105679-22-9Relevant articles and documents
INHIBITORS OF HIF PROLYL HYDROXYLASE
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Page/Page column 94, (2016/04/20)
The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
Perry, Benjamin,Alexander, Rikki,Bennett, Gavin,Buckley, George,Ceska, Tom,Crabbe, Tom,Dale, Verity,Gowers, Lewis,Horsley, Helen,James, Lynwen,Jenkins, Kerry,Crepy, Karen,Kulisa, Claire,Lightfoot, Helen,Lock, Chris,Mack, Stephen,Morgan, Trevor,Nicolas, Anne-Lise,Pitt, Will,Sabin, Verity,Wright, Sara
scheme or table, p. 4700 - 4704 (2009/04/08)
The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
Dihydro-benzo(1,4)oxazines
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Page/Page column 334, (2010/01/31)
The invention is directed to physiologically active compounds of formula (I): wherein R1represents R3—Z3—, R3—L2—R4—Z3—, R3—L3—Ar1—L4—Z3— or R3—L3—Ar1—L2—R4—Z3—; R2represents hydrogen, halogen, lower alkyl or lower alkoxy; A1represents a straight chain C2-3alkylene linkage optionally substituted by one or more groups chosen from alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, imino, oxo, thioxo, or alkyl substituted by —ZR6, —NY1Y2, —CO2R6or —C(═O)—NY1Y2; L1represents a direct bond; an alkenylene, alkylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage each optionally substituted by (a) an acidic functional group, cyano, oxo, —S(O)mR9, R3, —C(═O)—R3, —C(═O)—OR3, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R8)—SO2—R9, —NY4Y5or —[C(═O)—N(R10)—C(R5)(R11)]p—C(═O)—NY4Y5, or by (b) alkyl substituted by an acidic functional group, or by S(O)mR9, —C(═O)—NY4Y5or —NY4Y5; a —[C(═O)—N(R10)—C(R5)(R11)]p— linkage; a —Z2—R12— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R12—Z2—R12— linkage; a —C(R4)(R13)—[C(═O)—N(R10)—C(R5)(R11)]p— linkage; or a —L5—L6—L7— linkage; Z1is NR17or O; Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).