Nova Patents
IS1995B

Triazole derivatives useful in therapy

Abstract

The invention provides compounds of formula (I) :R<1>-OP(O)(OH)2, wherein R<1> represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful in the treatment of fungal infections, and have good aqueous solubility.

Term

Term ended

Expired 26 June 2018, 8.2 years ago.

  1. Priority
  2. Filed
  3. Granted
  4. Expired
  5. Today

13 claims: 12 independent, 1 dependent

  1. 1
    Krtfiir Krtfiir 1. Efoasamband með formúlu I, An compound of formula I, R'-OP (O) (OH) a in pairs as R1 represents the non-hydroxy portion of the triazole antisense compound of the species consisting of a tri-hydroxyl group;R’-OP(O)(OH)a I par sem R1 táknar hlutann án hýdroxý hjá tríasól andsveppa efaasambandinu af tegundinni sem samanstendur af þrígreindum hýdroxýhóp;eða lyfjafræðilega hæft salt par af. or a pharmaceutically acceptable salt pair.
  2. 3
    Compound as shown in krdfo 2, pair as R2 is 2,4-difluorophenyl. 3. Efoasamband eins og kemur fram i krdfo 2, par sem R2 er 2,4diflúrfenýl.
  3. 4
    Eftiasamband eins og kemur fram ί krdfo 2 eda krdfo 3, par sem R3 er H eða metýl. 4. Relationship as stated in the following paragraphs:3 is H or methyl.
  4. 5
    Efoasamband eins og kemur fram i hverri sem er af krdfum 2 til 4, þar sem R4 táknar eða samanstendur af triasólýl, pýrimídínýl eða þiasólýl hópl. A compound as claimed in any one of claims 2 to 4, wherein R4 represents or consists of triazolyl, pyrimidinyl or thiazolyl group.
  5. 6
    Eftiasamband eins og kemur fram i hverri sem er af undanfarandi 5 krdfum, sem er 2-(2,4-diflúrfenýl)-l,3-bls(lH-l,2,4-tríasól-l-ýl)-2própýl tvivetnis fosfat;eða (2R,3S)-2-(2,4-diflúrfenýl)-3-(5-flúr-4pýrimídmýl)-l-(lH-l,2,4-tríasól-l-ýl)-2-bútýl tvivetnis fosfat;eða lyfjafræðllega hæft salt þar af. A compound as claimed in any one of the preceding claims, which is 2- (2,4-difluorophenyl) -1,3-bis (1H-1,2,4-triazol-1-yl) -2-propyl tvivetnis phosphate;or (2R, 3S) -2- (2,4-difluorophenyl) -3- (5-fluoro-4-pyrimidinyl) -1- (1H-1,2,4-triazol-1-yl) -2-butyl triphenylphosphate ;or a pharmaceutically acceptable salt thereof.
  6. 7
    Lyfjasamsetning, sem samanstendur af Efnasambandi meti formúlu 1, eins og skilgreint er ί krdfii 1, eda lyfjafræðilega hæft salt þar af i bldndu með fyfjafræðllega hæfu hjálparefni, þynningarefni eda burdarefni. A pharmaceutical composition comprising a compound of formula 1 as defined in claim 1, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable excipient, diluent as a carrier.
  7. 8
    Eftiasamband með formúlu I, eins og skilgreint er ί krdfii 1, eda lyfjafrædllega hæft salt þar af, til notkunar sem læknislyf. A compound of formula I as defined in claim 1, or a pharmaceutically acceptable salt thereof, for use as a medicament.
  8. 9
    Notkun á eftiasambandi med formúlu 1, eins og skilgreint er i krdfii 1, eda lyfjafræðilega hæfu salti þar af vid framleidslu á laeknislyfi til ad medhdndla eda hindra sveppa sýkinga. Use of a compound of formula 1 as defined in claim 1, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for the treatment of fungal infections.
  9. 10
    A process for preparing a compound of Formula 1, as defined in claim 1, of a pharmaceutically acceptable salt thereof, comprising phosphorylation of Formula I, 10. Adferd fyrir framleidslu á Efnasambandi med formulu 1, eins og skilgreint er ί krdfii 1, eda lyfjafrsdilega hæfu salti þar af sem felst i fosfórun á eftiasambandi med formulu Π, ROH Π where R1 is as defined in claim 1;ROH Π þar sem R1 er eins og skilgreint er ί krdfii 1;and where your damn it is worthy is og þar, sem þess er dskad eda þad er naudsynlegt, er Efnasambandinu, sem faest, breytt í lyfjafrsdilega hæft salt eda fifugt. The resulting compound is converted to a pharmaceutically acceptable salt.
  10. 11
    A process as claimed in the present invention, in which the hydroxy protecting groups are derived from the compound of formula V 11. Adferd eins og fram kemur ί krdfii 10 sem felst í ad fjarlsgja hýdroxý vemdarhópana frá eftiasambandi med fonnúlu V R1-0P (O) (ORc) [OR 'I) where R1 is defined and defined in claim 1 and rc and r0 stand independently for hydroxy protecting groups selected from benzyl optionally substituted by one or more halogen atoms. R1-0P(O)(ORc)[OR‘I) þar sem R1 er elns og skilgreint er i kröfu 1 og Rc og R0 standa óháö öðru fyrir hýdroxý vemdarhópa sem eru valdir úr bensýl sem er mögulega setlð með einu eða fleiri halogen atdmum.
  11. 12
    A compound of formula V and defined in claim 11. 12. Efhasamband með formúlu V elns og skilgreint er f krfifu 11.
  12. 13
    A method of treating water solubility in a triazole antiparasitic compound of the species consisting of trihydric hydroxide which is converted into the three-membered hydroxy group in OPIO) (OH)2 a group, or a pharmaceutically acceptable salt thereof. 13. Aðferö til ad baeta vatnsleysnl hjá triasól andsveppa efiiasambandi af tegundlnnl, sem samanstendur af þrigrelndum hýdroxý hop, sem feist í þvi að breyta þrígreinda hýdroxý hópnum í OPÍO)(OH)2 hóp, eða fyfjafraedilega hæfii salti þar af.
Independent claims12