1194-16-7Relevant academic research and scientific papers
NEW PYRIDO[3',2':4,5]FURO[3,2-d]PYRIMIDINE DERIVATIVES
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Page/Page column 27, (2010/11/25)
The present invention provides a pyridofuropyrimidine derivative of formula (I): wherein G1 represents a group selected from -CR6R7- and -O- wherein R6 and R7 independently represent hydrogen atoms or C1-4 alkyl groups; R1 and R2 are independently selected from hydrogen atoms and C1-4 alkyl groups; R3 represents a group selected from C1-4 alkyl, C1-4 alkoxy, amino, hydroxy, mono- C1-4 alkylamino, di- C1-4 alkylamino, C3-8 cycloalkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups which are bound to the pyridine ring through their nitrogen atom, all of them being optionally substituted by one or more substituents selected from the group consisting of halogen atoms and hydroxy, C1-4 alkyl, C1-4 alkoxy- C1-4 alkyl, aryl-C1-4 4alkyl, -O(CO)O R8, C1-4 alkoxy, -(CO)NR8R9, -CN, -CF3, -NR8R9, -SR8 and -SO2NH2 groups wherein R8 and R9 each independently represent a hydrogen atom or a C1-4 alkyl group; R4 and R5 are independently selected from the group consisting of hydrogen atoms, C1-4 alkyl groups, hydroxyl- C1-4 alkyl groups and groups of formula (II): wherein p and q are integers selected from 0, 1 , 2 and 3; A is either a direct bond or a group selected from -CONR14-, -NR14CO-, -0-, -COO-, -OCO-, -S-, -SO- and -SO2-, wherein each R10, R11, R12, R13 and R14 independently represents a hydrogen atom or a C1-4 alkyl group and G2 is a group selected from aryl, heteroaryl or heterocyclyl groups; wherein the group G2 is optionally substituted by one or more substituents selected from group consisting of halogen atoms and C1-4 alkyl, hydroxy, oxo, C1-4 alkoxy- C1-4 alkyl, aryl- C1-4 alkyl, -(CO)OR16, C1-4 alkoxy, -(CO)NR16R17, -CN, -CF3, -NR16R17, -SR16 and -SO2NH2 groups; wherein R16 and R17 each independently represent a hydrogen atom or a C1-4 alkyl group and the pharmaceutically acceptable salts and N-oxides thereof.
NEW PYRIDOTHIENOPYRIMIDINE DERIVATIVES
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Page/Page column 30, (2008/06/13)
Use of a pyrido[3',2':4,5]thieno[3,2-d]pyrimidine derivative of formula (I), wherein n is an integer selected from 0 or 1 R1 and R2 are independently selected from hydrogen atoms and C1-4 alkyl groups R3 represe
4(SPIROPIPERIDINYL)METHYL SUBSTITUTED PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page 58-59, (2010/02/07)
3-Substituted pyrrolidines having a spiropiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER, COMPOSITIONS THEREOF AND METHODS THEREWITH
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Page 52, (2008/06/13)
The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.
Synthesis and biological activity of a novel class of pyridazine analogues as non-competitive reversible inhibitors of protein tyrosine phosphatase 1B (PTP1B).
Liljebris, Charlotta,Martinsson, Jessica,Tedenborg, Lars,Williams, Meredith,Barker, Emma,Duffy, James E S,Nygren, Alf,James, Stephen
, p. 3197 - 3212 (2007/10/03)
A series of novel pyridazine analogues were prepared and the structure-activity relationship of their behavior as inhibitors of PTP1B was evaluated. Most of the analogues had potencies in the low micromolar range. The in vitro kinetics of this compound series demonstrated that they were reversible non-competitive binders. This indicates that there may exist another site in the enzyme through which enzyme activity can be inhibited, which is not a recognized interaction domain. Some of the analogues exhibited high selectivity for other PTPases, for example, compound 12 mp showed 20-fold selectivity for PTP1B (IC50=5.6 microM) versus both TCPTP and LAR (>100 microM, respectively). In contrast to many tyrosine phosphatase mimetic inhibitors, this compound class lacks negative charge and thus showed high permeability across cell membranes. Selective analogues in the series were analyzed in an in vitro cellular assay, which showed increased insulin-stimulated insulin receptor phosphorylation.
DIARYL ETHER HETROCYCLES
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, (2008/06/13)
The invention concerns a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, wherein Ar1 is optionally substituted phenyl or naphthyl; X1 is oxy, thio, sulphinyl or sulphonyl; Ar2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms; Rl is (l-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(l-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and R2 and R3 together form a group of the formula ?A2?X2?A3? wherein each of A2 and A3 is (l-4C) alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino. The invention also concerns processes for the manufacture of a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said heterocycle. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
HETEROCYCLES FOR USE AS INHIBITORS OF LEUKOTRIENES
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, (2008/06/13)
The invention concerns a heterocycle of the formula I wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms; A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene; X is oxy, thio, sulphinyl, sulphonyl or imino; Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms; R 1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and R 2 and R 3 together form a group of the formula --A 2 --X 2 --A 3 -- which, together with the carbon atom to which A 2 and A 3 are attached, defines a ring having 4 to 7 ring atoms, wherein A 2 and A 3, which may be the same or different, each is (1-4C)alkylene and X 2 is oxy, thio, sulphinyl, sulphonyl or imino; or a pharmaceutically-acceptable salt thereof. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
HETEROCYCLIC DERIVATIVES
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, (2008/06/13)
The invention concerns a heterocyclic derivative of the formula I, or a pharmaceutically-acceptable salt there of. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
Diaryl ether heterocycles
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, (2008/06/13)
The invention concerns a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, wherein Ar1 is optionally substituted phenyl or naphthyl;, X1 is oxy, thio, sulphinyl or sulphonyl;, Ar2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;, R1 is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and, R2 and R3 together form a group of the formula -A2-X2-A3- wherein each of A2 and A3 is (1-4C)alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino. The invention also concerns processes for the manufacture of a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said heterocycle. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
