CA2814581C - Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt - Google Patents

Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt Download PDF

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Publication number
CA2814581C
CA2814581C CA2814581A CA2814581A CA2814581C CA 2814581 C CA2814581 C CA 2814581C CA 2814581 A CA2814581 A CA 2814581A CA 2814581 A CA2814581 A CA 2814581A CA 2814581 C CA2814581 C CA 2814581C
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Prior art keywords
cancer
peaks
tosylate salt
triazol
pyrido
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CA2814581A
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English (en)
French (fr)
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CA2814581A1 (en
Inventor
Bing Wang
Daniel Chu
Yongbo Liu
Shichun Peng
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Medivation Technologies LLC
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Medivation Technologies LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed 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
    • A61K31/495—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
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2814581A 2010-10-21 2011-10-20 Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt Active CA2814581C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40547610P 2010-10-21 2010-10-21
US61/405,476 2010-10-21
PCT/US2011/057039 WO2012054698A1 (en) 2010-10-21 2011-10-20 Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt

Publications (2)

Publication Number Publication Date
CA2814581A1 CA2814581A1 (en) 2012-04-26
CA2814581C true CA2814581C (en) 2019-02-12

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CA2814581A Active CA2814581C (en) 2010-10-21 2011-10-20 Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt

Country Status (24)

Country Link
US (3) US8735392B2 (https=)
EP (2) EP3757106A1 (https=)
JP (6) JP2013540158A (https=)
KR (4) KR20180069132A (https=)
CN (1) CN103282365B (https=)
AR (1) AR083502A1 (https=)
AU (2) AU2011317040B2 (https=)
BR (1) BR112013009117A2 (https=)
CA (1) CA2814581C (https=)
CY (1) CY1123356T1 (https=)
DK (1) DK2630146T3 (https=)
ES (1) ES2816600T3 (https=)
HU (1) HUE051535T2 (https=)
IL (2) IL225789B (https=)
MX (1) MX362563B (https=)
NZ (1) NZ609490A (https=)
PL (1) PL2630146T3 (https=)
PT (1) PT2630146T (https=)
RU (1) RU2598606C3 (https=)
SG (2) SG189939A1 (https=)
SI (1) SI2630146T1 (https=)
TW (2) TWI557123B (https=)
WO (1) WO2012054698A1 (https=)
ZA (1) ZA201302810B (https=)

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IL271497A (en) 2020-02-27
KR20180069132A (ko) 2018-06-22
JP2019034951A (ja) 2019-03-07
WO2012054698A1 (en) 2012-04-26
MX2013004195A (es) 2013-07-22
CN103282365B (zh) 2017-12-29
TW201713656A (en) 2017-04-16
EP2630146B1 (en) 2020-07-01
IL225789B (en) 2019-12-31
US20180009806A1 (en) 2018-01-11
PT2630146T (pt) 2020-07-20
JP2020169209A (ja) 2020-10-15
US10189837B2 (en) 2019-01-29
DK2630146T3 (da) 2020-08-10
MX362563B (es) 2019-01-25
KR20140009181A (ko) 2014-01-22
KR20210028747A (ko) 2021-03-12
AR083502A1 (es) 2013-02-27
PL2630146T3 (pl) 2020-11-02
SI2630146T1 (sl) 2020-12-31
US20140228369A1 (en) 2014-08-14
ES2816600T3 (es) 2021-04-05
JP2017061526A (ja) 2017-03-30
RU2598606C3 (ru) 2021-12-20
AU2011317040B2 (en) 2016-12-08
RU2013123036A (ru) 2014-11-27
US8735392B2 (en) 2014-05-27
JP2013540158A (ja) 2013-10-31
AU2017201564B2 (en) 2019-05-09
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IL225789A0 (en) 2013-06-27
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AU2017201564A1 (en) 2017-03-23
SG189939A1 (en) 2013-06-28
KR20190120458A (ko) 2019-10-23
BR112013009117A2 (pt) 2016-07-19
CY1123356T1 (el) 2021-12-31
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