Patent Landscape Report on Ritonavir - WIPO

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4.2.2 Innovation track 2: Synthesis of Ritonavir**Description of colored arrows can be found in table 1 in section 4.1.2.This innovation track was selected to illustrate the technical hurdles, which are present fordeveloping nations to synthesize Ritonavir. The innovation track shows how the complexity
of preparing a compound reaches beyond simply licensing for the initial disclosure and synthesisstrategies. One of the most important aspects that could easily be overlooked whentrying to prepare a compound is access to key synthetic intermediates. Key intermediatesare defined as a compound, which is produced in the course of a chemical synthesis, whichis not itself the final product, but is used in further reactions to produce the final product. Thekey intermediates are compounds that are converted to Ritonavir through common chemistrysynthetic routes. Often these intermediates that are critical precursor for preparing Ritonavirare under patent protection. The main key ingredient is the central portion of the moleculethat is described as 1,6-diphenylhexane. Key intermediates are also important because theycan often be used to prepare several Ritonavir analogs that are all described in the initialAbbott Laboratories patent application WO1994014436. This innovation track highlightsseveral key intermediates required to prepare Ritonavir. Using current synthetic strategiesRitonavir could not efficiently be prepared without licensing of these key intermediates.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 possible synthetic strategies, methods or intermediates.The second generation document is WO1995011224 (Abbott) and cites the ‘436 document.This document claims a synthesis of the Markush backbone for Ritonavir in the ‘436 document.While this intermediate is not claimed to be directly converted to Ritonavir it is still animportant intermediate worth noting. Claiming synthesis of this backbone would also be importantfor protecting synthesis of Ritonavir analogs.The third generation includes two patents WO1995023793 (Daicel) and WO2001021603 (Archimica/Clariant)and a 2B document US6407252 (Clariant). WO1995023793 describesnovel synthetic methods to prepare the substituted 1,6-diaminohexane present as the backboneof Ritonavir. This document was published shortly after the key patent(WO1994014436) so this is not the only intermediate but it could be a very important documentin the future for new methods of preparing Ritonavir or similar analogs. The ‘793document and its granted EP0748801 both describe the same preparation of key intermediates.The second third-generation document is WO2001021603, and its granted patentUS6407252 (2B). These documents describe a process to prepare Ritonavir using only fiveintermediate stages. This synthetic route is extremely efficient. The important advantage ofthis synthesis is that it uses the same starting materials as the first generation ‘436 document,but performs the synthesis with fewer reactants and materials making this a particularlyattractive route because it is both environmentally and economically conservative. Theclaims are more restrictive than expected for a second generation synthesis, but due to thehighly efficient method of preparing this severely limits other patents from preparing Ritonavirin a similar manner. IT999MI01950, which is located below the ‘603 and ‘252 documentsis the priority document for this family from which the broader family members coveringsynthesis than the ‘252 document claim priority.Please note PCT application WO1995023793 (Daicel) is included in the associated database;although the database only contains documents that specifically describe or are relatedto Ritonavir. However, this document is note-worthy in the context of this report, and
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
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Page 40 and 41: portant because of the thermal inst
Page 44 and 45: the Synthesis of Ritonavir Innovati
Page 46 and 47: several different ways. This partic
Page 48 and 49: 4.2.4 Innovation track 4: Solid Dos
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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
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OR US7632853 OR WO9746222 OR US7364
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161 PN=(WO2007071055 OR US5747490 o
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Total PatentAuthor
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Thomson InnovationCollection: US Gr
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STN- Transcript of Search History=>
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=> s l3S L3 SSS SAM FILE=REGISTRYSA
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Patent Landscape Report on Ritonavir - WIPO

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