Patent classifications
C07D311/02
Compounds and methods for detection of enzymes that remove formyl, succinyl, methyl succinyl or myristoyl groups from ε-amino lysine moieties
Provided is a compound that comprises the structure: ##STR00001## where SIG is a signaling molecule and R.sup.3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an -amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an -amino of a lysine.
Method for diagnosing cancer
Methods for identifying the presence of cancerous cells or tissue by: applying a compound of formula (I), or salts thereof, to a living body, ##STR00001##
wherein R.sup.1 represents hydrogen or the same or different one to four substituents; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 independently represent hydrogen, hydroxy, alkyl, or halogen; R.sup.8 and R.sup.9 independently represent hydrogen or alkyl; and X represents C.sub.1-C.sub.3 alkylene; and detecting fluorescence emitted by a compound of formula (II), ##STR00002##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as defined above; wherein fluorescence emitted by a compound of formula (II) is indicative of the presence of cancerous cells or tissue.
Substituted chroman compounds as calcium sensing receptor modulators
The present invention provides calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention. ##STR00001##
THERAPEUTIC AGENTS FOR ENHANCING EPITHELIAL AND/OR ENDOTHELIAL BARRIER FUNCTION
The present invention relates to novel compounds and compositions thereof. The compositions are useful in the treatment of an epithelial or endothelial barrier dysfunction disorder in a subject.
THERAPEUTIC AGENTS FOR ENHANCING EPITHELIAL AND/OR ENDOTHELIAL BARRIER FUNCTION
The present invention relates to novel compounds and compositions thereof. The compositions are useful in the treatment of an epithelial or endothelial barrier dysfunction disorder in a subject.
Compositions and methods for treatment of anticancer-drug resistant cancers
Embodiments of the instant disclosure relate to novel methods and compositions for treating tumors resistant to one or more anticancer drugs, such as platinum-based chemotherapeutics.
Compositions and methods for treatment of anticancer-drug resistant cancers
Embodiments of the instant disclosure relate to novel methods and compositions for treating tumors resistant to one or more anticancer drugs, such as platinum-based chemotherapeutics.
Methods and compositions for site-specific labeling of peptides and proteins
Methods and compositions are provided for covalently linking a chemical species to a recombinant or synthetic polypeptide. The methods involve the reaction of a thioester-comprising polypeptide with a reagent comprising a reactive amino-thiol group connected to the chemical species which is to be covalently linked to the polypeptide, via a linker. Such chemical species can be a functional group, a label or tag molecule, a biological molecule, a ligand, or a solid support. Efficient and catalyst-free methods for C-terminal protein labeling are also provided. The methods expand current capabilities in the area of protein functionalization, providing useful and complementary tools for the isolation, detection, characterization, and analysis of proteins in a variety of in vitro and in vivo applications.
Extended-release topiramate capsules
An extended-release topiramate capsule that includes a capsule shell containing a single population of coated particles; wherein each coated particle includes a core and a coating thereon; wherein each particle core includes a homogeneous mixture comprising topiramate throughout its core; and wherein the coating includes one or more release controlling agent(s).
Use of coumarin derivatives for the preparation of drugs for treating skin diseases
A compound of formula (I-1) ##STR00001##
wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a OR12 group, wherein R12 is a C1-C7 alkyl, a group CH.sub.2OCOR5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group OR13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a CH.sub.2-amine, R1 represents a group chosen among hydrogen and OR14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.