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AR099936A1 - Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados - Google Patents

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

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Publication number
AR099936A1
AR099936A1 ARP150100989A ARP150100989A AR099936A1 AR 099936 A1 AR099936 A1 AR 099936A1 AR P150100989 A ARP150100989 A AR P150100989A AR P150100989 A ARP150100989 A AR P150100989A AR 099936 A1 AR099936 A1 AR 099936A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently
groups
substituted
cycloalkyl
Prior art date
Application number
ARP150100989A
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English (en)
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Sanofi Sa
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Publication of AR099936A1 publication Critical patent/AR099936A1/es

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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
    • 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D249/18Benzotriazoles
    • CCHEMISTRY; METALLURGY
    • 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
    • AHUMAN NECESSITIES
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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

Compuestos heterocíclicos condensados sustituidos. Los compuestos heterocíclicos condensados sustituidos son moduladores de GPR119 y son útiles para la prevención y/o el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados. Además el uso de compuestos heterocíclicos condensados sustituidos como ingredientes activos en productos farmacéuticos, y a composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto de la fórmula (1) en la que A es N o C; B es CO, N o CH; E es N o C; G es N o CR³⁰; en donde al menos uno de los grupos A, B, E o G es N; R³⁰ es H o (CR¹¹R¹²)ₙ-R³²; R¹¹, R¹² son independientemente uno de otro H o alquilo C₁₋₆; n es 0, 1, 2 ó 3; R³² es alquilo C₁₋₆, cicloalquilo C₃₋₈, COOR¹³, CONR¹⁴R¹⁵, SO₂R¹⁶ o OH; R¹³ es H o alquilo C₁₋₆; R¹⁴, R¹⁵ son independientemente uno de otro H, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con OR¹⁷, o cicloalquilo C₃₋₆; o R¹⁴ y R¹⁵ forman junto con el átomo de N al que están unidos, un heterociclo de 4, 5 ó 6 miembros, que opcionalmente contiene un heteroátomo adicional seleccionado de la lista de O, S y NR¹⁸; en donde el heterociclo de 4, 5 ó 6 miembros puede estar opcionalmente sustituido con 1 a 3 grupos seleccionados de la lista de alquilo C₁₋₄ y OR¹⁷; R¹⁶ es alquilo C₁₋₆; R¹⁷ es H o alquilo C₁₋₆; R¹⁸ es H o alquilo C₁₋₆; R¹ᵃ, R¹ᵇ, R¹ᶜ son independientemente uno de otro H, F, Cl, Br, alquilo C₁₋₆ o CN; R²ᵃ, R²ᵇ, R²ᶜ son independientemente uno de otro H, F, Cl, Br, alquilo C₁₋₆ o CN; Y es N o CH; Z es un enlace, O, CR⁵R⁵, NR⁶, C=O, S, SO o SO₂; R⁵, R⁵, R⁶ son independientemente uno de otro H o alquilo C₁₋₄; R³ es un enlace o (CR⁷R⁷)ₚ; p es 0, 1, 2, 3 ó 4; R⁷, R⁷ son independientemente uno de otro H o alquilo C₁₋₆; R⁴ es alquilo C₁₋₆, OR⁸, cicloalquilo C₃₋₈, bicicloalquilo C₅₋₈, heterociclo de 4, 5 ó 6 miembros, fenilo o anillo heteroarilo de 5 ó 6 miembros; en donde los grupos cicloalquilo C₃₋₈, bicicloalquilo C₅₋₈, heterociclo de 4, 5 ó 6 miembros, fenilo, anillo heteroarilo de 5 ó 6 miembros pueden estar opcionalmente sustituidos con 1 a 3 grupos seleccionados de alquilo C₁₋₄, alcanoilo C₁₋₄, hidroxi, hidroxi-alquilo C₁₋₄, alquiloxi C₁₋₃-alquilo C₁₋₄, oxo, F o Cl; R⁸ es H, alquilo C₁₋₆, hidroxi-alquilo C₁₋₄ o alquiloxi C₁₋₃-alquilo C₁₋₄; en donde en cada aparición los átomos de hidrógeno de los grupos alquilo pueden estar parcial o totalmente reemplazados por átomos de flúor; en cualquiera de sus formas estereoisómeras, o una mezcla de formas estereoisómeras en cualquier proporción, o una de sus sales fisiológicamente aceptables.
ARP150100989A 2014-04-04 2015-04-01 Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados AR099936A1 (es)

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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)

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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
PL3126354T3 (pl) 2014-04-04 2020-06-15 H. Lundbeck A/S Fluorowcowane chinazolino-THF-aminy jako inhibitory PDE1
TWI784968B (zh) 2016-09-09 2022-12-01 丹麥商西蘭製藥公司 澱粉素類似物
WO2018153849A1 (en) 2017-02-21 2018-08-30 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
JP7265276B2 (ja) * 2018-05-31 2023-04-26 華領医薬技術(上海)有限公司 グルコキナーゼ活性化剤およびsglt-2阻害薬を含む医薬品の組合せ、組成物、配合剤、ならびにその調製方法および使用
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
TWI867086B (zh) * 2019-11-05 2024-12-21 加拿大商瑞斯弗洛吉克斯公司 以rvx-208及sglt2抑制劑治療及/或預防主要不良心血管事件(mace)的方法
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
JP2023531726A (ja) 2020-06-26 2023-07-25 キャリーオペ,インク. Ampkアクチベーター

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EP3126336A1 (en) 2017-02-08
DOP2016000212A (es) 2016-11-15
MA39346A1 (fr) 2017-09-29
US9758520B2 (en) 2017-09-12
CL2016002497A1 (es) 2017-03-31
MX2016013033A (es) 2017-01-09
US20170022198A1 (en) 2017-01-26
EA030410B1 (ru) 2018-07-31
PE20161378A1 (es) 2016-12-26
CN106164073A (zh) 2016-11-23
MA39346B1 (fr) 2019-03-29
AU2015239021A1 (en) 2016-10-13
SG11201606758SA (en) 2016-09-29
KR20160132885A (ko) 2016-11-21
ECSP16078779A (es) 2017-02-24
CA2942753A1 (en) 2015-10-08
IL248129A0 (en) 2016-11-30
PH12016501619A1 (en) 2017-02-06
EA201692008A1 (ru) 2017-02-28
JP2017509679A (ja) 2017-04-06
EP3126336B1 (en) 2018-12-05
CR20160460A (es) 2017-02-21
WO2015150564A1 (en) 2015-10-08
TW201625605A (zh) 2016-07-16

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