KR20220137694A - 면역억제제로서 유용한 마크로시클릭 pad4 억제제 - Google Patents
면역억제제로서 유용한 마크로시클릭 pad4 억제제 Download PDFInfo
- Publication number
- KR20220137694A KR20220137694A KR1020227030292A KR20227030292A KR20220137694A KR 20220137694 A KR20220137694 A KR 20220137694A KR 1020227030292 A KR1020227030292 A KR 1020227030292A KR 20227030292 A KR20227030292 A KR 20227030292A KR 20220137694 A KR20220137694 A KR 20220137694A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- substituted
- alkyl
- alkylene
- compound
- 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
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Classifications
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- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D471/22—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 systems contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062970832P | 2020-02-06 | 2020-02-06 | |
| US62/970,832 | 2020-02-06 | ||
| PCT/US2021/016698 WO2021158840A1 (en) | 2020-02-06 | 2021-02-05 | Macrocyclic pad4 inhibitors useful as immunosuppressant |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20220137694A true KR20220137694A (ko) | 2022-10-12 |
Family
ID=74798090
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227030292A Pending KR20220137694A (ko) | 2020-02-06 | 2021-02-05 | 면역억제제로서 유용한 마크로시클릭 pad4 억제제 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US12492202B2 (https=) |
| EP (1) | EP4100405A1 (https=) |
| JP (1) | JP7711073B2 (https=) |
| KR (1) | KR20220137694A (https=) |
| CN (1) | CN115298175B (https=) |
| WO (1) | WO2021158840A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 (13)
| 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 |
| CA3015482A1 (en) | 2016-02-23 | 2017-08-31 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| WO2018022897A1 (en) | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| US11026937B2 (en) | 2016-09-12 | 2021-06-08 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of PAD4 |
| MX2021001471A (es) | 2018-08-08 | 2021-04-28 | Bristol Myers Squibb Co | Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4). |
| 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). |
| US20220348562A1 (en) | 2018-08-08 | 2022-11-03 | Bristol-Myers Squibb Company | Benzimidazole inhibitors of pad enzymes |
| 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 |
-
2021
- 2021-02-05 WO PCT/US2021/016698 patent/WO2021158840A1/en not_active Ceased
- 2021-02-05 CN CN202180022507.5A patent/CN115298175B/zh active Active
- 2021-02-05 JP JP2022547846A patent/JP7711073B2/ja active Active
- 2021-02-05 EP EP21708867.3A patent/EP4100405A1/en active Pending
- 2021-02-05 KR KR1020227030292A patent/KR20220137694A/ko active Pending
- 2021-02-05 US US17/760,309 patent/US12492202B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021158840A1 (en) | 2021-08-12 |
| JP7711073B2 (ja) | 2025-07-22 |
| US20230203039A1 (en) | 2023-06-29 |
| EP4100405A1 (en) | 2022-12-14 |
| US12492202B2 (en) | 2025-12-09 |
| CN115298175B (zh) | 2024-05-07 |
| CN115298175A (zh) | 2022-11-04 |
| JP2023512557A (ja) | 2023-03-27 |
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| Publication | Publication Date | Title |
|---|---|---|
| KR102851932B1 (ko) | Pad4 억제제로서의 치환된 티에노피롤 | |
| US12492202B2 (en) | Macrocyclic PAD4 inhibitors useful as immunosuppressant | |
| CN112805067B (zh) | Pad酶的吲哚及氮杂吲哚抑制剂 | |
| KR102825194B1 (ko) | Pad4 억제제로서의 치환된 벤즈이미다졸 | |
| ES2956090T3 (es) | Inhibidores de bencimidazol de enzimas PAD | |
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| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
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| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
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| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
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| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
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| D21 | Rejection of application intended |
Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE) |
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| E13 | Pre-grant limitation requested |
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| P11-X000 | Amendment of application requested |
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