BEFORE THE CONTROLLER OF PATENTS,

THE PATENT OFFICE,

KOLKATA

In the matter of The Patents Act, 1970 as amended by The Patents

(Amendment) Act 2005;

And

In the matter of The Patents (Amendment) Rules, 2006 and as

amended in 2016;

And

In the matter of Patent Application No. 202037007161 dated

11/07/2018 (Nationalization date: 19-02-2020), “Co-Crystal of an
Orally Available HIF Prolyl Hydroxylase Inhibitor” filed in the
name of SANDOZ AG, a Swiss company of Lichtstrasse 35, 4056
Basel, Switzerland

……… Applicant

AFFIDAVIT

I, …….., aged …… years, residing at ………, solemnly affirm and declare as under:

1. I pursued and completed my …… degree, …… in the year …… I possess around ….

Years of experience in the field of ….. I am working as a …… in ……..

2. From …… up till the present, I have employed by the company and have been engaged
in ….. field. And I am the ….. in …… group and exploring to improving the ……..
through my expertise in …….

3. In view of my position, qualifications, experience and knowledge in the field of …… in

particular, my expertise in ……, I am competent to depose this affidavit.

4. I have been provided with the copy of Indian Application No. 202037007161, filed in the
name of SANDOZ AG, on 11/07/2018 entitled “Co-Crystal of an Orally Available HIF
Prolyl Hydroxylase Inhibitor”.
 5. I have also been informed that the said Application is under prosecution before Indian
Patent Office. The Indian Patent Office has issued First Examination Report (FER) on
24/06/2021.

6. I understand that during the examination proceeding of the aforesaid application the
Examiner in the FER has raised objections directed to lack of inventive step and non-
patentability of presently claimed invention in view of documents D1: IN 201741028591,
D2: WO2014014835A2 and D3: Anaelle Tilborg et al.

7. I have been asked to consider the invention disclosed and claimed in the specification to
show that the invention claimed in the patent specification involves inventive step. I have
also been asked to demonstrate that the claimed compounds and process have unexpected
superior solubility properties and stable against variations in temperature and due to the
unexpected technical enhancement, the compounds and preparation process are inventive
over the compounds of the cited prior art documents.

8. I say the invention relates to a co-crystal of roxadustat with L-proline and a process for
the preparation of the aforementioned roxadustat L-proline co-crystal.

9. I say that the Figures 13 and 14 show that the compounds and process of the present
invention provide unexpected superior effects. For such purpose, experiments have been
performed by under my supervision to demonstrate the superior effect of the claimed co-
crystal of roxadustat with L-proline and a process for the preparation of the
aforementioned roxadustat L-proline co-crystal.

10. I say that the document cited as D1 does not relate to co-crystal of roxadustat with L-
proline and a process for the preparation of the aforementioned roxadustat L-proline co-
crystal; and are thus not compared with the present invention.

11. I say that the experiments were conducted as follows:

Figure 13: illustrates a representative sorption isotherm of roxadustat L-proline in the range from
0 to 80% relative humidity. The x-axis displays the relative humidity in percent (%) measured at
a temperature of 25.0 ± 0.1°C, the y-axis displays the equilibrium mass change in weight percent
(w-%). Sample weight at 0% relative humidity is used as reference weight.

Figure 14: illustrates a representative sorption isotherm of L-proline in the range from 0 to 80%
relative humidity. The x-axis displays the relative humidity in percent (%) measured at a
temperature of 25.0 ± 0.1°C, the y-axis displays the equilibrium mass change in weight percent
(w-%). Sample weight at 0% relative humidity is used as reference weight.
Experimental parameters:
Moisture sorption isotherms were recorded with a SPSx-1μ moisture sorption analyzer
(ProUmid, Ulm. The measurement cycle was started at a relative humidity (r.h.) of 30%.
Relative humidity was then decreased to 5% r.h. in 5% steps, followed by a further decrease to
3% r.h. and to 0% r.h. Afterwards r.h. was increased from 0% to approximately 95% r.h. in a
sorption cycle and decreased to 0 % in a desorption cycle in 5% steps. Finally r.h. was increased
to 30% r.h. in 5% steps. The time per step was set to a minimum of 2 hours and a maximum of 6
hours. If an equilibrium condition with a constant mass of ± 0.01% within 1 hour was reached
before the maximum time for all examined samples the sequential humidity step was applied
before the maximum time of 6 hours. If no equilibrium was achieved the consecutive humidity
step was applied after the maximum time of 6 hours. The temperature was 25 ± 0.1 °C.

12. I say that, as evident from the results above, the present invention provides stability
against temperature, stability against moisture, stability against mechanical stress,
increased solubility/dissolution in phosphate buffer pH 6, high crystallinity, and low
residual solvent content. Accordingly, this demonstrates that the presently claimed
subject matter is more efficient in providing a slightly hygroscopic roxadustat co-crystal,
when introducing a deliquescent co-former.
VERIFICATION

I, …….., the deponent above-named, do hereby verify that the content of paragraphs 1 to 12 of
the above affidavit are true and correct to my knowledge and belief, no part of it is false and that
I have not suppressed any material fact.

Verified on this the … day of ……, 20…

……….
(Deponent)