Patent classifications
C07D311/12
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
MALDI-MS METHOD, PHOTO-SENSITIVE MALDI MATRIX COMPOSITE AND PHOTO-CAGED MALDI MATRIX COMPOUND FOR USE IN SAID METHOD AND RESPECTIVE USES
The present invention relates to a Photo-caged MALDI Matrix Compound for use in a method of matrix-assisted laser desorption/ionization mass spectrometry, as well as to a sprayable liquid composition and a Photo-sensitive MALDI Matrix Composite, both comprising said Photo-caged MALDI Matrix Compound. Moreover, the present invention pertains to a matrix-assisted laser desorption/ionization mass spectrometry method involving the Photo-sensitive MALDI Matrix Composite and the Photo-caged MALDI Matrix Compound. Under a further aspect, the present invention pertains to a method of identifying for a given type of analyte and predetermined vacuum conditions a suitable Photo-caged MALDI Matrix Compound.
IRE-1? inhibitors
Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
IRE-1? inhibitors
Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
Processes for preparing medicaments for the treatment of cardiovascular diseases and intermediates for use therein
The present invention provides a compound of formula N wherein: X is CH.sub.2, oxygen or sulphur; R.sub.1, R.sub.2 and R.sub.3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine--hydroxylase. ##STR00001##
Processes for preparing medicaments for the treatment of cardiovascular diseases and intermediates for use therein
The present invention provides a compound of formula N wherein: X is CH.sub.2, oxygen or sulphur; R.sub.1, R.sub.2 and R.sub.3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine--hydroxylase. ##STR00001##
MAO-B selective inhibitor compounds, pharmaceutical compositions thereof and uses thereof
Described herein are a series of compounds having the structure of Formula I: ##STR00001##
for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.
MAO-B selective inhibitor compounds, pharmaceutical compositions thereof and uses thereof
Described herein are a series of compounds having the structure of Formula I: ##STR00001##
for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.
MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT
A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colo-rectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds.