ES2579855T3 - Compuestos de imidazopiridinil-aminopiridina sustituidos - Google Patents
Compuestos de imidazopiridinil-aminopiridina sustituidos Download PDFInfo
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- ES2579855T3 ES2579855T3 ES12802947.7T ES12802947T ES2579855T3 ES 2579855 T3 ES2579855 T3 ES 2579855T3 ES 12802947 T ES12802947 T ES 12802947T ES 2579855 T3 ES2579855 T3 ES 2579855T3
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- substituted
- alkylaminocarbonyloxy
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- alkylamino
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (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
Un compuesto de fórmula I:**Fórmula** o una sal o éster farmacéuticamente aceptable del mismo, en la que: X es NRNRN', ORO, SRS o**Fórmula** en la que**Fórmula** está unido al anillo de imidazopiridinilo de fórmula I en la posición indicada por "**"; RO y RS son cada uno independientemente arilo C6-C10 sin sustituir o sustituido; RN es (CH2)mRhc o arilo C6-C10 sin sustituir o sustituido; RN' es H; o RN y RN', junto con el átomo de nitrógeno al que están unidos, forman una morfolina sin sustituir o sustituida; m es 1, 2, 3 o 4; Rhc es heterociclo sin sustituir o sustituido que comprende un anillo de 6 miembros y 1 o 2 heteroátomos seleccionados entre N, O y S; y Rph es alquilo C3-C6 sustituido o alquilo C4-C6 sin sustituir; en la que: dichos arilo sustituido y heterociclo sustituido están sustituidos en una o más posiciones del anillo con alquilo, alquenilo, alquinilo, halógeno, hidroxilo, alcoxi, alquilcarboniloxi, arilcarboniloxi, alcoxicarboniloxi, ariloxicarboniloxi, carboxilato, alquilcarbonilo, alquilaminocarbonilo, aralquilaminocarbonilo, alquenilaminocarbonilo, alquilcarbonilo, arilcarbonilo, aralquilcarbonilo, alquenilcarbonilo, alcoxicarbonilo, aminocarbonilo, alquiltiocarbonilo, fosfato, fosfonato, fosfinato, amino (incluyendo alquilamino, dialquilamino, arilamino, diarilamino y alquilarilamino), acilamino (incluyendo alquilcarbonilamino, arilcarbonilamino, carbamoílo y ureído), amidino, imino, sulfhidrilo, alquiltio, ariltio, tiocarboxilato, sulfatos, alquilsulfinilo, sulfonato, sulfamoílo, sulfonamido, nitro, trifluorometilo, ciano, azido, heterociclilo, alquilarilo o un resto aromático o heteroaromático; dicha morfolina sustituida está sustituida con uno o más grupos, cada uno de los cuales se selecciona independientemente entre hidroxilo, halógeno (incluyendo flúor, cloro, bromo y yodo), ciano, nitro, amino sin sustituir, alquilamino C1-C6, di-alquilamino C1-C6 sin sustituir o sustituido, alquilo C1-C6 sin sustituir o sustituido (incluyendo metilo, etilo, n-propilo, i-propilo, n-butilo, i-butilo, s-butilo, t-butilo, n-pentilo, s-pentilo y n-hexilo), y alcoxi C1-C6 sin sustituir o sustituido (incluyendo metoxi, etoxi, n-propiloxi, i-propiloxi, n-butoxi y t-butoxi); dicho alcoxi sustituido está sustituido con alquenilo, alquinilo, halógeno, hidroxilo, alquilcarboniloxi, arilcarboniloxi, alcoxicarboniloxi, ariloxicarboniloxi, carboxilato, alquilcarbonilo, arilcarbonilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, alquiltiocarbonilo, alcoxilo, fosfato, fosfonato, fosfinato, amino (incluyendo alquilamino, dialquilamino, arilamino, diarilamino y alquilarilamino), acilamino (incluyendo alquilcarbonilamino, arilcarbonilamino, carbamoílo y ureído), amidino, imino, sulfhidrilo, alquiltio, ariltio, tiocarboxilato, sulfatos, alquilsulfinilo, sulfonato, sulfamoílo, sulfonamido, nitro, trifluorometilo, ciano, azido, heterociclilo, alquilarilo, o un resto aromático o heteroaromático; y dicho alquilo sustituido, alquilamino sustituido o dialquilamino sustituido tienen sustituyentes que reemplazan uno o más átomos de hidrógeno en uno o más carbonos de la cadena principal de hidrocarburo, en la que los sustituyentes son alquilo, alquenilo, alquinilo, halógeno, hidroxilo, alquilcarboniloxi, arilcarboniloxi, alcoxicarboniloxi, ariloxicarboniloxi, carboxilato, alquilcarbonilo, arilcarbonilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, alquiltiocarbonilo, alcoxilo, fosfato, fosfonato, fosfinato, amino (incluyendo alquilamino, dialquilamino, arilamino, diarilamino y alquilarilamino), acilamino (incluyendo alquilcarbonilamino, arilcarbonilamino, carbamoílo y ureído), amidino, imino, sulfhidrilo, alquiltio, ariltio, tiocarboxilato, sulfatos, alquilsulfinilo, sulfonato, sulfamoílo, sulfonamido, nitro, trifluorometilo, ciano, azido, heterociclilo, alquilarilo, o un resto aromático o heteroaromático.
Description
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17
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Tabla 2
- Comp.
- Kd de Desplazamiento Térmico (nM) Elisa Celular (nM) GI50 (µM) CI50 del ensayo bioquímico de Akt1 AlphaScreen crosstide (µM)
- 1
- N.D. 235 N.T.
- 3
- 7 29 444 0,00309
- 4
- 0,4 17 265 0,0017
- 5
- 0,7 0,00446
- 6
- 1,4 0,00163
- 7
- 7,1 12 836 0,00245
- 8
- 1,2 8 1348 0,0015
- 9
- 0,2 2,1 0,00251
- 10
- 0,2 3,0 0,00415
- 11
- 0,2 1,7 0,00336
- 12
- 0,2 0,00144
- 13
- 1,4 9 335 0,00215
- 14
- 1,1 11 296 0,00184
- 15
- 1,1 4,0
- 16
- 1,7 0,00342
- 17
- 3,1 0,00436
- 18
- 0,8 0,00179
- 19
- N.D. 60 1423 0,00377
- 20
- 57,3 414 N.T. 0,00872
- 21
- 109,5 605
- 22
- 83,1
118
Claims (1)
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imagen1 imagen2 imagen3 imagen4 imagen5 imagen6 imagen7 imagen8
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161500889P | 2011-06-24 | 2011-06-24 | |
| US201161500889P | 2011-06-24 | ||
| PCT/US2012/043501 WO2012177844A2 (en) | 2011-06-24 | 2012-06-21 | Substituted imidazopyridinyl-aminopyridine compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2579855T3 true ES2579855T3 (es) | 2016-08-17 |
Family
ID=47362419
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12802947.7T Active ES2579855T3 (es) | 2011-06-24 | 2012-06-21 | Compuestos de imidazopiridinil-aminopiridina sustituidos |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US8609688B2 (es) |
| EP (1) | EP2723741B8 (es) |
| JP (1) | JP6046710B2 (es) |
| KR (2) | KR101974673B1 (es) |
| CN (1) | CN103748093B (es) |
| AU (2) | AU2012272937B2 (es) |
| BR (1) | BR112013033182A2 (es) |
| CA (1) | CA2837727C (es) |
| DK (1) | DK2723741T3 (es) |
| ES (1) | ES2579855T3 (es) |
| HK (1) | HK1196371A1 (es) |
| IL (3) | IL229719A0 (es) |
| MX (1) | MX339862B (es) |
| PH (1) | PH12013502565B1 (es) |
| TW (1) | TWI561522B (es) |
| WO (1) | WO2012177844A2 (es) |
| ZA (1) | ZA201308929B (es) |
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| CN100398540C (zh) | 2006-04-03 | 2008-07-02 | 大连理工大学 | 芳杂环基咪唑并萘酰亚胺类化合物及其应用 |
| MY157033A (en) | 2006-07-11 | 2016-04-15 | Dae Woong Pharma | Novel biaryl benzoimidazole derivatives and pharmaceutical composition comprising the same |
| AR064010A1 (es) * | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| CA2679809A1 (en) | 2007-03-02 | 2008-09-12 | Schering Corporation | Benzimidazole derivatives and methods of use thereof |
| WO2009000413A1 (en) | 2007-06-26 | 2008-12-31 | Sanofi-Aventis | A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles |
| TW200932872A (en) | 2007-10-17 | 2009-08-01 | Cheil Ind Inc | Novel compound for organic photoelectric device and organic photoelectric device including the same |
| KR20090007347U (ko) | 2008-01-16 | 2009-07-21 | 춘-치 왕 | 가속 페달 포지션 센서를 구비한 자동차용 연료 공급 기구 |
| US8501770B2 (en) * | 2009-12-30 | 2013-08-06 | Arqule, Inc. | Substituted imidazopyridinyl-aminopyridine compounds |
| KR101974673B1 (ko) * | 2011-06-24 | 2019-05-02 | 아르퀼 인코포레이티드 | 치환된 이미다조피리디닐-아미노피리딘 화합물 |
| WO2012177852A1 (en) | 2011-06-24 | 2012-12-27 | Arqule, Inc | Substituted imidazopyridinyl compounds |
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