BR112018071498A2 - novas formas em sal cristalino de 3-(1,2,4-triazol [4,3-a]piridina-3-iletinil)-4-metil-n-(4-((4-metilpiperazin-1- il)metil)-3-trifluorometilfenil)benzamida para aplicação médica - Google Patents
novas formas em sal cristalino de 3-(1,2,4-triazol [4,3-a]piridina-3-iletinil)-4-metil-n-(4-((4-metilpiperazin-1- il)metil)-3-trifluorometilfenil)benzamida para aplicação médicaInfo
- Publication number
- BR112018071498A2 BR112018071498A2 BR112018071498-4A BR112018071498A BR112018071498A2 BR 112018071498 A2 BR112018071498 A2 BR 112018071498A2 BR 112018071498 A BR112018071498 A BR 112018071498A BR 112018071498 A2 BR112018071498 A2 BR 112018071498A2
- Authority
- BR
- Brazil
- Prior art keywords
- methyl
- leukemia
- salt
- ylethynyl
- methylpiperazin
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 5
- -1 pyridin-3-ylethynyl Chemical group 0.000 title abstract 3
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 title abstract 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 title 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 3
- 108060006633 protein kinase Proteins 0.000 abstract 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 208000032839 leukemia Diseases 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 abstract 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 abstract 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 abstract 1
- 208000031295 Animal disease Diseases 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 abstract 1
- 206010025323 Lymphomas Diseases 0.000 abstract 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 abstract 1
- 229940098779 methanesulfonic acid Drugs 0.000 abstract 1
- 238000012986 modification Methods 0.000 abstract 1
- 230000004048 modification Effects 0.000 abstract 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical 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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
a invenção refere-se à química orgânica, farmacologia e medicina e trata da prevenção e tratamento de doenças humanas e animais associadas à interrupção na atividade de várias quinases, em particular abl quinase, por exemplo, doenças tais como leucemia, leucemia mieloide aguda, leucemia mieloide crônica, leucemia linfocítica aguda, câncer de mama, câncer de pulmão de células não pequenas, tumores estromais gastrointestinais, câncer de ovário, linfoma, usando uma nova forma em sal de 3-(1,2,4-triazol[4,3-a]piridina-3-iletinil)-4-metil-n-(4-((4-metilpiperazin-1-il)metil)-3-trifluorometilfenil)benzamida. o sal desse composto com ácido metanossulfônico, fórmula (i), ou seu hidrato, solvato, bem como modificações polimórficas, têm a capacidade de inibir a atividade de quinases, em particular de ab1 quinases. a presente invenção também se refere a composições farmacêuticas que compreendem uma quantidade terapeuticamente eficaz de um sal da invenção, a método para preparar um sal cristalino da invenção, bem como a método para tratar doenças oncológicas em paciente.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2016114904 | 2016-04-18 | ||
| RU2016114904A RU2652992C2 (ru) | 2016-04-18 | 2016-04-18 | Новая кристаллическая солевая форма 3-(1,2,4-триазоло[4,3-а]пиридин-3-илэтинил)-4-метил-n-(4-((4-метилпиперазин-1-ил)метил)-3-трифторметилфенил)бензамида для медицинского применения |
| PCT/RU2017/050025 WO2017184032A1 (en) | 2016-04-18 | 2017-04-18 | Novel crystalline salt forms of 3-(1,2,4-triazolo[4,3-a]pyridine-3-ylethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-trifluoromethylphenyl)benzamide for medical application |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112018071498A2 true BR112018071498A2 (pt) | 2019-02-19 |
| BR112018071498B1 BR112018071498B1 (pt) | 2024-08-06 |
Family
ID=
Also Published As
| Publication number | Publication date |
|---|---|
| MX389229B (es) | 2025-03-20 |
| RU2016114904A (ru) | 2017-10-23 |
| JP6463874B2 (ja) | 2019-02-06 |
| JP2018530598A (ja) | 2018-10-18 |
| IL262368A (en) | 2018-11-29 |
| EP3445763A4 (en) | 2019-12-04 |
| RU2652992C2 (ru) | 2018-05-04 |
| EA032865B1 (ru) | 2019-07-31 |
| CN108473492B (zh) | 2020-01-07 |
| CA3021306C (en) | 2023-05-16 |
| EP3445763A1 (en) | 2019-02-27 |
| CA3021306A1 (en) | 2017-10-26 |
| US11225474B2 (en) | 2022-01-18 |
| ES2906048T3 (es) | 2022-04-13 |
| WO2017184032A1 (en) | 2017-10-26 |
| DK3445763T3 (da) | 2022-01-31 |
| UA124627C2 (uk) | 2021-10-20 |
| CN108473492A (zh) | 2018-08-31 |
| KR20180037289A (ko) | 2018-04-11 |
| AU2017254345A1 (en) | 2018-11-22 |
| EA201600487A1 (ru) | 2017-10-31 |
| US20200325131A1 (en) | 2020-10-15 |
| HK1254731A1 (zh) | 2019-07-26 |
| PL3445763T3 (pl) | 2022-02-28 |
| EP3445763B1 (en) | 2021-11-10 |
| KR101929725B1 (ko) | 2018-12-14 |
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| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
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