EA030410B1 - Замещенные конденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений - Google Patents

Замещенные конденсированные гетероциклы в качестве модуляторов gpr119 для лечения диабета, ожирения, дислипидемии и связанных нарушений Download PDF

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Publication number
EA030410B1
EA030410B1 EA201692008A EA201692008A EA030410B1 EA 030410 B1 EA030410 B1 EA 030410B1 EA 201692008 A EA201692008 A EA 201692008A EA 201692008 A EA201692008 A EA 201692008A EA 030410 B1 EA030410 B1 EA 030410B1
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EA
Eurasian Patent Office
Prior art keywords
oxy
pyridyl
cyclopropylmethoxy
oxopyrrolidin
pyridin
Prior art date
Application number
EA201692008A
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English (en)
Russian (ru)
Other versions
EA201692008A1 (ru
Inventor
Лотар Швинк
Кристиан Бунинг
Хайнер Гломбик
Маттиас Госсель
Дитер Кадерайт
Нис Халланн
Маттиас Ломанн
Кристоф Пеферляйн
Курт Риттер
Original Assignee
Санофи
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.)
Filing date
Publication date
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 EA201692008A1 (ru) 2017-02-28
EA030410B1 true EA030410B1 (ru) 2018-07-31

Family

ID=50513859

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (enExample)
EP (1) EP3126336B1 (enExample)
JP (1) JP2017509679A (enExample)
KR (1) KR20160132885A (enExample)
CN (1) CN106164073A (enExample)
AR (1) AR099936A1 (enExample)
AU (1) AU2015239021A1 (enExample)
CA (1) CA2942753A1 (enExample)
CL (1) CL2016002497A1 (enExample)
CR (1) CR20160460A (enExample)
DO (1) DOP2016000212A (enExample)
EA (1) EA030410B1 (enExample)
EC (1) ECSP16078779A (enExample)
IL (1) IL248129A0 (enExample)
MA (1) MA39346B1 (enExample)
MX (1) MX2016013033A (enExample)
PE (1) PE20161378A1 (enExample)
PH (1) PH12016501619A1 (enExample)
SG (1) SG11201606758SA (enExample)
TW (1) TW201625605A (enExample)
WO (1) WO2015150564A1 (enExample)

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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
EA032579B1 (ru) 2014-04-04 2019-06-28 Х. Лундбекк А/С Галогенированные хиназолин-тгф-амины в качестве ингибиторов pde1
AR109514A1 (es) 2016-09-09 2018-12-19 Zealand Pharma As Análogos de amilina
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
BR112020024269A2 (pt) * 2018-05-31 2021-02-23 Hua Medicine (Shanghai) Ltd. combinação farmacêutica, composição e formulação de combinação contendo ativador de glucoquinase e ativador de receptor ppar e métodos de preparação e usos dos mesmos
KR102131359B1 (ko) * 2018-09-07 2020-07-07 오토텔릭바이오 주식회사 안정성이 향상된 의약 조성물
BR112021013924A2 (pt) 2019-01-18 2021-09-21 Astrazeneca Ab Inibidores de pcsk9 e métodos de uso do mesmo
WO2020150473A2 (en) 2019-01-18 2020-07-23 Dogma Therapeutics, Inc. Pcsk9 inhibitors and methods of use thereof
MX2021014410A (es) 2019-05-31 2022-03-17 Avolynt Composiciones y métodos para tratar la enfermedad metabólica.
US12551484B2 (en) * 2019-11-05 2026-02-17 Resverlogix Corp. Methods of treatment and/or prevention of major adverse cardiovascular events (MACE) with a combination of a BET bromodomain inhibitor and a sodium dependent glucose transport 2 inhibitor
MX2022010548A (es) 2020-02-28 2022-09-23 Kallyope Inc Agonistas de gpr40.
MX2022014505A (es) 2020-05-19 2022-12-13 Kallyope Inc Activadores de la ampk.
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
WO2022052958A1 (en) 2020-09-10 2022-03-17 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
IL312600B2 (en) 2022-05-30 2025-12-01 Zealand Pharma As Liquid formulations of amylin analogs
EP4612152A1 (en) * 2022-11-01 2025-09-10 Merck Sharp & Dohme LLC Preparation of triazolopyridine derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors

Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2004110994A1 (en) * 2003-06-18 2004-12-23 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
WO2007124254A2 (en) * 2006-04-21 2007-11-01 Eli Lilly And Company Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
WO2011146335A1 (en) * 2010-05-17 2011-11-24 Array Biopharma Inc. Piperidinyl-substituted lactams as gpr119 modulators
US20110306599A1 (en) * 2009-11-25 2011-12-15 Japan Tobacco Inc. Indole compounds and pharmaceutical use thereof

Family Cites Families (5)

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Publication number Priority date Publication date Assignee Title
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
AU2011202239C1 (en) 2010-05-19 2017-03-16 Sanofi Long-acting formulations of insulins
CN103221046A (zh) 2010-09-17 2013-07-24 阵列生物制药公司 作为gpr119调节剂的哌啶基取代的内酰胺
CA2853784A1 (en) 2011-11-11 2013-05-16 Glaxosmithkline Llc Treatment of blood lipid abnormalities and other conditions
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004110994A1 (en) * 2003-06-18 2004-12-23 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
WO2007124254A2 (en) * 2006-04-21 2007-11-01 Eli Lilly And Company Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
US20110306599A1 (en) * 2009-11-25 2011-12-15 Japan Tobacco Inc. Indole compounds and pharmaceutical use thereof
WO2011146335A1 (en) * 2010-05-17 2011-11-24 Array Biopharma Inc. Piperidinyl-substituted lactams as gpr119 modulators

Also Published As

Publication number Publication date
CA2942753A1 (en) 2015-10-08
MA39346A1 (fr) 2017-09-29
TW201625605A (zh) 2016-07-16
CR20160460A (es) 2017-02-21
ECSP16078779A (es) 2017-02-24
MA39346B1 (fr) 2019-03-29
DOP2016000212A (es) 2016-11-15
PH12016501619A1 (en) 2017-02-06
PE20161378A1 (es) 2016-12-26
CL2016002497A1 (es) 2017-03-31
AR099936A1 (es) 2016-08-31
AU2015239021A1 (en) 2016-10-13
JP2017509679A (ja) 2017-04-06
CN106164073A (zh) 2016-11-23
SG11201606758SA (en) 2016-09-29
US20170022198A1 (en) 2017-01-26
EP3126336B1 (en) 2018-12-05
EA201692008A1 (ru) 2017-02-28
MX2016013033A (es) 2017-01-09
IL248129A0 (en) 2016-11-30
EP3126336A1 (en) 2017-02-08
KR20160132885A (ko) 2016-11-21
WO2015150564A1 (en) 2015-10-08
US9758520B2 (en) 2017-09-12

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