ES2549327T3 - Derivados de pirimidilaminobenzamida para el tratamiento de la neurofibromatosis - Google Patents
Derivados de pirimidilaminobenzamida para el tratamiento de la neurofibromatosis Download PDFInfo
- Publication number
- ES2549327T3 ES2549327T3 ES10150521.2T ES10150521T ES2549327T3 ES 2549327 T3 ES2549327 T3 ES 2549327T3 ES 10150521 T ES10150521 T ES 10150521T ES 2549327 T3 ES2549327 T3 ES 2549327T3
- Authority
- ES
- Spain
- Prior art keywords
- treatment
- neurofibromatosis
- pyrimidylaminobenzamide derivatives
- formula
- brain tumors
- 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
- 208000009905 Neurofibromatoses Diseases 0.000 title 1
- 201000004931 neurofibromatosis Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 9
- 208000003174 Brain Neoplasms Diseases 0.000 abstract description 7
- 238000000034 method Methods 0.000 abstract description 4
- 150000003839 salts Chemical class 0.000 abstract description 3
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 102000007517 Neurofibromin 2 Human genes 0.000 abstract 1
- 108010085839 Neurofibromin 2 Proteins 0.000 abstract 1
- 208000002761 neurofibromatosis 2 Diseases 0.000 abstract 1
- 208000022032 neurofibromatosis type 2 Diseases 0.000 abstract 1
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 102000004169 proteins and genes Human genes 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 3
- 241000700605 Viruses Species 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000012528 membrane Substances 0.000 description 3
- 235000011007 phosphoric acid Nutrition 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 241000288906 Primates Species 0.000 description 2
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- YBYRMVIVWMBXKQ-UHFFFAOYSA-N phenylmethanesulfonyl fluoride Chemical compound FS(=O)(=O)CC1=CC=CC=C1 YBYRMVIVWMBXKQ-UHFFFAOYSA-N 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 230000000069 prophylactic effect Effects 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- HTSGKJQDMSTCGS-UHFFFAOYSA-N 1,4-bis(4-chlorophenyl)-2-(4-methylphenyl)sulfonylbutane-1,4-dione Chemical compound C1=CC(C)=CC=C1S(=O)(=O)C(C(=O)C=1C=CC(Cl)=CC=1)CC(=O)C1=CC=C(Cl)C=C1 HTSGKJQDMSTCGS-UHFFFAOYSA-N 0.000 description 1
- 206010061818 Disease progression Diseases 0.000 description 1
- 108010024636 Glutathione Proteins 0.000 description 1
- 229910021380 Manganese Chloride Inorganic materials 0.000 description 1
- GLFNIEUTAYBVOC-UHFFFAOYSA-L Manganese chloride Chemical compound Cl[Mn]Cl GLFNIEUTAYBVOC-UHFFFAOYSA-L 0.000 description 1
- SQJSKIXMQGHTHI-UHFFFAOYSA-N N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]benzamide Chemical compound CC=1N=CN(C=1)C=1C=C(C=C(C=1)C(F)(F)F)NC(C1=CC=CC=C1)=O SQJSKIXMQGHTHI-UHFFFAOYSA-N 0.000 description 1
- 229910020700 Na3VO4 Inorganic materials 0.000 description 1
- 239000002033 PVDF binder Substances 0.000 description 1
- 229920002684 Sepharose Polymers 0.000 description 1
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 208000013355 benign neoplasm of brain Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 239000013592 cell lysate Substances 0.000 description 1
- 230000005750 disease progression Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 108020001507 fusion proteins Proteins 0.000 description 1
- 102000037865 fusion proteins Human genes 0.000 description 1
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 230000002601 intratumoral effect Effects 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 239000012139 lysis buffer Substances 0.000 description 1
- 229910001629 magnesium chloride Inorganic materials 0.000 description 1
- 239000011565 manganese chloride Substances 0.000 description 1
- 235000002867 manganese chloride Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 229920002981 polyvinylidene fluoride Polymers 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 239000013049 sediment Substances 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- IHIXIJGXTJIKRB-UHFFFAOYSA-N trisodium vanadate Chemical compound [Na+].[Na+].[Na+].[O-][V]([O-])([O-])=O IHIXIJGXTJIKRB-UHFFFAOYSA-N 0.000 description 1
- 241000701447 unidentified baculovirus Species 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74278105P | 2005-12-06 | 2005-12-06 | |
| US742781P | 2005-12-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2549327T3 true ES2549327T3 (es) | 2015-10-27 |
Family
ID=37831665
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10150521.2T Active ES2549327T3 (es) | 2005-12-06 | 2006-12-05 | Derivados de pirimidilaminobenzamida para el tratamiento de la neurofibromatosis |
| ES06830381T Active ES2391199T3 (es) | 2005-12-06 | 2006-12-05 | Derivados de pirimidilaminobenzamida para el tratamiento de neurofibromatosis |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES06830381T Active ES2391199T3 (es) | 2005-12-06 | 2006-12-05 | Derivados de pirimidilaminobenzamida para el tratamiento de neurofibromatosis |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US20080318988A1 (enExample) |
| EP (2) | EP1959957B1 (enExample) |
| JP (4) | JP2009518358A (enExample) |
| KR (2) | KR101498848B1 (enExample) |
| CN (1) | CN101321532B (enExample) |
| AU (1) | AU2006323992B2 (enExample) |
| BR (1) | BRPI0619416A2 (enExample) |
| CA (1) | CA2629132C (enExample) |
| ES (2) | ES2549327T3 (enExample) |
| PL (1) | PL1959957T3 (enExample) |
| PT (1) | PT1959957E (enExample) |
| RU (1) | RU2450814C2 (enExample) |
| WO (1) | WO2007065898A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2450814C2 (ru) * | 2005-12-06 | 2012-05-20 | Новартис Аг | Производные пиримидиламинобензамида, предназначенные для лечения нейрофиброматоза |
| US8242271B2 (en) | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| WO2009158447A2 (en) * | 2008-06-27 | 2009-12-30 | Indiana University Research And Technology Corporation | Materials and methods for suppressing and/or treating neurofibroma and related tumors |
| KR20110053354A (ko) * | 2008-08-13 | 2011-05-20 | 노파르티스 아게 | 폐동맥 고혈압의 치료 |
| EP2186514B1 (en) | 2008-11-14 | 2016-06-29 | Kinki University | Treatment of Malignant Peripheral Nerve Sheath Tumors |
| BR112012009094A8 (pt) * | 2009-10-23 | 2017-10-10 | Novartis Ag | método de tratamento de transtornos proliferativos e outras condições patológicas mediadas por bcr-abl, c-kit, ddr1,ddr2 ou atividade pdgf-r quinase |
| JP7230817B2 (ja) | 2017-10-03 | 2023-03-01 | 凸版印刷株式会社 | 超音波シール用アンビル及び超音波シール装置 |
| TWI787523B (zh) | 2018-06-15 | 2022-12-21 | 漢達生技醫藥股份有限公司 | 達沙替尼十二烷基硫酸鹽之結晶 |
| WO2026035611A1 (en) * | 2024-08-05 | 2026-02-12 | Amo Pharma Ltd | Methods of treating neurofibromatosis using farnesyl dibenzodiazepinones |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0215676D0 (en) * | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| GB0325031D0 (en) | 2003-10-27 | 2003-12-03 | Novartis Ag | Organic compounds |
| SI1686997T1 (sl) * | 2003-11-18 | 2009-08-31 | Novartis Ag | Inhibitorji mutantne oblike KIT |
| PT1843771E (pt) * | 2005-01-28 | 2011-12-02 | Novartis Ag | Uso de pirimidilaminobenzamidas para o tratamento de doenças que respondem à modulação da atividade da cinase tie-2 |
| RU2450814C2 (ru) * | 2005-12-06 | 2012-05-20 | Новартис Аг | Производные пиримидиламинобензамида, предназначенные для лечения нейрофиброматоза |
-
2006
- 2006-12-05 RU RU2008127264/15A patent/RU2450814C2/ru not_active IP Right Cessation
- 2006-12-05 ES ES10150521.2T patent/ES2549327T3/es active Active
- 2006-12-05 CN CN2006800456624A patent/CN101321532B/zh not_active Expired - Fee Related
- 2006-12-05 PT PT06830381T patent/PT1959957E/pt unknown
- 2006-12-05 AU AU2006323992A patent/AU2006323992B2/en not_active Ceased
- 2006-12-05 BR BRPI0619416-8A patent/BRPI0619416A2/pt active Search and Examination
- 2006-12-05 WO PCT/EP2006/069335 patent/WO2007065898A1/en not_active Ceased
- 2006-12-05 EP EP06830381A patent/EP1959957B1/en not_active Not-in-force
- 2006-12-05 ES ES06830381T patent/ES2391199T3/es active Active
- 2006-12-05 JP JP2008543819A patent/JP2009518358A/ja not_active Withdrawn
- 2006-12-05 KR KR1020137034055A patent/KR101498848B1/ko not_active Expired - Fee Related
- 2006-12-05 PL PL06830381T patent/PL1959957T3/pl unknown
- 2006-12-05 CA CA2629132A patent/CA2629132C/en not_active Expired - Fee Related
- 2006-12-05 KR KR1020087013614A patent/KR101413387B1/ko not_active Expired - Fee Related
- 2006-12-05 EP EP10150521.2A patent/EP2177222B1/en not_active Not-in-force
- 2006-12-06 US US12/095,956 patent/US20080318988A1/en not_active Abandoned
-
2010
- 2010-03-24 US US12/730,590 patent/US20100234408A1/en not_active Abandoned
-
2012
- 2012-12-05 US US13/706,249 patent/US8604045B2/en not_active Expired - Fee Related
-
2013
- 2013-02-04 JP JP2013019700A patent/JP2013107893A/ja not_active Withdrawn
- 2013-11-08 US US14/075,256 patent/US20140073660A1/en not_active Abandoned
-
2014
- 2014-11-28 JP JP2014240970A patent/JP2015091818A/ja not_active Withdrawn
-
2017
- 2017-05-16 JP JP2017097077A patent/JP2017193553A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0619416A2 (pt) | 2011-10-04 |
| CN101321532A (zh) | 2008-12-10 |
| US20140073660A1 (en) | 2014-03-13 |
| JP2017193553A (ja) | 2017-10-26 |
| KR20080077973A (ko) | 2008-08-26 |
| PT1959957E (pt) | 2012-10-29 |
| PL1959957T3 (pl) | 2012-12-31 |
| KR101498848B1 (ko) | 2015-03-05 |
| KR101413387B1 (ko) | 2014-06-27 |
| RU2450814C2 (ru) | 2012-05-20 |
| ES2391199T3 (es) | 2012-11-22 |
| EP2177222B1 (en) | 2015-07-15 |
| CA2629132C (en) | 2014-05-27 |
| EP1959957B1 (en) | 2012-07-18 |
| US20080318988A1 (en) | 2008-12-25 |
| EP1959957A1 (en) | 2008-08-27 |
| AU2006323992A1 (en) | 2007-06-14 |
| KR20140022431A (ko) | 2014-02-24 |
| CA2629132A1 (en) | 2007-06-14 |
| JP2015091818A (ja) | 2015-05-14 |
| EP2177222A1 (en) | 2010-04-21 |
| RU2008127264A (ru) | 2010-01-20 |
| WO2007065898A1 (en) | 2007-06-14 |
| US20100234408A1 (en) | 2010-09-16 |
| JP2009518358A (ja) | 2009-05-07 |
| AU2006323992B2 (en) | 2010-07-08 |
| CN101321532B (zh) | 2011-06-29 |
| US8604045B2 (en) | 2013-12-10 |
| US20130123290A1 (en) | 2013-05-16 |
| JP2013107893A (ja) | 2013-06-06 |
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