JP2013520436A5 - - Google Patents
Download PDFInfo
- 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
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2536729A1 (enExample) |
| JP (1) | JP5858434B2 (enExample) |
| KR (1) | KR101836538B1 (enExample) |
| CN (1) | CN102844317B (enExample) |
| AU (1) | AU2011217961B2 (enExample) |
| BR (1) | BR112012020693B1 (enExample) |
| CA (1) | CA2790070C (enExample) |
| EA (1) | EA023444B1 (enExample) |
| MX (1) | MX2012009541A (enExample) |
| WO (1) | WO2011103423A1 (enExample) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1966202E (pt) | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| 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. |
| RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
| 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. |
| JOP20190231A1 (ar) * | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| PL2432472T3 (pl) | 2009-05-22 | 2020-03-31 | Incyte Holdings Corporation | 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| ES2435491T3 (es) | 2009-10-09 | 2013-12-19 | Incyte Corporation | Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
| MX354212B (es) | 2010-03-10 | 2018-02-19 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| 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 |
| EP2675451B9 (en) | 2011-02-18 | 2017-07-26 | Novartis Pharma AG | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| HK1198579A1 (en) | 2011-08-10 | 2015-04-30 | 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 |
| US9394282B2 (en) * | 2011-09-22 | 2016-07-19 | Merck Sharp & Dohme Corp. | Pyrazole carboxamides as Janus kinase inhibitors |
| CA2856722C (en) | 2011-11-30 | 2022-11-22 | Emory University | Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| BR112015009942A2 (pt) | 2012-11-01 | 2017-07-11 | Incyte Corp | derivados de tiofeno fundidos tricíclicos como inibidores de jak |
| NZ708157A (en) | 2012-11-15 | 2019-07-26 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| US20160123982A1 (en) | 2013-02-04 | 2016-05-05 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| TWI634121B (zh) | 2013-03-06 | 2018-09-01 | 英塞特控股公司 | 用於製備ｊａｋ抑制劑之方法及中間物 |
| US20140343034A1 (en) * | 2013-04-25 | 2014-11-20 | Japan Tobacco Inc. | Skin barrier function improving agent |
| WO2014186706A1 (en) | 2013-05-17 | 2014-11-20 | Incyte Corporation | Bipyrazole derivatives as jak inhibitors |
| MX394928B (es) | 2013-08-07 | 2025-03-24 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| 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 |
| HRP20201887T1 (hr) | 2014-04-08 | 2021-02-05 | Incyte Corporation | LIJEČENJE B-STANIČNIH MALIGNITETA S KOMBINACIJOM INHIBITORA JAK i PI3K |
| SG11201609016VA (en) | 2014-04-30 | 2016-11-29 | Incyte Corp | Processes of preparing a jak1 inhibitor and new forms thereto |
| 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 |
| US20200088732A1 (en) | 2017-04-13 | 2020-03-19 | INSERM (Institut National de la Santé et de la Recherche Mèdicale) | 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 |
| WO2019152374A1 (en) | 2018-01-30 | 2019-08-08 | Incyte Corporation | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| WO2019161098A1 (en) | 2018-02-16 | 2019-08-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
| HUE067471T2 (hu) | 2018-03-30 | 2024-10-28 | Incyte Corp | Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával |
| US11584961B2 (en) | 2018-03-30 | 2023-02-21 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| US11372003B2 (en) | 2018-04-13 | 2022-06-28 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| BR112020024427A2 (pt) | 2018-06-01 | 2021-03-23 | Incyte Corporation | regime de dosagem para o tratamento de distúrbios relacionados a pi3k |
| KR20210109522A (ko) | 2018-10-31 | 2021-09-06 | 인사이트 코포레이션 | 혈액 질환의 치료를 위한 병용 요법 |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| KR20220088699A (ko) | 2019-09-27 | 2022-06-28 | 디스크 메디슨, 인크. | 골수섬유증 및 관련 상태의 치료 방법 |
| 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 |
| CA3160312A1 (en) | 2019-11-22 | 2021-05-27 | Incyte Corporation | Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor |
| JP2023528868A (ja) | 2020-06-02 | 2023-07-06 | インサイト・コーポレイション | Ｊａｋ１阻害剤の調製プロセス |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| BR112023002939A2 (pt) | 2020-08-18 | 2023-04-25 | Incyte Corp | Processo e intermediários para preparar um inibidor de jak1 |
| WO2022040180A1 (en) | 2020-08-18 | 2022-02-24 | Incyte Corporation | Process and intermediates for preparing a jak inhibitor |
| JP2023552452A (ja) | 2020-12-08 | 2023-12-15 | インサイト・コーポレイション | 白斑治療用のｊａｋ１経路阻害薬 |
| US12268667B2 (en) | 2021-05-03 | 2025-04-08 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of prurigo nodularis |
| JP2024526762A (ja) | 2021-07-12 | 2024-07-19 | インサイト・コーポレイション | Ｊａｋ阻害剤を調製するためのプロセス及び中間体 |
Family Cites Families (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| US6232320B1 (en) * | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| BR9912938B1 (pt) | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| MXPA02006338A (es) * | 1999-12-24 | 2002-12-13 | Aventis Pharma Ltd | Azaindoles. |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US6335342B1 (en) * | 2000-06-19 | 2002-01-01 | Pharmacia & Upjohn S.P.A. | Azaindole derivatives, process for their preparation, and their use as antitumor agents |
| DE60141963D1 (de) * | 2000-06-23 | 2010-06-10 | Mitsubishi Tanabe Pharma Corp | Antitumoreffekt-verstärker |
| ES2225624T3 (es) | 2000-06-28 | 2005-03-16 | Smithkline Beecham Plc | Procedimiento de molienda por via humeda. |
| CA2446864C (en) * | 2001-05-16 | 2011-02-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of src and other protein kinases |
| ES2274986T3 (es) * | 2001-08-01 | 2007-06-01 | MERCK & CO., INC. | Derivados de benzimidazo 4,5-f/isoquinolinona. |
| ATE420879T1 (de) | 2001-09-19 | 2009-01-15 | Aventis Pharma Sa | Indolizine als kinaseproteinhemmer |
| US7973031B2 (en) | 2001-10-30 | 2011-07-05 | Novartis Ag | Staurosporine derivatives as inhibitors of FLT3 receptor tyrosine kinase activity |
| TW200403058A (en) * | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
| EP1506189A1 (en) * | 2002-04-26 | 2005-02-16 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| AR037647A1 (es) | 2002-05-29 | 2004-12-01 | Novartis Ag | Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| EP1541563A4 (en) * | 2002-07-10 | 2007-11-07 | Ono Pharmaceutical Co | ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE |
| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| WO2005067546A2 (en) * | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| US20060106020A1 (en) * | 2004-04-28 | 2006-05-18 | Rodgers James D | Tetracyclic inhibitors of Janus kinases |
| BRPI0511978A (pt) | 2004-06-10 | 2008-01-22 | Irm Llc | compostos e composições como inibidores de proteìnas quinases |
| WO2006001463A1 (ja) * | 2004-06-23 | 2006-01-05 | Ono Pharmaceutical Co., Ltd. | Ｓ１ｐ受容体結合能を有する化合物およびその用途 |
| JP2008520612A (ja) | 2004-11-24 | 2008-06-19 | ノバルティス アクチエンゲゼルシャフト | ＪＡＫ阻害剤およびＢｃｒ−Ａｂｌ、Ｆｌｔ−３、ＦＡＫまたはＲＡＦキナーゼ阻害剤のうち少なくとも１個の組合せ |
| AR054416A1 (es) * | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| KR20070104641A (ko) * | 2005-02-03 | 2007-10-26 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로 유용한 피롤로피리미딘 |
| NZ564065A (en) * | 2005-05-20 | 2011-03-31 | Vertex Pharma | Pyrrolopyridines useful as inhibitors of protein kinase |
| EP1926735A1 (en) * | 2005-09-22 | 2008-06-04 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| PT1966202E (pt) * | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| US20070208053A1 (en) * | 2006-01-19 | 2007-09-06 | Arnold Lee D | Fused heterobicyclic kinase inhibitors |
| EP1981887A2 (en) * | 2006-02-01 | 2008-10-22 | SmithKline Beecham Corporation | Pyrrolo[2,3,b]pyridine derivatives useful as raf kinase inhibitors |
| CA2648250A1 (en) * | 2006-04-05 | 2007-10-18 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| US8111686B2 (en) * | 2006-08-07 | 2012-02-07 | Microsoft Corporation | Aggregating endpoint capabilities for a user |
| EP1918291A1 (en) * | 2006-10-30 | 2008-05-07 | Novartis AG | 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators |
| EP2121692B1 (en) * | 2006-12-22 | 2013-04-10 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
| RS53245B2 (sr) * | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
| 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. |
| WO2009064835A1 (en) * | 2007-11-16 | 2009-05-22 | Incyte Corporation | 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors |
| WO2009073575A2 (en) * | 2007-11-30 | 2009-06-11 | Oregon Health & Science University | Methods for treating induced cellular proliferative disorders |
| BRPI0909040B8 (pt) * | 2008-03-11 | 2021-05-25 | Incyte Holdings Corp | derivados de azetidina e ciclobutano, seus usos, e composição |
| JOP20190231A1 (ar) * | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| TW201100429A (en) * | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| TW201113285A (en) * | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| ES2435491T3 (es) * | 2009-10-09 | 2013-12-19 | Incyte Corporation | Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
-
2011
- 2011-02-18 CN CN201180019267.XA patent/CN102844317B/zh active Active
- 2011-02-18 AU AU2011217961A patent/AU2011217961B2/en active Active
- 2011-02-18 KR KR1020127023358A patent/KR101836538B1/ko active Active
- 2011-02-18 EP EP11706997A patent/EP2536729A1/en not_active Withdrawn
- 2011-02-18 US US13/030,682 patent/US20110207754A1/en not_active Abandoned
- 2011-02-18 CA CA2790070A patent/CA2790070C/en active Active
- 2011-02-18 BR BR112012020693-1A patent/BR112012020693B1/pt active IP Right Grant
- 2011-02-18 WO PCT/US2011/025433 patent/WO2011103423A1/en not_active Ceased
- 2011-02-18 EA EA201290807A patent/EA023444B1/ru unknown
- 2011-02-18 MX MX2012009541A patent/MX2012009541A/es unknown
- 2011-02-18 JP JP2012554055A patent/JP5858434B2/ja active Active
-
2014
- 2014-09-29 US US14/499,916 patent/US20150087662A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013520436A5 (enExample) | ||
| JP2014520146A5 (enExample) | ||
| JP2010529208A5 (enExample) | ||
| JP2016519147A5 (enExample) | ||
| HRP20200955T1 (hr) | Dozni oblici s produženim oslobađanjem za jak1 inhibitor | |
| ME02904B (me) | DERIVATI PIROLO[2,3 -d]PIRIMIDINA KAO INHIBITORI JANUS KINAZA (JAK) | |
| NZ602313A (en) | Piperidin-4-yl azetidine derivatives as jak1 inhibitors | |
| HRP20140541T4 (hr) | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila | |
| JP2010529209A5 (enExample) | ||
| JP2015527401A5 (enExample) | ||
| HRP20170795T1 (hr) | Derivati bipirazola kao inhibitori jak | |
| ME02856B (me) | Aminopirimidinilni spojevi kao inhibitori jak | |
| SI3008053T1 (en) | PHOSPHATIDYLINOSITOL 3-KINATE INHIBITORS | |
| CL2013002228A1 (es) | Compuestos derivados de pirrolo[2,3-b]piridina, modulador de quinasa b-raf; composiciones farmaceuticas; procedimientos de preparacion; utiles en el tratamiento de la isquemia, alzheimer, parkinson, demencia, tumores, leucemia, artritis reumatoide, miastenia gravis, enfermedad renal, entre otras. | |
| NZ629432A (en) | Heterocyclyl compounds as mek inhibitors | |
| JP2016028076A5 (enExample) | ||
| JP2011252024A5 (enExample) | ||
| PE20121276A1 (es) | Compuestos espirociclicos que contienen nitrogeno y su uso medicinal | |
| HRP20192203T1 (hr) | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori | |
| JP2015501327A5 (enExample) | ||
| EA201290973A1 (ru) | Соединения и способы модулирования киназ и показания по их применению | |
| RS67061B1 (sr) | Deuterisani derivati ruksolitiniba | |
| JP2013514356A5 (enExample) | ||
| IN2012CH01573A (enExample) | ||
| NZ590320A (en) | Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases |