TWI557126B - 絲胺酸／蘇胺酸激酶抑制劑 - Google Patents
絲胺酸／蘇胺酸激酶抑制劑 Download PDFInfo
- Publication number
- TWI557126B TWI557126B TW103142501A TW103142501A TWI557126B TW I557126 B TWI557126 B TW I557126B TW 103142501 A TW103142501 A TW 103142501A TW 103142501 A TW103142501 A TW 103142501A TW I557126 B TWI557126 B TW I557126B
- Authority
- TW
- Taiwan
- Prior art keywords
- methyl
- pyrazol
- dihydro
- amine
- pyrimidin
- Prior art date
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Classifications
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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
- A61K31/495—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
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/5365—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 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—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
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-condensed systems
-
- 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
- C07D498/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/16—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912905P | 2013-12-06 | 2013-12-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201522338A TW201522338A (zh) | 2015-06-16 |
| TWI557126B true TWI557126B (zh) | 2016-11-11 |
Family
ID=52350292
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW103142501A TWI557126B (zh) | 2013-12-06 | 2014-12-05 | 絲胺酸／蘇胺酸激酶抑制劑 |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US9867833B2 (https=) |
| EP (1) | EP3077401B1 (https=) |
| JP (2) | JP6449293B2 (https=) |
| KR (1) | KR102359759B1 (https=) |
| CN (1) | CN106029672B (https=) |
| AR (1) | AR098647A1 (https=) |
| AU (1) | AU2014360455B2 (https=) |
| BR (1) | BR112016012844B1 (https=) |
| CA (1) | CA2932729C (https=) |
| CL (1) | CL2016001368A1 (https=) |
| CR (1) | CR20160309A (https=) |
| EA (1) | EA031243B1 (https=) |
| IL (1) | IL246017B (https=) |
| MA (1) | MA39170B1 (https=) |
| MX (1) | MX368443B (https=) |
| MY (1) | MY176049A (https=) |
| PE (1) | PE20160886A1 (https=) |
| PH (1) | PH12016501071B1 (https=) |
| SG (1) | SG11201604573WA (https=) |
| TW (1) | TWI557126B (https=) |
| UA (1) | UA120506C2 (https=) |
| WO (1) | WO2015085007A1 (https=) |
| ZA (1) | ZA201604461B (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015533151A (ja) | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| EP3077401B1 (en) | 2013-12-06 | 2018-04-18 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| KR102379517B1 (ko) | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| JP6642942B2 (ja) * | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| RS60155B1 (sr) * | 2015-11-09 | 2020-05-29 | Astrazeneca Ab | Derivati dihidroimidazopirazinona korisni za upotrebu u tretmanu raka |
| WO2017180581A1 (en) | 2016-04-15 | 2017-10-19 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
| AU2018329925B2 (en) | 2017-09-08 | 2025-05-29 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| CN119350306A (zh) * | 2018-12-13 | 2025-01-24 | 英特维特国际股份有限公司 | 1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺制备方法 |
| MX2021014961A (es) * | 2019-06-06 | 2022-01-24 | Hutchison Medipharma Ltd | Compuestos triciclicos y su uso. |
| TW202231282A (zh) * | 2021-02-03 | 2022-08-16 | 大陸商上海拓界生物醫藥科技有限公司 | 稠三環類細胞週期蛋白－依賴性激酶抑制劑及其製備方法和醫藥用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101679409A (zh) * | 2006-12-22 | 2010-03-24 | Astex治疗学有限公司 | 新颖化合物 |
| WO2013130976A1 (en) * | 2012-03-01 | 2013-09-06 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005508358A (ja) * | 2001-10-25 | 2005-03-31 | デポメド・インコーポレイテッド | 胃滞留型ロサルタン投与量を用いる治療方法 |
| BRPI0615930A2 (pt) * | 2005-09-15 | 2016-08-23 | Painceptor Pharma Corp | métodos de modular a interação de uma neurotrofina e um receptor de neurotrofina, de tratar dor em um indivíduo, de tratar distúrbio inflamatório em um indivíduo, de tratar um distúrbio neurológico em um indivíduo, e de tratar uma doença ou distúrbio associado aos sistemas geniturinário e/ou gastrointestinal de um indivíduo, e, composto |
| EP2002836B1 (en) * | 2007-05-31 | 2010-10-20 | Nerviano Medical Sciences S.r.l. | Cyclocondensed azaindoles active as kinase inhibitors |
| PT2643322T (pt) | 2010-11-23 | 2017-11-13 | Abbvie Inc | Sais e formas cristalinas de um agente indutor de apoptose |
| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン／スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| AR092253A1 (es) | 2012-08-27 | 2015-04-08 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| JP2015533151A (ja) | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| EP3077401B1 (en) | 2013-12-06 | 2018-04-18 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| KR102379517B1 (ko) | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| JP6642942B2 (ja) | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| MY188526A (en) | 2014-04-09 | 2021-12-18 | Genentech Inc | Process for the manufacturing of medicaments |
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2014
- 2014-12-03 EP EP14827591.0A patent/EP3077401B1/en active Active
- 2014-12-03 SG SG11201604573WA patent/SG11201604573WA/en unknown
- 2014-12-03 AU AU2014360455A patent/AU2014360455B2/en not_active Ceased
- 2014-12-03 KR KR1020167017847A patent/KR102359759B1/ko not_active Expired - Fee Related
- 2014-12-03 MY MYPI2016001051A patent/MY176049A/en unknown
- 2014-12-03 JP JP2016536560A patent/JP6449293B2/ja active Active
- 2014-12-03 CN CN201480074890.9A patent/CN106029672B/zh active Active
- 2014-12-03 PE PE2016000741A patent/PE20160886A1/es unknown
- 2014-12-03 WO PCT/US2014/068452 patent/WO2015085007A1/en not_active Ceased
- 2014-12-03 MX MX2016007352A patent/MX368443B/es active IP Right Grant
- 2014-12-03 US US14/559,786 patent/US9867833B2/en active Active
- 2014-12-03 CR CR20160309A patent/CR20160309A/es unknown
- 2014-12-03 EA EA201691177A patent/EA031243B1/ru not_active IP Right Cessation
- 2014-12-03 MA MA39170A patent/MA39170B1/fr unknown
- 2014-12-03 BR BR112016012844-3A patent/BR112016012844B1/pt not_active IP Right Cessation
- 2014-12-03 CA CA2932729A patent/CA2932729C/en active Active
- 2014-12-03 UA UAA201607281A patent/UA120506C2/uk unknown
- 2014-12-05 AR ARP140104549A patent/AR098647A1/es unknown
- 2014-12-05 TW TW103142501A patent/TWI557126B/zh not_active IP Right Cessation
-
2016
- 2016-06-03 CL CL2016001368A patent/CL2016001368A1/es unknown
- 2016-06-05 IL IL24601716A patent/IL246017B/en active IP Right Grant
- 2016-06-06 PH PH12016501071A patent/PH12016501071B1/en unknown
- 2016-06-30 ZA ZA2016/04461A patent/ZA201604461B/en unknown
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2017
- 2017-09-14 US US15/705,104 patent/US10278975B2/en active Active
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2018
- 2018-11-09 JP JP2018211421A patent/JP2019034970A/ja active Pending
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2019
- 2019-02-27 US US16/286,955 patent/US10517878B2/en active Active
- 2019-11-11 US US16/680,221 patent/US10842799B2/en active Active
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2020
- 2020-10-20 US US17/075,380 patent/US11376260B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101679409A (zh) * | 2006-12-22 | 2010-03-24 | Astex治疗学有限公司 | 新颖化合物 |
| WO2013130976A1 (en) * | 2012-03-01 | 2013-09-06 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Annulment or lapse of patent due to non-payment of fees |