AR064010A1 - Inhibidores de la actividad de la akt - Google Patents
Inhibidores de la actividad de la aktInfo
- Publication number
- AR064010A1 AR064010A1 ARP070105281A ARP070105281A AR064010A1 AR 064010 A1 AR064010 A1 AR 064010A1 AR P070105281 A ARP070105281 A AR P070105281A AR P070105281 A ARP070105281 A AR P070105281A AR 064010 A1 AR064010 A1 AR 064010A1
- Authority
- AR
- Argentina
- Prior art keywords
- aob
- alkyl
- cycloalkyl
- heterocyclyl
- aryl
- Prior art date
Links
- 230000000694 effects Effects 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 abstract 1
- 108010029485 Protein Isoforms Proteins 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 150000005054 naphthyridines Chemical class 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
-
- 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
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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
- A61P17/06—Antipsoriatics
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- 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
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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
- A61P37/08—Antiallergic agents
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
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Abstract
La presente proporciona compuestos de naftiridina sustituidos que inhiben la actividad de la Akt. En particular, los compuestos descritos inhiben de manera selectiva una o dos de las isoformas de la Akt. También proporciona composiciones que comprenden tales compuestos inhibidores y procedimientos de inhibicion de la actividad de la Akt mediante la administracion del compuesto a un paciente en necesidad de tratamiento de cáncer. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en la que: a es 0 o 1; b es 0 o 1; m es 0, 1 o 2; p es 0, 1 o 2; R2 se selecciona independientemente entre alquilo C1-6, alcoxi C1-6, CO2H, halo, OH y NH2; el anillo Y es cicloalquilo C4-7; R1 se selecciona entre: H, oxo, (C=O)aOb-alquilo C1-10, (C=O)aOb-arilo, (C=O)aOb-alquenilo C2-10, (C=O)aOb-alquinilo C2-10, CO2H, halo, OH, Ob perfluoroalquilo C1-6, (C=O)aNR7R8, CN, (C=O)aOb cicloalquilo C3-8, S(O)mNR7R8, SH, S(O)m-alquilo C1-10 y (C=O)aOb-heterociclilo, dicho alquilo, arilo, alquenilo, alquinilo, cicloalquilo, y heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6 es; R6 es (C=O)aOb-alquilo C1-10, (C=O)aOb-arilo, alquenilo C2-10, alquinilo C2-10, (C=O)aOb-heterociclilo, CO2H, halo, OH, Ob perfluoroalquilo C1-6, Oa(C=O)bNR7R8, oxo, CHO, (N=O)R7R8, S(O)mNR7R8, SH, S(O)m-alquilo C1-10 o (C=O)aOb-cicloalquilo C3-8, dicho alquilo, arilo, alquenilo, alquinilo, heterociclilo, y cicloalquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a; R6a se selecciona entre (C=O)aOb alquilo C1-10, Oa perfluoroalquilo C1-3, alquileno C0-6, -S(O)mRa, SH, oxo, OH, halo, CN, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-6, alquileno C0-6-arilo, alquileno C0- 6-heterociclilo, alquilen C0-6-N(Rb)2, C(O)Ra, alquilen C0-6-CO2Ra, C(O)H, y alquilen C0-6-CO2H, dicho alquilo, alquenilo, alquinilo, cicloalquilo, arilo, y heterociclilo está opcionalmente sustituido con uno a tres sustituyentes seleccionados entre Rb, OH, alcoxi C1-6, halogeno, CO2H, CN, Oa(C=O)b alquilo C1-6, oxo, y N(Rb)2, R7 y R8 se seleccionan independientemente entre: H, (C=O)aOb alquilo C1-10, (C=O)aOb cicloalquilo C3-8, (C=O)aOb-arilo, (C=O)aOb-heterociclilo, alquenilo C2-10, alquinilo C2-10, SH, SO2Ra, y (C=O)aNRb2, dicho alquilo, cicloalquilo, arilo, heterociclilo, alquenilo, y alquinilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a, o R7 y R8 se pueden tomar juntos con el nitrogeno al que están unidos para formar a heterociclo monocíclico o bicíclico con 3-7 miembros en cada anillo conteniendo opcionalmente, además del nitrogeno, uno o dos heteroátomos adicionales seleccionados entre N, O y S, dicho heterociclo monocíclico o bicíclico opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a; Ra es alquilo C1-6, cicloalquilo C3-6, arilo, o heterociclilo; y Rb es independientemente: H, alquilo C1-6, arilo, heterociclilo, cicloalquilo C3-6, (C=O)aOb alquilo C1-6, o S(O)mRa; o una sal o estereoisomero farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87319806P | 2006-12-06 | 2006-12-06 | |
| US88066107P | 2007-01-16 | 2007-01-16 | |
| US96787207P | 2007-09-06 | 2007-09-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR064010A1 true AR064010A1 (es) | 2009-03-04 |
Family
ID=39492823
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070105281A AR064010A1 (es) | 2006-12-06 | 2007-11-28 | Inhibidores de la actividad de la akt |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US7576209B2 (es) |
| EP (1) | EP2104669B1 (es) |
| JP (2) | JP4431636B1 (es) |
| KR (1) | KR101110598B1 (es) |
| CN (1) | CN101600706B (es) |
| AR (1) | AR064010A1 (es) |
| AU (1) | AU2007328286B2 (es) |
| BR (1) | BRPI0719580A2 (es) |
| CA (1) | CA2670760C (es) |
| CL (1) | CL2007003495A1 (es) |
| CO (1) | CO6190528A2 (es) |
| CR (1) | CR10851A (es) |
| EA (1) | EA016195B1 (es) |
| EC (1) | ECSP099376A (es) |
| ES (1) | ES2527567T3 (es) |
| GE (1) | GEP20125469B (es) |
| GT (1) | GT200900146A (es) |
| HN (1) | HN2009001112A (es) |
| IL (2) | IL198826A (es) |
| MA (1) | MA31027B1 (es) |
| MX (1) | MX2009006052A (es) |
| NI (1) | NI200900106A (es) |
| NO (1) | NO20092569L (es) |
| NZ (2) | NZ577470A (es) |
| PE (1) | PE20081341A1 (es) |
| SV (1) | SV2009003283A (es) |
| TN (1) | TN2009000224A1 (es) |
| TW (1) | TWI386410B (es) |
| WO (2) | WO2008070041A2 (es) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006135627A2 (en) * | 2005-06-10 | 2006-12-21 | Merck & Co., Inc. | Inhibitors of akt activity |
| AR064010A1 (es) * | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| EP2120951A4 (en) * | 2006-12-06 | 2012-02-15 | Merck Sharp & Dohme | HAMMER OF ACT ACTIVITY |
| US20100048912A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| AU2009255329A1 (en) * | 2008-06-03 | 2009-12-10 | Msd K.K. | Inhibitors of Akt activity |
| WO2009148916A1 (en) * | 2008-06-03 | 2009-12-10 | Merck & Co., Inc. | Inhibitors of akt activity |
| WO2010002010A1 (en) | 2008-07-04 | 2010-01-07 | Banyu Pharmaceutical Co.,Ltd. | Novel spirochromanone carboxylic acids |
| CN102203067B (zh) | 2008-08-25 | 2014-01-15 | Irm责任有限公司 | Hedgehog通路调节剂 |
| DE102008043724A1 (de) * | 2008-11-13 | 2010-05-20 | Biotronik Vi Patent Ag | Erhöhung der Effizienz pharmazeutische Wirkstoffe-freisetzender Medizinprodukte durch Kombination mit einem Inhibitor des Transportproteins P-Glycoprotein |
| JP2012516847A (ja) * | 2009-02-02 | 2012-07-26 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性の阻害剤 |
| AU2010210422A1 (en) | 2009-02-05 | 2011-08-18 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal CYP17 inhibitors/antiandrogens |
| EP2403339B1 (en) * | 2009-03-06 | 2017-01-18 | Merck Sharp & Dohme Corp. | Combination cancer therapy with an akt inhibitor and other anticancer agents |
| WO2010104705A1 (en) | 2009-03-12 | 2010-09-16 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
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| EP1379251B1 (en) | 2001-04-10 | 2008-07-09 | Merck & Co., Inc. | Inhibitors of akt activity |
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| JP4451136B2 (ja) | 2002-04-08 | 2010-04-14 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性阻害薬 |
| JP4394959B2 (ja) | 2002-04-08 | 2010-01-06 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害剤 |
| EP1494676B1 (en) | 2002-04-08 | 2013-05-08 | Merck Sharp & Dohme Corp. | Fused quinoxaline derivatives as inhibitors of akt activity |
| CA2480800C (en) | 2002-04-08 | 2008-09-23 | Mark T. Bilodeau | Inhibitors of akt activity |
| EP1558586B1 (en) | 2002-10-30 | 2011-03-30 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| CN100422158C (zh) | 2003-04-24 | 2008-10-01 | 麦克公司 | Akt活性抑制剂 |
| CN1809351A (zh) * | 2003-04-24 | 2006-07-26 | 麦克公司 | Akt活性抑制剂 |
| EP1622616B1 (en) | 2003-04-24 | 2011-06-15 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| ATE446752T1 (de) | 2003-04-24 | 2009-11-15 | Merck & Co Inc | Hemmer der akt aktivität |
| WO2005007099A2 (en) | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| CA2542609C (en) * | 2003-10-15 | 2013-06-04 | Ube Industries, Ltd. | Novel indazole derivatives |
| JP2007008816A (ja) * | 2003-10-15 | 2007-01-18 | Ube Ind Ltd | 新規イソキノリン誘導体 |
| WO2005100356A1 (en) | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| DE602005026509D1 (de) | 2004-04-09 | 2011-04-07 | Merck Sharp & Dohme | Hemmer der akt aktivität |
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| CN101068811A (zh) * | 2004-12-02 | 2007-11-07 | 默克公司 | Akt活性抑制剂 |
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| WO2006135627A2 (en) | 2005-06-10 | 2006-12-21 | Merck & Co., Inc. | Inhibitors of akt activity |
| EP1978966A4 (en) * | 2006-01-23 | 2010-11-10 | Amira Pharmaceuticals Inc | TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE |
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| EP2137177B1 (en) * | 2007-04-05 | 2014-05-07 | Amgen, Inc | Aurora kinase modulators and method of use |
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