公开(公告)号：WO2012069420A3

公开(公告)日：2012-05-31

申请号：PCT/EP2011/070574

申请日：2011-11-21

Applicant: LEO Pharma A/S ,  VEDSØ, Per ,  BLÆHR, Lars, Kristian, Albert

Inventor： VEDSØ, Per ,  BLÆHR, Lars, Kristian, Albert

IPC: C07C229/46 ,  C07C235/10 ,  C07C311/05 ,  C07C311/46 ,  C07C69/738 ,  C07D205/04 ,  C07D317/58 ,  C07D295/185 ,  A61K31/4965 ,  A61K31/4409 ,  A61K31/18 ,  A61K31/165 ,  A61P3/14

Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

公开(公告)号：WO2012069419A1

公开(公告)日：2012-05-31

申请号：PCT/EP2011/070572

申请日：2011-11-21

Applicant: LEO PHARMA A/S ,  VEDSØ, Per ,  BLÆHR, Lars, Kristian, Albert

Inventor： VEDSØ, Per ,  BLÆHR, Lars, Kristian, Albert

IPC: C07C217/74 ,  C07C235/10 ,  C07C237/22 ,  C07C311/46 ,  C07C59/90 ,  C07C69/734 ,  C07D211/58 ,  C07D295/185 ,  C07D295/194 ,  A61K31/4965 ,  A61K31/4409 ,  A61K31/18 ,  A61K31/165 ,  A61P3/14

CPC classification number: C07C235/20 ,  C07C217/74 ,  C07C235/10 ,  C07C237/22 ,  C07C311/03 ,  C07C311/46 ,  C07C2601/08 ,  C07D211/58 ,  C07D241/08 ,  C07D295/185 ,  C07D295/192 ,  C07D295/194

Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract translation: 通式（I）的化合物，它们作为钙受体活性化合物用于预防，治疗或改善与CaSR活性紊乱相关的生理障碍或疾病的用途，例如甲状旁腺机能亢进，包含所述化合物的药物组合物和治疗疾病的方法 与所述化合物。

公开(公告)号：WO2007006761A1

公开(公告)日：2007-01-18

申请号：PCT/EP2006/064028

申请日：2006-07-07

Applicant: NOVO NORDISK A/S ,  MURRAY, Anthony ,  LAU, Jesper ,  VEDSØ, Per ,  JEPPESEN, Lone ,  KRISTIANSEN, Marit

Inventor： MURRAY, Anthony ,  LAU, Jesper ,  VEDSØ, Per ,  JEPPESEN, Lone ,  KRISTIANSEN, Marit

IPC: C07C275/14 ,  C07C275/52 ,  C07C275/62 ,  A61K31/33

CPC classification number: C07C275/62 ,  C07C2601/02 ,  C07C2601/14

Abstract: This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

Abstract translation: 本发明涉及式（I）的二环烷基氨基甲酰基脲，其为葡糖激酶的活化剂，因此可用于治疗，治疗，控制或辅助治疗疾病，其中葡萄糖激酶活性增加是有益的。

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

Applicant: NOVO NORDISK A/S ,  EBDRUP, Søren ,  VEDSØ, Per ,  JACOBSEN, Poul ,  NIELSEN, Flemming, Elmelund ,  CORNELIS DE JONG, Johannes

Inventor： EBDRUP, Søren ,  VEDSØ, Per ,  JACOBSEN, Poul ,  NIELSEN, Flemming, Elmelund ,  CORNELIS DE JONG, Johannes

IPC: C07D401/12

CPC classification number: C07D211/34 ,  C07D211/44 ,  C07D211/66 ,  C07D211/88 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2003105860A1

公开(公告)日：2003-12-24

申请号：PCT/DK2003/000315

申请日：2003-05-14

Applicant: NOVO NORDISK A/S ,  EBDRUP, Søren ,  VEDSØ, Per ,  JACOBSEN, Poul

Inventor： EBDRUP, Søren ,  VEDSØ, Per ,  JACOBSEN, Poul

IPC: A61K31/69

CPC classification number: A61K31/69

Abstract: Use of compounds to inhibit hormone-sensitive lipase, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, method of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitve lipase and may be useful in the treatment and/or prevention of a range of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Abstract translation: 使用化合物抑制激素敏感性脂肪酶，这些化合物作为药物组合物的使用，包含该化合物的药物组合物，使用这些化合物和组合物的治疗方法以及新化合物。 本发明化合物是激素敏感性脂肪酶的抑制剂，并且可用于治疗和/或预防一系列需要激素敏感性脂肪酶活性降低的医学疾病。

公开(公告)号：WO2007125105A3

公开(公告)日：2007-11-08

申请号：PCT/EP2007/054173

申请日：2007-04-27

Applicant: NOVO NORDISK A/S ,  MURRAY, Anthony ,  LAU, Jesper ,  JEPPESEN, Lone ,  VEDSØ, Per ,  POLISETTI, Dharma Rao ,  GADDAM, Bapu Reddy ,  CHRISTEN, Daniel P. ,  SANTHOSH, Kalpathy Chidambareswaran ,  COOPER, Jeremy T. ,  ANDREWS, Robert Carl

Inventor： MURRAY, Anthony ,  LAU, Jesper ,  JEPPESEN, Lone ,  VEDSØ, Per ,  POLISETTI, Dharma Rao ,  GADDAM, Bapu Reddy ,  CHRISTEN, Daniel P. ,  SANTHOSH, Kalpathy Chidambareswaran ,  COOPER, Jeremy T. ,  ANDREWS, Robert Carl

IPC: C07D277/44 ,  A61K31/4168 ,  A61P3/10

Abstract: The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.

公开(公告)号：WO2007006760A1

公开(公告)日：2007-01-18

申请号：PCT/EP2006/064026

申请日：2006-07-07

Applicant: NOVO NORDISK A/S ,  MURRAY, Anthony ,  LAU, Jesper ,  VEDSØ, Per ,  KRISTIANSEN, Marit ,  JEPPESEN, Lone

Inventor： MURRAY, Anthony ,  LAU, Jesper ,  VEDSØ, Per ,  KRISTIANSEN, Marit ,  JEPPESEN, Lone

IPC: C07D277/48 ,  C07D417/12 ,  C07D417/04 ,  C07D417/14 ,  C07D277/54 ,  A61K31/426 ,  A61K31/427 ,  A61P3/10

CPC classification number: C07D277/54 ,  C07D277/48 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. (I)

Abstract translation: 二环烷基脲葡糖激酶活化剂化合物是可用于治疗糖尿病的葡糖激酶抑制剂。 （一世）

公开(公告)号：WO2005066145A1

公开(公告)日：2005-07-21

申请号：PCT/DK2005/000002

申请日：2005-01-06

Applicant: NOVO NORDISK A/S ,  MURRAY, Anthony ,  LAU, Jesper ,  JEPPESEN, Lone ,  VEDSØ, Per ,  ANKERSEN, Michael ,  LUNDBECK, Jane, Marie ,  KRISTIANSEN, Marit ,  VALCARCE-LOPEZ, Maria Carmen ,  POLISETTI, Dharma, Rao ,  SUBRAMANIAN, Govindan ,  ANDREWS, Robert, Carl ,  CHRISTEN, Daniel, P. ,  COOPER, Jeremy, T. ,  SANTHOSH, Kalpathy, Chidambareswaran

Inventor： MURRAY, Anthony ,  LAU, Jesper ,  JEPPESEN, Lone ,  VEDSØ, Per ,  ANKERSEN, Michael ,  LUNDBECK, Jane, Marie ,  KRISTIANSEN, Marit ,  VALCARCE-LOPEZ, Maria Carmen ,  POLISETTI, Dharma, Rao ,  SUBRAMANIAN, Govindan ,  ANDREWS, Robert, Carl ,  CHRISTEN, Daniel, P. ,  COOPER, Jeremy, T. ,  SANTHOSH, Kalpathy, Chidambareswaran

IPC: C07D277/48

CPC classification number: C07D417/12 ,  A61K31/4168 ,  A61K31/427 ,  A61K31/433 ,  C07D213/75 ,  C07D233/88 ,  C07D241/20 ,  C07D261/14 ,  C07D271/08 ,  C07D277/48 ,  C07D277/56 ,  C07D277/60 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

Abstract: This invention relates to compounds that are of formula (I) wherein A is heteroaryl and R 1 and R 2 are both cyclic residues, that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial .

Abstract translation: 本发明涉及式（I）化合物，其中A是杂芳基，R 1和R 2都是环状残基，其是葡糖激酶的活化剂，因此可用于治疗，治疗，对照或 疾病的辅助治疗，其中增加葡萄糖激酶活性是有益的。

公开(公告)号：WO2004111006A1

公开(公告)日：2004-12-23

申请号：PCT/DK2004/000401

申请日：2004-06-10

Applicant: NOVO NORDISK A/S ,  VEDSØ, Per ,  EBDRUP, Søren ,  JACOBSEN, Poul

Inventor： VEDSØ, Per ,  EBDRUP, Søren ,  JACOBSEN, Poul

IPC: C07D213/68

CPC classification number: C07D213/30 ,  C07D213/68 ,  C07D233/84

Abstract: Novel para-substituted phenyl 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.

Abstract translation: 新型对位取代的苯基氨基甲酸酯，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。

公开(公告)号：WO2012083954A1

公开(公告)日：2012-06-28

申请号：PCT/DK2011/000155

申请日：2011-12-22

Applicant: LEO Pharma A/S ,  GRUE-SØRENSEN, Gunnar ,  LIANG, Xifu ,  HÖGBERG, Thomas ,  MÅNSSON, Kristoffer ,  VEDSØ, Per

Inventor： GRUE-SØRENSEN, Gunnar ,  LIANG, Xifu ,  HÖGBERG, Thomas ,  MÅNSSON, Kristoffer ,  VEDSØ, Per

IPC: C07C69/74 ,  C07C69/75 ,  C07C69/753 ,  C07C229/56 ,  C07C255/46 ,  A61K31/215 ,  A61K31/245 ,  A61K31/277 ,  A61P35/00 ,  A61K31/216

CPC classification number: C07C69/74 ,  A61K31/215 ,  A61K31/235 ,  A61K31/245 ,  A61K31/277 ,  A61K45/06 ,  C07C69/013 ,  C07C69/75 ,  C07C69/753 ,  C07C69/76 ,  C07C69/78 ,  C07C69/92 ,  C07C229/56 ,  C07C229/58 ,  C07C229/64 ,  C07C233/54 ,  C07C255/46 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/86

Abstract: The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)- cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Abstract translation: 本发明涉及通式I（I）的化合物，其中R是其中R是被R3取代的芳基; 或R 3为任选被R 4取代的（C 3 -C 13） - 环烷基，（C 3 -C 13） - 环烯基或（C 7 -C 13） - 环炔基; 其药学上可接受的盐，水合物或溶剂合物，用于在治疗中单独或与一种或多种其它药学活性化合物组合使用，用于预防，治疗或改善响应于刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。