JP2014521725A - JAKPI3K/mTOR併用療法 - Google Patents
JAKPI3K/mTOR併用療法 Download PDFInfo
- Publication number
- JP2014521725A JP2014521725A JP2014525162A JP2014525162A JP2014521725A JP 2014521725 A JP2014521725 A JP 2014521725A JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014521725 A JP2014521725 A JP 2014521725A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- pharmaceutically acceptable
- methyl
- alkyl
- 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
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 true JP2014521725A (ja) | 2014-08-28 |
| JP2014521725A5 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) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014533294A (ja) * | 2011-11-15 | 2014-12-11 | ノバルティス アーゲー | ホスホイノシチド3−キナーゼ阻害剤およびヤヌスキナーゼ2−シグナル伝達兼転写活性化因子5経路の調節剤の組合せ |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| 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. |
| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| PE20211639A1 (es) | 2009-01-15 | 2021-08-24 | Incyte Holdings Corp | Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| MY156727A (en) * | 2009-05-22 | 2016-03-15 | 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 |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| 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 |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | 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 |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/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 |
| 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 |
| JP6359546B2 (ja) | 2012-11-01 | 2018-07-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害薬としての三環式縮合チオフェン誘導体 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
| CA2928568A1 (en) | 2013-07-26 | 2015-01-29 | Update Pharma Inc. | Combinatorial methods to improve the therapeutic benefit of bisantrene |
| SG11201600815WA (en) | 2013-08-07 | 2016-03-30 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| 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 |
| CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
| BR112016025427A2 (pt) | 2014-04-30 | 2017-08-15 | Incyte Corp | processos de preparação de um inibidor de jak1 e formas do mesmo |
| 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 |
| EP3297629A1 (en) | 2015-05-20 | 2018-03-28 | Novartis AG | Pharmaceutical combination of everolimus with dactolisib |
| WO2016196385A1 (en) * | 2015-05-29 | 2016-12-08 | Portola Pharmaceuticals, Inc. | Cerdulatinib for the treatment of b-cell malignancies |
| WO2017096303A2 (en) | 2015-12-04 | 2017-06-08 | Portola Pharmaceuticals, Inc. | Cerdulatinib for treating hematological cancers |
| EP3442980B1 (en) | 2016-04-15 | 2021-06-09 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| RS63609B1 (sr) | 2016-04-15 | 2022-10-31 | Cancer Research Tech Ltd | Heterociklična jedinjenja kao inhibitori ret kinaze |
| BR112019010470A2 (pt) | 2016-11-23 | 2019-09-10 | Novartis Ag | métodos de realce de resposta imune com everolimo, dactolisib ou ambos |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| IL303660A (en) | 2017-05-02 | 2023-08-01 | Revolution Medicines Inc | Rapamycin analogs as mtor inhibitors |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| JP7393348B2 (ja) | 2018-01-30 | 2023-12-06 | インサイト・コーポレイション | (1-(3-フルオロ-2(トリフルオロメチル)イソニコチニル)ピぺリジン―4-オン)を作製するためのプロセス及び中間体 |
| US10596165B2 (en) | 2018-02-12 | 2020-03-24 | resTORbio, Inc. | Combination therapies |
| UA127519C2 (uk) | 2018-02-16 | 2023-09-20 | Інсайт Корпорейшн | Інгібітори шляху jak1, призначені для лікування порушень, пов'язаних із цитокінами |
| CN113768934A (zh) | 2018-03-30 | 2021-12-10 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| JP7565798B2 (ja) | 2018-03-30 | 2024-10-11 | インサイト・コーポレイション | 炎症性皮膚疾患のバイオマーカー |
| MX2020010815A (es) | 2018-04-13 | 2020-12-11 | Incyte Corp | Biomarcadores para enfermedad de injerto contra hospedero. |
| CA3098698A1 (en) | 2018-05-01 | 2019-11-07 | Revolution Medicines, Inc. | C26-linked rapamycin analogs as mtor inhibitors |
| CN118978535A (zh) | 2018-05-01 | 2024-11-19 | 锐新医药公司 | 作为mTOR抑制剂的C40-、C28-及C-32连接的雷帕霉素类似物 |
| EP3788035B1 (en) | 2018-05-04 | 2024-08-07 | Alexion Pharmaceuticals, Inc. | Solid forms of cerdulatinib |
| MX2020012826A (es) | 2018-06-01 | 2021-03-09 | Incyte Corp | Regimen de dosificacion para el tratamiento de trastornos relacionados con fosfatidilinositol 3-cinasas (pi3k). |
| EA202191170A1 (ru) | 2018-10-31 | 2021-07-27 | Инсайт Корпорейшн | Комбинированная терапия для лечения гематологических заболеваний |
| JP2022549506A (ja) | 2019-09-27 | 2022-11-25 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症および関連状態を処置するための方法 |
| 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 |
| BR112022009710A2 (pt) | 2019-11-22 | 2022-08-09 | Incyte Corp | Terapia de combinação compreendendo um inibidor de alk2 e um inibidor de jak2 |
| KR20230012539A (ko) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| 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 |
| EP4696710A3 (en) | 2021-05-03 | 2026-05-06 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| JP2025522296A (ja) | 2022-05-25 | 2025-07-15 | レヴォリューション・メディスンズ,インコーポレイテッド | mTOR阻害剤によりがんを処置する方法 |
| US20250295666A1 (en) * | 2024-03-22 | 2025-09-25 | Certis Oncology Solutions, Inc. | Pi3k-alpha inhibitor and mtor inhibitor combinations for cancer treatment |
| WO2026020084A1 (en) * | 2024-07-18 | 2026-01-22 | The Trustees Of The University Of Pennsylvania | Combination of topical kinase inhibitors to achieve synergistic clearance of skin cancers and related lesions |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010529209A (ja) * | 2007-06-13 | 2010-08-26 | インサイト・コーポレイション | JANUSキナーゼ阻害剤(R)−3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルの塩 |
Family Cites Families (99)
| 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 |
| DE69618959T2 (de) | 1995-07-05 | 2002-08-29 | E.I. Du Pont De Nemours And Co., Wilmington | Pyrimidone und ihre verwendug als fungizide |
| KR20010052570A (ko) | 1998-06-04 | 2001-06-25 | 스티븐 에프. 웨인스톡 | 세포 유착을 억제하는 소염성 화합물 |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| PL198640B1 (pl) | 1998-06-19 | 2008-07-31 | Pfizer Prod Inc | Związki pirolo[2,3-d]pirymidynowe, środek farmaceutyczny i zastosowanie tych związków |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| EP1107964B8 (en) | 1998-08-11 | 2010-04-07 | Novartis AG | Isoquinoline derivatives with angiogenesis inhibiting activity |
| 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 |
| EA006227B1 (ru) | 1999-12-10 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА |
| EP1990343B1 (en) | 1999-12-24 | 2012-04-04 | 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 |
| CA2413313C (en) | 2000-06-23 | 2011-06-14 | Mitsubishi Pharma Corporation | Antitumor effect potentiators |
| EA006153B1 (ru) | 2000-06-26 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ |
| KR100786927B1 (ko) | 2000-06-28 | 2007-12-17 | 스미스클라인비이참피이엘시이 | 습식 분쇄방법 |
| GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
| EP1363702A4 (en) | 2001-01-30 | 2007-08-22 | Cytopia Pty Ltd | PROCESS FOR INHIBITING KINASES |
| AU2002308748A1 (en) | 2001-05-16 | 2002-11-25 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| AU2002355732B2 (en) | 2001-08-01 | 2006-11-09 | Merck Sharp & Dohme Corp. | Benzimidazo[4,5-f]isoquinolinone derivatives |
| AU2002337142B2 (en) | 2001-09-19 | 2007-10-11 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| IL161156A0 (en) | 2001-10-30 | 2004-08-31 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
| PY0228255A (es) | 2001-12-06 | 2004-06-01 | Pfizer Prod Inc | Compuestos cristalinos novedosos |
| TW200403058A (en) | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
| AU2003237121A1 (en) | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| TW200406374A (en) | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| AU2003252478A1 (en) | 2002-07-10 | 2004-02-02 | Ono Pharmaceutical Co., Ltd. | Ccr4 antagonist and medicinal use thereof |
| US7259161B2 (en) | 2002-11-04 | 2007-08-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| AU2003276591A1 (en) | 2002-11-26 | 2004-06-18 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| AU2004212421B2 (en) | 2003-02-07 | 2009-08-20 | 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 |
| AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
| CA2545192A1 (en) | 2003-11-25 | 2005-06-09 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| CA2549485A1 (en) | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
| US20050187389A1 (en) | 2004-01-13 | 2005-08-25 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| US7507826B2 (en) | 2004-03-30 | 2009-03-24 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
| WO2005105988A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
| WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| MXPA06012663A (es) | 2004-05-03 | 2007-01-16 | Novartis Ag | Combinaciones que comprenden un agonista del receptor s1p y un inhibidor de quinasa jak3. |
| JP2007537296A (ja) | 2004-05-14 | 2007-12-20 | アボット・ラボラトリーズ | 治療薬としてのキナーゼ阻害薬 |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| JP5315611B2 (ja) | 2004-06-23 | 2013-10-16 | 小野薬品工業株式会社 | S1p受容体結合能を有する化合物およびその用途 |
| 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 |
| 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 |
| 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 |
| KR20070085433A (ko) | 2004-11-24 | 2007-08-27 | 노파르티스 아게 | Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물 |
| 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. |
| EP1844050B1 (en) | 2005-02-03 | 2009-01-14 | Vertex Pharmaceuticals, Inc. | Pyrrolopyrimidines useful as inhibitors of protein kinase |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| KR20080016659A (ko) | 2005-05-20 | 2008-02-21 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로서 유용한 피롤로피리딘 |
| 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 |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| JP2009513571A (ja) | 2005-09-30 | 2009-04-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | ヤヌスキナーゼ阻害剤として有用なデアザプリン |
| WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| 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 |
| EP1968568A4 (en) | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| TW201412738A (zh) | 2006-01-17 | 2014-04-01 | Vertex Pharma | 適合作為傑納斯激酶(janus kinase)抑制劑之氮雜吲哚 |
| JP2009523812A (ja) | 2006-01-19 | 2009-06-25 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | 融合へテロ二環式キナーゼ阻害剤 |
| JP2009525350A (ja) | 2006-02-01 | 2009-07-09 | スミスクライン ビーチャム コーポレーション | Rafキナーゼ阻害薬として有用なピロロ[2,3,b]ピリジン誘導体 |
| CA2648250A1 (en) | 2006-04-05 | 2007-10-18 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| ES2415863T3 (es) | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
| RU2478387C2 (ru) | 2007-02-20 | 2013-04-10 | Новартис Аг | ИМИДАЗОХИНОЛИНЫ В КАЧЕСТВЕ ДВОЙНЫХ ИНГИБИТОРОВ ЛИПИДКИНАЗЫ И mTOR |
| 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. |
| WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
| MX2010005300A (es) | 2007-11-16 | 2010-06-25 | Incyte Corp | 4-pirazolil-n-arilpirimidin-2-aminas y 4-pirazolil-n-heteroarilpir imidin-2-aminas como inhibidores de cinasas janus. |
| TWI444382B (zh) | 2008-03-11 | 2014-07-11 | Incyte Corp | 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物 |
| 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. |
| PE20211639A1 (es) | 2009-01-15 | 2021-08-24 | Incyte Holdings Corp | Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado |
| EP2210890A1 (en) | 2009-01-19 | 2010-07-28 | Almirall, S.A. | Oxadiazole derivatives as S1P1 receptor agonists |
| MY156727A (en) | 2009-05-22 | 2016-03-15 | 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 |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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 |
| MX2012004180A (es) | 2009-10-09 | 2012-07-17 | Incyte Corp | Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. |
| CA2790070C (en) | 2010-02-18 | 2018-03-06 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| 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 |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | 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 |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/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 |
-
2012
- 2012-08-10 CA CA2844507A patent/CA2844507A1/en not_active Abandoned
- 2012-08-10 JP JP2014525162A patent/JP2014521725A/ja active Pending
- 2012-08-10 HK HK14112079.3A patent/HK1198579A1/xx unknown
- 2012-08-10 EP EP12748346.9A patent/EP2741747A1/en not_active Withdrawn
- 2012-08-10 US US13/571,525 patent/US9358229B2/en active Active
- 2012-08-10 WO PCT/US2012/050252 patent/WO2013023119A1/en not_active Ceased
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010529209A (ja) * | 2007-06-13 | 2010-08-26 | インサイト・コーポレイション | JANUSキナーゼ阻害剤(R)−3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルの塩 |
Non-Patent Citations (2)
| Title |
|---|
| FISKUS WARREN ET AL.: "Synergistic Activity of Combination JAK2 Kinase Inhibitor with PI3K/mTOR, MEK or PIM Kinase Inhibito", BLOOD, vol. 116, no. 21, JPN7016002042, November 2010 (2010-11-01), pages 798, ISSN: 0003361495 * |
| QUINTAS-CARDAMA, ALFONSO ET AL.: "Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications", BLOOD, vol. 115, no. 15, JPN7016002043, April 2010 (2010-04-01), pages 3109 - 3117, XP055035457, ISSN: 0003361496, DOI: 10.1182/blood-2009-04-214957 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014533294A (ja) * | 2011-11-15 | 2014-12-11 | ノバルティス アーゲー | ホスホイノシチド3−キナーゼ阻害剤およびヤヌスキナーゼ2−シグナル伝達兼転写活性化因子5経路の調節剤の組合せ |
Also Published As
| Publication number | Publication date |
|---|---|
| US9358229B2 (en) | 2016-06-07 |
| CA2844507A1 (en) | 2013-02-14 |
| WO2013023119A1 (en) | 2013-02-14 |
| US20130040973A1 (en) | 2013-02-14 |
| HK1198579A1 (en) | 2015-04-30 |
| EP2741747A1 (en) | 2014-06-18 |
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