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US 8,710,055 B2Granted
Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
AssigneeBoehringer Ingelheim International GmbH
InventorSteffen Steurer
Life of this patent
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Abstract
The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
Claims37
A compound of the formula (I)
- wherein
- R2 is a group optionally substituted by one or more, identical or different Rb1 and/or Rc1, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-10aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl or R2 is —NRc1Rc1;
- each Rb1 is independently selected from among —ORc1, —NRc1Rc1, halogen, —CN, —C(O)Rc1, —C(O)ORc1, —C(O)NRc1Rc1, —S(O)2Rc1, —S(O)2NRc1Rc1, —NHC(O)Rc1 and —N(C1-4alkyl)C(O)Rc1 as well as the bivalent substituent ═O, wherein the latter may only be a substituent in non-aromatic ring systems;
- each Rc1 independently of one another denotes hydrogen or a group selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-10aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl;
- R3 is selected from among hydrogen, halogen, C1-4alkyl, C1-4alkyloxy, C2-4alkenyl, C2-4alkynyl, C1-4haloalkyl, —CN, —NH(C1-4alkyl) and —N(C1-4alkyl)2;
- ring A is a 5-10 membered heteroaryl;
- m denotes the number 0, 1 or 2;
- each R4 independently of one another denotes a group optionally substituted by one or more, identical or different Ra2 and/or Rb2, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-10aryl, 5-10 membered heteroaryl and 3-11 membered heterocyclyl, or is independently selected from among —ORa3, —NRa3Ra3, —N(ORa3)Ra3, halogen, —CN, —C(O)Ra3, —C(O)ORa3, —C(O)NRa3Ra3, —C(NH)NRa3Ra3, —S(O)2Ra3, —S(O)2NRa3Ra3, —NHC(O)Ra3 and —N(C1-4alkyl)C(O)Ra3
- each Ra2 independently of one another denotes a group optionally substituted by one or more, identical or different Rb2 and/or Rc2, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-6cycloalkyl, C4-6cycloalkenyl and 3-10 membered heterocyclyl;
- each Rb2 is independently selected from among —ORc2, —NRc2Rc2, halogen, —C(O)Rc2, —C(O)ORc2, —C(O)NRc2Rc2, —CN, —NHC(O)Rc2 and —NHC(O)ORc2;
- each Rc2 independently of one another denotes hydrogen or a group selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C4-6cycloalkenyl and 3-10 membered heterocyclyl, wherein this heterocyclyl is optionally substituted by one or more, identical or different substituents selected from among halogen, C1-6alkyl and —C(O)—C1-6alkyl;
- each Ra3 independently of one another denotes hydrogen or a group optionally substituted by one or more, identical or different Rb3 and/or Rc3, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-6cycloalkyl, C4-6cycloalkenyl and 3-10 membered heterocyclyl;
- each Rb3 is independently selected from among —ORc3, —NRc3Rc3, halogen, —C(O)Rc3, —C(O)ORc3, —C(O)NRc3Rc3, —CN, —NHC(O)Rc3 and —NHC(O)ORc3;
- each Rc3 independently of one another denotes hydrogen or a group selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C4-6cycloalkenyl, C1-6alkyl-O—C1-6alkyl, (C1-4alkyl)HN—C1-6alkyl, (C1-4alkyl)2N—C1-6alkyl, C1-6haloalkyl, 4-16 membered heterocyclylalkyl and 3-10 membered heterocyclyl, wherein the heterocyclyl ring in aforementioned groups is optionally substituted by one or more, identical or different C1-6alkyl;
- X denotes chlorine or fluorine;
- wherein the compounds (I) may optionally also be present in the form of the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof or as the respective salts of all the above-mentioned forms.
13 more elements
A compound, or pharmaceutically acceptable salts thereof, selected from among:
Dependencies are inferred from the claim text.