发明名称 HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF
摘要 The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I:;;as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
申请公布号 US2014323502(A1) 申请公布日期 2014.10.30
申请号 US201414179694 申请日期 2014.02.13
申请人 PFIZER INC. 发明人 Fliri Anton Franz Joseph;Gallaschun Randall James;O'Donnell Christopher John;Schwarz Jacob Bradley;Segelstein Barbara Eileen
分类号 C07D409/12;C07D407/12;C07D307/22;C07C307/02;C07D405/12;C07D333/38 主分类号 C07D409/12
代理机构 代理人
主权项 1. A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein each R1 and each R2 and each R7 is independently selected from the group consisting of hydrogen, halogen, hydroxyl, —CF3, —CN, —(C═O)R8, —O—(C═O)—R8, —(NR8)—(C═O)—R8, —(C═O)—OR8, —(C═O)—N(R8)2, —OR8, —O—(C═O)—OR8, —O—(C═O)—N(R8)2, —NO2, —N(R8)2, —(NR8)—SO2—R8, —S(O)wR8, —SO2—N(R8)2, (C1-C6)alkyl, (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl, and (C3-C10)cycloalkyl; wherein said (C1-C6)alkyl, (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl, or (C3-C10)cycloalkyl are each independently optionally substituted with one, two, three or four R9; w is 0, 1 or 2; m is zero, one, two or three; n is zero, one, two or three; p is zero, one, two or three; q is zero, one, two or three; s is one and t is one; or one of s or t is one and the other of s or t is two; R3 is hydrogen or (C1-C6)alkyl; each R4 is independently selected from hydrogen, or (C1-C6)alkyl; wherein said (C1-C6)alkyl may be optionally substituted with one, two, three or four halogen, —CN, or —OR9; or two R4 groups on the same carbon atom may be taken together to form an oxo (═O) radical or a (C3-C6)spirocycloalkyl; R5 is hydrogen, or (C1-C6)alkyl; R6 is (C1-C6)alkyl-(C═O)—, [(C1-C6)alkyl]2N—(C═O)—, (C1-C6)alkyl-SO2—, (C3-C10)cycloalkyl-SO2—, or [(C1-C6)alkyl]2N—SO2—; wherein said (C1-C6)alkyl moieties of said [(C1-C6)alkyl]2N—(C═O)— and [(C1-C6)alkyl]2N—SO2— may optionally be taken together with the nitrogen atom to which they are attached to form a four to six membered heterocyclic ring; R8 is independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl, and (C3-C10)cycloalkyl; wherein said (C1-C6)alkyl may be optionally substituted with one, two or three substituents independently selected from hydrogen, halo, —CN, perfluoro(C1-C6)alkyl, hydroxy, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, (C1-C6)alkoxy, perfluoro(C1-C6)alkoxy, HO—(C═O)—, (C1-C6)alkyl-O—(C═O)—, formyl, (C1-C6)alkyl-(C═O)—, H2N—(C═O)—, (C1-C6)alkyl]-(NH)—(C═O)—, [(C1-C6)alkyl]2N—(C═O)—, (C1-C6)alkyl-(C═O)—O—, H(C═O)—NH—, (C1-C6)alkyl(C═O)—NH—, (C1-C6)alkyl(C═O)—[N((C1-C6)alkyl)]-, (C1-C6)alkyl-SO2—, (C1-C6)alkyl-SO2—NH—, (C1-C6)alkyl-SO2—[N((C1-C6)alkyl)]-, H2N—SO2—, [(C1-C6)alkyl]-NH—SO2—, and [(C1-C6)alkyl]2N—SO2—; wherein said (C1-C6)alkyl may be additionally optionally substituted with an optionally substituted (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl, or (C3-C10)cycloalkyl; wherein said optional substituents may be independently selected from one, two, three or four radicals independently selected from halogen, hydroxyl, —CF3, —ON, (C1-C3)alkyl, (C1-C3)alkoxy, and amino; wherein each of said R8 (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl or (C3-C10)cycloalkyl substituents may be optionally additionally substituted with one, two, three or four radicals independently selected from halogen, hydroxyl, —CF3, —CN, (C1-C3)alkyl, (C1-C3)alkoxy and amino; each R9 is independently selected from the group consisting of halogen, hydroxyl, —CF3, —CN, —(C═O)R10, —O—(C═O)—R10, —(NR10)—(C═O)—R10, —(C═O)—OR10, —(C═O)—N(R10)2, —OR10, —O—(C═O)—OR10, —O—(C═O)—N(R10)2, —NO2, —N(R10)2, —(NR10)—SO2—R10, —S(O)uR10, —SO2—N(R10)2; R10 is independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl and (C3-C10)cycloalkyl; wherein said (C1-C6)alkyl may be optionally substituted with one, two or three substituents independently selected from hydrogen, halo, —CN, perfluoro(C1-C6)alkyl, hydroxy, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, (C1-C6)alkoxy, perfluoro(C1-C6)alkoxy, HO—(C═O)—, (C1-C6)alkyl-O—(C═O)—, formyl, (C1-C6)alkyl-(C═O)—, H2N—(C═O)—, (C1-C6)alkyl]-(NH)—(C═O)—, [(C1-C6)alkyl]2N—(C═O)—, (C1-C6)alkyl-(C═O)—O—, H(C═O)—NH—, (C1-C6)alkyl(C═O)—NH—, (C1-C6)alkyl(C═O)—[N((C1-C6)alkyl)]-, (C1-C6)alkyl-SO2—, (C1-C6)alkyl-SO2—NH—, (C1-C6)alkyl-SO2—[N((C1-C6)alkyl)]-, H2N—SO2—, [(C1-C6)alkyl]-NH—SO2—, and [(C1-C6)alkyl]2N—SO2—; wherein said (C1-C6)alkyl may also be additionally optionally substituted with an optionally substituted (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl or (C3-C10)cycloalkyl; wherein said optional substituents may be independently selected from one, two, three or four radicals independently selected from halogen, hydroxyl, —CF3, —CN, (C1-C3)alkyl, (C1-C3)alkoxy, and amino; wherein each of said R10 (C6-C10)aryl, (C1-C9)heteroaryl, (C1-C9)heterocycloalkyl, or (C3-C10)cycloalkyl substituents may be optionally additionally substituted with one, two, three or four radicals independently selected from halogen, hydroxyl, —CF3, —CN, (C1-C3)alkyl, (C1-C3)alkoxy, and amino; R11 is hydrogen or (C1-C6)alkyl; ring “A” is (C6-C10)aryl, (C1-C9)heteroaryl, (C4-C10)cycloalkyl, or (C1-C9)heterocycloalkyl; wherein two of said R1 substituents on said (C4-C10)cycloalkyl and (C1-C9)heterocycloalkyl may optionally be attached to the same carbon atom and may optionally be taken together to be oxo; ring “B” is (C6-C10)aryl, (C1-C9)heteroaryl, (C4-C10)cycloalkyl, or (C1-C9)heterocycloalkyl; “X” is —O— or >C(R4)2; “Y” is absent, >NR11, —(NR11)—(C═O)—, >C═O, —O— or >C(R7)2; and “Z” is —O—, —S—, —(S═O)—, or —(SO2)—.
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