Selective factor xa inhibitor

Rivaroxaban, an oral oxazolidinone-based anticoagulant, is a potent, selective direct inhibitor of factor Xa that is used in the prevention of.

SELECTIVE FACTOR Xa INHIBITORS WO1999007731A1 11 Aug 1998 18 Feb 1999 Cor Therapeutics, Inc.Unlike thrombin, which acts on a variety of protein substrates as well as at a specific receptor, factor Xa appears to have a single physiologic substrate, namely prothrombin.

Selective factor Xa inhibition for thromboprophylaxis

Studies of antistasin, a potent factor Xa inhibitor with anticoagulant properties, were performed wherein the properties of the full-length antistasin polypeptide.In the management of thrombotic disorders the compounds of this invention may be utilized in compositions such as tablets, capsules or elixirs for oral administration, suppositories, sterile solutions or suspensions or injectable administration, and the like, or incorporated into shaped articles.

This invention also encompasses all pharmaceutically acceptable isomers, salts, hydrates and solvates of the compounds of formulas I, II and III.A typical heterocyclic ring system will have five to ten members, 1-4 of which are heteroatoms.Update on anticoagulants: clinical support for the use of selective factor Xa inhibitors.


Selective factor Xa inhibition improves efficacy of venous

Development of Potent and Selective Factor Xa Inhibitors Roopa Rai, Aleksandr Kolesnikov, Yong Li, Wendy B.US6369080B2 - Selective factor Xa inhibitors - Google Patents.A non-occlusive thrombus is allowed to develop in the central venous circulation and inhibition of thrombus growth is then used as a measure of the antithrombotic activity of the compound being evaluated.Fondaparinux, a Synthetic Pentasaccharide: The First in a New Class of Antithrombotic Agents — The Selective Factor Xa Inhibitors Kenneth A.

FDA approves new blood thinner in Xa inhibitor class

The products may be further purified by column chromatography or other appropriate methods.

Aryl groups preferably have 6-14 carbon atoms making up the ring(s) structure, while heteroaryls preferably have 1-4 heteroatoms, with the remaining 4-10 atoms being carbon atoms.

Lack of Plasminogen Activator Inhibitor-1 Enhances the

It should be understood that various modifications can be made without departing from the spirit of the invention.Prodrug compounds of this invention may be called single, double, triple etc., depending on the number of biotransformation steps required to release the active drug within the organism, and indicating the number of functionalities present in a precursor-type form.

All of these references are incorporated herein by reference.The gum residue is dissolved in 10 mL of 0.1% TFA in water and 1 mL of 0.1% TFA in MeCN and purified by RP-HPLC to give the compound shown above, as a powder (78 mg, 100%).Effector functions include receptor or ligand binding, any enzyme activity or enzyme modulatory activity, any carrier binding activity, any hormonal activity, any activity in promoting or inhibiting adhesion of cells to an extracellular matrix or cell surface molecules, or any structural role.Prodrugs are variations or derivatives of the compounds of this invention which have groups cleavable under metabolic conditions.

The residue was extracted into 200 mL of EtOAc and washed with sat.The solution is neutralized with DIEA (3 mL) followed by the addition of coupling reagent BOP (2.7 g, 6 mmol).Publication Date (Web): October 3, 2007. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro,.

The pH of the preparations of this invention typically will be 3-11, more preferably 5-9 and most preferably 7-8.SELECTIVE FACTOR Xa INHIBITORS WO1999007732A1 11 Aug 1998 18 Feb 1999 Cor Therapeutics, Inc.The compounds of the invention may also be administered in the form of liposome delivery systems, such as small unilamellar vesicles, large unilamellar vesicles and multilamellar vesicles.The dose and method of administration will vary from subject to subject and be dependent upon such factors as the type of mammal being treated, its sex, weight, diet, concurrent medication, overall clinical condition, the particular compounds employed, the specific use for which these compounds are employed, and other factors which those skilled in the medical arts will recognize.

Selective Inhibition of Factor Xa in the Prothrombinase

Typical examples of monocyclic ring systems include piperidinyl, pyrrolidinyl, pyridinyl, piperidonyl, pyrrolidonyl and thiazolyl, while examples of bicyclic ring systems include benzimidazolyl, benzothiazolyl and benzoxazolyl, all of which may be substituted.Each of the asymmetric carbon atoms, when present in the compounds of this invention, may be in one of two configurations (R or S) and both are within the scope of the present invention.

Inhibitors of thrombosis WO1994021673A1 25 Mar 1994 29 Sep 1994 Corvas International, Inc.Antithrombotic Efficacy in a Rabbit Model of Venous Thrombosis.

Formulations typically will be stored in lyophilized form or as an aqueous solution.Thienylthiazole compounds US5028610 14 Mar 1988 2 Jul 1991 Sankyo Company Limited N-benzhydryl-substituted heterocyclic derivatives, their preparation and their use US5120718 13 Jun 1991 9 Jun 1992 Abbott Laboratories Candida acid protease inhibiting compounds US5164371 11 May 1988 17 Nov 1992 Ici Americas Inc.

Factor Xa Inhibitors: Next-Generation Antithrombotic Agents

Studies with SF303 and SK549, a New Class of Potent Antithrombotics.Thrombin is intimately involved in the process of thrombus formation, but under normal circumstances can also play an anticoagulant role in hemostasis through its ability to convert protein C into activated protein C in a thrombomodulin-dependent manner.