JP7483678B2 - Ｐａｄ４阻害剤としての置換ベンズイミダゾール - Google Patents
Ｐａｄ４阻害剤としての置換ベンズイミダゾール Download PDFInfo
- Publication number
- JP7483678B2 JP7483678B2 JP2021506621A JP2021506621A JP7483678B2 JP 7483678 B2 JP7483678 B2 JP 7483678B2 JP 2021506621 A JP2021506621 A JP 2021506621A JP 2021506621 A JP2021506621 A JP 2021506621A JP 7483678 B2 JP7483678 B2 JP 7483678B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- substituted
- methoxy
- indol
- cyclopropylmethyl
- 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.)
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Classifications
-
- 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
- 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
-
- 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
-
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (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 (4)
| Publication Number | Publication Date |
|---|---|
| JP2021534097A JP2021534097A (ja) | 2021-12-09 |
| JP2021534097A5 JP2021534097A5 (https=) | 2022-08-08 |
| JPWO2020033488A5 JPWO2020033488A5 (https=) | 2022-08-08 |
| JP7483678B2 true JP7483678B2 (ja) | 2024-05-15 |
Family
ID=67766299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506621A Active JP7483678B2 (ja) | 2018-08-08 | 2019-08-07 | Ｐａｄ４阻害剤としての置換ベンズイミダゾール |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20220402950A1 (https=) |
| EP (1) | EP3833438B1 (https=) |
| JP (1) | JP7483678B2 (https=) |
| KR (1) | KR102825194B1 (https=) |
| CN (1) | CN112805066A (https=) |
| AU (1) | AU2019318415A1 (https=) |
| BR (1) | BR112021002089A2 (https=) |
| CA (1) | CA3108871A1 (https=) |
| CL (1) | CL2021000292A1 (https=) |
| CO (1) | CO2021001219A2 (https=) |
| EA (1) | EA202190464A1 (https=) |
| ES (1) | ES2973714T3 (https=) |
| IL (1) | IL280641A (https=) |
| MX (1) | MX2021001471A (https=) |
| PE (1) | PE20211067A1 (https=) |
| SG (1) | SG11202101176YA (https=) |
| TW (1) | TW202019411A (https=) |
| WO (1) | WO2020033488A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3833671B1 (en) * | 2018-08-08 | 2022-08-24 | Bristol-Myers Squibb Company | Substituted thienopyrroles as pad4 inhibitors |
| AU2019319835A1 (en) | 2018-08-08 | 2021-03-25 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of PAD enzymes |
| EP4100405A1 (en) | 2020-02-06 | 2022-12-14 | 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 |
| EP4143189A1 (en) | 2020-04-30 | 2023-03-08 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| TW202241884A (zh) | 2020-12-22 | 2022-11-01 | 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 |
| WO2022140428A2 (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 |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015522628A (ja) | 2012-07-26 | 2015-08-06 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌ | Ｐａｄ４阻害剤としての２−（アザインドール−２−イル）ベンズイミダゾール |
| WO2017100601A1 (en) | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Aza-benzimidazole inhibitors of pad4 |
| WO2017100594A1 (en) | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Bicyclic inhibitors of pad4 |
| JP2018520105A (ja) | 2015-05-21 | 2018-07-26 | グラクソスミスクライン、インテレクチュアル、プロパテ | Ｐａｄ４阻害剤としてのベンゾイミダゾール誘導体 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102398941B1 (ko) * | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
-
2019
- 2019-08-07 WO PCT/US2019/045424 patent/WO2020033488A1/en not_active Ceased
- 2019-08-07 JP JP2021506621A patent/JP7483678B2/ja active Active
- 2019-08-07 EP EP19759133.2A patent/EP3833438B1/en active Active
- 2019-08-07 TW TW108128157A patent/TW202019411A/zh unknown
- 2019-08-07 PE PE2021000170A patent/PE20211067A1/es unknown
- 2019-08-07 BR BR112021002089-6A patent/BR112021002089A2/pt not_active Application Discontinuation
- 2019-08-07 KR KR1020217006450A patent/KR102825194B1/ko active Active
- 2019-08-07 CN CN201980064958.8A patent/CN112805066A/zh active Pending
- 2019-08-07 EA EA202190464A patent/EA202190464A1/ru unknown
- 2019-08-07 US US17/265,844 patent/US20220402950A1/en active Pending
- 2019-08-07 CA CA3108871A patent/CA3108871A1/en active Pending
- 2019-08-07 SG SG11202101176YA patent/SG11202101176YA/en unknown
- 2019-08-07 MX MX2021001471A patent/MX2021001471A/es unknown
- 2019-08-07 AU AU2019318415A patent/AU2019318415A1/en not_active Abandoned
- 2019-08-07 ES ES19759133T patent/ES2973714T3/es active Active
-
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
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015522628A (ja) | 2012-07-26 | 2015-08-06 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌ | Ｐａｄ４阻害剤としての２−（アザインドール−２−イル）ベンズイミダゾール |
| JP2018520105A (ja) | 2015-05-21 | 2018-07-26 | グラクソスミスクライン、インテレクチュアル、プロパテ | Ｐａｄ４阻害剤としてのベンゾイミダゾール誘導体 |
| WO2017100601A1 (en) | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Aza-benzimidazole inhibitors of pad4 |
| WO2017100594A1 (en) | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Bicyclic inhibitors of pad4 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3833438A1 (en) | 2021-06-16 |
| US20220402950A1 (en) | 2022-12-22 |
| IL280641A (en) | 2021-03-25 |
| JP2021534097A (ja) | 2021-12-09 |
| CA3108871A1 (en) | 2020-02-13 |
| WO2020033488A1 (en) | 2020-02-13 |
| MX2021001471A (es) | 2021-04-28 |
| ES2973714T3 (es) | 2024-06-24 |
| CO2021001219A2 (es) | 2021-02-17 |
| CN112805066A (zh) | 2021-05-14 |
| KR102825194B1 (ko) | 2025-06-24 |
| KR20210042932A (ko) | 2021-04-20 |
| BR112021002089A2 (pt) | 2021-05-04 |
| PE20211067A1 (es) | 2021-06-09 |
| EA202190464A1 (ru) | 2021-06-16 |
| AU2019318415A1 (en) | 2021-03-25 |
| EP3833438B1 (en) | 2024-02-07 |
| TW202019411A (zh) | 2020-06-01 |
| SG11202101176YA (en) | 2021-03-30 |
| CL2021000292A1 (es) | 2021-06-11 |
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