AU2016366405A1 - Aza-benzimidazole inhibitors of PAD4 - Google Patents

Aza-benzimidazole inhibitors of PAD4 Download PDF

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Publication number
AU2016366405A1
AU2016366405A1 AU2016366405A AU2016366405A AU2016366405A1 AU 2016366405 A1 AU2016366405 A1 AU 2016366405A1 AU 2016366405 A AU2016366405 A AU 2016366405A AU 2016366405 A AU2016366405 A AU 2016366405A AU 2016366405 A1 AU2016366405 A1 AU 2016366405A1
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AU
Australia
Prior art keywords
pad4
pharmaceutically acceptable
compound
pct
compound according
Prior art date
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Abandoned
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AU2016366405A
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English (en)
Inventor
Rajesh Devraj
Laura Gleave
Adrian KOTEY
Thomas Krulle
Gnanasambandam Kumaravel
Cristina Lecci
Heather Tye
Ian WIGGINTON
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Padlock Therapeutics Inc
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Padlock Therapeutics Inc
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Publication of AU2016366405A1 publication Critical patent/AU2016366405A1/en
Abandoned legal-status Critical Current

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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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AU2016366405A 2015-12-09 2016-12-09 Aza-benzimidazole inhibitors of PAD4 Abandoned AU2016366405A1 (en)

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WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
CN110248934B (zh) 2016-09-12 2022-05-24 帕德罗科治疗公司 杂芳基pad4抑制剂
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル-マイヤーズ スクイブ カンパニー Pad4阻害剤としての置換チエノピロール
US20220402950A1 (en) * 2018-08-08 2022-12-22 Bristol-Myers Squibb Company Substituted benzimidazoles as pad4 inhibitors
EP3833439B1 (en) * 2018-08-08 2023-07-12 Bristol-Myers Squibb Company Benzimidazole inhibitors of pad enzymes
AU2019319835A1 (en) * 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Indole and azaindole inhibitors of PAD enzymes
KR20220137694A (ko) 2020-02-06 2022-10-12 브리스톨-마이어스 스큅 컴퍼니 면역억제제로서 유용한 마크로시클릭 pad4 억제제
TW202140477A (zh) * 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑
CN115551862B (zh) 2020-04-30 2024-04-12 吉利德科学公司 肽基精氨酸脱亚胺酶的大环抑制剂
EP4267587A2 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
EP4267562A1 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
KR20260041867A (ko) 2023-07-21 2026-03-27 브리스톨-마이어스 스큅 컴퍼니 Pad4 조정제의 시트룰린화 및 활성을 평가하는 방법
WO2025199042A1 (en) * 2024-03-18 2025-09-25 Seattle Children's Hospital D/B/A Seattle Children's Research Institute Methods for treating severe tuberculosis
WO2026020127A2 (en) 2024-07-19 2026-01-22 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad2 modulators

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GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
FR2826653B1 (fr) * 2001-06-29 2005-10-14 Servier Lab Nouveaux derives de pyrido-pyrido-pyrrolo[3,2-g]pyrrolo [3,4-e]-indole et pyrido-pyrrolo[2,3-a]pyrrolo[3,4-c] carbazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP5039268B2 (ja) * 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
FR2862971B1 (fr) * 2003-11-28 2006-03-24 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament
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DK2877467T3 (en) * 2012-07-26 2017-02-13 Glaxo Group Ltd 2- (AZAINDOL-2-YL) BENZIMIDAZOLES AS PAD4 INHIBITORS

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IL259796A (en) 2018-07-31
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US20170166592A1 (en) 2017-06-15
JP6810156B2 (ja) 2021-01-06
BR112018011633A2 (pt) 2018-11-27
UY37017A (es) 2017-06-30
CN108601770B (zh) 2021-06-04
WO2017100601A1 (en) 2017-06-15
AR107030A1 (es) 2018-03-14
EP3386505A1 (en) 2018-10-17
SG11201804671SA (en) 2018-06-28
CN108601770A (zh) 2018-09-28
JP2018537535A (ja) 2018-12-20
KR102683681B1 (ko) 2024-07-09
US9765093B2 (en) 2017-09-19
MX2018006700A (es) 2019-02-20
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EA201891347A1 (ru) 2018-12-28

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