7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 MOOT PROBLEM BEFORE THE HIGH COURT OF MUNAIN, REPUBLIC OF BHARANESIA
O.S. No. 707/2014 BETWEEN 1. B.Z. Mate University ……Plaintiff AND 1. Bristo Pharmaceuticals Pvt. Ltd. and Bristo Pharmaceuticals Inc. ……..Defendants
BEFORE THE INTELLECTUAL PROPERTY APPELLATE BOARD (IPAB) OF BHARANESIA OA/7/2014/PT/DH BETWEEN 1. Bristo Pharmaceuticals Pvt. Ltd. AND 1. B.Z. Mate University 2. Controller of Patents, Bharanesia AND
……..Appellant
……..Respondents
ORA/14/2014/PT/DH BETWEEN 1. Bristo Pharmaceuticals Pvt. Ltd. AND 1. B.Z. Mate University
……..Applicant ………Respondent
a) This hypothetical problem is conceived and prepared by Sunil B Krishna, Disha Jeswani and Rahul Vartak and scrutinized by R Muralidharan, Manish Saurastri and Vinod Kotabagi of Krishna & Saurastri Associates. b) The authors assert the moral right to be identified as the creators of this fictional legal educational tool. The authors would encourage Law Schools to use the Problem either as study material or instructional tool after due acknowledgement to the authors. c) To the knowledge of the authors, there is no similar proceeding pending anywhere in the world. The problem is purely hypothetical and fictional. Any similarity with situations or names is purely coincidental and unintentional. e) One speaker shall argue on the matter pending before the IPAB and the other speaker on the matter pending before the High Court of Munain.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 1.
B.Z. Mate University (hereinafter referred to as Mate) is a University based in the Republic of Bharanesia. Bharanesia is a Sovereign Nation located in South Asian Region. Its Constitution, Laws, Institutions and Social Ethos are substantially similar to that of Union of India.
2.
Mate has a well established Intellectual Property Cell which protects its inventions in various fields. The research and development at Mate is mostly conducted by the Professors of Mate’s various departments. Mate is the leading educational institute which applies for patent applications before the Patent Office of the Republic of Bharanesia. It is also amongst the top 100 PCT applicants in the world in the category of universities & educational institutes.
3.
Bristo Pharmaceuticals Pvt. Ltd. (hereinafter referred to as Bristo) is a company registered under the laws of Bharanesia. Bristo is a wholly owned subsidiary of Bristo Pharmaceuticals Inc. The business activities of Bristo Pharmaceuticals Pvt. Ltd. are controlled by Bristo Pharmaceuticals Inc. Bristo Pharmaceuticals Inc. is registered under the laws of Federation of Pandora whose constitution, laws and social ethos are substantially similar to that of the United States of America.
4.
Prof. Dr. M. Vaidya and Prof. Dr. P. Bhattacharya have been working with Mate for many years and are the most active researchers who are named as inventors in many PCT and national applications filed by Mate. The inventors published their provisional conclusion on a possible pain killer employing ABC Receptor antagonists in June 2008 in a leading publication, which was available to public on June 5, 2008. The research project continued at Mate after the said publication. After months of research, the Researchers were able to develop a line of pharmaceutical products and filed patent application 8456/MN/2009 on June 5, 2009 titled “Abc receptor antagonist for the treatment of chronic pain”. The inventors named in the application were Vaidya M. and Bhattacharya P.
5.
When the application 8456/MN/2009 was examined, the Examiner vide his letter dated December 12, 2011 objected the grant of patent. The copy of the First Examination Report is enclosed as Exhibit-A.
6.
Mate, through their Attorneys’ letter dated December 10, 2012, responded to the First Examination Report. Regarding the missing signatures on Form 1 and assignment, 2
7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Mate stated that the inventors moved to a company outside Bharanesia and their whereabouts are not known. Mate pointed out that the inventors were on the Rolls of the University. The Standing Rules of the Contract of Employment (which has the force of law) specifically stipulates that only the University will be the owner of any IP generated by their employees in the course of their employment. There were documents available with the Patent Office that the same inventors, during the past, had assigned all their inventions to the Mate University. Non-signing of Form 1 endorsement by the inventors in this case was due to an oversight. Hence, Mate was entitled to apply for the patent. Mate’s submissions were taken on record by the Examiner. Before the final decision could be made by the Examiner, Bristo filed a pre-grant opposition against the grant of a patent for the application 8456/MN/2009 inter-alia on the following grounds: i.
that Mate wrongfully obtained the invention from the inventors as duly signed Form 1/ assignment which is mandatory was not submitted;
ii.
that the claimed Compound of formula I is obvious in view of earlier disclosures known in the art;
iii. 7.
that the invention does not involve an inventive step;
The notice of opposition was taken on record and Mate was informed accordingly. Mate responded with a written statement with primarily the same submissions and evidence as provided at the time of responding to the First Examination Report. A hearing was held and both parties were allowed to present their arguments. Based on Mate’s submissions, the Controller of Patents dismissed the pre-grant opposition proceedings filed by Bristo. The Controller, in an elaborate order, stated the reasons for dismissing the pre-grant opposition. A patent was granted to the application 8456/MN/2009 which was given the Patent No. 1234567 on January 11, 2013. A copy of the granted patent No. 1234567 is enclosed as Exhibit B. The decision of grant was published in the journal on March 10, 2013.
8.
On June 10, 2013, Bristo filed a post grant opposition to the Patent No. 1234567 with further documents claiming that the piperidine derivates were obvious to a person skilled in the art.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015
Bristo relied upon several prior art documents to show that many compounds were structurally and functionally similar to Compound of formula I claimed and the latter is a new form of earlier compounds;
Bristo further alleged that the inventors Vaidya M and Bhattacharya P were working on pain receptor antagonists for many years and hence their level of skill in the art was high. It was obvious for them to come up with the claimed piperidine derivatives when earlier compounds were known.
A lot of the inventors’ own earlier publications and similar patents have been relied upon to state that the invention was obvious.
9.
While the post-grant opposition proceedings were going on, an RTI application by Mate revealed that Bristo had applied for a manufacturing licence before the Drug Controller Licensing Authority, Munain for manufacturing abc bulk drug. Also, Bristo Inc.’s website has listed abc in their product list under ‘developed antagonist APIs’. Mate also realized that Bristo Inc. had applied for marketing approval with the FDA of Pandora and has advertised its intention of launching the product abc in India and Pandora through various media. Mate, sent a letter dated September 15, 2013 through their Attorneys addressed to Bristo and Bristo Inc. which inter alia contained the following: a. that Mate is the owner of the patent bearing no. 1234567 which is registered with the Bharanesian Patent Office, in relation to Compound of formula I and compositions thereto; b. that the impugned product is identical to the product which forms a part of the subject matter of Patent bearing No. 1234567 and the actions of Bristo and Bristo Inc. clearly amount to infringement of the said Patent; c. that Bristo and Bristo Inc. should immediately cease and desist from advertising, manufacturing, marketing and using in any way the impugned product;
10.
The said letter was not responded to by Bristo and Bristo Inc. Mate filed a quia timet suit for infringement before the District Court of Suriya (a district in Munain) on
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 January 10, 2014 for restraining Bristo and Bristo Inc. from advertising, manufacturing, marketing and using in any way the impugned product. Mate, in its plaint also mentioned Bristo’s zealous efforts at opposing the patent which indicated Bristo’s intentions to launch the product. The Hon’ble District Court while taking note of Mate’s submissions and evidence, vide an order dated January 15, 2014, granted a quia timet
ex-parte injunction restraining Bristo and Bristo Inc. from manufacturing,
marketing and in any way using the impugned product in Bharanesia and exporting the same outside Bharanesia. 11.
In the opposition proceedings, the Controller of Patents constituted an Opposition Board who conducted a fresh examination. Both parties made their submissions along with evidence by experts in the field of pharmaceuticals. After thorough examination, the Opposition Board recommended that the claimed invention was obvious due to the following reasons: R2
X
Compound of formula I(Mate’s invention as claimed in Patent 1234567)
The Compound of formula I can be considered to be a derivative of Compound T as it is structurally very similar to earlier Compound T, which is as follows: R2 H3C
O NHR 1
N
OH X
H3C
Compound T as taught by Hensky
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015
Compound of formula I is different in that methylbenzene is attached to cyclopentane ring and the presence of the methyl group (-CH3) [instead of ethyl group (-CH2-CH3)] on the piperidine ring. However, Compound of formula I can be said to be a new form of a known substance under section 3(d) of the Patents Act. Also, one skilled in the art would have been motivated to modify the structure of compound T to remove deficiencies in the art and arrive at the Compound of formula I. By virtue of the vast amount of publications and due to the high level of skill of the inventors, Compound of formula I can be considered to be obvious. The finding of the Opposition Board is enclosed as Exhibit-C.
12.
Nonetheless, the Controller, after hearing both parties, ignored the recommendations of the Opposition Board and maintained the patent. The complete order of the Controller is enclosed as Exhibit D. The earlier order of the Controller under Sec. 25 (1) stated as follows:
Compound of formula I is structurally different from compound T and the structural difference does not make Compound of formula I fall under section 3(d) by virtue of explanation to 3(d);
Compound of formula I is structurally and functionally advanced than compound T and all other known compounds. The inventor’s own earlier publications cannot be considered for obviousness or lack of inventive step. Reliance is placed on decisions of other countries which state that the inventor’s own publications should not be considered for determining obviousness;
Compound of formula I is more efficacious and has more beneficial properties than other known antagonists due to the positive effects such as mood elevation, lack of side effects and withdrawal symptoms as demonstrated in the specification and based on independent expert evidence submitted by Mate.
13.
Dissatisfied with the decision of the Controller, Bristo appealed the decision at the IPAB. Simultaneously, it also filed for a revocation of the patent IN 1234567 at the IPAB on the following grounds: a. that Mate was not entitled to apply for the patent as duly signed Form 1/ assignment which is mandatorily required to be submitted was not submitted. Bristo provided
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 the whereabouts and details of the inventors and alleged that Mate had in fact made false submissions before the Patent Office that the inventors Vaidya and Bhattacharya were not traceable; b. that the claimed compound is obvious in view of earlier disclosures and inventor’s own earlier publications relating to neuropathic antagonists; c. that the claimed compound is a new form of a known substance (compound T) disclosed in prior art. The claimed Compound of formula I has almost negligible structural and functional difference with compound T. d. that the invention does not involve an inventive step; 14.
Since the appeal and the application for revocation involved the same patent, both the matters were taken up simultaneously at the IPAB.
15.
While the IPAB matters were pending, Bristo challenged the claims of the patent IN 1234567 in a counter-claim of infringement. The suit, along with the counter- claim got transferred to the High court of Munain.
16.
The IPAB and the High Court matters are listed for final disposal on February 8, 2015.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 The Moot Court problem involves the adjudication of the following issues:
1. The obligation to provide a Proof of right if the assignment is not in place and if the inventors are not traceable. Whether the Patent Office can conclude on ownership of a patent from other circumstances? 2. ‘Obviousness’ in case the level of skill is high. 3. Whether prior publication by the inventors can defeat novelty? 4. If a pre-grant opposition is filed and dismissed, is the aggrieved party stopped from filing a post-grant opposition on primarily the same grounds? 5. If a Post Grant opposition has been filed, can the same party file for a revocation and also challenge the patent in a counter claim for infringement. 6. Can a quia timet injunction be granted to a party for a patent whose validity is under challenge before various bodies?
The participants are advised that if there be real need, additional issues can also be formulated with the permission of the Court/Board
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 EXHIBIT-A GOVERNMENT OF BHARANESIA PATENT OFFICE MUNAIN LETTER NO.: CHEM/2011/E-1440
DATE: 12/12/2011
To ______ ______ ______ SUB: First Examination Report
Application No Date of Filing Date of Request for Examination Date of Publication
: : : :
8456/MN/2009 05/06/2009 10/06/2009 15/02/2011
a) With reference to the Request for Examination dated 10/06/2009 in the above mentioned application for Grant of Patent, Examination has been conducted under Sec.12 and 13 of the Patents Act 1970, the following objections are hereby communicated.
b) Objections: 1. The applicant has not furnished credible proof of ownership of the invention. The inventors have not signed the Form 1. 2. The application relates to non-patentable subject matter more specifically falling under Sec.3 (d) and it’s Explanation. 3. The specification does not disclose any inventive step. 4. Considering that the reactants, process steps and other parameters are known to the industry, the invention lacks absolute novelty. 5. The experimental data as shown in the specification does not disclose that the composition has a new, significant and different beneficial property of the composition.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 6. There is no verifiable data available in the specification to show there is a significant improvement of the therapeutic efficacy of the product. c) You are requested to comply with the objections by filing your reply by way of explanation and/or amendments within 12 months from the date of issue of FER failing which your application will be treated as “Deemed to have been abandoned” under Sec. 21(1) of the Act. The last date is 12/12/2012. d) You are advised to file reply at the earliest so that the office can proceed with application and complete the process within the prescribed period.
Sd/Examiner of Patents & Designs Patent Office, Bharanesia
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 EXHIBIT-B FIELD OF INVENTION This invention relates to compounds used for the treatment of chronic pain. BACKGROUND Pain is a sensory as well as emotional disturbance associated with actual or potential tissue damage. The two basic types of pain are acute pain and chronic pain. Chronic pain is persistent pain, which persists over a long period after the onset of any known or suspected physical cause, usually of duration greater than 6 months. Chronic pain can be mild or excruciating, episodic or continuous, merely inconvenient or totally incapacitating. The most common sources of pain include injuries, muscular dystrophy, headaches, joint pain, etc. Neuropathy is an example of chronic pain and is considered to be a result of damage to peripheral nerves or to regions of the central nervous system (CNS). However, abnormal functioning of pain-related regions of the nervous system can also occur with chronic inflammatory conditions such as certain types of arthritis and metabolic disorders such as diabetes. Currently the main classes of drugs used to treat neuropathic pain include serotoninnorepinephrine reuptake inhibitors, opiates and opiate-like substances, and topical medications. Side effects related to serotonin-norepinephrine reuptake inhibitors include drowsiness, dizziness, fatigue, headache, and increase in suicidal thoughts, nausea /vomiting, sexual dysfunction, and urinary retention. U.S.Pat. No. 4,176,186 discloses similar agents suggested in the prior art for alleviating the constipation problems of chronic pain patients suffer from a number of drawbacks. Although these substances do not cross the blood-brain barrier, and therefore do not substantially interfere with those analgesic effects of the opioid agents that are mediated through the brain, the antagonists suggested by the prior art may well interfere with analgesic activity mediated through the spinal cord, the peripheral sensory system, the pituitary gland and possibly the basal hypothalamus, all of which are believed to contain important opioid receptors.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Indian patent application 7987/MUMNP/2008 discloses synthesis of novel abc receptor antagonists wherein the document teaches that a lower alkyl groups must be attached to a 5 membered ring. However substitution of a higher alkyl groups to a 5 membered ring would decrease the activity of the compound as an antagonist, thus decreasing the effect of such a compound. Presently known compounds and formulations fail to provide complete relief from chronic pain and are accompanied by side effects and withdrawal symptoms. Also they do not provide for mood elevation which is necessary as the conditions such as chronic pain are often accompanied by depression or trauma. Further the compounds are difficult to administer especially for geriatric and pediatric patients as they are not available in different formulations. Therefore, there is a need to solve the problems mentioned above. SUMMARY OF THE INVENTION The present invention relates to a Compound of formula I: R2
X
Wherein R1 is selected from H, C1-C10alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl group R2 is selected from C1-C10alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl group, NH2, CN X is selected from halogens such as chlorine, bromine
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Brief description of the drawings Fig. 1 is a graphical representation of the pain intensity (%) on administering the present invention of compound of formula Ic at a dosage of 45 mg/day in comparison with a placebo. Fig. 2. is a graphical representation of the pain intensity (%) on administering compound of formula Ia , drug M and Drug N at a dosage of 125mg/day. Fig3. is a graphical representation of reduction in pain and mood elevation on administering the present invention.
DETAILED DESCRIPTION The present invention discloses a compound used for the treatment of chronic pain which results from nerve injury, wherein the compound acts as an antagonist to the abc receptors. Definitions The term ‘antagonist’ used herein refers to a substance that acts against and blocks an action. The term ‘receptors’ used herein refers to regulatory protein macromolecules located on the cell surface membrane or within the cytoplasm. The receptors referred to in the present invention are glutamate receptors. The term ‘receptor antagonist’ used herein is a type of receptor ligand or drug that blocks or dampens agonist-mediated responses rather than provoking a biological response itself upon binding to a receptor. The term ‘abc’ is the name of a selective agonist that binds to abc receptors but not to other glutamate receptors. The ‘abc receptor’ is a specific type of glutamate receptor. The ‘abc receptor antagonist’ refers to a class of of anesthetics that work to antagonize, or inhibit the action of, the abc receptors and are used as anaesthetics for humans. They are used for pains that result from nerve injury.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 The term ‘ligand’ used herein refers to molecules that bind to receptors. A ligand may activate or inactivate a receptor; activation may increase or decrease a particular cell function. Various embodiments of the present invention disclose an abc receptor antagonist and its pharmaceutical composition used for the treatment of chronic pain and its varieties. An embodiment of the present invention discloses compounds of formula I, and pharmaceutically acceptable salts thereof. Compound of formula I: R2
X
Wherein R1 is selected from H, C1-C10 alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl and C3-C20 cycloalkenyl group R2 is selected from C1-C10 alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl group, NH2 and CN X is selected from halogens such as bromine An embodiment of the present invention relates to non-toxic substances belonging to a group of compounds that are capable of binding to the abc receptors and blocking the abc receptors thus acting as antagonists. In another embodiment of the present invention, a pharmaceutical composition containing the non toxic abc receptor antagonist is disclosed. The composition comprises of adding one or more pharmaceutically acceptable excipients thereof.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 The pharmaceutically acceptable excipients are selected from colorants, sweetening agents combinations thereof. The colorants are selected from ponceau, quinoline yellow WS and titanium dioxide. The sweetening agents are selected from sucrose, saccharin or sodium or calcium cyclamate, glycerol, sorbitol. The sweetening agents are preferably selected from sorbitol, sucrose or a combination thereof. The pharmaceutical excipients, include a pharmaceutically acceptable carrier selected from one or more diluents or fillers; one or more binders; one or more lubricants; one or more disintegrants; one or more preservatives The diluents or fillers are selected from but are not limited to lactose, hydroxyethylcellulose, sodium carboxymethylcellulose, carboxymethylene, and other cellulose derivatives, starches or modified starches, or their combinations thereof. The binders are selected from but are not limited to cellulosic bingers, gelatine, gum acacia, or mixtures thereof. The lubricants are selected from but are not limited to purified water and Magnesium Stearate. The disintegrants are selected from but are not limited to hydroxylpropyl cellulose (HPC), low density HPC, carboxymethylcellulose (CMC), sodium CMC, calcium CMC. The Preservative are selected from but are not limited to ethyl or n-propyl-p-hydroxy benzoate. In an embodiment of the present invention the composition may be in the form of a liquid, powder, elixir, injectable solution, capsules, suspensions, syrups. In the aforementioned embodiments, the abc receptor antagonist can be formulated as a hard gelatin capsules or soft gelatin capsule, aqueous suspensions. In yet another embodiment of the present invention, the non toxic abc receptor antagonist is administered by way of oral administration, intravenous, intramuscular, subcutaneous, intrathecal, epidural or intracerebroventricular injection. Preferably, the abc receptor antagonist is administered intravenously.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Effective dosage levels vary from 10 to 400 mg/day depending on the form of administration. In the synthesis of the present invention compounds of formula P and Q are mixed under the required temperature conditions. The mixture is then further distilled and the residue obtained is poured onto ice wherein the product precipitates. The slurry obtained is stirred and the product is then filtered and dried to obtain compounds of the present invention. R2 H3C
O
N CH3
X
Compound P
NHR 1 HO
OH
H3C
Compound Q
Table 1: Certain exemplary compounds of the present invention. Compound CH3
CH3
O H3C
NH
N
OH Br
(1a)
H3C
CH2
CH3 O H3C
NH
N
OH Br
(1b)
H3C
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 CH3 CH3
O H3C
NH
N
OH Br
(1c)
H3C
Use of Invention Compounds of the present invention act as antagonists to abc receptors and are used for the treatment of chronic pain which result from nerve injury. abc receptor antagonism results in analgesia by preventing central sensitization in dorsal horn neurons; in other words, the actions of the compounds of the present invention interfere with pain transmission in the spinal cord. Further, the compounds of the present invention are used for the treatment of a wide range of conditions such as, neuropathic pains, memory loss, arthritis related pains, and diabetes related pains such as diabetic peripheral neuropathy amongst others. The compounds of the present invention also result in mood elevation. The compounds of the present invention are preferably used in paediatric and geriatric patients as it is non-toxic and there are no withdrawal symptoms observed. Another advantage of the compounds of formula I is that it can be administered in various forms. The advantageous process of the present invention is demonstrated in the experimental data. Example 1 50g of compound P [1-(4-bromo-1,6-dimethylpiperidin-2-yl)] ethanone] was reacted with 20g of compound Q [1-(ethylamino)-4-(3-methylphenyl)cyclopentane-1,3-diol] at a temperature of 50°C for 3 hours. The mixture was then further distilled and the residue obtained was the poured onto 200ml ice wherein the product precipitates. The slurry obtained is then stirred for another 30 minutes and the product is further filtered and dried to obtain a 45g of the desired product of the compound of formula Ia.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 H3C H3C
O
N CH3
Br
Compound P
CH3 NH HO
OH
H3C
Compound Q
Experimental data The compound was administered to a group of 40 individuals suffering from neuropathic pain and thus suffering from chronic pain. 45mg/day of the compound of formula Ic, was administered to such individuals intravenously for a period of 28 days. After the given duration the pain was observed to be reduced by 65% and mood elevation of the patient was also observed. Fig. 1 is a graphical representation of pain intensity (%) on administering the compound of formula Ic in comparison with a placebo. The compound of formula Ia was administered to a group of 30 individuals at a dosage of 125mg/day wherein the drug was administered orally over a period of 28 days. Another set of 30 individuals suffering from chronic pain were administered with the same dosage as the present invention with drug M and an additional 30 individuals were administered with drug N. Drugs M and N are commonly available drugs in the market. The effects of the three drugs was studied and compared. The reduction of pain observed in individuals administered with the present invention was much more as compared to patients administered with drugs M and N as shown in Fig. 2 indicates the reduction in pain Moreover, mood elevation was also observed which is indicated in graph 3.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Compound
IC50 against xyz receptor (nM)
M (prior art)
=270
CH3 O H3C
CH3
NH
N
OH Br
H3C
(1a)
50 CH3
CH3
O H3C
NH
N
OH Br H3C
(1b)
70 CH2
CH3 O H3C
NH
N
OH Br H3C
(1c)
130 CH3 CH3
O H3C
NH
N
OH Br H3C
IC 50 values of the present invention at 125mg/day
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015
We claim: 1. A compound formula I: R2
X
Wherein R1 is selected from H, C1-C10alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl, C3C20 cycloalkenyl group R2 is selected from C1-C10alkyl, C2-C10 alkenyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl group, NH2, CN X is selected from halogens such as chlorine, bromine 2. The compound according to claim 1, wherein R1 is preferably a methyl 3. The compound according to claim 1, Wherein R2, is preferably ethyl 4. The compound according to claim 1, wherein X is preferably bromine 5. A pharmaceutical composition comprising of compound of formula I as claimed in claim 1 and pharmaceutically acceptable excipients. 6. The compound as claimed in claim I, wherein the compound is selected from the compounds delineated in Table A and pharmaceutically acceptable salts thereof. (1a) CH3
CH3
O H3C
NH
N
OH Br H3C
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 CH2
CH3 O H3C
NH
N
OH Br H3C
(1b)
CH3 CH3
O H3C
NH
N
OH Br
(1c)
H3C
Table A Dated 5th day of June 2009.
FOR B.Z. Mate University
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 Abstract Title: abc Receptor antagonist for the treatment of chronic pain. The present invention discloses compounds used in the treatment of chronic pain and its varieties more specifically for neuropathic pain which results from nerve injury. The compounds disclosed in the present invention acts as an antagonist to the abc receptors and have the formula I.
R2
X
(I)
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 120
pain intensity (%)
100 80 60
Compound of formula Ic placebo
40 20 0 day 0
day 7
day 14
day 21
day 28
Days
Fig. 1
day 28
days
day 21
drug N
day14
drug M Compound of formula Ia
day 7
day 0 0
20
40
60
80
pain intensity (%)
Fig 2.
23
100
120
7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015
100 90 80 70
%
60 50
pain
40
mood elevation
30 20 10 0 day 0
day 7
day 14
day 21
days
Fig3.
24
day28
7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 EXHIBIT-C FINDINGS OF THE OPPOSITION BOARD. 1) Findings on proof of ownership filing: Even though the Examiner had raised a question on the proof of ownership, the applicant has furnished credible evidence to show that during the relevant period of the genesis of the invention, the inventors had a contract of employment which explicitly stipulated that all the inventions of their employees in the course of employment automatically vest in the company. Hence, the applicant sought withdrawal of the objection. However, even assuming that this is correct, since patents are territorial, the assignment clause contained in the earlier and later application will not ipso facto convey the right to file patent applications. The patent offices have a right to demand proof of ownership of the invention in every case, specifically in respect of their territory. Hence, on the ground of applicant’s failure to furnish credible proof of ownership, the application deserves rejection. 2) Contrary to the objection of the Examiner, the Board finds the existence of relative novelty if not absolute novelty. 3) The Examiners Board is of the opinion that the Patent Specification does not disclose any inventive step. Inventive step, in addition to the statutory definition, should also be decided in the light of teaching, suggestion and motivation available in the industry. Pharmaceuticals, specially, pain killers, are among the highly researched areas and a person skilled in the art can arrive at the composition after reasonable trial and error. Hence, the Board is of the opinion that the application lacks inventive step. 4) Regarding the applicability of Sec. 3(d) and its Explanation, it is found that the actions of the composition under issue interfere with pain transmission in the spinal cord. In addition to that, the compound results in mood elevation, which is an important factor in reduction of pain. Considering that the composition has fewer toxic side effects, we believe that the operation of sec.3 (d) and its explanation is not attracted. In view of our findings on Point 1 and 3, we recommend the Controller to revoke the patent.
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 EXHIBIT-D GOVERNMENT OF BHARANESIA PATENT OFFICE MUNAIN IN THE MATTER OF POST-GRANT OPPOSITION FILED IN PATENT NO. 1234567 TITLED ‘ABC RECEPTOR ANTAGONIST FOR THE TREATMENT OF CHRONIC PAIN’ DATED 05/06/2009
BETWEEN …OPPONENT
BRISTO PHARMACEUTICAL PVT LTD
AND …PATENTEE
B.Z. MATE UNIVERSITY
ORDER OF THE CONTROLLER 1. The opponent originally filed a representation under Sec. 25 (1) of Bharanesian Patent Act against the grant of Patent. The grant of patent was opposed on the grounds of: (a) failure to furnish proof of ownership of invention (b) the application lacks novelty (c) the specification does not disclose any inventive step (d) the application falls under the non-patentable invention category as enumerated under Sec. 3(d) and its Explanation. 2. The pre-grant representation of the opponent was considered and order on merit was passed by the Patent Office rejecting the opposition and ordering the grant of patent. The same applicant, on the very same grounds albeit on additional material, has sought to avail the other procedure available under Sec. 25 (2) of the Patents Act. 3. At the outset, I am of the opinion that sec.25 (1) adopts a summary procedure for determining the issues in controversy. No elaborate evidence is taken. A right of oral hearing by Opponent is not even mandatory if it is not specifically sought either by the Opponent or by the Applicant. The Patent Office, more particularly, the Examiner has to prima facie 26
7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 satisfy himself that the representation is either tenable or untenable and accordingly decide to reject or grant the patent. Furthermore, the order passed under Sec. 25(1) is not an appealable order. However, I am aware that since the doctrine of judicial review is part of the basic structure of the Constitution, if the opponent is aggrieved by the order of the Controller under Sec. 25 (1) of the Patent Act, they could have availed the constitutional remedies. Failure to do so would normally mean that as between the parties and in the given application, the order of the Patent Office becomes final and it cannot be re-agitated again on the same grounds. 4. However, subsequent to the opponent availing the statutory right of post-grant opposition under sec. 25 (2), the Patent Office had constituted an Opposition Board as required under Sec. 25 (2) and Rule 55-A to 62 of the Patent Rules 2003. The Opposition Board did not include the Examiner who originally issued the First Examination Report and recommended the grant of Patent. The members of the Board had actually found that there is relative novelty in the application and the specification does not attract the vice of Sec. 3(d) and it’s Explanation. However, the Board in its wisdom, found that the applicant has not furnished credible proof of ownership of the invention and that the patent specification does not disclose inventive step. The Board has also further found that the composition and the process of making the composition are obvious to a person skilled in the art in view of the high level of inventive activity prevalent in pharmaceutical industry, particularly, the pain killers sector. 5. In light of the above factual situation, the following issues arise for consideration. (a) Whether the opposition board is correct in holding that the Applicant has not furnished credible proof of ownership to the invention covered under the patent specification? (b) Whether the specification under adjudication evinces inventive step? 6. My findings on Issue (a): It is not in dispute that the inventors were employed as full time scientists of the applicants. The invention, undoubtedly, is in the course of employment of evolving new drugs. It is also not in dispute that the applicant has filed hundreds of PCT applications all over the world. Even assuming that this particular application does not contain endorsement from the inventors, earlier, the same inventors have several assignments in respect of different inventions. On the relevant date, they were shown on the rolls of the Applicant as full time employees. Assuming that the inventors may have a right to retain ownership in respect of an invention which they have already assigned to the employer, such
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7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 assumptions can only be on credible documentary proof. The inventors, being accomplished scientists, should be aware (or capable of being aware of it, had they exercised due diligence) of the patent filings of their invention. If they do not file objections on the ground of wrongful obtaining in Patent Office, the Patent Office may well be within its rights to hold that the fact and duration of the full time employment is proved, the patent offices should not once again demand proof of ownership. Furthermore, the ownership of an invention, more particularly, the right to file patent applications in respect of a original invention which was already assigned to the employer in pursuant of a contract of employment is a legal question and not a technical issue. Because of this, I chose to disregard the findings of the Opposition Board. 7. My findings on Issue (b): The Examiners Board itself has found despite objections from the Examiner, that: (a) the specification discloses Relative Novelty (b) the specification does not attract the operation of sec. 3(d) and its Explanation. 8. However, the Board came to a conclusion that the level of inventive activity in the pharmaceutical industry is high and the inventive step should be decided in the light of “teaching-suggestion-motivation” test. This test is alien to the Bharanesian Patent Act. The Bharanesian Patent Act defines inventive step as “a feature of an invention that involves technical advance as compared to the existing knowledge or having economic significance or both and that makes the invention not obvious to a person skilled in the art”. While assessing the concepts like novelty and inventive step, examiners have a tendency to avail the benefit of hindsight and conclude erroneously that the specification does not disclose inventive step. It is well known that mere simplicity of invention is no bar to its patentability. Considering that the employment of a receptor and an antagonist to block the receptor has the twin advantages of interfering with pain transmission and mood elevation, it solves an existing problem which the person skilled in the art did not earlier know. Absence of withdrawal symptoms and possibility of pediatric and geriatric prescription of the same compound substantially increases the ease of administration and could revolutionalize, in future, the treatment to pain. Furthermore, being an Organic Chemist with a substantial experience in examining pharmaceutical compositions, I have no hesitation in holding that the Opposition Board was incorrect in its conclusion that there is no inventive step. 28
7th Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015 ORDER In view of my above findings, I uphold the finding of the Examiner of Patents and the post-grant opposition is hereby dismissed. In the circumstances of the case, parties to bear their own costs.
Sd/Controller of Patents & Designs Patent Office, Bharanesia
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