API and IP Newsletter

 Contents

• ANDA approvals in September 2023

• General information

• 'Chandrika' Soap Trademark Case: Supreme Court Restrains Mariyas Soaps & Chemicals From Using Trademark 'Chandra

• What is the complete Humans of Bombay v. People of India controversy?

• Intellectual Property

• T 0429/21 (PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DRY EYE)

ANDA approvals in September 2023

We follow ANDA approvals. In September there are about 47 ANDA approvals. Out of which 11 are tentative approvals. Aurobindo received 5 ANDA approvals in September whereas Amneal and Hetero received 3 approvals each. 

Some of our observations are as below.

Drug Name	Company	Comments
CLINDAMYCIN PHOSPHATE; TRETINOIN ANDA  #216943	ENCUBE ETHICALS PRIVATE LTD	This approval is 1.2%; 0.025% gel. Clindamycin and tretinoin topical is used to treat acne. Exact US sales information is not available in public domain, but based on other similar products’ sales in US, it could be estimated that US sales would be < USD 80-100/a.
SPIRONOLACTONE     ANDA  #215572	AMNEAL PHARM	This is 25MG/5ML Oral suspension. Several composition patents listed in OB, expiration 2036. Those could have been circumvented by Amneal. Spironolactone is used to treat certain patients with hyperaldosteronism. In 2020, it was the 51st most commonly prescribed medication in the United States, with more than 13 million prescriptions
LOPERAMIDE HYDROCHLORIDE          ANDA  #218122	AUROBINDO PHARMA LTD	This approval is for 2 MG capsule. There are few ANDA approvals already, this is a small product in US. Loperamide Hydrochloride Capsules USP, 2 mg had annual sales of US $34.7 million in the United States (IQVIA MAT, January 2023). Loperamide is a medicine to treat diarrhoea.
THEOPHYLLINE              ANDA  #217422	ANNORA PHARMA PRIVATE LTD	This is 300 MG and 450 MG ER tablets. There are many approvals in US. This is very small product in US. Theophylline extended-release tablets had annual sales of US$ 8 million as per public domain information.
ACETAZOLAMIDEANDA  #211151	AJANTA PHARMA LTD	This approval is for 125 MG and 250 MG Tablets.  Acetazolamide tablets 125 mg and 250 mg had annual sales of 16 million in the US, as per IQVIA MAT December 2022 data. There are too many ANDA approvals. Acetazolamide is a diuretic medication that treats swelling caused by heart disease.

General information

'Chandrika' Soap Trademark Case: Supreme Court Restrains Mariyas Soaps & Chemicals From Using Trademark 'Chandra 

The Supreme Court in the case M/S. Wipro Enterprises Limited V. M/S. Mariyas Soaps and Chemicals observed and has restrained M/s Mariyas Soaps and Chemicals from using the registered trademark of them ‘Chandra’, wherein an appeal is made by Wipro for being similar to its trademarked soap range ‘Chandrika’. 

News here.

What is the complete Humans of Bombay v. People of India controversy?

The “Humans of Bombay” a storytelling platform based in Mumbai has witnessed massive criticism, all due to a lawsuit that the platform filed against “People of India”. The lawsuit alleged that the latter violated the former’s copyright. Here is the complete story explained to you. 

News here

Intellectual Property 

T 0429/21 (PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DRY EYE)

1. This is regarding patent application EP2614860, filed by Consejo Superior de Investigaciones Cientificas CSIC, Universidad. ( The Spanish National Research Council)

2. The invention relates to Xerophthalmia or dry eye syndrome. 

Xerophthalmia

3. Xerophthalmia or dry eye syndrome is a disease characterised by persistent dryness of the conjunctiva and opacity of the cornea.

4. Treatments used to treat xeropthalmia include corticosteroids which may be effective in early stages of the disease, vitamin A supplements and pilocarpine which is a drug that increases tear production. 

5. Among improve dryness preparations (artificial teras) solutions Hypromellose and carbomer gel which are applied to the conjunctiva are used. 

Alleged invention

6. According to the patentee, the available treatments have clear limitations regarding its efficacy and toxicity. Therefore, inventors of this patent application allegedly provided new improved treatments for xeropthalmia. 

7. Inventors used TRPM8 agonists or of combinations thereof for manufacturing a medicament for the treatment or prevention of a disease selected from xerophthalmia.

8. The claim which was prosecuted was briefly as below

9. “An ophthalmic composition for use in a method of treatment or prevention of xerophthalmia or dry eye syndrome, said composition comprising a therapeutically effective amount of a TRPM8 agonist, wherein said TRPM8 agonist is 2-isopropyl-5- methylcyclohexanecarboxylic acid (4-methoxyphenyl)-amide (WS-12)."

Prior Art documents

10. Key prior art references discussed during prosecution are as below

1. D8: DAVID D MCKEMY: "Therapeutic potential of TRPM8 modulators", OPEN DRUG DISCOVERY JOURNAL, BENTHAM SCIENCE PUBLISHERS B.V,NL, vol. 2, no. Special Issue 2, 1 January 2010 (2010-01 -01), pages 81 -88 here

2. D9: SHERKHELI MUHAMMAD AZHAR ET AL: "Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship", JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES, CANADIAN SOCIETY FOR PHARMACEUTICAL SCIENCES, EDMONTON, CA, vol. 13, no. 2, 22 July 2010 (2010-07-22), pages 242-253

3. D12: A Robbins ET AL: "Menthol stimulated lacrimation and induction of Fos in the trigeminal nucleus", Chicago, 21 October 2009 (2009-10-21), & DATABASE BIOSIS [Online]BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; 21 October2009 (2009-10-21) A.Robbins et al: "Menthol stimulated lacrimation and induction of Fos in the trigeminal nucleus"

4. D14: BÖDDING ET AL: "Characterisation of TRPM8 as a pharmacophore receptor", CELL CALCIUM, CHURCHILL LIVINGSTONE, GB,vol. 42, no. 6, 29 September 2007 (2007-09-29), pages 618-628

5. D15: BECK ET AL: "Prospects for prostate cancer imaging and therapy using high-affinity TRPM8 activators", CELL CALCIUM, CHURCHILL LIVINGSTONE, GB, vol.41, no. 3, 4 February 2007 (2007-02-04), pages 285-294

6. D16: SHERKHELI M A ET AL: "Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels", PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES, FACULTY OF PHARMACY, UNIVERSITY OF KARACHI, PK, vol. 21, no. 4, 1 October 2008(2008-10-01), pages 370-378.

7. D17: Steven J Charlton: "Agonist efficacy and receptor desensitization: from partial truths to a fuller picture", BRITISH JOURNAL OF PHARMACOLOGY, vol. 158, no.1, 1 September 2009 (2009-09-01), pages 165-168, XP055695488

8. D22: AERIE An Emerging Leader in Ophthalmology

11. D12 was considered to be the closest prior art. The problem was the provision of a better TRPM8 agonist for use in dry eye syndrome. The solution was obvious in view of D8, as well as of D9 and D14-D17.

12. Based on these prior art documents the Examination Division at European Patent Office (EPO) refused to grant the application. Patentee filed an appeal against the decision. Oral proceedings before the Board at European Patent Office took place on 6 July 2023.

13. The patentee’s arguments can be summarised as follows:

Patentee’s argument

14. According to the patentee, in D12 the activity of menthol as TRPM8 agonist was a simple assumption, since there was no absolute proof of its action through the TRPM8 channels; the tear secretion in D12 could for instance have been triggered by a simple eye irritation.

15. The application showed that the compound WS-12 provided a better effect, as shown in Table 2, with the lowest EC50 value of all TRPM8 agonists. This was confirmed by D22. The problem was the provision of a better agent and medicament for the treatment of xerophthalmia. There was no clear pointer in the prior art for the selection of WS-12, and it was not a try and see approach that could be taken either.

Board’s view

16. The Board noted that TPM8 agonists were known at the effective date of the present application, and that WS-12 was identified as the TRPM8 agonist with the lowest EC50.

17. The Board commented, D8 is a study on the therapeutic potential of TRPM8 modulators, which discloses that WS-12 is the most potent TRPM8 agonist (D8, page 83, right-hand column, third paragraph). This result is illustrated by the EC50 given in Table 1 of D8 on pages 84 and 85. (Here). This Table gives for menthol and for WS-12 the same EC50 values reported in Table 2 of the patent application, namely 66.7 µM for menthol and 193 µM for WS-12. (Here)

18. Hence, in the Board's view, it was known from D12 that the TRPM8 receptors act on the tear production; this document clearly identified menthol as a TRPM8 agonist acting through this pathway on the tear production. When looking for a potentially better TRPM8 agonist, i.e. a substance more effective than menthol, the skilled person would test the known TRPM8 agonists and would focus in particular on those agonist(s) providing the best activity. This would inevitably lead the skilled person to the selection of the compound WS-12 which is disclosed as the compound having the lowest EC50 value for TRPM8 receptors and represents therefore the most promising TRPM8 agonist.

19. Under these circumstances, the Board is convinced that the person skilled in the art looking for a solution to the problem would have been led by the technical teaching of inter alia documents D8 and D9 to test the molecules described therein, starting with the most effective molecules, and this test would have resulted in the selection of the compound WS-12.

20. The appeal from Patentee is rejected by the Board. 

Decision here