181997-13-7Relevant articles and documents
CATHEPSIN K INHIBITOR AND APPLICATION THEREOF
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Paragraph 0375; 0427, (2018/07/29)
The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
PIPERAZINE COMPOUNDS FOR THE INHIBITION OF HAEMATOPOIETIC PROSTAGLANDIN D SYNTHASE
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Page/Page column 112, (2008/12/04)
The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnoea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.
Novel high affinity thiophene-based and furan-based kinase ligands
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Page/Page column 57-58, (2010/11/25)
Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
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Page/Page column 77, (2010/10/20)
The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
ANTIINFECTIVE 1,2,3-TRIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page 65, (2008/06/13)
The present invention relates to novel triazole compounds of formula (I), thie pharmaceutically acceptable salts and their pharmaceutical compositions, where all symbols have meaning as defined in the description, for use in the treatment of bacterial inf
Substituent effects on the antibacterial activity of nitrogen-carbon- linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis
Genin, Michael J.,Allwine, Debra A.,Anderson, David J.,Barbachyn, Michael R.,Emmert, D. Edward,Garmon, Stuart A.,Graber, David R.,Grega, Kevin C.,Hester, Jackson B.,Hutchinson, Douglas K.,Morris, Joel,Reischer, Robert J.,Ford, Charles W.,Zurenko, Gary E.,Hamel, Judith C.,Schaadt, Ronda D.,Stapert, Douglas,Yagi, Betty H.
, p. 953 - 970 (2007/10/03)
A series of new nitrogen-carbon-linked (azolylphenyl)oxazolidinone antibacterial agents has been prepared in an effort to expand the spectrum of activity of this class of antibiotics to include Gram-negative organisms. Pyrrole, pyrazole, imidazole, triazole, and tetrazole moieties have been used to replace the morpholine ring of linezolid (2). These changes resulted in the preparation of compounds with good activity against the fastidious Gram- negative organisms Haemophilus influenzae and Moraxella catarrhalis. The unsubstituted pyrrolyl analogue 3 and the 1H-1,2,3-triazolyl analogue 6 have MICs against H. influenzae = 4 μg/mL and M. catarrhalis = 2 μg/mL. Various substituents were also placed on the azole moieties in order to study their effects on antibacterial activity in vitro and in vivo. Interesting differences in activity were observed for many analogues that cannot be rationalized solely on the basis of sterics and position/number of nitrogen atoms in the azole ring. Differences in activity rely strongly on subtle changes in the electronic character of the overall azole systems. Aldehyde, aldoxime, and cyano azoles generally led to dramatic improvements in activity against both Gram-positive and Gram-negative bacteria relative to unsubstituted counterparts. However, amide, ester, amino, hydroxy, alkoxy, and alkyl substituents resulted in no improvement or a loss in antibacterial activity. The placement of a cyano moiety on the azole often generates analogues with interesting antibacterial activity in vitro and in vivo. In particular, the 3-cyanopyrrole, 4-cyanopyrazole, and 4-cyano-1H-1,2,3- triazole congeners 28, 50, and 90 had S. aureus MICs ≤ 0.5-1 μg/mL and H. influenzae and M. catarrhalis MICs = 2-4 μg/mL. These analogues are also very effective versus S. aureus and S. pneumoniae in mouse models of human infection with ED50s in the range of 1.2-1.9 mg/kg versus 2.8-4.0 mg/kg for the eperezolid (1) control.
Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials
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, (2008/06/13)
A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula I wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen atoms where R1 is independentlyl H, OCH3, F, or Cl; and R2 is hydrogen, C1-C8 alkyl (optionally substituted with one or more of F, Cl, hydroxy, C1-C8 alkoxy, C1-C8 acyloxy), C3-C6 cycloalkyl, amino, C1-C8 alkylamino, C1-C8 dialkylamino, C1-C8 alkoxy.
Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials
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, (2008/06/13)
A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula (I) wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen a