- MITOCHONDRIA-TARGETED ISOKETAL/ISOLEVUGLANDIN SCAVENGERS AND USES THEREOF
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The use of novel 2-hydroxybenzylamine derivatives as scavengers of isolevuglandins.
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Paragraph 0062
(2021/08/06)
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- Phosphine-catalyzed sequential (2+3)/(2+4) annulation of γ-vinyl allenoates: Access to the synthesis of chromeno[4,3-: B] pyrroles
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A phosphine-catalyzed cascade (2+3)/(2+4) cyclization reaction of γ-vinyl allenoates with aldimine esters has been developed to provide a series of chromeno[4,3-b]pyrrole derivatives that contain three contiguous stereogenic centers. The method gives a good yield, excellent chemoselectivity and diastereoselectivity under mild conditions.
- Huang, You,Li, Xiaohu
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supporting information
p. 9934 - 9937
(2021/10/12)
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- NEW COMPOUNDS AND USES THEREOF FOR DETECTION OF TARGET MOLECULES IN A SAMPLE
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The present invention relates to new profluorophores and conjugates thereof and their use for the detection of target molecule in a sample, in particular nucleic acid target molecules. The invention relates to new profluorophores and new fluorophores and methods of use thereof particularly useful in the fields of diagnostics and quality control.
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Page/Page column 46; 47
(2018/04/27)
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- Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study
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Screening of a small compound library at the three excitatory amino acid transporter subtypes 1-3 (EAAT1-3) resulted in the identification of compound (Z)-4-chloro-3-(5-((3-(2-ethoxy-2-oxoethyl)-2,4-dioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic aci
- Hansen, Stinne W.,Erichsen, Mette N.,Fu, Bingru,Bj?rn-Yoshimoto, Walden E.,Abrahamsen, Bjarke,Hansen, Jacob C.,Jensen, Anders A.,Bunch, Lennart
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p. 8757 - 8770
(2016/10/22)
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- FACTOR VIIA INHIBITOR
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The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
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Paragraph 0176
(2014/04/03)
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- LIQUID PHARMACEUTICAL COMPOSITION OF FACTOR VII POLYPEPTIDE
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The invention concerns a liquid pharmaceutical composition comprising: A Factor VIIa polypeptide; A buffering agent suitable for keeping pH in the range of from about 5.5 to about 8.5; and An active site stabilizing agent, which is a compound exhibiting a
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Page/Page column 39; 40
(2014/05/07)
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- COMPOUNDS AND METHODS
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The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORy.
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Page/Page column 82
(2013/03/26)
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- COMPOUNDS AND METHODS
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The present invention relates to no vel retinoid-related orphan receptor gamma (RQRy) modulators and their use in the treatment of diseases mediated by RORy.
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Page/Page column 24
(2013/03/26)
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- The development of benzimidazoles as selective rho kinase inhibitors
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Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC50 10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
- Sessions, E. Hampton,Smolinski, Michael,Wang, Bo,Frackowiak, Bozena,Chowdhury, Sarwat,Yin, Yan,Chen, Yen Ting,Ruiz, Claudia,Lin, Li,Pocas, Jennifer,Schr?ter, Thomas,Cameron, Michael D.,LoGrasso, Philip,Feng, Yangbo,Bannister, Thomas D.
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scheme or table
p. 1939 - 1943
(2010/09/03)
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- FACTOR VIIA INHIBITOR
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The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders
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Page/Page column 39
(2010/02/15)
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- (Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
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The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
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Page/Page column 80
(2010/02/11)
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- 2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS
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The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
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- Optimization of a screening lead for factor VIIa/TF
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The structure-based design and progression of a screening lead to a 3 nM factor VIIa/TF inhibitor with improved selectivity versus related enzymes is described.
- Young, Wendy B,Kolesnikov, Aleksandr,Rai, Roopa,Sprengeler, Paul A,Leahy, Ellen M,Shrader, William D,Sangalang, Joan,Burgess-Henry, Jana,Spencer, Jeff,Elrod, Kyle,Cregar, Lynne
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p. 2253 - 2256
(2007/10/03)
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