1. New Uses For Old Compounds September 12, 2013 Chris Curfman, JD, PhD ccurfman@mcciplaw.com Phone (404) 645-7700 www.mcciplaw.com

2. Agenda A word about patents and the role of the claims Is it truly an old compound? References that are not enabled References that disclose a broad genus References that do not disclose uses or properties Intermediates / Metabolites The compounds old, now what? Is the method truly new? Inherency cases Exemplary claims Foreign considerations

3. A property right it is a right to exclude others. – Tangible: real property, personal property – Intangible: right of publicity, right of privacy A patent is a property right and the right is defined by the claims. Patents and the role of the claims The name of the game is the claim. -- Hon. Rich

4. 1.A compound having Formula I. 1.A method of treating cancer comprising administering a compound having Formula I. Patents and the role of the claims

5. 35 USC 102 Is it truly an old compound? (1)The claimed invention was patented, described in a printed publication, or in public use, on sale or otherwise available to the public before the effective filing date of the claimed invention; or (2)The claimed invention was described in a patent or published application that as effectively filed before the effective date of the claimed invention. the differences between the subject matter sought to be patented and the prior art are such that the subject matter as a whole would have been obvious at the time the invention was made to a person having ordinary skill in the art to which said subject matter pertains. 35 USC 10235 USC 103

6. The question is whether the claimed compound is described in the reference or not. The description of the compound must be enabled. If the prior art offers no more than a starting point for further experiments, if its teachings will sometimes succeed and sometimes fail, if it does not inform the art without more how to practice the new invention, it has not correspondingly enriched the store of common knowledge, and it is not an anticipation. Hon. Learned Hand, 1942. Is it truly an old compound?

7. References that are not enabled In re Brown, 329 F.2d 1006 (CCPA 1964) Reference disclosed compositions comprising copolymers of a perfluoroalkylsiloxane. Reference stated attempt to prepare fluorine containing silicone homopolymers have been unsuccessful. Claims recited compositions comprising homopolymers of perfluoroalkylsiloxane. Ct. the true test of any prior art relied on to show or suggest that a chemical compound is old, is whether the prior art is such as to place the disclosed "compound" in the possession of the public.

8. A reference listed two compounds within the claims, but evidence suggested a method of synthesis was not developed until later. Ct. Mere naming of a compound in a reference, without more, cannot constitute a description of the compound. The more is--a person having ordinary skill in the art's ability to make the claimed compound. It is not necessary that the compound have actually been made. Prior Arts description + PHOSITAs skill = publics possession. It is applicants burden to prove this is not so. References that are not enabled In re Wiggins 488 F.2d 538 (CCPA 1973)

9. No use described in the reference In re Hafner, 410 F.2d 1403 (CCPA 1969) Hafner invented new chemical compounds and filed Application 1. Problem: He didnt disclose a use for the compounds in the application. Rejected under §112. Hafner found a use for the compounds and filed Application 2 four years later. This application was enabled under 112. Problem: now anticipated under §102 in view of Application 1. Double Standard! How can PTO say App 1 was not enabled enough for it to be granted but then say it was enabled enough to be used as prior art against App 2? Look to the statutes: §112 requires description of how to make and use the compound, §102 does not.

10. Reference is silent as to a property Titanium Metals Corp. v. Banner, 778 F.2d 778 (Fed. Cir. 1985) 1. A titanium based alloy consisting essentially of 0.6-0.9 wt.% Ni, 0.2-0.4 wt.% Mo, up to 0.2 wt.% Fe, said alloy being characterized by good corrosion resistance in hot brine environments. Russian article had graph with data point corresponding to alloy. No mention of properties. Ct. Discovery of a new property of a known compound cannot impart patentability to claims to the known compound. A compound and its properties are inseparable.

11. Reference forms compounds as an intermediate or metabolite Shering Corp. v. Geneva Pharm et al., 348 F.3d 992 (Fed. Cir. 2003) 1. A compound of the formula Prior Art Claritin TM Enabled! ^ Isolated

12. Reference generically describes compound In re Baird, 16 F.3d 380 (Fed. Cir. 1994) Prior Art wherein R is selected from substitute and unsubstituted alkylene radicals having from about 2 to about 12 carbon atoms, alkylidene radicals having from 1 to 12 carbon atoms and cycloalkylidene radicals having from 3 to 12 carbon atoms; R and R are selected from substituted and unsubstituted alkylene radicals having from 2 to 12 carbon atoms, alkylene arylene radicals having from 8 to 12 carbon atoms and arylene radicals; X and X are selected from hydrogen or an alkyl radical having from 1 to 4 carbon atoms; and each n is a number from 0 (zero) to 4. Baird Invention The same as Prior Art when n 1 and n 2 = 0, X and X = H, and R = C 3.

13. Genus / Species Issues Claim Art Claim

14. Whether an earlier disclosed genus anticipates or renders obvious a later species depends on the facts. A broad genus does not necessarily describe every species within the genusyour compound may still be new. Can youat once envisage each member of the genus? Genus / Species Issues

15. Guidelines for determining whether a compound is old Does the reference describe the compound clearly? If so, can PHOSITA make it? Must one develop a unique synthesis or purification to arrive at the compound? If not, is there a close analog described and the differences are minimal or suggested? Does the reference necessarily make the compound (intermediate or metabolite)? Must one make vast numbers of selections from numerous variables to arrive at the compound? Are there valuable subgenus? Dont give up too easily on compound claims.

16. A truly old compound: Now What? Cannot claim the compound. Must claim its method of use. But is the method truly new (and non-obvious)? Again, the name of the game is the claim. The steps recited in claim must define a different act that in the prior art.

17. Inventor A patents a shoe polish for shinning shoes (A composition for polishing shoes comprising X.) Inventor B claims – A method of polishing shoes comprising applying X to shoes? – A method of repelling water on shoes comprising applying X to shoes? – A method of growing hair comprising applying X to skin? Inherency: a classic hypo Catalina Marketing Intl, v. Coolsavings.com, 289 F.3d 801 (Fed. Cir. 2002)

18. Inherency Rules Under the principles of inherency, if the prior art necessarily functions in accordance with, or includes, the claim limitations, it anticipates. A limitation or the entire invention is inherent in the prior art if its the natural result flowing from the explicit disclosure of the prior art. Inherency is not necessarily coterminous with knowledge of ordinary skill in the art. Artisans of ordinary skill may not recognize the inherent characteristics or functioning of the prior art.

19. 19 Inherency - Perricone Case Perricone v. Medicis Pharmaceutical, 432 F.3d 1368 (Fed. Cir. 2005) 1.A method for treating skin sunburn comprising topically applying to the skin sunburn [a ascorbic acid fatty acid ester]. 8.A method for preventing sunburn damage to exposed skin surfaces, comprising applying to exposed skin surface.... 1.A method for the treatment of skin disorders which arises because of depleted or inhibited collagen synthesis [which happens to all skin] comprising topically applying to affected skin areas.... 9.A method for the treatment of damaged or aging skin and epithelial tissue disorders comprising topically applying to affected tissue areas [skin that ages].... Prior Art: A composition for topical application to skin containing... ascorbyl palmitate.

20. Inherency – Rapoport Rapoport v. Dement, 254 F.3d 1053 (Fed. Cir. 2001) 1.A method for treatment of sleep apneas comprising administering a therapeutically effective regimen of a compound of Formula I (buspirone). Application referred to administration at bedtime and at higher doses. Prior art disclosed treatment of anxiety in patients suffering from sleep apnea with buspirone. Did not address treatment of underlying disorder. Did not actually administer to those suffering with sleep apnea. Disclosed lower doses. 20

21. 1. A method of preparing a food product rich in glucosinolates, comprising germinated cruciferous seeds... harvesting sprouts before the 2-leaf stage to form a food product comprising a plurality of sprouts. Prior art was nature. Ct. A new sprout was not claimed nor a new way of growing it. Patentee simply describes unexpected benefit of a known process. Inherency – Cruciferous In re Cruciferous Sprout Litigation, 301 F.3d 1343 (Fed. Cir. 2002)

22. 22 Scenarios to look out for Treatment and the mechanism underlying the treatment. Related methods of treatment or prevention. Discovered benefits or advantages of a method.

23. Now that you know what you know, what can you do differently? Give compound to a different group of people? Give compound in a different way (route or timing)? Give compound in a different dose? Combine compound with a different composition, therapy, or test?

24. Example claims Claims reference a different patient population. – Method of treating a patient with disease X, comprising administering to said patient compound Y. – Method of treating disease X, comprising screening/identifying a patient with disease X and administering to said patient compound Y. Caution: recite intended purpose for which the method is performed not merely a desired effect the method may achieve

25. Claims reference a different regimen. – A method of treating disease X, comprising administering an amount of compound Y effective to treat disease X. – A method of treating disease X, comprising administering twice daily compound Y. – A method of treating disease X, comprising co- administering compounds Y and Z. – A method of treating disease X, comprising topically administering a composition comprising Y. Example claims

26. Compositions – A composition comprising compound Y and a pharmaceutically acceptable carrier. – An emulsion for optical administration comprising compound Y, an emulsifier, and a preservative. – A composition (or kit) comprising compound Y and compound Z. – A pill comprising 10 mg of compound Y. – A kit comprising an assay for detecting disease X and a composition comprising compound Y. Example claims

27. Claims for screening – A method of identifying a compound that treats disease X, comprising contacting a cell with compound Y and a test compound; and determining whether the test compound is more efficacious than compound Y Example claims

28. Domination Domination of second party by first party – First partys compound claim dominates all subsequent uses of that compound – Second party is infringing first partys compound claim even for new use of claimed compound – Second party, to avoid liability on compound patent, has to 1. Take a license 2. Invalidate patent 3. Await expiration of patent – Second party has a blocking patent on the new use. First party cannot practice new use without infringing Second party.

29. Problems with method of use claims Dominated by a patent on composition. Difficult to detect infringement of the method If detected, it is usually the end user. Sue manufacturer under contributory infringement – Sale of compound isnt infringement if sale is connected to non-infringing use / not directed to infringing use

30. Foreign considerations Methods of use in non-medical fields are ok. Compositions are patentable –even if only used in medical treatment. Methods of medial treatment are NOT eligible subject matter in foreign countries. – First medical use claims. Compound Y (novel) for use in therapy. Compound Y (known) for use in therapy. A purpose limited product claim. – Second medical use or Swiss-style claims Use of compound Y (known) for the manufacture of a medicament for treating disease X (a secondary indication).

31. Foreign considerations Is it really a medical method? – Contraception is not a medical method. – Solely cosmetic effects are not medical methods (e.g., weight loss in non-obese people). – Cosmetic and therapeutic are medical methods (e.g., removing plaque in teeth). – Diagnosis is a medical method if it leads to concrete diagnosis.

32. Thank You Chris Curfman, JD, PhD ccurfman@mcciplaw.com Phone (404) 645-7700 www.mcciplaw.com Its all in how you claim it