Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.

Abstract: The present invention is directed to the succinate salts of 5,7,13-triazatetracyclo[9.3.1.02,10.04,8]-pentadeca-2(10),3,5,8-tetraene and pharmaceutical compositions thereof. The invention is also directed to a process for preparation of the succinate salts.

Abstract: The present invention is directed to the citrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention is also directed to the various forms of the citrate salt, particularly its hydrate and its anhydrous/nearly anhydrous polymorph. The invention is also directed to processes for preparation of these citrate salt forms.

Abstract: The present invention provides an essentially nonaqueous, liquid pharmaceutical concentrate composition for oral administration containing sertraline or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients. The present invention also provides a use of this concentrate composition to prepare an aqueous solution of sertraline. In addition, the present invention provides a method of using this concentrate composition to treat or prevent a variety of diseases or conditions. Finally, the present invention provides the compound, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine methanesulfonate.

Abstract: This invention relates to compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, this invention relates to synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.

Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: The present invention relates to compounds of the formula wherein R1 through R4, X, Y, m and n are defined as in the specification. Such compounds are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.

Abstract: The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(−) or L-(+)naproxen as a resolving agent.

Abstract: This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R1 through R6 are as defined in the specification These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.

Abstract: A method and device for mass spectrometry analysis, wherein a mass spectrometer is adapted for use with helium droplets, as an ionization site medium, with a proton being initially captured by a large helium droplet (˜10,000 helium atoms) and then cooled evaporatively to 0.4 Kelvin. The protonated helium droplet then picks up a neutral molecule of interest and the neutral molecule is protonated inside of the droplet with the liquid helium droplet acting as a heat bath to provide rapid cooling of the newly formed protonated molecule. As a result, there is essentially no energy available, at 0.4 Kelvin, for the protonated molecule to fragment. Remaining liquid helium is removed and the stably maintained protonated molecule is detected by a mass spectrometer. Since the molecules do not fragment when protonated (ionized), each compound in a mixture analyses gives one mass and the number of ions of a particular mass detected is directly proportional to the molar percentage of that mass in the sample.

Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.

Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.

Abstract: The present invention relates to a novel process for the preparation of a compound of formula I: wherein R1 is defined herein and compounds of formula II: wherein R1 and R2 are defined herein. Said compound of formula I is useful in the treatment of various central nervous system disorders including depression.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: A compound of the formula wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.

Abstract: The present invention relates to compounds of formula I: and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.

Abstract: A composition comprising eletriptan and a p-glycoprotein (p-gp) inhibitor useful for the treatment of migraine. The bioavailability of eletriptan can be increased by co-administering eletriptan with a p-gp inhibitor. The eletriptan and p-gp inhibitor can be administered together in a composition or as separate components. If administered separately, they can be embodied as a kit. Also provided is a method of treating migraine using said composition or sequential administration of components.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.