CA2592119C - Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors - Google Patents

Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors Download PDF

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Publication number
CA2592119C
CA2592119C CA2592119A CA2592119A CA2592119C CA 2592119 C CA2592119 C CA 2592119C CA 2592119 A CA2592119 A CA 2592119A CA 2592119 A CA2592119 A CA 2592119A CA 2592119 C CA2592119 C CA 2592119C
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Prior art keywords
alkyl
methyl
pyridin
pyrrolo
amino
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Expired - Lifetime
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CA2592119A
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English (en)
French (fr)
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CA2592119A1 (en
Inventor
James D. Rodgers
Haisheng Wang
Andrew P. Combs
Richard B. Sparks
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Incyte Holdings Corp
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Incyte Corp
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Publication of CA2592119A1 publication Critical patent/CA2592119A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Biotechnology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2592119A 2004-12-22 2005-12-21 Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors Expired - Lifetime CA2592119C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US63847404P 2004-12-22 2004-12-22
US60/638,474 2004-12-22
US72628905P 2005-10-13 2005-10-13
US60/726,289 2005-10-13
PCT/US2005/046207 WO2006069080A2 (en) 2004-12-22 2005-12-21 Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2m3-b]pyrimidin-4-yl-amines as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2592119A1 CA2592119A1 (en) 2006-06-29
CA2592119C true CA2592119C (en) 2014-07-15

Family

ID=36602272

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CA2592119A Expired - Lifetime CA2592119C (en) 2004-12-22 2005-12-21 Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors

Country Status (18)

Country Link
US (7) US7335667B2 (enExample)
EP (2) EP1828181B1 (enExample)
JP (2) JP5048514B2 (enExample)
AR (1) AR054416A1 (enExample)
CA (1) CA2592119C (enExample)
CY (1) CY1120257T1 (enExample)
DK (1) DK2671882T3 (enExample)
ES (2) ES2536331T3 (enExample)
HR (1) HRP20180578T1 (enExample)
HU (1) HUE037435T2 (enExample)
LT (1) LT2671882T (enExample)
ME (1) ME03017B (enExample)
PL (1) PL2671882T3 (enExample)
PT (1) PT2671882T (enExample)
RS (1) RS57302B1 (enExample)
SI (1) SI2671882T1 (enExample)
TW (2) TWI439459B (enExample)
WO (1) WO2006069080A2 (enExample)

Families Citing this family (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
MX2007001399A (es) 2004-08-02 2007-04-18 Osi Pharm Inc Compuestos que inhiben pirrolopirimidina multi-cinasa aril-amino sustituidas.
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.
US7884109B2 (en) 2005-04-05 2011-02-08 Wyeth Llc Purine and imidazopyridine derivatives for immunosuppression
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
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
JP5071374B2 (ja) * 2005-07-14 2012-11-14 アステラス製薬株式会社 ヘテロ環ヤヌスキナーゼ３阻害剤
WO2007038215A1 (en) * 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
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
US7989459B2 (en) 2006-02-17 2011-08-02 Pharmacopeia, Llc Purinones and 1H-imidazopyridinones as PKC-theta inhibitors
TW200837064A (en) 2006-10-04 2008-09-16 Pharmacopeia Inc 8-substituted 2-(benzimidazolyl)purine derivatives for immunosuppression
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
KR20100014271A (ko) * 2006-11-16 2010-02-10 파마코페이아, 엘엘씨. 면역 억제를 위한 7-치환된 퓨린 유도체
KR20090082507A (ko) 2006-11-20 2009-07-30 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 통증 및 소양증 치료용 방법, 조성물 및 키트
US20100022517A1 (en) * 2006-12-18 2010-01-28 Richards Lori A Ophthalmic formulation of rho kinase inhibitor compound
US8071779B2 (en) 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
ES2415863T3 (es) * 2006-12-22 2013-07-29 Incyte Corporation Heterociclos sustituidos como inhibidores de Janus Quinasas
WO2008083491A1 (en) 2007-01-11 2008-07-17 Critical Outcome Technologies Inc. Compounds and method for treatment of cancer
US20100105661A1 (en) * 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
US8063094B2 (en) 2007-02-08 2011-11-22 Boehringer Ingelheim International Gmbh Anti-cytokine heterocyclic 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.
DE102007027800A1 (de) * 2007-06-16 2008-12-18 Bayer Healthcare Ag Substituierte bicyclische Heteroaryl-Verbindungen und ihre Verwendung
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
US8466151B2 (en) 2007-12-26 2013-06-18 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
MY165582A (en) * 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
AU2009259853A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
PE20110063A1 (es) * 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
EP3023426A1 (en) 2008-07-17 2016-05-25 Critical Outcome Technologies, Inc. Thiosemicarbazone inhibitor compounds and cancer treatment methods
RU2011105768A (ru) * 2008-08-01 2012-09-10 Биокрист Фармасьютикалз, Инк. (Us) Производные пиперидина в качестве ингибиторов jakз
RS53382B (sr) 2008-08-20 2014-10-31 Zoetis Llc Jedinjenja pirol [2,3-d]pirimidina
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.
WO2010083283A2 (en) 2009-01-15 2010-07-22 Incyte Corporation Processes for preparing jak inhibitors and related intermediate compounds
EP2396004A4 (en) * 2009-02-11 2012-07-25 Reaction Biology Corp SELECTIVE KINASE HEMMER
MX2011010923A (es) * 2009-04-14 2011-11-18 Astellas Pharma Inc Derivado de pirrolopiridina condensado.
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
JP5690823B2 (ja) 2009-07-08 2015-03-25 レオ ファーマ アクティーゼルスカブ Ｊａｋ受容体およびタンパク質チロシンキナーゼ阻害薬としての複素環化合物
WO2011006073A1 (en) 2009-07-10 2011-01-13 President And Fellows Of Harvard College Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
AU2010289143A1 (en) 2009-08-24 2012-02-16 Ascepion Pharmaceuticals, Inc. 5,6-bicyclic heteroaryl-containing urea compounds as 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
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
AU2010308028A1 (en) * 2009-10-15 2012-04-19 Pfizer Inc. Pyrrolo[2,3-d] pyrimidine compounds
KR20120124428A (ko) 2009-12-30 2012-11-13 아르퀼 인코포레이티드 치환된 피롤로-아미노피리미딘 화합물
US20110207754A1 (en) * 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
WO2011109217A2 (en) * 2010-03-02 2011-09-09 Immunodiagnostics, Inc. Methods of treating or preventing rna polymerase dependent viral disorders by administration of jak2 kinase inhibitors
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2011120153A1 (en) 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
US8937077B2 (en) 2010-10-22 2015-01-20 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
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
CN103298817A (zh) * 2011-01-07 2013-09-11 利奥制药有限公司 作为蛋白酪氨酸激酶抑制剂的新磺酰胺哌嗪衍生物及其药物用途
WO2012112847A1 (en) 2011-02-18 2012-08-23 Novartis Pharma Ag mTOR/JAK INHIBITOR COMBINATION THERAPY
CN103459394B (zh) * 2011-04-08 2016-04-27 辉瑞大药厂 结晶和非结晶形式的托法替尼，以及包含托法替尼和渗透增强剂的药物组合物
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
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
JP6075736B2 (ja) * 2011-12-21 2017-02-08 ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． ピロール−６員ヘテロアリール環誘導体、その合成法およびその医薬用途
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
US20150182490A1 (en) 2012-06-26 2015-07-02 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
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
US10130632B2 (en) 2012-11-27 2018-11-20 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
US9260426B2 (en) * 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
CN103896946B (zh) * 2012-12-28 2018-04-03 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
EP2945630A4 (en) * 2013-01-16 2016-06-22 Merck Sharp & Dohme 4-FLUORPIPERIDINOREXIN receptor antagonists
EA027879B1 (ru) 2013-02-22 2017-09-29 Пфайзер Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-РОДСТВЕННЫХ КИНАЗ (JAK)
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
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).
CA2921956C (en) * 2013-08-22 2021-10-19 Genentech, Inc. Process for preparing (r)-5-bromo-4-(3-amino)piperidin-1-yl)-3-(cyclopropanecarboxamido)-1h-pyrrolo[2,3-b]pyridine
WO2015027090A1 (en) * 2013-08-22 2015-02-26 Genentech, Inc. Intermediates and processes for preparing compounds
LT3077395T (lt) 2013-12-05 2018-02-12 Pfizer Inc. Pirolo[2,3-d]pirimidinilo, pirolo[2,3-b]pirazinilo ir pirolo[2,3-d]piridinilo akrilamidai
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
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
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
US11021443B2 (en) 2015-08-03 2021-06-01 President And Fellows Of Harvard College Charged ion channel blockers and methods for use
KR101771219B1 (ko) 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
CN108472298B (zh) 2015-11-24 2021-04-20 深圳阿拉丁医疗科技有限公司 选择性激酶抑制剂
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
AU2017315343A1 (en) 2016-08-24 2019-02-28 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
CN110300590A (zh) * 2016-10-21 2019-10-01 林伯士拉克许米公司 Tyk2抑制剂及其用途
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
AU2018223192A1 (en) * 2017-02-27 2019-06-20 Janssen Pharmaceutica Nv [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as OGA inhibitors
BR112020008850A2 (pt) 2017-11-03 2020-10-20 Aclaris Therapeutics, Inc. composto, composição farmacêutica e método para tratar uma doença mediada por jak1 e jak3
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
JP7591500B2 (ja) 2018-08-10 2024-11-28 アクラリス セラピューティクス，インコーポレイテッド ピロロピリミジンｉｔｋ阻害剤
KR20210109522A (ko) 2018-10-31 2021-09-06 인사이트 코포레이션 혈액 질환의 치료를 위한 병용 요법
ES2974634T3 (es) 2018-12-21 2024-06-28 Celgene Corp Inhibidores de tienopiridinas de RIPK2
NL2022471B1 (en) 2019-01-29 2020-08-18 Vationpharma B V Solid state forms of oclacitinib
US10828287B2 (en) 2019-03-11 2020-11-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CN113811305A (zh) 2019-03-11 2021-12-17 诺西恩医疗公司 带电的离子通道阻滞剂及其使用方法
CA3129089A1 (en) 2019-03-11 2020-09-17 Bridget Mccarthy Cole Ester substituted ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US11377422B2 (en) 2019-03-11 2022-07-05 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
PH12021552036A1 (en) 2019-05-02 2022-05-23 Aclaris Therapeutics Inc Substituted pyrrolopyridines as jak inhibitors
WO2021022178A1 (en) * 2019-07-31 2021-02-04 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
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
CA3155568A1 (en) 2019-11-06 2021-05-14 Bridget Mccarthy Cole Charged ion channel blockers and methods for use
AU2020380118B2 (en) 2019-11-06 2026-06-11 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US12162851B2 (en) 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US11332446B2 (en) 2020-03-11 2022-05-17 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
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
CA3192055A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
IL300555A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK inhibitor
WO2022053931A1 (en) 2020-09-08 2022-03-17 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
EP4210828A1 (en) * 2020-09-11 2023-07-19 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
IL303238A (en) 2020-12-08 2023-07-01 Incyte Corp Jak1 pathway inhibitors for the treatment of vitiligo
WO2022194782A1 (en) * 2021-03-15 2022-09-22 Chiesi Farmaceutici S.P.A. Heterocyclic derivatives as janus kinase inhibitors
AU2022270072A1 (en) 2021-05-03 2023-11-02 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
US20240309095A1 (en) 2021-07-07 2024-09-19 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
CA3226714A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
UY40062A (es) 2021-12-08 2023-06-30 Incyte Corp Anticuerpos anti-calreticulina (calr) mutante y usos de estos
EP4554584A4 (en) * 2022-07-14 2026-07-15 Jnana Therapeutics Inc SMALL MOLECULES THAT INHIBIT SLC6A19 FUNCTION IN A MAMMAL
JP2026507883A (ja) 2023-03-06 2026-03-06 ゾエティス・サービシーズ・エルエルシー ヤヌスキナーゼ阻害剤を含む局所組成物
WO2025096716A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Anti-mutant calreticulin (calr) antibody-drug conjugates and uses thereof

Family Cites Families (31)

* 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
ES2148179T3 (es) * 1991-09-06 2000-10-16 Yoshitomi Pharmaceutical Compuesto de 4-amino(alquil)ciclohexan-1-carboxamida y uso del mismo.
PT956865E (pt) * 1996-08-12 2007-07-30 Mitsubishi Pharma Corp Medicamentos compreendendo inibidores da rho cinase.
JPH11130751A (ja) * 1997-10-30 1999-05-18 Yoshitomi Pharmaceut Ind Ltd アミド化合物およびそれらの酸付加塩の標識化合物
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AU4231299A (en) 1998-06-04 1999-12-20 Abbott Laboratories Cell adhesion-inhibiting antinflammatory 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
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
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
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.
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
CA2486183C (en) 2002-05-23 2012-01-10 Cytopia Pty Ltd. Protein kinase inhibitors
WO2004047843A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
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
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
WO2005105146A1 (en) 2004-05-03 2005-11-10 Novartis Ag Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
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
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.
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

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