AR105483A1 - Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona - Google Patents
Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanonaInfo
- Publication number
- AR105483A1 AR105483A1 ARP160101900A ARP160101900A AR105483A1 AR 105483 A1 AR105483 A1 AR 105483A1 AR P160101900 A ARP160101900 A AR P160101900A AR P160101900 A ARP160101900 A AR P160101900A AR 105483 A1 AR105483 A1 AR 105483A1
- Authority
- AR
- Argentina
- Prior art keywords
- fumarate salt
- nmr spectrum
- azetidin
- piperidin
- difluoro
- Prior art date
Links
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 title abstract 4
- CUMTUBVTKOYYOU-UHFFFAOYSA-N 2-fluoro-4-iodoaniline Chemical compound NC1=CC=C(I)C=C1F CUMTUBVTKOYYOU-UHFFFAOYSA-N 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 abstract 3
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 abstract 3
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 3
- 239000007787 solid Substances 0.000 abstract 2
- -1 2-fluoro-4-iodophenylamino Chemical group 0.000 abstract 1
- 229910016523 CuKa Inorganic materials 0.000 abstract 1
- 238000000113 differential scanning calorimetry Methods 0.000 abstract 1
- 238000005259 measurement Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004574 piperidin-2-yl group Chemical group N1C(CCCC1)* 0.000 abstract 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 abstract 1
- 238000001757 thermogravimetry curve Methods 0.000 abstract 1
Classifications
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- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
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- 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
-
- 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
-
- 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
-
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Una sal de fumarato cristalina de (S)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona. Reivindicación 2: La sal de fumarato cristalina de la reivindicación 1, designada como forma A, en donde la sal de fumarato cristalina se caracteriza por al menos uno de lo siguiente: (i) un espectro ¹H NMR en d₆ DMSO sustancialmente como se describe en la figura 2; (ii) un espectro ¹³C NMR en d₆ DMSO sustancialmente como se describe en la figura 3; (iii) un espectro ¹³C NMR en estado sólido con tres o más picos seleccionados de 175,3, 173,6, 117,5, 155,5 y 153,5 ± 0,2 ppm; (iv) un espectro ¹³C NMR en estado sólido sustancialmente como se describe en la figura 4; (v) un patrón de difracción de rayos X en polvo (CuKa l = 1,5418 Å) que comprende tres o más valores de 2q seleccionados de 4,6, 12,1, 13,2, 13,6 y 14,5 ± 0,2 º2q, en donde la medición de la forma cristalina es a temperatura ambiente; (vi) un patrón de difracción de rayos X en polvo (XRPD) sustancialmente de acuerdo con el patrón que se muestra en la figura 10; y (vii) un termograma de calorimetría diferencial de barrido sustancialmente de acuerdo con la figura 8.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562187009P | 2015-06-30 | 2015-06-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR105483A1 true AR105483A1 (es) | 2017-10-11 |
Family
ID=56411938
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160101900A AR105483A1 (es) | 2015-06-30 | 2016-06-24 | Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US10590102B2 (es) |
| EP (1) | EP3317264B1 (es) |
| JP (3) | JP7338950B2 (es) |
| KR (1) | KR102695324B1 (es) |
| CN (2) | CN107810183A (es) |
| AR (1) | AR105483A1 (es) |
| AU (2) | AU2016288209B2 (es) |
| CA (1) | CA2990222C (es) |
| CL (1) | CL2017003475A1 (es) |
| CO (1) | CO2018000086A2 (es) |
| CR (1) | CR20180056A (es) |
| DK (1) | DK3317264T3 (es) |
| FI (1) | FI3317264T3 (es) |
| HK (1) | HK1252433A1 (es) |
| IL (2) | IL295052A (es) |
| MA (1) | MA42301A (es) |
| MX (1) | MX390250B (es) |
| MY (1) | MY192545A (es) |
| PE (1) | PE20180692A1 (es) |
| PH (1) | PH12017502414A1 (es) |
| RU (2) | RU2762181C2 (es) |
| SG (1) | SG10202105196YA (es) |
| TW (2) | TWI775187B (es) |
| UA (1) | UA124728C2 (es) |
| WO (1) | WO2017004393A1 (es) |
| ZA (1) | ZA201708760B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015008113B1 (pt) | 2012-10-12 | 2022-05-24 | Exelixis, Inc. | Novo processo para preparar compostos para uso no tratamento de câncer |
| AR105483A1 (es) | 2015-06-30 | 2017-10-11 | Exelixis Inc | Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona |
| SI3316867T1 (sl) * | 2015-06-30 | 2021-08-31 | Genentech, Inc. | Tablete s takojšnjim sproščanjem, ki vsebujejo zdravilo in postopek za pripravo tablet |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| GB201717809D0 (en) * | 2017-10-30 | 2017-12-13 | Azad Pharmaceutical Ingredients Ag | Process for the production of cobimetinib |
| WO2020187674A1 (en) | 2019-03-15 | 2020-09-24 | Sandoz Ag | Crystalline (s)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl]methanone hemisuccinate |
| WO2024111001A1 (en) * | 2022-11-25 | 2024-05-30 | Msn Laboratories Private Limited, R&D Center | Crystalline forms of n-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide fumarate and process for its preparation |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2007004781A (es) | 2004-10-20 | 2007-05-11 | Applied Research Systems | Derivados de 3-arilamino piridina. |
| EP2270000B1 (en) | 2005-05-23 | 2015-07-29 | Novartis AG | Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts |
| SI1934174T1 (sl) | 2005-10-07 | 2011-08-31 | Exelixis Inc | Inhibitorji MEK in postopki za njihovo uporabo |
| AU2007284562B2 (en) | 2006-08-16 | 2013-05-02 | Exelixis, Inc. | Using PI3K and MEK modulators in treatments of cancer |
| AU2007334402B2 (en) | 2006-12-14 | 2014-02-13 | Exelixis, Inc. | Methods of using MEK inhibitors |
| WO2008124085A2 (en) | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
| BR112015008113B1 (pt) | 2012-10-12 | 2022-05-24 | Exelixis, Inc. | Novo processo para preparar compostos para uso no tratamento de câncer |
| CN109568312A (zh) | 2013-03-05 | 2019-04-05 | 田纳西大学研究基金会 | 用于治疗癌症的化合物 |
| EP2968540A2 (en) | 2013-03-14 | 2016-01-20 | Genentech, Inc. | Combinations of a mek inhibitor compound with an her3/egfr inhibitor compound and methods of use |
| AR105483A1 (es) | 2015-06-30 | 2017-10-11 | Exelixis Inc | Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona |
-
2016
- 2016-06-24 AR ARP160101900A patent/AR105483A1/es unknown
- 2016-06-30 AU AU2016288209A patent/AU2016288209B2/en active Active
- 2016-06-30 KR KR1020187000067A patent/KR102695324B1/ko active Active
- 2016-06-30 JP JP2017568050A patent/JP7338950B2/ja active Active
- 2016-06-30 IL IL295052A patent/IL295052A/en unknown
- 2016-06-30 CA CA2990222A patent/CA2990222C/en active Active
- 2016-06-30 FI FIEP16738971.7T patent/FI3317264T3/fi active
- 2016-06-30 HK HK18111734.8A patent/HK1252433A1/zh unknown
- 2016-06-30 WO PCT/US2016/040444 patent/WO2017004393A1/en not_active Ceased
- 2016-06-30 PE PE2017002869A patent/PE20180692A1/es unknown
- 2016-06-30 IL IL256423A patent/IL256423B/en unknown
- 2016-06-30 UA UAA201800769A patent/UA124728C2/uk unknown
- 2016-06-30 RU RU2018103172A patent/RU2762181C2/ru active
- 2016-06-30 MY MYPI2017001962A patent/MY192545A/en unknown
- 2016-06-30 TW TW109136325A patent/TWI775187B/zh active
- 2016-06-30 CN CN201680039354.4A patent/CN107810183A/zh active Pending
- 2016-06-30 MA MA042301A patent/MA42301A/fr unknown
- 2016-06-30 SG SG10202105196YA patent/SG10202105196YA/en unknown
- 2016-06-30 RU RU2021132394A patent/RU2021132394A/ru unknown
- 2016-06-30 TW TW105120825A patent/TWI710556B/zh active
- 2016-06-30 CN CN202410400619.5A patent/CN118290395A/zh active Pending
- 2016-06-30 DK DK16738971.7T patent/DK3317264T3/da active
- 2016-06-30 MX MX2017017037A patent/MX390250B/es unknown
- 2016-06-30 EP EP16738971.7A patent/EP3317264B1/en active Active
- 2016-06-30 CR CR20180056A patent/CR20180056A/es unknown
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2017
- 2017-12-21 ZA ZA2017/08760A patent/ZA201708760B/en unknown
- 2017-12-22 US US15/852,280 patent/US10590102B2/en active Active
- 2017-12-22 PH PH12017502414A patent/PH12017502414A1/en unknown
- 2017-12-29 CL CL2017003475A patent/CL2017003475A1/es unknown
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2018
- 2018-01-05 CO CONC2018/0000086A patent/CO2018000086A2/es unknown
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2020
- 2020-01-17 US US16/746,161 patent/US11254649B2/en active Active
- 2020-11-05 JP JP2020184868A patent/JP2021035967A/ja not_active Withdrawn
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2021
- 2021-01-14 AU AU2021200202A patent/AU2021200202B2/en active Active
- 2021-11-08 US US17/521,396 patent/US20220056010A1/en not_active Abandoned
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2022
- 2022-11-07 JP JP2022178184A patent/JP2023025000A/ja active Pending
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