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US 7,803,830 B2Granted
3-amino-1-arylpropyl indoles and AZA-substituted indoles and uses thereof
AssigneeRoche Palo Alto LLC
InventorsPravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
Life of this patent
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Abstract
The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
Claims20
A compound of formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- p is 1 or 2;
- Y is CRe;
- Ar is indazolyl selected from indazol-4-yl, indazol-5-yl, indazol-6-yl, and indazol-7-yl, each optionally substituted;
- R1 is:
- (a) aryl selected from phenyl and naphthyl, each optionally substituted;
- or
- (b) heteroaryl selected from indolyl, indazolyl, pyridinyl, thienyl, furanyl, pyrimidinyl, pyridazinyl, pyrazinyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, imidazolyl, pyrazolyl, quinolinyl, isoquinolinyl, quinoxalinyl, benzothiazolyl, benzofuranyl, benzothiophenyl or benzoxazinyl, each optionally substituted;
- (c) optionally substituted arylalkyl;
- (d) optionally substituted heteroarylalkyl;
- (e) cycloalkyl;
- or
- (f) cycloalkylmethyl;
- R2 and R3 each independently is:
- (a) hydrogen;
- (b) alkyl;
- (c) hydroxyalkyl;
- (d) alkoxyalkyl;
- (e) benzyl;
- or
- (f) R2 and R3 together with the nitrogen to which they are attached may form an optionally substituted four to seven membered ring that optionally includes an additional heteroatom selected from N, O and S;
- or
- (g) one of R2 and R3 together with one of Ra and Rb and the atoms to which they are attached may form a five or six membered ring that optionally includes an additional heteroatom selected from O, N and S;
- Ra is:
- hydrogen;
- fluoro;
- or
- alkyl;
- Rb is:
- hydrogen;
- alkyl;
- hydroxy;
- alkoxy;
- fluoro;
- or
- hydroxyalkyl;
- Rc and Rd each independently is:
- hydrogen;
- or
- alkyl;
- or Rc and Rd together form ═O, ═S, or ═NRf, wherein Rf is hydrogen, alkyl, or
- —ORg, wherein Rg is hydrogen or alkyl;
- or one of R2 and R3 together with one of Rc and Rd together with the atoms to which they are attached may form a four to six membered ring that optionally includes an additional heteroatom selected from O, N and S;
- and
- Re is hydrogen or alkyl.
43 more elements
Dependencies are inferred from the claim text.