Patent Landscape Report on Ritonavir - WIPO

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several different ways. This particular area has seen a lot of patenting activity since Abbottdiscovered the issue of heat instability of crystalline Ritonavir in its solid dosage forms in thelate 1990’s. The innovation track is particularly note worthy because the documents in latergenerations can be important in the innovation tracks related to both liquid and solid dosageforms.The first generation patent application WO1994014436, assigned to Abbott Laboratories, isthe first disclosure of Ritonavir. The ‘436 document claims a broad Markush structure describingRitonavir. This initial document only claims a retroviral protease inhibitor and doesnot describe structural considerations or conformational polymorphs of Ritonavir.The second generation contains two documents, WO1996039398 and WO1995009614,both assigned to Abbott. The ‘398 document family claims a method of preparing an HIVprotease inhibiting compound. This also describes preparing an acid addition salt of thecompound. The Markush group prepared broadly covers Ritonavir because the Markushstructure is very general. The addition salt allows for this compound to be considered acrystalline solid. This document does not specifically disclose the crystalline conformation.The second second-generation document ‘614 family, claims a solid pharmaceutical compositioncomprising Ritonavir. This document does not disclose Ritonavir as crystalline. Thisdocument was included because it is one of the first patents to describe a solid pharmaceuticalcomposition comprising Ritonavir. The ‘614 document is also present in the next innovationtrack.The third generation documents claim a version of Ritonavir polymorphs. WO200004016(Abbott) and its published patent EP1097148 describe a crystalline polymorph of Ritonavirand methods of its use and preparation. These documents claim X-ray diffraction patterns ofa polymorph. As will be described in subsequent generations, the actual crystal form is notspecifically described because this is the first X-ray characterization. These claims leave potentialfor patenting around the crystal structure of Ritonavir.The fourth generation contains three patent families including US2004024031 (TransformPharm), US20050009756 (Abbott) and US20050203152 (Abbott). US2004024031 cites theAbbott PCT ‘016 and further describes polymorphs, solvates and compositions. The ‘031document claims five specific forms of Ritonavir with unique melting points and X-ray diffractionpatterns. The document also claims specific methods for preparing each form of Ritonavir.The preparation methods do not describe reaction conditions, but do generally describe“a solvent system comprised of formamide and an immiscible or partially miscible solventto provide a mixture, and reducing the solubility of Ritonavir”. These reaction conditionsare general in their description, but this document contains five lengthy independent claims.This application has since been granted as US7205413. The second document in the fourthgeneration, US20050203152, claims a pure amorphous form of Ritonavir with a specificglass transition temperature. This document is important because a pure compound with aglass transition temperature below room temperature would need to be stored in refrigerationto prevent conformational polymorphism. The third document in the fourth generation,US20050009756, describes the similar claims and has the same priority data asEP1097148. The ‘031 document describes the same crystal structure as the EP1097148document but also includes an independent claim describing substantially pure amorphousRitonavir.
The fifth generation contains two PCT applications from Ranbaxy Laboratories,WO2006129276 and WO2008041176. These documents were also included in innovationtrack 1. These documents cite both US2004024031 and WO2000004016. These documentsfurther refine the claims by describing a process for preparing Form I of Ritonavirsimilar to the cited document US2004024031. The novel limitation compared to the ‘031document is that a seed crystal was not used to prepare the Form I crystals. The dependentclaims also provide detailed about reaction conditions for the preparation of the crystals.The sixth generation contains three documents. The first is US7205413, which is thegranted patent of the fourth generation document US200402031 and contains the same listof claims describing very specific forms of Ritonavir and methods of making the same. Thesecond in the sixth generation documents is EP2017269 (Abbott). This documents sharespriority data and also cites the second generation document US5567823 (Abbott) which describesRitonavir synthesis. EP2017269 claims a method for preparing a pharmaceuticalcomposition comprising Form II crystalline Ritonavir. The Form II crystals have the samecrystalline structure identified in the third generation document WO2000004016 (Abbott).The earlier document did not appear to assign the crystal structure with a “form” becausethis was one of the first references to crystal structures of Ritonavir.This is still a very active area of patenting because many of the patents during the last decadehave been focused on characterizing crystal structures. Once all stable crystal structuresare determined and characterized there is expected to be an increase in patent filingsrelated to specific delivery forms containing the various Ritonavir polymorphs.
Page 1 and 2: Patent Lan
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Page 6 and 7: STN- Transcript of Search History .
Page 8 and 9: priority to an earlier Italian pate
Page 10 and 11: Section 2 - Search Process2.1 Intro
Page 12 and 13: these documents differed from WO199
Page 14 and 15: prevented along with compound names
Page 16 and 17: Section 3 - Statistical Analysis3.1
Page 18 and 19: Figure 2 shows that the overall pat
Page 20 and 21: Figures 4 and 5 show the most commo
Page 22 and 23: Figure 6 illustrates the percentage
Page 24 and 25: Figure 8 shows the distribution of
Page 26 and 27: Patent AuthorityNu
Page 28 and 29: Figure 11a: Geographic distribution
Page 30 and 31: PatentAuthorityNum
Page 32 and 33: Figure 14 shows the most common inv
Page 34 and 35: Intellixir was used in concert with
Page 36 and 37: 4.1.2 Brief description of innovati
Page 38 and 39: The fourth innovation track focuses
Page 40 and 41: portant because of the thermal inst
Page 42 and 43: 4.2.2 Innovation track 2: Synthesis
Page 44 and 45: the Synthesis of Ritonavir Innovati
Page 48 and 49: 4.2.4 Innovation track 4: Solid Dos
Page 50 and 51: The broad independent claim languag
Page 52 and 53: are cited by more than one other do
Page 54 and 55: US6765019 cites WO9404193 (describe
Page 56 and 57: WO9933815. Also, the ‘869 documen
Page 58 and 59: Section 5 - Report
Page 60 and 61: AppendicesAppendix 1 - Innovation T
Page 62 and 63: 1.3 Polymorphs
Page 64 and 65: 1.5 Prodrugs of RitonavirInnovation
Page 66 and 67: ECLA Classification System: ECLA st
Page 68 and 69: Appendix 3 - Ritonavir Pate
Page 70 and 71: US4725583 OR US4725584 OR US4826815
Page 76 and 77: "HOFFMANN_LA_ROCHE_F_AND_CO_A_G" OR
Page 78 and 79: "A61K9/50" OR "A61K9/52" OR "A61K9/
Page 80 and 81: WO08051039 OR US2006205697 OR WO050
Page 82 and 83: WO09045975 OR US2009226431 OR WO071
Page 84 and 85: WO08141227 OR WO08098789 OR WO09047
Page 86 and 87: US7754718 OR WO10077317 OR US201017
Page 90 and 91: US2006099170 OR EP1219605 OR CN1768
Page 92 and 93: OR US7632853 OR WO9746222 OR US7364
Page 94 and 95: 161 PN=(WO2007071055 OR US5747490 o
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Total PatentAuthor
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Thomson InnovationCollection: US Gr
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