CN109563088B - MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 - Google Patents
MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 Download PDFInfo
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- CN109563088B CN109563088B CN201780049835.8A CN201780049835A CN109563088B CN 109563088 B CN109563088 B CN 109563088B CN 201780049835 A CN201780049835 A CN 201780049835A CN 109563088 B CN109563088 B CN 109563088B
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- cancer
- disease
- pi3k
- mek
- tumors
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
- A61K41/0057—Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662359001P | 2016-07-06 | 2016-07-06 | |
| US62/359,001 | 2016-07-06 | ||
| US201762454163P | 2017-02-03 | 2017-02-03 | |
| US62/454,163 | 2017-02-03 | ||
| PCT/US2017/040866 WO2018009638A1 (en) | 2016-07-06 | 2017-07-06 | MULTIFUNCTIONAL INHIBITORS OF MEK/PI3K AND mTOR/MEK/PI3K BIOLOGICAL PATHWAYS AND THERAPEUTIC METHODS USING THE SAME |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109563088A CN109563088A (zh) | 2019-04-02 |
| CN109563088B true CN109563088B (zh) | 2022-10-11 |
Family
ID=59363277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780049835.8A Active CN109563088B (zh) | 2016-07-06 | 2017-07-06 | MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10919877B2 (https=) |
| EP (2) | EP4086250B1 (https=) |
| JP (2) | JP2019519593A (https=) |
| CN (1) | CN109563088B (https=) |
| AU (2) | AU2017291838B2 (https=) |
| CA (1) | CA3029875C (https=) |
| ES (2) | ES3002745T3 (https=) |
| WO (1) | WO2018009638A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018316175B2 (en) | 2017-08-11 | 2023-02-23 | The Regents Of The University Of Michigan | Inhibitors of MEK/PI3K, JAK/MEK, JAK/PI3K/mTOR and MEK/PI3K3k/mTOR biological pathways and methods for improving lymphatic uptake, bioavailability, and solubility of therapeutic compounds |
| CN112143700B (zh) * | 2019-06-26 | 2024-07-19 | 上海细胞治疗集团股份有限公司 | 制备过表达外源基因的免疫效应细胞的方法 |
| CN117396470A (zh) * | 2021-04-09 | 2024-01-12 | 巴塞尔大学 | 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物 |
| EP4320115A1 (en) * | 2021-04-09 | 2024-02-14 | Universität Basel | Triazine derivative as reversible and irreversible covalent inhibitors of pi3k |
| WO2023170107A1 (en) | 2022-03-07 | 2023-09-14 | Centre Hospitalier Universitaire Vaudois (Chuv) | Pi3k/akt/mtor inhibitor for improving the cellular uptake of a radiopharmaceutical |
| JP2023180347A (ja) * | 2022-06-09 | 2023-12-21 | 国立大学法人金沢大学 | ハイブリッド型化合物又はその塩 |
| WO2025072796A1 (en) * | 2023-09-27 | 2025-04-03 | Totus Medicines Inc. | Pharmaceutical compositions and methods of use thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009155121A2 (en) * | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| CN103748099A (zh) * | 2011-05-19 | 2014-04-23 | 西班牙国家癌症研究中心 | 作为蛋白激酶抑制剂的大环化合物 |
| CN105283454A (zh) * | 2013-04-12 | 2016-01-27 | 阿萨纳生物科技有限责任公司 | 作为ras/raf/mek/erk和pi3k/akt/pten/mtor通路双重抑制剂的喹唑啉和氮杂喹唑啉 |
| CN105358156A (zh) * | 2013-03-13 | 2016-02-24 | 密执安大学评议会 | 双重mek/pi3k抑制剂和使用其的治疗方法 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA197701A (en) | 1920-03-02 | Mcgoldrick Timothy | Arm cushion for crutches | |
| CA85878A (en) | 1903-08-19 | 1904-03-08 | George W. Peyton | Carpenter's gauge |
| US5608110A (en) | 1993-06-15 | 1997-03-04 | Bracco International B.V. | Heteroatom-bearing ligands and metal complexes thereof |
| DZ3401A1 (fr) | 2000-07-19 | 2002-01-24 | Warner Lambert Co | Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques |
| TW200505834A (en) | 2003-03-18 | 2005-02-16 | Sankyo Co | Sulfamide derivative and the pharmaceutical composition thereof |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| AR059339A1 (es) | 2006-02-09 | 2008-03-26 | Chugai Pharmaceutical Co Ltd | Derivados de la cumarina para trastornos proliferativos de celulas, composicion farmaceutica y agente terapeutico que los contiene |
| DK2074122T5 (da) | 2006-09-15 | 2014-03-17 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer |
| US8569378B2 (en) | 2007-07-20 | 2013-10-29 | Toshiyuki Sakai | p27 protein inducer |
| EP2276750A2 (en) | 2008-03-27 | 2011-01-26 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
| EP2143819A1 (de) | 2008-07-11 | 2010-01-13 | Siemens Aktiengesellschaft | Beschichtungsverfahren und Korrosionsschutzbeschichtung für Turbinen-Komponenten |
| SG174527A1 (en) | 2009-03-27 | 2011-11-28 | Pathway Therapeutics Inc | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| US8486939B2 (en) | 2009-07-07 | 2013-07-16 | Pathway Therapeutics Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
| US20110166191A1 (en) | 2010-01-07 | 2011-07-07 | Shijun Zhang | 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and its derivatives as multiple signaling pathway inhibitors and for the treatment of cancer |
| GB201007227D0 (en) | 2010-04-30 | 2010-06-16 | Univ Basel | Piperazinotriazines |
| KR101759762B1 (ko) * | 2010-08-10 | 2017-07-19 | 아스텔라스세이야쿠 가부시키가이샤 | 헤테로환 화합물 |
| EP2640367A2 (en) | 2010-11-15 | 2013-09-25 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| WO2013071698A1 (zh) | 2011-11-17 | 2013-05-23 | 山东轩竹医药科技有限公司 | 三环类PI3K和/或mTOR抑制剂 |
| CN105130960B (zh) * | 2015-07-31 | 2018-07-06 | 沈阳药科大学 | 1,3,5-三嗪类衍生物及其应用 |
-
2017
- 2017-07-06 ES ES22179630T patent/ES3002745T3/es active Active
- 2017-07-06 EP EP22179630.3A patent/EP4086250B1/en active Active
- 2017-07-06 EP EP17740578.4A patent/EP3481822B1/en active Active
- 2017-07-06 US US16/313,923 patent/US10919877B2/en active Active
- 2017-07-06 JP JP2018568930A patent/JP2019519593A/ja active Pending
- 2017-07-06 ES ES17740578T patent/ES2922898T3/es active Active
- 2017-07-06 CA CA3029875A patent/CA3029875C/en active Active
- 2017-07-06 CN CN201780049835.8A patent/CN109563088B/zh active Active
- 2017-07-06 WO PCT/US2017/040866 patent/WO2018009638A1/en not_active Ceased
- 2017-07-06 AU AU2017291838A patent/AU2017291838B2/en active Active
-
2021
- 2021-04-28 AU AU2021202619A patent/AU2021202619B2/en active Active
- 2021-11-24 JP JP2021190205A patent/JP7475062B2/ja active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009155121A2 (en) * | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| CN103748099A (zh) * | 2011-05-19 | 2014-04-23 | 西班牙国家癌症研究中心 | 作为蛋白激酶抑制剂的大环化合物 |
| CN105358156A (zh) * | 2013-03-13 | 2016-02-24 | 密执安大学评议会 | 双重mek/pi3k抑制剂和使用其的治疗方法 |
| CN105283454A (zh) * | 2013-04-12 | 2016-01-27 | 阿萨纳生物科技有限责任公司 | 作为ras/raf/mek/erk和pi3k/akt/pten/mtor通路双重抑制剂的喹唑啉和氮杂喹唑啉 |
Non-Patent Citations (3)
| Title |
|---|
| "Discovery of bifunctional oncogenic target inhibitors against allosteric mitogen-activated protein kinase (MEK1) and phosphatidylinositol 3-kinase (PI3K)";Marcian E. Van Dort,et al.;《Journal of medicinal chemistry》;20160304;第59卷(第6期);第2512-2623页 * |
| "Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure Activity Relationships of a Series of Quinoline and Quinoxaline Derivatives";Nobuko Nishimura,et al.;《Journal of medicinal chemistry》;20110525;第54卷;第4735-4751页 * |
| Marcian E. Van Dort,et al.."Discovery of bifunctional oncogenic target inhibitors against allosteric mitogen-activated protein kinase (MEK1) and phosphatidylinositol 3-kinase (PI3K)".《Journal of medicinal chemistry》.2016,第59卷(第6期),第2512-2623页. * |
Also Published As
| Publication number | Publication date |
|---|---|
| ES3002745T3 (en) | 2025-03-07 |
| EP4086250B1 (en) | 2024-12-11 |
| EP4086250A3 (en) | 2023-03-22 |
| JP7475062B2 (ja) | 2024-04-26 |
| JP2019519593A (ja) | 2019-07-11 |
| CA3029875A1 (en) | 2018-01-11 |
| CN109563088A (zh) | 2019-04-02 |
| CA3029875C (en) | 2023-12-19 |
| EP4086250C0 (en) | 2024-12-11 |
| JP2022019812A (ja) | 2022-01-27 |
| EP3481822A1 (en) | 2019-05-15 |
| AU2017291838B2 (en) | 2021-01-28 |
| AU2017291838A1 (en) | 2019-01-17 |
| US10919877B2 (en) | 2021-02-16 |
| AU2021202619A1 (en) | 2021-05-27 |
| WO2018009638A1 (en) | 2018-01-11 |
| EP4086250A2 (en) | 2022-11-09 |
| AU2021202619B2 (en) | 2022-03-10 |
| ES2922898T3 (es) | 2022-09-21 |
| EP3481822B1 (en) | 2022-06-22 |
| US20190224207A1 (en) | 2019-07-25 |
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