C07D207/273

METHODS OF SYNTHESIZING A DIFLUOROLACTAM ANALOG

The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, and L.sup.1 are as defined herein. Compounds of formula (IA) have been found useful as EP.sub.4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.

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METHODS OF SYNTHESIZING A DIFLUOROLACTAM ANALOG

The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, and L.sup.1 are as defined herein. Compounds of formula (IA) have been found useful as EP.sub.4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.

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Cyclopropyl urea formyl peptide 2 receptor and formyl peptide 1 receptor agonists

The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases. ##STR00001##

Cyclopropyl urea formyl peptide 2 receptor and formyl peptide 1 receptor agonists

The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases. ##STR00001##

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

##STR00001##

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

##STR00001##

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I):

##STR00001## wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I):

##STR00001## wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

##STR00001##

as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

##STR00001##

as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.