JP2013520436A5 - - Google Patents
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- Publication number
- JP2013520436A5 JP2013520436A5 JP2012554055A JP2012554055A JP2013520436A5 JP 2013520436 A5 JP2013520436 A5 JP 2013520436A5 JP 2012554055 A JP2012554055 A JP 2012554055A JP 2012554055 A JP2012554055 A JP 2012554055A JP 2013520436 A5 JP2013520436 A5 JP 2013520436A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- disease
- pyrrolo
- pyrazol
- 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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- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 239000003814 drug Substances 0.000 claims 11
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 206010028537 myelofibrosis Diseases 0.000 claims 4
- 150000002825 nitriles Chemical class 0.000 claims 4
- 208000003476 primary myelofibrosis Diseases 0.000 claims 4
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 3
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 3
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 3
- 208000037244 polycythemia vera Diseases 0.000 claims 3
- 208000017520 skin disease Diseases 0.000 claims 3
- LHYYCYCHHCXVEN-UHFFFAOYSA-N 3-(3-methylcyclobutyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1C(C)CC1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 LHYYCYCHHCXVEN-UHFFFAOYSA-N 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- YUSIGUNTDAETHP-CQSZACIVSA-N (3r)-3-cyclobutyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCC1 YUSIGUNTDAETHP-CQSZACIVSA-N 0.000 claims 1
- YUSIGUNTDAETHP-AWEZNQCLSA-N (3s)-3-cyclobutyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1([C@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCC1 YUSIGUNTDAETHP-AWEZNQCLSA-N 0.000 claims 1
- YUSIGUNTDAETHP-UHFFFAOYSA-N 3-cyclobutyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1=C(C=2C=3C=CNC=3N=CN=2)C=NN1C(CC#N)C1CCC1 YUSIGUNTDAETHP-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- LHYYCYCHHCXVEN-ODOQXGPZSA-N C1[C@@H](C)C[C@H]1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 Chemical group C1[C@@H](C)C[C@H]1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 LHYYCYCHHCXVEN-ODOQXGPZSA-N 0.000 claims 1
- WCQNXTBVZJREQF-ZOWXZIJZSA-N CC[C@@H]([C@H]1C[C@@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 Chemical compound CC[C@@H]([C@H]1C[C@@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 WCQNXTBVZJREQF-ZOWXZIJZSA-N 0.000 claims 1
- WCQNXTBVZJREQF-HUBLWGQQSA-N CC[C@@H]([C@H]1C[C@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 Chemical compound CC[C@@H]([C@H]1C[C@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 WCQNXTBVZJREQF-HUBLWGQQSA-N 0.000 claims 1
- WCQNXTBVZJREQF-TYNCELHUSA-N CC[C@H]([C@H]1C[C@@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 Chemical compound CC[C@H]([C@H]1C[C@@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 WCQNXTBVZJREQF-TYNCELHUSA-N 0.000 claims 1
- WCQNXTBVZJREQF-LALPHHSUSA-N CC[C@H]([C@H]1C[C@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 Chemical compound CC[C@H]([C@H]1C[C@H](C)C1)N1N=CC(C2=NC=NC3=C2C=CN3)=C1 WCQNXTBVZJREQF-LALPHHSUSA-N 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010070834 Sensitisation Diseases 0.000 claims 1
- 206010070835 Skin sensitisation Diseases 0.000 claims 1
- 208000005485 Thrombocytosis Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- 230000008313 sensitization Effects 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 231100000370 skin sensitisation Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30563010P | 2010-02-18 | 2010-02-18 | |
| US61/305,630 | 2010-02-18 | ||
| PCT/US2011/025433 WO2011103423A1 (en) | 2010-02-18 | 2011-02-18 | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013520436A JP2013520436A (ja) | 2013-06-06 |
| JP2013520436A5 true JP2013520436A5 (https=) | 2014-03-20 |
| JP5858434B2 JP5858434B2 (ja) | 2016-02-10 |
Family
ID=44227587
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012554055A Active JP5858434B2 (ja) | 2010-02-18 | 2011-02-18 | Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20110207754A1 (https=) |
| EP (1) | EP2536729A1 (https=) |
| JP (1) | JP5858434B2 (https=) |
| KR (1) | KR101836538B1 (https=) |
| CN (1) | CN102844317B (https=) |
| AU (1) | AU2011217961B2 (https=) |
| BR (1) | BR112012020693B1 (https=) |
| CA (1) | CA2790070C (https=) |
| EA (1) | EA023444B1 (https=) |
| MX (1) | MX2012009541A (https=) |
| WO (1) | WO2011103423A1 (https=) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| 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 |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| CA3121743A1 (en) | 2009-01-15 | 2010-07-22 | Incyte Holdings Corporation | Processes for preparing jak inhibitors and related intermediate compounds |
| 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 |
| SG176111A1 (en) * | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| 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 |
| KR101921850B1 (ko) | 2009-10-09 | 2018-11-23 | 인사이트 홀딩스 코포레이션 | 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| PT3354652T (pt) | 2010-03-10 | 2020-07-20 | Incyte Holdings Corp | Derivados de piperidin-4-ilazetidina como inibidores de jak1 |
| RS54824B1 (sr) | 2010-05-21 | 2016-10-31 | Incyte Holdings Corp | Topikalna formulacija za inhibiciju jak-a |
| 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 |
| CA2827673C (en) | 2011-02-18 | 2020-10-27 | Novartis Pharma Ag | Mtor/jak inhibitor combination therapy |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | Novartis Pharma AG | JAK P13K/mTOR COMBINATION THERAPY |
| 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 |
| WO2013041042A1 (en) * | 2011-09-22 | 2013-03-28 | Merck Sharp & Dohme Corp. | Pyrazole carboxamides as janus kinase inhibitors |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| 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 |
| CN113384546A (zh) | 2012-11-15 | 2021-09-14 | 因赛特公司 | 鲁索利替尼的缓释剂型 |
| EP2951590A1 (en) | 2013-02-04 | 2015-12-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| WO2014138168A1 (en) | 2013-03-06 | 2014-09-12 | Incyte Corporation | Processes and intermediates for making a jak inhibitor |
| US20140343034A1 (en) * | 2013-04-25 | 2014-11-20 | Japan Tobacco Inc. | Skin barrier function improving agent |
| 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 |
| CN105555313A (zh) | 2013-08-20 | 2016-05-04 | 因赛特公司 | 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处 |
| PH12020552277A1 (en) | 2014-04-08 | 2023-07-17 | Incyte Holdings Corp | Treatment of b-cell malignancies by a combination jak and pi3k 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 |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
| WO2018189335A1 (en) | 2017-04-13 | 2018-10-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| EA202091830A1 (ru) | 2018-01-30 | 2020-12-29 | Инсайт Корпорейшн | Способы и промежуточные соединения для получения ингибитора jak |
| IL311485B1 (en) | 2018-02-16 | 2026-01-01 | Incyte Corp | JAK1 pathway inhibitors for the treatment of cytokine-related disorders |
| WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| MD3773593T2 (ro) | 2018-03-30 | 2024-10-31 | Incyte Corp | Tratament hidradenitei supurative utilizând inhibitori ai JAK |
| CA3097025A1 (en) | 2018-04-13 | 2019-10-17 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| CA3101323A1 (en) | 2018-06-01 | 2019-12-05 | Incyte Corporation | Dosing regimen for the treatment of pi3k related disorders |
| CA3117969A1 (en) | 2018-10-31 | 2020-05-07 | Incyte Corporation | Combination therapy for treatment of hematological diseases |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| EP4041204A1 (en) | 2019-10-10 | 2022-08-17 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| CN115038443A (zh) | 2019-11-22 | 2022-09-09 | 因西特公司 | 包含alk2抑制剂和jak2抑制剂的组合疗法 |
| FI4157831T3 (fi) | 2020-06-02 | 2024-12-02 | Incyte Corp | Menetelmiä jak1-estäjän valmistamiseksi |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CA3192099A1 (en) | 2020-08-18 | 2022-02-24 | Incyte Corporation | Process and intermediates for preparing a jak inhibitor |
| CR20230130A (es) | 2020-08-18 | 2023-07-13 | Incyte Corp | Proceso e intermedios para preparar un inhibidor de jak1 |
| WO2022125670A1 (en) | 2020-12-08 | 2022-06-16 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of vitiligo |
| RS67455B1 (sr) | 2021-05-03 | 2025-12-31 | Incyte Corp | Inhibitori jak1 puta za lečenje prurigo nodularisa |
| CN118317946A (zh) | 2021-07-12 | 2024-07-09 | 因赛特公司 | 用于制备巴瑞替尼的方法和中间体 |
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-
2011
- 2011-02-18 EP EP11706997A patent/EP2536729A1/en not_active Withdrawn
- 2011-02-18 EA EA201290807A patent/EA023444B1/ru unknown
- 2011-02-18 JP JP2012554055A patent/JP5858434B2/ja active Active
- 2011-02-18 US US13/030,682 patent/US20110207754A1/en not_active Abandoned
- 2011-02-18 WO PCT/US2011/025433 patent/WO2011103423A1/en not_active Ceased
- 2011-02-18 BR BR112012020693-1A patent/BR112012020693B1/pt active IP Right Grant
- 2011-02-18 CN CN201180019267.XA patent/CN102844317B/zh active Active
- 2011-02-18 MX MX2012009541A patent/MX2012009541A/es unknown
- 2011-02-18 KR KR1020127023358A patent/KR101836538B1/ko active Active
- 2011-02-18 AU AU2011217961A patent/AU2011217961B2/en active Active
- 2011-02-18 CA CA2790070A patent/CA2790070C/en active Active
-
2014
- 2014-09-29 US US14/499,916 patent/US20150087662A1/en not_active Abandoned
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