API and IP Newsletter

 

Contents

  • Analysis of Sun Pharma’s patent filing strategy Part I 

  • General information. 

    • Adamas Pharma (ADMS) Announces Agreement to Settle Patent Litigation with Osmotica

    • HHS Shuts Down FDA's Unapproved Drugs Initiative.

  • Intellectual Property.

Analysis of Sun Pharma’s patent filing strategy Part I

Many generic companies do work on their IP strategies soon after the innovator launches the product. Earlier, we analysed the import-export database of Sun Pharmaceuticals and we discovered Sun is no different than the other top generic companies in terms of molecule selection for development. However, there were a few very interesting products in their development portfolio.

This week, we started analysing the patent portfolio of Sun Pharma where priority filing dates would be from late 2012 to late 2014. This means research activities must have started at least one year prior to the priority date. So, patent families listed below could have been reflecting research period between 2012 and 2014. Sun (Ranbaxy) used to file many patent applications for processes and polymorphs within one year of the molecule approval by FDA.

Couple of NCE molecules from acquired companies are still being prosecuted!

This is only a part of the analysis as mentioned, i.e. research carried out till late 2014. Further analysis will follow in the subsequent weeks. 

Most of the IP is now abandoned!

 

Publication Number

Title

Publication Date

Related To

Product

SIDVIM Comments

WO2015186065A1

Preparing 4-dimethylaminocrotonic acid or its salt used to prepare Afatinib, comprises converting 2,2-diethoxy-N,N-dimethylethanamine to ethyl-4-(dimethylamino) crotonate and hydrolyzing resultant product

2015-12-10

Process

Afatinib

Approval in July 2013 and priority in June 2014. Development must have started soon after the approval.

WO2016001844A1

New amorphous form of Afatinib dimaleate is tyrosine kinase inhibitor, useful for treating metastatic non-small cell lung cancer

2016-01-07

Crystalline Form

Afatinib

Not prosecuted, and could be reproducibility issue, this form would not have been commercialised and hence must have been withdrawn.

WO2015145286A1

New amorphous form of Baricitinib useful for treating diseases including inflammatory diseases, autoimmune disorders, diabetic nephropathy, and cancer

2015-10-01

Crystalline Form

Baricitinib

Approval in 2018! Development started much earlier than FDA approval.

WO2015166434A1

New crystalline form of Baricitinib having specified X-ray powder diffraction pattern with peaks is Janus Kinase inhibitor useful for treating inflammatory diseases, autoimmune disorders, diabetic nephropathy, and cancer

2015-11-05

Crystalline Form

Baricitinib

 

WO2015121769A1

Preparing methyl N-((benzyloxy)carbonyl)-L-leucyl-L-phenylalaninate, used to prepare carfilzomib, comprises condensing methyl L-phenylalaninate or its salt with N-((benzyloxy)carbonyl)-L-leucine in the presence of boric acid

2015-08-20

Process

Carfilzomib

2012 approval, Ranbaxy must have started working on the process immediately upon FDA approval and later given up the prosecution and abandoned the family!

WO2015040571A1

Preparing Dapagliflozin involves hydrolyzing the dapagliflozin derivative in the presence of an amine base

2015-03-26

Process

Dapagliflozin

Approved in January 2014, priority date of this application is 23-09-2013. Ranbaxy had started working much before FDA approval! This application is withdrawn.

WO2015044849A1

Preparation of ((2R,3R,4R,5S)-3,4,5-tris(acetyloxy)-6-(4-chloro-3-((4-ethoxyphenyl) methyl) phenyl) oxan-2-yl) methyl acetate used for treating type-2 diabetes mellitus, involves acetylating Dapagliflozin in solvent in absence of pyridine

2015-04-02

Process

Dapagliflozin

Withdrawn

WO2015063726A1

Preparation of 4-bromo-1-chloro-2-(4-ethoxy-benzyl)-benzene, used as intermediate to prepare Dapagliflozin, comprises reacting substituted 5-bromo-2-chloro-benzoyl compounds with phenetole and reducing the obtained reaction product

2015-05-07

Process

Dapagliflozin

Withdrawn

WO2015128853A1

Pharmaceutical composition used for treating diabetes comprises of solid dispersion of Dapagliflozin and pharmaceutical excipient

2015-09-03

Composition

Dapagliflozin

Unlike above Ranbaxy applications for API, this was Sun’s application for composition, it was also withdrawn in key jurisdictions.

WO2015198227A1

New Dapagliflozin citric acid co-crystal used in pharmaceutical composition used for treatment of type 2 diabetes mellitus

2015-12-30

Crystalline Form

Dapagliflozin

This was a co-crystal application by Sun. This is active in US, maybe Sun was thinking of a 505 (b) (2) filing in US.

WO2015087239A1

Preparation of Darapladib involves reacting 2-((4-fluorobenzyl) sulfanyl)-1,5,6,7-tetrahydro-4H-cyclopenta(d)pyrimidin-4-one with ethyl bromoacetate, hydrolyzing, and reacting with diamine in presence of boric acid (derivatives)

2015-06-18

Process

Darapladib

Originally a Ranbaxy application. Study failed in May 2014, priority application filed in 2013, in an anticipation of approval, which GSK never got! Ranbaxy abandoned after filing PCT.

WO2015092687A2

Purification of Darapladib used for treatment of atherosclerosis involves providing solution of crude Darapladib in organic solvent including n-heptane or denatured alcohol, and isolating pure Darapladib

2015-06-25

Process

Darapladib

Ranbaxy application, withdrawn.

WO2015114479A1

New crystalline forms of e.g. Darapladib oxalate, Darapladib adipate, Darapladib succinate, Darapladib phosphate or Darapladib sulfate are lipoprotein associated phospholipase-2 inhibitors useful to treat atherosclerosis

2015-08-06

Crystalline Form

Darapladib

 

WO2015063720A1

Preparation of Enzalutamide used as intermediate for pharmaceuticals, involves reacting 2-((4-acetyl-3-fluorophenyl) amino)-2-methylpropanal compound with 1-isocyano-2-methyl-4-(propa-1,2-dien-1-yl)benzene, and isolating Enzalutamide

2015-05-07

Process

Enzalutamide

Approval of capsule in 2012. Ranbaxy must have started working on it immediately upon approval. Tablet approval in 2020 by innovator, might improve the market.

WO2015092617A1

Preparing Enzalutamide used to treat metastatic castration-resistant prostate cancer, comprises reacting O-phenyl carbonochloridothioate with amino-2-(trifluoromethyl)benzonitrile, and reacting product with substituted phenylamino compound

2015-06-25

Process

Enzalutamide

Ranbaxy application withdrawn.

WO2015121768A1

Preparation of Enzalutamide involves reacting 4-amino-2-fluoro-N-methylbenzamide and 1,1,1-trichloro-2-methylpropan-2-ol in alcohol, and reacting obtained compound with 4-isothiocyanato-2-(trifluoromethyl)benzonitrile

2015-08-20

Process

Enzalutamide

Ranbaxy application withdrawn.

WO2015105652A1

Treating subject after ocular surgery, involves administering composition comprising corticosteroid in vehicle that provides sustained release of corticosteroid to eye of subject

2015-07-16

Eye Care

Eye Care

Eye care. Application by Insite Vision Incorporated. Active only in JP.

WO2015179527A1

Ophthalmic formulation useful for treating or preventing ocular disease or condition comprises active agent comprising Brinzolamide, Latanoprost, Brimonidine, and/or Bosentan, polyoxyl lipid or fatty acid, and polyalkoxylated alcohol

2015-11-26

Composition

Eye Care

Ophthalmic product filed by Ocular Technologies. Being prosecuted in many countries.

WO2015181802A2

Oral pharmaceutical composition of Isotretinoin used for treating e.g. acne is prepared using process that comprises wet or dry granulation, using fluidized bed granulator or high shear mixer granulator and direct compression

2015-12-03

Composition

Isotretinoin

Roche decided to discontinue manufacturing due to diminishing market share, availability of many generic versions and the settling of multiple lawsuits over side effects. It continues to be manufactured as of 2019 by Absorica, Amnesteem, Claravis, Myorisan, Sotret, and Zenatane.

WO2015186039A1

Oral composition useful for treating e.g. acne, musculoskeletal and connective tissue inflammations and emphysema, comprises Isotretinoin, and a solvent comprising monoalkyl ether of diethylene glycol, oily vehicle and/or optionally ethanol

2015-12-10

Composition

Isotretinoin

Sun application, being prosecuted in many key jurisdictions.

WO2015011609A1

Preparation of tert-butyloxycarbonyl-protected intermediate for preparing Linagliptin for treating diabetes mellitus type-2, involves reacting quinazoline bromoxanthine intermediate with tert-butyl N-piperidinyl-carbamate intermediate

2015-01-29

Process

Linagliptin

 

WO2015087240A1

Preparation of 1-(4-methyl-2-quinazolinyl)methyl-3-methyl-7-(2-butyn-1-yl)-8-bromoxanthine used for preparing Linagliptin, involves reacting 2-chloromethyl-4-methyl-quinazoline and 8-bromo-7-but-2-ynyl-3-methyl-3,7-dihydropurine-2,6-dione

2015-06-18

Process

Linagliptin

 

WO2014042043A9

Pharmaceutical composition used to treat disease caused by fungus comprises Luliconazole; and at least one component of carboxylic acid, ketone, phosphoric acid, local anesthetic, antihistamine, or polyoxyethylene-based nonionic surfactant

2015-05-21

Composition

Luliconazole

Luliconazole, 2013 November approval. Pola must have started working on the molecule much before the approval! Priority of application September 2012! Sun Pharma acquired Pola in 2018.

WO2014136282A8

Luliconazole crystal for preparing pharmaceutical composition for vaginitis and pneumonia, has monoclinic crystal system having specified space group and lattice constants, and is recrystallized from alcohol optionally containing water

2015-08-20

Crystalline Form

Luliconazole

Luliconazole crystal

WO2015033612A1

New luliconazole crystals used as raw material in pharmaceutical composition for providing antifungal effect and treating fungal diseases e.g. dermatomycosis

2015-03-12

Crystalline Form

Luliconazole

Lot of work is being done on Luliconazole in 2013-2014.

WO2015076352A1

Pharmaceutical composition used for treating pneumonia associated with Fusarium fungus and potentially with protozoan and/or intracellular parasite as causative microorganism, comprises Luliconazole or Lanoconazole

2015-05-28

Composition

Luliconazole

 

WO2015166472A1

Extended-release liquid composition of Metformin used for treating type II diabetes comprises cores of Metformin coated with release controlling polymer, and suspension base

2015-11-05

Composition

Metformin

 

WO2015004617A1

Timed extended-release pharmaceutical composition useful for treating e.g. hypertension, comprises core comprising Metoprolol; extended-release coating comprising extended-release polymer; and outer coating layer comprising enteric polymer

2015-01-15

Composition

Metoprolol

Metoprolol ER is always difficult to make formulation. Ranbaxy must have tried to develop a bioequivalent formulation. Perhaps it would not have met BE and hence later withdrew or stopped prosecution.

WO2015040573A1

New mirabegron dimethylsulfoxide solvate having specified X-ray diffraction peaks is beta-3 adrenergic agonist used to treat overactive bladder with symptoms of urinary incontinence, urgency and urinary frequency

2015-03-26

Crystalline Form

Mirabegron

Mirabegron June 2012 approval and September 2013 Polymorph application!

WO2015040605A1

New crystalline form of mirabegron useful for treating urinary incontinence, urgency and urinary frequency

2015-03-26

Crystalline Form

Mirabegron

 

WO2015130957A1

New substituted heterocyclic compounds are sodium channel, voltage gated, type IX alpha subunit inhibitors useful for treating e.g. pain, epilepsy, Parkinson's disease, mood disorders, psychosis, tinnitus and amyotrophic lateral sclerosis

2015-09-03

NCE

NCE

New compounds by filed by Zalicus Pharmaceuticals, Ltd. Sun acquired Canadian company in 2015. This application is still under prosecution in US. Something could be interesting here.

WO2015173590A1

New isolated polypeptide useful for transformation of (S)-reticuline to (R)-reticuline and for producing Papaver plant, comprises domain comprising specific amino acid sequence

2015-11-19

NCE

NCE

Application filed by The University of York, Sun Pharmaceutical Industries (Australia) Pty Limited. Application granted in US, being prosecuted in EU, AU and few other countries. Something must be very interesting here in cDNA nucleotide sequence.

WO2015092624A1

New Nilotinib mono-oxalate is kinase inhibitor useful for e.g. treating adult patients with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia in chronic phase

2015-06-25

Crystalline Form

Nilotinib

2007 approval. Launch possible in 2023. However, this Ranbaxy application is withdrawn.

WO2015001488A1

Extended-release tablet of Paliperidone used to treat neurological disorders, comprises core comprising first and second drug layer comprising e.g. rate-controlling polymer, seal coating layer, and extended-release coating

2015-01-08

Composition

Paliperidone

First ER composition approved in 2006. This must be reasonably late filing by Ranbaxy and hence later withdrawn.

WO2015015390A1

Closure assembly for dispensing liquid drug formulation to patient, has metered dosing system installed upon liquid drug formulation container and comprising cap with piston attached to cap, doser, and dip tube attached to doser

2015-02-05

Platform

General Purpose

Ranbaxy application for dispensing metered dose. This could not have prosecuted due to commercial unattractiveness of the product.

WO2015028972A1

Pulsatile-release dosage form, useful for treating e.g. hypertension, Parkinson's syndrome and arthritis, comprises core comprising drug and excipients, and coating layer comprising water-soluble polymer and water-insoluble polymer

2015-03-05

Platform

General Purpose

Ranbaxy application, withdrawn.

WO2015044880A1

Palatable oral liquid composition useful for treating diabetes, comprises a dipeptidyl peptidase-IV inhibitor, and an excipient

2015-04-02

Platform

General Purpose

Ranbaxy application, withdrawn.

WO2015071859A1

Oral dispersible composition useful for treating diabetes, comprises dipeptidyl peptidase 4 inhibitor and excipients

2015-05-21

Platform

General Purpose

Diabetes treatment, Ranbaxy application, withdrawn.

WO2015087241A1

Crush-resistant oral solid dosage form comprises a drug prone to abuse, and chewing gum base comprising chewable plastic polymer e.g. polyisobutylene, butadiene styrene and terpene resins

2015-06-18

Platform

General Purpose

Chewing gum-based composition. Ranbaxy application, withdrawn.

WO2015145459A1

Immediate release biphasic matrix solid dosage form useful as abuse deterrent, comprises intragranular phase comprising drug susceptible to abuse and reverse enteric polymer, and extragranular phase comprising alkalizer

2015-10-01

Platform

General Purpose

Sun Pharma application, being prosecuted in many jurisdictions. Must be an interesting composition.

WO2015166473A1

Extended-release suspension composition comprises multiple coated cores comprising core which comprises active ingredient, and coating layer over core comprising release-controlling polymers, and suspension base

2015-11-05

Platform

General Purpose

Sun Pharma application, being prosecuted in many jurisdictions. Must be an interesting composition.

WO2015186040A1

Clear nanoemulsion composition used to treat e.g. heart disorder and attention deficit disorder, comprises active ingredient, oily phase comprising medium-chain or short-chain glycerides, surfactant, optionally co-solvent, and aqueous phase

2015-12-10

Platform

General Purpose

Nanoemulsion composition by Sun Pharma. Abandoned!

WO2015114509A1

Stabilized gastroretentive tablet comprises Pregabalin, swellable polymer, pH modifier, and other excipients

2015-08-06

Composition

Pregabalin

Ranbaxy application, abandoned.

WO2015011617A1

Preparing 5-chloro-N-(2-hydroxy-3-((4-(3-oxo-4-morpholinyl)-phenyl) amino) propyl)-thiophenecarboxamide intermediate for Rivaroxaban, comprises reacting 5-chloro-N-(2-oxiranylmethyl)-2-thiophenecarboxamide with 4-(4-aminophenyl) morpholinone

2015-01-29

Process

Rivaroxaban

Rivaroxaban approved in November 2013, originally Ranbaxy application filed in July 2013. Ranbaxy must have started working on molecule soon after approval. Later did not prosecute, could be commercially non-viable process.

WO2015166466A1

New crystalline Saxagliptin acetate form II is dipeptidyl peptidase IV enzyme inhibitor, useful for treating type 2 diabetes mellitus

2015-11-05

Crystalline Form

Saxagliptin

2009 approval, Sun Pharma application, withdrawn

WO2015071887A1

Oral pharmaceutical composition useful in treatment of type-II diabetes mellitus, comprises core comprising Saxagliptin, and coating layer comprising coating polymer, surrounding core

2015-05-21

Composition

Saxagliptin

Ranbaxy application, withdrawn.

WO2015071889A1

Oral composition used to treat type 2 diabetes mellitus, comprises core, optionally seal layer comprising coating polymer coated over the core, drug layer comprising Saxagliptin and coating polymer and outer layer comprising coating polymer

2015-05-21

Composition

Saxagliptin

Ranbaxy application, withdrawn.

WO2015087262A1

Preparing Saxagliptin which is useful for treating type 2 diabetes mellitus comprises e.g. deprotecting ((S)-2-((1S,3S,5S)-3-cyano-2-aza-bicyclo (3.1.0) hex-2-yl)-1-(3-hydroxy-adamantan-1-yl)-2-oxo-ethyl)-carbamic acid tert-butyl ester

2015-06-18

Process

Saxagliptin

Ranbaxy application, withdrawn.

WO2015145333A1

Preparing Sitagliptin, comprises treating (3R)-3-((tert-butoxycarbonyl) amino)-4-(2,4,5-trifluorophenyl) butanoic acid with 3-(trifluoromethyl)-5,6,7,8-tetrahydro (1,2,4) triazolo(4,3-a) pyrazine, and deprotecting the obtained product

2015-10-01

Process

Sitagliptin

Sun Pharma application, withdrawn.

WO2014039340A3

Method of inhibiting growth of hair in skin, involves epilation of follicles in the skin, waiting until within five days of commencement of metanagen, applying photodynamic agent to skin, and exposing skin to photoactivating light

2015-07-16

Skin Care

Skin Care

Application filed by Dusa Pharmaceuticals, Inc. Sun Pharma acquired Dusa. This is being prosecuted in key countries.

WO2015005419A1

Composition useful for preparing topical foam formulation, comprises N-alkyl-2-pyrrolidone, carbonate diester, and surfactant

2015-01-15

Composition

Skin Care

 

WO2015015384A1

Topical applicator for use by patient for applying e.g. ointment, onto affected area and massaging area during treatment of muscle aches, has tube for containing semi-solid dosage form, and massaging assembly snap-sealed to neck region

2015-02-05

Skin Care

Skin Care

Originally Ranbaxy application, which was not prosecuted, maybe due to commercial reasons. 

WO2015044857A1

Topical spray composition used for treating a topical skin condition (e.g. dermatoses, psoriasis and eczema) comprises Halobetasol, emollient, non-aqueous solvent, and propellant

2015-04-02

Skin Care

Skin Care

Ranbaxy application prosecuted in Mexico! Business of this composition in Mexico?

WO2015063723A1

Stable topical pharmaceutical composition useful for treating skin disorder e.g. psoriasis, keratosis, eczema, rosacea, acne vulgaris, dermatitis and pruritus, comprises acitretin, and one or more gelling agents

2015-05-07

Skin Care

Skin Care

Ranbaxy application, prosecuted in many countries and must be interesting.

WO2015092602A1

Topical pharmaceutical composition of retinoid useful for treating acne, comprises microspheres comprising retinoid and microsphere-forming polymers, and coating layer

2015-06-25

Skin Care

Skin Care

Ranbaxy application, withdrawn.

WO2015107542A2

Treating acne or psoriasis, by topically administering Tazarotene free of dimer impurity

2015-07-23

Skin Care

Skin Care

Sun Pharma application, being prosecuted in few countries including US.

WO2015147296A1

Producing composition used as skin external preparation for treating inflammation, by cooling oil-in-water emulsion to or below cloud point of non-ionic surfactant, adding carboxyvinyl polymer and neutralizing with alkali agent

2015-10-01

Skin Care

Skin Care

Withdrawn in many countries.

WO2015156219A1

External pharmaceutical composition used for treating dermatomycosis, comprises acetonitrile derivative and steroids including Dexamethasones, Hydrocortisones, Clobetasones, Clobetasols, Betamethasones, and Mometasones

2015-10-15

Skin Care

Skin Care

Withdrawn in many countries

WO2015056247A1

Pure crystalline form-II of L-malic acid salt of Sunitinib used as oral multi-kinase inhibitor and is useful for treatment of gastrointestinal stromal tumors and advanced renal cell carcinoma

2015-04-23

Crystalline Form

Sunitinib

Ranbaxy application, granted in US

WO2015056250A1

New ascorbic acid salt of Sunitinib useful for treating or preventing a protein kinase related disorder, and gastrointestinal stromal tumors and advanced renal cell carcinoma

2015-04-23

Composition

Sunitinib

Ranbaxy application, granted in US

WO2015075744A1

Preparing Tapentadol useful as analgesic, comprises reacting (2S,3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methylpentan-3-ol with isocyanate followed by hydrogenating and dimethylation

2015-05-28

Process

Tapentadol

Sun application, being prosecuted in many key jurisdictions.

WO2015019238A1

Manufacture of N-protected (5S) (thiazolidinylcarbonyl) pyrrolidin-3-one for manufacturing (3-methylphenyl-1H-pyrazolyl) piperazinyl-pyrrolidinyl (thiazolidinyl) methanone, involves condensing N-protected oxo-1-proline with thiazolidine

2015-02-12

Process

Teneligliptin

Teneligliptin approved for use in Japan, Argentina, Korea and India, in 2012-2013. Ranbaxy must have started working upon approval. No approval in other countries! Family withdrawn.

WO2015019239A1

Preparing 1-(3-methyl-1-phenyl-1H-pyrazol-5-yl) piperazine comprises e.g. reacting substituted protected piperazine compounds with alkylacetoacetate and phenylhydrazine, and cyclizing the resultant

2015-02-12

Process

Teneligliptin

Ranbaxy application, withdrawn.

WO2015063709A1

Preparation of 1-(3-methyl-1-phenyl-1H-pyrazol-5-yl) piperazine or its salt used for preparation of (1,3-thiazolidin-3-yl) methanone derivative or its salt involves cyclizing aniline derivative in presence of Lawesson's reagent

2015-05-07

Process

Teneligliptin

Ranbaxy application, withdrawn

WO2015001489A1

Composition, useful for treating cardiovascular diseases such as thrombotic cardiovascular events e.g. unstable angina, comprises amorphous ticagrelor, and excipients including diluent, binder, disintegrant and/or lubricant

2015-01-08

Composition

Ticagrelor

Ticagrelor is 2011 approval. Priority of this application is 2013 and it is clear Ranbaxy must be working on Ticagrelor immediately after the approval. Sun now doesn't seem to be interested in this composition, application withdrawn.

WO2015198225A1

Dry process to make composition comprising Tofacitinib, and diluent, disintegrant or excipient by dry granulation, comprises blending Tofacitinib and diluent, blending with disintegrant and diluent, blending with lubricant and compressing

2015-12-30

Composition

Tofacitinib

First approval in 2018! Sun filed composition patent application of Tofacitinib in 2014! Work on the molecule must have started at least two-three years prior to 2014. They must have prepared API for FDF development! Sun withdrew application in most of the jurisdiction, perhaps thought against of approval and had not prosecuted!

WO2015056219A1

Preparing micronized Valsartan, useful for treatment of hypertension and heart failure, comprises subjecting Valsartan to drying and micronization simultaneously

2015-04-23

Composition

Valsartan

Ranbaxy application, withdrawn.

WO2015019237A1

Composition used to treat or prevent CNS disorder e.g. major depressive disorder, anxiety disorders, bipolar disorders, mania, eating disorders or sleeping disorders, comprises micronized particles of Vilazodone, and excipient e.g. binder

2015-02-12

Composition

Vilazodone

Vilazodone approved in 2011, application filed in 2013, this is another example where Ranbaxy would have started FDF development immediately after approval! Now withdrawn, composition or product must be uninteresting to Sun now.

WO2015019256A1

Pharmaceutical composition used for treating and/or preventing central nervous system disorder, e.g. major depressive disorder, comprises Vilazodone and nonionic surfactants

2015-02-12

Composition

Vilazodone

Ranbaxy application, withdrawn.

WO2016001843A1

Extended-release gastroretentive tablet of Voglibose for once-a-day therapy useful for treating diabetes, comprises Voglibose and release controlling polymers

2016-01-07

Composition

Voglibose

Takeda’s old product did not do well outside Japan. Sun Pharma application, now withdrawn.

General information  

Adamas Pharma (ADMS) Announces Agreement to Settle Patent Litigation with Osmotica

As a result of this agreement, both parties will drop their respective claims relating to the patent litigation, and Adamas will acquire the global rights to OSMOLEX ER® for $7.5 million. The agreement is expected to close early in 2021. (Read more) 

HHS Shuts Down FDA's Unapproved Drugs Initiative

On November 20, 2020, the Department of Health and Human Services (HHS) announced it was terminating the U.S. Food and Drug Administration's (FDA) Unapproved Drugs Initiative (UDI), which is further described in a Notice published in the Federal Register on November 25, 2020. (Read more

Intellectual Property  

Methylphenidate Liquid formulation (Quillivant XR) case in US  

Quillivant XR had approximately 636,000 prescriptions and gross sales of approximately $192 million. This is 2016 data and sales could have gone up in last four years as ADHD market is worth around $4 billion a year and its growth is outstripping the overall pharma market. 

Pfizer acquired Quillivant XR as part of its purchase of NextWave Pharmaceuticals.  

In September 2018, Tris Pharma, Inc. announced the acquisition of NextWave Pharmaceuticals (NextWave), a wholly owned subsidiary of Pfizer Inc., including two key Attention Deficit Hyperactivity Disorder (ADHD) treatments.  

Here are OB patents of Tris Pharma.

OB Patent Data

Patent No

Patent Expiration

Drug Product

Patent Use Code

Submission Date

8062667

03/29/2029

DP

10/22/2012

8287903

02/15/2031

DP

10/22/2012

8465765

02/15/2031

DP

U-1415

06/10/2013

8563033

02/15/2031

DP

U-1415

11/15/2013

8778390

02/15/2031

DP

U-1543

08/04/2014

8956649

02/15/2031

DP

U-1665

03/13/2015

9040083

02/15/2031

DP

06/09/2015

Tris Pharma filed suit against Actavis for alleged infringement of U.S. Patent Nos. 8,465,765; 8,563,033; 8,778,390; 8,956,649 and 9,040,083. 

Actavis challenged the validity based on obviousness and obviousness-type double patenting.

The lower court found claims to be invalid for obviousness.

Tris appealed.  

CAFC (The Federal Circuit) reversed the decision stating that the lower court judge errored in his observations and asked the district court for further fact-finding analysis.  

Claims of contested patent are very narrow. For example, US`765 claims specific liquid ER composition:  

1. A methylphenidate aqueous extended-release oral suspension comprising (1) an immediate release methylphenidate component, (2) a sustained release methylphenidate component comprising a water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex, and (3) water, wherein said suspension has a pH of about 3.5 to about 5 and said suspension provides a single mean average plasma concentration peak for methylphenidate and a therapeutically effective plasma profile for methylphenidate for about 12 hours. 

Claims in the other challenged patents are also very specific to the marketed formulation.  

CAFC ordered further fact-finding to address whether a liquid methylphenidate formulation with 1. a single mean PK profile, 

2. 12-hour duration of effect,

3. 45-minute onset of action,

4. Tmax range of 4 to 5.25 hours would have been obvious over the prior art?  

Prior arts cited were disclosing one or more limitations but not all. Most of the prior arts were related to ER solid formulations of Methylphenidate. Only one art cited was related to liquid formulation but that disclosed IR composition.  

In view of this CAFC concluded that all asserted claims are valid and Actavis would infringe each of the asserted claims. More details here



Disclaimer

 

Sidvim LifeSciences Private Ltd has taken due care and caution in developing this document. Since the data used for analysis in this document is based on the information available in the public domain, its adequacy or accuracy or completeness cannot be guaranteed. This document is for information only and Sidvim is not responsible for losses that may or may not arise due to any decisions made based on the same. No part of the document shall constitute or be represented as a legal opinion of any kind or nature. No warranties or guarantees, expressed or implied, are included in or intended by the document, except that it has been prepared in accordance with the current generally accepted practices and standards consistent with the level of care and skill exercised under similar circumstances by professional consultants or firms that perform the same or similar services.

 


Popular posts from this blog

List of Off-Patent, Off-Exclusivity Drugs without an Approved Generic and Trademark case for J&J's ORS-L brand (Delhi HC decision)

API and IP Newsletter- Recent ANDA approvals and Roxadustat decision by EPO: T 0072/23

DMF filings by Indian companies in May 2025 and F-Hoffmann-La Roche AG Vs Zydus Lifesciences Limited- Delhi High Court decision