Nps Pharmaceuticals, Inc.

Smithkline Beecham Corporation

Other

Robert M Barmore

Bradford C Van Wagenen

James Francis Callahan

Maria Amparo Lago

Eric G Del Mar

Derek Sheehan

Linda Sue Southall

Mervyn Thompson

Richard McCulloch Keenan

Scott T Moe

Nikesh R Kotecha

Manuel F Balandrin

Eric G DelMar

Daryl Lynn Smith

Bradford C VanWagenen

Alan L Mueller

Linda D Artman

Thomas M Stormann

Ruth J Walton

Susan M Sheehan

Eric Delmar

Irina V Shcherbakova

Robert L Smith

Pradip Kumar Bhatnagar

Joelle Lorraine Burgess

Richard Trovato

Thomas The Nguyen

William M Bryan

Raul Rolando Calvo

Richard Travato

The present invention features calcilytic compounds. 'Calcilytic compounds' refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Calcilytic compounds

The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases

The present invention features calcilytic compounds. &ldquo;Calcilytic compounds&rdquo; refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

The present invention features calcilytic compounds. &ldquo;calcilytic compounds&rdquo; refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Novel arylalkylamino compounds exhibiting calcilytic properties are provided.

Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Compounds active at a novel site on receptor-operated calcium channels

Method of using calcilytic compounds

Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

A process for preparing an R enantiomer of a compound of the formula (I): ##STR1## wherein Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF.sub.3, CF.sub.2 H, CFH.sub.2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH.sub.2 CF.sub.3, OH, CN, NO.sub.2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH--Me), C(O)N-lower alkyl.sub.2 (e.g., C(O)NMe.sub.2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH--C(O)-lower alkyl (e.g., NH--C(O)Me), where 'lower alkyl' is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I). The process is especially useful to produce compounds (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorophenyl)propanamine and (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(phenyl)propanamine. Enantiomeric excess of the R enantiomer over S enantiomer of greater than 65% have been achieved.

Chiral reductions of imines leading to the syntheses of optically active

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Salt Lake City, UT, United States of America

Robert M Barmore