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Methods and compositions for inhibiting the interaction of Menin Protein Mill
专利权人:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN;KURA ONCOLOGY, INC.
发明人:
SZYMON KLOSSOWSKI,YI LIU,PINGDA REN,JUN FENG,TAO WU,LIANSHENG LI,JONATHAN POLLOCK,DMITRY BORKIN,TOMASZ CIERPICKI,JOLANTA GREMBECKA
申请号:
ARP160100689
公开号:
AR104020A1
申请日:
2016.03.15
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Ingredients and methods for inhibiting the interaction of meningitis with PVC Mll1, mll2 and MLL. Compounds and methods of use contribute to the treatment of leukemia, solid cancer, diabetes and other diseases caused by mixed protein activity Mll1, mll2, MLL and / or meningitis. 1. Characteristic 1: a formula compound (1) or a pharmaceutically acceptable salt in the formula, wherein H-I is the formula compound (2);X1 and X2 are independent CR2 or N; X3 and x83088 are independent C or N; 1 and 2 are independent CR3,N. 830808,Or s, as long as X1 is CR2,X2 is 2 or N, X3 is C, x8308es is C, 1 is 1, 2 is s, 1 is n, 1 is n, 1 and 2 are independent links, carbide, O, s, n8309a,-8310; - ch832222;-No. 8310; (= O) -,-8310; - 1832222;Tar, tonsil, isopar, tar, carbonate, tonsil or isopar carbide; a is a link, a saturated ring of 3-7 members, or an unsaturated ring of 3-7 members; n is an integer of 0-12; B is selected from B-I, b-II, b-iii and B-IV; B is connected by any atom of b-iv. Ring in L2B-I is a formula compound (3);B-II is a formula compound (4);B-iii is a compound formula (5);B-IV is a compound formula (6);Each Z1,Uh...Z3 and z830808 independent cr831183;N o NRZ8309ees C or N; each z8310a;Z831182 and z831222 are independent of cr831222,N. No. 8313,Or s, each z8313,Z1 83041 and Z1 are independent CR1 83044,RequestNumber 3,O o o s, n is an integer between 0 and 6, each R1,R2,R3,R830808,R83099,R8310,R8311th,R8322,R8313,R830404,R1,R¹² and R¹³ are each independently selected from H, halo, hydroxyl, amino, cyano, dialkylphosphine oxide, oxo, carboxyl, amido, acyl, alkyl, cycloalkyl, heteroalkyl, haloalkyl, aminoalkyl, hydroxyalkyl, alkoxy, alkylamino, cycloalkylalkyl, cycloalkyloxy, cycloalkylakyloxy, cycloalkylamino, cycloalkylakylamino, heterocyclyl, heterocyclylalkyl, heterocyclyloxy, heterocyclylarylakylarylarylakylarylarylaryl, arylakylaryl, arylakylarylaryl, aryl, arylakylaryl, aryl, and each of RA and RB is selected,In each case, halo, hydroxy, amino, cyanogen, oxysu
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