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(12) Patent Application Publication (10) Pub. No.: US 2016/0346294 A1 SENGUPTA Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2016/0346294 A1 SENGUPTA Et Al US 2016.0346294A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2016/0346294 A1 SENGUPTA et al. (43) Pub. Date: Dec. 1, 2016 (54) TREATMENTS FOR RESISTANT ACNE Publication Classification (71) Applicant: VYOME BIOSCIENCES PVT. LTD., (51) Int. Cl. New Delhi (IN) A6II 3/55 (2006.01) A63L/92 (2006.01) (72) Inventors: Shiladitya SENGUPTA, Delhi (IN); A6II 47/08 (2006.01) Suresh Rameshlal CHAWRAI, Pune A6II 47/8 (2006.01) (IN); Shamik GHOSH, Delhi (IN); C07D 53/04 (2006.01) Sumana GHOSH, Delhi (IN); Nilu A6II 47/38 (2006.01) JAIN, New Delhi (IN); Suresh A6II 47/32 (2006.01) SADHASIVAM, Salem (IN); Richard A6II 47/36 (2006.01) BUCHTA, Melbourne (AU); Anamika A6II 47/02 (2006.01) BHATTACHARYYA, Delhi (IN) A6II 45/06 (2006.01) A6II 47/10 (2006.01) (73) Assignee: VYOME BIOSCIENCES PVT. LTD., (52) U.S. Cl. New Delhi (IN) CPC ............... A6 IK3I/55 (2013.01); A61K 45/06 (2013.01); A61K 31/192 (2013.01); A61 K (21) Appl. No.: 15/115,143 47/08 (2013.01); A61K 47/183 (2013.01); A61K 47/10 (2013.01); A61K 47/38 (2013.01); (22) PCT Fed: Jan. 29, 2015 A61K 47/32 (2013.01); A61K 47/36 (2013.01); PCT No.: PCT/N2O15/000057 A61K 47/02 (2013.01); C07D 513/04 (86) (2013.01) S 371 (c)(1), (2) Date: Jul. 28, 2016 (57) ABSTRACT (30) Foreign Application Priority Data The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial Jan. 29, 2014 (IN) ............................. 269/DELA2014 infections in general and more specifically to bacterial Nov. 10, 2014 (IN) ........................... 3247/DELA2014 infections with antibiotic resistant pathogens Patent Application Publication Dec. 1, 2016 Sheet 1 of 14 US 2016/0346294 A1 50 Cephalothin O O Nadioxacin Roxythromycin Besifloxacin Pulifloxacin Clindamycin -- Cefoxitin --- Ulifloxacin FIG. IA 5 Cephalothin Nadifloxacin OO Roxithromycin Besifloxacin Ulifloxacin Pulifloxacin Cindamycin Cefoxitin FIG. IB Patent Application Publication Dec. 1, 2016 Sheet 2 of 14 US 2016/0346294 A1 DART molecules Dose response Curve Against P. acnes MTCC 1951 80 0.25 s a 2 s SS 0.00 0.05 0.10 0.45 0.20 0.25 Antibiotic Concentration (u FIG. ID Patent Application Publication Dec. 1, 2016 Sheet 3 of 14 US 2016/0346294 A1 omp. 91 conc. (M) 0.25- 0.50 100 2.50 5.00 ane 1- Relaxed DNA (Negative Control) ane2- DNA+ Gyrase (Positive Control) ne3-7 Comp, 91 with increasing conc. ne8- Supercoiled DNA marker o e an sh Gyrase t t t compound 91 0.25 0.50 1.00 2.50 5.00 Compound Conc. (M) FIGS 2A and 2B Patent Application Publication Dec. 1, 2016 Sheet 4 of 14 US 2016/0346294 A1 Z Compound 113 S Compound 94 8 Compound 115 Compound 90 (III) Compound 116 EEEEEEEE Compound 91 1MCompound 2.5M Compound FIG. 3A Nadifloxacin Compound 91 Ø [IIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIII FIG. 3B Patent Application Publication Dec. 1, 2016 Sheet 5 of 14 US 2016/0346294 A1 P. acneS Compound 91 (25pg/ml) Dexamethasone (0.4 ug/ml) Vehicle P. acnes Compound 91 (25pg/ml) Dexamethasone (0.4 g/ml) Vehicle Data expressed as Meant SD, n=3 FIGS 4A and 4B Patent Application Publication Dec. 1, 2016 Sheet 6 of 14 US 2016/0346294 A1 O P. acnes Compound 91 (25pg/ml) Dexamethasone (0.4 g/ml) Vehicle S o O. Ye c v s P. acnes Compound 91 (25pg/ml) Dexamethasone (0.4 g/ml) Vehicle Data expressed as Meant SD, n=3 FIGS 5A and 5B Patent Application Publication Dec. 1, 2016 Sheet 7 of 14 US 2016/0346294 A1 MICValue of the Formulations against P. acnes 0.5 O.3 - 0.25 0.13- 0.25 Besifloxacingel Besifloxacint-Adapatene Placebo ge gel FIG. 6 Dose Respose Curve of Gels Against P, acnes K Besifloxacingel O Besifloxacin-i-Adapalenegel A Placebo ge a log. (Besifloxacingel) Log. Besifloxacint-Adapalene gel) . Log. Placebogel) a-as-as-as-as-as-as-a-A 0.25 O.5 O.75 1 Besifloxacin Concentration (ppm) FIG. 7 Patent Application Publication Dec. 1, 2016 Sheet 8 of 14 US 2016/0346294 A1 Time Kill Kinetics of the Formulations against P. acnes -----. Besigel (1ppm) 8. 5:::::: -- Besigel(10ppm) "A" Besi-Adagel (1 ppm) 7 - A - Besi-Adagel (10ppm) ---O-- Placebo gel (1ppm) -O- Placebo gel(10ppm) Time (h) -----------------...-...------------,-,-,------------------l SSO --Besifloxacin gel -- Placebo get --------------------------------------------- --- - --- --- Fig. 9 Patent Application Publication Dec. 1, 2016 Sheet 9 of 14 US 2016/0346294 A1 Besifloxacinformulations Time Kill Against P. acnes MTCC 1951 O 5 1 O 15 2O 25 30 Time (Hrs.) -O- GL10201 ug?ml -O- GL102010 ugml -v- CR/0031 ug/ml -4- CR/00310 ug/mt -- CR/0291 ug/ml -- CR/029 10 ugm -0-- Broth Control FIG. IO Patent Application Publication Dec. 1, 2016 Sheet 10 of 14 US 2016/0346294 A1 Besifloxacin Time Kill against S. aureus MTCC 6908 2 3 4 5 Time (Hrs.) -o- BTK-12.5ug/ml -o- BTK-2 2.5ugiml -v- BTK-32.5ug/ml -A- BTK-42.5ug/ml -- BTK-52.5ug/ml -- BTK-62.5ug/ml -- Broth Control FIG II Patent Application Publication Dec. 1, 2016 Sheet 11 of 14 US 2016/0346294 A1 Besifloxacintime kill against P. acnes CCARM 9010 7 . 6 O 5 10 15 20 25 30 Time (hrs.) -0- Besifloxain 2.5ug/ml water -O- Besifloxacin 2.5ug/ml DMSO -v- Both Control FIG. 12 Patent Application Publication Dec. 1, 2016 Sheet 12 of 14 US 2016/0346294 A1 7. S 5 O --------------------- : O 8 12 6 2O A. Time Point (h) -WLN-F19/BSF/GL1068 --a-WLN-F21/BSF/G/OOA -WLN-F2OBSF/CRF004 Fig. 13 Patent Application Publication Dec. 1, 2016 Sheet 13 of 14 US 2016/0346294 A1 P. acneS Besifloxacin (10 pg/ml) Besifloxacin (30 pg/ml) Dexamethasone (0.4 pg/ml) Vehicle 1OOO - 500 O P. acneS Besifloxacin (10 g/ml) Besifloxacin (30 g/ml) DexamethaSone (0.4 g/ml) Vehicle Data expressed as Meant SD, n=3 FIGS. 14A and 14B Patent Application Publication Dec. 1, 2016 Sheet 14 of 14 US 2016/0346294 A1 P. acres Besifloxacin (10 g/ml) Adapalene (0.04 g/ml) Adapalene (0.4 g/ml) Dexamethasone (0.4 g/ml) Vehicle 2S S c O. ase o ad Besifloxacin (10pg/ml) Adapalene (0.04 g/ml) Adapalene (0.4 ug/ml) Dexamethasone (0.4 g/ml) Vehicle Data expressed as Meant SD, n=3 FIGS, 15A and 15B US 2016/0346294 A1 Dec. 1, 2016 TREATMENTS FOR RESISTANT ACNE and nicotinamide; minerals such as zinc.; benzoyl peroxide; octopirox, triclosan; azelaic acid; phenoxyethanol; phenoxy RELATED APPLICATIONS propanol; and flavinoids, these agents tend to lack in poten 0001. This application claims benefit priority of Indian tial to mitigate the acne condition and may have negative Patent Application No. 269/DEL/2014, filed Jan. 29, 2014 side effects when devised in conventional topical formula and No. 3247/DEL/2014, filed Nov. 10, 2014, the content of tions. A key challenge that has limited the use of topical both applications is incorporated herein by reference in their formulations is the absence of formulations with the desired entirety. physicochemical properties and high drug loading, which maintains a concentration significantly higher than the MIC at the site of application by facilitating the right degree of FIELD OF THE INVENTION penetration over time but with minimal systemic exposure. 0002 The present disclosure relates generally to novel A formulation that addresses these unmet needs can be a molecules, compositions, and formulations for treatment of significant advance in the treatment of acne. bacterial infections in general and more specifically to 0007 Furthermore, as articulated in Taglietti et al. bacterial infections with antibiotic-tolerant pathogens. 2008, when it comes to the delivery of a drug to a specific site, topical formulations that are efficacious are probably BACKGROUND OF THE INVENTION among the most challenging products to develop. Once the 0003) Acne Vulgaris is a skin condition that affects over product is applied on the skin, a complex interaction occurs 85% of all people. Acne is a term for a medical condition of between the formulation, the active compounds, and the skin plugged pores typically occurring on the face, neck, and itself. The penetration of the active compound(s) into the upper torso. Following are four primary factors that are skin follows Fick's first law of diffusion, which describes the currently known to contribute to the formation of acne transfer rate of Solutes as a function of the concentration of Vulgaris; (1) increased sebum output resulting in oily, greasy the various ingredients, the size of the treatment Surface skin; (2) increased bacterial activity, normally due to an area, and the permeability of the skin. However, the skins overabundance of Propionibacterium acnes bacteria; (3) permeability can be influenced by many factors, such as the plugging (hypercornification) of the follicle or piloseba drying, moisturizing, or occluding effects of the excipients ceous duct; and (4) and inflammation. The plugged pores in the formulation, which, in combination, can modulate the result in blackheads, whiteheads, pimples or deeper lumps release of the product at the treatment site. In acne, the site such as cysts or nodules. Severe cases of acne can result in of action is inside the pilosebaceous unit and, therefore, an permanent scarring or disfiguring. efficacious anti-acne formulation should facilitate the pen 0004 Though acne Vulgaris is multifactoral, a commen etration of the active compound(s) into this extremely lipo sal skin bacteria (P. acnes) plays a major role in the philic environment. An effective topical formulation there formation of acne lesion.
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