BR112017021075A2 - Formas cristalinas de maleato de 1-((2r,4r)-2-(1h- benzo[d]imidazol-2-il)-1-metilpiperidin-4-il)-3-(4-ciano fenil)ureia - Google Patents
Formas cristalinas de maleato de 1-((2r,4r)-2-(1h- benzo[d]imidazol-2-il)-1-metilpiperidin-4-il)-3-(4-ciano fenil)ureiaInfo
- Publication number
- BR112017021075A2 BR112017021075A2 BR112017021075-4A BR112017021075A BR112017021075A2 BR 112017021075 A2 BR112017021075 A2 BR 112017021075A2 BR 112017021075 A BR112017021075 A BR 112017021075A BR 112017021075 A2 BR112017021075 A2 BR 112017021075A2
- Authority
- BR
- Brazil
- Prior art keywords
- crystalline forms
- imidazol
- benzo
- urea
- methylipiperidin
- Prior art date
Links
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 title 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- SFNSLLSYNZWZQG-VQIMIIECSA-N glasdegib Chemical compound N([C@@H]1CCN([C@H](C1)C=1NC2=CC=CC=C2N=1)C)C(=O)NC1=CC=C(C#N)C=C1 SFNSLLSYNZWZQG-VQIMIIECSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000012450 pharmaceutical intermediate Substances 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
a presente invenção refere-se a uma forma cristalina de maleato de 1-((2r,4r)-2-(1h-benzo[d]imidazol-2-il)-1-metilpiperidin-4-il)-3-(4-ciano fenil)ureia, e a suas composições farmacêuticas, a inter-mediários e métodos para a produção e isolamento de tais formas cris-talinas e composições, e a métodos de uso de tais formas cristalinas e composições no tratamento de crescimento anormal de células em mamíferos, especialmente humanos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562152108P | 2015-04-24 | 2015-04-24 | |
| US62/152,108 | 2015-04-24 | ||
| PCT/IB2016/052107 WO2016170451A1 (en) | 2015-04-24 | 2016-04-13 | Crystalline forms of 1-((2r,4r)-2-(1h-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112017021075A2 true BR112017021075A2 (pt) | 2018-07-03 |
| BR112017021075B1 BR112017021075B1 (pt) | 2021-08-03 |
Family
ID=55806563
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017021075-4A BR112017021075B1 (pt) | 2015-04-24 | 2016-04-13 | Forma cristalina de maleato de 1-((2r,4r)-2-(1h- benzo[d]imidazol-2-il)-1-metilpiperidin-4-il)-3-(4- cianofenil)ureia e composição farmacêutica |
Country Status (24)
| Country | Link |
|---|---|
| US (4) | US10414748B2 (pt) |
| EP (2) | EP3286176B1 (pt) |
| JP (1) | JP6345728B2 (pt) |
| KR (2) | KR20190038677A (pt) |
| CN (1) | CN107531667A (pt) |
| AR (1) | AR104391A1 (pt) |
| AU (1) | AU2016251940C1 (pt) |
| BR (1) | BR112017021075B1 (pt) |
| CA (2) | CA2983387C (pt) |
| CY (1) | CY1124056T1 (pt) |
| DK (2) | DK3666768T3 (pt) |
| ES (2) | ES2923593T3 (pt) |
| HK (1) | HK1243416A1 (pt) |
| HU (2) | HUE048664T2 (pt) |
| IL (1) | IL255224B (pt) |
| MX (1) | MX2017013645A (pt) |
| PL (2) | PL3666768T3 (pt) |
| PT (2) | PT3666768T (pt) |
| RU (1) | RU2717564C2 (pt) |
| SG (1) | SG11201707863QA (pt) |
| SI (2) | SI3666768T1 (pt) |
| TW (1) | TWI646093B (pt) |
| WO (1) | WO2016170451A1 (pt) |
| ZA (1) | ZA201706391B (pt) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190038677A (ko) * | 2015-04-24 | 2019-04-08 | 화이자 인코포레이티드 | 1-((2r,4r)-2-(1h-벤조[d]이미다졸-2-일)-1-메틸피페리딘-4-일)-3-(4-시아노페닐)우레아 말레에이트의 결정질 형태 |
| HRP20240302T1 (hr) | 2020-01-28 | 2024-05-10 | Assia Chemical Industries Ltd | Postupci za pripremu glasdegiba i njegove soli i krutih oblika glasdegib maleata i postupak za njihovu pripremu |
| EP4126237B1 (en) | 2020-03-26 | 2024-04-10 | LEK Pharmaceuticals d.d. | Dimaleate form of 1-((2r,4r)-2-(1h-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea |
| WO2023002362A1 (en) | 2021-07-22 | 2023-01-26 | Pfizer Inc. | Treatment of hematological malignancy |
| WO2023017541A1 (en) * | 2021-08-12 | 2023-02-16 | Msn Laboratories Private Limited, R&D Center | Improved process for the preparation of 1-((2r,4r)-2-(1h-benzo[d]imidazol-2-yl)-1-methyl piperidin-4-yl)-3-(4-cyanophenyl)urea maleate |
| CN114668849B (zh) * | 2021-12-31 | 2024-01-23 | 中国人民解放军军事科学院军事医学研究院 | Shh通路调控生物节律及其相关应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2008001575A1 (fr) | 2006-06-28 | 2008-01-03 | Nikon Corporation | Dispositif de localisation, dispositif de mise au point automatique et appareil photographique |
| ME00962B (me) | 2007-06-29 | 2012-06-20 | Pfizer | Benzimidazolski derivati |
| KR20190038677A (ko) | 2015-04-24 | 2019-04-08 | 화이자 인코포레이티드 | 1-((2r,4r)-2-(1h-벤조[d]이미다졸-2-일)-1-메틸피페리딘-4-일)-3-(4-시아노페닐)우레아 말레에이트의 결정질 형태 |
-
2016
- 2016-04-13 KR KR1020197009092A patent/KR20190038677A/ko active Application Filing
- 2016-04-13 SI SI201631561T patent/SI3666768T1/sl unknown
- 2016-04-13 ES ES20151107T patent/ES2923593T3/es active Active
- 2016-04-13 BR BR112017021075-4A patent/BR112017021075B1/pt active IP Right Grant
- 2016-04-13 EP EP16718016.5A patent/EP3286176B1/en active Active
- 2016-04-13 PT PT201511078T patent/PT3666768T/pt unknown
- 2016-04-13 US US15/567,433 patent/US10414748B2/en active Active
- 2016-04-13 PL PL20151107.8T patent/PL3666768T3/pl unknown
- 2016-04-13 HU HUE16718016A patent/HUE048664T2/hu unknown
- 2016-04-13 ES ES16718016T patent/ES2774053T3/es active Active
- 2016-04-13 WO PCT/IB2016/052107 patent/WO2016170451A1/en active Application Filing
- 2016-04-13 MX MX2017013645A patent/MX2017013645A/es active IP Right Grant
- 2016-04-13 DK DK20151107.8T patent/DK3666768T3/da active
- 2016-04-13 SI SI201630639T patent/SI3286176T1/sl unknown
- 2016-04-13 PL PL16718016T patent/PL3286176T3/pl unknown
- 2016-04-13 AU AU2016251940A patent/AU2016251940C1/en active Active
- 2016-04-13 RU RU2017137269A patent/RU2717564C2/ru active
- 2016-04-13 EP EP20151107.8A patent/EP3666768B1/en active Active
- 2016-04-13 HU HUE20151107A patent/HUE059506T2/hu unknown
- 2016-04-13 SG SG11201707863QA patent/SG11201707863QA/en unknown
- 2016-04-13 CA CA2983387A patent/CA2983387C/en active Active
- 2016-04-13 KR KR1020177030098A patent/KR102078444B1/ko active IP Right Grant
- 2016-04-13 DK DK16718016.5T patent/DK3286176T3/da active
- 2016-04-13 PT PT167180165T patent/PT3286176T/pt unknown
- 2016-04-13 CN CN201680023699.0A patent/CN107531667A/zh active Pending
- 2016-04-20 CA CA2927736A patent/CA2927736A1/en not_active Abandoned
- 2016-04-20 JP JP2016084307A patent/JP6345728B2/ja active Active
- 2016-04-22 AR ARP160101150A patent/AR104391A1/es unknown
- 2016-04-22 TW TW105112723A patent/TWI646093B/zh active
-
2017
- 2017-09-21 ZA ZA2017/06391A patent/ZA201706391B/en unknown
- 2017-10-24 IL IL255224A patent/IL255224B/en active IP Right Grant
-
2018
- 2018-03-02 HK HK18103046.8A patent/HK1243416A1/zh unknown
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2019
- 2019-07-25 US US16/521,742 patent/US11168066B2/en active Active
-
2020
- 2020-02-19 CY CY20201100155T patent/CY1124056T1/el unknown
-
2021
- 2021-10-06 US US17/494,923 patent/US11891372B2/en active Active
- 2021-10-06 US US17/494,938 patent/US11891373B2/en active Active
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B15K | Others concerning applications: alteration of classification |
Free format text: A CLASSIFICACAO ANTERIOR ERA: C07D 401/04 Ipc: C07D 401/04 (2006.01), A61K 31/454 (2006.01), A61P |
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| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 13/04/2016, OBSERVADAS AS CONDICOES LEGAIS. |
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| B25G | Requested change of headquarter approved |
Owner name: PFIZER INC. (US) |