首页> 外国专利> Fluoroglicosidicos Derivatives of pyrazoles with Inhibitory activity of SGLT 1, medicaments containing these compounds and their use in the treatment of Type I and Type II diabetes.

Fluoroglicosidicos Derivatives of pyrazoles with Inhibitory activity of SGLT 1, medicaments containing these compounds and their use in the treatment of Type I and Type II diabetes.

机译:具有SGLT 1抑制活性的吡唑的氟糖苷衍生物,包含这些化合物的药物及其在I型和II型糖尿病治疗中的用途。

摘要

These compounds are appropriate, for example, as a drug for the treatment of type I and type II diabetes. Item 1: a formula compound (1), wherein R1 and R2 independently mean,F or h, definitely one of the R1 or R2 radicals; a means o, NH, CH2, s or link; R3 means h, F, Cl, Br, I, oh, CF3, NO2, CN, cooph, co - (C1-6 tar),COO (C1-6 tar)CONH 2, CONH - (C1-6 asphalt)And (C1-6) 2, C1-6, C1-6, cycloquilo C3-6, alquenilo c2-6, c12-6, or - (C1-6, hydrocarbon),Ho - (C1-6 tar)(C1-6) - O - (C1-6 asphalt)1. Benzene, benzene (Alcoy C1-6) - carbide, can be replaced by one or more f or all h of tar, acyl chloride, tar and o-tar; so2-nh2, so2-nh (C1-6 tar);So2n (C1-6 tar) 2, s - (C1-6 tar),S - (CH2) o-phenyl, so - (C1-6 tar),So - (CH2) o-phenyl, SO2 - (C1-6 tar),SO2 - (CH2) o-phenyl has the value of 0-6 or 0-6, and can be replaced by F, Cl, Br, oh, CF3, NO2, CN, ocf3 or - (C1-6 tar) up to twice;C1-6, NH2; NH2, NH - (C1-6 tar),N (C1-6 tar) 2, nh-co - (c1-7 tar),1. Phenyl, O - (CH2) or - phenyl, having the value of 0-6 or 0-6, and the phenyl ring can be replaced one to three times, with F, Cl, Br, I, oh, CF3, NO2, CN, ocf3, or - (C1-6 tar),C1-6, NH2, NH (C1-6 tar),N (C1-6 tar) 2, so2-ch3, COOH, COO - (C1-6 tar),CONH2; R4 refers to h, C1-6 asphalt, c2-6 alquenilo C3-6, or phenyl which can be replaced by C1-4 halogen or aspha B refers to c0-15 asphalt, which can be replaced independently by one or more asphalt C atoms,I am me.- (C 3DO) --CH=CH---C::C--- yes.-Ch (OH)- Shh...-CF2...- (S 3DO) -- (SO2) --N (C1-6 tar) -,-N ((C1-6) - phenyl) - o-nh -;R5, R6, R7 stand for independence,H. F, Cl, Br, I, oh, CF3, NO2, CN, COO h, COO (C1-6 tar),2. CO (C1-4 tar);CONH 2, CONH (C1-6 asphalt)And (C1-6) 2, C1-6, C1-6, alquenilo c2-6, c2-6, or - (c1-8, asphalt),Hu - (C1-6) - O - (pitch C1-6)It may be replaced by more than one f, or all h from the radical tar, aluminum, tar and o-tar; so2-nh2, so2nh (C1-6 tar),So2n (C1-6 tar) 2, s - (C1-6 tar),S - (CH2) o-phenyl, ScF3, so - (C1-6 tar),So - (CH2) o-phenyl, SO2 (C1-6 tar),SO2 - (CH2) o-phenyl has or may have a value of 0-6, and can be replaced by F, Cl, Br, oh, CF3, NO2, CN, ocf3 or - (C1-6 tar) for up to two times,C1-6, NH2; NH2, NH - (C1-6 tar),N (C1-6 tar) 2, nh-co - (C1-6 tar),1. Phenyl, O - (CH2) or - phenyl, having the value of 0-6 or 0-6, and the phenyl ring can be replaced one to three times, with F, Cl, Br, I, oh, CF3, NO2, CN, ocf3, or - (c1-8 tar),C1-6, NH2, NH (C1-6 tar),N (C1-6 tar) 2, so2-ch3, COOH, COO - (C1-6 tar),C12; or R6 and R7, together with the C atom supporting them, refer to a 5-7-ring, saturated, partially unsaturated, unsaturated or completely unsaturated CC1. The 1-2 C atoms of the ring may also be replaced by N, O or s, and CC1 can be replaced by C1-6 tar or alquenilo c2-5, C2-5 tar, in which case a CH2 group may have been replaced or replaced by H, F, Cl, oh, CF3, NO2, CN, COO (C1-4 tar),CONH 2, CONH (C1-4 tar)X means Co, O, NH, s, so, SO2 or link; l means asphalt C1-6, alquenileno c2-5, c12-5, asphalt c2-5, which may be replaced by NH or NH respectively by one or two CH2 groups; and it means Co, nhco, so, SO2, or link; R8, R9 means independent,H. SO3H, massive sugar, C1-6 tar, can be independently replaced by one or more different tar CH2 groups,And C1-6, oh, (tar C1-6) - Oh, (alquenilen c2-6) - Oh, O - (sugar radical).Oso3h, NH2, NH - (C1-6 tar)N (C1-6 tar) 2, nh-co - (C1-6 tar),NH - (sugar radical)Nh-so3h (asphalt C1-6) - NH2 (alquenilen c2-6) - NH2 (asphalt c0-6) - NH2 (asphalt c0-6) - COH (asphalt c0-6) - CONH2 (asphalt c0-6) - CONH - (asphalt C1-6),(pitch c0-6) - sonh2 (pitch c0-6) - sonh - (pitch C1-6),(tar c0-6) - 2nh2 (tar c0-6) - 2nh (tar C1-6, adamantilo; or R8 and R9, together with the N atoms that support them, means that a ring of 5 to 7 rings, saturated, C22, may also be replaced by one or more CH2 groups with O, s, NH, ns3h, N - (glycoradical type),N - (C1-6 tar)One or more CH2 groups of infrastructure may be replaced independently of each other,And C1-6, ha ha, (tar C1-6) - Oh, (alquenilen c2-6) - Oh, NH2, NH - (tar C1-6),N (C1-6 tar) 2, nh-co - (C1-6 tar, NH - (sugar radical type),(asphalt company C1-6) - NH2 (alquenilen c2-6) - NH2 (asphalt company c0-6) - COOH (asphalt company c0-6) - CONH2 (asphalt company c0-6) - CONH - (asphalt company C1-6),(pitch c0-6) - sonh2 (pitch c0-6) - sonh - (pitch C1-6),(tar layer C0-6) -SO2NH2 (tar layer C0-6) -SO2NH- (tar layer C1-6);And medically acceptable salts.
机译:这些化合物适合作为例如治疗I型和II型糖尿病的药物。第1项:式(1)的化合物,其中R 1和R 2独立地表示F或h,绝对是R 1或R 2基团之一; a表示o,NH,CH 2,s或连接; R3表示h,F,Cl,Br,I,oh,CF3,NO2,CN,cooph,co-(C1-6焦油),COO(C1-6焦油)CONH 2,CONH-(C1-6沥青) (C1-6)2,C1-6,C1-6,环quilo C3-6,alquenilo c2-6,c12-6或--(C1-6,烃),Ho-(C1-6焦油)(C1- 6)-O-(C1-6沥青)1。苯,苯(Alcoy C1-6)-碳化物,可以被焦油,酰氯,焦油和邻焦油中的一个或多个h或全部h取代; so2-nh2,so2-nh(C1-6 tar); So2n(C1-6 tar)2,s-(C1-6 tar),S-(CH2)邻苯基,so-(C1-6 tar),因此-(CH2)邻苯基,SO2-(C1-6焦油),SO2-(CH2)邻苯基的值为0-6或0-6,可以被F,Cl,Br,oh取代,CF3,NO2,CN,ocf3或-(C1-6焦油)最多两次; C1-6,NH2; NH 2,NH-(C 1-6焦油),N(C 1-6焦油)2,nh-co-(c1-7焦油),1。苯基,O-(CH2)或-苯基,值为0-6或0-6,并且苯环可以被F,Cl,Br,I,OH,CF3,NO2取代1-3次CN,ocf3或-(C1-6焦油),C1-6,NH2,NH(C1-6焦油),N(C1-6焦油)2,so2-ch3,COOH,COO-(C1-6焦油) ,CONH2; R4是指h,C1-6沥青,c2-6alquenilo C3-6或可以被C1-4卤素或沥青取代的苯基; B是指c0-15沥青,可以被一个或多个沥青C原子独立取代,我是。-(C 3DO)--CH = CH --- C :: C ---是的.-Ch( OH)-Shh ...- CF2 ...-(S 3DO)-(SO2)-N(C1-6 tar)-,-N((C1-6)-苯基)-o-nh-; R5,R6,R7代表独立性,H。 F,Cl,Br,I,哦,CF3,NO2,CN,COO h,COO(C1-6焦油),2。 CO(C1-4焦油); CONH 2,CONH(C1-6沥青)和(C1-6)2,C1-6,C1-6,alquenilo c2-6,c2-6或-(c1-8,沥青),Hu-(C1-6)-O-(沥青C1-6)可以用基团焦油,铝,焦油和邻位焦油中的一个以上f或全h取代; so2-nh2,so2nh(C1-6焦油),So2n(C1-6焦油)2,s-(C1-6焦油),S-(CH2)邻苯基,ScF3,so-(C1-6焦油),因此-(CH2)邻苯基,SO2(C1-6焦油),SO2-(CH2)邻苯基具有或可能具有0-6的值,并可被F,Cl,Br,oh,CF3取代,NO2,CN,ocf3或-(C1-6焦油)最多两次,C1-6,NH2; NH2,NH-(C1-6焦油),N(C1-6焦油)2,nh-co-(C1-6焦油),1。苯基,O-(CH2)或-苯基,值为0-6或0-6,并且苯环可以被F,Cl,Br,I,OH,CF3,NO2取代1-3次CN,ocf3或-(c1-8焦油),C1-6,NH2,NH(C1-6焦油),N(C1-6焦油)2,so2-ch3,COOH,COO-(C1-6焦油) ,C12;或R 6和R 7,连同支持它们的C原子,是指5-7环,饱和,部分不饱和,不饱和或完全不饱和的CC 1。环的1-2个C原子也可以被N,O或s取代,而CC1可以被C1-6焦油或alquenilo c2-5,C2-5焦油取代,在这种情况下,CH2基团可能已经被被H,F,Cl,OH,CF3,NO2,CN,COO(C1-4焦油),CONH 2,CONH(C1-4焦油)取代或替换X表示Co,O,NH,s,SO2或链接; l表示沥青C1-6,alquenileno c2-5,c12-5,沥青c2-5,可以分别被一个或两个CH2基团取代为NH或NH。表示Co,nhco,so,SO2或链接; R8,R9表示独立的H。 SO3H,块状糖,C1-6焦油可以独立地被一个或多个不同的焦油CH2基团取代,并且C1-6哦,(焦油C1-6)-哦,(alquenilen c2-6)-哦,O- (糖基).Oso3h,NH2,NH-(C1-6焦油)N(C1-6焦油)2,nh-co-(C1-6焦油),NH-(糖基)Nh-so3h(沥青C1- 6)-NH2(alquenilen c2-6)-NH2(沥青c0-6)-NH2(沥青c0-6)-COH(沥青c0-6)-CONH2(沥青c0-6)-CONH-(沥青C1-6 ),(螺距c0-6)-sonh2(螺距c0-6)-sonh-(螺距C1-6),(tar c0-6)-2nh2(tar c0-6)-2nh(tar C1-6,adamantilo;或R8和R9,连同支持它们的N原子,是指5至7个饱和碳原子的环C22也可以被一个或多个带有O,s,NH,ns3h,N-的CH2取代。糖基类型),N-(C1-6焦油)一个或多个CH2基团可以彼此独立取代,并且C1-6,哈哈,(焦油C1-6)-哦,(alquenilen c2-6) -哦,NH2,NH-(焦油C1-6),N(C1-6焦油)2,nh-co-(C1-6焦油,NH-(糖基类型),(沥青公司C1-6)-NH2 ( Alquenilen c2-6)-NH2(沥青公司c0-6)-COOH(沥青公司c0-6)-CONH2(沥青公司c0-6)-CONH-(沥青公司C1-6),(沥青c0-6)- sonh2(间距c0-6)-sonh-(间距C1-6),(焦油层C0-6)-SO2NH2(焦油层C0-6)-SO2NH-(焦油层C1-6);以及医学上可接受的盐。

著录项

  • 公开/公告号AR049393A1

    专利类型

  • 公开/公告日2006-07-26

    原文格式PDF

  • 申请/专利权人 SANOFI-AVENTIS DEUTSCHLAND GMBH;

    申请/专利号AR2005P102406

  • 发明设计人

    申请日2005-06-13

  • 分类号C07H17/02;A61K31/7056;A61P3/10;

  • 国家 AR

  • 入库时间 2022-08-21 21:40:28

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