Patent number: 9801961
Abstract: The present invention relates to compounds of general formula wherein R1 is (a) phenyl, optionally substituted by one or two substituents selected from 3H, halogen, lower alkyl, di-methyl-amino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(3H)3, O11CH3, OCH2CH218F, lower alkoxy substituted by halogen, hydroxy, lower alkyl substituted by hydroxy, S-lower alkyl, (b) heterocyclyl group, (c) benzo[d][1,3]dioxol-5-yl, (d) 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, (e) indolin-2-one, or (f) heteroaryl, selected from the group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl, and benzothiazolyl; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is lower alkyl, C(3H)3, 11CH3, lower alkyl substituted by halogen, —(CH2)2—O-lower alkyl substituted by halogen or cycloalkyl; or R2 and R3 form together with the N-atom to which they are attach a ring containing —CH2CH2CHRCH2CH2—, —CH2CH2CHRCH2—, —CH2CHRCH2—, —CH2CH2—NR—CH2CH2—, —CH2CH2—O—CH2CH2—, or, R is hydrogen, halog
Type:
Grant
Filed:
November 19, 2015
Date of Patent:
October 31, 2017
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Luca Gobbi, Henner Knust, Matthias Koerner, Dieter Muri
Publication number: 20170128598
Abstract: The present invention relates to compounds of general formula wherein R1 is (a) phenyl, optionally substituted by one or two substituents selected from 3H, halogen, lower alkyl, di-methyl-amino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(3H)3, O11CH3, OCH2CH218F, lower alkoxy substituted by halogen, hydroxy, lower alkyl substituted by hydroxy, S-lower alkyl, (b) heterocyclyl group, (c) benzo[d][1,3]dioxol-5-yl, (d) 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, (e) indolin-2-one, or (f) heteroaryl, selected from the group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl, and benzothiazolyl; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is lower alkyl, C(3H)3, 11CH3, lower alkyl substituted by halogen, —(CH2)2—O-lower alkyl substituted by halogen or cycloalkyl; or R2 and R3 form together with the N-atom to which they are attach a ring containing —CH2CH2CHRCH2CH2—, —CH2CH2CHRCH2—, —CH2CHRCH2—, —CH2CH2—NR—CH2CH2—, —CH2CH2—O—CH2CH2—, or, R is hydrogen, haloge
Type:
Application
Filed:
November 19, 2015
Publication date:
May 11, 2017
Applicant:
HOFFMANN-LA ROCHE INC.
Inventors:
Luca Gobbi, Henner Knust, Matthias Koerner, Dieter Muri
Publication number: 20160244441
Abstract: The invention relates to compounds of formulas I and II wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH2)2-lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH2-lower alkoxy, CH2-lower alkoxy substituted by halogen or hydroxy; or R1 and R2 form together with the carbon atoms to which they are attached a ring containing —OCH2CH2O—, OCH2O—, OCH2CH2CH2O— or —NHC(O)CH2O—; R3 is hydrogen or lower alkoxy; R4 is hydrogen or lower alkyl; R5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R4 and R5 form together with the nitrogen at
Type:
Application
Filed:
October 28, 2015
Publication date:
August 25, 2016
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Edilio Borroni, Luca Gobbi, Michael Honer, Henner Knust, Matthias Koerner, Dieter Muri