Patent classifications
C07D295/182
INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES
The invention relates to compounds of general formula I
##STR00001##
wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for usealone or in combination with one or more other pharmaceutically active compoundsin therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
Ingenol-3-acylates III and ingenol-3-carbamates
The invention relates to compounds of general formula I ##STR00001##
wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for usealone or in combination with one or more other pharmaceutically active compoundsin therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL
The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
Substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives and their use as sodium and/or calcium channel modulators
Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
Substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives and their use as sodium and/or calcium channel modulators
Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators
Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators
Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
Opsin-Binding Ligands, Compositions and Methods of Use
Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
Opsin-binding ligands, compositions and methods of use
Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
Opsin-binding ligands, compositions and methods of use
Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.