CA2827673C - Mtor/jak inhibitor combination therapy - Google Patents

Mtor/jak inhibitor combination therapy Download PDF

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Publication number
CA2827673C
CA2827673C CA2827673A CA2827673A CA2827673C CA 2827673 C CA2827673 C CA 2827673C CA 2827673 A CA2827673 A CA 2827673A CA 2827673 A CA2827673 A CA 2827673A CA 2827673 C CA2827673 C CA 2827673C
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CA
Canada
Prior art keywords
compound
formula
mtor inhibitor
administration
pharmaceutically acceptable
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.)
Active
Application number
CA2827673A
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English (en)
French (fr)
Other versions
CA2827673A1 (en
Inventor
Alessandro M. Vannucchi
Costanza BOGANI
Paola Guglielmelli
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.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45755586&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2827673(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Pharma AG, Incyte Corp filed Critical Novartis Pharma AG
Publication of CA2827673A1 publication Critical patent/CA2827673A1/en
Application granted granted Critical
Publication of CA2827673C publication Critical patent/CA2827673C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K31/495—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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2827673A 2011-02-18 2012-02-17 Mtor/jak inhibitor combination therapy Active CA2827673C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161444581P 2011-02-18 2011-02-18
US61/444,581 2011-02-18
US201161503789P 2011-07-01 2011-07-01
US201161503785P 2011-07-01 2011-07-01
US61/503,789 2011-07-01
US61/503,785 2011-07-01
PCT/US2012/025581 WO2012112847A1 (en) 2011-02-18 2012-02-17 mTOR/JAK INHIBITOR COMBINATION THERAPY

Publications (2)

Publication Number Publication Date
CA2827673A1 CA2827673A1 (en) 2012-08-23
CA2827673C true CA2827673C (en) 2020-10-27

Family

ID=45755586

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2827673A Active CA2827673C (en) 2011-02-18 2012-02-17 Mtor/jak inhibitor combination therapy

Country Status (14)

Country Link
US (1) US9993480B2 (enExample)
EP (1) EP2675451B9 (enExample)
JP (1) JP5936628B2 (enExample)
KR (1) KR102024948B1 (enExample)
CN (1) CN103732226B (enExample)
AU (1) AU2012219395B2 (enExample)
BR (1) BR112013020798B1 (enExample)
CA (1) CA2827673C (enExample)
EA (1) EA026317B1 (enExample)
ES (1) ES2547916T3 (enExample)
MX (1) MX357939B (enExample)
PL (1) PL2675451T3 (enExample)
PT (1) PT2675451E (enExample)
WO (1) WO2012112847A1 (enExample)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
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.
WO2010083283A2 (en) 2009-01-15 2010-07-22 Incyte Corporation Processes for preparing jak inhibitors and related intermediate compounds
NZ596479A (en) * 2009-05-22 2014-01-31 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
BRPI1012108B8 (pt) 2009-05-22 2021-05-25 Incyte Corp composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico
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
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
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
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
WO2012112847A1 (en) 2011-02-18 2012-08-23 Novartis Pharma Ag mTOR/JAK INHIBITOR COMBINATION THERAPY
CN103608012A (zh) * 2011-06-14 2014-02-26 诺华股份有限公司 在癌症如骨髓增殖性肿瘤治疗中的帕比司他与鲁索利替尼的组合
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
US20140343128A1 (en) * 2011-11-15 2014-11-20 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the Janus Kinase 2 - Signal Transducer and Activator of Transcription 5 pathway
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
CA2888816A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
KR102242077B1 (ko) 2012-11-15 2021-04-20 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
US10335380B2 (en) * 2013-05-10 2019-07-02 CNIC Fundacion Centro Nacional de Investigaciones Cardiovasculares Carlos III Compounds suitable for the treatment of myeloproliferative neoplasms as well as methods for the diagnosis/prognosis of myeloproliferative neoplasms
MX376856B (es) 2013-08-07 2025-03-07 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
TW201545749A (zh) * 2014-04-25 2015-12-16 Univ Nat Cheng Kung 樟芝酸a、一種jak2/3酪胺酸激酶抑制劑及有潛力的肝炎治療劑
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
WO2015168621A1 (en) * 2014-05-02 2015-11-05 Oncoethix Sa Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
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
WO2016035014A1 (en) * 2014-09-01 2016-03-10 Sun Pharmaceutical Industries Limited Processes for the preparation of ruxolitinib phosphate
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
US10123997B2 (en) 2015-06-15 2018-11-13 Yong Liao Target for treating hepatitis B virus
US11612595B2 (en) * 2017-05-16 2023-03-28 Generos Biopharma Ltd. Compositions and methods for treating rheumatoid arthritis
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
CA3091339A1 (en) 2018-02-16 2019-08-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of cytokine-related disorders
KR20260080448A (ko) 2018-03-30 2026-06-02 인사이트 코포레이션 Jak 억제제를 사용하는 화농성 한선염의 치료
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
CN112567247A (zh) 2018-04-13 2021-03-26 因赛特公司 用于移植物抗宿主病的生物标志物
KR20210109522A (ko) 2018-10-31 2021-09-06 인사이트 코포레이션 혈액 질환의 치료를 위한 병용 요법
WO2021013942A1 (en) * 2019-07-24 2021-01-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of myeloperoxidase inhibitors for the treatment of cardiovascular diseases in patients suffering from myeloproliferative neoplasms
CA3156007A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072116A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
TW202131926A (zh) 2019-11-22 2021-09-01 美商英塞特公司 包含alk2抑制劑及jak2抑制劑的組合療法
ES3075793T3 (en) 2020-05-13 2026-08-07 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
AU2021273014A1 (en) 2020-05-13 2022-11-17 AbbVie Deutschland GmbH & Co. KG Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
IL303238A (en) 2020-12-08 2023-07-01 Incyte Corp Jak1 pathway inhibitors for the treatment of vitiligo
US20220305000A1 (en) * 2021-03-23 2022-09-29 Cellworks Group Inc. Combination Comprising Chloroquine, Metformin and Statin for Management of Cancer, Composition and Methods Thereof
AU2022270072A1 (en) 2021-05-03 2023-11-02 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis

Family Cites Families (114)

* 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
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
BR9408323A (pt) 1993-12-17 1997-08-19 Sandoz Ag Derivados de rapamicina
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
DE69624921T2 (de) 1995-06-09 2003-09-11 Novartis Ag, Basel Rapamycinderivate
MX9800136A (es) 1995-07-05 1998-03-29 Du Pont Pirimidinonas fungicidas.
WO1998002441A2 (en) 1996-07-12 1998-01-22 Ariad Pharmaceuticals, Inc. Non immunosuppressive antifungal rapalogs
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
AU4231299A (en) 1998-06-04 1999-12-20 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
AU3951899A (en) 1998-06-19 2000-01-05 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
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
IL147803A0 (en) 1999-08-24 2002-08-14 Ariad Gene Therapeutics Inc 28-epirapalogs
OA12118A (en) 1999-12-10 2006-05-04 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds.
HUP0203895A3 (en) 1999-12-24 2004-09-28 Aventis Pharma Ltd West Mallin Substituted azaindoles and pharmaceutical compositions containing them and their use
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
WO2001081345A1 (en) 2000-04-20 2001-11-01 Mitsubishi Pharma 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
OA12292A (en) 2000-06-26 2003-11-11 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents.
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
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
JP4316893B2 (ja) 2001-05-16 2009-08-19 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 Srcおよび他のプロテインキナーゼのインヒビター
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
CA2455181C (en) 2001-08-01 2010-04-06 Merck & Co., Inc. Benzimidazo[4,5-f]isoquinolinone derivatives
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
PT1441737E (pt) 2001-10-30 2006-12-29 Dana Farber Cancer Inst Inc Derivados de estrutura como inibidores da actividade do receptor de tirosina cinase flt3
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
EP1506189A1 (en) 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as 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
WO2004007472A1 (ja) 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ccr4アンタゴニストおよびその医薬用途
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
WO2004047843A1 (en) 2002-11-26 2004-06-10 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
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles 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
CA2545192A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
RU2006120956A (ru) 2003-12-17 2008-01-27 Пфайзер Продактс Инк. (Us) Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата
US20050153989A1 (en) 2004-01-13 2005-07-14 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
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
WO2005105146A1 (en) 2004-05-03 2005-11-10 Novartis Ag Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
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
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
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.
US8633205B2 (en) 2005-02-03 2014-01-21 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
JP2008545660A (ja) 2005-05-20 2008-12-18 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阻害剤として有用なピロロピリジン化合物
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
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
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
WO2007038215A1 (en) 2005-09-22 2007-04-05 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
CA2626456C (en) 2005-10-18 2018-01-09 George Mason Intellectual Properties, Inc. Mtor pathway theranostic
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
HUE028588T2 (hu) * 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
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
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
NZ592968A (en) 2006-01-17 2012-08-31 Vertex Pharma Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2
WO2007084667A2 (en) 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. 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
JP2009532475A (ja) 2006-04-05 2009-09-10 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 ヤヌスキナーゼの阻害剤として有用なデアザプリン
EP1898396A1 (en) 2006-09-07 2008-03-12 Deutsche Thomson-Brandt Gmbh Method and apparatus for encoding/decoding symbols carrying payload data for watermarking of an audio or video signal
ES2415863T3 (es) 2006-12-22 2013-07-29 Incyte Corporation Heterociclos sustituidos como inhibidores de Janus Quinasas
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
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.
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
EA020777B1 (ru) 2007-11-16 2015-01-30 Инсайт Корпорейшн 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus
ES2370378T3 (es) * 2008-01-30 2011-12-14 Cephalon, Inc. Derivados sustituidos de piperidina espirocíclica como ligandos del receptor de histamina h3.
MY165582A (en) 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
KR101084528B1 (ko) 2008-04-15 2011-11-18 인비트로겐 싱가포르 피티이. 엘티디. 전기천공 장치용 파이펫 팁
US20110129456A1 (en) * 2008-05-05 2011-06-02 Yaolin Wang Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
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.
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US20100209929A1 (en) * 2009-01-14 2010-08-19 Nodality, Inc., A Delaware Corporation Multiple mechanisms for modulation of jak/stat activity
WO2010083283A2 (en) 2009-01-15 2010-07-22 Incyte Corporation Processes for preparing jak inhibitors and related intermediate compounds
EP2210890A1 (en) 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
WO2010108328A1 (en) 2009-03-27 2010-09-30 Rht Limited Rejuvenated foam support filter
BRPI1012108B8 (pt) 2009-05-22 2021-05-25 Incyte Corp composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico
NZ596479A (en) 2009-05-22 2014-01-31 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
WO2012033537A1 (en) * 2010-09-08 2012-03-15 Nodality, Inc. Benchmarks for normal cell identification
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
US20110207754A1 (en) 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
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
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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

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