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公开(公告)号：US5635518A
公开(公告)日：1997-06-03
申请号：US263634
申请日：1994-06-22
IPC分类号： A61K31/445 , A61P25/00 , C07D211/60 , C07D211/78
CPC分类号： C07D211/78 , C07D211/60
摘要： The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
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公开(公告)号：US5604242A
公开(公告)日：1997-02-18
申请号：US263641
申请日：1994-06-22
IPC分类号： A61K31/445 , A61P25/00 , C07D211/60 , C07D211/78 , C07D211/68 , C07D211/80
CPC分类号： C07D211/78 , C07D211/60
摘要： The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
摘要翻译： 本发明涉及治疗活性的氮杂杂环化合物，其制备方法和包含该化合物的药物组合物。 新化合物可用于治疗与GABA摄取相关的中枢神经系统疾病。
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公开(公告)号：US5608069A
公开(公告)日：1997-03-04
申请号：US263635
申请日：1994-06-22
申请人： Hans Petersen , Knud E. Andersen , Per O. S.o slashed.rensen , Jesper Lau , Henning B. Petersen , Behrend F. Lundt
发明人： Hans Petersen , Knud E. Andersen , Per O. S.o slashed.rensen , Jesper Lau , Henning B. Petersen , Behrend F. Lundt
IPC分类号： A61K31/445 , A61P25/00 , C07D211/60 , C07D211/78 , C07D211/68 , C07D211/80
CPC分类号： C07D211/78 , C07D211/60
摘要： The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
摘要翻译： 本发明涉及治疗活性的氮杂杂环化合物，其制备方法和包含该化合物的药物组合物。 新化合物可用于治疗与GABA摄取相关的中枢神经系统疾病。
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公开(公告)号：US5348965A
公开(公告)日：1994-09-20
申请号：US882788
申请日：1992-05-14
申请人： Knud E. Andersen , Lars J. S. Knutsen , Per O. Sorensen , Behrend F. Lundt , Jesper Lau , Hans Petersen
发明人： Knud E. Andersen , Lars J. S. Knutsen , Per O. Sorensen , Behrend F. Lundt , Jesper Lau , Hans Petersen
IPC分类号： A61K31/395 , A61K31/4427 , A61K31/445 , A61K31/455 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/554 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07D207/08 , C07D207/16 , C07D211/36 , C07D211/60 , C07D279/22 , C07D281/02 , C07D281/16 , C07D281/18 , C07D335/10 , C07D337/14 , C07D337/16 , C07D401/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D211/14 , C07D211/70
CPC分类号： C07D401/12 , C07D211/60 , C07D403/12 , C07D413/10 , C07D417/12
摘要： The invention relates to therapeutically active azaheterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
摘要翻译： 本发明涉及治疗活性的氮杂环化合物和包含该化合物的药物组合物。 新化合物可用于治疗与GABA摄取相关的中枢神经系统疾病。
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公开(公告)号：US5639766A
公开(公告)日：1997-06-17
申请号：US263863
申请日：1994-06-22
申请人： Hans Petersen , Knud Erik Andersen , Per Olaf S.o slashed.rensen , Jesper Lau , Behrend Friedrich Lundt
发明人： Hans Petersen , Knud Erik Andersen , Per Olaf S.o slashed.rensen , Jesper Lau , Behrend Friedrich Lundt
IPC分类号： A61K31/445 , A61P25/00 , C07D211/60 , C07D211/78
CPC分类号： C07D211/78 , C07D211/60
摘要： The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
摘要翻译： 本发明涉及治疗活性的氮杂杂环化合物，其制备方法和包含该化合物的药物组合物。 新化合物可用于治疗与GABA摄取相关的中枢神经系统疾病。
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公开(公告)号：US07541373B2
公开(公告)日：2009-06-02
申请号：US11365534
申请日：2006-03-01
申请人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M. M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen , Jesper Lau
发明人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M. M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen , Jesper Lau
IPC分类号： A61K31/426 , C07D277/38
CPC分类号： C07D213/75 , C07D277/48 , C07D277/52 , C07D277/54 , C07D277/56 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D473/38
摘要： This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
摘要翻译： 本发明涉及作为葡萄糖激酶活化剂的芳基羰基衍生物，其可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。
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7.发明申请Condensed Thiophene Derivatives and Their Use as Cyclic Glp-1 Agonists 审中-公开缩合噻吩衍生物及其作为循环Glp-1激动剂的用途公开(公告)号：US20080275066A1
公开(公告)日：2008-11-06
申请号：US11630007
申请日：2005-06-21
申请人： Sanne Moller Knudsen , Ingrid Pettersson , Jesper Lau , Carsten Behrens , Anders Klarskov Petersen , Jesper Lau , Patrick William Garibay
发明人： Sanne Moller Knudsen , Ingrid Pettersson , Jesper Lau , Carsten Behrens , Anders Klarskov Petersen , Jesper Lau , Patrick William Garibay
IPC分类号： A61K31/519 , C07D333/62 , A61K31/381 , A61K31/4365 , C07D495/04
CPC分类号： C07D495/04 , C07D333/72 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/14
摘要： The invention provides compounds of formula (I) for use as GLP-1 receptor agonists.
摘要翻译： 本发明提供用作GLP-1受体激动剂的式（I）化合物。
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公开(公告)号：US08772232B2
公开(公告)日：2014-07-08
申请号：US13212439
申请日：2011-08-18
申请人： Jesper Lau , Thomas Kruse Hansen
发明人： Jesper Lau , Thomas Kruse Hansen
IPC分类号： A61K38/26
CPC分类号： C07K14/57563 , A61K38/00
摘要： Novel protracted exendin-4 compounds and therapeutic uses thereof.
摘要翻译： 新型延长的毒蜥外泌肽-4化合物及其治疗用途。
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公开(公告)号：US20130338068A1
公开(公告)日：2013-12-19
申请号：US13883946
申请日：2011-11-09
IPC分类号： C07K14/605
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 HOOC—(CH2)x—CO-*, and Chem. 1: HOOC—C6H4-0-(CH2)y—CO-*, Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *-NH—(CH2)q—CH[(CH2)w—NH2]—CO-*, Chem. 3: wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; 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 potent, protracted, and 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HOOC-（CH 2）x -CO- *和Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，Chem。 2：其中x是6-18的整数，y是3-17的整数; 并且连接体包含* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO - *， 3：其中q是0-5的整数，w是0-5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。 衍生物有效，延长，适合口服。
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