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US 8,569,505 B2Granted
Aminotetralin-derived urea modulators of vanilloid VR1 receptor
AssigneeJanssen Pharmaceutica NV
InventorsEllen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
Life of this patent
Estimating the term…
Abstract
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to β-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
Claims52
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of fluoro, chloro, bromo, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of fluoro, chloro, bromo, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl;
- and a heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
40 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cyclo alkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy and fluorinated alkanyl;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy and fluorinated alkanyl;
- pyridyl;
- pyrimidyl;
- furyl;
- thienyl and imidazolyl;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is elected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
43 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of fluoro, chloro, bromo, and fluorinated alkanyl;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
37 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is 1;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cyclo alkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 1;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is 1;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond or C1-8alkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound comprising a compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, fluoro, chloro, bromo, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, fluoro, chloro, bromo, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, fluoro and chloro, wherein said heteroaryl is quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyloxy and hydroxy;
- naphthyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyloxy and hydroxy;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl and chloro wherein said heteroaryl is quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl and pyridyl-N-oxide;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1 -8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of naphthyl substituted with hydroxyl;
- quinolinyl optionally substituted with one or more substituents selected from the group consisting of methyl and chloro, quinolinyl-N-oxide, isoquinolinyl optionally substituted with one or more substituents selected from the group consisting of methyl and chloro and isoquinolinyl-N-oxide;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
46 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is 2-hydroxynaphth-8-yl, isoquinolin-5-yl and isoquinolinyl-5-yl-N-oxide;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
45 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is hydrogen;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is hydrogen;
- X is selected from the group consisting of O and S;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
A compound of Formula (I):
- wherein:
- R1 is a substituent independently selected from the group consisting of C1-8alkanyl optionally independently substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- fluorinated alkanyloxy;
- fluorinated alkanyl;
- C1-8alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy;
- C3-8cycloalkanyl;
- C3-8cycloalkanyloxy;
- nitro;
- amino;
- C1-8alkanylamino;
- C1-8dialkanylamino;
- C3-8cycloalkanylamino;
- cyano;
- carboxy;
- C1-7alkanyloxycarbonyl;
- C1-7alkanylcarbonyloxy;
- formyl;
- carbamoyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxyl, nitro, amino and cyano;
- aroyl;
- carbamoyl;
- amidino;
- (C1-8alkanylamino)carbonyl;
- (arylamino)carbonyl and aryl(C1-8alkanyl)carbonyl;
- n is an integer from 1 to 3;
- m is an integer from 0 to 3;
- R2 is independently selected from the group consisting of hydrogen;
- hydroxy;
- C1-8alkanyl;
- C2-8alkenyl;
- C1-8alkylidenyl;
- C1-8alkylidynyl;
- fluoro;
- chloro;
- C3-8cycloalkanyl;
- phenyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, phenyl(C1-8)alkanyloxy, fluorinated alkanyl, cyano, nitro, amino, C1-8alkanylamino, and C1-8dialkanylamino;
- phenoxy optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, C1-8alkanyl, C1-8alkanyloxy, fluorinated alkanyl, cyano and nitro;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6alkanyl and halogen wherein said heteroaryl is pyridyl, pyrimidyl, furyl, thienyl or imidazolyl;
- pyrrolidino;
- and piperidino;
- L is a direct bond, C1-8alkandiyl, C2-8alkendiyl, C2-8alkyndiyl, or C3-8cycloalkandiyl;
- R3 is selected from the group consisting of phenyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, C1-8alkanyloxy, hydroxy, fluorinated alkanyl, nitro, amino, di(C1-8)alkanylamino, C1-8alkanylamino and cyano;
- and heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, halogen, nitro, amino and cyano wherein said heteroaryl is quinolinyl, quinolinyl-N-oxide, isoquinolinyl, isoquinolinyl-N-oxide, pyridyl, pyridyl-N-oxide, pyrimidyl, furyl, thienyl or imidazolyl;
- R4 is selected from the group consisting of hydrogen and C1-8alkanyl;
- R5 is selected from the group consisting of hydrogen and C1-8alkanyl;
- X is O;
- and
- an enantiomer, a diastereomer, a tautomer, or a pharmaceutically acceptable salt thereof.
47 more elements
Dependencies are inferred from the claim text.