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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (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 (https=) |
| EP (1) | EP1848719B1 (https=) |
| JP (1) | JP5274842B2 (https=) |
| AT (1) | ATE543821T1 (https=) |
| AU (1) | AU2005322085B2 (https=) |
| CA (1) | CA2590961C (https=) |
| WO (1) | WO2006071819A1 (https=) |
Families Citing this family (98)
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| BRPI0418078A8 (pt) | 2003-12-23 | 2018-01-02 | Astex Therapeutics Ltd | composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | 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 |
| EP1902032A1 (en) | 2005-06-22 | 2008-03-26 | Astex Therapeutics Limited | Pharmaceutical compounds |
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| EP2029592A1 (en) * | 2006-04-25 | 2009-03-04 | Astex Therapeutics Limited | Pharmaceutical compounds |
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| SG10201800741QA (en) | 2012-11-29 | 2018-03-28 | Merck Patent Gmbh | BENZO-[d][1,2,3]TRIAZINE COMPOUNDS AND USE AS p70S6K INHIBITORS |
| USRE48622E1 (en) | 2012-12-20 | 2021-07-06 | UCB Biopharma SRL | Therapeutically active pyrazolo-pyrimidine derivatives |
| SG11201504291SA (en) * | 2012-12-20 | 2015-07-30 | Ucb Biopharma Sprl | Therapeutically active pyrazolo-pyrimidine derivatives |
| SG11201505999VA (en) | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| CA2944573C (en) | 2014-04-03 | 2022-10-25 | Merck Patent Gmbh | Combinations of cancer therapeutics |
| US20150291606A1 (en) | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Mertk-specific pyrrolopyrimidine 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 |
| 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 |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| CA3092677A1 (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 |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| GB201918815D0 (en) * | 2019-12-19 | 2020-02-05 | Imperial College Innovations Ltd | Treatment of cancer |
| TWI908780B (zh) * | 2020-03-17 | 2025-12-21 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合二環類衍生物、其製備方法及其在醫藥上的應用 |
| 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 |
| WO2021216548A1 (en) * | 2020-04-21 | 2021-10-28 | 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 |
| WO2022101459A1 (en) | 2020-11-16 | 2022-05-19 | 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 |
| CN117122602B (zh) * | 2023-09-26 | 2026-03-20 | 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE69943144D1 (de) * | 1998-03-31 | 2011-03-03 | 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 |
| 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. |
| CA2546754A1 (en) | 2003-11-21 | 2005-06-09 | Array Biopharma Inc. | Akt protein kinase inhibitors |
| KR100843526B1 (ko) | 2004-02-27 | 2008-07-03 | 에프. 호프만-라 로슈 아게 | 피라졸의 접합 유도체 |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
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- 2005-12-27 WO PCT/US2005/046938 patent/WO2006071819A1/en not_active Ceased
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- 2005-12-27 EP EP05855490A patent/EP1848719B1/en not_active Expired - Lifetime
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| JP5274842B2 (ja) | 2013-08-28 |
| US7994172B2 (en) | 2011-08-09 |
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| JP2008525526A (ja) | 2008-07-17 |
| WO2006071819A1 (en) | 2006-07-06 |
| EP1848719A1 (en) | 2007-10-31 |
| CA2590961A1 (en) | 2006-07-06 |
| US20080188482A1 (en) | 2008-08-07 |
| AU2005322085A1 (en) | 2006-07-06 |
| CA2590961C (en) | 2013-11-26 |
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