PE20161378A1 - Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y transtornos relacionados - Google Patents

Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y transtornos relacionados

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Publication number
PE20161378A1
PE20161378A1 PE2016001909A PE2016001909A PE20161378A1 PE 20161378 A1 PE20161378 A1 PE 20161378A1 PE 2016001909 A PE2016001909 A PE 2016001909A PE 2016001909 A PE2016001909 A PE 2016001909A PE 20161378 A1 PE20161378 A1 PE 20161378A1
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PE
Peru
Prior art keywords
diabetes
treatment
related disorders
dyslipidemia
obesity
Prior art date
Application number
PE2016001909A
Other languages
English (en)
Inventor
Christian Buning
Heiner Glombik
Matthias Gossel
Nis Halland
Lothar Schwink
Matthias Lohmann
Christoph Poverlein
Kurt Ritter
Dieter Kadereit
Original Assignee
Sanofi Sa
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 Sanofi Sa filed Critical Sanofi Sa
Publication of PE20161378A1 publication Critical patent/PE20161378A1/es

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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

Landscapes

  • 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)

Abstract

La presente invencion se refiere a heterociclicos condensados sustituidos de formula (I) donde: A y E son N o C; B es CO, N o CH; G es N o CR30; en donde al menos uno de A, B, E o G es N; R30 es H o (CR11R12)n-R32; R11 y R12 son H o alquilo C1-C6; n es 0, 1, 2 o 3; R32 es alquilo C1-C6, cicloalquilo C3-C8, entre otros; R1a, R1b, R1c, R2a, R2b y R2c son H, F, entre otros; Y es N o CH; Z es un enlace, O, entre otros; R3 es enlace o (CR7R7´)p; p es 0, 1, 2, 3 o 4; R7 y R7´son H o alquilo C1-C6; R4 es alquilo C1-C6, cicloalquilo C3-C8, entre otros. Son compuestos preferidos: (3R)-3-[[6-(Ciclopropilmetoxi)-3-piridil]oxi]-1-(2-ciclopropil-[1,2,4]triazolo[1,5-a]piridin-6-il)pirrolidin-2-ona; (3R)-3-[[6-(Ciclopropilmetoxi)-3-piridil]oxi]-1-([1,2,4]triazolo[1,5-a]piridin-6-il)pirrolidin-2-ona; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos modulan el receptor GPR19 siendo utiles en la prevencion y/o tratamiento de diabetes o trastornos relacionados
PE2016001909A 2014-04-04 2015-04-02 Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y transtornos relacionados PE20161378A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14305494 2014-04-04

Publications (1)

Publication Number Publication Date
PE20161378A1 true PE20161378A1 (es) 2016-12-26

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ID=50513859

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PE2016001909A PE20161378A1 (es) 2014-04-04 2015-04-02 Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y transtornos relacionados

Country Status (21)

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

Families Citing this family (9)

* 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
MA39837B1 (fr) 2014-04-04 2020-05-29 H Lundbeck As Quinazoline-thf-amines halogénées en tant qu'inhibiteurs de la pde1
EP3585775B1 (en) 2017-02-21 2022-04-06 Sanofi Azetidine compounds as gpr119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders
WO2019043635A1 (en) 2017-09-01 2019-03-07 Richter Gedeon Nyrt. COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE
CN114209694A (zh) * 2018-05-31 2022-03-22 华领医药技术（上海）有限公司 含有葡萄糖激酶激活剂和ppar受体激活剂的药物组合及其制备方法和用途
KR102131359B1 (ko) * 2018-09-07 2020-07-07 오토텔릭바이오 주식회사 안정성이 향상된 의약 조성물
BR112021024165A2 (pt) * 2019-05-31 2022-04-26 Avolynt Composições e métodos para o tratamento de doenças metabólicas
EP4153589A1 (en) 2020-05-19 2023-03-29 Kallyope, Inc. Ampk activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators

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MXPA05013756A (es) * 2003-06-18 2006-03-08 Pfizer Prod Inc Piperazinil-ariloxi y piperazinil-heteroariloxi-n-aril-lactamas novedosas.
MY148128A (en) * 2006-04-21 2013-02-28 Lilly Co Eli Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
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
US8754226B2 (en) * 2010-05-17 2014-06-17 Array Biopharma Inc. Piperidinyl-substituted lactams as GPR119 modulators
AU2011202239C1 (en) 2010-05-19 2017-03-16 Sanofi Long-acting formulations of insulins
RU2013117403A (ru) 2010-09-17 2014-10-27 Эррэй Биофарма Инк. Пиперидинил-замещенные лактамы как модуляторы gpr119
AU2012336157A1 (en) 2011-11-11 2014-05-29 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

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Publication number Publication date
DOP2016000212A (es) 2016-11-15
EP3126336A1 (en) 2017-02-08
CN106164073A (zh) 2016-11-23
US9758520B2 (en) 2017-09-12
CL2016002497A1 (es) 2017-03-31
CR20160460A (es) 2017-02-21
EA201692008A1 (ru) 2017-02-28
EA030410B1 (ru) 2018-07-31
EP3126336B1 (en) 2018-12-05
AR099936A1 (es) 2016-08-31
SG11201606758SA (en) 2016-09-29
AU2015239021A1 (en) 2016-10-13
KR20160132885A (ko) 2016-11-21
PH12016501619A1 (en) 2017-02-06
WO2015150564A1 (en) 2015-10-08
CA2942753A1 (en) 2015-10-08
IL248129A0 (en) 2016-11-30
MA39346B1 (fr) 2019-03-29
TW201625605A (zh) 2016-07-16
MX2016013033A (es) 2017-01-09
JP2017509679A (ja) 2017-04-06
ECSP16078779A (es) 2017-02-24
US20170022198A1 (en) 2017-01-26
MA39346A1 (fr) 2017-09-29

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