Abstract: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the formula IA and IB.

Abstract: A dye-forming coupler of formula (I), a silver halide photographic light-sensitive material containing the coupler, and an azomethine dye compound derived from the coupler: wherein Q is a residue that forms, together with the —N—C?N— moiety, a nitrogen-containing 6-membered ring; RA is a certain alkyl group having at least 7 carbon atoms, or -L-R1; X is an aryl group; Y is a hydrogen atom, or a group capable of being split-off upon a coupling reaction; wherein, when RA is -L-R1, L is a divalent linking group, and R1 is a substituent; and -L-R1 does not represent an alkyl, alkenyl, alkynyl, or aryl group, and -L-R1 does not represent a heterocyclic group that bonds, with a carbon atom therein, to the nitrogen atom of the nitrogen-containing 6-membered ring formed by Q and the —N—C?N— moiety.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is

Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compnounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.

Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.

Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided

Abstract: The invention relates to the use of compounds of the formula I: wherein: ring C is a 5-6 membered heterocyclic moiety; Z is —O—, —S—, or —CH2—; R1 is hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4)alkoxy)methyl, C1-4alkanoyl, trifluoromethyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, carboxy, C3-7cycloalkyl, C3-7-cycloalkylC1-3alkyl, or an optionally substituted group selected from phenyl, benzyl, phenylC2-4alkyl and a 5-6 membered heterocyclic group; n is an integer from 0 to 5; m is an integer from 0 to 3; R2 represents hydrogen, hydroxy, halgeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein X1 represents a direct bond, —CH2—, or a heteroatom linker group and R5 is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl an

Abstract: The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1–3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.

Abstract: Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R?, R5 and R10 are as defined herein.

Abstract: A process for preparing quinazolin-4-one or its derivative by reacting anthranilic acid or its derivative with formic acid or its derivative in the presence of ammonia, or by reacting ammonium anthranilate or its derivative with formic acid or its derivative.

Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R1, Z, n and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal

Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.

Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The compounds can be used for the treatment or prevention of obesity.

Abstract: A yellow dye-forming coupler represented by formula (I): wherein Q represents a group of nonmetallic atoms that form a 5- to 7-membered ring in combination with the —N?C—N(R1)—; R1 and R2 each represent a substituent; R4 represents an alkyl group; m represents an integer of 0 to 4; and X represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent; and when R4 represents a primary alkyl group, R1 represents —(CH2)3O—R101 in which R101 is an alkyl group having 4 to 8 carbon atoms. A silver halide color photographic light-sensitive material having at least one yellow dye-forming coupler represented by formula (I) in at least one layer provided on a support.

Abstract: A dye-forming coupler and compound of formula (I): wherein Q represents a residue that forms, together with —N—C?N—, a nitrogen-containing 6-membered ring; RA represents an aryl, heterocyclic, or —(R1)r—(R4)m group; X represents an aryl group; Y represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent: wherein, when RA represents an —(R1)r—(R4)m group, R1 represents a methylene group, a methine group, or a carbon atom; r is 1 to 30; R4 represents a substituent except for a hydrogen atom; m is 1 to 30; and the —(R1)r—(R4)m group does not represent a straight-chain alkyl group.

Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.

Abstract: An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis. Disclosed are compounds represented by formula (I) and a pharmaceutically acceptable salts and solvates thereof and pharmaceutical compositions comprising said compounds: wherein X and Z each independently represent CH or N; R1 to R3 represent H, substituted alkoxy, unsubstituted alkoxy or the like; R4 represents H; R5 to R8 represent H, halogen, alkyl, alkoxy, alkylthio, nitro, or amino, provided that R5 to R8 do not simultaneously represent H; R9 and R10 represent H, alkyl, or alkylcarbonyl; and R11 represents alkyl, alkenyl, alkynyl, or aralkyl.

Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.

Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

Abstract: A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.

Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.

Abstract: The present invention relates to phosphate-binding compounds that find use in binding, detecting and isolating phosphorylated target molecules including the subsequent identification of target molecules that interact with phosphorylated target molecules or molecules capable of being phosphorylated. A binding solution is provide that comprises a phosphate-binding compound, an acid and a metal ion wherein the metal ion simultaneously interacts with an exposed phosphate group on a target molecule and the metal chelating moiety of the phosphate-binding compound forming a bridge between the phosphate-binding compound and a phosphorylated target molecule resulting in a ternary complex. The binding solution of the present invention finds use in binding and detecting immobilized and solubilized phosphorylated target molecules, isolation of phosphorylated target molecules from a complex mixture and aiding in proteomic analysis wherein kinase and phosphatase substrates and enzymes can be identified.

Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of sub-formula (i) where R5, R6 and R7 are various specific organic groups, in the preparation of a medicament for use in the inhibtion of aurora 2 kinase. Novel compounds of formula (I) and pharmaceutical compositions useful in the treatment of cancer are also described and claimed.

Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): useful as integrin antagonists and methods for the treatment of integrin-mediated disorders.

Abstract: The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1–3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH2— or a direct bond; n is 0–5; m is 0–3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein X1 and R5 are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N—C1-4alkylcarbamoyl, N,N-di(C1-4alkylcarbamoyl, aminosulphonyl, N—C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N—(C1-4alkylsulphonyl)amino, N—(C1-4alkylsulph

Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists

Abstract: The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib: wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto; lower alkyl; or a nitrogen or oxygen protecting group; R3 is hydrogen; hydroxy; alkoxy; trifluoromethyl alkoxy; halo; sulfhydryl or alkylthio; R4 is —C(O)—X; X is hydroxy; alkoxy; or an amino acid residue; in which process a 2-amino-5-nitro-benzonitrile starting reagent is cyclized to form 2,4-diamino-6-nitro-quinazoline, which is converted to 2,4,6-triamino-quinazoline, which is converted to 2,4-diamino-6-cyano-quinazoline, which is converted to 2,4-diamino-6-formyl-quinazoline; in which the improvement includes: reacting an R4-p-benzoic acid alkylene moiety with triethyl phosphite to form a 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite; and reacting the 2,4-diamino-6-formyl-quinazoline with the 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite to form the compound of formula Ib.

Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or —(CH2)nCH(R7)NR8R9, where n is 0–6 inclusive, R7 is H, lower alkyl, aryl, or aralkyl, R8 is H, lower alkyl, cyclo-alkyl, aryl, or aralkyl, and R9 is R, RCO—, ROCO—, or RNHCO—, where R is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0–3 substituents selected from the group consisting of lower alkyl, halo, nitro, —OH, trifluoromethyl, or lower alkoxy; R2 is lower alkyl, aryl, aralkyl, or —(CHR10)m—(CO)—R11, wherein m is 0–4, R10 is H or lower alkyl, and R11 is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0–3 substituents selected from the group consisting of lower alkyl, halo, nitro, —OH, trifluoromethyl, or lower alkoxy; R3, R4, R5, and R6, are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkylamino), trifluoromethyl, or SH; or a pharmaceutically acce

Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease

Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

Abstract: Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.

Abstract: The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0–3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0–2; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R3 is hydrogen, halogeno, (1–6C)alkyl or (1–6C)alkoxy. q is 0–4; and Q is a group such as aryl, aryloxy, aryl—(1–6C)alkoxy, arylamino and N—(1–6C)alkyl-arylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable caters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the mo

Abstract: Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. In one embodiment is provided reagents that have the following formula: wherein Q is carbonyl, thiocarbonyl, or sulfonyl, and R5 is -L-Z; L is arylene, or a C1-6 perfluoroalkylene, or a single covalent bond; Z is a carbonyl hydrazide, hydrazide, sulfonyl hydrazide, or a thiocarbonyl hydrazide; R11-R14 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, or sulfo; and R21-R24 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12-alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, sulfo, or -L-Z. The method of treating a sample with the derivativization reagents is described.

Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.

Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1 represents C1-4 alkyl; R2 represents halo, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyloxy, —SO2(C1-4 alkyl), optionally substituted C1-4 alkyloxy, Het or —OHet; R3 represents a bicyclic group of the formula ?wherein X and Y are selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic ring containing 0, 1, 2 or 3 nitrogen atoms in the ring; n is), 1 or 2 L represents a direct link, C1-4 alkylene or C1-4 alkoxyalkylene; R4 represents H, —NR5R6, C3-6 cycloalkyl, —OR7, Het1 or Het4; R5 and R6 are independently selected from H, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkylene, —SO2(C1-4 alkyl) and optionally substituted C1-4 alkyl R7 is selected from H, C1-4 alkyl, C1-4 alkoxyalkyl, C3-6cycloalkyl, Het2 and C1-4alkyl-Het3; R8 is H or C1-4 alkyl; Het, Het1, Het2 and Het3 independently represent an optionally substituted 4 to 7 membered saturat

Abstract: Inhibitors of JAK3 kinase for the treatment of allergy, and others are described.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a

Abstract: Novel quinazolinone derivatives with good binding affinity for the CCK-A and CCK-B receptors, pharmaceutical compositions containing them and methods of using them are taught. The compounds are useful agents to suppress appetite, reduce gastric acid secretion, and the like.

Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, Z, and m have the meaning indicated in patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.

Abstract: A febrifugine represented by Formula (A): and an isofebrifugine represented by Formula (B): which exhibit extremely strong activities against tropical malarial protozoan are provided, together with a total synthesis route which enables efficient large scale synthesis of the same.

Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.

Abstract: An objective of the present invention is to provide compounds having potent antitumor activity.

Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.