Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Neuromed Pharmaceuticals Ltd.

Prasun K Chakravarty

William J Greenlee

Arthur A Patchett

Thomas F Walsh

Nathan B Mantlo

William H Parsons

Malcolm MacCoss

Dooseop Kim

Scott William Bagley

James R Tata

Ralph A Rivero

Eric E Allen

Daljit S Dhanoa

Kenneth J Fitch

Stephen E De Laszlo

Elizabeth M Naylor

David L Williams

Wallace T Ashton

Linda L Chang

Nancy J Kevin

Sriram Tyagarajan

Bishan Zhou

Min K Park

Douglas J Pettibone

Brenda L Palucki

Tomasz W Glinka

Anna Chen

Theodore P Broten

Lihu Yang

Ravi P Nargund

Michael H Fisher

David B Johnston

Peter T Meinke

Richard B Toupence

Richard W Ransom

Louis L Zuegner, Iii, Legal Representative

Jay M Matthews

Howard C H Kuo

Matthew J Wyvratt

Steven L Colletti

William R Schoen

Hyun O Ok

Hassan Pajouhesh

Richard Berger

Yanbing Ding

Joseph Leslie Duffy

Mu T Wu

Pengcheng Patrick Shao

Feng Ye

Thomas L Shih

Meng Hsin Chen

Gerard R Kieczykowski

Marlene A Jacobson

Rosemary Sisco

Robert W Marquis, Jr

Christine L Cantone

Richard Norton

Kelly Flanagan

Philip Escola

Paul F Schuda

E M Naylor

Malcolm MacCross

Louis L Zuegner Iii, Legal Representative

Michelle B Ayer

Edward Gonzalez

Jeffrey M Fisher, Legal Representative

Brenda Palucki

A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Substituted aryl sulfone derivatives as calcium channel blockers

Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.

Biaryl substituted pyrazoles as sodium channel blockers

Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Biaryl substituted triazoles as sodium channel blockers

Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Substituted triazoles as sodium channel blockers

Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds and a pharmaceutically acceptable carrier, and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as initable bowel syndrome, Cnohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar depression, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are described.

Aryl-link-aryl substituted thiazolidine-dione and oxazolidine-dione as sodium channel blockers

The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

C1 to C4 side chain modified nodulisporic acid analogs

The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Piperidines, pyrrolidines and hexahydro-1H-azepines promote release of

The invention is a method for inhibiting activation of the human A3 adenosine receptor with adenosine, by treating the receptor a compound of the formula ##STR1## to treat asthma.

Method for inhibiting activation of the human A3 adenosine receptor to

Phenoxyphenylacetic acid derivatives

Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Substituted phthalazinones as neurotensin antagonists

Biphenyl compounds useful or endothelin antagonists

The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.

3-substituted piperidines promote release of growth hormone

Substituted biphenylmethylimidazopyridines

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Edison, NJ, United States of America

Prasun K Chakravarty