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US 2017/0320889 A1Published application
Heterocyclic derivatives and use thereof
AssigneeC&C Research Laboratories
InventorsChan Hee PARK, Sang Hwi LEE, Junhwan IM, Soon Ok LEE, Jongmin KIM, Kwang Seok KO, Byungho KIM, Minjung KONG, Mi Sun KIM, Hyung Jo MOON
Life of this patent
Estimating the term…
Abstract
A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
Claims14
A compound selected from the group consisting of a heterocyclic derivative represented by formula (I), and a pharmaceutically acceptable salt and a stereoisomer thereof:
- wherein
- one of X1, X2, X3 and X4 is —C(-Rx)=, and the others are each independently —C(-Rx′)= or —N═;
- one of Y and Z is —S— or —NH—, and the other is —CH═ or —N═;
- Rx is
- Xs is ═O or ═NH;
- Ls is —C(—Rs′)(-Rs″)- or —N(-Rs′)-;
- Rs is C1-6alkyl, haloC1-6alkyl, C1-6alkoxy-C1-6alkyl, C1-6alkylcarbonyl-C1-6alkyl, C2-7alkenyl, amino, aminoC1-6alkyl or 5- to 10-membered heterocyclyl, or Rs is linked to Rs′ to form a chain;
- Rs′ and Rs″ are each independently hydrogen, halogen, C1-6alkyl, carbamoyl-C1-6alkyl, C1-6alkylamino-C1-6alkyl or diC1-6alkylamino-C1-6alkyl, or Rs′ and Rs″ are linked together to form a chain, or Rs′ is linked to Rs to form a chain;
- Rx′ is each independently hydrogen, halogen, nitro, amino, C1-6alkoxy, haloC1-6alkoxy, or C1-6alkylsulfonyl;
- A and B are each independently a monocyclic- or bicyclic-saturated or unsaturated C3-10carbocycle or 5- to 12-membered heterocycle;
- Rc is ═O, ═NH, ═N(—C1-6alkyl), or ═N(—OH);
- RN is hydrogen or C1-6alkyl, or RN is linked to RA to form a chain;
- LB is —[C(—RL)(—RL′)]m—, —[C(—RL)(—RL′)]n—O—, —O—, —NH—, —N(C1-6alkyl)-, —S(═O)2—, —C(═O)—, or —C(═CH2)—, wherein m is an integer of 0 to 3, n is an integer of 1 to 3, RL and RL′ are each independently hydrogen, hydroxy, halogen or C1-6alkyl, or RL and RL′ are linked together to form a chain;
- RA is hydrogen, halogen, cyano, C1-6alkyl, haloC1-6alkyl, cyanoC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy, haloC1-6alkoxy, cyanoC1-6alkoxy, C1-6alkylamino, diC1-6alkylamino, C1-6alkylthio, C1-6alkylaminocarbonyl, diC1-6alkylaminocarbonyl, C2-8alkynyl, C1-6alkoxycarbonylamino-C1-6alkoxy, aminoC1-6alkoxy or 3- to 6-membered heterocyclyl, or RA is linked to RN to form a chain;
- RB is hydrogen, halogen, hydroxy, cyano, nitro, amino, oxo, aminosulfonyl, sulfonylamido, C1-6alkylamino, C1-6alkyl, haloC1-6alkyl, cyanoC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, cyanoC1-6alkoxy, C3-8cycicoalkyloxy, C2-8alkenyl, C2-8alkenyloxy, C2-8alkynyl, C2-8alkynyloxy, C1-6alkylamino-C1-6alkoxy, diC1-6alkylamino-C1-6alkoxy, C1-6alkoxycarbonyl, carbamoyl, carbamoyl-C1-6alkoxy, C1-6alkylthio, C1-6alkylsulfinyl, C1-6alkylsulfonyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heterocyclyl-C1-6alkyl, 5- to 10-membered heterocyclyl-C1-6alkoxy, or 5- to 10-membered heterocyclyl-oxy;
- p is an integer of 0 to 4, and, when p is 2 or higher, RA moieties are the same as or different from each other;
- q is an integer of 0 to 4, and, when q is 2 or higher, RB moieties are the same as or different from each other;
- and
- each of said chains is independently a saturated or unsaturated C2-10 hydrocarbon chain not containing or containing at least one heterogroup selected from the group consisting of —O—, —NH—, —N═, —S—, —S(═O)— and —S(═O)2— in the chain, and unsubstituted or substituted with at least one selected from the group consisting of halogen, C1-6alkyl and C1-6alkoxy;
- and
- each of said heterocycle and heterocyclyl moieties independently contains at least one heterogroup selected from the group consisting of —O—, —NH—, —N═, —S—, —S(═O)— and —S(═O)2—.
18 more elements
Dependencies are inferred from the claim text.