AR069802A1 - Compuestos de carbamoilo como inhibidores de dgat1 190 - Google Patents

Compuestos de carbamoilo como inhibidores de dgat1 190

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Publication number
AR069802A1
AR069802A1 ARP080105523A ARP080105523A AR069802A1 AR 069802 A1 AR069802 A1 AR 069802A1 AR P080105523 A ARP080105523 A AR P080105523A AR P080105523 A ARP080105523 A AR P080105523A AR 069802 A1 AR069802 A1 AR 069802A1
Authority
AR
Argentina
Prior art keywords
ring
alkyl
alkoxy
carbon atom
optionally substituted
Prior art date
Application number
ARP080105523A
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English (en)
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Astrazeneca Ab
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40427160&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR069802(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR069802A1 publication Critical patent/AR069802A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • A61P3/08—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings

Landscapes

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

Abstract

Se describen compuestos inhibidores de DGAT-1 de la formula (1), sales y prodrogas farmacéuticamente aceptables de los mismos, conjuntamente con composiciones farmacéuticas, y su uso en el tratamiento, por ejemplo, de la obesidad. Reivindicacion 1: Un compuesto de la formula (1), o una sal, o prodroga farmacéuticamente aceptable del mismo, en donde El anillo A es 2,6-pirazindiilo, 3,5-piridindiilo o 2,6-piridindiilo, cada uno opcionalmente sustituido sobre un átomo de carbono disponible con uno o dos sustituyentes independientemente seleccionados de alquilo C1-3 lineal, alquenilo C2-3; alquinilo C2-3; alcoxi C1-2, metoximetilo, amino y ciano; X es =O o =S; el anillo B es 1,4-fenileno o el anillo B es un anillo di-unido (excluyendo las uniones a través de los mismos átomos o de átomos adyacentes) seleccionado de piridindiilo, furandiilo, tiofendiilo, pirroldiilo, oxazoldiilo, tiazoldiilo, imidazoldiilo, isoxazoldiilo, isotiazoldiilo y pirazoldiilo; cada uno opcionalmente sustituido sobre un átomo de carbono disponible con uno o dos sustituyentes independientemente seleccionados de halo, amino, ciano, alquilo C1-4, alquenilo C2-3; alquinilo C2-3; alcoxi C1-4 y alcoxi C1-4-alquilo C1-4; Y1 es un enlace directo entre el anillo B y el anillo C o Y1 es -O-, -S- o -NRa- en donde Ra es hidrogeno o alquilo C1-4; Y2 es -(CH2)r en donde r es 2 o 3, e Y2 está unido en el mismo átomo de carbono que Y1 en el anillo C e Y2 está unido a un átomo de carbono adyacente a Y1 en el anillo B; n es 0 o n es 1 cuando Y1 es un enlace directo entre el anillo B y el anillo C y cuando el anillo B es 1,4-fenileno y el anillo C es cicloalcano C4-6, de modo que se forme un sistema de anillos espiro de 5 o 6 miembros y el anillo C se encuentre tri-unido; el anillo C es un anillo o sistema de anillos di-unido (excluyendo las uniones a través de los mismos átomos o de átomos adyacentes) seleccionado de cicloalcano C4-6, bicicloalcano C7-10 y tricicloalcano C8-12 cada uno opcionalmente sustituido sobre un átomo de carbono disponible, incluyendo el átomo de carbono del anillo que porta al grupo que contiene a Z, con un sustituyente seleccionado de hidroxi, alquilo C1-4, alcoxi C1-4 y alcoxi C1-4-alquilo C1-4; o el anillo C es un anillo di-unido (excluyendo las uniones a través de los mismos átomos o de átomos adyacentes) seleccionado de fenileno, piridindiilo, piperidindiilo N-unido a Y1, piperazindiilo, furandiilo, tiofendiilo, pirroldiilo, oxazoldiilo, tiazoldiilo, imidazoldiilo, isoxazoldiilo, isotiazoldiilo, pirazoldiilo y azabiciclo[3.1.0]hexandiilo; cada uno opcionalmente sustituido sobre un átomo de carbono disponible con hasta cuatro sustituyentes independientemente seleccionados de fluor, cloro, bromo, ciano, alquilo C1-4, alcoxi C1-4 y alcoxi C1-4-alquilo C1-4; L es un enlace directo al anillo C, -O-, -S- o -NH-; p es 0, 1 o 2 y cuando p es 1 RA1 y RA2 son cada uno independientemente hidrogeno o alquilo C1-4 o RA1 y RA2 están unidos conjuntamente para formar un anillo espiroalquilo C3-6; Z es carboxi o un mímico o bioisostero del mismo, hidroxi o -CONRbRc en donde Rb y Rc están independientemente seleccionados de hidrogeno y alquilo C1-4, cuyo grupo alquilo C1-4 puede estar opcionalmente sustituido con carboxi o un mímico o bioisostero del mismo; y en donde cualquier átomo de carbono en un grupo que contiene alquilo C1-3 lineal, alcoxi C1-2, alquilo C1-4 o alcoxi C1-4 definido precedentemente puede estar opcionalmente sustituido con hasta 3 átomos de fluor; con la condicion de que el compuesto ácido (4-(4-(6-carbamoil-piridin-2-il)fenil)ciclohexil)acético se encuentre excluido.
ARP080105523A 2007-12-20 2008-12-18 Compuestos de carbamoilo como inhibidores de dgat1 190 AR069802A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1539707P 2007-12-20 2007-12-20

Publications (1)

Publication Number Publication Date
AR069802A1 true AR069802A1 (es) 2010-02-17

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ID=40427160

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ARP080105523A AR069802A1 (es) 2007-12-20 2008-12-18 Compuestos de carbamoilo como inhibidores de dgat1 190

Country Status (23)

Country Link
US (2) US7994179B2 (es)
EP (1) EP2234978B1 (es)
JP (1) JP5662803B2 (es)
KR (1) KR20100099738A (es)
CN (1) CN101932562B (es)
AR (1) AR069802A1 (es)
AU (1) AU2008339570B2 (es)
BR (1) BRPI0821274A2 (es)
CA (1) CA2707660A1 (es)
CL (1) CL2008003847A1 (es)
CO (1) CO6290685A2 (es)
CR (1) CR11518A (es)
DO (1) DOP2010000192A (es)
EA (1) EA201001015A1 (es)
EC (1) ECSP10010274A (es)
ES (1) ES2535083T3 (es)
IL (1) IL206045A0 (es)
NI (1) NI201000108A (es)
NZ (1) NZ586104A (es)
PE (1) PE20091682A1 (es)
TW (1) TW200932235A (es)
WO (1) WO2009081195A1 (es)
ZA (1) ZA201003979B (es)

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EP2234978A1 (en) 2010-10-06
BRPI0821274A2 (pt) 2017-06-13
US20090298853A1 (en) 2009-12-03
ECSP10010274A (es) 2010-07-30
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US7994179B2 (en) 2011-08-09
CN101932562B (zh) 2013-06-12
AU2008339570B2 (en) 2012-04-12
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CL2008003847A1 (es) 2009-11-27
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CR11518A (es) 2010-07-15
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US20120108602A1 (en) 2012-05-03
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