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1. 发明申请

WO2004089471A3 NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：新型吡咯并[1,5-a]吡啶衍生物及其药物用途
公开(公告)号：WO2004089471A3
公开(公告)日：2004-12-23
申请号：PCT/DK2004000253
申请日：2004-04-06
申请人： NOVO NORDISK AS , ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL
发明人： ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL
IPC分类号： A61K31/519 , A61K45/06 , A61P3/04
CPC分类号： A61K31/519 , A61K45/06
摘要： The use of substituted pyrazolo[1,5-a]pyrimidines for modulating the activity of 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) and the use of these compounds as phar-maceutical compositions are described. Also a novel class of substituted pyrazolo[1,5-a]pyrimidines their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described The present com-pounds are modulators and more specifically inhibitors of the activity of 11betaHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译：描述了使用取代的吡唑并[1,5-a]嘧啶来调节1β-羟基类固醇脱氢酶（11betaHSD1）的活性以及这些化合物作为药物组合物的用途。还有一类新的取代的吡唑并[1,5-a]嘧啶在治疗中的用途，包含该化合物的药物组合物以及它们在制备药物中的用途。本发明是调节剂，更具体地说是抑制剂 11betaHSD1的活性，并且可用于治疗，预防和/或预防一系列医学病症，其中期望活性糖皮质激素的细胞内浓度降低。

2. 发明申请

WO2005058845A3 NOVEL GLUCAGON ANTAGONISTS/INVERSE AGONISTS 审中-公开
标题翻译：新的GLUCAGON ANTAGONISTS / INVERSE AGONISTS
公开(公告)号：WO2005058845A3
公开(公告)日：2005-10-20
申请号：PCT/EP2004053580
申请日：2004-12-17
申请人： NOVO NORDISK AS , MADSEN PETER , LAU JESPER , KODRA JANOS TIBOR , CHRISTENSEN INGE THOEGER
发明人： MADSEN PETER , LAU JESPER , KODRA JANOS TIBOR , CHRISTENSEN INGE THOEGER
IPC分类号： A61K31/198 , A61K31/275 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/50 , C07C235/84 , C07C237/12 , C07D207/32 , C07D207/323 , C07D233/70 , C07D233/96 , C07D237/02 , C07D237/08 , C07D261/02 , C07D261/08 , C07D261/18 , C07D413/12 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D207/323 , C07C235/84 , C07C2601/02 , C07C2601/14 , C07D233/96 , C07D237/08 , C07D261/18
摘要： Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists. (I) wherein A is (II), (III) or (IV), Y is a valence bond, >C=O, =CR -, -(CR R )m-, -NR -,=N-, E is: C1-10-alkyl or C2-10-alkenyl; C3-10-cycloalkyl, C3-10-cycloalkenyl, C7-10-bicycloalkyl, C3-10-cycloakyl-C1-6-alkyl, C3-10-cycloalkenyl-C1-6-alkyl or C7-10-bicycloalkyl-C1-6-alkyl, wherein the rings may optionally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6-alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2 and -SCHF2; aryl, aryloxy, arylthio, heteroaryl, aryl-C1-6-alkyl, aryloxy-C1-6-alkyl, arylthio-C1-6-alkyl, heteroaryl-C1-6-alkyl, diaryl-C1-6-alkyl or (C1-6 -alkyl)(aryl)-C1-7-alkyl, wherein the non-aromatic and aromatic rings may optinally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6 -alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2, SCHF2, C3-10-cycloalkyl and C3-10-cycloalkenyl, or with two substituents on adjacent positions which are combined to form a bridge C1-6-alkylene, C2-6-alkenylene or -O-C1-6-alkylene-O-; (V) represents a phenyl, C3-8-cycloalkyl, or a 4-, 5-, 6- or 7-membered heterocycle, D is aryl or heteroaryl.
摘要翻译：用于拮抗胰高血糖素肽激素对胰高血糖素受体的作用的新型化合物。更具体地，涉及胰高血糖素拮抗剂或反向激动剂。（I）其中A是（II），（III）或（IV），Y是价键，C = O，= CR 1 - ， - （CR 1 R 2）m - ，-NR 1 - ，= N-，E是：C 1-10 - 烷基或C 2-10 - 烯基; C 3-10 - 环烷基，C 3-10 - 环烯基，C 7-10 - 双环烷基，C 3-10 - 环烷基-C 1-6 - 烷基，C 3-10 - 环烯基-C 1-6 - 烷基或C 3-10 - 双环烷基-C 其中所述环可以任选地被一个或多个选自卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1-6 - 烷氧基，C 1-6 - 硫代烷基，-CF 3，-OCF 3， -SCF 3，-OCHF 2和-SCHF 2; 芳基，芳氧基，芳硫基，杂芳基，芳基-C 1-6 - 烷基，芳氧基-C 1-6 - 烷基，芳硫基-C 1-6 - 烷基，杂芳基-C 1-6 - 烷基，二芳基-C 1-6 - 烷基或（C 1 （芳基）-C 1-7 - 烷基，其中非芳族和芳族环可以选择性地被一个或多个选自卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6 - 6-烷氧基，C 1-6 - 硫代烷基，-CF 3，-OCF 3，-SCF 3，-OCHF 2，SCHF 2，C 3-10 - 环烷基和C 3-10 - 环烯基，或与相邻位置上的两个取代基组合形成桥 C 1-6亚烷基，C 2-6亚烯基或-O-C 1-6 - 亚烷基-O-; （V）代表苯基，C 3-8 - 环烷基或4-，5-，6-或7-元杂环，D是芳基或杂芳基。

3. 发明申请

WO2004089380A3 PHARMACEUTICAL USE OF FUSED 1,2,4-TRIAZOLES 审中-公开
标题翻译：融合1,2,4-三唑的药物使用
公开(公告)号：WO2004089380A3
公开(公告)日：2004-12-23
申请号：PCT/DK2004000251
申请日：2004-04-06
申请人： NOVO NORDISK AS , ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL
发明人： ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL
IPC分类号： A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , A61P3/04 , C07D471/04 , C07D487/04 , C07D487/08
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , C07D487/04 , C07D487/08
摘要： The use of fused 1,2,4-triazoles for modulating the activity of 11 beta-hydroxysteroid dehydrogenase type 1 (11 betaHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11 betaHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译：已经描述了使用稠合的1,2,4-三唑来调节11型β-羟基类固醇脱氢酶1型（11βHSD1）的活性以及这些化合物作为药物组合物的用途。还描述了一类新的稠合的1,2,4-三唑，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。本发明化合物是11βHSD1的调节剂，更具体地说是抑制活性的βHSD1，并且可用于治疗，预防和/或预防一系列需要减少活性糖皮质激素细胞内浓度的医学疾病。

4. 发明申请

WO2004089470A2 PHARMACEUTICAL USE OF SUBSTITUTED AMIDES 审中-公开
标题翻译：药物使用替代药物
公开(公告)号：WO2004089470A2
公开(公告)日：2004-10-21
申请号：PCT/DK2004000250
申请日：2004-04-06
申请人： NOVO NORDISK AS , ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL , KILBURN JOHN PAUL
发明人： ANDERSEN HENRIK SUNE , KAMPEN GITA CAMILLA TEJLGAARD , CHRISTENSEN INGE THOEGER , MOGENSEN JOHN PATRICK , LARSEN ANNETTE ROSENDAL , KILBURN JOHN PAUL
IPC分类号： A61K31/16 , A61K31/415 , A61K45/06 , A61P3/04 , A61P3/10
CPC分类号： C07D209/02 , A61K31/16 , A61K31/415 , A61K45/06 , C07D401/06 , C07D401/12 , C07D403/12 , C07D487/08
摘要： The use of substituted amides for modulating the activity of 11 beta-hydroxysteroid dehydrogenase type 1 (11 betaHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11 betaHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译：描述了使用取代的酰胺调节11型β-羟基类固醇脱氢酶1型（11βHSD1）的活性以及这些化合物作为药物组合物的用途。还描述了一类新颖的取代的酰胺，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。本发明化合物是11βHSD1的调节剂，更具体地说是抑制活性的βHSD1，并且可用于治疗，预防和/或预防一系列需要减少活性糖皮质激素细胞内浓度的医学疾病。

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