JPWO2020132210A5 - - Google Patents
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- Publication number
- JPWO2020132210A5 JPWO2020132210A5 JP2021535585A JP2021535585A JPWO2020132210A5 JP WO2020132210 A5 JPWO2020132210 A5 JP WO2020132210A5 JP 2021535585 A JP2021535585 A JP 2021535585A JP 2021535585 A JP2021535585 A JP 2021535585A JP WO2020132210 A5 JPWO2020132210 A5 JP WO2020132210A5
- Authority
- JP
- Japan
- Prior art keywords
- pathway inhibitor
- pharmaceutically acceptable
- acceptable salt
- medicament
- jak1 pathway
- 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
- 239000003112 inhibitor Substances 0.000 claims description 57
- 230000037361 pathway Effects 0.000 claims description 57
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims description 54
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims description 54
- 150000003839 salts Chemical class 0.000 claims description 46
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 27
- 208000010643 digestive system disease Diseases 0.000 claims description 27
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 27
- 238000000034 method Methods 0.000 claims description 27
- WEVYAHXRMPXWCK-UHFFFAOYSA-N methyl cyanide Natural products CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 26
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims description 12
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 12
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 9
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 9
- 230000036470 plasma concentration Effects 0.000 claims description 8
- 208000015943 Coeliac disease Diseases 0.000 claims description 7
- 208000011231 Crohn disease Diseases 0.000 claims description 7
- 239000002552 dosage form Substances 0.000 claims description 6
- 238000013268 sustained release Methods 0.000 claims description 6
- 239000012730 sustained-release form Substances 0.000 claims description 6
- KTBSXLIQKWEBRB-UHFFFAOYSA-N 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical group C1=CN=C(C(F)(F)F)C(F)=C1C(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 KTBSXLIQKWEBRB-UHFFFAOYSA-N 0.000 claims description 5
- CEGWJIQFBNFMHQ-UHFFFAOYSA-N 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile;hexanedioic acid Chemical group OC(=O)CCCCC(O)=O.C1=CN=C(C(F)(F)F)C(F)=C1C(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 CEGWJIQFBNFMHQ-UHFFFAOYSA-N 0.000 claims description 2
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims description 2
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims description 2
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims description 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims description 2
- 206010009887 colitis Diseases 0.000 claims description 2
- 230000002269 spontaneous effect Effects 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 30
- 239000012458 free base Substances 0.000 claims 1
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 2
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862781877P | 2018-12-19 | 2018-12-19 | |
| US62/781,877 | 2018-12-19 | ||
| US201962854801P | 2019-05-30 | 2019-05-30 | |
| US62/854,801 | 2019-05-30 | ||
| US201962901377P | 2019-09-17 | 2019-09-17 | |
| US62/901,377 | 2019-09-17 | ||
| PCT/US2019/067418 WO2020132210A1 (en) | 2018-12-19 | 2019-12-19 | Jak1 pathway inhibitors for the treatment of gastrointestinal disease |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022514089A JP2022514089A (ja) | 2022-02-09 |
| JP2022514089A5 JP2022514089A5 (https=) | 2022-12-26 |
| JPWO2020132210A5 true JPWO2020132210A5 (https=) | 2022-12-26 |
| JP7624922B2 JP7624922B2 (ja) | 2025-01-31 |
Family
ID=69326646
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021535585A Active JP7624922B2 (ja) | 2018-12-19 | 2019-12-19 | 胃腸疾患の治療のためのｊａｋ１経路阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11596632B2 (https=) |
| EP (1) | EP3897627A1 (https=) |
| JP (1) | JP7624922B2 (https=) |
| KR (1) | KR20210116487A (https=) |
| CN (1) | CN113692278A (https=) |
| AU (1) | AU2019403304B2 (https=) |
| CA (1) | CA3123596A1 (https=) |
| IL (1) | IL284034A (https=) |
| MA (1) | MA54544A (https=) |
| MX (1) | MX2021007260A (https=) |
| PH (1) | PH12021551455A1 (https=) |
| SG (1) | SG11202106470TA (https=) |
| TW (1) | TWI884142B (https=) |
| UA (1) | UA130221C2 (https=) |
| WO (1) | WO2020132210A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3710431A4 (en) | 2017-11-03 | 2021-07-07 | Aclaris Therapeutics, Inc. | SUBSTITUTED PYRROLOPYRIMIDINE-BASED JAK INHIBITORS AND THEIR MANUFACTURING AND USE PROCEDURES |
| WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| CA3097025A1 (en) | 2018-04-13 | 2019-10-17 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| WO2020033955A1 (en) | 2018-08-10 | 2020-02-13 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine itk inhibitors |
| CA3117969A1 (en) | 2018-10-31 | 2020-05-07 | Incyte Corporation | Combination therapy for treatment of hematological diseases |
| CA3123596A1 (en) | 2018-12-19 | 2020-06-25 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of gastrointestinal disease |
| MA55201A (fr) | 2019-03-05 | 2022-01-12 | Incyte Corp | Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire |
| EP4041204A1 (en) | 2019-10-10 | 2022-08-17 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
| EP4351584A4 (en) * | 2021-06-07 | 2025-04-23 | The Regents of the University of California | COMPOSITIONS AND METHODS FOR TREATING CELIAC DISEASE |
| EP4615440A1 (en) * | 2022-11-08 | 2025-09-17 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine compositions for treatment of itk mediated conditions |
| WO2025144781A1 (en) * | 2023-12-28 | 2025-07-03 | Aclaris Therapeutics, Inc. | Crystalline polymorph of an itk inhibitor |
| CN120699157B (zh) * | 2025-07-16 | 2025-12-16 | 安康市中心医院 | 一种治疗溃疡性结肠炎的恢复肠屏障功能抗体及其应用 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2376596C (en) | 1999-06-25 | 2009-10-06 | Genentech, Inc. | Humanized anti-erbb2 antibodies and treatment with anti-erbb2 antibodies |
| ATE273695T1 (de) | 2000-06-28 | 2004-09-15 | Smithkline Beecham Plc | Nassvermahlung |
| US20040132101A1 (en) | 2002-09-27 | 2004-07-08 | Xencor | Optimized Fc variants and methods for their generation |
| ES2392525T3 (es) | 2002-07-15 | 2012-12-11 | F. Hoffmann-La Roche Ag | Tratamiento del cáncer con el anticuerpo dirigido contra ErbB2 rhuMAb 2C4 |
| JP5775070B2 (ja) | 2009-05-22 | 2015-09-09 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| PT3354652T (pt) | 2010-03-10 | 2020-07-20 | Incyte Holdings Corp | Derivados de piperidin-4-ilazetidina como inibidores de jak1 |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| CN104918945B (zh) | 2012-11-01 | 2018-01-05 | 因赛特公司 | 作为jak抑制剂的三环稠合噻吩衍生物 |
| WO2014138168A1 (en) | 2013-03-06 | 2014-09-12 | Incyte Corporation | Processes and intermediates for making a jak inhibitor |
| SMT201900223T1 (it) | 2013-05-17 | 2019-07-11 | Incyte Corp | Sale di bipirazolo come inibitore di jak |
| SG10201801069QA (en) * | 2013-08-07 | 2018-03-28 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| CN106687462A (zh) | 2014-04-30 | 2017-05-17 | 因赛特公司 | Jak1抑制剂的制备方法以及其新形式 |
| ES2784523T3 (es) | 2015-11-24 | 2020-09-28 | Theravance Biopharma R&D Ip Llc | Profármacos de un compuesto inhibidor de JAK para el tratamiento de enfermedades inflamatorias gastrointestinales |
| EP3554485B9 (en) * | 2016-12-14 | 2023-09-27 | Biora Therapeutics, Inc. | Treatment of a disease of the gastrointestinal tract with a jak inhibitor and devices |
| WO2018111327A1 (en) * | 2016-12-14 | 2018-06-21 | Progenity Inc. | Methods and ingestible devices for the regio-specific release of jak inhibitors at the site of gastrointestinal tract disease |
| CA3123596A1 (en) | 2018-12-19 | 2020-06-25 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of gastrointestinal disease |
-
2019
- 2019-12-19 CA CA3123596A patent/CA3123596A1/en active Pending
- 2019-12-19 JP JP2021535585A patent/JP7624922B2/ja active Active
- 2019-12-19 KR KR1020217022692A patent/KR20210116487A/ko active Pending
- 2019-12-19 EP EP19842939.1A patent/EP3897627A1/en active Pending
- 2019-12-19 PH PH1/2021/551455A patent/PH12021551455A1/en unknown
- 2019-12-19 MA MA054544A patent/MA54544A/fr unknown
- 2019-12-19 TW TW108146771A patent/TWI884142B/zh active
- 2019-12-19 CN CN201980090047.2A patent/CN113692278A/zh active Pending
- 2019-12-19 SG SG11202106470TA patent/SG11202106470TA/en unknown
- 2019-12-19 UA UAA202104150A patent/UA130221C2/uk unknown
- 2019-12-19 US US16/720,465 patent/US11596632B2/en active Active
- 2019-12-19 MX MX2021007260A patent/MX2021007260A/es unknown
- 2019-12-19 WO PCT/US2019/067418 patent/WO2020132210A1/en not_active Ceased
- 2019-12-19 AU AU2019403304A patent/AU2019403304B2/en active Active
-
2021
- 2021-06-15 IL IL284034A patent/IL284034A/en unknown
-
2023
- 2023-01-31 US US18/103,662 patent/US12150943B2/en active Active
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