Patent application EP17162132A (EP), filed 2017-03-21
Publication number: EP3222324A1
Title: VALPROATE AS A TOPICAL ANTI-FUNGAL TREATMENT
Abstract: Valproate is useful as an antifungal agent. The valproate compositions can be used to treat antifungal infections. The valproate compositions can be formulated as topical antifungals.
IPC codes: A61K  31/    19            A I
A61P  31/    10            A I
A61K  33/    14            A I
A61K   9/    00            A I
A61K   9/    06            A I
A61K   9/   107            A I
A61K   9/    12            A I
A61K   9/    14            A I
A61K   9/    70            A I
Claims: number: 1
text: A topical formulation comprising a therapeutically effective amount of valproate (VPA) or valproic acid and salt.
number: 2
text: The topical formulation of claim 1, wherein the formulation further comprises a penetration enhancer.
number: 3
text: The topical formulation of claim 2, wherein the penetration enhancer is a sulphoxide, an ether, a surfactant, an alcohol, a polyol, a fatty acid, an amide, a pyrrolidone, a terpene, or an azone.
number: 4
text: The topical formulation of claim 1, wherein the VPA is sodium VPA.
number: 5
text: The topical formulation of claim 1, wherein the salt is sodium chloride, potassium chloride, calcium chloride, sodium hydrogen phosphate, or potassium hydrogen phosphate.
number: 6
text: The topical formulation of claim 5, wherein the salt is sodium chloride.
number: 7
text: The topical formulation of claim 1 for use in a method of treating a fungal infection in a subject, wherein the method comprises administering the topical formulation to the subject, thereby treating a fungal infection.
number: 8
text: The topical formulation for use of claim 7, wherein the fungal infection is athlete's foot , penile thrush , ringworm , oncomycosis, thrush, vaginal yeast infection, or fungal eye infection.
number: 9
text: The topical formulation for use claim 7, wherein the fungal infection is caused by Candida, Histoplasma, Microsporum , Epidermophyton , Trichophyton, or a combination thereof .
number: 10
text: A formulation including VPA or valproic acid and a salt for use in amethod of treating a fungal infection in a subject, wherein the method comprises administering the formulation to the subject.
number: 11
text: The formulation for use of claim 10, wherein the fungal infection comprises systemic mycoses.
number: 12
text: The formulation for use of claim 10, wherein the fungal infection is caused by Aspergillus, Blastomyces, Candida, Cryptococcus, Histoplasma, Pneumocystis, Stachybotrys, Coccidioides, Microsporum , Epidermophyton, Trichophyton, or a combination thereof .
number: 13
text: The formulation for use of claim 10, wherein the salt is sodium chloride, potassium chloride, calcium chloride, sodium hydrogen phosphate, or potassium hydrogen phosphate.
number: 14
text: The formulation for use of claim 10, wherein the salt is sodium chloride.
Office action: search_report, dated 2017-09-27
Rejection reasons: novelty_epc_54
inventive_step_epc_56
Prior art cited: ref_id: - SMITH ET AL.: "Percutaneous Penetration Enhancers", 1995, CRC PRESS, INC.
ref_type: npl
severity: background
ref_id: - "Webster's Dictionary"
ref_type: npl
severity: background
ref_id: - "Oxford Dictionary of Biochemistry and Molecular Biology", 2004, OXFORD UNIVERSITY PRESS
ref_type: npl
severity: background
ref_id: WO2011097577A2
ref_type: patent
severity: background
ref_id: WO2010093564A1
ref_type: patent
severity: background
ref_id: US4689334A
ref_type: patent
severity: background
ref_id: WO02069983A1
ref_type: patent
severity: background
ref_id: - DATABASE WPI Week 201714, Derwent World Patents Index; AN 2016-74130Y, XP002771133
ref_type: npl
severity: background
ref_id: - NWADIUTO ESIOBU ET AL: "An assessment of the in vitro antimicrobial effects of two antiepileptic drugs - sodium valproate and phenytoin", ANTONIE VAN LEEUWENHOEK, KLUWER ACADEMIC PUBLISHERS, DO, vol. 83, no. 1, 1 March 2003 (2003-03-01), pages 63 - 68, XP019228783, ISSN: 1572-9699, DOI: 10.1023/A:1022992224594
ref_type: npl
severity: background
ref_id: - LIU ZHENGCAI ET AL: "Synergistic effects of hypertonic saline and valproic acid in a lethal rat two-hit model", JOURNAL OF TRAUMA AND ACUTE CARE SURGERY, vol. 74, no. 4, April 2013 (2013-04-01), pages 991 - 997, XP008184923
ref_type: npl
severity: background
ref_id: CN106135290
ref_type: patent
severity: novelty_destroying
ref_id: US4689334
ref_type: patent
severity: novelty_destroying
ref_id: WO02069983
ref_type: patent
severity: obviousness
ref_id: WO2010093564
ref_type: patent
severity: novelty_destroying
ref_id: WO2011097577
ref_type: patent
severity: novelty_destroying
ref_id: - DATABASE WPI, 0, Derwent World Patents Index, vol. 2017, no. 14, Database accession no. 2016-74130Y, XP002771133 & CN106135290 A 20161123 (ZHENGZHOU TOBACCO RES INST CNDC) [XP] 1,7 * abstract *
ref_type: npl
severity: novelty_destroying
ref_id: - NWADIUTO ESIOBU ET AL, "An assessment of the in vitro antimicrobial effects of two antiepileptic drugs - sodium valproate and phenytoin", ANTONIE VAN LEEUWENHOEK, KLUWER ACADEMIC PUBLISHERS, DO, (20030301), vol. 83, no. 1, doi:10.1023/A:1022992224594, ISSN 1572-9699, pages 63 - 68, XP019228783 [Y] 1-5,7-13 * page  67, column  2, paragraph  2 *
ref_type: npl
severity: obviousness
ref_id: - LIU ZHENGCAI ET AL, "Synergistic effects of hypertonic saline and valproic acid in a lethal rat two-hit model", JOURNAL OF TRAUMA AND ACUTE CARE SURGERY, (201304), vol. 74, no. 4, pages 991 - 997, XP008184923 [X] 1,4-6 * abstract * * page  992, column  2, paragraph  2 *
ref_type: npl
severity: novelty_destroying
Final disposition: pending (2017-09-27)