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EA201790254A1 - Новые модуляторы рецептора glp-1 - Google Patents

Новые модуляторы рецептора glp-1

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Publication number
EA201790254A1
EA201790254A1 EA201790254A EA201790254A EA201790254A1 EA 201790254 A1 EA201790254 A1 EA 201790254A1 EA 201790254 A EA201790254 A EA 201790254A EA 201790254 A EA201790254 A EA 201790254A EA 201790254 A1 EA201790254 A1 EA 201790254A1
Authority
EA
Eurasian Patent Office
Prior art keywords
glp
receptor modulators
peptide
compounds
receptor
Prior art date
Application number
EA201790254A
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English (en)
Other versions
EA032525B1 (ru
Inventor
Маркус Ф. Боэм
Эстер Мартинборо
Маниша Мурджани
Дзунко Тамия
Лимин Хуан
Адам Р. Йиджер
Энугуртхи Брахмачари
Томас Фаулер
Эндрю Новак
Премдзи Мегхани
Майкл Нэггз
Original Assignee
Селджин Интернэшнл Ii Сарл
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.)
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Publication date
Application filed by Селджин Интернэшнл Ii Сарл filed Critical Селджин Интернэшнл Ii Сарл
Publication of EA201790254A1 publication Critical patent/EA201790254A1/ru
Publication of EA032525B1 publication Critical patent/EA032525B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7004Monosaccharides having only carbon, hydrogen and oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Zoology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Предложены соединения, которые модулируют рецептор глюкагонподобного пептида 1 (GLP-1), а также способы их синтеза и способы их терапевтического и/или профилактического применения. Такие соединения могут воздействовать в качестве модуляторов или потенциаторов рецептора GLP-1 самостоятельно или с инкретиновыми пептидами, такими как GLP-1(7-36), GLP-1(9-36) и оксинтомодулин, или с основанными на пептидах препаратами, такими как эксенатид и лираглутид, и имеют следующую общую структуру (где "" представляет любую из двух или обе R- и S-формы данного соединения):где А, В, С, R, R, R, R, R, n, p и q являются такими, как определено в описании изобретения.
EA201790254A 2014-07-25 2015-07-24 Модуляторы рецептора glp-1 EA032525B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462028962P 2014-07-25 2014-07-25
US201462090040P 2014-12-10 2014-12-10
US201562161650P 2015-05-14 2015-05-14
PCT/US2015/042114 WO2016015014A1 (en) 2014-07-25 2015-07-24 Novel glp-1 receptor modulators

Publications (2)

Publication Number Publication Date
EA201790254A1 true EA201790254A1 (ru) 2017-07-31
EA032525B1 EA032525B1 (ru) 2019-06-28

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EA201790254A EA032525B1 (ru) 2014-07-25 2015-07-24 Модуляторы рецептора glp-1

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US (2) US9474755B2 (ru)
EP (1) EP3172199B1 (ru)
JP (2) JP6556237B2 (ru)
KR (1) KR102564946B1 (ru)
CN (2) CN112457301A (ru)
AU (1) AU2015292356B2 (ru)
CA (1) CA2955836C (ru)
EA (1) EA032525B1 (ru)
ES (1) ES2819534T3 (ru)
IL (1) IL249896B (ru)
MX (1) MX2017000972A (ru)
SG (1) SG11201700364PA (ru)
WO (1) WO2016015014A1 (ru)
ZA (1) ZA201700342B (ru)

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US9278910B2 (en) 2011-05-31 2016-03-08 Receptos, Inc. GLP-1 receptor stabilizers and modulators
KR102271179B1 (ko) 2013-06-11 2021-07-01 셀진 인터내셔널 Ii 에스에이알엘 신규의 glp-1 수용체 조절제
US9474755B2 (en) * 2014-07-25 2016-10-25 Celgene International Ii Sarl GLP-1 receptor modulators
CA2969944A1 (en) 2014-12-10 2016-06-16 Celgene International Ii Sarl Glp-1 receptor modulators
HRP20211938T1 (hr) * 2016-09-30 2022-03-18 Receptos Llc Sol dimetilaminoetanola od modulatora receptora glp-1
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IL300155A (en) 2020-08-06 2023-03-01 Gasherbrum Bio Inc Heterocyclic GLP-1 agonists
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US9474755B2 (en) * 2014-07-25 2016-10-25 Celgene International Ii Sarl GLP-1 receptor modulators

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JP6556237B2 (ja) 2019-08-07
IL249896B (en) 2021-02-28
EP3172199A1 (en) 2017-05-31
US20170216392A1 (en) 2017-08-03
AU2015292356B2 (en) 2020-02-06
US20160038487A1 (en) 2016-02-11
AU2015292356A1 (en) 2017-02-02
CA2955836C (en) 2023-02-14
US9474755B2 (en) 2016-10-25
ES2819534T3 (es) 2021-04-16
US9839664B2 (en) 2017-12-12
WO2016015014A1 (en) 2016-01-28
MX2017000972A (es) 2017-07-27
JP2017526734A (ja) 2017-09-14
KR102564946B1 (ko) 2023-08-08
IL249896A0 (en) 2017-03-30
KR20170040233A (ko) 2017-04-12
EA032525B1 (ru) 2019-06-28
CN112457301A (zh) 2021-03-09
EP3172199B1 (en) 2020-07-01
JP2019142984A (ja) 2019-08-29
CN107074820B (zh) 2021-05-18
CN107074820A (zh) 2017-08-18
SG11201700364PA (en) 2017-02-27
CA2955836A1 (en) 2016-01-28
ZA201700342B (en) 2018-12-19

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