18 results about "Integrin antagonist" patented technology

The invention belongs to the technical field of chemical drugs, and relates to a compound as shown in a general formula (I), or a racemate thereof, or an isomer thereof, or a pharmaceutically acceptable salt thereof, as a small molecule antagonist of alpha4beta7 integrin, and a method for treating various specific diseases or symptoms by using the compound. # imgabs0 #

The invention provides stable ophthalmic formulations, a unit dose containing such formulations, medical kits, and methods for making and using such formulations and unit doses to treat patients suffering from a disorder mediated by an αv integrin, such as diabetic retinopathy.

The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Relates to a compound preparation and application thereof. The compound preparation comprises an anti-VEGF antibody or antigen binding fragment and an integrin GPIIb / IIIa antagonist. According to the compound preparation, the anti-VEGF antibody or antigen binding fragment and the integrin GPIIb / IIIa antagonist in the compound can be kept stable and have good binding activity, and the clinical use safety and effectiveness are improved.

This invention relates to the ability of formula (I) to function as α v Novel compounds of β6 integrin antagonists, their use in treating diseases, methods of their manufacture, and compositions comprising said compounds for this purpose, wherein R 1 Selected from: R 1a 、-C(O)R 1a -C(O)OR 1a -C(O)NHR 1a 、-C(O)N(R 1a )2、-SO2R 1a , where R 1a Each is independently selected from: alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylaryl, or alkylheteraryl, wherein each can be optionally substituted; R 2 Selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxy; R 2a Each is independently selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxy; R 3 Selected from: hydrogen, optionally substituted alkyl, or optionally substituted alkoxy; R 4 For hydroxyl group; Ar 1 It is optionally substituted heteroaryl or bicyclic heteroaryl; and L is a linker; or a pharmaceutically acceptable salt thereof.

Described herein are [alpha] 4 [beta] 7 integrin inhibitors and pharmaceutical compositions comprising the inhibitors. The compounds and compositions of the invention are useful for the treatment of alpha4beta7 integrin mediated conditions, such as inflammatory bowel disease (IBD), ulcerative colitis (UC), and Crohn's disease (CD).

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):

The application belongs to the field of medicinal chemistry, and relates to N-(benzoyl)-phenylalanine compounds as alpha4beta7 integrin antagonists, pharmaceutical compositions containing the same and uses thereof. Specifically, the application relates to a compound as shown in general formula (1), which exhibits good alpha4beta7 integrin binding inhibition activity, can be used as an efficient alpha4beta7 integrin antagonist, and is used for preventing and / or treating autoimmune diseases and inflammatory diseases related to alpha4beta7 integrin and the like.

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 discloses a linker compound of an integrin alpha v beta 3 inhibitor, which is shown as a formula (1) and can be used for a prodrug delivery system, or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer of the linker compound, or a mixture form of the linker compound, or a pharmaceutically acceptable salt, a prodrug or a solvate of the linker compound, and a synthesis method and application of the linker compound. The structure of the formula (1) comprises an alpha v beta 3 integrin antagonist, a connecting unit, a polyethylene glycol (PEG) spacer and a cytotoxic element. IA-LI-PD (1).

To provide a method for treating inflammatory bowel disease (IBD).SOLUTION: The present invention relates to methods of treating inflammatory bowel diseases, including with engineered peptides (e.g. peptide monomers and dimers comprising disulfide or thioether intramolecular bonds) that bind α4β7 integrin. In one aspect, the disclosure provides a method of treating an inflammatory bowel disease (IBD) in a subject in need thereof, comprising administering to the subject an α4β7 integrin antagonist, wherein the antagonist is administered to the patient orally at a dose of about 100 mg to about 500 mg, once or twice daily, wherein the antagonist is a peptide dimer compound comprising two peptides, or a pharmaceutically acceptable salt thereof.SELECTED DRAWING: Figure 22

The present application provides compounds of Formula (Ia) or (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all variables are as defined herein. These compounds are antagonists of alphaV-containing integrins. The present application also relates to pharmaceutical compositions comprising these compounds, and methods of treating diseases, disorders, or conditions associated with dysregulation of alphaV-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Described herein are α4β7 integrin inhibitors and pharmaceutical compositions containing the inhibitors. The subject compounds and compositions are useful for treating α4β7 integrin-mediated conditions, such as inflammatory bowel disease (IBD), ulcerative colitis (UC), and Crohn's disease (CD). Integrins are heterodimeric cell surface receptors composed of noncovalently associated α and β subunits and are involved in numerous cellular processes, including cell adhesion. The adhesive properties of cells can be regulated by differential expression of integrins, thus allowing different leukocyte populations to be recruited to specific organs in response to inflammatory signals.

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: