DK1999114T3 - Pyrazoler som 11-beta-hsd-1 - Google Patents

Pyrazoler som 11-beta-hsd-1 Download PDF

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DK1999114T3
DK1999114T3 DK07726783.9T DK07726783T DK1999114T3 DK 1999114 T3 DK1999114 T3 DK 1999114T3 DK 07726783 T DK07726783 T DK 07726783T DK 1999114 T3 DK1999114 T3 DK 1999114T3
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carboxylic acid
adamantan
pyrazole
mmol
hydroxy
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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
Anderson Kevin William Dr
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Hoffmann La Roche
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    • 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
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    • A61K31/415—1,2-Diazoles
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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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Claims (23)

1
1. Forbindelse med formlen (I):
i? hvor: Ri er hydrogen; R2 er adamantan, der er usubstitueret eller substitueret med hydroxy eller halogen; R3 er en trifluormethyl-, pyrazol-, triazol-, piperidin-, pyrrolidin-, hydroxymethylpiperidin-, benzylpiperazin-, hydroxypyrrolidin-, tert-butylpyrrolidin-, hydroxyethylpiperazin-, hydroxypiperidin- eller thiomorpholingruppe; R4 er cyclopropyl, tert-butyl, -C(CH3)2CH2OH, methyl, -CF3 eller en -(CH2)nCF3-gruppe, hvor n er 1 eller 2; R5 er hydrogen eller Ci-C7-alkyl, der er usubstitueret eller substitueret med halogen; og farmaceutisk acceptable salte deraf.
2. Forbindelse ifølge krav 1, hvor R2 er usubstitueret adamantan; og R3 er en trifluormethyl-, pyrazol-, triazol-, piperidin-, pyrrolidin-, hydroxymethylpiperidin-, benzylpiperazin-, hydroxypyrrolidin-, tert-butylpyrrolidin-, hydroxyethylpiperazin-, hydroxypiperidin- eller thiomorpholingruppe.
3. Forbindelse ifølge krav 1, hvor R2 er adamantan substitueret med hydroxy eller halogen; og R3 er en trifluormethyl-, pyrazol-, triazol-, piperidin-, pyrrolidin-, hydroxymethylpiperidin-, benzylpiperazin-, hydroxypyrrolidin-, tert-butylpyrrolidin-, hydroxyethylpiperazin-, hydroxypiperidin- eller thiomorpholingruppe. 2
4. Forbindelse ifølge et hvilket som helst af kravene 1 og 2, hvor R2 er usubstitueret adamantan; og R4 er en cyclopropyl-, tert-butyl-, -C(CH3)2CH2OH-, methyl-, -CF3- eller -CH2)nCF3-gruppe, hvor n er 1 eller 2.
5. Forbindelse ifølge et hvilket som helst af kravene 1 og 3, hvor R2 er adamantan substitueret med hydroxy eller halogen; og R4 er en cyclopropyl-, tert-butyl-, -C(CH3)2CH2OH-, methyl-, -CF3- eller -(CH2)nCF3-gruppe, hvor n er 1 eller 2.
6. Forbindelse ifølge et hvilket som helst af kravene 1, 3 og 5, hvor R2 er trans-hydroxyadamantan.
7. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor R3 er en trifluormethyl-gruppe.
8. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor R3 er en pyrazol-, triazol-, piperidin-, pyrrolidin-, hydroxymethylpiperidin-, benzylpiperazin-, hydroxypyrrolidin-, tert-butylpyrrolidin-, hydroxyethylpiperazin-, hydroxypiperidin- eller thiomorpholingruppe.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 8, hvor R5 er en trifluormethyl-gruppe.
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 9, valgt fra 2'-methyl-2'H-[l,3']bipyrazolyl-4'-carboxylsyre-adamantan-2-ylamid; methyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; tert-butyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; trans-l-tert-butyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-amid cis-l-tert-butyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-amid; trans-2'-methyl-2'H-[l,3']bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid; cyclopropyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; cyclopropyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid; methyl-5-[l,2,4]triazol-l-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; methyl-5-pyrrolidin-l-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; 5-(3-hydroxy-pyrrolidin-l-yl)-l-methyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; 5-(4-hydroxy-piperidin-l-yl)-l-methyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; methyl-5-piperidin-l-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; 5-(4-hydroxymethyl-piperidin-l-yl)-l-methyl-lH-pyrazol-4-carboxylsyre-adamantan-2- 3 ylamid; 5-(4-benzyl-piperazin-l-yl)-l-methyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; 5-(R-3-hydroxy-pyrrolidin-l-yl)-l-methyl-lH-pyrazol-4-carboxylsyre-adamantan-2- ylamid; tert-butyl-5-pyrrolidin-l-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; 5-[4-(2-hydroxy-ethyl)-piperazin-l-yl]-l-methyl-lH-pyrazol-4-carboxylsyre-adamantanylamid; 2'-fert-butyl-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-adamantan-2-ylamid; trans-2'-tert-butyl-2'H-[l,3']bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; tert-butyl-5-(3-hydroxy-pyrrolidin-l-yl)-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; tert-butyl-5-(4-hydroxy-piperidin-l-yl)-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; methyl-5-thiomorpholin-4-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; tert-butyl-5-piperidin-l-yl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; trans-l-tert-butyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-fluor-adamantan-2-yl)- amid; trans-l-cyclopropyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid; trans-2,-cyclopropyl-2,H-[l,3']bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; trans-l-(2-hydroxy-l,l-dimethyl-ethyl)-5-trifluomnethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid; trans-2,-tert-butyl-4-methyl-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan- 2-yl)-amid; trans-2,-tert-butyl-4-chlor-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2- yl)-amid.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 10 valgt fra trans-2,-tert-butyl-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; 2,-methyl-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-adamantan-2-ylamid; l-methyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-adamantan-2-ylamid; trans-l-tert-butyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2- yl)-amid; c/s-l-tert-butyl-5-trifluormethyl-l/-/-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; irans-2,-methyl-2'/7-[l,3,]bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adannantan-2-yl)-annid; l-cyclopropyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; 4 2'-tert-butyl-277-[l,3']bipyrazolyl-4'-carboxylsyre-adamantan-2-ylamid; og
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 11, hvor forbindelsen er valgt fra gruppen bestående af i trans-l-cyclopropyl-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid; trans-2'-cyclopropyl-2'H-[l,3']bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan-2-yl)- amid; trans-l-(2-hydroxy-l,l-dimethyl-ethyl)-5-trifluormethyl-lH-pyrazol-4-carboxylsyre-(5-i hydroxy-adamantan-2-yl)-amid; frans-2,-terf--butyl-4-methyl-2'H-[l,3']bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan- 2-yl)-amid; trans-2'-tert--butyl-4-chlor-2'H-[l,3,]bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan-2- yl)-amid;
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 12 bestående af trans-2'-tert-butyl-2'H-[l,3,]bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid.
14. Farmaceutisk sammensætning, omfattende en terapeutisk effektiv mængde af en forbindelse ifølge et hvilket som helst af kravene 1 til 13 eller farmaceutisk acceptable salte deraf, og en farmaceutisk acceptabel bærer.
15. Farmaceutisk sammensætning ifølge krav 14, hvor forbindelsen er trans-2’-tert-buty\-2,H-[l,3,]bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid.
16. Forbindelser ifølge et hvilket som helst af kravene 1 til 13 til anvendelse som terapeutisk aktivstof.
17. Forbindelse til anvendelse ifølge krav 16, hvor forbindelsen er trans-2'-tert-butyl-2'H-[l,3,]bipyrazolyl-4'-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid.
18. Forbindelser ifølge et hvilket som helst af kravene 1 til 13 til anvendelse ved behandling af diabetes, obesitas eller metabolisk syndrom.
19. Forbindelse til anvendelse ifølge krav 18, hvor forbindelsen er trans-2'-tert-butyl-2'H-[l,3']bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid. 5
20. Forbindelser ifølge et hvilket som helst af kravene 1 til 13 til anvendelse ved fremstilling af medikamenter til behandling af en metabolisk lidelse.
21. Forbindelse til anvendelse ifølge krav 20, hvor forbindelsen er trans-2'-tert-butyl-2'H-[l,3']bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid.
22. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1 til 13 til fremstilling af medikamenter til behandling af diabetes, obesitas eller metabolisk syndrom.
23. Anvendelse ifølge krav 22 til fremstilling af medikamenter til behandling af diabetes, obesitas eller metabolisk syndrom, hvor forbindelsen er trans-2'-tert-butyl-2'FI-[l,3']bipyrazolyl-4,-carboxylsyre-(5-hydroxy-adamantan-2-yl)-amid.
DK07726783.9T 2006-03-22 2007-03-12 Pyrazoler som 11-beta-hsd-1 DK1999114T3 (da)

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AU2006316087B2 (en) 2005-11-21 2011-03-10 Shionogi & Co., Ltd. Heterocyclic compound having inhibitory activity on 11-beta-hydroxysteroid dehydrogenase type I
CN101578257A (zh) * 2006-11-02 2009-11-11 盐野义制药株式会社 羟基金刚烷胺的制造方法
TW200827346A (en) 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
US20100144717A1 (en) * 2006-12-15 2010-06-10 Janelle Comita-Prevoir 2-quinolinone and 2-quinoxalinone-derivatives and their use as antibacterial agents
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