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
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 4- (4,4,4-TRIFLUOROBUTOXY) PHENYL Chemical class 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non 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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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D211/84—Heterocyclic 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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- C07D211/84—Heterocyclic 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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- C07F9/40—Esters thereof
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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
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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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 |
Publications (1)
Publication Number | Publication Date |
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PE20141307A1 true PE20141307A1 (es) | 2014-10-01 |
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PE2014000853A PE20141307A1 (es) | 2011-12-02 | 2012-11-30 | Aril dihidropiridinona y piperidinona como inhibidores de monoacilglicerol aciltransferasa (mgat2) |
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JP (2) | JP5806417B2 (es) |
KR (2) | KR101666729B1 (es) |
CN (2) | CN107266416B (es) |
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HR (1) | HRP20161011T1 (es) |
HU (1) | HUE030547T2 (es) |
IL (1) | IL232727A (es) |
IN (1) | IN2014CN03803A (es) |
MA (1) | MA35753B1 (es) |
MX (1) | MX355988B (es) |
MY (1) | MY173478A (es) |
PE (1) | PE20141307A1 (es) |
PH (1) | PH12014501162B1 (es) |
PL (1) | PL2785693T3 (es) |
PT (1) | PT2785693T (es) |
RS (1) | RS54985B1 (es) |
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SI (1) | SI2785693T1 (es) |
SM (1) | SMT201600272B (es) |
TN (1) | TN2014000238A1 (es) |
TW (1) | TWI636044B (es) |
WO (1) | WO2013082345A1 (es) |
ZA (1) | ZA201404867B (es) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
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US8791091B2 (en) * | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
BR112015010649A2 (pt) | 2012-11-16 | 2017-07-11 | Bristol Myers Squibb Co | moduladores de gpr40 à base de pirrolidina |
BR112015011031A2 (pt) | 2012-11-16 | 2017-07-11 | Bristol Myers Squibb Co | moduladores de grp40 de di-hidropirazol |
SG11201503562PA (en) | 2012-11-16 | 2015-06-29 | Bristol Myers Squibb Co | Dihydropyrazole gpr40 modulators |
PL2920165T3 (pl) | 2012-11-16 | 2017-04-28 | Bristol-Myers Squibb Company | Dihydropirazolowe modulatory gpr40 |
MX2015006516A (es) | 2012-11-29 | 2015-08-14 | Merck Patent Gmbh | Derivados de azaquinolin-carboxamida. |
AU2014274354A1 (en) | 2013-05-29 | 2016-01-28 | Bristol-Myers Squibb Company | Dihydropyridinone MGAT2 inhibitors |
SMT201900256T1 (it) | 2014-03-07 | 2019-07-11 | Bristol Myers Squibb Co | Inibitori dell'mgat2 diidropiridinonici sostituiti con tetrazolone |
JP6498705B2 (ja) * | 2014-03-07 | 2019-04-10 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 代謝障害の治療に用いるためのジヒドロピリジノンmgat2阻害剤 |
EP3154944B1 (en) | 2014-06-11 | 2018-03-14 | Bristol-Myers Squibb Company | Substituted pyridinones as mgat2 inhibitors |
KR101750392B1 (ko) * | 2014-12-03 | 2017-06-26 | 한국도로공사 | 교량 점검용 거더의 유도 레일장치 및 그 교량 점검장치 |
WO2017069224A1 (ja) * | 2015-10-22 | 2017-04-27 | 塩野義製薬株式会社 | Mgat2阻害活性を有するスピロ環誘導体 |
WO2017110841A1 (ja) * | 2015-12-21 | 2017-06-29 | 塩野義製薬株式会社 | Mgat2阻害活性を有する非芳香族複素環誘導体 |
EP3301094A1 (en) * | 2016-09-30 | 2018-04-04 | Mutabilis | Heterocyclic compounds and their use in preventing or treating bacterial infections |
JP2020158390A (ja) * | 2017-06-20 | 2020-10-01 | 塩野義製薬株式会社 | Mgat2阻害活性を有する非芳香族複素環誘導体およびそれらを含有する医薬組成物 |
TWI782056B (zh) * | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
CN107759498A (zh) * | 2017-11-08 | 2018-03-06 | 南京大学 | 抗肿瘤化合物、制备方法及其用途 |
BR112021012428A2 (pt) | 2019-01-11 | 2021-09-08 | Shionogi & Co., Ltd. | Derivado de dihidropirazolopirazinona tendo atividade inibitória de mgat2 |
JP7413346B2 (ja) | 2019-03-06 | 2024-01-15 | 第一三共株式会社 | ピロロピラゾール誘導体 |
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US3073838A (en) * | 1963-01-15 | Derivatives of hydkogenateb pyridones | ||
US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
AU2005286648A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
US8344132B2 (en) * | 2005-06-22 | 2013-01-01 | BioCryst Pharmaceticals, Inc. | Methods for the preparation of 9-deazapurine derivatives |
EP2078719A4 (en) * | 2006-09-28 | 2009-11-11 | Dainippon Sumitomo Pharma Co | COMPOUND WITH BICYCLIC PYRIMIDINE STRUCTURE AND THE COMPOUND CONTAINING PHARMACEUTICAL COMPOSITION |
US8232447B2 (en) | 2007-01-31 | 2012-07-31 | Msd K.K. | Animal having modification in MGAT2 gene |
AU2010216633A1 (en) | 2009-02-23 | 2011-09-08 | Msd K.K. | Pyrimidin-4(3H)-one derivatives |
WO2012124744A1 (ja) | 2011-03-14 | 2012-09-20 | 大正製薬株式会社 | 含窒素縮合複素環化合物 |
US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
JP6498705B2 (ja) | 2014-03-07 | 2019-04-10 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 代謝障害の治療に用いるためのジヒドロピリジノンmgat2阻害剤 |
SMT201900256T1 (it) | 2014-03-07 | 2019-07-11 | Bristol Myers Squibb Co | Inibitori dell'mgat2 diidropiridinonici sostituiti con tetrazolone |
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