227751-47-5Relevant academic research and scientific papers
Pyrrolidine integrin regulator and application thereof
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Paragraph 0228; 0236-0238, (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:
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Paragraph 0337; 0338, (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; 0455; 0456; 0457; 0458, (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 0348, (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; 0339, (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 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; 0380, (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
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Coleman, Paul J,Brashear, Karen M,Askew, Ben C,Hutchinson, John H,McVean, Carol A,Duong,Feuston, Bradley P,Fernandez-Metzler, Carmen,Gentile, Michael A,Hartman, George D,Kimmel, Donald B,Leu, Chih-Tai,Lipfert, Lorraine,Merkle, Kara,Pennypacker, Brenda,Prueksaritanont, Thomayant,Rodan, Gideon A,Wesolowski, Gregg A,Rodan, Sevgi B,Duggan, Mark E
, p. 4829 - 4837 (2007/10/03)
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.
Alpha v integrin receptor antagonists
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, (2008/06/13)
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
