http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-092607-A1

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filingDate 2013-09-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4f75435b75196c10ca10bcbbc8d83974
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publicationDate 2015-04-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-092607-A1
titleOfInvention PIRROLOPIRIMIDINILAMINO-BENZOTIAZOLONAS REPLACED
abstract Substituted pyrrolopyrimidinylamino-benzothiazolone compounds, methods for preparing said compounds, intermediates useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds to make a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and / or angiogenesis disorder, as the sole agent or in combination with other active ingredients. Claim 1: A compound of the general formula (1), wherein R¹ᵃ represents a hydrogen atom or a halogen atom or a hydroxy-, cyano-, C₁₋₆- alkyl, halo-C₁₋₆ alkyl, C₁ alkoxy ₋₆-, halo C₁₋₆- alkoxy, C₃₋₆ cycloalkyloxy, (3-10 membered heterocycloalkyl) -O-, -NR⁵ᵃR⁵ᵇ, -SCF₃ or -SF₅; R¹ᵇ represents a hydrogen atom or a halogen atom or a hydroxy-, cyano-, C₁₋₆- alkyl, halo C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ halo-alkoxy, C₃ cycloalkyloxy group ₋₆, (3-10 membered heterocycloalkyl) -O-, -NR⁵ᵃR⁵ᵇ, -SCF₃ or -SF₅; R¹ᶜ represents a hydrogen atom or a halogen atom or a hydroxy-, cyano-, C₁₋₆- alkyl, halo-C₁₋₆-alkyl, C alco-alkoxy, C₁₋₆-halo-alkoxy, cycloalkyloxy group C₃₋₆-, (3-10 membered heterocycloalkyl) -O-, -NR⁵ᵃR⁵ᵇ, -SCF₃ or -SF₅; Y represents N or CR²ᵃ; Z represents N or CR²ᵇ; with the proviso that no more than one of Y and Z represents N; R²ᵃ represents a hydrogen atom or a halogen atom or a group selected from: C₁₋₆- alkyl, C₂₋₆ alkenyl, C₂₋₆- alkynyl, C₃₋₆- cycloalkyl, heterocycloalkyl of between 3 and 10 members, 4-10-membered heterocycloalkenyl, aryl-, heteroaryl-, halo-C₁₋₃- alkyl, cyano-, - (CH₂) qX- (CH₂) ₚ-R³; wherein said C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl, 4-10 membered heterocycloalkenyl, aryl- or heteroaryl- groups are optionally substituted, identically or differently, with 1, 2 , 3, 4 or 5 R⁴ groups; R²ᵇ represents a hydrogen atom or a halogen atom or a group selected from: C₁₋₆- alkyl, C₂₋₆ alkenyl, C₂₋₆- alkynyl, C₃₋₆- cycloalkyl, heterocycloalkyl of between 3 and 10 members, 4 to 10 membered heterocycloalkenyl, aryl-, heteroaryl-, halo-C₁₋₃ alkyl, cyano-, - (CH₂) qX- (CH₂) ₂-R³; wherein said C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl, 4-10 membered heterocycloalkenyl, aryl- or heteroaryl-optionally groups are substituted, identically or differently, with 1, 2 , 3, 4 or 5 R⁴ groups; X represents a union or a bivalent group that is selected from: -O-, -S-, -S (= O) -, -S (= O) ₂-, -S (= O) - (NR³ᵃ) -, - (NR³ᵃ) -S (= O) -, -C (= O) -, - (NR³ᵃ) -, -C (= O) -O-, -OC (= O) -, -C (= S) -O-, -OC (= S) -, -C (= O) - (NR³ᵃ) -, - (NR³ᵃ) -C (= O) -, - (NR³ᵃ) -C (= O) - (NR³ᵇ) -, -OC (= O) - (NR³ᵃ) -, - (NR³ᵃ) -C (= O) -O-; R³ represents a hydrogen atom or a group selected from C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl, aryl-, heteroaryl-, halo-C₁₋₃- alkyl; wherein said C₁₋₆- alkyl, C₃₋₆-heterocycloalkyl groups of 3-10 members, aryl heteroaryl- optionally are substituted, identically or differently, with 1, 2, 3, 4 or 5 R⁴ groups; R³ᵃ represents a hydrogen atom or a group selected from C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl, aryl-, heteroaryl-, halo-C₁₋₃- alkyl; wherein said C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl groups, heteroaryl aryl- are optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R⁴ groups; R³ᵇ represents a hydrogen atom or a group selected from C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl, aryl-, heteroaryl-, halo-C₁₋₃ alkyl; wherein said C₁₋₆- alkyl, C₃₋₆- cycloalkyl, 3-10 membered heterocycloalkyl groups, heteroaryl aryl- are optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R⁴ groups; or R³ together with R³ᵃ or R³ᵇ represents a 3-10 membered heterocycloalkyl group or 4-10 membered heterocycloalkenyl, which are optionally substituted, one or more times, identically or differently, with halo-, hydroxyl-, cyano-; R⁴ represents halo-, hydroxy-, oxo- (O =), cyano-, nitro-, C₁₋₆- alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, haloC₁₋₆ alkyl, C₁₋₆ alkoxy -, halo-C₁₋₆-alkoxy, hydroxy-C₁₋₆-alkyl, Cxi-alkoxy-C₁₋₆-alkyl, halo-C₁₋₆-alkoxy-C₁₋₆-alkyl, R⁵-O-, -C (= O) -R⁵, -C (= O) -O-R⁵, -OC (= O) -R⁵, -N (R⁵ᵃ) -C (= O) -R⁵ᵇ, -N (R⁵ᵃ) -C (= O) -NR⁵ᵇR⁵ᶜ, -NR⁵ᵃR⁵ᵇ, -C (= O) -NR⁵ᵃR⁵ᵇ, R⁵-S-, R⁵-S (= O) -, R⁵-S (= O) ₂-, -N (R⁵ᵃ) -S (= O) -R⁵ᵇ, -S (= O) -NR⁵ᵃR⁵ᵇ, -N (R⁵ᵃ) -S (= O) ₂-R⁵ᵇ, -S (= O) ₂-NR⁵ᵃR⁵ᵇ, -S (= O) (= NR⁵ᵃ) R⁵ᵇ, - S (= O) (= NR⁵ᵃ) R⁵ᵇ or -N = S (= O) (R⁵ᵃ) R⁵ᵇ; R⁵ represents a hydrogen atom, a C₁₋₆- alkyl or C₃₋₆- cycloalkyl group; R⁵ᵃ represents a hydrogen atom, a C₁₋₆- alkyl or C₃₋₆- cycloalkyl group; R⁵ᵇ represents a hydrogen atom, a C₁₋₆- alkyl or C₃₋₆- cycloalkyl group; R⁵ᶜ represents a hydrogen atom, a C₁₋₆- alkyl or C₃₋₆- cycloalkyl group; or R⁵ᵃ and R⁵ᵇ together can form a C₂₋₆ alkylene group, in which optionally a methylene can be replaced by -O-, -C (= O) -, -NH-, or -N (C₁₋₄ alkyl) - ; or R⁵ᵃ and R⁵ᶜ together can form a C₂₋₆ alkylene group, in which optionally a methylene can be replaced by -O-, -C (= O) -, -NH-, or -N (C₁₋₄ alkyl) - ; or R⁵ᵇ and R⁵ᶜ together can form a C₂₋₆ alkylene group, in which optionally a methylene can be replaced by -O-, -C (= O) -, -NH-, or -N (C₁₋₄ alkyl) - ; p represents an integer of 0, 1, 2 or 3; q represents an integer of 0, 1, 2 or 3; or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture thereof. Claim 15: A compound of general formula (2), (3) or (4) wherein R²ᵃ and R²ᵇ are as defined in any of claims 1 to 7, PG represents a hydrogen atom or a protecting group and LG Represents an outgoing group.
priorityDate 2012-09-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 34.