HRP20120791T1 - Derivati 5-hidroksimetil-oksazolidin-2-ona za lijeäśenje bakterijskih bolesti crijeva - Google Patents
Derivati 5-hidroksimetil-oksazolidin-2-ona za lijeäśenje bakterijskih bolesti crijeva Download PDFInfo
- Publication number
- HRP20120791T1 HRP20120791T1 HRP20120791AT HRP20120791T HRP20120791T1 HR P20120791 T1 HRP20120791 T1 HR P20120791T1 HR P20120791A T HRP20120791A T HR P20120791AT HR P20120791 T HRP20120791 T HR P20120791T HR P20120791 T1 HRP20120791 T1 HR P20120791T1
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- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- formula
- prevention
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- 208000028774 intestinal disease Diseases 0.000 title claims 9
- 230000001580 bacterial effect Effects 0.000 title claims 2
- LSYOFPBORRARMF-UHFFFAOYSA-N 5-(hydroxymethyl)-1,3-oxazolidin-2-one Chemical class OCC1CNC(=O)O1 LSYOFPBORRARMF-UHFFFAOYSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 230000002265 prevention Effects 0.000 claims 9
- 241000193163 Clostridioides difficile Species 0.000 claims 8
- 241000193468 Clostridium perfringens Species 0.000 claims 6
- 241000191967 Staphylococcus aureus Species 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 241000894006 Bacteria Species 0.000 claims 4
- 108010059993 Vancomycin Proteins 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 210000000936 intestine Anatomy 0.000 claims 4
- 229960003165 vancomycin Drugs 0.000 claims 4
- MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims 4
- MYPYJXKWCTUITO-LYRMYLQWSA-O vancomycin(1+) Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C([O-])=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)[NH2+]C)[C@H]1C[C@](C)([NH3+])[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-O 0.000 claims 4
- 206010012735 Diarrhoea Diseases 0.000 claims 2
- 231100000249 enterotoxic Toxicity 0.000 claims 2
- 230000002242 enterotoxic effect Effects 0.000 claims 2
- XWFCFMXQTBGXQW-GOSISDBHSA-N cadazolid Chemical group O=C1O[C@@H](CO)CN1C(C=C1F)=CC=C1OCC1(O)CCN(C=2C(=CC=3C(=O)C(C(O)=O)=CN(C=3C=2)C2CC2)F)CC1 XWFCFMXQTBGXQW-GOSISDBHSA-N 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
Classifications
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P31/14—Antivirals for RNA viruses
-
- 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
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (14)
1. Spoj, naznačen time, da ima formulu (I)
[image]
gdje A je N ili CH; te
n je 0 ili 1;
ili njegova farmaceutski prihvatljiva sol, koji služi za uporabu u prevenciji ili liječenju crijevnih bolesti uzrokovanih bakterijama odabranima od Clostridium difficile, Clostridium perfringens ili Staphylococcus aureus.
2. Spoj formule I prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu kako je navedeno u zahtjevu 1, pri čemu A je CH.
3. Spoj formule I prema zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu kako je navedeno u zahtjevu 1, pri čemu n je 1.
4. Spoj formule I određen u zahtjevu 1, naznačen time, da je odabran od sljedećih:
-1-ciklopropil-6-fluoro-7-{4-[2-fluoro-4-((R)-5-hidroksimetil-2-okso-oksazolidin-3-il)-fenoksimetil]-4-hidroksi-piperidin-1-il}-4-okso-1,4-dihidro-kinolin-3-karboksilna kiselina;
-1-ciklopropil-6-fluoro-7-{4-[2-fluoro-4-((R)-5-hidroksimetil-2-okso-oksazolidin-3-il)-fenoksimetil]-4-hidroksi-piperidin-1-il}-4-okso-1,4-dihidro-[1,8]naftiridin-3-karboksilna kiselina; i
-1-ciklopropil-6-fluoro-7-{3-[2-fluoro-4-((R)-5-hidroksimetil-2-okso-oksazolidin-3-il)-fenoksimetil]-3-hidroksi-pirolidin-1-il}-4-okso-1,4-dihidro-kinolin-3-karboksilna kiselina;
ili njegova farmaceutski prihvatljiva sol, koji služi za uporabu u prevenciji ili liječenju crijevnih bolesti koje su uzrokovane bakterijama odabranima od Clostridium difficile, Clostridium perfringens ili Staphylococcus aureus.
5. Spoj formule I prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je to 1-ciklopropil-6-fluoro-7-{4-[2-fluoro-4-((R)-5-hidroksimetil-2-okso-oksazolidin-3-il)-fenoksimetil]-4-hidroksi-piperidin-1-il}-4-okso-1,4-dihidro-kinolin-3-karboksilna kiselina ili njezina farmaceutski prihvatljiva sol, te služi u prevenciji ili liječenju crijevnih bolesti uzrokovanih bakterijama odabranima od Clostridium difficile, Clostridium perfringens ili Staphylococcus aureus.
6. Spoj formule I prema jednom od zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u prevenciji ili liječenju crijevnih bolesti koje su uzrokovane sa Clostridium difficile.
7. Spoj formule I prema jednom od zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u prevenciji ili liječenju crijevnih bolesti uzrokovanih bakterijskim sojem Clostridium difficile koji proizvodi toksin.
8. Spoj formule I prema jednom od zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u prevenciji ili liječenju bolesti diareje povezanih s enterotoksičnim sojevima od Clostridium difficile, Clostridium perfringens ili Staphilococcus aureus, bez povećanja koncentracije enterokoka otpornih na vankomicin u crijevima.
9. Spoj formule I prema jednom od zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u prevenciji ili liječenju bolesti diareje povezanih s enterotoksičnim sojevima od Clostridium difficile, Clostridium perfringens ili Staphilococcus aureus, ujedno za smanjenje koncentracije enterokoka otpornih na vankomicin u crijevima.
10. Uporaba spoja formule I prema jednom od zahtjeva 1 do 5, ili njegove farmaceutski prihvatljive soli, naznačena time, da je za proizvodnju lijeka namijenjenog za prevenciju ili liječenje crijevne bolesti uzrokovane bakterijom odabranom od Clostridium difficile, Clostridium perfringens ili Staphilococcus aureus.
11. Uporaba prema zahtjevu 10, naznačena time, da je proizvedeni lijek namijenjen za liječenje crijevne bolesti.
12. Uporaba prema zahtjevu 10, naznačena time, da je proizvedeni lijek namijenjen za prevenciju crijevne bolesti.
13. Uporaba prema zahtjevu 10, naznačena time, da je proizvedeni lijek također namijenjen da spriječi povećanje koncentracije enetrokoka otpornih na vankomicin u crijevima.
14. Uporaba prema zahtjevu 10, naznačena time, da je proizvedeni lijek također namijenjen za smanjivanje koncentracije enetrokoka otpornih na vankomicin u crijevima.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IBPCT/IB2008/051854 | 2008-05-09 | ||
| PCT/IB2009/051896 WO2009136379A1 (en) | 2008-05-09 | 2009-05-08 | 5-hydroxymethyl-oxazolidin-2-one derivatives for treating bacterial intestinal diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120791T1 true HRP20120791T1 (hr) | 2012-11-30 |
Family
ID=40955145
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120791AT HRP20120791T1 (hr) | 2008-05-09 | 2012-10-03 | Derivati 5-hidroksimetil-oksazolidin-2-ona za lijeäśenje bakterijskih bolesti crijeva |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP2296651B1 (hr) |
| JP (1) | JP4819980B2 (hr) |
| KR (1) | KR101283222B1 (hr) |
| CN (1) | CN102014903B (hr) |
| AR (1) | AR071762A1 (hr) |
| AU (1) | AU2009245351B2 (hr) |
| BR (1) | BRPI0911991B8 (hr) |
| CA (1) | CA2723232C (hr) |
| CY (1) | CY1113197T1 (hr) |
| DK (1) | DK2296651T3 (hr) |
| ES (1) | ES2390405T3 (hr) |
| HK (1) | HK1155086A1 (hr) |
| HR (1) | HRP20120791T1 (hr) |
| IL (1) | IL209105A0 (hr) |
| MA (1) | MA32375B1 (hr) |
| MX (1) | MX2010011918A (hr) |
| MY (1) | MY156304A (hr) |
| NZ (1) | NZ589734A (hr) |
| PL (1) | PL2296651T3 (hr) |
| PT (1) | PT2296651E (hr) |
| RU (1) | RU2527769C2 (hr) |
| SI (1) | SI2296651T1 (hr) |
| TW (1) | TWI447115B (hr) |
| WO (1) | WO2009136379A1 (hr) |
| ZA (1) | ZA201008841B (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003031443A1 (en) | 2001-10-04 | 2003-04-17 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Dual actions antibiotics comprising a oxazoldinone and a quinolone or naphthyridinone moiety |
| WO2004096221A1 (en) | 2003-04-30 | 2004-11-11 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections |
| DE10340485B4 (de) | 2003-09-03 | 2015-05-13 | Morphochem AG Aktiengesellschaft für kombinatorische Chemie | Verfahren zur Herstellung von Oxazolidinon-Chinolon Hybriden |
| CA2549675C (en) | 2003-12-18 | 2012-11-20 | Morphochem Aktiengesellschaft Fur Kombinatorische Chemie | Oxazolidinone-quinolone hybrid antibiotics |
| US8158797B2 (en) | 2003-12-18 | 2012-04-17 | Morphochem Aktiengesellschaft Fur Kombinatorische Chemie | Oxazolidinone-quinolone hybrid antibiotics |
| WO2014191075A1 (en) * | 2013-05-28 | 2014-12-04 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Oxazolidinone-quinolone hybrid antibacterials for the parenteral treatment or prophylaxis of bacterial diseases |
| US9993469B2 (en) * | 2013-05-28 | 2018-06-12 | Morphochem Aktiengesellschaft Für Kombinatorishe Chemie | Combination therapy comprising oxazolidinone-quinolones for use in treating bacterial infections |
| US10087171B2 (en) | 2016-12-19 | 2018-10-02 | Actelion Pharmaceuticals Ltd | Crystalline forms of cadazolid |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU1156597A3 (ru) * | 1982-04-28 | 1985-05-15 | Е.И.Дюпон Де Немур Энд Компани (Фирма) | Способ получени производных 3-( @ -алкилсульфонилфенил)оксазолидинона или их фармацевтически приемлемых кислотно-аддитивных солей |
| US4461773A (en) * | 1982-09-15 | 1984-07-24 | E. I. Dupont De Nemours And Company | P-Oxooxazolidinylbenzene compounds as antibacterial agents |
| US6689769B2 (en) * | 2000-12-21 | 2004-02-10 | Pharmacia & Upjohn Company | Antimicrobial quinolone derivatives and use of the same to treat bacterial infections |
| ES2186550B2 (es) * | 2001-06-27 | 2003-11-16 | Vita Lab | Nuevos derivados de oxazolidinonas como antibacterianos. |
| WO2003031443A1 (en) * | 2001-10-04 | 2003-04-17 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Dual actions antibiotics comprising a oxazoldinone and a quinolone or naphthyridinone moiety |
| WO2004096221A1 (en) * | 2003-04-30 | 2004-11-11 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections |
| KR100854211B1 (ko) | 2003-12-18 | 2008-08-26 | 동아제약주식회사 | 신규한 옥사졸리디논 유도체, 그의 제조방법 및 이를유효성분으로 하는 항생제용 약학 조성물 |
| DK2086968T3 (da) * | 2006-11-10 | 2012-03-19 | Actelion Pharmaceuticals Ltd | 5-hydroxymethyl-oxazolidin-2-on-derivater |
-
2009
- 2009-05-08 PL PL09742552T patent/PL2296651T3/pl unknown
- 2009-05-08 EP EP09742552A patent/EP2296651B1/en active Active
- 2009-05-08 KR KR1020107025774A patent/KR101283222B1/ko active IP Right Grant
- 2009-05-08 CA CA2723232A patent/CA2723232C/en active Active
- 2009-05-08 SI SI200930338T patent/SI2296651T1/sl unknown
- 2009-05-08 CN CN2009801143512A patent/CN102014903B/zh active Active
- 2009-05-08 ES ES09742552T patent/ES2390405T3/es active Active
- 2009-05-08 BR BRPI0911991A patent/BRPI0911991B8/pt active IP Right Grant
- 2009-05-08 WO PCT/IB2009/051896 patent/WO2009136379A1/en active Application Filing
- 2009-05-08 DK DK09742552.4T patent/DK2296651T3/da active
- 2009-05-08 AU AU2009245351A patent/AU2009245351B2/en active Active
- 2009-05-08 RU RU2010149994/15A patent/RU2527769C2/ru active
- 2009-05-08 PT PT09742552T patent/PT2296651E/pt unknown
- 2009-05-08 JP JP2011508044A patent/JP4819980B2/ja active Active
- 2009-05-08 MX MX2010011918A patent/MX2010011918A/es active IP Right Grant
- 2009-05-08 TW TW098115466A patent/TWI447115B/zh active
- 2009-05-08 AR ARP090101672A patent/AR071762A1/es unknown
- 2009-05-08 NZ NZ589734A patent/NZ589734A/xx unknown
- 2009-05-08 MY MYPI2010005226A patent/MY156304A/en unknown
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2010
- 2010-11-04 IL IL209105A patent/IL209105A0/en active IP Right Grant
- 2010-12-03 MA MA33391A patent/MA32375B1/fr unknown
- 2010-12-08 ZA ZA2010/08841A patent/ZA201008841B/en unknown
-
2011
- 2011-09-06 HK HK11109417.3A patent/HK1155086A1/xx unknown
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2012
- 2012-10-03 HR HRP20120791AT patent/HRP20120791T1/hr unknown
- 2012-10-12 CY CY20121100949T patent/CY1113197T1/el unknown
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