SG11201804671SA - Aza-benzimidazole inhibitors of pad4 - Google Patents

Aza-benzimidazole inhibitors of pad4

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Publication number
SG11201804671SA
SG11201804671SA SG11201804671SA SG11201804671SA SG11201804671SA SG 11201804671S A SG11201804671S A SG 11201804671SA SG 11201804671S A SG11201804671S A SG 11201804671SA SG 11201804671S A SG11201804671S A SG 11201804671SA SG 11201804671S A SG11201804671S A SG 11201804671SA
Authority
SG
Singapore
Prior art keywords
international
oxfordshire
abingdon
milton
park
Prior art date
Application number
SG11201804671SA
Inventor
Rajesh Devraj
Gnanasambandam Kumaravel
Laura Gleave
Adrian Kotey
Thomas Krulle
Cristina Lecci
Heather Tye
Ian Wigginton
Original Assignee
Padlock Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Padlock Therapeutics Inc filed Critical Padlock Therapeutics Inc
Publication of SG11201804671SA publication Critical patent/SG11201804671SA/en

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau ristsplid (43) International Publication Date .... .....r .,„.1 15 June 2017(15.06.2017) WIPO I PCT ID Hit (10) WO 1111111111111111111111111111 International III 2017/100601 Publication IIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIII Al Number (51) International Patent Classification: TON, Ian; 114 Innovation Drive, Milton Park; Abingdon A61K 31/4188 (2006.01) CO7D 235/00 (2006.01) Oxfordshire OX14 4RZ (GB). A61K 31/407 (2006.01) CO7D 471/04 (2006.01) CO7D 209/00 (2006.01) CO7D 487/04 (2006.01) (74) Agents: REID, Andrea L.C. et al.; One International Place, 40th Floor, 100 Oliver Street, Boston, Massachu- (21) International Application Number: setts 02110-2605 (US). PCT/US2016/065865 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 9 December 2016 (09.12.2016) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (25) Filing Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (26) Publication Language: English HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (30) Priority Data: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 62/264,919 9 December 2015 (09.12.2015) US NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (71) Applicant: PADLOCK THERAPEUTICS, INC. RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, [US/US]; Route 206 & Province Line Road, Princeton, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, New Jersey 08543-4000 (US). ZA, ZM, ZW. (72) Inventors: DEVRAJ, Rajesh; 301 Palomino Hill Court, (84) Designated States (unless otherwise indicated, for every Chesterfield, Missouri 63005 (US). KUMARAVEL, Gna- kind of regional protection available): ARIPO (BW, GH, nasambandam; 21 Appletree Lane, Lexington, Massachu- GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, setts 02420 (US). GLEAVE, Laura; 114 Innovation TJ, TM), European AT, BE, BG, CH, CY, CZ, DE, Drive, Milton Park; Abingdon Oxfordshire OX14 4RZ (AL, KOTEY, Adrian; 114 Innovation Drive, Milton DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, (GB). LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Park; Abingdon Oxfordshire OX14 4RZ (GB). KRULLE, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Thomas; 114 Innovation Drive, Milton Park; Abingdon GW, KM, ML, MR, NE, SN, TD, TG). Oxfordshire OX14 4RZ (GB). LECCI, Cristina; 114 In- novation Drive, Milton Park; Abingdon Oxfordshire OX14 Published: 4RZ (GB). TYE, Heather; 114 Innovation Drive, Milton — with international search report (Art 21(3)) Park; Abingdon Oxfordshire OX14 4RZ WIGGIN- (GB). 1-1 .4t 11 C::: , 0 0 1-1 IN 1-1 0 ei (54) Title: AZA-BENZIMIDAZOLE INHIBITORS OF PAD4 ci ) (57) : The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treat- ing PAD4-related disorders.
SG11201804671SA 2015-12-09 2016-12-09 Aza-benzimidazole inhibitors of pad4 SG11201804671SA (en)

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CN109071497B (en) 2016-02-23 2021-10-22 帕德罗科治疗公司 PAD4 heteroaryl inhibitors
JP6987843B2 (en) 2016-07-27 2022-01-05 パドロック・セラピューティクス・インコーポレイテッドPadlock Therapeutics, Inc. Covalent inhibitor of PAD4
CN110248934B (en) 2016-09-12 2022-05-24 帕德罗科治疗公司 Heteroaryl PAD4 inhibitors
WO2020033520A1 (en) * 2018-08-08 2020-02-13 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
US20220402950A1 (en) * 2018-08-08 2022-12-22 Bristol-Myers Squibb Company Substituted benzimidazoles as pad4 inhibitors
US11981680B2 (en) 2018-08-08 2024-05-14 Bristol-Myers Squibb Company Substituted thienopyrroles as PAD4 inhibitors
JP2023512557A (en) * 2020-02-06 2023-03-27 ブリストル-マイヤーズ スクイブ カンパニー Macrocyclic PAD4 inhibitors useful as immunosuppressants
TW202140477A (en) * 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 Heterocyclic pad4 inhibitors
WO2021222353A1 (en) 2020-04-30 2021-11-04 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases

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