JPWO2022150676A5 - - Google Patents
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- JPWO2022150676A5 JPWO2022150676A5 JP2023541734A JP2023541734A JPWO2022150676A5 JP WO2022150676 A5 JPWO2022150676 A5 JP WO2022150676A5 JP 2023541734 A JP2023541734 A JP 2023541734A JP 2023541734 A JP2023541734 A JP 2023541734A JP WO2022150676 A5 JPWO2022150676 A5 JP WO2022150676A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrimidin
- pyrrolo
- pyrazol
- pharmaceutical combination
- trifluoromethyl
- 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
Links
- 229940122245 Janus kinase inhibitor Drugs 0.000 claims description 41
- 239000003112 inhibitor Substances 0.000 claims description 33
- 239000011435 rock Substances 0.000 claims description 27
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 14
- 208000024908 graft versus host disease Diseases 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 13
- GKHIVNAUVKXIIY-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-propan-2-ylacetamide Chemical group CC(C)NC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 GKHIVNAUVKXIIY-UHFFFAOYSA-N 0.000 claims description 8
- 206010039710 Scleroderma Diseases 0.000 claims description 8
- 208000017760 chronic graft versus host disease Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- WEVYAHXRMPXWCK-UHFFFAOYSA-N methyl cyanide Natural products CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 8
- 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 5
- JFMWPOCYMYGEDM-XFULWGLBSA-N ruxolitinib phosphate Chemical group OP(O)(O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 JFMWPOCYMYGEDM-XFULWGLBSA-N 0.000 claims description 5
- 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 compound 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 4
- 101000669921 Homo sapiens Rho-associated protein kinase 2 Proteins 0.000 claims description 4
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims description 4
- 102100039314 Rho-associated protein kinase 2 Human genes 0.000 claims description 4
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- YMFIMTJNSGCVCV-GRYCIOLGSA-N ((2r,5s)-5-{2-[(1r)-1-hydroxyethyl]-1h-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2h-pyran-2-yl)acetonitrile Chemical compound C[C@@H](O)C1=NC2=CN=C3C=CSC3=C2N1[C@H]1CC[C@H](CC#N)OC1 YMFIMTJNSGCVCV-GRYCIOLGSA-N 0.000 claims description 2
- SVEBIMSTUSDJQC-UHFFFAOYSA-N 2-[1-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]-3-[4-[2-(trifluoromethyl)pyrimidine-4-carbonyl]piperazin-1-yl]cyclobutyl]acetonitrile Chemical compound FC(F)(F)C1=NC=CC(C(=O)N2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 SVEBIMSTUSDJQC-UHFFFAOYSA-N 0.000 claims description 2
- GDLFDECNYGKCOB-UHFFFAOYSA-N 2-[1-[4-[4-(ethylaminomethyl)-6-(trifluoromethyl)pyridin-2-yl]oxycyclohexyl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical compound FC(F)(F)C1=CC(CNCC)=CC(OC2CCC(CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 GDLFDECNYGKCOB-UHFFFAOYSA-N 0.000 claims description 2
- UMIFYBHMXIAHSA-NSQNTRMNSA-N 2-[1-[4-[4-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]-6-(trifluoromethyl)pyridin-2-yl]oxycyclohexyl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical compound C1[C@H](O)CCN1CC1=CC(OC2CCC(CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 UMIFYBHMXIAHSA-NSQNTRMNSA-N 0.000 claims description 2
- RXXCVKTUMMDIRR-UHFFFAOYSA-N 2-[1-[4-[6-(2-hydroxyethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxycyclohexyl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical compound FC(F)(F)C1=NC(CCO)=CC(OC2CCC(CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 RXXCVKTUMMDIRR-UHFFFAOYSA-N 0.000 claims description 2
- QFPGZAJRDFHPCE-UHFFFAOYSA-N 2-[3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]-1-[1-[2-(trifluoromethyl)pyrimidine-4-carbonyl]piperidin-4-yl]azetidin-3-yl]acetonitrile Chemical compound FC(F)(F)C1=NC=CC(C(=O)N2CCC(CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 QFPGZAJRDFHPCE-UHFFFAOYSA-N 0.000 claims description 2
- VMDIAUWVXRUPFS-OPZQEPJFSA-N 2-[3-[4-[4-[[[(2S)-1-hydroxypropan-2-yl]amino]methyl]-6-(trifluoromethyl)pyridin-2-yl]oxypiperidin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]cyclobutyl]acetonitrile Chemical compound FC(F)(F)C1=CC(CN[C@H](CO)C)=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 VMDIAUWVXRUPFS-OPZQEPJFSA-N 0.000 claims description 2
- UHPOZFYNJIMRCT-UHFFFAOYSA-N 3-[1-(6-chloropyridin-2-yl)pyrrolidin-3-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound ClC1=CC=CC(N2CC(CC2)C(CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 UHPOZFYNJIMRCT-UHFFFAOYSA-N 0.000 claims description 2
- HTGGWBJDPLPEPS-UHFFFAOYSA-N 3-[1-([1,3]oxazolo[5,4-b]pyridin-2-yl)pyrrolidin-3-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1CN(C=2OC3=NC=CC=C3N=2)CC1C(CC#N)N(N=C1)C=C1C1=NC=NC2=C1C=CN2 HTGGWBJDPLPEPS-UHFFFAOYSA-N 0.000 claims description 2
- MSGYSFWCPOBHEV-AWEZNQCLSA-N 4-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1h-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-n-[(2s)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC(F)=C1N1CC(CC#N)(N2N=CC(=C2)C2=C(NN=C2C)C)C1 MSGYSFWCPOBHEV-AWEZNQCLSA-N 0.000 claims description 2
- UHEIPWYAZVECGS-ZDUSSCGKSA-N 4-[3-(cyanomethyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-n-[(2s)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC(F)=C1N1CC(CC#N)(N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)C1 UHEIPWYAZVECGS-ZDUSSCGKSA-N 0.000 claims description 2
- RZUCZMLSGAQMJN-UHFFFAOYSA-N 4-[3-(cyanomethyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-1-yl]-n-[4-fluoro-2-(trifluoromethyl)phenyl]piperidine-1-carboxamide Chemical compound FC(F)(F)C1=CC(F)=CC=C1NC(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 RZUCZMLSGAQMJN-UHFFFAOYSA-N 0.000 claims description 2
- VCJFOLMEZCAWFO-UHFFFAOYSA-N 4-[4-(2-fluoro-4-isocyanobenzoyl)piperazin-1-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]butanenitrile Chemical compound FC1=CC([N+]#[C-])=CC=C1C(=O)N1CCN(CC(CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 VCJFOLMEZCAWFO-UHFFFAOYSA-N 0.000 claims description 2
- CEIFLXZQZIUBTK-UHFFFAOYSA-N 4-[4-[3-[(dimethylamino)methyl]-5-fluorophenoxy]piperidin-1-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]butanenitrile Chemical compound CN(C)CC1=CC(F)=CC(OC2CCN(CC(CC#N)N3N=CC(=C3)C=3C=4C=CNC=4N=CN=3)CC2)=C1 CEIFLXZQZIUBTK-UHFFFAOYSA-N 0.000 claims description 2
- VQDFOOLMNPPTBD-UHFFFAOYSA-N 4-[4-[3-cyano-2-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propyl]piperazine-1-carbonyl]-3-fluorobenzonitrile Chemical compound FC1=CC(C#N)=CC=C1C(=O)N1CCN(CC(CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 VQDFOOLMNPPTBD-UHFFFAOYSA-N 0.000 claims description 2
- MDDZCYJCJQHUCB-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(1h-pyrrolo[2,3-b]pyridin-4-yl)pyrazol-1-yl]azetidin-1-yl]-n-propan-2-ylpyrazine-2-carboxamide Chemical compound C1=NC(C(=O)NC(C)C)=CN=C1N1CC(CC#N)(N2N=CC(=C2)C=2C=3C=CNC=3N=CC=2)C1 MDDZCYJCJQHUCB-UHFFFAOYSA-N 0.000 claims description 2
- NQSJETFQTIKWPX-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-1-yl]-n-propan-2-ylpyrazine-2-carboxamide Chemical compound C1=NC(C(=O)NC(C)C)=CN=C1N1CC(CC#N)(N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)C1 NQSJETFQTIKWPX-UHFFFAOYSA-N 0.000 claims description 2
- UMIFYBHMXIAHSA-KMDXXIMOSA-N C1[C@@H](O)CCN1CC1=CC(O[C@@H]2CC[C@@H](CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 Chemical compound C1[C@@H](O)CCN1CC1=CC(O[C@@H]2CC[C@@H](CC2)N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 UMIFYBHMXIAHSA-KMDXXIMOSA-N 0.000 claims description 2
- RUJXSBAUCVPXQZ-UHFFFAOYSA-N CC(C)(O)c1cc(OC2CCC(CC2)N2C[N+](CC#N)(C2)n2cc(cn2)-c2ncnc3[nH]ccc23)nc(c1)C(F)(F)F Chemical compound CC(C)(O)c1cc(OC2CCC(CC2)N2C[N+](CC#N)(C2)n2cc(cn2)-c2ncnc3[nH]ccc23)nc(c1)C(F)(F)F RUJXSBAUCVPXQZ-UHFFFAOYSA-N 0.000 claims description 2
- CMKBSHGTPCCVOM-UHFFFAOYSA-N FC(F)(F)C1=CC(CCO)=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 Chemical compound FC(F)(F)C1=CC(CCO)=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 CMKBSHGTPCCVOM-UHFFFAOYSA-N 0.000 claims description 2
- FHTRVONXSDSHCU-SPCUYXFBSA-N FC(F)(F)C1=CC(CNC[C@H](O)C)=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 Chemical compound FC(F)(F)C1=CC(CNC[C@H](O)C)=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=N1 FHTRVONXSDSHCU-SPCUYXFBSA-N 0.000 claims description 2
- 101000844245 Homo sapiens Non-receptor tyrosine-protein kinase TYK2 Proteins 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
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 claims description 2
- 102100032028 Non-receptor tyrosine-protein kinase TYK2 Human genes 0.000 claims description 2
- WQXUGBZSZWSUTM-VVTYCJQISA-N OC[C@@H]1CCCN1CC1=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 Chemical compound OC[C@@H]1CCCN1CC1=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 WQXUGBZSZWSUTM-VVTYCJQISA-N 0.000 claims description 2
- WQXUGBZSZWSUTM-AUIVBKOASA-N OC[C@H]1CCCN1CC1=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 Chemical compound OC[C@H]1CCCN1CC1=CC(OC2CCN(CC2)C2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)=NC(C(F)(F)F)=C1 WQXUGBZSZWSUTM-AUIVBKOASA-N 0.000 claims description 2
- 206010029888 Obliterative bronchiolitis Diseases 0.000 claims description 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 2
- 206010042953 Systemic sclerosis Diseases 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
- 201000003848 bronchiolitis obliterans Diseases 0.000 claims description 2
- 208000023367 bronchiolitis obliterans with obstructive pulmonary disease Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 230000004064 dysfunction Effects 0.000 claims description 2
- 230000002685 pulmonary effect Effects 0.000 claims description 2
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical group C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims description 2
- 229940000425 combination drug Drugs 0.000 claims 3
- 238000000034 method Methods 0.000 description 32
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163135969P | 2021-01-11 | 2021-01-11 | |
| US63/135,969 | 2021-01-11 | ||
| US202163253384P | 2021-10-07 | 2021-10-07 | |
| US63/253,384 | 2021-10-07 | ||
| PCT/US2022/011756 WO2022150676A1 (en) | 2021-01-11 | 2022-01-10 | Combination therapy comprising jak pathway inhibitor and rock inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024503021A JP2024503021A (ja) | 2024-01-24 |
| JP2024503021A5 JP2024503021A5 (https=) | 2025-01-24 |
| JPWO2022150676A5 true JPWO2022150676A5 (https=) | 2025-01-24 |
Family
ID=80119468
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023541734A Pending JP2024503021A (ja) | 2021-01-11 | 2022-01-10 | Ｊａｋ経路阻害剤及びｒｏｃｋ阻害剤を含む併用療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11918581B2 (https=) |
| EP (1) | EP4274578A1 (https=) |
| JP (1) | JP2024503021A (https=) |
| KR (1) | KR20230157307A (https=) |
| AU (1) | AU2022206313A1 (https=) |
| CA (1) | CA3207859A1 (https=) |
| CL (2) | CL2023002004A1 (https=) |
| IL (1) | IL304320A (https=) |
| MX (1) | MX2023008141A (https=) |
| TW (1) | TW202237083A (https=) |
| WO (1) | WO2022150676A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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) |
| WO2024153147A1 (zh) * | 2023-01-18 | 2024-07-25 | 北京普祺医药科技股份有限公司 | 一种氮杂环烷烃化合物、药物组合物及其用途 |
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| WO1990005723A1 (fr) | 1988-11-24 | 1990-05-31 | Yoshitomi Pharmaceutical Industries, Ltd. | Composes de trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane et leur utilisation en medecine |
| PT868186E (pt) | 1995-12-21 | 2005-05-31 | Alcon Lab Inc | Utilizacao de certos compostos de isoquinolinossulfonilo para tratamento de glaucoma e isquemia ocular |
| NZ513800A (en) | 1996-08-12 | 2001-09-28 | Welfide Corp | Treatment of diseases using Rho kinase inhibitors |
| DE69922494T2 (de) | 1998-02-04 | 2005-05-25 | Banyu Pharmaceutical Co., Ltd. | Zyklische n-acylamin-derivate |
| JP4212149B2 (ja) | 1998-06-11 | 2009-01-21 | 株式会社デ・ウエスタン・セラピテクス研究所 | 医薬 |
| AU5198199A (en) | 1998-08-17 | 2000-03-06 | Senju Pharmaceutical Co., Ltd. | Preventives/remedies for glaucoma |
| US7217722B2 (en) | 2000-02-01 | 2007-05-15 | Kirin Beer Kabushiki Kaisha | Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same |
| ATE273695T1 (de) | 2000-06-28 | 2004-09-15 | Smithkline Beecham Plc | Nassvermahlung |
| US20030125344A1 (en) | 2001-03-23 | 2003-07-03 | Bayer Corporation | Rho-kinase inhibitors |
| MXPA03008659A (es) | 2001-03-23 | 2005-04-08 | Bayer Ag | Inhibidores de rho-cinasa. |
| JPWO2002100833A1 (ja) | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Ｒｈｏキナーゼ阻害剤 |
| WO2005080394A1 (en) | 2004-02-24 | 2005-09-01 | Bioaxone Therapeutique Inc. | 4-substituted piperidine derivatives |
| TWI367098B (en) | 2004-12-23 | 2012-07-01 | Kowa Co | Treating agent for glaucoma |
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| EP3053913B1 (en) | 2009-05-01 | 2018-03-07 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| 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 |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines 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 |
| AU2013274030B2 (en) | 2012-06-15 | 2016-07-07 | Sun Pharmaceutical Industries, Inc. | Deuterated derivatives of ruxolitinib |
| CA2880083A1 (en) | 2012-08-17 | 2014-02-20 | Concert Pharmaceuticals, Inc. | Deuterated baricitinib |
| CN113620933A (zh) | 2012-10-05 | 2021-11-09 | 卡德门企业有限公司 | Rho激酶抑制剂 |
| 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 |
| 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 |
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2022
- 2022-01-10 EP EP22702088.0A patent/EP4274578A1/en active Pending
- 2022-01-10 CA CA3207859A patent/CA3207859A1/en active Pending
- 2022-01-10 TW TW111100922A patent/TW202237083A/zh unknown
- 2022-01-10 KR KR1020237027442A patent/KR20230157307A/ko active Pending
- 2022-01-10 AU AU2022206313A patent/AU2022206313A1/en active Pending
- 2022-01-10 JP JP2023541734A patent/JP2024503021A/ja active Pending
- 2022-01-10 MX MX2023008141A patent/MX2023008141A/es unknown
- 2022-01-10 US US17/571,844 patent/US11918581B2/en active Active
- 2022-01-10 WO PCT/US2022/011756 patent/WO2022150676A1/en not_active Ceased
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2023
- 2023-07-09 IL IL304320A patent/IL304320A/en unknown
- 2023-07-10 CL CL2023002004A patent/CL2023002004A1/es unknown
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2024
- 2024-02-01 US US18/430,205 patent/US20240293411A1/en active Pending
- 2024-03-14 CL CL2024000773A patent/CL2024000773A1/es unknown
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