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11. 发明申请

WO2008092681A1 GHRELIN RECEPTOR MODULATORS 审中-公开
标题翻译： GHRELIN受体调节剂
公开(公告)号：WO2008092681A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/000758
申请日：2008-01-29
申请人： 7TM PHARMA A/S , LINNANEN, Tero , RIST, Øystein , GRIMSTRUP, Marie , FRIMURER, Thomas , HOEGBERG, Thomas , NIELSEN, Flemming, Elmelund , GERLACH, Lars-Ole
发明人： LINNANEN, Tero , RIST, Øystein , GRIMSTRUP, Marie , FRIMURER, Thomas , HOEGBERG, Thomas , NIELSEN, Flemming, Elmelund , GERLACH, Lars-Ole
IPC分类号： C07D307/00 , C07D491/08 , A61K31/075 , A61K31/34 , A61K31/407 , C07D209/56 , C07D307/93 , C07D491/18 , C07D491/153 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/02 , A61P43/00
CPC分类号： C07D491/18 , A61K31/075 , A61K31/34 , A61K31/407
摘要： Compounds of Formula (IA) or (IB) modulate ghrelin receptor activity, and are useful in the treatment of, for example, obesity and eating disorders: wherein W is, in either orientation, -C(=O)N(R 3 )-, or -C(=O)O-; R is hydrogen or C 1 -C 4 alkyl; R 1 is selected from hydrogen, (C 1 -C 4 )alkyl, cycloalkyl, fully or partially fluorinated (C 1 -C 4 )alkyl, or -OR 10 ; and R 2 is selected from (i) hydrogen and (ii) (C 1 -C 4 )alkyl, cycloalkyl, cycloalkenyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, C 1 -C 4 alkyl, cyclopropyl, -NR 7 COR 0 , -NR 7 SO 2 R 0 , -COR 0 , -COOH, -SOR 9 , -SO 2 R 0 , -OR 10 , -NR 7 R 8 , or -NR 7 COOR 8 ; and (iii) aryl, aryl-(C 1 -C 2 )alkyl-, heteroaryl and heteroaryl-(C 1 -C 2 alkyl)- each optionally substituted in the ring part or R 1 and R 2 , together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; R 3 is selected from hydrogen, (C 1 -C 4 )alkyl, cycloalkyl, fully or partially fluorinated (C 1 -C 4 )aIkyl, or -OR 10 ; and R 4 is selected from (iv) hydrogen and (v) (C 1 -C 4 )alkyl, cycloalkyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, -NR 7 COR 0 , -NR 7 SO 2 R 0 , -COR 0 , - COOH, -SOR 9 , -SO 2 R 0 , -OR 10 , -NR 7 R 8 , or -NR 7 COOR 8 ; and (vi) aryl, aryl-(C 1 -C 2 )alkyl-, heteroaryl and heteroaryl-(C 1 -C 2 alkyl)- each optionally substituted in the ring part thereof; or R 3 and R 4 , together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; L is a linker radical of formula -(CR 11 R 13 ) a B(CR 12 R 14 )b- as defined in the specification; R 0 , R 7 , R 8 , R 9 and R 10 are as defined in the specification.
摘要翻译：式（IA）或（IB）的化合物调节生长素释放肽受体活性，并且可用于治疗例如肥胖症和进食障碍：其中W为任一取向-C（= O）N（R _{或-C（= O）O-; R是氢或C 1 -C 4烷基; R 1选自氢，（C 1 -C 4 -C 4）烷基，环烷基，完全或部分氟化（C 1 -C 4）烷基，烷基或-OR 10; 和R 2选自（i）氢和（ii）（C 1 -C 4 -C 4）烷基，环烷基，环烯基和非环烷基芳基杂环基，各自任选被-F，-CN，C 1 -C 4烷基，环丙基，-NR 7 - 0，-NR 7，SO 2，-SO 2，-COOH， - SOR 9，-SO 2 R 0，-OR 10，-NR 7，/ SO 2， R 8，或-NR 7 COOR 8; 和（iii）芳基，芳基 - （C 1 -C 2 -C 2）烷基 - ，杂芳基和杂芳基 - （C 1 -C 3 > - >烷基） - 各自任选在环部分或R 1和R 2中被取代，与它们所连接的氮一起形成任选地取代的环状氨基; R 3选自氢，（C 1 -C 4 - ）烷基，环烷基，完全或部分氟化（C 1 -C 4）烷基， C 1 -C 4烷基或-OR 10; 和R 4选自（iv）氢和（v）（C 1 -C 4 -C 4）烷基，环烷基和非芳族杂环基，各自任选被-F，-CN，-NR 7 COR 0，-NR 7 SO 2取代， R 0 0，-COR 0，-COOH，-SOR 9，-SO 2 R 0 -OR 10，-NR 7 R 8或-NR 7 COOR _{> 8 ; 和（vi）芳基，芳基 - （C 1 -C 2 -C 2）烷基 - ，杂芳基和杂芳基 - （C 1 -C 3 > - >烷基） - 各自任选在其环部分取代; 或R 3和R 4与它们所连接的氮一起形成任选取代的环状氨基; L是式 - （CR 11 R 13）a B的连接基团（CR 12 R 12） > 14 b-如说明书中所定义; R 0，R 7，R 8，R 9和R 10是如说明书中所定义。}}

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