IL259796A - Aza-benzimidazole inhibitors of pad4 - Google Patents

Aza-benzimidazole inhibitors of pad4

Info

Publication number
IL259796A
IL259796A IL259796A IL25979618A IL259796A IL 259796 A IL259796 A IL 259796A IL 259796 A IL259796 A IL 259796A IL 25979618 A IL25979618 A IL 25979618A IL 259796 A IL259796 A IL 259796A
Authority
IL
Israel
Prior art keywords
pad4
aza
benzimidazole inhibitors
benzimidazole
inhibitors
Prior art date
Application number
IL259796A
Other languages
English (en)
Hebrew (he)
Inventor
Rajesh Devraj
Gnanasambandam Kumaravel
Laura Gleave
Adrian Kotey
Thomas Krulle
Cristina Lecci
Heather Tye
Ian Wigginton
Original Assignee
Padlock Therapeutics Inc
Rajesh Devraj
Gnanasambandam Kumaravel
Laura Gleave
Adrian Kotey
Thomas Krulle
Cristina Lecci
Heather Tye
Ian Wigginton
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, Rajesh Devraj, Gnanasambandam Kumaravel, Laura Gleave, Adrian Kotey, Thomas Krulle, Cristina Lecci, Heather Tye, Ian Wigginton filed Critical Padlock Therapeutics Inc
Publication of IL259796A publication Critical patent/IL259796A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • 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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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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    • 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
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IL259796A 2015-12-09 2018-06-04 Aza-benzimidazole inhibitors of pad4 IL259796A (en)

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AR107694A1 (es) 2016-02-23 2018-05-23 Padlock Therapeutics Inc Heteroarilos inhibidores de pad4
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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US6087380A (en) * 1949-11-24 2000-07-11 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions
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
EP2358202B1 (en) * 2008-11-03 2016-06-15 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
DK2877467T3 (en) * 2012-07-26 2017-02-13 Glaxo Group Ltd 2- (AZAINDOL-2-YL) BENZIMIDAZOLES AS PAD4 INHIBITORS

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KR20180098573A (ko) 2018-09-04
CA3007954A1 (en) 2017-06-15
EP3386505A4 (en) 2019-06-26
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
AU2016366405A1 (en) 2018-07-19
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
EP3386505B1 (en) 2020-09-23
ES2830353T3 (es) 2021-06-03
EA201891347A1 (ru) 2018-12-28

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