7 results about "Integrin antagonist" patented technology

The present invention belongs to the field of pharmaceutical chemistry, and relates to an N-(benzoyl)-phenylalanine compound used as an α4β7 integrin antagonist, including the pharmaceutical composition and the use, and in particular to a compound represented by general formula (1). The compound exhibits good α4β7 integrin binding inhibitory activity, can be used as a high-efficiency α4β7 integrin antagonist, and used for preventing and / or treating α4β7 integrin-related diseases such as autoimmune diseases and inflammatory diseases.

This invention proposes a new class of compounds that effectively antagonize integrin α4β7, which are compounds represented by formula (Y), or stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs of compounds represented by formula (Y):

Provided are a compound that effectively antagonizes integrin α4β7, which is a compound represented by formula (Y), or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug of the compound represented by formula (Y).

The present application provides compounds / compositions, synthetic methods, methods of use. The compounds / compositions are directed to thyroid integrin antagonists conjugated to polymers. The compounds / compositions further include additional substituents that are also conjugated to the polymers. The compounds / compositions exhibit increased absorption across the blood brain barrier and increased retention therein and within tumors. The compounds / compositions can also include improved synthetic scalability, improved purity, improved water solubility, and solid products or intermediates. The compounds / compositions can exhibit improved anti-angiogenic effects, and improved efficacy against diseases, particularly cancers that require blood brain barrier permeability, such as malignant gliomas (GBM).

Provided in the present invention are a new compound that effectively antagonizes integrin α4β7, which is a compound as represented by the following formula (II), or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound as represented by the following formula (II).

The invention relates to novel compounds of formula (I), the compounds being capable of acting as avβ6 integrin antagonists, their use in the treatment of disease, their methods of manufacture and compositions comprising said compounds for such purposes (I) wherein R1 is selected from: R1a, —C(O)R1a, —C(O)OR1a —C(O)NHR1a, —C(O)N(R1a)2, —SO2R1a, wherein R1a are each independently selected from: alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl, each of which may be optionally substituted; R2 is selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R2a are each independently selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R3 is selected from: hydrogen, optionally substituted alkyl or optionally substituted alkoxyl; R4 is hydroxyl; Ar1 is an optionally substituted heteroaryl or bicyclic heteroaryl; and L is a linker; or a pharmaceutically acceptable salt thereof.

This invention proposes a new class of compounds that effectively antagonize integrin α4β7, which are compounds represented by formula (II) below, or tautomers, stereoisomers, hydrates, solvates, pharmaceutically acceptable salts, or prodrugs of compounds represented by formula (II) below: