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IN THE UN@ZD ZjXW-& PA&NT AND TRADEMARK OFFICE5196,40423 March 1993Filed:6 July 1990Inventors:Maraganore et al.REcP/m- -Title: INHIBITORS OF THROMBINFEB id 0 ?ijOlCommissioner for PatentsWashington, D.C. 20231Box Patent Ext.OFFlCEOFPETiTlONSAPPLICATION PURSUANT TO 35 U.S.C 9156(d)(l) AND37 C.F.R. 5j1.740FOR EXTENSION OF PATENT TERMHon. CommissionerApplicants hereby request that the term of the above-identified United States Patentbe extended pursuant to 35 U.S.C. 156. The information required by 37 C.F.R. §1.74O(a) sprovided below and in the Appendices.
(1)
The generic name of the approved product is bivalirudin. Its chemical nameand physical characteristics are provided in Appendix A.
(2)
The regulatory review of the approved product occurred pursuant to section505(b) of the Federal Food Drug and Cosmetic Act (SeeAppendix B).(3)The date on which the approved product received permission forcommercial marketing was 15 December 2000.(4)The active ingredient in the approved product is bivalirudin. Bivalirudinhas not been previously approved for commercial marketing or use under theFederal Food, Drug and Cosmetic Act, the Public Health Service Act, or the Virus-Serum-Toxin Act.1
(6)
The patent for which an extension is being sought is in the name of theinventors John M. Maraganore, John W. Fenton, II and Toni Kline. The UnitedStates Patent No. is 5,196,404 “The Patent”). The patent issued on 23 March 1993and will expire on 23 March 2010. The patent is exclusively licensed by theapplicant. (SeeExhibit C)(7)A copy of The Patent is provided herewith as Appendix D.
03)
A copy of a certificate of correction dated 18 October 1994 s providedherewith as Appendix E. A reexamination certificate issued 10 September 1996 sprovided herewith as Appendix F. A receipt for a maintenance fee paid in August1996 s provided herewith as Appendix G. A receipt for a maintenance fee paid inAugust 2000 s provided herewith as Appendix H. No disclaimer has been madefor this patent.OFFICEOFPETITIONS2
(9)
The approved product is covered by claims l-6,9,13, 14, 16 and 21 of ThePatent. This is illustrated for claim 1 below.a catalytic site -directed moiety that bindsto and inhibits the active site of thrombin;wherein said catalytic site -directed moietyis selected from serine protease inhibitors
. . .
a linker moiety characterized by a backbone
t
hain having a calculated length of betweenabout 18A and about 42A; andan anion binding exocite associating moiety;catalytic site-directed moiety beingound to said linker moiety and said linkerbeing bound to said anion bindingassociating moiety; (SeeAppendix Dsaid inhibitor is capable ofbinding to the catalytic sitend the anion binding exosite of thrombin.Elements of the amroved moductBivalirudin is a thrombin inhibitor (seeAppendix I).The catalytic site -directed moiety ofbivalirudin binds to and inhibits the activesite of thrombin (seeAppendix I).The catalytic site -directed moiety ofbivalirudin is a serine protease inhibitorwhich inhibits the serine proteasethrombin (SeeAppendix I).Yhe inker region of bivalirudin is thejeptide Gly-Gly-Gly-Asp-Gly-Asp-Phe, aIreferred linker within the 18A to 42Aength range (SeeAppendix I and Appendix1 at Col. 9,1. 25-47).livalirudin has a moiety that specificallybinds he anion-binding exosite of thrombinSeeAppendix I and Appendix D) .ippendix D, at Col. 9,1. 50-67, defines theIreferred anion-binding exosite associatingnoiety as W-Bl-B2-B3-B4-B5-B6-B7-B8-2,vherein W is a bond, Bl is Glu, B2 is Glu, B3seeAppendix E, first page) is Ile, B4 is Pro,15 s Glu, B6 is Glu, B7 is Tyr-Leu, B8 is abondand 2 is OH. As shown in Appendix 1.his section of Appendix D describes the.nion-binding exosite associating moiety oflivalirudin.n bivalirudin, the catalytic site-directednoiety is bound to the linker moiety by abeptide bond and the linker moiety is bound3 the said anion binding exosite associatingnoiety by a peptide bond (SeeAppendix I).1ivalirudin is capable of simultaneouslyiinding to the catalytic site and the aniontinding exosite of thrombin (SeeAppendixI.3
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