CO6241119A2 - Compuestos de pirido 2,3-d pirimidina-7-ona como inhibidores de pi3k-alfa para el tratamiento del cancer - Google Patents
Compuestos de pirido 2,3-d pirimidina-7-ona como inhibidores de pi3k-alfa para el tratamiento del cancerInfo
- Publication number
- CO6241119A2 CO6241119A2 CO09126919A CO09126919A CO6241119A2 CO 6241119 A2 CO6241119 A2 CO 6241119A2 CO 09126919 A CO09126919 A CO 09126919A CO 09126919 A CO09126919 A CO 09126919A CO 6241119 A2 CO6241119 A2 CO 6241119A2
- Authority
- CO
- Colombia
- Prior art keywords
- optionally
- heterocycloalkyl
- optionally substituted
- additionally
- alkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 206010028980 Neoplasm Diseases 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 150000004677 hydrates Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 239000012453 solvate Substances 0.000 abstract 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- -1 cyano, amino Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/025—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus inorganic Tc complexes or compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
- A61N5/1001—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy
-
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pathology (AREA)
- Immunology (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Radiology & Medical Imaging (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Inorganic Chemistry (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
1.- Un compuesto de la fórmula Io uno de sus isómeros individuales, opcionalmente como una sal farmacéuticamente aceptable, de modo adicional opcionalmente como un solvato y de modo adicional opcionalmente como uno de sus hidratos, donde R1 es heterocicloalquilo de 5 ó 6 miembros opcionalmente sustituido; R2 es hidrógeno o alquilo; R4 es alquilo opcionalmente sustituido; R6 es heteroarilo de 5 ó 6 miembros opcionalmente sustituido con 1, 2, 3, 4 ó 5 grupos R9; cada R9, cuando está presente, es, de modo independiente, halo, alquilo, haloalquilo, alcoxi, haloalcoxi, ciano, amino, alquilamino, dialquilamino, alcoxialquilo, carboxialquilo, alcoxicarbonilo, aminoalquilo, cicloalquilo, arilo, arilalquilo, ariloxi, heterocicloalquilo o heteroarilo y cuando el cicloalquilo, arilo, heterocicloalquilo y heteroarilo, cada uno solo o como parte de otro grupo dentro de R9, están opcionalmente sustituidos, de modo independiente, con 1, 2, 3 ó 4 grupos seleccionados de halo, alquilo, haloalquilo, hidroxi, alcoxi, haloalcoxi, amino, alquilamino y dialquilamino. 2.- El compuesto de acuerdo con la reivindicación 1 o uno de sus isómeros individuales, en donde R1 es un heterocicloalquilo de 5 ó 6 miembros opcionalmente sustituido, donde el heterocicloalquilo comprende un heteroátomo y el heteroátomo es -O-; donde el compuesto es opcionalmente como una sal farmacéuticamente aceptable, de modo adicional opcionalmente como un solvato y de modo adicional opcionalmente como uno de sus hidratos. 3.- El compuesto de acuerdo con la reivindicación 1 ó 2 o uno de sus isómeros individuales, donde R6 es un heteroarilo de 5 miembros opcionalmente sustituido con 1, 2 ó 3 grupos R9; donde el compuesto es opcionalmente como una sal farmacéuticamente aceptable, de modo adicional opcionalmente como un solvato y de modo adicional opcionalmente como uno de sus hidratos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91116007P | 2007-04-11 | 2007-04-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6241119A2 true CO6241119A2 (es) | 2011-01-20 |
Family
ID=39642739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO09126919A CO6241119A2 (es) | 2007-04-11 | 2009-11-09 | Compuestos de pirido 2,3-d pirimidina-7-ona como inhibidores de pi3k-alfa para el tratamiento del cancer |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20100209340A1 (es) |
| EP (1) | EP2142544B8 (es) |
| JP (1) | JP2010523681A (es) |
| KR (1) | KR20090130104A (es) |
| CN (1) | CN101711249A (es) |
| AU (1) | AU2008239596B2 (es) |
| BR (1) | BRPI0810175A2 (es) |
| CA (1) | CA2683820A1 (es) |
| CO (1) | CO6241119A2 (es) |
| CR (1) | CR11098A (es) |
| DO (1) | DOP2009000242A (es) |
| EA (1) | EA018964B1 (es) |
| EC (1) | ECSP099722A (es) |
| ES (1) | ES2425068T3 (es) |
| IL (1) | IL201209A0 (es) |
| MA (1) | MA31336B1 (es) |
| MX (1) | MX2009010815A (es) |
| MY (1) | MY150747A (es) |
| NI (1) | NI200900183A (es) |
| NZ (1) | NZ579945A (es) |
| SV (1) | SV2009003389A (es) |
| TN (1) | TN2009000389A1 (es) |
| UA (1) | UA101315C2 (es) |
| WO (1) | WO2008127712A1 (es) |
| ZA (1) | ZA200906648B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2590294A1 (en) * | 2004-12-13 | 2006-06-22 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| UA116188C2 (uk) * | 2005-10-07 | 2018-02-26 | Екселіксіс, Інк. | Інгібітори фосфатидилінозит-3-кінази і способи їх застосування |
| US8044062B2 (en) * | 2005-10-07 | 2011-10-25 | Exelixis, Inc. | Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha |
| CA2658725A1 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| BRPI0716749B8 (pt) | 2006-09-15 | 2021-05-25 | Pfizer Prod Inc | compostos pirido (2,3-d) pirimidinona, seu uso como inibidores pi3 e composição farmacêutica que os compreende |
| WO2008124161A1 (en) | 2007-04-10 | 2008-10-16 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha |
| AU2008239655B2 (en) * | 2007-04-11 | 2013-06-20 | Exelixis, Inc. | Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer |
| UY32153A (es) * | 2008-09-30 | 2011-04-29 | Exelixis Inc | Inhibidores de piridomidinona de pi13ka(alfa) y mtor |
| SG10201502073PA (en) * | 2009-12-22 | 2015-05-28 | Vertex Pharma | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| CA2812089C (en) | 2010-09-14 | 2020-02-18 | Exelixis Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| WO2013056067A1 (en) * | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| WO2013067141A1 (en) | 2011-11-01 | 2013-05-10 | Exelixis, Inc. | N- (3- { [ (3- { [2-chloro-5- (methoxy) phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3 - kinase inhibitor for the treatment of lymphoproliferative malignancies |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2937284A (en) * | 1958-05-01 | 1960-05-17 | Burroughs Wellcome Co | 2, 4-diamino-5, 6-dialkylpyrido (2, 3-d) pyrimidines and method |
| IL117923A (en) * | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| US7019002B2 (en) * | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| ES2292130T3 (es) * | 2004-05-04 | 2008-03-01 | Warner-Lambert Company Llc | Pirido(2,3-d)pirimidin-7-onas pirrolil-sustituidas y derivados de las mismas como agentes terapeuticos. |
| US8044062B2 (en) * | 2005-10-07 | 2011-10-25 | Exelixis, Inc. | Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha |
| JP5480503B2 (ja) * | 2005-10-07 | 2014-04-23 | エクセリクシス， インク． | ＰＩ３Ｋαのピリドピリミジノン型阻害剤 |
| CA2658725A1 (en) * | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| BRPI0716749B8 (pt) * | 2006-09-15 | 2021-05-25 | Pfizer Prod Inc | compostos pirido (2,3-d) pirimidinona, seu uso como inibidores pi3 e composição farmacêutica que os compreende |
-
2008
- 2008-04-11 AU AU2008239596A patent/AU2008239596B2/en not_active Ceased
- 2008-04-11 BR BRPI0810175-2A2A patent/BRPI0810175A2/pt not_active IP Right Cessation
- 2008-04-11 CA CA002683820A patent/CA2683820A1/en not_active Abandoned
- 2008-04-11 JP JP2010503085A patent/JP2010523681A/ja active Pending
- 2008-04-11 US US12/595,233 patent/US20100209340A1/en not_active Abandoned
- 2008-04-11 EA EA200970936A patent/EA018964B1/ru not_active IP Right Cessation
- 2008-04-11 KR KR1020097023146A patent/KR20090130104A/ko not_active Ceased
- 2008-04-11 CN CN200880018758A patent/CN101711249A/zh active Pending
- 2008-04-11 MX MX2009010815A patent/MX2009010815A/es active IP Right Grant
- 2008-04-11 NZ NZ579945A patent/NZ579945A/en not_active IP Right Cessation
- 2008-04-11 EP EP08742864.5A patent/EP2142544B8/en active Active
- 2008-04-11 ES ES08742864T patent/ES2425068T3/es active Active
- 2008-04-11 UA UAA200911451A patent/UA101315C2/ru unknown
- 2008-04-11 WO PCT/US2008/004807 patent/WO2008127712A1/en not_active Ceased
- 2008-04-11 MY MYPI20094194 patent/MY150747A/en unknown
-
2009
- 2009-09-23 ZA ZA200906648A patent/ZA200906648B/xx unknown
- 2009-09-24 TN TNP2009000389A patent/TN2009000389A1/fr unknown
- 2009-09-29 IL IL201209A patent/IL201209A0/en unknown
- 2009-10-09 SV SV2009003389A patent/SV2009003389A/es not_active Application Discontinuation
- 2009-10-09 DO DO2009000242A patent/DOP2009000242A/es unknown
- 2009-10-09 NI NI200900183A patent/NI200900183A/es unknown
- 2009-10-30 MA MA32314A patent/MA31336B1/fr unknown
- 2009-11-09 EC EC2009009722A patent/ECSP099722A/es unknown
- 2009-11-09 CO CO09126919A patent/CO6241119A2/es not_active Application Discontinuation
- 2009-11-09 CR CR11098A patent/CR11098A/es unknown
-
2013
- 2013-01-03 US US13/694,772 patent/US20130343988A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MA31336B1 (fr) | 2010-04-01 |
| IL201209A0 (en) | 2010-05-31 |
| NZ579945A (en) | 2012-05-25 |
| EP2142544B1 (en) | 2013-05-22 |
| CA2683820A1 (en) | 2008-10-23 |
| JP2010523681A (ja) | 2010-07-15 |
| WO2008127712A1 (en) | 2008-10-23 |
| AU2008239596B2 (en) | 2013-08-15 |
| NI200900183A (es) | 2010-10-05 |
| AU2008239596A1 (en) | 2008-10-23 |
| US20100209340A1 (en) | 2010-08-19 |
| ECSP099722A (es) | 2009-12-28 |
| HK1139941A1 (en) | 2010-09-30 |
| MX2009010815A (es) | 2009-10-29 |
| EP2142544B8 (en) | 2013-07-03 |
| SV2009003389A (es) | 2010-04-27 |
| ES2425068T3 (es) | 2013-10-11 |
| MY150747A (en) | 2014-02-28 |
| ZA200906648B (en) | 2010-04-28 |
| EA018964B1 (ru) | 2013-12-30 |
| EP2142544A1 (en) | 2010-01-13 |
| KR20090130104A (ko) | 2009-12-17 |
| EA200970936A1 (ru) | 2010-02-26 |
| CN101711249A (zh) | 2010-05-19 |
| TN2009000389A1 (en) | 2010-12-31 |
| US20130343988A1 (en) | 2013-12-26 |
| UA101315C2 (ru) | 2013-03-25 |
| BRPI0810175A2 (pt) | 2014-12-30 |
| DOP2009000242A (es) | 2010-04-30 |
| CR11098A (es) | 2010-01-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |