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US 7,094,788 B2Granted
Esters of hydroxyl-substituted nitrogen heterocycles, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsMatthias Grauert, Michael P. Pieper, Gerald Pohl, Georg Speck, Steffen Breitfelder
Life of this patent
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Abstract
The present invention relates to new compounds of general formula 1 wherein X− and the groups A, B, R, R1, R2, R3, R3′, R4, R4′, Rx and Rx′ may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharmaceutical compositions.
Claims9
A compound of the formula 1
- wherein:
- X− denotes an anion with a single negative charge;
- A and B denote —CH═CH—;
- R denotes hydrogen, hydroxy, —C1–C4-alkyl, —C1–C4-alkyloxy, —C1–C4-alkylene-halogen, —O—C1–C4-alkylene-halogen, —C1–C4-alkylene-OH, —CF3, CHF2, —C1–C4-alkylene-C1–C4-alkyloxy, —O—COC1–C4-alkyl, —O—COC1–C4-alkylene-halogen, —C1–C4-alkylene-C3–C6-cycloalkyl, —O—COCF3 or halogen;
- R1 and R2 which may be identical or different denote —C1–C5-alkyl, which may optionally be substituted by —C3–C6-cycloalkyl, hydroxy or halogen, or
- R1 and R2 together denote a —C3–C5-alkylene-bridge;
- R3, R4, R3′ and R4′, which may be identical or different denote hydrogen, C1–C4-alkyl, C1–C4-alkyloxy, hydroxy, —CF3, —CHF2, CN, NO2 or halogen;
- and
- Rx and Rx ′ which may be identical or different denote hydrogen, C1–C4-alkyl, C1–C4-alkyloxy, hydroxy, —CF3, —CHF2, CN, NO2 or halogen or
- Rx and Rx ′ together denote a single bond or a bridging group selected from the class of bridges consisting of —O—, —S—, —NH—, —CH2—, —CH2—CH2—, —N(C1–C4-alkyl)-, —CH(C1–C4-alkyl)- and —C(C1–C4-alkyl)2-;
- or an acid addition salt thereof.
8 more elements
A compound of the formula 4
- wherein:
- A and B denote —CH═CH—,;
- R denotes hydrogen, hydroxy, —C1–C4-alkyl, —C1–C4-alkyloxy, —C1–C4-alkylene-halogen, —O—C1–C4-alkylene-halogen, —C1–C4-alkylene-OH, —CF3, CHF2, —C1–C4-alkylene-C1–C4-alkyloxy, —O—COC1–C4-alkyl, —O—COC1–C4-alkylene-halogen, —C1–C4-alkylene-C3–C6-cycloalkyl, —O—COCF3 or halogen;
- R1 and R2 which may be identical or different denote —C1–C5-alkyl, which may optionally be substituted by —C3–C6-cycloalkyl, hydroxy or halogen, or
- R1 and R2 together denote a —C3–C5-alkylene-bridge;
- R3, R4, R3′ and R4′, which may be identical or different denote hydrogen, C1–C4-alkyl, C1–C4-alkyloxy, hydroxy, —CF3, —CHF2, CN, NO2 or halogen;
- and
- Rx and Rx ′ which may be identical or different denote hydrogen, C1–C4-alkyl, C1–C4-alkyloxy, hydroxy, —CF3, —CHF2, CN, NO2 or halogen or
- Rx and Rx ′ together denote a single bond or a bridging group selected from the class of bridges consisting of —O—, —S—, —NH—, —CH2—, —CH2—CH2—, —N(C1–C4-alkyl)-, —CH(C1–C4-alkyl)- and —C(C1–C4-alkyl)2-;
- or an acid addition salts thereof.
7 more elements
Dependencies are inferred from the claim text.