Quinazolinone compounds as calcilytics
AssigneeNPS Pharmaceuticals, Inc.
InventorsIrina Shcherbakova, Manuel Balandrin, John Fox, William Heaton, Rebecca Conklin, Damon Papac
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Abstract
Various calcilytic compounds and pharmaceutical compositions containing these compounds are disclosed. Calcilytic compounds are compounds capable of inhibiting calcium receptor activity. Techniques which can be used to obtain calcilytic compounds and uses of calcilyitc compounds as calcium receptor antagonists are also disclosed.
Claims19
A compound having the chemical formula:
- wherein:
- R1, R2 and R3 is each independently selected from one of:
- H, halogen, CN, CF3, OCF3, lower alkyl, lower alkoxy, NH-acetyl, NH-lower alky, NH-alkylaryl;
- N(lower alkyl)2, C(O)OH, C(O)O-lower alkyl, C(O)NH-lower alkyl, C(O)N(lower alkyl)2, OH, OC(O)-lower alkyl, OC(O)-lower alkyalamino, OC(O)-lower alkyl-N(lower alkyl)2, and OP(O)(OH)2;
- R4 is optional and may be selected from one of:
- H, halogen, CN, CF3, OCF3, lower alkyl, lower alkoxy, NH-acetyl, NH-lower alky, NH-alkylaryl, N(lower alkyl)2, C(O)OH, C(O)O-lower alkyl, C(O)NH-lower alkyl, C(O)N(lower alkyl)2, OH, OC(O)-lower alkyl, OC(O)-lower alkyalamino, OC(O)-lower alkyl-N(lower alkyl)2, and OP(O)(OH)2;
- X1 is selected from one of C and N,
- R5 is selected from one of:
- H lower alkyl, a furyl, thienyl, styryl, pyridyl and phenyl group optionally substituted with 1 to 3 substituents selected from one of H, halogen, CN, CF3, OCF3, lower alkyl, NH-alkylaryl, N(lower alkyl)2, lower alkoxy, OH, OC(O)-lower alkyl, OC(O)-lower alkyalamino, OC(O)-lower alkyl-N(lower alkyl)2, and OP(O)(OH)2;
- R6 is selected from one of:
- H, lower alkyl, and a group comprising —(CH2)n—X2—R7 wherein n is 0, 1, or 2, X2 is O, C(O), CH(OH), lower alkyl or a single bond, and
- R7 is an aromatic group optionally substituted with 1 to 3 substituents selected from one of:
- H, halogen, CN, CF3, OCF3, lower alkyl, lower alkoxy, NH-lower alkyl, NH-alkylaryl, N(lower alkyl)2, OH, OC(O)-lower alkyl, OC(O)-lower alkyalamino, OC(O)-lower alkyl-N(lower alkyl)2, and OP(O)(OH)2;
- or a pharmaceutically acceptable salt or complex thereof.
A method for preparing 2,3,5,6,7,8-substituted 3H-quinazolin-4-ones by reacting 2,4,5,6,7,8-substituted benzo[d][1,3]oxazin-4-ones with primary amines under microwave irradiation conditions.
Dependencies are inferred from the claim text.