SI3124481T1 - Modulatorji androgenskega receptorja in njihove uporabe - Google Patents

Modulatorji androgenskega receptorja in njihove uporabe Download PDF

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Publication number
SI3124481T1
SI3124481T1 SI201131455T SI201131455T SI3124481T1 SI 3124481 T1 SI3124481 T1 SI 3124481T1 SI 201131455 T SI201131455 T SI 201131455T SI 201131455 T SI201131455 T SI 201131455T SI 3124481 T1 SI3124481 T1 SI 3124481T1
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SI
Slovenia
Prior art keywords
diazaspiro
thioxo
oxo
octan
phenyl
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SI201131455T
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English (en)
Inventor
Nicholas D Smith
Celine Bonnefous
Jackaline D. Julien
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Aragon Pharmaceuticals, Inc.
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Publication of SI3124481T1 publication Critical patent/SI3124481T1/sl

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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Claims (15)

  1. Modulatorji androgenskega receptorja in njihove uporabe Patentni zahtevki
    1. A farmacevtski sestavek za uporabo v zdravljenju raka odvisnega od androgenskega receptorja ali pri katerem posreduje androgenski receptor, ki vsebuje od 0.5 mg do 1000 mg derivata 8-okso-6-tiokso-5,7-diazaspiro[3.4]oktana ali njegove farmacevtsko sprejemljive soli ali njegovega N-oksida, skupaj z vsaj enim farmacevtsko sprejemljivo neaktivno učinkovino, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro[3.4]oktana: 5-(5-(3-fluoro-4-(2-(pirolidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((1-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-morfolinoetoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro [3.4] oktan- 7-il)-3 -(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-morfolinopropoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-(4-metilpiperazin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(2-morfolinoetoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(3-morfolinopropoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro [3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(3-(4-metilpiperazin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-metilpikonitril; 5-(5-(3-fluoro-4-(2-(piperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-tiomorfolinoetoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(piperidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(tetrahidro-2H-piran-4-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5 -(5 -(2-fluoro-4-(3 -(4-metilpiperazin-1 -il)propoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-(pirolidin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-(2-(1, l-dioksidotiomorfolino)etoksi)-3-fluorofenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-(2-(piperidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(5-(4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)pikonitril; 5-(5-(3-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3 -metilpikonitril; 5-(5-(3-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(8-okso-5-(4-((tetrahidro-2H-piran-4-il)oksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)pikonitril; 3-metil-5-(8-okso-5-(4-((tetrahidro-2H-tiopiran-4-il)oksi)fenil)-6-tiokso-5,7-diazaspiro [3.4] oktan-7-il)pikonitril; 5 -(8-okso-5 -(4-((tetrahidro-2H-piran-4-il)oksi)fenil)-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 3-metil-5-(8-okso-6-tiokso-5-(4-(2-(4-(2,2,2-trifluoroetil)piperazin-l-il)etoksi)fenil)- 5,7-diazaspiro [3.4] oktan-7-il)pikonitril; 3-metil-5-(5-(4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)pikonitril; 5-(5-(4-(( l,l-Dioksidotetrahidro-2H-tiopiran-4-il)oksi)fenil)-8-okso-6-tiokso- 5,7-diazaspiro[3.4]oktan-7-il)-3-metilpikonitril; 5-(5-(4-(2-(4-acetilpiperazin-l-il)etoksi)-3-fluorofenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)pikonitril; 5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(8-okso-5-(4-((l-propionilpiperidin-4-il)oksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((1-izobutirilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; etil 4-(4-(7-(6-ciano-5-(trifluorometil)piridin-3-il)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-5-il)fenoksi)piperidin-1 -carboksilate; 5-(5-(4-((1 -acetilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -metilpikonitril; 5-(5-(4-((1-etilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -metilpikonitril; 5-(5-(4-((l-(2-hidroksietil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -metilpikonitril; 5-(5-(4-((1-(2-hidroksietil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((l-(metilsulfonil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((1-izopropilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; etil 2-(4-(4-(7-(6-ciano-5-(trifluorometil)piridin-3-il)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-5-il)fenoksi)piperidin-1 -il)acetat; 4- (4-(7-(6-ciano-5-(trifluorometil)piridin-3-il)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-5-il)fenoksi)piperidin-1 -karboksamid; ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  2. 2. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro [3,4]oktana: 5- (5-(4-(( 1 -metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(piperidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-(2-(piperidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(5-(4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4] oktan-7-il)pikonitril; 5-(5-(3-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-metilpikonitril; 5-(5-(3-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)pikonitril; 5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)- 3-(trifluorometil)pikonitril; 5-(8-okso-5-(4-((l-propionilpiperidin-4-il)oksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((l-izobutirilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; etil 4-(4-(7-(6-ciano-5-(trifluorometil)piridin-3-il)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-5-il)fenoksi)piperidin-1 -carboksilate; 5-(5-(4-((l-acetilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-metilpikonitril; 5-(5-(4-((1-etilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4] oktan-7-il)-3 -metilpikonitril; 5-(5-(4-((1-(2-Hidroksietil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4] oktan-7-il)-3 -metilpikonitril; 5-(5-(4-((l-(2-hidroksietil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((l-(metilsulfonil)piperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((1-izopropilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; etil 2-(4-(4-(7-(6-ciano-5-(trifluorometil)piridin-3-il)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-5 -il)fenoksi)piperidin-1 -il)acetat; 4- (4-(7-(6-ciano-5 -(trifluorometil)piridin-3 -il)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-5-il)fenoksi)piperidin-1 -karboksamid; ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  3. 3. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro[3.4]oktana: 5- (5-(3-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-(4-metilpiperazih-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(3-(4-metilpiperazin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-metilpikonitril; 5-(5-(3-fluoro-4-(2-(piperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro [3,4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(5-(4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(2-fluoro-4-(3-(4-metilpiperazin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 3-metil-5-(8-okso-6-tiokso-5-(4-(2-(4-(2,2,2-trifluoroetil)piperazin-l- il)etoksi)fenil)-5,7-diazaspiro[3.4]oktan-7-il)pikonitril; 3-metil-5-(5-(4-(2-(4-metilpiperazin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro [3.4] oktan-7-il)pikonitril; 5-(5-(4-(2-(4-acetilpiperazin-l-il)etoksi)-3-fluorofenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  4. 4. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro [3.4]oktana: 5-(5-(3-fluoro-4-(2-morfolinoetoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-morfolinopropoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(2-morfolinoetoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-fluoro-3-(3-morfolinopropoksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  5. 5. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro [3.4] oktana: 5-(5-(3-fluoro-4-(2-(pirolidin-l-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-tiomorfolinoetoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(2-(tetrahidro-2H-piran-4-il)etoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(3-fluoro-4-(3-(pirolidin-l-il)propoksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro [ 3.4]oktan-7-il)-3 -(trifluorometil)pikonitril; 3-metil-5-(8-okso-5-(4-((tetrahidro-2H-piran-4-il)oksi)fenil)-6-tiokso-5,7-diazaspiro [3.4] oktan-7-il)pikonitril; 3-metil-5-(8-okso-5-(4-((tetrahidro-2H-tiopiran-4-il)oksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)pikonitril; 5-(8-okso-5-(4-((tetrahidro-2H-piran-4-il)oksi)fenil)-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; 5-(5-(4-((1, l-Dioksidotetrahidro-2H-tiopiran-4-il)oksi)fenil)-8-okso-6-tiokso- 5,7-diazaspiro [3.4] oktan-7-il)-3 -metilpikonitril; 5-(5-(4-(2-(1,1 -Dioksidotiomorfolino)etoksi)-3-fluorofenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril; ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  6. 6. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro[3.4]oktana:
    ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  7. 7. Farmacevtski sestavek za uporabo po zahtevku 1, kjer je derivat 8-okso-6-tiokso-5,7-diazaspiro [3.4]oktana: (i) 5-(5-(4-((1 -metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (ii) 5-(5-(2-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso- 5.7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (iii) 3-metil-5-(5-(4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (iv) 5-(5-(3-fluoro-4-((l-metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso- 5.7- diazaspiro[3.4]oktan-7-il)-3-metilpikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (v) 5 -(5-(3 -fluoro-4-(( 1 -metilpiperidin-4-il)oksi)fenil)-8-okso-6-tiokso- 5.7- diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (vi) 3-metil-5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid; ali (vii) 5-(8-okso-5-(4-(piperidin-4-iloksi)fenil)-6-tiokso-5,7-diazaspiro[3.4]oktan-7-il)-3-(trifluorometil)pikonitril ali njegova farmacevtsko sprejemljiva sol ali njegov N-oksid.
  8. 8. Farmacevtski sestavek za uporabo po kateremkoli zahtevku od 1 do 7, kjer je odmerek za administracijo enkrat dnevno ali je razdeljen v odmerke za uporabo v intervalih preko dneva.
  9. 9. Farmacevtski sestavek za uporabo po kateremkoli zahtevku od 1 do 8, za uporabo v zdravljenju raka prostate ali raka dojke v pacientu, ki je človek.
  10. 10. Farmacevtski sestavek za uporabo po zahtevku 9, kjer je rak od hormonov odvisen rak.
  11. 11. Sestavek za uporabo po kateremkoli zahtevku od 1 do 10 v enem odmerku ali v razdeljenih odmerkih.
  12. 12. Farmacevtski sestavek za uporabo po kateremkoli zahtevku od 1 do 11, ki nadalje vsebuje dodatno farmacevtsko aktivno sredstvo, na primer sredstvo proti raku, na primer, kjer sredstvo proti raku vsebuje: (i) gosipol, genasense, polifenol E, klorofusin, vse trans-retinojsko kislino (ATRA), briostatin, ligand indukcije apoptoze, povezan s faktorjem tumorske nekroze, 5-aza-2’-deoksicitidin, vse trans-retinojsko kislino, doksorubicin, vinkristin, etopozid, gemcitabine, imatinib, geldanamicin, 17-N-alilamino-17-demetoksigeldanamicin (17-AAG), flavopiridol, LY294002, bortezomib, trastuzumab, ΒΑΥ 11-7082, PKC412 ali PD184352, paklitaksel ali analog paklitaksela, ali (ii) abirateron, adriamicin, daktinomicin, bleomicin, vinblastin, cisplatin, acivicin; aklarubicin; akodazol hidroklorid; akronin; adozelesin; aldeslevkin; altretamin; ambomicin; ametantron acetat; aminoglutetimid; amsakrin; anastrozol; antramicin; asparaginazo; asperlin; azacitidin; azetepo; azotomicin; batimastat; benzodepo; bikalutamid; bisantren hidroklorid; bisnafid dimesilat; bizelesin; bleomicin sulfat; brekinar natrij; bropirimin; busulfan; kaktinomicin; kalusteron; karacemid; karbetimer; karboplatin; karmustine; karubicin hidroklorid; karzelesin; cedefingol; klorambucil; cirolemicin; kladribin; krisnatol mesilat; ciklofosfamid; citarabin; dakarbazin; daunorubicin hidroklorid; decitabin; deksormaplatin; dezagvanin; dezagvanin mesilat; diazikon; doksorubicin; doksorubicin hidroklorid; droloksifen; droloksifen citrat; dromostanolon propionat; duazomicin; edatreksat; eflomitin hidroklorid; elsamitrucin; enloplatin; enpromat; epipropidin; epirubicin hidroklorid; erbulozol; esorubicin hidroklorid; estramustin; estramustin fosfat natrij; etanidazol; etoposid; etoposid fosfat; etoprin; fadrozol hidroklorid; fazarabin; fenretinid; floksuridin; fludarabin fosfat; fluorouracil; fluorocitabin; foskidon; fostriecin natrij; gemcitabin; gemcitabin hidroklorid; hidroksiureo; idarubicin hidroklorid; ifosfamid; iimofosin; interlevkin II (vključno z rekombinantnim interlevkinom II ali rlL2), interferon alfa-2a; interferon alfa-2b; interferon alfa-nl; interferon alfa-n3; interferon beta-1 a; interferon gama-1 b; iproplatin; irinotecan hidroklorid; lanreotid acetat; letrozol; leuprolid acetat; liarozol hidroklorid; lometreksol natrij; lomustin; losoksantron hidroklorid; mazoprokol; maitansin; mekloretamin hidroklorid; megestrol acetat; melengestrol acetat; melfalan; menogaril; mercaptopurin; metotreksat; metotreksat natrij; metoprin; meturedep; mitindomid; mitocarcin; mitocromin; mitogilin; mitomalcin; mitomicin; mitosper; mitotan; mitoksantron hidroklorid; mikofenolno kislino; nokodazol; nogalamicin; alimaplatin; oksisuran; pegaspargazo; peliomicin; pentamustin; peplomicin sulfat; perfosfamid; pipobroman; piposulfan; pirksantrone hidroklorid; plicamicin; plomestan; porfimer natrij; porfiromicin; prednimustin; prokarbazin hidroklorid; puromicin; puromicin hidroklorid; pirazofurin; riboprin; rogletimid; safingol; safingol hidroklorid; semustin; simtrazen; sparfosat natrij; sparsomicin; spirogermanium hidroklorid; spiromustin; spiroplatin; streptonigrin; streptozocin; sulofenur; talisomicin; tekogalan natrij; tegafur; teloksantron hidroklorid; temoporfin; tenipozide; teroksiron; testolacton; tiamiprin; tiogvanin; tiotep; tiazofurin; tirapazamin; toremifen citrat; trestolon acetat; triciribin fosfat; trimetreksat; trimetreksat glukuronat; triptorelin; tubulozol hidroklorid; uracil gorčica; uredepa; vapreotid; verteporfin; vinblastin sulfat; vinkristin sulfat; vindesin; vindesin sulfat; vinepidin sulfat; vinglicinat sulfat; vinleurozin sulfat; vinorelbin tartrat; vinrozidin sulfat; vinzolidin sulfat; vorozol; zeniplatin; zinostatin; ali zorubicin hidroklorid, ali (iii) Dolastatin 10, Mivobulin izetionat, Vinkristin, NSC-639829, Diskodermolid, ABT-751, Altorhirtine (kot na primer Altorhirtin A in Altorhirtin C), Spongistatine (kot na primer Spongistatin 1, Spongistatin 2, Spongistatin 3, Spongistatin 4, Spongistatin 5, Spongistatin 6, Spongistatin 7, Spongistatin 8 in Spongistatin 9), Cemadotin hidroklorid, Epotilone (kot na primer Epotilon A, Epotilon B, Epotilon C, Epotilon D, Epotilon E, Epotilon F, Epotilon B, N-oksid Epotilona A, 16-aza-Epotilon B, 21-aminoEpotilon B, 21-hidroksi Epotilon D, 26-fluoroEpotilon, Avristatin PE, Soblidotin, Vinkristin sulfat, Criptoficin 52, Vitilevuamid, Tubulizin A, Kanadensol, Centaureidin, Onkocidin Al Fijianolid B, Laulimalid, Narkozin, Naskapin, Hemiasterlin, Vanadocen acetilacetonat, Indanocin Eleuterobin (kot na primer Dezmetileleuterobin, Dezaetileleuterobin, Izoeleuterobin A in Z-Eleuterobin), Karibaeozid, Karibaeolin, Halihondrin B, Diazonamid A, Takalonolid A, Diozostatin, (-)-Fenilahistin, Mioseverin B ali Resverastatin fosfat natrij.
  13. 13. Farmacevtski sestavek za uporabo po zahtevku 12, kjer je dodatno farmacevtsko aktivno sredstvo antibiotik, antiestrogen, antiandrogen, analog hormona, ki sprošča gonadotropin, trombolitično sredstvo, antiemetično sredstvo, sredstvo uporabno v zdravljenju anemije, sredstvo uporabno v zdravljenju nevtropenije, kortikosteroid, analgetik, inhibitor kinaze, inhibitor HSP90, inhibitor histon deacetilaze (HDAC) ali ne-steroidno protivnetno zdravilo.
  14. 14. Farmacevtski sestavek za uporabo po kateremkoli zahtevku od 1 do 13, formulirano v oralni dozirni obliki.
  15. 15. Farmacevtski sestavek za uporabo po kateremkoli zahtevku od 1 do 14, formulirano v oralni dozirni obliki in, ki vsebuje derivat 8-okso-6-tiokso-5,7-diazaspiro[3.4]oktana v količini od 1 mg do 500 mg.
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