AR040580A1 - Derivados de pirazol heterobiciclico como inhibidores de la quinasa - Google Patents
Derivados de pirazol heterobiciclico como inhibidores de la quinasaInfo
- Publication number
- AR040580A1 AR040580A1 AR20030102551A ARP030102551A AR040580A1 AR 040580 A1 AR040580 A1 AR 040580A1 AR 20030102551 A AR20030102551 A AR 20030102551A AR P030102551 A ARP030102551 A AR P030102551A AR 040580 A1 AR040580 A1 AR 040580A1
- Authority
- AR
- Argentina
- Prior art keywords
- group selected
- heterobiciclic
- aryl
- compounds
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- -1 Heterobicyclic pyrazole derivatives Chemical class 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000002074 deregulated effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/02—Immunomodulators
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/42—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms with nitro or nitroso radicals directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Derivados de pirazol heterobicíclico como inhibidores de la quinasa, un procedimiento para su preparación y composiciones farmacéuticas que los comprenden; los compuestos de la presente pueden ser útiles en terapéutica, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como por ejemplo el cáncer. Y una biblioteca combinatoria de compuestos. Reivindicación 1: Un compuesto de biciclo-pirazol de fórmula (1) caracterizado porque: X es un grupo seleccionado entre NR´ , O, S, SO, o SO2; cada uno de R y R1, siendo iguales o diferentes, es seleccionado independientemente entre H o un grupo opcionalmente sustituido seleccionado entre -R´, -COR´, COOR´, -CONHR´,-CONR´R", -SO2R´, -SO2NHR´ o -SO2NR´R"; en donde cada uno de R´y R", siendo iguales o diferentes, es seleccionado independientemente entre H o un grupo alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heterociclilo o arilo-alquilo C1-6, recto o ramificado, sustituido además opcionalmente; R2 es un grupo opcionalmente sustituido seleccionado entre -R´, -CH2OR´ y OR´, en donde R´ es como se definió más arriba; y las sales farmacéuticamente aceptables del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39617402P | 2002-07-17 | 2002-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040580A1 true AR040580A1 (es) | 2005-04-13 |
Family
ID=30115981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AR20030102551A AR040580A1 (es) | 2002-07-17 | 2003-07-16 | Derivados de pirazol heterobiciclico como inhibidores de la quinasa |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP1534716B1 (es) |
| JP (1) | JP2006501191A (es) |
| AR (1) | AR040580A1 (es) |
| AT (1) | ATE393159T1 (es) |
| AU (1) | AU2003254337A1 (es) |
| BR (1) | BR0312722A (es) |
| CA (1) | CA2492673A1 (es) |
| DE (1) | DE60320560T2 (es) |
| ES (1) | ES2304531T3 (es) |
| MX (1) | MXPA05000629A (es) |
| TW (1) | TWI284645B (es) |
| WO (1) | WO2004007504A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1694686A1 (en) | 2003-12-19 | 2006-08-30 | Takeda San Diego, Inc. | Kinase inhibitors |
| TW200526204A (en) * | 2004-02-03 | 2005-08-16 | Pharmacia Italia Spa | 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors |
| EP1778669A2 (en) | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| DE602005023333D1 (de) | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| FR2878442B1 (fr) * | 2004-11-29 | 2008-10-24 | Aventis Pharma Sa | THIENO(2,3-c)PYRAZOLES SUBSTITUES, PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET UTILISATION |
| FR2882751B1 (fr) | 2005-03-04 | 2007-09-14 | Aventis Pharma Sa | Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, procede de preparation, compositions les contenant et utilisation |
| WO2007009898A1 (en) | 2005-07-19 | 2007-01-25 | Nerviano Medical Sciences S.R.L. | 1h-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| JP2009534307A (ja) | 2006-03-30 | 2009-09-24 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 特定の耐性腫瘍の治療のためのキナーゼ阻害剤の使用 |
| EP2010521A1 (en) | 2006-04-19 | 2009-01-07 | Novartis Ag | Indazole compounds and methods for inhibition of cdc7 |
| JP5303454B2 (ja) * | 2006-05-31 | 2013-10-02 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害薬として有用な1h−フロ[3,2−c]ピラゾール化合物 |
| EA200970361A1 (ru) | 2006-10-09 | 2010-02-26 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы киназы |
| US8334301B2 (en) | 2007-09-28 | 2012-12-18 | Takeda Pharmaceutical Company Limited | 5-Membered heterocyclic compound |
| EP2058315A1 (en) | 2007-10-30 | 2009-05-13 | Nerviano Medical Sciences S.r.l. | 1H-Furo[3,2-C]Pyrazoles active as aurora kinase inhibitors |
| DK2692728T3 (en) | 2011-03-31 | 2018-10-08 | Carna Biosciences Inc | UNKNOWN FURANONDERIVATE |
| BR112014020173A8 (pt) | 2012-03-16 | 2017-07-11 | Hoffmann La Roche | Métodos para o tratamento de um melanoma, utilizações de um inibidor, composições, conjunto, método de inibição, método de identificação, método de ajuste do tratamento e invenção |
| WO2015008234A1 (en) * | 2013-07-17 | 2015-01-22 | Glenmark Pharmaceuticals S.A. | Bicyclic heterocyclic compounds as ror gamma modulators |
| US9974795B2 (en) | 2014-01-31 | 2018-05-22 | Carna Biosciences, Inc. | Anticancer agent composition |
| WO2017144546A1 (en) | 2016-02-23 | 2017-08-31 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of nasopharyngeal carcinoma |
| EP3663299B1 (en) * | 2017-08-01 | 2023-03-08 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Bicyclic compound acting as ror gamma inhibitor |
| EP3956446A1 (en) | 2019-04-17 | 2022-02-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for treatment of nlrp3 inflammasome mediated il-1beta dependent disorders |
| CN114981298B (zh) | 2019-12-12 | 2024-08-20 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| WO2021198511A1 (en) | 2020-04-03 | 2021-10-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for treatment of sars-cov-2 infection |
| WO2022008597A1 (en) | 2020-07-08 | 2022-01-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical composition for the treatment of infectious diseases |
| CN113072562B (zh) * | 2021-04-06 | 2022-01-14 | 山东大学 | 一种GSK-3β抑制剂及其制备方法与应用 |
| WO2024261302A1 (en) | 2023-06-22 | 2024-12-26 | Institut National de la Santé et de la Recherche Médicale | Nlrp3 inhibitors, pak1/2 inhibitors and/or caspase 1 inhibitors for use in the treatment of rac2 monogenic disorders |
| WO2025078334A1 (en) | 2023-10-09 | 2025-04-17 | Institut National de la Santé et de la Recherche Médicale | Combination of pak1 inhibitors and clk inhibitors for preventing resistance to chemotherapy in patients suffering from acute myeloid leukemia |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4140785A (en) * | 1978-05-08 | 1979-02-20 | E. I. Du Pont De Nemours And Company | N-(benzothienopyrazol)amide antirhinoviral agents |
| US4420476A (en) * | 1982-05-24 | 1983-12-13 | Averst McKenna & Harrison, Inc. | Benzofuro[3,2-c]pyrazol-3-amine derivatives |
| IL153997A0 (en) * | 2000-08-10 | 2003-07-31 | Pharmacia Italia Spa | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| CZ2003468A3 (cs) * | 2000-08-31 | 2004-05-12 | Pfizeráproductsáinc | Deriváty pyrazolu a jejich použití jako inhibitorů proteinkinázy |
| ES2242771T5 (es) * | 2000-09-15 | 2011-10-14 | Vertex Pharmaceuticals Incorporated | Compuestos de pirazol útiles como inhibidores de proteína quinasas. |
| WO2003051847A1 (en) * | 2001-12-19 | 2003-06-26 | Smithkline Beecham P.L.C. | (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors |
-
2003
- 2003-07-11 AU AU2003254337A patent/AU2003254337A1/en not_active Abandoned
- 2003-07-11 JP JP2004520596A patent/JP2006501191A/ja not_active Abandoned
- 2003-07-11 WO PCT/EP2003/007529 patent/WO2004007504A1/en not_active Ceased
- 2003-07-11 AT AT03763818T patent/ATE393159T1/de not_active IP Right Cessation
- 2003-07-11 EP EP03763818A patent/EP1534716B1/en not_active Expired - Lifetime
- 2003-07-11 CA CA002492673A patent/CA2492673A1/en not_active Abandoned
- 2003-07-11 MX MXPA05000629A patent/MXPA05000629A/es not_active Application Discontinuation
- 2003-07-11 ES ES03763818T patent/ES2304531T3/es not_active Expired - Lifetime
- 2003-07-11 BR BR0312722-2A patent/BR0312722A/pt not_active IP Right Cessation
- 2003-07-11 DE DE60320560T patent/DE60320560T2/de not_active Expired - Fee Related
- 2003-07-14 TW TW092119120A patent/TWI284645B/zh not_active IP Right Cessation
- 2003-07-16 AR AR20030102551A patent/AR040580A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200413389A (en) | 2004-08-01 |
| ATE393159T1 (de) | 2008-05-15 |
| TWI284645B (en) | 2007-08-01 |
| WO2004007504A1 (en) | 2004-01-22 |
| DE60320560T2 (de) | 2008-12-11 |
| EP1534716B1 (en) | 2008-04-23 |
| CA2492673A1 (en) | 2004-01-22 |
| MXPA05000629A (es) | 2005-04-25 |
| AU2003254337A1 (en) | 2004-02-02 |
| EP1534716A1 (en) | 2005-06-01 |
| BR0312722A (pt) | 2005-05-10 |
| DE60320560D1 (de) | 2008-06-05 |
| JP2006501191A (ja) | 2006-01-12 |
| ES2304531T3 (es) | 2008-10-16 |
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