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
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
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 (26)
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) |
HK (1) | HK1139941A1 (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 |
---|---|---|---|---|
AU2005316668B2 (en) * | 2004-12-13 | 2012-09-06 | Millennium Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
EA016945B1 (ru) * | 2005-10-07 | 2012-08-30 | Экселиксис, Инк. | ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα |
GEP20115199B (en) * | 2005-10-07 | 2011-04-11 | Exelixis Inc | Phosphatidylinositol 3-kinase inhibitors and their use |
ATE539752T1 (de) | 2006-08-16 | 2012-01-15 | Exelixis Inc | Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung |
ES2366489T3 (es) | 2006-09-15 | 2011-10-20 | Pfizer Products Inc. | Compuesto de pirido (2,3-d) piridinona y sus uso como inhibidores de pi3. |
EA020022B1 (ru) | 2007-04-10 | 2014-08-29 | Экселиксис, Инк. | Способы лечения с применением пиридопиримидиноновых ингибиторов pi3k-альфа |
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 |
NZ600954A (en) * | 2009-12-22 | 2013-11-29 | Isoindolinone inhibitors of phosphatidylinositol 3-kinase | |
US8901137B2 (en) | 2010-02-09 | 2014-12-02 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K and mTOR in combination with autophagy inhibitors |
JP5792819B2 (ja) | 2010-09-14 | 2015-10-14 | エクセリクシス, インク. | Pi3k−デルタの阻害剤ならびにそれらの使用法および製造法 |
WO2013056067A1 (en) * | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
BR112014010492A2 (pt) | 2011-11-01 | 2017-04-25 | Exelixis Inc | n-(3-{[(3-{[2-cloro-5-(metóxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inibidor de fosfatidilinositol 3-cinase para o tratamento de malignidades linfoproliferativas |
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. |
EA016945B1 (ru) * | 2005-10-07 | 2012-08-30 | Экселиксис, Инк. | ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα |
CA2624965A1 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k.alpha. |
ATE539752T1 (de) * | 2006-08-16 | 2012-01-15 | Exelixis Inc | Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung |
ES2366489T3 (es) * | 2006-09-15 | 2011-10-20 | Pfizer Products Inc. | Compuesto de pirido (2,3-d) piridinona y sus uso como inhibidores de pi3. |
-
2008
- 2008-04-11 WO PCT/US2008/004807 patent/WO2008127712A1/en active Application Filing
- 2008-04-11 NZ NZ579945A patent/NZ579945A/en not_active IP Right Cessation
- 2008-04-11 EA EA200970936A patent/EA018964B1/ru not_active IP Right Cessation
- 2008-04-11 EP EP08742864.5A patent/EP2142544B8/en active Active
- 2008-04-11 MX MX2009010815A patent/MX2009010815A/es active IP Right Grant
- 2008-04-11 JP JP2010503085A patent/JP2010523681A/ja active Pending
- 2008-04-11 KR KR1020097023146A patent/KR20090130104A/ko not_active Application Discontinuation
- 2008-04-11 CA CA002683820A patent/CA2683820A1/en not_active Abandoned
- 2008-04-11 CN CN200880018758A patent/CN101711249A/zh active Pending
- 2008-04-11 UA UAA200911451A patent/UA101315C2/ru unknown
- 2008-04-11 ES ES08742864T patent/ES2425068T3/es active Active
- 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 US US12/595,233 patent/US20100209340A1/en not_active Abandoned
- 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 DO DO2009000242A patent/DOP2009000242A/es unknown
- 2009-10-09 SV SV2009003389A patent/SV2009003389A/es not_active Application Discontinuation
- 2009-10-09 NI NI200900183A patent/NI200900183A/es unknown
- 2009-10-30 MA MA32314A patent/MA31336B1/fr unknown
- 2009-11-09 CR CR11098A patent/CR11098A/es unknown
- 2009-11-09 CO CO09126919A patent/CO6241119A2/es not_active Application Discontinuation
- 2009-11-09 EC EC2009009722A patent/ECSP099722A/es unknown
-
2010
- 2010-07-07 HK HK10106576.7A patent/HK1139941A1/xx not_active IP Right Cessation
-
2013
- 2013-01-03 US US13/694,772 patent/US20130343988A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
NI200900183A (es) | 2010-10-05 |
SV2009003389A (es) | 2010-04-27 |
UA101315C2 (ru) | 2013-03-25 |
BRPI0810175A2 (pt) | 2014-12-30 |
CN101711249A (zh) | 2010-05-19 |
CR11098A (es) | 2010-01-27 |
CA2683820A1 (en) | 2008-10-23 |
US20100209340A1 (en) | 2010-08-19 |
AU2008239596B2 (en) | 2013-08-15 |
EP2142544B1 (en) | 2013-05-22 |
KR20090130104A (ko) | 2009-12-17 |
ES2425068T3 (es) | 2013-10-11 |
MA31336B1 (fr) | 2010-04-01 |
MY150747A (en) | 2014-02-28 |
TN2009000389A1 (en) | 2010-12-31 |
ECSP099722A (es) | 2009-12-28 |
EP2142544A1 (en) | 2010-01-13 |
ZA200906648B (en) | 2010-04-28 |
HK1139941A1 (en) | 2010-09-30 |
DOP2009000242A (es) | 2010-04-30 |
IL201209A0 (en) | 2010-05-31 |
US20130343988A1 (en) | 2013-12-26 |
EA018964B1 (ru) | 2013-12-30 |
WO2008127712A1 (en) | 2008-10-23 |
EA200970936A1 (ru) | 2010-02-26 |
EP2142544B8 (en) | 2013-07-03 |
MX2009010815A (es) | 2009-10-29 |
NZ579945A (en) | 2012-05-25 |
JP2010523681A (ja) | 2010-07-15 |
AU2008239596A1 (en) | 2008-10-23 |
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Legal Events
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