JP2012508239A - Ｐ７０ｓ６キナーゼ阻害剤およびｍｔｏｒ阻害剤の併用療法 - Google Patents
Ｐ７０ｓ６キナーゼ阻害剤およびｍｔｏｒ阻害剤の併用療法 Download PDFInfo
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- JP2012508239A JP2012508239A JP2011535632A JP2011535632A JP2012508239A JP 2012508239 A JP2012508239 A JP 2012508239A JP 2011535632 A JP2011535632 A JP 2011535632A JP 2011535632 A JP2011535632 A JP 2011535632A JP 2012508239 A JP2012508239 A JP 2012508239A
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- cancer
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- trifluoromethyl
- phenyl
- imidazol
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- HKVAMNSJSFKALM-CPXURSODSA-N everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)\C(C)=C\C=C\C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-CPXURSODSA-N 0.000 description 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 description 1
- 239000012065 filter cake Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 235000010299 hexamethylene tetramine Nutrition 0.000 description 1
- VKYKSIONXSXAKP-UHFFFAOYSA-N hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 150000002678 macrocyclic compounds Chemical class 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 108010082117 matrigel Proteins 0.000 description 1
- 229960004011 methenamine Drugs 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000002297 mitogenic effect Effects 0.000 description 1
- 230000014399 negative regulation of angiogenesis Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 238000001243 protein synthesis Methods 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- IDXKTTNFXPPXJY-UHFFFAOYSA-N pyrimidin-1-ium;chloride Chemical compound Cl.C1=CN=CN=C1 IDXKTTNFXPPXJY-UHFFFAOYSA-N 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 230000022983 regulation of cell cycle Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 229960001302 ridaforolimus Drugs 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
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- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P35/02—Antineoplastic agents specific for leukemia
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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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
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- Epidemiology (AREA)
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- Endocrinology (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11327908P | 2008-11-11 | 2008-11-11 | |
| US61/113,279 | 2008-11-11 | ||
| PCT/US2009/063188 WO2010056574A1 (en) | 2008-11-11 | 2009-11-04 | P70 s6 kinase inhibitor and mtor inhibitor combination therapy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508239A true JP2012508239A (ja) | 2012-04-05 |
| JP2012508239A5 JP2012508239A5 (OSRAM) | 2012-12-20 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535632A Withdrawn JP2012508239A (ja) | 2008-11-11 | 2009-11-04 | Ｐ７０ｓ６キナーゼ阻害剤およびｍｔｏｒ阻害剤の併用療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20110212977A1 (OSRAM) |
| EP (1) | EP2355820A1 (OSRAM) |
| JP (1) | JP2012508239A (OSRAM) |
| KR (1) | KR20110075014A (OSRAM) |
| CN (1) | CN102209539B (OSRAM) |
| AU (1) | AU2009314335B2 (OSRAM) |
| BR (1) | BRPI0921840A2 (OSRAM) |
| CA (1) | CA2743242A1 (OSRAM) |
| EA (1) | EA018824B1 (OSRAM) |
| MX (1) | MX2011005003A (OSRAM) |
| WO (1) | WO2010056574A1 (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023507188A (ja) * | 2019-12-19 | 2023-02-21 | インペリアル・カレッジ・イノベーションズ・リミテッド | 白金耐性がんの治療に有用な１ｈ－ピラゾロ［３，４－ｄ］ピリミジン化合物 |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140378500A1 (en) * | 2012-02-01 | 2014-12-25 | 20/20 Gene Systems, Inc. | Methods for predicting tumor reponse to targeted therapies |
| SG11201505999VA (en) * | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108861A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US20230061319A1 (en) * | 2020-01-10 | 2023-03-02 | Coimmune, Inc. | Methods of treating tumors |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA83484C2 (uk) * | 2003-03-05 | 2008-07-25 | Уайт | Спосіб лікування раку грудей комбінацією похідного рапаміцину і інгібітора ароматази - летрозолу, фармацевтична композиція |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| US7994172B2 (en) * | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| WO2007047754A2 (en) * | 2005-10-18 | 2007-04-26 | George Mason Intellectual Properties, Inc. | Mtor pathway theranostic |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
-
2009
- 2009-11-04 WO PCT/US2009/063188 patent/WO2010056574A1/en not_active Ceased
- 2009-11-04 EA EA201170681A patent/EA018824B1/ru not_active IP Right Cessation
- 2009-11-04 KR KR1020117010616A patent/KR20110075014A/ko not_active Abandoned
- 2009-11-04 AU AU2009314335A patent/AU2009314335B2/en not_active Expired - Fee Related
- 2009-11-04 BR BRPI0921840A patent/BRPI0921840A2/pt not_active IP Right Cessation
- 2009-11-04 CA CA2743242A patent/CA2743242A1/en not_active Abandoned
- 2009-11-04 MX MX2011005003A patent/MX2011005003A/es not_active Application Discontinuation
- 2009-11-04 US US13/126,489 patent/US20110212977A1/en not_active Abandoned
- 2009-11-04 CN CN2009801449528A patent/CN102209539B/zh not_active Expired - Fee Related
- 2009-11-04 JP JP2011535632A patent/JP2012508239A/ja not_active Withdrawn
- 2009-11-04 EP EP09752048A patent/EP2355820A1/en not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023507188A (ja) * | 2019-12-19 | 2023-02-21 | インペリアル・カレッジ・イノベーションズ・リミテッド | 白金耐性がんの治療に有用な１ｈ－ピラゾロ［３，４－ｄ］ピリミジン化合物 |
| JP7740804B2 (ja) | 2019-12-19 | 2025-09-17 | インペリアル・カレッジ・イノベーションズ・リミテッド | 白金耐性がんの治療に有用な１ｈ－ピラゾロ［３，４－ｄ］ピリミジン化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20110212977A1 (en) | 2011-09-01 |
| CN102209539A (zh) | 2011-10-05 |
| BRPI0921840A2 (pt) | 2018-10-09 |
| AU2009314335B2 (en) | 2013-09-12 |
| AU2009314335A1 (en) | 2010-05-20 |
| CA2743242A1 (en) | 2010-05-20 |
| EA201170681A1 (ru) | 2011-10-31 |
| WO2010056574A1 (en) | 2010-05-20 |
| KR20110075014A (ko) | 2011-07-05 |
| CN102209539B (zh) | 2013-06-12 |
| MX2011005003A (es) | 2011-05-25 |
| EA018824B1 (ru) | 2013-10-30 |
| EP2355820A1 (en) | 2011-08-17 |
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