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US 2008/0167294 A1Published application
Pyrazoline Compounds
AssigneePfizer Inc.
InventorsMarvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
Life of this patent
Estimating the term…
Abstract
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.
Claims116
A compound, or a pharmaceutically acceptable salt of the compound, wherein the compound has the structure of Formula I:
- wherein:
- X is selected from the group consisting of —CH2— and —O—;
- R1 is selected from the group consisting of alkyl, cycloalkyl, cycloalkenyl, phenyl, and heterocyclyl;
- wherein the heterocyclyl substituent is a five- or six-membered ring heterocyclyl comprising at least one ring heteroatom selected from oxygen, sulfur and nitrogen;
- and wherein the alkyl, cycloalkyl, cycloalkenyl, phenyl, and heterocyclyl substituents may be optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, halogen, alkyl, and haloalkyl;
- R2 is selected from the group consisting of hydrogen and alkyl;
- R3A and R3B are independently selected from the group consisting of hydrogen and alkyl;
- R4, R6, and R7 are independently selected from the group consisting of hydrogen, halogen, hydroxy, alkyl, haloalkyl, hydroxyalkyl, and alkoxy;
- R5 is selected from the group consisting of hydrogen, —(CH2)mOR50, (CH2)mC(O)R50, —(CH2)mC(O)OR50, —(CH2)mC(O)NR51R52, —(CH2)mNR51R52, (CH2)nN(R51)C(O)R52, and —(CH2)mS(O)nR50;
- m is 0, 1, 2,3, 4, 5, or 6;
- n is 0, 1, or 2;
- R50 is selected from the group consisting of hydrogen and alkyl;
- R51 and R52 are independently selected from the group consisting of hydrogen and alkyl;
- or R51 and R52 together with the nitrogen to which they are attached form a five- or six-membered ring heterocyclyl;
- wherein the R50, R51 and R52 alkyl substituents and the R51/R52 heterocyclyl substituent may be independently and optionally substituted with one or more substituents selected from the group consisting of halogen, pyrrolidinyl, —OR53, —C(O)R53, —C(O)OR53, —C(O)NR54R55, —NR54R55, —N(R56)C(O)R53;
- —S(O)pR53, and —S(O)pNR54R55;
- p is 0, 1, or 2;
- R53 is selected from the group consisting of hydrogen, alkyl, haloalkyl, hydroxyalkyl, and carboxyalkyl;
- R54 and R55 are independently selected from the group consisting of hydrogen, alkyl, haloalkyl, hydroxyalkyl, and carboxyalkyl;
- or R54 and R55 together with the nitrogen to which they are attached form a five- or six-membered ring heterocyclyl;
- R56 is selected from the group consisting of hydrogen and alkyl;
- and
- R8 is selected from the group consisting of phenyl, pyridinyl and pyrimidinyl;
- wherein the phenyl, pyridinyl and pyrimidinyl substituents may be optionally substituted with one or more substituents independently selected from the group consisting of halogen, cyano, hydroxy, carboxy, alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, carboxyalkyl, alkoxy, haloalkoxy, cyanoalkoxy, amino, alkylamino, dialkylamino, and alkoxycarbonyl.
21 more elements
A compound, or a pharmaceutically acceptable salt of the compound, wherein the compound has the structure of Formula II:
- wherein:
- X is selected from the group consisting of —CH2— and —O—;
- Z is selected from the group consisting of —C(R81)— and —N—;
- R1 is selected from the group consisting of cyclopentyl and phenyl;
- wherein the R1 cyclopentyl and phenyl substituents may be optionally substituted with one or more substituents independently selected from the group consisting of chloro, fluoro, methyl, ethyl, propyl, chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl and trifluoromethyl;
- R2 is selected from the group consisting of hydrogen or (C1-C4)-alkyl;
- R5 is selected from the group consisting of —(CH2)mOR50, —(CH2)mC(O)OR50, and —(CH2)mC(O)NR51R52;
- wherein:
- m is 0, 1, 2, or 3;
- R50 is selected from the group consisting of hydrogen and (C1-C6)-alkyl;
- R51 and R52 are independently selected from the group consisting of hydrogen and (C1-C6)-alkyl;
- wherein the R50, R51 and R52 (C1-C6)-alkyl substituents may be independently and optionally substituted with one or more substituents selected from the group consisting of halogen, —OR53, —C(O)R53, —C(O)OR53, —C(O)NR54R55, —NR54R55, —N(R56)C(O)R53;
- —S(O)pR53, and —S(O)pNR54R55;
- p is 0, 1 or 2;
- R53 is selected from the group consisting of hydrogen, (C1-C6)-alkyl, halo-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, and carboxy-(C1-C6)-alkyl;
- R54 and R55 are independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, halo-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, and carboxy-(C1-C6)-alkyl;
- and
- R81, R82, R83, R84, and R85 are independently selected from the group consisting of hydrogen, chloro, fluoro, cyano, hydroxy, carboxy, methyl, ethyl, trichloromethyl, trifluoromethyl, cyanomethyl, hydroxymethyl, carboxymethyl, methoxy, amino, methylamino, and dimethylamino.
15 more elements
Dependencies are inferred from the claim text.