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1. 发明授权

US07897628B2 Aryl carbonyl derivatives as therapeutic agents 有权
公开(公告)号：US07897628B2
公开(公告)日：2011-03-01
申请号：US11982248
申请日：2007-10-31
申请人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M.M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
发明人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M.M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
IPC分类号： A61K31/426 , C07D277/46
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , 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.

2. 发明申请

US20110301158A1 ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂的ARYL CARBONYL衍生物
公开(公告)号：US20110301158A1
公开(公告)日：2011-12-08
申请号：US13209565
申请日：2011-08-15
申请人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce-Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M.M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
发明人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce-Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M.M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
IPC分类号： A61K31/5355 , A61P3/10 , A61K31/497 , A61K31/426 , A61K31/433
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , 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。

3. 发明授权

US08063081B2 Aryl carbonyl derivatives as therapeutic agents 有权
标题翻译：芳基羰基衍生物作为治疗剂
公开(公告)号：US08063081B2
公开(公告)日：2011-11-22
申请号：US11981997
申请日：2007-10-31
申请人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M. M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
发明人： Dharma Rao Polisetti , Janos Tibor Kodra , Jesper Lau , Paw Bloch , Maria Carmen Valcarce Lopez , Niels Blume , Mustafa Guzel , Kalpathy Chidambareswaran Santhosh , Adnan M. M. Mjalli , Robert Carl Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
IPC分类号： A61K31/425 , A61K31/44 , C07D277/04 , C07D211/72
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , 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。

4. 发明授权

US07541373B2 Aryl carbonyl derivatives as therapeutic agents 有权
标题翻译：芳基羰基衍生物作为治疗剂
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。

5. 发明授权

US07384967B2 Aryl carbonyl derivatives as therapeutic agents 有权
标题翻译：芳基羰基衍生物作为治疗剂
公开(公告)号：US07384967B2
公开(公告)日：2008-06-10
申请号：US10679887
申请日：2003-10-06
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
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
IPC分类号： A61K31/425 , A61K31/44 , C07D277/04 , C07D211/72
CPC分类号： C07D277/38 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/55 , A61K45/06 , C07D213/75 , C07D277/46 , 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。

6. 发明授权

US06881746B2 Glucagon antagonists/inverse agonists 失效
标题翻译：胰高血糖素拮抗剂/反向激动剂
公开(公告)号：US06881746B2
公开(公告)日：2005-04-19
申请号：US10448529
申请日：2003-05-30
申请人： Jesper Lau , Inge Thoger Christensen , Peter Madsen , Paw Bloch , Carsten Behrens , Janos Tibor Kodra , Poul Enrico Nielsen
发明人： Jesper Lau , Inge Thoger Christensen , Peter Madsen , Paw Bloch , Carsten Behrens , Janos Tibor Kodra , Poul Enrico Nielsen
IPC分类号： A61K31/195 , A61K31/198 , A61K31/41 , A61K31/4439 , A61K45/06 , A61K31/425 , A61P3/00 , C07D277/04
CPC分类号： A61K45/06 , A61K31/195 , A61K31/198 , A61K31/41 , A61K31/4439 , A61K2300/00
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.
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。

7. 发明申请

US20090240028A1 Synthesis and Application of New Structural Well Defined Branched Polymers as Conjugating Agents for Peptides 审中-公开
标题翻译：新型结构定义的支化聚合物作为多肽共轭剂的合成与应用
公开(公告)号：US20090240028A1
公开(公告)日：2009-09-24
申请号：US12276885
申请日：2008-11-24
申请人： Carsten Behrens , Florencio Zaragoza Dorwald , Mikael Kofod-Hansen , Jesper Lau , Janos Tibor Kodra , Thomas Kruse Hansen , Paw Bloch
发明人： Carsten Behrens , Florencio Zaragoza Dorwald , Mikael Kofod-Hansen , Jesper Lau , Janos Tibor Kodra , Thomas Kruse Hansen , Paw Bloch
IPC分类号： C07K14/00
CPC分类号： C12P21/005 , A61K47/549 , A61K47/60 , C12N9/6437
摘要： The invention provides synthesis and application of new structural well defined branched polymers as protraction agents for peptide and protein.
摘要翻译：本发明提供新的结构明确的支化聚合物作为肽和蛋白质的助剂的合成和应用。

8. 发明申请

US20090036353A1 Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers 审中-公开
标题翻译：与结构定义良好的支化聚合物共轭的胰岛素衍生物
公开(公告)号：US20090036353A1
公开(公告)日：2009-02-05
申请号：US11814184
申请日：2006-01-26
申请人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
发明人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/641 , A61K47/6949
摘要： Insulin conjugated with structurally well defined, bifurcated and trifurcated polymers can be use by pulmonary delivery for systemic absorption through the lungs to reduce or eliminate the need for administering other insulins by injection.
摘要翻译：与结构良好定义的分叉和三化聚合物结合的胰岛素可以通过肺部递送用于通过肺的全身吸收，以减少或消除通过注射施用其它胰岛素的需要。

9. 发明授权

US09708383B2 Double-acylated GLP-1 derivatives 有权
公开(公告)号：US09708383B2
公开(公告)日：2017-07-18
申请号：US13882947
申请日：2011-11-09
申请人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
发明人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
IPC分类号： A61K38/00 , C07K14/605 , A61K47/48
CPC分类号： C07K14/605 , A61K47/542
摘要： The invention relates to a derivative of a GLP-1 analog, which analog 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: HOOC—(CH2)x—CO—* Chem. 1: HOOC—C6H4—O—(CH2)y—CO—* Chem. 2: R2—C6H4—(CH2)z—CO—*, Chem. 3: 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 R2 is a group having a molar mass not higher than 150 Da; and the linker comprises *—NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—*. Chem. 4: 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.

10. 发明申请

US20130288960A1 Double-Acylated GLP-1 Derivatives 有权
标题翻译：双酰化GLP-1衍生物
公开(公告)号：US20130288960A1
公开(公告)日：2013-10-31
申请号：US13882947
申请日：2011-11-09
申请人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
发明人： Alice Ravn Madsen , Birgit Wieczorek , Jacob Kofoed , Jesper Lau , Jane Spetzler , Janos Tibor Kodra , Lars Linderoth , Patrick William Garibay , Per Sauerberg , Thomas Kruse
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 Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH2)x—CO—* Chem. 2: HOOC—C6H4-0-(CH2)y—CO—* Chem. 3: R2—C6H4—(CH2)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 R2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *—NH—(CH2)2-(0-(CH2)2)k-0-(CH2)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：化学式：HOOC-（CH2）x-CO- * 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。

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