AR074686A1 - Formas polimorficas de dihidrogeno-fosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2h-piridazin-3-ona, procesos para su preparacion, composiciones farmaceuticas que las comprenden y su em-pleo en medicamentos para el tratamiento del cancer - Google Patents
Formas polimorficas de dihidrogeno-fosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2h-piridazin-3-ona, procesos para su preparacion, composiciones farmaceuticas que las comprenden y su em-pleo en medicamentos para el tratamiento del cancerInfo
- Publication number
- AR074686A1 AR074686A1 ARP090104909A ARP090104909A AR074686A1 AR 074686 A1 AR074686 A1 AR 074686A1 AR P090104909 A ARP090104909 A AR P090104909A AR P090104909 A ARP090104909 A AR P090104909A AR 074686 A1 AR074686 A1 AR 074686A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- pyridazin
- morpholin
- pyrazol
- pyrimidin
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
Dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona, sus solvatos y modificaciones cristalinas. También se refiere a procesos de preparación de estas modificaciones cristalinas, así como a su uso en el tratamiento y/o la prevención de condiciones fisiológicas y/o patofisiológicas que son causadas, mediadas y/o propagadas por la inhibición, regulación y/o modulación de la transducción de senales de quinasa, en particular por la inhibición de tirosina quinasas, por ejemplo, condiciones patofisiológicas como el cáncer. Reivindicación 1: Dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona. Reivindicación 2: Ssolvato de dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona, con preferencia hidrato de dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona. Reivindicación 4: Anhidrato de dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona. Reivindicación 8: El compuesto de acuerdo con cualquiera de las reivindicaciones 4 a 7 en su modificación cristalina A1, que se caracteriza por los siguientes datos de XRD: Forma A1: 27,45, 3,2; 13,62, 6,5; 9,02, 9,8; 6,75, 13,1; 6,15, 14,4; 5,59, 15,8; 5,07, 17,5; 4,81, 18,4; 4,72, 18,8; 4,55, 19,5; 4,06, 21,9; 3,75, 23,7; 3,68, 24,2; 3,37, 26,4; 3,16, 28,2 + - 0,1s s2theta radiación Cu-Kalfa1. Reivindicación 9: Dihidrato de dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona. Reivindicación 14: El compuesto de acuerdo con cualquiera de las reivindicaciones 9 a 13 en su modificación cristalina H1, que se caracteriza por los siguientes datos de XRD: Forma H1: 28,42, 3,1; 9,40, 9,4; 6,13, 14,4; 6,01, 14,7; 5,89, 15,0; 4,97, 17,8; 4,77, 18,6; 4,71, 18,8; 4,64, 19,1; 3,89, 22,8; 3,83, 23,2; 3,73, 23,8; 3,38, 26,4; 3,33, 26,8; 3,22, 27,6 + - 0,1s s2theta radiación Cu-Kalfa1. Reivindicación 15: Dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona en su modificación cristalina NF3, que se caracteriza por picos de XRD que comprenden 15,3s, 16,7s, 21,6s y 23,1s 2(todos + - 0,1s 2, usando radiación Cu-Kalfa1). Reivindicación 16: El compuesto de acuerdo con la reivindicación 15 en su modificación cristalina NF3, que se caracteriza por los siguientes datos de XRD: Forma NF3: 27,30, 3,2; 13,62, 6,5; 9,02, 9,8; 6,71, 13,2; 6,11, 14,5; 5,79, 15,3; 5,57, 15,9; 5,32, 16,7; 5,05, 17,5; 4,81, 18,4; 4,58, 19,4; 4,12, 21,6; 4,04, 22,0; 3,84, 23,1; 3,75, 23,7; 3,69, 24,1; 3,37, 26,4; 3,16, 28,3 + - 0,1s s2theta radiación Cu-Kalfa1. Reivindicación 17: Hidrato de dihidrógeno-fosfato de 6-(1-metil-1H-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2H-piridazin-3-ona. Reivindicación 19: El compuesto de acuerdo con cualquiera de las reivindicaciones 17 a 18 en su modificación cristalina NF5, que se caracteriza por los siguientes datos de XRD: Forma NF5: 28,54, 3,1; 9,41, 9,4; 6,37, 13,9; 6,10, 14,5; 5,98, 14,8; 5,82, 15,2; 5,62, 15,7; 5,32, 16,6; 5,13, 17,3; 4,96, 17,9; 4,80, 18,5; 4,69, 18,9; 4,63, 19,2; 4,48, 19,8; 4,02, 22,1; 3,90, 22,8; 3,85, 23,1; 3,73, 23,9; 3,38, 26,3; 3,32, 26,8; 3,23, 27,6 + - 0,1s s2theta radiación Cu-Kalfa1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08022253 | 2008-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074686A1 true AR074686A1 (es) | 2011-02-02 |
Family
ID=41609799
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104909A AR074686A1 (es) | 2008-12-22 | 2009-12-16 | Formas polimorficas de dihidrogeno-fosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-bencil}-2h-piridazin-3-ona, procesos para su preparacion, composiciones farmaceuticas que las comprenden y su em-pleo en medicamentos para el tratamiento del cancer |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8586599B2 (es) |
| EP (1) | EP2361250B1 (es) |
| JP (2) | JP5690741B2 (es) |
| KR (1) | KR101663335B1 (es) |
| CN (1) | CN102264729B (es) |
| AR (1) | AR074686A1 (es) |
| AU (1) | AU2009331990B2 (es) |
| BR (1) | BRPI0923480B8 (es) |
| CA (1) | CA2748218C (es) |
| CL (1) | CL2011001278A1 (es) |
| CO (1) | CO6331435A2 (es) |
| CY (1) | CY1114659T1 (es) |
| DK (1) | DK2361250T3 (es) |
| EA (1) | EA019320B1 (es) |
| EC (1) | ECSP11011219A (es) |
| ES (1) | ES2434247T3 (es) |
| HR (1) | HRP20130993T1 (es) |
| IL (1) | IL213647A (es) |
| MX (1) | MX2011006682A (es) |
| MY (1) | MY160526A (es) |
| NZ (1) | NZ594172A (es) |
| PE (1) | PE20120016A1 (es) |
| PL (1) | PL2361250T3 (es) |
| PT (1) | PT2361250E (es) |
| SG (1) | SG172128A1 (es) |
| SI (1) | SI2361250T1 (es) |
| SM (1) | SMT201300133B (es) |
| TW (1) | TWI448463B (es) |
| UA (1) | UA103646C2 (es) |
| WO (1) | WO2010072295A1 (es) |
| ZA (1) | ZA201105394B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102008062826A1 (de) * | 2008-12-23 | 2010-07-01 | Merck Patent Gmbh | Pyridazinonderivate |
| KR20180092096A (ko) * | 2017-02-08 | 2018-08-17 | 에이비온 주식회사 | 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법 |
| ES2946551T3 (es) | 2017-10-17 | 2023-07-20 | Palau Pharma S L U | Síntesis de compuestos de 4-aminopirimidina |
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2009
- 2009-11-24 MY MYPI2011002864A patent/MY160526A/en unknown
- 2009-11-24 BR BRPI0923480A patent/BRPI0923480B8/pt not_active IP Right Cessation
- 2009-11-24 PE PE2011001264A patent/PE20120016A1/es not_active Application Discontinuation
- 2009-11-24 HR HRP20130993AT patent/HRP20130993T1/hr unknown
- 2009-11-24 WO PCT/EP2009/008358 patent/WO2010072295A1/en not_active Ceased
- 2009-11-24 KR KR1020117017081A patent/KR101663335B1/ko not_active Expired - Fee Related
- 2009-11-24 JP JP2011542688A patent/JP5690741B2/ja not_active Expired - Fee Related
- 2009-11-24 AU AU2009331990A patent/AU2009331990B2/en not_active Ceased
- 2009-11-24 EP EP09756445.4A patent/EP2361250B1/en active Active
- 2009-11-24 MX MX2011006682A patent/MX2011006682A/es active IP Right Grant
- 2009-11-24 SG SG2011043171A patent/SG172128A1/en unknown
- 2009-11-24 CA CA2748218A patent/CA2748218C/en active Active
- 2009-11-24 CN CN200980151790.0A patent/CN102264729B/zh not_active Expired - Fee Related
- 2009-11-24 EA EA201100973A patent/EA019320B1/ru not_active IP Right Cessation
- 2009-11-24 UA UAA201109101A patent/UA103646C2/ru unknown
- 2009-11-24 PT PT97564454T patent/PT2361250E/pt unknown
- 2009-11-24 ES ES09756445T patent/ES2434247T3/es active Active
- 2009-11-24 PL PL09756445T patent/PL2361250T3/pl unknown
- 2009-11-24 DK DK09756445.4T patent/DK2361250T3/da active
- 2009-11-24 SI SI200930754T patent/SI2361250T1/sl unknown
- 2009-11-24 US US13/141,142 patent/US8586599B2/en not_active Expired - Fee Related
- 2009-11-24 NZ NZ594172A patent/NZ594172A/xx not_active IP Right Cessation
- 2009-12-16 AR ARP090104909A patent/AR074686A1/es not_active Application Discontinuation
- 2009-12-21 TW TW098143944A patent/TWI448463B/zh not_active IP Right Cessation
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2011
- 2011-05-31 CL CL2011001278A patent/CL2011001278A1/es unknown
- 2011-06-19 IL IL213647A patent/IL213647A/en active IP Right Grant
- 2011-06-22 CO CO11078454A patent/CO6331435A2/es active IP Right Grant
- 2011-07-21 ZA ZA2011/05394A patent/ZA201105394B/en unknown
- 2011-07-21 EC EC2011011219A patent/ECSP11011219A/es unknown
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2013
- 2013-11-07 CY CY20131100991T patent/CY1114659T1/el unknown
- 2013-11-13 SM SM201300133T patent/SMT201300133B/xx unknown
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2014
- 2014-11-14 JP JP2014231392A patent/JP5860125B2/ja not_active Expired - Fee Related
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