Patent classifications
C07K5/06104
Selective caspase inhibitors and uses thereof
The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).
Compositions and methods for treating ischemia and ischemia-reperfusion injury
The present invention relates to compositions comprising a substantially pure compound represented by Structural Formula I: ##STR00001##
and methods of using such compounds to activate cytoprotective kinases. The values and preferred values of the variables in Structural Formula I are defined herein.
CONTEMPORANEOUS, HETEROGENEOUSLY-ORIENTED, MULTI-TARGETED THERAPEUTIC MODIFICATION AND/OR MODULATION OF DISEASE BY ADMINISTRATION OF SULFUR-CONTAINING, AMINO ACID-SPECIFIC SMALL MOLECULES
The present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the contemporaneous, heterogeneously-oriented, multi-targeted therapeutic modification and/or modulation of cellular metabolic anomalies or other undesirable physiological conditions, including cancer, where the normal cellular biochemical function and/or the expression levels of various proteins/enzymes (i.e., the target molecules) are abnormal and must be modified and/or modulated in order to treat these metabolic anomalies or other undesirable physiological conditions, including cancer. The aforementioned target molecules, by way of non-limiting example, include: anaplastic lymphoma kinase (ALK), mesenchymal epithelial transition (MET) kinase, the receptor tyrosine kinase (ROS1), epidermal growth factor receptor (EGFR), peroxiredoxin (Prx), excision repair cross-complementing protein 1 (ERCC1), insulin growth factor 1 receptor (IGF1R), ribonucleotide reductase (RNR), tubulin, farnesyltransferase, and various other classes of proteins/enzymes. Additionally, the present invention discloses and claims methods and kits for (a) the selection of subjects for treatment; (b) the determination of the most effective medicinal agent(s) to be administered in combination with the administration of the sulfur-containing, amino acid-specific small molecules of the present invention; (c) the dosage of the medicinal agent(s) to be administered; (d) the determination of the length and/or number of treatment cycles; (e) the adjustment of the specific medicinal agent(s) used and the dosage administered during treatment; and/or (f) ascertaining the potential treatment responsiveness of the specific disease to the medicinal agents (s) selected for administration to a subject suffering from one or more types of: (i) cancer or (ii) metabolic anomalies or other undesirable physiological conditions by quantitatively determining the level of the abnormal biochemical activity and/or abnormal expression of any combination of the aforementioned target molecules; by use of quantitative measurement methodologies including, but not limited to: fluorescence in situ hybridization (FISH), nucleic acid microarray analysis, immunohistochemistry (IHC), radioimmunoassay (RIA), quantitative immunofluorescence and/or automated quantitative analysis; ELISA and flow cytometry-based analyses; PCR coupled with MS approaches; mass spectroscopy-based methods; and X-ray crystallography, and other related analytic methodologies.
Pea peptide with auxiliary hypoglycemic function and preparation method thereof
The present disclosure provides a pea peptide with auxiliary hypoglycemic function, and preparation method and application thereof. The pea peptide includes at least peptide segments pEE, pEK and pER in its composition; and based on a mass of the pea peptide, a content of the peptide segment pEE is 100.00 mg/100 g, a content of the peptide segment pEK is 80.00 mg/100 g and a content of the peptide segment pER is 90.00 mg/100 g. The pea peptide has a significant efficacy in an aspect of reducing blood glucose.
Delivery systems for controlled drug release
The present invention provides a compound having the structure of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof, for the controlled delivery and release of Agent. ##STR00001##
NMDA antagonist prodrugs
Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.