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US 2007/0191374 A1Published application
Substituted cinnolin-4-ylamines
AssigneeNeurogen Coroperation
InventorKevin Hodgetts
Life of this patent
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Abstract
Substituted cinnolin-4-ylamines are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Claims56
A compound of the formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- W, Y and Z are independently N or CRz;
- Rz is independently selected at each occurrence from hydrogen, halogen, cyano, amino, C1-C6alkyl, haloC1-C6alkyl, C1-C6alkoxy and haloC1-C6alkoxy;
- R3 is hydrogen, halogen, cyano, amino, C1-C4alkyl or haloC1-C4alkyl;
- Ar1 and Ar2 are independently selected from 5- to 10-membered aromatic carbocycles and heterocycles, each of which is substituted with from 0 to 3 substituents independently selected from halogen, cyano, nitro and groups of the formula LRa;
- L is independently selected at each occurrence from a single covalent bond, O, C(═O), OC(═O), C(═O)O, O—C(═O)O, S(O)m, N(Rx), C(═O)N(Rx), N(Rx)C(═O), N(Rx)S(O)m, S(O)mN(Rx) and N[S(O)mRx]S(O)m;
- wherein m is independently selected at each occurrence from 0, 1 and 2;
- and Rxis independently selected at each occurrence from hydrogen and C1-C8alkyl, or Rx is taken together with Ra to form an optionally substituted 4- to 7-membered heterocyclic ring;
- and
- Ra is independently selected at each occurrence from:
- (i) hydrogen;
- and
- (ii) C1-C8alkyl, C2-C8alkenyl, C2-C8alkynyl, (C3-C8cycloalkyl)C0-C4alkyl, haloC1-C8alkyl, C2-C8alkyl ether, mono- and di-(C1-C8alkyl)amino, (3- to 10-membered heterocycle)C0-C4alkyl and groups that are taken together with Rx to form a 4- to 7-membered heterocyclic ring, each of which is substituted with from 0 to 6 substituents independently selected from (a) hydroxy, halogen, amino, aminocarbonyl, cyano, nitro, oxo and COOH;
- and (b) C1-C8alkyl, C1-C8alkenyl, C1-C8alkynyl, (C3-C8cycloalkyl)C0-C4alkyl, C1-C8alkoxy, C1-C8alkylthio, C2-C8alkyl ether, C1-C8alkanoyl, C3-C8alkanone, C1-C8alkanoyloxy, C1-C8alkoxycarbonyl, hydroxyC1-C8alkyl, haloC1-C8alkyl, cyanoC1-C8alkyl, phenylC0-C8alkyl, mono- and di-(C1-C6alkyl)aminoC1-C8alkyl, C1-C8alkylsulfonyl, mono- or di-(C1-C8alkyl)aminosulfonyl and (5- to 7-membered heterocycle)C0-C2alkyl.
11 more elements
Dependencies are inferred from the claim text.