227751-46-4Relevant academic research and scientific papers
Non-peptide αvβ3 antagonists. Part 4: Potent and orally bioavailable chain-shortened RGD mimetics
Coleman, Paul J.,Askew, Ben C.,Hutchinson, John H.,Whitman, David B.,Perkins, James J.,Hartman, George D.,Rodan, Gideon A.,Leu, Chih-Tai,Prueksaritanont, Thomayant,Fernandez-Metzler, Carmen,Merkle, Kara M.,Lynch, Robert,Lynch, Joseph J.,Rodan, Sevgi B.,Duggan, Mark E.
, p. 2463 - 2465 (2002)
Potent non-peptidic αvβ3 antagonists have been prepared where deletion of an amide bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened αvβ3 antagonists with significantly improved oral pharmacokinetics. These chain-shortened αvβ3 antagonists represent structurally novel integrin inhibitors.
Pyrrolidine integrin regulator and application thereof
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Paragraph 0228; 0233-0235, (2021/09/08)
Disclosed are a compound as represented by formula I, and a racemate, a stereoisomer, a tautomer, an isotopic marker, a nitrogen oxide, a solvate, a polymorph, a metabolite, an ester, and a prodrug thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, a preparation method therefor, and the medical use thereof. The structure of formula I is as follows:
RNAI AGENTS FOR INHIBITING EXPRESSION OF HIF-2 ALPHA (EPAS1), COMPOSITIONS THEREOF, AND METHODS OF USE
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Paragraph 0240; 0342, (2020/07/25)
The present disclosure relates to RNAi agents, for example, double stranded RNAi agents, able to inhibit HIF-2 alpha ( EPAS1 ) gene expression. Also disclosed are pharmaceutical compositions that include HIF-2 alpha RNAi agents and methods of use thereof. The HIF-2 alpha RNAi agents disclosed herein may be linked or conjugated to targeting ligands (such as compounds that have affinity for integrins, including alpha-v-beta-3 and alpha-v-beta-5 integrins) and pharmacokinetic (PK) enhancers, to facilitate the delivery to cells and tissues, including to clear cell renal cell carcinoma (ccRCC) cells and tumors. Delivery of compositions comprising the HIF-2 alpha RNAi agents in vivo provides for inhibition of HIF-2 alpha gene expression. The HIF-2 alpha RNAi agents can be used in methods of treatment of various diseases and disorders, including ccRCC.
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Paragraph 0335; 0336, (2018/09/16)
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Page/Page column 54; 55, (2018/09/21)
Disclosed are small molecule inhibitors of ανβ6 integrin, and methods of using them to treat a number of specific diseases or conditions.
METHOD FOR MANUFACTURING NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF AND MANUFACTURING INTERMEDIATE OF NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF
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Paragraph 0447; 0450; 0451; 0452; 0453; 0454, (2018/02/28)
Provided are a method for efficiently manufacturing a nitrogen-containing compound, which is used for manufacturing a treatment agent for integrin-related diseases, or a salt thereof and a manufacturing intermediate of the compound or a salt thereof. A me
N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
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Paragraph 0347, (2018/03/28)
The invention relates to compounds of formula (I), or a salt thereof wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are ανβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.
NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
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Paragraph 0336; 0338, (2016/08/17)
The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A1 represents a chelate group; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; and Z1, Z2, Z3, Z4, and Z5 are the same or different and each represent a nitrogen atom or CR3 or the like wherein R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group or the like; L1 represents a group represented by the formula (3) wherein R13, R14, R15, and R16 are the same or different and each represent a hydrogen atom or the like; L2 represents an optionally substituted C1-6 alkylene group; and L3 represents an optionally substituted C1-6 alkylene group.
COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE
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Page/Page column 46; 47, (2016/10/11)
This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administrat
TREATMENT AGENT FOR DIAGNOSIS OR TREATMENT OF DISEASE ASSOCIATED WITH INTEGRIN
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Paragraph 0376; 0377; 0379, (2018/10/03)
PROBLEM TO BE SOLVED: To provide a treatment agent for diagnosis or treatment of disease associated with integrin. SOLUTION: A treatment agent comprises a complex of a compound represented by formula (1) or salt thereof and metal. In the formula (1), A1 is a chelate group; R1 and R2 independently represent H, alkyl, or an amino protective group; Z1-Z5 independently represent N or CR3; R3 is H or a substituted/unsubstituted C1-6 alkyl group or the like; L1 is a group represented by formula (3); L2 and L3 independently represent a substituted/unsubstituted C1-6 alkylene group. In the formula (3), R13-R16 independently represent H, alkyl or the like. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
