CRYSTALLINE MONOHYDRATE OF 3 - {(S) -1- [4- (1-CYCLOPROPYL-2-OXO-1,2-DIHYDROPYRIDIN-4-IL) PHENYL] ETHYL} - (S) -6- (2-HYDROXY- 2-METHYLPROPYL) -6-PHENYL- [1,3] OXAZINAN-2-ONA
Номер патента: PE20120794A1
Опубликовано: 26-07-2012
Автор(ы): Martin Renz, Martin Schuele, Zhenrong Xu
Принадлежит: Boehringer Ingelheim Int, Vitae Pharmaceuticals Inc
Опубликовано: 26-07-2012
Автор(ы): Martin Renz, Martin Schuele, Zhenrong Xu
Принадлежит: Boehringer Ingelheim Int, Vitae Pharmaceuticals Inc
Реферат: SE REFIERE A UN HIDRATO DEL COMPUESTO DERIVADO DE OXAZINAN-2-ONA DE FORMULA (Ip3) Y (Ip1) DONDE G1 ES ALQUILO(C1-C4), ALCOXI(C1-C4), HALOGENO, ENTRE OTROS; G2a ES ALQUILO(C1-C4), HALOALQUILO(C1-C2), CICLOALQUILO(C3-C4), ENTRE OTROS; G2b ES H, METILO O ETILO; R1 ES METILO O ETILO; R2 ES FENILO O FLUOROFENILO; R3 ES 2-HIDROXI-2-METILPROPILO O 2-CIANO-2-METILPROPILO; n ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: (S)-3-((S)-1-(4-(1-CICLOPROPIL-2-OXO-1,2-DIHIDROPIRIDIN-4-IL)FENIL)ETIL)-6-(2-FLUOROFENIL)-6-(2-HIDROXI-2-METILPROPIL)-1,3-OXAZINAN-2-ONA; 2,2-DIMETIL-3-((R)-3-((S)-1-(4-(1-METIL-2-OXO-1,2-DIHIDROPIRIDIN-4-IL)FENIL)ETIL)-2-OXO-6-FENIL-1,3-OXAZINAN-6-IL)PROPANONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE 11B-HIDROXIESTEROIDE DESHIDROGENASA DE TIPO 1 (11B-HSD1) SIENDO UTILES EN EL TRATAMIENTO DE DIABETES REFERS TO A HYDRATE OF THE COMPOUND DERIVED FROM OXAZINAN-2-ONA FROM THE FORMULA (Ip3) AND (Ip1) WHERE G1 IS ALKYL (C1-C4), ALCOXY (C1-C4), HALOGEN, AMONG OTHERS; G2a IS ALKYL (C1-C4), HALOALKYL (C1-C2), CYCLOALKYL (C3-C4), AMONG OTHERS; G2b IS H, METHYL OR ETHYL; R1 IS METHYL OR ETHYL; R2 IS PHENYL OR FLUOROPHENYL; R3 IS 2-HYDROXY-2-METHYLPROPYL OR 2-CYANE-2-METHYLPROPYL; n IS FROM 0 TO 2. PREFERRED COMPOUNDS ARE: (S) -3 - ((S) -1- (4- (1-CYCLOPROPYL-2-OXO-1,2-DIHYDROPYRIDIN-4-IL) PHENYL) ETHYL) -6- (2-FLUOROPHENYL) -6- (2-HYDROXY-2-METHYLPROPYL) -1,3-OXAZINAN-2-ONA; 2,2-DIMETHYL-3 - ((R) -3 - ((S) -1- (4- (1-METHYL-2-OXO-1,2-DIHYDROPYRIDIN-4-IL) PHENYL) ETHYL) -2 -OXO-6-PHENYL-1,3-OXAZINAN-6-IL) PROPANONITRILE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF 11B-HYDROXIESTEROID DEHYDROGENASE TYPE 1 (11B-HSD1), BEING USEFUL IN THE TREATMENT OF DIABETES
Substituted 4-benzyl-3,4-dihydro-2H-benzo[B][1,4]oxazine-2-carboxamide analogs as positive allosteric modulators of muscarinic acetycholine receptor M1
Номер патента: US09708278B2. Автор: Craig W. Lindsley,P. Jeffrey Conn,Shaun R. Stauffer,Joseph D. Panarese. Владелец: VANDERBILT UNIVERSITY. Дата публикации: 2017-07-18.