JPWO2019213445A5 - - Google Patents
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- JPWO2019213445A5 JPWO2019213445A5 JP2021510283A JP2021510283A JPWO2019213445A5 JP WO2019213445 A5 JPWO2019213445 A5 JP WO2019213445A5 JP 2021510283 A JP2021510283 A JP 2021510283A JP 2021510283 A JP2021510283 A JP 2021510283A JP WO2019213445 A5 JPWO2019213445 A5 JP WO2019213445A5
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- Prior art keywords
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- 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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- 150000001875 compounds Chemical class 0.000 claims 23
- 125000002619 bicyclic group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 102100022501 Receptor-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 4
- 101710138589 Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 4
- 239000003153 chemical reaction reagent Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 125000001931 aliphatic group Chemical group 0.000 claims 3
- -1 amine compound Chemical class 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 239000007819 coupling partner Substances 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- PAQZWJGSJMLPMG-UHFFFAOYSA-N 2,4,6-tripropyl-1,3,5,2$l^{5},4$l^{5},6$l^{5}-trioxatriphosphinane 2,4,6-trioxide Chemical compound CCCP1(=O)OP(=O)(CCC)OP(=O)(CCC)O1 PAQZWJGSJMLPMG-UHFFFAOYSA-N 0.000 claims 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- 239000007858 starting material Substances 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000006242 amine protecting group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 229910052723 transition metal Inorganic materials 0.000 claims 1
- 150000003624 transition metals Chemical class 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical group [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862666452P | 2018-05-03 | 2018-05-03 | |
| US62/666,452 | 2018-05-03 | ||
| PCT/US2019/030473 WO2019213445A1 (en) | 2018-05-03 | 2019-05-02 | Rip1 inhibitory compounds and methods for making and using the same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021523225A JP2021523225A (ja) | 2021-09-02 |
| JPWO2019213445A5 true JPWO2019213445A5 (de) | 2022-04-13 |
| JP7379467B2 JP7379467B2 (ja) | 2023-11-14 |
Family
ID=66554488
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021510283A Active JP7379467B2 (ja) | 2018-05-03 | 2019-05-02 | Ｒｉｐ１阻害剤化合物並びにそれを製造及び使用するための方法 |
Country Status (35)
| Country | Link |
|---|---|
| US (2) | US10975064B2 (de) |
| EP (1) | EP3788045B1 (de) |
| JP (1) | JP7379467B2 (de) |
| KR (1) | KR20210006407A (de) |
| CN (1) | CN112384510A (de) |
| AU (1) | AU2019262142A1 (de) |
| BR (1) | BR112020022423A2 (de) |
| CA (1) | CA3099018A1 (de) |
| CL (1) | CL2020002840A1 (de) |
| CO (1) | CO2020015153A2 (de) |
| CR (1) | CR20200582A (de) |
| CY (1) | CY1126152T1 (de) |
| DK (1) | DK3788045T3 (de) |
| DO (1) | DOP2020000197A (de) |
| EA (1) | EA202092581A1 (de) |
| EC (1) | ECSP20077518A (de) |
| ES (1) | ES2947446T3 (de) |
| FI (1) | FI3788045T3 (de) |
| HR (1) | HRP20230909T1 (de) |
| HU (1) | HUE062277T2 (de) |
| IL (1) | IL278416B2 (de) |
| JO (1) | JOP20200277A1 (de) |
| LT (1) | LT3788045T (de) |
| MA (1) | MA52492B1 (de) |
| MD (1) | MD3788045T2 (de) |
| MX (1) | MX2020011622A (de) |
| PE (1) | PE20210414A1 (de) |
| PH (1) | PH12020551848A1 (de) |
| PL (1) | PL3788045T3 (de) |
| PT (1) | PT3788045T (de) |
| RS (1) | RS64418B1 (de) |
| SG (1) | SG11202010913PA (de) |
| SI (1) | SI3788045T1 (de) |
| WO (1) | WO2019213445A1 (de) |
| ZA (1) | ZA202007487B (de) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202010913PA (en) | 2018-05-03 | 2020-12-30 | Rigel Pharmaceuticals Inc | Rip1 inhibitory compounds and methods for making and using the same |
| BR112020022420A2 (pt) * | 2018-05-03 | 2021-03-02 | Rigel Pharmaceuticals, Inc. | composto, composição farmacêutica, método, método para tratar uma doença em um indivíduo e método para produzir o composto |
| WO2021046515A1 (en) | 2019-09-06 | 2021-03-11 | Board Of Regents, The University Of Texas System | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| TW202122397A (zh) | 2019-09-06 | 2021-06-16 | 美商雷傑製藥公司 | Ｒｉｐ１抑制性化合物及用於製備和使用其之方法 |
| CN115279763A (zh) | 2019-09-06 | 2022-11-01 | 里格尔药品股份有限公司 | Rip1抑制化合物以及制备和使用所述化合物的方法 |
| AU2020353663A1 (en) | 2019-09-27 | 2022-04-07 | Board Of Regents, The University Of Texas System | Inhibitors of Receptor Interacting Protein Kinase I for the treatment of disease |
| TW202132307A (zh) * | 2019-11-07 | 2021-09-01 | 美商雷傑製藥公司 | 雜環ｒｉｐ１抑制性化合物 |
| CA3162605A1 (en) * | 2019-11-26 | 2021-06-03 | Board Of Regents, The University Of Texas System | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| AR121717A1 (es) | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| AR122703A1 (es) | 2020-07-01 | 2022-09-28 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| TW202311261A (zh) * | 2021-05-14 | 2023-03-16 | 大陸商中國醫藥研究開發中心有限公司 | 氮呯類稠環化合物及其醫藥用途 |
| CN115894489A (zh) * | 2021-09-22 | 2023-04-04 | 中国药科大学 | 一种受体相互作用蛋白激酶1的抑制剂及其制备方法、应用 |
| WO2023076133A1 (en) * | 2021-10-27 | 2023-05-04 | Merck Sharp & Dohme Llc | Spirotricycle ripk1 inhibitors and methods of uses thereof |
| WO2023119210A1 (ko) * | 2021-12-24 | 2023-06-29 | 제일약품주식회사 | Ripk1 저해제로서의 신규한 화합물 및 이를 포함하는 약학적 조성물 |
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| US4921475A (en) | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
| US5087240A (en) | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
| US4738851A (en) | 1985-09-27 | 1988-04-19 | University Of Iowa Research Foundation, Inc. | Controlled release ophthalmic gel formulation |
| US5163899A (en) | 1987-03-20 | 1992-11-17 | Drug Delivery Systems Inc. | Transdermal drug delivery system |
| US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
| GB8804164D0 (en) | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
| US4882150A (en) | 1988-06-03 | 1989-11-21 | Kaufman Herbert E | Drug delivery system |
| US5008110A (en) | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
| US5088977A (en) | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
| US5521222A (en) | 1989-09-28 | 1996-05-28 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| ES2055280T3 (es) | 1989-12-04 | 1994-08-16 | Searle & Co | Sistema monocapa para la administracion transdermica de farmacos. |
| US5077033A (en) | 1990-08-07 | 1991-12-31 | Mediventures Inc. | Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide |
| EP0495421B1 (de) | 1991-01-15 | 1996-08-21 | Alcon Laboratories, Inc. | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5352456A (en) | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
| WO1993011938A1 (en) | 1991-12-18 | 1993-06-24 | Minnesota Mining And Manufacturing Company | Multilayered barrier structures |
| ATE132381T1 (de) | 1992-01-29 | 1996-01-15 | Voelkl Franz Ski | Ballspielschläger, insbesondere tennisschläger |
| IL114193A (en) | 1994-06-20 | 2000-02-29 | Teva Pharma | Ophthalmic pharmaceutical compositions based on sodium alginate |
| ES2094688B1 (es) | 1994-08-08 | 1997-08-01 | Cusi Lab | Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion. |
| IT1283911B1 (it) | 1996-02-05 | 1998-05-07 | Farmigea Spa | Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo |
| US5800807A (en) | 1997-01-29 | 1998-09-01 | Bausch & Lomb Incorporated | Ophthalmic compositions including glycerin and propylene glycol |
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| EP2192838A4 (de) | 2007-08-15 | 2011-07-27 | Harvard College | Heterocyclische nekroptose-hemmer |
| TWI648273B (zh) * | 2013-02-15 | 2019-01-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺類（三） |
| WO2014145022A1 (en) | 2013-03-15 | 2014-09-18 | President And Fellows Of Harvard College | Hybrid necroptosis inhibitors |
| CN106573006A (zh) * | 2014-08-21 | 2017-04-19 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为药物的rip1激酶抑制剂杂环酰胺 |
| WO2016128936A1 (en) | 2015-02-13 | 2016-08-18 | Glaxosmithkline Intellectual Property Development Limited | Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide |
| TWI763630B (zh) * | 2015-07-02 | 2022-05-11 | 瑞士商赫孚孟拉羅股份公司 | 雙環內醯胺及其使用方法 |
| WO2017064217A1 (en) | 2015-10-13 | 2017-04-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Sibiriline derivatives for use for preventing and/or treating disorders associated with cellular necroptosis |
| US10787462B2 (en) | 2015-10-23 | 2020-09-29 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| WO2017109724A1 (en) | 2015-12-21 | 2017-06-29 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
| KR20180114910A (ko) * | 2016-02-05 | 2018-10-19 | 데날리 테라퓨틱스 인크. | 수용체-상호작용 단백질 키나제 1의 억제제 |
| CN109843886B (zh) | 2016-10-17 | 2022-04-19 | 豪夫迈·罗氏有限公司 | 二环吡啶酮内酰胺及其使用方法 |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
| BR112019017738A2 (pt) | 2017-02-27 | 2020-04-07 | Glaxosmithkline Ip Dev Ltd | combinação, composição farmacêutica, uso de uma combinação ou composição farmacêutica, método para tratar câncer em um humano, e, composto |
| BR112020022420A2 (pt) | 2018-05-03 | 2021-03-02 | Rigel Pharmaceuticals, Inc. | composto, composição farmacêutica, método, método para tratar uma doença em um indivíduo e método para produzir o composto |
| SG11202010913PA (en) | 2018-05-03 | 2020-12-30 | Rigel Pharmaceuticals Inc | Rip1 inhibitory compounds and methods for making and using the same |
| EP3816163A4 (de) | 2018-06-26 | 2022-04-13 | Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences | Zellnekrosehemmer, herstellungsverfahren dafür und verwendung davon |
| WO2020088194A1 (zh) | 2018-11-02 | 2020-05-07 | 中国科学院上海药物研究所 | 抑制rip1激酶的杂环酰胺及其用途 |
| CN115279763A (zh) | 2019-09-06 | 2022-11-01 | 里格尔药品股份有限公司 | Rip1抑制化合物以及制备和使用所述化合物的方法 |
| TW202122397A (zh) | 2019-09-06 | 2021-06-16 | 美商雷傑製藥公司 | Ｒｉｐ１抑制性化合物及用於製備和使用其之方法 |
| AR121717A1 (es) | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
-
2019
- 2019-05-02 SG SG11202010913PA patent/SG11202010913PA/en unknown
- 2019-05-02 HR HRP20230909TT patent/HRP20230909T1/hr unknown
- 2019-05-02 WO PCT/US2019/030473 patent/WO2019213445A1/en active Application Filing
- 2019-05-02 CA CA3099018A patent/CA3099018A1/en active Pending
- 2019-05-02 CN CN201980045150.5A patent/CN112384510A/zh active Pending
- 2019-05-02 MD MDE20210214T patent/MD3788045T2/ro unknown
- 2019-05-02 MX MX2020011622A patent/MX2020011622A/es unknown
- 2019-05-02 RS RS20230648A patent/RS64418B1/sr unknown
- 2019-05-02 DK DK19724662.2T patent/DK3788045T3/da active
- 2019-05-02 US US16/402,103 patent/US10975064B2/en active Active
- 2019-05-02 HU HUE19724662A patent/HUE062277T2/hu unknown
- 2019-05-02 IL IL278416A patent/IL278416B2/en unknown
- 2019-05-02 AU AU2019262142A patent/AU2019262142A1/en active Pending
- 2019-05-02 BR BR112020022423-5A patent/BR112020022423A2/pt unknown
- 2019-05-02 SI SI201930550T patent/SI3788045T1/sl unknown
- 2019-05-02 JP JP2021510283A patent/JP7379467B2/ja active Active
- 2019-05-02 PT PT197246622T patent/PT3788045T/pt unknown
- 2019-05-02 CR CR20200582A patent/CR20200582A/es unknown
- 2019-05-02 ES ES19724662T patent/ES2947446T3/es active Active
- 2019-05-02 EA EA202092581A patent/EA202092581A1/ru unknown
- 2019-05-02 PL PL19724662.2T patent/PL3788045T3/pl unknown
- 2019-05-02 FI FIEP19724662.2T patent/FI3788045T3/fi active
- 2019-05-02 PE PE2020001796A patent/PE20210414A1/es unknown
- 2019-05-02 KR KR1020207034544A patent/KR20210006407A/ko unknown
- 2019-05-02 LT LTEPPCT/US2019/030473T patent/LT3788045T/lt unknown
- 2019-05-02 EP EP19724662.2A patent/EP3788045B1/de active Active
- 2019-05-02 MA MA52492A patent/MA52492B1/fr unknown
- 2019-05-02 JO JOP/2020/0277A patent/JOP20200277A1/ar unknown
-
2020
- 2020-11-02 DO DO2020000197A patent/DOP2020000197A/es unknown
- 2020-11-02 CL CL2020002840A patent/CL2020002840A1/es unknown
- 2020-11-03 PH PH12020551848A patent/PH12020551848A1/en unknown
- 2020-12-01 ZA ZA2020/07487A patent/ZA202007487B/en unknown
- 2020-12-01 CO CONC2020/0015153A patent/CO2020015153A2/es unknown
- 2020-12-01 EC ECSENADI202077518A patent/ECSP20077518A/es unknown
-
2021
- 2021-03-23 US US17/210,261 patent/US11919890B2/en active Active
-
2023
- 2023-07-25 CY CY20231100349T patent/CY1126152T1/el unknown
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