JP2018515555A5 - - Google Patents
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- Publication number
- JP2018515555A5 JP2018515555A5 JP2017560303A JP2017560303A JP2018515555A5 JP 2018515555 A5 JP2018515555 A5 JP 2018515555A5 JP 2017560303 A JP2017560303 A JP 2017560303A JP 2017560303 A JP2017560303 A JP 2017560303A JP 2018515555 A5 JP2018515555 A5 JP 2018515555A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- optionally substituted
- halo
- membered
- 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
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 28
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000005843 halogen group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 16
- 229920001577 copolymer Chemical group 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 11
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 2
- CEAVVDCFWISQCZ-INIZCTEOSA-N 1-[4-[(3S)-3-(3,5-difluorophenyl)-3,4-dihydropyrazole-2-carbonyl]piperidin-1-yl]ethanone Chemical compound FC=1C=C(C=C(C=1)F)[C@@H]1CC=NN1C(=O)C1CCN(CC1)C(C)=O CEAVVDCFWISQCZ-INIZCTEOSA-N 0.000 claims 2
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- MUQJZMRWJDLBIO-UHFFFAOYSA-N cyclohexyl-(3-phenyl-3,4-dihydropyrazol-2-yl)methanone Chemical compound N1=CCC(C=2C=CC=CC=2)N1C(=O)C1CCCCC1 MUQJZMRWJDLBIO-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 238000001144 powder X-ray diffraction data Methods 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020079670A JP6893271B2 (ja) | 2015-05-19 | 2020-04-28 | キナーゼ阻害剤である複素環式アミド |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562163552P | 2015-05-19 | 2015-05-19 | |
| US62/163,552 | 2015-05-19 | ||
| US201562167359P | 2015-05-28 | 2015-05-28 | |
| US62/167,359 | 2015-05-28 | ||
| US201562197602P | 2015-07-28 | 2015-07-28 | |
| US62/197,602 | 2015-07-28 | ||
| PCT/IB2016/052948 WO2016185423A1 (en) | 2015-05-19 | 2016-05-19 | Heterocyclic amides as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020079670A Division JP6893271B2 (ja) | 2015-05-19 | 2020-04-28 | キナーゼ阻害剤である複素環式アミド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018515555A JP2018515555A (ja) | 2018-06-14 |
| JP2018515555A5 true JP2018515555A5 (https=) | 2019-06-20 |
| JP6700311B2 JP6700311B2 (ja) | 2020-05-27 |
Family
ID=56080431
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017560303A Active JP6700311B2 (ja) | 2015-05-19 | 2016-05-19 | キナーゼ阻害剤である複素環式アミド |
| JP2020079670A Active JP6893271B2 (ja) | 2015-05-19 | 2020-04-28 | キナーゼ阻害剤である複素環式アミド |
| JP2021091574A Active JP7204821B2 (ja) | 2015-05-19 | 2021-05-31 | キナーゼ阻害剤である複素環式アミド |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020079670A Active JP6893271B2 (ja) | 2015-05-19 | 2020-04-28 | キナーゼ阻害剤である複素環式アミド |
| JP2021091574A Active JP7204821B2 (ja) | 2015-05-19 | 2021-05-31 | キナーゼ阻害剤である複素環式アミド |
Country Status (35)
Families Citing this family (46)
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| LT2502911T (lt) | 2004-06-24 | 2017-09-11 | Vertex Pharmaceuticals Incorporated | Atp surišančios kasetės transporterių moduliatoriai |
| EP1945632B1 (en) | 2005-11-08 | 2013-09-18 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of atp-binding cassette transporters |
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| US8969386B2 (en) | 2007-05-09 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| SI2225230T1 (sl) | 2007-12-07 | 2017-03-31 | Vertex Pharmaceuticals Incorporated | Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline |
| EP2639224B1 (en) | 2007-12-07 | 2016-08-24 | Vertex Pharmaceuticals Incorporated | Process for producing cycloalkylcarboxiamido-pyridine benzoic acids |
| NZ720282A (en) | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| SI2408750T1 (sl) | 2009-03-20 | 2015-11-30 | Vertex Pharmaceuticals Incorporated | Postopek za izdelavo modulatorjev cistično-fibroznega transmembranskega regulatorja prevodnosti |
| HRP20211752T1 (hr) | 2010-04-07 | 2022-02-18 | Vertex Pharmaceuticals Incorporated | Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena |
| WO2013112804A1 (en) | 2012-01-25 | 2013-08-01 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2.2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| EP2819670A1 (en) | 2012-02-27 | 2015-01-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administration thereof |
| JP6963896B2 (ja) | 2013-11-12 | 2021-11-10 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Ｃｆｔｒ媒介性疾患の処置のための医薬組成物を調製する方法 |
| PT3221692T (pt) | 2014-11-18 | 2021-09-10 | Vertex Pharma | Processo de realização de testagem de alta produtividade por cromatografia líquida de alta eficiência |
| EP3224245B1 (en) | 2014-12-24 | 2018-09-12 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 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 |
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| US20200062735A1 (en) | 2017-02-27 | 2020-02-27 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
| CA3063934A1 (en) | 2017-05-17 | 2018-11-22 | Denali Therapeutics Inc. | Kinase inhibitors and uses thereof |
| AR113811A1 (es) | 2017-10-31 | 2020-06-10 | Hoffmann La Roche | Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos |
| WO2019224773A1 (en) * | 2018-05-23 | 2019-11-28 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as rip1 kinase inhibitors |
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| WO2020044206A1 (en) | 2018-08-29 | 2020-03-05 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors for use in the treatment cancer |
| CN113302193A (zh) | 2019-01-11 | 2021-08-24 | 豪夫迈·罗氏有限公司 | 双环吡咯并三唑酮化合物及其使用方法 |
| CN109912574A (zh) * | 2019-05-06 | 2019-06-21 | 合肥工业大学 | 一种二氢吡唑类化合物及其制备方法和用途 |
| JP7367062B2 (ja) * | 2019-05-09 | 2023-10-23 | ▲勁▼方医▲薬▼科技（上海）有限公司 | ビス複素環式カルボニル置換ジヒドロピラゾール化合物、その調製方法、及びその医薬的使用 |
| WO2020237047A1 (en) * | 2019-05-22 | 2020-11-26 | Agios Pharmaceuticals, Inc. | Crystalline salt forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
| 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 |
| IL291665B2 (en) | 2019-09-27 | 2025-07-01 | Univ Texas | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| BR112022010082A2 (pt) | 2019-11-26 | 2022-08-30 | Univ Texas | Composto de fórmula estrutural i ou sal do mesmo, composição farmacêutica, uso do composto e uso da composição farmacêutica |
| IL298188A (en) | 2020-05-20 | 2023-01-01 | Sironax Ltd | Circular structures of piperazine |
| JP7774579B2 (ja) * | 2020-05-20 | 2025-11-21 | シロナックス リミテッド． | ピペラジン複素環アミド尿素類を含む受容体共役タンパク質１阻害剤 |
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| CN117500795A (zh) * | 2021-03-18 | 2024-02-02 | 维泰瑞隆有限公司 | 受体相互作用蛋白1抑制剂、其制备及用途 |
| IL308348A (en) * | 2021-05-20 | 2024-01-01 | Sironax Ltd | RIP1 modulators including cyclic ureas aztidine, their preparation and uses |
| CN117460722A (zh) | 2021-08-10 | 2024-01-26 | 艾伯维公司 | 烟酰胺ripk1抑制剂 |
| JP2024544533A (ja) | 2021-11-11 | 2024-12-03 | ジェンザイム・コーポレーション | Ｒｉｐｋ１阻害剤としてのイソオキサゾリジン及びその使用 |
| CN116496256B (zh) * | 2022-01-04 | 2025-03-28 | 北京赛特明强医药科技有限公司 | 羰基桥连杂环类化合物、及其组合物与应用 |
| US11816144B2 (en) * | 2022-03-31 | 2023-11-14 | Pinterest, Inc. | Hair pattern determination and filtering |
| CN115326999B (zh) * | 2022-10-12 | 2022-12-27 | 深圳市海滨制药有限公司 | 一种奥司他韦环氧中间体及其异构体的检测方法 |
| WO2024233544A1 (en) | 2023-05-10 | 2024-11-14 | Genzyme Corporation | Isoxazolidines as ripk1 inhibitors and use thereof |
| CN121079291A (zh) | 2023-05-10 | 2025-12-05 | 建新公司 | 作为ripk1抑制剂的异噁唑烷及其使用 |
| CN121487930A (zh) | 2023-05-10 | 2026-02-06 | 建新公司 | 作为ripk1抑制剂的异噁唑烷及其用途 |
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| JPH062742B2 (ja) | 1987-06-17 | 1994-01-12 | 三井東圧化学株式会社 | 新規２‐ピラゾリン類及びそれを有効成分とする脳血管障害治療剤 |
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| CL2004000366A1 (es) | 2003-02-26 | 2005-01-07 | Pharmacia Corp Sa Organizada B | USO DE UNA COMBINACION DE UN COMPUESTO DERIVADO DE PIRAZOL INHIBIDOR DE QUINASA p38, Y UN INHIBIDOR DE ACE PARA TRATAR DISFUNCION RENAL, ENFERMEDAD CARDIOVASCULAR Y VASCULAR, RETINOPATIA, NEUROPATIA, EDEMA, DISFUNCION ENDOTELIAL O INSULINOPATIA. |
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| TWI637951B (zh) * | 2013-02-15 | 2018-10-11 | 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 |
| EP3224245B1 (en) * | 2014-12-24 | 2018-09-12 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 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 |
| WO2017096301A1 (en) | 2015-12-04 | 2017-06-08 | Denali Therapeutics Inc. | Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (ripk 1) |
| TW201831464A (zh) | 2016-11-18 | 2018-09-01 | 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 |
| US20200062735A1 (en) | 2017-02-27 | 2020-02-27 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
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2016
- 2016-05-17 TW TW105115117A patent/TWI730959B/zh not_active IP Right Cessation
- 2016-05-17 UY UY0001036680A patent/UY36680A/es active IP Right Grant
- 2016-05-19 DK DK16724975.4T patent/DK3298002T3/da active
- 2016-05-19 CN CN202011082608.5A patent/CN112370452A/zh active Pending
- 2016-05-19 MX MX2017014809A patent/MX383935B/es unknown
- 2016-05-19 US US15/575,235 patent/US10590085B2/en active Active
- 2016-05-19 HR HRP20210300TT patent/HRP20210300T1/hr unknown
- 2016-05-19 HU HUE16724975A patent/HUE053564T2/hu unknown
- 2016-05-19 PE PE2017002383A patent/PE20180508A1/es unknown
- 2016-05-19 CA CA2986102A patent/CA2986102C/en active Active
- 2016-05-19 MY MYPI2017704350A patent/MY192059A/en unknown
- 2016-05-19 EP EP16724975.4A patent/EP3298002B1/en active Active
- 2016-05-19 KR KR1020177033029A patent/KR20180004733A/ko active Pending
- 2016-05-19 SI SI201631070T patent/SI3298002T1/sl unknown
- 2016-05-19 WO PCT/IB2016/052948 patent/WO2016185423A1/en not_active Ceased
- 2016-05-19 AU AU2016263156A patent/AU2016263156B2/en not_active Ceased
- 2016-05-19 RS RS20210313A patent/RS61568B1/sr unknown
- 2016-05-19 CN CN201680029135.8A patent/CN107624111B/zh active Active
- 2016-05-19 SM SM20210101T patent/SMT202100101T1/it unknown
- 2016-05-19 CR CR20170524A patent/CR20170524A/es unknown
- 2016-05-19 JP JP2017560303A patent/JP6700311B2/ja active Active
- 2016-05-19 EA EA201792535A patent/EA036452B1/ru not_active IP Right Cessation
- 2016-05-19 SG SG11201708707UA patent/SG11201708707UA/en unknown
- 2016-05-19 PL PL16724975T patent/PL3298002T3/pl unknown
- 2016-05-19 LT LTEP16724975.4T patent/LT3298002T/lt unknown
- 2016-05-19 NZ NZ736665A patent/NZ736665A/en unknown
- 2016-05-19 PT PT167249754T patent/PT3298002T/pt unknown
- 2016-05-19 MA MA42109A patent/MA42109B1/fr unknown
- 2016-05-19 ES ES16724975T patent/ES2848398T3/es active Active
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2017
- 2017-10-23 ZA ZA2017/07176A patent/ZA201707176B/en unknown
- 2017-10-24 IL IL255246A patent/IL255246A0/en active IP Right Grant
- 2017-11-16 CL CL2017002908A patent/CL2017002908A1/es unknown
- 2017-11-17 CO CONC2017/0011754A patent/CO2017011754A2/es unknown
- 2017-11-17 DO DO2017000267A patent/DOP2017000267A/es unknown
- 2017-11-17 PH PH12017502090A patent/PH12017502090A1/en unknown
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2019
- 2019-03-04 AU AU2019201480A patent/AU2019201480C1/en not_active Ceased
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2020
- 2020-01-31 US US16/778,206 patent/US10899716B2/en active Active
- 2020-04-28 JP JP2020079670A patent/JP6893271B2/ja active Active
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2021
- 2021-01-22 US US17/156,478 patent/US11485710B2/en active Active
- 2021-03-11 CY CY20211100210T patent/CY1124187T1/el unknown
- 2021-05-31 JP JP2021091574A patent/JP7204821B2/ja active Active
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2022
- 2022-09-27 US US17/935,791 patent/US20230120185A1/en not_active Abandoned