AR074870A1 - DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINA - Google Patents
DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINAInfo
- Publication number
- AR074870A1 AR074870A1 ARP090105067A ARP090105067A AR074870A1 AR 074870 A1 AR074870 A1 AR 074870A1 AR P090105067 A ARP090105067 A AR P090105067A AR P090105067 A ARP090105067 A AR P090105067A AR 074870 A1 AR074870 A1 AR 074870A1
- Authority
- AR
- Argentina
- Prior art keywords
- 4alkyl
- alkyl
- ring
- optionally
- haloc1
- Prior art date
Links
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 22
- 125000004432 carbon atom Chemical group C* 0.000 abstract 9
- 229910052799 carbon Inorganic materials 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 229920006395 saturated elastomer Polymers 0.000 abstract 6
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- 125000004434 sulfur atom Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 101100134922 Gallus gallus COR5 gene Proteins 0.000 abstract 1
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 abstract 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- 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
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Estos compuestos son útiles como inhibidores de la cinasa JAK3. Composición farmacéutica y proceso. Reivindicación 1: Un compuesto caracterizado por la fórmula 1 o una sal del mismo, donde R1 representa hidrógeno, alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R7-alquilo C1-4, halógeno, -CN, -CONR4R4, -COR5, -CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R2 representa hidrógeno, alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R7-alquilo C1-4 o Cy2, donde Cy2 puede estar opcionalmente sustituido por uno o más R8; R3 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4, -CONR9R9, -COR10, -CO2R10, -SO2R10, -SO2NR9R9 o Cy3, donde Cy3 puede estar opcionalmente sustituido por uno o más R12; o bien R2 y R3 pueden estar unidos formando, junto con el átomo de N, un grupo Cy4, donde Cy4 puede estar opcionalmente sustituido por uno o más grupos R12; R4 representa hidrógeno o R5; R5 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, Cy1-alquilo C1-4 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R6 representa hidrógeno o alquilo C1-4; R7 representa -CN, -CONR4R4, -COR5, --CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R8 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, halógeno o hidroxilo; R9 representa hidrógeno o R10; R10 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R11 representa halógeno, -CN, -CONR14R14, -COR15, -CO2R15, -OR14, -OCONR14R14, -SO2R15, -SO2NR14R4, -NR14R14, -NR6COR14, -NR5CONR14R14, -NR6CO2R15, -NR6SO2R15 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R12 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4; o bien R12 representa cualquiera de los significados descritos para R11; R13 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, halógeno, -CN, -CONR16R16, -COR17, -CO2R17, -OR16, -OCONR16R16, -SO2R17, -SO2NR16R16, -NR16R16, -NR6COR16, -NR6CONR16R16, -NR6CO2R17 o -NR6SO2R17; R14 representa hidrógeno o R15; R15 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo,Cy5-alquilo C1-4 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R16 representa H o R17; R17 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo o cianoC1-4alquilo, Cy1 representa un anillo carbocíclico monocíclico de 3 a 7 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 3 heteroátomos seleccionados de N, S y O, donde dicho anillo puede estar unido al resto de la molécula a través de cualquier átomo de C o N disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy2 representa un anillo carbocíclico monocíclico de 3 a 7 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 3 heteroátomos seleccionados de N, S y O donde dicho anillo esta unido al resto de la molécula a través de cualquier átomo de C disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy3 representa un anillo carbocíclico monocíclico de 3 a 7 miembros o bicíclico de 8 a 12 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 4 heteroátomos seleccionados de N, S y O donde dicho anillo está unido al resto de la molécula a través de cualquier átomo de C disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy4 representa un anillo heterocíclico monocíclico de 3 a 7 miembros saturado o parcialmente insaturado, que puede estar opcionalmente fusionado a un anillo de 5 o 6 miembros carbocíclico o heterocíclico saturado, parcialmente insaturado o aromático, donde Cy4 puede contener en total de 1 a 4 heteroátomos seleccionados de N, O y S, y donde uno o más átomos de C o S de Cy4 pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; y Cy5 representa un anillo carbocíclico monocíclico de 3 a 7 miembros o bicíclico de 8 a 12 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 4 heteroátomos seleccionados de N, S y O, donde dicho anillo puede estar unido al resto de la molécula a través de cualquier átomo de C o N disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2.These compounds are useful as inhibitors of JAK3 kinase. Pharmaceutical composition and process. Claim 1: A compound characterized by the formula 1 or a salt thereof, wherein R1 represents hydrogen, C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R7-C1-4 alkyl, halogen, -CN, -CONR4R4, - COR5, -CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 or Cy1, where Cy1 can be optionally substituted by one or more R8; R2 represents hydrogen, C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R7-C1-4 alkyl or Cy2, where Cy2 may be optionally substituted by one or more R8; R3 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl, -CONR9R9, -COR10, -CO2R10, -SO2R10, -SO2NR9R9 or Cy3, where Cy3 may be optionally substituted by one or more R12 ; or R2 and R3 can be linked together, together with the N atom, a Cy4 group, where Cy4 can be optionally substituted by one or more R12 groups; R4 represents hydrogen or R5; R5 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy1-C1-4alkyl or Cy1, where Cy1 may be optionally substituted by one or more R8; R6 represents hydrogen or C1-4 alkyl; R7 represents -CN, -CONR4R4, -COR5, --CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 or Cy1, where Cy1 may be optionally substituted plus R8; R8 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, halogen or hydroxyl; R9 represents hydrogen or R10; R10 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl or Cy5, where Cy5 may be optionally substituted by one or more R13; R11 represents halogen, -CN, -CONR14R14, -COR15, -CO2R15, -OR14, -OCONR14R14, -SO2R15, -SO2NR14R4, -NR14R14, -NR6COR14, -NR5CONR14R14, -NR6CO2R15, -NR6SO2, can optionally be replaced by one or more R13; R12 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl; or R12 represents any of the meanings described for R11; R13 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, halogen, -CN, -CONR16R16, -COR17, -CO2R17, -OR16, -OCONR16R16, - SO2R17, -SO2NR16R16, -NR16R16, -NR6COR16, -NR6CONR16R16, -NR6CO2R17 or -NR6SO2R17; R14 represents hydrogen or R15; R15 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy5-C1-4 alkyl or Cy5, where Cy5 may be optionally substituted by one or more R13; R16 represents H or R17; R17 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl or cyanoC1-4alkyl, Cy1 represents a 3- to 7-membered monocyclic carbocyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 3 heteroatoms selected from N, S and O, where said ring can be attached to the rest of the molecule through any available C or N atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy2 represents a 3- to 7-membered monocyclic carbocyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 3 heteroatoms selected from N, S and O where said ring is attached to the rest of the molecule through of any available C atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy3 represents a 3- to 7-membered monocyclic carbocyclic or 8 to 12-membered bicyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 4 heteroatoms selected from N, S and O where said ring is attached to the rest of the molecule through any available C atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy4 represents a 3 to 7-membered saturated or partially unsaturated monocyclic heterocyclic ring, which may be optionally fused to a saturated, partially unsaturated or aromatic carbocyclic or heterocyclic 5 or 6-membered ring, where Cy4 may contain a total of 1 to 4 heteroatoms selected from N, O and S, and where one or more C or S atoms of Cy4 may optionally be oxidized forming CO, SO or SO2 groups; and Cy5 represents a 3- to 7-membered monocyclic carbocyclic or 8 to 12-membered bicyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 4 heteroatoms selected from N, S and O, wherein said ring it can be attached to the rest of the molecule through any available C or N atom, and where one or more C or S atoms of the ring can be optionally oxidized forming CO, SO or SO2 groups.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08382087 | 2008-12-24 | ||
| US15571309P | 2009-02-26 | 2009-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074870A1 true AR074870A1 (en) | 2011-02-16 |
Family
ID=40680391
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090105067A AR074870A1 (en) | 2008-12-24 | 2009-12-22 | DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINA |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR074870A1 (en) |
| TW (1) | TW201035095A (en) |
| WO (1) | WO2010072823A1 (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY33213A (en) * | 2010-02-18 | 2011-09-30 | Almirall Sa | PIRAZOL DERIVATIVES AS JAK INHIBITORS |
| SG183426A1 (en) * | 2010-04-28 | 2012-09-27 | Daiichi Sankyo Co Ltd | [5,6] heterocyclic compound |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| EP3080101A1 (en) | 2013-12-10 | 2016-10-19 | Cleave Biosciences, Inc. | Monocyclic pyrimidine/pyridine compounds as inhibitors of p97 complex |
| KR101922317B1 (en) | 2014-01-20 | 2018-11-26 | 클리브 바이오사이언스 인코포레이티드 (클리브) | FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX |
| AU2017275657B2 (en) | 2016-06-02 | 2021-08-19 | Novartis Ag | Potassium channel modulators |
| RS62899B1 (en) | 2017-01-23 | 2022-03-31 | Cadent Therapeutics Inc | Potassium channel modulators |
| MX2021004647A (en) | 2018-10-22 | 2021-08-16 | Novartis Ag | CRYSTALLINE FORMS OF POTASSIUM CHANNELS MODULATORS. |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN114761013A (en) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | Methods of treating myelofibrosis and related disorders |
| KR20230012539A (en) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | Anti-hemojuvelin (HJV) antibodies to treat myelofibrosis |
| WO2025029897A1 (en) * | 2023-08-03 | 2025-02-06 | Neuro3 Therapeutics, Inc. | Substituted pyrazolopyridines |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE323706T1 (en) * | 2001-12-17 | 2006-05-15 | Smithkline Beecham Corp | PYRAZOLOPYRIDAZINE DERIVATIVES |
| EP2332940B1 (en) * | 2004-03-30 | 2012-10-31 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
| JP5352452B2 (en) * | 2006-06-06 | 2013-11-27 | メディシノバ， インコーポレイテッド | Substituted pyrazolo [1,5-a] pyridine compounds and methods of use thereof |
-
2009
- 2009-12-22 AR ARP090105067A patent/AR074870A1/en unknown
- 2009-12-23 WO PCT/EP2009/067883 patent/WO2010072823A1/en not_active Ceased
- 2009-12-24 TW TW098144821A patent/TW201035095A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010072823A1 (en) | 2010-07-01 |
| TW201035095A (en) | 2010-10-01 |
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