SK10372002A3 - Etanolový solvát (-)-cis-2-(2-chlórgenyl)-5,7-dihydroxy-8[4R- (3S-hydroxy-1-metyl)piperidinyl]-4H-1-benzopyran-4-ón hydrochloridu, spôsob jeho prípravy a farmaceutická kompozícia, ktorá ho obsahuje - Google Patents
Etanolový solvát (-)-cis-2-(2-chlórgenyl)-5,7-dihydroxy-8[4R- (3S-hydroxy-1-metyl)piperidinyl]-4H-1-benzopyran-4-ón hydrochloridu, spôsob jeho prípravy a farmaceutická kompozícia, ktorá ho obsahuje Download PDFInfo
- Publication number
- SK10372002A3 SK10372002A3 SK1037-2002A SK10372002A SK10372002A3 SK 10372002 A3 SK10372002 A3 SK 10372002A3 SK 10372002 A SK10372002 A SK 10372002A SK 10372002 A3 SK10372002 A3 SK 10372002A3
- Authority
- SK
- Slovakia
- Prior art keywords
- weak
- cis
- benzopyran
- chlorophenyl
- piperidinyl
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Description
Hodnota D-Ä | Relatívna intenzita |
12,763 | silná |
6, 389 | stredná |
3, 194 | slabá |
' 13,244 | sl'abá |
4,259 | slabá |
12,036 | slabá |
2,824 | slabá |
8,659 | slabá |
6,012 | slabá |
5,397 | . slabá |
3,447 | slabá |
Uhol 2 teta (°) | Hodnota D-Ä | Relatívna intenzita | Relatívna intenzita (%) |
6, 920 | 12,763 | silná | 100, 0 |
13,850 | 6,389 | stredná | 35, 7 |
27,908 | 3, 194 | slabá | 22,2 |
6, 669 | 13,244 | slabá | 18, 0 |
20,838 | 4,259 | slabá | 13, 8 |
7,339 | 12,036 | slabá | 13, 8 |
31,660 | 2,824 | slabá | 9,5 |
10,208 | 8,659 | slabá | 8, 3 |
14,722 | 6,012 | slabá | 7,2 |
16, 413 | 5, 397 | slabá | 6,9 |
25,829 | 3,447 | slabá | 6, 5 |
Claims (10)
- PATENTOVÉ NÁROKY1. Forma II (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hy droxy-l-metyl) piperidinyl ] -4íí-l-benzopyrán-4-ónu.
- 2. Forma II (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hy droxy-ľmetyl) piperidinyl]-4H-l-benzopyrán-4-ónu, vyznačujúca sa tým, že jej obrazec získaný rontgenovou práš kovou difrakciou, pomocou Cu K-alfa radiácie, je:hodnota D-Ä12,7636,.389
- 3,19413,244
- 4,2593. Forma II (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hy droxy-l-metyl)piperidinyl]-4/í-l-benzopyrán-4-ónu, vyznačujúca sa tý m , že jej obrazec získaný rontgenovou práš kovou difrakciou, pomocou Cu K-alfa radiácie, je:Hodnota D-Ä 'Relatívna intenzita12,763 6, 389 3, 194 13,244 4,259 12,036 2,824 8, 659 6, 012 5, 397 3, 447 silná stredná slabá slabá slabá slabá slabá slabá slabá slabá slabá4. Forma II (-) -cis-2-(2-chlórfenyl)-5,7-dihydroxy~8-[4R-(3S-hydroxy-l-metyl) piperidinyl] -4íí-l-benzopyrán-4-ónu, vyznačujúca sa tým, že jej obrazec získaný róntgenovou práškovou difrakciou, pomocou Cu K-alfa radiácie, je:
Uhol 2 teta (°) Hodnota D-Ä Relatívna intenzita Relatívna intenzita (%) 6/920 · 12,763 silná 100,0 13,850 6, 389 stredná 35,7 27,908 3, 194 slabá 22,2 6, 669 13,244 slabá 18,0 20,838 4,259 slabá 13,8 7,339 12,036 slabá 13,8 31,660 2,824 slabá 9,5 ' . 10,208 8,659 slabá 8,3 14,722 6, 012 slabá 7,2 16,413 5, 397 slabá 6,9 25,829 3,447 slabá 6, 5 - 5. Spôsob prípravy formy II (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hydroxy-l-metyl)piperidinyl]-4H-l-benzopyrán-4-ónu, vyznačujúci sa tým, že (a) sa rozpustí dostatočné množstvo hydrochloridu (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3Sghydroxy-l-metyl)piperidinyl] -47í-l-benzopyrán-4-ónu v dostatočnom množstve etanolu za vzniku zmesi;(b) zmes sa zahrieva na teplotu približne 50 až 80° C;(c) zo zmesi sa prípadne odfiltruje nerozpustený materiál, pričom sa vytvorí roztok;(d) roztok sa koncentruje dovtedy, kým sa neodstráni približne 50 až 90 % prchavých látok;(e) roztok sa ochladí, a prípadne sa izolujú takto získané kryštály hydrochloridu (-) -cis-2- (2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hydroxy-l-metyl)piperidinyl]-4tf-l-benzopyrán-4-ónu; a (f) získané kryštály sa prípadne sušia.
- 6. Spôsob podlá nároku 5, vyznačujúci sa tým, že sa roztok ochladí na približne 0 až 10° C.
- 7. Forma II (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4F-(3S-hydroxy-l-metyl)piperidinyl]-4tf-l-benzopyrán-4-ónu, vyznačujúca sa tým, že sa pripraví spôsobom, ktorý zahŕňa nasledujúce stupne:(a) rozpustenie dostatočného množstva hydrochloridu (-)-cis-2-(2-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hydroxy-l—metyl)piperidinyl·] -4H-l-benzopyrán-4-ónu v dostatočnom množstve etanolu za vzniku zmesi, (b) zahrievanie zmesi na približne 50 až 80° C;(c) poprípade odfiltrovanie nerozpusteného materiálu zo' zmesi, pričom sa vytvorí roztok;(ď) koncentrovanie roztoku dovtedy, kým sa neodstráni približne 50 až 90 % prchavých látok, (e) ochladenie roztoku, a prípadne izolácia takto získaných kryštálov hydrochloridu (-) -cis-2-(2-chlórfenyl)-5, 7-dihydroxy-8-[4Ä-(3S-hydroxy-l-metyl)piperidinyl]-4#-l-benzopyrán-4-ónu; a (f) prípadne sušenie získaných kryštálov.
- 8. Farmaceutická kompozícia, vyznačujúca sa tým, že obsahuje terapeuticky účinné množstvo formy II (-)-cis-2-(214-chlórfenyl)-5,7-dihydroxy-8-[4R-(3S-hydroxy-l-metyl)piperidinyl]-4 Jí-l-benzopyrán-4-ónu a farmaceutický prijateľný nosič.
- 9. Použitie formy II podľa nároku 1, 2, 3 alebo 4 na prípravu farmaceutické j kompozície na liečenie pacienta, ktorý má rako-: vinu.
- 10. Použitie formy II podľa nároku 1, 2, 3 alebo 4 ako farmaceutický účinnej zlúčeniny.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US48781500A | 2000-01-18 | 2000-01-18 | |
PCT/US2001/000520 WO2001053294A1 (en) | 2000-01-18 | 2001-01-08 | Ethanol solvate of (-)-cis-2-(2-chlorophenyl)-5,7-dihydroxy-8[4r-(3s-hydroxy-1-methyl)piperidinyl]-4h-1-benzopyran-4-one |
Publications (2)
Publication Number | Publication Date |
---|---|
SK10372002A3 true SK10372002A3 (sk) | 2002-12-03 |
SK287216B6 SK287216B6 (sk) | 2010-03-08 |
Family
ID=23937213
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SK1037-2002A SK287216B6 (sk) | 2000-01-18 | 2001-01-08 | Hydrochloridová etanolová solvátová forma (-)-cis-2-(2- chlórfenyl)-5,7-dihydroxy-8[4R-(3S-hydroxy-1-metyl)piperidinyl]- 4H-1-benzopyran-4-ónu, spôsob jej prípravy, farmaceutická kompozícia, ktorá ju obsahuje, a jej použitie |
Country Status (26)
Country | Link |
---|---|
EP (1) | EP1252155B1 (sk) |
JP (1) | JP2003520798A (sk) |
KR (1) | KR100825530B1 (sk) |
CN (1) | CN1395577A (sk) |
AR (1) | AR027226A1 (sk) |
AT (1) | ATE284400T1 (sk) |
AU (1) | AU2001230869A1 (sk) |
BR (1) | BR0107724A (sk) |
CA (1) | CA2397594C (sk) |
CZ (1) | CZ301235B6 (sk) |
DE (1) | DE60107652T2 (sk) |
DK (1) | DK1252155T3 (sk) |
EA (1) | EA005182B1 (sk) |
ES (1) | ES2228800T3 (sk) |
HU (1) | HU225155B1 (sk) |
IL (2) | IL150643A0 (sk) |
MX (1) | MXPA02006965A (sk) |
NO (1) | NO322626B1 (sk) |
NZ (1) | NZ520281A (sk) |
PL (1) | PL201690B1 (sk) |
PT (1) | PT1252155E (sk) |
SI (1) | SI1252155T1 (sk) |
SK (1) | SK287216B6 (sk) |
TW (1) | TWI293072B (sk) |
WO (1) | WO2001053294A1 (sk) |
ZA (1) | ZA200205640B (sk) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA3034875C (en) | 2016-08-23 | 2024-05-28 | Eisai R&D Management Co., Ltd. | Combination therapies for the treatment of hepatocellular carcinoma |
MA47776A (fr) | 2017-03-16 | 2020-01-22 | Eisai R&D Man Co Ltd | Polythérapies pour le traitement du cancer du sein |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IN164232B (sk) * | 1986-04-11 | 1989-02-04 | Hoechst India | |
US5284856A (en) * | 1988-10-28 | 1994-02-08 | Hoechst Aktiengesellschaft | Oncogene-encoded kinases inhibition using 4-H-1-benzopyran-4-one derivatives |
DE3836676A1 (de) * | 1988-10-28 | 1990-05-03 | Hoechst Ag | Die verwendung von 4h-1-benzopyran-4-on-derivaten, neue 4h-1-benzopyran-4-on-derivate und diese enthaltende arzneimittel |
US5908934A (en) * | 1996-09-26 | 1999-06-01 | Bristol-Myers Squibb Company | Process for the preparation of chiral ketone intermediates useful for the preparation of flavopiridol and analogs |
-
2001
- 2001-01-08 CZ CZ20022467A patent/CZ301235B6/cs not_active IP Right Cessation
- 2001-01-08 WO PCT/US2001/000520 patent/WO2001053294A1/en active IP Right Grant
- 2001-01-08 SI SI200130293T patent/SI1252155T1/xx unknown
- 2001-01-08 ES ES01902993T patent/ES2228800T3/es not_active Expired - Lifetime
- 2001-01-08 JP JP2001553768A patent/JP2003520798A/ja active Pending
- 2001-01-08 KR KR1020027009140A patent/KR100825530B1/ko not_active IP Right Cessation
- 2001-01-08 CN CN01803857A patent/CN1395577A/zh active Pending
- 2001-01-08 CA CA2397594A patent/CA2397594C/en not_active Expired - Fee Related
- 2001-01-08 PT PT01902993T patent/PT1252155E/pt unknown
- 2001-01-08 PL PL355992A patent/PL201690B1/pl not_active IP Right Cessation
- 2001-01-08 EA EA200200776A patent/EA005182B1/ru not_active IP Right Cessation
- 2001-01-08 IL IL15064301A patent/IL150643A0/xx unknown
- 2001-01-08 BR BR0107724-4A patent/BR0107724A/pt not_active Application Discontinuation
- 2001-01-08 SK SK1037-2002A patent/SK287216B6/sk not_active IP Right Cessation
- 2001-01-08 MX MXPA02006965A patent/MXPA02006965A/es active IP Right Grant
- 2001-01-08 DE DE60107652T patent/DE60107652T2/de not_active Expired - Lifetime
- 2001-01-08 AT AT01902993T patent/ATE284400T1/de active
- 2001-01-08 HU HU0204297A patent/HU225155B1/hu not_active IP Right Cessation
- 2001-01-08 NZ NZ520281A patent/NZ520281A/en not_active IP Right Cessation
- 2001-01-08 DK DK01902993T patent/DK1252155T3/da active
- 2001-01-08 AU AU2001230869A patent/AU2001230869A1/en not_active Abandoned
- 2001-01-08 EP EP01902993A patent/EP1252155B1/en not_active Expired - Lifetime
- 2001-01-17 AR ARP010100186A patent/AR027226A1/es not_active Application Discontinuation
- 2001-01-17 TW TW090101052A patent/TWI293072B/zh not_active IP Right Cessation
-
2002
- 2002-07-08 IL IL150643A patent/IL150643A/en not_active IP Right Cessation
- 2002-07-12 NO NO20023385A patent/NO322626B1/no not_active IP Right Cessation
- 2002-07-15 ZA ZA200205640A patent/ZA200205640B/en unknown
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PC4A | Assignment and transfer of rights |
Owner name: AVENTIS HOLDINGS INC., GREENVILLE, DELAWARE, US Free format text: FORMER OWNER: HMR PHARMA, INC., GREENVILLE, DELAWARE, US Effective date: 20011228 Owner name: HMR PHARMA, INC., GREENVILLE, DELAWARE, US Free format text: FORMER OWNER: AVENTIS PHARMACEUTICALS INC., BRIDGEWATER, NJ, US Effective date: 20011228 |
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Owner name: AVENTISUB II INC., GREENVILLE, DELAWARE, US Free format text: FORMER OWNER: AVENTIS HOLDINGS INC., GREENVILLE, DELAWARE, US Effective date: 20100303 |
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MM4A | Patent lapsed due to non-payment of maintenance fees |
Effective date: 20140108 |