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ATE482213T1 - Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine - Google Patents

Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

Info

Publication number
ATE482213T1
ATE482213T1 AT05816516T AT05816516T ATE482213T1 AT E482213 T1 ATE482213 T1 AT E482213T1 AT 05816516 T AT05816516 T AT 05816516T AT 05816516 T AT05816516 T AT 05816516T AT E482213 T1 ATE482213 T1 AT E482213T1
Authority
AT
Austria
Prior art keywords
inhibitors
protein kinases
aüpyrimidines
compounds
compositions
Prior art date
Application number
AT05816516T
Other languages
English (en)
Inventor
Juan-Miguel Jimenez
Ronald Knegtel
Jean-Damien Charrier
Dean Stamos
Pan Li
Jon Come
Alex Aronov
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE482213T1 publication Critical patent/ATE482213T1/de

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    • 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
    • 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
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    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
AT05816516T 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine ATE482213T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62544604P 2004-11-04 2004-11-04
PCT/US2005/040344 WO2006052913A1 (en) 2004-11-04 2005-11-04 PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES

Publications (1)

Publication Number Publication Date
ATE482213T1 true ATE482213T1 (de) 2010-10-15

Family

ID=35809833

Family Applications (1)

Application Number Title Priority Date Filing Date
AT05816516T ATE482213T1 (de) 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

Country Status (20)

Country Link
US (1) US7528138B2 (de)
EP (1) EP1812440B1 (de)
JP (2) JP5030229B2 (de)
KR (1) KR20070090172A (de)
CN (1) CN101094853B (de)
AT (1) ATE482213T1 (de)
AU (1) AU2005304784B2 (de)
CA (1) CA2586375A1 (de)
DE (1) DE602005023763D1 (de)
DK (1) DK1812440T3 (de)
ES (1) ES2354824T3 (de)
IL (1) IL182893A0 (de)
MX (1) MX337817B (de)
NO (1) NO20072795L (de)
NZ (1) NZ555236A (de)
PT (1) PT1812440E (de)
RU (1) RU2417996C2 (de)
SI (1) SI1812440T1 (de)
WO (1) WO2006052913A1 (de)
ZA (1) ZA200704476B (de)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
CN101094853B (zh) * 2004-11-04 2011-07-13 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶
RU2405780C2 (ru) * 2005-02-16 2010-12-10 Астразенека Аб Химические соединения
US20090156617A1 (en) * 2005-05-12 2009-06-18 Northrup Alan B Tyrosine kinase inhibitors
WO2006123113A2 (en) * 2005-05-16 2006-11-23 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
WO2007046867A2 (en) * 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
ATE540948T1 (de) * 2005-05-20 2012-01-15 Vertex Pharma Pyrrolopyridine als proteinkinasehemmer
TW200800963A (en) * 2005-10-28 2008-01-01 Astrazeneca Ab Chemical compounds
HUE025173T2 (hu) 2005-12-13 2016-01-28 Incyte Corp Heteroaril-szubsztituált pirrollo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
GB0601638D0 (en) * 2006-01-27 2006-03-08 Merck Sharp & Dohme Therapeutic treatment
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20121506A1 (es) * 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
AU2008228768A1 (en) * 2007-03-22 2008-09-25 Vertex Pharmaceuticals Incorporated N-heterocyclic compounds useful as inhibitors of Janus Kinases
EP2155742A1 (de) * 2007-04-18 2010-02-24 AstraZeneca AB 5-aminopyrazol-3-yl-3h-imidazo[4,5-b]pyridinderivate und ihre verwendung zur behandlung von krebs
UA99459C2 (en) * 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
JP2010526048A (ja) * 2007-05-04 2010-07-29 アストラゼネカ アクチボラグ アミノ−チアゾリル−ピリミジン誘導体、および癌の治療のための該誘導体の使用
EP3070090B1 (de) 2007-06-13 2018-12-12 Incyte Holdings Corporation Verwendung der salze des janus-kinasehemmers (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropannitril
WO2009041663A1 (ja) 2007-09-28 2009-04-02 Kyowa Hakko Kirin Co., Ltd. 皮膚疾患の予防及び／または治療剤
KR101580482B1 (ko) * 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 ４－피라졸릴－ｎ－아릴피리미딘－２－아민 및 ４－피라졸릴－ｎ－헤테로아릴피리미딘－２－아민
AU2008343173A1 (en) * 2007-12-19 2009-07-09 Aj Park Pyrazolo [1,5-a] pyrimidines useful as JAK2 inhibitors
CL2008003798A1 (es) * 2007-12-19 2009-10-09 Amgen Inc Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades.
US8507501B2 (en) 2008-03-13 2013-08-13 The Brigham And Women's Hospital, Inc. Inhibitors of the BMP signaling pathway
TW201006830A (en) * 2008-06-11 2010-02-16 Astrazeneca Ab Chemical compounds
US8394802B2 (en) * 2008-09-19 2013-03-12 Nerviano Medical Sciences S.R.L. 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
TW201018693A (en) * 2008-09-30 2010-05-16 Astrazeneca Ab Chemical compounds 496-1p
RU2539568C2 (ru) * 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
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
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
EP2435445A1 (de) * 2009-05-28 2012-04-04 Vertex Pharmaceuticals Incorporated C-met-proteinkinasehemmer
JP5721706B2 (ja) 2009-06-17 2015-05-20 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルス複製の阻害剤
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
AR078012A1 (es) * 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
NZ598985A (en) 2009-09-04 2013-07-26 Biogen Idec Inc Bruton's tyrosine kinase inhibitors
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2011130515A1 (en) * 2010-04-14 2011-10-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production
EA025281B9 (ru) 2010-05-17 2017-08-31 Инкозен Терапьютикс Пвт. Лтд. СОЕДИНЕНИЯ 3,5-ДИЗАМЕЩЕННОГО-3H-ИМИДАЗО[4,5-b]ПИРИДИНА И 3,5-ДИЗАМЕЩЕННОГО-3H-[1,2,3]ТРИАЗОЛО[4,5-b]ПИРИДИНА КАК МОДУЛЯТОРЫ ПРОТЕИНКИНАЗ
WO2011146336A1 (en) 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Ｊａｋ抑制劑的局部製劑
GB2480814A (en) * 2010-06-01 2011-12-07 Summit Corp Plc Compounds for the treatment of clostridium difficile-associated disease
AU2011260097B2 (en) 2010-06-01 2015-01-22 Summit (Oxford) Limited Compounds for the treatment of clostridium difficile associated disease
JP5917544B2 (ja) 2010-11-19 2016-05-18 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阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
AU2011329734B2 (en) 2010-11-19 2015-05-28 Incyte Holdings Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
WO2012083117A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP2014517016A (ja) * 2011-06-10 2014-07-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害活性を有するピリミジンおよびピリミジン化合物の組成物と製造方法
ES2560611T3 (es) 2011-06-20 2016-02-22 Incyte Holdings Corporation Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
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
US9096605B2 (en) * 2011-08-24 2015-08-04 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN104321322A (zh) 2012-03-30 2015-01-28 理森制药股份公司 作为c-met蛋白激酶调节剂的新型3,5-二取代-3h-咪唑并[4,5-b]吡啶和3,5-二取代-3h-[1,2,3]三唑并[4,5-b]吡啶化合物
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
AR091273A1 (es) * 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
EP3584246A1 (de) 2012-08-16 2019-12-25 The Scripps Research Institute Neuartige kappa-opioid-liganden
SG10202111768XA (en) 2012-11-15 2021-11-29 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
WO2014081996A1 (en) * 2012-11-23 2014-05-30 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
SMT202100425T1 (it) 2012-12-07 2021-09-14 Vertex Pharma 2-ammino-n-(piperidin-1-il-piridin-3-il) pirazolo[1,5alpha]piirimidina-3-carbossiammide come inibitore di atr chinasi
TW201501713A (zh) * 2013-03-01 2015-01-16 Kyowa Hakko Kirin Co Ltd 眼炎症性疾病之預防及／或治療劑
PE20200298A1 (es) 2013-03-06 2020-02-06 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak
EP2970311A4 (de) * 2013-03-14 2016-11-23 Brigham & Womens Hospital Bmp-hemmer und verfahren zur verwendung davon
EP2970289A1 (de) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Als atr-kinaseinhibitoren nützliche verbindungen
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
WO2014175370A1 (ja) * 2013-04-25 2014-10-30 塩野義製薬株式会社 ピロリジン誘導体およびそれらを含有する医薬組成物
CN114010611B (zh) 2013-08-07 2023-11-28 因赛特控股公司 Jak1抑制剂的持续释放剂型
PT3068782T (pt) 2013-11-13 2018-10-08 Vertex Pharma Métodos de preparação de inibidores da replicação de vírus da gripe
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
WO2015073267A1 (en) * 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
PE20170663A1 (es) 2014-05-23 2017-05-22 Hoffmann La Roche Compuestos de 5- cloro- 2- difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
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
SI3152212T1 (sl) 2014-06-05 2020-06-30 Vertex Pharmaceuticals Inc. Radioaktivno označeni derivati 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)-pirazolo (1,5-A)pirimidin-3- karboksamidne spojine, koristni kot inhibitor kinaze ATR, priprava navedene spojine in njene različne trdne oblike
SG10201811175WA (en) 2014-06-17 2019-01-30 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
US10513521B2 (en) 2014-07-15 2019-12-24 The Brigham And Women's Hospital, Inc. Compositions and methods for inhibiting BMP
ES2941630T3 (es) 2014-11-16 2023-05-24 Array Biopharma Inc Forma cristalina de sulfato de hidrógeno de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida
EP3294717B1 (de) 2015-05-13 2020-07-29 Vertex Pharmaceuticals Inc. Verfahren zur herstellung von inhibitoren der influenzavirenreplikation
MA42422A (fr) 2015-05-13 2018-05-23 Vertex Pharma Inhibiteurs de la réplication des virus de la grippe
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PE20190437A1 (es) 2016-05-18 2019-03-27 Loxo Oncology Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
JP6961675B2 (ja) 2016-07-18 2021-11-05 ユニバーシティー ヘルス ネットワーク Ｔｔｋ阻害剤の固体形態
JP7214632B2 (ja) 2016-07-21 2023-01-30 バイオジェン エムエー インク． ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
EP3615538B1 (de) * 2017-04-27 2024-02-07 The Brigham and Women's Hospital, Inc. Neue alk2-inhibitoren und verfahren zur hemmung der bmp-signalisierung
PL233595B1 (pl) * 2017-05-12 2019-11-29 Celon Pharma Spolka Akcyjna Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK
CA3061236A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
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
KR20200116481A (ko) * 2018-01-29 2020-10-12 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
SG11202006832YA (en) 2018-01-29 2020-08-28 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
RS63312B1 (sr) 2018-01-30 2022-07-29 Incyte Corp Procesi za pripremu (1-(3-fluoro-2-(trifluorometil)izonikotinil)piperidin-4-on)
MX2020010322A (es) 2018-03-30 2022-11-30 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak).
JP7504880B2 (ja) * 2018-10-26 2024-06-24 ケロス セラピューティクス インコーポレイテッド Ａｌｋ２阻害剤の結晶形
TW202504901A (zh) 2018-12-20 2025-02-01 美商英塞特公司 咪唑并嗒嗪及咪唑并吡啶化合物及其用途
WO2021222875A1 (en) 2020-04-30 2021-11-04 Keros Therapeutics, Inc. Methods of using alk2 inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022098812A1 (en) 2020-11-04 2022-05-12 Keros Therapeutics, Inc. Methods of treating iron overload
EP4392418A4 (de) * 2021-08-24 2025-06-18 The Johns Hopkins University Zusammensetzungen und verfahren zur behandlung von proteotoxizitätsbedingten erkrankungen
CN116987083A (zh) * 2022-04-25 2023-11-03 杭州健崃生物科技有限公司 吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途
KR102912267B1 (ko) 2023-04-20 2026-01-15 한국화학연구원 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
US6245759B1 (en) * 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
US7550470B2 (en) * 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
CN101094853B (zh) * 2004-11-04 2011-07-13 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶

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