BR112018073951A2 - forma cristalina inovadora de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)-benzamida - Google Patents
forma cristalina inovadora de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)-benzamidaInfo
- Publication number
- BR112018073951A2 BR112018073951A2 BR112018073951A BR112018073951A BR112018073951A2 BR 112018073951 A2 BR112018073951 A2 BR 112018073951A2 BR 112018073951 A BR112018073951 A BR 112018073951A BR 112018073951 A BR112018073951 A BR 112018073951A BR 112018073951 A2 BR112018073951 A2 BR 112018073951A2
- Authority
- BR
- Brazil
- Prior art keywords
- indazol
- ylamino
- piperazin
- benzamide
- pyran
- Prior art date
Links
- HAYYBYPASCDWEQ-UHFFFAOYSA-N n-[5-[(3,5-difluorophenyl)methyl]-1h-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide Chemical compound C1CN(C)CCN1C(C=C1NC2CCOCC2)=CC=C1C(=O)NC(C1=C2)=NNC1=CC=C2CC1=CC(F)=CC(F)=C1 HAYYBYPASCDWEQ-UHFFFAOYSA-N 0.000 title abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
a presente invenção se refere a uma forma cristalina inovadora de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)-benzamida, processo para sua preparação, sua utilidade no tratamento de doenças causadas por atividade de proteína quinase desregulada e composições farmacêuticas que contêm a mesma.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662340797P | 2016-05-24 | 2016-05-24 | |
PCT/EP2017/061919 WO2017202674A1 (en) | 2016-05-24 | 2017-05-18 | New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112018073951A2 true BR112018073951A2 (pt) | 2019-02-26 |
Family
ID=58709993
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018073951A BR112018073951A2 (pt) | 2016-05-24 | 2017-05-18 | forma cristalina inovadora de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)-benzamida |
Country Status (14)
Country | Link |
---|---|
US (2) | US10738037B2 (pt) |
EP (2) | EP3464276B1 (pt) |
JP (2) | JP7094228B2 (pt) |
KR (1) | KR102441736B1 (pt) |
CN (1) | CN109153669B (pt) |
AU (1) | AU2017271458B2 (pt) |
BR (1) | BR112018073951A2 (pt) |
CA (1) | CA3024208C (pt) |
ES (1) | ES2899953T3 (pt) |
HK (1) | HK1259405A1 (pt) |
IL (1) | IL263004B (pt) |
MX (1) | MX2018014298A (pt) |
PL (1) | PL3464276T3 (pt) |
WO (1) | WO2017202674A1 (pt) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2899953T3 (es) * | 2016-05-24 | 2022-03-15 | Nerviano Medical Sciences Srl | Nueva forma cristalina de n-[5-(3,5-difluoro-bencil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida |
AU2020319662B2 (en) | 2019-07-31 | 2024-02-29 | F. Hoffmann-La Roche Ag | New pharmaceutical formulation |
US20220372024A1 (en) * | 2019-11-01 | 2022-11-24 | Johnson Matthey Public Limited Company | Crystalline forms of entrectinib |
CN113024521B (zh) * | 2019-12-09 | 2023-01-17 | 武汉九州钰民医药科技有限公司 | 一种制备恩曲替尼的方法 |
CN111171009B (zh) * | 2020-01-10 | 2022-07-12 | 安礼特(上海)医药科技有限公司 | 恩曲替尼晶型及其制备方法 |
CN113801062B (zh) * | 2020-06-15 | 2023-05-26 | 沈阳药科大学 | 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法 |
CN112336723B (zh) * | 2020-12-11 | 2023-09-26 | 江南大学 | 制备用于降低trpv4与nox2耦联度的药物的方法 |
EP4273144A1 (en) * | 2021-02-03 | 2023-11-08 | Qilu Pharmaceutical Co., Ltd. | Crystal form of entrectinib and preparation method therefor |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5506674B2 (ja) * | 2007-07-20 | 2014-05-28 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性な置換インダゾール誘導体 |
RU2602071C2 (ru) * | 2012-05-23 | 2016-11-10 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Способ получения n-[5-(3,5-дифторбензил)-1н-индазол-3-ил]-4-(4-метилпиперазин-1-ил)-2-(тетрагидропиран-4-иламино)бензамида |
TWI672141B (zh) * | 2014-02-20 | 2019-09-21 | 美商醫科泰生技 | 投予ros1突變癌細胞之分子 |
ES2899953T3 (es) | 2016-05-24 | 2022-03-15 | Nerviano Medical Sciences Srl | Nueva forma cristalina de n-[5-(3,5-difluoro-bencil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida |
-
2017
- 2017-05-18 ES ES17724052T patent/ES2899953T3/es active Active
- 2017-05-18 CN CN201780031576.6A patent/CN109153669B/zh active Active
- 2017-05-18 PL PL17724052T patent/PL3464276T3/pl unknown
- 2017-05-18 US US16/301,826 patent/US10738037B2/en active Active
- 2017-05-18 AU AU2017271458A patent/AU2017271458B2/en active Active
- 2017-05-18 CA CA3024208A patent/CA3024208C/en active Active
- 2017-05-18 JP JP2018561474A patent/JP7094228B2/ja active Active
- 2017-05-18 MX MX2018014298A patent/MX2018014298A/es unknown
- 2017-05-18 BR BR112018073951A patent/BR112018073951A2/pt active Search and Examination
- 2017-05-18 WO PCT/EP2017/061919 patent/WO2017202674A1/en unknown
- 2017-05-18 EP EP17724052.0A patent/EP3464276B1/en active Active
- 2017-05-18 KR KR1020187037182A patent/KR102441736B1/ko active IP Right Grant
- 2017-05-18 EP EP21188238.6A patent/EP3967689A1/en not_active Withdrawn
-
2018
- 2018-11-14 IL IL263004A patent/IL263004B/en unknown
-
2019
- 2019-01-31 HK HK19101774.9A patent/HK1259405A1/zh unknown
-
2020
- 2020-06-26 US US16/912,965 patent/US11091469B2/en active Active
- 2020-11-06 JP JP2020185594A patent/JP7154271B2/ja active Active
Also Published As
Publication number | Publication date |
---|---|
US11091469B2 (en) | 2021-08-17 |
EP3464276B1 (en) | 2021-09-01 |
MX2018014298A (es) | 2019-03-14 |
JP2021042213A (ja) | 2021-03-18 |
AU2017271458A1 (en) | 2019-01-17 |
ES2899953T3 (es) | 2022-03-15 |
US10738037B2 (en) | 2020-08-11 |
WO2017202674A1 (en) | 2017-11-30 |
US20190169173A1 (en) | 2019-06-06 |
US20200325122A1 (en) | 2020-10-15 |
KR102441736B1 (ko) | 2022-09-13 |
PL3464276T3 (pl) | 2022-04-04 |
JP2019516749A (ja) | 2019-06-20 |
JP7154271B2 (ja) | 2022-10-17 |
HK1259405A1 (zh) | 2019-11-29 |
CA3024208C (en) | 2022-07-26 |
AU2017271458B2 (en) | 2020-11-26 |
CA3024208A1 (en) | 2017-11-30 |
IL263004B (en) | 2022-04-01 |
IL263004A (en) | 2018-12-31 |
KR20190005236A (ko) | 2019-01-15 |
JP7094228B2 (ja) | 2022-07-01 |
CN109153669B (zh) | 2021-12-24 |
EP3967689A1 (en) | 2022-03-16 |
CN109153669A (zh) | 2019-01-04 |
EP3464276A1 (en) | 2019-04-10 |
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B09A | Decision: intention to grant [chapter 9.1 patent gazette] |