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Azaheterociclobencilaminas biciclicas as PI3K inhibitors
专利权人:
INCYTE CORPORATION
发明人:
申请号:
ARP130101033
公开号:
AR090548A1
申请日:
2013.03.27
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
They regulate the activity of 3-quinine (PI3K) and help to treat diseases related to PI3K activity, such as inflammation, immune disorders, cancer and other diseases. 1. Characteristic 1: a formula compound (1) or a salt from which drug acceptance can be obtained, where V is C (= O),S (3DO)CH8322;CHR³ᶜ,and CR³ᶜR³ᶜ;T is C (= O),S (3DO)CH8322;CHR³ᵃ,and CR³ᵃR³ᵃ;it is life.S (3DO)(CH₂) ₙ,(CHR)y (CR R)where n is 0, 1, or 2; U is O or NR³ᵈ;If t is C (= O) or s (= O) 832222,Q is (CH₂) ₙ, (CHR³ᵃ) ₙ,o - (CR R)If q is C (= O) or s (= O) 832222,T is ch8322;CHR³ᵃ,o CR R y U es NRRA is H or C₁₋₃ alkyl;Comment more than a month ago(3)(4) (5)X1 is ch or N; Y1 is ch or N; on the contrary, RA and Ar are connected with n to form a practical equation group (6);X is cr8313o n; W is cr8311o n; and cr831222;CR⁸ᵃ,Or N, Z is a link or C (= O);If - w = y-z-es-cr-8311a = cr831222 -,-N = CR⁸-,-CR 3DCR -C (3DO) --N 3DCR -C (3DO) -o -CR 3DN-C (3DO) -R1 is lease No. c83217c83238a;each R³ᵃ is independently selected from C₁₋₆ alkyl,C₂₋₆ alkenyl,1. C 83228331 asphalt;C₁₋₆ haloalkyl,And Cy1.where said C₁₋₆ alkyl,C₂₋₆ alkenyl,e. C832283316c1 and c833326c1 were replaced by group 1, 2 or 3R1, respectively; R3 7495es h, cy, - (acquileno c83321c833318326cy, acquiro c832626c;C₂₋₆ alkenyl,1. C 83228331 asphalt;C₁₋₆ haloalkyl,C 833333832 or 8334r7495;C (3DO) NR RC (3DO) ORC (= No. 74977) r7495;C (= No. 74977); r74966;S (3DO) Ro S (3DO) NR Rwhere said C₁₋₆ alkyl,C₂₋₆ alkenyl,and C₂₋₆ alkynyl is each optionally substituted by 1, 2, 3, or 4 independently selected R¹³ᵇ groups; each R³ᶜ is independently selected from C₁₋₄ alkyl,C₁₋₄ haloalkyl,C₁₋₄ alkoxy-C₁₋₄ alkyl,and C₁₋₄-C₁₋₄ alkyl haloalkoxy;R³ᵈ is H, C₁₋₄ alkyl,C₁₋₄ haloalkyl,C₁₋₄ alkoxy-C₁₋₄ alkyl,O haloalcoxy c833217d.833183248a - rent c833218d.83312248a;R⁴ is H, halo, OH, CN, C₁₋₄ alkyl,C₁₋₄ haloalkyl,C₁₋₄ alkoxy,or C₁₋₄ haloalkoxy;R83099es halo, oh, CN, lease c8321c83318324;C₁₋₄ haloalkyl,C₁₋₄ alkoxy,C₁₋₄ haloalkoxy,o ciclopropilo R es H halo OH CN alqu
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