moot problem before the high court of … symbiosis-b. krishna memorial national ipr moot court...

7th

Symbiosis-B. Krishna Memorial National IPR Moot Court Competition, 2015

1

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. ……..Appellant

AND

1. B.Z. Mate University

2. Controller of Patents, Bharanesia ……..Respondents

AND

ORA/14/2014/PT/DH

BETWEEN

1. Bristo Pharmaceuticals Pvt. Ltd. ……..Applicant

AND

1. B.Z. Mate University ………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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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,

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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. that the invention does not involve an inventive step;

7. 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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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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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:

X

R2

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:

NCH3

X

NHR 1

OH

O

CH3

R2

Compound T as taught by Hensky

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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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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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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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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 : 8456/MN/2009

Date of Filing : 05/06/2009

Date of Request for Examination : 10/06/2009

Date of Publication : 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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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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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 serotonin-

norepinephrine 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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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:

X

R2

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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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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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:

X

R2

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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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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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.

Compound P

NCH3

X

CH3

OR2

Compound Q CH3

NHR 1

OHOH

Table 1: Certain exemplary compounds of the present invention.

Compound

(1a)

N

CH3

CH3

Br

NH

OH

CH3

OCH3

(1b)

N

CH3

CH3NH

OH

CH3

O

CH2

Br

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(1c)

N

CH3

CH3NH

OH

O

Br

CH3

CH3

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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Compound P

NCH3

Br

CH3

OCH3

CH3

NH

OH

CH3

OH

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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Compound IC50 against xyz receptor

(nM)

M (prior art)

NCH3NH

OH

CH3

O

CH3

BrCH3

=270

(1a)

N

CH3

CH3

Br

NH

OH

CH3

OCH3

50

(1b)

N

CH3

CH3NH

OH

CH3

O

CH2

Br

70

(1c)

N

CH3

CH3NH

OH

O

Br

CH3

CH3

130

IC 50 values of the present invention at 125mg/day

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We claim:

1. A compound formula I:

X

R2

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

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)

N

CH3

CH3

Br

NH

OH

CH3

OCH3

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(1b)

N

CH3

CH3NH

OH

CH3

O

CH2

Br

(1c)

N

CH3

CH3NH

OH

O

Br

CH3

CH3

Table A

Dated 5th

day of June 2009.

FOR B.Z. Mate University

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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.

X

R2

(I)

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Fig. 1

Fig 2.

0

20

40

60

80

100

120

day 0 day 7 day 14 day 21 day 28

pai

n in

ten

sity

(%

)

Days

Compound of formula Ic

placebo

0 20 40 60 80 100 120

day 0

day 7

day14

day 21

day 28

pain intensity (%)

day

s

drug N

drug M

Compound of formula Ia

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Fig3.

0

10

20

30

40

50

60

70

80

90

100

day 0 day 7 day 14 day 21 day28

%

days

pain

mood elevation

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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.

7th


26

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

BRISTO PHARMACEUTICAL PVT LTD …OPPONENT

AND

B.Z. MATE UNIVERSITY …PATENTEE

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

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27

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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28

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.

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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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