AR072559A1 - Amidas sustituidas, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por dgat1. - Google Patents

Amidas sustituidas, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por dgat1.

Info

Publication number
AR072559A1
AR072559A1 ARP090102662A ARP090102662A AR072559A1 AR 072559 A1 AR072559 A1 AR 072559A1 AR P090102662 A ARP090102662 A AR P090102662A AR P090102662 A ARP090102662 A AR P090102662A AR 072559 A1 AR072559 A1 AR 072559A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
hetero
alkylene
alkenylene
cycloalkyl
Prior art date
Application number
ARP090102662A
Other languages
English (en)
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41136646&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR072559(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR072559A1 publication Critical patent/AR072559A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14Nitrogen atoms
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61P3/08Drugs 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
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Estos compuestos son utiles para el tratamiento de los trastornos mediados por acil-transferasa de acil-CoA-diacilglicerol 1 (DGAT1), por ejemplo, trastornos metabolicos. Su uso en el tratamiento de estos trastornos, y las composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de la formula (1) o un derivado farmacéuticamente aceptable del mismo, en donde R3 es H o alquilo C1-10 opcionalmente sustituido, heteroalquilo C1-10, -(Alkb)g-cicloalquilo C3-10, -(Alkb)g-heterocicloalquilo C3-10, alquenilo C2-10, hetero-alquenilo C2-10, -(Alkb)g-cicloalquenilo C3-10, -(Alkb)g-heterocicloalquenilo C3-10, alquinilo C2-10, heteroalquinilo C2-10, -(Alkb)g-ariIo C6-14, -(Alkb)g-heteroarilo (en donde heteroarilo contiene de 6 a 13 miembros del anillo), en donde. Alkb es alquileno C1-6 o hetero-alquileno C1-6 opcionalmente sustituidos, g es 0 o 1; r es 0 o 1; Z es O o NR6, en donde R6 es H o alquilo C1-6 opcionalmente sustituido, heteroalquilo C1-6, cicloalquilo C3-6, hetero-cicloalquilo C3-6, alquenilo C2-6, heteroalquenilo C2-6, cicloalquenilo C3-6, hetero-cicloalquenilo C3-6, fenilo, o heteroarilo que contiene 5 o 6 miembros del anillo; s es 0 o 1; M es -C(O)- o -S(O)t-, en donde: t es 1 o 2; R4 es H o alquilo C1-6 opcionalmente sustituido, heteroalquilo C1-6, cicloalquilo C3-6, hetero-cicloalquilo C3-6, alquenilo C2-6, heteroalquenilo C2-6, cicloalquenilo C3-6, hetero-cicloalquenilo C3-6, fenilo, o heteroarilo que contiene 5 o 6 miembros del anillo; R1 y R2 son independientemente H o alquilo C1-6 opcionalmente sustituido, heteroalquilo C1-6, -(Alkc)h-cicloalquilo C3-6, -(Alkc)h-hetero-cicloalquilo C3-6, alquenilo C2-6, hetero-alquenilo C2-6, -(Alkc)h-cicloalquenilo C3-6, -(Alkc)h-hetero-cicloalquenilo C3-6, -(Alkc)h-fenilo, o -(Alkc)h-heteroariIo (en donde heteroarilo contiene 5 o 6 miembros del anillo), en donde AIkc es independientemente alquileno C1-6 o hetero-alquileno C1-6 opcionalmente sustituidos, h es independientemente 0 o 1; R5 es H o alquilo C1-6 opcionalmente sustituido, heteroalquilo C1-6, cicloalquilo C3-6, hetero-cicloalquilo C3-6, alquenilo C2-6, heteroalquenilo C2-6, cicloalquenilo C3-6, hetero-cicloalquenilo C3-6, fenilo, o heteroarilo que contiene 5 o 6 miembros del anillo: o uno de R1 y R4 forman juntos alquileno C3-5, alquenileno C3-5, hetero-alquileno C3-5, o hetero-alquenileno C3-5 opcionalmente sustituidos; R1 y R2 forman juntos alquileno C2-8, alquenileno C2-8, hetero-alquileno C2-8, o hetero-alquenileno C2-8 opcionalmente sustituidos; o R1 y R5 forman juntos alquileno C2-4, alquenileno C2-4, hetero-alquileno C2-4, o hetero-alquenileno C2-4 opcionalmente sustituidos; A es heteroarilo opcionalmente sustituido que contiene de 5 a 13 miembros del anillo; a es de 0 a 3; b es de 0 a 3;R10a es -Q-R7a, y R10b es -R7b, en donde Q es independientemente alquileno C1-6, hetero-alquileno C1-6, alquenileno C2-6 o hetero-alquenileno C2-6 opcionalmente sustituidos, u O, S, NR8, o -C(O)-, en donde R8 es H o alquilo C1-6 opcionalmente sustituido; y R7a es H o alquilo C1-10 opcionalmente sustituido, heteroalquilo C1-10, cicloalquilo C3-10, hetero-cicloalquilo C3-10, arilo C6-14 o heteroarilo que contiene de 5 a 13 miembros del anillo, R7b es alquilo C1-10 opcionalmente sustituido, heteroalquilo C1-10, cicloalquilo C3-10, hetero-cicloalquilo C3-10, arilo C6-14 o heteroarilo que contiene de 5 a 13 miembros del anillo; y en el entendido de que cuando menos uno de R3 y R4 no es H.
ARP090102662A 2008-07-15 2009-07-14 Amidas sustituidas, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por dgat1. AR072559A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US8091308P 2008-07-15 2008-07-15

Publications (1)

Publication Number Publication Date
AR072559A1 true AR072559A1 (es) 2010-09-08

Family

ID=41136646

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102662A AR072559A1 (es) 2008-07-15 2009-07-14 Amidas sustituidas, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por dgat1.

Country Status (23)

Country Link
US (1) US8703761B2 (es)
EP (4) EP2548618A3 (es)
JP (1) JP5401544B2 (es)
KR (1) KR20110028661A (es)
CN (1) CN102119047B (es)
AR (1) AR072559A1 (es)
AU (1) AU2009272826A1 (es)
BR (1) BRPI0916216A2 (es)
CA (1) CA2731097A1 (es)
CL (1) CL2011000087A1 (es)
CO (1) CO6341581A2 (es)
CR (1) CR20110013A (es)
EA (1) EA201100189A1 (es)
EC (1) ECSP11010830A (es)
IL (1) IL210292A0 (es)
MA (1) MA32558B1 (es)
MX (1) MX2011000628A (es)
NZ (1) NZ590285A (es)
PE (1) PE20110105A1 (es)
SV (1) SV2011003809A (es)
TW (1) TW201006832A (es)
UY (1) UY31986A (es)
WO (1) WO2010007046A2 (es)

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CL2011000087A1 (es) 2011-07-01
CO6341581A2 (es) 2011-11-21
JP2011528016A (ja) 2011-11-10
IL210292A0 (en) 2011-03-31
BRPI0916216A2 (pt) 2018-03-13
US20100022513A1 (en) 2010-01-28
SV2011003809A (es) 2011-07-05
EP2380631A1 (en) 2011-10-26
KR20110028661A (ko) 2011-03-21
TW201006832A (en) 2010-02-16
MX2011000628A (es) 2011-02-25
WO2010007046A3 (en) 2010-07-22
NZ590285A (en) 2012-10-26
CN102119047B (zh) 2014-09-24
EP2349484A2 (en) 2011-08-03
WO2010007046A2 (en) 2010-01-21
CN102119047A (zh) 2011-07-06
AU2009272826A1 (en) 2010-01-21
UY31986A (es) 2010-02-26
EP2559455A1 (en) 2013-02-20
US8703761B2 (en) 2014-04-22
EP2548618A2 (en) 2013-01-23
PE20110105A1 (es) 2011-02-25
EP2548618A3 (en) 2013-02-27
ECSP11010830A (es) 2011-03-31
CA2731097A1 (en) 2010-01-21
CR20110013A (es) 2011-02-11
EA201100189A1 (ru) 2011-08-30
MA32558B1 (fr) 2011-08-01
JP5401544B2 (ja) 2014-01-29

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