AU2010299816C1 - Benzoxazepin PI3K inhibitor compounds and methods of use - Google Patents
Benzoxazepin PI3K inhibitor compounds and methods of use Download PDFInfo
- Publication number
- AU2010299816C1 AU2010299816C1 AU2010299816A AU2010299816A AU2010299816C1 AU 2010299816 C1 AU2010299816 C1 AU 2010299816C1 AU 2010299816 A AU2010299816 A AU 2010299816A AU 2010299816 A AU2010299816 A AU 2010299816A AU 2010299816 C1 AU2010299816 C1 AU 2010299816C1
- Authority
- AU
- Australia
- Prior art keywords
- triazol
- isopropyl
- imidazo
- oxazepin
- dihydrobenzo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 0 C*=CCc1ncn[n]1CC(F)(F)F Chemical compound C*=CCc1ncn[n]1CC(F)(F)F 0.000 description 5
- RYSBJBYIMBBOHX-UHFFFAOYSA-N CC(C)[n](c(C)n1)nc1SC Chemical compound CC(C)[n](c(C)n1)nc1SC RYSBJBYIMBBOHX-UHFFFAOYSA-N 0.000 description 1
- AIUVAZQMVWSJEN-UHFFFAOYSA-N CC(C)[n]1nc(C)cc1C Chemical compound CC(C)[n]1nc(C)cc1C AIUVAZQMVWSJEN-UHFFFAOYSA-N 0.000 description 1
- ZKSIWEDWIIWGFW-UHFFFAOYSA-N CC(C)[n]1nc(C)nc1-c1c[n](CCOc2cc(F)ccc2-2)c-2n1 Chemical compound CC(C)[n]1nc(C)nc1-c1c[n](CCOc2cc(F)ccc2-2)c-2n1 ZKSIWEDWIIWGFW-UHFFFAOYSA-N 0.000 description 1
- UVRLGILFHWSWKE-UHFFFAOYSA-N CC(C)[n]1nc(N)nc1C Chemical compound CC(C)[n]1nc(N)nc1C UVRLGILFHWSWKE-UHFFFAOYSA-N 0.000 description 1
- BYBLWSSQJBNLJB-UHFFFAOYSA-N CC(C)[n]1ncc(C#N)c1C Chemical compound CC(C)[n]1ncc(C#N)c1C BYBLWSSQJBNLJB-UHFFFAOYSA-N 0.000 description 1
- PGANWJYTXZPWMI-UHFFFAOYSA-N CC(C)[n]1nccc1C Chemical compound CC(C)[n]1nccc1C PGANWJYTXZPWMI-UHFFFAOYSA-N 0.000 description 1
- HSATUUZNCWZCKQ-UHFFFAOYSA-N CC(C)c1c[n](C)nc1C Chemical compound CC(C)c1c[n](C)nc1C HSATUUZNCWZCKQ-UHFFFAOYSA-N 0.000 description 1
- USMBFLYKCBFMHY-UHFFFAOYSA-N CC(C)c1n[n](C)cc1C Chemical compound CC(C)c1n[n](C)cc1C USMBFLYKCBFMHY-UHFFFAOYSA-N 0.000 description 1
- OMQVYTOOFMGFGD-UHFFFAOYSA-N Cc1n[n]2-c(cccc3)c3OCCc2n1 Chemical compound Cc1n[n]2-c(cccc3)c3OCCc2n1 OMQVYTOOFMGFGD-UHFFFAOYSA-N 0.000 description 1
- YLFPSUHELVAAGL-UHFFFAOYSA-N Cc1ncc[n]1-c1ccccc1C Chemical compound Cc1ncc[n]1-c1ccccc1C YLFPSUHELVAAGL-UHFFFAOYSA-N 0.000 description 1
- QYITUSTUCZWHNI-UHFFFAOYSA-N Cc1ncc[n]1CC(NC)=O Chemical compound Cc1ncc[n]1CC(NC)=O QYITUSTUCZWHNI-UHFFFAOYSA-N 0.000 description 1
- KNQOUJKUKKBBGG-UHFFFAOYSA-N Cc1ncn[n]1C(CC1)CS1(=O)=O Chemical compound Cc1ncn[n]1C(CC1)CS1(=O)=O KNQOUJKUKKBBGG-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2015252149A AU2015252149B2 (en) | 2009-09-28 | 2015-11-06 | Benzoxazepin PI3K inhibitor compounds and methods of use |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24638109P | 2009-09-28 | 2009-09-28 | |
| US61/246,381 | 2009-09-28 | ||
| US33068510P | 2010-05-03 | 2010-05-03 | |
| US61/330,685 | 2010-05-03 | ||
| PCT/EP2010/064208 WO2011036280A1 (en) | 2009-09-28 | 2010-09-27 | Benzoxazepin pi3k inhibitor compounds and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2015252149A Division AU2015252149B2 (en) | 2009-09-28 | 2015-11-06 | Benzoxazepin PI3K inhibitor compounds and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2010299816A1 AU2010299816A1 (en) | 2012-02-02 |
| AU2010299816B2 AU2010299816B2 (en) | 2015-11-12 |
| AU2010299816C1 true AU2010299816C1 (en) | 2018-02-01 |
Family
ID=43037239
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2010299816A Active AU2010299816C1 (en) | 2009-09-28 | 2010-09-27 | Benzoxazepin PI3K inhibitor compounds and methods of use |
Country Status (31)
| Country | Link |
|---|---|
| US (7) | US8242104B2 (enExample) |
| EP (3) | EP2845592A1 (enExample) |
| JP (2) | JP5540101B2 (enExample) |
| KR (1) | KR101428346B1 (enExample) |
| CN (2) | CN102762576B (enExample) |
| AR (1) | AR078187A1 (enExample) |
| AU (1) | AU2010299816C1 (enExample) |
| BR (1) | BR112012006807A2 (enExample) |
| CA (1) | CA2772691C (enExample) |
| CL (1) | CL2012000754A1 (enExample) |
| CO (1) | CO6491026A2 (enExample) |
| CR (1) | CR20120121A (enExample) |
| DK (1) | DK2483278T3 (enExample) |
| EC (1) | ECSP12011755A (enExample) |
| ES (2) | ES2570569T3 (enExample) |
| HR (1) | HRP20140229T1 (enExample) |
| IL (2) | IL217558A (enExample) |
| MA (1) | MA33531B1 (enExample) |
| MX (1) | MX2012003591A (enExample) |
| MY (2) | MY184074A (enExample) |
| NZ (1) | NZ597833A (enExample) |
| PE (1) | PE20121025A1 (enExample) |
| PL (1) | PL2483278T3 (enExample) |
| PT (1) | PT2483278E (enExample) |
| RS (1) | RS53164B (enExample) |
| RU (2) | RU2600927C2 (enExample) |
| SG (1) | SG10201405049RA (enExample) |
| SI (1) | SI2483278T1 (enExample) |
| TW (1) | TWI423980B (enExample) |
| WO (1) | WO2011036280A1 (enExample) |
| ZA (1) | ZA201202199B (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| NZ598942A (en) | 2009-07-27 | 2014-02-28 | Gilead Sciences Inc | Fused heterocyclic compounds as ion channel modulators |
| NZ599090A (en) * | 2009-09-28 | 2014-02-28 | Hoffmann La Roche | Benzoxepin pi3k inhibitor compounds and methods of use |
| PE20121025A1 (es) * | 2009-09-28 | 2012-08-06 | Hoffmann La Roche | Compuestos de benzoxazepina como inhibidores de la p13k |
| CN103096977B (zh) | 2010-07-02 | 2017-02-15 | 吉利德科学公司 | 作为离子通道调节剂的稠杂环化合物 |
| CA2825966A1 (en) * | 2011-03-21 | 2012-09-27 | F. Hoffmann-La Roche Ag | Benzoxazepin compounds selective for pi3k p110 delta and methods of use |
| TWI577670B (zh) | 2011-05-10 | 2017-04-11 | 基利科學股份有限公司 | 充當離子通道調節劑之稠合雜環化合物 |
| WO2012156379A1 (en) | 2011-05-13 | 2012-11-22 | Universität Zürich | PIK3/P110α INHIBITORS FOR PREVENTION OF RESTENOSIS BY APPLICATION AS AN IMPLANT COATING |
| NO3175985T3 (enExample) | 2011-07-01 | 2018-04-28 | ||
| TWI622583B (zh) | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| HK1206024A1 (en) * | 2012-02-17 | 2015-12-31 | F. Hoffmann-La Roche Ag | Tricyclic compounds and methods of use therefor |
| NZ702244A (en) * | 2012-06-08 | 2017-06-30 | Hoffmann La Roche | Mutant selectivity and combinations of a phosphoinositide 3 kinase inhibitor compound and chemotherapeutic agents for the treatment of cancer |
| BR112014032346A2 (pt) | 2012-06-26 | 2017-06-27 | Del Mar Pharmaceuticals | métodos para tratamento de malignidades resistentes ao inibidor de tirosina-quinase em pacientes com polimorfismos genéticos ou desregulações de ahi1 mutações empregando dianidrogalactitol, diacetildianidrogalactitol, dibromodulcitol, ou análogos ou derivados destes |
| CN102775395A (zh) * | 2012-07-12 | 2012-11-14 | 江苏七洲绿色化工股份有限公司 | 一种丙环唑的制备方法及丙环唑中间体 |
| US9303046B2 (en) * | 2012-08-07 | 2016-04-05 | Janssen Pharmaceutica Nv | Process for the preparation of heterocyclic ester derivatives |
| EP3404032B1 (en) * | 2013-03-13 | 2025-07-02 | F. Hoffmann-La Roche AG | Process for making benzoxazepin compounds |
| AU2014251038A1 (en) | 2013-04-08 | 2015-11-26 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| RU2018119749A (ru) * | 2013-12-16 | 2018-11-09 | Ф. Хоффманн-Ля Рош Аг | Полиморфы 2-(4-(2-(1-изопропил-3-метил-1h-1,2,4-триазол-5-ил)-5,6-дигидробензо[f]имидазо[1,2-d][1,4]оксазепин-9-ил)-1h-пиразол-1-ил)-2-метилпропанамида, способы их получения и фармацевтические применения |
| SG11201607334YA (en) | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Therapeutic combinations with estrogen receptor modulators |
| SG11201708622UA (en) | 2015-02-02 | 2017-11-29 | Forma Therapeutics Inc | 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors |
| US10183934B2 (en) | 2015-02-02 | 2019-01-22 | Forma Therapeutics, Inc. | Bicyclic [4,6,0] hydroxamic acids as HDAC inhibitors |
| AR104068A1 (es) | 2015-03-26 | 2017-06-21 | Hoffmann La Roche | Combinaciones de un compuesto inhibidor de fosfoinosítido 3-cinasa y un compuesto inhibidor de cdk4/6 para el tratamiento del cáncer |
| WO2016174616A1 (en) * | 2015-04-30 | 2016-11-03 | Novartis Ag | Fused tricyclic pyrazole derivatives useful for modulating farnesoid x receptors |
| JP6871919B2 (ja) | 2015-06-16 | 2021-05-19 | ナノファギックス エルエルシー | 薬物送達及びイメージング化学コンジュゲート、製剤及びその使用方法 |
| EP3314265B1 (en) | 2015-06-29 | 2019-07-24 | H. Hoffnabb-La Roche Ag | Methods of treatment with taselisib |
| TW202108592A (zh) * | 2015-07-02 | 2021-03-01 | 瑞士商赫孚孟拉羅股份公司 | 苯并氧氮呯噁唑啶酮化合物及其用途 |
| US9643980B2 (en) | 2015-07-02 | 2017-05-09 | Genentech, Inc. | Benzoxazepin oxazolidinone compounds and methods of use |
| US10065970B2 (en) | 2015-09-08 | 2018-09-04 | Genentech, Inc. | Tricyclic PI3K inhibitor compounds and methods of use |
| US9721369B2 (en) * | 2015-09-15 | 2017-08-01 | Facebook, Inc. | Systems and methods for utilizing multiple map portions from multiple map data sources |
| WO2017218950A1 (en) | 2016-06-17 | 2017-12-21 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| MX2019003714A (es) | 2016-09-29 | 2019-06-24 | Bayer Cropscience Ag | Novedosos derivados de imidazolilmetilo 5-sustituidos. |
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