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1. 发明申请

WO2005105726A1 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型化合物，其制备和使用
公开(公告)号：WO2005105726A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/052014
申请日：2005-05-03
申请人： NOVO NORDISK A/S , HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid , PIHERA, Pavel , EBDRUP, Søren
发明人： HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid , PIHERA, Pavel , EBDRUP, Søren
IPC分类号： C07C59/70
CPC分类号： C07C323/20 , C07C2602/08 , C07D207/333 , C07D213/30 , C07D213/70
摘要： Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hypertriglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
摘要翻译：通式（I）的新型化合物，其中变量如权利要求1所定义，这些化合物用作药物组合物，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARδ亚型，即1型糖尿病，2型糖尿病，血脂异常，综合征X（包括代谢综合征即葡萄糖耐量异常，胰岛素抵抗，高甘油三酯血症和/或肥胖），心血管疾病（包括动脉粥样硬化）和高胆固醇血症。

2. 发明申请

WO2007071766A2 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型化合物，其制备和使用
公开(公告)号：WO2007071766A2
公开(公告)日：2007-06-28
申请号：PCT/EP2006/070096
申请日：2006-12-21
申请人： NOVO NORDISK A/S , SAUERBERG, Per , PIHERA, Pavel , POLIVKA, Zdenék , HAVRANEK, Miroslav , PETTERSSON, Ingrid , MOGENSEN, John, Patrick
发明人： SAUERBERG, Per , PIHERA, Pavel , POLIVKA, Zdenék , HAVRANEK, Miroslav , PETTERSSON, Ingrid , MOGENSEN, John, Patrick
IPC分类号： C07C323/16 , A61K31/44 , A61P3/10 , C07D213/30 , C07D211/46 , C07D333/54 , C07D333/16 , C07D231/12 , C07D307/79 , C07C59/68 , C07D295/08
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as phar- maceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物是PPARd的活化剂，应用于治疗由其介导的病症。

3. 发明申请

WO2005105725A1 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新化合物，他们的准备和使用
公开(公告)号：WO2005105725A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/052010
申请日：2005-05-03
申请人： NOVO NORDISK A/S , HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid
发明人： HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid
IPC分类号： C07C59/70
CPC分类号： C07C323/20 , C07D213/30 , C07D295/092 , C07D333/16
摘要： Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hypertriglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
摘要翻译：其中变量如权利要求1中所定义的通式（I）的新化合物，这些化合物作为药物组合物的用途，包含所述化合物的药物组合物和使用这些化合物的治疗方法和组合物。本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARδ亚型，即1型糖尿病，2型糖尿病，血脂障碍，X综合征（包括代谢综合征，即葡萄糖耐量受损，胰岛素抵抗，高甘油三酯血症和/或肥胖），心血管疾病（包括动脉粥样硬化）和高胆固醇血症。

4. 发明申请

WO2005105735A1 PHENOXYACETIC ACID DERIVATIVES AS PPAR AGONISTS 审中-公开
标题翻译：作为PPAR激动剂的苯氧基酸衍生物
公开(公告)号：WO2005105735A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/052012
申请日：2005-05-03
申请人： NOVO NORDISK A/S , POLIVKA, Zdenék , SINDELAR, Karel , SAUERBERG, Per , PETTERSSON, Ingrid
发明人： POLIVKA, Zdenék , SINDELAR, Karel , SAUERBERG, Per , PETTERSSON, Ingrid
IPC分类号： C07C323/20
CPC分类号： C07D333/18 , C07C323/20 , C07C323/29 , C07C323/60 , C07D207/27 , C07D207/333 , C07D213/30 , C07D213/32 , C07D233/54 , C07D295/096 , C07D295/185 , C07D307/38 , C07D333/20
摘要： Novel compounds of the general formula (I), the use of these compounds as phar- maceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ suptype.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARdelta suptype。

5. 发明申请

WO2012080471A1 SOLID COMPOSITIONS COMPRISING A GLP-1 AGONIST AND A SALT OF N-(8-(2-HYDROXYBENZOYL)AMINO)CAPRYLIC ACID 审中-公开
标题翻译：包含GLP-1激动剂和N-（8-（2-羟基苯甲酰基）氨基酸的盐）的固体组合物
公开(公告)号：WO2012080471A1
公开(公告)日：2012-06-21
申请号：PCT/EP2011/073060
申请日：2011-12-16
申请人： NOVO NORDISK A/S , SAUERBERG, Per , BJERREGAARD, Simon , NIELSEN, Flemming Seier
发明人： SAUERBERG, Per , BJERREGAARD, Simon , NIELSEN, Flemming Seier
IPC分类号： A61K9/20 , A61K38/26 , A61P3/04 , A61P3/10
CPC分类号： A61K38/26 , A61K9/0053 , A61K9/2013 , A61K9/2077 , A61K45/06 , A61K47/18 , A61K31/195 , A61K2300/00
摘要： The present invention relates to solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.
摘要翻译：本发明涉及包含GLP-1激动剂和N-（8-（2-羟基苯甲酰基）氨基）辛酸的盐的固体组合物及其在药物中的用途。

6. 发明申请

WO2011080103A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双酚A-GLP-1衍生物
公开(公告)号：WO2011080103A1
公开(公告)日：2011-07-07
申请号：PCT/EP2010/069932
申请日：2010-12-16
申请人： NOVO NORDISK A/S , GARIBAY, Patrick, William , SPETZLER, Jane , KODRA, János, Tibor , LINDEROTH, Lars , LAU, Jesper , SAUERBERG, Per
发明人： GARIBAY, Patrick, William , SPETZLER, Jane , KODRA, János, Tibor , LINDEROTH, Lars , LAU, Jesper , SAUERBERG, Per
IPC分类号： C07K14/605 , A61K47/48
CPC分类号： C07K14/65 , A61K38/00 , A61K47/542 , A61K47/60 , C07K14/605 , G01N2333/605
摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1 (7-37), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37), wherein the first K residue is designated K 37 , and the second K residue is designated K 26 , which derivative comprises two albumin binding moieties attached to K 26 and K 37 , respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1 : HOOC-(CH 2 ) X -CO-* Chem. 2: HOOC-C 6 H 4 -O-(CH 2 ) y -CO-* Chem. 3: R 1 -C 6 H 4 -(CH 2 ) Z -CO-* Chem. 4: HOOC-C 4 SH 2 -(CH 2 ) W -CO-* in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, R 1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH 2 ) 2 -(O-(CH 2 ) 2 ) k -O-(CH 2 ) n -CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第37位的位置处的第一个K残基，相对于GLP-1（7-37）的位置26的位置和与GLP-1（7-37）相比最多10个氨基酸修饰，其中第一个K残基指定为K37，第二个K残基是命名为K26，该衍生物分别包含与K26和K37连接的两个白蛋白结合部分，其中白蛋白结合部分包含选自下列的伸长部分： 1：HOOC-（CH2）X-CO- * Chem。 2：HOOC-C6H4-O-（CH2）y-CO- * 3：R1-C6H4-（CH2）Z-CO- * Chem。 4：HOOC-C4SH2-（CH2）W-CO- *，其中x是6-18的整数，y是3-17的整数，z是1〜 5，R1是摩尔质量不高于150Da的基团，w是6-18的整数; 条件是当伸长部分是Chem。如图1所示，白蛋白结合部分还包含式Chem的接头。 5：* -NH-（CH2）2-（O-（CH2）2）kO-（CH2）n-CO- *，其中k是1-5的整数，n是范围1-5; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。该衍生物适合口服给药。

7. 发明申请

WO2012062803A1 DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
标题翻译：双取代的GLP-1衍生物
公开(公告)号：WO2012062803A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069738
申请日：2011-11-09
申请人： NOVO NORDISK A/S , MADSEN, Alice Ravn , WIECZOREK, Birgit , KOFOED, Jacob , LAU, Jesper , SPETZLER, Jane , KODRA, János Tibor , LINDEROTH, Lars , GARIBAY, Patrick William , SAUERBERG, Per , KRUSE, Thomas
发明人： MADSEN, Alice Ravn , WIECZOREK, Birgit , KOFOED, Jacob , LAU, Jesper , SPETZLER, Jane , KODRA, János Tibor , LINDEROTH, Lars , GARIBAY, Patrick William , SAUERBERG, Per , KRUSE, Thomas
IPC分类号： A61K47/48 , C07K14/605 , A61P3/10
CPC分类号： C07K14/605 , A61K47/542
摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1 ), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem. : HOOC-(CH 2 ) x -CO-* Chem. 2: HOOC-C 6 H 4 -0-(CH 2 ) y -CO-* Chem. 3: R 2 -C 6 H 4 -(CH 2 ) z -CO-*, in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, and R 2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *-NH-(CH 2 ) 2 -(0-(CH 2 ) 2 ) k -0-(CH 2 ) n -CO-*. wherein k is an integer in the range of 1 -5, and n is an integer in the range of 1 -5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
摘要翻译：本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自Chem。 1，Chem。 2和Chem。 3：Chem。：HOOC-（CH2）x-CO- * Chem。 2：HOOC-C6H4-0-（CH2）y-CO- * Chem。 3：R2-C6H4-（CH2）z-CO- *，其中x是6-18的整数，y是3-17的整数，z是1的整数 -5和R2是摩尔质量不高于150Da的基团; 连接体包括Chem。 4：* -NH-（CH 2）2 - （O-（CH 2）2）k -O-（CH 2）n -CO- *。其中k是1-5的整数，n是1-5的整数; 或其药学上可接受的盐，酰胺或酯。本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。该衍生物适用于口服给药。

8. 发明申请

WO2007101864A2 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型化合物，其制备和使用
公开(公告)号：WO2007101864A2
公开(公告)日：2007-09-13
申请号：PCT/EP2007/052130
申请日：2007-03-07
申请人： NOVO NORDISK A/S , SAUERBERG, Per
发明人： SAUERBERG, Per
IPC分类号： C07C59/70 , C07D295/096 , A61K31/192 , A61K31/4453
CPC分类号： C07C59/70 , C07D295/096
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物是PPARd的活化剂，应用于治疗由其介导的病症。

9. 发明申请

WO2016083499A1 GLP-1 DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： GLP-1衍生物及其用途
公开(公告)号：WO2016083499A1
公开(公告)日：2016-06-02
申请号：PCT/EP2015/077757
申请日：2015-11-26
申请人： NOVO NORDISK A/S
发明人： SAUERBERG, Per , KOFOED, Jacob
IPC分类号： A61K47/48 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K47/542 , A61K47/59
摘要： The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1 st and a 2 nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1 st or 2 nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
摘要翻译：本发明涉及通式I的GLP-1类似物的衍生物，该衍生物包含与GLP-1类似物的第34,35,36,37或38位的Lys残基连接的侧链，该侧链包含分支连接体，选自C18二酸，C20二酸和磺酸C16的第一和第二分选机，以及至少一个结合乙二醇单元的连接子-1。接头元件-1可以结合在可选的预链接器中，和/或在第一或第二后连接器中。本发明还涉及新型GLP-1类似物，新型侧链中间产物及其制备和用于制备生物活性肽和蛋白质的衍生物，以及类似物和衍生物的药物组合物和医学用途。衍生物具有非常长的半衰期，同时保持令人满意的效力，这使得它们潜在地适合于每月一次的管理。

10. 发明申请

WO2015022400A1 GLP-1 DERIVATIVES, AND USES THEREOF 审中-公开
标题翻译： GLP-1衍生物及其用途
公开(公告)号：WO2015022400A1
公开(公告)日：2015-02-19
申请号：PCT/EP2014/067413
申请日：2014-08-14
申请人： NOVO NORDISK A/S
发明人： SAUERBERG, Per , KOFOED, Jacob
IPC分类号： A61K47/48 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K47/54 , A61K47/58 , A61K47/60
摘要： The present invention relates to tri-acylated GLP-1 derivatives, acylated at positions corresponding to positions (18, 22, 30), (18, 26, 37), (18, 27, 37), (26, 30, 37), or (27, 30, 37) of the native human glucagon-like peptide 1 (GLP-1 (7-37) (SEQ ID NO: 1); or pharmaceutically acceptable salts, amides, or esters thereof. The acylated side chains comprise a protracting moiety selected from Chem. 1 : HOOC-(CH 2 ) 16 -CO-*, Chem. 1a: HOOC-(CH 2 ) 18 -CO-*, and Chem. 2: HO 3 S-(CH 2 ) 15 -CO-*, and the protracting moieties are connected, via a linker, to a Lys residue of the GLP-1 peptide. The GLP-1 peptide has a maximum of seven amino acid changes as compared to GLP-1 (7-37) (SEQ ID NO: 1). The invention also relates to intermediate products in the form of novel GLP-1 analogues, as well as to pharmaceutical compositions and uses of the derivatives and analogues, in particular for the treatment of type 2 diabetes. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
摘要翻译：本发明涉及三酰化GLP-1衍生物，其在对应于位置（18,22,30），（18,26,37），（18,27,37），（26,30,37），，或天然人胰高血糖素样肽1（GLP-1（7-37）（SEQ ID NO：1））的（27,30,37）或其药学上可接受的盐，酰胺或酯。酰化侧链包括选自化学式1：HOOC-（CH 2）16 -CO- *，化学式1a：HOOC-（CH 2）18 -CO- *和化学式2：HO 3 S-（CH 2）15 -CO- *，并且延伸部分通过接头连接到GLP-1肽的Lys残基。与GLP-1（7-37）（SEQ ID NO：1）相比，GLP-1肽具有最多7个氨基酸变化本发明还涉及新型GLP-1类似物形式的中间产物，以及衍生物和类似物的药物组合物和用途，特别是用于治疗2型糖尿病。衍生物具有很长的半生，同时保持令人满意的效力 h使他们潜在地适合每月一次的管理。

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