Polymerase inhibitors and their use in treating tumours

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This patent describes novel polymerase inhibitors, specifically compounds that modulate DNA polymerase alpha, for the treatment of various skin tumours and cell modifications. The invention focuses on certain nucleoside analogs that demonstrate superior anti-proliferative effects on malignant melanomas, squamous cell carcinomas, and basal cell carcinomas, among other abnormal skin tissue growths. The compounds can be formulated into a range of pharmaceutical preparations for topical, oral, or systemic administration.

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• Topical treatment of skin cancers such as malignant melanoma, basal cell carcinoma, and squamous cell carcinoma.
• Therapy for pre-cancerous skin conditions, such as actinic keratosis.
• Use as a pharmaceutical composition in dermatology for controlling abnormal cell proliferation.
• Adjunct therapy in combination with surgery or immunotherapy for treating metastases from skin tumours.
• Potential template or reference compound for designing new polymerase inhibitors in drug discovery.
• Treatment of benign skin lesions displaying abnormal cell growth.

BenefitsContent extracted from patent full text and abstract with AI.

• Targeted inhibition of DNA polymerase alpha offers specificity in combating tumor cell proliferation.
• Greater selectivity for tumor cells over normal skin cells, minimizing damage to healthy tissue and reducing side effects.
• Potential to be administered in various forms (creams, gels, tablets, injections), increasing flexibility and patient compliance.
• Demonstrated higher anti-proliferative activity compared to some existing therapeutic agents (such as diclofenac or 5-FU).
• Ability to address several types of cell modification, including pre-cancerous and cancerous lesions.
• Basis for designing further improved polymerase inhibitors for use in oncology.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

Agent (Q) to treat cell-modification in a skin region, preferably malignant melanoma, spinocellular carcinoma and/or basalioma, which modulates a polymerase, comprises: 3-(6-amino-9H-purine-2-ylamino)-phenol compound (I); (R)-5-[(R)-6-amino-2-(3-hydroxy-phenylamino)-purine-9-yl]-tetrahydro-furan-3-ol compound (II); (2R,3R)-5-[(R)-6-amino-2-(3-hydroxy-phenylamino)-purine-9-yl]-2-(2-phosphanyl-ethyl)-tetrahydro-furan-3-ol compound (III); and 3-[6-amino-9-(2-phosphanylmethoxy-ethyl)-9H-purine-2-ylamino]-phenol compound (IV). Agent (Q) to treat cell-modification in a skin region, preferably malignant melanoma, spinocellular carcinoma and/or basalioma, which modulates a polymerase, comprises: 3-(6-amino-9H-purine-2-ylamino)-phenol compound of formula (I); (R)-5-[(R)-6-amino-2-(3-hydroxy-phenylamino)-purine-9-yl]-tetrahydro-furan-3-ol compound of formula (II); (2R,3R)-5-[(R)-6-amino-2-(3-hydroxy-phenylamino)-purine-9-yl]-2-(2-phosphanyl-ethyl)-tetrahydro-furan-3-ol compound of formula (III); and 3-[6-amino-9-(2-phosphanylmethoxy-ethyl)-9H-purine-2-ylamino]-phenol compound of formula (IV). R 1>H or mono-, di- or tri-phosphate; R 2>butyl, pentyl, hexyl or isohexyl derivative; and R 4>O or NOH. Independent claims are included for: (1) a pharmaceutical agent comprising (Q) and a carrier; and (2) a kit comprising the pharmaceutical agent together with an instruction for combining the contents of the kit. [Image] [Image] ACTIVITY : Cytostatic; Keratolytic; Dermatological. MECHANISM OF ACTION : DNA polymerase-alpha modulator.