Recent advances in factor Xa inhibitors

Expert Opinion on Therapeutic Patents

Volumn 11, Issue 6, 2001, Pages 1007-1017

  Betz, A ^a  

^a Dendreon   (United States)

Author keywords

Factor Xa inhibitors; Oral bioavailability

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; 4 AMINO BENZO PYRIMIDINE; 4 AMINO BENZOPYRIDINE; AMINOIMINOMETHYL; AMIOBENZOHETEROARYL; ANTICOAGULANT AGENT; AROMATIC COMPOUND; BENZAMIDINE; BENZAMIDINE DERIVATIVE; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; CAPROLACTAM DERIVATIVE; CATION; DX 9065 A; HEPARIN; ISOQUINOLINE DERIVATIVE; ISOXAZOLINE DERIVATIVE; LOW MOLECULAR WEIGHT HEPARIN; MALONIC ACID DERIVATIVE; METHYL GROUP; PARACETAMOL; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; PYRAZOLE DERIVATIVE; PYRAZOLINE DERIVATIVE; PYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; QUINOXALINE DERIVATIVE; THIAZOLE DERIVATIVE; TRIAZOLINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN;

ANIMAL EXPERIMENT; BINDING SITE; BLOOD CLOTTING; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; NONHUMAN; PATENT; REVIEW; THROMBOCYTOPENIA;

EID: 0034976145     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.11.6.1007     Document Type: Review

References (28)

1. Cofactor proteins in the assembly and expression of blood clotting enzyme complexes
2. Low-molecular-weight heparins
3. Guide to anticoagulant therapy, Part 2: Oral anticoagulants
4. Design of benzamidine-type Inhibitors of Factor Xa
5. Recent advances in inhibitors of Factor Xa in the prothrombinase complex
6. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for Factor Xa
7. X-ray structure of active site-inhibited clotting Factor Xa. Implications for drug design and substrate recognition
8. Crystal structures of Factor Xa specific inhibitors in complex with trypsin: Structural grounds for inhibition of Factor Xa and selectivity against thrombin
9. Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation Factor Xa inhibitors
10. Structural basis for chemical inhibition of human blood coagulation Factor Xa
11. Design and synthesis of isoxazoline derivatives as Factor Xa inhibitors. 2
12. Crystal structures of human Factor Xa complexed with potent inhibitors
13. Design and synthesis of isoxazoline derivatives as Factor Xa inhibitors. 2
14. Synthesis and SAR of benzamidine Factor Xa inhibitors containing a vicinally-substituted heterocyclic core
15. Structure-based design and discovery of orally bioavailable potent nonbenzamidine factor Xa inhibitors
16. Discovery of 1- [3- (aminomethyl)phenyl] -N-3-fluoro- 2¢-(methylsulfonyl) -[1,1′-biphenyl] -4-yl]-3-(trifluoromethyl)- 1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and bioavailable inhibitor of blood coagulation Factor Xa
17. Effects of a Factor Xa inhibitor, DX-9065a, in a novel rabbit model of venous thrombosis
18. Unexpected binding mode of tick anticoagulant peptide complexed to bovine Factor Xa
19. Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as Factor Xa inhibitors
20. Nonbenzamidine compounds as selective Factor Xa inhibitors
21. 1,2-Dibenzamidobenzene inhibitors of human Factor Xa
22. Non-amidine-containing 1,2-dibenzamidobenzene inhibitors of human Factor Xa with potent anticoagulant and antithrombotic activity
23. N(2)-Aroylanthranilamide inhibitors of human Factor Xa
24. Crystallographic analysis of potent and selective Factor Xa inhibitors complexed to bovine trypsin
25. Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with Factor Xa
26. Discovery of N-[2-[5- [Amino(imino)methyl]-2- hydroxyphenoxy]-3, phenoxy]pyridin-4-yl]-N-methylglycine (ZK-807834): A potent, selective, inhibitor of the blood coagulation enzyme Factor Xa
27. 1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors
28. Factor Xa inhibitors