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1. 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。}}

2. 发明申请

WO2008059026A1 NOVEL 2-(2-HYDROXYPHENYL)BENZIMIDAZOLES USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译：新型2-（2-羟基苯基）苯并咪唑可用于治疗糖尿病和糖尿病
公开(公告)号：WO2008059026A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062409
申请日：2007-11-15
申请人： NOVO NORDISK A/S , OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
发明人： OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
IPC分类号： C07D235/18 , A61K31/4184 , A61P3/04 , A61P3/10
CPC分类号： C07D235/18
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物尤其可用于治疗，包括预防肥胖症，糖尿病和与其相关的许多疾病或病症。

3. 发明申请

WO2008059025A1 NOVEL 2-(2-HYDROXYPHENYL) BENZOTHIADIAZINES USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译：新的2-（2-羟基苯基）苯并二氮杂用于治疗糖尿病和糖尿病
公开(公告)号：WO2008059025A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062408
申请日：2007-11-15
申请人： NOVO NORDISK A/S , OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
发明人： OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
IPC分类号： C07D285/24 , A61K31/549 , A61P3/04
CPC分类号： C07D285/24
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物尤其可用于治疗，包括预防肥胖症，糖尿病和与其相关的许多疾病或病症。

4. 发明申请

WO1996008492A1 [1,2,4]TRIAZOLO[4,3-a]QUINOXALINONE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译： [1,2,4]三唑并[4,3-a]喹唑啉酮衍生物，其制备和使用
公开(公告)号：WO1996008492A1
公开(公告)日：1996-03-21
申请号：PCT/DK1995000364
申请日：1995-09-12
申请人： NOVO NORDISK A/S , NIELSEN, Flemming, Elmelund
发明人： NOVO NORDISK A/S
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： [1,2,4]triazolo[4,3-a]quinoxalinone compounds of general formula (I) wherein R is POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R , R , R and R independently are hydrogen; alkyl; halogen; NH2, NO2, CN, CF3, SO2NY'-Y", COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl; triazolyl; imidazolyl, piperidino, piperazinyl, morpholino or thiomorpholino all rings optionally being subtituted, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
摘要翻译： [1,2,4]三唑并[4,3-a]喹喔啉酮化合物，其中R 1是POX'X“或被COX'或POX'X”取代的烷基，X'和X “独立地是羟基或烷氧基，R 6，R 7，R 8和R 9独立地是氢;烷基;卤素; NH 2，NO 2，CN，CF 3，SO 2 NY'-Y”，COZ 其中Z'为NY'Y“或烷基，Y'和Y”独立地为氢或烷基; 三唑; 咪唑基，哌啶子基，哌嗪基，吗啉代或硫代吗啉代任选被取代的所有环都可用于治疗由兴奋性神经递质的多动症引起的适应症。

5. 发明申请

WO2008059023A1 NEW HALOALKYLSULFONE SUBSTITUTED COMPOUNDS USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译：用于治疗肥胖和糖尿病的新型HALOALKYLSULFONE替代化合物
公开(公告)号：WO2008059023A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062405
申请日：2007-11-15
申请人： NOVO NORDISK A/S , OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown
发明人： OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown
IPC分类号： C07D213/56 , C07D261/08 , A61K31/5355 , A61P3/04
CPC分类号： C07D261/08 , C07D213/56
摘要： The present invention relates to novel compounds of formula [I], wherein R 1 represernts heteroaryl, at least one substituent among R 5 , R 6 and R 7 represent -SR 12 , -S(O)R 12 or -S(O) 2 R 12 and the remaining substituents are as defined in the claims, that act as chemical uncouplers. Compounds of the invention are useful inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases associated therewith.
摘要翻译：本发明涉及式[I]的新化合物，其中R 1表示杂芳基，R 5，R 6，和R 7表示-SR 12，-S（O）R 12或-S（O）2 O 2， R 12和其余取代基如权利要求中所定义，其用作化学解偶联剂。本发明的化合物尤其可用于治疗，包括预防肥胖症，糖尿病和与其相关的许多疾病。

6. 发明申请

WO2004111032A1 SUBSTITUTED PIPERIDINE CARBAMATES FOR USE AS INHIBITORS OF HORMONE SENSITIVE LIPASE 审中-公开
标题翻译：取代的哌啶碳酸氢盐用作HORMONE敏感性脂质体的抑制剂
公开(公告)号：WO2004111032A1
公开(公告)日：2004-12-23
申请号：PCT/DK2004/000398
申请日：2004-06-10
申请人： NOVO NORDISK A/S , EBDRUP, Søren , VEDSØ, Per , JACOBSEN, Poul , NIELSEN, Flemming, Elmelund , CORNELIS DE JONG, Johannes
发明人： EBDRUP, Søren , VEDSØ, Per , JACOBSEN, Poul , NIELSEN, Flemming, Elmelund , CORNELIS DE JONG, Johannes
IPC分类号： C07D401/12
CPC分类号： C07D211/34 , C07D211/44 , C07D211/66 , C07D211/88 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Novel substituted piperidine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.
摘要翻译：新型取代的哌啶氨基甲酸酯，包含它们的药物组合物及其用于治疗和/或预防与激素敏感性脂肪酶相关的疾病和病症的用途。更具体地，这些化合物可用于治疗和/或预防激素敏感性脂肪酶的活性调节有益的疾病和病症。

7. 发明申请

WO2006125781A2 NOVEL HALOALKOXY-SUBSTITUTED SALICYLIC ANILIDES 审中-公开
标题翻译：新型卤代烷氧基取代的烷基酰胺
公开(公告)号：WO2006125781A2
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062533
申请日：2006-05-23
申请人： NOVO NORDISK A/S , OLESEN, Preben, Houlberg , HANSEN, Holger, Claus , CHRISTIANSEN, Lise, Brown , PETERSEN, Anders, Klarskov , NIELSEN, Flemming, Elmelund , HANSEN, Birgit, Sehested
发明人： OLESEN, Preben, Houlberg , HANSEN, Holger, Claus , CHRISTIANSEN, Lise, Brown , PETERSEN, Anders, Klarskov , NIELSEN, Flemming, Elmelund , HANSEN, Birgit, Sehested
CPC分类号： C07C255/60
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物可用于治疗，包括预防肥胖，糖尿病和与其相关的许多疾病或病症。

8. 发明申请

WO2006125778A1 NOVEL TRIFLUOROMETHOXY-SUBSTITUTED ARYL ANILIDES 审中-公开
标题翻译：新的三氟乙酰胺取代的ARYL抗体
公开(公告)号：WO2006125778A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062527
申请日：2006-05-23
申请人： NOVO NORDISK A/S , OLESEN, Preben, Houlberg , HANSEN, Holger, Claus , CHRISTIANSEN, Lise, Brown , PETERSEN, Anders, Klarsko , NIELSEN, Flemming, Elmelund , HANSEN, Birgit, Sehested
发明人： OLESEN, Preben, Houlberg , HANSEN, Holger, Claus , CHRISTIANSEN, Lise, Brown , PETERSEN, Anders, Klarsko , NIELSEN, Flemming, Elmelund , HANSEN, Birgit, Sehested
IPC分类号： C07C255/60 , A61K31/275 , A61P3/10
CPC分类号： C07C255/60
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物可用于治疗，包括预防肥胖，糖尿病和与其相关的许多疾病或病症。

9. 发明申请

WO2006120178A1 NEW HALOALKYLSULFONE SUBSTITUTED COMPOUNDS USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译：用于治疗肥胖和糖尿病的新型HALOALKYLSULFONE替代化合物
公开(公告)号：WO2006120178A1
公开(公告)日：2006-11-16
申请号：PCT/EP2006/062121
申请日：2006-05-11
申请人： NOVO NORDISK A/S , OLESEN, Preben, Houlberg , HANSEN, Holger Claus , CHRISTIANSEN, Lise, Brown , NIELSEN, Flemming, Elmelund , PETERSEN, Anders, Klarskov
发明人： OLESEN, Preben, Houlberg , HANSEN, Holger Claus , CHRISTIANSEN, Lise, Brown , NIELSEN, Flemming, Elmelund , PETERSEN, Anders, Klarskov
IPC分类号： C07C317/40 , C07D295/26 , A61P3/04 , C07C317/46 , C07D307/79 , A61P3/10 , C07C317/50 , C07D317/60 , C07C323/42 , C07D333/38 , C07C323/62 , A61K31/167
CPC分类号： C07C317/46 , C07C317/40 , C07C317/50 , C07C323/42 , C07C323/62 , C07C2602/08 , C07C2602/10 , C07C2603/72 , C07D295/26 , C07D307/79 , C07D317/60 , C07D333/38
摘要： The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
摘要翻译：本发明涉及式I化合物，其中R 5，R 6和R 7中的至少一个是SR 12，S（O）R 12或S（O）2 R 12基团，其中R 12是C 1-6卤代烷基，其作为化学解偶联剂。本发明的化合物可用于治疗，包括预防肥胖症，糖尿病以及与其相关的许多疾病或病症。

10. 发明申请

WO2008059024A1 2- ( 2 -HYDROXYPHENYL) -QUINAZOLIN-4-ONES USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译： 2-（2-羟基苯基） - 喹唑啉-4-酮有助于治疗糖尿病和糖尿病
公开(公告)号：WO2008059024A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062407
申请日：2007-11-15
申请人： NOVO NORDISK A/S , OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
发明人： OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
IPC分类号： C07D239/91 , A61K31/517 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/12
CPC分类号： C07D239/91
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物尤其可用于治疗，包括预防肥胖症，糖尿病和与其相关的许多疾病或病症。

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