AR078673A1 - Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826 - Google Patents

Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826

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Publication number
AR078673A1
AR078673A1 ARP100103811A ARP100103811A AR078673A1 AR 078673 A1 AR078673 A1 AR 078673A1 AR P100103811 A ARP100103811 A AR P100103811A AR P100103811 A ARP100103811 A AR P100103811A AR 078673 A1 AR078673 A1 AR 078673A1
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AR
Argentina
Prior art keywords
carboxamide
pyrimidin
hydroxiadamantan
cyclopentyl
amino
Prior art date
Application number
ARP100103811A
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English (en)
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Astrazeneca Ab
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.)
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Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR078673A1 publication Critical patent/AR078673A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

También se describen su uso en la inhibicion de 11betaHSD1, los procesos para prepararlos y las composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable de este donde R1 es trifluorometilo, propilo, ciclobutilo, ciclopentilo, etoxi, propoxi, ciclobutoxi, pirrolidinilo o pirazolilo; R2 es tetrahidrofuranilo, 1-acetilpiperidilo, oxopiperidilo, dioxotiolanilo, hidroxiciclopentilo, hidroxietilo, hidroxipropilo, 2-(dimetilamino)-2-oxoetilo, metoxietilo, oxopirrolidinilo, 1-acetilpirrolidinilo, oxetanilo, hidroxidimetiletilo, 1,1-dioxotianilo, tetrahidropiranilo, (tetrahidrofuranil)metilenilo, (oxopirrolidinil)metilenilo, (metiloxopirrolidinil)metilenilo o pirrolidinilo; R3 es hidroxi, carboxi, carbamoílo o metilsulfonilo; R4 es hidrogeno o metilo; con la condicion de que dicho compuesto no sea: 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[(2-hidroXi-1,1-dimetiletil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxietil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxi-2-metilpropil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-(oxetan-3-ilamino)pirimidin-5- carboxamida; 4-ciclobutil-2-[(1,1-dioxidotetrahidro-2H-tiopiran-4-il)amino]-N-[(2r,5s)-5-hidroxiadamantan-2-il]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2-r,5s)-5-hidroxiadamantan-2-il]-2-oxetan-3-ilamino)pirimidin-5-carboxamida; 4-ciclopentil-2-[(1,1-dioxotian-4-il)amino]-N-[(2r,5s)-5-hidroxiadamantan-2-il]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxi-2-metilpropil)amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-(2-hidroxietilamino)pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r5s)-5-hidroxiadamantan-2-il]-2-[(1-hidroxi-2-metilpropan-2-il)amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-(oxan-4-ilamino)pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[[(3R)-oxolan-3-il]amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[[(3S)-oxolan-3-il]amino]pirimidin-5-carboxamida; 4-etoxi-N-[(2r,5s)-5-hidroxitriciclo[3.3.1.13,7]dec-2-il]-2-(oxetan-3-ilamino)pirimidin-5-carboxamida; o N-[(2r,5s)-5-hidroxitriciclo[3.3.1.13,7]dec-2-il]-4-(1-metiletoxi)-2-(oxetan-3-ilamino)pirimidin-5-carboxamida.
ARP100103811A 2009-10-20 2010-10-19 Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826 AR078673A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US25319109P 2009-10-20 2009-10-20

Publications (1)

Publication Number Publication Date
AR078673A1 true AR078673A1 (es) 2011-11-23

Family

ID=43879772

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103811A AR078673A1 (es) 2009-10-20 2010-10-19 Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826

Country Status (5)

Country Link
US (1) US20110092526A1 (es)
AR (1) AR078673A1 (es)
TW (1) TW201118085A (es)
UY (1) UY32954A (es)
WO (1) WO2011049520A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200827346A (en) * 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
TW200836719A (en) * 2007-02-12 2008-09-16 Astrazeneca Ab Chemical compounds
AU2009211215B2 (en) * 2008-02-04 2011-11-03 Astrazeneca Ab Novel crystalline forms of 4- [4- (2-adamantylcarbam0yl) -5-tert-butyl-pyrazol-1-yl] benzoic acid
JP2011518216A (ja) * 2008-04-22 2011-06-23 アストラゼネカ アクチボラグ 置換ピリミジン−５−カルボキサミド
CN103649066B (zh) * 2011-06-10 2016-08-17 爱思开生物制药株式会社 5-氨甲酰基-金刚烷-2-基酰胺衍生物、其药学上可接受的盐及其制备方法
EP3235813A1 (en) 2016-04-19 2017-10-25 Cidqo 2012, S.L. Aza-tetra-cyclo derivatives
KR102006547B1 (ko) * 2017-11-16 2019-08-01 서울대학교산학협력단 벤즈아미드 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 염증질환의 치료 또는 예방용 약학적 조성물

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE482747T1 (de) * 2003-04-11 2010-10-15 High Point Pharmaceuticals Llc Neue amide derivate und deren pharmazeutische verwendungen
US20050245534A1 (en) * 2004-04-29 2005-11-03 Link James T Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
TW200827346A (en) * 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
JP2011518216A (ja) * 2008-04-22 2011-06-23 アストラゼネカ アクチボラグ 置換ピリミジン−５−カルボキサミド

Also Published As

Publication number Publication date
US20110092526A1 (en) 2011-04-21
TW201118085A (en) 2011-06-01
UY32954A (es) 2011-05-31
WO2011049520A1 (en) 2011-04-28

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