JP2014521725A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014521725A5 JP2014521725A5 JP2014525162A JP2014525162A JP2014521725A5 JP 2014521725 A5 JP2014521725 A5 JP 2014521725A5 JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014521725 A5 JP2014521725 A5 JP 2014521725A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- pharmaceutically acceptable
- acceptable salt
- methyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 239000000203 mixture Substances 0.000 claims 17
- 238000009472 formulation Methods 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 9
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims 9
- 239000002552 dosage form Substances 0.000 claims 8
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 8
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 5
- 208000003476 primary myelofibrosis Diseases 0.000 claims 5
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 206010028537 myelofibrosis Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 208000037244 polycythemia vera Diseases 0.000 claims 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 239000002207 metabolite Substances 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- -1 (3R) -3-cyclopentyl-3- [4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl] propanenitrile phosphorus Chemical compound 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 208000033755 Neutrophilic Chronic Leukemia Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 208000021668 chronic eosinophilic leukemia Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161522001P | 2011-08-10 | 2011-08-10 | |
| US61/522,001 | 2011-08-10 | ||
| PCT/US2012/050252 WO2013023119A1 (en) | 2011-08-10 | 2012-08-10 | JAK P13K/mTOR COMBINATION THERAPY |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014521725A JP2014521725A (ja) | 2014-08-28 |
| JP2014521725A5 true JP2014521725A5 (enExample) | 2015-09-17 |
Family
ID=46690743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014525162A Pending JP2014521725A (ja) | 2011-08-10 | 2012-08-10 | ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9358229B2 (enExample) |
| EP (1) | EP2741747A1 (enExample) |
| JP (1) | JP2014521725A (enExample) |
| CA (1) | CA2844507A1 (enExample) |
| HK (1) | HK1198579A1 (enExample) |
| WO (1) | WO2013023119A1 (enExample) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| 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. |
| JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| ES2487542T3 (es) * | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2010135621A1 (en) * | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| JP2014521725A (ja) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 |
| 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 |
| BR112014011645A2 (pt) * | 2011-11-15 | 2017-05-02 | Novartis Ag | combinação de um inibidor da fosfoinositida 3-quinase e um modulador da quinase janus 2-transdutor de sinal e ativador da via de transcrição 5 |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| US9181271B2 (en) | 2012-11-01 | 2015-11-10 | Incyte Holdings Corporation | Tricyclic fused thiophene derivatives as JAK inhibitors |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| KR20160104612A (ko) | 2013-07-26 | 2016-09-05 | 업데이트 파마 인코포레이트 | 비산트렌의 치료 효과 개선용 조성물 |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| CN104744302A (zh) * | 2013-12-31 | 2015-07-01 | 上海药谷药业有限公司 | 一种2-(4-氨基苯基)-2-甲基丙腈化合物的制备方法 |
| MA39984B1 (fr) * | 2014-04-08 | 2020-12-31 | Incyte Corp | Traitement d'affections malignes par lymphocytes b par un inhibiteur jak et pi3k combiné |
| MA39987A (fr) | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US10576076B2 (en) | 2015-05-20 | 2020-03-03 | Novartis Ag | Pharmaceutical combination of everolimus with dactolisib |
| US20180147203A1 (en) * | 2015-05-29 | 2018-05-31 | Portola Pharmaceuticals, Inc. | Cerdulatinib for the treatment of b-cell malignancies |
| EP3383396B1 (en) | 2015-12-04 | 2023-07-12 | Alexion Pharmaceuticals, Inc. | Cerdulatinib and venetoclax for treating non-hodgkin's lymphoma |
| ES2886587T3 (es) | 2016-04-15 | 2021-12-20 | Cancer Research Tech Ltd | Compuestos heterocíclicos como inhibidores de la quinasa RET |
| EP4104837A3 (en) | 2016-04-15 | 2023-04-26 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| AU2017363970A1 (en) | 2016-11-23 | 2019-06-20 | Novartis Ag | Methods of enhancing immune response with everolimus, dactolisib or both |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| CN110770243A (zh) | 2017-05-02 | 2020-02-07 | 锐新医药公司 | 作为mtor抑制剂的雷帕霉素类似物 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| IL276302B2 (en) | 2018-01-30 | 2023-11-01 | Incyte Corp | Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one) |
| WO2019157516A1 (en) | 2018-02-12 | 2019-08-15 | resTORbio, Inc. | Combination therapies |
| CN118490690A (zh) | 2018-02-16 | 2024-08-16 | 因赛特公司 | 用于治疗细胞因子相关的病症的jak1通路抑制剂 |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| US11584961B2 (en) | 2018-03-30 | 2023-02-21 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| AU2019252259A1 (en) | 2018-04-13 | 2020-12-03 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US20190336609A1 (en) | 2018-05-01 | 2019-11-07 | Revolution Medicines, Inc. | C40-, C28-, and C-32-Linked Rapamycin Analogs as mTOR Inhibitors |
| MX2020011564A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina unidos a c26 como inhibidores de mtor. |
| JP7324778B2 (ja) | 2018-05-04 | 2023-08-10 | ポートラ ファーマシューティカルズ， エルエルシー | セルデュラチニブ（ｃｅｒｄｕｌａｔｉｎｉｂ）の固体形態 |
| CN112469418A (zh) | 2018-06-01 | 2021-03-09 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| CN113490484B (zh) | 2018-10-31 | 2024-08-23 | 因赛特公司 | 治疗血液疾病的组合疗法 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| US12203942B2 (en) | 2019-10-10 | 2025-01-21 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| CR20220280A (es) | 2019-11-22 | 2022-09-02 | Incyte Corp | Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2 |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US11957661B2 (en) | 2020-12-08 | 2024-04-16 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of vitiligo |
| IL308216A (en) | 2021-05-03 | 2024-01-01 | Incyte Corp | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| US20240082249A1 (en) | 2022-05-25 | 2024-03-14 | Revolution Medicines, Inc. | Methods of treating cancer with an mtor inhibitor |
Family Cites Families (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3036390A1 (de) | 1980-09-26 | 1982-05-13 | Troponwerke GmbH & Co KG, 5000 Köln | Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| JP4010563B2 (ja) | 1995-07-05 | 2007-11-21 | イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー | 殺菌・殺カビ性のピリミジノン類 |
| EP1090009A2 (en) | 1998-06-04 | 2001-04-11 | Abbott Laboratories | Cell adhesion-inhibiting antinflammatory compounds |
| 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 |
| CZ20004727A3 (cs) | 1998-06-19 | 2002-03-13 | Pfizer Products Inc. | Deriváty pyrrolo[2,3-d] pyrimidinu |
| CN1152031C (zh) | 1998-08-11 | 2004-06-02 | 诺瓦提斯公司 | 具有血管生成抑制活性的异喹啉衍生物 |
| 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 |
| AU777911B2 (en) | 1999-12-10 | 2004-11-04 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| WO2001047922A2 (en) | 1999-12-24 | 2001-07-05 | Aventis Pharma Limited | Azaindoles |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| AU4878601A (en) | 2000-04-20 | 2001-11-07 | Mitsubishi Corporation | Aromatic amide 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 |
| EP1295607B9 (en) | 2000-06-23 | 2011-10-05 | Mitsubishi Tanabe Pharma Corporation | Antitumor effect potentiators |
| UA74370C2 (uk) | 2000-06-26 | 2005-12-15 | Пфайзер Продактс Інк. | Піроло(2,3-d)піримідинові сполуки як імуносупресори |
| PL202623B1 (pl) | 2000-06-28 | 2009-07-31 | Smithkline Beecham Plc | Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna |
| GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
| WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
| US6884804B2 (en) | 2001-05-16 | 2005-04-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and other protein kinases |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| US6852727B2 (en) | 2001-08-01 | 2005-02-08 | Merck & Co., Inc. | Benzimisazo[4,5-f]isoquinolinone derivatives |
| AU2002337142B2 (en) | 2001-09-19 | 2007-10-11 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| TWI302836B (en) | 2001-10-30 | 2008-11-11 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
| GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
| TW200403058A (en) | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
| US7304061B2 (en) | 2002-04-26 | 2007-12-04 | Vertex Pharmaceuticals Incorporated | Heterocyclic inhibitors of ERK2 and uses thereof |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| JPWO2004007472A1 (ja) | 2002-07-10 | 2005-11-17 | 小野薬品工業株式会社 | Ｃｃｒ４アンタゴニストおよびその医薬用途 |
| ATE371656T1 (de) | 2002-11-04 | 2007-09-15 | Vertex Pharma | Heteroaryl-pyrimidinderivate als jak-inhibitoren |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| BR0316487A (pt) | 2002-11-26 | 2005-10-11 | Pfizer Prod Inc | Método todo de tratamento da rejeição de transplantes |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| WO2004072063A1 (en) | 2003-02-07 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrolls useful as inhibitors of protein kinases |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| SE0301373D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| US20050043346A1 (en) | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| BRPI0416909A (pt) | 2003-11-25 | 2007-01-16 | Pfizer Prod Inc | método de tratamento de aterosclerose |
| SG133602A1 (en) | 2003-12-17 | 2007-07-30 | Pfizer Prod Inc | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
| US20050165029A1 (en) | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| CA2560454C (en) | 2004-03-30 | 2013-05-21 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of jak and other protein kinases |
| US20060106020A1 (en) | 2004-04-28 | 2006-05-18 | Rodgers James D | Tetracyclic inhibitors of Janus kinases |
| WO2005105988A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
| EP2363149A1 (en) | 2004-05-03 | 2011-09-07 | Novartis AG | Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor |
| CA2566158A1 (en) | 2004-05-14 | 2005-11-24 | Abbott Laboratories | Kinase inhibitors as therapeutic agents |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| US8039674B2 (en) | 2004-06-23 | 2011-10-18 | Ono Pharmaceutical Co., Ltd. | Compound having S1P receptor binding potency and use thereof |
| WO2006013114A1 (en) | 2004-08-06 | 2006-02-09 | Develogen Aktiengesellschaft | Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome |
| UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| 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. |
| ES2320487T3 (es) | 2005-02-03 | 2009-05-22 | Vertex Pharmaceuticals, Inc. | Pirrolopirimidinas utiles como inhibidores de proteina quinasas. |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| ES2380795T3 (es) | 2005-05-20 | 2012-05-18 | Vertex Pharmaceuticals, Inc. | Pirrolopiridinas útiles como inhibidores de proteínas quinasas |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| WO2006136823A1 (en) | 2005-06-21 | 2006-12-28 | Astex Therapeutics Limited | Heterocyclic containing amines as kinase b inhibitors |
| DK2395004T3 (en) | 2005-06-22 | 2016-03-21 | Plexxikon Inc | Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors |
| CN102127078A (zh) | 2005-07-14 | 2011-07-20 | 安斯泰来制药株式会社 | Janus激酶3的杂环类抑制剂 |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| ES2401192T3 (es) | 2005-09-30 | 2013-04-17 | Vertex Pharmceuticals Incorporated | Deazapurinas útiles como inhibidores de janus cinasas |
| WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
| US20130137681A1 (en) | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP1968568A4 (en) | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| EP2537849A3 (en) | 2006-01-17 | 2013-04-03 | Vertex Pharmaceuticals, Inc. | Azaindoles useful as inhibitors of janus kinases |
| EP1979353A2 (en) | 2006-01-19 | 2008-10-15 | OSI Pharmaceuticals, Inc. | Fused heterobicyclic kinase inhibitors |
| WO2007090141A2 (en) | 2006-02-01 | 2007-08-09 | Smithkline Beecham Corporation | Pyrrolo [2, 3, b] pyridine derivatives useful as raf kinase inhibitors |
| RU2008143361A (ru) | 2006-04-05 | 2010-05-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Деазапурины в качестве ингибиторов янус-киназ |
| US8513270B2 (en) | 2006-12-22 | 2013-08-20 | Incyte Corporation | Substituted heterocycles as Janus kinase inhibitors |
| CN101616672A (zh) | 2007-02-20 | 2009-12-30 | 诺瓦提斯公司 | 作为脂质激酶和mTOR双重抑制剂的咪唑并喹啉类 |
| GB0710528D0 (en) | 2007-06-01 | 2007-07-11 | Glaxo Group Ltd | Novel compounds |
| 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. |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
| BRPI0820544A2 (pt) | 2007-11-16 | 2015-06-16 | Incyte Corp | 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase |
| ES2602577T3 (es) | 2008-03-11 | 2017-02-21 | Incyte Holdings Corporation | Derivados de azetidina y ciclobutano como inhibidores de JAK |
| KR101084528B1 (ko) | 2008-04-15 | 2011-11-18 | 인비트로겐 싱가포르 피티이. 엘티디. | 전기천공 장치용 파이펫 팁 |
| 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 |
| EP2210890A1 (en) | 2009-01-19 | 2010-07-28 | Almirall, S.A. | Oxadiazole derivatives as S1P1 receptor agonists |
| ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| CA2777114C (en) * | 2009-10-09 | 2018-10-23 | Incyte Corporation | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| AU2011217961B2 (en) | 2010-02-18 | 2016-05-05 | Incyte Holdings Corporation | Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| JP2014521725A (ja) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 |
| 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 |
-
2012
- 2012-08-10 JP JP2014525162A patent/JP2014521725A/ja active Pending
- 2012-08-10 HK HK14112079.3A patent/HK1198579A1/xx unknown
- 2012-08-10 CA CA2844507A patent/CA2844507A1/en not_active Abandoned
- 2012-08-10 WO PCT/US2012/050252 patent/WO2013023119A1/en not_active Ceased
- 2012-08-10 EP EP12748346.9A patent/EP2741747A1/en not_active Withdrawn
- 2012-08-10 US US13/571,525 patent/US9358229B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014521725A5 (enExample) | ||
| JP2014505735A5 (enExample) | ||
| US9358229B2 (en) | JAK PI3K/mTOR combination therapy | |
| JP2014505696A5 (enExample) | ||
| EP2488178B1 (en) | Combinations of a pi3k inhibitor and a mek inhibitor | |
| JP2014139226A5 (enExample) | ||
| JP2013529196A5 (enExample) | ||
| JP2019510832A5 (enExample) | ||
| JP2012520861A5 (enExample) | ||
| JP2015529194A5 (enExample) | ||
| JP2011507854A5 (enExample) | ||
| JP2015518894A5 (enExample) | ||
| JP2016522835A5 (enExample) | ||
| JP2013510120A5 (enExample) | ||
| JP2016523974A5 (enExample) | ||
| RU2016141569A (ru) | Комбинации | |
| JP2018517686A5 (enExample) | ||
| JP2014513110A5 (enExample) | ||
| JP2016525076A5 (enExample) | ||
| RU2015108755A (ru) | Комбинация ингибитора pik3 и ингибитора с-мет | |
| JP2017504635A5 (enExample) | ||
| RU2014154009A (ru) | Комбинация ингибитора 17-альфа-гидроксилазы (с17,20-лиазы) и специфического ингибитора pi-3k для лечения онкологического заболевания | |
| JP2017517538A5 (enExample) | ||
| JP2013523814A5 (enExample) | ||
| JP2013518904A5 (enExample) |