Pfizer Corporation

Other

Eisai Company, Limited

Arthur A Nagel

Yuhpyng Liang Chen

Anabella Villalobos

John Adams Lowe, Iii

Steven Wayne Goldstein

James P Rizzi

Terry J Rosen

James R Hauske

Brian Thomas O'Neill

Thomas Allen Chappie

Fredric J Vinick

John Michael Humphrey

James F Blake, Jr

Susan Beth Sobolov-Jaynes

Lawrence Albert Vincent

Robin W Spencer

Kelly P Longo

Peter H Dorff

Jianhua Huang

Eric Platt Arnold

Stanley Jung

W Stephen Faraci

The present invention relates to certain benzoamide piperidine containing compounds and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.

Benzoamide piperidine containing compounds and related compounds

Heterocyclic-cyclic amine derivatives as cholinesterase inhibitors

Heterocyclic-cyclic amine derivatives

A method of treating hyperproliferation diseases in mammals in need of such treatment which method includes administering to said mammal a therapeutically effective amount of a compound of the formula:

Benzazepine derivatives as inhibitors of hyperproliferation diseases

Heteroaryl amines as novel acetylcholinesterase inhibitors

Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.

Heteroaryl amines as novel acetyl cholinesterase inhibitors

This invention relates to novel azabicyclic compounds of the formula ##STR1## wherein R.sup.1, Q and Z are defined as in the specification, pharmaceutical compositions containing them, and the use of such compounds for the treatment of neurodegenerative diseases and other disorders involving nerve damage.

Azabicyclic rotomase inhibitors

An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.

(N-(pyridinylmethyl)-heterocyclic)ylideneamine compounds as nicotinic

Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.

A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.

Aromatic pyrrolidine amide prolyl endopeptidase inhibitors

Described herein are compounds of the formula ##STR1## wherein R.sup.1 R.sup.2, R.sup.7, R.sup.8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.

Benzisoxazole and benzisothizole derivatives as cholinesterase inhibitors

Benzothiazepine and benzoxazepine derivatives as cholecystokinin

Disclosed herein are compounds of the formula ##STR1## wherein R.sup.1 R.sup.2, R.sup.7, R.sup.8, X, Y, M and L are defined as below The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.

Methods of using piperidyl-benzisoxazole and benisothiazole derivatives

A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.

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Gales Ferry, CT, United States of America

Arthur A Nagel