227751-47-5

Upstream product

• 7521-41-7 2-Aminonicotinaldehyde 
• 227751-46-4 5-[1,8]-naphthyridin-2-yl-pentanoic acid methyl ester 
• 7440-44-0 pyrographite 
• 2046-21-1 methyl 6-oxoheptanoate 
• 3128-07-2 6-oxoheptanoic acid 

Relevant academic research and scientific papers

Pyrrolidine integrin regulator and application thereof

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:

METHOD FOR MANUFACTURING NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF AND MANUFACTURING INTERMEDIATE OF NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF

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

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.

INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN

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

Disclosed are small molecule inhibitors of ανβ6 integrin, and methods of using them to treat a number of specific diseases or conditions.

COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE

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

NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF

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.

TREATMENT AGENT FOR DIAGNOSIS OR TREATMENT OF DISEASE ASSOCIATED WITH INTEGRIN

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

Alpha v integrin receptor antagonists

The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin recep

Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.

3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5f) were identified as potent and selective antagonists of the alpha(v)beta(3) receptor. These compounds have excellent in vitro profiles (IC(50) = 0.07 and 0.08 nM, respectively), significant unbound fractions in human plasma (6 and 4%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in an in vivo model of bone turnover following once-daily oral administration, these two compounds were selected for clinical development for the treatment of osteoporosis.