Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Compounds, compositions, and methods

Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein: X represents NR or O; R represents hydrogen, C1-8 alkyl or SO2[C,1-8 alkyl]; W represents N or CH; Y and Y' independently represent hydrogen, halogen, OH, CF3, OCF3, CN, NH2 C1-8 alkyl, C1-8 alkyloxy or C3-8cycloalkyl; Ring A represents a heterocyclic ring containing at least one nitrogen atom; Z represents a direct link, C1-8 alkyl or C3-8 cycloalkyl; R1 represents R2, OR2, OR 3-R4, N(R2)[C1-8 alkylene]aR4; NCOR2, or SR4; R2 and R4 independently represent hydrogen, C3-8 cycloalkyl, CF3, Ar or Het; R3 represents a direct link or C1-8 alkyl; is 0 or 1; Ar represents an aromatic ring, optionally fused to a heterocyclic ring, and/or optionally substituted with one or more groups as described below; Het represents a heterocyclic ring optionally substituted with one or more groups as described below, and/or optionally fused to an aromatic ring which is optionally substituted with one or more groups as described below; at each occurrence C1-8alkyl, C1-8alkylene and C3-8cycloalkyl may be independently optionally substituted with one or more groups as described below; substituent groups for Ar, Het, C1-8alkyl, C1-8alkylene and C3-8cycloalkyl referred to the above are independently selected from hydrogen, halogen, C1-8alkyl, C1-8alkyloxy, S[C1-8alkyl], CN, CF3, NH2 and OH; are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittelschmerz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.

Compounds useful in therapy

This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

Selective melanin concentrating hormone-1 (mch1) receptor antagonists and uses thereof

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Alpha 1a adrenergic receptor antagonists

The invention provides compounds of formula (I) wherein R?1, R2, R3, R6?, Z, Q, m, n, X?1, X2, X3, X4? and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.

Substituted piperidine compounds useful as modulators of chemokine receptor activity

This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α1A receptors This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α1A receptor may be useful The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier

Dihydropyrimidines and uses thereof

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Dihydropyrimidines and uses thereof