Patent classifications
A61K31/517
Dihydroquinazolinone compound or pharmacologically acceptable salt, and cell growth inhibitor
Provided is a cell proliferation inhibitor comprising a compound of the formula (1) or a pharmacologically acceptable salt thereof: ##STR00001## wherein J.sup.1 and J.sup.2 each represent CH or N, with the proviso that J.sup.1 and J.sup.2 are not simultaneously CH; r represents 0 to 4; each R.sup.101 is the same or different when r is 2 or more, and R.sup.101 represents a C.sub.1-6 alkyl group optionally substituted with a halogen atom or the like; s represents 0 to 5; each R.sup.102 is the same or different when s is 2 or more, and R.sup.102 represents a halogen atom or the like; R.sup.103 represents a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.3-6 cycloalkyl group, or a C.sub.3-6 cycloalkyl C.sub.1-6 alkyl group; and R.sup.101 and R.sup.103 are optionally linked together to form a five- to seven-membered ring hetero ring when R.sup.101 is present at the 8-position.
Method for Prohibiting and/or Treating an Eye Condition
A method for prohibiting and/or treating an eye condition is provided. The method comprises inserting an implantable device into a suprachoroidal space of a patient. The device comprises a core defining an outer peripheral surface. The core comprises a core polymer matrix within which is dispersed a therapeutic agent, the polymer matrix containing an ethylene vinyl acetate copolymer.
Method for Prohibiting and/or Treating an Eye Condition
A method for prohibiting and/or treating an eye condition is provided. The method comprises inserting an implantable device into a suprachoroidal space of a patient. The device comprises a core defining an outer peripheral surface. The core comprises a core polymer matrix within which is dispersed a therapeutic agent, the polymer matrix containing an ethylene vinyl acetate copolymer.
Crystalline forms of therapeutic compounds and uses thereof
Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
Crystalline forms of therapeutic compounds and uses thereof
Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
BIARYL ETHER-TYPE QUINAZOLINE DERIVATIVES
The present invention provides a novel compound or a pharmaceutically acceptable salt thereof having an inhibitory action on an EGFR tyrosine kinase having an exon 20 insertion mutation and/or a HER2 tyrosine kinase having an exon 20 insertion mutation, a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 in the Formula (I) are each as defined in the description.
##STR00001##
INHIBITORS OF ENL/AF9 YEATS
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula
##STR00001##
inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
INHIBITORS OF ENL/AF9 YEATS
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula
##STR00001##
inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
Compounds for the treatment of kinase-dependent disorders
Disclosed herein are compounds of Formula (I′). Compounds of Formula (I′) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. ##STR00001##
EXPANDED DOSAGE REGIMENS FOR INTEGRIN INHIBITORS
The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I):
##STR00001##
or a salt thereof, wherein R.sup.1, R.sup.2, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).