EA201290906A1 - Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида - Google Patents
Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамидаInfo
- Publication number
- EA201290906A1 EA201290906A1 EA201290906A EA201290906A EA201290906A1 EA 201290906 A1 EA201290906 A1 EA 201290906A1 EA 201290906 A EA201290906 A EA 201290906A EA 201290906 A EA201290906 A EA 201290906A EA 201290906 A1 EA201290906 A1 EA 201290906A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- oxy
- phenyl
- photorphenyl
- diparboxamide
- cyclopropan
- Prior art date
Links
Classifications
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- 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
Abstract
Изобретение относится к кристаллогидрату N-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-N'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, соединение (I). Изобретение представляет способы лечения рака путем применения модуляции протеинкиназной активности. Изобретение также представляет фармацевтические композиции, содержащие кристаллогидрат соединения (I) и фармацевтически приемлемый эксципиент.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31319210P | 2010-03-12 | 2010-03-12 | |
PCT/US2011/028035 WO2011112896A1 (en) | 2010-03-12 | 2011-03-11 | Hydrated crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201290906A1 true EA201290906A1 (ru) | 2013-03-29 |
Family
ID=43875241
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201290906A EA201290906A1 (ru) | 2010-03-12 | 2011-03-11 | Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида |
Country Status (14)
Country | Link |
---|---|
US (1) | US20130143881A1 (ru) |
EP (1) | EP2545038A1 (ru) |
JP (1) | JP2013522232A (ru) |
KR (1) | KR20130038206A (ru) |
CN (1) | CN102933551A (ru) |
AR (1) | AR080584A1 (ru) |
AU (1) | AU2011224203A1 (ru) |
CA (1) | CA2792852A1 (ru) |
EA (1) | EA201290906A1 (ru) |
MX (1) | MX2012010506A (ru) |
SG (1) | SG184040A1 (ru) |
TW (1) | TW201202228A (ru) |
WO (1) | WO2011112896A1 (ru) |
ZA (1) | ZA201206679B (ru) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010083414A1 (en) | 2009-01-16 | 2010-07-22 | Exelixis, Inc. | Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer |
UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
NZ607118A (en) | 2010-07-16 | 2015-05-29 | Exelixis Inc | C-met modulator pharmaceutical compositions |
EP2621481B2 (en) | 2010-09-27 | 2022-10-19 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
EP4019498A1 (en) | 2011-02-10 | 2022-06-29 | Exelixis, Inc. | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
KR20140025496A (ko) | 2011-05-02 | 2014-03-04 | 엑셀리시스, 인코포레이티드 | 암 및 뼈 암 통증의 치료방법 |
CN103957915A (zh) | 2011-09-22 | 2014-07-30 | 埃克塞里艾克西斯公司 | 治疗骨质疏松症的方法 |
ES2765013T3 (es) | 2011-10-20 | 2020-06-05 | Exelixis Inc | Procedimiento para preparar derivados de quinolina |
JP2015515988A (ja) | 2012-05-02 | 2015-06-04 | エクセリクシス, インク. | 溶骨性骨転移を治療するためのmet−vegf二重調節剤 |
WO2014145715A1 (en) | 2013-03-15 | 2014-09-18 | Exelixis, Inc. | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide |
WO2014165786A1 (en) | 2013-04-04 | 2014-10-09 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
CA3181899A1 (en) | 2014-02-14 | 2015-08-20 | Exelixis, Inc. | Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use |
EA201691850A1 (ru) | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
CA2956810C (en) | 2014-07-31 | 2022-10-04 | Exelixis, Inc. | Method of preparing fluorine-18 labeled cabozantinib and its analogs |
BR112017002318A2 (pt) | 2014-08-05 | 2018-07-17 | Exelixis, Inc. | combinações de fármacos para tratar mieloma múltiplo. |
CA3020749A1 (en) | 2016-04-15 | 2017-10-19 | Exelixis, Inc. | Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate |
EP3476835A4 (en) | 2016-05-16 | 2020-01-01 | GB001, Inc. | QUINOLEIN DERIVATIVE CRYSTAL |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK2210607T3 (da) | 2003-09-26 | 2011-12-12 | Exelixis Inc | N-[3-fluor-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid til behandling af kræft |
AU2010274012A1 (en) * | 2009-07-17 | 2012-02-09 | Exelixis, Inc. | Crystalline forms of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy] -quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide |
-
2011
- 2011-03-11 JP JP2012557269A patent/JP2013522232A/ja active Pending
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 2011-03-11 CA CA2792852A patent/CA2792852A1/en not_active Abandoned
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 2011-03-11 TW TW100108394A patent/TW201202228A/zh unknown
- 2011-03-11 WO PCT/US2011/028035 patent/WO2011112896A1/en active Application Filing
- 2011-03-11 EP EP11709589A patent/EP2545038A1/en not_active Withdrawn
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 2011-03-11 US US13/634,275 patent/US20130143881A1/en not_active Abandoned
- 2011-03-11 EA EA201290906A patent/EA201290906A1/ru unknown
- 2011-03-11 KR KR1020127025322A patent/KR20130038206A/ko not_active Application Discontinuation
- 2011-03-14 AR ARP110100801A patent/AR080584A1/es unknown
-
2012
- 2012-09-06 ZA ZA2012/06679A patent/ZA201206679B/en unknown
Also Published As
Publication number | Publication date |
---|---|
CN102933551A (zh) | 2013-02-13 |
TW201202228A (en) | 2012-01-16 |
US20130143881A1 (en) | 2013-06-06 |
EP2545038A1 (en) | 2013-01-16 |
MX2012010506A (es) | 2012-10-15 |
AU2011224203A1 (en) | 2012-10-04 |
CA2792852A1 (en) | 2011-09-15 |
WO2011112896A1 (en) | 2011-09-15 |
JP2013522232A (ja) | 2013-06-13 |
ZA201206679B (en) | 2013-05-29 |
SG184040A1 (en) | 2012-10-30 |
AR080584A1 (es) | 2012-04-18 |
KR20130038206A (ko) | 2013-04-17 |
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