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US 2012/0238542 A1Published application
Aminopyrazoloquinazolines
AssigneeBoehringer Ingelheim International GmbH
InventorMatthias Treu
Life of this patent
Estimating the term…
Abstract
Compounds of general formula (I) wherein the groups R1 to R3 and X 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 such compounds and their use as medicaments.
Claims44
A compound of the formula (I)
- wherein
- R1 denotes hydrogen or a group optionally substituted by one or more identical or different Ra and/or Rb, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl;
- R2 denotes hydrogen or a group optionally substituted by one or more identical or different Ra and/or Rb, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl;
- R3 denotes a group
- A is selected from among C6-10aryl and 5-12 membered heteroaryl;
- B denotes a 5- to 7-membered, non-aromatic hetero ring with at least one heteroatom, selected from among nitrogen, sulphur and oxygen, which optionally carries one or more substituents selected from among C1-6alkyl and ═O;
- each R4 is independently selected from among Ra and Rb;
- m denotes 0, 1, 2 or 3;
- R5 is selected from among Ra and Rb;
- n denotes 0 or 1;
- X denotes a bond or is selected from among —CH2— and —CH2—CH2— and in the above-mentioned —CH2— and —CH2—CH2— one or two hydrogen atoms are optionally substituted independently of one another by C1-4alkyl, C1-4haloalkyl, —O—C1-4alkyl or halogen;
- each Ra independently denotes a group optionally substituted by one or more identical or different Rb and/or Rc, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl;
- each Rb is independently selected from among —ORc, —SRc, —NRcRc, halogen, —CN, —NO2, —C(O)Rc, —C(O)ORc, —C(O)NRcRc, —C(NRh)NRcRc, —OC(O)Rc, —OC(O)ORc, —S(O)2Rc, —S(O)2NRcRc, —NRhC(O)Rc, —NRhC(O)ORc, —NRhC(O)NRcRc, —NRhC(NRh)NRcRc and —NRhS(O)2Rc, as well as the bivalent substituent ═O, while the latter may only be a substituent in non-aromatic ring systems;
- each Rc independently denotes hydrogen or a group optionally substituted by one or more identical or different Rd and/or Re, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl;
- each Rd is independently selected from among —ORe, —SRe, —NReRe, halogen, —CN, —NO2, —C(O)Re, —C(O)ORe, —C(O)NReRe, —C(NRh)NReRe, —OC(O)Re, —OC(O)ORe, —S(O)2Re, —S(O)2NReRe, —NRhC(O)Re, —NRhC(O)ORe, —NRhC(O)NReRe, —NRhC(NRh)NReRe and —NRhS(O)2Re, as well as the bivalent substituent ═O, while the latter may only be a substituent in non-aromatic ring systems;
- each Re independently denotes hydrogen or a group optionally substituted by one or more identical or different Rf and/or Rg, selected from among C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-10cycloalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl;
- each Rf is independently selected from among —ORg, —SRg, —NRgRg, halogen, —CN, —NO2, —C(O)Rg, —C(O)ORg, —C(O)NRgRg, —C(NRh)NRgRg, —OC(O)Rg, —OC(O)ORg, —S(O)2Rg, —S(O)2NRgRg, —NRhC(O)Rg, —NRhC(O)ORg, —NRhC(O)NRgRg, —NRhC(NRh)NRgRg and —NRhS(O)2Rg, as well as the bivalent substituent ═O, while the latter may only be a substituent in non-aromatic ring systems;
- each Rg is independently selected from among hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-10cycloalkyl, C4-10cycloalkylalkyl, C4-10cycloalkenyl, C6-10aryl, 5-12 membered heteroaryl and 3- to 14-membered heterocyclyl, and
- each Rh is independently selected from among hydrogen and C1-6alkyl,
- or a tautomer or salt thereof.
17 more elements
Dependencies are inferred from the claim text.