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WO 2013/042140 A4 28 March 2013 (28.03.2013) P O P C T

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WO 2013/042140 A4 28 March 2013 (28.03.2013) P O P C T (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2013/042140 A4 28 March 2013 (28.03.2013) P O P C T (51) International Patent Classification: NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, A61K 31/197 (2006.01) A61K 45/06 (2006.01) RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, A61K 31/60 (2006.01) A61P 31/00 (2006.01) TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, A61K 33/22 (2006.01) ZM, ZW. (21) International Application Number: (84) Designated States (unless otherwise indicated, for every PCT/IN20 12/000634 kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (22) International Filing Date UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 24 September 2012 (24.09.2012) TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (25) Filing Language: English EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (26) Publication Language: English TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (30) Priority Data: ML, MR, NE, SN, TD, TG). 2792/DEL/201 1 23 September 201 1 (23.09.201 1) IN Declarations under Rule 4.17 : (72) Inventor; and — of inventorship (Rule 4.17(iv)) (71) Applicant : CHAUDHARY, Manu [IN/IN]; 51-52, In dustrial Area Phase- 1, Panchkula 1341 13 (IN). Published: — with international search report (Art. 21(3)) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, — with amended claims and statement (Art. 19(1)) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (88) Date of publication of the international search report: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, 23 May 20 13 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, Date of publication of the amended claims and statement: 25 KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, July 2013 ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, < © © (54) Title: NON ANTIBIOTIC, NON PEPTIDE COMPOUNDS FOR ANTIBIOTIC EFFICACY & SAFETY ENHANCEMENT o (57) Abstract: The present invention provides one or more non antibiotic non peptidic entity to augment antimicrobial activity of one or more antimicrobial agent for combating microbial resistance The non antibiotic non peptidic entity is used individually or in combination with one or more antibiotic as single unit dose or is presented through a suitable medium The non antibiotic non pep - tidic entity make one or more accompanying antibiotic effective by rendering eradication of antimicrobial resistance broadening spectrum and reducing multi bacterial resistance AMENDED CLAIMS received by the International Bureau on 4 June 2013 (04.06.2013) 1. A non-antibiotic, non-peptidic entity to potentiate activity of one or more antibiotic(s) in treatment of infection(s) caused by one or more microbial resistant strain(s), wherein said entity is selected from the group comprising an effective amount of EDTA disodium, sodium tetraborate, Sodium salicylate, boric acid or a pharmaceutically acceptable salt thereof wherein, said entity is present in range of about 0.15 % to about 15% of said antibiotic. 2. The non-antibiotic, non-peptidic entity of claim 1 , wherein each entity is present in range of about 0.0015 to 1.5%. 3. The non-antibiotic, non-peptidic entity of claim 1 , wherein said microbial resistant strain is selected from the group comprising ESBL, MRSA, VRSA, VISA, VRJE, NDM- 1 , MBL producing strain, aminoglycoside resistance strains, efflux over expressed strains, bio-film producing strains or a combination thereof. 4. The non-antibiotic, non-peptidic entity of claim 1 , wherein said non-antibiotic, non-peptidic entity further comprises citric acid, tannic acid, reserpine, arylpiperazines, alkylaminoquinolones, nocardamines or a pharmaceutically acceptable salt thereof. 5. The entity of claim 1 , wherein said entity is administered either together as a single unit dose with said antibiotic or is administered separately before/after/during administration of said antibiotic. 6. The entity of claim 1 , wherein said entity is delivered in route selected from the group comprising topical, oral, parenteral and ocular route. 7. The entity of claim 1 , wherein said entity is presented in a form selected from the group comprising nano-particles, dry powder, gel, solution or a pharmaceutically acceptable forms thereof. 8. A synergistic antibiotic composition for treatment and containment of bacterial resistance, said composition comprising a non-antibiotic, non-peptidic entity to potentiate activity of one or more antibiotic(s) component in treatment of infection(s) caused by one or more microbial resistant strain(s), wherein said entity is selected from the group comprising an effective amount of EDTA disodium, sodium tetraborate, Sodium salicylate, boric acid or a pharmaceutically acceptable salt thereof; wherein said antibiotic component is selected form the group comprising penicillins, cephalosporins, carbapenems, aminoglycosides, sulfonamides, quinolones, tetracyclines, macrolides, glycopeptide , oxazolidinones or combinations thereof; and wherein proportion of said non-antibiotic, non-peptidic entity and said antibiotic component is in a range of about 0.15 % to about 15% of said antibiotic. 9. The synergistic composition of claim 4, wherein said non-antibiotic, non-peptidic entity is present either as a single unit dose with said antibiotic component or is present in a suitable solvent medium. 10. The synergistic composition of claim 4, wherein said non-antibiotic, non-peptidic entity further comprising citric acid, tannic acid, reserpine, arylpiperazines, alkylaminoquinolones, nocardamines or a pharmaceutically acceptable salt thereof. 11. The synergistic composition of claim 4, wherein said antibiotic component further comprises one more betalactamase inhibitor selected from the group comprising sulbactam, tazobactarn, Λ clauvulanic acid or a combination thereof. 12. A method of of treating one ore more bacterial infection caused by drug-resistant bacterium, comprising route of administration of selected from the group comprising oral, parenteral (Intravascular IV, Intramuscular IM, Subcutaneous SC), occular, transdermal or combinational administration of an effective amount of a non-antibiotic, non-peptidic entity to a patent under medication of one or more antibiotics in pharmaceutically acceptable dosage form of tablet, capsule, syrup, suspension, solution, powder, granules, gel, lotion, ointment, spray and liposomes or a combination thereof. 13. The method of treatment of claim 13, wherein said non-antibiotici non-peptidic entity is present in a proportion of 0.15 % to about 15% of the antibiotic component. 14. The method of treatment of claim 13, drug-resistant bacterium is selected from the group comprising ESBL, MRSA, VRSA, VISA, VRE, NDM- 1 , MBL producing strain, aminoglycoside resistance strains, efflux over expressed strains, bio-film producing strains, Haemophilus influenzae, Neisseria gonorrhoeaea, N. meningitis, Staph. Epidermidis, pneumococci, Streptococcus mitis, Enterococcus faecalis, Streptococcus pneumoni; Staphylococcus haemolyticus. 15. The method of treatment of claim 13, wherein said bacteria responsible for the infection bei treated is at least Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonii Streptococcus pneumoniae, Haemophilus influenzae, Neisseria gonorrhoeae, Proteus mirabil Staphylococcus aureus, A. baumannii, Enterobacter spp., Serratia spp, Serratia marcescei Streptococcus species, Mycoplasma pneumoniae, Chlamydophila pneumoniae, Legione ,Moraxella catarrhalis, Streptococcus pyogenes, Streptococcus viridans, Staphylococc epidermidis, Klebsiella oxytoca, Morganella morganii, Acinetobacter calcoaceticus, Bacteroic fragilis , Peptostreptococcus species, Proteus vulgaris enterococci, Chlamydia trachomat Clostridium species, Neisseria meningitidis, Streptococcus agalactiae, Bartonella bacilliform Bartonella henselae, Listeria monocytogenes, Tropheryma whipplei, staphylococcus a saprophyticus c.braakii and other species thereof showing resistance to one or more antibiotic: 16. The method of treatment of claim 13, wherein said bacterial infection being treated is select from the group consisting of lower respiratory tract infection, skin and skin structure infectk urinary tract infection, Gonorrhea, Pelvic inflammatory disease, sepsis, soft tissue infectioi wound infections,renal infections, nocardial pulmonary infections, mycobacterial lymphaden leprosy, gastrointestinal infections; infections related to abdominal trauma, bloodstrei infections, anthrax, plagues; scarlet fever, rheumatic fever, cholera, Haverhill fever, Potom fever, brucellosis, Carrion's disease, trench fever, bacillary epithelioid angiomatos leptospirosis, Lyme disease, rickettsiosis, Q fever, human monocytotropic ehrlichiosis, < scratch disease, tularemia, pseudo-infections, legionellosis, noscoccomial infectioi erysipeloid, osteomyehtis, prostatitis, peritonitis, encephalitis, cerebrospinal infectioi infection of cerebrospinal fluid shunt, meningoencephalitis, joint infections, prosthetic jo infections, septic arthritis, myonecrosis, echyma gangrenosum, cholecystitis, 'melioidos mastoiditis, epididymitis, bursitis. 17. The method of treatment of claim 13, wherein said bacterial infection comprises infecti condition
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