HRP20130959T1 - Antikancerozni spojevi i farmaceutski pripravci koji ih sadrže - Google Patents
Antikancerozni spojevi i farmaceutski pripravci koji ih sadrže Download PDFInfo
- Publication number
- HRP20130959T1 HRP20130959T1 HRP20130959AT HRP20130959T HRP20130959T1 HR P20130959 T1 HRP20130959 T1 HR P20130959T1 HR P20130959A T HRP20130959A T HR P20130959AT HR P20130959 T HRP20130959 T HR P20130959T HR P20130959 T1 HRP20130959 T1 HR P20130959T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- compound
- image
- group
- benzimidazole
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 20
- 230000001093 anti-cancer Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 229940124639 Selective inhibitor Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Classifications
-
- 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
- C07D471/04—Ortho-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
- A61K31/435—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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/26—Oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (15)
1. Spoj, naznačen time što je spoj formule (I):
[image]
.
2. Spoj u skladu s patentnom zahtjevom 1, naznačen time što je u svom lijevokretnom obliku.
3. Spoj u skladu s patentnom zahtjevom 2, naznačen time što pokazuje optičko zakretanje [α]D = –38,6 ± 0,7 u koncentraciji od 0,698 mg/ml u metanolu.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je u obliku baze ili adicijske soli s kiselinom, osobito s farmaceutski prihvatljivom kiselinom.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što se upotrebljava kao selektivni inhibitor Aurora A i B kinaze.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što se upotrebljava kao antikancerozno sredstvo.
7. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačena time što je spoj namijenjen pripravi medikamenta za liječenje raka.
8. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6 i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
9. Medikament, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6.
10. Postupak dobivanja spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što se sastoji u:
■ međusobnoj reakciji tri niže prikazane komponente, gdje PG označuje zaštitnu skupinu za funkcionalnu skupinu NH u benzimidazolu
[image]
kako bi se dobio spoj:
[image]
;
■ uklanjanju zaštite s funkcionalne skupine NH u benzimidazolu, kako bi se dobio spoj formule (I);
■ kada je to prikladno, izdvajanju lijevokretnog spoja.
11. Postupak u skladu s patentnom zahtjevom 10, naznačen time što reakcija između tri spoja se provodi u alkoholu na refluksu, osobito u 1-butanolu.
12. Postupak u skladu s bilo kojim od patentnih zahtjeva 10 do 11, naznačen time što PG predstavlja skupinu
[image]
.
13. Spoj, naznačen time što ga se bira iz sljedećeg spiska:
[image]
,
gdje PG označuje zaštitnu skupinu za funkcionalnu skupinu NH u benzimidazolu.
14. Spoj u skladu s patentnom zahtjevom 13, naznačen time što PG predstavlja skupinu
[image]
.
15. Upotreba spoja u skladu s patentnim zahtjevom 13 ili 14, naznačena time što se spoj upotrebljava kao međuprodukt u dobivanju spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 4.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0902392A FR2945535B1 (fr) | 2009-05-18 | 2009-05-18 | Compose anticancereux et composition pharmaceutique le contenant |
PCT/FR2010/050948 WO2010133794A1 (fr) | 2009-05-18 | 2010-05-17 | Compose anticancéreux et composition pharmaceutique le contenant |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20130959T1 true HRP20130959T1 (hr) | 2013-11-22 |
Family
ID=40973187
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20130959AT HRP20130959T1 (hr) | 2009-05-18 | 2013-10-09 | Antikancerozni spojevi i farmaceutski pripravci koji ih sadrže |
Country Status (35)
Country | Link |
---|---|
US (2) | US9073917B2 (hr) |
EP (1) | EP2432766B1 (hr) |
JP (1) | JP5656981B2 (hr) |
KR (1) | KR20120032483A (hr) |
CN (1) | CN102459193B (hr) |
AR (1) | AR076686A1 (hr) |
AU (1) | AU2010251013B2 (hr) |
BR (1) | BRPI1012201A2 (hr) |
CA (1) | CA2762233C (hr) |
CL (1) | CL2011002930A1 (hr) |
CO (1) | CO6400138A2 (hr) |
CY (1) | CY1114850T1 (hr) |
DK (1) | DK2432766T3 (hr) |
EA (1) | EA021084B1 (hr) |
ES (1) | ES2430989T3 (hr) |
FR (1) | FR2945535B1 (hr) |
HK (1) | HK1167388A1 (hr) |
HR (1) | HRP20130959T1 (hr) |
IL (1) | IL216361A0 (hr) |
JO (1) | JO2852B1 (hr) |
MA (1) | MA33356B1 (hr) |
ME (1) | ME01542B (hr) |
MX (1) | MX2011012356A (hr) |
MY (1) | MY152995A (hr) |
NZ (1) | NZ596464A (hr) |
PL (1) | PL2432766T3 (hr) |
PT (1) | PT2432766E (hr) |
RS (1) | RS53002B (hr) |
SG (1) | SG176169A1 (hr) |
SI (1) | SI2432766T1 (hr) |
SM (1) | SMT201400005B (hr) |
TW (1) | TWI441822B (hr) |
UY (1) | UY32644A (hr) |
WO (1) | WO2010133794A1 (hr) |
ZA (1) | ZA201108447B (hr) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2945535B1 (fr) | 2009-05-18 | 2011-06-10 | Sanofi Aventis | Compose anticancereux et composition pharmaceutique le contenant |
FR2967413A1 (fr) * | 2010-11-17 | 2012-05-18 | Sanofi Aventis | Compose 8-oxo-9-[3-(1h-benzimidazol-2-yloxy)-phenyl]-4,5,6,7,8,9-hexahydro-2h-pyrrolo[3,4-b]quinoline-3-carboxylate d'ethyle, sel, forme cristalline, co-cristal, formulation, procedes de preparation, application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteur des kinases aurora. |
ES2719776T3 (es) * | 2012-10-12 | 2019-07-16 | Broad Inst Inc | Inhibidores de GSK3 y métodos de uso de los mismos |
TW201609751A (zh) | 2014-07-01 | 2016-03-16 | 武田藥品工業股份有限公司 | 雜環化合物 |
SG11201909115WA (en) | 2017-04-05 | 2019-10-30 | Broad Inst Inc | Tricyclic compounds as glycogen synthase kinase 3 (gsk3) inhibitors and uses thereof |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001036422A1 (en) | 1999-11-19 | 2001-05-25 | Abbott Laboratories | Tricyclic dihydropyrimidine potassium channel openers |
CN1630656A (zh) | 2001-02-02 | 2005-06-22 | 三菱制药株式会社 | 二氢吡唑并吡啶化合物及其制药用途 |
US7037902B2 (en) | 2002-07-03 | 2006-05-02 | Receptron, Inc. | Affinity small molecules for the EPO receptor |
AU2004264834A1 (en) * | 2003-06-13 | 2005-02-24 | Zentaris Gmbh | Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof |
DK1746097T3 (da) * | 2005-07-20 | 2010-05-25 | Aventis Pharma Sa | 1,4-dihydropyridin-kondenserede heterocykliske ringe, fremgangsmåde til fremstilling af disse, anvendelse og sammensætninger, der indeholder dem |
FR2945535B1 (fr) | 2009-05-18 | 2011-06-10 | Sanofi Aventis | Compose anticancereux et composition pharmaceutique le contenant |
-
2009
- 2009-05-18 FR FR0902392A patent/FR2945535B1/fr not_active Expired - Fee Related
-
2010
- 2010-05-16 JO JO2010163A patent/JO2852B1/en active
- 2010-05-17 NZ NZ596464A patent/NZ596464A/en not_active IP Right Cessation
- 2010-05-17 EP EP10728768.2A patent/EP2432766B1/fr active Active
- 2010-05-17 AR ARP100101705A patent/AR076686A1/es unknown
- 2010-05-17 PT PT107287682T patent/PT2432766E/pt unknown
- 2010-05-17 WO PCT/FR2010/050948 patent/WO2010133794A1/fr active Application Filing
- 2010-05-17 US US13/320,965 patent/US9073917B2/en not_active Expired - Fee Related
- 2010-05-17 BR BRPI1012201A patent/BRPI1012201A2/pt not_active IP Right Cessation
- 2010-05-17 PL PL10728768T patent/PL2432766T3/pl unknown
- 2010-05-17 ES ES10728768T patent/ES2430989T3/es active Active
- 2010-05-17 ME MEP-2013-121A patent/ME01542B/me unknown
- 2010-05-17 SI SI201030384T patent/SI2432766T1/sl unknown
- 2010-05-17 DK DK10728768.2T patent/DK2432766T3/da active
- 2010-05-17 AU AU2010251013A patent/AU2010251013B2/en not_active Ceased
- 2010-05-17 KR KR1020117030136A patent/KR20120032483A/ko active Search and Examination
- 2010-05-17 EA EA201171429A patent/EA021084B1/ru not_active IP Right Cessation
- 2010-05-17 MY MYPI2011005531 patent/MY152995A/en unknown
- 2010-05-17 MA MA34441A patent/MA33356B1/fr unknown
- 2010-05-17 TW TW099115713A patent/TWI441822B/zh not_active IP Right Cessation
- 2010-05-17 RS RS20130444A patent/RS53002B/en unknown
- 2010-05-17 SG SG2011085529A patent/SG176169A1/en unknown
- 2010-05-17 CA CA2762233A patent/CA2762233C/fr not_active Expired - Fee Related
- 2010-05-17 JP JP2012511323A patent/JP5656981B2/ja not_active Expired - Fee Related
- 2010-05-17 CN CN201080032327.7A patent/CN102459193B/zh not_active Expired - Fee Related
- 2010-05-17 MX MX2011012356A patent/MX2011012356A/es active IP Right Grant
- 2010-05-18 UY UY0001032644A patent/UY32644A/es not_active Application Discontinuation
-
2011
- 2011-11-14 IL IL216361A patent/IL216361A0/en unknown
- 2011-11-17 ZA ZA2011/08447A patent/ZA201108447B/en unknown
- 2011-11-18 CO CO11157425A patent/CO6400138A2/es active IP Right Grant
- 2011-11-18 CL CL2011002930A patent/CL2011002930A1/es unknown
-
2012
- 2012-08-15 HK HK12108002.5A patent/HK1167388A1/xx not_active IP Right Cessation
-
2013
- 2013-10-09 HR HRP20130959AT patent/HRP20130959T1/hr unknown
- 2013-10-17 CY CY20131100920T patent/CY1114850T1/el unknown
-
2014
- 2014-01-16 SM SM201400005T patent/SMT201400005B/xx unknown
-
2015
- 2015-06-02 US US14/728,846 patent/US9221817B2/en not_active Expired - Fee Related
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