AR086318A1 - Piridil aminopiridinas como inhibidores de syk - Google Patents
Piridil aminopiridinas como inhibidores de sykInfo
- Publication number
- AR086318A1 AR086318A1 ARP120101625A ARP120101625A AR086318A1 AR 086318 A1 AR086318 A1 AR 086318A1 AR P120101625 A ARP120101625 A AR P120101625A AR P120101625 A ARP120101625 A AR P120101625A AR 086318 A1 AR086318 A1 AR 086318A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- cycloalkyl
- independently selected
- haloalkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- WGNUNYPERJMVRM-UHFFFAOYSA-N 3-pyridylacetic acid Chemical compound OC(=O)CC1=CC=CN=C1 WGNUNYPERJMVRM-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000000551 Syk Kinase Human genes 0.000 abstract 1
- 108010016672 Syk Kinase Proteins 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Son fuertes inhibidores de la tirosina quinasa de bazo y son útiles en el tratamiento y prevención de enfermedades tales como asma, EPOC y artritis reumatoide y cáncer, mediadas por dicha enzima. Composición farmacéutica.Reivindicación 1: Un compuesto que tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que A es un carbociclo, o el resto A-(R7)n(R8) representa un compuesto de formula (2), (3) ó (4); n es 0, 1, 2 ó 3; p y q se seleccionan independientemente entre 1, 2 y 3; R1 es alquilo C1-4, fluoroalquilo C1-4, cicloalquilo C3-6 o alcoxi C1-4; R2 es H o halógeno; R3 es H, halógeno, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-6 o hidroxialquilo C1-4; R4 es H o halógeno; R5 es OH, alcoxi C1-4, halógeno o NH2; o N(H)(alquilo C1-4); R6 es H, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-6 o hidroxialquilo C1-4; o R7 se selecciona entre OH y alquilo C1-4; R8 se selecciona entre (CRaRb)nCO2Rc, CONRdRe, tetrazolilo, OH, CH2OH, oxo, CN, NHCO2Rf y NHSO2Rf; con la condición de que R8 y -C(R5)(R6)- no estén unidos al mismo átomo de carbono del anillo; cada uno de Ra y Rb se selecciona independientemente entre H y metilo; Rc es H o alquilo C1-4, Rd y Re se seleccionan cada uno independientemente entre H y alquilo C1-4; y Rf es alquilo C1-4 o bencilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161484431P | 2011-05-10 | 2011-05-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086318A1 true AR086318A1 (es) | 2013-12-04 |
Family
ID=47139532
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101625A AR086318A1 (es) | 2011-05-10 | 2012-05-09 | Piridil aminopiridinas como inhibidores de syk |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9120785B2 (es) |
| EP (1) | EP2707357B1 (es) |
| JP (1) | JP2014513687A (es) |
| AR (1) | AR086318A1 (es) |
| AU (1) | AU2012253886A1 (es) |
| CA (1) | CA2834062A1 (es) |
| TW (1) | TW201249839A (es) |
| WO (1) | WO2012154520A1 (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112013010552A2 (pt) * | 2010-10-28 | 2016-08-02 | Nippon Shinyaku Co Ltd | derivado de piridina e agente medicinal |
| BR112013028430A2 (pt) | 2011-05-04 | 2017-08-01 | Merck Sharp & Dohme | composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto |
| EP2706852B1 (en) | 2011-05-10 | 2018-08-22 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as syk inhibitors |
| JP2014513686A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｓｙｋ阻害薬としてのアミノピリミジン |
| CA2871695A1 (en) * | 2012-05-22 | 2013-11-28 | F. Hoffmann-La Roche Ag | Substituted dipyridylamines and uses thereof |
| WO2013192125A1 (en) | 2012-06-20 | 2013-12-27 | Merck Sharp & Dohme Corp. | Pyrazolyl derivatives as syk inhibitors |
| WO2013192128A1 (en) | 2012-06-20 | 2013-12-27 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
| WO2013192088A1 (en) | 2012-06-22 | 2013-12-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| US9376418B2 (en) | 2012-06-22 | 2016-06-28 | Merck Sharp & Dohme Corp. | Substituted pyridine spleen tyrosine kinase (SYK) inhibitors |
| WO2014031438A2 (en) | 2012-08-20 | 2014-02-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2900665B1 (en) | 2012-09-28 | 2018-01-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| EP2931281B1 (en) | 2012-12-12 | 2018-01-17 | Merck Sharp & Dohme Corp. | Amino-pyrimidine-containing spleen tyrosine kinase inhibitors |
| WO2014100314A1 (en) * | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors |
| EP2988744A4 (en) | 2013-04-26 | 2016-11-02 | Merck Sharp & Dohme | THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR |
| WO2014176216A1 (en) | 2013-04-26 | 2014-10-30 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors |
| KR20160002850A (ko) | 2013-05-01 | 2016-01-08 | 에프. 호프만-라 로슈 아게 | C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도 |
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| US9783531B2 (en) | 2013-12-20 | 2017-10-10 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| US9670196B2 (en) | 2013-12-20 | 2017-06-06 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors |
| WO2015138273A1 (en) | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
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| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| NZ593460A (en) | 2008-12-08 | 2013-11-29 | Gilead Connecticut Inc | Imidazopyrazine syk inhibitors |
| TWI529172B (zh) | 2008-12-08 | 2016-04-11 | 吉李德康乃狄克公司 | 作爲脾臟酪胺酸激酶（Ｓｙｋ）抑制劑之咪唑並吡化合物 |
| WO2011075560A1 (en) | 2009-12-17 | 2011-06-23 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| PE20121480A1 (es) | 2009-12-17 | 2012-11-10 | Merck Sharp & Dohme | Aminopirimidinas como inhibidores de syk |
| JP5734313B2 (ja) | 2010-01-12 | 2015-06-17 | アーべー・シオンス | チアゾールおよびオキサゾールキナーゼ阻害剤 |
| EP2441755A1 (en) | 2010-09-30 | 2012-04-18 | Almirall, S.A. | Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors |
| BR112013010552A2 (pt) | 2010-10-28 | 2016-08-02 | Nippon Shinyaku Co Ltd | derivado de piridina e agente medicinal |
| BR112013028430A2 (pt) | 2011-05-04 | 2017-08-01 | Merck Sharp & Dohme | composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto |
| EP2706852B1 (en) | 2011-05-10 | 2018-08-22 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as syk inhibitors |
| JP2014513686A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｓｙｋ阻害薬としてのアミノピリミジン |
-
2012
- 2012-05-04 WO PCT/US2012/036426 patent/WO2012154520A1/en not_active Ceased
- 2012-05-04 JP JP2014510372A patent/JP2014513687A/ja active Pending
- 2012-05-04 US US14/116,205 patent/US9120785B2/en active Active
- 2012-05-04 EP EP12782164.3A patent/EP2707357B1/en active Active
- 2012-05-04 CA CA2834062A patent/CA2834062A1/en not_active Abandoned
- 2012-05-04 AU AU2012253886A patent/AU2012253886A1/en not_active Abandoned
- 2012-05-09 AR ARP120101625A patent/AR086318A1/es not_active Application Discontinuation
- 2012-05-09 TW TW101116552A patent/TW201249839A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2012253886A1 (en) | 2013-10-31 |
| US20140100250A1 (en) | 2014-04-10 |
| JP2014513687A (ja) | 2014-06-05 |
| TW201249839A (en) | 2012-12-16 |
| EP2707357A4 (en) | 2014-12-03 |
| US9120785B2 (en) | 2015-09-01 |
| CA2834062A1 (en) | 2012-11-15 |
| EP2707357B1 (en) | 2017-01-18 |
| WO2012154520A1 (en) | 2012-11-15 |
| EP2707357A1 (en) | 2014-03-19 |
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