EA201692008A1 - Замещенные сконденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений - Google Patents

Замещенные сконденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений

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Publication number
EA201692008A1
EA201692008A1 EA201692008A EA201692008A EA201692008A1 EA 201692008 A1 EA201692008 A1 EA 201692008A1 EA 201692008 A EA201692008 A EA 201692008A EA 201692008 A EA201692008 A EA 201692008A EA 201692008 A1 EA201692008 A1 EA 201692008A1
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EA
Eurasian Patent Office
Prior art keywords
substituted condensed
dyslipidemia
obesity
diabetes
treatment
Prior art date
Application number
EA201692008A
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English (en)
Other versions
EA030410B1 (ru
Inventor
Лотар ШВИНК
Кристиан БУНИНГ
Хайнер Гломбик
Маттиас Госсель
Дитер КАДЕРАЙТ
Нис ХАЛЛАНН
Маттиас Ломанн
Кристоф Пеферляйн
Курт Риттер
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Санофи
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Application filed by Санофи filed Critical Санофи
Publication of EA201692008A1 publication Critical patent/EA201692008A1/ru
Publication of EA030410B1 publication Critical patent/EA030410B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/702Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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    • C07ORGANIC CHEMISTRY
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Изобретение относится к замещенным сконденсированным гетероциклическим соединениям. Замещенные сконденсированные гетероциклические соединения представляют собой модуляторы GPR119 и пригодны для предупреждения и/или лечения диабета, ожирения, дислипидемии и связанных нарушений. Настоящее изобретение также относится к применению замещенных сконденсированных гетероциклических соединений в качестве активных ингредиентов в лекарственных средствах и фармацевтических композиций, содержащих их.
EA201692008A 2014-04-04 2015-04-02 Замещенные конденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений EA030410B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14305494 2014-04-04
PCT/EP2015/057414 WO2015150564A1 (en) 2014-04-04 2015-04-02 Substituted fused heterocycles as gpr119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders

Publications (2)

Publication Number Publication Date
EA201692008A1 true EA201692008A1 (ru) 2017-02-28
EA030410B1 EA030410B1 (ru) 2018-07-31

Family

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Family Applications (1)

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EA201692008A EA030410B1 (ru) 2014-04-04 2015-04-02 Замещенные конденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений

Country Status (21)

Country Link
US (1) US9758520B2 (ru)
EP (1) EP3126336B1 (ru)
JP (1) JP2017509679A (ru)
KR (1) KR20160132885A (ru)
CN (1) CN106164073A (ru)
AR (1) AR099936A1 (ru)
AU (1) AU2015239021A1 (ru)
CA (1) CA2942753A1 (ru)
CL (1) CL2016002497A1 (ru)
CR (1) CR20160460A (ru)
DO (1) DOP2016000212A (ru)
EA (1) EA030410B1 (ru)
EC (1) ECSP16078779A (ru)
IL (1) IL248129A0 (ru)
MA (1) MA39346B1 (ru)
MX (1) MX2016013033A (ru)
PE (1) PE20161378A1 (ru)
PH (1) PH12016501619A1 (ru)
SG (1) SG11201606758SA (ru)
TW (1) TW201625605A (ru)
WO (1) WO2015150564A1 (ru)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR099936A1 (es) 2014-04-04 2016-08-31 Sanofi Sa Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados
DK3126354T3 (da) 2014-04-04 2020-03-09 H Lundbeck As Halogenerede quinazolin-thf-aminer som pde1-inhibitorer
AR110988A1 (es) 2017-02-21 2019-05-22 Sanofi Sa Compuestos de azetidina como moduladores de gpr119 para el tratamiento de la diabetes, la obesidad, la dislipidemia y trastornos relacionados
WO2019043635A1 (en) 2017-09-01 2019-03-07 Richter Gedeon Nyrt. COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE
SG11202011883RA (en) * 2018-05-31 2020-12-30 Hua Medicine Shanghai Ltd Pharmaceutical combination, composition, and combination formulation containing glucokinase activator and ppar receptor activator, and preparation methods and uses thereof
KR102131359B1 (ko) * 2018-09-07 2020-07-07 오토텔릭바이오 주식회사 안정성이 향상된 의약 조성물
CA3142325A1 (en) * 2019-05-31 2020-12-03 Avolynt Compositions and methods for treating metabolic disease
UY39222A (es) 2020-05-19 2021-11-30 Kallyope Inc Activadores de la ampk
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators

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EP1638932A1 (en) * 2003-06-18 2006-03-29 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
JP5161869B2 (ja) * 2006-04-21 2013-03-13 イーライ リリー アンド カンパニー 11−β−ヒドロキシステロイドデヒドロゲナーゼ1の阻害剤としての、シクロヘキシルピラゾール−ラクタム誘導体
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8299070B2 (en) * 2009-11-25 2012-10-30 Japan Tobacco Inc. Indole compounds and pharmaceutical use thereof
JP2013530947A (ja) * 2010-05-17 2013-08-01 アレイ バイオファーマ、インコーポレイテッド Gpr119調節薬としてのピペリジニル置換ラクタム
AU2011202239C1 (en) 2010-05-19 2017-03-16 Sanofi Long-acting formulations of insulins
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AR099936A1 (es) 2014-04-04 2016-08-31 Sanofi Sa Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados

Also Published As

Publication number Publication date
EA030410B1 (ru) 2018-07-31
AR099936A1 (es) 2016-08-31
US20170022198A1 (en) 2017-01-26
TW201625605A (zh) 2016-07-16
CN106164073A (zh) 2016-11-23
MA39346A1 (fr) 2017-09-29
EP3126336A1 (en) 2017-02-08
EP3126336B1 (en) 2018-12-05
US9758520B2 (en) 2017-09-12
AU2015239021A1 (en) 2016-10-13
SG11201606758SA (en) 2016-09-29
PH12016501619A1 (en) 2017-02-06
JP2017509679A (ja) 2017-04-06
CL2016002497A1 (es) 2017-03-31
ECSP16078779A (es) 2017-02-24
PE20161378A1 (es) 2016-12-26
WO2015150564A1 (en) 2015-10-08
CA2942753A1 (en) 2015-10-08
DOP2016000212A (es) 2016-11-15
KR20160132885A (ko) 2016-11-21
IL248129A0 (en) 2016-11-30
CR20160460A (es) 2017-02-21
MX2016013033A (es) 2017-01-09
MA39346B1 (fr) 2019-03-29

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