AR023659A1 - Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicos - Google Patents
Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicosInfo
- Publication number
- AR023659A1 AR023659A1 ARP990104643A ARP990104643A AR023659A1 AR 023659 A1 AR023659 A1 AR 023659A1 AR P990104643 A ARP990104643 A AR P990104643A AR P990104643 A ARP990104643 A AR P990104643A AR 023659 A1 AR023659 A1 AR 023659A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- inhibitor compound
- hydrogen
- prevention
- treatment
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 2
- 230000001575 pathological effect Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000002265 prevention Effects 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 239000012826 P38 inhibitor Substances 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 230000030833 cell death Effects 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 230000036755 cellular response Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- -1 methoxy, cyano, nitro, amino, hydroxy, methyl Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
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- 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
-
- 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
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychology (AREA)
- AIDS & HIV (AREA)
Abstract
Un compuesto inhibidor de la p38, la que es una proteinquinasa implicada en proliferacion celular, muerte celular y respuesta a estímulos extracelulares.Más particularmente, la presente invencion se refiere a un compuesto inhibidor de p38,caracteriz ado por la formula (1) o tautomeros del mismo o salesfarmacéuticamente aceptables del mismo; en donde: HET es un heterociclo de 5-7 miembros con 1 a 4 átomos de N, S u O, heterociclo que está sustituido con 1 a 3grupos alquilo C1-4, decadena recta o ramificada, y está sustituido opcionalmente con halo, ciano, N(R)2, OR, CO2R, CON(R)2, y SO2N(R2)2; X es O o NR;n es 1 a 3; R es seleccionado de hidrogeno, alquilo C1-3, alquenilo C2-3 o alquinilo C2-3 fenilo o fenilo sustituido con 1a 3 sustituyen tes seleccionadosindependientemente de halo, metoxi, ciano, nitro, amino, hidroxi, metilo o etilo; R1 es seleccionado de hidrogeno, alquilo C1-3, OH, u O-(alquilo C1-3); R2 esseleccionado de hidrogeno, alquilo C1-3, o alquenilo C1-3;estando cada uno sustituido opcionalmente con -N(R)2, -OR, SR, -C(O)-N(R)2, --S(O2)-N(R)2, C(O)-OR,o R3 es seleccionado de sistemas de un anillo carbocíclico aromático de 5-6 miembros o heterocíclico. La invencion se refiere también a métodosparaproducir estos inhi bidores, a composiciones farmacéuticas que los comprenden y al uso de dichas composiciones en el tratamiento y la prevencion de variosestados patologicos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10101398P | 1998-09-18 | 1998-09-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR023659A1 true AR023659A1 (es) | 2002-09-04 |
Family
ID=22282668
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990104643A AR023659A1 (es) | 1998-09-18 | 1999-09-15 | Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicos |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US6635644B2 (es) |
| EP (1) | EP1114051B1 (es) |
| JP (1) | JP2002526501A (es) |
| AR (1) | AR023659A1 (es) |
| AT (1) | ATE236167T1 (es) |
| AU (1) | AU761599B2 (es) |
| CA (1) | CA2339253C (es) |
| DE (1) | DE69906554T2 (es) |
| DK (1) | DK1114051T3 (es) |
| ES (1) | ES2192864T3 (es) |
| MY (1) | MY117696A (es) |
| PT (1) | PT1114051E (es) |
| WO (1) | WO2000017204A1 (es) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE266399T1 (de) | 1998-08-20 | 2004-05-15 | Smithkline Beecham Corp | Neue substituierte triazolverbindungen |
| WO2002014281A1 (en) * | 2000-08-11 | 2002-02-21 | Vertex Pharmaceuticals Incorporated | Pyridine derivatives as inhibitors of p38 |
| ATE415162T1 (de) | 2001-06-11 | 2008-12-15 | Vertex Pharma | Isochinolin-inhibitoren von p38 |
| JP2005519895A (ja) * | 2002-01-18 | 2005-07-07 | ファルマシア・コーポレーション | Ｐ３８阻害剤としての置換ピリダジノン |
| ES2278170T3 (es) | 2002-07-09 | 2007-08-01 | BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG | Composiciones farmaceuticas de anticolinergicos e inhibidores de la quinasa p38 en el tratamiento de enfermedades respiratorias. |
| US7268139B2 (en) | 2002-08-29 | 2007-09-11 | Scios, Inc. | Methods of promoting osteogenesis |
| NZ541234A (en) | 2002-12-20 | 2008-06-30 | Amgen Inc | Asthma and allergic inflammation modulators |
| EP2251343A1 (en) | 2003-05-15 | 2010-11-17 | Arqule, Inc. | Imidazothiazoles as p38-kinase-inhibitors |
| WO2005007632A1 (en) * | 2003-07-18 | 2005-01-27 | Pharmacia Corporation | Substituted pyridazinones as inhibitors of p38 |
| WO2005030091A2 (en) | 2003-09-25 | 2005-04-07 | Scios Inc. | Stents and intra-luminal prostheses containing map kinase inhibitors |
| JP4608888B2 (ja) * | 2004-01-23 | 2011-01-12 | 宇部興産株式会社 | ２−シアノ−２−（４−テトラヒドロピラニル）酢酸エステルの製法 |
| WO2006010082A1 (en) | 2004-07-08 | 2006-01-26 | Arqule, Inc. | 1,4-disubstituted naphtalenes as inhibitors of p38 map kinase |
| US20060035893A1 (en) | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| US20070054916A1 (en) * | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| CA2584368A1 (en) | 2004-10-19 | 2006-04-27 | Arqule, Inc. | Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| EP1676574A3 (en) | 2004-12-30 | 2006-07-26 | Johnson & Johnson Vision Care, Inc. | Methods for promoting survival of transplanted tissues and cells |
| US20060178388A1 (en) * | 2005-02-04 | 2006-08-10 | Wrobleski Stephen T | Phenyl-substituted pyrimidine compounds useful as kinase inhibitors |
| US7759337B2 (en) * | 2005-03-03 | 2010-07-20 | Amgen Inc. | Phthalazine compounds and methods of use |
| CN101228135B (zh) | 2005-07-21 | 2011-08-31 | 霍夫曼-拉罗奇有限公司 | 作为甲状腺激素受体激动剂的哒嗪酮衍生物 |
| US7482345B2 (en) | 2005-12-05 | 2009-01-27 | Meng-Hsin Chen | P38 kinase inhibiting agents |
| LT1976828T (lt) | 2005-12-29 | 2017-04-25 | Celtaxsys, Inc. | Diamino dariniai, kaip leukotrieno a4 hidrolazės inhibitoriai |
| WO2007124181A2 (en) * | 2006-04-21 | 2007-11-01 | Amgen Inc. | Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use |
| EP2049503B1 (en) * | 2006-07-17 | 2012-12-19 | Amgen Inc. | Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors |
| DE602007013079D1 (de) * | 2006-09-05 | 2011-04-21 | Amgen Inc | Phthalazin-, aza- und diazaphthalazinverbindungen und anwendungsverfahren |
| CA2665195C (en) * | 2006-10-11 | 2011-08-09 | Amgen Inc. | Imidazo- and triazolo-pyridine compounds and methods of use thereof |
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| CA2685597C (en) | 2007-05-07 | 2012-10-02 | Amgen Inc. | Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as p38 modulators, process for their preparation, and their pharmaceutical use |
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| WO2009078992A1 (en) * | 2007-12-17 | 2009-06-25 | Amgen Inc. | Linear tricyclic compounds as p38 kinase inhibitors |
| EA201001029A1 (ru) | 2007-12-19 | 2011-06-30 | Амген Инк. | Производные фенилуксусной кислоты в качестве модуляторов процесса воспаления |
| US8367671B2 (en) * | 2008-03-21 | 2013-02-05 | Amgen Inc. | Pyrazolo[3.4-B]pyrazine compounds as p38 modulators and methods of use as anti-inflamatory agents |
| EP2334673A1 (en) | 2008-08-29 | 2011-06-22 | Amgen Inc. | PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF |
| EP2334674B1 (en) | 2008-08-29 | 2012-06-06 | Amgen, Inc | Pyridazino- pyridinone compounds for the treatment of protein kinase mediated diseases. |
| WO2010042646A1 (en) | 2008-10-10 | 2010-04-15 | Amgen Inc. | Aza- and diaza-phthalazine compounds as p38 map kinase modulators and methods of use thereof |
| US8497269B2 (en) | 2008-10-10 | 2013-07-30 | Amgen Inc. | Phthalazine compounds as p38 map kinase modulators and methods of use thereof |
| EP3312269A1 (en) | 2008-12-17 | 2018-04-25 | The Scripps Research Institute | Generation and maintenance of stem cells |
| GB0902648D0 (en) * | 2009-02-17 | 2009-04-01 | Argenta Discovery Ltd | Pharmaceutical compounds and compositions |
| GB0908317D0 (en) * | 2009-05-14 | 2009-06-24 | Argenta Discovery Ltd | Pharmaceutical compounds and compositions |
| US8809372B2 (en) | 2011-09-30 | 2014-08-19 | Asana Biosciences, Llc | Pyridine derivatives |
| US9199975B2 (en) | 2011-09-30 | 2015-12-01 | Asana Biosciences, Llc | Biaryl imidazole derivatives for regulating CYP17 |
| EP2843049B1 (en) | 2012-04-27 | 2018-04-11 | Keio University | Neuronal differentiation promoter |
| JP6527851B2 (ja) | 2013-03-12 | 2019-06-05 | セルタクシス，インコーポレイテッド | ロイコトリエンａ４加水分解酵素を阻害する方法 |
| MX2015011678A (es) | 2013-03-14 | 2016-07-08 | Celtaxsys Inc | Inhibidores de leucotrieno a4 hidrolasa. |
| AU2014239585B2 (en) | 2013-03-14 | 2019-04-04 | Celtaxsys, Inc. | Inhibitors of leukotriene A4 hydrolase |
| BR112015022226A2 (pt) | 2013-03-14 | 2017-07-18 | Celtaxsys Inc | inibidores de leucotrieno a4 hidrolase |
| DK3368052T3 (da) | 2015-10-27 | 2022-03-14 | Childrens Hospital Med Ct | Anvendelse af mapk-hæmmere for at nedbringe tabet af hæmatopoietiske stamceller under ex vivo-dyrkning og -genmanipulation |
| US20190060286A1 (en) | 2016-02-29 | 2019-02-28 | University Of Florida Research Foundation, Incorpo | Chemotherapeutic Methods |
| JP2021519334A (ja) | 2018-03-26 | 2021-08-10 | クリア クリーク バイオ， インコーポレイテッド | ジヒドロオロト酸デヒドロゲナーゼを阻害するための組成物および方法 |
| US10898484B2 (en) | 2018-05-31 | 2021-01-26 | Celltaxis, Llc | Method of reducing pulmonary exacerbations in respiratory disease patients |
| US20210300873A1 (en) | 2020-03-20 | 2021-09-30 | Clear Creek Bio, Inc. | Stable polymorphic compositions of brequinar sodium and methods of use and manufacture thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6147080A (en) * | 1996-12-18 | 2000-11-14 | Vertex Pharmaceuticals Incorporated | Inhibitors of p38 |
| WO2002014281A1 (en) * | 2000-08-11 | 2002-02-21 | Vertex Pharmaceuticals Incorporated | Pyridine derivatives as inhibitors of p38 |
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1999
- 1999-09-15 AR ARP990104643A patent/AR023659A1/es unknown
- 1999-09-16 ES ES99948314T patent/ES2192864T3/es not_active Expired - Lifetime
- 1999-09-16 AU AU61521/99A patent/AU761599B2/en not_active Ceased
- 1999-09-16 DE DE69906554T patent/DE69906554T2/de not_active Expired - Lifetime
- 1999-09-16 AT AT99948314T patent/ATE236167T1/de not_active IP Right Cessation
- 1999-09-16 PT PT99948314T patent/PT1114051E/pt unknown
- 1999-09-16 EP EP99948314A patent/EP1114051B1/en not_active Expired - Lifetime
- 1999-09-16 DK DK99948314T patent/DK1114051T3/da active
- 1999-09-16 JP JP2000574113A patent/JP2002526501A/ja active Pending
- 1999-09-16 WO PCT/US1999/021567 patent/WO2000017204A1/en not_active Ceased
- 1999-09-16 CA CA002339253A patent/CA2339253C/en not_active Expired - Fee Related
- 1999-09-17 MY MYPI99004032A patent/MY117696A/en unknown
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2001
- 2001-03-16 US US09/809,921 patent/US6635644B2/en not_active Expired - Fee Related
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2003
- 2003-09-08 US US10/658,111 patent/US7169779B2/en not_active Expired - Fee Related
Also Published As
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|---|---|
| DE69906554T2 (de) | 2004-07-01 |
| EP1114051A1 (en) | 2001-07-11 |
| ES2192864T3 (es) | 2003-10-16 |
| MY117696A (en) | 2004-07-31 |
| JP2002526501A (ja) | 2002-08-20 |
| ATE236167T1 (de) | 2003-04-15 |
| US20040142927A1 (en) | 2004-07-22 |
| US7169779B2 (en) | 2007-01-30 |
| AU761599B2 (en) | 2003-06-05 |
| US20020010170A1 (en) | 2002-01-24 |
| AU6152199A (en) | 2000-04-10 |
| CA2339253C (en) | 2009-04-07 |
| PT1114051E (pt) | 2003-07-31 |
| EP1114051B1 (en) | 2003-04-02 |
| DK1114051T3 (da) | 2003-07-14 |
| CA2339253A1 (en) | 2000-03-30 |
| WO2000017204A1 (en) | 2000-03-30 |
| US6635644B2 (en) | 2003-10-21 |
| DE69906554D1 (de) | 2003-05-08 |
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