AU2005322085B2 - [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases - Google Patents

[1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases Download PDF

Info

Publication number
AU2005322085B2
AU2005322085B2 AU2005322085A AU2005322085A AU2005322085B2 AU 2005322085 B2 AU2005322085 B2 AU 2005322085B2 AU 2005322085 A AU2005322085 A AU 2005322085A AU 2005322085 A AU2005322085 A AU 2005322085A AU 2005322085 B2 AU2005322085 B2 AU 2005322085B2
Authority
AU
Australia
Prior art keywords
pyrazolo
bromo
piperazin
pyrimidine
methyl
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.)
Ceased
Application number
AU2005322085A
Other languages
English (en)
Other versions
AU2005322085A1 (en
Inventor
Lynn Canne Bannen
Joerg Bussenius
Erick Wang Co
Moon Hwan Kim
Rhett Ronald Klein
Donna Le
John Nuss
Ken Rice
Amy Lew Tsuhako
Yong Wang
Wei Xu
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.)
Exelixis Inc
Original Assignee
Exelixis Inc
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 Exelixis Inc filed Critical Exelixis Inc
Publication of AU2005322085A1 publication Critical patent/AU2005322085A1/en
Application granted granted Critical
Publication of AU2005322085B2 publication Critical patent/AU2005322085B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2005322085A 2004-12-28 2005-12-27 [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases Ceased AU2005322085B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64020004P 2004-12-28 2004-12-28
US60/640,200 2004-12-28
PCT/US2005/046938 WO2006071819A1 (en) 2004-12-28 2005-12-27 [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases

Publications (2)

Publication Number Publication Date
AU2005322085A1 AU2005322085A1 (en) 2006-07-06
AU2005322085B2 true AU2005322085B2 (en) 2012-07-19

Family

ID=36121369

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005322085A Ceased AU2005322085B2 (en) 2004-12-28 2005-12-27 [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases

Country Status (7)

Country Link
US (1) US7994172B2 (enExample)
EP (1) EP1848719B1 (enExample)
JP (1) JP5274842B2 (enExample)
AT (1) ATE543821T1 (enExample)
AU (1) AU2005322085B2 (enExample)
CA (1) CA2590961C (enExample)
WO (1) WO2006071819A1 (enExample)

Families Citing this family (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004303602C1 (en) 2003-12-23 2009-05-28 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
AU2005249380C1 (en) * 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
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
WO2006136821A1 (en) 2005-06-22 2006-12-28 Astex Therapeutics Limited Pharmaceutical compounds
WO2006136837A2 (en) 2005-06-23 2006-12-28 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
FI3719018T3 (fi) * 2006-04-25 2025-10-07 Astex Therapeutics Ltd Puriini- ja deatsapuriinijohdannaisia farmaseuttisina yhdisteinä
US20100016340A1 (en) * 2006-04-25 2010-01-21 Astex Therapeutics Limited Pharmaceutical compounds
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
DK2049500T3 (da) * 2006-07-06 2011-12-12 Array Biopharma Inc Cyclopenta [d]-pyrimidiner som AKT-proteinkinase-inhibitorer
WO2008006025A1 (en) 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
SI2054418T1 (sl) 2006-07-06 2012-02-29 Array Biopharma Inc Dihidrotieno pirimidini kot AKT protein kinazni inhibitorji
EP2131656A4 (en) 2006-11-15 2011-12-07 Forest Lab Holdings Ltd phthalazine
AR064415A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
EP2125750B1 (en) * 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
CN101801955B (zh) 2007-07-05 2013-05-08 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
KR20150091196A (ko) * 2007-07-05 2015-08-07 어레이 바이오파마 인크. Akt 단백질 키나제 억제제로서의 피리미딜 시클로펜탄
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009017671A1 (en) * 2007-07-26 2009-02-05 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
DK2188291T3 (da) * 2007-08-14 2013-01-07 Bayer Ip Gmbh Fusionerede bicykliske pyrimidiner
EP2050748A1 (en) * 2007-10-18 2009-04-22 Bayer Schering Pharma Aktiengesellschaft Novel fused pyrimidines
MX2010003927A (es) 2007-10-11 2010-04-30 Astrazeneca Ab Derivados de pirrolo [2,3-d] pirimidina como inhibidores de proteinas cinasas b.
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
US8440658B2 (en) 2007-12-11 2013-05-14 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009089352A1 (en) 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors
KR101624752B1 (ko) 2008-01-09 2016-05-26 어레이 바이오파마 인크. Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄
CA2711699A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
WO2009089462A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
JP5608098B2 (ja) 2008-01-09 2014-10-15 アレイ バイオファーマ、インコーポレイテッド キナーゼ阻害薬としてのピラゾロピリジン
US8592409B2 (en) 2008-01-24 2013-11-26 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11β-hydroxysteroid dehydrogenase 1
CN101981037B (zh) * 2008-01-30 2013-09-04 吉宁特有限公司 吡唑并嘧啶pi3k抑制剂化合物及使用方法
JP5734666B2 (ja) * 2008-02-11 2015-06-17 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の1,3−オキサアゼパン−2−オン及び1,3−ジアゼパン−2−オン阻害剤
CA2715290A1 (en) * 2008-02-15 2009-08-20 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009117109A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
JP5301563B2 (ja) * 2008-05-01 2013-09-25 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状インヒビター
EP2291373B1 (en) * 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291371B1 (en) 2008-05-01 2015-06-10 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
PL2324018T3 (pl) 2008-07-25 2014-02-28 Boehringer Ingelheim Int Cykliczne inhibitory dehydrogenazy 11 beta-hydroksysteroidowej typu 1
CA2729998A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
AU2009314335B2 (en) * 2008-11-11 2013-09-12 Eli Lilly And Company P70 S6 kinase inhibitor and mTOR inhibitor combination therapy
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
BRPI0921888A2 (pt) * 2008-11-11 2015-12-29 Lilly Co Eli terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase
JP5689069B2 (ja) 2008-11-20 2015-03-25 ジェネンテック, インコーポレイテッド ピラゾロピリジンpi3k阻害剤化合物及び使用方法
JP5679997B2 (ja) 2009-02-04 2015-03-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状阻害剤
CN102317269B (zh) 2009-02-11 2015-06-17 默克专利有限公司 新氨基氮杂杂环甲酰胺类
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
KR20120061771A (ko) * 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
EP2448928B1 (en) 2009-07-01 2014-08-13 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
SG178273A1 (en) 2009-08-07 2012-03-29 Merck Patent Gmbh Novel azaheterocyclic compounds
HUE043522T2 (hu) 2009-09-04 2019-08-28 Biogen Ma Inc Bruton tirozinkináz inhibitorok
KR101398268B1 (ko) * 2009-10-23 2014-05-23 일라이 릴리 앤드 캄파니 Akt 억제제
US8933072B2 (en) 2010-06-16 2015-01-13 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
EP2585444B1 (en) 2010-06-25 2014-10-22 Boehringer Ingelheim International GmbH Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
WO2012016001A1 (en) 2010-07-29 2012-02-02 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
WO2012059416A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
CA2818706C (en) 2010-11-24 2019-07-23 Merck Patent Gmbh Quinazoline carboxamide azetidines
WO2012135759A1 (en) 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt inhibitor compounds and abiraterone, and methods of use
KR101851820B1 (ko) 2011-04-01 2018-06-04 아스트라제네카 아베 치료적 요법
CN103841976A (zh) 2011-04-01 2014-06-04 基因泰克公司 Akt和mek抑制剂化合物的组合及其使用方法
ES2644536T3 (es) 2011-09-12 2017-11-29 Merck Patent Gmbh Imidazol-aminas novedosas como moduladores de la actividad cinasa
JP6082011B2 (ja) 2011-09-12 2017-02-15 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Merck Patent Gesellschaft mit beschraenkter Haftung キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体
SG11201401471PA (en) 2011-11-30 2014-08-28 Astrazeneca Ab Combination treatment of cancer
CN104169258B (zh) 2011-12-22 2017-03-01 默克专利有限公司 用作激酶活性调节剂的新颖的杂环羧酰胺
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
AR091273A1 (es) 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
JP6318156B2 (ja) * 2012-09-06 2018-04-25 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼをモジュレートするための化合物および方法、ならびにその指標
EP2909211A4 (en) 2012-10-17 2016-06-22 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
ES2620119T3 (es) 2012-11-16 2017-06-27 Merck Patent Gmbh Derivados heterocíclicos novedosos como moduladores de la actividad de quinasa
ES2807539T3 (es) 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
EP2925752A4 (en) 2012-11-27 2016-06-01 Univ North Carolina PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
ES2821102T3 (es) 2012-11-29 2021-04-23 Merck Patent Gmbh Derivados de azaquinazolincarboxamida
PL2935269T3 (pl) 2012-12-20 2018-09-28 Ucb Biopharma Sprl Terapeutycznie czynne pochodne pirazolo-pirymidyny
USRE48622E1 (en) 2012-12-20 2021-07-06 UCB Biopharma SRL Therapeutically active pyrazolo-pyrimidine derivatives
AR095202A1 (es) 2013-03-11 2015-09-30 Merck Patent Gmbh Heterociclos como moduladores de la actividad quinasa
KR102410696B1 (ko) 2014-04-03 2022-06-17 메르크 파텐트 게엠베하 암 치료법의 조합
CA2945128A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Mertk-specific pyrimidine compounds
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
EP3487852A1 (en) 2016-07-21 2019-05-29 Biogen MA Inc. Succinate forms and compositions of bruton's tyrosine kinase inhibitors
AU2017348322B8 (en) 2016-10-28 2021-12-23 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating EZH2-mediated cancer
WO2019173516A1 (en) * 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
CN110396067B (zh) * 2018-04-25 2022-07-08 复旦大学 1,4-二取代-2-哌嗪酮类化合物及其药物用途
CN112996518A (zh) 2018-06-21 2021-06-18 西奈山伊坎医学院 Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法
WO2020227325A1 (en) 2019-05-06 2020-11-12 Icahn School Of Medicine At Mount Sinai Heterobifunctional compounds as degraders of hpk1
GB201918815D0 (en) 2019-12-19 2020-02-05 Imperial College Innovations Ltd Treatment of cancer
CA3167999A1 (en) 2020-03-17 2021-09-23 Xin Li Fused bicyclic derivative, preparation method therefor, and pharmaceutical use thereof
CN113444110B (zh) * 2020-03-25 2023-05-12 江苏恒瑞医药股份有限公司 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用
US20230220395A1 (en) * 2020-04-21 2023-07-13 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
MX2023005520A (es) 2020-11-16 2023-05-23 Merck Patent Gmbh Combinaciones de inhibidores de cinasa para tratamiento de cancer.
JP2024535857A (ja) 2021-09-17 2024-10-02 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 縮合二環系誘導体の薬学的に許容される塩、結晶及びそれらの調製方法
CN117122602A (zh) * 2023-09-26 2023-11-28 赣南创新与转化医学研究院 化合物在制备治疗和/或预防脂肪肝病及相关疾病的药物中的用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6423716B1 (en) * 1998-03-31 2002-07-23 Kyowa Hakko Kogyo Co., Ltd. Nitrogenous heterocyclic compounds

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003252871A (ja) * 2001-03-29 2003-09-10 Tanabe Seiyaku Co Ltd スピロイソキノリン誘導体、その製法およびその合成中間体
JP2004115450A (ja) * 2002-09-27 2004-04-15 Tanabe Seiyaku Co Ltd 医薬組成物
ES2304252T3 (es) * 2003-05-28 2008-10-01 Universita Degli Studi Di Siena Derivados sustituidos en posicion 4 de pirazolo(3,4-d)pirimidina y utilizaciones de los mismos.
AU2004293026B2 (en) * 2003-11-21 2012-01-19 Array Biopharma Inc. AKT protein kinase inhibitors
JP2007523938A (ja) * 2004-02-27 2007-08-23 エフ.ホフマン−ラ ロシュ アーゲー ピラゾールの縮合誘導体
AU2005249380C1 (en) * 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6423716B1 (en) * 1998-03-31 2002-07-23 Kyowa Hakko Kogyo Co., Ltd. Nitrogenous heterocyclic compounds

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Chern et al, Bioorg. Med. Chem. Lett., 14, 2519-25 (2004) *
Quintela et al, Bioorg. Med. Chem., 11, 863-8 (2003) *

Also Published As

Publication number Publication date
CA2590961C (en) 2013-11-26
US20080188482A1 (en) 2008-08-07
EP1848719B1 (en) 2012-02-01
JP2008525526A (ja) 2008-07-17
US7994172B2 (en) 2011-08-09
EP1848719A1 (en) 2007-10-31
WO2006071819A1 (en) 2006-07-06
CA2590961A1 (en) 2006-07-06
AU2005322085A1 (en) 2006-07-06
ATE543821T1 (de) 2012-02-15
JP5274842B2 (ja) 2013-08-28

Similar Documents

Publication Publication Date Title
AU2005322085B2 (en) [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
US8076338B2 (en) Kinase modulators and methods of use
AU2006304875B2 (en) Pyrazolo-pyrimidines as casein kinase II (CK2) modulators
AU2005322855B2 (en) Pyrimidine derivatives as kinase modulators and method of use
EP1678168B1 (en) P70s6 kinase modulators and method of use
CA2491191C (en) Receptor-type kinase modulators and methods of use
AU2010241235A1 (en) Tie-2 modulators and methods of use
US20060122171A1 (en) Kinase modulators

Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ [1H-PYRAZOLO[3, 4-D]PYRIMIDIN-4-YL]-PIPERIDINE OR -PIPERAZINE COMPOUNDS AS SERINE-THEONINE KINASE MODULATORS (P70S6K, ATK1 AND ATK2) FOR THE TREATMENT OF IMMUNOLOGICAL, INFLAMMATORY AND PROLIFERATIVE DISEASES

TH Corrigenda

Free format text: IN VOL 21, NO 47, PAGE(S) 5363 UNDER THE HEADING AMENDMENTS, SECTION 104 - AMENDMENTS MADE UNDER THE NAME EXELIXIS, INC., APPLICATION NO. 2005322085, UNDER INID (54), CORRECT THE INVENTION TITLE TO READ [1H-PYRAZOLO[3, 4-D]PYRIMIDIN-4-YL]-PIPERIDINE OR -PIPERAZINE COMPOUNDS AS SERINE-THREONINE KINASE MODULATORS (P70S6K, ATK1 AND ATK2) FOR THE TREATMENT OF IMMUNOLOGICAL, INFLAMMATORY AND PROLIFERATIVE DISEASES

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired