HRP20120007T1 - Polimorfni oblik 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2h-ftalazin-1-ona - Google Patents
Polimorfni oblik 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2h-ftalazin-1-ona Download PDFInfo
- Publication number
- HRP20120007T1 HRP20120007T1 HR20120007T HRP20120007T HRP20120007T1 HR P20120007 T1 HRP20120007 T1 HR P20120007T1 HR 20120007 T HR20120007 T HR 20120007T HR P20120007 T HRP20120007 T HR P20120007T HR P20120007 T1 HRP20120007 T1 HR P20120007T1
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- Prior art keywords
- compound
- phthalazin
- cyclopropanecarbonyl
- compound according
- carbonyl
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- FDLYAMZZIXQODN-UHFFFAOYSA-N olaparib Chemical compound FC1=CC=C(CC=2C3=CC=CC=C3C(=O)NN=2)C=C1C(=O)N(CC1)CCN1C(=O)C1CC1 FDLYAMZZIXQODN-UHFFFAOYSA-N 0.000 title claims abstract 8
- 150000001875 compounds Chemical class 0.000 claims abstract 12
- 239000000843 powder Substances 0.000 claims abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 9
- 229940126062 Compound A Drugs 0.000 claims 8
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 8
- 239000002904 solvent Substances 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 238000001035 drying Methods 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 238000002425 crystallisation Methods 0.000 claims 2
- 230000008025 crystallization Effects 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 230000005865 ionizing radiation Effects 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 210000004881 tumor cell Anatomy 0.000 claims 2
- 208000032456 Hemorrhagic Shock Diseases 0.000 claims 1
- 206010029350 Neurotoxicity Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010049771 Shock haemorrhagic Diseases 0.000 claims 1
- 206010044221 Toxic encephalopathy Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 230000002950 deficient Effects 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000004821 distillation Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000007135 neurotoxicity Effects 0.000 claims 1
- 231100000228 neurotoxicity Toxicity 0.000 claims 1
- 238000010899 nucleation Methods 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000011084 recovery Methods 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Spoj, naznačen time, da je to 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2H-ftalazin-1-on kao kristalni oblik A, koji ima sljedeće karakteristične vršne točke u prahu XRD:
Claims (13)
1. Spoj, naznačen time, da je to 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2H-ftalazin-1-on kao kristalni oblik A, koji ima sljedeće karakteristične vršne točke u prahu XRD:
[image]
2. Spoj prema zahtjevu 1, naznačen time, da ima sljedeće karakteristične vršne točke u prahu XRD:
[image]
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time, da se počinje taliti na 210,1°C ± 1°C kada se zagrijava od 25°C do 325°C po 10°C u minuti u DSC.
4. Postupak dobivanja 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluorobenzil]-2H-ftalazin-1-ona (spoj A) kao kristalnog oblika A, kako je definiran u bilo kojem od zahtjeva 1 do 3, naznačen time, da se sastoji od sljedećih koraka:
(i) kristalizacija 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2H-ftalazin-1-ona iz otapala;
(ii) ako izvorno otapalo nije etanol, tretiranje kristalnog spoja A etanolom;
(iii) tretiranje kristalnog spoja A vodom da se odstrani zaostali etanol;
(iv) sušenje rezultirajućeg proizvoda.
5. Postupak dobivanja 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluorobenzil]-2H-ftalazin-1-ona (spoj A) kao kristalnog oblika A, kako je definiran u bilo kojem od zahtjeva 1 do 3, naznačen time, da se sastoji od sljedećih koraka:
(i) kristalizacija 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2H-ftalazin-1-ona iz otapala;
(ii) ako izvorno otapalo korišteno u sintezi spoja A u kristalnom obliku nije mješavina vode i C1-2 alkohola, zagrijavanje spoja mješavinom vode i C1-2 alkohola;
(iii) destilacija mješavine uz tlak okoline; i
(iv) sušenje rezultirajućeg proizvoda.
6. Postupak dobivanja 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluorobenzil]-2H-ftalazin-1-ona (spoj A) kao kristalnog oblika A, kako je definiran u bilo kojem od zahtjeva 1 do 3, naznačen time, da se sastoji od sljedećih koraka:
(i) suspendiranje spoja A u mješavini vode i C1-2 alkohola kao otapala;
(ii) zagrijavanje suspenzije do refluksa;
(iii) hlađenje otopine i zasijavanje spojem A koji je u obliku A;
(iv) sušenje rezultirajućeg proizvoda.
7. Farmaceutski sastav, naznačen time, da sadrži spoj prema bilo kojem od zahtjeva 1 do 3 i farmaceutski prihvatljiv nosač ili razrjeđivač.
8. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se koristi u postupku liječenja ljudskog ili životinjskog tijela.
9. Uporaba spoja prema bilo kojem od zahtjeva 1 do 3, naznačena time, da je za pripravljanje lijeka za liječenje: vaskularnih bolesti; septičkog šoka; ishemijskih ozljeda; neurotoksičnosti; hemoragijskog šoka; ili virusnih infekcija.
10. Uporaba spoja prema bilo kojem od zahtjeva 1 do 3, naznačena time, da je za pripravljanje lijeka koji se koristi kao dopuna u liječenju raka ili za potencijaciju tumorskih stanica za liječenje s ionizacijskom radijacijom ili sa kemoterapeutskim sredstvima.
11. Uporaba spoja prema bilo kojem od zahtjeva 1 do 3, naznačena time, da je za proizvodnju lijeka koji se koristi u liječenju raka kod pojedinca, pri čemu je spomenuti rak deficijentan u putevima oporavka DNA DSB mehanizma u ovisnosti o HR.
12. Uporaba spoja prema zahtjevu 11, naznačena time, da spomenuti rak sadrži jednu ili više tumorskih stanica koje imaju smanjenu ili ukinutu sposobnost oporavka DNA DSB mehanizma pomoću HR u odnosu na normalne stanice.
13. Uporaba spoja prema zahtjevu 11 ili zahtjevu 12, naznačena time, da spomenuto liječenje nadalje obuhvaća primjenu ionizacijske radijacije ili kemoterapeutskog sredstva.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US82969406P | 2006-10-17 | 2006-10-17 | |
PCT/GB2007/003888 WO2008047082A2 (en) | 2006-10-17 | 2007-10-15 | Polymorphic form of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120007T1 true HRP20120007T1 (hr) | 2012-01-31 |
Family
ID=38952365
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20120007T HRP20120007T1 (hr) | 2006-10-17 | 2012-01-03 | Polimorfni oblik 4-[3-(4-ciklopropankarbonil-piperazin-1-karbonil)-4-fluoro-benzil]-2h-ftalazin-1-ona |
Country Status (35)
Country | Link |
---|---|
US (2) | US7692006B2 (hr) |
EP (3) | EP2374800A3 (hr) |
JP (3) | JP5248513B2 (hr) |
KR (2) | KR20140011425A (hr) |
CN (3) | CN104649979B (hr) |
AR (1) | AR063320A1 (hr) |
AT (1) | ATE528296T1 (hr) |
AU (1) | AU2007311766B2 (hr) |
BR (1) | BRPI0717125B8 (hr) |
CA (2) | CA2875147C (hr) |
CL (1) | CL2007002967A1 (hr) |
CO (1) | CO6210728A2 (hr) |
CY (1) | CY1112345T1 (hr) |
DK (1) | DK2064189T3 (hr) |
ES (2) | ES2587129T3 (hr) |
HK (2) | HK1126483A1 (hr) |
HR (1) | HRP20120007T1 (hr) |
IL (2) | IL197420A (hr) |
ME (1) | ME01987B (hr) |
MX (1) | MX2009004103A (hr) |
MY (2) | MY147389A (hr) |
NO (2) | NO341963B1 (hr) |
NZ (1) | NZ575627A (hr) |
PE (1) | PE20081175A1 (hr) |
PL (1) | PL2064189T3 (hr) |
PT (1) | PT2064189E (hr) |
RS (1) | RS52112B (hr) |
RU (1) | RU2465270C3 (hr) |
SA (2) | SA07280551B1 (hr) |
SG (2) | SG168523A1 (hr) |
SI (1) | SI2064189T1 (hr) |
TW (1) | TWI404716B (hr) |
UA (1) | UA97494C2 (hr) |
UY (1) | UY30639A1 (hr) |
WO (1) | WO2008047082A2 (hr) |
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GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
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