CN112805066A - 作为pad4抑制剂的经取代的苯并咪唑 - Google Patents
作为pad4抑制剂的经取代的苯并咪唑 Download PDFInfo
- Publication number
- CN112805066A CN112805066A CN201980064958.8A CN201980064958A CN112805066A CN 112805066 A CN112805066 A CN 112805066A CN 201980064958 A CN201980064958 A CN 201980064958A CN 112805066 A CN112805066 A CN 112805066A
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Classifications
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- 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
- 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)
- 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 (1)
| Publication Number | Publication Date |
|---|---|
| CN112805066A true CN112805066A (zh) | 2021-05-14 |
Family
ID=67766299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980064958.8A Pending CN112805066A (zh) | 2018-08-08 | 2019-08-07 | 作为pad4抑制剂的经取代的苯并咪唑 |
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=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112566916A (zh) * | 2018-08-08 | 2021-03-26 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104470919A (zh) * | 2012-07-26 | 2015-03-25 | 葛兰素集团有限公司 | 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑 |
| 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 |
| WO2018022897A1 (en) * | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| CN107849015A (zh) * | 2015-05-21 | 2018-03-27 | 葛兰素知识产权发展有限公司 | 作为pad4抑制剂的苯并咪唑衍生物 |
-
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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104470919A (zh) * | 2012-07-26 | 2015-03-25 | 葛兰素集团有限公司 | 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑 |
| CN107849015A (zh) * | 2015-05-21 | 2018-03-27 | 葛兰素知识产权发展有限公司 | 作为pad4抑制剂的苯并咪唑衍生物 |
| 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 |
| WO2018022897A1 (en) * | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112566916A (zh) * | 2018-08-08 | 2021-03-26 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
| KR20210042935A (ko) * | 2018-08-08 | 2021-04-20 | 브리스톨-마이어스 스큅 컴퍼니 | Pad4 억제제로서의 치환된 티에노피롤 |
| CN112566916B (zh) * | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
| KR102851932B1 (ko) | 2018-08-08 | 2025-08-27 | 브리스톨-마이어스 스큅 컴퍼니 | Pad4 억제제로서의 치환된 티에노피롤 |
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 |
| JP7483678B2 (ja) | 2024-05-15 |
| MX2021001471A (es) | 2021-04-28 |
| ES2973714T3 (es) | 2024-06-24 |
| CO2021001219A2 (es) | 2021-02-17 |
| 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination |