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PE20141307A1 - Aril dihidropiridinona y piperidinona como inhibidores de monoacilglicerol aciltransferasa (mgat2) - Google Patents

Aril dihidropiridinona y piperidinona como inhibidores de monoacilglicerol aciltransferasa (mgat2)

Info

Publication number
PE20141307A1
PE20141307A1 PE2014000853A PE2014000853A PE20141307A1 PE 20141307 A1 PE20141307 A1 PE 20141307A1 PE 2014000853 A PE2014000853 A PE 2014000853A PE 2014000853 A PE2014000853 A PE 2014000853A PE 20141307 A1 PE20141307 A1 PE 20141307A1
Authority
PE
Peru
Prior art keywords
alkyl
aciltransferase
mgat2
piperidinone
inhibitors
Prior art date
Application number
PE2014000853A
Other languages
English (en)
Inventor
Huji Turdi
Jon J Hangeland
Dong Cheng
Saleem Ahmad
Wei Meng
Robert Paul Brigance
Guohua Zhao
R Michael Lawrence
Pratik Devasthale
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20141307A1 publication Critical patent/PE20141307A1/es

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    • 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • 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
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • 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
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • C07D211/84Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
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    • C07D211/84Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ARIL DIHIDROPIRIDINONA Y PIPERIDINONA DE FORMULA (I) DONDE x E y SON UN ENLACE SIMPLE O DOBLE; R1 ES -CONH(ALQUILO C4-C8), -CONHCH2CO-ALQUILO(C2-C8), ENTRE OTROS; R2 ES ALQUILO(C1-C4), CICLOALQUILO(C3-C4) O HALOALQUILO(C1-C4); R3 ES H, F, Cl, CN, ENTRE OTROS; R4 Y R5 SON CADA UNO H, F, Cl O ALQUILO(C1-C4); R6 ES H, HALO, CN, NO2, ENTRE OTROS; R11, R12, R13, R14 Y R15 SON CADA UNO H, HALO, ALCOXI(C1-C4), HALOALQUILO(C1-C4), ENTRE OTROS; R16 ES H O ALQUILO(C1-C4). SON COMPUESTOS PREFERIDOS: (S)-3-(1H-TETRAZOL-5-IL)-4-(p-TOLIL)-6-(4-(4,4,4-TRIFLUOROBUTOXI)FENIL)-6-(TRIFLUOROMETIL)-5,6-DIHIDROPIRIDIN-2(1H)-ONA; (S)-N-(4-METOXIFENIL)-2-OXO-4-(p-TOLIL)-6-(4-(4,4,4-TRIFLUOROBUTOXI)FENIL)-6-(TRIFLUOROMETIL)-1,2,5,6-TETRAHIDROPIRIDIN-3-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE MONOACILGLICEROL ACILTRANSFERASA (MGAT2) SIENDO UTILES EN EL TRATAMIENTO DE DIABETES, RESISTENCIA A LA INSULINA, NEFROPATIA
PE2014000853A 2011-12-02 2012-11-30 Aril dihidropiridinona y piperidinona como inhibidores de monoacilglicerol aciltransferasa (mgat2) PE20141307A1 (es)

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US201161566039P 2011-12-02 2011-12-02
US13/688,584 US8791091B2 (en) 2011-12-02 2012-11-29 Aryl dihydropyridinone and piperidinone MGAT2 inhibitors

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PE20141307A1 true PE20141307A1 (es) 2014-10-01

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