Indole-based small molecule antivirals against SARS-COV-2

Abstract

The present invention relates to the preparation of indole-based compounds in free form or an acceptable salt form potential therapeutic target as an antiviral agent against SARS-Cov2. The indole-based small molecules are, capable of antiviral activity in RT-qPCR and cell-based assay in SARS-CoV-2 infected VERO E6 cells, that may ultimately be used to achieve improved human health in patients against covid- 19 or other similar viral diseases.

Description

[0001]PT / 2025 / 10975 Indole-based small molecule antivirals against SARS-COV-2 FIELD OF THE INVENTION The present invention relates to indole-based compounds in free form or an acceptable salt form as potential antiviral agents against SARS-Cov2. The invention relates to indole-based small molecules capable of showing antiviral activity against SARS-Cov2, having improved EC50value, improved toxicity profile and DMPK thus, have better efficacy as a potential therapeutic target against SARS- Cov2 or other similar viral disease. BACKGROUND OF THE INVENTION Arbidol (ARB) is a synthetic antiviral drug, developed by the All-Russian Chemical and Pharmaceutical Research Institute. It was originally developed to combat influenza viruses and was first marketed in Russia in 1992. ARB is currently used clinically in several countries except in North America effective for the prevention of influenza A and B and other acute respiratory viruses (J. Med. Virol. DOI 10.1002 / jmv). The mechanism of action is quite different from the commonly used antiviral drugs such as ribavirin, amantadine, and rimantadine. It can prevent the influenza virus by inducing interferon and enhancing immune function. It can effectively treat influenza and other acute respiratory virus infections. It has a wider antiviral spectrum than amantadine and has antagonistic effects on influenza A and B viruses. ARB inhibits in vitro hepatitis C virus (HCV) by blocking HCV entry and replication (doi: 10.1186 / 1743-422X-3-56). It also has the function of activating macrophages as well and recent studies have shown that the drug also has a good inhibitory effect on the SARS virus at a lower safe concentration. Nowadays, domestically developed dosage forms include tablets, capsules, dispersible tablets, granules, and ordinary sustained-release tablets. Because of the short half-life of Abidol, the blood concentration of common dosage forms is unstable, and the daily administration is three to four times. The patient's compliance is poor. Although the ordinary sustained-release preparation reduces the number of daily administrations, it improves. The patient's compliance, but the effect is slow, cannot quickly exert the efficacy of the drug to produce a therapeutic effect, and clinically due to the problem of drug resistance, antibacterial antiviral drugs are not advocated to develop a general-purpose sustained-release preparation. However, the main disadvantage of Arbidol is its high cellular toxicity (CC50= 10-20 mM) with low selectivity index (SI50) (US2011160197A1). The present invention provides Indole-based small molecule essentially having nitrogen substituents at specific positions and acts as better antivirals against SARS-COV-2 as compared to Arbidol derivatives showing improved EC50value, improved toxicity profile and DMPK profiles than the Arbidol molecule, thus, have better efficacy as a potential therapeutic target against SARS-Cov2 or other similar viral disease. OBJECTIVES OF THE INVENTION The main objective of the present invention is to provide Indole-based small molecules having antiviral property against SARS-COV-2 in free and acceptable salt form. Another objective of the present invention is to provide a process for the design and synthesis of such compounds. Another objective is to identify the role of C-4 amine substituents and switch the nitrogen-containing substituents from C-4 to C-6 (R5) and / or C-3 (R3) and C-5 (R4) positions in the compound. Yet another objective of the present invention is to study the toxicity, metabolic stability, and ADME profile of the compounds. PT / 2025 / 10975 Still, another objective of the present invention is to synthesize different compounds with a basic amine group containing pro-drug derivatives. Yet another objective of the present invention is to establish a structure-activity relationship (SAR) against SARS-CoV2. Still, another objective of the present invention is to provide a composition comprising compounds use in several clinical applications, including pharmaceutical agents and methods for treating other viral disease conditions like Covid-19. SUMMARY OF THE INVENTION Accordingly, the present invention provides a compound of formula I, salts and metabolite thereof, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO, napthyl and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is selected from the group consisting of ethyl ester, tertbutyl amide, N-(1-methylpiperidin-4-yl) amide, N-(1-isopropylpiperidin-4-yl) amide, N-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-(1- isopropyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-((dimethylamino)methyl) amide, N- ((dimethylamino)ethyl) amide, N-((dimethylamino)propyl) amide, N-((methylamino)ethyl) amide, N- (1-methylpyrrolidin-3-yl)amide, N-(2-(piperidin-1-yl)ethyl)amide; R4 is selected from the group consisting of OH, OR’4, and OCOR’4, wherein R’4 is substituted or unsubstituted 5 to 6 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle; R5 is Br or a substituted or unsubstituted aminoalkyl or a 5 to 6 membered N containing heterocycle, wherein the substituents are selected from the group consisting of alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino; wherein at least one of R3, R4 or R5 is a nitrogen containing substituent. In a preferred embodiment, R4 in the compound of formula I is selected from the group consisting of: In a preferred embodiment, R5in the compound of formula I is selected from the group consisting of: PT / 2025 / 10975 In a preferred embodiment, the compound of formula I is selected from the group consisting of: ethyl 6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indole-3- carboxylate (26). ethyl 6-bromo-2-(((4-fluorophenyl)thio) methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H- indole-3-carboxylate (28a). ethyl 6-bromo-2-(((4-fluoro-2-methylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (29a). ethyl 6-bromo-5-hydroxy-2-((mesitylthio) methyl)-1-(naphthalen-1-ylmethyl)-1H-indole-3- carboxylate (30a). ethyl 6-bromo-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)- 1H-indole-3-carboxylate (31). ethyl 6-bromo-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)- 1H-indole-3-carboxylate hydrochloride (31a). ethyl 1-benzyl-6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-2-((phenyl thio)methyl)-1H-indole-3-carboxylate (37) ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-2-((phenylthio)methyl)-1H-indole- 3-carboxylate (40) ethyl6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)meth yl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate (42) ethyl 5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H- indole-3-carboxylate (45) ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate (48) ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(piperidin-4-yl)-1H-indole-3- carboxylate hydrochloride (48a) PT / 2025 / 10975 ethyl 5-hydroxy-1-methyl-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (49) ethyl 5-hydroxy-1-methyl-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3- carboxylate hydrochloride (49a) ethyl 2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (50) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate (51) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate hydrochloride (51a) ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate (52) ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate hydrochloride (52a) ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((mesitylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate (53) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate (54) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (54a) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahydro pyridin-4-yl)-1H-indole-3-carboxylate (55) ethyl 5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate (56) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahy dropyridin-4-yl)-1H-indole-3-carboxylate (57) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahy dropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (57a) ethyl 5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate (58) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate (59) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (59a) ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1-methyl-1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate (60) PT / 2025 / 10975 ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1- methyl-1H-indole-3-carboxylate (61) ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1- methyl-1H-indole-3-carboxylate hydrochloride (61a) ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxylate (62) ethyl 5-hydroxy-1-methyl-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-2-phenylthio)methyl)-1H- indole-3-carboxylate (63) ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-methyl-2-((phenylthio) methyl)-1H- indole-3-carboxylate (64) ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-methyl-2-((phenylthio) methyl)-1H- indole-3-carboxylate hydrochloride (64a) ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate (65) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridine-4-yl)-1-methyl-1H-indole-3-carboxylate (66) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridine-4-yl)-1-methyl-1H-indole-3-carboxylate hydrochloride (66a) ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((phenylthio) methyl)-1H-indole-3-carboxylate (67) ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((phenylthio) methyl)-1H-indole-3-carboxylate hydrochloride (67a) ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio) methyl)-1H-indole-3-carboxylate (68) ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio) methyl)-1H-indole-3-carboxylate hydrochloride (68a) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl- 1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3-carboxylate (69) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl- 1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (69a) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)- 1-(4-methylbenzyl)-1H-indole-3-carboxylate (70) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)- 1-(4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (70a) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1- (4-methylbenzyl)-1H-indole-3-carboxylate (71) PT / 2025 / 10975 ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1- (4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (71a) ethyl 6-(1-cyclohexyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate (72) ethyl 6-(1-cyclohexyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (72a) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1- (4-methylbenzyl)-1H-indole-3-carboxylate (73) ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxylate (74) ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxylate hydrochloride (74a) ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxylate (75) ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)- 1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate (76) ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyri din- 4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate (77) 6-bromo-N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide (85) 6-bromo-N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide (86) 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indole-3- carboxamide (87) 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(naphthalen-1-ylmethyl)-1H-indole-3- carboxamide (88) 6-bromo-N-(tert-butyl)-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)- 1H-indole-3-carboxamide (89) N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydro pyridin- 4-yl) -1H-indole-3-carboxamide (92) N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydro Pyridin-4-yl)-1H-indole-3-carboxamide (93) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio) methyl)- 5-hydroxy-1-methyl-1H-indole-3-carboxamide (94) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxamide (95) PT / 2025 / 10975 N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxamide hydrochloride (95a) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide (96) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide hydrochloride (96a) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide (97) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide hydrochloride (97a) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone (98) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H-indole-3- carboxamide (99) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H-indole-3- carboxamide hydrochloride (99a) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide (100) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide hydrochloride (100a) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone(101) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone hydrochloride (101a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide (102) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide hydrochloride (102a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone (103) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone hydrochloride (103a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-N-(1H-pyrazol-3- yl)-1H-indole-3-carboxamide (104) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide (105) PT / 2025 / 10975 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3-yl)(4- morpholinopiperidin-1-yl)methanone (106) (R)-(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(2- (hydroxymethyl)piperazin-1-yl)methanone (107) 6-bromo-5-hydroxy-N-(1-methylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl) - 1H-indole-3-carboxamide (108) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio)meth yl)-1H-indole-3-carboxamide (109) (6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indol-3-yl)(4-isopro pylpiperazin-1-yl)methanone(110) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide (111) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide hydrochloride (111a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1H-pyrazol-3-yl)-1H-indole-3- carboxamide (112) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H- indole-3-carboxamide (113) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H- indole-3-carboxamide hydrochloride (113a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-1H- indole-3-carboxamide (114) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-1H- indole-3-carboxamide hydrochloride (114a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-isopropylpipera zin-1-yl)methanone(115) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)-1H- indole-3-carboxamide (116) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-morpholinopipe ridin-1-yl)methanone(117) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-2-((phenylthio)methyl)-1H-indole-3- carboxamide (118) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-2-((phenylthio)methyl)-1H-indole-3- carboxamide hydrochloride (118a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-isopropylpipera zin-1-yl)methanone(119) PT / 2025 / 10975 (6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indol-3-yl)(4-morpholinopiperidin-1- yl)methanone (120) (6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indol-3-yl)(4-morpholinopiperidin-1-yl) methanone dihydrochloride (120a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)-1H- indole-3-carboxamide (121) 6-bromo-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxamide (122) N-(1-benzylpiperidin-4-yl)-6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide (123) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(piperidin-4-yl)-1H-indole-3- carboxamide (124) (4-aminopiperidin-1-yl)(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3- yl)methanone (125) 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide(126) 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide hydrochloride (126a) ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-(pyrrolidin-3-yloxy)-1H-indole-3- carboxylate (127) ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-((1-isopropylpyrrolidin-3-yl)oxy)-1-methyl-1H- indole-3-carboxylate (128) ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3-yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1-methyl-1H- indole-3-carboxylate (129) ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3-yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1-methyl-1H- indole-3-carboxylate hydrochloride (129a) ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-((1-methylpyrrolidin-3-yl)oxy)-1H- indole-3-carboxylate (130) and 3-((6-bromo-3-(ethoxycarbonyl)-2-(((4-fluorophenyl)thio)methyl)-1-methyl-1H-indol-5-yl)oxy)-1, 1- dimethylpyrrolidin-1-ium iodide (135). In an aspect of the present invention the salt of the compound of formula I, is a hydrochloride or quaternary ammonium salt having inhibitory activity against SARS CoV-2. In an embodiment, the present invention provides a process for the preparation of the compound of formula I, comprising: a) treating 1, 4 Benzoquinone (A) with ethyl (Z)-3-aminobut-2-enoate (B) to produce a substituted indole C; PT / 2025 / 10975 b) dissolving the substituted indole C and pyridine in dry DCM and acetic anhydride under a nitrogen atmosphere to produce D; c) treating D with alkyl or 4-substituted benzyl bromide to produce intermediate E, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; d) heating the intermediate E in CCl4 in the presence of a bromination reagent to produce F, wherein R1 is as defined above; e) adding F to the reaction mixture of benzothiol or substituted benzothiol in presence of a solvent system to produce ester intermediate G, wherein the substituent Y is selected from the group consisting of H, alkyl, alkoxy, haloalkyl, haloalkoxy and halo; and R1is as defined above; f) to the intermediate G adding aqueous solution of K3PO4and boronic ester tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1-methyl-4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2 and Xantphos and extracting with ethyl acetate to obtain the protected compound H followed by deprotecting H by stirring in DCM and HCl in 1,4-Dioxane to produce amine compound I and treating I with R’2- X’, wherein R’2 is alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino and X’ is a halo to obtain J, wherein J is the compound of formula I, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO. napthyl and Ph; R2is PT / 2025 / 10975 thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3is ethyl ester, R4is OH and R5is 3, 4 unsaturated piperidine optionally substituted with alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl or morpholino; g) alternatively treating the ester intermediate G, in a 3:1 EtOH and water solution in a nitrogen atmosphere with NaOH to produce the acid intermediate K; heating the intermediate K in DMF with tert butyl amine, HATU, and DIPEA to produce L wherein R3 is tert butyl amine R1 and Y are as define above, followed by adding aqueous solution of K3PO4and compound L, boronic ester tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1-methyl-4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2and Xantphos and extracting with ethyl acetate to obtain the protected compound M followed by deprotecting M by stirring in DCM and HCl in 1,4-Dioxane to produce N and treating N with R’2- X’, wherein R’2 is alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino and X’ is a halo to obtain O, wherein N and O are the compound of formula I, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is a tert butyl amine , R4 is OH and R5 is 3, 4 unsaturated piperidine optionally substituted with alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl or morpholino; h. alternatively treating the acid intermediate K in DMF with an amine selected from 1- benzylpiperidin-4-amine or 1-benzylpiperidin-4-amine or piperidin-4-amine or tert butyl amine or 1- PT / 2025 / 10975 isopropyl piperazine and 4-(piperidin-4-yl) morpholin or 1-methyl-1H-pyrazol-4-amine, in presence of HATU, and DIPEA to produce P, wherein P is the compound of formula I, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is selected from N-(1- methylpiperidin-4-yl) amide, N-(1-isopropylpiperidin-4-yl) amide, N-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl) amide, N-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N- ((dimethylamino)methyl) amide, N-((dimethylamino)ethyl) amide, N-((dimethylamino)propyl) amide, N-((methylamino)ethyl) amide, N-(1-methylpyrrolidin-3-yl)amide and N-(2-(piperidin-1- yl)ethyl)amide, , R4is OH and R5is Br; i. alternatively treating the ester intermediate G with a Br-R4, wherein R4is substituted or unsubstituted 5 to 6 membered N containing heterocycle; OR’4, and OCOR’4, wherein R’4is substituted or unsubstituted 5 to 6 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle to produce S, wherein S is the compound of formula I, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO, napthyl and Ph; R2 is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3is ethyl ester, R4is as defined above; and R5 is Br. In a embodiment in i ester intermediate G is treated with Br-R4, wherein R4 is a substituted or unsubstituted 5 to 7 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle, Cs2CO3 in DMF to produce Q and treating Q is with an R’4-X’ wherein R’4 is a alkyl or cycloalkyl group and X’ is a halo to obtain R. In a preferred embodiment the bromination agent in step d in Bromine. In an embodiment of the present invention the solvent system in step e comprises of KOH in hexane and MeOH. The present invention provides a pharmaceutical composition comprising the compound of formula I and pharmaceutically acceptable excipient. PT / 2025 / 10975 BRIEF DESCRIPTION OF THE DRAWING The objects and features of the present invention will become apparent from the following description of the invention when taken in conjunction with the accompanying drawings. The objects and features of the present invention will become apparent from the following description of the invention when taken in conjunction with the accompanying drawings. Fig.1 describes hERG binding assay and dose-response curve of representative antiviral compounds. Fig.2 describes Cell-based ELISA EC50and EC90curve for compounds 31 and 97. The assay was done in SARS-CoV-2 infected VERO E6 cells. Fig.3 describes Cell-based ELISA EC50and EC90curve: for compounds 43, 56, 55 and 57. The assay was done SARS-CoV-2 infected VERO E6 cells. Fig.4 describes the Cytotoxicity data of the Antiviral compounds. The assay was done in VERO E6 cells. Abbreviations DMF N,N-dimethylformamide TEA Triethylamine DIPEA N,N-Diisopropylethylamine MeOH Methanol CHCl3 Chloroform DCM Dichloromethane Cs2CO3 Cesium carbonate THF Tetrahydrofuran Ar Argon HATU Hexafluorophosphate Azabenzotriazole Tetramethyl Uronium NaBH(OAc)3Sodium triacetoxyborohydride NaBH4 Sodium borohydride NaH Sodium hydride KOH Potassium hydroxide CCl4 Carbon tetrachloride AcOH Acetic Acid Br2Bromine CAN Ceric Ammonium Nitrate DMAP 4-Dimethylaminopyridine K2CO3 Potassium carbonate DETAILED DESCRIPTION OF THE INVENTION Several structural modification strategies have been applied to improve the physicochemical properties of patent Arbidol drug. Arbidol has six different substitutions in the indole scaffold, which is a unique feature among all the drug molecules. These unique features create more attraction for medicinal chemistry-based optimization. The central core of the Arbidol is an indole scaffold that consists of six different groups at the N1, C2, C3, C4, C5, and C6 positions. It has one flexible substitution methyl (phenyl) sulfane group at the C2position, methyl group at the N1position, ethyl carboxylate group at the C3 position, basic amine N, N dimethyl methyl amine group at C4 position, hydroxyl group at C5 position, and a bromo substitution at C6 position. The indole core of Arbidol presents enormous PT / 2025 / 10975 opportunities for the development of novel antivirals. For example, basic nitrogen-containing groups such as a piperidine ring are substituted at its C-6 position. Initially, the reported metabolite profiling of Arbidol in human plasma, urine, and faces was investigated (doi.org / 10.1128 / aac.02282-12). Themajor Phase I metabolism reaction involves, a) Sulfoxidation b) N-demethylation at C4,and c)hydroxylation at the para position of the benzothiol group. The ester group at C-3 is also susceptible to hydrolysis in plasma. The proposed strategy of optimization was initiated keeping in mind the stability profile of Arbidol. In the very first strategy, the importance of the basic amine group at the C4 position was checked and subsequently, if repositioning the basic amine moiety to another position on the indole ring for better inhibitory potency against the SARS-CoV-2 virus was checked. Our next strategy was to modulate the benzothiol group at the C2position to deter the sulfoxidation reaction. The Third objective was to check the chemical space available at N1position of the indole scaffold by incorporating bulky hydrophobic group and their relationship with inhibitory activity against SARS-CoV-2. Our fourth strategy is to investigate the significance of the -Br group and identify if the basic amine group can be repositioned at C6. The hydrophobic Br group can be used as a handle to substitute various groups. Our fifth objective is basic amine-containing amine substitution instead of metabolically less stable ester group and the sixth objective is the importance of the basic amine group at C3position. We aimed to improve the antiviral activity, associated toxicity, and stability. Starting from Arbidol, sequentially probing the significance of different substituents to improve the efficacy of the Arbidol derivatives was aimed. The present disclosure represents the benchmarking of these antiviral inhibitors of Arbidol derivatives containing nitrogen substituents either at R5 and / or R3 and / or R4 positions instead of C4 position for improved EC50value, improved toxicity profile and DMPK profiles than the parent Arbidol molecule, thus, have better efficacy as a potential therapeutic target against SARS-Cov2 or other similar viral disease. Further, the role of nitrogen-containing substituents at C-6 (R5) and / or C-3 (R3) and / or C-5 (R4) positions were studied in correlation with different substituents at N-1 (R1) and C-2 (R2) positions. the present invention provides a compound of formula I, salts and metabolite thereof, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is selected from the group consisting of ethyl ester, tertbutyl amide, N-(1-methylpiperidin-4-yl) amide, N-(1-isopropylpiperidin-4-yl) amide, N-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-(1- isopropyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-((dimethylamino)methyl) amide, N- ((dimethylamino)ethyl) amide, N-((dimethylamino)propyl) amide, N-((methylamino)ethyl) amide, N- (1-methylpyrrolidin-3-yl)amide, N-(2-(piperidin-1-yl)ethyl)amide; R4 is selected from the group consisting of OH, OR’4, and OCOR’4, wherein R’4 is substituted or unsubstituted 5 to 6 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle; R5 is Br or a substituted or unsubstituted aminoalkyl or a 5 to 6 membered N containing heterocycle, wherein the substituents are selected from the group consisting of alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino; PT / 2025 / 10975 wherein at least one of R3, R4 or R5 is a nitrogen containing substituent. In another embodiment of the present invention provides a process for the preparation of compounds having Formula I, wherein the process comprises the steps of: a) treating 1, 4 Benzoquinone (A) with ethyl (Z)-3-aminobut-2-enoate to produce a substituted indole C. b) dissolving the substituted indole C and pyridine in dry DCM and Acetic anhydride under a nitrogen atmosphere to produce D; c) treating D with alkyl or 4-substituted benzyl bromide to produce intermediate E, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; d) heating the intermediate E in CCl4in the presence of a bromination reagent such as bromine to produce F and R1 is as defined above. e) adding F to the reaction mixture of benzothiol or substituted benzothiol and KOH in hexane and MeOH to produce G, wherein Y is selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; and R1is as defined above; PT / 2025 / 10975 f) adding aqueous solution of K3PO4 and boronic ester tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1-methyl-4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2 and Xantphos and extracting with ethyl acetate to obtain the protected compound H followed by deprotecting H by stirring in DCM and HCl in 1,4-Dioxane to produce I and treating I with an alkyl or cycloalkyl iodide or bromide to obtain J, wherein J is the compound of formula I, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO napthyl and Ph; R2 is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3is ethyl ester, R4is OH and R5is 3, 4 unsaturated piperidine wherein R’2 is alkyl or cycloalkyl substituent (scheme 1) g) heating the intermediate G in a 3:1 EtOH & water solution in a nitrogen atmosphere with NaOH to produce compound K. h) heating the intermediate Kin DMF with suitable tert butyl amine, HATU, and DIPEA to produce L and R1, Y already define above. i) adding aqueous solution of K3PO4 and compound L, boronic ester tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1-methyl-4- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2and Xantphos and extracting with ethyl acetate to obtain the protected compound M followed by deprotecting M by stirring in DCM and HCl in 1,4-Dioxane to produce N and treating N with an alkyl or cycloalkyl iodide or bromide to obtain O, wherein N is the compound of formula I, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, PT / 2025 / 10975 haloalkoxy and halo; R3 is ethyl ester, R4 is OH and R5 is 3, 4 unsaturated piperidine wherein R”2is alkyl or cycloalkyl substituent (scheme 2); j) heating the intermediate Kin DMF with suitable amine like 1-benzylpiperidin-4-amine or 1- benzylpiperidin-4-amine or piperidin-4-amine or tert butyl amine or 1-isopropyl piperazine or 4-(piperidin-4-yl) morpholin or 1-methyl-1H-pyrazol-4-amine, HATU, and DIPEA to produce P. Wherein R1, Y already define above and R’3 are N-(1-methylpiperidin-4-yl), N-(1- isopropylpiperidin-4-yl), N-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl), N-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl), N-((dimethylamino)methyl), N-((dimethylamino)ethyl), N- ((dimethylamino)propyl), N-((methylamino)ethyl), N-(1-methylpyrrolidin-3-yl), N-(2- (piperidin-1-yl)ethyl). k) heating the intermediate G with tert-butyl 3-bromopyrrolidine-1-carboxylate, Cs2CO3 in DMF to produce Boc protected compound. After deprotecting Boc protected compound by stirring in DCM and HCl in 1,4-Dioxane to produce Q and treating Q with an alkyl or cycloalkyl iodide or bromide to obtain R. l) adding intermediate G to the reaction mixture of dimethyl amine, 37 % Formaldehyde in AcOH at 0 ºC to produce compound S. Treating of triphosgene in DCM with 4-(piperidin-4- yl)morpholine or 1,4'-bipiperidine or (3S,5R)-3,5-dimethylpiperidine and K2CO3to produce corresponding amine carbonyl chloride. m) dissolving compound Q in DMF and cold to 0oC then NaH, excess MeI to produce compound U (scheme 3). PT / 2025 / 10975 n) treating Compound V with 4 (N) HCl in dioxane at rt to produce compound W. Table 1: Structure of the compounds synthesized Compound Compound code Number Structure IUPAC Name Ethyl 1-benzyl-6-(1-(tert-butoxycarbonyl)- TIH-02-86 37 1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-2- ((phenylthio)methyl)-1H-indole-3- carboxylate (37) Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetra TIH-02-87 42 hydropyridin-4-yl)-2-(((2,4-dimethyl phenyl) thio)methyl)-5-hydroxy-1-(4-methylbenzyl)- 1H-indole-3-carboxylate (42) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-02-88 55 5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (55) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-02-89 71 5-hydroxy-6-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate (71) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-02-90 70 5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate (70) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-4-30 70a 5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate hydrochloride (70a) Ethyl 2-(((4-fluoro-2- TIH-02-119 57 methylphenyl)thio)methyl)-5-hydroxy-1-(4- methylbenzyl)-6-(1,2,3,6-tetrahydropyridin- 4-yl)-1H-indole-3-carboxylate (57) Ethyl 2-(((4-fluoro-2- methylphenyl)thio)methyl)-5-hydroxy-6-(1- TIH-02-127 25 isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1- (4-methylbenzyl)-1H-indole-3-carboxylate (25) PT / 2025 / 10975 Ethyl 5-hydroxy-2-((mesitylthio)methyl)-1- TIH-02-105 56 (4-methylbenzyl)-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (56) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6- TIH-02-106 74 tetrahydropyridin-4-yl)-2-((mesitylthio) methyl) -1-(4-methylbenzyl)-1H-indole-3- carboxylate (74) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6- TIH-4-31 74a tetrahydropyridin-4-yl)-2-((mesitylthio) methyl) -1-(4-methylbenzyl)-1H-indole-3- carboxylate hydrochloride (74a) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2- TIH-02-98 52 ((phenylthio)methyl)-6-(1,2,3,6- tetrahydropyri din-4-yl)-1H-indole-3- carboxylate (52) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1- TIH-02-104 67 isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((phenylthio)methyl)-1H-indole-3- carboxylate (67) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2- TIH-02-99 53 ((mesitylthio)methyl)-6-(1,2,3,6-tetrahydro Pyridin-4-yl)-1H-indole-3-carboxylate (53) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1- TIH-02-103 68 isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((mesitylthio)methyl)-1H-indole-3- carboxylate (68) Ethyl 2-(((4-fluoro-2-methylphenyl)thio) TIH-02-122 54 methyl)-1-(4-fluorobenzyl)-5-hydroxy-6- (1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (54) Ethyl 2-(((4-fluoro-2-methylphenyl)thio) TIH-02-124 69 methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1- isopropyl-1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (69) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1- TIH-02-190 40 methyl -1H-pyrazol-4-yl)-2-((phenylthio) methyl)-1H-indole-3-carboxylate (40) Ethyl 5-hydroxy-1-methyl-2-((phenylthio) TIH-02-126 49 methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (49) PT / 2025 / 10975 Ethyl 5-hydroxy-1-methyl-6-(1-methyl- TIH-02-132 63 1,2,3,6-tetrahydropyridin-4-yl)-2- ((phenylthio)methyl)-1H-indole-3- carboxylate (63) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6- TIH-02-133 64 tetrahydropyridin-4-yl)-1-methyl-2- ((phenylthio)methyl)-1H-indole-3- carboxylate (64) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-100 48 hydroxy-1-methyl-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (48) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-149 60 hydroxy-1-methyl-6-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (60) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-102 61 hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-methyl-1H-indole- 3-carboxylate (61) Ethyl 2-(((4-fluoro-2- IH-02-118 51 methylphenyl)thio)methyl)-5-hydroxy-1- methyl-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (51) Ethyl 2-(((4-fluoro-2-methylphenyl) thio) TIH-02-128 66 methyl) -5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-methyl-1H-indole- 3-carboxylate (66) Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydro TIH-02-158 62 pyridin-4-yl)-2-(((4- fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxylate (62) Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydro TIH-4-32 62a pyridin-4-yl)-2-(((4- fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxylate (62a) Ethyl 2-(((2,4-difluorophenyl)thio)methyl)-5- TIH-02-155 50 hydroxy-1-methyl-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (50) Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydro TIH-02-156 65 pyridin-4-yl)-2-(((2,4-difluorophenyl) thio) methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxylate (65) 6-bromo-N-(tert-butyl)-2-(((4-fluorophenyl) TIH-02-138 86 thio)methyl)-5-hydroxy-1-methyl-1H-indole- 3-carboxamide (86) PT / 2025 / 10975 (6-bromo-2-(((4-fluorophenyl)thio)methyl)- TIH-2-185 86a 5-hydroxy-1-methyl-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone (86a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-139 111 hydroxy-1-methyl-N-(1-methylpiperidin-4- yl)-1H-indole-3-carboxamide (111) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-140 114 hydroxy-N-(1-isopropylpiperidin-4-yl)-1- methyl-1H-indole-3-carboxamide (114) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-4-33 114a hydroxy-N-(1-isopropylpiperidin-4-yl)-1- methyl-1H-indole-3-carboxamide hydrochloride(114a) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4- TIH-02-141 113 fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxamide (113) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4- TIH-4-34 113a fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxamide (113a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-193 112 hydroxy-1-methyl-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide (112) Ethyl 6-bromo-2-(((4-fluorophenyl) thio) TIH-02-175 127 methyl)-1-methyl-5-(pyrrolidin-3-yloxy)-1H- indole-3-carboxylate (127) 3-((6-bromo-3-(ethoxycarbonyl)-2-(((4- TIH-02-176 135 fluorophenyl)thio)methyl)-1-methyl-1H- indol-5-yl)oxy)-1,1-dimethylpyrrolidin-1- ium iodide (135) Ethyl 6-bromo-2-(((4-fluorophenyl) thio) TIH-02-177 128 methyl)-5-((1-isopropylpyrrolidin-3-yl)oxy)- 1-methyl-1H-indole-3-carboxylate (128) PT / 2025 / 10975 Ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3- TIH-02-178 129 yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1- methyl-1H-indole-3-carboxylate (129) N-(tert-butyl)-2-(((4- TIH-02-163 93 fluorophenyl)thio)methyl)-5-hydroxy-1- methyl-6-(1,2,3,6-tetrahydro pyridin-4-yl)- 1H-indole-3-carboxamide (93) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6- TIH-02-164 95 tetrahydropyridin-4-yl)-2-(((4-fluorophenyl) thio)methyl)-5-hydroxy-1-methyl-1H-indole- 3-carboxamide (95) N-(tert-butyl)-2-(((2,4-difluorophenyl) TIH-02-154 92 thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3- carboxamide (92) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6- TIH-02-167 94 tetrahydropyridin-4-yl)-2-(((2,4- difluorophenyl) thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxamide (94) Ethyl 6-bromo-2-(((4-fluorophenyl) thio) TIH-02-179 130 methyl)-1-methyl-5-((1-methylpyrrolidin-3- yl)oxy)-1H-indole-3-carboxylate (130) 6-bromo-N-(tert-butyl)-5-hydroxy-2- TIH-02-134 87 ((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indole-3-carboxamide (87) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-02-135 96 1-(4-methylbenzyl)-N-(1-methylpiperidin-4- yl)-1H-indole-3-carboxamide (96) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-4-35 96a 1-(4-methylbenzyl)-N-(1-methylpiperidin-4- yl)-1H-indole-3-carboxamide hydrochloride (96a) PT / 2025 / 10975 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-02-136 97 4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxamide (97) N-(1-benzylpiperidin-4-yl)-6-bromo-5- TIH-02-117 123 hydroxy-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxamide (123) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-02-192 99 1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide (99) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-4-36 99a 1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide hydrochloride (99a) Ethyl 6-bromo-5-hydroxy-1-(naphthalen- TIH-02-180 26 1-ylmethyl)-2-((phenylthio)methyl)-1H- indole-3-carboxylate (26) Ethyl 6-bromo-2-(((2,4-dimethylphenyl) TIH -1-202 31 thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (31) Ethyl 6-bromo-2-(((2,4-dimethylphenyl) TIH-3-36 31a thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate hydrochloride (31a) Ethyl 6-bromo-2-(((4-fluorophenyl)thio) TIH-3-43 28a methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (28a). PT / 2025 / 10975 Ethyl 6-bromo-2-(((4-fluoro-2- TIH-3-44 29b methylphenyl) thio)methyl)-5-hydroxy-1- (naphthalen-1-ylmethyl)-1H-indole-3- carboxylate (29a). Ethyl 6-bromo-5-hydroxy-2- IH-03-35 30a ((mesitylthio) methyl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (30a). (6-bromo-2-(((4-fluorophenyl)thio)methyl)- TIH-02-184 103 5-hydroxy-1-(naphthalen-1-ylmethyl)-1H- indol-3-yl)(4-isopropylpiperazin-1- yl)methanone (103) (6-bromo-2-(((4-fluorophenyl)thio)methyl)- TIH-4-38 103a 5-hydroxy-1-(naphthalen-1-ylmethyl)-1H- indol-3-yl)(4-isopropylpiperazin-1- yl)methanone hydrochloride (103a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-02-183 102 hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3- carboxamide (102) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-4-39 102a hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3- carboxamide hydrochloride (102a) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-03-01 97a 4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxamide hydrochloride (97a) (6-bromo-5-hydroxy-2- TIH-02-200 101 ((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indol-3-yl)(4-morpholino piperidin-1- yl)methanone (101) PT / 2025 / 10975 (6-bromo-5-hydroxy-2- TIH-4-39 101a ((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indol-3-yl)(4-morpholino piperidin-1- yl)methanone hydrochloride (101a) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-02-199 100 N-(1-methyl-1H-pyrazol-4-yl)-1-(4- methylbenzyl) -1H-indole-3-carboxamide (100) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-4-40 100a N-(1-methyl-1H-pyrazol-4-yl)-1-(4- methylbenzyl) -1H-indole-3-carboxamide hydrochloride (100a) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-02-196 118 4-yl)-1-methyl-2-((phenylthio)methyl)-1H- indole-3-carboxamide (118) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-4-41 118a 4-yl)-1-methyl-2-((phenylthio)methyl)-1H- indole-3-carboxamide hydrochloride (118a) (6-bromo-5-hydroxy-1-methyl-2- TIH-02-195 119 ((phenylthio)methyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone (119) 6-bromo-5-hydroxy-1-methyl-N-(1-methyl- TIH-02-197 121 1H-pyrazol-4-yl)-2-((phenylthio)methyl)-1H- indole-3-carboxamide (121) PT / 2025 / 10975 (6-bromo-5-hydroxy-1-methyl-2- TIH-02-198 120 ((phenylthio)methyl)-1H-indol-3-yl)(4- morpholinopiperidin-1-yl)methanone (120) (6-bromo-5-hydroxy-1-methyl-2- TIH-3-72 120a ((phenylthio)methyl)-1H-indol-3-yl)(4- morpholinopiperidin-1-yl)methanone dihydrochloride (120a) 6-bromo-N-(tert-butyl)-2-(((2,4- TIH-02-151 85 difluorophenyl)thio)methyl)-5-hydroxy-1- methyl-1H-indole-3-carboxamide (85) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-02-164 73 5-hydroxy-6-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate (73) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-4-42 73a 5-hydroxy-6-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate hydrochloride (73a) (6-bromo-5-hydroxy-2- TIH-4-43 98 ((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indol-3-yl)(4-isopropylpiperazin-1- yl)methanone (98) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-(naphthalen-1-ylmethyl)-N-(1H- pyrazol-3-yl)-1H-indole-3-carboxamide (104) TIH-4-44 104 PT / 2025 / 10975 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3- carboxamide (105) TIH-4-45 105 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-(naphthalen-1-ylmethyl)-1H- indol-3-yl)(4-morpholinopiperidin-1- TIH-4-46 106 yl)methanone (106) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2- ((mesityl thio)methyl)-6-(1,2,3,6- tetrahydropyri din-4-yl)-1H-indole-3- TIH-4-47 144 carboxylate (144) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1- isopro pyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((mesityl thio)methyl)-1H-indole-3- TIH-4-48 145 carboxylate (145) Ethyl 5-hydroxy-1-(naphthalen-1-ylmethyl)- 2-((phenylthio)methyl)-6-(1,2,3,6- tetrahydropyri din-4-yl)-1H-indole-3- TIH-4-55 58 carboxylate (58) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetra hydropyridin-4-yl)-1-(naphthalen-1- TIH-4-51 75 ylmethyl)-2-((phenylthio)methyl)-1H-indole- 3-carboxylate (75) 6-bromo-N-(tert-butyl)-5-hydroxy-2- ((mesitylthio)methyl)-1-(naphthalen-1- TIH-4-50 88 ylmethyl)-1H-indole-3-carboxamide (88) PT / 2025 / 10975 6-bromo-5-hydroxy-N-(1-methylpiperidin-4- yl)-1-(naphthalen-1-ylmethyl)-2- TIH-4-49 108 ((phenylthio) methyl)-1H-indole-3- carboxamide (108) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- 4-yl)-1-(naphthalen-1-ylmethyl)-2- TIH-4-52 109 ((phenylthio) methyl)-1H-indole-3- carboxamide (109) (6-bromo-5-hydroxy-1-(naphthalen-1- ylmethyl) -2-((phenylthio)methyl)-1H-indol- TIH-4-53 110 3-yl)(4-isopro pylpiperazin-1-yl)methanone (110) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-4-54 115 hydroxy-1-methyl-1H-indol-3-yl)(4-isopropyl piperazin-1-yl)methanone (115) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-N-(1-methyl-1H-pyrazol- TIH-4-65 116 4-yl)-1H-indole-3-carboxamide (116) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5- TIH-4-60 117 hydroxy-1-methyl-1H-indol-3-yl)(4- morpholino piperidin-1-yl)methanone (117) PT / 2025 / 10975 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-4-56 59 5-hydroxy-1-(naphthalen-1-ylmethyl)-6- (1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3- carboxylate (59) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)- TIH-4-61 76 5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyri din-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (76) 6-bromo-N-(tert-butyl)-2-(((2,4-dimethyl TIH-4-62 89 phenyl)thio)methyl)-5-hydroxy-1- (naphthalen-1-ylmethyl)-1H-indole-3- carboxamide (89) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)- TIH-4-59 124 1-(4-methylbenzyl)-N-(piperidin-4-yl)-1H- indole-3-carboxamide (124 (4-aminopiperidin-1-yl)(6-bromo-5-hydroxy- TIH-4-58 125 2-((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indol-3-yl)methanone (125) Ethyl 2-(((4-fluoro-2-methylphenyl) thio) TIH-4-57 77 methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6- tetra hydro pyridin-4-yl)-1-(4-methylbenzyl)- 1H-indole-3-carboxylate (77) 6-bromo-2-(((2,4- TIH-03-12 126 dimethylphenyl)thio)methyl)-5-hydroxy-N- (1-isopropylpiperidin-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide (126) PT / 2025 / 10975 6-bromo-2-(((2,4- dimethylphenyl)thio)methyl)-5-hydroxy-N- TIH-4-63 126a (1-isopropylpiperidin-4-yl)-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide hydrochloride (126a) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-03-21 109 4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio) methyl)-1H-indole-3- carboxamide (109) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin- TIH-4-64 109a 4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio) methyl)-1H-indole-3- carboxamide hydrochloride (109a) Provided below are the schemes for preparing the compounds disclosed in the present application. Scheme 1aReagents and conditions: (a) Acetic acid, 20°C, ON, (b) Ac2O, Pyridine, DCM, 80°C, 2 hr, (c)MeI,NaH, 20°C, DMF, 1 hr, (d) Neat Br2, CCl4, 90°C, 3 hr, (e) Substituted benzothiol, KOH, MeOH, 5-6 hr, (f)N-Boc-1,2,3,6-Tetrahydropyridine-4-boronic acid ester, K3PO4(2.5M), Xantphos, Pd(PPh3)2Cl2,1,4 Dioxane : H2O (3:1), (g) 4 (N) HCl in Dioxane, DCM, rt, 4 hr, (h) R-X, TEA, DMF, rt or 100°C. PT / 2025 / 10975 Scheme 2aReagents and conditions: (i) NaOH, EtOH, H2O 100°C, ON, (j) tert-butyl amine, HATU, TEA,DMF, rt to 80°C, 4 hr, (k) N-Boc-1,2,3,6-Tetrahydropyridine-4-boronic acid ester, K3PO4(2.5M),Xantphos, Pd(PPh3)2Cl2,1,4 Dioxane : H2O (3:1), (l) 4 (N) HCl in Dioxane, DCM, rt, 4 hr, (m) R-X, TEA, DMF, rt or 100°C. Scheme 3 PT / 2025 / 10975aReagents and conditions: (n) NaOH, EtOH, H2O 100°C, ON, (o) Basic amine, HATU, TEA,DMF, rt to 80°C, 4 hr. (p) (i) tert-butyl 3-bromopyrrolidine-1-carboxylate, Cs2CO3, DMF, 100oC, 16 h; (ii) 4 (N) HCl in Dioxane, DCM, rt, 4 hr, (q) Alkyl halide or cyclopentyl halide, NaH, DMF, rt, 12 h, (r)Manich Reaction:CH2O + NHMe2, AcOH, 0°C to rt. 24 hr, (s) Excess MeI, NaH, DMF, rt, 12 h, (u) 4(N) HCl in Dioxane, DCM, rt, 4 hr. Still another embodiment of the present application provides compounds having Formula I in free form or an acceptable salt. Still another embodiment of the present application provides a process for the design, synthesis, and optimization of a series of compounds having Formula I. Still another embodiment of the present application provides to identify potential small molecule inhibitors having Formula I against SARS-CoV-2. Yet another embodiment of the present application provides the significance of switching the nitrogen- containing substituents from C-4 to C-6 (R5) and / or C-3 (R3) and C-5 (R4) positions. Yet another embodiment of the present application provides the improvement of Arbidol or Umifenovir toxicity, metabolic stability, and ADME profile. Still, another embodiment of the present application providesan enlargement of the selectivity index (SI50) in comparison with the parent antiviral indole-based molecule Arbidol or Umifenovir. Yet another embodiment of the present application providesto improve the hERG-related toxicity among the compounds having Formula I. Still, another embodiment of the present application providesto synthesize different compounds having the Formula I with a basic amine group containing pro-drug derivatives. Yet another embodiment of the present application provides to establisha structure-activity relationship (SAR) among compounds having Formula I against SARS-CoV-2 in both in biological assay. Still, another embodiment of the present application provides a composition comprising compounds of Formula I for use in several clinical applications, including pharmaceutical agents and methods for treating other viral disease conditions like COVID-19. BIOLOGICAL ASSAY Umifenovir / Arbidol (131) drug shows <90 % inactivation at 5 µM concentration in RT-qPCR assay and in SARS-CoV-2 infected VERO E6 cells-based assay EC50 value of <5 µM. Compounds 48, 63, 51, 17, 18, 20, 55, 71, 70, 80, 87, 97, 129 and 123 are showing >99 % inactivation at 5 µM concentration in RT-qPCR assay (table 3). Whereas 31, 48, 63, 51, 18, 20, 87, 97, 129 and 123 molecules are having their EC50 value in SARS-CoV-2 infected VERO E6 cells are 0.1 µM, 0.3 µM, 1.2 µM, 2.3 µM, 1 µM, 1.8 µM, 1.07 µM, 2 nM, 1 µM and 2.1 µM respectively (table 3). Some of our best active molecules 31, 48 and 97 shows 0.1 µM, 0.3 µM, 2 nM potency in SARS-CoV-2 infected VERO E6 cells, which is 16 to 2055-fold improvement in the potency as compared to Umifenovir / Arbidol (131). In both RT- qPCR and Cell-based assay these molecules show better potency. We not only improved the activity potency compared to Arbidol but also improved the hERG toxicity of the parent Arbidol drug. Several drugs have been withdrawn from late-stage clinical trials or even many marketed drugs due to these cardiotoxic effects, therefore it is important to identify inhibitors early in drug discovery. As a drug Arbidol is not safe for humans due to very low hERG IC50 (0.54 µM) which as a drug. We rationally designed and synthesized many potential molecules like 31, 131a, 48, 61, 62, 52, 40, 97, 99, 100, 101, 102, 103, 112, 113, 118, 120, 121, 123, 97a, 132, 133, and 134 shows their hERG IC50values are >30 µM, 0.54 µM, 0.95µM, 0.83µM, 0.89 µM, >30 µM, 3.56 µM, >30 µM, 3.85 µM, >30 µM, >30 µM, PT / 2025 / 10975 15.89 µM, 9.45 µM, 3.75 µM, >30 µM, 9.51 µM, 6.03 µM, >30 µM, 7.09 µM, 13.04 µM, >30 µM, 4.20 µM, 10.54 µM, 3.85 µM, 5.73 µM, 6.88 µM, 1.79 µM, 8.37 µM, and 3.75 µM respectively (table 10). These all molecules hERG IC50 is greater than parent Arbidol IC50 (0.54 µM). This huge hERG toxicity improvement is another inventive feature and molecules could be used as safe drugs compared to parent Arbidol. Table 2: RT-qPCR based assay data in VERO E6 cell against SARS CoV-2. Compounds ΔCt % SARS-CoV-2 ΔCt % SARS-CoV-2 SL.No No. (5µM) inactivation (5µM) (1µM) inactivation (1µM) 131 1 (Arbidol / Umifenovir) 3 <90 2 N / S 213 3.4 <90N / S N / S3 28a - > 90 - - 4 29a - 99.9 - - 5 55 15.5 >99.9 19 >99.9 6 71 14.5 >99.9 9.5 >99 7 70 14.8 >99.9 14 >99.9 8 53 14.6 >99.9 14.2 >99.9 9 48 13.5 >99.9 7.2 99 10 59 - >99 - - 11 58 - 99 - - 12 67 - 99 - - Table 3: Biological assay: Cell-based ELISA for Screening Antiviral Compound data with their EC50 and EC90 SL No. Compound No. EC50 (µM) EC90 (µM) 1 131 <5 - 2 119 >2 - 3 87 1.07 - 4 123 2.1 3.1 5 31 0.10 9.68 6 51 2.3 - 7 63 1.2 - 8 129 < 1 - 9 97 0.002 ± 0.05 0.02 ± 0.04 10135 1 - 11130 > 3 - 1240 5 - 1348 0.3 ± 0.23 1.3 ± 3.3 PT / 2025 / 10975 14control 1.02 ± 9.93 129.5 ± 2245.7 EXAMPLES The following examples are given by way of illustration and therefore should not be construed to limit the scope of the present invention. Temperatures are given in degree Celsius. The structures of final products, intermediates, and starting materials are confirmed by standard analytical methods, and spectroscopic characterization e.g., MS, and NMR. Abbreviations used are those conventional in the art. All starting materials, reagents, catalysts, building blocks, acids, bases, dehydrating agents, and solvents utilized to synthesize the compounds of the present invention are either commercially available or can be produced by known organic synthesis methods in the art. Example 1 General procedure A:Selective Acyl protection of Phenolic OH group Substituted 5 hydroxy Indole. Substituted 5 hydroxy Indole (1.0 equivalent)& pyridine (0.06 equivalent) were dissolved in dry DCM and Acetic anhydride (2.0 equivalent) was added at room temperature under a nitrogen atmosphere. Then the reaction mixture was allowed to heat at 100ºC for 2 hours. After completion of the reaction, confirmed by TLC, DCM was evaporated in a vacuum and the crude was washed with cold water followed by 1(N) HCl solution and the desired compound was extracted with Ethyl Acetate. The compound was purified in Teledyne ISCO Combiflash Rfsystem using 230-400 mesh size silica gels and 25 % Ethyl acetate in hexane solution was used as eluents and pure product was isolated with a 93- 95 % yield. General procedure B: Indole N1-Alkylation & substituted benzylation reaction. Different Substituted 5-acetoxy indole (1.0 equivalent) was dissolved in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (1.5 equivalent) was added portion-wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then appropriate alkyl or benzyl bromide or iodide (1.2 equivalent) was added very slowly at 0 ºC and the reaction mass was stirred for 45 minutes. Full consumption of both starting materials was confirmed by TLC and then the reaction mixture was quenched with cooled water. This reaction mass was diluted with Ethyl acetate and the ethyl acetate part was separated followed by several times washing with cooled water. Then the organic part was concentrated under reduced pressure and the crude was then purified by column chromatography using an Ethyl acetate / Hexane solvent system. After silica gel column purification pure product was isolated with a yield of 92-95 %. General procedure C: Dibromination reaction. Appropriate indole substitute compound (1.0 equivalent) was dissolved in CCl4 under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2 (3 equivalents) was added very carefully to the reaction mixture with the help of a dropwise in an inert atmosphere. This reaction mixture was stirred for 3 hours. TLC confirmed the consumption of starting material then solvent and excess Br2evaporated under reduced pressure. Then several times diluted with CHCl3 and evaporated under reduced pressure to get the crude product. This crude product was triturated with diethyl ether to get the solid precipitate and this solid precipitate was filtered off to get the pure dibromo product with 90-96 % yield. PT / 2025 / 10975 General procedure D: Thioalkylation reaction followed by OAc deprotection reaction. Appropriate benzothiol compound (1.03 equivalent) was dissolved in dry hexane and KOH (3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then Appropriate Dibromo compound (1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. After full consumption of both starting materials was confirmed by TLC and then the reaction mixture was quenched with cooled water. This reaction mass was diluted with cold water & ethyl acetate. Then water part was neutralized with 1 N HCl and the ethyl acetate part was separated. Then the organic part was concentrated under reduced pressure and the crude was then purified by column chromatography using an Ethyl acetate / Hexane solvent system. After silica gel column purification corresponding pure compound was isolated with a yield of 90-95 %. General procedure E: Mannich reaction. 37 % Formaldehyde solution (1.2 equivalents) was taken in AcOH a nitrogen atmosphere and cooled the solution to 0ºC. Then dimethyl amine (1.3 equivalents) was added to this reaction mixture at the same temperature & stirred reaction mixture for 4 hours at room temperature. An appropriate hydroxy compound was added to this reaction mixture and the reaction mass was stirred overnight at room temperature. TLC confirmed the consumption of the starting material then the reaction mass was diluted with water and CHCl3. Then water part was neutralized with 1 (N) HCl and the organic part was separated. Then the organic part was concentrated under reduced pressure and the crude was then purified by column chromatography using a MeOH & CHCl3solvent system. After silica gel column purification corresponding pure compound was isolated with a yield of 90-98 %. General procedure F: Suzuki reaction. To a solution of Bromo compound (1 equivalent), 2.5 M aqueous solutionof K3PO4and boronic ester (1 equivalent) was taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (0.05 equivalent) and Xantphos (0.10 equivalent) were added to this reaction mixture, and stirred this reaction mixture for 12 hours at 110ºC. After completion of the reaction, the mixture was diluted with water and extracted with ethyl acetate. The Ethyl acetate part was concentrated in rota vapor to get the crude product. This crude product was purified by using silica gel column purification to get a pure productwith 75-90 % yield. General procedure G: Boc deprotection reaction. To a solution of Boc-protected substituted compound (1.0 mmol) in DCM (4.0 mL), 4M HCl in 1,4- Dioxane (2.0 mL) was added at 0-5 ºC and the reaction mixture was stirred at 25-30 ºC for 12 hours. Completion of the reaction was confirmed by TLC and then NaHCO3 solution was added at 0-5ºC to the reaction mixture to neutralize and extracted by CHCl3which was then dried over Na2SO4and CHCl3was removed under vacuum and the crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get the pure productwith a yield of 67 – 86 %. General procedure H: N-Alkylation reaction. Appropriate amine compound (1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane was added. The reaction mass was stirred for 3 hours at 90ºC.TLC confirmed the consumption of starting material then the reaction mass was quenched with cold water. The reaction mixture was diluted with ethyl acetate (EA) and water. TheEA part was separated and washed with cold water several times. Then the organic part was concentrated under reduced pressure and the crude was purified by column chromatography usingaMeOH / CHCl3 solvent system. After silica gel column purification pure product was isolated with 92 % yield. PT / 2025 / 10975 General procedure I: Ester hydrolysis Appropriate ester (1.0 equivalent), and NaOH (10.0 equivalent) were taken in a 3:1 EtOH & water solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. TLC confirmed the consumption of the starting material then the reaction mass was diluted with water & ethyl acetate. The water part was neutralized by 1 (N) HCl solution and the ethyl acetate part was separated and concentrated in rota vapor to get the pure product with 95 % yield. General procedure J: Amidation reaction To a stirred solution of appropriate acid compound (1.3 equivalent) in DMF under nitrogen atmosphere. HATU (1.3 equivalent), DIPEA (3.5 equivalents), or TEA (3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added Appropriateamine compound. The reaction mixture was stirred at room temperature for 24 hours. After completion of the reaction, the mixture was quenched with water and extracted with ethyl acetate. The ethyl acetate part was washed with cooled water several times and then an organic part was concentrated in rota vapor to get the crude product. This crude product was purified by using silica gel column purification to get the pure product with a yield of 65-70 %. General procedure K: Carbamate reaction To a stirring solution of triphosgene (150 mg) in 10 mL DCM, 4-(piperidin-4-yl)morpholine or 1,4'- bipiperidine or (3S,5R)-3,5-dimethylpiperidine (150 mg) was added at 0 ºC. The reaction mass was stirred for 2 hours then K2CO3(212 mg) was added and again stirred for another 2 hours. Then the reaction mixture was filtered and subsequently, the filtrated was concentrated in rota vapor to give the crude product which was solidified with hexane to give the corresponding carbonyl chloride. Compound 131 (1 equivalent) was dissolved in 6 mL DCM, cooled it to 0ºC, and then NaH (2 equivalent) was added. The reaction mass was stirred for 15 minutes and then TEA (10 equivalents), suitable amine carbonyl chloride (2 equivalent) in DCM, and a catalytic amount of DMF were added. The reaction mixture was stirred for 3 hours at 60 ºC. The crude product was purified by column purification to get desired compound with a 41 % yield. Example 2 Ethyl 5-hydroxy-2-methyl-1H-indole-3-carboxylate: 1, 4 Benzoquinone (10 gm, 92.5069 mmol, 1.0 equivalent) was dissolved in dry acetic acid under a nitrogen atmosphere at 10-15°C. The reaction mixture was stirred for 3 hours at 10-15°C. At this temperature ethyl (Z)-3-aminobut-2-enoate (14.3 gm, 111.0083 mmol, 1.2 equivalent) was added dropwise after the complete addition the reaction mixture was stirred overnight at room temperature. After overnight, the progress of the reaction was monitored by checking TLC at 50% EtOAc in Hexane (V / V). After full consumption of the starting material, the solvent was evaporated under reduced pressure and the crude was washed with cold water and extracted with ethyl acetate which was then dried over Na2SO4. Column chromatography was performed using the Hexane / EtOAc solvent system to get pure 14.1 gm compound 1 as a white solid with a yield of 70%.1H NMR (400 MHz, DMSO-d6) δ 11.42 (s, 1H), 8.77 (s, 1H), 7.21 (d, J = 2.4 Hz, 1H), 7.03 (d, J = 8.7 Hz, 1H), 6.53 – 6.48 (m, 1H), 4.14 (q, J = 7.1 Hz, 2H), 2.49 (s, 3H), 1.23 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C12H13NO3, is219.0895; found, 219.0893. Melting point = 202°C. Example 3 Ethyl 5-acetoxy-2-methyl-1H-indole-3-carboxylate: Compound 1 (12 gm, 54.7720 mmol, 1.0 equivalent) & pyridine (0.5 mL, 6.57264 mmol, 0.06 equivalent) was dissolved in dry DCM and Acetic anhydride (10.4 mL, 109.544 mmol, 2.0 equivalent) was added at room temperature under a nitrogen atmosphere. The reaction was performed according to the generalprocedure A. After column purification 13.3 gm of pure compound 2 was isolated with a 93 % yield.1H NMR (400 MHz, PT / 2025 / 10975 Chloroform-d) δ 8.60 (s, 1H), 7.68 (s, 1H), 7.12 – 7.01 (m, 1H), 6.81 (d, J = 8.6 Hz, 1H), 4.36 (q, J = 7.1 Hz, 2H), 2.62 (s, 3H), 2.34 (s, 3H), 1.41 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C14H15NO4, is261.1001; found, 261.1000. Melting point = 161°C. Example 4 Ethyl 5-acetoxy-1,2-dimethyl-1H-indole-3-carboxylate: Compound 2 (10 gm, 38.2731 mmol, 1.0 equivalent) was dissolved in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (758 mg, 57.4097 mmol, 1.5 equivalents) was added portion-wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then MeI (23 mL, 45.9277 mmol, 1.2 equivalent) was added very slowly at 0 ºC and the reaction mass was stirred for 45 minutes. The reaction was performed according to general procedure B. After silica gel column purification 10 gm of white color pure compound 3 was isolated with a yield of 95 %.Melting point of compound 3 is 131°C.1H NMR (400 MHz, Chloroform-d) δ 7.79 (d, J = 2.3 Hz, 1H), 7.24 (d, J = 8.8 Hz, 1H), 6.95 (dd, J = 8.7, 2.3 Hz, 1H), 4.38 (q, J = 7.1 Hz, 2H), 3.66 (s, 3H), 2.75 (s, 3H), 2.33 (s, 3H), 1.43 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C15H17NO4, is275.1158; found, 275.1156. Melting point = 131°C. Example 5 Ethyl 5-acetoxy-1-benzyl-2-methyl-1H-indole-3-carboxylate: Compound 2 (500 mg, 1.9137 mmol, 1.0 equivalent) was dissolved 2.5 mL in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (69 mg, 2.8705 mmol, 1.5 equivalent) was added portion-wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then benzylbromide (206 µL, 2.2964 mmol, 1.2 equivalent) was added very slowly at 0ºC and the reaction mass was stirred for 45 minutes. The reaction was performed according to general procedure B. 638 mg of the pure compound 4 was isolated with 95 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.84 (s, 1H), 7.23-7.29 (m, 3H), 7.18 (d, J = 8.8 Hz, 1H), 6.97 (d, J = 8.2 Hz, 2H), 6.89 (dd, J = 8.8, 2.3 Hz, 1H), 5.31 (s, 2H), 4.39 (q, J = 7.1 Hz, 2H), 2.71 (s, 3H), 2.32 (s, 3H), 1.43 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C21H21NO4, is 351.1471; found, 351.1470. Example 6 Ethyl 5-acetoxy-1-(4-fluorobenzyl)-2-methyl-1H-indole-3-carboxylate: Compound 2 (500 mg,1.9137 mmol,1.0 equivalent) was dissolved 2.5 mL in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (69 mg, 2.8705 mmol, 1.5 equivalent) was added portion-wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then 4-fluorobenzyl bromide (434 mg, 2.2964 mmol, 1.2 equivalent) was added very slowly at 0 ºC and the reaction mass was stirred for 45 minutes. The reaction was performed according to general procedure B. 657 mg of the pure compound 5 was isolated with 93 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.85 (d, J = 2.3 Hz, 1H), 7.17 (d, J = 8.8 Hz, 1H), 6.96 (dd, J = 6.8, 4.7 Hz, 4H), 6.92 – 6.89 (m, 1H), 5.27 (s, 2H), 4.41 (t, J = 7.1 Hz, 2H), 2.70 (s, 3H), 2.33 (s, 3H), 1.45 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C21H20FNO4, is 369.1376; found, 369.1374. Example 7 Ethyl 5-acetoxy-2-methyl-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 2 (500 mg, 1.9137 mmol,1.0 equivalent) was dissolved 2.5 mL in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (69 mg, 2.8705 mmol, 1.5 equivalents) was added portion- wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then 4-methylbenzyl bromide (425 mg, 2.2964 mmol, 1.2 equivalent) was added very slowly at 0 ºC and the reaction mass was stirred for 45 minutes. The reaction was performed according to general procedure B. 681 mg of the pure compound 6 was PT / 2025 / 10975 isolated with 95 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.84 (d, J = 2.3 Hz, 1H), 7.19 (d, J = 8.8 Hz, 1H), 7.08 (d, J = 8.0 Hz, 2H), 6.91 – 6.85 (m, 3H), 5.28 (s, 2H), 4.40 (q, J = 7.1 Hz, 2H), 2.72 (s, 3H), 2.33 (s, 3H), 2.30 (s, 3H), 1.45 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C22H23NO4, is 365.1627; found, 365.1626. Example 8 Ethyl 5-acetoxy-2-methyl-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate: Compound 2 (500 mg, 1.9137 mmol,1.0 equivalent) was dissolved 2.5 mL in dry DMF under a nitrogen atmosphere at room temperature and cooled to 0 ºC. Then NaH (69 mg, 2.8705 mmol, 1.5 equivalents) was added portion-wise at the same temperature. The reaction mixture was stirred at 0ºC under a nitrogen atmosphere for 30 minutes and the reaction mass became greenish. Then 1-(bromomethyl)naphthalene (508 mg, 2.2964 mmol, 1.2 equivalent) was added very slowly at 0 ºC and the reaction mass was stirred for 45 minutes. The reaction was performed according to general procedure B. 736 mg of the pure Compound 7 was isolated with 90 % yield.1H NMR (600 MHz, Chloroform-d) δ 8.09 (d, J = 8.3 Hz, 1H), 7.94 (d, J = 8.1 Hz, 1H), 7.90 (d, J = 2.2 Hz, 1H), 7.77 (d, J = 8.2 Hz, 1H), 7.66 (ddd, J = 8.3, 6.9, 1.3 Hz, 1H), 7.61 – 7.57 (m, 1H), 7.23 (t, J = 7.4 Hz, 1H), 7.12 (d, J = 8.8 Hz, 1H), 6.87 (dd, J = 8.8, 2.3 Hz, 1H), 6.37 (d, J = 7.2 Hz, 1H), 5.80 (s, 2H), 4.44 (q, J = 7.1 Hz, 2H), 2.72 (s, 3H), 2.35 (s, 3H), 1.48 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C25H23NO4, is 401.1627; found, 401.1625. Example 9 Ethyl 5-acetoxy-6-bromo-2-(bromomethyl)-1-methyl-1H-indole-3-carboxylate: Compound 3 (5 gm, 18.1620 mmol, 1.0 equivalent) was dissolved in CCl4 (120 mL) under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2(2.75 mL, 54.4860 mmol, 3 equivalent) was added very carefully to the reaction mixture with the help of a dropping funnel in an inert atmosphere. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure C.7.55 gm of the white color pure compound 8 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.87 (s, 1H), 7.57 (s, 1H), 5.09 (s, 2H), 4.41 (q, J = 7.1 Hz, 2H), 3.75 (s, 3H), 2.38 (s, 3H), 1.44 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C15H15Br2NO4, is430.9368; found,430.9366. Melting point = 180°C. Example 10 Ethyl 5-acetoxy-1-benzyl-6-bromo-2-(bromomethyl)-1H-indole-3-carboxylate: Compound 4 (500 mg, 1.4229 mmol, 1.0 equivalent) was dissolved in 20 mL CCl4under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2 (214 µL, 4.2686 mmol, 3 equivalents) was added very carefully to the reaction mixture with the help of a dropwise in an inert atmosphere. The reaction was performed according to general procedure C. 681 mg of the pure compound 9 was isolated with 94 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.94 (s, 1H), 7.51 (s, 1H), 7.32 – 7.28 (m, 3H), 7.00 (d, J = 7.2 Hz, 2H), 5.46 (s, 2H), 5.00 (s, 2H), 4.42 (t, J = 7.1 Hz, 2H), 2.38 (s, 3H), 1.44 (d, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C21H19Br2NO4, is 506.9681; found, 506.9681. Example 11 Ethyl 5-acetoxy-6-bromo-2-(bromomethyl)-1-(4-fluorobenzyl)-1H-indole-3-carboxylate: Compound 5 (500 mg, 1.3536 mmol, 1.0 equivalent) was dissolved in 20 mL CCl4 under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2 (204 µL, 4.0607 mmol, 3 equivalents) was added very carefully to the reaction mixture with the help of a dropwise in an inert atmosphere. The reaction was performed according to general procedure C. 671 mg of the pure compound 10 was isolated with 94 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.95 (s, 1H), 7.50 (s, 1H), 7.04 – 7.00 (m, 4H), 5.44 (s, 2H), 5.00 (s, 2H), 4.44 (q, J = 7.1 Hz, 2H), 2.39 PT / 2025 / 10975 (s, 3H), 1.45 (d, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C21H18Br2FNO4, is 524.9587; found, 524.9586. Example 12 Ethyl 5-acetoxy-6-bromo-2-(bromomethyl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 6 (500 mg, 1.3683 mmol, 1.0 equivalent) was dissolved in 20 mL CCl4under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2 (206 µL, 4.1048 mmol, 3 equivalent) was added very carefully to the reaction mixture with the help of a dropwise in an inert atmosphere. The reaction was performed according to general procedure C. 673 mg of the pure compound 11 was isolated with 94 % yield.1H NMR (400 MHz, DMSO-d6) δ 7.82 (s, 2H), 7.09 (d, J = 6.2 Hz, 2H), 6.95 (d, J = 6.2 Hz, 2H), 5.57 (s, 2H), 5.18 (s, 2H), 4.40 - 4.27 (q, J = 7.3 Hz, 2H), 2.30 (s, 3H), 2.21 (s, 3H), 1.35 (t, J = 6.4 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C22H21NO4, is 520.9837; found, 520.9835. Example 13 Ethyl 5-acetoxy-6-bromo-2-(bromomethyl)-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate: Compound 51 (500 mg, 1.2454 mmol, 1.0 equivalent) was dissolved in 20 mL CCl4 under a nitrogen atmosphere at room temperature and this reaction mass was heated to 80 ºC. At this temperature, neat Br2 (187 µL, 3.9850 mmol, 3 equivalents) was added very carefully to the reaction mixture with the help of a dropwise in an inert atmosphere. The reaction was performed according to general procedure C. 627 mg of the pure Compound 12 was isolated with 90 % yield.1H NMR (400 MHz, Chloroform-d) δ 8.12 (d, J = 8.5 Hz, 1H), 8.01 (s, 1H), 7.96 (d, J = 7.6 Hz, 1H), 7.81 (d, J = 8.3 Hz, 1H), 7.70 (t, J = 7.0 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.46 (s, 1H), 7.28 (d, J = 7.4 Hz, 1H), 6.39 (s, 1H), 5.95 (s, 2H), 4.97 (s, 2H), 4.48 (d, J = 7.2 Hz, 2H), 2.40 (s, 3H), 1.48 (d, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C25H21Br2NO4, is 556.9837; found, 556.9837. Example 14 Ethyl 6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indole-3-carboxylate: Benzothiol (26 mg, 0.2378 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (39 mg, 0.6927 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 8 (100 mg, 0.2309 mmol,1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D. 92 mg of the light yellowish solid pure compound 13 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.71 (s, 1H), 7.40 (s, 1H), 7.33 (dd, J = 6.4, 3.2 Hz, 2H), 7.22 (dd, J = 4.2, 1.4 Hz, 3H), 5.35 (s, 1H), 4.68 (s, 2H), 4.27 (q, J = 7.1 Hz, 2H), 3.59 (s, 3H), 1.36 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C19H18BrNO3S, is419.0191; found,419.0189.Melting Point = 196°C. HPLC purity = 97.36 % Example 15 Ethyl 6-bromo-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxylate: 2,4-difluorobenzenethiol (35 mg, 0.2378 mmol, 1.03 equivalent) was dissolved in dry hexane and KOH (39 mg, 0.6927 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 8 (100 mg, 0.2309 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.101 mg of the pure compound 14 was isolated with 95 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.74 (s, 1H), 7.70 (s, 1H), 7.47 (s, 1H), 7.28 – 7.17 (m, 2H), 6.92 (td, J = 8.6, 2.7 Hz, 1H), 4.63 (s, 2H), 4.05 (q, J = 7.4 Hz, 2H), 3.68 (s, 3H), 1.22 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C19H16BrF2NO3S, is 455.0002; found, 455.0001.Melting Point = 192°C. HPLC purity = 97.36 % Example 16 PT / 2025 / 10975 Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate: 4-Fluoro benzothiol (31 mg, 0.2634 mmol, 1.03 equivalents) was dissolved in dry hexane and KOH (39 mg, 0.6927 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 8 (100 mg, 0.2309 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.96 mg of the off white solid pure compound 15 was isolated with 95 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.66 (s, 1H), 7.39 (s, 1H), 7.24 (d, J = 3.5 Hz, 1H), 7.22 (s, 1H), 6.87 (t, J = 8.7 Hz, 2H), 5.37 (s, 1H), 4.59 (s, 2H), 4.21 (q, J = 7.1 Hz, 2H), 3.58 (s, 3H), 1.32 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C19H17BrFNO3S, is 437.0097; found, 437.0095. Melting Point = 178°C. Example 17 Ethyl 1-benzyl-6-bromo-5-hydroxy-2-((phenylthio)methyl)-1H-indole-3-carboxylate: Benzothiol (67 mg, 0.6068 mmol, 1.03 equivalents) was dissolved in dry hexane and KOH (99 mg, 1.7675 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 9 (300 mg, 0.5892 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D. 281 mg of the pure compound 16 was isolated with 96 % yield.1H NMR (400 MHz, Acetone-d6) δ 8.49 (s, 1H), 7.74 (s, 1H), 7.53 (s, 1H), 7.35 (s, 1H), 7.31 – 7.20 (m, 7H), 6.99 (d, J = 8.2 Hz, 2H), 5.51 (s, 2H), 4.76 (s, 2H), 4.23 (q, J = 7.1 Hz, 2H), 1.32 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C25H22BrNO3S, is 495.0504; found, 495.0504. HPLC purity = 99.83 % Example 18 Ethyl 6-bromo-1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-1H-indole-3-carboxylate: Benzothiol (65 mg, 0.5861 mmol, 1.03 equivalents) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3 equivalents) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 10 (300 mg, 0.5691 mmol,1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D. 281 mg of the pure compound 17 was isolated with 97 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.89 (s, 1H), 7.61 (s, 1H), 7.58 (s, 1H), 7.34 – 7.26 (m, 5H), 7.13 (t, J = 8.9 Hz, 2H), 7.01 (dd, J = 8.6, 5.5 Hz, 2H), 5.47 (s, 2H), 4.75 (s, 2H), 4.20 (q, J = 7.1 Hz, 2H), 1.30 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C25H21BrFNO3S, is 513.0410; found, 513.0408. Example 19 Ethyl 6-bromo-1-(4-fluorobenzyl)-5-hydroxy-2-((mesitylthio)methyl)-1H-indole-3-carboxylate: 2, 4, 6-Trimethyl benzenethiol (89 mg, 0.5861 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 10 (300 mg, 0.5691 mmol,1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.294 mg of the pure compound 18 was isolated with 93 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.79 (s, 1H), 7.60 (s, 1H), 7.51 (s, 1H), 7.10 (t, J = 8.7 Hz, 2H), 7.03 – 6.95 (m, 2H), 6.85 (s, 2H), 5.35 (s, 2H), 4.31 (s, 2H), 4.01 (q, J = 7.0 Hz, 2H), 2.16 (s, 3H), 2.13 (s, 6H), 1.20 (t, J = 7.0 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C28H27BrFNO3S, is 555.0879; found, 555.0879. HPLC purity = 97.41 % Example 20 Ethyl 6-bromo-2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-1H- indole-3-carboxylate: 4-fluoro-2-methylbenzenethiol (83 mg, 0.5861 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3.0 equivalent) was added under a nitrogen PT / 2025 / 10975 atmosphere at room temperature and stirred for 2 hours. Then compound 10 (300 mg, 0.5691 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to generalprocedure D. 289 mg of the pure compound 19 was isolated with 93 % yield.1H NMR (400 MHz,Chloroform-d) δ 7.84 (s, 1H), 7.45 (s, 1H), 7.18 (dd, J = 8.5, 5.9 Hz, 1H), 6.98 (t, J = 8.6 Hz, 2H), 6.94 – 6.87 (m, 3H), 6.73 (td, J = 8.4, 2.9 Hz, 1H), 5.33 (s, 2H), 4.43 (s, 2H), 4.22 (q, J = 7.1 Hz, 2H), 2.38 (s, 3H), 2.31 (s, 3H), 1.33 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C26H22BrF2NO3S, is 545.0472; found, 545.0472. HPLC purity = 99.59 % Example 21 Ethyl 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3- carboxylate: 2, 4-dimethyl benzenethiol (82 mg, 0.5906 mmol,1.03 equivalents) was dissolved in dry hexane and KOH (97 mg, 1.7201 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 11 (300 mg, 0.5734 mmol,1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.294 mg of the pure compound 20 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.77 (s, 1H), 7.34 (s, 1H), 7.18 (d, J = 7.8 Hz, 1H), 7.07 (d, J = 7.9 Hz, 2H), 7.00 (s, 1H), 6.88 (d, J = 7.7 Hz, 1H), 6.79 (d, J = 7.9 Hz, 2H), 5.39 (s, 1H), 5.24 (s, 2H), 4.47 (s, 2H), 4.27 (q, J = 7.1 Hz, 2H), 2.30 (s, 3H), 2.28 (s, 3H), 2.28 (s, 3H), 1.37 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C28H28BrNO3S, is 537.0973; found, 537.0972. HPLC purity = 99.96 % Example 22 Ethyl 6-bromo-2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxylate: 4-fluoro-2-methylbenzenethiol (34 mg, 0.2378 mmol, 1.03 equivalent) was dissolved in dry hexane and KOH (39 mg, 0.6927 mmol, 3.0 equivalents) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 8 (100 mg, 0.2309 mmol,1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.100 mg of the pure compound 21 was isolated with 96 % yield.13C NMR (100 MHz, CHLOROFORM-D) δ 164.99, 147.65, 144.10, 137.15, 132.45, 126.96, 117.18, 116.97, 113.51, 113.30, 112.45, 107.46, 106.83, 106.30, 104.91, 59.77, 33.63, 30.05, 29.50, 20.90, 14.55. HRMS (ESI): calculated m / z (M + H)+for C20H19FBrNO3S, is 451.0253; found, 526.2102.Melting Point = 199°C. HPLC purity = 99.82 % Example 23 Ethyl 6-bromo-2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-1H- indole-3-carboxylate: 4-fluoro-2-methylbenzenethiol (84 mg, 0.5906 mmol,1.03 equivalents) was dissolved in dry hexane and KOH (97 mg, 1.7201 mmol, 3.0 equivalents) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 11 (300 mg, 0.5734 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D. 286 mg of the pure compound 22 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.74 (s, 1H), 7.36 (s, 1H), 7.22 (s, 1H), 7.08 (s, 2H), 6.81 (t, J = 27.4 Hz, 4H), 5.50 (s, 1H), 5.28 (s, 2H), 4.45 (s, 2H), 4.35 – 4.17 (m, 2H), 2.30 (s, 6H), 1.36 (s, 3H). Example 24 Ethyl 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: 2, 4, 6-Trimethylbenzenethiol (90 mg, 0.5906 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (97 mg, 1.7201 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 11 (300 mg, 0.5734 mmol, 1.0 equivalent) in dry PT / 2025 / 10975 Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.317 mg of the pure compound 23 was isolated with 92 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.75 (s, 1H), 7.34 (s, 1H), 7.07 (d, J = 7.9 Hz, 2H), 6.87 (s, 2H), 6.78 (d, J = 8.0 Hz, 2H), 5.39 (br.s, 1H), 5.19 (s, 2H), 4.28 (s, 2H), 4.21 (q, J = 7.1 Hz, 2H), 2.30 (s, 3H), 2.27 (s, 6H), 2.25 (s, 3H), 1.34 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C29H30BrNO3S, is 551.1130; found, 551.1128. HPLC purity =96.52 % Example 25 Ethyl 5-acetoxy-6-bromo-2-(bromomethyl)-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate: 4-fluorobenzenethiol (71 mg, 0.5525 mmol, 1.03 equivalenst) was dissolved in dry hexane and KOH (90 mg, 1.6093 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 12 (300 mg, 0.5364 mmol, 1.0 equivalents) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.278 mg of the pure compound 24 was isolated with 92 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.89 (s, 1H), 8.06 (d, J = 8.2 Hz, 1H), 7.95 (d, J = 7.8 Hz, 1H), 7.78 (d, J = 8.2 Hz, 1H), 7.60 (td, J = 11.9, 5.5 Hz, 4H), 7.22 (q, J = 8.2 Hz, 2H), 7.03 (d, J = 10.0 Hz, 1H), 6.84 (t, J = 8.5 Hz, 1H), 6.12 (d, J = 7.1 Hz, 1H), 5.92 (s, 2H), 4.46 (s, 2H), 4.14 (q, J = 7.1 Hz, 2H), 2.09 (s, 3H), 1.27 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C29H23BrFNO3S, is 563.0566; found, 563.0566. Example 26 Ethyl 6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indole-3- carboxylate: Benzenethiol (66 mg, 0.5974 mmol, 1.03 equivalents) was dissolved in dry hexane and KOH (97 mg, 1.7401 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 12 (300 mg, 0.5800 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.292 mg of the pure compound 25 was isolated with 92 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.92 (s, 1H), 8.03 (dd, J = 38.6, 7.9 Hz, 2H), 7.82 (d, J = 8.3 Hz, 1H), 7.68 (s, 1H), 7.65 – 7.57 (m, 2H), 7.56 (s, 1H), 7.29 – 7.17 (m, 6H), 6.14 (d, J = 7.1 Hz, 1H), 5.96 (s, 2H), 4.66 (s, 2H), 4.23 (q, J = 7.1 Hz, 2H), 1.32 (t, J = 7.1 Hz, 3H). Example 27 Ethyl 6-bromo-1-(4-fluorobenzyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1H-indole-3- carboxylate: 4-Fluorobenzothiol (75 mg, 0.5861 mmol, 1.03 equivalent) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3.0 equivalents) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 10 (300 mg, 0.5691 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.290 mg of the pure compound 26 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.75 (s, 1H), 7.31 (s, 1H), 7.31 – 7.26 (m, 2H), 7.00 – 6.88 (m, 6H), 5.40 (s, 1H), 5.31 (s, 2H), 4.55 (s, 2H), 4.26 (t, J = 7.1 Hz, 2H), 1.37 (t, J = 7.1 Hz, 3H). Example 28 Ethyl 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-1H-indole-3- carboxylate: 2,4-dimethyl benzothiol (81 mg, 0.5861 mmol, 1.03 equivalent) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 10 (300 mg, 0.5691 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.296 mg PT / 2025 / 10975 of the pure compound 27 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.61 (s, 1H), 7.28 (s, 1H), 7.11 (d, J = 7.8 Hz, 1H), 6.95 (s, 1H), 6.90 (t, J = 8.6 Hz, 2H), 6.82 (q, J = 8.8, 6.8 Hz, 3H), 5.16 (s, 2H), 4.36 (s, 2H), 4.19 (q, J = 7.1 Hz, 2H), 2.23 (s, 3H), 2.20 (s, 3H), 1.30 (t, J = 7.1 Hz, 3H). Example 29 Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3- carboxylate: 4-Fluorobenzothiol (75 mg, 0.5861 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (96 mg, 1.7072 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 11 (300 mg, 0.5691 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.290 mg of the pure compound 28 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.75 (s, 1H), 7.35 (s, 1H), 7.31 – 7.27 (m, 2H), 7.09 (d, J = 7.9 Hz, 2H), 6.91 (t, J = 8.7 Hz, 2H), 6.81 (d, J = 8.1 Hz, 2H), 5.38 (s, 1H), 5.29 (s, 2H), 4.55 (s, 2H), 4.27 (q, J = 7.1 Hz, 2H), 2.31 (s, 3H), 1.37 (t, J = 7.1 Hz, 3H). Example 30 Ethyl 1-benzyl-6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1H-indole-3- carboxylate: 2, 4-dimethyl benzenethiol (84 mg, 0.6068 mmol, 1.03 equivalent) was dissolved in dry hexane and KOH (99 mg, 1.7675 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 16 (300 mg, 0.5892 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.278 mg of the pure compound 29 was isolated with 90 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.78 (s, 1H), 7.33 (s, 1H), 7.27 (d, J = 6.1 Hz, 3H), 7.18 (d, J = 7.8 Hz, 1H), 7.00 (s, 1H), 6.91 – 6.87 (m, 3H), 5.39 (s, 1H), 5.29 (s, 2H), 4.47 (s, 2H), 4.28 (q, J = 7.1 Hz, 2H), 2.29 (s, 3H), 2.28 (s, 3H), 1.37 (t, J = 7.1 Hz, 3H). Example 31 Ethyl 6-bromo-5-hydroxy-1-(4-methylbenzyl)-2-((phenylthio)methyl)-1H-indole-3-carboxylate: Benzothiol (65 mg, 0.5906 mmol, 1.03 equivalents) was dissolved in dry hexane and KOH (96 mg, 1.7201 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 11 (300 mg, 0.5734 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D. 284 mg of the pure compound 30 was isolated with 97 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.83 (s, 1H), 7.56 (s, 1H), 7.52 (s, 1H), 7.30 – 7.22 (m, 5H), 7.06 (d, J = 7.9 Hz, 2H), 6.82 (d, J = 8.0 Hz, 2H), 5.37 (s, 2H), 4.68 (s, 2H), 4.16 (q, J = 7.0 Hz, 3H), 2.20 (s, 3H), 1.26 (t, J = 7.1 Hz, 4H). Example 32 Ethyl 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H- indole-3-carboxylate: 2,4-dimethyl benzenethiol (82 mg, 0.5974 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (97 mg, 1.7401 mmol, 3.0 equivalent) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 12 (300 mg, 0.5800 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.303 mg of the pure compound 31 was isolated with 91 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.88 (s, 1H), 7.96 (dd, J = 16.7, 7.8 Hz, 2H), 7.77 (d, J = 8.1 Hz, 1H), 7.66 – 7.50 (m, 4H), 7.22 (t, J = 7.6 Hz, 1H), 7.10 (d, J = 7.8 Hz, 1H), 6.96 (s, 1H), 6.82 (d, J = 7.6 Hz, 1H), 6.13 – 6.04 (m, 1H), 5.82 (s, 2H), 4.42 PT / 2025 / 10975 (s, 2H), 4.18 (q, J = 7.1 Hz, 2H), 2.18 (s, 3H), 2.04 (s, 3H), 1.28 (t, J = 7.0 Hz, 3H). HPLC purity = 99.05 % Example 33 Ethyl 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-methyl-1H-indole-3-carboxylate: 2,4,6- trimethyl benzenethiol (65 mg, 0.5946 mmol,1.03 equivalent) was dissolved in dry hexane and KOH (97 mg, mmol, 1.7317 mmol, 3.0 equivalents) was added under a nitrogen atmosphere at room temperature and stirred for 2 hours. Then compound 8 (300 mg, 0.5772 mmol, 1.0 equivalent) in dry Methanol was added and this reaction mixture was stirred for 30-45 minutes at 0 ºC. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure D.256 mg of the pure compound 32 was isolated with 96 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.72 (s, 1H), 7.67 (s, 1H), 7.47 (s, 1H), 6.83 (s, 2H), 4.39 (s, 2H), 4.00 (q, J = 7.1 Hz, 2H), 3.54 (s, 3H), 2.15 (s, 3H), 2.12 (s, 6H), 1.19 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C25H29BrFIN2O3S, is 662.0111; found662.0110. Melting Point = 179°C. Example 34 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-1-methyl-2- ((phenylthio)methyl)-1H-indole-3-carboxylate: To a solution of compound 13 (200 mg, 0.47583 mmol, 1 equivalent), 1.2 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5-tetramethyl- 1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (171 mg, 0.52341 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (16 mg, 0.02379 mmol, 0.05 Equivalent) and Xantphos (27 mg, 0.04758 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 203 mg pure compound 33 was isolated with82 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.14 (d, J = 31.6 Hz, 1H), 7.38 (s, 1H), 7.34 – 7.21 (m, 6H), 7.17 (s, 1H), 5.80 (s, 1H), 4.77 (s, 2H), 4.18 – 4.12 (m, 2H), 3.95 (s, 2H), 3.64 (s, 3H), 3.48 (s, 2H), 3.26 (t, J = 4.9 Hz, 2H), 1.40 (s, 9H), 1.25 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C29H34N2O5S, is 522.2188; found, 522.2168. Melting Point = 189°C, HPLC purity = 99.83 % Example 35 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio) methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate: To a solution of compound 15 (200 mg, 0.45630 mmol, 1 equivalent), 1.14 mL 2.5 M aqueous solution of K3PO4and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (164 mg, 0.50193 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(16 mg, 0.02281 mmol, 0.05 Equivalent) and Xantphos (26 mg, 0.04563 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 204 mg pure sticky liquid compound 34 was isolated with83 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.11 (s, 1H), 7.36 (s, 1H), 7.32 (dd, J = 8.8, 5.4 Hz, 2H), 7.17 (s, 1H), 7.09 (t, J = 8.8 Hz, 2H), 5.80 (s, 1H), 4.71 (s, 2H), 4.14 – 4.08 (m, 2H), 3.95 (s, 2H), 3.63 (s, 3H), 3.48 (t, J = 5.0 Hz, 2H), 1.40 (s, 9H), 1.24 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C29H33FN2O5S, is 540.2094; found, 540.2092. Example 36 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio) methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate: To a solution of compound 14 (200 mg, 0.43831 mmol, 1 equivalent), 1.0 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (157 mg, 0.48214 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (15 mg, 0.02192 mmol, 0.05 equivalent) and Xantphos (25 mg, 0.04383 PT / 2025 / 10975 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 196 mg pure sticky compound 35 was isolated with 80 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.04 (d, J = 45.5 Hz, 1H), 7.32 (s, 1H), 7.27 (dd, J = 8.4, 6.3 Hz, 2H), 7.19 (s, 1H), 6.96 (d, J = 8.5 Hz, 1H), 5.80 (s, 1H), 4.66 (s, 2H), 4.07 – 4.03 (m, 2H), 3.93 (d, J = 19.4 Hz, 2H), 3.68 (s, 3H), 3.48 (t, J = 5.3 Hz, 2H), 3.27 (d, J = 5.8 Hz, 2H), 1.40 (s, 9H), 1.21 (d, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C29H32F2N2O5S, is 558.2000; found, 558.1998. HPLC purity = 99.03 % Example 37 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluoro-2-methylphen yl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate: To a solution of compound 21 (200 mg, 0.45630 mmol, 1 equivalent), 1.10 mL 2.5 M aqueous solution of K3PO4and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (159 mg, 0.48636 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(15 mg, 0.02211 mmol, 0.05 equivalent) and Xantphos (25 mg, 0.04421 mmol, 0.10 equivalent) were added.The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 203 mg sticky solid compound 36 was isolated with83 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.08 (s, 1H), 7.34 (s, 1H), 7.29 – 7.24 (m, 1H), 7.18 (s, 1H), 7.07 (dd, J = 10.0, 2.8 Hz, 1H), 6.91 (td, J = 8.6, 2.9 Hz, 1H), 5.81 (s, 1H), 4.62 (s, 2H), 4.08 (q, J = 7.1 Hz, 2H), 3.92 (d, J = 26.1 Hz, 2H), 3.64 (s, 3H), 3.48 (t, J = 5.3 Hz, 2H), 2.19 (s, 3H), 1.40 (s, 9H), 1.22 (d, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C30H35FN2O5S, is 554.2251; found, 554.2250. Example 38 Ethyl 1-benzyl-6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-2- ((phenylthio) methyl)-1H-indole-3-carboxylate: To a solution of compound 16 (200 mg, 0.40288 mmol, 1 equivalent), 1 mL 2.5 M aqueous solution of K3PO4and tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (145 mg, 0.4431 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(14 mg, 0.02014 mmol, 0.05 equivalent) and Xantphos (23 mg, 0.04029 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 181 mg pure compound 37 was isolated with75 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.17 (s, 1H), 7.43 (s, 1H), 7.36 – 7.17 (m, 10H), 7.07 (s, 1H), 6.92 (d, J = 6.9 Hz, 2H), 5.68 (s, 1H), 5.43 (d, J = 10.1 Hz, 2H), 4.71 (d, J = 18.0 Hz, 2H), 4.16 (dq, J = 7.1, 3.8 Hz, 2H), 3.89 (s, 2H), 3.43 (t, J = 5.6 Hz, 2H), 2.39 (s, 2H), 1.38 (s, 9H), 1.26 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C35H38N2O5S, is 598.2501; found, 598.2501. HPLC purity = 99.90 % Example 39 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-1-(4-fluorobenzyl)-5-hydroxy- 2-((phenylthio)methyl)-1H-indole-3-carboxylate: To a solution of compound 17 (200 mg, 0.3888 mmol, 1 equivalent), 1 mL2.5 M aqueous solution of K3PO4and tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (140 mg, 0.42767 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(13 mg, 0.01944 mmol, 0.05 Equivalent) and Xantphos (22 mg, 0.03888 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 182 mg pure compound 38 was isolated with 80 % yield. HRMS (ESI): calculated m / z (M + H)+for C35H37FN2O5S, is 616.2407; found, 616.2406. Example 40 PT / 2025 / 10975 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-1-(4-fluorobenzyl)-5-hydroxy- 2-((mesitylthio)methyl)-1H-indole-3-carboxylate: To a solution of compound 18 (200 mg, 0.3594 mmol, 1 equivalent), 0.89 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5-tetramethyl- 1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (129 mg, 0.39533 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (12 mg, 0.01797 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.03594 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 182 mg pure compound 39 was isolated with77 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.60 (s, 1H), 6.95 (t, J = 8.7 Hz, 2H), 6.92 – 6.84 (m, 5H), 5.83 (s, 1H), 5.24 (s, 2H), 4.27 (s, 2H), 4.22 (q, J = 7.1 Hz, 2H), 4.07 (s, 2H), 3.63 (t, J = 5.6 Hz, 2H), 2.46 (s, 2H), 2.29 (s, 6H), 2.25 (s, 3H), 1.49 (s, 9H), 1.33 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C38H43FN2O5S, is 555.0879; found, 658.2876. Example 41 Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-2-((phenylthio)methyl)-1H- indole-3-carboxylate: To a solution of compound 17 (200 mg, 0.3594 mmol, 1 equivalent), 0.89 mL 2.5 M aqueous solution of K3PO4and 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H- pyrazole (87 mg, 0.39533 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (12 mg, 0.01797 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.03594 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 142 mg pure compound 40 was isolated with77 % yield.1H NMR (400 MHz, Chloroform-d) δ 10.45 (s, 1H), 7.67 (d, J = 4.5 Hz, 1H), 7.54 (s, 1H), 7.49 (s, 1H), 7.46 (s, 1H), 7.42 – 7.39 (m, 2H), 7.24 (d, J = 2.2 Hz, 1H), 7.22 (d, J = 1.8 Hz, 1H), 6.87 (t, J = 8.5 Hz, 2H), 6.81 – 6.75 (m, 2H), 6.55 (d, J = 14.2 Hz, 1H), 5.14 (s, 2H), 4.74 (s, 2H), 4.31 (q, J = 7.2 Hz, 2H), 1.61 (s, 3H), 1.38 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C38H43FN2O5S, is 555.0879; found, 658.2876. Example 42 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluoro-2-methylphen yl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-1H-indole-3-carboxylate: To a solution of compound 19 (200 mg, 0.36601 mmol, 1 equivalent), 0.91 mL 2.5 M aqueous solution of K3PO4and tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (132 mg, 0.40262 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(13 mg, 0.01830 mmol, 0.05 Equivalent) and Xantphos (21 mg, 0.0366 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 187 mg pure compound 41 was isolated with 76 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.19 (d, J = 14.2 Hz, 1H), 7.39 (s, 1H), 7.26 (dd, J = 8.6, 6.0 Hz, 1H), 7.09 (d, J = 8.4 Hz, 2H), 7.08 – 7.03 (m, 2H), 6.99 (dd, J = 8.7, 5.5 Hz, 2H), 6.94 – 6.88 (m, 1H), 5.70 (s, 1H), 5.44 (s, 2H), 4.55 (s, 2H), 4.10 (q, J = 7.1 Hz, 2H), 3.90 (s, 2H), 3.44 (t, J = 5.3 Hz, 2H), 2.40 (s, 2H), 2.17 (s, 3H), 1.38 (s, 9H), 1.24 (d, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C36H38F2N2O5S, is 648.2469; found, 648.2469. Example 43 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate: To a solution of compound 20 (200 mg, 0.3714 mmol, 1 equivalent), 0.92 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (134 mg, 0.40854 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (13 mg, 0.01857 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.03714 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 190 mg pure PT / 2025 / 10975 compound 42 was isolated with 80 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.62 (s, 1H), 7.20 (d, J = 7.8 Hz, 1H), 7.06 (d, J = 7.9 Hz, 2H), 7.00 (s, 1H), 6.94 (s, 1H), 6.89 (d, J = 7.8 Hz, 1H), 6.80 (d, J = 8.0 Hz, 2H), 5.82 (s, 1H), 5.52 (s, 1H), 5.29 (s, 2H), 4.47 (s, 2H), 4.28 (q, J = 7.1 Hz, 2H), 4.10 – 4.01 (m, 2H), 3.62 (t, J = 5.6 Hz, 2H), 2.45 (d, J = 6.3 Hz, 2H), 2.29 (s, 6H), 2.28 (s, 3H), 1.49 (s, 9H), 1.36 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C38H44N2O5S, is 640.2971; found, 640.2971. Example 44 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-2-((mesitylthio) methyl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: To a solution of compound 23 (200 mg, 0.36197 mmol, 1 equivalent), 0.9 mL 2.5 M aqueous solutionof K3PO4and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (130 mg, 0.39817 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(12 mg, 0.01810 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.0362 mmol, 0.10 equivalent) were added.The reaction was performed according to general procedure F.The crude product was purified by using silica gel column purification to get 187 mg pure compound 43 was isolated with79 % yield. HRMS (ESI): calculated m / z (M + H)+for C39H46N2O5S, is 654.3127; found, 654.3127. HPLC purity = 99.97 % Example 45 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluoro-2-methyl phenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate: To a solution of compound 22 (200 mg, 0.36869 mmol, 1 equivalent), 1mL 2.5 M aqueous solution of K3PO4and tert- butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (133 mg, 0.40556 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (13 mg, 0.01843 mmol, 0.05 Equivalent) and Xantphos (21 mg, 0.03888 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 192 mg pure compound 44 was isolated with81 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.17 (s, 1H), 7.39 (s, 1H), 7.31 – 7.23 (m, 1H), 7.11 (s, 1H), 7.05 (d, J = 8.2 Hz, 2H), 6.91 (s, 1H), 6.83 (d, J = 8.0 Hz, 2H), 5.71 (s, 1H), 5.38 (s, 2H), 4.51 (s, 2H), 4.11 (t, J = 7.1 Hz, 2H), 3.90 (s, 2H), 3.43 (t, J = 5.2 Hz, 2H), 2.40 (s, 2H), 2.18 (d, J = 5.8 Hz, 6H), 1.38 (s, 9H), 1.23 (t, J = 7.1 Hz, 3H). Example 46 Ethyl 5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio) methyl)-1H-indole-3-carboxylate: To a solution of compound 25 (200 mg, 0.36598 mmol, 1 equivalent), 0.87 mL 2.5 M aqueous solution of K3PO4and 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)-1H-pyrazole (83 mg, 0.40258 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(12 mg, 0.0183 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.0366 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 154 mg pure compound 45 was isolated with 77 % yield. Example 47 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-2-((phenylthio)methyl)-1H-indole-3-carboxylate: To a solution of compound 25 (200 mg, 0.36598 mmol, 1 equivalent), 1 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (132 mg, 0.40556 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (13 mg, 0.0183 mmol, 0.05 Equivalent) and Xantphos (21 mg, 0.0366 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The PT / 2025 / 10975 crude product was purified by using silica gel column purification to get 183 mg pure compound 46 was isolated with 77 % yield. HRMS (ESI): calculated m / z (M + H)+for C39H40N2O5S, is 648.2658; found, 648.2656. Melting Point = 189°C, HPLC purity = XX %. Example 48 Ethyl 6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate: To a solution of compound 31 (200 mg, 0.34811 mmol, 1 equivalent), 0.87 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (125 mg, 0.38292 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2(12 mg, 0.01741 mmol, 0.05 equivalent) and Xantphos (21 mg, 0.03481 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 188 mg pure compound 47 was isolated with 80 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.19 (s, 1H), 7.97 (dd, J = 29.2, 7.7 Hz, 2H), 7.76 (d, J = 8.3 Hz, 1H), 7.64 – 7.52 (m, 2H), 7.49 (s, 1H), 7.23 (d, J = 7.7 Hz, 1H), 7.12 (d, J = 7.8 Hz, 1H), 7.06 (s, 1H), 6.96 (s, 1H), 6.81 (d, J = 8.5 Hz, 1H), 6.14 (d, J = 6.7 Hz, 1H), 5.85 (s, 2H), 5.62 (s, 1H), 4.42 (s, 2H), 4.18 (q, J = 7.1 Hz, 2H), 3.82 (s, 2H), 3.37 (t, J = 5.5 Hz, 2H), 2.36 (s, 2H), 2.18 (s, 3H), 2.06 (s, 3H), 1.34 (s, 9H), 1.28 (t, J = 7.1 Hz, 3H). Example 49 Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate: To a solution of compound 34 (180 mg, 0.33293 mmol, 1.0 equivalent) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 137 mg pure compound 48 with a yield of 94 %.1H NMR (400 MHz, One drop MeOD in Chloroform-d) δ 7.37 (s, 1H), 7.17 (s, 2H), 6.96 (s, 1H), 6.80 (t, J = 8.6 Hz, 2H), 5.73 (s, 1H), 4.47 (s, 2H), 4.08 (q, J = 7.1 Hz, 2H), 3.71 (s, 2H), 3.52 (s, 3H), 3.30 (s, 2H), 2.77 (s, 2H), 1.22 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C24H25FN2O3S, is 440.1570; found, 440.1568. Melting Point = 220°C. Example 50 Ethyl 5-hydroxy-1-methyl-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole- 3-carboxylate: To a solution of compound 33 (180 mg, 0.34439 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5 ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 136 mg pure sticky compound 49 with a yield of 94 %.1H NMR (400 MHz, Methanol- d4) δ 7.47 – 7.43 (m, 1H), 7.3-7.26 (m 2H), 7.22 – 7.20 (m, 3H), 7.15-7.14 (m, 1H), 5.87 (s, 1H), 4.65 (d, J = 5.8 Hz, 2H), 4.18 (q, J = 7.0 Hz, 2H), 3.82 (s, 2H), 3.60 (s, 3H), 3.42 (t, J = 5.7 Hz, 2H), 2.87 (d, J = 7.4 Hz, 2H), 1.33 (t, J = 7.1 Hz, 3H. HRMS (ESI): calculated m / z (M + H)+for C24H26N2O3S, is 422.1664; found, 422.1662. HPLC purity = 99.35 % Example 51 Ethyl 2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate: To a solution of compound 35 (180 mg, 0.32221 mmol, 1.0 equivalent) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5 ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 140 mg pure compound 50 with a yield of 95 %.1H NMR (400 MHz, One drop MeOD in Chloroform-d) δ 7.43 – 7.32 (m, 1H), 7.19 – 7.09 (m, 1H), 7.01 – 6.93 (m, 1H), 6.71 (td, J = 8.8, 2.2 Hz, 1H), 6.63 (t, J = 9.4 Hz, 1H), 5.74 (s, 1H), 4.47 (s, 2H), 4.11 (q, J = 7.1 Hz, 2H), 3.73 (s, 2H), 3.61 (s, 3H), 3.32 (t, J = 6.8 Hz, 2H), 3.05 – 3.03 (m, 1H), 3.03 – 3.02 (m, PT / 2025 / 10975 1H), 2.78 (s, 2H), 1.27 – 1.26 (m, 3H).HRMS (ESI): calculated m / z (M + H)+for C24H24F2N2O3S, is 458.1476; found, 458.1477. HPLC purity = 99.83 % Example 52 Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropy ridin-4-yl)-1H-indole-3-carboxylate: To a solution of compound 36 (180 mg, 0.32451 mmol, 1.0 mmol) in DCM (4.0 mL), 0.4 mL 4M HCl in 1,4-Dioxane was added at 0-5 ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 110 mg pure compound 51 with a yield of 96%.1H NMR (400 MHz, Methanol-d4) δ 7.40 (s, 1H), 7.15 (q, J = 6.0, 5.1 Hz, 2H), 6.89 (dd, J = 9.7, 2.5 Hz, 1H), 6.75 – 6.66 (m, 1H), 5.87 (s, 1H), 4.51 (d, J = 4.1 Hz, 2H), 4.11 (q, J = 7.1 Hz, 2H), 3.82 (s, 2H), 3.62 (d, J = 3.0 Hz, 3H), 3.42 (t, J = 5.9 Hz, 2H), 2.87 (s, 2H), 2.21 (s, 3H), 1.30 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C25H27FN2O3S, is 454.1726; found, 454.1724. HPLC purity = 97.15 % Example 53 Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate: To a solution of compound 38 (180 mg, 0.29185 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 143 mg pure compound 52 with a yield of 95 %.1H NMR (400 MHz, Chloroform-d) δ 7.47 (s, 1H), 7.25 – 7.21 (m, 2H), 7.20 – 7.13 (m, 3H), 6.89 – 6.78 (m, 5H), 5.64 (s, 1H), 5.20 (s, 2H), 4.47 (s, 2H), 4.16 (q, J = 7.1 Hz, 2H), 3.67 (s, 2H), 3.27 (t, J = 6.1 Hz, 2H), 2.71 (s, 2H), 1.26 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C30H29FN2O3S, is 516.1883; found, 516.1882. HPLC purity = 99.28 % Example 54 Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((mesitylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate: To a solution of compound 39 (180 mg, 0.27321 mmol, 1.0 equivalent) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 145 mg pure compound 53 with a yield of 95 %.1H NMR (400 MHz, Chloroform-d) δ 9.38 (s, 2H), 7.67 (s, 1H), 6.87 (d, J = 12.4 Hz, 5H), 6.82 (s, 2H), 5.73 (s, 1H), 5.20 (s, 2H), 4.23 (s, 2H), 4.17 (q, J = 7.0 Hz, 2H), 3.85 (s, 2H), 3.44 (s, 2H), 2.80 (s, 2H), 2.27 (s, 6H), 2.22 (s, 3H), 1.28 (t, J = 7.0 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C33H35FN2O3S, is 558.2352; found, 558.2350. HPLC purity = 99.96 % Example 55 Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate: To a solution of compound 41 (180 mg, 0.27745 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 146 mg pure compound 54 with a yield of 96 %.1H NMR (400 MHz, Methanol-d4) δ 7.47 (s, 1H), 7.18 (dd, J = 8.5, 6.0 Hz, 1H), 7.04 (s, 1H), 6.94 (ddd, J = 20.8, 9.1, 3.8 Hz, 5H), 6.73 (td, J = 8.5, 2.8 Hz, 1H), 5.76 (s, 1H), 5.40 (s, 2H), 4.47 (s, 2H), 4.15 (q, J = 7.1 Hz, 2H), 3.80 – 3.72 (m, 2H), 3.63 (s, 3H), 3.37 (t, J = 6.0 Hz, 2H), 2.81 (s, 2H), 2.23 (s, 3H), 1.32 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C31H30F2N2O3S, is 548.1945; found, 548.1944. HPLC purity = 99.01 % Example 56 PT / 2025 / 10975 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahy dropyridin-4-yl)-1H-indole-3-carboxylate: To a solution of compound 42 (180 mg, 0.28088 mmol, 1.0 equivalent) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5 ºC. The reactionwas performed according to general procedure G. The crude was purified in a flash column using CHC3 1l ,MeOH, as eluents in 230-400 mesh size silica to get 147 mg pure compound 55 with a yield of 97 %. H NMR (400 MHz, Chloroform-d) δ 7.68 (s, 1H), 7.18 (d, J = 7.9 Hz, 1H), 6.99 (d, J = 8.3 Hz, 3H), 6.90 (s, 1H), 6.87 (d, J = 9.2 Hz, 1H), 6.74 (d, J = 8.1 Hz, 2H), 5.70 (s, 1H), 5.23 (s, 2H), 4.44 (s, 2H), 4.22 (q, J = 7.1 Hz, 2H), 3.83 (s, 2H), 3.41 (t, J = 5.3 Hz, 2H), 2.78 (s, 2H), 2.26 (s, 6H), 2.23 (s, 3H), 1.30 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C33H36N2O3S, is 540.2447; found, 540.2447. HPLC purity = 99.97 % Example 57 Ethyl 5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate: To a solution of compound 43 (180 mg, 0.27487 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 146 mg pure compound 56 with a yield of 96 %.1H NMR (400 MHz, Chloroform-d) δ 7.64 (s, 1H), 6.98 (d, J = 8.0 Hz, 2H), 6.90 (s, 1H), 6.84 (s, 2H), 6.71 (d, J = 8.1 Hz, 2H), 5.72 (s, 1H), 5.17 (s, 2H), 4.23 (s, 2H), 4.16 (q, J = 7.1 Hz, 2H), 3.80 (s, 2H), 3.38 (t, J = 5.6 Hz, 2H), 2.75 (s, 2H), 2.26 (s, 6H), 2.22 (d, J = 4.5 Hz, 6H), 1.27 (t, J = 7.1 Hz, 4H). HRMS (ESI): calculated m / z (M + H)+for C34H38N2O3S, is 554.2603; found, 554.2603. HPLC purity = 99.81 %. Example 58 Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate: To a solution of compound 44 (180 mg, 0.27916 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 147 mg pure product 57 with a yield of 97 %.1H NMR (400 MHz, Methanol-d4) δ 7.47 (s, 1H), 7.18 (ddd, J = 8.7, 5.9, 3.4 Hz, 1H), 7.04 (d, J = 9.2 Hz, 3H), 6.94 – 6.87 (m, 1H), 6.80 (d, J = 8.0 Hz, 2H), 6.73 (t, J = 9.8 Hz, 1H), 5.76 (s, 1H), 5.34 (s, 2H), 4.47 – 4.40 (m, 2H), 4.20 – 4.09 (m, 2H), 3.76 (s, 2H), 3.37 (t, J = 5.9 Hz, 2H), 2.81 (s, 2H), 2.23 (d, J = 2.4 Hz, 6H), 1.31 (t, J = 7.1 Hz, 3H). Example 59 Ethyl 5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyri din-4-yl)-1H-indole-3-carboxylate: To a solution of compound 46 (150 mg, 0.23119 mmol, 1.0 equivalent) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 120 mg pure product 58 with a yield of 95 %. Example 60 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate: To a solution of compound 47 (160 mg, 0.26593 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5 ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 145 mg pure compound 59 with a yield of 95%.1H NMR (400 MHz, DMSO-d6) δ 9.41 (s, 1H), 9.08 (s, 1H), 8.04 (d, J = 8.2 Hz, 1H), 7.95 (d, J = 8.9 Hz, 1H), 7.77 (d, J = 8.2 Hz, 1H), 7.66 – 7.56 (m, 2H), 7.53 (s, 1H), 7.26 – 7.18 (m, 1H), 7.12 (d, J = 7.9 Hz, 1H), 7.02 (s, 1H), 6.96 (s, 1H), 6.82 (d, J = 7.9 Hz, 1H), 6.13 (d, J = 7.0 Hz, 1H), 5.87 (s, 2H), 5.73 (s, 1H), 4.46 (s, 2H), 4.18 (q, J = 7.1 Hz, 2H), 3.53 (s, 3H), 3.10 (t, J = 5.6 Hz, 2H), 2.59 (s, 2H), 2.18 (s, 3H), 2.06 (s, 3H), 1.29 (t, J = 7.1 Hz, 3H). PT / 2025 / 10975 Example 61 Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4- yl)-1-methyl-1H-indole-3-carboxylate: Compound 48 (80 mg, 0.18160 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (88 µL, 0.63559 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2 M methyl iodide (181µL, 0.37866 mmol, 2.0 equivalents) was added. Compound 60 was synthesized according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 67 mg pure Compound 60 with a yield of 81%.1H NMR (400 MHz, DMSO-d6) δ 9.10 (s, 1H), 7.36 (s, 1H), 7.32 (dd, J = 8.8, 5.4 Hz, 2H), 7.15 (s, 1H), 7.09 (t, J = 8.9 Hz, 2H), 5.82 (s, 1H), 4.71 (s, 2H), 4.11 (q, J = 7.1 Hz, 2H), 3.64 (s, 3H), 3.13 (s, 2H), 2.67 (t, J = 5.4 Hz, 2H), 2.59 – 2.53 (m, 2H), 2.36 (s, 3H), 1.24 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C25H27FN2O3S, is 454.1726; found, 454.1726.Melting Point = 215°C. HPLC purity = 99.82 % Example 62 Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate: Compound 48 (80 mg, 0.18160 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (88 µL, 0.63559 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (36µL, 0.36320 mmol, 2.0 equivalents) was added. The compound 61 was synthesized according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 70 mg pure Compound 61 with a yield of 85%.1H NMR (400 MHz, Chloroform-d) δ 7.54 (s, 1H), 7.29 (dd, J = 8.8, 5.3 Hz, 2H), 7.00 (s, 1H), 6.90 (t, J = 8.7 Hz, 2H), 5.89 (dt, J = 3.4, 1.8 Hz, 1H), 4.64 (s, 2H), 4.23 (q, J = 7.1 Hz, 2H), 3.60 (s, 3H), 3.32 (q, J = 2.6 Hz, 2H), 2.95 (quintet, J = 6.6 Hz, 1H), 2.85 (t, J = 5.7 Hz, 2H), 2.62 – 2.59 (m, 2H), 1.34 (t, J = 7.1 Hz, 3H), 1.17 (d, J = 6.5 Hz, 6H).HRMS (ESI): calculated m / z (M + H)+for C27H31FN2O3S, is 482.2039; found, 482.2039. Melting Point = 180°C. HPLC purity = 99.56 % Example 63 Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate: Compound 48 (80 mg, 0.18160 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (88 µL, 0.63559 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (37µL, 0.36320 mmol, 2.0 equivalents) was added. The compound 62 was synthesized according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 67 mg pure compound 62 with a yield of 86%.1H NMR (400 MHz, DMSO-d6) δ 9.10 (s, 1H), 7.39 (s, 1H), 7.36 (dd, J = 8.8, 5.4 Hz, 2H), 7.18 (s, 1H), 7.13 (d, J = 17.8 Hz, 2H), 5.84 (s, 1H), 4.75 (s, 2H), 4.15 (q, J = 7.1 Hz, 2H), 3.67 (s, 3H), 3.18 (s, 2H), 2.70 (s, 2H), 2.56 (s, 2H), 1.87 (s, 2H), 1.65 (t, J = 7.0 Hz, 2H), 1.57 – 1.48 (m, 2H), 1.48 – 1.36 (m, 2H), 1.28 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C29H33FN2O3S, is 508.2196; found, 508.2196. Melting Point = 174°C. HPLC purity = 99.92 % Example 64 Ethyl 5-hydroxy-1-methyl-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((phenylthio) methyl)- 1H-indole-3-carboxylate: Compound 49 (80 mg, 0.18933 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (93 µL, 0.66265 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2 M methyl iodide (189µL, 0.37866 mmol, 2.0equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 66 mg sticky pure compound 63 with a yield of 80%. 1H NMR (400 MHz, Chloroform-d) δ 7.56 (s, 1H), 7.37 – 7.34 (m, 2H), 7.24 – 7.20 (m, 3H), 6.99 (s, 1H), PT / 2025 / 10975 5.84 (t, J = 3.3, 1.7 Hz, 1H), 4.69 (s, 2H), 4.26 (q, J = 7.1 Hz, 2H), 3.60 (s, 3H), 3.34-3.33 (m, 2H), 2.93 (t, J = 5.8 Hz, 2H), 2.71 (s, 2H), 2.58 (s, 3H), 1.34 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C25H28N2O3S, is 436.1821; found, 436.1820. HPLC purity = 98.75 % Example 65 Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-methyl-2-((phenylthio) methyl)-1H-indole-3-carboxylate: Compound 49 (80 mg, 0.18933 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (93 µL, 0.66265 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (38µL, 0.37866 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 70 mg sticky pure compound 64 with a yield of 85%.1H NMR (400 MHz, Chloroform-d) δ 7.57 (s, 1H), 7.36 – 7.33 (m, 2H), 7.22 (dd, J = 5.1, 2.0 Hz, 3H), 6.97 (s, 1H), 5.83 (s, 1H), 4.68 (s, 2H), 4.28 – 4.22 (m, 2H), 3.57 (s, 3H), 3.49 – 3.47 (m, 2H), 3.31 – 3.25 (m, 1H), 3.05 (t, J = 5.7 Hz, 2H), 2.75 (s, 2H), 1.34 (t, J = 7.1 Hz, 3H), 1.27 (d, J = 6.6 Hz, 6H).HRMS (ESI): calculated m / z (M + H)+for C27H32N2O3S, is 436.1821; found, 464.2134. HPLC purity = 99.77 % Example 66 Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate: Compound 50 (80 mg, 0.17447 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (85 µL, 0.61066 mmol, 3.5 equivalents) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (35µL, 0.34895 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 69 mg pure compound 65 with a yield of 86%.1H NMR (400 MHz, DMSO-d6) δ 9.25 (s, 1H), 7.40 (s, 1H), 7.37 – 7.27 (m, 2H), 7.25 (d, J = 6.8 Hz, 1H), 7.00 (td, J = 8.5, 2.8 Hz, 1H), 5.93 (s, 1H), 4.72 (s, 2H), 4.10 (q, J = 7.1 Hz, 2H), 3.74 (s, 3H), 3.59-3.51 (m, 2H), 3.19-3.15 (m, 1H), 3.15 – 3.01 (m, 2H), 2.78-2.68 (m, 2H), 2.02- 1.95 (m, 2H), 1.75-1.71 (m,, 2H), 1.63-1.49 (m, 4H), 1.27 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C29H32F2N2O3S, is 526.2102; found, 526.2102.HPLC purity = 99.71 % Example 67 Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridin-4-yl)-1-methyl-1H-indole-3-carboxylate: Compound 51 (80 mg, 0.17599 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (86 µL, 0.61598 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (35µL, 0.35199 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 74 mg pure compound 66 with a yield of 85%.1H NMR (400 MHz, Methanol-d4) δ 7.40 (s, 1H), 7.18 (dd, J = 8.5, 5.9 Hz, 1H), 7.14 (s, 1H), 6.92 (dd, J = 9.9, 2.8 Hz, 1H), 6.76 – 6.71 (m, 1H), 5.89 (dt, J = 3.4, 1.8 Hz, 1H), 4.54 (s, 2H), 4.13 (q, J = 7.1 Hz, 2H), 3.63 (s, 3H), 3.56 (s, 2H), 3.19 (p, J = 6.6 Hz, 1H), 3.11 (t, J = 5.8 Hz, 2H), 2.81 (s, 2H), 2.24 (s, 3H), 1.32 (s, 3H), 1.28 (d, J = 6.6 Hz, 6H).HRMS (ESI): calculated m / z (M + H)+for C28H33FN2O3S, is 496.2196; found, 496.2195. HPLC purity = 99.98 % Example 68 Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesityl thio)methyl)-1H-indole-3-carboxylate: Compound 52 (80 mg, 0.15485 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (75 µL, 0.54197 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen PT / 2025 / 10975 atmosphere for 30 minutes and then 2-iodopropane (75 µL, 0.54197 mmol, 3.5 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 79 mg pure compound 67 with ayield of 92 %.1H NMR (400 MHz, Chloroform-d) δ 7.61 (s, 1H), 7.35 – 7.31 (m, 2H), 7.22 (dd, J = 5.0,2.0 Hz, 3H), 6.93 (t, J = 8.6 Hz, 2H), 6.89 – 6.84 (m, 3H), 5.82 (s, 1H), 5.28 (s, 2H), 4.62 (s, 2H), 4.29 (q, J = 7.1 Hz, 2H), 3.35 (d, J = 2.8 Hz, 2H), 3.07 – 3.00 (m, 1H), 2.89 (t, J = 5.8 Hz, 2H), 2.58 (s, 2H), 1.36 (t, J = 7.1 Hz, 3H), 1.19 (d, J = 6.6 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C33H35FN2O3S, is 558.2352; found, 558.2350. Example 69 Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl- 1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3-carboxylate: Compound 53 (80 mg, 0.14319 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (70 µL, 0.50115 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (29 µL, 0.28637 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 79 mg pure compound 68 with a yield of 92 %.1H NMR (400 MHz, Chloroform-d) δ 7.58 (s, 1H), 6.95 – 6.90 (m, 3H), 6.87 (s, 3H), 6.84 (d, J = 5.4 Hz, 1H), 5.80 (s, 1H), 5.21 (s, 2H), 4.26 (s, 2H), 4.20 (q, J = 7.1 Hz, 2H), 3.50 – 3.46 (m, 2H), 3.28 – 3.23 (m, 1H), 3.05 (t, J = 5.7 Hz, 2H), 2.74 (s, 2H), 2.28 (s, 6H), 2.23 (s, 3H), 1.31 (t, J = 7.1 Hz, 2H), 1.91 (s, 6H). HRMS (ESI): calculated m / z (M + H)+for C36H41FN2O3S, is 600.2822; found, 600.2820.HPLC purity = 99.78 % Example 70 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridin- 4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 54 (80 mg, 0.14581 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (71 µL, 0.51034 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (29 µL, 0.29163 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 77 mg pure compound 69 with a yield of 90 %.1H NMR (400 MHz, Chloroform-d) δ 7.57 (s, 1H), 7.22 (dd, J = 8.6, 5.9 Hz, 1H), 6.96 – 6.92 (m, 2H), 6.90 – 6.86 (m, 4H), 6.74 (td, J = 8.5, 3.1 Hz, 1H), 5.86 – 5.80 (m, 1H), 5.30 (s, 2H), 4.46 (s, 2H), 4.23 (q, J = 7.1 Hz, 2H), 3.26 (d, J = 3.1 Hz, 2H), 2.93 – 2.87 (m, 1H), 2.78 (t, J = 5.7 Hz, 2H), 2.50 (s, 2H), 2.30 (s, 3H), 1.34 (t, J = 7.1 Hz, 3H), 1.13 (d, J = 6.5 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C34H36F2N2O3S, is 590.2415; found, 590.2414. HPLC purity = 99.75 % Example 71 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin-4- yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 55 (80 mg, 0.14795 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (72 µL, 0.51783 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (35 µL, 0.2959 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 77 mg pure Compound 70 with a yield of 90 %.1H NMR (400 MHz, Chloroform-d) δ 7.60 (s, 1H), 7.20 (d, J = 7.8 Hz, 1H), 7.03 (d, J = 7.8 Hz, 2H), 6.98 (s, 1H), 6.92 (s, 1H), 6.87 (d, J = 7.8 Hz, 1H), 6.78 (d, J = 8.0 Hz, 2H), 5.85 (s, 1H), 5.26 (s, 2H), 4.48 (s, 2H), 4.26 (t, J = 7.1 Hz, 2H), 3.27 (d, J = 3.0 Hz, 2H), 2.96 – 2.88 (m, 1H), 2.79 (t, J = 5.7 Hz, 2H), 2.51 (s, 2H), 2.28 (d, J = 2.3 Hz, 6H), 2.27 (s, 3H), 1.35 (t, J = 7.1 Hz, 3H), 1.14 (d, J = 6.6 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C36H42N2O3S, is 582.2916; found, 582.2914. HPLC purity = 99.97 % PT / 2025 / 10975 Example 72 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin-4- yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 70 (80 mg, 0.15485 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (73 µL, 0.51783 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2 M methyl iodide (147µL, 0.29590 mmol, 2.0 equivalents) was added.The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 65 mg pure compound 71 with a yield of 80%.1H NMR (400 MHz, Chloroform-d) δ 7.60 (s, 1H), 7.21 (d, J = 7.8 Hz, 1H), 7.05 (d, J = 7.9 Hz, 2H), 7.00 (s, 1H), 6.94 (s, 1H), 6.89 (d, J = 8.6 Hz, 1H), 6.80 (d, J = 8.0 Hz, 2H), 5.82 (dt, J = 3.2, 1.7 Hz, 1H), 5.28 (s, 2H), 4.49 (s, 2H), 4.28 (q, J = 7.1 Hz, 2H), 3.12 (d, J = 2.9 Hz, 2H), 2.68 (t, J = 5.7 Hz, 2H), 2.52 (s, 2H), 2.44 (s, 3H), 2.29 (d, J = 2.7 Hz, 6H), 2.28 (s, 3H), 1.36 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C34H38N2O3S, is 554.2603; found, 554.2602. HPLC purity = 99.90 % Example 73 Ethyl 6-(1-cyclohexyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 55 (80 mg, 0.14795 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (72 µL, 0.51783 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclohexyl (28 µL, 0.2959 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 60 mg pure compound 72 with a yield of 90 %.1H NMR (400 MHz, Methanol-d4) δ 7.53 – 7.44 (m, 1H), 7.17 (s, 1H), 7.11 (d, J = 7.7 Hz, 1H), 7.04 (t, J = 7.6 Hz, 2H), 6.98 (s, 2H), 6.86 – 6.76 (m, 3H), 5.75 (s, 1H), 5.27 (d, J = 12.0 Hz, 2H), 4.44 (s, 2H), 4.16 (q, J = 7.1 Hz, 2H), 3.60 (d, J = 3.8 Hz, 1H), 3.42 (s, 1H), 2.97 (t, J = 5.2 Hz, 1H), 2.79 (t, J = 6.7 Hz, 1H), 2.66 (s, 1H), 2.24 (s, 6H), 2.20 (s, 3H), 1.99 (s, 1H), 1.88 – 1.81 (m, 1H), 1.66 (d, J = 12.5 Hz, 1H), 1.44 (td, J = 14.7, 6.5 Hz, 1H), 1.33 (d, J = 7.1 Hz, 3H), 1.28 (d, J = 18.7 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C39H46N2O3S, is 622.3229; found, 622.3228. HPLC purity = 99.01 % Example 74 Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate: Compound 55 (80 mg, 0.14795 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (72 µL, 0.51783 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (30 µL, 0.2959 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 60 mg pure compound 73 with a yield of 90 %.1H NMR (400 MHz, Methanol-d4) δ 7.49 (s, 1H), 7.14 (d, J = 7.8 Hz, 1H), 7.06 (s, 2H), 7.02 (s, 2H), 6.87 (d, J = 5.7 Hz, 1H), 6.81 (d, J = 7.7 Hz, 2H), 5.77 (s, 1H), 5.30 (s, 2H), 4.47 (s, 2H), 4.18 (t, J = 7.1 Hz, 2H), 3.64 (s, 1H), 3.51 (s, 2H), 3.12 – 3.08 (m, 2H), 2.75 (s, 2H), 2.27 (s, 6H), 2.23 (s, 3H), 2.06 (d, J = 8.3 Hz, 2H), 1.79 (s, 2H), 1.68 – 1.58 (m, 4H), 1.35 (t, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C39H46N2O3S, is 622.3229; found, 622.3228. HPLC purity = 99.07 % Example 75 Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxylate: Compound 56 (80 mg, 0.14421 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (70 µL, 0.50473 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen PT / 2025 / 10975 atmosphere for 30 minutes and then 2-iodopropane (29 µL, 0.28842 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 80 mg pure compound 74 with ayield of 93 %.1H NMR (400 MHz, Chloroform-d) δ 7.57 (s, 1H), 7.03 (d, J = 7.8 Hz, 2H), 6.92 (s, 1H),6.86 (s, 2H), 6.77 (d, J = 8.0 Hz, 2H), 5.85 (dt, J = 3.3, 1.8 Hz, 1H), 5.21 (s, 2H), 4.28 (s, 2H), 4.20 (q, J = 7.1 Hz, 2H), 3.23 (d, J = 3.0 Hz, 2H), 2.87 – 2.79 (m, 1H), 2.74 (t, J = 5.6 Hz, 2H), 2.51 – 2.45 (m, 2H), 2.29 (s, 6H), 2.23 (s, 3H), 1.32 (t, J = 7.1 Hz, 3H), 1.11 (d, J = 6.5 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C37H44N2O3S, is 596.3073; found, 596.3073. HPLC purity = 99.38 % Example 76 Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxylate: Compound 58 (80 mg, 0.1458 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (72 µL, 0.5103 mmol, 3.5 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (30 µL, 0.1750 mmol, 2.0 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 60 mg pure compound 75 with a yield of 90 %. HRMS (ESI): calculated m / z (M + H)+for C37H38N2O3S, is 648.2658; found, 648.2656. Melting Point = 189°C. Example 77 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridin- 4-yl)-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate: Compound 59 (100 mg, 0.1734 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (85 µL, 0.6068 mmol, 3.5 equivalents) was added at room temperature. The reaction mixture stirred under a nitrogen atmosphere for 30 minutes and then 2-iodopropane (60 µL, 0.54197 mmol, 3.5 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 96 mg pure compound 76 with a yield of 90 %. HRMS (ESI): calculated m / z (M + H)+for C39H42N2O3S, is 618.2916; found, 618.2914. Melting Point = 187°C. Example 78 6-bromo-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylic acid: Compound 14 (300 mg, 0.65746 mmol, 1.0 equivalent), and NaOH (263 mg, 6.5746, 10.0 equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110 ºC for 24 hours. The reaction was performed according to general procedure I.279 mg of the pure compound 78 was isolated with 99 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.51 (s, 1H), 7.36 (s, 1H), 7.16 – 7.10 (m, 1H), 6.72 – 6.60 (m, 2H), 4.49 (s, 2H), 3.59 (s, 3H).HRMS (ESI): calculated m / z (M + H)+for C17H12BrF2NO3S, is 426.9689; found, 426.9689. Melting Point = 192°C. Example 79 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylic acid: Compound 15 (300 mg, 0.68444 mmol, 1.0 Equivalent), and NaOH (273 mg, 6.8444, 10.0 Equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. The reaction was performed according to general procedure I.269 mg of the pure compound 79 was isolated with 96 % yield. HRMS (ESI): calculated m / z (M + H)+for C17H13BrFNO3S, is 408.9784; found, 408.9782.Melting Point = 178°C. Example 80 PT / 2025 / 10975 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indole-3-carboxylic acid: Compound 23 (300 mg, 0.54296 mmol, 1.0 equivalent), and NaOH (217 mg, 6.5746, 10.0 equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110 ºC for 24 hours. The reaction was performed according to general procedure I.273 mg of the pure compound 80 was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.84 (s, 1H), 7.35 (s, 1H), 7.08 (d, J = 8.1 Hz, 2H), 6.87 (s, 2H), 6.79 (d, J = 8.0 Hz, 2H), 5.19 (s, 2H), 4.28 (s, 2H), 2.30 (s, 3H), 2.28 (s, 6H), 2.20 (s, 3H). HRMS (ESI): calculated m / z (M + H)+for C27H28BrNO3S, is 523.0817; found, 523.0816. Melting Point = 194°C, Example 81 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indole-3- carboxylic acid: Compound 24 (300 mg, 0.53147 mmol, 1.0 Equivalent), and NaOH (212 mg, 5.31473, 10.0 Equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. The reaction was performed according to the general procedure I. 271 mg of the pure compound 81 was isolated with 95 % yield.1H NMR (400 MHz, DMSO-d6) δ 12.33 (s, 1H), 9.84 (s, 1H), 8.08 (d, J = 8.2 Hz, 1H), 7.98 (d, J = 8.7 Hz, 1H), 7.81 (d, J = 8.3 Hz, 1H), 7.69 (s, 1H), 7.67 – 7.58 (m, 2H), 7.54 (s, 1H), 7.31 – 7.27 (m, 2H), 7.26 (s, 1H), 7.02 (t, J = 8.9 Hz, 2H), 6.14 (d, J = 7.0 Hz, 1H), 5.94 (s, 2H), 4.65 (s, 2H). HRMS (ESI): calculated m / z (M + H)+for C27H19BrFNO3S, is 535.0253; found, 535.0252 Melting Point = 194°C. Example 82 6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indole-3-carboxylic acid: Compound 25 (300 mg, 0.54897 mmol, 1.0 equivalent), and NaOH (219 mg, 5.31473, 10.0 equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. The reaction was performed according to general procedure I. 270 mg of the pure compound 82 was isolated with 95 % yield.1H NMR (400 MHz, DMSO-d6) δ 12.37 (s, 1H), 9.82 (s, 1H), 8.02 (d, J = 8.2 Hz, 1H), 7.94 (d, J = 9.4 Hz, 1H), 7.78 (d, J = 8.3 Hz, 1H), 7.67 (s, 1H), 7.63 – 7.51 (m, 2H), 7.50 (s, 1H), 7.24 – 7.13 (m, 5H), 6.11 (d, J = 7.1 Hz, 1H), 5.90 (s, 2H), 4.66 (s, 2H). HRMS (ESI): calculated m / z (M + H)+for C27H20BrNO3S, is 517.0347; found, 517.0346. Melting Point = 194°C. Example 83 6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indole-3-carboxylic acid: Compound 13 (300 mg, 0.71374 mmol, 1.0 equivalent), and NaOH (285 mg, 7.1374, 10.0 equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. The reaction was performed according to general procedure I.266 mg of the pure compound 83 was isolated with 95 % yield.1H NMR (400 MHz, DMSO-d6) δ 12.16 (s, 1H), 9.71 (s, 1H), 7.67 (s, 1H), 7.56 (s, 1H), 7.34 (d, J = 6.9 Hz, 2H), 7.28 – 7.19 (m, 3H), 4.79 (s, 2H), 3.62 (s, 3H).HRMS (ESI): calculated m / z (M + H)+for C17H14BrNO3S, is 390.9878; found, 390.9875. Melting Point = 194°C. Example 84 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indole- 3-carboxylic acid: Compound 31 (300 mg, 0.52216 mmol, 1.0 equivalent), and NaOH (209 mg, 5.22163, 10.0 equivalent) were taken in a 3:1 EtOH (3 mL) & water (1 mL) solution in a nitrogen atmosphere. This reaction mixture was stirred at 110ºC for 24 hours. The reaction was performed according to general procedure I. 271 mg of the pure compound 84 was isolated with 95 % yield. HRMS (ESI): calculated m / z (M + H)+for C29H24BrNO3S, is 545.0660; found, 545.0658. Melting Point = 194°C. Example 85 PT / 2025 / 10975 6-bromo-N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide: To a stirred solution of compound 78 (250 mg, 0.5838 mmol, 1.0 equivalent) in DMF under nitrogen atmosphere, HATU (533 mg, 1.4011 mmol, 1.2 equivalent), TEA (364 µL, 2.0432 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl amine (85 mg, 1.1675 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 211 mg pure product85 was isolated with 75% yield.1H NMR (400 MHz, Chloroform-d) δ 7.32 (s, 1H), 7.31 – 7.26 (m, 1H), 7.21 (s, 1H), 6.80 – 6.68 (m, 2H), 6.49 (s, 1H), 5.69 (s, 1H), 4.50 (s, 2H), 3.64 (s, 3H), 1.41 (s, 9H). HRMS (ESI): calculated m / z (M + H)+for C21H21BrF2N2O2S, is 482.0475; found, 482.0475. Melting Point = 182°C. Example 86 6-bromo-N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide: To a stirred solution of compound 79 (250 mg, 0.6094 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (556 mg, 1.4625 mmol, 1.2 equivalent), TEA (297 µL, 2.1328 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl amine (89 mg, 1.2187 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 212 mg pure compound 86was isolated with 75% yield.1H NMR (400 MHz, Chloroform-d) δ 7.48 – 7.38 (m, 1H), 7.32 – 7.16 (m, 3H), 6.98 – 6.84 (m, 2H), 4.45 (s, 2H), 3.58 (s, 3H), 1.40 (s, 9H). HRMS (ESI): calculated m / z (M + H)+for C21H22BrFN2O2S, is 464.0569; found, 464.0567. Melting Point = 182°C. Example 87 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indole-3- carboxamide: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl amine (69 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 204 mg pure productcompound 87 was isolated with 74% yield.1H NMR (400 MHz, Chloroform-d) δ 7.36 (s, 1H), 7.30 (s, 1H), 7.04 (d, J = 7.9 Hz, 2H), 6.85 (s, 2H), 6.74 (d, J = 8.0 Hz, 2H), 5.71 (s, 1H), 5.12 (s, 2H), 4.16 (s, 2H), 2.28 (s, 3H), 2.26 (s, 6H), 2.24 (s, 3H), 1.41 (s, 9H). HRMS (ESI): calculated m / z (M + H)+for C21H21BrF2N2O2S, is 578.1603; found, 578.1602. Melting Point = 187°C. Example 88 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(naphthalen-1-ylmethyl)-1H- indole-3-carboxamide: To a stirred solution of compound 82 (100 mg, 0.1907 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (174 mg, 0.3813 mmol, 1.2 equivalent), TEA (93 µL, 0.6673 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl amine (28 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 204 mg compound 88 was isolated with 74% yield. HRMS (ESI): calculated m / z (M + H)+for C34H35BrN2O2S, is 614.1603; found, 614.1602. Melting Point = 187°C. Example 89 6-bromo-N-(tert-butyl)-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide: To a stirred solution of compound 84 (100 mg, 0.1830 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (167 mg, 0.4392 mmol, 1.2 equivalent), TEA (89 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-Butyl Amine (27 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 69 mg pure PT / 2025 / 10975 compound 89 was isolated with 63 % yield. HRMS (ESI): calculated m / z (M + H)+for C23H27BrFN3O2S, is 600.1446; found, 600.1444. Melting Point = 167°C. Example 90 tert-butyl 4-(3-(tert-butylcarbamoyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl- 1H-indol-6-yl)-3,6-dihydropyridine-1(2H)-carboxylate: To a solution of compound 85 (200 mg, 0.45630 mmol, 1 equivalent), 1.14 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (164 mg, 0.50193 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (16 mg, 0.02281 mmol, 0.05 Equivalent) and Xantphos (26 mg, 0.04563 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 204 mg pure sticky liquid compound 90 was isolated with 83 % yield.1H NMR (400 MHz, DMSO-d6) δ 8.94 (d, J = 38.2 Hz, 1H), 7.62 – 7.50 (m, 1H), 7.40 – 7.32 (m, 1H), 7.25 – 7.20 (m, 1H), 7.10 (d, J = 39.9 Hz, 1H), 6.98 (dt, J = 5.8, 3.0 Hz, 1H), 6.59 (d, J = 21.1 Hz, 1H), 5.80 (s, 1H), 4.61 (s, 2H), 3.95 (s, 1H), 3.66 (s, 3H), 3.48 (t, J = 5.3 Hz, 1H), 1.40 (s, 9H), 1.30 (s, 9H).HRMS (ESI): calculated m / z (M + H)+for C31H37F2N3O4S, is 585.2473; found, 585.2472. Melting Point = 188°C. HPLC purity = 98.75 % Example 91 tert-butyl 4-(3-(tert-butylcarbamoyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H- indol-6-yl)-3,6-dihydropyridine-1(2H)-carboxylate: To a solution of compound 86 (200 mg, 0.42976 mmol, 1 equivalent), 1.07 mL 2.5 M aqueous solution of K3PO4 and tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate (154 mg, 0.47273 mmol, 1.1 equivalent) were taken in 1,4-Dioxane under Argon atmosphere. Degassed with Argon gas for 30 minutes and then Pd(PPh3)2Cl2 (15 mg, 0.02149 mmol, 0.05 Equivalent) and Xantphos (25 mg, 0.04298 mmol, 0.10 equivalent) were added. The reaction was performed according to general procedure F. The crude product was purified by using silica gel column purification to get 187 mg pure sticky liquid compound 91 was isolated with 83 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.48 – 7.38 (m, 1H), 7.32 – 7.16 (m, 3H), 6.98 – 6.84 (m, 2H), 4.45 (s, 2H), 3.58 (s, 3H), 1.40 (s, 9H). HRMS (ESI): calculated m / z (M + H)+for C31H38FN3O4S, is 567.2567; found, 567.2565. Melting Point = 198°C. Example 92 N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydro pyridin-4-yl)-1H-indole-3-carboxamide: To a solution of compound 90 (150 mg, 0.31032 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 119 mg pure compound 92 was isolated with a 96 % yield. HRMS (ESI): calculated m / z (M + H)+for C26H29F2N3O2S, is 485.1949; found, 485.1947. Melting Point = 180°C. Example 93 N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyri din-4-yl)-1H-indole-3-carboxamide: Compound 92 (80 mg, 0.1847 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (90 µL, 0.6465 mmol,3.5 equivalents) was added at room temperature. The reaction mixture stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (33 mg, 0.2217 mmol, 3.5 equivalents) was added. The reaction was performed according to general procedure H.118 mg pure compound 94 was isolated with a 96 % yield. HRMS (ESI): calculated m / z (M + H)+for C31H37F2N3O2S, is 553.2575; found, 553.2572. Melting Point = 191°C. Example 94 PT / 2025 / 10975 N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio) methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxamide: To a solution of compound 91 (150 mg, 0.6094 mmol, 1.0 mmol) in DCM (4.0 mL), 0.5 mL 4M HCl in 1,4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 117 mg pure compound 93 was isolated with a95 % yield.1H NMR (400 MHz, Methanol-d4) δ 7.28 (s, 2H), 7.18 (s, 1H), 7.13 (s, 1H), 6.98 (d, J = 8.2 Hz, 2H), 6.65 (s, 0H), 5.89 (s, 1H), 4.54 (s, 2H), 3.84 (s, 2H), 3.67 (s, 3H), 3.44 (s, 2H), 3.30 (s, 3H), 2.89 (s, 2H), 1.41 (s, 9H).HRMS (ESI): calculated m / z (M + H)+for C26H30FN3O2S, is 467.2043; found, 467.2043. Melting Point = 186°C. Example 95 N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio) methyl)- 5-hydroxy-1-methyl-1H-indole-3-carboxamide: Compound 93 (80 mg, 0.1847 mmol, 1.0 equivalent) was dissolved in 0.5 mL dry DMF under a nitrogen atmosphere then TEA (90 µL, 0.6465 mmol, 3.5 equivalents) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (33 mg, 0.2217 mmol, 3.5 equivalents) was added. The reaction was performed according to general procedure H.118 mg pure compound 95 was isolated with a96 % yield.1H NMR (400 MHz, Methanol-d4) δ 7.27 (dd, J = 8.7, 5.3 Hz, 2H), 7.12 (s, 1H), 7.08 (s, 1H), 6.97 (t, J = 8.8 Hz, 2H), 6.57 (s, 1H), 5.85 (s, 1H), 4.54 (s, 2H), 3.66 (s, 3H), 2.85 (t, J = 5.7 Hz, 2H), 2.82 – 2.72 (m, 1H), 2.72 – 2.64 (m, 2H), 1.99 (dt, J = 10.9, 5.8 Hz, 2H), 1.82 – 1.69 (m, 2H), 1.62 (dt, J = 9.1, 4.6 Hz, 2H), 1.57 – 1.48 (m, 2H), 1.41 (s, 9H), 1.28 (s, 2H).HRMS (ESI): calculated m / z (M + H)+for C31H37F2N3O2S, is 553.2575; found, 553.2572. Melting Point = 191°C. Example 96 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-methylpiperidin-4-amine (109 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 216 mg pure compound 96 was isolated with 73% yield.1H NMR (400 MHz, Chloroform-d) δ 7.47 (s, 1H), 7.33 (s, 1H), 7.04 (d, J = 7.9 Hz, 2H), 6.87 (s, 2H), 6.73 (d, J = 8.0 Hz, 2H), 5.90 (d, J = 7.4 Hz, 1H), 5.07 (s, 2H), 4.13 (s, 2H), 3.98 – 3.80 (m, 2H), 3.72 – 3.65 (m, 2H), 3.14 (t, J = 7.4 Hz, 1H), 2.42 (s, 3H), 2.28 (s, 3H), 2.24 (s, 10H), 2.01 (d, J = 12.9 Hz, 2H), 1.64 (t, J = 11.2 Hz, 2H). HRMS (ESI): calculated m / z (M + H)+for C33H38BrN3O2S, is 619.1868; found, 619.1866. Melting Point = 196°C. Example 97 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-2-((mesitylthio)methyl)-1-(4-methylbenzyl) - 1H-indole-3-carboxamide: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (136 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 225 mg pure compound 97 was isolated with 76% yield.1H NMR (400 MHz, Chloroform-d) δ 7.51 (s, 1H), 7.34 (s, 1H), 7.05 (d, J = 7.9 Hz, 2H), 6.86 (s, 2H), 6.74 (d, J = 8.0 Hz, 2H), 5.85 (s, 1H), 5.11 (s, 2H), 4.17 (s, 2H), 3.91 (tt, J = 10.0, 4.9 Hz, 1H), 3.09 (d, J = 11.3 Hz, 2H), 2.54 (t, J = 10.6 Hz, 2H), 2.29 (s, 4H), 2.24 (s, 9H), 2.03 (d, J = 10.6 Hz, 2H), 1.69 (q, J = 13.0, 12.5 Hz, 2H), 1.16 (d, J = 6.5 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C35H42BrN3O2S, is 647.2181; found, 647.2180. Melting Point = 199°C. HPLC purity = 99.98 % Example 98 PT / 2025 / 10975 (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-isopropyl piperazin-1-yl)methanone: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperazine (122 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 230 mg pure compound 98 was isolated with 76% yield.1H NMR (400 MHz, DMSO-d6) δ 9.65 (s, 1H), 7.53 (s, 1H), 7.22 (s, 2H), 7.06 (d, J = 7.9 Hz, 2H), 6.87 (s, 2H), 6.82 (d, J = 8.1 Hz, 2H), 5.33 (s, 2H), 4.18 (s, 2H), 3.55 (s, 1H), 2.75 (s, 2H), 2.23 (s, 6H), 1.72 (s, 3H), 1.41 (s, 3H), 0.95 (s, 6H). HRMS (ESI): calculated m / z (M + H)+for C35H42BrN3O2S, is 633.2025; found, 633.2024. Melting Point = 188°C. Example 99 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H-indole- 3-carboxamide: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (79 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 213 mg pure compound 99 was isolated with 76% yield. HRMS (ESI): calculated m / z (M + H)+for C30H29BrN4O2S, is 588.1195; found, 588.1193. Melting Point = 179°C. Example 100 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1-(4-methylbenzyl) - 1H-indole-3-carboxamide: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (89 mg, 0.9533 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 224 mg pure compound 100 was isolated with 78% yield. HRMS (ESI): calculated m / z (M + H)+for C30H29BrN4O2S, is 602.1351; found, 602.1350. Melting Point = 199°C. Example 101 (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone: To a stirred solution of compound 80 (250 mg, 0.4767 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (435 mg, 1.1440 mmol, 1.2 equivalent), TEA (232 µL, 1.6683 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (89 mg, 0.9533 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 213 mg pure compound 101 was isolated with 74% yield.1H NMR (400 MHz, Chloroform-d) δ 7.32 (s, 1H), 7.05 (t, J = 8.6 Hz, 2H), 6.99 (d, J = 15.5 Hz, 1H), 6.92 (s, 1H), 6.87 (s, 1H), 6.85 (s, 2H), 6.80 (d, J = 7.8 Hz, 1H), 5.27 (d, J = 92.8 Hz, 2H), 4.09 (d, J = 16.6 Hz, 2H), 3.78 – 3.66 (m, 6H), 3.08 – 2.94 (m, 1H), 2.59 – 2.51 (m, 6H), 2.42 (s, 4H), 2.32 (s, 3H), 2.30 (s, 3H), 2.27 (d, J = 7.7 Hz, 4H), 2.23 (s, 3H), 1.86 – 1.79 (m, 2H), 1.55-1.47 (m, 2H). HRMS (ESI): calculated m / z (M + H)+for C36H42BrN3O3S, is 675.2130; found, 675.2128. Melting Point = 189°C. Example 102 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide: To a stirred solution of compound 81 (250 mg, 0.4661 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (425 mg, 1.1185 mmol, 1.2 equivalent), TEA (227 µL, 1.6312 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (89 mg, PT / 2025 / 10975 0.9321 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 228 mg pure compound 102 was isolated with 74% yield.1H NMR (400 MHz, DMSO-d6) δ 9.81 (s, 1H), 8.16 (d, J = 8.2 Hz, 1H), 8.00 (d, J = 7.7 Hz, 1H), 7.83 (d, J = 8.2 Hz, 1H), 7.68 – 7.59 (m, 2H), 7.49 (s, 1H), 7.36 (s, 1H), 7.29 – 7.21 (m, 3H), 7.05 (t, J = 8.9 Hz, 2H), 6.15 (s, 1H), 5.98 (s, 2H), 4.56 (s, 2H), 3.95 – 3.76 (m, 1H), 3.22 – 2.85 (m, 4H), 2.05 – 1.91 (m, 2H), 1.82 – 1.63 (m, 2H), 1.12 (s, 6H). HRMS (ESI): calculated m / z (M + H)+for C35H35BrFN3O2S, is 659.1617; found, 659.1615. Melting Point = 189°C. Example 103 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3- yl)(4-isopropylpiperazin-1-yl)methanone: To a stirred solution of compound 81 (250 mg, 0.4661 mmol, 1.0 Equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (425 mg, 1.1185 mmol, 1.2 Equivalent), TEA (227 µL, 1.6312 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperazine (119 mg, 0.9321 mmol, 2 Equivalents). The reaction was performed according to general procedure J. After column purification 223 mg pure compound 103 was isolated with 74% yield.1H NMR (400 MHz, DMSO-d6) δ 9.78 (s, 1H), 8.09 (d, J = 8.2 Hz, 1H), 7.98 – 7.91 (m, 1H), 7.79 (d, J = 8.3 Hz, 1H), 7.63 – 7.54 (m, 2H), 7.48 (s, 1H), 7.29 – 7.21 (m, 3H), 7.06 – 7.01 (m, 2H), 7.00 (s, 1H), 6.14 (d, J = 7.0 Hz, 1H), 5.94 (s, 2H), 4.33 (s, 2H), 3.44 (dt, J = 18.3, 8.8 Hz, 2H), 3.25 – 3.08 (m, 2H), 2.67 – 2.60 (m, 1H), 2.41 (s, 4H), 0.94 (d, J = 6.5 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C34H33BrFN3O2S, is 645.1461; found, 645.1460. Melting Point = 180°C. Example 104 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-N-(1H-pyrazol- 3-yl)-1H-indole-3-carboxamide: To a stirred solution of compound 81 (250 mg, 0.4661 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (425 mg, 1.1185 mmol, 1.2 equivalent), TEA (227 µL, 1.6312 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (77 mg, 0.9321 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 210 mg pure compound 104 was isolated with 75% yield. HRMS (ESI): calculated m / z (M + H)+for C30H22BrFN4O2S, is 600.0631; found, 600.0629. Melting Point = 190°C. Example 105 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1-(naph thalene-1-ylmethyl)-1H-indole-3-carboxamide: To a stirred solution of compound 81 (250 mg, 0.4661 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (425 mg, 1.1185 mmol, 1.2 equivalent), TEA (227 µL, 1.6312 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-methyl-1H-pyrazol-4-amine (87 mg, 0.9321 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 218 mg pure compound 105 was isolated with 75% yield. HRMS (ESI): calculated m / z (M + H)+for C31H24BrFN4O2S, is 614.0787; found, 614.0785. Melting Point = 188°C. Example 106 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3- yl)(4-morpholinopiperidin-1-yl)methanone: To a stirred solution of compound 81 (250 mg, 0.4661 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (425 mg, 1.1185 mmol, 1.2 equivalent), TEA (227 µL, 1.6312 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 4-(piperidin-4-yl) morpholine (158 mg, 0.9321 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 250 mg pure compound 106 was isolated with 75% yield. HRMS (ESI): calculated m / z (M + H)+for C36H35BrFN3O3S, is 687.1567; found, 687.1567. Melting Point = 189°C. PT / 2025 / 10975 Example 107 (R)-(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(2- (hydroxymethyl)piperazin-1-yl)methanone: To a stirred solution of compound 80 (50 mg, 0.0953 mmol, 1.0 equivalent) in0.2 mL DMF under nitrogen atmosphere, HATU (87 mg, 0.2288 mmol, 1.2 equivalent), TEA (46 µL, 0.3337 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl (R)-3-(hydroxymethyl)piperazine-1- carboxylate (42 mg, 0.1907 mmol, 2 equivalents). The reaction was performed according to the general procedure J to get crude product which was carried forward to the next step Boc deprotection reaction according to general procedure F. After silica gel column purification 33 mg pure compound 107 was isolated with 56 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.87 (d, J = 11.7 Hz, 1H), 7.45 (d, J = 28.7 Hz, 1H), 7.10 (d, J = 8.0 Hz, 3H), 6.90 (s, 1H), 6.83 (d, J = 8.1 Hz, 1H), 6.80 (d, J = 8.1 Hz, 1H), 6.75 (s, 1H), 5.22 (d, J = 10.0 Hz, 2H), 4.30 (s, 2H), 4.22 – 4.14 (m, 1H), 3.36 – 3.23 (m, 1H), 3.10 – 2.98 (m, 2H), 2.96 – 2.83 (m, 1H), 2.32 (s, 6H), 2.30 – 2.27 (m, 3H), 2.27 (s, 2H), 2.25 (s, 4H), 2.15 (s, 3H). HRMS (ESI): calculated m / z (M + H)+for C32H36BrN3O3S, is 621.1661; found, 621.1660. Melting Point = 189°C. Example 108 6-bromo-5-hydroxy-N-(1-methylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio) methyl)-1H-indole-3-carboxamide: To a stirred solution of compound 82 (100 mg, 0.1907 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (174 mg, 0.3813 mmol, 1.2 equivalent), TEA (93 µL, 0.6673 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-methylpiperidin-4-amine (43 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 77 mg pure compound 108 was isolated with 66 % yield. HRMS (ESI): calculated m / z (M + H)+for C33H32BrN3O2S, is 613.1399; found, 613.1398. Melting Point = 197°C. Example 109 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio) methyl)-1H-indole-3-carboxamide: To a stirred solution of compound 82 (100 mg, 0.1907 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (174 mg, 0.3813 mmol, 1.2 equivalent), TEA (93 µL, 0.6673 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (54 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 86 mg pure compound 109 was isolated with 70 % yield. HRMS (ESI): calculated m / z (M + H)+for C33H32BrN3O2S, is 641.1712; found 641.1710. Example 110 (6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone: To a stirred solution of compound 82 (100 mg, 0.1907 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (174 mg, 0.3813 mmol, 1.2 equivalent), TEA (93 µL, 0.6673 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (49 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 83 mg pure compound 110 was isolated with 76 % yield. HRMS (ESI): calculated m / z (M + H)+for C33H32BrN3O2S, is 627.1555; found 627.1550. Melting Point = 187°C. Example 111 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 PT / 2025 / 10975 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-methylpiperidin-4-amine (69 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 87 mg pure stickycompound 111 was isolated with 71 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.40 (s, 1H), 7.24 –7.15 (m, 3H), 6.92 – 6.79 (m, 2H), 4.48 (d, J = 3.9 Hz, 2H), 3.81 (dq, J = 10.5, 5.2 Hz, 1H), 3.57 (d, J = 3.1 Hz, 3H), 2.89 (d, J = 11.0 Hz, 3H), 2.33 (d, J = 2.7 Hz, 3H), 2.20 (t, J = 11.8 Hz, 2H), 1.95 (d, J = 12.9 Hz, 2H), 1.57 (t, J = 11.7 Hz, 2H). HRMS (ESI): calculated m / z (M + H)+for C23H25BrFN3O2S, is 505.0835; found, 505.0834. Example 112 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1H-pyrazol-3-yl)-1H-indole- 3-carboxamide: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 µL, 0.8531 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (41 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 80 mg pure compound 112 was isolated with 69 % yield.1H NMR (400 MHz, Methanol-d4) δ 7.60 (s, 1H), 7.51 (d, J = 2.7 Hz, 1H), 7.20 – 7.16 (m, 2H), 6.84 (s, 1H), 6.78 (t, J = 8.7 Hz, 2H), 5.92 – 5.90 (m, 1H), 4.55 (s, 1H), 4.45 (s, 2H), 3.73 (s, 3H). HRMS (ESI): calculated m / z (M + H)+for C20H16BrFN4O2S, is 474.0161; found, 474.0159. Melting Point = 188°C. Example 113 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H- indole-3-carboxamide: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added N1, N1-dimethylbutane-1, 4-diamine (56 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 80 mg pure compound 113 was isolated with 65 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.41 (d, J = 3.4 Hz, 1H), 7.23 – 7.14 (m, 3H), 6.84 (t, J = 8.7 Hz, 2H), 4.49 (d, J = 7.2 Hz, 2H), 3.58 (s, 3H), 3.26 (d, J = 5.9 Hz, 2H), 2.60 (s, 2H), 2.43 (s, 6H), 1.72 (s, 2H), 1.57 (s, 2H). HRMS (ESI): calculated m / z (M + H)+for C23H27BrFN3O2S, is 507.0991; found, 507.0989. Melting Point = 177 °C. Example 114 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl- 1H-indole-3-carboxamide: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (69 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 86 mg pure compound 114 was isolated with 66 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.39 (s, 1H), 7.23 – 7.13 (m, 3H), 6.84 (t, J = 8.6 Hz, 2H), 4.47 (s, 2H), 3.84 (s, 1H), 3.56 (s, 3H), 3.02 (d, J = 11.1 Hz, 2H), 2.95 (d, J = 6.3 Hz, 1H), 2.47 (t, J = 11.2 Hz, 2H), 2.01 – 1.92 (m, 2H), 1.71 (dd, J = 13.9, 7.0 Hz, 2H), 1.14 (d, J = 6.6 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C25H29BrFN3O2S, is 533.1148; found, 533.1146. Melting Point = 189°C. Example 115 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-isopropyl piperazin-1-yl)methanone: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 PT / 2025 / 10975 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperazine (62 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 83 mg pure compound 115 was isolated with 66 % yield.1H NMR (400 MHz, Acetone-d6) δ 7.58 (s, 1H), 7.41 (dd, J = 8.9, 5.3 Hz, 2H), 7.07 (t, J = 8.9 Hz, 2H), 7.01 (s, 1H), 4.51 (s, 2H), 3.74 (s, 3H), 3.51 – 3.27 (m, 4H), 2.66 (p, J = 6.5 Hz, 1H), 2.44 (d, J = 15.6 Hz, 4H), 0.98 (d, J = 6.6 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C24H27BrFN3O2S, is 520.4614; found, 520.4612. Melting Point = 179°C. Example 116 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)- 1H-indole-3-carboxamide: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 Equivalent), TEA (118 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1H-pyrazol-3-amine (47 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 83 mg pure compound 116 was isolated with 66 % yield. HRMS (ESI): calculated m / z (M + H)+for C21H18BrFN4O2S, is 488.0318; found, 488.0316. Melting Point = 170 °C. Example 117 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone: To a stirred solution of compound 79 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (222 mg, 0.5850 mmol, 1.2 equivalent), TEA (118 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 4-(piperidin-4-yl) morpholine (83 mg, 0.4875 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 96 mg pure compound 117 was isolated with 70 % yield. HRMS (ESI): calculated m / z (M + H)+for C21H18BrFN4O2S, is 488.0318; found, 488.0316. Melting Point = 186 °C. Example 118 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-2-((phenylthio)methyl)-1H-indole-3- carboxamide: To a stirred solution of compound 83 (100 mg, 0.2549 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (232 mg, 0.6118 mmol, 1.2 equivalent), TEA (124 µL, 0.8922 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperidin-4-amine (73 mg, 0.5099 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 109 mg pure compound 118 was isolated with 83 % yield.1H NMR (400 MHz, DMSO-d6) δ 9.67 (s, 1H), 7.68 (s, 1H), 7.35 – 7.26 (m, 5H), 7.25 – 7.19 (m, 1H), 4.71 (s, 2H), 3.96 – 3.76 (m, 1H), 3.68 (s, 3H), 3.25 – 2.67 (m, 4H), 1.95 (s, 2H), 1.66 (s, 2H), 1.12 (s, 6H). HRMS (ESI): calculated m / z (M + H)+for C25H30BrN3O2S, is 515.1242; found, 515.1240. Melting Point = 187°C. Example 119 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4-isopropyl piperazin-1-yl) methanone: To a stirred solution of compound 83 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (232 mg, 0.6118 mmol, 1.2 equivalent), TEA (124 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperazine (63 mg, 0.4850 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 109 mg pure compound 119 was isolated with 83 % yield. HRMS (ESI): calculated m / z (M + H)+for C24H27BrFN3O2S, is 519.0991; found, 519.0989. Melting Point = 195 °C. PT / 2025 / 10975 Example 120 (6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indol-3-yl)(4-morpholinopiperidin-1- yl) methanone: To a stirred solution of compound 79 (100 mg, 0.2549 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (232 mg, 0.6118 mmol, 1.2 equivalent), TEA (124 µL, 0.8922 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 4-(piperidin-4-yl)morpholine (86 mg, 0.5099 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 109 mg pure compound 120 was isolated with 83 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.33 (d, J = 1.7 Hz, 1H), 7.31 (d, J = 1.3 Hz, 2H), 7.29 (s, 1H), 7.24 (s, 1H), 7.22 (s, 1H), 7.20 (s, 1H), 6.93 (s, 1H), 4.51 – 4.39 (m, 2H), 3.84 (s, 2H), 3.70 (s, 2H), 3.64 (s, 3H), 3.54 (s, 2H), 3.00 – 2.93 (m, 1H), 2.75 (s, 2H), 2.51 (s, 2H), 2.47 – 2.40 (m, 2H), 1.89 (dd, J = 14.3, 7.8 Hz, 2H), 1.81 – 1.75 (m, 2H). HRMS (ESI): calculated m / z (M + H)+for C26H30BrN3O2S, is 543.1191; found, 543.1189. Melting Point = 185 °C. Example 121 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)- 1H-indole-3-carboxamide: To a stirred solution of compound 83 (100 mg, 0.2437 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (232 mg, 0.6118 mmol, 1.2 equivalent), TEA (124 µL, 0.8531 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-isopropylpiperazine (47 mg, 0.4850 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 109 mg pure compound 121 was isolated with 83 % yield. HRMS (ESI): calculated m / z (M + H)+for C24H27BrFN3O2S, is 488.0318; found, 488.0316. Melting Point = 187 °C. Example 122 6-bromo-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2-((phenylthio) methyl)-1H-indole-3-carboxamide: To a stirred solution of compound 82 (100 mg, 0.1907 mmol, 1.0 equivalent) in0.5 mL DMF under nitrogen atmosphere, HATU (176 mg, 0.4629 mmol, 1.2 equivalent), DIPEA (120 µL, 0.6753 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-methyl-1H-pyrazol-4-amine (37 mg, 0.3858 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 104 mg compound 122 was isolated with 90 % yield. HRMS (ESI): calculated m / z (M + H)+for C34H35BrN2O2S, is 614.1603; found, 614.1602. Melting Point = 188 °C. Example 123 N-(1-benzylpiperidin-4-yl)-6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indole-3-carboxamide: To a stirred solution of compound 80 (100 mg, 0.1907 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (173 mg, 0.4576 mmol, 1.2 equivalent), DIPEA (120 µL, 0.6673 mmol, 3.5 Equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added 1-benzylpiperidin-4-amine (72 mg, 0.3813 mmol, 2 equivalents).The reaction was performed according to general procedure J. After column purification 119 mg compound 123 was isolated with 90 % yield. HRMS (ESI): calculated m / z (M + H)+for C39H42BrN3O2S, is 695.2181; found, : 695.2179. Melting Point = 197 °C. Example 124 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(piperidin-4-yl)-1H-indole-3- carboxamide: To a stirred solution of compound 80 (100 mg, 0.1907 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (173 mg, 0.4576 mmol, 1.2 equivalent), DIPEA (118 µL, 0.6673 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added piperidin-4-amine (38 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J. After column purification 119 mg compound 124 was PT / 2025 / 10975 isolated with 90 % yield. HRMS (ESI): calculated m / z (M + H)+for C39H42BrN3O2S, is 605.1712; found : 605.1710. Melting Point = 187 °C. Example 125 (4-aminopiperidin-1-yl)(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indol-3-yl)methanone: To a stirred solution of compound 80 (100 mg, 0.1907 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (173 mg, 0.4576 mmol, 1.2 equivalent), DIPEA (118 µL, 0.6673 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added tert-butyl piperidin-4-ylcarbamate (76 mg, 0.3813 mmol, 2 equivalents). The reaction was performed according to general procedure J to get the crude product. This crude product was carried forded to next Boc deprotection. After column purification 53 mg compound 125 was isolated with 40 % yield. HRMS (ESI): calculated m / z (M + H)+for C32H36BrN3O2S, is 605.1712; found, : 605.1710. Melting Point = 187°C, HPLC purity = 99.5 %. Example 126 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalene-1-ylmethyl)-1H-indole-3-carboxamide: To a stirred solution of compound 82 (100 mg, 0.1830 mmol, 1.0 equivalent) in 0.5 mL DMF under nitrogen atmosphere, HATU (166 mg, 0.4392 mmol, 1.2 equivalent), DIPEA (114 µL, 0.6405 mmol, 3.5 equivalents) was added to this reaction mixture and stirred for 10 min at room temperature, and then added piperidin-4-amine (37 mg, 0.3660 mmol, 2 Equivalents). The reaction was performed according to general procedure J to get the crude product. This crude product was carried forward to the next Boc deprotection. After column purification 110 mg compound 126 was isolated with 90 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.92 – 7.88 (m, 2H), 7.76 (s, 1H), 7.69 (d, J = 8.7 Hz, 1H), 7.66 – 7.54 (m, 2H), 7.25 (s, 1H), 7.19 – 7.16 (m, 1H), 7.14 (t, J = 3.7 Hz, 1H), 7.00 (s, 1H), 6.88 (d, J = 7.8 Hz, 1H), 6.46 (d, J = 7.5 Hz, 1H), 6.26 (d, J = 7.1 Hz, 1H), 5.62 (s, 2H), 4.25 (s, 2H), 4.10 (dt, J = 8.1, 3.6 Hz, 1H), 3.12 (d, J = 11.5 Hz, 2H), 3.08 – 3.03 (m, 1H), 2.65 (t, J = 10.7 Hz, 2H), 2.29 (s, 3H), 2.21 (s, 3H), 2.14 (d, J = 11.1 Hz, 2H), 1.96 – 1.89 (m, 2H), 1.20 (d, J = 6.6 Hz, 6H). HRMS (ESI): calculated m / z (M + H)+for C37H40BrN3O2S, is 669.2025; found, : 669.2023. Melting Point = 188 °C. Example 127 Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-(pyrrolidin-3-yloxy)-1H-indole-3- carboxylate: To a stirred solution of compound 15 (500 mg, 1.1407 mmol, 1.0 equivalent) in 2 mL DMF under nitrogen atmosphere, Cs2CO3(929 mg, 2.8519 mmol, 2 equivalent) was added to this reaction mixture and stirred for 15 min at room temperature, and then added tert-butyl 3- bromopyrrolidine-1-carboxylate (571 mg, 2.2815 mmol, 2 equivalents). The crude product was synthesized according to general procedure J. This crude compound (400 mg, 0.6584 mmol, 1.0 equivalent) wasdissolved in DCM (10 mL) then1 mL 4M HCl in 1, 4-Dioxane was added at 0-5ºC. The reaction was performed according to general procedure G. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 317 mg pure compound 127 with a yield of 95 %. Example 128 Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-((1-isopropylpyrrolidin-3-yl)oxy)-1-methyl- 1H-indole-3-carboxylate: To a solution of compound 127 (120 mg, 0.2365 mmol, 1equivalent), NaH (48 mg, 0.2838 mmol, 1.2 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2-Iodopropane (48mg, 0.2838mmol, 1.2 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 117 mg pure compound 128 with a yield of 90 %. HRMS (ESI): calculated m / z (M + H)+for C26H30BrFN2O3S, is 548.1145; found, 548.1141. Melting Point = 189°C. PT / 2025 / 10975 Example 129 Ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3-yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1-methyl- 1H-indole-3-carboxylate: To a solution of compound 127 (120 mg, 0.2365mmol, 1equivalent), NaH (12 mg, 0.2838 mmol, 1.2 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then bromo cyclopentane (42 mg, 0.2838 mmol, 1.2 equivalents)was added. The reaction was performed according to general procedure H. The crude was purified in flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 118 mg pure compound 129 with a yield of 90 %. HRMS (ESI): calculated m / z (M + H)+for C28H32BrFN2O3S, is 574.1301; found, 574.1298. Melting Point = 169°C. Example 130 Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-((1-methylpyrrolidin-3-yl)oxy)-1H- indole-3-carboxylate: 37 % Formaldehyde (24 µL, 0.2365 mmol, 1.2 equivalents) was taken in 0.5 mL AcOH a nitrogen atmosphere and cooled the solution to 0ºC. Then compound 127 (100 mg, 0.1971 mmol, 1 equivalent) was added to this reaction mixture at the same temperature & stirred reaction mixture for 4 hours at room temperature. NaBH(OAc)3 (59 mg, 0.2759 mmol, 1.4 equivalents) was added to this reaction mixture and was stirred the reaction mass overnight at room temperature. The reaction was performed according to general procedure E.92 mg of pure sticky compound 130 was isolated with 90 % yield.1H NMR (400 MHz, Methanol-d4) δ 7.63 (s, 1H), 7.48 (s, 1H), 7.27 – 7.21 (m, 2H), 6.91 (t, J = 8.8 Hz, 2H), 4.90 (dt, J = 6.2, 3.3 Hz, 1H), 4.60 (s, 2H), 4.15 (q, J = 7.1 Hz, 2H), 3.62 (s, 3H), 3.05 – 3.00 (m, 1H), 2.89 (dd, J = 14.1, 6.9 Hz, 2H), 2.67 – 2.61 (m, 1H), 2.44 (s, 3H), 2.37 (dd, J = 13.9, 6.6 Hz, 1H), 2.10 (dd, J = 13.0, 7.4 Hz, 1H), 1.32 (d, J = 7.1 Hz, 3H). HRMS (ESI): calculated m / z (M + H)+for C24H26BrFN2O3S, is 520.0832; found, 520.0830. Example 131 Ethyl 6-bromo-4-((dimethylamino)methyl)-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H- indole-3-carboxylate: 37 % Formaldehyde solution (22 µL, 0.2855 mmol, 1.2 equivalents) was taken in 0.5 mL AcOH in a nitrogen atmosphere and cooled the solution to 0 ºC. Then dimethyl amine (119 µL, 0.3093 mmol, 1.3 equivalents) was added to this reaction mixture at the same temperature & stirred reaction mixture for 4 hours at room temperature. Compound 13 (100 mg, 0.2379 mmol,1 equivalent) was added to this reaction mixture, and the reaction mass was stirred overnight at room temperature. This reaction mixture was stirred for 3 hours. The reaction was performed according to general procedure E.109 mg of the white solid pure Compound 131 (Arbidol / Umifenovir) was isolated with 96 % yield.1H NMR (400 MHz, Chloroform-d) δ 7.40 (s, 1H), 7.32 – 7.30 (m, 1H), 7.26 – 7.23 (m, 4H), 4.49 (s, 2H), 4.18 (q,J = 7.1 Hz, 2H), 4.15 (s, 2H), 3.54 (s, 3H), 2.35 (s, 6H), 1.31 (t, J = 7.2 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C22H25BrN2O3S, is 476.0769; found, 476.0769. Melting Point = 133°C. HPLC purity = 98.27 % Example 132 3-((6-bromo-3-(ethoxycarbonyl)-2-(((4-fluorophenyl)thio)methyl)-1-methyl-1H-indol-5-yl) oxy)- 1,1-dimethylpyrrolidin-1-ium iodide: To a solution of compound 127 (120 mg, 0.2365mmol, 1 equivalent), NaH (12 mg, 0.2838 mmol, 1.2 equivalent) was added at room temperature. The reaction mixture was stirred under a nitrogen atmosphere for 30 minutes and then 2 M methyl Iodide (355 µL, 0.7095 mmol, 3 equivalents) was added. The reaction was performed according to general procedure H. The crude was purified in a flash column using CHCl3, MeOH, as eluents in 230-400 mesh size silica to get 117 mg pure sticky compound 135 with a yield of 90 %.1H NMR (400 MHz, Methanol-d4) δ 7.75 (s, 1H), 7.56 (s, 1H), 7.27 (dd, J = 8.8, 5.4 Hz, 2H), 6.88 (t, J = 8.8 Hz, 2H), 6.03 (s, 1H), 5.36 (s, 1H), 4.26 (q, J = 7.1 Hz, 2H), 4.03 (d, J = 4.9 Hz, 2H), 4.01 (s, 2H), 3.95 (dd, J = 13.6, 6.6 Hz, 2H), 3.81 (td, J = 19.2, 18.1, 7.4 Hz, 2H), 3.65 – 3.57 (m, 1H), 3.47 (s, 3H), 3.35 (s, 3H), 2.87 (dd, J = 15.4, 6.8 Hz, 1H), 2.52 (dt, J = 13.8, 6.7 Hz, 1H), 1.77 (d, J = 7.5 Hz, 3H), 1.37 (t, J = 7.1 Hz, 3H).HRMS (ESI): calculated m / z (M + H)+for C25H29BrFIN2O3S, is 662.0111; found, 662.0111. PT / 2025 / 10975 BIOLOGICAL ASSAY Several structural modification strategies have been applied to improve the physicochemical properties of antiviral drug Arbidol. Arbidol has six different substitutions in the indole scaffold, which is a unique feature among all the drug molecules. These unique features create more attraction for medicinal chemistry-based optimization. The central core of the Arbidol is an indole scaffold that consists of six different groups at the N1, C2, C3, C4, C5, and C6 positions. It has one flexible substitution methyl (phenyl)sulfane group at the C2 position, methyl group at the N1 position, ethyl carboxylate group at the C3position, basic amine N, N dimethyl methyl amine group at C4position, hydroxyl group at C5position, and a bromo substitution at C6 position. The indole core of Arbidol presents enormous opportunities for the development of novel antivirals. For example, basic nitrogen-containing groups such as a piperidine ring are substituted at its C-6 position. For example, basic amine-containing amide derivatives at C3 position of the indole scaffold, basic amine group at C4 position, and a piperidine ring at its C-6 position they are not limited to improving the potency but also improve the solubility. Technically, the stability, solubility, and permeability have been determined with in vitro Absorption, Distribution, Metabolism, and Excretion (ADME), drug toxicity, Caco-2 cell permeability assay, and human Ether-a-go-go Related Gene (hERG) assay. Example 136 Methodology of antiviral assays RT-PCR Based method for Screening Antiviral Compounds 1. VEROE6 cells seeded at a density of 50, 000 cells / well in the 48-well plate. 2. After ~ 12 h, cells are incubated in the presence of 2X concentrations of all compound dilutions at 37°C, 5 % CO2 for 15 min. 3. After 15 min media with compounds is discarded and cells are incubated in the presence of the virus for 1.0 h. The virus culture being used is diluted in the ratio of 1:1000 in DMEM + 5 % FBS media. 4. After 1.0 h, the virus culture is discarded and cells are allowed to grow in the presence of 1X concentration of all the compound dilutions at 37°C, 5 % CO2 for 48 h. 5. After 48 h, the supernatant is collected and processed further for RNA extraction and RT-PCR. 6. Steps for RNA extraction and RT-qPCR RNA extraction is done using a Gsure RNA isolation kit and RT-qPCR is further performed with GCC Diagsure RT-qPCRkit according to kit manufacturer’s protocol. Example 137 Analysis of RT-PCR data ∆Ct for all the samples is calculated using the Ct value difference between Virus control and test samples for the respective fluorophores used. ∆Ct = Ct (Virus Control) – Ct (Test Sample) Example 138 PT / 2025 / 10975 The table given below represents the ∆Ct difference corresponding to the respective percentage of SARS-CoV inactivation. Table:4 ∆Ct Percent SARS-CoV inactivation ∆Ct Percent SARS-CoV inactivation 2 75 3 87.5 4 93.75 5 96.875 6 98.4375 7 99.21875 8 99.60938 9 99.80464 10 99.90234 Example 139 The procedure of Cell-Based ELISA for Screening Antiviral Compounds 1. VEROE6 cells seeded at a density of 10, 000 cells / well in the 96 well plate. 2. After ~ 12 h of cell seeding, compounds are serially diluted (one-fourth dilutions) in DMEM + 2 % FBS media. 3. Cells are incubated in the presence of 2X concentrations of all compound dilutions at 37°C, 5 % CO2 for 15 min. 4. After 15 min media with compounds is discarded and cells are incubated in the presence of the virus for 1.0 h. The virus culture being used is diluted in the ratio of 1:1000 in DMEM + 2 % FBS media. 5. After 1.0 h, the virus culture is discarded and cells are allowed to grow in the presence of 1X concentration of all the compound dilutions at 37°C, 5 % CO2for 24 h. 6. After 24 h, media with compounds is discarded; cells are fixed with 4 % Formalin for 40 min, and taken out from BSL3 for cell-based ELISA. Example 140 Steps for cell-based ELISA a. Washing with 1X PBS b. Blocking in 5 % BSA for 1 h. c. Washing with 1X PBS, Cells permeabilization for 30 min with permeabilization buffer containing 1 % w / v Saponin. d. Washing with 1X PBS, Incubation with HRP-Conjugated Nanobody against spike protein for 1h. e. Washing with 1X PBST, addition of HRP substrate, the addition of stop solution (2N H2SO4) after blue color development, followed by taking absorbance of the yellow color so obtained, at 450 nm. PT / 2025 / 10975 Example 141 Analysis of ELISA data: Estimation of the antiviral potential of a compound corresponds to a reduction in viral content as compared to viral content in cells incubated with the virus in the absence of a test compound. O. D450(Viru )Percent Antigen = s − infected Cells incubated with Test compound X 100O. D450 (Virus − infected cells)The percent antigen content is plotted against the concentrations of the test compound being used in the assay. The half maximal effective concentration (EC50) value from the data is further derived which corresponds to 50 % Inactivation of the virus at that particular concentration. Example 142 Controls used in cell-based ELISA: The validation of the antiviral efficacy of tested compounds is done by comparing the EC50of test compounds concerning the EC50of reported compounds being used against SARS CoV in VERO E6 cells. Table: 5 Compound Reported EC50 in VERO E6 Cells against EC50 from cell-based ELISA SARS CoV-2 Assay Niclosamide < 0.1 µM (Wen et al., 2007) 0.12 ± 0.03 Remdesivir 0.77 µM (Wang et al., 2020) 0.87 ± 0.41 Example 143 Lipophilicity Assay: 1.56 g NaH2PO4.2H2O was dissolved in 0.5 L water in a 1 L beaker. After adjusting pH to 7.4 using NaOH solution, the volume was made up to 1 L. Equal volumes of sodium phosphate buffer (10 mM, pH 7.4) and n-octanol were added to a separation funnel and mixed thoroughly by shaking and inverting the funnel several times. The two layers were allowed to separate overnight and then dispensed in two separate glass bottles.10 mM stock solution was prepared in 100% DMSO and stored at 4oC. 495 µL of the organic phase (1-octanol) was added to each well of a 2 mL deep well plate, followed by 495 µL of buffer and 10 µL of test substance was added. The plate was incubated for 3 hr at room temperature on a plate shaker at 500 rpm. After incubation, the samples were allowed to equilibrate for 20 min and then centrifuged at 4000 rpm for 30 min for complete phase separation and analyzed by LC-UV. Log D = Log (area of octanol / area of buffer) Table: 6 Comp No LogD 23 3.03 87 3.54 PT / 2025 / 10975 31 3.76 52 3.24 97 3.95 Ketoconazole 3.43 (Control) Metroprolol -0.32 (Control) Propranolol 1.12 (Control) Log D Criteria: <0: Low lipophilicity; 0-1: Moderate lipophilicity; >2: High lipophilicity Example 144 Mouse Plasma stability: 1 mM stock of test compound was prepared in Acetonitrile: water by diluting from 10 mM stock (i.e. 10 µL of 10 mM stock solution was added to 90 µL of Acetonitrile: water (50:50)). 50 µM stock of test compound was prepared in Acetonitrile: water by diluting from 1mM stock (i.e.5 µL of 1mM stock solution was added to 95 µL of Acetonitrile: water (50:50)). The frozen plasma was thawed at room temperature and centrifuged at 1400 rpm at 4 ºC, for 15 minutes. Approximately 90% of the clear supernatant fraction was transferred to a separate tube and was used for the assay. The final working stock of 2 µM was prepared by diluting in plasma ((i.e. 16 µL of 50 µM Acetonitrile: water stock was added to 384 µL of plasma). 300 µL of plasma containing the test compound was incubated for 120min at 37 ºC in a shaker water bath with gentle shaking.25 µL aliquot of the sample at 0,10,30, 60, and 120 min was precipitated immediately with 200 µL of acetonitrile containing internal standard and centrifuged at 4000x RCF, 4ºC for 20 minutes.150 µL of supernatant was diluted with 150 µL of water and analyzed by LC-MS / MS. Table: 7 Comp No Mean % remaining at 2 hrs in mouse Plasma 23 110.6 % 87 103 % 31 61.61 % 52 100.3 % Propanthalene (Control) 17.44 Example 145 Human Plasma stability: 1 mM stock of test compound was prepared in Acetonitrile: water by diluting from 10 mM stock (i.e. 10 µL of 10 mM stock solution was added to 90 µL of Acetonitrile: water (50:50)). 50 µM stock of test compound was prepared in Acetonitrile: water by diluting from 1mM stock (i.e.5 µL of 1mM stock solution was added to 95 µL of Acetonitrile: water (50:50)). The frozen plasma was thawed at room temperature and centrifuged at 1400x RCF 4ºC, for 15 minutes. Approximately 90% of the clear supernatant fraction was transferred to a separate tube and was used for the assay. The final working stock of 2 µM was prepared by diluting in plasma ((i.e. 16 µL of 50 µM Acetonitrile: water stock was added to 384 µL of plasma). 300 µL of plasma containing the test PT / 2025 / 10975 compound was incubated for 120min at 37 ºC in a shaker water bath with gentle shaking.25 µL aliquot of the sample at 0,10,30, 60, and 120 min was precipitated immediately with 200 µL of acetonitrile containing internal standard and centrifuged at 4000x RCF, 4ºC for 20 minutes.150 µL of supernatant was diluted with 150 µL of water and analyzed by LC-MS / MS. Table: 8 Comp No Mean % remaining at 2 hrs in Human Plasma 23 80.3 % 87 96.8 % 31 98.65 % 52 94.53 % Propanthalene (Control) 17.44 Example 146 In-Vitro Evaluation of Metabolic Stability Using Human Liver Microsomes (Human Liver Microsomal Stability-HLM) Assay Procedure: 1mM stock solution of the test compound was prepared in DMSO and diluted with Acetonitrile:Water (1:1) to get a 100µM working concentration.100 mL of Milli Q water was added to K2HPO4 (1.398 g) and KH2PO4 (0.27g) to get the final pH 7.4 solution of potassium phosphate buffer. 3.333mg / mL microsomal suspension was prepared by diluting 499.95 µL of 20mg / mL microsomal stock to 2500.05µL with buffer.532.5µL of 16mM NADPH stock was added to 2467.5µL of potassium phosphate buffer to get 2.84mM working stock. 75µL of 3.333mg / mL working stock of liver microsomes and 85µL of buffer were added to 2.5 µL of test compounds (100 µM). The above mixture was pre-incubated for 15 minutes at 37 ºC. After pre-incubation, 32.5 µL of the mixture was added to 17.5µL of buffer, this was incubated for 60 minutes at 37 ºC [60 min Without Cofactor (NADPH)]. 16.25µL of the pre-incubated mixture and 8.75µL of cofactor were added to 150µL of acetonitrile containing internal standard [0 min Sample]. 62µL of cofactor was added to the remaining pre- incubation mixture [Incubation mixture].25µL of incubation mixture at 0,5, 15, 30, 60 min, and 60 min without cofactor were precipitated with 150 µL of acetonitrile containing internal standard, vortexed, and centrifuged at 4000 rpm at4ºC for 20 minutes.120 µL of supernatant was diluted with 120 µL of water and analyzed by LC-MS / MS [sample preparation]. Table: 9 Comp No Half life (min) 23 31.31 87 9.703 31 28.29 52 89.78 Verapamil (Control) 5.946 Example 147 In-Vitro Evaluation of Metabolic Stability Using Mouse Liver Microsomes (Mouse Liver Microsomal Stability-HLM) Assay Procedure: 1mM stock solution of the test compound was prepared in DMSO and diluted with Acetonitrile:Water (1:1) to get a 100µM working concentration.100 mL of Milli Q water was added to K2HPO4 (1.398 g) and KH2PO4 (0.27g) to get the final pH 7.4 solution of potassium phosphate buffer. 3.333mg / mL microsomal suspension was prepared by diluting 499.95 µL of 20mg / mL microsomal PT / 2025 / 10975 stock to 2500.05µL with buffer.532.5µL of 16mM NADPH stock was added to 2467.5µL of potassium phosphate buffer to get 2.84mM working stock. 75µL of 3.333mg / mL working stock of liver microsomes and 85µL of buffer were added to 2.5 µL of test compounds (100 µM). The above mixture was pre-incubated for 15 minutes at 37 ºC. After pre-incubation, 32.5 µL of the mixture was added to 17.5µL of buffer, this was incubated for 60 minutes at 37 ºC [60 min Without Cofactor (NADPH)]. 16.25µL of the pre-incubated mixture and 8.75µL of cofactor were added to 150µL of acetonitrile containing internal standard [0 min Sample]. 62µL of cofactor was added to the remaining pre- incubation mixture [Incubation mixture].25µL of incubation mixture at 0,5, 15, 30, 60 min, and 60 min without cofactor were precipitated with 150 µL of acetonitrile containing internal standard, vortexed, and centrifuged at 4000 rpm at4ºC for 20 minutes.120 µL of supernatant was diluted with 120 µL of water and analyzed by LC-MS / MS [sample preparation]. Table: 10 Comp No Half life (min) 23 7.168 87 5.732 31 42.73 52 120 97 120 Verapamil (Control) 5.946 Example 148 In-vitro evaluation of cardiotoxicity through hERG channel binding: Assay Protocol to measure hERG Activity: The hERG Fluorescence Polarization Assay was performed using the Predictor™ Herg Fluorescence Polarization Assay Kit by Invitrogen (cat no. PV5365). The kit includes Predictor™ hERG Tracer Red (250 nM), Predictor™ hERG Membrane, Predictor™ hERG FP Assay Buffer, and E-4031 (positive control). The kit components were thawed at room temperature and the hERG membrane was mixed before adding to the assay plate. The 4 nM tracer was prepared by diluting the Predictor™ hERG Tracer Red by 62.5-fold and the 120 μM E-4031 was prepared by diluting the stock. The test compounds were prepared as 10 mM DMSO stocks. The compounds were first diluted 3.33 fold in 100% DMSO and further diluted for six concentrations in 100% DMSO. A dilution series of E-4031 was prepared in 4% DMSO assay buffer as a reference compound. During the assay, buffer or compound was added first, followed by membrane and tracer. The assay plate was incubated at 25°C for 4 h and fluorescence polarization was measured using EnVision (Perkin Elmer) with a set of polarized filters. The obtained mp values were used to calculate the % inhibition and the IC50of the potent compounds was calculated using Graph Pad Prism software. Table: 11 Compound No IC50(µM) 131 0.54 31 > 30 131a 0.54 118 7.09 112 > 30 132 1.79 113 9.50 102 >9.49 103 3.73 100 > 30 PT / 2025 / 10975 40 > 30 99 > 30 97a 10.58 101 15.89 121 > 30 120 13.04 Control 9.5 - 95 nM ADVANTAGES OF THE INVENTION The compounds of the present invention having Formula I have several advantages including: 1. Compounds having Formula I have potent inhibitory activity against SARS-CoV-2. 2. Compound having Formula I have nitrogen-containing substituents at C-6 (R5) and / or C-3 (R3) and C-5 (R4) positions showing inhibitory activity against SARS-CoV-2. 3. Compound having Formula I have potent inhibitory activity in the cell-based assay in SARS- CoV-2 infected VERO E6 cells. 4. Compounds having Formula I can have inhibitory potency in against other viruses. 5. Compound having Formula I showed improvement in toxicity and DMPK profile as compared to Arbidol / Umifenovir. 6. Compound having Formula I have improved hERG-related toxicity profile as compared to Arbidol / Umifenovir. 7. Compound having Formula I as claimed in claim 1 with a basic amine group containing pro- drug property. 8. Compound having Formula I as claimed in claim 1 for use in several clinical applications, including pharmaceutical agents and methods for treating other viral disease conditions.

Claims

PT / 2025 / 10975 WE CLAIM 1. A compound of formula I, salts and metabolite thereof,wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO, napthyl and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is selected from the group consisting of ethyl ester, tertbutyl amide, N-(1-methylpiperidin-4-yl) amide, N-(1-isopropylpiperidin-4-yl) amide, N-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-(1- isopropyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-((dimethylamino)methyl) amide, N- ((dimethylamino)ethyl) amide, N-((dimethylamino)propyl) amide, N-((methylamino)ethyl) amide, N- (1-methylpyrrolidin-3-yl)amide, N-(2-(piperidin-1-yl)ethyl)amide; R4 is selected from the group consisting of OH, OR’4, and OCOR’4, wherein R’4 is substituted or unsubstituted 5 to 6 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle; and R5 is Br or a substituted or unsubstituted aminoalkyl or a 5 to 6 membered N containing heterocycle, wherein the substituents are selected from the group consisting of alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino; wherein at least one of R3, R4 or R5 is a nitrogen containing substituent.

2. The compound as claimed in claim 1, wherein R4 is selected from the group consisting of:

3. The compound as claimed in claim 1, wherein R5 is selected from the group consisting of:PT / 2025 / 109754. The compound as claimed in claim 1, selected from a group consisting of: Ethyl 6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H- indole-3-carboxylate (26). Ethyl 6-bromo-2-(((4-fluorophenyl)thio) methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)- 1H-indole-3-carboxylate (28a). Ethyl 6-bromo-2-(((4-fluoro-2-methylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (29a). Ethyl 6-bromo-5-hydroxy-2-((mesitylthio) methyl)-1-(naphthalen-1-ylmethyl)-1H- indole-3-carboxylate (30a). Ethyl 6-bromo-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate (31). Ethyl 6-bromo-2-(((2,4-dimethylphenyl) thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxylate hydrochloride (31a). Ethyl 1-benzyl-6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-hydroxy-2-((phenyl thio)methyl)-1H-indole-3-carboxylate (37) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-2-((phenylthio)methyl)-1H- indole-3-carboxylate (40) Ethyl6-(1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4- dimethylphenyl)thio)meth yl)-5-hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate (42) Ethyl 5-hydroxy-6-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxylate (45) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (48) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(piperidin-4-yl)-1H-indole-3- carboxylate hydrochloride (48a)PT / 2025 / 10975 Ethyl 5-hydroxy-1-methyl-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate (49) Ethyl 5-hydroxy-1-methyl-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-1H- indole-3-carboxylate hydrochloride (49a) Ethyl 2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate (50) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate (51) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (51a) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (52) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((phenylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate hydrochloride (52a) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-2-((mesitylthio)methyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)- 1H-indole-3-carboxylate (53) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate (54) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1,2,3,6-tetra hydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (54a) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6- tetrahydro pyridin-4-yl)-1H-indole-3-carboxylate (55) Ethyl 5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-6-(1,2,3,6-tetrahydropyridin-4- yl)-1H-indole-3-carboxylate (56) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6- tetrahy dropyridin-4-yl)-1H-indole-3-carboxylate (57) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-1-(4-methylbenzyl)-6-(1,2,3,6- tetrahy dropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (57a) Ethyl 5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-6-(1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate (58) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-6-(1,2,3,6- tetra hydropyridin-4-yl)-1H-indole-3-carboxylate (59) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-6-(1,2,3,6- tetra hydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (59a) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1-methyl-1,2,3,6- tetrahydropyridin-4-yl)-1H-indole-3-carboxylate (60)PT / 2025 / 10975 Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4- yl)-1-methyl-1H-indole-3-carboxylate (61) Ethyl 2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4- yl)-1-methyl-1H-indole-3-carboxylate hydrochloride (61a) Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4-fluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate (62) Ethyl 5-hydroxy-1-methyl-6-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-2-phenylthio)methyl)- 1H-indole-3-carboxylate (63) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-methyl-2-((phenylthio) methyl)-1H-indole-3-carboxylate (64) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-methyl-2-((phenylthio) methyl)-1H-indole-3-carboxylate hydrochloride (64a) Ethyl 6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio)methyl)-5- hydroxy-1-methyl-1H-indole-3-carboxylate (65) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridine-4-yl)-1-methyl-1H-indole-3-carboxylate (66) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydro pyridine-4-yl)-1-methyl-1H-indole-3-carboxylate hydrochloride (66a) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((phenylthio) methyl)-1H-indole-3-carboxylate (67) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((phenylthio) methyl)-1H-indole-3-carboxylate hydrochloride (67a) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((mesitylthio) methyl)-1H-indole-3-carboxylate (68) Ethyl 1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2- ((mesitylthio) methyl)-1H-indole-3-carboxylate hydrochloride (68a) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl- 1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3-carboxylate (69) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-1-(4-fluorobenzyl)-5-hydroxy-6-(1-isopropyl- 1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-3-carboxylate hydrochloride (69a) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate (70) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (70a) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin- 4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate (71)PT / 2025 / 10975 Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin- 4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (71a) Ethyl 6-(1-cyclohexyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate (72) Ethyl 6-(1-cyclohexyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-dimethylphenyl)thio)methyl)-5- hydroxy-1-(4-methylbenzyl)-1H-indole-3-carboxylate hydrochloride (72a) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-methyl-1,2,3,6-tetrahydropyridin- 4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate (73) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxylate (74) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-2-((mesitylthio)methyl)-1-(4- methylbenzyl)-1H-indole-3-carboxylate hydrochloride (74a) Ethyl 5-hydroxy-6-(1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxylate (75) Ethyl 2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyridin-4-yl)-1-(naphthalen-1-ylmethyl)-1H-indole-3-carboxylate (76) Ethyl 2-(((4-fluoro-2-methylphenyl)thio)methyl)-5-hydroxy-6-(1-isopropyl-1,2,3,6- tetrahydropyri din-4-yl)-1-(4-methylbenzyl)-1H-indole-3-carboxylate (77) 6-bromo-N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide (85) 6-bromo-N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3- carboxamide (86) 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indole-3- carboxamide (87) 6-bromo-N-(tert-butyl)-5-hydroxy-2-((mesitylthio)methyl)-1-(naphthalen-1-ylmethyl)-1H- indole-3-carboxamide (88) 6-bromo-N-(tert-butyl)-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1- ylmethyl)-1H-indole-3-carboxamide (89) N-(tert-butyl)-2-(((2,4-difluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydro pyridin-4-yl) -1H-indole-3-carboxamide (92) N-(tert-butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-6-(1,2,3,6-tetrahydro Pyridin-4-yl)-1H-indole-3-carboxamide (93) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((2,4-difluorophenyl)thio) methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxamide (94) N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4- fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxamide (95)PT / 2025 / 10975 N-(tert-butyl)-6-(1-cyclopentyl-1,2,3,6-tetrahydropyridin-4-yl)-2-(((4- fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxamide hydrochloride (95a) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)- 1H-indole-3-carboxamide (96) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)- 1H-indole-3-carboxamide hydrochloride (96a) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-2-((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indole-3-carboxamide (97) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-2-((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indole-3-carboxamide hydrochloride (97a) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4- isopropylpiperazin-1-yl)methanone (98) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide (99) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide hydrochloride (99a) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1-(4- methylbenzyl)-1H-indole-3-carboxamide (100) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1-(4- methylbenzyl)-1H-indole-3-carboxamide hydrochloride (100a) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone(101) (6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(4-morpholino piperidin-1-yl)methanone hydrochloride (101a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide (102) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide hydrochloride (102a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3- yl)(4-isopropylpiperazin-1-yl)methanone (103) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3- yl)(4-isopropylpiperazin-1-yl)methanone hydrochloride (103a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-N-(1H- pyrazol-3-yl)-1H-indole-3-carboxamide (104) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide (105)PT / 2025 / 10975 (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-(naphthalen-1-ylmethyl)-1H-indol-3- yl)(4-morpholinopiperidin-1-yl)methanone (106) (R)-(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H-indol-3-yl)(2- (hydroxymethyl)piperazin-1-yl)methanone (107) 6-bromo-5-hydroxy-N-(1-methylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl) -1H-indole-3-carboxamide (108) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)meth yl)-1H-indole-3-carboxamide (109) (6-bromo-5-hydroxy-1-(naphthalen-1-ylmethyl)-2-((phenylthio)methyl)-1H-indol-3-yl)(4- isopro pylpiperazin-1-yl)methanone(110) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide (111) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methylpiperidin-4-yl)-1H- indole-3-carboxamide hydrochloride (111a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1H-pyrazol-3-yl)-1H- indole-3-carboxamide (112) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl- 1H-indole-3-carboxamide (113) 6-bromo-N-(4-(dimethylamino)butyl)-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl- 1H-indole-3-carboxamide hydrochloride (113a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl- 1H-indole-3-carboxamide (114) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl- 1H-indole-3-carboxamide hydrochloride (114a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4- isopropylpipera zin-1-yl)methanone(115) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)- 1H-indole-3-carboxamide (116) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4- morpholinopipe ridin-1-yl)methanone(117) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-2-((phenylthio)methyl)-1H-indole- 3-carboxamide (118) 6-bromo-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1-methyl-2-((phenylthio)methyl)-1H-indole- 3-carboxamide hydrochloride (118a) (6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-1H-indol-3-yl)(4- isopropylpipera zin-1-yl)methanone(119)PT / 2025 / 10975 (6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indol-3-yl)(4-morpholinopiperidin- 1-yl)methanone (120) (6-bromo-5-hydroxy-1-methyl-2-((phenylthio)methyl)-1H-indol-3-yl)(4-morpholinopiperidin- 1-yl) methanone dihydrochloride (120a) 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-hydroxy-1-methyl-N-(1-methyl-1H-pyrazol-4-yl)- 1H-indole-3-carboxamide (121) 6-bromo-5-hydroxy-N-(1-methyl-1H-pyrazol-4-yl)-1-(naphthalen-1-ylmethyl)-2- ((phenylthio)methyl)-1H-indole-3-carboxamide (122) N-(1-benzylpiperidin-4-yl)-6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)- 1H-indole-3-carboxamide (123) 6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-N-(piperidin-4-yl)-1H-indole- 3-carboxamide (124) (4-aminopiperidin-1-yl)(6-bromo-5-hydroxy-2-((mesitylthio)methyl)-1-(4-methylbenzyl)-1H- indol-3-yl)methanone (125) 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide(126) 6-bromo-2-(((2,4-dimethylphenyl)thio)methyl)-5-hydroxy-N-(1-isopropylpiperidin-4-yl)-1- (naphthalen-1-ylmethyl)-1H-indole-3-carboxamide hydrochloride (126a) Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-(pyrrolidin-3-yloxy)-1H-indole-3- carboxylate (127) Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-5-((1-isopropylpyrrolidin-3-yl)oxy)-1-methyl- 1H-indole-3-carboxylate (128) Ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3-yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1- methyl-1H-indole-3-carboxylate (129) Ethyl 6-bromo-5-((1-cyclopentylpyrrolidin-3-yl)oxy)-2-(((4-fluorophenyl)thio)methyl)-1- methyl-1H-indole-3-carboxylate hydrochloride (129a) Ethyl 6-bromo-2-(((4-fluorophenyl)thio)methyl)-1-methyl-5-((1-methylpyrrolidin-3-yl)oxy)- 1H-indole-3-carboxylate (130) and 3-((6-bromo-3-(ethoxycarbonyl)-2-(((4-fluorophenyl)thio)methyl)-1-methyl-1H-indol-5- yl)oxy)-1, 1-dimethylpyrrolidin-1-ium iodide (135).

5. The compound as claimed in claim 1, wherein the salt is a hydrochloride or quaternary ammonium salt having inhibitory activity against SARS CoV-2.

6. A process for the preparation of the compound of formula I as claimed in claim 1, comprising: a) treating 1, 4 Benzoquinone (A) with ethyl (Z)-3-aminobut-2-enoate (B) to produce a substituted indole C;PT / 2025 / 10975b) dissolving the substituted indole C and pyridine in dry DCM and acetic anhydride under a nitrogen atmosphere to produce D;c) treating D with alkyl or 4-substituted benzyl bromide to produce intermediate E, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph;d) heating the intermediate E in CCl4 in the presence of a bromination reagent to produce F, wherein R1is as defined above;e) adding F to the reaction mixture of benzothiol or substituted benzothiol in presence of a solvent system to produce ester intermediate G, wherein the substituent Y is selected from the group consisting of H, alkyl, alkoxy, haloalkyl, haloalkoxy and halo; and R1 is as defined above;f) to the intermediate G adding aqueous solution of K3PO4 and boronic ester tert-butyl 4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1-methyl-4- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2and Xantphos and extracting with ethyl acetate to obtain the protected compound H followed by deprotecting H by stirring in DCM and HCl in 1,4-Dioxane to produce amine compound I and treating I with R’2- X’, wherein R’2is alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino and X’ is a halo to obtain J, wherein J is the compound of formula I, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy,PT / 2025 / 10975 haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2 is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is ethyl ester, R4 is OH and R5 is 3, 4 unsaturated piperidine optionally substituted with alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl or morpholino;g) alternatively treating the ester intermediate G, in a 3:1 EtOH and water solution in a nitrogen atmosphere with NaOH to produce the acid intermediate K; heating the intermediate K in DMF with tert butyl amine, HATU, and DIPEA to produce L wherein R3 is tert butyl amine R1 and Y are as define above,followed by adding aqueous solution of K3PO4and compound L, boronic ester tert-butyl 4- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydropyridine-1(2H)-carboxylate or 1- methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole in 1,4-Dioxane, Pd(PPh3)2Cl2 and Xantphos and extracting with ethyl acetate to obtain the protected compound M followed by deprotecting M by stirring in DCM and HCl in 1,4-Dioxane to produce N and treating N with R’2- X’, wherein R’2 is alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl and morpholino and X’ is a halo to obtain O, wherein N and O are the compound of formula I, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2 is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3is a tert butyl amine, R4is OH and R5is 3, 4 unsaturated piperidine optionally substituted with alkyl, benzyl alkyl, cycloalkyl, aminoalkyl, heterocycloalkyl or morpholino; h. alternatively treating the acid intermediate K in DMF with an amine selected from 1- benzylpiperidin-4-amine or 1-benzylpiperidin-4-amine or piperidin-4-amine or tert butyl aminePT / 2025 / 10975 or 1-isopropyl piperazine and 4-(piperidin-4-yl) morpholin or 1-methyl-1H-pyrazol-4-amine, in presence of HATU, and DIPEA to produce P, wherein P is the compound of formula I, wherein R1 is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and halo; R3 is selected from N-(1-methylpiperidin-4-yl) amide, N-(1- isopropylpiperidin-4-yl) amide, N-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-(1- isopropyl-1,2,3,6-tetrahydropyridin-4-yl) amide, N-((dimethylamino)methyl) amide, N- ((dimethylamino)ethyl) amide, N-((dimethylamino)propyl) amide, N-((methylamino)ethyl) amide, N-(1-methylpyrrolidin-3-yl)amide and N-(2-(piperidin-1-yl)ethyl)amide, R4is OH and R5 is Br;i. alternatively treating the ester intermediate G with a Br-R4, wherein R4 is substituted or unsubstituted 5 to 6 membered N containing heterocycle; OR’4, and OCOR’4, wherein R’4is substituted or unsubstituted 5 to 6 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle to produce S, wherein S is the compound of formula I, wherein R1is alkyl or aryl alkyl, wherein the aryl group is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, halo, amino, hydroxy alkyl, CHO, napthyl and Ph; R2is thiophenol optionally substituted with one or more substituents independently selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy and is R4 is as defined and is Br.. The as claimed in claim 6, wherein in i ester intermediate G is treated with Br-R4,wherein R4is a substituted or unsubstituted 5 to 7 membered N containing heterocycle; wherein the substituents are selected from the group consisting of alkyl, halo, hydroxyalkyl and N containing heterocycle, Cs2CO3 in DMF to produce Q and treating Q is with an R’4-X’ wherein R’4 is a alkyl or cycloalkyl group and X’ is a halo to obtain R.

8. The process as claimed in claim 6, wherein the bromination agent in step d in Bromine.

9. The process as claimed in claim 6, wherein the solvent system in step e comprises of KOH in hexane and MeOH.

10. A pharmaceutical composition comprising the compound of formula I as claimed in claim 1 and pharmaceutically acceptable excipient.

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