Back to results
US 6,472,418 B1Granted
Non-peptide NK1 receptors antagonists
AssigneeWarner-Lambert Company
InventorsMark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
Life of this patent
Estimating the term…
Abstract
Non-peptide acetamide derivatives of Formula I are specific NK1 antagonist, where R is aryl, R1 and R2 are H or alkyl, m, n and q are integers from 0 to 4, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, R5 and R2 are H or alkyl, and R6 is aryl. The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.
Claims18
A compound of Formula I
- and the pharmaceutically acceptable salt thereof, wherein
- ▪, [Circlesolid], ▴, indicate all stereoisomers,
- R is:
- furyl
- benzofuryl, or
- benzoxazolyl, wherein each of the foregoing is unsubstitute, mono-, di- or trisubstituted by
- alkyl,
- hydroxy,
- alkoxy,
- halogen,
- —CF3,
- carboxy,
- sulfonamide, or
- nitro;
- R1 and R2 are each independently H or C1-C4 alkyl;
- m is an integer from 0 to 3;
- X is NR8 where R8 is H or C1-C4alkyl;
- R3 is hydrogen or C1-C4 alkyl;
- n is an integer from 1 to 2;
- R4 is indolyl, wherein said groups are substituted, mono, di- or trisubstituted by alkyl, hydroxy or formyl;
- R9 is hydrogen or C1-C4 alkyl;
- R5 and R7 are each independently hydrogen or (CH2)pR10 where:
- p is an integer of 1 to 3, and
- R10 is H, CH3, CN, OH, OCH3, CO2CH3, NH2, NHCH3, or N(CH3)2;
- q is integer of 0 to 4;
- R6 is phenyl,
- wherein the foregoing is unsubstituted, mono-, di- or trisubstituted by
- alkyl,
- hydroxy,
- alkoxy,
- halogen,
- CF3,
- NO2,
- N(CH3)2,
- OCF3,
- SONH2,
- NH2,
- CONH2,
- CO2CH3, or
- CO2H, and
- R5 and R6 when joined by a bond, can form a ring.
38 more elements
A compound of the Formula II
- wherein:
- R is
- benzofuryl, or
- benzoxazolyl;
- R3 is hydrogen or methyl;
- X is NH or NHCONH;
- R5 and R7 independently are hydrogen or CH2R10, where R10 is H, CH3 or OH;
- R6 is phenyl;
- and the pharmaceutically acceptable salts thereof.
6 more elements
Dependencies are inferred from the claim text.