HUE030883T2 - Deuterált 1-piperazino-3-fenil-indánok, skizofrénia kezelésére - Google Patents

Deuterált 1-piperazino-3-fenil-indánok, skizofrénia kezelésére Download PDF

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HUE030883T2
HUE030883T2 HUE12748046A HUE12748046A HUE030883T2 HU E030883 T2 HUE030883 T2 HU E030883T2 HU E12748046 A HUE12748046 A HU E12748046A HU E12748046 A HUE12748046 A HU E12748046A HU E030883 T2 HUE030883 T2 HU E030883T2
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compound
deuterium
atom
phenyl
chloro
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Morten Jorgensen
Peter Hongaard Andersen
Klaus Gjervig Jensen
Mette Graulund Hvenegaard
Lassina Badolo
Mikkel Fog Jacobsen
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H Lundbeck As
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    • 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
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A—HUMAN NECESSITIES
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
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    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Claims (8)

  1. Deyteréit l-'pip^raiino^feryl-IndârKik, skizofrénia kataléséra SZARJU)A1:H1 IGEHY PONTOK 1, E.gy
    {V) képletü vegyulet amelyben R‘«RU> jelentései egymástél függétlenöí hidrogénatom vagy deutériumafom, ahol Rk.R':0 mindegyikének jelentése! deutérium. ahol az. R-~R10 legalább egyike legalább körülbelül 50% deutériumot tartalmaz.: vagy ennek egy gy og ys ze része ti I eg elfogadható savadé Icios sója.
  2. 2, Az 1. Igénypont szerint! vegyülök amelyben Ra~R' mindegyikének jelentése hidrogénatom, 3* Az 1« igénypont szerinti vegyútetasmelybbri mindegyikének jelentése deutériumsiom. 4, A 2. igénypont szerinti vegyület ahol a vegyület
    (ifi- S, A 2. igénypont szerinti vegyûiet ahol a vegyOiet
    CVíí). S, A 3. igénypont szerinti vegyuiet; ahoi a vegyulé!
    (ÍV), 7. A 3. igénypont szerinti vegyuieí, ahol a vegyülei
    (VI)- 8» Az 1. igénypont szerinti vegyület, amelyben R* és W mindegyikének jelén* lése üeutériumaiorn. i, A 8, igénypont szerinti vegyület, amelyben R3~R5 mindegyikének jelentése deutériumatom. 10. A 8. igénypont szerinti vegyület amelyben R3-Rs mindegyikének jelentése hidrogénatom
  3. 11. Az 1-10. igénypontok bármelyike szerinti vegyület amelyben a vegyület legalább körülbelül 8S%-a rendelkezik egy deutériumatommal minden deutérium* atomként megjelölt helyzetben, és bármely, deuíériumatornként nem jelölt atom körülbelül ennek természetes Izotópos gyakoriságában varr jelen.
  4. 12. Az 1-11. igénypontok bármelyike szerinti vegyület amelyben a vegyület legalább körülbelül 90%-a rendelkezik egy deutériumatommal minden deutérium* atomként megjelölt helyzetben, és bármely, deutériumatomként nem jelölt atom körülbelül ennek természetes Izotópos gyakoriságában van jelen,
  5. 13. Az 1. igénypont szerinti vegyület, ahol a vegyület a
    Élröpmtá rta rá tj a. 14. A 13. igénypont szerinti vegyület, ahol a vegyület ennek polimorf formájában van jelen, az XRPD diffrakciós mintázata pedig a 18. ébrén van meghatározva. 1S« A 13. igénypontok bármelyike szerinti vegyület, amelyben a vegyület legalább körülbelül 85%-a rendelkezik egy deuténumatommal minden deutérium-atomként megjelölt helyzetben, és bármely, d e úté ri u malom ként nem jelölt atom körülbelül ennek természetéé izoto^ jelen.
  6. 19. Gyógyszerkészítmény, amely tartalmazza az 141 ke szerinti vegyüietet valamint egy ;eÉ^Âiié vív#:. anyagot, oldószert vagy kötőanyagot: im á 11, f|Éőypenf szerinti gyógyszerkészítmény. ahoi a vegyidet a hid regé n -ta ria rát-sója.
    11» A 18. vagy 17. igénypont szerinti készítmény, amelyben a vivőanyag tartalmaz híciroxipropiklVcíkiodextrlnt vízben, és ifnetyben a vegyidet legalább 85%-a rendelkezik egy deuiénumatommal minden deutériunialomkénlmegjelölf helyzetben, és bármely, deuténumatomként nem jelölt atom körülbelül ennek természetes izotópos gyakoriságában van jelen. 1S. Az 1-15. igénypontok bármelyike szerinti vegyület vagy a 16-18. igénypontok bármelyike szerinti készítmény alkalmazása pszichizip más, psztobőtlküié tüneti-két. pszichotlkus rendellenességeket magában foglaló betegség vagy olyan betegségek kezelésére szolgáló gyógyszer előállítására, amely pszichotlkus tüneteket mutat 30. A 19. igénypont szerinti alkalmazás, ahol a pszichózis vagy a pszichotlkus tüneteket magában foglaló betegség skizofrénia, skízofrénía-jeííegú rendellenesség, Skizoaffektsv rendellenesség, hailucinációs rendellenesség, rövid pszichotlkus rendellenesség, osztott pszichotlkus rendellenesség, bipoláris rendellenesség vagy bipoláris rendellenességben jelentkező mánia. 21. A 19-20 igénypontok bármelyike szerinti alkalmazás, amely továbbá magiban foglal egy, m sertindol. olanzapin, őspepdort goeflpio, anpiprazoi, hálopenlei, clozapine, zíprasldon és az esanetant által alkotott csoportból kiválasztott vegyüféíet. 22. A 19-20, igénypontok bármelyike szerinti alkalmazás, ahol a pszichózis vagy a pszlchotíkus tüneteket magában foglaló betegség skizofrénia. 23, A 19-20 igénypontok bármelyike s^mi alkalmazás, ahol a pszichózis vagy a pszlchotíkus tüneteket magéban foglaló betegség skizofrénia, ahol a gyógy-aiérkêélft.nii^: lártafraieiía
    hibrögén-fartérifesé|éhak égy hatékony mennyiségét valamint Ndroxipröpil-ß-cikfo-élkftht vízben, és a (IV) legalább körülbelül 8S%-a rendelkezik egy áeuténumatom-mál nifndso^^ megtérít helyzetben. és bármely, deutériumatoio- ként nem leiéit atom izetópos gyakonsáiáfean van jelen. 14 A
    képieíű vegyidet. 2$, Eljárás a
    képiéül vegyiket elbáiiitására, amely magában foglalja a
    íXAb vegyületnek [(S)-BlhlAP]Rh(i}BF*~el való kezelését 2$, A 25. igénypont szedné eljárás, amelyben az [($}'8ÍNAP1Rb{í}BF<í--et katalitikus mennyiségben alkalmazzuk,
  7. 27, Eljárás a ÍXIV) vegyüiet előállítására, amely magában foglalja a) a
    S' <XH) yegyáletnek blszlpínákoláfldibór-al való kezelését, és b} 2"brôm~5--klôr-benzaldehk!dei való kezelését. 28, A 27, igénypont szerinti eljárás, amelyben a
    iXii) vegyületnek bisz{pinakοIát}clibór - a I való kezelése továbbá magában foglalja Pdfll) m Ä 28, Igénypont szerinti eljárás, amelyben a 2-brôrn-5-kiór-henzaidehkidel való kezelés továbbá magában foglalja Pd(Ö) hozzáadását is,
  8. 30, Eljárás C1R.3S}-gV) iartaraf vegyiket előállítására, amely magában foglalja raoérn transz-1 -(6-ktör-3-fenil(ds)>incían-1 díRI(ás), 2.2-trimeUI-piperazínnak L-{+)« -borosfyánkösavval való kezelését 31, a 30. igénypont szerinti mmtyimn. M itóm ïmmz-HWMSr -fenilCdsHndan-l -AM (els), 2,2-tnrnetíi-pipérazint -énnek megfelelő szukosnát-sójából hozzuk léire.
HUE12748046A 2011-06-20 2012-06-19 Deuterált 1-piperazino-3-fenil-indánok, skizofrénia kezelésére HUE030883T2 (hu)

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ME03375B (me) 2011-06-20 2020-01-20 H Lundbeck As Deuterizovani 1-piperazin0-3-fenil indani za tretiranje šizofrenije
AR094054A1 (es) * 2012-12-19 2015-07-08 H Lundbeck As 6-cloro-3-(fenil-d₅)-inden-1-ona y uso de la misma
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