ES2527831T3 - Combinación que comprende el inhibidor de MEK: N-{3-[3-ciclopropil-5-(2-fluoro-4-yodo-fenilamino)-6,8-dimetil-2,4,7-trioxo-3,4,6,7-tetrahidro-2H-pirido[4,3-d]pirimidin-1-il]fenil}acetamida y el inhibidor de Akt: N-{(1S)-2-amino-1-[(3-fluorofenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1H-pirazol-5-il)-2-tiofenocarboxamida - Google Patents
Combinación que comprende el inhibidor de MEK: N-{3-[3-ciclopropil-5-(2-fluoro-4-yodo-fenilamino)-6,8-dimetil-2,4,7-trioxo-3,4,6,7-tetrahidro-2H-pirido[4,3-d]pirimidin-1-il]fenil}acetamida y el inhibidor de Akt: N-{(1S)-2-amino-1-[(3-fluorofenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1H-pirazol-5-il)-2-tiofenocarboxamida Download PDFInfo
- Publication number
- ES2527831T3 ES2527831T3 ES10819438.2T ES10819438T ES2527831T3 ES 2527831 T3 ES2527831 T3 ES 2527831T3 ES 10819438 T ES10819438 T ES 10819438T ES 2527831 T3 ES2527831 T3 ES 2527831T3
- Authority
- ES
- Spain
- Prior art keywords
- chloro
- methyl
- inhibitor
- thiophenecarboxamide
- trioxo
- 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.)
- Active
Links
- 229940126638 Akt inhibitor Drugs 0.000 title 1
- 229940124647 MEK inhibitor Drugs 0.000 title 1
- AFJRDFWMXUECEW-LBPRGKRZSA-N N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methyl-3-pyrazolyl)-2-thiophenecarboxamide Chemical compound CN1N=CC(Cl)=C1C1=C(Cl)SC(C(=O)N[C@H](CN)CC=2C=C(F)C=CC=2)=C1 AFJRDFWMXUECEW-LBPRGKRZSA-N 0.000 title 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 239000003197 protein kinase B inhibitor Substances 0.000 title 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 1
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
- A61K31/41—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
- A61K31/4155—1,2-Diazoles non condensed and containing further 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
- A61K31/495—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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Gastroenterology & Hepatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24502709P | 2009-09-23 | 2009-09-23 | |
| US245027P | 2009-09-23 | ||
| PCT/US2010/049952 WO2011038085A1 (en) | 2009-09-23 | 2010-09-23 | Combination |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2527831T3 true ES2527831T3 (es) | 2015-01-30 |
Family
ID=43796199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10819438.2T Active ES2527831T3 (es) | 2009-09-23 | 2010-09-23 | Combinación que comprende el inhibidor de MEK: N-{3-[3-ciclopropil-5-(2-fluoro-4-yodo-fenilamino)-6,8-dimetil-2,4,7-trioxo-3,4,6,7-tetrahidro-2H-pirido[4,3-d]pirimidin-1-il]fenil}acetamida y el inhibidor de Akt: N-{(1S)-2-amino-1-[(3-fluorofenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1H-pirazol-5-il)-2-tiofenocarboxamida |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US20120283278A1 (enExample) |
| EP (1) | EP2480085B1 (enExample) |
| JP (2) | JP5890310B2 (enExample) |
| KR (1) | KR101739158B1 (enExample) |
| CN (1) | CN102762098B (enExample) |
| AU (1) | AU2010298280B2 (enExample) |
| BR (1) | BR112012006485A2 (enExample) |
| CA (1) | CA2775125C (enExample) |
| EA (2) | EA201270453A1 (enExample) |
| ES (1) | ES2527831T3 (enExample) |
| IL (1) | IL218801A (enExample) |
| MX (1) | MX2012003547A (enExample) |
| SG (1) | SG179144A1 (enExample) |
| WO (1) | WO2011038085A1 (enExample) |
| ZA (1) | ZA201201940B (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI505828B (zh) | 2010-12-20 | 2015-11-01 | 葛蘭素史克智慧財產（第二）有限公司 | 新穎醫藥組成物 |
| EP2913048A1 (en) | 2014-02-27 | 2015-09-02 | ratiopharm GmbH | Pharmaceutical composition comprising trametinib |
| CN115916779B (zh) * | 2020-05-11 | 2025-09-16 | 克立弗治疗学股份有限公司 | 用于治疗癌症的VCP/p97抑制剂 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7378423B2 (en) * | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| KR100883289B1 (ko) * | 2004-06-11 | 2009-02-11 | 니뽄 다바코 산교 가부시키가이샤 | 암 치료용5-아미노-2,4,7-트리옥소-3,4,7,8-테트라히드로-2ｈ-피리도[2,3-ｄ]피리미딘 유도체 및 관련 화합물 |
| JP3821154B1 (ja) * | 2005-03-16 | 2006-09-13 | いすゞ自動車株式会社 | 排気ガス浄化方法及び排気ガス浄化システム |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
-
2010
- 2010-09-23 BR BR112012006485A patent/BR112012006485A2/pt active Search and Examination
- 2010-09-23 EP EP10819438.2A patent/EP2480085B1/en active Active
- 2010-09-23 EA EA201270453A patent/EA201270453A1/ru unknown
- 2010-09-23 SG SG2012018164A patent/SG179144A1/en unknown
- 2010-09-23 ES ES10819438.2T patent/ES2527831T3/es active Active
- 2010-09-23 JP JP2012531020A patent/JP5890310B2/ja not_active Expired - Fee Related
- 2010-09-23 CN CN201080052973.XA patent/CN102762098B/zh not_active Expired - Fee Related
- 2010-09-23 AU AU2010298280A patent/AU2010298280B2/en not_active Ceased
- 2010-09-23 US US13/497,580 patent/US20120283278A1/en not_active Abandoned
- 2010-09-23 MX MX2012003547A patent/MX2012003547A/es active IP Right Grant
- 2010-09-23 WO PCT/US2010/049952 patent/WO2011038085A1/en not_active Ceased
- 2010-09-23 KR KR1020127010301A patent/KR101739158B1/ko not_active Expired - Fee Related
- 2010-09-23 CA CA2775125A patent/CA2775125C/en not_active Expired - Fee Related
-
2012
- 2012-03-15 ZA ZA2012/01940A patent/ZA201201940B/en unknown
- 2012-03-22 IL IL218801A patent/IL218801A/en not_active IP Right Cessation
-
2014
- 2014-06-27 US US14/317,775 patent/US20140309243A1/en not_active Abandoned
-
2015
- 2015-09-25 EA EA201500882A patent/EA201500882A1/ru unknown
- 2015-12-18 JP JP2015246841A patent/JP6148320B2/ja not_active Expired - Fee Related
-
2016
- 2016-02-02 US US15/013,228 patent/US20160143913A1/en not_active Abandoned
-
2018
- 2018-03-27 US US15/936,659 patent/US20180214451A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010298280A1 (en) | 2012-04-05 |
| EA201500882A1 (ru) | 2016-05-31 |
| WO2011038085A1 (en) | 2011-03-31 |
| EP2480085A1 (en) | 2012-08-01 |
| BR112012006485A2 (pt) | 2015-09-08 |
| ZA201201940B (en) | 2012-11-28 |
| EP2480085A4 (en) | 2013-03-27 |
| CA2775125C (en) | 2019-01-08 |
| KR101739158B1 (ko) | 2017-05-23 |
| MX2012003547A (es) | 2012-04-30 |
| KR20120099218A (ko) | 2012-09-07 |
| US20140309243A1 (en) | 2014-10-16 |
| CN102762098A (zh) | 2012-10-31 |
| IL218801A0 (en) | 2012-06-28 |
| EP2480085B1 (en) | 2014-11-12 |
| EA201270453A1 (ru) | 2013-12-30 |
| IL218801A (en) | 2015-03-31 |
| JP5890310B2 (ja) | 2016-03-22 |
| US20180214451A1 (en) | 2018-08-02 |
| JP2016104765A (ja) | 2016-06-09 |
| AU2010298280B2 (en) | 2014-07-03 |
| US20120283278A1 (en) | 2012-11-08 |
| US20160143913A1 (en) | 2016-05-26 |
| JP2013505940A (ja) | 2013-02-21 |
| SG179144A1 (en) | 2012-05-30 |
| CN102762098B (zh) | 2015-10-14 |
| CA2775125A1 (en) | 2011-03-31 |
| JP6148320B2 (ja) | 2017-06-14 |
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