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FarmaPatent Limited http://www. farmapatent .com.tr. CERN "Big Bang“ Experiment 10 September 2008 Gravitons and Bosons "Missing Dark Matter“ Higgs particles. IPTS 2008 Pharmaceutical Patents Dr.Ecz . PINAR BULUT. Electronic Orange Book. Patent Data *. Exclusivity Data

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slide1

FarmaPatentLimited

http://www.farmapatent.com.tr

  • CERN
  • "Big Bang“ Experiment
  • 10 September 2008
  • Gravitons and Bosons"Missing Dark Matter“
  • Higgs particles

IPTS 2008

PharmaceuticalPatents

Dr.Ecz. PINAR BULUT

slide2

Electronic Orange Book

Patent Data *

Exclusivity Data

There is no unexpired exclusivity for this product.

* GLIMEPIRIDE; PIOGLITAZONE HYDROCHLORIDE

slide3

Marketing Exclusivity Codes:

New Combination

New Chemical Entity

New Dosage Form

New Ester or Salt of an Active Ingredient

New Product

New Route

New Strength

Thepatentsthat FDA regards as claimingthesedrugpatentsare:

1)Patentsthatclaimtheactiveingredient(s)

2)Drugproductpatent, whichincludeformulation/compositionpatents

3)Usepatentsfor a particularapprovedindicationormethod of usingtheproduct.

slide4

Council Regulation (EEC) No 1768/92 of 18 June 1992 concerning the creation of a supplementary protection certificate for medicinal products

Article 3 . Conditions for obtaining a certificate

A certificate shall be granted if, in the Member State in which the application referred to in Article 7 is submitted and at the date of that application:

(a) the product is protected by abasic patent in force;

  • Article 1 . Definitions For the purposes of this Regulation:
  • 'medicinal product' means any substance or combination of substances presented for treating or preventing disease in human beings or animals …..;
  • (b) 'product' means the active ingredient or combination of active ingredients of a medicinal product;
  • (c) 'basic patent' means a patent which protects a product as defined in (b) as such, a process to obtain a product or an application of a product, and which is designated by its holder for the purpose of the procedure for grant of a certificate;
slide5

SPC number: SPC/GB02/049 Patent No: EP0347066 (New Enantiomers and Their Isolation )Community authorisation:Sweden (7 December 2001) Product description: Escitalopram oxalate

Supplementary Protection Certificate (SPC)

slide6

SPC number: SPC/GB01/053Patent No: EP 0397831(Treatment of Obesity )Community authorisation:Germany (14 January 1999) Product description: Sibutramine hydrochloride monohydrate

Supplementary Protection Certificate

  • Claims
  • The use of N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride in the manufacture of a medicament for the treatment of obesity.
  • The use of N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride monohydrate in the manufacture of a medicament for the treatment of obesity.
caution
CAUTION ! *

For most Generic Drug Developments, Molecule Patent expiry dates are the

‘Tip of the Iceberg’

* Presented by Leighton Howard – ICSE2005 , Madrid

secondary patent s evergreening
Drug Substance

Polymorphs

Salt/Hydrate/Solvate

Prodrug, Metabolite

Impurity Profile, Substantially pure

Physicochemical properties

Particle size

Synthetic Route

New intermediates, Starting materials, Catalysts

Purification Method

Assay Technique

DrugProduct

Formulation / Composition

Combination

Manufacturingmethod

Excipients

Packaging

Medical Use

Route of Administration

Dosing Regimen

Secondary Patents (Evergreening)
polymorph patents donepezil eisai
POLYMORPH PATENTS (Donepezil – EISAI)

Claims

1. Donepezil hydrochloride ………….. in the form of polymorph (III), being specified ……… X-ray diffraction pattern and ……… infrared absorption spectra ……….

polymorph patents rosiglitazone skb
POLYMORPH PATENTS (Rosiglitazone – SKB)
  • Claims
  • A polymorphic form of …… maleicacid salt (thePolymorph) characterised in that it provides:
  • an infraredspectrumcontainingpeaks at ………. ; and/or
  • a Ramanspectrumcontainingpeaks at ………. ; and/or
  • a solid-state 13C NMRspectrumcontainingpeaks at ……; and/or
  • an XRPDpattern ……………
slide12
Scientific Considerations of Polymorphism in Pharmaceutical Solids: Abbreviated New Drug Applications *
  • POLYMORPHISM IN PHARMACEUTICAL SOLID DRUG SUBSTANCE AND THE ISSUE OF "SAMENESS“
  • A drug substance in a generic drug product is generally considered to be the same as the drug substance in the reference listed drug if it meets the same standards for identity. In most cases, the standards for identity are described in the USPalthough FDA may prescribe additional standards when necessary.
  • Because drug product performance depends on the product formulation, the drug substance in a proposed generic drug product need not have the same physical form (particle size, shape, or polymorph form) as the drug substance in the reference listed drug.

* FDA

slide13
Scientific Considerations of Polymorphism in Pharmaceutical Solids: Abbreviated New Drug Applications *
  • An ANDA applicant is required to demonstrate that the proposed product meets the standards for identity, exhibits sufficient stability and is bioequivalentto the reference listed drug.
  • Over the years FDA has approved many generic drug products based upon a drug substance with different physical form from that of the drug substance in the respective reference listed drug (e.g., warfarin sodium, famotidine, and ranitidine).
  • Also many ANDAs have been approved in which the drug substances differed from those in the corresponding reference listed drugs with respect to solvation or hydration state (e.g., terazosin hydrochloride, ampicillin, and cefadroxil).

* FDA

case 1 ranitidine
CASE 1: RANITIDINE

1. Form 2 ranitidine hydrochloride characterised by an infra-red spectrum as a mull in mineral oil showing the following main peaks:

slide16

PATENT ACT (INDIA) Amendment (5th April 2005)

INVENTIONS NOT PATENTABLE

3. What are not inventions

“(d) the mere discovery of a new form of a known substance which does not result in the enhancement of the known efficacy of that substance or the mere discovery of any new property or new use for a known substance or of the mere use of a known process, machine or apparatus unless such known process results in a new product or employs at least one new reactant.

Explanation – For the purposes of this clause, salts, esters, ethers, polymorphs, metabolites, pure form, particle size, isomers, mixtures of isomers, complexes, combinations and other derivatives of known substance shall be considered to be the same substance, unless they differ significiantly in properties with regard to efficacy.”

slide17

RESULT LISTApproximately 662 results found in the Worldwide database for:

polymorp* in the title or abstract AND

wo as the publication number AND

C07D as the IPC classification

Search International Patent Applications

Results of searching in PCT for:

ABSTRACT: POLYMORPH OR POLYMORPHS OR POLYMORPHISM

PRIORITY COUNTRY: INDIA

IPC: C07D 99 records

slide18

Search International Patent Applications

Results of searching in PCT for:

ABSTRACT: POLYMORPH OR POLYMORPHS OR POLYMORPHISM

IPC: A61K

APPLICANT: TEVA 7 records

APPLICANT: PFIZER 12 records

APPLICANT: ROCHE 3 records

Results of Search in US Patent Collection db for:

(ACLM/(crystalline AND form) AND a61k): 184 patents.

isomeric form salt and hydrate
ISOMERIC FORM, SALT and HYDRATE

Claims

1. The magnesium salt of (-)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)sulfinyl]-1H-benzimidazole (Mg-salt of the (-) enantiomer of omeprazole)

Claims

1. The magnesium salt of S-omeprazole trihydrate

impurity
IMPURITY

Claims

1. Use of escitalopram comprising less than 3% w/w of R-citalopram for the preparation of a pharmaceutical composition.

slide22

FDA TALK PAPER

Feb. 27, 1998

SELDANE AND GENERIC TERFENADINE WITHDRAWN FROM MARKET

Hoescht Marion Roussel and Baker Norton Pharmaceuticals have voluntarily discontinued distribution and marketing of all terfenadine-containing antihistamine product lines in the United States.

Terfenadine-containing products, such as Seldane and Seldane-D, have been associated with rare, but serious heart problems when taken with certain other drugs, including certain antibiotics and antifungals.

In January 1997, FDA proposed removing all terfenadine products from the marketplace because of the approval of a safer alternative drug: Allegra (fexofenadine hydrochloride).

substantially pure
SUBSTANTIALLY PURE

13.An HPLC method comprising the steps of:

  • combining an R- Tolterodine tartrate sample with a mixture of acetonitrile: water …

(b) injecting the solution into a …. column ……

(c) gradient eluting the sample from the column at about 8 min using a mixture of ……

(d) measuring the impurity content in the relevant sample with a UV detector …..

I . R-Tolterodinetartrate having less than about 0.5% area by HPLC of total impurities.

formulations compositions excipients
FORMULATIONS – COMPOSITIONS - EXCIPIENTS

Clopidogrelbisulfate tablet formulation

1. A pharmaceutical tablet which comprises clopidogrel bisulfate and a lubricant selected from the group consisting of zinc stearate, sodium stearylfumarate and stearic acid.

DryMixFormulationforBisphosphonicacids

1. A pharmaceuticalcompositioncomprisingfrom 0.5 to 40% byweight of 4-amino-1-hydroxybutylidene-1,1-bisphosphonicacidor a pharmaceuticalacceptable salt thereofandfrom 60 to 99.5% byweight of excipients, saidexcipientscomprising a diluentselectedfromanhydrouslactoseorhydrousfastflowlactose, a drybinder, a disintegrant, and a lubricant.

combinations
COMBINATIONS

1. Pharmaceuticalcompositionwhichcomprises an insulinsensitivityenhancerselectedfrompioglitazoneor a pharmaceuticallyacceptable salt thereofin combinationwithmethormin.

1. Pharmaceuticalcompositionwhichcomprises an insulinsensitivityenhancerselectedfrompioglitazoneor a pharmaceuticallyacceptable salt thereofin combinationwiththeinsulinsecretionenhancerglimepiride.

second medical use swiss claim
SECOND MEDICAL USE – SWISS CLAIM

Claims

1. Use of tomoxetine for the manufacture of a medicament for treating attention-deficit/hyperactivity disorder.

Indications

STRATTERA is indicated for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD).

dose use boniva tablet 2 5 mg 150 mg roche
DOSE / USEBONIVA Tablet 2.5 mg, 150 mg - ROCHE
  • Claims
  • Use of ibandronicacid of pharmaceuticalacceptable salt thereofforthemanufacture of a medicamentforthepreventionorthetreatment of disorderscharacterizedbypathologicalincreased bone resorptionwhereinthemedicament
  • comprises at least 120% of theexpectedefficaciousdailydose, i.e. 50 – 250 mg of ibandronicacidor a pharmaceuticalacceptable salt thereofandone of morepharmaceuticalacceptableexcipientsthereof; and
  • themedicament is orallyadministered on onedaypermonth.
use administration method
USE / ADMINISTRATION METHOD

USE OF ZOLEDRONATE FOR THE MANUFACTURE OF A MEDICAMENT OF BONE METABOLISM DISEASE

1. A method of administering 2-(imidazol-1yl)-1-hydroxyethane-1, 1-diphosphonicacidto a patient in need of bisphosphonatetreatmentcomprisingintravenouslyadministering4 mg of2-(imidazol-1yl)-1-hydroxyethane-1, 1-diphosphonicacidor a pharmaceuticalacceptable salt thereofover a period of 15 minutesto a patient in need of saidtreatment.

Zometa

(zoledronicacid) InjectionConcentrateforIntravenousInfusion

Method of Administration

Due to the risk of clinically significant deterioration in renal function, which may progress to renal failure, single doses of Zometa should not exceed 4 mg and the duration of infusion should be no less than 15 minutes

slide29

CASE 2: PERINDOPRIL Erbumine

SPC number: SPC/GB93/141

Maximumexpirydate: 21 June 2003

Product description : Perindopril,….. or an addition salt obtained with a pharmaceutically compatible mineral or organic acid, for example the tert.- butylamine salt

slide31

1. α crystalline form of a compound of Formula (I):

characterised by the following powder X-ray diffraction diagram, ……….

OPPOSITIONS

Quimica Sintetica Krka (WITHDRAWN)

Norton Healthcare Ltd Lupin Limited (WITHDRAWN )

Glenmark Pharmaceuticals Ltd Niche Generics Limited (WITHDRAWN)

Polpharma

Hetero Drugs Limited

Ratiopharm GmbH

slide32

KRKA / SERVIER

Prenessa Tablet (Perindopril erbumine)

slide33

KRKA / SERVIER

UnauditedInterimReportfortheKrkaCompanyandtheKrkaGroupforJanuary – September 2006

Based on thesettlementthecompanieswillwithdrawall legal actionsfiledagainsteachother in variouscountries.

Based on settlement, Krkawill market a productwiththeactiveingredientperindopril in alpha-crystalline form on themarketsof Slovenia, CzechRepublic, Hungary, Latvia, Lithuania, PolandandSlovakia.

slide35

APOTEX / SERVIER

Decision:

1. This is an appealfromone of thelastfirstinstancedecisions of thelate

LordJusticePumfrey. He heldthatServier’s EP (UK) 1296947 was

invalidforlack of noveltyandobviousness, but thatif patent had been

valid, Apotex’sproductwouldhaveinfringed.

Perindopriltert-butyl amine polymorph patent heldinvalidby UK SupremeCourt(GenericPharmaceuticalsandPatents, 14 May 2008)

Inthe patent spatbetweenServier (innovator) andApotex (Generic), UK supremecourtheldthe patent (EP1296947), coveringcrystallinepolymorphic form α of perindopriltert-butylamine salt,invalidovertheprior art patents i.e.EP0049658 * andEP0380341 **

* Basic patent

** Process patent

slide36

Perindopril Products in UK

SPC Expiry Date: 21 June 2003

slide40

LUPIN / SERVIER

  • India's Lupin sells further Perindopril patent rights to Servier for 20 mln eur *
  • MUMBAI (Thomson Financial) - India's Lupin Ltd said it has earned 20 mln eur by selling additional patent rights of its hypertension drug Perindopril to France-based Laboratoires Servier.
  • In April this year, Servier had reportedly bought the process patents on the drug -- marketed in Europe as Coversyl -- for 20 mln eur, while Lupin retained other patent rights.

* Forbes.com 10.12.2007

slide41

FarmaPatentLimited

http://www.farmapatent.com.tr

THANKS

PharmaceuticalPatents

Dr.Ecz. PINAR BULUT

pbulut@farmapatent.com.tr