Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.

Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

Abstract: The compound of the formula or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of anxiety are disclosed.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the

Abstract: Disclosed are nociceptin ORL-1 receptor agonists of the formula wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is —C(H)(R)—NR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is —(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0-10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2 is —NHR7 or and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.

Abstract: Disclosed are nociceptin ORL-1 receptor agonists of the formula 1

Abstract: Novel compounds of the formula 1

Abstract: Novel compounds of the formula wherein R is optionally substituted heteroaryl or R1 is H or C1-C6 alkyl; and R2 and R3 are —CH3, —OCH3 or halo; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

Abstract: The present invention relates to the method of treating cough with ORL-1 agonists, alone or in combination with additional agents for treating symptoms of cough, allergy or asthma, pharmaceutical compositions comprising the combinations, and to compounds of the formula 1

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicepti

Abstract: Disclosed are nociceptin ORL-1 receptor agonists of the formula 1

Abstract: Novel compounds of the formula 1

Abstract: Novel compounds of the formula 1

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicep

Abstract: Novel compounds of the formula 1

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused Spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicepti