RU2542362C2 - Аналоги оксинтомодулина - Google Patents

Аналоги оксинтомодулина Download PDF

Info

Publication number: RU2542362C2
Authority: RU; Russia
Prior art keywords: seq; peptide; residue; amino; acid
Prior art date: 2009-02-19

Application number

RU2011134596/04A

Other languages

English (en)

Russian (ru)

Other versions

RU2011134596A (ru

Inventor

Паул И. КАРРИНГТОН

Джордж Дж. ИРМАНН

Доналд Дж. МАРШ

Джозеф М. МЕТЦГЕР

Алессандро ПОКАИ

РОЙ Ранабир СИНХА

Элизабетта БИАНЧИ

Паоло ИНГАЛЛИНЕЛЛА

Антонэлло ПЕССИ

Алессиа САНТОПРЕТЕ

Елена КАПИТО

Ричард ДИМАРЧИ

Брайн УАРД

Original Assignee

Мерк Шарп & Доум, Корп.

Иституто Ди Рикерке Ди Биологиа Молеколаре П. Ангелетти С.П.А.

Индиана Юниверсити Ресёрч Энд Технолоджи Корпорэйшн

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2009-02-19

Filing date

2009-12-18

Publication date

2015-02-20

2009-12-18 Application filed by Мерк Шарп & Доум, Корп., Иституто Ди Рикерке Ди Биологиа Молеколаре П. Ангелетти С.П.А., Индиана Юниверсити Ресёрч Энд Технолоджи Корпорэйшн filed Critical Мерк Шарп & Доум, Корп.

2013-03-27 Publication of RU2011134596A publication Critical patent/RU2011134596A/ru

2015-02-20 Application granted granted Critical

2015-02-20 Publication of RU2542362C2 publication Critical patent/RU2542362C2/ru

Links

108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 470
101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims abstract description 26
239000003814 drug Substances 0.000 claims abstract description 18
238000003776 cleavage reaction Methods 0.000 claims abstract description 16
208000030159 metabolic disease Diseases 0.000 claims abstract description 16
230000007017 scission Effects 0.000 claims abstract description 16
230000002779 inactivation Effects 0.000 claims abstract description 10
102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims abstract 3
HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 215
235000001014 amino acid Nutrition 0.000 claims description 109
235000012000 cholesterol Nutrition 0.000 claims description 103
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FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims description 91
125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims description 86
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125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 71
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125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 58
125000006850 spacer group Chemical group 0.000 claims description 58
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WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 55
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WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 49
125000006239 protecting group Chemical group 0.000 claims description 45
125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 43
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LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims description 34
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210000004899 c-terminal region Anatomy 0.000 claims description 33
238000006467 substitution reaction Methods 0.000 claims description 33
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QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 28
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Diabetes (AREA)
Endocrinology (AREA)
Biochemistry (AREA)
Molecular Biology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Gastroenterology & Hepatology (AREA)
Zoology (AREA)
Toxicology (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
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Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Hematology (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Obesity (AREA)
Child & Adolescent Psychology (AREA)
Emergency Medicine (AREA)
Peptides Or Proteins (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicinal Preparation (AREA)
Physical Water Treatments (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)

RU2011134596/04A 2009-02-19 2009-12-18 Аналоги оксинтомодулина RU2542362C2 (ru)

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CA2913805A1 (en)	2005-11-07	2007-05-18	Indiana University Research And Technology Corporation	Glucagon analogs exhibiting physiological solubility and stability
RU2477286C2 (ru)	2007-01-05	2013-03-10	Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн	АНАЛОГИ ГЛЮКАГОНА, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ В БУФЕРАХ С ФИЗИОЛОГИЧЕСКИМ ЗНАЧЕНИЕМ pH
CA2677932A1 (en)	2007-02-15	2008-08-21	Indiana University Research And Technology Corporation	Glucagon/glp-1 receptor co-agonists
ES2509883T3 (es)	2007-10-30	2014-10-20	Indiana University Research And Technology Corporation	Antagonistas de glucagón
MX2010004298A (es)	2007-10-30	2010-05-03	Univ Indiana Res & Tech Corp	Compuestos que exhiben actividad antagonista de glucagon y agonista de glp-1.
AR072160A1 (es)	2008-06-17	2010-08-11	Univ Indiana Res & Tech Corp	Co-agonistas del receptor de glucagon/glp-1
CN102105159B (zh)	2008-06-17	2015-07-08	印第安纳大学研究及科技有限公司	基于gip的混合激动剂用于治疗代谢紊乱和肥胖症
US8450270B2 (en)	2008-06-17	2013-05-28	Indiana University Research And Technology Corporation	Glucagon analogs exhibiting enhanced solubility and stability in physiological pH buffers
PE20120332A1 (es)	2008-12-19	2012-04-14	Univ Indiana Res & Tech Corp	Profarmacos de peptido de la superfamilia de glucagon basado en amida
WO2010096052A1 (en)	2009-02-19	2010-08-26	Merck Sharp & Dohme Corp.	Oxyntomodulin analogs
EP2443146B1 (en)	2009-06-16	2016-10-05	Indiana University Research And Technology Corporation	Gip receptor-active glucagon compounds
AU2010272944B2 (en)	2009-07-13	2015-11-19	Zealand Pharma A/S	Acylated glucagon analogues
US8703701B2 (en)	2009-12-18	2014-04-22	Indiana University Research And Technology Corporation	Glucagon/GLP-1 receptor co-agonists
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ZA201106051B (en)	2014-07-30
MX2011008717A (es)	2012-09-28
BRPI0924307A8 (pt)	2017-12-12
SG173791A1 (en)	2011-10-28
CN102573872A (zh)	2012-07-11
CL2011002036A1 (es)	2012-02-03
BRPI0924307A2 (2)	2017-08-22
US20120165503A1 (en)	2012-06-28
PL2398483T3 (pl)	2015-03-31
IL214729A (en)	2016-06-30
RU2011134596A (ru)	2013-03-27
EP2398483A4 (en)	2013-03-06
HRP20141215T1 (hr)	2015-02-13
HK1165333A1 (en)	2012-10-05
CY1116917T1 (el)	2017-04-05
DK2398483T3 (da)	2014-10-27
CA2754350A1 (en)	2010-08-26
US9593155B2 (en)	2017-03-14
AU2009340439A1 (en)	2011-09-15
KR101634139B1 (ko)	2016-06-28
CN102573872B (zh)	2016-03-23
ES2524477T3 (es)	2014-12-09
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