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1. 发明授权

US09758560B2 GLP-1 derivatives 有权
公开(公告)号：US09758560B2
公开(公告)日：2017-09-12
申请号：US14343152
申请日：2012-09-06
申请人： Jesper Lau , Paw Bloch , Patrick William Garibay
发明人： Jesper Lau , Paw Bloch , Patrick William Garibay
IPC分类号： C07K14/605 , A61K38/26 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.

2. 发明授权

US09732137B2 Semi-recombinant preparation of GLP-1 analogues 有权
公开(公告)号：US09732137B2
公开(公告)日：2017-08-15
申请号：US12810934
申请日：2008-12-22
申请人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
发明人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
IPC分类号： C07K14/605 , C07K1/107 , C07K1/02 , C07K1/06 , C07K1/36 , C07K1/00
CPC分类号： C07K14/605 , C07K1/006 , C07K1/02 , C07K1/061 , C07K1/107 , C07K1/1077
摘要： A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.

3. 发明申请

US20140303083A1 GLP-1 Derivatives 有权
标题翻译： GLP-1衍生物
公开(公告)号：US20140303083A1
公开(公告)日：2014-10-09
申请号：US14343152
申请日：2012-09-06
申请人： Jesper Lau , Paw Bloch , Jacob Kofoed , Patrick William Garibay
发明人： Jesper Lau , Paw Bloch , Jacob Kofoed , Patrick William Garibay
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.
摘要翻译：本发明涉及GLP-1肽的衍生物，该肽与GLP-1（7-37）（SEQ）相比具有两个Lys残基，即第一和第二Lys残基，最多八个氨基酸变化 SEQ ID NO：3），该衍生物分别包含通过接头分别连接到所述第一和第二Lys残基的ε氨基的两个伸长部分，其中伸长部分选自Chem。 15：HOOC-（CH 2）x-CO- *，和Chem。 16：HOOC-C6H4-O-（CH2）y-CO- *，其中x是10-16的整数，y是8-12的整数; 并且连接体包含第一连接体元件* -NH-CH（CH 2 OH）-CO- *。优选的接头是g Glu-Ser-Ser-Gly-Ser-Ser-Gly（SEQ ID NO：2）。本发明的衍生物具有非常好的效力，并且与GLP-1受体具有非常好的结合。本发明还涉及衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。

4. 发明申请

US20120295847A1 Acylated GLP-1 Compounds 有权
标题翻译：酰化GLP-1化合物
公开(公告)号：US20120295847A1
公开(公告)日：2012-11-22
申请号：US13412283
申请日：2012-03-05
申请人： Jesper Lau , Florencio Zaragoza Dörwald , Henrik Stephensen , Paw Bloch , Thomas Kruse Hansen , Kjeld Madsen
发明人： Jesper Lau , Florencio Zaragoza Dörwald , Henrik Stephensen , Paw Bloch , Thomas Kruse Hansen , Kjeld Madsen
IPC分类号： A61K38/26 , A61P3/10 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00
摘要： Protracted GLP-1 compounds and therapeutic uses thereof.
摘要翻译：延长的GLP-1化合物及其治疗用途。

5. 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。

6. 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。

7. 发明申请

US20080119455A1 Aryl carbonyl derivatives as therapeutic agents 有权
公开(公告)号：US20080119455A1
公开(公告)日：2008-05-22
申请号：US11982248
申请日：2007-10-31
申请人： Dharma Polisetti , Janos Kodra , Jesper Lau , Paw Bloch , Maria Valcarce-Lopez , Niels Blume , Mustafa Guzel , Kalpathy Santhosh , Adnan Mjalli , Robert Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
发明人： Dharma Polisetti , Janos Kodra , Jesper Lau , Paw Bloch , Maria Valcarce-Lopez , Niels Blume , Mustafa Guzel , Kalpathy Santhosh , Adnan Mjalli , Robert Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
IPC分类号： A61K31/55 , A61K31/454 , A61K31/427 , C07D417/02
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.

8. 发明申请

US20070203058A1 Novel Glp-1 Derivatives 审中-公开
标题翻译：新型Glp-1衍生物
公开(公告)号：US20070203058A1
公开(公告)日：2007-08-30
申请号：US10572348
申请日：2004-09-17
申请人： Jesper Lau , Thomas Hansen , Kjeld Madsen , Paw Bloch , Florencio Dorwald , Nils Johansen
发明人： Jesper Lau , Thomas Hansen , Kjeld Madsen , Paw Bloch , Florencio Dorwald , Nils Johansen
IPC分类号： A61K38/26
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/54 , A61K47/542 , A61K47/60 , C07K14/001
摘要： Novel polypeptide derivatives having protracted profile of action. The present invention relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer. The present invention also relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer that separates the polypeptide and the albumin binding residue with a chemical moiety comprising at least 5 non-hydrogen atoms where 30-50% of these atoms are either N or O. In one embodiment of this invention the spacer is defined as —(CH2)lD[(CH2)nE]m(CH2)pQq-, wherein l, m and n independently are 1-20 and p is 0-10, Q is -Z-(CH2)lD[(CH2)nG]m(CH2)p—, q is an integer in the range from 0 to 5, each D, E and G independently are selected from —O—, NR3—, —N(COR4)—, —PR5(O)—, and —P(OR6)(O)—, wherein R3, R4, R5, and R6 independently represent hydrogen or C1-6-alky, Z is selected from —C(O)NH—, —C(O)NHCH2—, —OC(O)NH—, —C(O)NHCH2CH2—, —C(O)CH2—, —C(O)CH═CH—, —(CH2)s—, —C(O)—, —C(O)O— or —NHC(O)—, wherein s is 0 or 1.
摘要翻译：新型多肽衍生物具有延长的作用特征。本发明涉及包含通过亲水间隔物与白蛋白结合残基连接的治疗性多肽的化合物。本发明还涉及一种化合物，其包含通过亲水间隔物与白蛋白结合残基连接的治疗性多肽，其将多肽和白蛋白结合残基与包含至少5个非氢原子的化学部分分开，其中30-50％这些原子是N或O.在本发明的一个实施方案中，间隔基被定义为 - （CH 2）2 D [（CH 2）2 （CH 2）n） - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 其中l，m和n独立地是1-20，p是0-10，Q是-Z-（CH 2）2 D [（CH 2）（CH 2） - - - - - - - - - - - - - - - - 范围为0至5，每个D，E和G各自独立地选自-O-，NR 3 - ， - N（COR 4 - ） - ， - PR

9. 发明申请

US20060183783A1 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：US20060183783A1
公开(公告)日：2006-08-17
申请号：US11365534
申请日：2006-03-01
申请人： Dharma Polisetti , Janos Kodra , Jesper Lau , Paw Bloch , Maria Lopez , Niels Blume , Mustafa Guzel , Kalpathy Santhosh , Adnan Mjalli , Robert Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
发明人： Dharma Polisetti , Janos Kodra , Jesper Lau , Paw Bloch , Maria Lopez , Niels Blume , Mustafa Guzel , Kalpathy Santhosh , Adnan Mjalli , Robert Andrews , Govindan Subramanian , Michael Ankersen , Per Vedso , Anthony Murray , Lone Jeppesen
IPC分类号： A61K31/426 , C07D277/18
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 derivativeswhich 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：本发明涉及芳基羰基衍生物，其是可用于治疗，治疗，控制或辅助治疗疾病的葡糖激酶的活化剂，其中增加葡糖激酶活性是有益的。

10. 发明申请

US20060182714A1 Synthesis and application of new structural well defined branched polymers as conjugating agents for peptides 审中-公开
标题翻译：新结构明确的支化聚合物作为肽缀合剂的合成和应用
公开(公告)号：US20060182714A1
公开(公告)日：2006-08-17
申请号：US11344767
申请日：2006-02-01
申请人： Carsten Behrens , Florencio Dorwald , Mikael Kofod-Hansen , Jesper Lau , Janos Kodra , Thomas Hansen , Paw Bloch
发明人： Carsten Behrens , Florencio Dorwald , Mikael Kofod-Hansen , Jesper Lau , Janos Kodra , Thomas Hansen , Paw Bloch
IPC分类号： A61K39/395 , A61K38/28 , A61K38/22 , A61K38/20 , C07K14/62 , C07K14/54 , C07K16/46
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。

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