JP2014521725A - ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 - Google Patents

ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 Download PDF

Info

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
Application number
JP2014525162A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014521725A5 (OSRAM
Inventor
アレッサンドロ・エンメ・ヴァンヌッキ
コスタンツァ・ボガーニ
ニッコロ・ヴァルタルッチ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis Pharma AG
Incyte Corp
Original Assignee
Novartis Pharma AG
Incyte Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Pharma AG, Incyte Corp filed Critical Novartis Pharma AG
Publication of JP2014521725A publication Critical patent/JP2014521725A/ja
Publication of JP2014521725A5 publication Critical patent/JP2014521725A5/ja
Pending legal-status Critical Current

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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2014525162A 2011-08-10 2012-08-10 ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 Pending JP2014521725A (ja)

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 (OSRAM) 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 (OSRAM)
EP (1) EP2741747A1 (OSRAM)
JP (1) JP2014521725A (OSRAM)
CA (1) CA2844507A1 (OSRAM)
HK (1) HK1198579A1 (OSRAM)
WO (1) WO2013023119A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
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 (55)

* Cited by examiner, † Cited by third party
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
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.
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
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
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
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
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
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
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
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).
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
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
EP3297629A1 (en) 2015-05-20 2018-03-28 Novartis AG Pharmaceutical combination of everolimus with dactolisib
CN107683139A (zh) * 2015-05-29 2018-02-09 博尔托拉制药公司 用于治疗b细胞恶性肿瘤的赛度替尼
WO2017096303A2 (en) 2015-12-04 2017-06-08 Portola Pharmaceuticals, Inc. Cerdulatinib for treating hematological cancers
LT3442535T (lt) 2016-04-15 2022-10-25 Cancer Research Technology Limited Heterocikliniai junginiai kaip ret kinazės inhibitoriai
RS62322B1 (sr) 2016-04-15 2021-10-29 Cancer Research Tech Ltd Heterociklična jedinjenja kao inhibitori ret kinaze
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
WO2018204416A1 (en) 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
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)
WO2019157516A1 (en) 2018-02-12 2019-08-15 resTORbio, Inc. Combination therapies
WO2019161098A1 (en) 2018-02-16 2019-08-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of cytokine-related disorders
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
KR102859103B1 (ko) 2018-05-01 2025-09-12 레볼루션 메디슨즈, 인크. mTOR 억제제로서의 C26-연결된 라파마이신 유사체
PE20212112A1 (es) 2018-05-01 2021-11-04 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 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
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
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
JP2023528223A (ja) 2020-05-13 2023-07-04 ディスク・メディシン・インコーポレイテッド 骨髄線維症を処置するための抗ヘモジュベリン（ｈｊｖ）抗体
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
US12268667B2 (en) 2021-05-03 2025-04-08 Incyte Corporation JAK1 pathway inhibitors for the treatment of prurigo nodularis
CA3256390A1 (en) 2022-05-25 2023-11-30 Revolution Medicines, Inc. CANCER TREATMENT METHODS USING AN MTOR INHIBITOR

Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
PL324486A1 (en) 1995-07-05 1998-05-25 Du Pont Fungicidal pyrimidinones
WO1999062908A2 (en) 1998-06-04 1999-12-09 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
EP1087970B1 (en) 1998-06-19 2004-04-28 Pfizer Products Inc. PYRROLO 2,3-d]PYRIMIDINE 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
CN1195755C (zh) 1999-12-10 2005-04-06 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物
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
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
DE60141963D1 (de) 2000-06-23 2010-06-10 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
SK17342002A3 (sk) 2000-06-26 2004-06-08 Pfizer Products Inc. Derivát pyrolo[2,3-d]pyrimidínu ako činidlo potlačujúce imunitu
ES2225624T3 (es) 2000-06-28 2005-03-16 Smithkline Beecham Plc Procedimiento de molienda por via humeda.
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
US20040102455A1 (en) 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
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
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
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
ES2289349T3 (es) 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
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
NZ539901A (en) 2002-11-26 2007-09-28 Pfizer Prod 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
JP2006518381A (ja) 2003-02-07 2006-08-10 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 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
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
MXPA06005882A (es) 2003-11-25 2006-06-27 Pfizer Prod Inc Metodo de tratamiento de la aterosclerosis.
CN1893952A (zh) 2003-12-17 2007-01-10 辉瑞产品公司 用于治疗移植排斥的吡咯并[2,3－d]嘧啶化合物
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
EP2332940B1 (en) 2004-03-30 2012-10-31 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
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
BRPI0510627A (pt) 2004-05-03 2007-10-30 Novartis Ag combinações que compreendem um agonista do receptor s1p e um inibidor da jak3 quinase
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
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
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.
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
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
TWI473808B (zh) 2005-06-22 2015-02-21 Plexxikon Inc 用於激酶調節的化合物及方法及其適應症
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
EP1926735A1 (en) 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
CN101801971A (zh) 2005-09-30 2010-08-11 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的脱氮嘌呤
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
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
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
CN102532134A (zh) 2006-01-17 2012-07-04 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的吖吲哚类
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
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
KR101472607B1 (ko) 2007-02-20 2014-12-15 노파르티스 아게 지질 키나제 및 ｍＴＯＲ의 이중 억제제로서의 이미다조퀴놀린
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
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
BRPI0909040B8 (pt) 2008-03-11 2021-05-25 Incyte Holdings Corp derivados de azetidina e ciclobutano, seus usos, e composição
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
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
CN102844317B (zh) 2010-02-18 2015-06-03 因西特公司 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
CA2844507A1 (en) 2013-02-14
EP2741747A1 (en) 2014-06-18
HK1198579A1 (en) 2015-04-30
US20130040973A1 (en) 2013-02-14
US9358229B2 (en) 2016-06-07
WO2013023119A1 (en) 2013-02-14

Similar Documents

Publication Publication Date Title
JP2014521725A (ja) ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法
RU2560153C2 (ru) Триазолпиридиновые соединения, ингибирующие jak, и способы
CN104428298B (zh) 取代的吡啶并嘧啶化合物及其作为flt3抑制剂的用途
TW202007396A (zh) Bcl-2抑制劑或Bcl-2/Bcl-xL抑制劑與BTK抑制劑的組合產品及其在預防和/或治療疾病中的用途
TWI726362B (zh) Bcl-2抑制劑與利妥昔單抗和/或苯達莫司汀或Bcl-2抑制劑與CHOP聯合用藥的協同抗腫瘤作用
US20240246915A1 (en) Aminonaphthoquinone compounds and pharmaceutical composition for blocking ubiquitination-proteasome system in diseases
CA2954999C (en) Fused quinoline compounds as pi3k, mtor inhibitors
AU2018251118A1 (en) Pharmaceutical composition containing MOR agonist and KOR agonist, and uses thereof
US20210386738A1 (en) Combination of prmt5 inhibitors and bcl-2 inhibitors
CA3145864A1 (en) Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof
TWI803541B (zh) 對於蛋白激酶具抑制活性之噻吩并[3,2-d]嘧啶化合物
TW202327611A (zh) 使用ｂｔｋ抑制劑和ｐ１３激酶抑制劑的組合治療癌症之方法
CN101137379B (zh) 用于治疗医学病症的cxcr4拮抗剂
HK40029610B (zh) 一种哒嗪类衍生物抑制剂、其制备方法和应用
HK40011011A (en) Cannabinoid receptor modulators
HK1208453B (en) Substituted pyridopyrimidine compounds and their use as flt3 inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150731

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150731

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20160712

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160719

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20170228