发明名称 BISARYLSULFONAMIDES USEFUL IN THE TREATMENT OF INFLAMMATION AND CANCER
摘要 A compound of formula (I);;useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
申请公布号 US2016221938(A1) 申请公布日期 2016.08.04
申请号 US201615078502 申请日期 2016.03.23
申请人 Kancera AB 发明人 MARTINSSON Jessica;FAERNEGARDH Katarina;JOENSSON Mattias;RINGOM Rune;GUSTAFSSON SHEPPARD Nina;HELLEDAY Thomas;GROTH Petra
分类号 C07C311/21;A61K31/381;C07D409/10;A61K31/235;C07D307/82;A61K31/343;C07D307/64;A61K31/341;C07D213/71;A61K31/44;C07D333/62;C07D285/14;A61K31/433;A61K31/277;C07D409/12;A61K31/4025;A61K31/5377;A61K31/4178;A61K31/496;C07D215/14;A61K31/47;C07D409/04;A61K31/4436;A61K31/4453;C07D211/06;C07D277/587;A61K31/426;A61K45/06;C07D333/34 主分类号 C07C311/21
代理机构 代理人
主权项 1. A compound of formula (I) wherein n is 0 or 1; A is O, S, —CR4═CR4— or —CR4═N—; R1 is selected from H; halogen; C1-C6 alkyl, optionally substituted with at least one halogen; and C1-C6 alkoxy, optionally substituted with at least one halogen; R2 and R3 are each independently selected from H; halogen; C1-C6 alkyl; C1-C6 alkoxy; carbamoyl; secondary or tertiary C1-C6 alkylamido; carbocyclylcarbonylamino-C0-C2 alkyl; 5- or 6-membered cyclic aminocarbonyl optionally containing a further heteroatom in the ring; C1-C6 alkylcarbonylamino; C1-C6 alkylsulfonyl; hydroxy-C0-C6 alkyl, C1-C6 alkylcarbonyl; carboxy; C1-C6 alkoxycarbonyl; cyano; carbocyclyloxy; heterocyclyloxy; carbocyclyl-C0-C3 alkyl; carbocyclyl-C2-C3 alkenyl; hetero-cyclyl-C0-C3 alkyl; and heterocyclyl-C2-C3 alkenyl; wherein any alkyl is optionally substituted with at least one halogen; any carbocyclyl or heterocyclyl is 5- or 6-membered monocyclyl or 9- or 10-membered bicyclyl; and any carbocyclyl or heterocyclyl is optionally substituted with at least one R5; or R2 and R3 form, together with the carbon atoms to which they are attached, a 5- or 6-membered carbocyclic or heterocyclic ring, which ring is optionally substituted with at least one R5; provided that R1, R2 and R3 are not all hydrogen; each R4 is independently selected from H, halogen, monocyclic C3-C6 carbocyclyl and C1-C6 alkyl, wherein any alkyl is optionally substituted with at least one halogen; each R5 is independently selected from halogen; C1-C6 alkyl; C1-C6 alkoxy; phenoxy; amino; cyano; nitro; secondary or tertiary C1-C6 alkylamino; 5- or 6-membered cyclic amino, optionally containing at least one further heteroatom in the ring; C1-C6 alkylcarbonylamino; carbamoyl; secondary or tertiary C1-C6 alkylamido; 5- or 6-membered cyclic aminocarbonyl; C1-C6 alkoxycarbonylamino; hydroxy-C0-C6 alkyl; C1-C6-alkylthio; carboxy-C0-C6-alkyl; C1-C6 alkoxycarbonyl; C1-C6 alkylcarbonyl; C1-C6-alkylsulfonyl; and C1-C6 alkylsulfonylamino; wherein any alkyl is optionally substituted with at least one halogen; Ra is selected from H and C1-C6 alkylcarbonyl; Rb is selected from H, C1-C6 alkyl, C1-C6 alkyl substituted with at least one R6; carbocyclyl-C0-C5 alkyl; and heterocyclyl-C0-C5 alkyl; wherein any carbocyclyl and heterocyclyl is 5- or 6-membered and is optionally substituted with at least one R7 and optionally comprises at least one oxo group in the ring; provided that Ra and Rb are not both H; each R6 is independently selected from hydroxy; C1-C6 alkoxy; hydroxy-C1-C6 alkoxy; C1-C6 alkylcarbonyloxy; C1-C6 alkoxycarbonyloxy; 5- or 6-membered carbocyclylcarbonyl or heterocyclylcarbonyl; amino; secondary or tertiary C1-C6 alkylamino; secondary or tertiary hydroxy-C1-C6 alkylamino; 5- or 6-membered cyclic amino optionally containing at least one further heteroatom in the ring and wherein the ring is optionally substituted with at least one C1-C6 alkyl; C1-C6 alkylcarbonylamino; C1-C6 alkoxycarbonylamino; (C1-C6 alkoxycarbonyl)(C1-C6 alkyl)amino; (C1-C6 alkoxycarbonyl)(5- or 6-membered carbocyclyl or heterocyclyl)amino; (C1-C6 alkylcarbonyl)(C1-C6 alkyl)amino; carbamoyl; secondary or tertiary C1-C6 alkylamido wherein any alkyl is optionally substituted by OH or CONH2; 5- or 6-membered carbocyclyl- or heterocyclylcarbamoyl; 5- or 6-membered cyclic aminocarbonyl, optionally containing at least one further heteroatom in the ring, and wherein the ring is optionally substituted with at least one C1-C6 alkyl; 5- or -6-membered carbocyclylamino or heterocyclylamino; 5- or -6-membered carbocyclyloxy or heterocyclyloxy; wherein any alkyl is optionally substituted with at least one halogen and any 5- or 6-membered carbocyclyl or heterocyclyl is optionally substituted with at least one R8; each R7 and R8 is independently selected from C1-C6 alkyl; hydroxy-C0-C3 alkyl; C1-C6 alkoxy-C0-C3 alkyl; C1-C6 alkoxycarbonyl; carbocyclyl-C0-C4 alkyl; heterocyclyl-C0-C4 alkyl; C1-C6 alkylsulfinyl; amino; nitro; C1-C6 secondary or tertiary amino; halogen; carbamoyl; secondary or tertiary C1-C6 alkylamido-C0-C3 alkyl; C1-C6 alkylcarbonylamino; and 5- or 6-membered cyclic amino, optionally containing at least one further heteroatom in the ring and wherein the ring is optionally substituted with at least one C1-C6 alkyl; wherein any alkyl is optionally substituted with at least one halogen; wherein any carbocyclyl and heterocyclyl is 5- or 6-membered; or a pharmaceutically acceptable salt thereof, provided that the compound is not 5-(N-(3-hydroxy-4-(methoxycarbonyl)phenyl)sulfamoyl)-2-methoxybenzoic acid, methyl 2-hydroxy-4-(4-propylphenylsulfonamido)benzoate, methyl 4-(4-ethylphenylsulfonamido)-2-hydroxybenzoate, methyl 4-(4-butylphenylsulfonamido)-2-hydroxybenzoate, methyl 4-(3-bromophenylsulfonamido)-2-hydroxybenzoate, methyl 4-(4-(tert-butyl)phenylsulfonamido)-2-hydroxybenzoate, methyl 4-(3,5-dichlorophenylsulfonamido)-2-hydroxybenzoate, methyl 2-hydroxy-4-(3-methylphenylsulfonamido)benzoate, methyl 4-(3-fluorophenylsulfonamido)-2-hydroxybenzoate, ethyl 4-(4-acetamidophenylsulfonamido)-2-hydroxybenzoate, methyl 4-(4-acetamidophenylsulfonamido)-2-hydroxybenzoate, phenyl 2-hydroxy-4-(4-methylphenylsulfonamido)benzoate, phenyl 4-(4-chlorophenylsulfonamido)-2-hydroxybenzoate, methyl 2-hydroxy-4-(4-(4-oxo-1,4-dihydropyrazolo[1,5-a][1,3,5]triazin-8-yl)phenylsulfonamido)benzoate, methyl 2-hydroxy-4-(4-methylphenylsulfonamido)benzoate, 2-acetoxy-4-(4-methylphenylsulfonamido)benzoic acid, methyl 2-hydroxy-4-(3-(methylcarbamoyl)phenylsulfonamido)benzoate, methyl 2-hydroxy-4-(3-(piperidine-1-carbonyl)phenylsulfonamido)benzoate, methyl 4-(3-bromo-5-(trifluoromethyl)phenylsulfonamido)-2-hydroxybenzoate, 3-(N-(3-hydroxy-4-(methoxycarbonyl)phenyl)sulfamoyl)benzoic acid, methyl 4-((3-bromophenyl)methylsulfonamido)-2-hydroxybenzoate, or methyl 4-(4,5-dichlorothiophene-2-sulfonamido)-2-hydroxybenzoate.
地址 Solna SE