ATE543821T1 - Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen - Google Patents
Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungenInfo
- Publication number
- ATE543821T1 ATE543821T1 AT05855490T AT05855490T ATE543821T1 AT E543821 T1 ATE543821 T1 AT E543821T1 AT 05855490 T AT05855490 T AT 05855490T AT 05855490 T AT05855490 T AT 05855490T AT E543821 T1 ATE543821 T1 AT E543821T1
- Authority
- AT
- Austria
- Prior art keywords
- ylü
- düpyrimidine
- atk2
- atk1
- p70s6k
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 101100181122 Arabidopsis thaliana KIN14C gene Proteins 0.000 title 1
- 101100234530 Arabidopsis thaliana KIN14M gene Proteins 0.000 title 1
- 101100288145 Arabidopsis thaliana KNAT2 gene Proteins 0.000 title 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 title 1
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 title 1
- 230000001900 immune effect Effects 0.000 title 1
- 230000002757 inflammatory effect Effects 0.000 title 1
- 230000002062 proliferating effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102000001253 Protein Kinase Human genes 0.000 abstract 3
- 108091000080 Phosphotransferase Proteins 0.000 abstract 2
- 230000001413 cellular effect Effects 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 102000020233 phosphotransferase Human genes 0.000 abstract 2
- 108060006633 protein kinase Proteins 0.000 abstract 2
- 108010013238 70-kDa Ribosomal Protein S6 Kinases Proteins 0.000 abstract 1
- 101100322915 Caenorhabditis elegans akt-1 gene Proteins 0.000 abstract 1
- 101100162366 Caenorhabditis elegans akt-2 gene Proteins 0.000 abstract 1
- 238000003782 apoptosis assay Methods 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000004069 differentiation Effects 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 230000005012 migration Effects 0.000 abstract 1
- 238000013508 migration Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000005522 programmed cell death Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 230000019491 signal transduction Effects 0.000 abstract 1
Classifications
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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
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- 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
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical 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)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US64020004P | 2004-12-28 | 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 (1)
Publication Number | Publication Date |
---|---|
ATE543821T1 true ATE543821T1 (de) | 2012-02-15 |
Family
ID=36121369
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AT05855490T ATE543821T1 (de) | 2004-12-28 | 2005-12-27 | Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen |
Country Status (7)
Country | Link |
---|---|
US (1) | US7994172B2 (de) |
EP (1) | EP1848719B1 (de) |
JP (1) | JP5274842B2 (de) |
AT (1) | ATE543821T1 (de) |
AU (1) | AU2005322085B2 (de) |
CA (1) | CA2590961C (de) |
WO (1) | WO2006071819A1 (de) |
Families Citing this family (93)
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US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
US8541461B2 (en) | 2005-06-23 | 2013-09-24 | Astex Therapeutics Limited | Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators |
WO2007125325A1 (en) * | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical compounds |
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EP3129377A4 (de) | 2014-04-11 | 2017-12-20 | The University of North Carolina at Chapel Hill | Mertk-spezifische pyrimidinverbindungen |
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 |
MX2019000884A (es) | 2016-07-21 | 2019-09-04 | Biogen Ma Inc | Formas de succinato y composiciones de inhibidores de la tirosina cinasa de bruton. |
CN112154146A (zh) * | 2018-03-06 | 2020-12-29 | 西奈山伊坎医学院 | 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法 |
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 |
GB201918815D0 (en) * | 2019-12-19 | 2020-02-05 | Imperial College Innovations Ltd | Treatment of cancer |
MX2022011188A (es) | 2020-03-17 | 2022-11-08 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Derivado biciclico fusionado, metodo de preparacion y uso farmaceutico del mismo. |
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 |
AU2021259440A1 (en) * | 2020-04-21 | 2022-12-08 | University Of Massachusetts | Methods and compositions for treatment of age-related macular degeneration |
AU2021376892A1 (en) | 2020-11-16 | 2023-06-29 | Merck Patent Gmbh | Kinase inhibitor combinations for cancer treatment |
CN117940410A (zh) | 2021-09-17 | 2024-04-26 | 江苏恒瑞医药股份有限公司 | 一种稠合二环类衍生物的可药用盐、晶型及其制备方法 |
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EP1067123B1 (de) | 1998-03-31 | 2011-01-19 | Kyowa Hakko Kirin Co., Ltd. | Stickstoffenthaltende heterocyclische verbindungen |
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 |
US7589086B2 (en) * | 2003-05-28 | 2009-09-15 | Universita Degli Studi Di Siena | Substituted pyrazolo[3,4-D]pyrimidines as anti-tumor agents |
CN1882347A (zh) | 2003-11-21 | 2006-12-20 | 阿雷生物药品公司 | Akt蛋白激酶抑制剂 |
BRPI0508036A (pt) * | 2004-02-27 | 2007-07-17 | Hoffmann La Roche | derivados fundidos de pirazola |
CA2563699C (en) | 2004-04-23 | 2014-03-25 | Exelixis, Inc. | Kinase modulators and method of use |
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JP2008525526A (ja) | 2008-07-17 |
CA2590961A1 (en) | 2006-07-06 |
EP1848719B1 (de) | 2012-02-01 |
JP5274842B2 (ja) | 2013-08-28 |
AU2005322085A1 (en) | 2006-07-06 |
WO2006071819A1 (en) | 2006-07-06 |
US7994172B2 (en) | 2011-08-09 |
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