Fusion heteromorphic or binocular compounds

摘要

Compounds, pharmaceutical ingredients, therapeutic methods, synthetic methods and related intermediaries. 1. Requirement 1: a compound (1) with formula characteristics,Where x and X are independent,N o -N -OThis is an independent n-n-8314; - O - or cr831222;1. The condition is that at least one of X, X or Y is not N-N 8314; - or 8315; and no more than x, X or y-n 8314; - or 8315;;R¹ is C₁₋₆alkyl; Cquealkenyl; Calquinyl; - (CR³ᵃR³ᵇ) ₘ- (3-7 membered cycloalkyl);-(Cr: 74919; R: 749544); - (3-7 members of isopropene) is composed of 1-3 heteroatoms; - (Cr: 7491); R 749544; - (5-10 members of pagan),that it has 1 to 3 heteroatoms; or - (CR³ᵃR³ᵇ) ₘ-C₆₋₁₂aryl; wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, heteroaryl or aryl are optionally substituted with 1 to 5 halogen, deuterium, -OR⁵,-SR83099;-No. 74191; r7495;ciano C alquilo C cicloalquilo o -C alcoxi R es - (CR R) - (cicloalquilo de 3 a 10 miembros)(c) (based on) and listed below; in the straight straight ring ring ring ring ring ring ring ring ring cycloethane, listed below, from the straight ring joint joint joint joint joint joint joint joint joint joint joint 1-5 r830808;If the heterosexual atom in heterosexual and heterosexual is n, then n can choose to change to r83088;or R² is C₁₋₆alkyl, where alkyl is optionally substituted with NH₂,OH or cyano; R³ᵃ and R³ᵇ are, in each case independently, hydrogen or C₁₋₃alkyl; R⁴ is, for each case independently, a bond, deuterium, halogen, cyano, C₁₋₆alkyl, C₂₋₆alkenyl, oxo, -OR⁵,-SR83099;-S (O) R-S (O) R-No. 74191; r7495;-C (O) R-(Cr: 7491; R: 74955) - 8345; - (cycloquilo, 3-7 members);-(Cr: 7491; R: 74955) - 8345; - (4-10 members of isopropene)The substance has 1 to 3 heteroatoms, - (Cr: 7491; R: 749595); - 8345; - (5 to 10 heteroatoms),having 1 to 3 heteroatoms, or - (CR³ᵃR³ᵇ) ₙ-C₆₋₁₂aryl wherein the alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or aryl are each independently and optionally substituted with 1 to 5 deuterium, halogen, OR⁵ ,-SR83099;-No. 74191; r7495;cyano, C₁₋₆alkyl, C₃₋₆cycloalkyl or C₁₋₆alkoxy; or two R⁴,They form a cyclopentadiene of 3 to 6 members or a non cyclopentadiene of 4 to 6 members together with the carbon to which they are attached. In this case, cyclopentadiene or non cyclopentadiene can be replaced by 1 to 3 halogens, deuterium and O 83099;-SR83099;-No. 74191; r7495;cyano or C₁₋₆alkyl or C₁₋₆alkoxy, where the alkyl or alkoxy is optionally substituted with halogen, deuterium, -OR⁵,-SR83099;-No. 1.74191; r1.7495 or Ciano; if the heterosexual atom is n, then n may choose to change to r83088;R⁴ is independently C₁₋₆alkyl, C₂₋₆alkenyl, -C (O) R¹⁰,-S (O) R-(Cr: 7491; R: 74955) - 8345; - (cycloquilo, 3-7 members);- (CR³ᵃR³ᵇ) ₙ- (4- to 10-membered heterocycloalkyl) or C (O) (CH₂) ₜCN; wherein the alkyl, alkenyl, cycloalkyl or heterocycloalkyl are each independently and optionally substituted with 1 to 5 deuterium, halogen, OH, cyano or C₁₋₆alkoxy; or R⁴ and R⁴,Together with their respective atoms, they form a cyclopentadiene composed of 3 to 6 members or a non cyclopentadiene composed of 4 to 6 members. In cyclopentadiene or non cyclopentadiene, 1 to 3 halogen, deuterium-or83099 can be used instead;-SR83099;-No. 74191; r7495;cyano, C₁₋₆alkyl or C₁₋₆alkoxy, wherein the alkyl or alkoxy is optionally substituted with halogen, deuterium, -OR⁵,-SR83099;-NR R o ciano R es independientemente hidr geno o C alquilo en donde alquilo se sustituye opcionalmente con hal geno deuterio C alcoxi C alquiltiolilo -NR Rcyano, C₁₋₆alkyl or Cycloalkyl; or two R⁵,R8310es-c (o) nhr8311; r8310es-c (o) nhr8311;CO₂R⁷ or cyano; R⁷ is hydrogen or C₁₋₆alkyl; each R⁸ is independently hydrogen, halogen, cyano, -OR⁵,-SR83099;-No. 74191; r7495;C₁₋₆alkyl, C₃₋₆cycloalkyl, 3-10 membered heterocycloalkyl or 5-6 membered heteroaryl or aryl, wherein alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or aryl are optionally substituted with 1 to 3 halogen, -NR¹¹ᵃR¹¹ᵇ,-Or83099,-SR83099;cyano, C₁₋₃alkyl, -C (O) R¹⁰ or oxo; R⁸ is hydrogen, deuterium, halogen, cyano, -OR⁵,-SR⁵ or NR¹¹ᵃNR¹¹ᵇ;R⁹ is - (CR³ᵃR³ᵇ) ₚ- (C₁₋₃alkyl),-(Cr: 7491; R: 74955) - 8346; - (cycloquilo, 4-6 members);- (CR³ᵃR³ᵇ) ₚ- (4- to 6-membered heterocycloalkyl) or - (CR³ᵃRᵇ) ₚ- (C₅₋₉aryl),wherein the alkyl, cycloalkyl, heterocycloalkyl, or aryl are each optionally substituted with fluoro or C₁₋₃alkyl; R¹⁰ is C₁₋₆alkyl, where alkyl is optionally substituted with deuterium, halogen, OH, C₁₋₆alkoxy or cyano; R¹¹ᵃ and R¹¹ᵇ are each independently hydrogen or C₁₋₆alkyl, where alkyl is optionally substituted with deuterium, C₁₋₆alkoxy or cyano; and in the case of C₂₋₆alkyl, this alkyl is optionally substituted with deuterium, C₁₋₆alkoxy, cyano, halogen or OH; m is independently 0, 1, 2 or 3; n is independently 0, 1, 2 or 3; p is, independently, 0 or 1; and t is 1, 2 or 3;Or a salt acceptable in medicine, or a compound or salt of Tao Qiang Ji. Claim 10: a compound characterized by formula (2), wherein X and X are cr831222 or n respectively and N or cr831222 independently;provided that at least one of X, X or Y is not N; R¹ is C₁₋₆alkyl or C₁₋₆cycloalkyl, wherein the alkyl or cycloalkyl are optionally substituted with deuterium, halogen, OH, cyano, C₁₋₃alkyl, C₃₋₆cycloalkyl, C₁₋₆alkoxy or C₁₋₆alkylthiolyl; R³ᵃ and R³ᵇ are each independently hydrogen or C₁₋₃alkyl; R⁴ is, for each case (1, 2, 3, 4 or 5) independently and optionally, halogen, C₁₋₆alkyl, C₂₋₆alkenyl, -OR⁵,-(Cr: 7491; R: 74955) - 8345; - (cycloquilo, 3-6 members);-(Cr: 7491; R: 74955) - 8345; - (4-6 members of isopropene)1. In place of asphalt, cyclopentadiene or non cyclopentadiene, each asphalt, halogen, oh, cn-c (o) (ch832222248cn o-c832183316; - Alcoy; - NR1 74191;; R1 74955;2 R830808,together with the respective carbons to which they are attached, they form a cyclopropyl, cyclobutyl or cyclopentyl, where cyclopropyl, cyclobutyl or cyclopentyl are optionally substituted with 1 to 3 F, Cl, OH, methyl, ethyl, propyl, C₁₋ Lufluoroalkyl, C₁₋₃difluoroalkyl, C₁₋₃trifluoroalkyl, C₁₋₃hydroxyalkyl, methoxy or ethoxy; R⁵ is hydrogen or C₁₋₆alkyl, where the alkyl is optionally substituted with fluoro; R⁸ is independently hydrogen, halogen, cyano, -NR¹¹ᵃR¹¹ᵇ,5-6 membered C₁₋₆alkyl, heteroaryl or aryl, wherein the alkyl or heteroaryl or aryl are optionally substituted with 1, 2 or 3 halogen, -NR¹¹ᵃR¹¹ᵇ,C₁₋₃alkyl or oxo; R⁸ is hydrogen, deuterium, halogen or cyano; R¹⁰ is C₁₋₆alkyl, where alkyl is optionally substituted with fluoro or cyano; R¹¹ᵃ and R¹¹ᵇ are each independently hydrogen or C₁₋₆alkyl, where alkyl is optionally substituted with OH; n is independently 0 or 1; and t is 1, 2 or 3; or a pharmaceutically acceptable salt of the compound or a tautomer of the compound.