1072009-08-5Relevant academic research and scientific papers
THIENOPYRIMIDIENE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 60-61, (2009/05/28)
Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
PURINE DERIVATIVES USEFUL AS PI3 KINASE INHIBITORS
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Page/Page column 46; 62-63, (2009/05/28)
This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arisi from abnormal cell growth, function or behaviour associated with PI3 kinase such as cance immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
QUINAZOLINE DERIVATIVES AS PI3 KINASE INHIBITORS
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Page/Page column 33, (2009/01/24)
The invention provides a compound which is a quinazoline of formula (I): and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and
2-MORPHOLIN-4-YL-PYRIMIDINES AS PI3K INHIBITORS
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Referential example 10, (2008/12/08)
The invention provides compounds which are pyrimidines of formula (I) wherein R1 is a group -NR-(CHR)m-X; R2 is a substituted indolyl group; R is H or C1-C6 alkyl; m is 1, 2, 3 or 4; and X is a pyridyl ring; and the pharmaceutically acceptable salts thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 21; 34, (2008/12/08)
The invention provides compounds which are pyrimidines of formula (I): wherein R2 is bonded at ring position 2 and -YR1 is bonded at ring position 5 or 6, or YR1 is bonded at ring position 2 and R2 is bonded at ring position 6; R is an indol-4-yl group which is substituted at the 5- or 6-position; either: (a) Y is selected from -O-(CH2)n-, -NH-(CH2)n-,. -NHC(O)-(CH2)n and -C(O)NH-(CH2)n- wherein n is 0 or an integer of 1 to 3, and R1 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group -NR3R4 wherein R3 and R4, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3 - C10 cycloalkyl which is unsubstituted or substituted, -C(O)R, -C(O)N(R)2 and -S(O)mR, or R3 and R4 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted; (b) Y is a direct bond and R1 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted, and a group -NR3R4 wherein R3 and R4, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3-C10 cycloalkyl which is unsubstituted or substituted, -C(O)R, -C(O)N(R)2 and -S(O)mR; R is selected from H, C1-C6 alkyl, C3-C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, which group is unsubstituted or substituted; and m is 1 or 2; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PO K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PB kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 28; 43, (2008/12/08)
The invention provides a compound which is a pyrimidine of formula (I): The compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
PHARMACEUTICAL COMPOUNDS
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, (2009/01/24)
Furanopyrimidines of formula (I): wherein W represents a furan ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is selected from: (a) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O, the ring being fused to a second ring selected from a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, a 5- to 12-membered unsaturated heterocyclic ring, a 5- to 7-membered saturated O-containing heterocyclic ring, a 3- to 12- membered saturated carbocyclic ring and an unsaturated 5- to 12- membered carbocyclic ring to form a heteropolycyclic ring system, the heteropolycyclic ring system being unsubstituted or substituted; (b) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and which further comprises, linking two constituent atoms of the ring, a bridgehead group selected from -(CR'2)n- and -(CR'2)r-O-(CR'2)s- wherein each R' is independently H or C1 - C6 alkyl, n is 1, 2 or 3, r is 0 or 1 and s is 0 or 1, the remaining ring positions being unsubstituted or substituted; and (c) a group of formula (IIb): wherein ring B is a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and ring B' is a 3- to 12- membered saturated carbocyclic ring, a 5- to 7- membered saturated O-containing heterocyclic ring or a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, each of B and B' being unsubstituted or substituted; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; R4 is an indole group which is unsubstituted or substituted; and Ra is selected from R, halo, CN, C(O)NR2, halo(C1-C6)alkyl, SO2R, SO2NR2, NRSO2R, NRC(O)R, NRC(O)OR and NRC(O)NR2 wherein each R is independently H or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
THIAZOLIOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE
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, (2009/01/24)
Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; Rsup
PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 74, (2008/06/13)
Thienopyrimidines of formula (Ia) or (Ib): wherein R1, R2, R3, are as defined in the claims.
