Patent classifications
A61P35/02
Peptide conjugates
Methods and compositions related to the selective, specific disruption of multiple ligand-receptor signaling interactions, such as ligand-receptor interactions implicated in disease, are disclosed. These interactions may involve multiple cytokines in a single receptor family or multiple ligand receptor interactions from at least two distinct ligand-receptor families. The compositions may comprise polypeptides having composite sequences that comprise sequence fragments of two or more ligand binding sites. The methods and compositions may involve sequence fragments of two or more ligand binding sites that are arranged to conserve the secondary structure of each of the ligands from which the sequence fragments were taken.
Peptide conjugates
Methods and compositions related to the selective, specific disruption of multiple ligand-receptor signaling interactions, such as ligand-receptor interactions implicated in disease, are disclosed. These interactions may involve multiple cytokines in a single receptor family or multiple ligand receptor interactions from at least two distinct ligand-receptor families. The compositions may comprise polypeptides having composite sequences that comprise sequence fragments of two or more ligand binding sites. The methods and compositions may involve sequence fragments of two or more ligand binding sites that are arranged to conserve the secondary structure of each of the ligands from which the sequence fragments were taken.
Resorcinol Derivative As HSP90 Inhibitor
The present invention relates to a compound represented by formula (I) of a resorcinol derivative as an HSP90 inhibitor or pharmaceutically accepted salts thereof. The compound in the present invention has the activity of inhibiting heat shock protein HSP90. Therefore, the compound in the present invention is used to treat proliferative diseases such as cancer and neurodegenerative diseases. The present invention further provides the compounds and preparation methods for pharmaceutical compositions comprising the compounds, a method for treating diseases, and pharmaceutical compositions comprising the compounds.
##STR00001##
2-oxo-1,2-dihydrobenzo[cd]indole compound and use thereof
The present invention relates to the technical field of medicinal chemistry, and in particular discloses a 2-oxo-1,2-dihydrobenzo[cd]indole compound and use thereof. The compound and pharmaceutically acceptable salt, isomer, racemate, prodrug, co-crystallized complex, hydrate, and solvate thereof can effectively inhibit the BET bromodomain receptor, and can be used for preparing a medicine for treating cancers, cell proliferative disorders, inflammatory diseases, and autoimmune disorders, sepsis, and viral infections.
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CHRONIC MYELOID LEUKEMIA AND METHOD USING THE SAME
Provided are a pharmaceutical composition for preventing or treating chronic myeloid leukemia and a method of preventing or treating chronic myeloid leukemia using the same, thereby being effectively applied to the prevention or treatment of chronic myeloid leukemia.
Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors
A compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is LY; each L is a direct bond, C.sub.1-C.sub.10 alkylene, C.sub.2-C.sub.10 alkenylene or C.sub.2-C.sub.10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, halogen, fluoro C.sub.1-C.sub.10 alkyl, O—C.sub.1-C.sub.10 alkyl, NH—C.sub.1-C.sub.10 alkyl, S—C.sub.1-C.sub.10 alkyl, O-fluoro C.sub.1-C.sub.10 alkyl, NH-acyl, NH—C(O)—NH—C.sub.1-C.sub.10 alkyl, C(O)—NH—C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.
ANTI-ROR1 ANTIBODIES
The invention relates to antibodies, and in particular, to antibodies exhibiting specificity for Receptor tyrosine kinase-like Orphan Receptors (ROR), and to uses thereof, for example in the treatment of cancer. The invention extends to polynucleotide and polypeptide sequences encoding the antibodies, and therapeutic uses thereof, and to diagnostic kits comprising these molecules. The invention also extends to antibody-drug conjugates and to uses thereof in therapy.
FUSED PYRIMIDINE COMPOUND OR SALT THEREOF
The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof:
##STR00001##
wherein A, R.sup.1 to R.sup.3, X, and n are as defined in the specification.
HETEROCYCLIC COMPOUNDS AS PI3K-y INHIBITORS
This application relates to compounds of Formula (I):
##STR00001##
or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
TYROSINE KINASE INHIBITORS
Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure
##STR00001##
and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.