CO6251254A2 - Uso de inhibidores de piridopirimidinona de pi3k en el tratamiento del cancer - Google Patents
Uso de inhibidores de piridopirimidinona de pi3k en el tratamiento del cancerInfo
- Publication number
- CO6251254A2 CO6251254A2 CO09126924A CO09126924A CO6251254A2 CO 6251254 A2 CO6251254 A2 CO 6251254A2 CO 09126924 A CO09126924 A CO 09126924A CO 09126924 A CO09126924 A CO 09126924A CO 6251254 A2 CO6251254 A2 CO 6251254A2
- Authority
- CO
- Colombia
- Prior art keywords
- optionally substituted
- alkyl
- heteroaryl
- optionally
- heterocycloalkyl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003282 alkyl amino group Chemical group 0.000 abstract 3
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl 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
- 239000003814 drug Substances 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000002252 acyl 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
- 239000002246 antineoplastic agent Substances 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
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 229940127089 cytotoxic agent Drugs 0.000 abstract 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 238000001794 hormone therapy Methods 0.000 abstract 1
- 238000009169 immunotherapy Methods 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 229940036571 iodine therapy Drugs 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
- 230000002285 radioactive effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/28—Compounds containing heavy metals
- A61K31/282—Platinum compounds
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- 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
- 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
- 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
Abstract
1.- Uso de un compuesto de Fórmula I:o un isómero simple de este donde el compuesto está opcionalmente como una sal farmacéuticamente aceptable y en forma adicional opcionalmente como un hidrato y en forma adicional opcionalmente como un solvato de este, para la fabricación de un medicamento caracterizado porque dicho medicamento es para el tratamiento del cáncer y contiene el compuesto de Fórmula I y al menos uno de un portador, excipiente o diluyente farmacéuticamente aceptable en combinación con uno o más agentes quimioterapéuticos, una o más de las terapias hormonales, uno o más anticuerpos, una o más inmunoterapias, terapia de iodo radiactivo, y radiación donde el Compuesto de Fórmula I es aquel donde: R1 es hidrógeno, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, arilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heteroarilalquilo opcionalmente sustituido; R2 es hidrógeno o alquilo donde el alquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 grupos R8;X es -NR3-: R3 es hidrógeno; R4 es alquilo opcionalmente sustituido; R5 es hidrógeno; y R6 es fenilo, acilo, o heteroarilo donde el fenilo y heteroarilo están opcionalmente sustituidos con 1, 2, 3, 4, o 5 grupos cada R9;cada R8, cuando está presente, es de modo independiente hidroxi, halo, alcoxi, haloalcoxi, amino, alquilamino, dialquilaminoalquilo, o alcoxialquilamino; y 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 donde el cicloalquilo, arilo, heterocicloalquilo, y heteroarilo, cada uno solo o como parte de otro grupo de R9, están opcionalmente sustituidos de modo independiente con 1, 2, 3, o 4 grupos seleccionados de halo, alquilo, haloalquilo, hidroxi, alcoxi, haloalcoxi, amino, alquilamino, y dialquilamino.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US92289907P | 2007-04-10 | 2007-04-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6251254A2 true CO6251254A2 (es) | 2011-02-21 |
Family
ID=39627802
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO09126924A CO6251254A2 (es) | 2007-04-10 | 2009-11-09 | Uso de inhibidores de piridopirimidinona de pi3k en el tratamiento del cancer |
Country Status (32)
Country | Link |
---|---|
US (1) | US8513266B2 (es) |
EP (1) | EP2139484B9 (es) |
JP (3) | JP2010523670A (es) |
KR (1) | KR101626435B1 (es) |
CN (2) | CN101715345A (es) |
AU (1) | AU2008236562B2 (es) |
BR (1) | BRPI0810206A2 (es) |
CA (1) | CA2683641C (es) |
CO (1) | CO6251254A2 (es) |
CR (1) | CR11100A (es) |
DK (1) | DK2139484T3 (es) |
DO (1) | DOP2009000243A (es) |
EA (1) | EA020022B1 (es) |
EC (1) | ECSP099724A (es) |
ES (1) | ES2430614T3 (es) |
HK (1) | HK1139863A1 (es) |
HN (1) | HN2009003002A (es) |
HR (1) | HRP20130688T1 (es) |
IL (1) | IL201284A (es) |
MA (1) | MA31358B1 (es) |
ME (1) | ME00936B (es) |
MX (1) | MX2009010930A (es) |
MY (1) | MY150697A (es) |
NZ (1) | NZ580110A (es) |
PL (1) | PL2139484T3 (es) |
PT (1) | PT2139484E (es) |
RS (1) | RS52939B (es) |
SI (1) | SI2139484T1 (es) |
TN (1) | TN2009000400A1 (es) |
UA (1) | UA100979C2 (es) |
WO (1) | WO2008124161A1 (es) |
ZA (1) | ZA200906764B (es) |
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TW200726767A (en) * | 2005-07-04 | 2007-07-16 | Astrazeneca Ab | Chemical compounds 2 |
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CA2623768C (en) * | 2005-10-07 | 2016-04-12 | Exelixis, Inc. | N-(3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
WO2008021389A2 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
US8188113B2 (en) * | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
SA08280783B1 (ar) * | 2007-01-11 | 2011-04-24 | استرازينيكا ايه بي | مشتقات بيريدوبيريميدين كمثبطات pde4 |
SI2139484T1 (sl) | 2007-04-10 | 2013-10-30 | Exelixis, Inc. | Postopki za zdravljenje raka s pirido pirimidin PI3K alfa inhibitorji |
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WO2010022125A1 (en) | 2008-08-20 | 2010-02-25 | Schering Corporation | Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
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EP2326626B1 (en) * | 2008-08-20 | 2013-10-16 | Merck Sharp & Dohme Corp. | Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
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TW201306842A (zh) * | 2011-06-15 | 2013-02-16 | Exelixis Inc | 使用pi3k/mtor吡啶並嘧啶酮抑制劑及苯達莫司汀及/或利妥昔單抗治療惡性血液疾病之組合療法 |
CN104010494B (zh) * | 2011-07-28 | 2017-07-04 | 霍夫曼-拉罗奇有限公司 | Pik3ca h1047r敲入非人动物乳腺癌模型 |
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US20140303172A1 (en) | 2011-11-01 | 2014-10-09 | Exelixis, Inc. | Phosphatidylinositol 3-Kinase Inhibitors for the Treatment of Lymphoproliferative Malignancies |
EP2776837A4 (en) * | 2011-11-11 | 2015-05-20 | Intellikine Llc | COMBINATION OF KINASEINHIBITORS AND THEIR USE |
EP2797628A4 (en) | 2011-12-27 | 2015-07-29 | Kadmon Corp Llc | METHODS OF TREATING BREAST CANCER NOT RESPONDING TO TRASTUZUMAB |
US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
CN104797267A (zh) | 2012-06-26 | 2015-07-22 | 德玛医药 | 使用卫康醇、二乙酰二脱水卫矛醇、二溴卫矛醇或类似物或其衍生物治疗具有基因多型性或ahi1失调或突变患者的抗酪氨酸激酶抑制剂的恶性肿瘤的方法 |
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PT2882440T (pt) | 2012-08-07 | 2019-04-23 | Array Biopharma Inc | Combinações farmacêuticas compreendendo um inibidor de braf, um inibidor de egfr e opcionalmente um inibidor de pi3k-alfa |
CN105492011A (zh) | 2013-04-08 | 2016-04-13 | 丹尼斯·M·布朗 | 不理想给药化学化合物的治疗增效 |
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US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
GEP20217234B (en) * | 2016-08-15 | 2021-03-25 | Pfizer | Pyridopyrimdinone cdk2/4/6 inhibitors |
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CA3094431C (en) | 2018-03-19 | 2023-06-27 | Taiho Pharmaceutical Co., Ltd. | Pharmaceutical composition including sodium alkyl sulfate |
MX2022001863A (es) | 2019-08-12 | 2022-05-30 | Deciphera Pharmaceuticals Llc | Metodos para tratar los tumores del estroma gastrointestinal. |
TW202122082A (zh) | 2019-08-12 | 2021-06-16 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
WO2021119242A1 (en) * | 2019-12-10 | 2021-06-17 | The Trustees Of Indiana University | Replication protein a (rpa)-dna interaction inhibitors |
IL293864A (en) | 2019-12-30 | 2022-08-01 | Deciphera Pharmaceuticals Llc | Preparations of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3- phenylurea |
LT4084778T (lt) | 2019-12-30 | 2024-01-25 | Deciphera Pharmaceuticals, Llc | Amorfinės kinazės inhibitoriaus vaistinės formos ir jų panaudojimo būdai |
KR102195221B1 (ko) | 2019-12-31 | 2020-12-24 | 서울대학교산학협력단 | 포스파티딜이노시톨 3-키나아제 억제제 및 프로그램화 세포 사멸 단백질 1 억제제를 포함하는, 삼중음성 유방암의 방사선 병용 치료용 약학적 조성물 |
CN111358952B (zh) * | 2020-04-15 | 2022-03-15 | 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) | 一种抗肿瘤药物组合物及其制剂和应用 |
WO2023092104A1 (en) * | 2021-11-18 | 2023-05-25 | Onconova Therapeutics, Inc. | Methods and compositions for treating cancer |
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NZ594628A (en) | 2005-10-07 | 2013-04-26 | Exelixis Inc | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka |
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SI2139484T1 (sl) | 2007-04-10 | 2013-10-30 | Exelixis, Inc. | Postopki za zdravljenje raka s pirido pirimidin PI3K alfa inhibitorji |
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WO2010039740A1 (en) * | 2008-09-30 | 2010-04-08 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα AND MTOR |
-
2008
- 2008-04-09 SI SI200831004T patent/SI2139484T1/sl unknown
- 2008-04-09 PL PL08742677T patent/PL2139484T3/pl unknown
- 2008-04-09 CA CA2683641A patent/CA2683641C/en not_active Expired - Fee Related
- 2008-04-09 PT PT87426771T patent/PT2139484E/pt unknown
- 2008-04-09 AU AU2008236562A patent/AU2008236562B2/en not_active Ceased
- 2008-04-09 UA UAA200911419A patent/UA100979C2/ru unknown
- 2008-04-09 DK DK08742677.1T patent/DK2139484T3/da active
- 2008-04-09 MY MYPI20094214 patent/MY150697A/en unknown
- 2008-04-09 MX MX2009010930A patent/MX2009010930A/es active IP Right Grant
- 2008-04-09 BR BRPI0810206-6A2A patent/BRPI0810206A2/pt not_active IP Right Cessation
- 2008-04-09 EA EA200970932A patent/EA020022B1/ru not_active IP Right Cessation
- 2008-04-09 ME MEP-2009-303A patent/ME00936B/me unknown
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