AR073079A1 - Compuestos triazolopiridina como inhibidores de pim cinasa - Google Patents
Compuestos triazolopiridina como inhibidores de pim cinasaInfo
- Publication number
- AR073079A1 AR073079A1 ARP090103170A ARP090103170A AR073079A1 AR 073079 A1 AR073079 A1 AR 073079A1 AR P090103170 A ARP090103170 A AR P090103170A AR P090103170 A ARP090103170 A AR P090103170A AR 073079 A1 AR073079 A1 AR 073079A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- ring
- optionally substituted
- membered
- Prior art date
Links
Classifications
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- 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
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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
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- 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
- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Estos compuestos son inhibidores de tirosina de receptor utiles en el tratamiento de enfermedades asociadas con células inmunes, tales como enfermedades inflamatorias y autoinmunes. Se proveen además una composicion farmacéutica que los comprende y un método para su preparacion. Reivindicacion 1: Un compuesto de la formula general (1) o una sal farmacéuticamente aceptable de él, en donde: A es OR10 o NR11R12; B es H, F, Cl, ORa, alquilo C1-6NRbRc, alquilo C1-6OH, CH(OH)CH2OH o alquilo C1-4; R1 es H, F, Cl, Br, Me, ciclopropilo o CN; R1a, R2, R3 y R4 son independientemente H, F, Cl, Br, Me o CN; R5 y R7 son independientemente H, F, Me o CN; R6 es H, F, Me, Br, CN, ciclopropilo, fenilo, MeO- o MeOCH2CH2O-; R10 es H, hetCyc1, alquilo C1-3hetCyc1a, hetCyc2, (CR17R18)p(CR13R14)CH2NR15R16, -(CR17R18)p(CR13R14)CH2OH, alquilo C1-6, hetAr1, alquilo C1-3hetAr1a, o cicloalquilo C3-7 sustituido con NH2, NH-alquilo C1-6 o N(alquilo C1-6)2; R11 es H o alquilo C1-6; R12 es hetCyc3, alquilo C1-6NR15R16, C(O)alquilo C1-6NR15R16, alquilo C1-6NHC(O)O-alquilo C1-6, o cicloalquilo C4-7 optativamente sustituido con OH, NH2, NH-alquilo C1-6 o N(alquilo C1-6)2; R13 es H, alquilo C1-6, F o OH, y R14 es H, alquilo C1-6 o F, o R13 y R14 junto con el átomo de carbono al cual están unidos forman un anillo carbocíclico de 3-6 miembros; cada R15, R16, R17 y R18 es independientemente H o alquilo C1-6, o cada R15, R17, y R18 es independientemente H o alquilo C1-6 y R16 es H, alquilo C1-6, C(=O)CH2F, CH2CHF2 o CH2CF3; o NR15R16 forma un anillo heterocíclico de 5-6 miembros que tiene un primer heteroátomo del anillo que es N y que optativamente tiene un segundo heteroátomo del anillo que es N y O; hetCyc1, hetCyc1a y hetCyc3 son independientemente un heterociclo de 4-7 miembros que tiene un átomo del anillo de nitrogeno y optativamente sustituido con uno o más grupos R9, o hetCyc1 y hetCyc3 son independientemente un heterociclo de 4-7 miembros que tiene un átomo de N y optativamente sustituido con uno o más grupos R9, y hetCyc1a se selecciona de un morfolinilo y un anillo azacíclico de 4-7 miembros optativamente sustituido con uno o más grupos R9; cada R9 se selecciona independientemente de halogeno, alquilo C1-6, ciclopropilmetilo, bencilo, NRfRg, alquilo C1-6NRhRi, ORj, alquilo C1-6ORk, fluoroalquilo C1-6, C(O)NRmRn, alquilo C1-6C(O)NRpRq, y C(O)O-alquilo C1-6; hetCyc2 es un heterociclo de puente de 8 miembros que tiene un átomo de nitrogeno del anillo; hetAr1 y hetAr1a son independientemente un heteroarilo de 5 o 6 miembros que tiene 1-2 átomos de nitrogeno del anillo y optativamente sustituido con uno o más sustituyentes, que se seleccionan independientemente de F, Cl, Br, Me, ciclopropilo, CN, NH2, NH-alquilo C1-6 y N(alquilo C1-6)2; Ra es H, alquilo C1-6, alquilo C1-6-O-alquilo C1-6, o alquilo C1-6-O-cicloalquilo C3-6; cada Rb, Rf, Rg, Rh, Ri, Rk, Rm, Rp, y Rq se selecciona independientemente de H y alquilo C1-6; Rj es H, alquilo C1-6 o ciclopropilo; Rn es H, alquilo C1-6, -O-alquilo C1-6 o -O-cicloalquilo C3-6; y p es 0, 1 o 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8995208P | 2008-08-19 | 2008-08-19 | |
| US17527709P | 2009-05-04 | 2009-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073079A1 true AR073079A1 (es) | 2010-10-13 |
Family
ID=41227138
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103170A AR073079A1 (es) | 2008-08-19 | 2009-08-18 | Compuestos triazolopiridina como inhibidores de pim cinasa |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8575145B2 (es) |
| EP (1) | EP2334677B1 (es) |
| JP (2) | JP5518072B2 (es) |
| CN (1) | CN102186851B (es) |
| AR (1) | AR073079A1 (es) |
| CA (1) | CA2734831C (es) |
| DK (1) | DK2334677T3 (es) |
| ES (1) | ES2439501T3 (es) |
| HR (1) | HRP20131140T1 (es) |
| PL (1) | PL2334677T3 (es) |
| PT (1) | PT2334677E (es) |
| RS (1) | RS53079B (es) |
| SI (1) | SI2334677T1 (es) |
| SM (1) | SMT201400154B (es) |
| TW (1) | TWI496779B (es) |
| UY (1) | UY32057A (es) |
| WO (1) | WO2010022076A1 (es) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| LT2474545T (lt) | 2005-12-13 | 2017-02-27 | Incyte Holdings Corporation | Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai |
| TWI417095B (zh) | 2006-03-15 | 2013-12-01 | Janssen Pharmaceuticals Inc | １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途 |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| CA2689663C (en) | 2007-06-13 | 2016-08-09 | Incyte Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| PT2203439E (pt) | 2007-09-14 | 2011-02-11 | Ortho Mcneil Janssen Pharm | 4-fenil-3,4,5,6-tetra-hidro-2h,1'h-[1,4']bipiridinil-2'- onas 1',3'-dissubstituídas |
| TW200927731A (en) | 2007-09-14 | 2009-07-01 | Ortho Mcneil Janssen Pharm | 1,3-disubstituted-4-phenyl-1H-pyridin-2-ones |
| WO2009033702A1 (en) | 2007-09-14 | 2009-03-19 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones |
| EP2220083B1 (en) | 2007-11-14 | 2017-07-19 | Janssen Pharmaceuticals, Inc. | Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
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| EA202191349A1 (ru) | 2018-11-15 | 2021-08-10 | Ниппон Синяку Ко., Лтд. | 1,3,4-оксадиазолон и фармацевтический препарат |
| AU2020221247A1 (en) | 2019-02-12 | 2021-08-05 | Sumitomo Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| CN111138429A (zh) * | 2019-12-31 | 2020-05-12 | 西安邮电大学 | 1,2,4-三氮唑并吡啶类衍生物的合成方法 |
| CN111171023B (zh) * | 2020-01-10 | 2021-12-21 | 中国药科大学 | 一种具有Pim1抑制活性的化合物及其制备方法与医药用途 |
| CN113620942A (zh) * | 2020-05-06 | 2021-11-09 | 北京鼎材科技有限公司 | 一种化合物及其应用 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
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| WO2001034603A2 (en) | 1999-11-12 | 2001-05-17 | Neurogen Corporation | Bicyclic and tricyclic heteroaromatic compounds |
| DK1277754T3 (da) | 2000-04-27 | 2005-11-14 | Astellas Pharma Inc | Imidazopyridinderivater |
| DE10038019A1 (de) | 2000-08-04 | 2002-02-14 | Bayer Ag | Substituierte Triazolopyrid(az)ine |
| MXPA03008144A (es) | 2001-03-09 | 2003-12-12 | Pfizer Prod Inc | Nuevos compuestos antiinflamatorios de triazolopiridinas. |
| US7227006B2 (en) | 2002-01-19 | 2007-06-05 | Sanofi-Aventis Deutschland Gmbh | PIM-3 kinase as a target for type 2 diabetes mellitus |
| WO2004058749A1 (en) | 2002-12-18 | 2004-07-15 | Vertex Pharmaceuticals Incorporated | Benzisoxazole derivatives useful as inhibitors of protein kinases |
| ATE473980T1 (de) * | 2002-12-18 | 2010-07-15 | Vertex Pharma | Triazolopyridazine als proteinkinase-inhibitoren |
| US20050164300A1 (en) | 2003-09-15 | 2005-07-28 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
| US20050256309A1 (en) * | 2004-05-12 | 2005-11-17 | Altenbach Robert J | Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands |
| EP1781655A2 (en) | 2004-08-18 | 2007-05-09 | Pharmacia & Upjohn Company LLC | Triazolopyridine compounds useful for the treatment of inflammation |
| AU2005311451A1 (en) | 2004-12-01 | 2006-06-08 | Merck Serono Sa | [1,2,4]triazolo[4,3-a]pyridine derivatives for the treatment of hyperproliferative diseases |
| JP5238506B2 (ja) | 2005-10-06 | 2013-07-17 | エグゼリクシス， インコーポレイテッド | Ｐｉｍ−１および／またはｐｉｍ−３のピリドピリミジノンインヒビター |
| WO2007087250A2 (en) * | 2006-01-23 | 2007-08-02 | Amira Pharmaceuticals, Inc. | Tricyclic inhibitors of 5-lipoxygenase |
| TW200808802A (en) | 2006-06-06 | 2008-02-16 | Schering Corp | Imidazopyrazines as protein kinase inhibitors |
| WO2008022164A2 (en) * | 2006-08-16 | 2008-02-21 | Boehringer Ingelheim International Gmbh | Pyrazine compounds, their use and methods of preparation |
| CA2667487C (en) | 2006-11-06 | 2017-04-04 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| WO2008082839A2 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
| EP2139888A2 (en) * | 2007-03-28 | 2010-01-06 | Array Biopharma, Inc. | Imidazoý1,2-a¨pyridine compounds as receptor tyrosine kinase inhibitors |
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- 2009-08-18 JP JP2011523939A patent/JP5518072B2/ja not_active Expired - Fee Related
- 2009-08-18 UY UY0001032057A patent/UY32057A/es active IP Right Grant
- 2009-08-18 PT PT97916258T patent/PT2334677E/pt unknown
- 2009-08-18 DK DK09791625.8T patent/DK2334677T3/da active
- 2009-08-18 SI SI200930782T patent/SI2334677T1/sl unknown
- 2009-08-18 AR ARP090103170A patent/AR073079A1/es active IP Right Grant
- 2009-08-18 RS RS20130557A patent/RS53079B/en unknown
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- 2009-08-18 ES ES09791625.8T patent/ES2439501T3/es active Active
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| CN102186851A (zh) | 2011-09-14 |
| EP2334677B1 (en) | 2013-10-09 |
| JP2014129409A (ja) | 2014-07-10 |
| CA2734831A1 (en) | 2010-02-25 |
| DK2334677T3 (da) | 2013-11-18 |
| TWI496779B (zh) | 2015-08-21 |
| PT2334677E (pt) | 2013-11-26 |
| UY32057A (es) | 2011-01-31 |
| SMT201400154B (it) | 2015-01-15 |
| JP5518072B2 (ja) | 2014-06-11 |
| ES2439501T3 (es) | 2014-01-23 |
| SI2334677T1 (sl) | 2013-12-31 |
| PL2334677T3 (pl) | 2014-03-31 |
| HRP20131140T1 (hr) | 2014-01-03 |
| EP2334677A1 (en) | 2011-06-22 |
| JP2012500277A (ja) | 2012-01-05 |
| CA2734831C (en) | 2017-04-18 |
| US20110144085A1 (en) | 2011-06-16 |
| US8575145B2 (en) | 2013-11-05 |
| WO2010022076A1 (en) | 2010-02-25 |
| RS53079B (en) | 2014-06-30 |
| TW201008940A (en) | 2010-03-01 |
| CN102186851B (zh) | 2013-06-12 |
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