CA3108871A1 - Substituted benzimidazoles as pad4 inhibitors - Google Patents
Substituted benzimidazoles as pad4 inhibitors Download PDFInfo
- Publication number
- CA3108871A1 CA3108871A1 CA3108871A CA3108871A CA3108871A1 CA 3108871 A1 CA3108871 A1 CA 3108871A1 CA 3108871 A CA3108871 A CA 3108871A CA 3108871 A CA3108871 A CA 3108871A CA 3108871 A1 CA3108871 A1 CA 3108871A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- occurrence
- independently selected
- alkyl
- nrara
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D471/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862715858P | 2018-08-08 | 2018-08-08 | |
| US62/715,858 | 2018-08-08 | ||
| PCT/US2019/045424 WO2020033488A1 (en) | 2018-08-08 | 2019-08-07 | Substituted benzimidazoles as pad4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3108871A1 true CA3108871A1 (en) | 2020-02-13 |
Family
ID=67766299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3108871A Pending CA3108871A1 (en) | 2018-08-08 | 2019-08-07 | Substituted benzimidazoles as pad4 inhibitors |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20220402950A1 (enExample) |
| EP (1) | EP3833438B1 (enExample) |
| JP (1) | JP7483678B2 (enExample) |
| KR (1) | KR102825194B1 (enExample) |
| CN (1) | CN112805066A (enExample) |
| AU (1) | AU2019318415A1 (enExample) |
| BR (1) | BR112021002089A2 (enExample) |
| CA (1) | CA3108871A1 (enExample) |
| CL (1) | CL2021000292A1 (enExample) |
| CO (1) | CO2021001219A2 (enExample) |
| EA (1) | EA202190464A1 (enExample) |
| ES (1) | ES2973714T3 (enExample) |
| IL (1) | IL280641A (enExample) |
| MX (1) | MX2021001471A (enExample) |
| PE (1) | PE20211067A1 (enExample) |
| SG (1) | SG11202101176YA (enExample) |
| TW (1) | TW202019411A (enExample) |
| WO (1) | WO2020033488A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MX2021001565A (es) | 2018-08-08 | 2021-04-19 | Bristol Myers Squibb Co | Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad). |
| WO2021158840A1 (en) | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| 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 |
| WO2021222353A1 (en) | 2020-04-30 | 2021-11-04 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| TW202233174A (zh) | 2020-12-22 | 2022-09-01 | 美商基利科學股份有限公司 | 肽基精胺酸去亞胺酶之抑制劑 |
| WO2022140390A1 (en) | 2020-12-22 | 2022-06-30 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| CN116492462B (zh) * | 2023-02-03 | 2023-09-22 | 山东第一医科大学附属眼科医院(山东省眼科医院) | Pad4抑制剂在防治角膜移植术后免疫排斥反应中的应用 |
| KR20260041867A (ko) | 2023-07-21 | 2026-03-27 | 브리스톨-마이어스 스큅 컴퍼니 | Pad4 조정제의 시트룰린화 및 활성을 평가하는 방법 |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101916443B1 (ko) | 2012-07-26 | 2018-11-08 | 글락소 그룹 리미티드 | Pad4 억제제로서의 2-(아자인돌-2-일) 벤즈이미다졸 |
| KR20180005250A (ko) * | 2015-05-21 | 2018-01-15 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | Pad4 억제제로서의 벤조이미다졸 유도체 |
| AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| WO2018022897A1 (en) * | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
-
2019
- 2019-08-07 MX MX2021001471A patent/MX2021001471A/es unknown
- 2019-08-07 US US17/265,844 patent/US20220402950A1/en active Pending
- 2019-08-07 EP EP19759133.2A patent/EP3833438B1/en active Active
- 2019-08-07 PE PE2021000170A patent/PE20211067A1/es unknown
- 2019-08-07 TW TW108128157A patent/TW202019411A/zh unknown
- 2019-08-07 CA CA3108871A patent/CA3108871A1/en active Pending
- 2019-08-07 KR KR1020217006450A patent/KR102825194B1/ko active Active
- 2019-08-07 SG SG11202101176YA patent/SG11202101176YA/en unknown
- 2019-08-07 JP JP2021506621A patent/JP7483678B2/ja active Active
- 2019-08-07 AU AU2019318415A patent/AU2019318415A1/en not_active Abandoned
- 2019-08-07 ES ES19759133T patent/ES2973714T3/es active Active
- 2019-08-07 BR BR112021002089-6A patent/BR112021002089A2/pt not_active Application Discontinuation
- 2019-08-07 EA EA202190464A patent/EA202190464A1/ru unknown
- 2019-08-07 WO PCT/US2019/045424 patent/WO2020033488A1/en not_active Ceased
- 2019-08-07 CN CN201980064958.8A patent/CN112805066A/zh active Pending
-
2021
- 2021-02-03 CL CL2021000292A patent/CL2021000292A1/es unknown
- 2021-02-03 CO CONC2021/0001219A patent/CO2021001219A2/es unknown
- 2021-02-04 IL IL280641A patent/IL280641A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20211067A1 (es) | 2021-06-09 |
| CO2021001219A2 (es) | 2021-02-17 |
| WO2020033488A1 (en) | 2020-02-13 |
| TW202019411A (zh) | 2020-06-01 |
| EA202190464A1 (ru) | 2021-06-16 |
| AU2019318415A1 (en) | 2021-03-25 |
| BR112021002089A2 (pt) | 2021-05-04 |
| JP7483678B2 (ja) | 2024-05-15 |
| CN112805066A (zh) | 2021-05-14 |
| IL280641A (en) | 2021-03-25 |
| KR102825194B1 (ko) | 2025-06-24 |
| CL2021000292A1 (es) | 2021-06-11 |
| US20220402950A1 (en) | 2022-12-22 |
| ES2973714T3 (es) | 2024-06-24 |
| JP2021534097A (ja) | 2021-12-09 |
| EP3833438B1 (en) | 2024-02-07 |
| MX2021001471A (es) | 2021-04-28 |
| SG11202101176YA (en) | 2021-03-30 |
| EP3833438A1 (en) | 2021-06-16 |
| KR20210042932A (ko) | 2021-04-20 |
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| CN112805067B (zh) | Pad酶的吲哚及氮杂吲哚抑制剂 | |
| JP7434281B2 (ja) | Ｐａｄ酵素のベンズイミダゾール阻害剤 | |
| US12492202B2 (en) | Macrocyclic PAD4 inhibitors useful as immunosuppressant | |
| CA3120514A1 (en) | Cyclic ureas | |
| CN122003422A (zh) | 杂环pad4抑制剂 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220922 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20260122 |