CO6140024A2 - Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancer - Google Patents
Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancerInfo
- Publication number
- CO6140024A2 CO6140024A2 CO09126923A CO09126923A CO6140024A2 CO 6140024 A2 CO6140024 A2 CO 6140024A2 CO 09126923 A CO09126923 A CO 09126923A CO 09126923 A CO09126923 A CO 09126923A CO 6140024 A2 CO6140024 A2 CO 6140024A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- hydrogen
- compound
- optionally
- haloalkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003282 alkyl amino group Chemical group 0.000 abstract 3
- 125000004663 dialkyl 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
- -1 hydroxy, cyano, amino Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 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
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 229940127089 cytotoxic agent Drugs 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000000262 haloalkenyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 238000001794 hormone therapy Methods 0.000 abstract 1
- 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 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
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
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
- A61K31/335—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
- A61K31/435—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
- A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/517—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
- A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92316407P | 2007-04-11 | 2007-04-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6140024A2 true CO6140024A2 (es) | 2010-03-19 |
Family
ID=39864581
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO09126923A CO6140024A2 (es) | 2007-04-11 | 2009-11-09 | Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancer |
Country Status (33)
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20140975T1 (hr) * | 2005-10-07 | 2014-11-21 | Exelixis, Inc. | Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova uporaba kao inhibitora fosfatidilinozitol 3-kinaze |
| HRP20130902T1 (hr) * | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| CA2658725A1 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| PT2139484E (pt) * | 2007-04-10 | 2013-10-31 | Exelixis Inc | Métodos de tratamento de cancro usando inibidores piridopirimidinona de pi3k-alfa |
| WO2010053182A1 (ja) * | 2008-11-10 | 2010-05-14 | 協和発酵キリン株式会社 | キヌレニン産生抑制剤 |
| DE102009049679A1 (de) | 2009-10-19 | 2011-04-21 | Merck Patent Gmbh | Pyrazolopyrimidinderivate |
| 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 |
| JP2013539453A (ja) | 2010-07-09 | 2013-10-24 | エクセリクシス， インク． | 癌の治療のためのキナーゼ阻害物質の組み合わせ |
| TWI642670B (zh) | 2010-09-14 | 2018-12-01 | 伊塞利克斯公司 | Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法 |
| AU2011317675A1 (en) | 2010-10-20 | 2013-05-02 | Merck Serono S.A. Geneva | Method for preparing substituted N-(3-amino-quinoxalin-2-yl)-sulfonamides and their intermediates N-(3-chloro-quinoxalin-2-yl)sulfonamides |
| DE102010048800A1 (de) * | 2010-10-20 | 2012-05-10 | Merck Patent Gmbh | Chinoxalinderivate |
| DE102010049595A1 (de) | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
| WO2012065057A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors and methods of their use |
| TW201325592A (zh) * | 2011-09-14 | 2013-07-01 | Exelixis Inc | 用於治療癌症之磷脂醯肌醇－３激酶抑制劑 |
| EP2763994A4 (en) * | 2011-10-04 | 2015-08-26 | Gilead Calistoga Llc | NEW QUINOXALINE INHIBITORS OF THE PI3K PATH |
| WO2013056067A1 (en) | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| RU2014120792A (ru) * | 2011-10-28 | 2015-12-10 | Новартис Аг | Способ лечения стромальных опухолей желудочно-кишечного тракта |
| SG11201401961UA (en) * | 2011-11-01 | 2014-05-29 | 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 |
| WO2013067306A1 (en) * | 2011-11-02 | 2013-05-10 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers |
| CA2860051A1 (en) | 2011-12-27 | 2013-07-04 | Kadmon Corporation, Llc | Methods for treatment of breast cancer nonresponsive to trastuzumab |
| CN103467482B (zh) | 2012-04-10 | 2017-05-10 | 上海璎黎药业有限公司 | 稠合嘧啶类化合物，其制备方法，中间体，组合物和应用 |
| US9487526B2 (en) | 2012-08-13 | 2016-11-08 | Takeda Pharmaceutical Company Limited | Quinoxaline derivatives as GPR6 modulators |
| JP6441910B2 (ja) | 2013-09-30 | 2018-12-19 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用 |
| CN106831722B (zh) | 2013-10-16 | 2019-08-30 | 上海璎黎药业有限公司 | 稠合杂环化合物、其制备方法、药物组合物和用途 |
| JP6526034B2 (ja) | 2014-02-14 | 2019-06-05 | 武田薬品工業株式会社 | Ｇｐｒ６のピリドピラジンモジュレーター |
| US9950194B2 (en) | 2014-09-09 | 2018-04-24 | Mevion Medical Systems, Inc. | Patient positioning system |
| WO2019119206A1 (en) * | 2017-12-18 | 2019-06-27 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| US20250313524A1 (en) * | 2022-05-10 | 2025-10-09 | Relay Therapeutics, Inc. | Pi3k-alpha inhibitors and methods of use thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1599196A4 (en) * | 2003-01-17 | 2006-05-31 | Threshold Pharmaceuticals Inc | COMBINATION THERAPIES FOR CANCER TREATMENT |
| ZA200801822B (en) | 2005-08-26 | 2009-09-30 | Serono Lab | Pyrazine derivatives and use as p13k inhibitors |
| HRP20130902T1 (hr) | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| HRP20140975T1 (hr) | 2005-10-07 | 2014-11-21 | Exelixis, Inc. | Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova uporaba kao inhibitora fosfatidilinozitol 3-kinaze |
| CA2658725A1 (en) * | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| ZA200904857B (en) * | 2007-02-22 | 2010-09-29 | Merck Serono Sa | Quinoxaline compounds and use thereof |
| PT2139484E (pt) | 2007-04-10 | 2013-10-31 | Exelixis Inc | Métodos de tratamento de cancro usando inibidores piridopirimidinona de pi3k-alfa |
| JP4623164B2 (ja) * | 2008-08-21 | 2011-02-02 | セイコーエプソン株式会社 | プロジェクタ |
-
2008
- 2008-04-08 UA UAA200911452A patent/UA98141C2/ru unknown
- 2008-04-08 CA CA002684056A patent/CA2684056A1/en not_active Abandoned
- 2008-04-08 NZ NZ580009A patent/NZ580009A/xx not_active IP Right Cessation
- 2008-04-08 ES ES08742674.8T patent/ES2438998T3/es active Active
- 2008-04-08 KR KR1020097023536A patent/KR101586774B1/ko not_active Expired - Fee Related
- 2008-04-08 US US12/595,236 patent/US8481001B2/en not_active Expired - Fee Related
- 2008-04-08 PL PL08742674T patent/PL2139483T3/pl unknown
- 2008-04-08 PT PT87426748T patent/PT2139483E/pt unknown
- 2008-04-08 EA EA200970935A patent/EA019064B1/ru not_active IP Right Cessation
- 2008-04-08 CN CN2013101161222A patent/CN103202842A/zh active Pending
- 2008-04-08 WO PCT/US2008/004570 patent/WO2008127594A2/en not_active Ceased
- 2008-04-08 MY MYPI20094215 patent/MY150797A/en unknown
- 2008-04-08 RS RS20130486A patent/RS53020B/sr unknown
- 2008-04-08 AU AU2008239668A patent/AU2008239668B2/en not_active Ceased
- 2008-04-08 ME MEP-2009-304A patent/ME00937B/me unknown
- 2008-04-08 SI SI200831061T patent/SI2139483T1/sl unknown
- 2008-04-08 DK DK08742674.8T patent/DK2139483T3/da active
- 2008-04-08 JP JP2010503043A patent/JP5726515B2/ja active Active
- 2008-04-08 HR HRP20131081AT patent/HRP20131081T1/hr unknown
- 2008-04-08 CN CN2008800173944A patent/CN101959516B/zh not_active Expired - Fee Related
- 2008-04-08 EP EP08742674.8A patent/EP2139483B9/en active Active
- 2008-04-08 BR BRPI0810208-2A2A patent/BRPI0810208A2/pt not_active IP Right Cessation
- 2008-04-08 MX MX2009010929A patent/MX2009010929A/es active IP Right Grant
-
2009
- 2009-09-29 IL IL201211A patent/IL201211A/en active IP Right Grant
- 2009-09-29 ZA ZA200906765A patent/ZA200906765B/xx unknown
- 2009-09-30 TN TNP2009000399A patent/TN2009000399A1/fr unknown
- 2009-10-09 SV SV2009003390A patent/SV2009003390A/es unknown
- 2009-10-09 NI NI200900184A patent/NI200900184A/es unknown
- 2009-10-09 GT GT200900263A patent/GT200900263A/es unknown
- 2009-10-30 MA MA32313A patent/MA31335B1/fr unknown
- 2009-11-09 EC EC2009009723A patent/ECSP099723A/es unknown
- 2009-11-09 CO CO09126923A patent/CO6140024A2/es unknown
- 2009-11-09 CR CR11099A patent/CR11099A/es unknown
-
2013
- 2013-11-01 JP JP2013228684A patent/JP2014074031A/ja active Pending
- 2013-11-15 CY CY20131101016T patent/CY1114608T1/el unknown
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