4 -radical,? Bilo bite -1 -yl or p-pyrrole, the di-2-one-1 -yl is particularly preferred. In -Hel ^ -Ar, Het1 and Ar have any of the above preferred definitions, and Ar is preferably phenyl. For HeP-Ar, 4-phenylthiazol-2-yl, 5-phenyl [1,3,4] -4diazol-2-yl, or 1,5-dimethyl-2-phenyl- The 1,2-dihydropyrazole-3_one-4 ^-group is particularly preferred. Among -Het ^ R3, Het1 is preferably 2,3-dihydro-1H-pyridin-6-yl and R3 is more preferably CO (A). And CH, who is the best of Het1-Ar.

Het is preferably a substituted or unsubstituted 2-or 3 -anyl group, a 2-or 3-p tether, 1 ·-, 2-or 3-pyrrolyl, 1-, 2-, 4-or 5 -Imidazolyl, 3-, 4-or 5-17 than tonyl, 2-, 4_ or 5_ρ 咢 mouth base, 3-, 4-or 5-iso p mouth base, 2-, 4- or 5-pyrimazolyl, 3-, 4-, or 5-isoxazolyl, 2-, 3-, or 4-p than yodo, 2-, 4-, 5-, or 6-methyl. It is preferably 1,2,3.-Sankougui-1-, -4-, or -5-yl, 1,2,4-tri '° sitting -1-, -4-, or -5-yl'1- Or 5-four-ton basis, 1,2,3-11 ditu-4- or -5-base, 1,2,4-p ebjun-3- or -5- -58- This paper size applies China National Standard (CNS) A4 Specification (210 X 297 mm) -------------------- Order --------- Line (Please read first Note on the back, please fill out this page again) Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by 473474 A7 B7 -2- or-5-yl, 1,2,4-pyrimidazol-3- or -5-yl, 1,2,3- > 2-, 3-, 4-, 5- or 6-211-sulfanyl 15-pyranyl, 2-, 3-or 4-4H-thiopiperan Base, 3-or 4-daphthyl, pyrgyl, 2-, 3-, 4-, 5-, 6-or 7-phenylsulfanyl '2-, 3-, 4-, 5-, 6- or 7-phenylfluorenyl, 1-, 2-, 3-, 4-, 5-, 6- or 7-1 fluoren-4 indolyl. 1-, 2-, 4- or 5-benzimidazolyl, 1-, 3-, 4-, 5-, 6-, or 7-phenylhydrazone p-ratio sigma group, 2-, 4-, 5-, 6- or 7-benzene moin 17-synthesis, 3--, 4-, 5--, 6- or 7-benzo-isoisosoryl, 2-, 4-, 5-, 6-, or 7-benzoρ σ seat group, 2-, 4-, 5-, 6-or 7-benzoisoρ plug 17 seat group, 4-, 5-, 6-or 7-benzo-2,1,3-humidazole Base, 1-, 2-, 3-, 4-, 5-, 6, ·, 7-, or 8_ 喳 4 wooden base, 1, 2-, 3--, 4-, 5--, 6-, 7-, or 8 -Isophylline '# base, 1-, 2-, 3-, 4-or 9-leaf spit base, 1-, 2-, 3-, 4-' 5-'6-' 7-, 8- or 9-1? Ya bite base, 3_, 4_, 5-, 6_, 7- or 8-peak ρ Linji, 2-, 4-, 5-, 6-, 7-or 8-ρ Kui β sitting on 11 forests base. Heterocyclyls can also be partially or fully amidated. Het can also be 2,3-dihydro-2-,-3-,-4- or -5-p-furanyl '2,5 -diazine-2-,-3-,-4-or -5 -Branyl '2,5 -diaza- 2-,-3-,-4-or -5-11 sulfanyl, tetrahydro-2-or -3-creanyl, 1,3 -Nisaki n-membered-4-yl, tetrahydro-2-or -3-p cephenyl, 2,3-dihydro-1-,-2-,-3-,-4 -or -5-p ratio p each Radical '2,5 -dimur-1-,-2-,-3-,-4-or -5-p-bilocyl' 2,5--ML-1-,-2-,-3-, -4 -or- 5-p ratio p radicals, 1-, 2- or 3-leaf !: pyrrolyl, tetrahydro- 1-, 2- or 3-p pyrrolyl, tetrahydro-l -, -2- or -4-imidyl, 2,3-dihydro-1_, _2_, -3 -'- 4-,-5-,-6-, -7-1H-W indolyl, 2 , 3-dihydro-1-,-2-,-3-,-4-, or -5-p ratio ° radical, tetrahydro-1-,-3- or -4-p ratio σ radical, 1 , 4-dihydro-1-,-2-,-3- or -4-ρ specific octyl, 1,2,3,4-tetrahydro-1-,-2-,-3-,--59 -This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) -------------------- Order --------- Line ^ 1 ^ · (Please read the notes on the back before filling out this page) Inch "474 A7 B7 V. Description of the invention (57 4, · 5- or -6-p ratio lake base, 1, 2, 3, 6 -four _1_, _2_, _3., _4 6_pyridyl, 1- '2-, 3-, or 4-hexahydropyridyl, p, 2_, 4-azimidyl, 2 ·, 3-, or 4-morpholinyl , Tetrahydro_2_, -3_, or radical '1,4-diazine, glutamyl, 1,3-dioxinyl, _2_, _4_, or _5_, tetrachloro_1-, -3-, or -4-Da-4, hexahydro-1-, _2_, _4_, or _5_ octayl, ^, 2- or 3-hexahydropyridyl, 1,2,3,4-tetrahydro_1_ , _2-, _3-, _4_, 5 6-, -7- or -8-quinolinyl, 1,2,3,4-tetrahydro_1_ '_2_, _3_, _4_, 5 6_, -7- or -8-Isofluorinyl. _ Tetrahydro M-pyrrolyl, 2,3_dihydro_; ιη-indole 4yl, 1 dioxolite i _ 7T Leptide pyridine '2,6-tetramethyl Hexahydroepi-4-yl, 4_morpholinyl, 丨 hexamethylpyridyl, 4-methylhexahydropyridin-1-yl, 4_phenylhexahydropyridyl, 3-yl The hydrogen p-quinolin-1_ group or the 1,2,3,4-tetrahydroiso-jun plin-1_ group is particularly preferred. In -Het-S02-Ar, Het and Ar have any of the above-mentioned comparisons. Good definition, -5-or-3-or Het in Weinan is preferably hexahydro I »

N

N-SO

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. In -H.et-R5, Het and Ar have any of the above-mentioned preferred definitions, in which hexahydro p is more than 4-1,4-diyl and R5 is preferably phenyl, methyl, meclome Trifluoromethyl

N ----; ---------------- Order --------- Line AW. F Please read the notes on the back before filling in this page) -60 -4/34/4

—N N —N N

A7 V. Description of Invention (58) is the best of -Het-R5. In -Het- (CH2) n-Ar, Het & Ar has any of the above-mentioned preferred definitions, wherein Het is preferably hexahydrogen, and the ratio of the diyl group may be 0, 2, 3, or 4 — NN—CH2 ~ NCvN ~~ CH2 ~~ ^ Zy > or the best pair of -Het- (CH2) n-Ar. X and / or X 1 and / or X 2 is an alkylene group and is preferably a methyl group, an ethyl group, a propyl group, or a butyl group, and is also a pentyl group or a hexyl group. Y is preferably 0, S, NΗ, or N A. In -Y- (CH2) n-Het, γ is preferably 0, s, NH or NA, wherein Het has any of the above-mentioned preferred definitions and η is preferably 0, 1, 2, 3 or 4. Factory-NH- (CH2) 2-N 〇 .-NH- (CH2) 3 — ^^ N-CH3

-61- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) i Clothing! ----- Order ------- line (Please read the precautions on the back before filling out this page) Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs.

473474. A7 -------- B7 V. Description of the Invention (59) is the best of -Y- (CH2) n-Het.

In -Y-Ar'-R3, Y is preferably 0, s, NH or NA having any of the above-mentioned preferred definitions and R3 is preferably an alkoxycarbonyl group. Best for -Y-Ar'-R3. In -Y- (CH2) n-Ar, Y is preferably 0, s, NH or NA, wherein Ar has any of the above-mentioned preferred definitions and n is preferably 0, 1, 2, 3 or 4. (Please read the notes on the back before filling this page) Ν = λ

NH-CH 2 '

-NH- (CH2) 3—

-NH-CH o2-nh2 NH- (CH2) 2 — ^ —〇H NH2

-NH-CH 2-0

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

OH -N (CH3HCH2) 2

OH -62-

F The size of this paper is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) ^ / ^ 474 V. The description of the invention (60) is the best of -Y- (CH2) n-Ar. In -Y- (CHA-Ar '-(CHA-R6, γ is preferably 0, s, NH, or Nα: where Ar has the above-mentioned preferred definition, r6 is preferably an amine or alkylamino group and η is 〇, Bu, 2, 4 5 8'9, i〇, ii or 12 ° 'Mi- NH, NH-CH, — or NH-CH, • ch2-nh. Pair -Y- (CH2) n-Ari -(CH2) rR6 is excellent. In -Y- (CH2) nD- (CH2) iV, Y is preferably 0, s, nh $ ΝA, wherein 0 has the above-mentioned preferred definition, and R6 is preferably an amine group. Or read 0, 1, 2, 3 or 4 and $ 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 ° Printed by the Intellectual Property Bureau Employees Consumer Cooperatives of the Ministry of Economic Affairs system

Pair of -Y- (CH2) nD- (CH2) i-R6 Excellent -63- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --------- ---------- Order --------- Line AW. (Please read the note on the back? Matters before filling out this page) 473474 A7 B7 5, 6, 7

-NH- (CH2) 3-N V. Explanation of the invention (61) In -Y- (CH2) n-Het- (CH2) rR6, γ is preferably 0, s, NH or NA, where Het has the A good definition is that R6 is preferably an amino group or an alkylamino group and n is 0, 1, 2, 3, or 4 and i is 0, 1, 2, 3, 4 8, 9, 10, 1.1, or 12. N— (CH2) 3 —NH2 is excellent for -YqCHzVHeWCHA-R6. In -Y- (CH2) n-NA- (CH2) rR6, γ is preferably 0, s, NH, or NA, R6 is preferably an amine group or an alkylamine group, and n is 0, 1, 2, 3, or 4 and i is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12. For -Y- (CH2) n-NA- (CH2) i-R6, _NH- (CH2) 3-N (CH3)-(CH2) 3-NH2 is particularly good. In -Y- (CH2) nD- (CH2) i_R8, Y is preferably 0, S, NH or NA, wherein D has the above-mentioned preferred definitions, R8 is preferably an amine or alkylamino group and η is 0, 1., 2, 3 or 4 and i is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 ° ------------- ------ Order— 丨 —Line (Please read the notes on the back before filling this page)

.nh-ch2 .NH-CH

OR-64- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 public love) 473474 Printed clothing A7 of the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (62) Right -Y- (CH2 ) nD ^ CH2) rR8 is an excellent person. In -Υ-((: Η2) η-Αι · '-((: Η2) Γη8, Y is preferably 0, S, NH or NA, of which Ar' has the above-mentioned preferred definition, and R8 is preferably a guanidino group Or burned. Guanidyl and η is 0, 1, 2, 3, or 4 and i is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12 °

-Y- (CH2) n-Ar '-(CH2) rR8 is particularly preferred. In -Y- (CH2) n-NA- (CH2) i-R8, Y is preferably 0, S, NH or NA, where A has the above-mentioned preferred definitions, and R8 is preferably guanidino or alkylguanidino Whereas η is 0, 1, 2, 3, or 4 and i is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12. For -Y- (CH2) n-Ar '-(CH2) rR8, -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 is particularly good . In -Υ-ίΧ-ΟΙΗΧ ^ ΟΙχ2-: ^ 6, Y is preferably 0, S, NH, or NA, and X, X1, and X2 have the above-mentioned preferred definitions. In addition, R6 is preferably -65- This paper size is applicable to China National Standard (CNS) A4 specifications (2〗 0 X 297 male f) -------------------- Order --------- line (please read the precautions on the back before filling this page) 473474

• N A7 V. Description of the invention (63) Amine group, amine: group or dialkylamino group; t is 0, 1 or 2 and u is 1 or 2. For -Y-tX-OL-tXi-OL-X'R6, -NH- (CH2) 3-0- (CH2) 4-0- (ch2) 3-nh2 is particularly preferred. In addition, 'Y in -Y-tX-NHL-XLOH is preferably 0, s, NH or NA, wherein X and X1 have the above-mentioned preferred definitions and u may be 1 or 2. _NH_ (CH2) 2-NH- (CH2) 2-OH is particularly good for -Y-tX-NHU-X ^ OH. R is preferably Η or N02. R1 is preferably -Het, -Het-S02-Ar, -Het-R5, -Het- (CH2) n-Ar, NO !, -N = CH-Ar, NHAlk, NAAlk, NHA ', NA'2, , R6

NH -YDH, -Y-Ar'-R3, -Y- (CH2) 〇-R3, -Y- (CH2) n- (CHR4) -R5, -YC [(CH2) 0-OH] 3, -Y -(CH2) m-NA2, -Y- (CH2) m-NHA ', -Y- (CH2) 0-OH, -Y- (CH2) k-R6, -Y- (CH2) i-R8,- Y- (CH2) n-Het, -Y- (CH2) n-Ar, -Y- (CH2) n-Ar,-(CH2) i-R6, -Y- (CH2) nD- (CH2) i- R6, -Y- (CH2) n-

Het- (CH2) i-R6J -Y- (CH2) n-NA- (CH2) i-R6, -Y- (CH2) n-NH- (CH2) i-R6, -Y- (CH2) nD- (CH2) i-R8, -Y- (CH2) n-Ar,-(CH2) i-R8, -Y- (CH2) n-NH- (CH2) i-R8, -Y- (CH2) n- NA- (CH2) i-R8,, R6 -Y- (CH2) ri— (-Y-tX-OL-tX ^ OJu-X2-! ^ Or -Y-tX-NHL-X ^ OH, where -Het , -Het-S02-Ar, -Het-R5, -Het- (CH2) „-Ar, -Y-Ar'-R3, -Y- (CH2), -66- This paper size applies to the Chinese National Standard (CNS ) A4 size (210 x 297 mm) ------------------- 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

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 Α7 _______ Β7 V. Description of Invention (64)

Het, -Y- (CH2) „-Ar, -Y- (CH2) n-Ar '-(CH2) i-R6, -Y- (CH2) nD- (CH2) iR, -Y- (CH2) n -Het- (CH2) i-R6, -Y- (CH2) n-NA- (CH2) rR6, -Y- (CH2) nD- (CH2) i-R8, -Y- (CH2) n-Ar ' -(CH2) i-R8, -Y- (CH2) n-NA- (CH2) rR8, -Y- [X-〇] r [xi_0] u_x2_R6 and _y_ [x_nh] u_x1〇h have the above-mentioned best In addition, Ar is preferably 2-hydroxyphenyl in -N = CH-Ar. In NHAlk, Aik has the above-mentioned preferred definition. For NHAlk, NH- (n-C5H 丨 丨) In NAAlk, A and Aik have the above-mentioned preferred definitions, of which N (CH3) _ (n_.C4H9) is an excellent one in NAAlk. In NHA, A 'has the above-mentioned preferred definition. NH_ ( n_C3H7) is particularly good for NHA. In addition, NA and A have the above-mentioned preferred definitions, of which ν ((: 2Η5) 2 is NA'j and especially good. In -YDH, Y is as The R1 substituent is preferably 0, s, or Ni ^ tNA, where D has the above-mentioned preferred definition. Or -1 \ ^-(: 5119 pairs of -YD-H- are particularly preferred. In -y- (ch2) In 0-r3, γ is preferably 0, s, Ν ^^ ΝΑ, in which chi 3 is preferably an alkoxycarbonyl group and 0 may be 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 Or 1 0. -NH- (CH2) 2-C OOMe is especially good for -Y- (CH2) 0-R3. Among -Y- (CH2) n- (CHR4) -R5, Y is preferably 0, s, NH ^ tNA, and R4 is preferably benzene Group or hydroxy group, R5 is preferably methyl, chloromethyl or trifluoromethyl and η is 0, 1, 2, 3 or 4. -67- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------------------- Order --------- ^ AW. (Please read the phonetic notes on the back before filling out this page) 473474 A7 B7

V. Description of the invention (65)

0H -NH 一 ~ (-H or -NH-CH2--Η CH ^ ch2ci is particularly good for -Y- (CH2) n- (CHR4) -R5. Yu-Υ-(: [((: Η2) 0-〇Η] 3, γ is preferably 0, s, where 0 may be 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. -1 ^ 11-(: [(: 112- OH] 3 is particularly good for -Y-CKCHA-OHh. In -Y- (CH2) m-NA2, Y is preferably 0 and s, where A has the above-mentioned preferred definition and m may be 0, 1 or 2. -NH- (CH2) 2_N (C2H5) 2 or _n (CH3)-(CH2) 2-N (C2H5) 2 vs. -Y- (CI ^ U-NAdM ^ Better. In -Y- (CH2.) M-NHA ', Y is preferably 0, s, NH or NA, wherein A' has the above-mentioned preferred definition and m may be 0, 1 or 2. _NH_ (CH2) 2_NH_ (C3H7) vs.- Y- (CH2) m-NHA 'is particularly preferred. Among -Y- (CH2), Y is preferably o's, NH, or NA, where o is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.-; ^ 11-((: 112) 2-〇11 or _NH- (CH2) 5-OH p-Υ-((Η2) 0-〇Η is particularly good In -Y- (CH2) k-R6, y is preferably 0, s, NΗ, or NA, where R6 is preferably an amino group, an alkylamino group, a dialkylamino group, or a cycloalkylamino group and k may be 3, 4, 5, 6, 7, 8, e, 10, liai2 ° _NH- (CH2) 3-NH2, _NH- (CH2) 4-NH2, -NH- (CH2) 5-NH2, -N H- (CH2) 7-NH2, -NH- (CH2) 8-NH2, -NH- (CH2) 3-N (CH3) 2, -NH- (CH2) 3-NH (CH3) 5 -N (CH3 )--68- This paper size is applicable to China 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 473474 A7 B7 V. Description of the invention (66) (CH2) 3-NH (CH3) or- NH— (CH2) 3

NIH

Particularly good for -Y- (CH2) k-R6. In -Y- (CH2) rR8, -γ is preferably 0, s, NH or NA, wherein R8 is preferably -NH- (C = NH) -NH2, -NH- (C = NH) -NHA, -NH- (C = NH) -NA2, -NA- (C = NH) -NH2, -NA- (C = NH) -NHA, -NA- (C = NH) -NA2 and i can be 0, 1 , 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12. -NH- (CH2) 2-NH-C (= NH) -NH2, -NH- (CH2) 3-NH-C (= NH) -NH2, -NH- (CH2) 4-NH-C (= NH ) -NH2, -NH- (CH2) 5-NH-C (= NH) -NH2, -NH- (CH2) 6-NH-C (= NH) -NH2, -NH- (CH2) 7-NH- C (-NH) -NH2il

NH

NIH • (CH2) 3-N NH2 CH, especially for -Y- (CH2) rR8. > _ R6 / \ / In —N N— ^

NH and -Y_ (CH2) n

N— ^ R6

NH -------------------- Order --------- line (Please read the notes on the back before filling this page) Intellectual Property Bureau of the Ministry of Economic Affairs The Y printed by the employee consumer cooperative is preferably 0, S, N 、, or NA, where R6 is preferably an amino group, an alkylamino group, or a dialkylamino group and η may be 0, 1, 2, 3, or 4. ΝΗ, -Ν ΝΗ and -NH-CH,

'Ν— / ΝΗ;

NH -69- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 public love) 473474 A7 B7 V. Description of invention (67)

I pair / ~ \ / R6 J R6 (please read the precautions on the back before filling this page) -Ν ^ Ν-Υη ^ .Y. (CH2) n- ^ N- / H. It is the best person. R2 is preferably -eight 1 *, -eight 1 ',-0-11, -1 ^ 11, -11611-eight 1', -eight 1 * ^ 6 {1, -eight 1 ·,-(CH2) n -R3, -Ar'-Y- (CH2) n-R3, -Ar'-YC (A) 2-R3, -Het'-R3, -Ar'-Het ^ R3, -Ar '-(CH2) n -R6, -Ar'-S02-Het, -Ar'-NH-S02-Het, Ar'-S02-R7, -Ar '-(CH2) n_ (CO-NH)-(CH2) i-R6,- Ar '-(CH2) n- (CO-NH)-(CH2) i-R11, -Ar'-(CH2) n-CO-Het, -Ar '-(CH2) n- (CO-NH)-( CH2) rD-H, -Ar '-(CH2) n- (CO-NH)-(CH2) i-Ar, -Ar'-(CH2) n- (CO-NH)-(CH2) i-Het1, -Ar '-(CH2) n- (CH (CN))-(CH2) i-Ar, -Ar'-(CH2) n- (CO-NH)-(CH2) i-CH (Ar1) -Ar2, -Ar'-S- (CH2) n- (CO-NH)-(CH2) r Ar, -Ar'-S- (CH2) n- (CO-NH)-(CH2) rRn, -Ar'-S -(CH2) n- (CO-NH)-(CH2) rHet1, -Ar, -S- (CH2) n- (CO-NH)-(CH2) i-CH (Ar1) -Ar24-Ar, -S -(CH2) n- (CO-NH)-(CH2) iDH, Ar, Ar ', Ar1, Ar2, A, D, Het, Het1, R3, R6, R11, Y, n and i in particular have any of the above Better or better definition. The R3 printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is preferably C (0) A, CONH2, CONHA, CONA2, COOH, or COOA, where A has any of the aforementioned better definitions. R4 is preferably phenyl or hydroxyl. R5 is preferably methyl, chloromethyl, trifluoromethyl or phenyl.

R6 is preferably NH2, NHA, NA2, NH (D-H) or NHC (0) A, wherein A and D have the above-mentioned preferred definitions. -70- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) ^ / ^ 474 ^ / ^ 474 Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of Invention (68) R7 Preferred are NA (DH), NHA, NH (DH) or NA2, wherein A and D have the above-mentioned preferred definitions. R8 is preferably -NH- (C = NH) -NH2, -NH- (C = NH) -NHA, -NH- (C Ν Η)-NA 2,-NA-(C = N Η)-ΝΉ 2 '-NA-(C = ΝΗ)-NHA,-NA-(C = NH)-NA2, where A has the above preferred definition. R " is preferably -CH (A) ~ Ph, where A has the above preferred definition.

Certain preferred groups of the compounds can be represented by the following formulae I a to I z and I 1 to I 5, which correspond to formula I

And the undefined more detailed bases have the definition of Formula I, but among them: in la R is No 2, R 1 is No 2 and R 2 is Ar; in I b R is Η, R 2 is Ar and R 1 is -Het , -Het-S02-Ar, -Het-R5, No2, NHAlk, NAAlk, NHA1, NA,, -YDH, -Y-Ar'-R3, -Y- (CH2) 0-R3, -Y- (CH2) n- (CHR4) -R5, -YC [(CH2) 0-OH] 3, -Y- (CH2) m-NA2, -71- This paper size applies to China National Standard (CNS) A4 specifications ( 210 X 297 mm) -------------------- Order --------- line (Please read the precautions on the back before filling this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7_ V. Description of Invention (69) -Y- (CH2) m-NHA ', -Y- (CH2) 〇-OH, -Y- (CH2) k-R6 , -Y- (CH2) n-Het, -Y- (CH2) n-Ar, _Y, (CH2) n-Ari- (CH2) rR6, -Y- (CH2) n-D_ (CH2) rR6,- Y- (CH2) n-Het- (CH2) rR6, -Y- (CH2) n-NA- (CH2) i-R6 or -Y- (CH2) n-NH- (CH2) rR6; _in I c R is H, R2 is -Het1 and R1 is No2; at I d R is H, R2 is -HeP-Ar and R1 is No2;

For I e R is H R2 is -Ar '_ (CH2) n-R3 and R1 is -Het, -Het-S02-Ar, -Het-R5, -Het- (CH2) n-Ar, N02, NHAlk, NAAlk, NHA1, NA'2 '-YDH' _Y-Ar'-R3 '_Y- (CH2) 〇_R3' -Y- (CH2) n- (CHR4) -R5, -YC [(CH2) 0-OH ] 3, _Y- (CH2) m-NA2, _Y- (CH2) m-NHA ,, _Y- (CH2) 0-OH, -Y- (CH2) k-R6, -Y- (CH2) n-Het , -Y- (CH2) n-Ar, -Y- (CH2) n-Ar '-(CH2) i-R6 ^ Y- (CH2) nD- (CH2) i-R6 ^ -Y- (CH2) n -Het- (CH2) i-R6, -Y- (CH2) n-NA- (CH2) i-R6 »-72- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm)- ----------- Clothing ---- (Please read the precautions on the back before filling out this page) Order --------- Line-Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs System 473474 A7 B7 V. Description of the invention (70) -Y-CCHDn-NH-CCHdi-R6, -Y-tX-OL-txLoju-XlRM-Y-tX-NHh-XLOH; In I f R system, R2 system -Ar'-Y- (CH2) n-R3 and R1 is -Y- (CH2) k-R6, -Y- (CH2) n-Ar '-(CH2) rR6 or -Y- (CH2) n-Ar ; For Ig R system, R2 is -Ar'-S02-Het and R1 is -Y- (CH2) k-R6 or -Y- (CH2) n-Ar '-(CH2) rR6; For Ih R system H, R2 is -Ar'-S02-R7 and R1 is -Y- (CH2) k-R6 or -Y -(CH2) n-Ar '-(CH2) i-R6; for I i R is H, R2 is -ArXCHA-CCONHHCHJi-R6 and R1 is -Y- (CH2) k-R6 or -Y- (CH2) n-Ar '-(CH2) i-R6; for I k R is H, R2 is -Ar'-CCHzh-CCONHHCHdrD-HJL Ri is _Y- (CH2) k-R6, _Y- (CH2) n-Ar '-(CH2) i-R6,, -Y ^ CHdn-D-CCHdi-R8, -Y ^ CP ^ h-Ar'-CCHdi-R8 or -Y- (CH2) n-NA- (CH2) i- R8; for II R is H, R2 is -Ar'-CCHyn-CCONHHCHdi-Ar and R1 is -Y- (CH2) k-R6, -Y- (CH2) n-Ar '-(CH2) i-R6, -73- 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) 蚪. 474 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (71) -Y- (CH2) n-Ar, _Y- (CH2) i-R8, -Y- (CH2) nD- (CH2) i-R8 »-Y ^ CHA-AiMCHA-R8, -Y- (CH2) n-NA- (CH2) i-R8,

For Im R is H, R2 is -Ar'qCHJn-iCONHHCHA-Het1 and R1 is -Y- (CH2) i-R8, -Y- (CH2) nD- (CH2) rR8, -Y- (CH2) n- Ar '-(CH2) i-R841 -Y- (CH2) n-NA- (CH2) i-R8; for I n R is H, R2 is -Ar' ^ CHdn-CCHCCIvOHCHdi-Ar and R1 is -Y- (CH2) k-R6, -Y- (CH2) nD- (CH2) rR6 or -Y- (CH2) n-Ar '-(CH2) i-R6; for Io_R is H, R2 is -Ar'- CCHJdCO-NHHCHA-CI ^ Arb-Ar2 and R1 is -Y- (CH2) i-R8, -Y- (CH2) nD- (CH2) i-R8, -Y- (CH2) n-Ar,-(CH2 ) rR8 or -Y- (CH2) n-NA- (CH2) i-R8; for Ip R series H, -74- ^ sheets are applicable to China National Standard (CNS) A4 (210 χ 297 male F)- --------- Clothing -------- Order --------- line (Please read the precautions on the back before filling this page) Cooperative seal * 1 473474 A7 B7 V. Description of the invention (72) R2 is -Ar'-Het1 and R1 is -Y- (CH2) k-R6, -Y- (CH2) n-Ar '-(CH2) rR6 , -Y- (CH2) n-Ar '-(CH2) rR8 or -Y- (CH2) nD- (CH2) rR6; for I q R, R, R2, -Ar'-HeP-R3 and R1,- Y- (CH2) k-R6 or -Y- (CH2) nD- (CH2) i-R6;

Sir R is H, R2 is -Ar '-(CH2) n-R6 and R1 is Y- (CH2) k-R6 or -Y- (CH2) n-D- (CH2) rR6;

Sis R is H, R2 is -Ar'-YC ^ Ah-R3 and R1 is -Y- (CH2) k-R6; In It R is H, R2 is -Ar'-NH-S02-Het and R1 is- Y- (CH2) k-R6; for I u R is H, R2 is -HeP-R3 and R1 is -Y- (CH2) k-R6; for I v R is H, R2 is -Ar'-DH and R1 is -Y- (CH2) k-R6; for Iw R is H, R2 is -Ar '-(CH2) n- (CONHHCH2) i-Rn and R1 is -Y-CCH ^ n-Ar' ^ CHA- R6; -75- 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) 473474 Α7 Β7 V. Description of the invention (73) In the IXR system, (Please read the precautions on the back before filling in this page) R2 series-Ar ' -(CH2) n-CO-Het and R1 is -Y- (CH2) nD- (CH2) rR6; for Iy R is Η, R2 is -Ar'-S- (CH2) n- (CO-NH)- (CH2) i-Ar and R1 is -Y- (CH2) n-Ar '-(CH2) i-R6 or -Y- (CH2) n-Ar'-(CH2) i-R8; for I z R series Η, R2 is -Ar'-S ^ CHzh-CCO-NHHCHdi-Het1 and R1 is -Y ^ CHJn-Ar'qCHdi-R6 or -Y- (CH2) n-Ar '-(CH2) rR8; in I 1 R is Η, R2 is -Ar'-SJCHJnKCO-NHHCHA-DH and R1 is -Y- (CH2) n-Ar '-(CH2) i-R6 or -Y- (CH2) n-Ar'-(CH2) i-R8 For 12 R series, R2 is -Ar'-S-CCHzh-iCO-NHHCHdi-R11 and R1 is -Y_ (CH2) n-Ar '-(CH2) rR6 or -Y- (CH2) n-Ar'- (CH2) rR8; Printed on the I 3 R Department, the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, R2 Department-Ar'-S ^ CHdn-CCO-NHHCHdi-Ci ^ Arb-Ar2 and R1 Department-Y- (CH2) n-Ar '-(CH2) i-R6 or -Y- (CH2) n-Ar'-(CH2) rR8; for I 4 R series, -76- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) μ / 4 Printed by A7 B7, Consumer Cooperatives of Smart Finance J Bureau of the Ministry of Economic Affairs 5. Description of the invention (74) R2 series -Ar, -Ar'-Het1, Ar '-(CH2) n- ( CO-NH)-(CH2) i-Ar and R1 is -Y- (CH2) k-R6, -Y- (CH2) rR8; -Y- (CH2) nD- (CH2) i-R8, -Y- (CH2) n-NA- (CH2) rR8 or -YJCHsVAiMCHA-R8; for I 5 R system H, R2 system -Ar, -Ar '-(CH2) n- (C〇-NH)-(CH2) i- Ar, -Ar'-S- (CH2) „-(CO-NH)-(CH2) i-Ar, -Ar '-(CH2) n- (CO-NH)-(CH2) i-Het1, -Ar '-S- (CH2) n- (CO-NH)-(CHA-Het1, -Ar,-(CH2) n- (CO-NH)-(CH2) rD-H, -Ar, -S- (CH2 ) n- (CO-NH)-(CH2) rD-H, -Ar,-(CH2) n- (CO-NH)-(CH2) i-CH (Ar))-Ar2 »-Ar'-S- (CH2) n- (CO-NH)-(CH2) i-CH (Ar1) -Ar2 ^ -Ar,-(CH2) n- (CO-NH)-(CH2) i- R11 ^ -Ar'-S- (CH2) n- (C0-NH)-(CH2) i-RniL R1 system -Υ-((: Η2) η-Αι · '-((: Η2) ΡΙΐ6 or -Y -(CH2) n-Ar '-(CH2) rR8. The preferred compound of formula I is the following: 3- {3- [6- (4-O-methylbenzylamino) -1,3-dioxophenylhydrazone [de] isofluorin-2-yl] -phenyl} -N- [2- (4-Aminopyridinyl) · ethyl] propanamidin; N- [2- (4-Gaphenyl) -ethyl] -3- {3- [6- (4 -Guanidinium benzylamino) _ι, 3_dioxo-1H, 3H-epifluorene [de] isobutydin-2-yl] -phenyl} propanilamine; 6- (3-aminopropylamino)- 2- (3,4,5-trimethoxyphenyl) benzyl [de] isoquinoline d,% dione; 6- (3-aminopropylamino) -2- (7-hydroxyfluoren-1-yl) Phenylhydrazone [de] isoxoline_ 丨, 3_dione; -77- This paper size applies to China National Standard (CNS) A4 (210 X 297 male f ") _ ---------- -——----- Order -------- ^ line (please read the note on the back? Matters before filling out this page) 473474 Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed Agriculture A7 B7 V. Description of Invention (75) M3-aminopropylamino group W'3-dioxo [de] hquinoline_2_yl] _4,5_dimethoxybenzonitrile; 6-0-aminopropylamino) -2- (2 , 3-dimethoxyphenyl) phenylhydrazone [cardio] isoquinoline_1,3-dione; N- [2- (3-chlorophenyl) -ethyl) -3- {3- [6- (4-guanidinecyclohexylmethylamino) _ 1 3 monooxy · 1Η, 3Η-benzo [de] isoquinolin-2-yl] -benzyl} Propanolamine; 'N- [2- (4-chlorophenyl) -ethyl) -3- {3- [6- (4-guanidinecyclohexylamino) _ 丨 3-dioxo-1H, 3H-benzo [de] isopyridin-2-ylbenzylbenzylamine; '6- (3-aminopropylamino) -2- (4'-methoxybiphenyl-4-yl) benzamine [de] Isomorpholine-n-dione; 6- (3-Aminopropylamino) -2- (4-carbazol-9-yl-phenyl) benz [de] isoisoline_i, 3-di Ketone; ό- (3-aminopropylamino) -2- (4'-hydroxy-2-fluorenyl_4-yl) · benzo [de] isojunlin-1,3-dione; N- ( 3-{[2- (4'-methoxybiphenyl-4-yl) -1,3-dioxo-2,3-dihydro-1H-phenylhydrazone [de] isofluorin-6-ylamine Phenyl] -methyl} -benzylpiguanidine; 3- {3- [6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-phenylhydrazone [de] isoazeline-2 -Yl] phenyl} -N- (4-phenylbutyl) -propylamine; N- (2- (4-chloro-phenyl) -ethyl] -3- {3- [6- (2- Guanidineethylamino) -1,3-dioxo-1H, 3H-benzo [de] isocarbin-2-yl] -phenyl} -propanamide; N- (2- (4-chloro- Phenyl) -ethyl] · 3- {3- [6- (3-guanpropylamino) -1,3-dioxo-1Η, 3Η-epi 幷 [de] isoρ 奎 4-2 -yl]- Phenyl} -propanamide; N- (2- (4-chloro-phenyl) -ethyl] -3- {3- [6- (3-guanidino) -methylamino) -propylamino) -1, 3-two -1H, 3H-Benzamidine [de] isoquinolin-2-yl] -phenyl} -propylammonium 78 · This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---- --- I --- < I ------ Order --------- line (Please read the notes on the back before filling this page) 473474 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Preparation of A7 B7 V. Description of the invention (76) Amine; N- (2- (3-Gas-phenyl) -ethyl] _3_ {3_ [6_ (3_guanpropylamino) 4,3-dioxo-1H, 3H-phenylhydrazone [de] isofluorin-2-yl] -phenylbupropionamine; 6- (3-aminopropylamino) -2- (4, -methoxybiphenyl_4_yl) _phenylhydrazone [de] Isophosphonline 1,3-dione; N- [3-({2- [4- (3,6-di-third butadiazole-9-yl) _phenyldioxy_2, 3_ dihydro-1H-phenylhydrazone [de] isofluorin-6-ylaminobmethyl) _benzyl] _guanidine; and 6- (3-aminopropylamino) -2- (4-carbazole_9_ -Phenyl) -benzo [de] isofluorinated difluorene. Compounds of formula I and their starting materials are prepared by methods known per se ', as set forth in the text (for example, standard operations such as Houben_Weyl, Methoden der organischen Chemie [Methods of Organic

Chemistry], Georg-Thieme-Verlag, Stuttgart), that is, under conditions known and suitable for the reaction. In this case, the use can be changed in a manner known per se but will not be described in detail herein. The starting materials can also be formed in situ, if desired, so that they are not separated from the reaction mixture, but are reacted immediately to further produce compounds of the formula. Compounds of formula I can be obtained by dissolving their functional group derivatives by solvent, especially by hydrolysis or hydrogen interpretation. The preferred starting material for the dissolution or hydrogenolysis of the agent is the compound of formula I, but it contains 3 or more free-state amine groups and / or hydroxyl groups, and contains the corresponding protected amine groups and / or Zhao Ji, and especially replaces ΗN The group bears a group, in which R1 is an amine protecting group and / or they substitute a fluorene atom of a hydroxyl group, and bears a -hydroxy protecting group, such as those corresponding to formula I, but those who replace COOH with _C00R, , Based on which R „is ------------------- Order --------- line (Please read the precautions on the back before filling this page)

rl The Ministry of Economic Affairs Bureau of Intellectual Property Bureau printed the protection base for consumer cooperatives. Many homo- or iso-protected amine groups and / or hydroxyl groups may also be present in the starter molecule. In many cases, if the protecting groups are different from each other, they can be selectively removed. '" Amine protecting groups, generally known as suitable for protecting (blocking) amine groups against chemical reactions, but easily shifted after the desired chemical reaction is carried out elsewhere: < group. This typical group is especially unsubstituted or substituted fluorenyl, aryl, aralkyloxymethyl or aralkyl. Since the amine protecting group is removed after the desired reaction (or reaction sequence), their properties and sizes are not critical unless indicated; however, 1 to 20, especially c atoms are preferred. "Methyl" is interpreted as the broadest definition in this method. It includes derivatives derived from aliphatic 'araliphatic, aromatic or heterocyclic carboxylic acids or sulfonic acids, especially alkoxycarbonyl, aryloxycarbonyl' and aryloxy A fluorenyl group derived from a carbonyl group. Examples of such fluorenyl groups are alkyl fluorenyl groups such as ethyl fluorenyl, propyl fluorenyl, and butyl fluorenyl; aralkyl fluorenyl such as benzyl fluorenyl; aryl fluorenyl such as fluorenyl or fluorenylmethyl; aryl Oxoxyalkyl groups such as POA; alkoxycarbonyl groups such as methoxycarbonyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl, Boc, 2-iodoethoxycarbonyl'aralkyloxycarbonyl groups such as CBZ (" benzyloxycarbonyl ", 4-methoxybenzyloxycarbonyl, Fmoc; arylsulfo such as Mtr. Preferred amine protecting groups are Boc, and CBZ, Fmoc, afyl and ethenyl. "M hydroxy protecting group" is generally known as a group suitable for protecting (blocking) an amine group against a chemical reaction, but easily removed after the desired chemical reaction proceeds elsewhere on the molecule. This typical group is the above-mentioned unsubstituted or Substituted aryl, arylyl, and other alkyl groups. Since the hydroxy protecting group is removed after the desired reaction (or reaction sequence), their properties and sizes are not critical unless indicated; -80 -This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ---------- II -------- Order ---- 丨 丨 丨 丨 -Line (Please read the precautions on the back before filling in this page) Dou / J4 / 4 Printed by the Consumer Property Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (78) Caution: There are 1 to 20, especially 1 to 1 〇 C atom is better. Hydroxyl group P 歹 " Preferred to be fluorenyl, p-nitropyridinyl ', sulfonylsulfonyl, p-butanyl and ethynyl, ethyl and tert-butyl are particularly good The release of the butyl / 'I compound from its functional group derivative depends on the use of polyether, such as strong acid, convenient use of TFA or peroxy acid:-or p-toluene ::: green trichloroacetic acid or Acids such as phenylhydrazone and methenium bismuth. Additional inert solvents may be present but often not necessary. "The inert solvents are preferably organic, such as carboxylic acids (such as acetic acid) tetrafuran or dipurinane), and amidine (such as ), Hydrocarbons (such as dichloride is also an alcohol (such as methanol, ethanol or isopropanol) and water: this, the cutting agent mixture is also possible. TFA is the best amount and not force ^ additional solvent 'perchlorine The acid is 7G% acetic acid and the ratio of perchloric acid is 9: ι: the reaction temperature is convenient to about 0 and about 5GX: between; the reaction is preferably 15 ^

(Room temperature). 3 U BOC and 0-butyl are best removed, for example with TFA in dichloromethane or HCI-1, 15 to 30. Use about 5 to 5 for one base, methyl 3 amine-ethylamine or hexahydropyridine in DMF solution, 15 to 3 Θ. (:. Chlorination removes protective groups (such as CBZ or hexyl), for example, hydrogen can be removed by treating hydrogen in the presence of a catalyst (such as Yinjin, such as her, convenient support, such as carbon): This 6-form compound is a suitable solvent As shown above, in particular, it is, for example, an alcohol (such as methanol or ethanol) or amidine (such as DMF). Generally, the temperature is about 0 to 100. (:, between about 1 to 200 bar, preferably between 20 to 3 〇τ and 1 to 丨 0 bar to explain. Hydrogenolysis of CBZ groups can easily occur, for example, "to", $ to Pd / C in methanol or ammonium formate (instead of hydrogen) in Pd / C at Methanol / DMF ...

-------- 11 -------- (Please read the precautions on the back before filling out this page) --line < -81 473474 A7 Printing of clothing by employees' cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (79) The compound of formula 1 is preferably obtained from the compound of formula 11 and the compound of formula m. Generally, the starting compounds of formula II and III are known or commercially available. < Response. The compounds can be prepared in a manner known per se. Compounds of formula II are unknown, and anhydride derivatives are unknown. Bizhu can also be prepared by appropriate methods:], 8-dicarboxylic acid, leptin or the corresponding derivative. It is also possible to introduce a suitable substituent into an aromatic group with the former known = tea two substitution. The compound of formula III is a primary amine, and is generally commercially available as a synthetic method such as the Gabriel synthesis method. The primary amine-like 'reaction is performed in an inert solvent. Depending on the conditions used, between minutes and days, the reaction temperature is between about zero. To. Should be between 20 ° and 13 °. (: Between. The reaction can be carried out similarly to ⑹ 'α⑹ 1981, 16, 20-7-212 and J_ Med. Chem 1982 = 714-719. 71925 Suitable inert solvents such as hydrocarbons (such as hexane, petroleum ether , Benzene, toluene, toluene) Chlorine fume (such as trigas ethylene, dichloroethane, tetragasification / monoimide or monochloromethane); alcohol (such as methanol, ethanol, isopropanol, n-propanol, n-butane Alcohols! Third-butanol "ethers (such as diethyl ether, isopropyl ether, tetrahydrofuran coffee) or dioxane); glycol ethers such as ethylene glycol monomethyl or monoethyl ether (fluorinated ethylene diethyl or ethyl ethylene 1 g) , Ethylene glycol dimethyl ether (diglyme); ketones such as ethyl ketone or ketones, amidine (such as acetamidine, N-fluorenylpyrrolidone (NMp), dimethylethylamine or monomethylmethanamine (DMF) ); Nitriles (such as acetonitrile); sulfoxides (such as dimethyl sulfoxide (DMSO); carbon disulfide; carboxylic acids such as formic acid or acetic acid; nitro compounds (such as nitromethane or nitrobenzene); esters (such as ethyl acetate) Or a mixture of the above solvents. Chloro-n-alcohol and sulfone in — — —! --------- line (please read the precautions on the back before filling this page) This paper size applies to China Standard (CNS) A4 Specification (210 X 297 mm) Leaf / J outer / 4 leaf / J outer / 4 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ~~ ----------- 5 2. Description of the invention (80) Derivatives with free-state primary or other secondary amine groups are conveniently used as protective groups. Possible protective groups are the ones described above. &Amp; 式 The compound of formula I is prepared, in which R1 and / or ruler 2 are In terms of H2N _ (= nh) _nh_, compounds which are suitably substituted with an amine group can be treated with a fluorene amination agent. The preferred fluorene amination agent is 1-fluorenyl-3,5-dimethylpyrazole (DPFN), which can be used The form is in particular its nitrate or pyrazole-1-carboxamidin. The reaction can be carried out by adding a base (such as triethylamine or ethyldiisopropylamine) in an inert solvent or a solvent mixture (such as dmf) to 15 ° C (preferably between 60 ° C and 12 ° C). A compound of formula I is prepared in which R2 is unsubstituted or substituted biphenyl, -Ar'-Het1, -Ar'-HetLR3, -Af |-(CH2) n-R3 and / or _Ar, _ (CH2) n-R6, compounds of the formula i where R2 is aryl bromide or aryl iodide can be reacted with a derivative of a suitable butterfly acid in the Suzuki reaction .Suzu] d reaction is convenient for palladium modulation In the formula, it is preferred to add Pd (PPh3) 4 in the presence of a base (such as potassium carbonate) in an inert solvent or a solvent mixture (such as DMF), 0. to 15 (rc (preferably 0. to 120 ° C) ). Depending on the conditions used, the reaction time ranges from a few minutes to several days. The acetic acid derivative can be prepared by known methods or commercially available. The reaction can be similar to Suzuki et al., J. Am. Chem S0C. 1989, 1 1 1,314ff and Suzuki et al., Chem. Rev. 1995, 95, 2457ff The method described in the above is carried out at 0 ° E, and the acid of formula I (Ri = C00H or -Y- (CH2) n-COOH and (Or R2 = COOH) can be used in excess of ether to facilitate the presence of a strong base (such as hydrochloric acid or sulfuric acid) at 0 ° C to 10 (TC (preferably between 20). To 500 t. In contrast, acids of formula I (RbCOOA or -Y- (CH2) n-C00A and / iLR2 = c〇〇A) can be conveniently dissolved in a solvent 'according to any of the methods described above (such as using NaOH or KOH at- 83- Clothes -------- Order --------- Line (Please read the precautions on the back before filling this page) 1 This paper is a Chinese National Standard (CNS) A4 specification (210 x 297 The public loved 473474 A7 B7 printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (81) Water-dihumane, the temperature is between 0. to 4 (TC (preferably between 10. to "π, Conversion to the corresponding acid of formula I. t) In addition, the free-form amine group can be used in a conventional manner, using acid chloride anhydride, conveniently in an inert solvent (such as dichloromethane or THF) and / or alkali hydrazine-ethylamine or In the presence of pyridine), the temperature is between -6 (TC and +3 (TC).-The base of formula I can be acid, for example, by the reaction of the same amount of base and acid, and then evaporated in an inert solvent (such as ethanol) and Into relevant acid addition salts. Acids that can accept physiologically acceptable salts are particularly suitable for this reaction. Therefore, inorganic acids such as sulfuric acid, acid, hydrohalic acid (such as hydrochloric acid or hydrobromic acid), and phosphoric acid (such as orthophosphoric acid) can be used. Thiamine In addition, organic acids, especially lipids, non-cyclic, araliphatic, aromatic heterocyclic mono- or polybasic acids, transverse acids or sulfuric acids (such as formic acid, acetic acid, propionic acid, pivalic acid, diethylacetic acid, Malonic acid, succinic acid, malic acid, semalic acid, maleic acid, lactic acid, tartaric acid, malic acid, citric acid, gluconic acid, ascorbic acid, nicotine acid, isonic nicotinic acid, ammonium or dibasic acid Acids, dibasic and dibasic acids or lauric sulfuric acid. There are physiologically unacceptable salts (such as picrates) that can be used to isolate and / or isolate compounds of formula I. On the other hand, compounds of formula I with a base ( (Such as sodium or potassium hydroxide, sodium carbonate or potassium) can be converted into corresponding metal salts, especially metal or soil metal salts, or into the corresponding ammonium salts. All synthetic methods described in the text and all other suitable for the preparation of compounds of formula I It can also be combined with novel methods of chemistry, that is, automated machinery and computer-assisted synthesis, and a large number of selections can be completed (this can be seen: US 5,463,564: MA Gallop et al., J. Med. Chem. 1994, 37, 1233-1251 And 1385-1401 and MJ Sofia, Drugs Di scovery Today 1996, 1, 27- -84- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -----: ------- clothing ------ --Order ---------- line " Please read the notes on the back before filling out this page} Dou / J4 / 4 A7 B7 V. Description of the invention (82 34). A pharmaceutical formulation comprises at least one compound of the formula and / or any medically acceptable salt thereof, which is especially prepared non-chemically. In this case, the compound of formula I can be brought into a suitable agent, combining at least one solid, liquid and / or semi-hard excipient or adjuvant and, if appropriate, one or more parallel compounds. '" K these preparations can be used as human or veterinary drugs. Possibly, the formulation is a thermo-organic substance, suitable for enteral (such as oral) or parenteral administration or topical administration and will not react with novel compounds, such as water, vegetable oil, alcohol, ethoxylated ethylene glycol Alcohol, ethylene glycol, glycerol triacetate, gelatin, water-blocking compounds (such as lactose or bactericides), stearic acid, talc and petroleum gels, bonding agents, pills, coated tablets, capsules, powders, Granules, polysaccharides, liquids or drops are available: especially for oral use. Suppositories can be administered rectally. Solutions, preferably oil or water solutions, or suspensions, emulsions, or human implants can be used for non-gum administration, while ointments, creams, or powders can be used for topical administration. The novel compounds can also be cold; dried and the resulting cold; dried materials can be expected, such as the production of injectable preparations. The formulation may be disinfected and / or may contain adjuvants (such as lubricants), preservatives, stabilizers and / or wetting agents, emulsifiers, salts, osmotic pressure of buffers, buffer substances, colorants, flavoring agents and / Or one or more other activated items such as one or more vitamins. Formula I and its pharmaceutically acceptable salts can be used as adhesion receptor antagonists, especially Cool Egg ™ antagonists, and can be used to prevent and / or treat thrombosis and its secondary complications. These diseases include acute angina pectoris, angina pectoris, myocardial infarction, peripheral circulation disease #, stroke, temporary ischemia and anti-blood attack. This paper is in accordance with the regulations of the Chinese Academy of Sciences (CNS) A4 " i⑵〇85 · A7 A7 5 Description of the invention (83) B7 channeling. Force sclerosis and angioplasty / transplantation membrane re-closing / re-narrowing h ^, medium, the substance of the present invention is generally administered to the glycoprotein Ilbllla antagonist ecxPr0 夂 per unit dose, preferably between about 1 work to π. Between milligrams, between J and 5 milligrams. The daily dose is preferably between about 0 and 0 milligrams of body weight. However, the specific dose for each patient depends on all factors: for example, the efficacy of the particular compound used, age, weight, health and sexuality, sadness, diet, time, route of administration, excretion rate, combination of medicines and special treatments to be treated The severity of the illness. Oral is preferred. In this context, all temperatures are given in. C means. In the following examples, "conventionally known" means: if necessary, add water, if necessary, according to the composition of the final product, adjust the mixture to a pH between 2 and 10 and extract with ethyl acetate or dichloromethane, and filter off the organic Phase 'was dried over sodium sulfate and evaporated, and the residue was purified by chromatography on silica gel and / or by crystallization. Mass spectrometry (MS) device Kratos Maldi III and

Finnigan LCQ. Decide (M + H) + 値. EXAMPLES Example 1: A suspension of 6.6 g of 6,7-dinitrophenylhydrazine [de] isoprene 1,3-dione in 100 ml of toluene with 3.3 g of 5-pyridin-2-ylamine, And the mixture was heated at reflux. After completion of the reaction, the reaction mixture was allowed to cool and operated in a conventional manner. 2- (5-chloropyridin-2-yl) -6,7-dinitrobenzene [de] isoquinoline · 1,3-difluorene is the same as 0 Example 2: 4 g of 6-chlorobenzo [de ] Isorpene 1,3-dione suspended in 100 ml of toluene 86- 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 Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

473474 A7 ^ B7 V. Description of the invention (84) The agent is treated with 4-6 g of 2,5-digasaniline and heated under reflux. After completion of the reaction, the reaction mixture was allowed to cool and operated as usual. 6-Ga_2- (2,5-digasphenyl) phenylhydrazone [de] isoxoline 1,3-dione was obtained. This compound is then heated in morpholine until the conversion is complete. After cooling the reaction mixture, it was operated in a conventional manner to obtain 2 (2,5-difluorophenyl) -6-morpholin-4-ylphenylhydrazone [de] isoxolinoline-; [, 3_di_. MS: meter: 426; actual-test: 427. Similarly '6 -Ga-2- (2,5-digasphenyl) benzo [de] iso'l-quinolin-1,3_-one is reacted with R1-H to give the following compound of formula Iba:

Iba ---------- I—— (Please read the notes on the back before filling out this page) Order --------- line | Printed by the Intellectual Property Bureau of the Ministry of Economy -87- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of invention (class) Intellectual Property Bureau of the Ministry of Economic Affairs Employee Co-operative Cooperative printed R1 on R1 -H and Iba MS calculation: actual measurement: 460 461 -νΓ) 424 425 —N _ 410 411 / —N * \ _ > 〇501 502 -NH- (CH2) 5-〇H-nh- (ch2) 3-n (ch3) 2 441 442 —N — 1 H CH2- ^ 3 —N — 1 H (ch2) 2-^ _) -NH- (CH2) 2-C〇〇Me 442 443 —N — 1 H ch2—S—S〇 2NH2 —N- H (CH2) 2— 476 477 qh3 / uh -N— (CH2) 2—OH H x '438 439 -88- ------------------ --Order --------- Line · (Please read the precautions on the back before filling in this page) The paper size applies the national standard (CNS) A4 (210 X 297 male f) 473474, A7 B7 V. Description of Invention (86) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-89- ----------- clothing -------- order --------- line (please read the precautions on the back before filling this page) Applicable to China National Standard (CNS) A4 (210 X 297 mm) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7 V. Description of the Invention (87) Example 3: Similar Example 2, 6-Chlorobenzo [de ] Isopinene-1,3-dione is reacted with 3-chloroaniline and then with ^ -fluorene. This gives the compound of the formula Ibb: R1

0 N 0

CI R1 calculated in R iH and Ibb MS measured actual price '% -〇—N 376 377 / ^ —N > -〇467 468 -NH-C (CH2OH) 3 -nh- (ch2) 3-n ( ch3) 2 407 408 —N — 1 H CH2- ^ 3 412 413 —N- H (CH2) 2 — \ _ j 426 427 -90- 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) 473474 A7 B7 5 、 Explanation of invention (88) The consumer cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs printed R1 on R, H and Ibb 'MS calculations (measured) ... 1 Η ch2 ~~ 《》 — so2nh2 —N — 1 Η-(〇η2) 2-^ _ ^-〇η 442 443 CH〇1 3 —Ν —-ϋΗ (CH2) 2- ^ J ^ -〇H —Ν— I ο 404 405 —Ν— 1 Η ο 390 391 Γ ^ Ί 438 439 i > --N — ι · Η -ch2- yCH2 ΝΗ2 441 442 —N — I Η -ch2 —N — 1 Η /-N-(CH2) 2— 427 428 —N — I Η Ν— \-(ch2) 2 —> 427 428 -91- ---- I ------------ (Please read the notes on the back before filling this page) Order --- ------ line one paper size applicable to China Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 5. Description of the invention (1) R1 in Ri-H and in: Ibb MS calculation (measured)-N-1 Η 413 414-Ν-1 Η / ~ \ (CH2) 2 ^ 〇435 436 —N-1 Η / ~ Λ (CH2) 3 -ch3 —N — " (CH2) 3—N, Ν Η 430 431 —N-Η —Ν-Η- 〇f -nh- (ch2) 2-co〇ch3 408. 409 -NH (C5Hu) 392 393 -NΗ (C3H7) -N (CH3) -C4H9 392 393 -n (c2h5) 2 378 379 Example 4 printed by the Bureau's Consumer Cooperative: Similar Example 2,6-Gastilbene [de] isobita-1,3-dione reacts with aniline and then reacts with Ri-H. The compound of the formula Ibc is obtained as follows: -92- The paper size applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ------------------- Order- ------- line (please read the notes on the back before filling this page) 473474, A7 B7 V. Description of the invention ... r1

0 The Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs printed R1 on R1- !! and calculated on Ibc MS (measured), / PIT ——N— < Γ ^ CH3 392 393 -〇-〇342 343 -〇-〇433 434 -ΝΗ- (CH2) 3-Ν (CH3) 2 373 374 _n_ch2- ^ 3) Η ~ 378 379 —r; j— (ch2) 2— H ~ 392 393 —N-CH2-》 SO2NH2 N (CH2) 2 — / " V〇HH ~ -93- ----- r ----------------- Order · ------- One (Please read the first Note: Please fill in this page again) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (91) R1 in ί ^ -Η and Ibc

MS calculation 値 actual measurement 〒 h3 • N —- (CH2) 2 ·

ΟΉ -OH

356 357 — 404 405

-----—, ------------ Order · -------- (Please read the notes on the back before filling out this page) Employee Cooperation of Intellectual Property Bureau of the Ministry of Economic Affairs Du printed

—N —— (CH2) 2 H

393 394

H This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 male f) -94- 473474 A7 B7 V. Description of the invention (92) The R1 printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is calculated by Ibc MS値 ted Measured 値 Γ ~ \ —n— (CH2) 2—N 0 Η, one '401 402 r ~ \ _N— (CH2) 3—NN — CH3 HN ^ / —N— (CH2) 3—N ^ N Mountain v = / 396 397 -NH- (CH2) 2-COOCH3 374 375 -NH (C5Hu) 358 359 -NH (C3H7) 330 331 -N (CH3) -C4H9 358 359 -N (C2H5) 2 344 345 -NH -CH2-CH (CH2C1) -OH —N = CH-(^> wo > -NH- (CH2) 5-OH 374 375 / ~ Λ —N 0 v_v 358 359 Example 5: Similar to Example 2, 6-Chlorine Benzo [de] isoprene-1,3-dione reacts with 3-nitroaniline and then reacts with R1 -H. The compound of formula Ibd is obtained as follows: Specifications (210 X 297 mm) -------------------- Order --------- Line (Please read the precautions on the back before filling in this (Page) 473474. A7 B7 V. Description of the Invention (93)

Printed by Employee Consumer Cooperatives, Bureau of Smart Finance, Ministry of Economic Affairs

-96- ----- r --------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 Invention description (94) Printed by R1 on R] -H and printed on Ibd MS by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. ΥΗ3 Γ ~ ^ —N (CH2) 2-C y ~ 〇Η 401 402 r < X) 449 450 / CH2-ΝΗ2 —rCH2 · ^ —N — CH2—C —ΝΗ2 Η Ν ~ Χ r ~ Ν _ν— ( ch2) 2 ~ (y Η 438 439 Ν— \ —Ν — (CH2) 2 ~~ ^〉 Η Ν / 438 439 Ν _n_ch2- ^ J > Η ~ / ~ \ —Ν 一 (〇Η2) 2— Ν 〇Η Ν ~~ / 446 447 Η Ν ~ '415 416 -97- This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 male f) -------- tT ---- ----- € # (Please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (95) R1 is calculated in R1- !! and Ibd MS is calculated (measured) / \ —N- ( CH2) 3—NN — CH3 Η '一 / —Ν — (CH2) 3—Ν ^ N 441 442 H--NH- (CH2) 2-COOCH3 419 420 -NH (C5Hu) 403 404 -NH (C3H7) 375 376 -N (CH3) -C4H9 403 404 -n (c2h5) 2 389 390 / ~ \ —NO 403 404 \ / Example 6: Similar to Example 2,6-chlorophenylhydrazone [de] isoprene-1,3-dione and 3-methyl Chloroaniline is then reacted with R ^ -H. The compound of the formula Ibe is obtained as follows: --------------------- Order --------- (Please read the notes on the back before filling this page) R1 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-98- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 male f) 473474, A7 _B7 V. Description of the invention (96) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

R1 is calculated from R1- !! and Ibe MS. Measured-N < Phsan'ch3 422 423 -〇386 387 -〇. 372 373 -〇-〇463 464 --NH- (CH2) 3_N (CH3) 2 403 404 -N—CH2- ^ 3 408 409 -N— (CH2) 2-7 HW 422 423 —N — CH2 ~~ —S〇2NH2 ~ ^ — —N — (CH2) 2—-386 387-\ _ r / CH2—NH2 437 438 _n_ch2- ^ J > H ------------ Cloth -------- Order --------- Line # (Please read the Please fill in this page again for note) -9 9-This paper size is in accordance with Chinese National Standard (CNS) A4 specification (210 χ29τ ¥ 4737 473474, A7 B7 Description of invention (97) R1 in R ^ -H and Ibe MS calculation 値 actual measurement値 N CH2- \ Η) —m2 ^ 23 424 N (CH2) 2 — \ H, 3 423 424 N — N CH2— H〉 409 410 -N— (CH2) 2-N ^ HV ^ 0 431 '' 432 Factory --N- (CH2) 3-NH, ~ \ '' N--CH3 -NH- (CH2) 2-COOCH3 404 405 -NH (C3H7) 360 361 -N (CH3) -C4H9 388 389 -n (c2h5) 2 374 375 -NH- (CH2) 5-〇H 404 405 r ~ \ —N 0 v_y 388 389 ------------------- Order · ------- -Line (Please read the precautions on the back before filling out this page) Employees ’Cooperatives, Intellectual Property Bureau, Ministry of Economic Affairs Printed -100- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of the Invention (98) Example 7: Similar to Example 2, 6-Gas Benzo [de] Isorpene-1,3-dione reacts with 4-phenylethylaniline and then with R1-!!. The compound of the formula Ibf is obtained as follows: ------------ Clothing ---- (Please read the precautions on the back before filling in this page) Printed R1 on Rj by the Consumer Cooperative of the Bureau of Wisdom and Finance, Ministry of Economic Affairs -H and calculated from Ibf MS (measured) -NH- (CH2) 3-N (CH3) 2 475 \ 476 / CH2——NH2 -n—ch2— 509 510 —ch2-/ —NH2 H 495 496 rN -n -(Ch2) 2- ^) H 495 496 N Fly-N— (CH2) 2— ^) HN ^ N— \ —N-CH2-J H 481 482 -101- subscription --------- Line · R1

This paper size applies to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (99) R1 is calculated in RLH and Ibf MS (measured) -N— (CH2) 2-N ^ ~ \) Η Ν '503 504 —N— (CH2) 3—N Ν—CH3 530 531 Η W -NH- (CH2) 5-〇H' —N- (CH2) 3—N, N Ν 498 499 Example 8: Similar to Example 2,6-Gasbenzo [de] isopinene-1,3-dione was reacted with H2N-Ar and then (if necessary) reacted with R 1 -fluorene. The following compounds of formula I b g are obtained: ----------------- (Please read the notes on the back before filling this page) R1

b9 Order --------- line. Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Invention Description (100

Ar R1 in R ^ -H and Ibg

NIH NIH N1H

Clothing -------- Order --------- Line (Please read the precautions on the back before filling this page) Printing of clothing by the staff consumer cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-103- This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the Invention (ι〇1) Example 9: Similar Example 2 , 6-Gabenzo [de] isofluorene], 3-dione reacts with 3-chloro-4-methylaniline 'and then reacts with Ri_H. The compound of formula Ibh is obtained:

Example 10: Similar to Example 2,6-Gastilbenz [de] isorene-i, 3-dione reacted with H2N-Ar and then with R1-!!. The ibi compound of the following formula is obtained: -104- The paper size is applicable to the Chinese National Standard (CNS) A4 specification (2) 0 X 297 mm) ---------------- (please first Read the note on the back? Matters and then fill out this page) Order --------- line · 473474 A7 B7 V. Description of the invention (1〇2)

b9

N 丨 A Printed by Employee Consumer Cooperatives, Bureau of Wisdom and Finance, Ministry of Economic Affairs

-105- This paper size applies Yin National Standard (CNSXA4 specification (210 x 297 male f) ------------------- Order --------- (Please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (103)

--------------------- Order --------- line- (Please read the precautions on the back before filling out this page) Staff Consumption of Intellectual Property Bureau, Ministry of Economic Affairs Cooperative printed example 1 1: 4 g of 6-nitrobenzo [de] isopinene-1,3-dione in 100 ml of toluene suspension was treated with 3.1 g of 4-iodine and the mixture was heated at reflux. After the reaction is completed, the reaction mixture is allowed to cool and is operated normally. Get 6-nitro-2- (4- -106- This paper size applies to Chinese National Standard (CNS) A4 specifications (210 X 297 mm) R1

473474 A7 __B7 V. Description of the invention (104) iodophenyl) phenylhydrazone [de] isoxolinoline: i, 3-dione. Add 12 equivalents of k2CO3, 2 equivalents of Ph-B- (OH) 2, and 10 mole percent Pd ((pph) 3) 4 to a solution of the compound in 80 ml of DMF and heat at 801 until The transition is complete. After the catalyst is filtered off, the 6-nitro-2-biphenyl-4-ylphenylhydrazone [de] isoxoline-1,3-dione and 1,3-diaminopropane are heated in a conventional operation until the conversion is completed until. After the reaction mixture was cooled, 6- (3-aminopropylamino) _2-biphenyl-4-ylbenzo [de] isoquine > lin-i, 3-dione was obtained in a conventional manner. Similarly, the reaction of Ph-B- (OH) 2 and WH with 6-nitro_2_ (4_iodophenyl) phenylhydrazone [de] isofluorin-1,3-dione gives Compound:

Ibk R on IΓ-Η and Ibk ----------- Ψ ------- 丨 Order -------- (Please read the notes on the back before filling this page ) Line. Printed by the Consumer Cooperatives of the Bureau of Wisdom and Finance, Ministry of Economic Affairs -NH- (CH2) 5 ~ NH2 -NH- (CH2) 7-NH,

Example 12:-Similar to Example 11, 6-nitro-2- (4-iodobenzyl) benzoquintene 1,3-dicopper reacted with Rig_B_ (0H) 2 and Rl_H. The following formula ιμ of the & compound -107- The paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (105) R1

Ibl

R1 at R ^ H and Ibl cf3 —NH— (CH2) 3—NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

-NH- (CH2) 3-NH2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2

-nh- (ch2) 3-nh2 -nh- (ch2) 5-nh2 -nh- (ch2) 7-nh2 ------------------- Order --- ------ line (Please read the notes on the back before filling this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-nh- (ch2) 3-nh2 ocf3 -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2

-108- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of invention (106) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-109- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ------------- Clothing ---- (Please read the precautions on the back before filling (This page) Order --------- Line-473474 A7 B7 V. Invention Description (107)

-n Ha 1 ^ 1 nnnnn I · 1 ^ 1 1 ^ 1 ^ ^ n-^ 1-Xikou (Please read the precautions on the back before filling this page) Line-Printed by the Employees' Cooperatives of the J Finance Bureau of the Ministry of Economic Affairs Agricultural Example 13: Similar to Example 1, 1,6-nitro-2- (3-iodophenyl) phenylhydrazone [de] isowaline-1,3-dione and R1Q-B- (OH) 2 and I ^ -Η reaction. The compound of the following formula Ibm is obtained: -1 1 0- The paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (108) R1

Ibm R1

R1 on Rf-H and Ibm

-NH- (CH2) 3-NH2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2

CF —NH— (CH2) 3—NH2 3 -NH- (CH2) 5-NH2 —NH- * (CH2) 7 " * NH2

------------ ♦ Clothing ------- 丨 Order --------- Line · (Please read the notes on the back before filling this page) Wisdom of the Ministry of Economic Affairs Printed by the Property Agency Staff Consumer Cooperative

—NH— (CH2) 3 ~ NH2 -NH— (CH2) 5-NH2 —NH— (CH2) 7—NH2

—N

-NH- (CH2) 3-NH2 ocf3 -NH- (CH2) 5-NH2 —NH— (CH2) 7 ~ NH2

111- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (109 PF5 R1 in Ri-H and Ibm -b -nh- (ch2) 3- nh2 -NH- (CH2) 5-NH2 -NH_ (CH2) 7_NH2

-NH- (CH2) 7-NH2

-NH- (CH2) 7-NH2

-nh- (ch2) 3-nh2 -nh- (ch2) 5-nh2 —NH_ (CH2) 7—NH2 (Please read the notes on the back before filling this page) Clothing

—NH— (CH2) 3—NH2 —NH- (CH2) 5 ~ NH2 -NH- (CH2) 7-NH2

This paper size applies to China National Standard (CNS) A4 specification (210 X 297 male f) -112- 473474 A7 B7 V. Description of invention (11〇)

R1 at R ^ -H and Ibm

2 -nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2 Ν—Η

2 Η Ν -NH- (CH2) 3-NH2 —NH— (CH2) 5 ~ NH2 -NH- (CH2) 7-NH2

—NH— (CH2) 7—NH2

Cl -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

(Please read the notes on the back before filling this page) -------- Order ------ I--.

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs -NH- (CH2) 3-NH2 -NH- (CH2) 5 ~ NH2 -NH- (CH2) 7 ~ NH2

Example 14 ·· Similar to Example 1 1,6-nitro-2- (3-iodo-4-fluorenylphenyl) phenylhydrazone [de] isop-quelin-1,3-dione and RIG-B- ( OH) 2 and WH reaction. The compound of the following formula Ibn is obtained: -113- The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 male f) 473474. A7 B7 V. Description of the invention (111) R1

R1

ch3 R1U R1 between R ^ -H and Ibn " 〇 -NH- (CH2) 3-NH2 -NH- (CH2) 5 " NH2 -nh- (ch2) 7-nh2 1 fly) ^ NH2 -O-0 ^ 3 -nh- (ch2) 3-nh2 -NH- (CH2) 5 " NH2 -NH- (CH2) 7-NH2

/ —Λ -ΝΗ- (CH2) 3 ~ Nh2 —CH3 -NH- (CH2) 5-NH2 \ ΜΠ ^ -nh- (ch2) 7-nh2 --- ^ ---------- clothing -------- Order --------- line (Please read the notes on the back before filling this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-NH- (CH2) 3-NH2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -114- Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474. A7 B7 V. Description of the invention (112) Example 1 5: Similar to the example 1 1,6 -Nitro-2- (4-iodo-3-tolyl) benzo [de] isopyridin-1,3-dione reacts with R1G-B- (OH) 2 and R1- !! . Iob compound of the following formula is obtained: ------------ clothing -------- order --------- line (please read the precautions on the back before filling this page ) R1

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (113) R10 R1 in R1- !! and Ibo -nh- (ch2) 3-nh2 -〇- NH- (CH2) 5-NH2 h3c) -NH- (CH2) 7-NH2 η Example 16: Similar to Example 2,6-nitrophenylhydrazone [de] isofluorene-1,3-dione and H2N -Het1 reaction. The compound of formula Ic is obtained:

------------- Ψ ------- I I I (Please read the precautions on the back before filling out this page) Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

Hetx R 丨 in Ic -N〇2 ch3-/, N -N〇2 1 乂 CF3 Example 17: similar to Example 2,6-nitrophenylhydrazone [de] isoprene-1,3-dione and H2N-Het ^ Ar reaction. The compound of the formula Id is obtained as follows: -116- The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 male f) line-473474 A7 B7 V. Description of the invention (114)

(Please read the notes on the back before filling this page) Example 18 printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs: similar to Example 2,6-Nitrobenzo [de] isopinene-1,3-di The ketone is reacted with 2- (3-aminophenyl) acetamidamine and then with Ri-H. The following formula lea compound is obtained: ---------- Order --------- Line _ -117- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of the invention (115) R1

0 N 0

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

R1 is calculated from R1- !! and lea MS. Measured 値 / CH2- ~ NH2 -N-CH2- / Η 乂 N (CH2) 2 N-Λ -〇Η _fvj- (0 ^ 2) 3_ N ^ N \ --Ί 455 456 -nh- (ch2) 3-n (ch3) 2 430 431 -nh- (ch2) 4-nh2 -NH- (CH2) 7-NH2 458 459 -NH- (CH2) 8-NH2 472 473 -N- (CH2) 2-N- < 444 445 HH -118- ----------- ♦ clothing ------- --order --------- line (Please read the notes on the back before filling this page) This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 _B7_ V. Description of the invention (116) Example 1 9: Similar to Example 2 , 6-Nitrophenylhydrazone [de] isoprene-1,3-dione is reacted with 2- (4-aminophenyl) acetamidamine and then with R1-!!. Get the following Ieb compound of the formula: 9

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of Invention (117) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-120- ------------- 衣 -------- tT --------- '^ # · (Please read the notes on the back before filling in this Page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of the Invention 〇18)

----------------- (Please read the notes on the back before filling out this page) Order --------- line Cooperative printed Example 2 0: Similar to Example 2, 6-Nitrophenylhydrazone [de] isoprene-1,3-dione reacted with 3-aminobenzidine and then with WH. The compound of formula lec is obtained as follows: -121- The paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474, A7 B7 V. Description of the invention (119) R1

R1 is calculated in rLH and Iec MS (measured)

-NH- (CH2) 5-0H -NH- (CH2) 3-N (CH3) 2 416 417 --------------------- 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

—N—CH2 · H

NIH — (CH2) 2 ^ 3

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (12) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-123- (Please read the note on the back? Matters before filling out this page) — Order --------- line-This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm)

473474 A7 B7 V. Description of the invention (121)

Example 2 1: Similar to Example 2,6 -Chlorobenzo [de] isorene-1,3-dione reacted with 4- (4-aminophenyl) butanamide and then with R1- !! . The following led compound is obtained: R1 叩 2) 3 conh2 (Please read the precautions on the back before filling this page) Line-Printed by R1 on R ^ -H and led — MS calculated by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 値Measured 値-nh- (ch2) 4-nh2 -NH- (CH2) 7-NH2 486 487 -nh- (ch2) 8-nh2 500 501 -N— (CH2) 2 —N ·-458 459 Η H -NH -(CH2) 3-N (CH3) 2 -N— (CH2) 3-N ^ NH -124- This paper size applies to China National Standard (CNS) A4 (210 X 297 male f) 473474 Intellectual Property Bureau, Ministry of Economic Affairs Printed by employee consumer cooperatives A7 B7

Example 22 ·· Similar to Example 2,6-Nitrophenylhydrazine [de] isorene-1,3-dione reacted with 3- (3-aminephenyl) propanilamide and then with R ^ -H . Get the following lee compound ...

R1 at RLH and lee MS R1 at R1- !! and at lee MS Calculate (measured) Calculated (measured) _f / " " " " \) 429 430 v_y -NH- (CH2) 3-NH (CH3) 430 431 _f / ~ ^ 427 428 —N — (CH2) 2 — N — * < ^ 444 Η H 445 —N ^] 413 414 -nQn-ch2-^-〇—N XN — (^ > 504 505 -〇, 2-〇 = -125- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) (Please read the precautions on the back before filling this page) ----- ---- Order · --------. 473474

7 7 AB V. Description of the invention (123) Printed by R1 of the Intellectual Property Bureau of the Ministry of Economic Affairs, Consumer Cooperatives, and calculated on lee MS. Measured on R1 in WH and on lee MS. Measured on -N- < Ph / ~ Λ / Ν = \ -NH- (CH2) 2-COOMe Α ~ Λ / N = \ _n_ch2- ^ 3 'Η 542 -NH * (CH2 > 3 — ^^ N— (CH2) 3 ~ ΝΗ2 543 —n— (ch2) 2—463 464 __] y 498 -ΝΗ — / — 499 —N — CHj—fy—SOjNHj HW -ΝΗ_ (CH2) 2_ΝΗ- (CH2) 2- 446 OH 447 -N— (CH2) 2 — / ~ V〇HHW -NH- (CH2) 2-NH (C3H7) -NH- (CH2) 5'〇H -NH- (CH2) a-ο- (CH2) 4-0- (CH2) 3- 54 6 nh2 '547 -N (CH3)-(CH2) 3- 444 445 NH (CH3) -N (CH3)-(CH2) 2- 472 N (C2H5) 2 473 -NH- (CH2) 3-N (CH3) 2 444 445 -NH- (CH2) 3-N-(^) 498 HN ~ / 499 one N — CH2—yy NH2 HX == / .ch2nh2 / 484 -nh-ch2 one · (> 485 / CHj-NH2 -J-CH.-0 -NH- (CH2) 3-n (ch3)-(CH2) 3- 487 nh2 488 -126- (Please read the precautions on the back before filling this page) ----- Order --------- Line · This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (1¾) R1 in Ri-H and lee MS calculation (measured); R1 calculated at rLh and lee MS calculated (measured) r ~ N-N— (CH2) 2 ~ \ y 464 465 -NH " (CH2) 2-NH (C2H5) 430 431 -N— ( CH2) 2- ^ 3 / ~ Λ —N —— (CH2) 2—Ν 〇 Ν ′ —Ν—CH2—450 451 Η -Ν— (CH2) 3-N ^ N-CH3 499 II V / π 500 — (CH2) 3—N \ = / Ν 469 470 —ΝΗ— (CH2) 5—ΝΗ2 -NH (C5Hu) -NH- (CH2) 7 " NH2 472 473 -NH (C3H7) —Ν—CH2 ~ —CH2 —ΝΗ2 -------- Order · -------- line (please read the notes on the back before filling out this page) Employees' Intellectual Property Bureau, Ministry of Economic Affairs, Consumer Consumption Du Yinchan -127- Paper size applies Chinese National Standard (CNS) A4 specifications (210 X 297 male f> 473474 A7 B7 V. Description of the invention (125) Example 2 3: Similar to Example 2, 6-Nitrophenylpyrene [de] iso bitene- 1,3-diketone reacts with 3-amino4-methoxybenzamide and then with R1-!!. The compound of the formula Ief is obtained: printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, R1

(Please read the note on the back? Matters before filling out this page) -----. Thread · This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) 473474. A7 B7 V. Description of the invention (126) Example 2 4: Similar to Example 2, 6-Nitrobenzo [de] isopinene 1,3-dione reacted with H2N-Ar '-(CH2) n-R3, and then reacted with R1- if necessary !!reaction. Gives the compound of the following formula leg R_1

leg

Ar,-(CH2) n-R3 Ar '-(CH2) n-RJ R1 is calculated in R ^ -H and in leg i MS. Measured. ---- cooch3 -NO2

O -NH- (CH2) 7-NH2 514 515 / (〇 «2) 2-^^ 〇3„ 7

-------------% clothing (Please read the notes on the back before filling this page) Order --------- Line Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs CHo— NH2 C5h11

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 129- R1

473474. A7 _B7 V. Description of the invention (127) Example 2 5: Similar to Example 1 1,6-nitro-2- (3-iodophenyl) benzo [de] isoquinoline-1,3-dione Or 6-nitro-2- (4-erphenyl) benzo [de] isoquinine-1,3-dione with R3- (CH2) n-Ph-B- (OH) 2 and R1-! !reaction. A compound of the formula Ieh (Ph-Ph = Ar ') is obtained: leh I 3

ArHCHA-R3 -Ar '-(CH2) n-RJ R1 at R ^ -H and leh -NH- (CH2) 3-NH2

COOH -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2 (Please read the precautions on the back before filling this page)

COOH -nh- (ch2) 3-nh2 ~ NH— (CH2) 5 ~ NH2 -NH- (CH2) 7-NH2 Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

ϋ -nh- (ch2) 3-nh2 〇CH3 -ΝΗ- (CH2) 5-ΝΗ2 -NH- (CH2) 7-NH2

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -130- 473474 A7 B7 V. Description of the invention (128) -Ar '-(CH2) nR R1 to R1- !! and Ieh -NH -(CH2) 3-NH2 OCH3 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

N 丨 Η

N

-nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

-^ 衣 (Please read the precautions on the back before filling this page) Q -nh- (ch2) 3-nh2

CH3 -NH- (CH2) 5 ~ NH2 -nh- (ch2) 7-nh2

Order --------- Line · Example 26: Similar to Example 2,6-Nitrobenzo [de] isopinene-1,3-dione and 2- (4-aminophenylsulfane Group) to react with acetamidine and then with R1-H. The compound of the formula Ifa is obtained:

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs——ch2-conh2 -131- This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 V. Description of the invention (129) R1 in Calculated in Ifa MS (measured) -NH- (CH2) 4-NH2 448 449 -nh- (ch2) 7-nh2 490 491 -NH- (CH2) 8-NH2 ——N-1 H-(CH2) 2 _ N — H 476 477 -NH- (CH2) 3-N (CH3) 2 —N — 1 H-(CH2) 3—N Two N 487 488 —N — 1 HN fly- (CH2) 2 ^ _》 / Ch2- -nh2 —N－1 H ch2- ^ 3 Φ clothing (please read the precautions on the back before filling in this page) Example 2 7: Similar to Example 2,6-nitrophenylhydrazone [de] isoprene- 1,3-diketone reacts with 2- (4-aminephenoxy) acetamidamine and then with R1-!!. This gives an Ifb compound of the formula:

-132- 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.

0 N 0 473474 A7 B7 V. Description of the invention (13) R1 is calculated from R ^ -H and Ifb MS. Actual measurement: -NH- (CH2) 4-NH2 -nh- (ch2) 7-nh2 474 475 -NH -(CH2) 8-NH2 488 489 —N— (CH2) 2—N- < ^ Η H. 460 461 -NH— (CH2) 3 ~ N (CH3) 2 446 447 —N— (CH2) 3— N, NH 471 472 N— \ -N— (CH2) 2-^ _ ^ y ^ CH2 ~ _n_ch2- ^ 3 H ^ -nh2 480 481 Example 2 8:, similar to Example 2, 6-nitrobenzo [ de] Isoamidine-1,3-dione is reacted with 5- (hexahydropyridine-1-sulfofluorenyl) fluorene-1-ylamine and then with R1-H. Get the compound of the formula Ig: ----------------- (Please read the precautions on the back before filling this page) Order --------- Line · Ministry of Economy Printed by the Intellectual Property Bureau Staff Consumer Cooperatives -133- This paper size applies to the Chinese National Standard (CNS) A4 specification (2) 0 X 297 gf) Printed by the Ministry of Economy ’s Smart Finance J Bureau employee consumer cooperatives 473474 A7 _ B7 5. Invention Instructions (131)

0 N 0

f〇2 0

R1 is calculated from R1- !! and Ig MS (measured) -nh- (ch2) 3-nh2 542 543 -NH- (CH2) 5 * NH2 570 571 -NH- (CH2) 7-NH2 / CH2 ~ -nh2 —N—ch2 ~ \ y 1 \ / H Example 2 9: Similar to Example 2,6-nitrobenzo [de] isopinene-1,3-dione reacted with H2N-Ar'-S02-R7, Then react with rLh. This gives the compound of formula Ih:

Ar, -S〇2-R7 -134- This paper size applies to China National Standard (CNS) A4 specification (210 X 297 male f) -------- Order --------- Line (Please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (132)

—-------- Φ Clothing (Please read the precautions on the back before filling this page) Order --------- Line-Printed Example of Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 3 0: It is similar to Example 2 ′ 6-Sterylbenzyl [de] isop-keline-1,3-—S, which reacts with H2N- and then reacts with Ϊ ^ -Η. The compound of formula Ii is obtained as follows: -135- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) "474 A7 B7

Friends, description of the invention (1 advise (CH2) 2-CONH- (CH2) j-NH2 R1 in R ^ -H and in Ii

MS 4 -nh- (ch2) 7-nh2 jCH2- monoNH2 543 544 _n_ch2- {J 549 550 2 -NH- (CH2) 7 * NH2 —nh2 515 516 Example 3 1: Similar to Example 2,6-nitro Phenylhydrazone [de] isoprene-13_dione reacts with h2N_ C6H4- (CH2) 2_C0NH-CH2_C6H | 1 'and then reacts with it. The compound of the formula Ika is obtained as follows: -136- This paper size applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) --------------------- Order --------- Line · (Please read the precautions on the back before filling out this page)% Qibu Intellectual Property Bureau employee clothing cooperative printed clothing 473474 A7 __ B7 V. Invention Description (134) R1

Calculated in Ri-H and Ika MS (measured) -NH- (CH2) 7-NH2 568 564 / CH2— -nh2 574 575 -N —CH2— < 7 7 H N1 ---------- -— (Please read the notes on the back before filling out this page) Example 3 2 printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs: Similar to Example 2, 6-Nitrobenzo [de] isop 克 晞 -1, 3-Dione reacts with H2N-C6H4- (CH2) 2-CONH- (CH2) 2-C6H9 and H2N- (CH2) 5-NH2. Then add 1 equivalent of (third butoxycarbonylimidazole-1 -ylfluorenyl) tertiary butyl amidate to 3- {3- [6- (5-aminopentylamino) -1,3- A solution of dioxo-1H, 3H-phenylhydrazone [de] isofluorin-2-yl] phenyl} -N- (2-cyclo-hex-enethyl) propanamide in 60 ml of DMF and the reaction is complete Then, the BOC protecting group was removed by adding TFA to 1,2-dichloroethane. N- (2-cyclo-hex-enethyl) -3- (3- [6- (5-guanpentylamino) -1,3-dioxo-1H, 3H-benzo [de] isoquine Porphyrin-2-yl] phenyl} propanamide. Compounds of the following formula Ikb can be borrowed from H2N-C6H4_ (CH2) 2-CONH- (CH2) 2-c6h9 with diamine and (third butoxycarbonylimide Azole-1-ylmethyl) carbamic acid-137- This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 G S) Order --------- Line-473474 A7 B7 V. Invention Explanation (135) The third butyl ester was removed and the protecting group was similar to obtain R1

Ikb (CH2) 2-CONH- (CH2) j · R1 in Ikb (Please read the notes on the back before filling this page) -NH- (CH2) s-NH-C (= NH) -NH2 -NH- ( CH2) 2-NH-C (-NH) -NH2 -NH- (CH2) 7-NH-C (= NH) -NH2

CH2-N NH.

H

It T ^ ^^ 1 n-* = 口

CH2—N

NH A

NK line-

H Printing of clothing by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-NH- (CH2) 3-NH-C (= NH) -NH2 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) NH2

NFT

X --N NH.

H -NH- (CH2) 6-NH-C (= NH) -NH2 -NH- (CH2) 4-NH-C (= NH) -NH2 This paper size applies to China National Standard (CNS) A4 specifications (2) 0 X 297 mm) • 138-

473474 A7, B7 V. Description of the invention (136) Example 3 3: Similar to Example 2, 6-nitrobenzo [de] isopinene-1,3-dione and H2N-C6H4- (CH2) 2-CONH -(CH2) rAr is reacted, followed by RJ-H. The compound of the formula Ila is obtained:-lla (CH2) 2-CONH- (CH2) rAr (Please read the precautions on the back before filling in this page) ♦ Order --------- line

Printed by the Employees ’Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs • 139- This paper size applies to the Chinese National Standard (CNS) A4 (210 X 297gf) Printed by the Employees’ Cooperatives of the Intellectual Property Bureau of the Ministry of Economics

Example 3 4: Similar to Example 3 2,6-nitrophenylhydrazone [de] isopinene-1,3-dione and H2N-c6h4- (ch2) 2-conh- (ch2) 3-c6h5, suitable two Amine and (third butoxycarbonylimidazole · 1-ylfluorenyl) aminoacetic acid tert-butyl ester are reacted. After removing the protective group, a compound of the following formula lib is obtained: -140- This paper size applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ------------------ --Order --------- line (please read the precautions on the back before filling this page) 473474, A7 B7 V. Description of the invention (138) R1

R1 calculated in lib MS (measured) -NH- (CH2) 7-NH2 / CH2-NH2 596 597 _n_ch2-/] 5 HW -NH- (CH2) s-NH-C (= NH) -NH2 604,8 605 , 3 -NH- (CH2) 2-NH-C (= NH) -NH2 562,7 563, 6 -NH- (CH2) 7-NH-C (= NH) -NH2 632,8 633,4 NH

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs—N—CH2-Η NH —N — CH2—CH2-q NH2 HH 638,8 639,5 -NH- (CH2) 3-NH-C (= NH) -NH2 576,7 577,5 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 647,8 648,4 NH -N-CH2— {\ — CH2- HH644,8645,7 -NH- (CH2) 6-NH-C (= NH) -NH2 -NH- (CH2) 4-NH-C (= NH) -NH2 590,7 591,7- 141- ----------- 4 ------- Order --------- line (Please read the precautions on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 Specification (210 X 297 mm) 473474 A7 B7 V. Description of the Invention (139) Example 3 5: Similar to Example 32,6-Nitrobenzo [de] isopinene-1,3- Dione and H2N-c6h4- (ch2) 2-conh- (ch2) 2-c6h4-so2-nh2, suitable diamine and (third butoxycarbonylimidazole-1 -ylfluorenyl) carbamic acid third Butyl ester reaction. After removing the protecting group, a compound of the following formula lie is obtained:

lie (ch2) 2-conh- (ch2) 2- General S〇2 * NH2 R1 Calculated in lie MS. Measured. -NH- (CH2) 5-NH-C (= NH) -nh2 669,8 670,5 -NH- (CH2) 2-NH-C (= NH) -nh2 627,7 628,4 -NH- (CH2) 7-NH-C (= NH) -nh2 697,9 698,5

{Please read the notes on the back side before filling out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs NH CH21 NHj JH —N — CH2 — ^ \ H -NH- (CH2) 3-NH-C (= NH) -NH2 641,8 642,3 -nh- (ch2) 3-n (ch3) C (= NH) -NH2 " (CH2) 3-NH- -N —CH2-Y " H NH CH2- 142 -This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (

Similar to Example 32, 6-Nitrobenzo [de] isopinene], ^ dione blood GHHCHA-CO Rexinza, suitable diamine and (third butoxycarbonylimidazol-1-ylmethyl) ) Tertiary Butyl Amino Acid Reaction. After removing the protective group, a compound of the following formula is obtained: ---------- 1 -------- Order · -------- (Please read the precautions on the back before (Fill in this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

This paper ruler family standard f (C \ TS) A4 specification (210 X 297 mm) '473474. A7 _B7 V. Description of the invention (141) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-144- -------------------- Order --------- line (Please read the precautions on the back before filling this page) Applicable to China National Standard (CNS) A4 specification (210 X 297 male f) 473474, A7 B7 V. Description of the invention (142) Example 37: Similar to Example 3 2,6-nitrophenylhydrazine [de] isobene- 1,3-dione with

Convenient reaction of diamine and (third butyl-oxoimidopyrazol-1-ylfluorenyl) amino acid ester. After removing the protecting group, a compound of the formula Ilea-IIef is obtained:

Ilea (CH2) 2-C〇NH- (CH2) 2

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, R1, calculated on Ilea MS,% measured, -NH- (CH2) s-NH-C (= NH) -m2 625,2 625,3 -NH- (CH2) 2- NH-C (= NH) -NH2 583,1 583,2 -NH- (CH2) 7-NH-C (= NH) -NH2 6,552 6,3 nH X ✓CH2_n nh -N—CH2H ^) HH ^ f 1665, 2,4 ΝΗΓ —N — CH, f ~ S—meaning NH: HWH 659,2 659,3 -NH- (CH2> 3-NH-C (= NH Bu NH2 597,1 597, 3 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C («NH) -NH2 668,2 668,3 145- ----------- Φ clothing- ------ Order --------- Line (Please read the precautions on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (143) R1 is calculated in Ilea MS (measured)

NIH

2/5 6 6 6, 4 -NH- (CH2) 6-NH-C (= NH) -NH2 639,2 639,4 -NH ~ (CH2) 4-NH-C (= NH) -NH2 611, 1 611,3

--N_ IH-(CH2) 3- RH ~ XN NH ch3 2 611,1 611,6

--Fjl — (CH2) 2 H

NH X N 八 NH2 659,2 659,0 (Please read the precautions on the back before filling this page)

—N

NH, CNH 609,1 609,6

/ -ν Νπ2 —N—CHg-N ~ ^ 637/2 631 ^ 6ΰ > --- // NH Intellectual Property Bureau Employee Consumption Cooperative Cooperative Seal #, 衣

R1 was calculated on Ileb MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 625,2 625,3 -ΝΗ »(CH2) 2-NH-C (* NH) -NH2 583, 1 583,3 -NH «(CH2) 7-NH-C (* = NH) -NH2 6,552 6,4 -146- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) Clothes Binding --------- Line _ 473474 A7 _; _B7 V. Description of Invention (144) Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

--------- See ------- --Order ------ I--line (Please read the precautions on the back before filling this page) -147- This paper size is applicable to China National Standard (CNS) A4 Specification (210 X 297 mm) 473474 A7 B7 V. Description of Invention (145)

Itec (ch2) 2-conh- (ch2) 2 — (^ j) —Cl Printed R1 by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs and calculated it on Ilec MS. Measured-NH- (CH2) 5-NH-C {= NH) -NH2 625,2 625, 4 -NH- (CH2) 2-NH-C (= NH) -NH2 583,1 583, 4 -NH- (CH2) 7-NH-C (= NH) -NH2 6,552, 5, 5 NH X / CH2—q nh2 / ~ (H 6,652,4 -N—CH2- < > HW NH —N — CH2 ~~ ^ ~ ^ —CH2_N NH2 659,2 ′ 659, 4 HWH -NH- (CH2) 3-NH-C (= NH) -NH2 597,1 597, 3 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH- 668,2 668,4 C (-NH) -NH2 NH —N-CHn- (^ -CH2-N ^^ NH2 2,652, 4 HWH -NH- (CH2) 6-NH-C (= NH) -NH2 639 , 2 639, 5 -NH- (CH2) 4-NH-C (= NH) -NH2 611,1 611, 4

• N— (CH2) 3-H NH XN ^ NH ch3 2 611, 612,4 (Please read the precautions on the back before filling this page) -------- Order ----- Line-14 8-This paper size is in accordance with Chinese National Standard (CNS) A4 (210 x 297 mm) 473474 A7 B7 V. Description of the invention (w)

R1 is calculated on the lid MS. Measured ΗNΗ-Ν-CH2-C ~ ^ -CH2_1 NH2 HH 637,2 637,3 -NH- (CH2) 6-NH-C (= NH) -NH2 611,1 611 , 3 -NH- (CH2) 4-NH-C (= NH) -NH2 583,1 583,3 NFT XN— (CH2) 3—N ^ NH2 H CH, 583, 583, -N I Η (CH2) 2

631,1 631,2 (Please read the notes on the back before filling out this page) —Ν νη2ΝΗ 581,1 581,3 Ν—CH〇 ι ά Η

ΝΗ7ΝΗ 609,1 609,3 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -150- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 'B7 V. Description of the invention (148)

CI R1 calculated on Ilee MS. Measured -NH- (CH2) 5-NH-C (= NH) -NH2 611,1 611,4 -NH- (CH2) 2-NH-C (= NH) -NH2 569 , 1 569,4 -NH- (CH2) 7-NH-C (= NH) -NH2 639,2 639,3 NH X CH2-N NH2 Η

651,2 651,5 Printed clothing for consumer cooperatives of employees of the Intellectual Property Bureau of the Ministry of Economic Affairs NH —N — CH2 — ^ ~ S—CH2 — NH2 HH 6,492 6,4 -NH- (CH2) 3-NH-C ( = NH) -NH2 583,1 583,5 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (-NH and NH2 654,2 654,2 NH -N —〉 -CH2 -651,2 651,6 -NH- (CH2) 6-NH-C (= NH) -NH2 625,2 625,3 -NH- (CH2) 4-NH-C (= NH) -NH2 597,1 597,4 Nh person-N— (CH2) 3—'NH2 H CH3 .151 —------------------- Order --------- line (please Please read the notes on the back before filling this page) This paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 'B7 V. Description of the invention (149) Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs system

-152- ------------ Cloth -------- Order --------- Thread (Please read the precautions on the back before filling this page) Standards apply to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7B7

V. Description of the invention (150)

Relief MS calculation (actually measured) NH -N — CH2 — factory)-CH2-q sense NH2 HH 637,2 > 637,5 -NH- (CH2) 6-NH-C (= NH) -NH2 611,1 611 , 3 -NH- (CH2) 4-NH-C (= NH) -NH2 583,1 583, 3 Example 38: similar to Example 3 2,6-nitrobenzo [de] isopinene-1, The 3-dione is reacted with the corresponding diamine of H2N-C6H4- (CH2) 2-CONH-CH2-Ar and the tertiary butyl ester of (third butoxycarbonylimidazole-l-ylmethyl) amine. Remove the protecting group and use h2n-C6H4_ (CH2) 2_CONH-CH2-CioH7 to obtain a compound of the formula Ilfa: R1 0 ^ ^^^ (CH2) 2-CONH-CH2- R1 Calculated in Ufa MS 値 found -NH -(CH2) s-NH-C (= NH) -NH2 626,8 627,3 -NH- (CH2) 2-NH-C (= NH) -NH2 584,7 585,3 -NH- (CH2) 7-NH-C (= NH) -NH2 654,8 655,4 -153- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 g t) ----------- -Install -------- order --------- line (please read the precautions on the back before filling this page)

Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 _: _ B7 V. Description of the Invention (151) Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the precautions on the back before filling this page) -154- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7. B7 V. Description of the invention (152) R1

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs on R1 and calculated on Ilfb MS. Measured -NH- (CH2) 5 ~ NH-C (= NH) -NH2 602,7 603,3 -NH- (CH2) 2-NH -C (= NH) -NH2 560,7 561, 4 -NH- (CH2) 7-NH-C (= NH) -NH2 630,8 631, 3 NH X .CH2—N NH2 j— \ H 642, 8641,5 -N—CH2— <) HN ~ f NH —N —CH2——CH2—N ^ NH2 HH 636, 8 637,3 -NH- (CH2) 3-NH-C (= NH)- NH2 574,7 575, 6 -NH- (CH2) -3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 6,548,5 RH ~ —N — CH2 — (— ) —CH2-Qiaoyi NH2 HN-'H 642,8 6,455 -NH- (CH2) 6-NH-C (= NH) -NH2 616, 8 617,4 -NH— (CH2) 4-NH- C (= NH) " NH2 588,7 589,4 -155- -------------------- Order --------- line (please Please read the notes on the back before filling this page) This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (153) R1 Calculated in Ilfb MS (measured) NH X -(CH2) 3—N NH2 ch3 —N— 1 H 612,7 613, 6 —N — 1 H NH-(CH2) 2 — \-N ^ NH2 660,8 661,0 Plant—N-Λ / NH2 J NH 610,7 611,6 Λ Wz 638, 639, 6 N—CH〇 I z Η

Ν--4 ΝΗ Example 3 9: Similar to Example 3 2,6-nitrobenzo [de] isorene-1,3-dione and 3- (3-aminephenyl) -N- (3- Gas 4-methoxyphenyl) propanamide, a suitable diamine and (third butoxycarbonylimidazol-1-ylmethyl) carbamic acid tert-butyl ester. After removing the protecting group, a compound of the formula Ilg is obtained: R1 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

CI och3 R1 Calculated in Ilg MS. Measured. -NH- (CH2) 5-NH-C (= NH) -NH2 627,1 627,3 -156- This paper size applies to China National Standard (CNS) A4 specification (210 X 297 mm) ------------------- Order --------- line (Please read the precautions on the back before filling this page) 473474 A7 B7 V. Description of Invention (154) '' Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-157- (Please read the precautions on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297mm f)

473474 A7 B7 V. Description of the invention (155 Example 40: similar to Example 32, 6-Nitrophenylhydrazone [de] isoprene-1,3-dione and 3- (3-aminephenyl) -N- (4-Phenylbutyl) propanamidin suitable diamine and (third butoxycarbonylimidazole-1 -ylfluorenyl) aminoacetic acid tert-butyl ester. After removing the protecting group, the following formula Ilh is obtained Compound: llh ^ (ch2) 2-conh- (ch2) 4— -u> R1 was calculated in Ilh MS. Measured 値 -NH- (CH2) s-NH-C (= NH) -NH2 618,8 619, 4 -NH- (CH2) 2-NH-C (= NH) -NH2 576,7 577,3 -nh- (ch2) 7-nh- -C (= NH) -NH2 6,648,647,4 —γ —Ch2—QH, NH X / CH2—q nh2 5 H 658,8 659,4 -N —CH2-/ " H NH -CH2-n ^^ nh2 JH 652,8 56,4 -NH- (CH2) 3-NH-C (= NH) -NH2 590,7 591,3 -NH- (CH2) 3-N (CH3) C (= NH) -NH2-(CH2) 3-NH- 661,8 662,4 NH Λ ί CH2—N NH2 JH 658,8 659,5 —ch2—LH -NH- (CH2) 6-NH-C (= NH) -NH2 632,8 633,4 This paper size applies to the Chinese National Standard (CNS ) A4 size (210 X 297 male f) -------------------- Order --------- line (Please read the precautions on the back before (Fill in this page) Staff Consumption of Intellectual Property Bureau, Ministry of Economic Affairs Printed by Sakusho-158- 473474 A7 B7 V. Description of the invention (156) R1 is calculated in Ilh MS. Actual measurement. -NH- (CH2) 4-NH-C (= NH) -NH2 604,8 605,4 NM X 1 NH2 ch3 — [sj- (. 2) 3 604,8 r .. 605,7 -N — (CH2) 2— &H; NM 652,8 56,3 / TVstrict—N N- ^ v__y nh 602,7 603, 8 —N—CH2- ^ H Λ / NM2 N— ^ J NH 630,8 631, 6 Example 4 1 ： Similar to Example 3 2,6-nitrophenylhydrazone [de] isorbene- 1,3-dione with

The appropriate diamine is reacted with (third butoxycarbonylimidazole-l-ylmethyl) carbamic acid tributyl ester. After removing the protecting group, the compound of the formula IIia_IIic is obtained: --------------------- Order --------- line (please read the back Please fill in this page for attention) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -159- 473474 A7 B7 V. Description of the invention (157) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-160- -------------------- Order --------- Line (Please read the notes on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 V. Description of invention (158)

Consumption cooperation between employees of the Intellectual Property Bureau of the Ministry of Economic Affairs, printed R1 and calculated in Ilib MS, measured directly -NH- (CH2) 5-NH-C (= NH) -NH2 ** 604,8 605,4 -NH- ( CH2) 2-NH-C (= NH) -NH2 562,7 563,3 -NH- (CH2) 7-NH-C (= NH) -NH2 632,8 633,4 —ch2— H ^ NH / CH2 -q sense NH2 5 H 6,408,6,6 NH V—ch2—n ^ nh2 / H Ch2 {H 638,8 639,5 -NH- (CH2) 3-NH-C (= NH) -NH2 576, 7 577,6 -NH- (CH2) 3-N (CH3) C (= NH) -NH2-(CH2) 3-NH- 647,8 648,4 NH λ x) —CH2—N NH2 / H644 8645,7 -NH- (CH2) 6-NH-C (= NH) -nh2 618,8 619,4 -NH- (CH2) 4-NH-C (= NH) -NH2 590,7 591,4 RTR u 1 eight nh2 ch3 —N- (CH2) 3— H 590,7 591,8 NH “NHz —fj! — (CH2) 2— H 638,8 639,3 -161- ------ ------------- Order --------- Line (Please read the precautions on the back before filling this page) This paper size applies to China National Standard (CNS) A4 specifications 210 X 297 male t) 473474 A7 B7

'C2H5

R1 calculated from Ilic MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 590,7 591,3 -NH- (CH2) 2-NH-C (= NH) -NH2 548, 6 549, 6 -NH- (CH2) 7-NH-C (= NH) -NH2 618,8 619,4 NH ------------ clothing -------- 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

Nh —N —CH2— < f ~ ^) — CH2-q NH2 H ^ = 7 H 624,7 625,4 -NH- (CH2) 3-NH-C (= NH) -NH2 562,7 563 , 5 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 633,8 634,4 -162- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 i. Description of the invention (160) R1 Calculated in Ilic MS. Η '^ / Η 630,8 631,8 -NH- (CH2) 6-NH-C (= NH) -NH2 604,8 605,2 -NH- (CH2) 4-NH-C (= NH)- NH2 576,7 577,5 Example 4 2: 4 · 1 g of 6-acylphenylhydrazone [< 16] iso (1 g of -1,3-dione in 100 ml of glacial acetic acid 4.3 g of 3- (3-aminophenyl) propionic acid was treated and the mixture was heated under reflux. After the reaction was completed, the reaction was allowed to cool and operated as usual. 3- [3- (6-nitro -1,3 -dioxo-2,3 -dichloro_1 ^^ _ benzene diphenyl-2-yl) phenyl] propanoic acid in 80 ml of THF, the mixture was stirred and 5 equivalents of 2-p-ethylethylamine were added. After the conversion is complete, the mixture is handled in the usual way. Treat i-propane-1,3-diamine with 3- [3- (6-nitro-1,3-dioxo-2,3-dihydro_1Hphenen-2-yl) phenyl] -N- (2-p-ethylethyl) propanamide The solution of DMF was heated under reflux and the mixture was heated under reflux. After normal operation, the amount of Ejuni carboxyamidamine and diisopropylethylamine were heated in 80 ml of DMF. After the reaction was completed, the obtained amine was obtained after normal operation. 3- {3- [6- (3 -guanidinopropylamino) 〖a _2,3-dihydro-1H-phenylen_2_yl] phenyl} -N- (2-p-ethylethyl) propyl Fermented amine. MS: Pair calculation: 576.7; Measured osmium: 577.4. Example 4 3: Similar to Example 32, 6-Nitrobenzo [de] isobate bridge, · A, h two-dimensional deficiency ----- ---------------- Order --------- Line '(Please read the notes on the back before filling this page)

This paper size applies Chinese National Standard (CNS) A4 specification (210 x 297 mm) 473474 A7 B7 V. Description of the invention (161) Convenient diamine and (third butoxycarbonylimidazole-pyridylmethyl) amine Tertiary formic acid reaction. After removing the protecting group ', a compound of the following formula Ilka-IIke is obtained: R1

CI (Please read the notes on the back before filling out this page) The Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs prints R1 and calculates it in Ilka-MS. Measured -NH- (CH2) 5-NH-C (= NH) -NH2 6456 \ 6454 -NH- (CH2) 2-NH-C (= NH) -NH2 603,5 603,3 -NH- (CH2) 7-NH-C (= NH) -NH2 673,6 673,4 r NH X / CH2—N NH2 i H 685,7 685,4 -IJJ—ch2— ^ -n- ^ ch2-h ^ " NH Λ—ch2-q senseNH2 679, 6 679,3 H ^ = 7 H -NH- (CH2) 3-NH-C (= NH) -NH2 617,5 617,3 NH X —N NH, \ 2 -N— (CH2) 3- 631,6 631, 4 H ch3 -164- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 χ 297 mm) 473474, A7 _B7 V. Description of the invention (162) Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

R1 was calculated from Ilkb MS. Measured: -NH- (CH2) s-NH-C (= NH) -NH2 4,656,645 -NH- (CH2) 2-NH-C (= NH) -NH2. 603 , 5 603,3 -NH- (CH2) 7-NH-C (= NH) -NH2 673,6 673,4 fTFT X yCH2—N NH2 -N —CH2—HH ~ '685,7 685,5 RH- N — 0Η2 — ^^ — 0Η2-Ν ^ ΝΗ2 Η H 679,6 679,3 -NH- 《CH2) 3-NH-C (= NH) -NH2 617,5 617,5 -NH- (CHZ) 3 -N (CH3)-(CH2) 3-NH- 688,7 688,4 -165- ϋ IIIIIIIII ϋ -111 n I n ϋ Order --------- line (Please read the precautions on the back first (Fill in this page again) This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 male f> 473474 A7 B7

R1 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-166- This paper size applies to China National Standard (CNS) A4 (210 X 297 male f) -------------------- Order ------- --Line (please read the notes on the back before filling this page) 473474 Α7 Β7 V. Description of the invention (164)

NH A

CH2_N 'NH2 Η 685,7 686,6 NH / " Λ X -N — CH2— (7 V-CH2—N NH2 H-Η 679, 6 681,3 -NH- (CH2) 3-NH-C ( = NH) -NH2 617,5 618, 6 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 688,7 688,5 NH / — \ Jl — N-CH2- (/ -CH2_N NH2 HH 685,7 686,5 -NH- (CH2) 6-NH-C (= NH) -NH2 659,6 659,4 -NH- (CH2) 4-NH-C (= NH) -NH2 631, 6 633, 3 Ί \ ίΗ -N— (CH2) 3-Η Ν NH, CH, 631,6 632,5 ~ N — (CH2) 2 Η

679,6 679,1 • Ν Λ 7 ^ 2 ΝΗ 629,5 630, clothing -------- order --------- line (Please read the precautions on the back before filling this page ) Printed Agriculture

657,6 658, 6 167- The size of this paper applies to the Chinese National Standard (CNS) A4 (210 X 297 mm) 473474, A7 B7 V. Description of the invention (165)

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

-168- ------------ Cloth -------- Order --------- ^ Ά-wi (Please read the notes on the back before filling this page ) This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (166) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

R1 is calculated based on like MS. -NH- (CH2) 5-NH-C (= NH) -NH2 631, 6 631,2 -NH- (CH2) 2-NH-C (= NH) -NH2 589 , 5 589,1 -NH- (CH2) 7-NH-C (= NH) -NH2 659,6 659,2 Plant NH X / CH2-n nh2-\ H 671, 6 671,2 ~ [ί | — ch2-\ _) NH \ —ch2—n ^ " nh2 JH —N—CH2 ~ ^ H ^ 6,656,1 -NH- (CH2) 3-NH-C (= NH) -NH2 603,5 603,2 -KH- (CH2) 3-N (CH3) C (-NH) -NH2-(CH2) 3-NH- 674,6 674,2 -169- ----------- --------- Order --------- Line (Please read the precautions on the back before filling this page) This paper size applies to China National Standard (CNS) A4 (210 X 297 male) f)

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474. A7 B7 V. Description of the invention (167) R1 is calculated on like MS. , 2 -NH- (CH2) 6-NH-C (= NH) -NH2 4,656,645 -NH- (CH2) 4-NH-C (= NH) -NH2 617,5 619,2 Example 4 4: Similar to Example 3 2,6-nitrobenzo [de] isopinene-1,3-dione and 3- (3-aminephenyl) -N- (3-chloro-4-fluorobenzyl The reaction of propylammonium diamine and (third butoxycarbonylimidazol-1-ylmethyl) aminoacetic acid tert-butyl ester. After removing the protecting group, a compound of the formula Ilm is obtained:

A

l ^^ (CH2) 2-C〇NH-CH2 — \ _) ~ F

Nci R1 calculated on Ilm MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 629,1 629,5 -NH- (CH2) 2-NH-C (= NH) -NH2 587 , 1 587,5 -NH- (CH2) 7-NH-C (= NH) -NH2 657,2 657,3 -170- 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) 473474 A7 B7 V. Description of the invention (168 ) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the precautions on the back before filling this page)

7 This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 male f 473474 A7 B7 V. Description of the invention (170) ’Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-173- I ---------- ^ 一! ^ 衣 -------- Order --------- line (Please read the precautions on the back before filling in this Page) This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 male f) 473474, A7 _B7 V. Description of the invention (171) Employees of the Intellectual Property Bureau of the Ministry of Economic Affairs, Consumer Cooperatives, Printed Agriculture

-174- ϋ K n I nn ϋ nn ϋ n 210 X 297 mm) 473474 A7 B7 V. Description of the invention (172) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

Example 4 6: Similar to Example 3 2,6-Nitrobenzo [de] isopinene-1,3-dione and -175- This paper size is applicable to China National Standard (CNS) A4 (210 X 297) f) I I --- nnn II f ϋ n · ϋ nn I n ϋ n Order --------- ^ (Please read the notes on the back before filling this page) 473474 A7 V. Description of the invention ( 173)

A suitable diamine is reacted with a tertiary butyl ester of (third butoxycarbonylimidazol-1-ylmethyl) carbamic acid. After removing the protective group, the following compounds II0a-IIoc are obtained: Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

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) 473474

F (Please read the notes on the back before filling this page) The Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs prints R1 and calculates it on Ilob MS. -NH- (CH2) 5-NH-C (= NH) -NH2 594,7 595,5 -NH- (CH2》 2-NH-C (= NH) -NH2 552, 6 553,4 -NH- (CH2) 7-NH- C (= NH) -NH2 622,7 623 , 2 -N —CH2-/ " H NH X / CH2—q nh2 5 H 634,8 635,5 -N —CH2— H NH y—CH2-q sense NH2 628,7 629,4 -NH- ( CH2) 3-NH-C (= NH) -NH2 566,6 567,5 -nh- (ch2) 3-n (ch3)-(ch2) 3-nh- 637,8 638,3 C (= NH) -NH2 —N — CH2— (H ^ —CH2-q sense NH2 634,8 635, 6 -NH- (CH2) 6-NH-C (= NH) -nh2 608,7 609, 3 -NH- (CH2 ) 4-NH-C (= NH) -NH2 580,7 581,4

Clothing -------- tr --------- line I -177- National Standard (CNS) A4 specification (210 x 297 male f) 473474 A7 B7 V. Description of the invention (175) R1

Hoc

(〇Η2) 2-〇〇ΝΗ R1 was calculated on Iloc MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 580,7 581,3 -NH- (CH2) 2-NH- C (= NH) -NH2 538,6 539,3 -NH- (CH2) 7-NH-C (= NH) -NH2 608,7 609,3

620,7 621, NH -N-CH2- (~ ^ -CH2_N ^^ NH2 HH 614,7 615,2 -NH- (CH2) 3-NH-C (= NH) -NH2 552,6 553,4- ----------- Clothing -------- Order --------- line (please read the precautions on the back before filling this page) Staff of Intellectual Property Bureau of Ministry of Economic Affairs Printed by Consumer Cooperative Example 4 7: Similar to Example 3 2,6-nitrobenzo [de] isopinene-1,3-dione and 3- (3-aminephenyl) -N- (3-benzene The reaction of oxyphenyl) propanilamine, expedient diamine and (third butoxycarbonylimidopyrazol-1-ylmethyl) carbamic acid third butyl ester. After removing the protecting group, a compound of the formula Πρ is obtained:- 178- The size of this paper applies to Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (176)

/ OPh 4 R1 Calculated in lip MS. Measured. Printed clothing for employees' cooperatives in the Intellectual Property Bureau of the Ministry of Economy. -NH- (CH2) 5'NH-C (= NH) -NH2 -NH- (CH2) 7-NH-C (= NH) -NH2 682,8 683,3 —N — 1 H NH X / CH2—N NH2 -〇h2- < 5 H 694,8 695,4 -NH- (CH2) 2-NH-C ( = NH) -NH2 —N — 1 H NH -ch2— (~ \ — ch2- H 688,8 689,4 -NH- (CH2) 3-NH-C (= NH) -NH2 626,7 627,4 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH 'C (= NH) -NH2 697,8 698,4 —N — 1 H NH CH2-H ^ V—ch2-n ^ nh2 N ~ / H 694,8 695,6 -NH- (CH2) 6-NH-C (= NH) -NH2 668,8 669,3 -NH- (CH2) 4-NH-C (= NH) -NH2 640,7 641,5 NH Sense- (CH2) 3—N NH2 ch3 —n— 1 H 640,7 641,5 NH-(ch2) 2 ^ 3 ~ n / nh2 —N — 1 H 688,8 689, 2 -179- ------------------ Order --------- Line (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 male f) 473474 A7 B7 V. Description of the invention (177)

Example 48: Similar to Example 3 2,6-nitrobenzo [de] isofluorene-1,3-dione and 3- (3-aminephenyl) -N- (3-benzyloxyphenyl) The reaction of propylammonium diamine and tertiary butyl amine ((third butoxycarbonylimidazole-l-ylmethyl) amine). After removing the protecting group, the following compound of formula Ilq is obtained: (Please read the precautions on the back before filling this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

R1 was calculated in Ilq MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 668,8 669, 3 -NH- (CH2) 2-NH-C (= NH) -NH2 626, 7 627,4 -NH- (CH2) 7-NH-C (= NH) -NH2 696,8 697,3 -180- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 _B7 V. Description of the Invention (178)

-------------------- Order --------- Line (Please read the notes on the back before filling this page) Employees of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by Consumer Cooperative Example 4 9: Similar to Example 32,6-Nitrobenzo [de] isopinene-1,3-dione and 3- (3-aminophenyl) -N-tea-2-yl The reaction of propylammonium diamine and (tertiary butoxycarbonylimidazole-1 -yl amidino) aminoacid third butyl ester. After removing the protecting group, the compound of the following formula is obtained: -181- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 ^ Description of the invention (179)

R1 at Ilr -NH- (CH2) 5-NH-C (= NH) -NH2 -NH- (CH2) 2-NH-C (= NH) -NH2 -NH- (CH2) 7-NH-C (= NH) -NH2 yCH2-

NH X • N NH, \ 2 H Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs—N-CH2 H —N — CH2— Η NH ch2-q Sense nh2 JH -NH- (CH2) 3-NH-C ( = NH) -NH2 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH- C (= NH) -NH2 —N-CH2— (H —CH2-ν " ^ νη2 -NH- ( CH2) 6-NH-C (= NH) -NH2 -NH- (CH2) 4-NH-C (= NH) -NH2 NH X -N nh3 ch3 -N— (CH2) 3-H 1 —— (CH2 ) 2— H NH Meaning NH2 ------ —Order --------- line (Please read the precautions on the back before filling out this page) -182 · This paper size applies to Chinese National Standards (CNS ) A4 size (210 X 297 mm) Printed by the Consumer Cooperatives of the Bureau of Wisdom and Finance, Ministry of Economic Affairs 473474 V. Description of invention (180) A7 B7

Example 5 0: ------ _ Similar to Example 32,6_Nitrobenzene [de] isobitazone- 丨 Hydroxydione% Γί ί η methyldi: amine diisodiamine and (section Tributoxycarbonylimide ertochemical compound) vinegar reaction. After removing the protective base, I get 1 -------------------- Order --------- line (Please read the phonetic on the back? Matters before filling in (This page)

This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 _B7 V. Description of the invention (181)

-------------------- Order --------- (Please read the note on the back before filling out this page) Example 5 1 ·· Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, similar to Example 3 2,6-Nitrophenylpyrene [de] isoprene-1,3-dione and 3- (3-aminephenyl) -N- (3 -Fluoro-4-amidophenyl) propanamidin suitable diamine and (third butoxycarbonylimidazolepyrazol-1-ylmethyl) amine formic acid tertiary ester reaction. After removing the protective group, a compound of the following formula is obtained: -184- This paper size applies the Chinese National Standard (CNS) A4 specification (210 x 297 male f) 473474 A7

B V. Description of the invention

185- Qingbo's scale is applicable to China National Standard (CNS) A4 (210 χ 297 mm) --------------------- Order ----- ---- Line 1 (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 473474 V. Description of Invention (183). A7 _B7

Example 5 2: Similar to Example 3 2,6-nitrobenzo [de] isopinene-1,3-dione and 3- (3-aminephenyl) -N- (3-fluoro-4-toluene The reaction of propylammonium diamine and tertiary butyl (3rd butoxycarbonylimidazole-l-methyl) carbamate. After removing the protecting group, the compound of the formula IIu is obtained as follows: --------------------- Order --------- line (Please read the precautions on the back before (Fill in this page)

-186- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (彳 84)

Similar to Example 32,6-Nitrobenz [de] isoniane η,% dione with

The reaction of och3, och3 diamine and (third butoxycarbonylimidazole-ylmethyl) carbamate. After removing the protecting group, the compound of the formula IIva_IIvb is obtained: ------------- φ clothing ------ --order --------- (Please read the Please fill in this page for attention) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

llva (CH2) 2-CONH- (CH2) 2

-187- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 x 297 male f 473474 A7 B7 V. Description of the invention (185) R1 Calculated in Ilva MS (measured) -NH- (CH2) s-NH-C (-NH) -NH2 650,8 651,5 -NH- (CH2) 2-NH-C (-NH) -NH2 608,7 609,5 -NH- (CH2) 7-NH-C (= NH) -NH2 678,8 67 9,4 NH X / CH2—N NH2 / ~ {H 690,8 691, 6 -N—CH2- < > HN / NH —N-CH2— (~ CH2-N " ^ NH2 HH 684,8 685,5 -NH- (CH2) 3-NH-C (= NH) -NH2 622,7 623,5 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH -C (= NH) -NH2 693,8 694,4 NH / ~ \ —N — CH2— () —CH2—N NH2 HN ~ f H 690,8 691,6 -NH- (CH2) 6-NH- C (= NH) -NH2 664,8 5,4 -NH- (CH2) 4-NH-C (= NH) -NH2 636,7 637,5 Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

C

OCH

OCH3 3 R1 Calculated in IWb MS (measured) -NH- (CH2) s-NH-C (= NH) -NH2 650,8 651,4 -NH- (CH2) 2-NH-C (= NH) -NH2 608,7 609,5 188- This paper size applies to China National Standard (CNS) A4 specification (210 X 297 male I) -------------------- Order- ------- line (please read the precautions on the back before filling this page) 473474 A7 B7 V. Description of the invention (186) R1 Calculated in llvb MS (Actual measurement) -NH- (CH2) 7-NH-C (= NH) -NH2 678,8 679,4 Plant Nh X .CH2—N NH2 5 H 690,8 691,8 —N—CH2— (HV NH ^ -CH2-ν ^ " νη2 -N — 684, 8 685,4 HJH -NH- (CH2) 3-NH-C (= NH) -NH2 622,7 623,4 -NH- (CH2) 3-N (CH3) C (= NH) -NH2-(CH2 ) 3-NH- 693,8 694,4 NH —ch2-q nh2 JH -CH2 ~ (~ H 690,8 691, 6 -NH- (CH2) 6-NH-C (= NH) -NH2 664, 8665,3 -NH- (CH2) 4-NH-C (= NH) -NH2 636,7 637,4 (Please read the notes on the back before filling this page) Example 5 4: Similar to Example 3 2 Economy Printed by the Ministry of Intellectual Property Bureau's Consumer Cooperative

6-Nitrophenylpyrene [de] isobitazone-1,3-dione and CH2) 2-C〇NH-CH2 ——ocf3 Convenient diamine and (third butoxycarbonylimine pyrazole-1-yl Amidino) tert-butyl carbamate reaction. After removing the protecting group, a compound of the following formula IIW is obtained ... -189- This paper size applies to the Chinese National Standard (CNS) A4 specification (210 X 297 male f) 473474 A7 ′ B7 V. Description of the invention (187)

-CV〇CF3 R1 at Ilw -NH- (CH2) s-NH-C (= NH) -NH2 -NH- (CH2) 2-NH-C (= NH) -NH2 -NH- (CH2) 7-NH -C (= NH) -NH2

NIT .1

CH2—N NH2 H

-NH- (CH2) 3-NH-C (-NH) -NH2 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 ------ -------------- 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

-NH- (CH2) 6-NH-C (= NH) -NH2 -NH- (CH2) 4-NH-C (= NH) -NH2 Example 5 5: Similar to Example 32,6-Nitrophenylhydrazone [ de] Isorpene-1,3-dione and 190 · This paper size is applicable to China National Standard (CNS) A4 (210 X 297 g t) 473474 A7 B7 V. Description of the invention (彳 88)

H2N

CH2) 2-C〇NH-CH2-

Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, the reaction of diamine and (third butoxycarbonylimidazol-1-ylmethyl) carbamic acid ester. After removing the protecting group, a compound of the following formula lm is obtained: lm (CH2) 2-C〇NH-CH2-0) R1 Calculated in lm MS. Measured -NH- (CH2) 5-NH-C (= NH)- NH2 -NH «(CH2) 2-NH-C (= NH) -NH2 524,6 525,3 -nh- (ch2) 7-nh-c (= NH) -NH2 594,7 595,3 NH X ^ Η2-N NH2 H 606,7 607,3 -N-CH2— () H ^ CH2-〇-Η λ ~ NH Ji -CH2-N NH2 H 600,7 601,2 -nh- (ch2) 3-nh -c (= nh) _nh2 538,6 539,4 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH- 609,7 610,3 C («= NH) -NH2 NH-ch2 -q meaning nh2 H —n—ch2 — /-y 606,7 607,4 -NH- (CH2) 6-NH-C (= NH) -NHz 580,7 581,3 -NH- (CH2) 4- NH-C (= NH) -NH2 9 This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)

4 347 V A7 B7 Description of the invention (189) 1 case 5 6: Similar to the conventional example, 2- (4-aminophenyl) -3- (4-dimethylamine benzyl) propionitrile and 6-nitrobenzo [de] Isoamidine-1,3-dione reaction followed by * Ri_H reaction. The following formula In compounds and compounds are obtained:

N: ch: (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

N R1 was calculated in In MS and measured. -NH- (CH2) 5-NH2 545 ~~~-546 -NH- (CH2) 7-NH2 573. 574 NH2 -N —CH2- / 7) HW Example 57: At room temperature, 10 ml of TFA was added to 2.4 g of [3- (2- {4- [1-cyano-2- (4 dimethylaminephenyl) ethyl] phenyl} -1,3 -Dioxo_2,3-dihydro-1H-benzene 幷 [de] 莫 • 192- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) Order -------- -Line · Doo. 4/4 Printed by the Intellectual Property of the Ministry of Economic Affairs, A7 B7 printed by the Consumer Cooperative of the Bureau V. Description of the invention (19〇) · Pyridin-6-ylamino) propyl] aminoacetic acid tert-butyl ester 40 ml of dichloromethane hydrazone solution [obtained from 6-nitrophenylhydrazine [de] isoprene decanedione and 2- (4-aminophenyl) -3- (4-dimethylaminephenyl) propionitrile And H2N_ (CH2) 3_Nhboc]] and the reaction mixture was discarded until removal was complete. After the routine operation is completed, 2- {4- [6- (3-Aminopropylamino) 4,% dioxo_1H 3H_benzo [de] isoquinolin_2_yl} -3- (4-di Methylamine phenyl) propionitrile. Similar to Example 32,6-Nitrobenzo [de] isofluoren-1,3-dione and / CH2) 2-CONH- (CH2) 2-CH (h2n-〇Ph suitable diamine and (third Butoxycarbonylimidazole-l-ylfluorenyl) carbamic acid third butyl alcohol reaction. After removing the protecting group, a compound of the formula Ioa is obtained: R1

-193-} The paper size applies the Chinese national standard (CNSM4 specification (210 X 297 male f) -------------------. I order -------- -Line (please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (191 R1 Calculated in Ioa MS (Actual measurement) -NH- (CH2) s-NH-C (= NH) -NH2 680 , 8 681,4 -NH- (CH2 > 2- -NH-C (= NH) -NH2 638,8 639, 6 -NH- (CH2) r -NH-C (= NH) -NH2 708,9 709 , 4 —N—CH2 ~ H Nh X / CH2-n nh2 < 5 H 720, 9 721,6 Nh ch2-n ^ nh2 \ = yh —N ——CH2— H 714,9 715,5 R1 in Ioa MS calculations 値 found -NH- (CH2) 3-NH-C (= NH) -NH2 652,8 56, 6 -NH- (CH2) 3-N (CH3)-(CH2) 3-NH-C (= NH) -NH2 723,9 724,4 NH -N-CH2- ^ ^ -CH2-N ^ " NH2 H,-/ H 720, 9 721, 6 -NH- (CH2) 6-NH-C (= NH) -NH2 694,9 695,4 -NH- (CH2) 4-NH-C (= NH) -NH2 666,8 667,3 ------------ clothing ---- ---- Order --------- line (please read the notes on the back before filling out this page) The employee's consumer cooperative stamp of the Intellectual Property Bureau of the Ministry of Economic Affairs * 1 clothing Example 5 9 ： Similar to Example 3 2

ch2) 2-conh-ch2-ch, -nitrobenzo [de] isopinene-1,3-dione and / Ph

Ph -194- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474. A7 B7 V. Description of the invention (192) Convenient diamine and (third butoxycarbonylimine pyrazole-1 -Methylmethyl) amino acid diester reaction. After removing the protecting group, a lob compound of the following formula is obtained: R1

R1 is calculated from lob MS. Measured: -NH- (CH2) 5-NH-C (= NH) -NH2 666,8 667,3 -NH- (CH2) 2-NH-C (= NH) -NH2 624, 7 625,5 -NH- (CH2) 7-NH-C (= NH) -NH2 694,9 695,4 NH h -N — CH2— < r ^) — CH2-N ^ NH2 700,8 701, 4 HWH NFT χ CH2-N NH2 706,9 H ------------ ^^ 衣 -------- Order --------- line (please read first Note on the back, please fill out this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 707, 6 —N-CH Η -NH- (CH2) 3-NH-C (= NH) -NH2 638, 639,6- 195- This paper size is applicable to China National Standard (CNS) A4 (210 X 297mm f)

473474, A7 B7 V. Description of the Invention (193) Example 60: Similar to Example 1 1,6-Azylphenylhydrazone [de] isotetrapine-1,3-dione and 4-anisidine or 3-iodoaniline ( = I-Ar'-NH2), HeP-BCOHh and reacts with R1-!!. A compound of the formula 'Ip is obtained: R1

Ar'-Het1 -Ar'-Het1 R1 in R ^ -H and Ip -nh- (ch2) 3-nh2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2 ------ ------ Cloths -------- Order --------- line (Please read the precautions on the back before filling this page) Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs -196-

This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of the invention (194) -Ar'-Het R1 in R1 · !! and Ip: nh: 1ch2} 3-nh2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2

-nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

-NH- (CH2) 3-NH2 -NH— (CH2) 5 ~ NH2 -NH- (CH2) 7-NH2

~ NH— (CH2) 3 ~ NH2 -nh- 《ch2) 5-nh2 -NH- (CH2) 7-NH2

-NH- (CH2) 3-NH2 —NH— (CH2) 5—NH2 -NH- (CH2) 7-NH2 -------------------- Order-- ------- (Please read the precautions on the back before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

—NH— (CH2) 3 ~ NH2 -nh- (ch2) 5-nh2 —NH- (CH2) 7 ~ NH2

-197- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of invention (195) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-198- -------------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7

-------------------- Order --------- (Please read the precautions on the back before filling this page) 473474 A7 B7 V. Description of the invention (Ph-Ph = A0. A compound of the formula

C

lr

Ar *-(CH2) n-R6 -Ar '-(CH2) n-R ° R1 at R ^ -H and Ir

-NH_ (CH2) 3-NH2 -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2

(Please read the notes on the back before filling this page)

-nh- (ch2) 3-nh2 -nh- (ch2) 5-nh2 -NH- (CH2) 7-NH2

2

• NT ^ NH

I

H

-NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2 ch3 Printed by the Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs

-nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 male f) -200- 4V3474 A7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (198) Example 6 3 Similar to Example 1 1, 6-nitro-2- (4-iodophenyl) benzo- [de] isoquinoline 1,3-diketone reacts with R10-B- (〇H) 2 and propane-1,3-diamine, Of which Ri〇

〇-C (CH3) 2-CO-〇c2H5 to obtain 2- {4 '-[6- (3-Aminopropylamino) _1,3-dioxy_1h, 3h_phenylhydrazone [de] isoxoline_2 · Yl] biphenyl-4-yl.oxy} -2-methylpropionate. Example 6 4: Similar to Example 2,6-Gas-benzo- [de] isosacene-1,3-dione and 5-oxopyrimidine-2-sulfonic acid (4-aminephenyl) -fluorenamine And propane-, 3-diamine. 5_methoxypyrimido-2-contanoic acid {4- [6- (3-aminopropylamino) _ι, 3-dioxo-1H, 3H-benzyl [de] iso Junplin-2-yl] -Phenyl} _amidamine. Example 6 5: Similar to Example 2,6-Phenylphenylene- [de] isopinene-i, 3-dione and 1_ (6_amino-2,3-dihydroindol-1-yl) _ Ethyl ketone reacts with propylene, 3_ diamine. We get 2- (1-ethyl S & yl-2,3-mono-l-1H-4 丨 h-6-yl) -6- (3-aminopropylamino) -benzyl [de] 异 p 奎 # -1 , 3-dione. Example 6 6: Similar to Example 2,6-chlorophenylhydrazone [de] isorene-1,3-dione and 4- (pyrrolidine-1-sulfonyl) -aniline and propane-1,3- Diamine reaction. 6- (3-Aminepropylamino) -2- [4- (pyrrolidine-1-sulfonyl) -phenyl] -benzo [de] isoquinoline-l, 3-dione is obtained. Example 6 7: —: ----------------- Order --------- Line (Please read the precautions on the back before filling this page) -201- 473474 A7 B7 V. Description of the invention (199) Printed by the Consumer Cooperatives of J Finance Bureau of the Ministry of Economic Affairs, similar to Example 2,6-Chlorobenzo [de] isobitazone-1,3-dione and 4-cyclohexylbenzene The base amine reacts with propane-1,3-diamine. 6- (3-Aminopropylamino) -2- (4-cyclohexylphenyl) -phenylhydrazone [de] isopyrrolidine-i, 3-dione was obtained. Example 6 8: Similar to Example 2,6-Phenylhydrazine_ [de] isopinene-1,3-dione and 3- (3-aminophenyl) -N- (2-phenylpropyl) -propane Amidine and 3-amine methylbenzylamine react. 3_ {3- [6- (3-Aminomethylamidoamine) -i, 3-dioxo-1H, 3H-phenylhydrazone [de] isoamidine_2_yl] -woodyl} -N- (2 -Phenylpropyl) -propanamide. Similarly '6-chlorobenzo- [de] isopinene-1,3-dione with 3- (3-aminebenzyl) N- (l-phenethyl) -propanamide and 3-amine Fluorenylamine reaction to give 3_ 丨 3 _ ^ (3-aminomethylbenzylamino) -1,3-dioxo-1H, 3H-benzo [de] isofluorinyl] phenyl-N- (l -Ethyl) -propanamine. Example 6 9: Similar to Example 2,6-chlorobenzo [de] isofluorene-υ-dione with 3, (3'aminophenyl) -1- (3,4-dihydro-2 丨 quinoline -1-yl) -propane_1-one is reacted with 3-aminomethylcycloamine. 6-[(3-Aminomethyl-Junlin-fluorenyl) _3_oxopropylbenzyl hexadecyl [de] isoρChalin-1,3-dione was obtained. I Example 7 0: Similar to Example 2,6-chlorobenzo [de] isopinene ·, 3-dione and Shishi (S- (CH2) n-CONH- (CH2) i-Ar and 3- Amine-benzylamine reaction. Iya compounds are obtained: The following formula (please read the note on the back? Matters before filling out this page) Order --------- line < -202- This paper size applies to Chinese national standards (CNS) A4 specifications (210 X 297 male f) '473474 A7 B7 V. Description of the invention (200)

Ar'-S- (CH2) n-CONH- (CH2) i-Ar Printed by Employee Consumer Cooperatives, Bureau of Intellectual Property, Ministry of Economy

-------------------- Order --------- Line (Please read the notes on the back before filling this page) This paper size is applicable to China Standard (CNS) A4 specification (210 X 297 mm) 473474, A7 B7 V. Description of invention (201) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

Ar1 -S- (CH2) n-CONH- (CH2) i-Ar in Iya _ ^ Q &gt; _s_ch2—conh-^-^ ch3 — ^^-s—qh2 —C0NH- (CH2) 2— Cl —S— CH2—CONH-CH2 ~~ Cl-<》-S—CH2-CONH * (CH2) 2 ^ Cl —S—CH2—CONH— ^ Cl》 —S—CH2-CONH-CH2 — ^ ^ Cl —s—CH2 —CONHHCH ^ —Cl — 《》 — s—ch2-conh-ch2 — (》 ~~ ci-《》 — S—CH2-CONH— 《—S—CH2 —CONH- (CHj) j— ^ ~ ^ -CH3 》 —S—CH2-CONH— 《~ CH3-^ ^ —S— CH2-CONH-CH2》》 — —S— CH2 — CONH ~~ — ^ ~ S —CH2-CONH 《^ &quot; ~ 〇CH3. Cl -204- -------------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 specification (210 x 297 mm) A7 B7 V. Description of invention (202) Printed by the Employees' Cooperative of the Bureau of Wisdom and Finance of the Ministry of Economic Affairs

-205- (Please read the precautions on the back before filling in this page) Loading -------- Order --------- The size of thread paper is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 V. Description of the invention (203) Printed by the Employees' Cooperative of the Bureau of Smart Finance J Ministry of Economy

_________I__________ Order --------- AW. (Please read the notes on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the Invention (204) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the precautions on the back before filling out this page) Order --------- line- -207- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)

2 473474 A7 B7

Similar to Example 3 2, (Third-butoxycarbonylimidazole-l-ylmethyl) aminophosphonic acid The third butyl ester was reacted with the compound of formula Iya above. After the protecting group is removed,

.NH /

NH ----------- clothing -------- order --------- line (Please read the note on the back first? Matters before filling out this page) Ministry of Economy Wisdom Printed by the Property Agency Staff Consumer Cooperative

Ar * -S- (CH2) n-CONH- (CH2) 「Ar

Ar '-S- (CH2) n-CONH- (CH2) i ~ Ar in Iyb — ^^ — S—CH2—CONH—, Br —CH2— CONH— CN -208- This paper size applies to the Chinese National Standard (CNS ) A4 specification (210 X 297 male f) 473474 A7 __B7 V. Description of invention (206) Printed by the staff consumer cooperative of J Finance Bureau, Ministry of Economic Affairs

(Please read the phonetic on the back? Matters before filling out this page) Φ ----- Order --------- Line. -209- This paper size applies to China National Standard (CNS) A4 specification (210 χ 297 male f) 473474 A7 B7 V. Description of invention (207) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- Line (Please read the notes on the back before filling this page) This paper size is applicable to China Standard (CNS) A4 size (210 X 297 mm) 473474 A7

B V. Description of Invention (208) Printing of clothing by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- Line (Please read the notes on the back before filling this page) This paper size is applicable to China Standard (CNS) A4 size (210 X 297 mm) 473474

7 7 A B V. Description of the invention (209) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------- Order --------- line (please read the precautions on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297mm f ) 473474, A7 _B7 V. Description of the invention (21〇) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order——line (Please read the precautions on the back before filling this page) This paper size applies to China National Standard (CNS) A4 specifications ( 210 X 297 mm) 473474 A7 B7 V. Description of the invention (211) Example 7 1: Similar to Example 2,6-chlorobenzo- [de] isopinene-1,3-dione and fluorene 2N · Ar'- S-iCHA-CONPMCHA-Het1 reacts with 3-amine formamidine. The following formula Iza compounds are obtained:

Ar, -S- (CH2) n-CONH- (CH2) rHet1

Ar '-S- (CH2) n-CONH- (CH2) i-Het1 at Iza — ^ y ~ S—CH2— CONH- (CH2> 2— 0 —s—ch2—conh- (ch2) 3_n people ^ — s—CH2—CONH-CCH;); — '—s—ch2—conh-ch2- ^ J] —s—ch2—conh-ch2 — Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, similar to Example 3 2, The third butoxycarbonylimidopyrazol-1-ylfluorenyl) carbamic acid tert-butyl acetate is reacted with the compound of the formula Iza. After the protecting group is removed, you get -214-

473474 A7 B7 V. Description of the invention (212 Compound of the formula Izb ·

, ΝΗ, ΝΗ 2

Ar'-S- (CH2) n-CONH- (CH2) rHet1

------------------- Order --------- line (Please read the notes on the back before filling this page) Example 7 2 printed by Consumer Cooperative: Similar to Example 2,6-chlorobenzo- [de] isopinene-1,3-dione and H2N-Ar'-S- (CH2) n-CONH- (CH2) rD-H is reacted with 3-aminophosphonium benzylamine. The compound of the formula Ila is obtained as follows: -215- This paper size is in accordance with the Chinese National Standard (CNS) A4 specification (210 X 297 gf)

473474 A7 B7 V. Description of the invention (213)

11a

Ar'-S- (CH2) n-CONH- (CH2) rD-H

Ar1 -S- (CH2) n-CONH- (CH2) i ^ DH in Ila — ^ J &gt; —s —ch2 conh — — ^^ rs—CH2—CONH- (CH2) 2 ~ ^) Similar to Example 3 2 (-(-Tributoxycarbonylimidazole-l-ylmethyl) carbamic acid tert-butyl ester is reacted with the compound of the above formula Ila. After the protecting group is removed, a compound of the following formula lib is obtained:

Ar'-S- (CH2) n-CONH- (CH2) rD-H

Ar'-S- (CH2) „-CONH- (CH2) iDH in I lb… ^^ S—CH2-CONH <〉 ^ —S—CH2— CONH-(CHA — ^ ^ -216- This paper size applies China National Standard (CNS) A4 specification (210 X 297 male f) -------------------- Order --------- line (Please read first Note on the back, please fill out this page again) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 ------- V. Description of the invention (214) ± m 7 3: Similar to Example 2,6-Gasbenzene -[de] isoprene-1,3-dione is reacted with 2- (3-aminephenylsulfanyl) -N- (2-phenylpropyl) -acetamidine and 3-aminomethylbenzylamine. To give 2- {3- [6- (3-Aminomethylbenzylamine) -u-dioxophenylene [de] iso4-line-2-yl] -phenylsulfanyl} _] ^ _ (2-benzyl Propyl) -acetamidine. Similar to Example 32,2- {3 · [6- (3-Aminomethylbenzylamino) -l, 3-dioxo-amidine, 3'-phenylamidine [de] isoamidine -2-yl] phenylsulfanyl group N_ (2-phenylpropyl) acetamidine and (second butoxycarbonylimidazole-1_ylfluorenyl) carbamic acid third butyl ester. After removal of the group, 2- {3- [6- (3-guanidinobenzylamino) _ι, 3_dioxo-1H, 3H-benzo [de] isoline-2-yl] phenylsulfanyl BU N_ (2_phenylpropyl) Example 7 4: Similar to Example 2, 6-chlorobenzo- [de] isopinene_u_dione and H2N_Ar, _S-iCHA-CONIHCHdi-CtKAi ^ -Ar2 and 3_amine group # Amine reaction. The compound of formula I3a is obtained as follows: ------------—— 丨 Order i ———— line (please read the precautions on the back before filling in this page) Staff of J Bureau, Ministry of Economic Affairs Printed by the Consumer Cooperative 217- This paper size applies to the Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 l, Description of the invention (215)

Ar * -S- (CH2) „-CONH- (CH2) rCH (Ari) -Ar2 Ar '-S- (CH2)„ -CONH- (CH2) i ~ CH (Ar1) -Ar2 in I3a X) ^ ~ S —GH2-CONhKCH ^ -CH —S —CH2-CONH-CHjOH \ wu -------- Order ----- (Please read the notes on the back before filling this page) Similar to Example 32, (Third butoxycarbonylimidazole-l-methyl) carbamic acid third butyl ester is reacted with the compound of formula I3a. After the protective group is removed, a compound of the following formula I3b is obtained: Line &lt; Consumption Cooperation by Employees, Intellectual Property Bureau, Ministry of Economic Affairs, Du Yin-218- This paper is compatible with China's national fL standard (CNS) A4 specification (210 X 297) ) 473474 A7 B7 Printed clothing by the Consumer Cooperative of the Intellectual Property Chief Staff of the Ministry of Economic Affairs

Ar'-S- (CH2) n-CONH- (CH2) rCH (Ari) -Ar2

Ar '-S'- (CH2) „-CONH- (CH2) i-CH (Ar1) -Ar2 at 13b eight X) — &quot; ((y—s—〇H2—conh- (ch2) 2-ch w X) — ^ V ~ s—CH2—CONH-CHrCH Ό Example 7 5: Similar to Example 2,6-Phenylhydrazone- [de] isopinene-1,3-dione and 2- (3-oxabenzene Group): N- (4_Arylidene) -acetamidine reacts with 4-aminemethylcyclohexylmethylamine. 2- (3_ {6-[(4-Aminemethylcyclohexylmethyl) _amine W,% dioxy_1H, 3H_benzene and [de] isoruline-2-ylbuphenyl-n_ (4_airanyl) _ethyl amine, and then compared with Example 3 2 and (the Tributoxycarboximide Ejunyl fluorenyl) carbamic acid tert-butyl alcohol reaction. Remove the protective group, get N • ⑷ 气 爷 POST

f-based cyclohexylmethyl) -aminohydrazone, 3_dioxo-deuterium, 31 ^ benzene ({[((M-based) -phenyl) -acetamidamine). Yirulin-2 '219- This paper size is applicable Zhongguanjia Standard (CNS) A4 Regulation &amp; (210 X 297 male f) -------------------- Order --------- line ( Please read the phonetic on the back? Matters before filling out this page) 473474 Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (217) Similarly, 6 · Benzene [de] isoprene_13 二Ketones with 3_ (3-aminophenylphenethylpropanamine and 4-aminemethylcyclohexylmethylamine and the following products 3_ (3_ {6_aminomethylcyclohexylmethyl) -amino] -1,3_ Dioxo-1H, 3H_phenylhydrazone [de] isoquinolinyl} -phenyl) -N-phenethylpropanamide and (third butoxycarbonylimidazolylmethyl) diaminocarbamate Vinegar. After removing the protecting group, 3_ (3_ {6-[(4-guanidinomethylcyclohexylmethyl) -amino] -l, 3-dioxol lH, 3H-benzo [de] isop-quine &lt; ^ Lin-2-yl} phenyl) -N-phenethyl-propanamine. Example 76: Similar to Example 2,6-Gaphenylhydrazine_ [de] isohydrazine-1,3-di The ketone is reacted with H2N-Ar,-(CHA-CONH-CCHJi-Ar and 3-aminomethylbenzylamine. The compound of formula I6a is obtained as follows:

〇 ν &quot; 〇

Ar '-(CH2) n-C0NH- (CH2) i-Ar at 16a 2 / i .CONH- ^} / (ch2) 2-conh—4 y -o, -220- This paper standard applies to Chinese national standards ( CNS) A4 specification (210 X 297 mm) --------------------- Order ------ I--line (Please read the note on the back first Please fill in this page again for matters) 473474 A7 B7 V. Description of Invention (218) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-221- -------------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 specifications (210 X 297 male f) 473474 B7 A7

-------------------- Order --------- ^ (Please read the notes on the back before filling this page) This paper size is applicable to China Standard (CNS) A4 specification (210 X 297 male f) 473474 A7 _B7 V. Description of invention (22) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-223- -------------------- Order --------- line-0 ^ 1- (Please read the notes on the back before filling in this Page) This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 male f) 473474 A7B7 V. Description of the invention (221) Printed by the Consumer Cooperative of the Ministry of Intellectual Property Bureau

------------________ Order --------- line (Please read the precautions on the back before filling this page) This paper size applies to China National Standard (CNS) A4 specifications ( 210 X 297 male f) 473474 A7 B7 V. Description of invention (222) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-225- -------------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Invention Description (223) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-226- -------------------- Order -----— line &quot; ^ 11 ^ (Please read the precautions on the back before filling this page) This Paper size applies to China National Standard (CNS) A4 (210 X 297 male f) 473474 A7 B7 V. Description of invention (224) Intellectual Property Bureau of the Ministry of Economic Affairs Consumer Cooperatives printed sashimi

(Please read the precautions on the back before filling out this page) -------- Order --------- Line. This paper size applies to China National Standard (CNS) A4 (210 X 297) f) 473474 A7 ___B7 V. Description of Invention (225) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-228- -------------------- Order --------- line (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 Gt) 473474. A7 _B7 V. Description of invention (226) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

------------________ Order --------- Line (Please read the precautions on the back before filling this page) -229- This paper size applies to China National Standards (CNS) A4 specification (210 X 297 mm) 473474 A7 _B7 V. Description of invention (227) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- Line (Please read the precautions on the back before filling this page) -230- This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 473474, A7 _B7 V. Description of invention (228) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- line (please read the precautions on the back before filling this page) -231- Standards are applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) 473474 A7 _B7 V. Description of invention (229) Employees ’Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs print clothes

(Please read the precautions on the back before filling this page) -232- This paper size is applicable to Chinese National Standard (CNS) A4 (210 χ 297 male f) 473474 A7 B7 V. Description of Invention (23〇) Ministry of Economic Affairs Intellectual Property Printed by Bureau Consumers Cooperative

Ar1-(CH2) n-CONH- (CH2) i-Ar at 16a / (CH2) r CONH-CCHjJj ——OCHj CONH-CH2 ——OCFj (CHj) 2- CONH-CH2 — (\ —OCFj -d ( CH2) 2- conh ~~ 0CH3 CONH ~ --OCH3 CONH- (CH2) 2 —;)-och3 (CH2) 2- CONH- (CH2) 2 -Ό-CONH- (CH2) 2 —F -o — -233 -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) 473474 A7 _B7 V. Description of Invention (231) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order ------ ^ (Please read the notes on the back before filling this page) -234- This paper size is applicable to China Standard (CNS) A4 Specification (210 X 297 mm) 473474 A7 _B7 V. Description of Invention (232) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- ^ (Please read the notes on the back before filling this page) -235- This paper size Applicable to China National Standard (CNS) A4 (210 χ 297 male f) 473474 A7 _B7 V. Description of Invention (233) Intellectual Property Bureau of the Ministry of Economic Affairs Consumer Cooperative Printed Bra

—I ----------------- Order --------- Line (Please read the precautions on the back before filling this page) -236- This paper size applies China National Standard (CNS) A4 (210 X 297 mm) 473474 A7

Printed by the Employees' Cooperative of the Bureau of Wisdom and Finance of the Ministry of Economic Affairs V. Invention Description (234)

Similar to Example 3 The 2 '(fluorenedibutoxycarbonylimide pbitul-1 -ylmethyl) carbamic acid third butyl ester was reacted with the compound of formula I6a above. After the protecting group is removed, a compound of the following formula I6b is obtained: -237- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) — — — — — — — — — — —. I ^ _ — I _ — Order --------- line (please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (235)

ArMCHA-CONH-iCHA-Ar Printing of clothing by employees' cooperatives in the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order ------ line (Please read the precautions on the back before filling this page) This paper size applies to Chinese National Standards (CNS ) A4 specification (210 X 297 male f) 473474. A7 _____B7 V. Description of invention (236) Consumption cooperation printed by employees of the Intellectual Property Bureau of the Ministry of Economic Affairs

— — — — — — —— — — — · IIIIIII Order --------- line &quot; ^ 11 ^ (Please read. Read the notes on the back before filling out this page) This paper size applies to China Standard (CNS) A4 specifications (210 X 297 male f) 473474 A7 B7 V. Description of invention (237) '' Printed clothing for employees' cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-240- -------------------- Order ------- line ^ (Please read the notes on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 Specification (210 X 297 mm) 473474 A7 B7 V. Description of Invention (238) Intellectual Property Bureau, Ministry of Economic Affairs, Consumer Consumption Cooperative Clothing

-241- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------- tT --------- ^ (Please read the precautions on the back before (Fill in this page) 473474 A7 B7 V. Description of invention (239) Printing of clothing by employees' cooperatives of the Bureau of Wisdom and Finance, Ministry of Economy

-242- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 male f) -------------------- Order ------- --Line (please read the notes on the back before filling this page) 473474. A7 _B7 V. Description of Invention (24) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- Line (Please read the precautions on the back before filling this page) -243- This paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 male f) 473474 A7B7 V. Description of invention (241) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Yunnan

-244- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------------------- Order ------- !! (Please read the precautions on the back before filling out this page) 473474 A7 B7 V. Description of Invention (242)-Printing of clothing by employees' cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- Line (Please read the notes on the back before filling this page) This paper size is applicable to China Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 V. Description of invention (243) Printing of clothing by employees' cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs

------------ · -------- Order --------- Line · (Please read the precautions on the back before filling this page) This paper size applies China National Standard (CNS) A4 Specification (2.10 X 297 mm) 473474 A7 B7 V. Invention Description (244) Printed by the Employees' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-------- tT --------- ^ (Please read the notes on the back before filling out this page) This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) ) 473474 A7 B7 V. Description of Invention (245) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-------------------- Order --------- ^ IAW. (Please read the precautions on the back before filling this page) This paper size applies China National Standard (CNS) A4 specification (210 X 297 mm) 473474 A7 B7 V. Description of invention (246) Printing of clothing by employees' cooperatives of J Finance Bureau, Ministry of Economic Affairs

(Please read the precautions on the back before filling out this page) Order --------- line_ This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) Employees of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Consumer Cooperative 473474, A7 B7 V. Description of the Invention (247) Example 7 7: Similar to Example 2, 6-Gas Benzo [de] isobite 埽 1,3._ 二 _ and h2N-Ar '-( CHA-CONtKCHA-Ar is reacted with 3-aminomethylcyclohexylmethylamine. The compound of formula I7a is obtained as follows:

ΑΓ ·-(ΟΗ2) η-ΟΟΝΗ- (ΟΗ2) ΓΑΓ

Ar1-(CH2) n-CONH- (CH2) ± -Ar in I7a. (CH2) 2-CONH— / (CH2) 2-CONH- ^ V, y (CH2) 2-CONH— \ Example 7 8: Similar In Example 2,6-chlorophenylhydrazone [de] iso-17gene-fluorene, 3-dione was reacted with H2N-Ar '-(CHA-CONH ^ CHA-Het1 and 3-aminomethylbenzyl). The following was obtained Compound of formula I8a: -250- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) ----------- 1 -------- IT --- ------ (Please read the note on the back before filling this page) 473474 A7 B7 V. Description of the invention (248)

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

-251- (Please read the precautions on the back before filling out this page) This paper size applies to China National Standard (CNS) A4 (210 X 297gf) Printed by the Consumers ’Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7 Description of the invention (249)

Similar to Example 3 2, (Third-butoxycarbonylimidazole-l-ylmethyl) carbamic acid The third butyl ester was reacted with the compound of formula I8a above. After the protective group is removed, a compound of the following formula I8b is obtained: -252- The paper size applies to the Chinese National Standard (CNS) A4 (210 X 297 mm) --------------- ----- Order --------- line (please read the notes on the back before filling this page) 473474 A7 B7 V. Description of the invention (25〇)

VNH, NH. 2 Printing of clothing by employees' cooperatives in the Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the precautions on the back before filling this page) # Order --------- line · This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 • A7 B7 5 , Invention description (25〇

(Please read the precautions on the back before filling out this page) Example 7 9: Similar to Example 2,6-chlorophenylhydrazone [de] isopinene-1,3-dione and H2N-Ar '-(CH2) n -CONH- (CH2) rD-H reacts with 3-aminophosphonium benzylamine. The following compound I9a is obtained: Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

Ar '-(CH2) n-CONH- (CH2) rD-H -254- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 Employees ’Cooperative Cooperation of Intellectual Property Bureau, Ministry of Economic Affairs Print

V. Description of the invention (252)

Ar1-(CH2) n-CONH- (CH2) iDH at I9a (CH2) 2-CONH — / ~ \ CONH — ^> conh- (ch2) 2 — ^〉 Similar to Example 3 2, (Third butoxycarbonyl The iminopyrazole-1 -ylmethyl) carbamate tert-butyl ester is reacted with the compound of formula I9a above. After the protecting group is removed, a compound of the following formula I9b is obtained:

NH, NH2

Ar '-(CH2) n-CONH- (CH2) rD-H

Ar '-(CH2) n-CONH- (CH2) iDH at 19b (CH2) 2-CONH— / \ -255- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --- --------- Aw -------- 1τ —----- ^ (Please read the notes on the back before filling out this page) 473474 A7 B7 V. Description of the invention (253)

Example 8 0: Similar to Example 2,6-chlorophenylhydrazone [de] isofluorene-1,3-dione and HaN-A〆- (CHJn-CONH-CCHJi-CHCAr 丨) -Ar2 and 3-amine Hemylamine reaction. Obtain the compound of formula 110a as follows: —--------- Aw -------- Order ——---- line (please read the precautions on the back before filling this page) Ministry of Economic Affairs Intellectual Property Printed by Bureau Consumers Cooperative

Ar,-(CH2) n-CONH- (CH2) i-CH (Ari) -Ar2 -256- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) Leaf 04/4 A7 Five inventions Instructions (254)

(Please read the note on the back? Matters before you fill out this page) Ordering --------- Line · Printed by the Consumer Consumption Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is similar to Example 3 2, (The third [Iminopyrazole]; [-methylmethyl] amidinic acid tert-butyl. Vinegar is reacted with the compound of the above formula [0a]. After the protecting group is removed, the compound of the following formula 110b is revealed ... -257- The paper size is applicable to the Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (255)

, 〆 ::

Ar '-(CH2) ri-CONH- (CH2) rCH (Ari) -Ar2 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-258- This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 male f) ------------ 着 -------- tT ------ --- (Please read the notes on the back before filling this page)

473474 A7 B7 V. Description of the invention (256) Example 8 1: Similar to Example 2, 6-nitrophenylhydrazone [de] isopinene-1,3-dione and fluorene 2N-C6H4- (CH2) n-R3 And Rl-Η reaction. The compound of the formula Ilia is obtained as follows: 111a (CH2) n-R3 (Please read the notes on the back before filling out this page) t Order --------- Line 'Printed by the Consumers' Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs- 259- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (257) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-260- (Please read the precautions on the back before filling out this page) This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474

7 7 A B Printed by the Consumer Cooperatives of the Bureau of Wisdom and Finance of the Ministry of Economy V. Invention Description (258)

Similar to Example 1 1,6-nitro-2- (3-iodophenyl) phenylhydrazone [de] isoquinoline-1,3-dione or 6-nitro-2- (4-iodophenyl) Benzo [de] isoquinoline-1,3-dione reacts with zaqin (: 1 through 8-((: 112) 11-113 and 111-11. The compound of the following formula 1111) is obtained: -261-this paper Standards are applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) -------------------- Order --------- line (please Read the notes on the back before filling this page) 473474, A7 B7 V. Description of the invention (259) R1

111b

(CH2) n-R3 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

• 262- ------------ 鮝 -------- IT --------- (Please read the precautions on the back before filling this page) This paper size Applicable to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 Printed by the Consumers ’Cooperative of the Ministry of Intellectual Property Bureau

V. Description of the invention (26〇) -C12H8- (CH2) n-R3 R1 produced in rLH and Illb h3c -nh- (ch2) 3-nh2 -NH— (CH2) 5 &quot; NH2 -NH- (CH2) 7 &quot; NH2 ~ N ^^ y ^ NH2 Example 8 2:. Similar to Example 11,6-nitrophenylhydrazone [de] isopinene-1,3-dione and 4-iodophenylamine or 3-iodophenyl Amine (= I-Ar'-NH2), Het ^ BCOHL and R ^ -H reaction. This gives the compound of formula Ip: R1

Ar'-Het1 -Ar'-Het1. R1 in Ri-H and Ip -nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

This paper size applies to China National Standard (CNS) A4 specification (21〇χ 297 公 f) --I ----------------- Order --------- (Please read the notes on the back before filling this page) -263- 473474 A7 B7 V. Description of the invention (261) R1 in R1-! ·! And Ip -NH- (CH2) 3-NH2 -NH- (CH2 ) 5-NH2

(Please read the precautions on the back before filling this page) --------- Order— Example 8 3:. Similar to Example 2,6-Nitrobenzene 幷 [de] 异 晞 晞 -1,3 -The dione reacts with R ([CH2) n-Ph-NH2 and I ^ -fluorene. The compound of formula 112 is obtained as follows: I I k- Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs R1

112 (CH2) n-R6 -264- This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7B7 V. Description of the invention (262) -Ar '-(CH2) n-R6 R1 in R ^ -H and 112-&lt; ^ &gt; -N human CH3 -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2, ch3 -NH- (CH2 ) 3-NH2 -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2 -n &quot; ^^ J ^ nh2, \\ and / ~ ^ CH3 o, ch3 -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2 ~ S ^ 〇 ^ NH2 Example 8 4: Similar to Example 2,6-nitrobenzyl [de] isop-g-1,3 -—Fluorene reacts with (4-aminophenyl) -phenylacetonitrile with R1-! · !. The compound of formula II3 is obtained as follows: Please read the memorandum of the memorandum first and then fill out this page. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, R1

R1 to R] -H and 113 -nh- (ch2) 3-nh2 -nh_ (ch2) 5-nh2 -NH- (CH2) 7-NH2 -265- This paper size applies to China National Standard (CNS) A4 specifications ( 210 X 297 mm) ^ —----- 473474 A7 B7 V. Description of the invention (263) R1 in R ^ -H and 113 1 &quot; 〇 ^ ΝΗ2-Example 8 5: Similar to '11, 6-nitrate The 2--2- (4-iodo-R12-phenyl) benzo- [de] isophosphorin-1,3-dione reacts with R1 ()-B- (OH) 2 and R1-!!. Get the following compound of formula 114: (Please read the precautions on the back before filling this page) 9 R1

Order --------- line- γ ^ R12 R10 Printed by R12 · R10 R1 on R1- !! and 114 员工 -NH- (CH2) 3-NH2 -266- This paper size applies to China National Standard (CNS) A4 specifications (2〗 0 X 297 male f) 473474 A7 B7 V. Description of the invention (264) R12 R10 R1 in R'-H and 114 Η -〇-cn -nh- ( ch2) 3-nh2 _NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2 ~ price &quot; ^ 0 ^ ΝΗ2 3-CH3 -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2 Η — ^ y ~ N〇2 —NH— (CH2) 3—NH2 -nh- (ch2) 5-nh2 -NH- (CH2) 7 ~ NH2 Η —OMe Ν〇2 —OMe -NH- (CH2) 3 ~ NH2 -NH- (CH2) 5-NH2 —NH— (CH2) 7-NH2 ~ ^^ 0 ^ Nh, 2 (Please read the precautions on the back before filling this page) # ---------- Line · Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs Example 8 6: Similar to Example 11,6-nitro-2- (3-iodo-R12-phenyl) benzene幷-[de] isowaline-1,3-dione reacts with R1G-B- (OH) 2 and R1-!!. Ibm compound of the following formula is obtained: -267- This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 _B7 V. Description of the invention (265) R1

R10 R1 in R1-}! And Ibm (Please read the notes on the back before filling this page) Example 8 7: Similar to Example 2,6-nitrobenzo [de] isobene-1,3-dione Reacts with H2N-Ar and Ri-H. A compound of the formula Ibg is obtained: R1

b9

Ar R1 prints clothes at R ^ -H and Ibg Intellectual Property Bureau Employees ’Cooperatives

CH2-Ph -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2

-268- This paper size is in accordance with China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 _B7 V. Description of Invention (266) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the precautions on the back before filling out this page) Reference --------- line · -269- This paper size applies to China National Standard (CNS) A4 (2) 0 X 297 mm 473474 A7 ___B7 V. Description of Invention (267) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

(Please read the notes on the back before filling this page) -270- This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of Invention (268) Intellectual Property Bureau, Ministry of Economic Affairs Printed by Employee Consumer Cooperative

-271- This paper size 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) 473474

7 7 A B V. Description of Invention (269) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

-272- This paper size applies to China National Standard (CNS) A4 specification (210 X 297 mm) ---------------------- Order -------- -Line (please read the notes on the back before filling this page) 473474 A7 B7 V. Description of invention (270) Printed by the Consumer Cooperative of Intellectual Property Bureau of the Ministry of Economic Affairs

-273- (Please read the note on the back? Matters before filling out this page) t Order --------- line · This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 V. Description of the invention (271)

Ar

S〇2NH2

och3 R1 in R ^ H and Ibg (Please read the notes on the back before filling this page)

—0CH3 OH

-NH- (CH2) 3-NH2 -nh- (ch2) 5-nh2 -nh- (ch2) 7-nh2 -nh- (ch2) 3-nh2 -NH- (CH2) 5-NH2 -nh- (ch2 ) 7-nh2 -NH- (CH2) 3-NH2 -NH- (CH2) 5-NH2 -nh- (ch2) 7-nh2 -NH- (CH2) 3-NH2 —NH— (CH2) 5 ~ NH2- nh- (ch2) 7-nh2

Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs -NH- (CH2) 3 -NH2 -NH- (CH2) 5-NH2 -NH- (CH2) 7-NH2 Example 8 8:. Example 8 Compound 1 of 3- { 4_ [6_ (3-Aminomethylamidoamino) -1,3-dioxo-1H, 3H-benzo [de] isofluorin-2-yl] -phenyl} -N- (3,3-di Methylbutyl) -propanamidin was reacted with tertiary butyl (tertiary butoxycarbonylimidazole-1 -ylfluorenyl) aminoacetate of Example 32. After removing the protecting group, N- (3 , 3-Dimethylbutyl) -3- {4- [6- (3-guanidiniumbenzylamino) -1,3-dioxo-1H, 3H-phenylhydrazone [de] isoquinolin-2-yl ] -Phenyl} -propionic acid amine. Example 8 9: Similar to Example 2,6-chlorophenylhydrazone [de] isoprene-1,3-dione and 3- (4-amine-274- Applicable to China National Standard (CNS) A4 specification (210 X 297 male f) 473474 A7 B7 V. Description of the invention (272) 'Phenyl) -N- (3-dimethylaminepropyl) _propanamide and c, ( 3-Aminemethylcyclohexyl) · methylamine reaction. 3- (4- {6-[(3-Aminomethylcyclohexylmethyl))-amino group 丨 dioxin_benzene hydrazine [de] isoxoline_2 _Yl} phenyl), n '(3-diamidopropyl) _propanamidin. Example 9: Similar to Example 2,6_-chlorobenzo [de] isofluorene% _13_dione 2_ (cardiamine phenylsulfanyl) -N- (3,3-dimethylbutyl) _ethyl is reacted with amine and brimonylamine. 2_ {4_ [6_ (3_amine methylamine) 13-Dioxo_ih, 3h_benzo [de] isofluorenyl 4--2-yl] phenylsulfanyl} -N- (3,3-difluorenylbutyl) -acetamidine. Example 91: Similar to Example 2, 6-Chlorobenzo [de] isopinene-i, 3-diones with fluorene 2N-Α〆- γ-(&lt;: ^ 2) 11-113 and 3-aminomethylfluorenylamine. The following are obtained Compound of Formula 112: -------------------- Order --------- Line IAMW (Please read the notes on the back before filling this page) Economy Printed by the Ministry of Intellectual Property Bureau's Consumer Cooperative

Ar, -Y- (CH2) n-R3

-275-

This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) 473474 A7 B7 Jade and invention description (273) Similar to Example 2 '6-chlorobenzo [eg] isopyrene · M_dione Reacts with 4- (pyrrolidine-b% acid group) -aniline and 3-amine formamidine. 6_ (3-Amininobenzylamino) -2- [4- (pyrrolidinylsulfonamido) _phenylbenzobenz [de] isop-quinoline-1,3-dione 0% M11-: Known process' isomolar amount [6_ (3_aminopropylamine group 丨,% dioxo 1H, 3H-benzyl [de] isofluorin-2-yl] _4,5_dimethoxybenzonitrile (According to Table 1, 256 1 'Example 87) to generate an acid addition salt [6_ (3_aminopropylamino ^, bisdioxy-1H, 3H-benzo [de] isoquinoline_2_yl] _4, 5_dimethoxybenzonitrile sulfonate. 'H-nmr (DMSO-d6): 8.80 (dd, J = 1.0 &amp; J = 8.6Hz, lH), 8.50 (dd, J = 0.8 &amp; J = 7.4Hz, 1H), 8.34 (d, J-8.6 Hz, 1H), 7.94 (t, (NH), J-5.8 Hz, 1H), 7.76 (dd, J = 7.4 and J = 8.4 Hz, 1H ), 7.71 (sbr, 2H (NH2)), 7.55 (s, 1H), 7,30 (s, 1H), 6.90 (d, J = 8.8 Hz, 1H), 3.90 (s, 3H), 3.81 (s , 3H), 3.60-3.45 (m, 2H), 2.96 (t, J = 7.6 Hz, 2H), 2.31 (s, 3H), 2.08-1.94 (m, 2H). Abbreviation for nmr signal (nmr = nuclear magnetic resonance ): -------------------- Order --------- Line (Please read the notes on the back before filling this page) Intellectual Property of the Ministry of Economic Affairs Bureau employee consumer cooperative prints S unimodal, d bimodal, dd bimodal, t peak, sbr wide single peak, -276- This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) Printed by the Employees ’Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7____ 5. Description of invention (274) m The peak, q *%, J coupling constant (expressed in Hz) is similar to that in Example 9 3, and the following acid addition salt is obtained: 3- {3- [6- (2-guanethanylamino) -1,3-di Oxobenzo [de] isoquinolin-2-ylphenyl} -N- (4-phenylbutyl) -propanamide (Example 40, page 145, table 2 row). 3- {3- [6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-benzo [de] isoquinolin-2-ylphenyl} -N- (4-benzylbutyl) -propanilamine, Sulfonate; 'H-nmr (DMSO-d6): 8.73 (dd, J = 1,0 and J = 8.5 Hz, 1H), 8.46 (dd, J = 1.〇 and J = 7.3 Hz, 1H) , 8.28 (d, J = 8.5 Hz, 1H), 7.88 (t, J = 5.6 Hz, 1H), 7.75 (dd, J = 7.3 and J = 8.4 Hz, 1H), 7.61 (t, J = 5.8 Hz, 1H), 7.40-7.36 (m, 1H), 7.28-7.23 (m, 3H), 7.16-7.10 (m, 4H), 6.89 (d, J = 8.7 Hz, 1H), 3.61-3.50 (m, 4H) , 3.06 (q, J = 7.0 Hz, 2H), 2.89-2.85 (m, 2H), 2.53 (d, J-7.6 Hz, 1H), 2.39 (t, J = 8.5 Hz, 2H), 2.36 (s, 3H), 1.56-1.49 ( m, 2H), 1.41-1.34 (m, 2H). N- [2- (4-chlorophenyl) -ethyl] -3- [3- (6- {3-[(3-guanpropyl) -fluorenylamino] -propylamino} -1,3- Dioxo-1H, 3H-benzo [de] isofluorin-2-yl) -phenyl] -propanamide (Example 37, page 135, table 7 line), N- [2- (4-Gasbenzene) ) -Ethyl] -3- [3- (6- {3-[(3-guanpropyl) -methylamino] -propylamino} -1,3-dioxo-1H, 3H-benzo [ de] Isofluorin-2-yl) -phenyl] -propanamine, reading acid methyl ester 'H-nmr (DMSO-d6): 10.49 (sbr, 1H), 8.85 (d, J = 8.5 Hz, 1H), 8.44 (dd, J = 0.9 and -277-) This paper size applies to China National Standard (CNS) A4 (210 x 297 mm) (Please read the precautions on the back before filling this page) Order --- ------ Line-Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7 V. Description of the invention (275) j = 7.3 Hz, lH), 8.27 (d, J = 8.5 Hz, 1H), 8.01 ( sbr, 1H (NH)), 7.94 (t? J = 5.6 Hz, 1H (NH)), 7.90 (t, J 5.9 Hz, 1H (NH)), 7.73 (dd, J = 7.4 and J = 8.4 Hz, 1H), 7.42-7.38 (m, 1H), 7.31 (d, J = 8.4 Hz, 2H), 7.26 (d, J = 7.7 Hz, 1H), 7.18 (d, J = 8.4 Hz, 2H), 7.14- 7.11 (m, 2H), 6.88 (d, J-8.7 Hz, 1H), 3.65-3.45 (m, 3H), 3.31-3.15 (m, 6H), 3.11-3.04 (m, 1H), 2.85 (t, J-7.3 Hz, 2H), 2.77 (d, J = 4.9 Hz, 3H), 2.67 (t, J = 7.3 Hz, 2H), 2.39 ( t, J = 5.7 Hz, 1H), 2.35 (s, 3H), 2.21-2.14 (m, 2H), 1.96-1.89 (m, 2H). N- [2- (4-chlorophenyl) -ethyl] -3- {3- [6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-phenylhydrazone [de] Isophosphon-2-yl] -phenyl} -propanamidin (Example 37, page 135, table 2 row) N- [2- (4-chlorophenyl) -ethyl] -3- {3- [ 6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-benz [de] isop-quineline-2-yl] -phenyl} -propanamide, methyl acetate; ^ -nmr (DMSO-d6): 8.74 (dd, J = 1.〇 and J = 8.6 Hz, 1H), 8.44 (dd, J = 1.0 and J = 7.3 Hz, 1H), 8.27 (d, J-8.5 Hz, 1H), 7.94 (t, J = 5.7 Hz, 1H (NH)), 7.80 (t, J = 5.2 Hz, 1H (NH)), 7.76 (t, J = 5.1 Hz, 1H (NH)), 7.74 (dd, J = 7.3 and J = 8.5 Hz, 1H), 7.40 (t, J = 7.9 Hz, 1H), 7.31 (d, J = 8.4 Hz, 2H), 7.26 (d, J-7.8 Hz, 1H ), 7.18 (d, J = 8.4 Hz, 2H), 7.14- 7.11 (m, 2H), 6.89 (d, J = 8.7 Hz, 1H), 3.61-3.56 (m, 2H), 3.55-3.50 (m, 2H), 3.28-3.23 (m, 2H), 2.86 (t, J = 8.2 Hz, 2H), 2.67 (t, J = 7.1 Hz, 2H), 2.40 (t, J = 7_3 hz, 2H), 2.35 ( s, 3H). [2- (4-chlorobenzyl) -ethyl] -3_ {3- [6- (3-guanpropylamino) -1,3-dioxo- _ -278- This paper size applies to Chinese national standards ( CNS) A4 specification (210 x 297 mm) -------------------- Order --------- line (Please read the precautions on the back first Refill this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 473474 A7 B7 V. Description of the invention (276) 1H, 3H-benzo [de] isofluorin-2-yl] -phenyl} -propanamide (Example 37, p. 135, Table 6) N- [2- (4-chlorophenyl) -ethyl] -3- {3- [6- (3-guanpropylaminoh1,3-dioxy · benzene Benzo [de] isofluorin-2-yl] -phenyl} -propanamide, diacetic acid; h-nmr (DMSO-d6): 8.76 (d, J = 8.5 Hz, 1H), 8.44 (d , J = 7.3 Hz, 1H), 8.27 (d, J = 8.5 Hz, 1H), 7.93 (t, J = 5.6 1H (NH)), 7.73 (t, J = 7.5 Hz, 1H), 7.65 (t, J = 5.6 Hz, 1H), 7.40 (t, J = 8.0 Hz, 1H), 7.31 (d, J = 8.4 Hz, 2H), 7.18 (d, J = 8.4 Hz, 2H), 71.4-7.11 (m, 2H), 6.84 (d, J = 8.7 Hz, 1H), 3.45 (t, J = 6.3 Hz, 2H), 3.31-3.22 (m, 4H), 2.86 (t, J = 8.0 Hz, 2H), 2.66 ( t, J = 7.1 Hz, 2H), 2.41 (d, J = 8.2 Hz, 2H), 2.37 (s, 3H), 199-1.91 (m, 2H). 6- (3-aminopropyl ) -2- (2,3-dioxophenyl) -benzo [de] isoquinoline-1,3-dione (Example 87, 255, Table 3) 6- (3-Aminepropylamine ) -2- (2,3-dimethoxyphenyl) -benzo [de] isoquinoline-1,3-dione, methyl sulfonate; 'H-nmr (DMSO-d6): 8.75 ( dd, J = 0.9 and J = 8.4 Hz, 1H), 8.46 (dd, J = 0.8 and J = 7.3 Hz, 1H), 8.30 (d, J = 8.5 Hz, 1H), 7.86 (sbr, 1H (NH) ), 7.75 (dd, J = 7.3 and J = 8.4 Hz, 1H), 7.65 (sbr, 2H (NH)), 7.17-7.15 (m, 2H), 6.89-6.85 (m, 2H), 3.89 (s, 3H), 3.60 (s, 3H), 3.51 (t, J = 7.0 Hz, 2H), 2.97 (t, J = 7.8 Hz, 2H), 2.31 (s, 3H), 2.03-1.96 (m, 2H). 6- (3-Aminepropylamino) -2- (4'-methoxybiphenyl_4_yl) -benzo [de] isoquinoline_ -279- This paper size applies to Chinese National Standard (CNS) A4 Specifications (210 X 297 male f) -------------------- Order --------- Line IAVW (Please read the precautions on the back before filling This page) 473474 A7 B7 V. Description of the invention (277) 1.3-Diketone (Example 12, page 98, table 3 line) 6- (3-Aminopropylamino) -2- (4'-fluorenyloxybiphenyl- 4-yl) -phenylhydrazone [de] isoamidine · Lin-1.3-dione, sulfonate; 'H-nmr (DMSO-d6): 8.75 (d, J = 8.5 Hz, 1H), 8.48 (d , J = 6.6 Hz, 1H), 8.31 (d, J = 8.5 Hz, 1H), 7.84 (sbr, 1H (NH)), 7.77-7.68 (m, 7H (2xNH)), 7.36 (d, J = 8.4 Hz, 2H), 7.07 (d, J = 8.8 Hz, 2H), 6.88 (d, J = 8.7 Hz, 1H), 3.83 (s, 3H), 3.54-3.48 (m, 2H), 2.98 (t, J = 7.8 Hz, 2H), 2.31 (s, 3H), 2.04-1.96 (m, 2H). 6- (3_Aminepropylamino) _2_ (4_Leaves 17-sat-9-ylphenyl) -benzyl [Heart] Isoquinine_i, 3_dione (Example 82, page 247, table 1 line) 6- (3-Aminopropylamino) -2- (4-carbazol-9-ylbenzyl) · benzidine [de] isopchaline_ 1.3-dione, sulfonate 'H-nmr (DMSO -d6): 8.77 (dd, J = 0.9 and J = 8.6 Hz, 1H), 8.57 (dd, J = 〇8 and J = 7 3 Hz 1H), 8.36 (d, J = 8.5 Hz, 1H), 8.29 (d, Ju Hz, 2H), 7 87 (t, J = 5.7 Hz, 1H (NH)), 7.81-7.77 (m, 3H), 7.72 (sbr, 2H (NH)), 7.64 (d, J = 8.6 Hz, 2H), 7.53-7.47 (m, 4H), 7.35.7 32 (m 2H) 6.91 (d, J = 8.7 Hz, 1H), 3.57 (q, J = 5.9 Hz, 2H), 3.03-2 95 (m Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs (please read the notes on the back before filling this page) 2H), 2.31 (s, 3H), 2.05-1.98 (m, 2H). N- (3-{[2- (4 -methoxybiphenyl-4-yl) -1,3-monooxy_2,3_ dihydro_1H_ phenylhydrazone [de] 兴 &lt; 4 琳 _2_ Phenyl] -phenyl} -N- (4-phenylbutyl) -propanamide (example 8 5, 2 5 1 on page 4, line 4) N- (3-{[2- (4'-methoxyl Phenyl-4-yl) -1,3-dioxo_2,3_dihydrazine ^ 280-Benzene-280- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 473474 A7 B7 5 Description of the invention (278) 幷 [de] isofluorolin-2-yl] -phenyl} -N- (4-phenylbutyl) -propanamidinium sulfonate 'H-nmr (DMSO-d6) : (Please read the precautions on the back before filling this page) 8.83 (d, J = 7.8 Hz, 1H), 8.56 (t, J = 6.5 Hz, 1H (NH)), 8.49 (dd, J2 0.8 and J = 7.3 Hz, 1H), 8.20 (d, J = 8.5 Hz, 1H), 7.84 (t, J = 5.8 Hz, 1H (NH)), 7.78 (dd, J = 7.4 and J: 8.4 Hz, 1H), 7.72 (d, J = 8.5 Hz, 2H), 7.68 (d, J = 8.8 Hz, 2H), 7.40-7.36 (m, 4H), 7.34 (d, J = 8.5 Hz, 2H), 7.22-7.19 (m , 1H), 7.07 (d, J = 8.8 Hz, 1H), 6.70 (d, J = 8.7 Hz, 1H), 4.70 (d, J = 5.9 Hz, 2H), 4.36 (d, J = 5.9 Hz, 2H ), 3.82 (s, 3H), 2_30 (s, 3H). 6- (3-Aminopropylamino) -2- (7-hydroxyfluoren-1-yl) -benzo [de] isoquinoline-1 , 3-dione (Example 87, page 257, Table 5) 6- (3-Aminopropylamino) -2- (7-hydroxyphenyl-1-yl) -benzo [de] isopyridin-1, 3-dione, methyl sulfonate; ^ -nmr (DMSO-d6): 9.61 (s, 1Η (ΟΗ)), 8.79 (dd, J = 0.9 and J = 8.6 Hz, 1H), 8.50 (dd, J = 0.8 and J = 7.3 Hz, 1H), 8.33 (d, J = 8.5 Hz, 1H), 7.93-7.87 (m, 2H), 7.79 (dd, J = 7.4 and / = 8.4 Hz, 1H), 7.74 ( sbr, 3H (NH)), 7.43-7.37 (m, 2H), 7.10 (dd, J = 2.4 and J = 8.9 Hz, 1H), 6.91 (d, printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, J = 8.7 Hz, 1H), 6.75 (d, J = 2.4 Hz, 1H), 3.53 (q, J = 6.3 Hz, 2H), 3.02-2.95 (m, 2H), 2.31 (s, 3H), 2.05-1.98 (m , 2H). N- [2- (4-chlorophenyl) -ethyl] -3- {3- [6- [4- (guanidinemethylbenzylamino) -l, 3-dioxo-lH, 3H-benzo [de ] Isofluorin-2-yl] -phenyl} -propanamidin (Example 37, page 135, line 5 of table) N- [2- (4-chlorophenyl) -ethyl] -3- {3- [6- (4-guanidinium benzylamine) -1,3-dioxo-281-This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 g) 473474 A7 B7 V. Description of the invention (279 ) -1H, 3H-Benzamidine [de] isofluorin-2-yl] -phenyl} -propanamidine, methyl sulfonate; ^ -nmr (DMSO-d6): (Please read the precautions on the back first Fill out this page again) 8.82 (dd, J = 0.8 and J = 8.5 Hz, 1H), 8.55 (sbr, 1H (NH)), 8.45 (dd, J = 0.8 and J = 7.3 Hz, 1H), 8_15 (d , J = 8.5 Hz, 1H), 7.91 (t, J = 5_7 Hz, 1H (NH)), 7.85 (t, J = 6.1 Hz, 1H (NH)), 7.76 (dd, J = 7.4 and J-8.4 Hz, 1H), 7.44 (d, J = 8.2 Hz, 2H), 7.39 (t, J = 8.1 Hz, 1H), 7.32-7.23 (m, 5H), 7.17 (d, J = 8.4 Hz, 2H), 7.12-7.09 (m, 2H), 6.58 (d, J = 8.7 Hz, 1H), 4.69 (d, J = 4.6 Hz, 2H), 4.33 (d, J = 6.1 Hz, 2H), 3.24 (q, J = 7.4 Hz, 2H), 2.84 (t, J = 8.3 Hz, 2H), 2.66 (t, J = 7.1 Hz, 2H), 2_39 (t, J = 8.0 Hz, 2H), 2.34 (s, 3H). N- [2- (3-chlorophenyl) -ethyl] -3- (3- {6-[(4-guanidinemethylcyclohexylmethyl) -amino] -1,3-dioxo-1H, 3H-Benzamidine [de] isoamidine-2-yl} -phenyl) -Propanamide (Example 3, p. 134, Table 5 row) Ν- [2- (3 · Azobenzyl) -ethyl ] -3- (3- {6-[(4-guanidinecyclohexylmethyl) -amino] -1,3-dioxobenzo [de] isoquinolin-2-yl} -phenyl)- Promethazine, methyl sulfonate; 'H-nmr (DMSO-d6): Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economy 8.79 (d, J = 8.5 Hz, 1H), 8.43 (d, J = 7.3 Hz , 1H), 8.24 (dd, J = 3.1 and J = 8.6 Hz, 1H), 7.94 (t, J = 5.7 Hz, 1H (NH)), 7.84 (sbr, 1H (NH)), 7.78-7.69 (m , 1H), 7.40 (t, J = 8.0 Hz, 1H), 7.30-7.22 (m, 4H), 7.14-7.10 (m, 3H), 6.82 (dd, J = 3.3 and J = 8.8 Hz, 1H), 3.27 (q, J = 6.8 Hz, 2H), 3.11 (t, J = 6.5 Hz, 2H), 2.85 (t, J = 7.3 Hz, 2H), 2.69 (t, J = 7.3 Hz, 2H), 2.39 ( t, J = 7.4 Hz, 2H), 2.34 (s, 3H), 1.94-1.74 (m, 2H), 1.60-1.40 (m, 4H), 1.05-0.90 -282- This paper size applies to the Chinese National Standard (CNS ) A4 specification (210 x 297 male f) 473474 A7 B7 V. Description of the invention (280) (m, 2H); (cis isomer: trans isomer = 2: 1). (Please read the precautions on the back before filling out this page) N- [2- (4-Gasphenyl) -ethyl μ3_ (3_ {6 _ [(4_guanidylcyclohexylmethylphenylamino) -1 , 3-—Oxygen-1Η, 3Η-phenylhydrazone [de] isoquinoline_2_ylbuphenyl) _propanamidin (Example 3 7, 13, 5 rows, table 8) &gt; 1- [2- (4-Gasphenyl) -ethyl; | _3_ (3_ {6 _ [(4_guanidinomethylcyclohexylmethyl) _amino] -1,3-dioxo-1H, 3H-phenylhydrazone [de] Isoquinoline_2_ylbuthylphenyl) _propanamide, methyl phosphonate; 'H-nmr (DMSO-d6): 8.79 (dd, J = 1.7 ^ J = 7.8 Hz, 1H), 8.43 (d , J = 7.3 Hz, 1H), 8.24 (dd, J = 3.2 and J = 8.6 Hz, 1H), 7.92 (t, J = 5.7 Hz, 1H (NH)), 7.83 (sbr, 1H (NH)), 7.73-7.69 (m, 1H), 7.41-7.37 (m, 1H), 7.30 (d, J = 8.4 Hz, 2H), 7.25 (d, J = 7.8 Hz, 1H), 7.17 (d, J-8.4 Hz , 2H), 7.13-7.10 (m, 2H), 6.81 (dd, J = 2.9 ^ J = 8.8 Hz, 1H), 3.25 (q, J = 7.3 hz, 2H), 3.11 (t, J = 6.4 Hz, 2H), 2.85 (t, J = 8.2 Hz, 2H), 2.66 (t,) = 1.2 Hz, 2H), 2.39 (t, J = 7.4 Hz, 2H), 2.33 (s, 3H), 1.95-1.75 ( m, 2H), 1.60-1.40 (m, 4H), 1.05-0.90 (m, 2H),); (cis isomer: trans isomer = 2: 1). Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs of 3- {3- [6- (4-guanidinecarboxamido) -1,3-dioxophenylhydrazone [de] isofluorin-2-yl] -phenyl } -N- [2- (4-sulfonamidophenyl) _ethyl] _propanamide (Example 35, page 129, table 5 row) 3- {3- [6- (4-guanidinebenzyl Amine) -1,3-dioxo-111,31 ^ phenylhydrazine [cardio] isofluorin-2-yl] -phenyl} -N- [2- (4-sulfonamidophenyl) -ethyl ] -Propanamide, methyl sulfonate; 'H-nmr (DMSO-d6): -283- This paper size applies to China National Standard (CNS) A4 (210 X 297 male f) 473474 Employees of Intellectual Property Bureau, Ministry of Economic Affairs Consumption cooperative printed clothing A7 B7 V. Invention description (281) 8.88 (d, J = 8.5 Hz, 1H), 8.66 (sbr, 1H (NH)), 8.50 (dd, J = 0.8 and J = 7.3 Hz, 1H ), 8.20 (d, J-8.5 Hz, 1H), 7.93 (t, J-6.0 Hz, 1H (NH)), 7.77 (d, J = 8.3 HZ, 1H), 7.49 (d5 J = 8.2 Hz, 2H ), 7.40 (d, J = 8.4 Hz, 2H), 7.35-7.30 (m, 4H), 7.19-7.14 (m, 3H), 6.73 (d, J = 8.7 Hz, 1H), 4.71 (d, J = 6.1 Hz, 2H), 4.39 (d, J = 6.1 Hz, 2H), 3.34 (q, J = 7.4 Hz, 2H), 2.90 (t, J-8.6 Hz, 2H), 2.81 (t, Bu 7.2 Hz, 2H), 2_45 (t, J = 8.3 Hz, 2H), 2.38 (s, 3H). The following examples are related to pharmaceutical preparations: Example A: A solution of 100 g of the active compound of formula I and 5 g of trans-ratine dinaphthalene in an injection bottle, the pH of which is adjusted to 6.5 with 2 n sleeping acid, repeated in 3 liters of distilled water, sterilized and filtered , Divided into injection bottles, freeze-dried under sterilized conditions and anti-corrosion sealed. Each injection vial contains 5 mg of active compound. Example B: suppository 20 g of a mixture of active compounds of formula I is melted with 100 g of soy scaly fat and 1400 g of cocoa butter, poured into a mold and allowed to cool. Each suppository contains 20 mg of a lingual compound. Example c: Solution A solution was prepared from 1 g of the active compound of formula I, 9.38 g of NaH2P04.2H2O, 28.48 g of Na2HP04-12H2O, and 0.1 g of benzyl chloride in distilled water. The mixture was adjusted to pH 6 8 and made up to 1 liter and irradiated; sterilized. This solution can be used in the form of eye drops. Example D: Under ointment-free conditions, 500 mg of active compound of formula I was mixed with 99.5 g of stone-284- This paper is sized to the Chinese National Standard (CNS) A4 (210 X 297 mm) -------- ----- I ------ Order ------ II--line (please read the notes on the back before filling this page) π / j 斗 / 4 A7 B7 V. Description of the invention (282) Clothing oil gels printed by employees' cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. Example E: Tablets were squeezed in a conventional manner to squeeze 1 kg of Tie Tau, Ren Shen Bu Bu &amp; eight scarred type I active compounds, 4 kg of potato starch, 〇2 complained to mill • g π stone and 0.1 kg of hard Mixtures of magnesium stearate to produce formulations such as 10 mg of active compound each. Example F: Coated Lozenges Similar to Example E, the lozenges were squeezed in a conventional manner and then coated with rigorous sugar, potato starch, talc, baicaleose, and toner. Example G: Capsules Two kilograms of a compound of the formula (I) are divided into hard shell capsules in a conventional manner so that each capsule contains 20 mg of active compound. Example Η: Ampoule A solution of 1 kg of the active compound of formula I in 60 ml of distilled water was filtered through bacteria, divided into ampoules, freeze-dried under sterilized conditions and sealed with antiseptic. Each ampoule contains 10 mg of active compound. The foregoing examples can be similarly and successfully repeated by replacing the reactants and / or operating conditions generally or specifically used in the examples described above. &quot; From the previous description, those skilled in the art can easily confirm the essential features of the present invention, and without departing from the spirit and scope of the present invention, 'make different changes and modifications to the present invention to facilitate different uses and conditions. Extinction Secret -------------------- Order --------- (Please read the precautions on the back before filling this page) -285-

Claims (1)

473474 Patent Application No. 88120540 Chinese Application for Amendment of Patent Scope (90/1 / January) Si Λ 8 B8 ..I 6. Application for Patent Park Amendment Supplement 1. A kind of benzo [de] isopyroline_丨, 3-diketide, which is a compound selected from the group consisting of: a) [6- (3-Aminepropylamino) -13-dioxo_1Η3Η · benzo [de] isoquinoline_2_ Group] -4,5-dimethoxybenzonitrile, b) 3- {3- [6- (2-guanethanylaminodioxy_1H 3H_benzo [de] isoquinolin-2-yl-benzene Phenyl] -N- (4-phenylbutyl) -propylamine, c) N- [2- (4-chlorophenyl) -ethyl] _3_ [3_ (6_ {3 · [(3guanidinopropyl) Methylamino: 1-propylamino} -1,3-dioxo-1Η, 3Η-benzo [de] isoquinolin-2-yl) -phenyl] -propanilamine, d) N- [2 . (4 · chlorophenylethyl] -3- {3- [6- (2-guanethanylamino)], 3-dioxo-1H, 3H-benzo [de] isofluorin-2-yl ] -Phenyl} -propanamidin, e) N- [2- (4-chlorophenyl) _ethyl] _3_ ^ 3- [6_ (3_guanpropylamino) _13_dioxo-1H, 3H- Benzo [de] isofluorin-2-yl] -phenylbuprofenamine, f) 6- (3-Aminopropylamino) -2- (2,3-dimethoxyphenyl) _benzo [de] Isoamidine 11 Lin · 1,3-Diamidine, g) 6- (3-Amine propionate Amine) -2- (4'-methoxybiphenylyl) _benzo [de] isoprene-1,3-dicopper, h) 6- (3-aminopropylamino) -2- (4 -Carbazole-9-ylphenyl) -benzo [de] isofluorene 11-lin-1,3-ditone, i) N · (3-{[2- (4'-methoxybiphenyl + yl )] &Gt; Dioxane. 2 Less Digassing_ 1 Η-Benzo [de] isoquinolin-2-yl] -phenylbenzene N_ (4-phenylbutyl) · Propanamide, j) 6- (3 _Aminopropylamino) -2- (7-hydroxynaphthalene- 丨 -yl) _benzy [de] isoxoline_ 1,3-dione, This paper is sized for China National Standard (CNS) A4 (210 X 297 mm) k) [2- (4-Chlorophenyl) -ethyl] veparine, one of them is -1Η, 3Η-benzyl [de] isoquinoline · 2-ylphenylbenzene τyl) -1,3 -l) N- [2- (3-chlorophenyl) .ethyl} · propanamide, Tilia, amine H, 3-dioxo] H, 3H • benzo [de] isoruline-propanamidin, kiprofen)-:) N- [2 ♦ chlorophenyl) .ethyl] _3- (3_ {6.Vamethylmethylcyclohexylmethyl) -amino] -1,3-dioxo-1Η 3Η · benzo [propyl] -propanamine, yesterday e] Yiru strain-2-ylbuben n) 3- {3- [6- (4-guanidinomethylamino)]], 3_dioxo · ih3h benzo ...] Lijunlin_2 · yl] -phenylbenzene N, [2_ (4- Continued Aminophenyl) _Ethylbuprofen, and their physiologically acceptable salts "2 · —A kind of [6_ (3_Aminopropylamino) ^, 3-dioxo_lfUH_benzo [de] Method for isoquinoline-2 · yl] -4,5-dioxobenzonitrile, which includes: /// 6-Nitrobenzo [de] isohydrazine, 3-dione With 2-amino_4,5. Dimethoxybenzonitrile 'and then with propane_1,3-diamine, and / or [6- (3-aminopropylaminoρυ · dioxy_1H , 3H-Benzamidine [de] isoquinoline_2_yl] -4,5-dimethoxybenzonitrile base, converted into one of its salts. 3 · One for the preparation of 3- {3- [ 6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-benzo [de] Xingkui >> lin-2-yl-phenyl] -N- (4-ben · butyl) -A method of propylammonamine, which includes: 6-Nitrobenzo [de] isopinene_ 1, 3-dione is reacted with (3-aminophenyl) -N-(4-phenylbutyl) · propanilamine and then with ethane-1 , 2-diamine and (third butoxycarbonylimine pyrazol-1-ylmethyl) carbamic acid tert-butyl-2- This paper is compatible with Chinese National Standard (CNS) A4 specifications (21〇x 297) Mm) 473474 A 8 Π8 C8 D8 Six, apply for patent Fanyuan cool reaction, and / or 3- {3- [6- (2-guanethanylamino) -1,3-dioxo-1H, 3H-benzo [de] isoquinoline- The base of 2-yl-phenyl] -N- (4-phenylbutyl) -propylamine is converted into one of its salts. A method for preparing N- [2- (4-chlorophenyl) _ethyl] -3- [3- (6- {3-[(3_guanpropyl) -methylamino] -propylamino group 丨, ^ Dioxo 1H, 3H_benzo [de] isopyridin-2-yl) -phenyl] -propanamine method, comprising: 6-nitrobenzo [de] isopinene- 1,3 -dione reacts with 3- (3-aminophenyl) _N · [2- (4 · murylphenyl) ethyl] -propanamine, and then with Ni_ (3-aminopropyl VN1- Methyl-propane-1,3-diamine and (third butoxycarbonylimine pyrazol-1-ylmethyl) carbamic acid tert-butyl ester, and / or the meaning [2- (4- Phenyl) -ethyl] _3- [3- (6- {3-[(3-guanpropyl) -methylamino] -propylamino} -1,3-dioxo-1H, 3H-benzo [de] Isoquinolin-2-yl) -phenyl] -propanamine base is converted into one of its salts. One is used to prepare N- [2- (4-Gaphenyl) · ethyl ] _3_ {3_ [6_ (2_guanethanylamino) -1,3-dioxo-1H, 3H-benzo [de] isofluorin-2-yl] -benzyl} _ method of propamidine, This includes: 6-Nitrobenzo [de] .Isognathine-1,3-dione and 3- (3-aminophenyl) · N- [2- (4-chlorophenyl) ethyl] -Propanamide and then react with ethane 1,2, -amine and (didioxy · Imine p than 唆 _ι_ylmethyl) carbamic acid third butyl ester, and / or N- [2- (4-chlorophenyl) -ethyl] _3_ {3- [6- ( 2-foxethamino) -1,3-dioxobenzo [de] iso4olin-2-yl] -phenyl} -propanamine base 'is converted into one of its salts.-Species In the preparation of N · [2- (4-chlorophenyl) · ethyl μ3- {3_ [6_ (3_guanpropylamino) -1,3-dioxo-1Η, 3Η-benzo [de] iso !! " Quirin_2-yl] -phenyl} _ -3- This paper size applies to Chinese National Standard (CNS) A4 (210X 297 gram) 473474 Λ 8 Β8 C8 D8 6. Method for applying propylamine with patent scope, It includes: 6-nitrobenzo [de] isopinene- 丨, 3_dione and 3_ (3_aminophenyl) _N- [2- (4-Gaphenyl) ethyl] -propyl Hydrazine reaction, and then with propane-1,3-diamine and (third butoxy alkynylimine ^ specific ol-[-fluorenyl) carbamic acid third butyl ester 'and / or N_ [ 2 · (4_chlorophenyl) _ethyl] _3_ {3- [6- (3-guanpropylaminopyrene,% dioxy_ιΗ, 3Η_benzo [de] isopyridin_2_yl] -benzene Base} -propanamine, converted to one of its salts. 7. A method for preparing 6- (3-aminopropylamino) -2- (2 , 3-Dimethoxyphenyl) _benzo [de] isoquinoline-i, 3-diones, comprising: 6-nitrobenzo [de] isopinene-1,3-di Ketones are reacted with 2,3-dimethoxy-aniline, and then with propane-1,3-diamine, and / or aminopropylamine) -2- (2,3-dimethoxybenzyl)- The base of benzo [de] isoquinolinone is converted into one of its salts. 8 'One for the preparation of 6- (3-aminopropylamino) -2- (4, -methoxybiphenyl_4_yl) _benzo [de] iso-4: «#-1,3-dione A method comprising: reacting 6-nitro-2- (4-kipropyl) benzo [de] iso} quinone-1,3-dione with 4-methoxyphenyl-borane 'and And then react with propane-1,3-diamine, and / or 6- (3-aminopropylamino) -2- (4, -methoxybiphenyl_4_yl) _benzo [de] isofluorene The base of phthaloline-1,3-dione is converted into one of its salts. 9 'A method for preparing 6- (3-aminopropylamino) -2- (4--11 cardul · 9-ylphenyl) · benzo [de] isoquinine-1,3-dione, It includes: reacting 6 · nitrobenzo [de] isosacene-1,3-dione with 4-carbol-9-yl-aniline 'and then with propane-1,3-diamine, and / Or 6_ (3_ Aminopropylamino) -2- (4-Kato-9-ylphenyl) -benzo [de] iso [Qui. Lin_ 丨 _ 4- This paper size applies Chinese National Standard (CNS ) A4 size (210X297 mm) Order Scope of patent application: The same base as two S is converted into one of its salts. 10.—Species for the preparation of N_ (3 _ {[2_ (4, _methoxybiphenyl_4_yl) _i, 3 • dioxo 2'3-dihydro-1H-benzo [de] isoquine A method for quinolin-2-yl] -phenylbenzene N- (4-phenylbutyl) -propanilamine, comprising: 6-nitro-2- (4-iodophenyl) benzo [de] iso Fluoroline_ 丨, 3_dione with 4-methoxyphenyl-borane, 3-aminomethyl-fluorenamine, and then with (third butoxyalkyliminopyrazol-1-ylmethyl ) Reaction of tert-butyl carbamate, and / or N- (3-{[2- (4'-methoxybiphenyl_4-yl) -1,3-dioxy · 2,3-dihydro -1'-Benzo [de] isofluorin-2-yl] • phenyl} -N- (4-phenylbutyl) _propanamidin base 'is converted into one of its salts β 1 1. A A method for preparing 6- (3-aminopropylamino) -2- (7-hydroxyfluoren-1-yl) -benzo [de] isoxoline-1,3 · dione, comprising: Nitrobenzo [de] iso bite-1,3-dione is reacted with 8-amino-tri-2-ol, and then reacted with propane-1,3-diamine, and / or 6- (3_amine Alaninyl) -2- (7- # to tea-1-yl.)-Benzo [de] isoquine "Lin-i, 3-dione test, converted to one of its salts" 1 2. —Species for the preparation of N- [2- (4-chlorophenyl)- Ethyl] -3 · {3- [6- (4-guanomethyloctylamino) -1,3-dioxo-1,3'-benzo [de] isoquinone, lin-2-yl] -phenyl } -Propanamine method, which includes: 6-Acrylobenzo [de] iso-11 grams of -1,3-dione and 3- (3-aminophenyl) _ N- [2- (4 -Chlorophenyl) ethyl] -propanamide, and then with 3-aminomethyl-ethanamine and (third butoxyepimine imino p-yl-1-ylmethyl) carbamic acid third Butyl ester reaction, and / or N- [2- (4-chlorophenyl) _ethyl] _3_ {3- [6- (4-guanidinomethylamino) -1,3-dioxo-1H, 3H-benzoxiu · -5- This paper size applies to Chinese national standard (CNS &gt; A4 size (210 X 297 mm) 473474 A8 B8 C8 D8 s --------------- VI 'Applicable patent scope. 2-Base] -phenyl} -propanamine base is converted into one of its salts. 13 · —Used to prepare N- [2- (3-Gaphenyl) -B Group] -3- (3- {6 · [(4-guanidinomethylcyclohexylmethyl) -amino] -1,3-dioxo-1Η, 3Η-benzo [de] isoquinoline_2_yl} -Phenyl) -Propanamine method, which includes: 6-Nitrobenzo [de] isobutyro-1,3-dione and 3- (3-aminophenyl) _N- [2- (3-Phenylphenyl) ethyl] -propylamine reaction Reacted with c_ (4-aminomethyl-cyclohexyl) -methylamine and (third butoxycarbonylimide pyrazol-1-ylmethyl) carbamic acid third butyl ester, and / or N- [2 -(3-Gaphenyl) -ethyl] -3- (3- {6-[(4-guanidinomethylcyclohexylmethyl) · amino group 丨,% —Oxygen-1H, 3H -benzo [de ] Iso0quinol 1 ^ -2 -yl} -Fungyl) -propyl amine, converted into one of its salts. 14. —A method for preparing N- [2- (4-chlorobenzyl) -ethyl] -3- (3- {6-[(4-guanidylcyclohexylmethyl) -amino] -1 A method of 1,3-dioxo-1H, 3H-benzo [de] isofluorin-2-yl} -phenyl) -propanamine, comprising: 6-nitrobenzo [de] isobite -1,3-dione is reacted with 3- (3-aminophenyl) -N- [2- (4-chlorophenyl) ethyl] -propanilamine and then with C- (4-aminemethyl -Cyclohexylmethylamine and (third butoxycarbonylimine pyrazol-1-ylmethyl) carbamic acid tert-butyl ester, and / or N- [2- (4-chlorophenyl) -ethyl Group] -3- (3- {6-[(4 · guanidinomethylcyclohexylmethyl) -amino] -1,3-dioxo-1Η, 3Η · benzo [de] isoquinoline-2- Base} -phenyl) -propanamidin base is converted into one of its salts. 15. —A kind of 3_ {3_ [6_ (4-guanmethylbenzylaminodioxo [de] iso The method of junlin_2 · yl] -phenylbenzene N- [2- (4-contamidamine phenyl) -ethyl] -propanamide includes: -6- This acreage scale is applicable to Chinese national standards (CNS) Eight-four specifications (210 X 297 mm) 473474 A8 B8 C8 D8 Six, the scope of patent application will be 6-nitrobenzo [de] isopinene-1,3-dione and 3_ (3_amine benzene ) -N- [2- (4-sulfo Amidino-phenyl) ethyl] -propanamide is then reacted with 4-aminomethyl-amidamine and (third butoxycarbonylimine pyrazol-1-ylmethyl) carbamic acid third Butyl ester reaction, and / or 3- {3- [6- (4-guanidiniumamino) -1,3-dioxo-111,3 ^ [-benzo [£ ^] isoxoline-2 -Base] -phenyl} -N- [2- (4-sulfonamidophenyl) -ethyl] -propanamide base, converted to one of its salts. The paper size applies to Chinese national standards ( CNS) A4 size (210 X 297 mm)