Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: This invention relates to a novel improved process for preparing the (+) enantiomer of N-[4(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine by reacting the (+) enantiomer of 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone with monomethylamine and titanium chloride or molecular sieves.

Abstract: Methods for monitoring and evaluating the efficacy of neuroprotective treatment of a patient suffering from neurological damage by measuring the amount of at least one biomarker in a biological sample taken from the patient during or after treatment.

Abstract: A pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal comprising administration of a nicotine receptor partial agonist or a pharmaceutically acceptable salt thereof; and an acetylcholinesterase inhibitor, butylcholinesterase inhibitor, an estrogenic agent, selective estrogen receptor modulator or muscarinic agonist or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The nicotine receptor partial agonist and acetylcholinesterase inhibitor, butylcholinesterase inhibitor, estrogen, selective estrogen receptor modulator or muscarinic agonist are present in amounts that render the composition effective enhancing cognition or in the treatment of diseases of cognitive dysfunction including but not limited to Alzheimer's Disease, mild cognitive impairment, age-related cognitive decline, vascular dementia, Parkinson's disease dementia, Huntington's Disease, Stroke, TBI, AIDS associated dementia and schizophrenia.

Abstract: This invention relates to a method of predicting the activity of a CNS drug on striatal dopamine transporter populations. The method uses SPECT brain imaging to predict the activity of antidepressants or anxiolytic agents on striatal dopamine transporter populations. The method uses the increase in dopamine transporter populations as a marker for predicting sexual dysfunction side effects, as well as to determine proper dosing for antidepressants or anxiolytics agents in order to avoid the sexual dysfunction side effects.

Abstract: The present invention relates to a method of treating alcoholism or alcohol dependence in a mammal, including a human, by administering to the mammal a monoamine reuptake inhibitor in combination with an opioid antagonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a monoamine reuptake inhibitor and an opioid antagonist.

Abstract: This invention relates to novel amorphous and crystallline forms of 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt, useful as inhibitors of protein kinases, and to their methods of preparation.

Abstract: The invention features non-human mammals and animal cells that contain a targeted disruption of a glutathione S-transferase-Omega-1 gene. The invention also features methods of treating an IL-1 mediated and/or inflammation mediated disorder in a mammal comprising administering an agent that inhibits GST-Omega-1 activity.

Abstract: The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or “chiral tetralone.” The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).

Abstract: A process for preparing alkanesulfonyl pyridines of the formula 1: is disclosed, wherein R1 is as defined herein. The compounds of formula 1 are useful in the preparation of pyridyl-substituted pyrazoles used in the treatment and alleviation of inflammation and other inflammation associated disorders.

Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.

Abstract: A method for treating or preventing a BPH in a mammal which comprises administering to said mammal an amount of a drug, comprising an &agr;1-adrenoreceptor antagonist or pharmaceutically acceptable acid addition salt thereof, effective for treating or preventing the BPH.

Abstract: A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.

Abstract: Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

Abstract: Compounds of Formula 1 [Region &agr;]-[Region &bgr;]-[Region &ggr;]-[Region &dgr;]  (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R1, R2, R3, R4, and R5 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment, and to methods of preparing compounds of formula 1.

Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.

Abstract: The invention features non-human mammals and animal cells that contain a targeted disruption of a phosphodiesterase 10A (PDE10A) gene.