Substituted purine derivative
AssigneeSumitomo Dainippon Pharma Co., Ltd.
InventorsShingo Tojo, Yoshiaki Isobe, Eiji Ideue, Hiroaki Fujiwara, Daisuke Urabe
Life of this patent
Estimating the term…
Abstract
The present invention relates to a substituted purine derivative of formula (1) wherein R1 is alkoxy or the like, R2 is alkyl or the like, Ring Q1 is aryl or the like, W1 is alkylene or the like, Ring Q2 is aromatic carbocyclyl or the like, n is 1-4, R3 is hydrogen atom or the like, X1 is single bond or the like, W2 is alkylene or the like, and R4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.
Claims27
A compound of formula (1):
- or a pharmaceutically acceptable salt thereof
- wherein
- R1 is optionally-substituted C1-6 alkoxy, optionally-substituted C3-7 cycloalkoxy, optionally-substituted 4- to 10-membered saturated heterocyclyloxy, optionally-substituted C1-6 alkyl, optionally-substituted C3-7 cycloalkyl, optionally-substituted C1-6 alkylthio, optionally-substituted 4- to 10-membered saturated heterocyclyl, optionally-substituted amino, halogen atom, or hydroxy;
- R2 is optionally-substituted C1-6 alkyl, optionally-substituted C3-7 cycloalkyl, or optionally-substituted amino;
- W1 is single bond, or optionally-substituted C1-4 alkylene;
- Ring Q1 is
- (1) pyridyl which may be substituted with 1-5 the same or different substituents selected from the group consisting of
- (a) halogen atom,
- (b) cyano,
- (c) C1-6 alkyl which may be substituted with 1-3 the same or different halogen atoms, and
- (d) C1-6 alkoxy which may be substituted with 1-3 the same or different halogen atoms, or
- (2) pyrimidinyl which may be substituted with 1-3 the same or different substituents selected from the group consisting of (a)-(d) in the above (1),
- Ring Q2 is C6-10 aromatic carbocyclyl, or 5- to 10-membered aromatic heterocyclyl;
- n is 1, 2, 3, or 4;
- R3 is, independently if there are plural R3, hydrogen atom, halogen atom, cyano, hydroxy, optionally-substituted C1-6 alkyl, optionally-substituted C1-6 alkoxy, optionally-substituted C3-7 cycloalkyl, optionally-substituted C3-7 cycloalkoxy, or optionally-substituted amino;
- Q2-X1— is Q2-(single bond)-, Q2-(CH2)m—O—, Q2-(CH2)m—S—, Q2-(CH2)m—S(O)2—, Q2-(CH2)m—NRaS(O)2—, Q2-(CH2)m—S(O)2NRa—, Q2-(CH2)m—C(O)—, Q2-(CH2)m—NRa—, Q2-(CH2)m—NRaC(O)—, or Q2-(CH2)m—C(O)NRa—, wherein Ra is hydrogen atom or C1-6 alkyl;
- m is 0, 1, or 2;
- W2 is single bond, or optionally-substituted C1-8 alkylene;
- and
- R4 is hydrogen atom, —ORb (wherein Rb is hydrogen atom, optionally-substituted C1-6 alkyl, optionally-substituted C1-6 alkylcarbonyl, optionally-substituted aminocarbonyl, or optionally-substituted C1-6 alkylsulfonyl), —NRcRd (wherein Rc is hydrogen atom or optionally-substituted C1-6 alkyl;
- and Rd is hydrogen atom, optionally-substituted C1-6 alkyl, optionally-substituted C1-6 alkylcarbonyl, optionally-substituted C1-6 alkoxycarbonyl, or optionally-substituted C1-6 alkylsulfonyl), optionally-substituted 4- to 10-membered saturated heterocyclyl, or optionally-substituted 5- to 10-membered heteroaryl.
Dependencies are inferred from the claim text.