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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (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)
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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| MXPA06007326A (es) | 2003-12-23 | 2007-01-26 | Astex Therapeutics Ltd | Derivados de pirazol como moduladores de proteina cinasa. |
| 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 |
| US8343953B2 (en) | 2005-06-22 | 2013-01-01 | 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 |
| JP2009534456A (ja) * | 2006-04-25 | 2009-09-24 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| DK3421471T3 (da) | 2006-04-25 | 2021-06-14 | Astex Therapeutics Ltd | Purin- og deazapurinderivater som farmaceutiske forbindelser |
| ATE532789T1 (de) | 2006-07-06 | 2011-11-15 | Array Biopharma Inc | Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren |
| ATE523499T1 (de) | 2006-07-06 | 2011-09-15 | Array Biopharma Inc | Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| CA2656566C (en) | 2006-07-06 | 2014-06-17 | Array Biopharma Inc. | Dihydrofuro pyrimidines as akt protein kinase inhibitors |
| CA2669687C (en) | 2006-11-15 | 2013-09-10 | Forest Laboratories Holdings Limited | Phthalazine derivatives |
| 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. |
| CA2678577A1 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
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| CN101918373B (zh) * | 2007-07-05 | 2013-06-05 | 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 |
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| JP5470557B2 (ja) * | 2007-07-26 | 2014-04-16 | 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型の阻害剤の合成 |
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| AR095202A1 (es) | 2013-03-11 | 2015-09-30 | Merck Patent Gmbh | Heterociclos como moduladores de la actividad quinasa |
| EP3125935B1 (en) | 2014-04-03 | 2019-10-23 | Merck Patent GmbH | Combinations of cancer therapeutics |
| US9555031B2 (en) | 2014-04-11 | 2017-01-31 | The University Of North Carolina At Chapel Hill | Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity |
| 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 |
| KR20190084063A (ko) | 2016-10-28 | 2019-07-15 | 이칸 스쿨 오브 메디슨 엣 마운트 시나이 | Ｅｚｈ２-매개성 암 치료용 조성물 및 방법 |
| JP2021515013A (ja) * | 2018-03-06 | 2021-06-17 | アイカーン スクール オブ メディスン アット マウント シナイ | セリンスレオニンキナーゼ（ａｋｔ）分解／破壊化合物および使用方法 |
| 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 |
| EP3810145A4 (en) | 2018-06-21 | 2022-06-01 | Icahn School of Medicine at Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| JP7503851B2 (ja) | 2019-05-06 | 2024-06-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Ｈｐｋ１の分解剤としてのヘテロ二官能性化合物 |
| GB201918815D0 (en) * | 2019-12-19 | 2020-02-05 | Imperial College Innovations Ltd | Treatment of cancer |
| CN115397815B (zh) * | 2020-03-17 | 2024-06-14 | 江苏恒瑞医药股份有限公司 | 稠合二环类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| CN116322773A (zh) * | 2020-04-21 | 2023-06-23 | 马萨诸塞大学 | 用于治疗年龄相关性黄斑变性的方法和组合物 |
| 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 |
| 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 |
| 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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| EP1067123B1 (en) * | 1998-03-31 | 2011-01-19 | Kyowa Hakko Kirin Co., Ltd. | Nitrogenous heterocyclic compounds |
| 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. |
| NZ590160A (en) | 2003-11-21 | 2012-07-27 | Array Biopharma Inc | AKT protein kinase inhibitors |
| WO2005085249A1 (en) | 2004-02-27 | 2005-09-15 | F. Hoffmann-La Roche Ag | Fused derivatives of pyrazole |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
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- 2005-12-27 EP EP05855490A patent/EP1848719B1/en not_active Expired - Lifetime
- 2005-12-27 CA CA2590961A patent/CA2590961C/en not_active Expired - Fee Related
- 2005-12-27 US US11/722,291 patent/US7994172B2/en not_active Expired - Fee Related
- 2005-12-27 WO PCT/US2005/046938 patent/WO2006071819A1/en not_active Ceased
- 2005-12-27 AU AU2005322085A patent/AU2005322085B2/en not_active Ceased
- 2005-12-27 AT AT05855490T patent/ATE543821T1/de active
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| WO2006071819A1 (en) | 2006-07-06 |
| AU2005322085A1 (en) | 2006-07-06 |
| JP5274842B2 (ja) | 2013-08-28 |
| CA2590961C (en) | 2013-11-26 |
| EP1848719B1 (en) | 2012-02-01 |
| US20080188482A1 (en) | 2008-08-07 |
| EP1848719A1 (en) | 2007-10-31 |
| US7994172B2 (en) | 2011-08-09 |
| CA2590961A1 (en) | 2006-07-06 |
| AU2005322085B2 (en) | 2012-07-19 |
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