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1-(4-PIPERIDINYL)-1,3-DIHYDRO-2H-INDOLE-2-ONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND THEIR USE IN THE MANUFACTURE OF MEDICAMENTS FOR THE TREATMENT OF PAIN
专利权人:
EURO-CELTIQUE S.A.;ZHENGMING CHEN;DONALD KYLE;SAM VICTORY;JOHN WHITEHEAD;QUN SUN;R. RICHARD GOEHRING
发明人:
ZHENGMING CHEN,DONALD KYLE,SAM VICTORY,JOHN WHITEHEAD,QUN SUN,R. RICHARD GOEHRING
申请号:
IL20890710
公开号:
IL208907A
申请日:
2010.10.24
申请国别(地区):
IL
年份:
2012
代理人:
摘要:
It is an object of certain embodiments of the present invention to provide compounds useful as analgesics, anti-inflammatories, diuretics, anesthetics and neuroprotective agents, anti-hypertensives, anti-anxioltics, agents for appetite control; hearing regulators; anti-tussives; anti-asthmatics; modulators of locomotor activity, modulators of learning and memory, regulators of neurotransmitter and hormone release, kidney function modulators, antidepressants, agents to treat memory loss due to Alzheimer's disease, or other dementias, anti-epileptics, anti-convulsants, agents to treat withdrawal from alcohol and drugs of addiction, agents to control water balance, agents to control sodium excretion and agents to control arterial blood pressure disorders and methods for administering said compounds. <;??>;The compounds of the present invention are useful for modulating a pharmacodynamic response from one or more opioid receptors (ORL-1, mu , delta and kappa ) centrally and/or peripherally. The response can be attributed to the compound stimulating (agonist) or inhibiting (antagonist) the one or more receptors. Certain compounds can stimulate one receptor (e.g., a mu agonist) and inhibit a different receptor (e.g., an ORL-1 antagonist). <;??>;Other objects and advantages of the present invention will become apparent from the following detailed description thereof. The present invention in certain embodiments comprises compounds having the general formula (I): <;CHEM>; wherein D is a 5-8 membered cycloalkyl, 5-8 membered heterocyclic or a 6 membered aromatic or heteroaromatic group; the other substituents are defined in the claims.
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