ES2746946T3 - Combinación de alisertib y paclitaxel para el tratamiento de cáncer - Google Patents
Combinación de alisertib y paclitaxel para el tratamiento de cáncer Download PDFInfo
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- ES2746946T3 ES2746946T3 ES13714455T ES13714455T ES2746946T3 ES 2746946 T3 ES2746946 T3 ES 2746946T3 ES 13714455 T ES13714455 T ES 13714455T ES 13714455 T ES13714455 T ES 13714455T ES 2746946 T3 ES2746946 T3 ES 2746946T3
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- aurora
- kinase inhibitor
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- cancer
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261613258P | 2012-03-20 | 2012-03-20 | |
| PCT/US2013/032962 WO2013142491A1 (en) | 2012-03-20 | 2013-03-19 | Methods of treating cancer using aurora kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2746946T3 true ES2746946T3 (es) | 2020-03-09 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13714455T Active ES2746946T3 (es) | 2012-03-20 | 2013-03-19 | Combinación de alisertib y paclitaxel para el tratamiento de cáncer |
Country Status (24)
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|---|---|
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| EP (1) | EP2827855B1 (enExample) |
| JP (1) | JP6373252B2 (enExample) |
| KR (1) | KR102128866B1 (enExample) |
| CN (1) | CN104271129A (enExample) |
| AU (1) | AU2013235275B2 (enExample) |
| CA (1) | CA2868024A1 (enExample) |
| EA (1) | EA036434B1 (enExample) |
| ES (1) | ES2746946T3 (enExample) |
| GE (1) | GEP20186900B (enExample) |
| IL (1) | IL234686B (enExample) |
| IN (1) | IN2014DN08477A (enExample) |
| JO (1) | JO3630B1 (enExample) |
| MA (1) | MA37438A1 (enExample) |
| MX (1) | MX358411B (enExample) |
| MY (1) | MY175225A (enExample) |
| NZ (1) | NZ700744A (enExample) |
| PH (1) | PH12014502109A1 (enExample) |
| SG (2) | SG10201607741RA (enExample) |
| TN (1) | TN2014000387A1 (enExample) |
| TW (1) | TWI649082B (enExample) |
| UA (1) | UA117455C2 (enExample) |
| WO (1) | WO2013142491A1 (enExample) |
| ZA (1) | ZA201407551B (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130303519A1 (en) | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
| CA2972076A1 (en) * | 2014-12-23 | 2016-06-30 | Millennium Pharmaceuticals, Inc. | Combination of raf inhibitors and aurora kinase inhibitors |
| EP3317427B1 (en) * | 2015-07-02 | 2020-12-23 | Millennium Pharmaceuticals, Inc. | Biomarkers of response to selective inhibitors of aurora a kinase |
| CN114681455A (zh) * | 2018-08-17 | 2022-07-01 | 深圳微芯生物科技股份有限公司 | 组蛋白去乙酰化酶抑制剂与蛋白激酶抑制剂之组合及其制药用途 |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4099012A (en) | 1975-08-28 | 1978-07-04 | Ciba-Geigy Corporation | 2-pyrazolyl-benzophenones |
| US4481142A (en) | 1979-02-07 | 1984-11-06 | Hoffmann-La Roche Inc. | Pyrimido-2-benzazepines |
| NZ192803A (en) | 1979-02-07 | 1984-08-24 | Hoffmann La Roche | Pyrimido-2-benzazepines and pharmaceutical compositions |
| US4469633A (en) | 1980-05-16 | 1984-09-04 | Hoffmann-La Roche Inc. | N-oxides of 5-oxo-1-phenyl-2-benzazepines |
| EP0273697A3 (en) | 1986-12-30 | 1989-11-29 | Merck & Co. Inc. | 2-benzazepines with 5- and 6- membered heterocyclic rings |
| US5166151A (en) | 1988-03-25 | 1992-11-24 | Merck & Co., Inc. | 2-Benzazepines with 5- and 6-membered heterocyclic rings, compositions and medical methods of use thereof |
| US5210082A (en) | 1991-05-16 | 1993-05-11 | Merck & Co., Inc. | 2-benzazepines with 5- and 6-membered heterocyclic rings to treat pain and anxiety disorders |
| US6096331A (en) | 1993-02-22 | 2000-08-01 | Vivorx Pharmaceuticals, Inc. | Methods and compositions useful for administration of chemotherapeutic agents |
| US5747487A (en) | 1993-07-29 | 1998-05-05 | American Cyanamid Company | Tricyclic benzazepine vasopressin antagonists |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| TW486480B (en) | 1996-03-08 | 2002-05-11 | Zeneca Ltd | Azolobenzazepine derivatives and compositions and method of use thereof |
| JP2001507349A (ja) | 1996-12-23 | 2001-06-05 | セルテック セラピューティックス リミテッド | 縮合多環式２−アミノピリミジン誘導体、それらの製造およびたんぱく質チロシンキナーゼ抑制因子としてのそれらの使用 |
| GB9713087D0 (en) | 1997-06-20 | 1997-08-27 | Celltech Therapeutics Ltd | Chemical compounds |
| KR100389140B1 (ko) | 1997-09-29 | 2003-06-25 | 메이지 세이카 가부시키가이샤 | 삼환성 트리아졸로벤즈아제핀 유도체 및 그의 제조방법 및항알레르기제 |
| US6277844B1 (en) | 1998-09-14 | 2001-08-21 | Sydney Spector | Compound for selective treatment of malignant cells by inhibiting cell cycle progression, decreasing Bcl2, and increasing apoptosis |
| US6417207B1 (en) | 1999-05-12 | 2002-07-09 | Nitromed, Inc. | Nitrosated and nitrosylated potassium channel activators, compositions and methods of use |
| US6638926B2 (en) | 2000-09-15 | 2003-10-28 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CA2432799C (en) | 2000-12-21 | 2008-08-19 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| SI20848A (sl) | 2001-03-14 | 2002-10-31 | Lek, Tovarna Farmacevtskih In Kemijskih Izdelkov, D.D. | Farmacevtska formulacija, ki vsebuje atorvastatin kalcij |
| US6686352B2 (en) | 2001-05-18 | 2004-02-03 | Hoffmann-La Roche Inc. | Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives |
| DE10135457A1 (de) | 2001-07-20 | 2003-02-06 | Adc Automotive Dist Control | Optische Sensoranordnung |
| AU2002328999B8 (en) | 2001-08-09 | 2008-06-05 | Actelion Pharmaceuticals Ltd. | Novel benzo-fused heterocycles as endothelin antagonists |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| EP1718303A4 (en) | 2004-02-10 | 2010-09-01 | Santarus Inc | COMBINATION OF INHIBITOR OF PROTON PUMP, BUFFER AND NON-STEROIDAL ANTI-INFLAMMATORY DRUG |
| HRP20080120T5 (hr) | 2004-05-14 | 2012-07-31 | Millennium@Pharmaceuticals | Spojevi i postupci za inhibiciju napredovanja mitoze s pomoću inhibicije aurora kinaze |
| CA2587427A1 (en) | 2004-11-17 | 2006-05-26 | Miikana Therapeutics, Inc. | Kinase inhibitors |
| JP2008526723A (ja) | 2004-12-30 | 2008-07-24 | アステックス、セラピューティックス、リミテッド | Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するピラゾール誘導体 |
| KR20080083680A (ko) | 2005-12-23 | 2008-09-18 | 스미스클라인 비참 코포레이션 | 오로라 키나제의 아자인돌 억제제 |
| JP2009523784A (ja) | 2006-01-16 | 2009-06-25 | ジュビラント・オルガノシス・リミテッド | 酸不安定化合物の安定な医薬製剤およびその製造方法 |
| US20070238716A1 (en) | 2006-03-14 | 2007-10-11 | Murthy Ayanampudi S R | Statin stabilizing dosage formulations |
| DE102006012301A1 (de) | 2006-03-15 | 2007-09-20 | Cemag-Anlagenbau-Dessau Gmbh | Herstellung von Zementklinker |
| EP2054413A2 (en) | 2006-08-09 | 2009-05-06 | Millennium Pharmaceuticals, Inc. | Pyridobenzazepine compounds and methods for inhibiting mitotic progression |
| CA2668267A1 (en) | 2006-10-31 | 2008-05-08 | Achillion Pharmaceuticals, Inc. | Elvucitabine pharmaceutical compositions |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| PE20081891A1 (es) | 2007-03-22 | 2008-12-27 | Opko Health Inc | Formulaciones de comprimidos que contienen sales de 8-[{1-(3,5-bis-(trifluorometil)fenil)-etoxi}-metil]-8-fenil-1,7-diaza-spiro[4.5]decan-2-ona y comprimidos elaborados a partir de estas |
| US20090203671A1 (en) | 2007-11-27 | 2009-08-13 | Abbott Laboratories | Method of treating cancer |
| WO2009114703A2 (en) * | 2008-03-12 | 2009-09-17 | Fox Chase Cancer Center | Combination therapy for the treatment of cancer |
| KR102080429B1 (ko) | 2008-06-26 | 2020-02-21 | 안테리오스, 인코퍼레이티드 | 경피 운반 |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| JO3434B1 (ar) | 2009-07-31 | 2019-10-20 | Millennium Pharm Inc | مركبات صيدلانية لمعالجة السرطان وامراض واضطرابات اخري |
| RU2012140021A (ru) * | 2010-02-19 | 2014-03-27 | Миллениум Фармасьютикалз, Инк. | КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 4-{[9-ХЛОР-7-(2-ФТОР-6-МЕТОКСИФЕНИЛ)-5Н-ПИРИМИДО[5,4-d][2]БЕНЗАЗЕПИН-2-ИЛ]АМИНО}-2-МЕТОКСИБЕНЗОАТА НАТРИЯ |
| US20130303519A1 (en) | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
-
2013
- 2013-03-14 US US13/804,570 patent/US20130303519A1/en not_active Abandoned
- 2013-03-18 JO JOP/2013/0075A patent/JO3630B1/ar active
- 2013-03-19 EP EP13714455.6A patent/EP2827855B1/en active Active
- 2013-03-19 AU AU2013235275A patent/AU2013235275B2/en active Active
- 2013-03-19 NZ NZ700744A patent/NZ700744A/en not_active IP Right Cessation
- 2013-03-19 MX MX2014011324A patent/MX358411B/es active IP Right Grant
- 2013-03-19 CN CN201380015806.1A patent/CN104271129A/zh active Pending
- 2013-03-19 JP JP2015501852A patent/JP6373252B2/ja active Active
- 2013-03-19 CA CA2868024A patent/CA2868024A1/en not_active Abandoned
- 2013-03-19 EA EA201491727A patent/EA036434B1/ru not_active IP Right Cessation
- 2013-03-19 MA MA37438A patent/MA37438A1/fr unknown
- 2013-03-19 IN IN8477DEN2014 patent/IN2014DN08477A/en unknown
- 2013-03-19 SG SG10201607741RA patent/SG10201607741RA/en unknown
- 2013-03-19 SG SG11201405621UA patent/SG11201405621UA/en unknown
- 2013-03-19 UA UAA201411324A patent/UA117455C2/uk unknown
- 2013-03-19 MY MYPI2014702635A patent/MY175225A/en unknown
- 2013-03-19 KR KR1020147028776A patent/KR102128866B1/ko active Active
- 2013-03-19 GE GEAP201313599A patent/GEP20186900B/en unknown
- 2013-03-19 ES ES13714455T patent/ES2746946T3/es active Active
- 2013-03-19 WO PCT/US2013/032962 patent/WO2013142491A1/en not_active Ceased
- 2013-03-20 TW TW102109912A patent/TWI649082B/zh active
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2014
- 2014-09-15 TN TNP2014000387A patent/TN2014000387A1/fr unknown
- 2014-09-16 IL IL234686A patent/IL234686B/en active IP Right Grant
- 2014-09-22 PH PH12014502109A patent/PH12014502109A1/en unknown
- 2014-10-17 ZA ZA2014/07551A patent/ZA201407551B/en unknown
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2015
- 2015-09-03 US US14/844,270 patent/US10213436B2/en active Active
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