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US 2016/0108026 A1Published application
Aldosterone synthase inhibitors
AssigneeBoehringer Ingelheim International GmbH
InventorsKeith R. HORNBERGER, Kenneth Michael MEYERS, Peter Allen NEMOTO, Simon SURPRENANT, Hui YU
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Abstract
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3, are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Claims13
A compound of the formula I
- wherein:
- R1 is selected from —C(O)NH2, —C(O)NH(CH3) and —CN;
- R2 is —(X)—R4, wherein
- —(X)— is a bond, —CH2—, or —O—;
- and
- R4 is selected from
- —H;
- C1-3alkyl, optionally substituted with one to four groups selected from —F and —OH;
- halogen;
- —CN;
- —SO2C1-3alkyl;
- —C(O)N(C1-3alkyl)2, provided —(X)— is not —O—;
- —NHC(O)R5 or —N(CH3)C(O)R5, provided that —(X)— is —CH2— and wherein R5 is selected from C3-6cycloalkyl and C1-3alkyl optionally substituted with one to three —F groups;
- —NHSO2C1-3alkyl;
- —CH(cyclopropyl)NHSO2C1-3alkyl;
- —OCH2C(O)N(C1-3alkyl)2, provided that —(X)— is —CH2—;
- —S(═O)(═NH)CH3, provided that —(X)— is —CH2—;
- heterocyclyl selected from tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, 1,1-dioxo[1,2]-thiazine, morpholinyl, oxazolidinyl, piperidinyl, azetidinyl, wherein said heterocyclyl is optionally substituted with one to three groups selected from —C(O)C1-3alkyl, halogen, —OH, oxo and C1-3alkyl;
- —C(O)-heterocyclyl, provided that —(X)— is —CH2, wherein said heterocyclyl is selected from morpholin-4-yl, pyrrolidin-1-yl and piperidin-1-yl, optionally substituted with one or two groups selected from —F and —OH;
- C3-6cycloalkyl optionally substituted with —CN or —OH;
- and
- phenyl, optionally substituted with —SO2NH2;
- and
- R3 is H, or C1-3alkyl optionally substituted with —OH;
- or
- R2 and R3 together form an annelated five-membered cycloalkyl ring optionally substituted with —OH;
- or a salt or a stereoisomer thereof.
24 more elements
Dependencies are inferred from the claim text.