CN106029672B - 丝氨酸/苏氨酸激酶抑制剂 - Google Patents
丝氨酸/苏氨酸激酶抑制剂 Download PDFInfo
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- CN106029672B CN106029672B CN201480074890.9A CN201480074890A CN106029672B CN 106029672 B CN106029672 B CN 106029672B CN 201480074890 A CN201480074890 A CN 201480074890A CN 106029672 B CN106029672 B CN 106029672B
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- Prior art keywords
- methyl
- base
- pyrazol
- compound
- dihydro
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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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912905P | 2013-12-06 | 2013-12-06 | |
| US61/912,905 | 2013-12-06 | ||
| PCT/US2014/068452 WO2015085007A1 (en) | 2013-12-06 | 2014-12-03 | Serine/threonine kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106029672A CN106029672A (zh) | 2016-10-12 |
| CN106029672B true CN106029672B (zh) | 2019-03-29 |
Family
ID=52350292
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480074890.9A Active CN106029672B (zh) | 2013-12-06 | 2014-12-03 | 丝氨酸/苏氨酸激酶抑制剂 |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US9867833B2 (enExample) |
| EP (1) | EP3077401B1 (enExample) |
| JP (2) | JP6449293B2 (enExample) |
| KR (1) | KR102359759B1 (enExample) |
| CN (1) | CN106029672B (enExample) |
| AR (1) | AR098647A1 (enExample) |
| AU (1) | AU2014360455B2 (enExample) |
| BR (1) | BR112016012844B1 (enExample) |
| CA (1) | CA2932729C (enExample) |
| CL (1) | CL2016001368A1 (enExample) |
| CR (1) | CR20160309A (enExample) |
| EA (1) | EA031243B1 (enExample) |
| IL (1) | IL246017B (enExample) |
| MA (1) | MA39170B1 (enExample) |
| MX (1) | MX368443B (enExample) |
| MY (1) | MY176049A (enExample) |
| PE (1) | PE20160886A1 (enExample) |
| PH (1) | PH12016501071B1 (enExample) |
| SG (1) | SG11201604573WA (enExample) |
| TW (1) | TWI557126B (enExample) |
| UA (1) | UA120506C2 (enExample) |
| WO (1) | WO2015085007A1 (enExample) |
| ZA (1) | ZA201604461B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2909206A1 (en) | 2012-10-16 | 2015-08-26 | F. Hoffmann-La Roche AG | Serine/threonine kinase inhibitors |
| 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 |
| EA031243B1 (ru) | 2013-12-06 | 2018-12-28 | Дженентек, Инк. | Ингибиторы серин/треонинкиназ |
| KR102379517B1 (ko) | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| MX375902B (es) | 2013-12-30 | 2025-03-07 | Genentech Inc | Inhibidores de serina/treonina cinasa. |
| SMT202000152T1 (it) | 2015-11-09 | 2020-05-08 | Astrazeneca Ab | Derivati di diidroimidazopirazinone utili nel trattamento di cancro |
| AU2017249229A1 (en) | 2016-04-15 | 2018-10-04 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
| KR102811888B1 (ko) | 2017-09-08 | 2025-05-27 | 에프. 호프만-라 로슈 아게 | 암의 진단 및 치료 방법 |
| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| CN113227077B (zh) * | 2018-12-13 | 2024-10-29 | 英特维特国际股份有限公司 | 一种制备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-甲酰胺的方法 |
| PH12021553058A1 (en) * | 2019-06-06 | 2022-07-25 | Hutchison Medipharma Ltd | Tricyclic compounds and their use |
| CN120682245A (zh) * | 2021-02-03 | 2025-09-23 | 江苏恒瑞医药股份有限公司 | 稠三环类细胞周期蛋白-依赖性激酶抑制剂及其制备方法和医药用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2002836A1 (en) * | 2007-05-31 | 2008-12-17 | Nerviano Medical Sciences S.r.l. | Cyclocondensed azaindoles active as kinase inhibitors |
| 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 (12)
| 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 |
| US20070099900A1 (en) | 2005-09-15 | 2007-05-03 | Painceptor Pharma Corporation | Methods of modulating neurotrophin-mediated activity |
| WO2012071336A1 (en) | 2010-11-23 | 2012-05-31 | Abbott Laboratories | Salts and crystalline forms of an apoptosis-inducing agent |
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| ES2552989T3 (es) | 2011-08-04 | 2015-12-03 | Array Biopharma, Inc. | Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina |
| CA2882750A1 (en) | 2012-08-27 | 2014-03-06 | Jim Blake | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| EP2909206A1 (en) | 2012-10-16 | 2015-08-26 | F. Hoffmann-La Roche AG | Serine/threonine kinase inhibitors |
| 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 |
| EA031243B1 (ru) | 2013-12-06 | 2018-12-28 | Дженентек, Инк. | Ингибиторы серин/треонинкиназ |
| KR102379517B1 (ko) | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| MX375902B (es) | 2013-12-30 | 2025-03-07 | Genentech Inc | Inhibidores de serina/treonina cinasa. |
| CN106659721B (zh) | 2014-04-09 | 2021-01-01 | 基因泰克公司 | 用于制备药物的方法 |
-
2014
- 2014-12-03 EA EA201691177A patent/EA031243B1/ru not_active IP Right Cessation
- 2014-12-03 JP JP2016536560A patent/JP6449293B2/ja active Active
- 2014-12-03 CN CN201480074890.9A patent/CN106029672B/zh active Active
- 2014-12-03 CA CA2932729A patent/CA2932729C/en 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 SG SG11201604573WA patent/SG11201604573WA/en unknown
- 2014-12-03 KR KR1020167017847A patent/KR102359759B1/ko not_active Expired - Fee Related
- 2014-12-03 BR BR112016012844-3A patent/BR112016012844B1/pt not_active IP Right Cessation
- 2014-12-03 MA MA39170A patent/MA39170B1/fr unknown
- 2014-12-03 MX MX2016007352A patent/MX368443B/es active IP Right Grant
- 2014-12-03 AU AU2014360455A patent/AU2014360455B2/en not_active Ceased
- 2014-12-03 UA UAA201607281A patent/UA120506C2/uk unknown
- 2014-12-03 MY MYPI2016001051A patent/MY176049A/en unknown
- 2014-12-03 EP EP14827591.0A patent/EP3077401B1/en active Active
- 2014-12-03 US US14/559,786 patent/US9867833B2/en active Active
- 2014-12-03 CR CR20160309A patent/CR20160309A/es 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
-
2017
- 2017-09-14 US US15/705,104 patent/US10278975B2/en active Active
-
2018
- 2018-11-09 JP JP2018211421A patent/JP2019034970A/ja active Pending
-
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
-
2020
- 2020-10-20 US US17/075,380 patent/US11376260B2/en not_active Expired - Fee Related
Patent Citations (3)
| 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 |
| EP2002836A1 (en) * | 2007-05-31 | 2008-12-17 | Nerviano Medical Sciences S.r.l. | Cyclocondensed azaindoles active as kinase inhibitors |
| WO2013130976A1 (en) * | 2012-03-01 | 2013-09-06 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
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