SG11201804668UA - Bicyclic inhibitors of pad4 - Google Patents
Bicyclic inhibitors of pad4Info
- Publication number
- SG11201804668UA SG11201804668UA SG11201804668UA SG11201804668UA SG11201804668UA SG 11201804668U A SG11201804668U A SG 11201804668UA SG 11201804668U A SG11201804668U A SG 11201804668UA SG 11201804668U A SG11201804668U A SG 11201804668UA SG 11201804668U A SG11201804668U A SG 11201804668UA
- Authority
- SG
- Singapore
- Prior art keywords
- abingdon
- oxfordshire
- drive
- milton park
- innovation
- Prior art date
Links
- 125000002619 bicyclic group Chemical group 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102220240796 rs553605556 Human genes 0.000 abstract 2
- 230000008520 organization Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A61K31/4353—Heterocyclic 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
- A61K31/437—Heterocyclic 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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Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau res., 00) (43) International Publication Date ..... ..sr ,„,„.1 15 June 2017(15.06.2017) WIPO I PCT II (10) 11111111111111111111 WO International IIIII IIIII II III 2017/100594 IIIIIIIIIIIIIIIIIIII Publication IIIIIIIII Al Number RIO IIII IIIIIIII (51) International Patent Classification: OX14 4RZ (GB). MONCK, Nat; 114 Innovation Drive, A61P 19/02 (2006.01) CO7D 401/14 (2006.01) Milton Park; Abingdon Oxfordshire OX14 4RZ (GB). A61K 31/00 (2006.01) CO7D 471/04 (2006.01) NORTH, Carl; 114 Innovation Drive, Milton Park; A61P 35/00 (2006.01) Abingdon Oxfordshire OX14 4RZ (GB). PALFREY, Jordan; 114 Innovation Drive, Milton Park; Abingdon Ox- (21) International Application Number: fordshire OX14 4RZ (GB). PARROTT, Shelley; 114 In- PCT/US2016/065857 novation Drive, Milton Park; Abingdon Oxfordshire OX14 (22) International Filing Date: 4RZ (GB). RIDGILL, Mark; 114 Innovation Drive, 9 December 2016 (09.12.2016) Milton Park; Abingdon Oxfordshire OX14 4RZ (GB). TYE, Heather; 114 Innovation Drive, Milton Park; Abing- (25) Filing Language: English don Oxfordshire OX14 4RZ (GB). (26) Publication Language: English (74) Agents: REID, Andrea L.C. et al.; Dechert LLP, One In- (30) Priority Data: ternational Place, 40th Floor, 100 Oliver Street, Boston, 62/264,925 9 December 2015 (09.12.2015) US MA 02110-2605 (US). (71) Applicant: PADLOCK THERAPEUTICS, INC. (81) Designated States (unless otherwise indicated, for every [US/US]; Route 206 & Province Line Road, Princeton, kind of national protection available): AE, AG, AL, AM, New Jersey 08543-4000 (US). 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, (72) Inventors: DEVRAJ, Rajesh; 301 Palomino Hill Court, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, Chesterfield, Missouri 63005 (US). KUMARAVEL, Gna- HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, ICH, KN, nasambandam; 21 Appletree Lane, Lexington, Massachu- KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, setts 02420 (US). PARKER, Michael F.; 45 Brainard Hill MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, Road, Higganum, Connecticut 06441 BEAUMONT, (US). NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, Edward; 114 Innovation Drive, Milton Park; Abingdon RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, Oxfordshire OX14 4RZ (GB). BOWLES, Lee; 114 Innov- TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ation Drive, Milton Park; Abingdon Oxfordshire OX14 ZA, ZM, ZW. 4RZ (GB). BROMBRIDGE, Steve; 114 Innovation Drive, (84) Designated States (unless otherwise indicated, for every Milton Park; Abingdon Oxfordshire OX14 4RZ (GB). COOPER, Sophie; 114 Innovation Drive, Milton Park; kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Abingdon Oxfordshire OX14 4RZ GADOULEAU, (GB). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, Elise; 114 Innovation Drive, Milton Park; Abingdon Ox- fordshire OX14 4RZ Laura; 114 Innov-TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (GB). GLEAVE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, ation Drive, Milton Park; Abingdon Oxfordshire OX14 LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, 4RZ (GB). KERRY, Philip; 114 Innovation Drive, Milton SM, TR), OAPI BJ, CF, CG, CI, CM, GA, GN, GQ, (BF, Park; Abingdon Oxfordshire OX14 4RZ (GB). KOTEY, GW, KM, ML, MR, NE, SN, TD, TG). Adrian; 114 Innovation Drive, Milton Park; Abingdon Ox- fordshire OX14 4RZ (GB). KRULLE, Thomas; 114 In- Published: novation Drive, Milton Park; Abingdon Oxfordshire OX14 — with international search report (Art 21(3)) 4RZ (GB). LECCI, Cristina; 114 Innovation Drive, — before limit Milton Park; Abingdon Oxfordshire OX14 4RZ (GB). the expiration of the time for amending the LOKE, Pui; 114 Innovation Drive, Milton Park; Abingdon claims and to be republished in the event of receipt of Oxfordshire OX14 4RZ MENICONI, Mirco; 114 amendments (Rule 48.2(h)) (GB). Innovation Drive, Milton Park; Abingdon Oxfordshire 1-1 .4t i t C\ In C::' C::: , Il IN Il C::: , ei (54) Title: BICYCLIC INHIBITORS OF PAD4 CH --..„ (57) : The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treat- ing PAD4-related disorders.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562264925P | 2015-12-09 | 2015-12-09 | |
| PCT/US2016/065857 WO2017100594A1 (en) | 2015-12-09 | 2016-12-09 | Bicyclic inhibitors of pad4 |
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| BR112017024678A2 (en) * | 2015-05-21 | 2018-07-31 | Glaxosmithkline Intellectual Property Development Limited | benzoimidazole derivatives as pad4 inhibitors |
| CN109071497B (en) | 2016-02-23 | 2021-10-22 | 帕德罗科治疗公司 | PAD4 Heteroaryl Inhibitors |
| KR102398941B1 (en) | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | covalent inhibitor of PAD4 |
| WO2018049296A1 (en) | 2016-09-12 | 2018-03-15 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| TWI762769B (en) * | 2018-02-26 | 2022-05-01 | 大陸商藥捷安康(南京)科技股份有限公司 | Peptidylarginine deiminase inhibitor and use thereof |
| CN112566916B (en) * | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | Substituted Thienopyrroles as PAD4 Inhibitors |
| KR102825194B1 (en) * | 2018-08-08 | 2025-06-24 | 브리스톨-마이어스 스큅 컴퍼니 | Substituted benzimidazoles as PAD4 inhibitors |
| EP3833439B1 (en) * | 2018-08-08 | 2023-07-12 | Bristol-Myers Squibb Company | Benzimidazole inhibitors of pad enzymes |
| SG11202101174RA (en) | 2018-08-08 | 2021-03-30 | Bristol Myers Squibb Co | Indole and azaindole inhibitors of pad enzymes |
| KR20210146370A (en) | 2019-03-28 | 2021-12-03 | 루핀 리미티드 | Macrocyclic Compounds as STING Agonists |
| CN112574230B (en) * | 2019-09-27 | 2022-10-28 | 药捷安康(南京)科技股份有限公司 | Peptidylarginine deiminase inhibitor and use thereof |
| WO2021158840A1 (en) * | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| 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 |
| TW202233174A (en) | 2020-12-22 | 2022-09-01 | 美商基利科學股份有限公司 | Inhibitors of peptidylarginine deiminases |
| US11878965B2 (en) | 2020-12-22 | 2024-01-23 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| CN112618546B (en) * | 2020-12-22 | 2022-03-01 | 陈昊 | Application of PAD4 inhibitor in preparation of radiotherapy sensitizing drug |
| AU2023387505A1 (en) * | 2022-11-24 | 2025-07-10 | Helios Huaming Biopharma Co., Ltd. | Selenium containing heterocycle compounds and use thereof |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| WO2025181830A2 (en) * | 2024-03-01 | 2025-09-04 | Jubilant Epipad LLC | Polyheterocyclic compounds as peptidyl arginine deiminase 4 (pad4) inhibitors |
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| ITMI20012060A1 (en) * | 2001-10-05 | 2003-04-05 | Recordati Chem Pharm | NEW N-ACYLATED HETEROCYCLES |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| WO2004041277A1 (en) | 2002-11-01 | 2004-05-21 | Merck & Co., Inc. | Carbonylamino-benzimidazole derivatives as androgen receptor modulators |
| EP2234486A4 (en) | 2007-12-19 | 2011-09-14 | Scripps Research Inst | BENZIMIDAZOLE AND ANALOGUE AS RHO-KINASEHEMMER |
| US8710039B2 (en) * | 2010-11-01 | 2014-04-29 | The Penn State Research Foundation | Therapeutic compositions and methods |
| JP5721484B2 (en) | 2011-03-17 | 2015-05-20 | 富士フイルム株式会社 | Polymerizable liquid crystal composition, polymer material and optically anisotropic film using the same, and polymerizable liquid crystal compound |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| CA2874303C (en) | 2012-06-11 | 2020-10-13 | Ucb Biopharma Sprl | Tnf -alpha modulating benz imidazoles |
| EP3255049A1 (en) | 2012-06-29 | 2017-12-13 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| PL2877467T3 (en) * | 2012-07-26 | 2017-08-31 | Glaxo Group Limited | 2-(azaindol-2-yl)benzimidazoles as pad4 inhibitors |
| BR112017024678A2 (en) | 2015-05-21 | 2018-07-31 | Glaxosmithkline Intellectual Property Development Limited | benzoimidazole derivatives as pad4 inhibitors |
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