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HUE026011T2 - Pirazolok mint 11-béta-HSD-1 - Google Patents

Pirazolok mint 11-béta-HSD-1 Download PDF

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Publication number
HUE026011T2
HUE026011T2 HUE07726783A HUE07726783A HUE026011T2 HU E026011 T2 HUE026011 T2 HU E026011T2 HU E07726783 A HUE07726783 A HU E07726783A HU E07726783 A HUE07726783 A HU E07726783A HU E026011 T2 HUE026011 T2 HU E026011T2
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Hungary
Prior art keywords
carboxylic acid
pyrazole
mmol
adamantan
amide
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HUE07726783A
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English (en)
Inventor
Anderson Kevin William Dr
Nader Fotouhi
Paul Gillespie
Robert Alan Goodnow Jr
Kevin Richard Guertin
Nancy-Ellen Haynes
Michael Paul Myers
Sherrie Lynn Pietranico-Cole
Lida Qi
Pamela Loreen Rossman
Nathan Robert Scott
Kshitij Chhabilbhai Thakkar
Jefferson Wright Tilley
Qiang Zhang
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Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of HUE026011T2 publication Critical patent/HUE026011T2/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Agricultural Chemicals And Associated Chemicals (AREA)

Claims (9)

  1. Az EF 1 999 114 lajstromszámú európai szabadalom igénypontjainak magyar fordítása: 1. képietű vegyület; ahol:
    R· jelentése hidrogénatom; Rj jelentése adamantán, amely heíyeftesítefíen vagy hidroxicsoporttaí vagy halogénatommai helyettesített; Rs jelentése trífíbormetib, prazpb, triazob, plpmém-, pírroiidín··, hidroxíroetíbpiperídín-benzlipiperazin-, hidroxlpirrolidio-, ferc~butibpirrolidin~, hidroxietibpiperazsn-, hldroxipípersdin- vagy tiomorfolinosoport; R* jelentése csklopropíb, ferc~butib, -G(GH3}2GNgöH, metib, -CF? vagy -(GH2)nCF3 csoport, aboi n jelentése 1 vagy 2; Rs jelentése hidmgenatQm vagy GrC-raíkibcsopoFi amely helyettesítetlen vagy halogènatomma! helyettesített; és gyogyászatiiag elfogadható sói. 2< Az 1 v Igénypont szerinti vegyiiiet, ahol Rs jelentése helyettesítetlen adamaniánesopúri; és R3 jelentése irifíuorrnetib, pirazob, triazob, pl parid i n~, pírroiidín-, hidroximetíí-piperidin-, benzítpiperazm-, hidroxípírrotidin-, ferc-butibpirroíidin-, hidroxietibpiperazin-, hidroxipiperidin- vagy tíomorfolsncsoport,
  2. 3, Az 1. Igénypont szerinti vegyidet, ahol R, jelentésé adamaníáncsoport, amely hídroxicsoporttal vagy halogénatommal R3 jelentése trifluormetib, pirazob, triazob, plperidin-, pírroiidín-, hidroxímetibpiperídín-, henziipiperazin-, hidraxipirrolidîn-, ferc-butibpirrolidin-, bidroxietsbpiperazin~, Híd roxipipendin- vagy hömöriolincsopört.
  3. 4. Az 1. és 2. igénypontok bármelyike Szerinti vegyület ahol R2 jéléhtésé helyeitessietlen axlamantáncsoport; és R* jelentése eiklöpropik tere-butih -C^H^CBsOH, metil-, -CF2 vagy -(ChbihCFj csoport, ahol n jelentése 1 vagy 2.
  4. 5, Az 1 vés 3. Igénypontok bármelyike szerinti vegyülei ahoi R2 jelentése adamantáncsapori, amely hidroxicsoporttal vagy halogênatommal helyettesített; és R4 Jelentése eikíOipropik terc-butil·, ~C{CHk)2CH20Hs roetií-, -CF? vagy ~{CH2}aCF3 csoport, ahoi n jelentése 1 vagy 2. &amp; Az 1„ 3. és 5, igénypontok bármelyike szerinti vegyület, ahol R2 jelentése transz-hidroxi-adamantán-csoport
  5. 7, Az; 1-8, Igénypontok bármelyike szerinti vegyülei ahol R3 jelentése trífíuorrnetilesoport,
  6. 8, Az 1-8. igénypontok bármelyike szerinti vegyöíet, ahol R;í Jelentése pirazok triazol-, piperidín-, pfrrolidin-, hidroximetil-piperídín-, benzilpiperazin-, hidroxspirrolidin-, tere-iMlbplrFolidin", hidroxieil-piperazin, hidroxipiperidin- vagy tíomorfoíincsoport &amp; Az t-8. igénypontok bármelyike szerinti vegyület, ahol R5 jelentése tnfluormetiicsoporL
  7. 18, Az 1-8. igénypontok bármelyike szerinti vegyület, amelyet a következik közöli választunk: meíii-54nfluörmetíj~1H-pirazoí~4-karbonsav-adamantán-2~tíamid; téró-búi-i-trilüörmetíl-IH^pirazöl-é-karbonsav-adamantáh-l-iiamid;; transZ“1-terc-bütil-5-thflüormetib1 H-pirazoi-4-karbonsav-amid oísz-1-törc-butíi-5-tnfiüormetiM H-pirazol-4-karbonsav-amíd; transz~2,~metil~2B-[1,3!]bipirazcdil-4,-karbonsav-{5-hkiroxi~adamántén~2-ii}-amid; dklopropíl-5-tnfluormetil-1H-pirazol-4“karbonsav-adamantán-2dlamid; cík!opropil~5-infiuormetií-1H~pírazoí-4~karbönsav-{5~hídrQxi-adamantán-2~íí}~amíd; metil-ö-CI );2,4]triazol-1 -0-1 H~psrazöl~4-karbonsav~adamantán-2bkamid; ma!î^0^lrrolidsû“14l»1 H-pir3zol-44íarbonsav~adamantánk24!amid; 5-{3-'Ν€ΐΓθχΙ-ρίΓΓθΒζϋη~1-ϋ)-1-πΊ6ίίΙ··1Η··ρΐΓ8ζο1-4-Κ3Γ5οηδ&amp;ν~β<^3?ϊ]3Πΐέη-2-ίΐ3?ΤΐίίΙ; 5-(4~Ηΐ4Γθχΐ'-ρίρβΓ5Ρίη~1-Η}~1-ηιβ!ΐί*ΊΗ"ρίΓ3ζοΙ~4^3ΓΡοη8βν~8€ΐ8Π'!3,π^η-2-ΐΐ9ίπ!€ΐ; iparid Ir>~ 1 1 H-pIré^áf l-^kar^ö^saa I ä m id s 5-'(4-hidroximetiS'-pfpendin“1--il)--1~metil-1H-pirazo!"4~karbonsav-adamaotan-2~yarnid; 544-foenzííi3iperazin~14í}-1:-meíi;i~1H~pírazül~4-karbonsav~adamantán-24lam!d; 5KR“3-bidroxí~pirroildin-14i)~1-meti!-1 H~pirazP!~4-karbödsav-adasTiaPtän-2-ilasißid; tarc~butsl“5-pirroHdin-1-il~1H-pirazol~4-karbonsav-adamantán~2''!!amid; 5-[4-C2^idröxi-eíji]pplperazín"14|-1~meti!-1H-pfrazof-4-karbonsa¥-adaman^aíiarnid;: 2Merc-butíl4bH41,3’]hipirazöliM ~karbonsav~adamantán4^i!amid: lransz~2,4erc-bydÍ^,H-[1,3,pipírazolMí“karbonsav (5-Nidroxbaciaaiaíiíán'.24l)-amíd: IMa-bytib5~f3-NÍdroxHpÍFmÍítíin-14IHH»pirazDb4“kafbonsav>'adaraantáa'>2''iIafnld; lβrc-butil·5''(4“hídroxi'pipeΓidlπ-1''iΓ|~îH"pïfazol·4-kaΓbΌΠ$av-âdamantáπ~2dlâmid; metib54tomorfolin--4--ib1 H-pbazo!-4~karbonsav~adamant:án~2"ílaniíd; terc~butíb5~pipendin~1*iM H~pirazcf“4^arbonsav~adamantán-24l3mfd; transZ“1'-terC“bytfl-54ríf]uormetíl'1H-pirazol-4~karbonsav~{5~fluor-adamantán-2-H)-amid; irábál-l -plklpprppil«b4ríffuGFráaik1 H-píraz©l-4-'karborisay {b-byraxbadamantáo^d^ arrifd; tFaaaz-2,^klapraptó,H--i1 Jlbipírazöi^-karboasav^S-bid íraaaz-1-#á^ídroxb1 fi ^ime8kaÍ!)~54rÍÍüormMií-1 H-piraioi^ adamantán-2~ií}~amid ; !fâbsz#4efo^ J’JbipímzoiiM-karbQasav-íi-bídrQíd-adamantin^ iparaid; fransz-2'4arc~but5l-4-kiór~2>H~[1l3>]bipírazolíl-4t~karbGnsaV"{5“hidroxí~adamanlán-24l> árpld; > 1.1. âz 1~m igénypontok bármelyike szerinti vegyüiet amelyet a következők közül választunk: transz~2,-terc~butil-2'H-l'í ^’Ibipirazolií^’-karbonsav^S-hldroxí-adamantán-S-ib-amid; 2-metiik2’:H~|1 .Slbipirazoíii-d’-kaFbonsav-adamantán^-íiamki; 1 -ηιβΙΗ-54πΑϋθΓΠΐβίϋ-1 H-pirazoí-4-karbonsav-adamantán-2dlamid ; 1H ~pt razoi ^-:|<^rföc>n#a a ritá n~2~ll>~ amid; cisz-î4&amp;rc~buÎû~5Aùf\ttQrrne$IAH~pïrazol-4~k&amp;TbQmav~{5^iàÎôX{~adamar\iàn~2~û}~ amid; ta/ís2~2,^eÍif-2*/^p>3,|bplrazolíl»4í-karboasa^5-hidroxí-adama«táa-Í-|í^ámid; 1"dkiopropil-'5-trífiuorm8l;il~1H-pirazoi-4~karbonsav-(5”hidroxi-adar^anián*2“il)-amíd; â;· rTte/r^lbU'tílk*^ . 3’] b ιés
    11, Az 1-11. igénypontok bármelyike szerinti vegyület, ahol az említett vegyüíetet a következők áltat alkotott csoportból választjuk; áansz-1^cikíopropib64riÍüormetih1H^pirazöb4^karbonsav-(5~hidTOXÍ~a:C!imant|r!-2”íl}~ amid;;: áaosz-i’-eiklopropl-S’H-ll J^hipirazö;iíl-4’~karhdPsay-fS~hjdm^^ IrmsM i'2-hidroxi-l, 1 -dimetl l-et il }-5-trifl u o r met! I -1 H-píraz^l-é-karbonsav^S-hidroxi-adamanián-2~il)~amid; áaosz-k’-ferc-butii-l-metil^'H-'II.SIbipirazoHI-é’-karbonsav-tö-hidroxi-adamartón-S- ilVaroki; íran&amp;z^’rtér^butil-^klé^'H-H J'!b!pirazaiM'”karbonsav^§-hldroxi-adamantan-24l^ amid' IS. Az 1-12. igénypontok bármelyike szerinti vegyület amely tran$z~T-t&amp;rc~buíM~TH~ |1 J(jbipirazolil^,-kafbonsav"(5--bidroxl^adamantán-2--ií}-amid.
    14. Gyógyászati készítmény» amely az 1-13. igénypontok bármelyike szerinti vegyület vagy gypgyaszatilag elfogadható sói terápiásán hatásos mennyiségét tartalmazza gyógyászatilag elfogadható hordozóanyaggal együtt. 15. A 14. igénypont szerinti gyógyászati készítmény, ahol az emíített vegyület transz-2í-íerC“büti!~2'H-f1,3']bípirazoi-4'~karbonsaV“(5-hidroxi-adamantán-2“íl>"amid. IS. Az 1-13. igénypontok bármelyike szerinti vegyületek terápiásán hatásos anyagként való alkalmazásra. 17, A 16. igénypont szerinti alkalmazásra szolgáló vegyüíet, ahol az említet vegyüíet lmr}az-2‘-áaro-hutíl“2!H-[1 (31foprazoiMókarhönsa^5diidrozí^^
    13, Az 1-13. Igénypontok bármelyike szerinti vegyű letek cukorbetegség, elhízás vagy anyagcsere szindróma kezelésében való alkalmazásra. 13. A 13. igénypont szerinti alkalmazásra szánt vegyidet, ahol az említett vegyüíet transZ"2’-fem”butil-2’H-[1,3,]hipirazoíiM'-kaíh0nsav-{5-bfdroxi~adamaníán~2-!!)-arníd.
  8. 20. Az 1-13. igénypontok bármelyike szerinti vegyületek anyagcsere-rendellenesség kezelésére alkalmas gyógyszerek előállításában való alkalmazásra. 21. A 20. Igénypont szerinti alkalmazásra szánt vegyilet, aha! az említett vegyilet íraf?sZ“2!~tefC-butí!“2^[1!3,]bípfrazokí~4,-karbonsav~(5~hídröxi-adamantán~2~i!}“amíd.
  9. 22. Az 1-I S. igénypontok bármelyike szerints vegyület alkalmazásé cukorbetegség, elhízás vagy anyagcsere-szindróma kezelésére alkalmas gyógyszerek előállítására. 23. A 22. igénypont szerinti alkalmazás gyógyszerek előállítására cukorbetegség, elhízás vagy anyagcsere^szindróma kezeléséne, ahol azemlített vegyötet tmmz~2’~ ferobut!Í~2’H~fi J'lbipírazőllH'-karbönsav-lS^hidrí^í-adamantan-Sei^mícl,
HUE07726783A 2006-03-22 2007-03-12 Pirazolok mint 11-béta-HSD-1 HUE026011T2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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