ES2422263T3 - Pirazoles bicíclicos como inhibidores de la proteinquinasa - Google Patents
Pirazoles bicíclicos como inhibidores de la proteinquinasaInfo
- Publication number
- ES2422263T3 ES2422263T3 ES09775222T ES09775222T ES2422263T3 ES 2422263 T3 ES2422263 T3 ES 2422263T3 ES 09775222 T ES09775222 T ES 09775222T ES 09775222 T ES09775222 T ES 09775222T ES 2422263 T3 ES2422263 T3 ES 2422263T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- heteroaryl
- optionally substituted
- group selected
- heterocyclyl
- 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.)
- Active
Links
- -1 Bicyclic pyrazoles Chemical class 0.000 title 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto de fórmula (I):**Fórmula** en donde: X es CH o N; R1 es hidrógeno, halógeno, NR7R8, NHCOR9, SR10 o SO2R, en donde: R7 y R8 son, independientemente uno de otro, hidrógeno, o un grupo opcionalmentesustituido seleccionado entre alquilo (C1-C8) alquilo lineal o ramificado, cicloalquilo (C3-C8), heterociclilo, arilo y heteroarilo, o R7 y R8 tomados juntos pueden formar un grupoftalilo, R9 es OR10, NR11R12 o un grupo opcionalmente sustituido seleccionado de alquilo (C1-C8) alquilo lineal o ramificado, alquenilo (C2-C8) o alquenilo (C2-C8), cicloalquilo (C3-C8),heterociclilo, arilo y heteroarilo, R10 es un grupo opcionalmente sustituido seleccionado entre alquilo (C1-C8) lineal oramificado, cicloalquilo (C3-C8), heterociclilo, arilo y heteroarilo, R11 y R12 son, independientemente uno de otro, hidrógeno o un grupo opcionalmentesustituido seleccionado de alquilo (C1-C8) lineal o ramificado, cicloalquilo (C3-C8),heterociclilo, arilo y heteroarilo, o tomados junto con el átomo de nitrógeno al cual estánunidos R11 y R12 pueden formar un heterociclilo o heteroarilo de 3 a 8 miembrosopcionalmente sustituido, que contiene opcionalmente un heteroátomo o grupoheteroatómico adicional seleccionado entre S, O, N o NH.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08172429 | 2008-12-19 | ||
| PCT/EP2009/067438 WO2010070060A1 (en) | 2008-12-19 | 2009-12-17 | Bicyclic pyrazoles as protein kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2422263T3 true ES2422263T3 (es) | 2013-09-10 |
Family
ID=41565939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09775222T Active ES2422263T3 (es) | 2008-12-19 | 2009-12-17 | Pirazoles bicíclicos como inhibidores de la proteinquinasa |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8524707B2 (es) |
| EP (1) | EP2373664B1 (es) |
| JP (1) | JP5490137B2 (es) |
| ES (1) | ES2422263T3 (es) |
| WO (1) | WO2010070060A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| EP2402339A1 (en) * | 2010-06-29 | 2012-01-04 | Basf Se | Pyrazolopyridine compounds |
| EP2739144A4 (en) * | 2011-06-20 | 2015-04-01 | Alzheimer S Inst Of America Inc | COMPOUNDS AND ITS THERAPEUTIC USE |
| UA114490C2 (uk) | 2011-10-06 | 2017-06-26 | Байєр Інтеллектуал Проперті Гмбх | Гетероциклілпіри(mі)динілпіразоли як фунгіциди |
| JP6150813B2 (ja) | 2011-11-11 | 2017-06-21 | ノバルティス アーゲー | 増殖性疾患の治療方法 |
| CA2856406C (en) | 2011-11-23 | 2020-06-23 | Novartis Ag | Pharmaceutical formulations |
| TWI679205B (zh) | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
| TWI712604B (zh) * | 2016-03-01 | 2020-12-11 | 日商日本新藥股份有限公司 | 具jak抑制作用之化合物之結晶 |
| CN106883266B (zh) * | 2017-01-23 | 2020-03-17 | 江苏七洲绿色化工股份有限公司 | 一种1-(4-氯苯基)-2-环丙基-1-丙酮的制备方法及其中间体 |
| EP4185568A1 (en) | 2020-07-24 | 2023-05-31 | The University of Rochester | Inhibitors of interleukin-1 receptor-associated kinases 1 and 4 |
| KR20240021143A (ko) * | 2021-01-22 | 2024-02-16 | 히버셀, 인크. | Gcn2 조정 화합물 및 그의 용도 |
| US20250051300A1 (en) * | 2021-11-19 | 2025-02-13 | The Board Of Trustees Of The University Of Illinois | Gram-negative specific antibiotics sparing effect on gut microbiome |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD103006A1 (es) | 1972-12-29 | 1974-01-05 | ||
| DD157803A1 (de) | 1980-03-20 | 1982-12-08 | Klaus Peseke | Verfahren zur herstellung von pyrazolo[5.1-b][1.3]thiazinen |
| JPS6438091A (en) * | 1986-03-20 | 1989-02-08 | Takeda Chemical Industries Ltd | Condensed heterocyclic sulfonylurea |
| AU672773B2 (en) | 1992-01-29 | 1996-10-17 | E.I. Du Pont De Nemours And Company | Substituted phenylheterocyclic herbicides |
| BR0113139A (pt) * | 2000-08-09 | 2003-06-24 | Agouron Pharma | Compostos, seus sais, formas multiméricas, pró-drogas ou metabólitos, composições farmacêuticas, método de tratamento de uma doença ou disfunção mediana através da inibição de cdk4 ou um complexo de cdk4/ciclina, método de tratamento de condição doentia em mamìferos mediada pela atividade de proteìna cinase e método de modulação ou inibição da atividade de um receptor de proteìna cinase |
| BR0116493A (pt) * | 2000-12-21 | 2003-09-30 | Vertex Pharma | Compostos de pirazol úteis como inibidores de proteìna cinase |
| US7153855B2 (en) * | 2001-03-08 | 2006-12-26 | Smithkline Beecham Corporation | Pyrazolopyridinyl pyrimidine therapeutic compounds |
| SI1397364T1 (sl) * | 2001-05-24 | 2007-12-31 | Lilly Co Eli | Novi pirolni derivati kot farmacevtske uäśinkovine |
| WO2006068826A2 (en) * | 2004-12-21 | 2006-06-29 | Smithkline Beecham Corporation | 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors |
| JP2009515998A (ja) * | 2005-11-16 | 2009-04-16 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | ピラゾロチアゾールタンパク質キナーゼモジュレータ |
| CA2643066A1 (en) * | 2006-03-16 | 2007-09-20 | Pfizer Products Inc. | Pyrazole compounds |
| WO2007123892A2 (en) * | 2006-04-17 | 2007-11-01 | Arqule Inc. | Raf inhibitors and their uses |
| FR2904626B1 (fr) | 2006-08-03 | 2008-09-19 | Sanofi Aventis | Derives de pyrazolo[4,3]thiazole, leur preparation et leur application en therapeutique |
-
2009
- 2009-12-17 ES ES09775222T patent/ES2422263T3/es active Active
- 2009-12-17 EP EP09775222.4A patent/EP2373664B1/en not_active Not-in-force
- 2009-12-17 US US13/140,915 patent/US8524707B2/en active Active
- 2009-12-17 WO PCT/EP2009/067438 patent/WO2010070060A1/en not_active Ceased
- 2009-12-17 JP JP2011541448A patent/JP5490137B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US8524707B2 (en) | 2013-09-03 |
| JP5490137B2 (ja) | 2014-05-14 |
| US20110257165A1 (en) | 2011-10-20 |
| JP2012512837A (ja) | 2012-06-07 |
| EP2373664A1 (en) | 2011-10-12 |
| EP2373664B1 (en) | 2013-06-12 |
| WO2010070060A1 (en) | 2010-06-24 |
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