HRP20100397T1 - INHIBITORI 11-ß-HIDROKSISTEROID-DEHIDROGENAZE 1 - Google Patents

INHIBITORI 11-ß-HIDROKSISTEROID-DEHIDROGENAZE 1 Download PDF

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HRP20100397T1
HRP20100397T1 HR20100397T HRP20100397T HRP20100397T1 HR P20100397 T1 HRP20100397 T1 HR P20100397T1 HR 20100397 T HR20100397 T HR 20100397T HR P20100397 T HRP20100397 T HR P20100397T HR P20100397 T1 HRP20100397 T1 HR P20100397T1
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alkyl
halogens
optionally substituted
halogen
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Kay Bush Julie
Martin Hansen Marvin
Li Renhua
Edward Mabry Thomas
June Snyder Nancy
Brendan Wallace Owen
Xu Yanping
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Eli Lilly And Company
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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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/50—Nitrogen atoms
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • 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
    • A61P3/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings

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Abstract

Spoj strukturno prikazan formulom: naznačen time štoR0 jegdje isprekidana linija predstavlja mjesto vezanja na položaj R0; gdje Ra je -halogen; Rb je -H ili halogen; R1 je -H, -halogen, -O-CH3 (izborno supstituiran s jednim do tri halogena) ili -CH3 (izborno supstituiran s jednim do tri halogena); R2 je -H, -halogen, -O-CH3 (izborno supstituiran s jednim do tri halogena) ili -CH3 (izborno supstituiran s jednim do tri halogena); R3 je -H ili -halogen; R4 je -OH, -halogen, -CN, -(C1-C4)alkil (izborno supstituiran s jednim do tri halogena), -O-(C1-C6)alkil (izborno supstituiran s jednim do tri halogena), -SCF3, -C(O)O(C1-C4)alkil, -O-CH2-C(O)NH2, -(C3-C8)cikloalkil, -O-fenil-C(O)O-(C1-C4)alkil, -CH2-fenil, -NHSO2-(C1-C4)alkil, -NHSO2-fenil(R21)(R21), -(C1-C4)akil-C(O)N(R10)(R11),gdje isprekidana linija predstavlja mjesto vezanja na položaj R4;R5 je -H, -halogen, -OH, -CN, -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)OH, -C(O) O-(C1-C4)alkil, -C(O)-(C1-C4)alkil, -O-(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena), -SO2-(C1-C4) alkil, -N(R8)(R8), -fenil(R21)(R21), -C(O)-NH-(C3-C6)cikloalkil, iligdje isprekidana linija predstavlja mjesto vezanja na položaj označen s R5;gdje m je 1, 2 ili 3; gdje n je 0, 1 ili 2, te gdje kada n je 0, "(CH2)n" je veza; R6 je -H, -halogen, -CN, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R7 je -H, -halogen, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R8 je svaki put neovisno -H, -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)(C1-C6)akil (izborno supstituiran s 1 do 3 halogena), -C(O)-(C3-C8)cikloalkil, -S(O2)-(C3-C8)cikloalkil ili -S(O2)-(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R9 je -H ili -halogen; R10 i R11 su svaki neovisno -H ili -(C1-C4)alkil, ili R10 i R11, uzeti zajedno s dušikom na kojeg su vezani, tvore piperidinil, piperazinil ili pirolidinil; R20 je svaki put neovisno -H, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R21 je svaki put neovisno -H, -halogen, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena), -CN, -C(O)-N(R22)(R22) (gdje izborno dva R22, zajedno s dušikom na kojeg su vezani, tvore azetidinil, pirolidinil ili piperidinil); R22 je svaki put neovisno -H ili -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena); iR23 je svaki put neovisno -H, -(C1-C4)alkil, ili -C(O)O-(C1-C4)akil, ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 12 patentnih zahtjeva.

Claims (13)

1. Spoj strukturno prikazan formulom: [image] naznačen time što R0 je [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj R0; gdje Ra je -halogen; Rb je -H ili halogen; R1 je -H, -halogen, -O-CH3 (izborno supstituiran s jednim do tri halogena) ili -CH3 (izborno supstituiran s jednim do tri halogena); R2 je -H, -halogen, -O-CH3 (izborno supstituiran s jednim do tri halogena) ili -CH3 (izborno supstituiran s jednim do tri halogena); R3 je -H ili -halogen; R4 je -OH, -halogen, -CN, -(C1-C4)alkil (izborno supstituiran s jednim do tri halogena), -O-(C1-C6)alkil (izborno supstituiran s jednim do tri halogena), -SCF3, -C(O)O(C1-C4)alkil, -O-CH2-C(O)NH2, -(C3-C8)cikloalkil, -O-fenil-C(O)O-(C1-C4)alkil, -CH2-fenil, -NHSO2-(C1-C4)alkil, -NHSO2-fenil(R21)(R21), -(C1-C4)akil-C(O)N(R10)(R11), [image] [image] [image] [image] [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj R4; R5 je -H, -halogen, -OH, -CN, -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)OH, -C(O) O-(C1-C4)alkil, -C(O)-(C1-C4)alkil, -O-(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena), -SO2-(C1-C4) alkil, -N(R8)(R8), -fenil(R21)(R21), -C(O)-NH-(C3-C6)cikloalkil, [image] [image] [image] [image] ili [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj označen s R5; gdje m je 1, 2 ili 3; gdje n je 0, 1 ili 2, te gdje kada n je 0, "(CH2)n" je veza; R6 je -H, -halogen, -CN, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R7 je -H, -halogen, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R8 je svaki put neovisno -H, -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)(C1-C6)akil (izborno supstituiran s 1 do 3 halogena), -C(O)-(C3-C8)cikloalkil, -S(O2)-(C3-C8)cikloalkil ili -S(O2)-(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R9 je -H ili -halogen; R10 i R11 su svaki neovisno -H ili -(C1-C4)alkil, ili R10 i R11, uzeti zajedno s dušikom na kojeg su vezani, tvore piperidinil, piperazinil ili pirolidinil; R20 je svaki put neovisno -H, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R21 je svaki put neovisno -H, -halogen, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena), -CN, -C(O)-N(R22)(R22) (gdje izborno dva R22, zajedno s dušikom na kojeg su vezani, tvore azetidinil, pirolidinil ili piperidinil); R22 je svaki put neovisno -H ili -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena); i R23 je svaki put neovisno -H, -(C1-C4)alkil, ili -C(O)O-(C1-C4)akil, ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što R0 je [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj R0 u formuli I; gdje Ra je -halogen; Rb je -H ili halogen; R1 je -klor, -fluor ili -brom; R2 je -klor, -fluor ili -brom; R3 je -H ili -halogen; R4 je [image] [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj R4 u formuli I; R5 je [image] [image] ili [image] gdje isprekidana linija predstavlja mjesto vezanja na položaj označen s R5; R6 je- H, -halogen, -CN, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R7 je -H, -halogen, ili -(C1-C4)alkil (izborno supstituiran s 1 do 3 halogena); R8 je svaki put neovisno -H, -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena), -C(O)-(C3-C8)cikloalkil, -S(O2)-(C3-C8)cikloalkil ili -S(O2)-(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R9 je -H ili -halogen; R20 je svaki put neovisno -H, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena); R21 je svaki put neovisno -H, -halogen, ili -(C1-C3)alkil (izborno supstituiran s 1 do 3 halogena), -CN, -C(O)-N(R22)(R22) (gdje izborno dva R22, zajedno s dušikom na kojeg su vezani, tvore azetidinil, pirolidinil ili piperidinil); R22 je svaki put neovisno -H ili -(C1-C6)alkil (izborno supstituiran s 1 do 3 halogena); i R23 je svaki put neovisno -H, -(C1-C4)alkil ili -C(O)O-(C1-C4)alkil.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što R0 je [image] ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što R0 je [image] ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što R1 i R2 su klor, ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što R3 je vodik, ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što R4 je [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj u skladu s patentnim zahtjevima 1 ili 2, naznačen time što R4 je [image] ili njegova farmaceutski prihvatljiva sol.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (R)-3-[3,5-diklor-4'-(4-trifluormetilpiperidin-1-karbonil)bifenil-4-ilmetil]-1-(4-hidroksipiperidin-1-il)pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (R)-3-[3,5-diklor-4'-(4,4-difluorpiperidin-1-karbonil)bifenil-4-ilmetil]-1-(4-hidroksipiperidin-1-il)pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 10, i farmaceutski prihvatljivu podlogu.
12. Spoj, ili njegova sol, u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen upotrebi kao medikament.
13. Spoj, ili njegova sol, u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen upotrebi u liječenju dijabetesa tip 2.
HR20100397T 2006-04-24 2010-07-20 INHIBITORI 11-ß-HIDROKSISTEROID-DEHIDROGENAZE 1 HRP20100397T1 (hr)

Applications Claiming Priority (2)

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US74547506P 2006-04-24 2006-04-24
PCT/US2007/067182 WO2007127688A2 (en) 2006-04-24 2007-04-23 Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

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