JP2018537535A5 - - Google Patents
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- Publication number
- JP2018537535A5 JP2018537535A5 JP2018549403A JP2018549403A JP2018537535A5 JP 2018537535 A5 JP2018537535 A5 JP 2018537535A5 JP 2018549403 A JP2018549403 A JP 2018549403A JP 2018549403 A JP2018549403 A JP 2018549403A JP 2018537535 A5 JP2018537535 A5 JP 2018537535A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- ring
- optionally substituted
- fluorine
- aliphatic group
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000001931 aliphatic group Chemical group 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 claims 1
- 101150094373 Padi4 gene Proteins 0.000 claims 1
- 229940122298 Peptidyl arginine deiminase IV inhibitor Drugs 0.000 claims 1
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- -1 difluoromethyl propyl Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- IUTWKWRTLRWYRA-ZJUUUORDSA-N CC(C)N1C[C@@H]2NCC[C@@H]2CC1 Chemical compound CC(C)N1C[C@@H]2NCC[C@@H]2CC1 IUTWKWRTLRWYRA-ZJUUUORDSA-N 0.000 description 1
- IUTWKWRTLRWYRA-VHSXEESVSA-N CC(C)N1C[C@H]2NCC[C@H]2CC1 Chemical compound CC(C)N1C[C@H]2NCC[C@H]2CC1 IUTWKWRTLRWYRA-VHSXEESVSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562264919P | 2015-12-09 | 2015-12-09 | |
| US62/264,919 | 2015-12-09 | ||
| PCT/US2016/065865 WO2017100601A1 (en) | 2015-12-09 | 2016-12-09 | Aza-benzimidazole inhibitors of pad4 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018537535A JP2018537535A (ja) | 2018-12-20 |
| JP2018537535A5 true JP2018537535A5 (https=) | 2020-01-23 |
| JP6810156B2 JP6810156B2 (ja) | 2021-01-06 |
Family
ID=59013635
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018549403A Active JP6810156B2 (ja) | 2015-12-09 | 2016-12-09 | Ｐａｄ４のアザベンゾイミダゾール阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9765093B2 (https=) |
| EP (1) | EP3386505B1 (https=) |
| JP (1) | JP6810156B2 (https=) |
| KR (1) | KR102683681B1 (https=) |
| CN (1) | CN108601770B (https=) |
| AR (1) | AR107030A1 (https=) |
| AU (1) | AU2016366405A1 (https=) |
| BR (1) | BR112018011633A2 (https=) |
| CA (1) | CA3007954A1 (https=) |
| EA (1) | EA201891347A1 (https=) |
| ES (1) | ES2830353T3 (https=) |
| IL (1) | IL259796A (https=) |
| MX (1) | MX2018006700A (https=) |
| SG (1) | SG11201804671SA (https=) |
| TW (1) | TW201726689A (https=) |
| UY (1) | UY37017A (https=) |
| WO (1) | WO2017100601A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6926126B2 (ja) | 2016-02-23 | 2021-08-25 | パドロック・セラピューティクス・インコーポレイテッドＰａｄｌｏｃｋ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | Ｐａｄ４のヘテロアリール阻害剤 |
| KR102398941B1 (ko) | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
| JP7118951B2 (ja) | 2016-09-12 | 2022-08-16 | パドロック・セラピューティクス・インコーポレイテッド | Ｐａｄ４のヘテロアリール阻害剤 |
| CN112789087B (zh) * | 2018-08-08 | 2024-08-13 | 百时美施贵宝公司 | Pad酶的苯并咪唑抑制剂 |
| 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 |
| WO2020033488A1 (en) * | 2018-08-08 | 2020-02-13 | Bristol-Myers Squibb Company | Substituted benzimidazoles as pad4 inhibitors |
| 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 |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| 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 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| RS55684B1 (sr) * | 2012-07-26 | 2017-07-31 | Glaxo Group Ltd | 2-(azaindol-2-il)benzimidazoli kao pad4 inhibitori |
-
2016
- 2016-12-07 AR ARP160103776A patent/AR107030A1/es unknown
- 2016-12-08 TW TW105140668A patent/TW201726689A/zh unknown
- 2016-12-09 JP JP2018549403A patent/JP6810156B2/ja active Active
- 2016-12-09 ES ES16873933T patent/ES2830353T3/es active Active
- 2016-12-09 CA CA3007954A patent/CA3007954A1/en not_active Abandoned
- 2016-12-09 BR BR112018011633A patent/BR112018011633A2/pt not_active Application Discontinuation
- 2016-12-09 AU AU2016366405A patent/AU2016366405A1/en not_active Abandoned
- 2016-12-09 UY UY0001037017A patent/UY37017A/es unknown
- 2016-12-09 EA EA201891347A patent/EA201891347A1/ru unknown
- 2016-12-09 US US15/374,208 patent/US9765093B2/en active Active
- 2016-12-09 KR KR1020187019381A patent/KR102683681B1/ko active Active
- 2016-12-09 MX MX2018006700A patent/MX2018006700A/es unknown
- 2016-12-09 WO PCT/US2016/065865 patent/WO2017100601A1/en not_active Ceased
- 2016-12-09 SG SG11201804671SA patent/SG11201804671SA/en unknown
- 2016-12-09 EP EP16873933.2A patent/EP3386505B1/en active Active
- 2016-12-09 CN CN201680081046.8A patent/CN108601770B/zh active Active
-
2018
- 2018-06-04 IL IL259796A patent/IL259796A/en unknown