Patent classifications
A61K31/5386
TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.
##STR00001##
Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
Methods for treating chronic obstructive pulmonary disease
Methods for treating chronic obstructive pulmonary disease (COPD) in a patient are disclosed. In the methods, a patient having COPD is selected for treatment based on the patient's peak inspiratory flow rate (PIFR) and percent predicted force expiratory volume in one second (FEV.sub.1); and a bronchodilator is administered to the selected patient using a nebulizer. Administration of a bronchodilator to patients having low PIFR and a percent predicted FEV.sub.1 less than 50 percent using a nebulizer as the inhalation delivery device provides significantly greater improvements in trough FEV.sub.1 and trough forced vital capacity (FVC) compared to administration of a bronchodilator to such patients using a dry powder inhaler.
PYRIDAZINONE DERIVATIVE
Provided are: a pyridazinone derivative and/or a pharmaceutically acceptable salt thereof, which is useful as a therapeutic agent and/or a prophylactic agent for diseases in which Nav1.1 is involved and various central nervous system diseases; and a medicine containing the pyridazinone derivative and/or the pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof.
##STR00001##
[In the formula, M.sup.1 represents a saturated or partially unsaturated C.sub.4-12 carbocyclic group or the like; R.sup.1 and R.sup.2 independently represent a hydrogen atom or the like; M.sup.2 represents a group represented by formula (2a) or the like; X.sup.1a, X.sup.1b and X.sup.1c independently represent N or the like; X.sup.2, X.sup.3 and X.sup.4 independently represent CR.sup.3 or the like; A.sup.1 and A.sup.2 independently represent N or the like; and R.sup.3 represents a hydrogen atom or the like.]
PYRIDAZINONE DERIVATIVE
Provided are: a pyridazinone derivative and/or a pharmaceutically acceptable salt thereof, which is useful as a therapeutic agent and/or a prophylactic agent for diseases in which Nav1.1 is involved and various central nervous system diseases; and a medicine containing the pyridazinone derivative and/or the pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof.
##STR00001##
[In the formula, M.sup.1 represents a saturated or partially unsaturated C.sub.4-12 carbocyclic group or the like; R.sup.1 and R.sup.2 independently represent a hydrogen atom or the like; M.sup.2 represents a group represented by formula (2a) or the like; X.sup.1a, X.sup.1b and X.sup.1c independently represent N or the like; X.sup.2, X.sup.3 and X.sup.4 independently represent CR.sup.3 or the like; A.sup.1 and A.sup.2 independently represent N or the like; and R.sup.3 represents a hydrogen atom or the like.]
2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.
2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.
COMPOUNDS AND METHODS FOR KRAS MODULATION AND INDICATIONS THEREFOR
Disclosed are compounds of Formula I:
##STR00001## or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer, or a deuterated analog thereof, wherein: R.sup.1, R.sup.2, R.sup.3, X, and Z are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
COMPOUNDS AND METHODS FOR KRAS MODULATION AND INDICATIONS THEREFOR
Disclosed are compounds of Formula I:
##STR00001## or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer, or a deuterated analog thereof, wherein: R.sup.1, R.sup.2, R.sup.3, X, and Z are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
SELECTIVE INHIBITORS OF ROCK1 AND ROCK2 PROTEIN KINASES AND USES THEREOF
The present invention relates to novel substituted bicyclic derivatives that can inhibit Rho-kinases and/or Rho-kinase mediated phosphorylation of myosin light chain phosphates, compositions comprising the derivatives, methods for preparing the derivatives, and methods for using the derivatives and/or compositions.
SELECTIVE INHIBITORS OF ROCK1 AND ROCK2 PROTEIN KINASES AND USES THEREOF
The present invention relates to novel substituted bicyclic derivatives that can inhibit Rho-kinases and/or Rho-kinase mediated phosphorylation of myosin light chain phosphates, compositions comprising the derivatives, methods for preparing the derivatives, and methods for using the derivatives and/or compositions.