PE20160886A1 - Inhibidores de serina/treonina cinasa - Google Patents
Inhibidores de serina/treonina cinasaInfo
- Publication number
- PE20160886A1 PE20160886A1 PE2016000741A PE2016000741A PE20160886A1 PE 20160886 A1 PE20160886 A1 PE 20160886A1 PE 2016000741 A PE2016000741 A PE 2016000741A PE 2016000741 A PE2016000741 A PE 2016000741A PE 20160886 A1 PE20160886 A1 PE 20160886A1
- Authority
- PE
- Peru
- Prior art keywords
- serine
- compounds
- kinase inhibitors
- threonine kinase
- triazabenzo
- Prior art date
Links
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
- A61K31/55—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
- 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
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (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)
Abstract
La presente invencion se refiere a compuestos de formula I donde R1 es un heterociclilo de 4 a 7 miembros o un heteroarilo de 5 a 6 miembros opcionalmente sustituidos; X1 es N o CH; X2 es O, S, entre otros; X3 es C(=O), C(=O)O, entre otros; X4 es CR2 o NR3; R2 es alquilo C1-C10, alquenilo C1-C10, entre otros; R3 es hidrogeno o alquilo C1-C3. Son compuestos preferidos: 4-(9-(4-clorobencil)-8,9-dihidro-7H-6-oxa-1,2,2a1-triazabenzo[cd]azulen-4-il)-N-(1-metil-1H-pirazol-5-il)pirimidin-2-amina; (R)-4-(9-(4-clorobencil)-8,9-dihidro-7H-6-oxa-1,2,2a1-triazabenzo[cd]azulen-4-il)-N-(1-metil-1H-pirazol-5-il)pirimidin-2-amina; entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tratamiento. Dichos compuestos son inhibidores selecitvos de la cinasa ERK, siendo utiles en el tratamiento de enfermedades hiperproliferativas
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912905P | 2013-12-06 | 2013-12-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160886A1 true PE20160886A1 (es) | 2016-09-14 |
Family
ID=52350292
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000741A PE20160886A1 (es) | 2013-12-06 | 2014-12-03 | Inhibidores de serina/treonina cinasa |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US9867833B2 (es) |
| EP (1) | EP3077401B1 (es) |
| JP (2) | JP6449293B2 (es) |
| KR (1) | KR102359759B1 (es) |
| CN (1) | CN106029672B (es) |
| AR (1) | AR098647A1 (es) |
| AU (1) | AU2014360455B2 (es) |
| BR (1) | BR112016012844B1 (es) |
| CA (1) | CA2932729C (es) |
| CL (1) | CL2016001368A1 (es) |
| CR (1) | CR20160309A (es) |
| EA (1) | EA031243B1 (es) |
| IL (1) | IL246017B (es) |
| MA (1) | MA39170B1 (es) |
| MX (1) | MX368443B (es) |
| MY (1) | MY176049A (es) |
| PE (1) | PE20160886A1 (es) |
| PH (1) | PH12016501071A1 (es) |
| SG (1) | SG11201604573WA (es) |
| TW (1) | TWI557126B (es) |
| UA (1) | UA120506C2 (es) |
| WO (1) | WO2015085007A1 (es) |
| ZA (1) | ZA201604461B (es) |
Families Citing this family (10)
| 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 |
| KR102359759B1 (ko) | 2013-12-06 | 2022-02-09 | 제넨테크, 인크. | 세린/트레오닌 키나제 저해제 |
| CN105848723B (zh) | 2013-12-30 | 2019-08-02 | 基因泰克公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| 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 |
| LT3374359T (lt) * | 2015-11-09 | 2020-03-25 | Astrazeneca Ab | Dihidroimidazopirazinono deriniai, tinkami panaudoti vėžio gydymui |
| MX2018012471A (es) | 2016-04-15 | 2019-02-21 | Genentech Inc | Metodos de diagnostico y terapeuticos para el cancer. |
| KR20200041387A (ko) | 2017-09-08 | 2020-04-21 | 에프. 호프만-라 로슈 아게 | 암의 진단 및 치료 방법 |
| WO2019158579A1 (en) | 2018-02-13 | 2019-08-22 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| JP7433898B2 (ja) | 2019-12-26 | 2024-02-20 | キヤノン株式会社 | 光電変換素子、光電変換システム |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7413751B2 (en) | 2001-10-25 | 2008-08-19 | Depomed, Inc. | Methods of treatment using a gastric retained losartan dosage |
| EP1931664A4 (en) | 2005-09-15 | 2010-12-08 | Painceptor Pharma Corp | PROCESS FOR MODULATING NEUROTROPHINE-MEDIATED ACTIVITY |
| AU2007337895C1 (en) * | 2006-12-22 | 2014-07-31 | Astex Therapeutics Limited | Tricyclic amine derivatives as protein tyrosine kinase inhibitors |
| DE602008003055D1 (de) * | 2007-05-31 | 2010-12-02 | Nerviano Medical Sciences Srl | Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken |
| JP6141188B2 (ja) | 2010-11-23 | 2017-06-07 | アッヴィ・インコーポレイテッド | アポトーシス誘導剤の塩および結晶の形態 |
| WO2012118850A1 (en) | 2011-02-28 | 2012-09-07 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| CN103958502B (zh) | 2011-08-04 | 2016-02-10 | 阵列生物制药公司 | 作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物 |
| PL3321262T3 (pl) | 2012-03-01 | 2021-06-28 | Array Biopharma, Inc. | Inhibitory kinaz serynowo/treoninowych |
| WO2014036015A1 (en) | 2012-08-27 | 2014-03-06 | Array Biopharma Inc. | 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 |
| KR102359759B1 (ko) | 2013-12-06 | 2022-02-09 | 제넨테크, 인크. | 세린/트레오닌 키나제 저해제 |
| CN105848723B (zh) | 2013-12-30 | 2019-08-02 | 基因泰克公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| 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 |
| PL3129025T3 (pl) | 2014-04-09 | 2019-11-29 | Genentech Inc | Sposób wytwarzania środków leczniczych |
-
2014
- 2014-12-03 KR KR1020167017847A patent/KR102359759B1/ko active IP Right Grant
- 2014-12-03 JP JP2016536560A patent/JP6449293B2/ja active Active
- 2014-12-03 US US14/559,786 patent/US9867833B2/en active Active
- 2014-12-03 CA CA2932729A patent/CA2932729C/en active Active
- 2014-12-03 SG SG11201604573WA patent/SG11201604573WA/en unknown
- 2014-12-03 CR CR20160309A patent/CR20160309A/es unknown
- 2014-12-03 MY MYPI2016001051A patent/MY176049A/en unknown
- 2014-12-03 EP EP14827591.0A patent/EP3077401B1/en active Active
- 2014-12-03 MX MX2016007352A patent/MX368443B/es active IP Right Grant
- 2014-12-03 UA UAA201607281A patent/UA120506C2/uk unknown
- 2014-12-03 AU AU2014360455A patent/AU2014360455B2/en not_active Ceased
- 2014-12-03 PE PE2016000741A patent/PE20160886A1/es unknown
- 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 CN CN201480074890.9A patent/CN106029672B/zh active Active
- 2014-12-03 WO PCT/US2014/068452 patent/WO2015085007A1/en active Application Filing
- 2014-12-03 EA EA201691177A patent/EA031243B1/ru not_active IP Right Cessation
- 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/PH12016501071A1/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
-
2020
- 2020-10-20 US US17/075,380 patent/US11376260B2/en active Active
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