HRP20090085T3 - MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED BY 5-MEMBER HETEROCYCLIC RINGS - Google Patents

MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED BY 5-MEMBER HETEROCYCLIC RINGS

Info

Publication number
HRP20090085T3
HRP20090085T3 HR20090085T HRP20090085T HRP20090085T3 HR P20090085 T3 HRP20090085 T3 HR P20090085T3 HR 20090085 T HR20090085 T HR 20090085T HR P20090085 T HRP20090085 T HR P20090085T HR P20090085 T3 HRP20090085 T3 HR P20090085T3
Authority
HR
Croatia
Prior art keywords
substituted
4alkyl
aryl1
halo
formula
Prior art date
Application number
HR20090085T
Other languages
Croatian (hr)
Inventor
Meerpoel Lieven
Jacobus J. Backx Leo
Jaroskova Libuse
W.M. Roevens Peter
J.E. Van Der Veken L.
Viellevoye Marcel
T.M. Linders Joannes
Original Assignee
Janssen Pharmaceutica N.V.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Priority claimed from PCT/EP2005/051010 external-priority patent/WO2005085226A1/en
Publication of HRP20090085T3 publication Critical patent/HRP20090085T3/en

Links

Classifications

    • 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
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/435—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D403/10—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 linked by a carbon chain containing aromatic 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Spoj naznačen time što ima formulu (I) njegovi N-oksidi, farmaceutski prihvatljive kisele adicijske soli i stereokemijski izomerni oblici, gdjeisprekidana linija je izborna veza i odsutna je kada X2 predstavlja dušik; radikal Y1-Y2- je radikal formule-N=CH (a-1), -CH=N- (a-2), -CH2-CH2- (a-3), -CH=CH- (a-4), pri čemu, u dvovalentnim radikalima formule (a-1) ili (a-2) atom vodika može izborno biti zamijenjen s C1-6alkil ili fenil; ili u dvovalentnim radikalima formule (a-3) ili (a-4) jedan ili dva atoma vodika mogu izborno biti zamijenjeni s C1-6alkil ili fenil; X1 je ugljik ili dušik; najmanje jedan od X2 ili X3 predstavlja dušik i drugi X2 ili X3 predstavlja CH ili ugljik kada isprekidana linija predstavlja vezu, ili X2 i X3 predstavljaju dušik; R1 je C1-6alkil; aril1;C1-6alkil supstituiran s hidroksi, C3-6cikloalkil, aril1 ili naftalenil; C3-6cikloalkil; C3-6cikloalkenil; C3-6alkenil; C3-6alkenil supstituiran s aril1;C3-C6alkinil; C3-6alkinil supstituiran s aril1;C1-4alkiloksiC1-4alkandiil izborno supstituiran s aril1;ili kada je -Y1-Y2- radikal formule (a-1) tada R1 može biti uzet zajedno s Y2 tako da formira radikal formule -CH=CH-CH=CH- gdje svaki vodik može izborno biti zamijenjen supstituentom koji je nezavisno izabran iz grupe koju čine C1-4alkil, C1-4alkiloksi, polihaloC1-4alkil, halo, cijano, trifluorometil ili aril1;gdje je aril1 jednak fenil; ili fenil supstituiran s od jedan do pet supstituenata od koji jje svaki nezavisno izabran iz grupe koju čine C1-4alkil, C1-4alkiloksi, polihaloC1-4alkil, halo, cijano ili trifluorometil; R2 je vodik, C1-4alkil ili halo; A je C1-6alkandiil; C1-6alkandiil supstituiran s jednom ili dvije grupe izabrane od aril2,heteroaril1 i C3-8cikloalkil; ili uz uvjet da X3 predstavlja CH, navedeni radikal A može također da predstavlja NH izborno supstituiran s aril2, heteroaril1 ili C3-8cikloalkil; gdje je aril2 jednako fenil; ili fenil supstituiran s od jedan do pet supstituenata gdje je svaki od njih nezavisno izabran iz grupe koju čine C1-4alkil, C1-4alkiloksi, halo, cijano ili trifluorometil; heteroaril1 je furanil, tienil, piridinil, pirazinil, pirimidinil ili piridazinil; i navedeni heteroaril1 je izborno supstituiran s jednim ili dva supstituenta gdje je svaki od njih nezavisno izabran iz grupe koju čine C1-4alkil, C1-4alkiloksi, halo, cijano ili trifluorometil; B je N3R4, iliOR9;gdje su svaki R3 i R4 nezavisno izabrani iz grupe koju činevodik, C1-8alkil, C1-8alkil supstituiran s jednim, dva ili tri supstituenta gdje je svaki od njih međusobno nezavisno izabran iz grupe koju čine hidroksi, halo, cijano, C1-4alkiloksi, C1-4alkiloksikarbonil, C3-8cikloalkil, polihaloC1-4alkil, NR5R6, CONR7R8, aril3, policikličan aril ili heteroaril2;C3-8cikloalkil; C3-8cikloalkil; C3-8alkenil; C3-8alkinil; aril3;policikličan aril; heteroaril2; iliR3 i R4 spojeni s atomom dušika koji nosi R3 i R4 mogu formirati azetidinil, pirolidinil, piperidinil, morfolinil, azepanil ili azocanil prsten pri čemu svaki od ovih prstenA compound having the formula (I) its N-oxides, pharmaceutically acceptable acid addition salts and stereochemically isomeric forms, wherein the dotted line is an optional bond and is absent when X2 represents nitrogen; the radical Y1-Y2- is a radical of the formula -N=CH (a-1), -CH=N- (a-2), -CH2-CH2- (a-3), -CH=CH- (a-4), wherein, in the divalent radicals of formula (a-1) or (a-2) the hydrogen atom may optionally be replaced by C1-6alkyl or phenyl; or in the divalent radicals of formula (a-3) or (a-4) one or two hydrogen atoms may optionally be replaced by C1-6alkyl or phenyl; X1 is carbon or nitrogen; at least one of X2 or X3 represents nitrogen and the other X2 or X3 represents CH or carbon when the dotted line represents a bond, or X2 and X3 represent nitrogen; R1 is C1-6alkyl; aryl1;C1-6alkyl substituted with hydroxy, C3-6cycloalkyl, aryl1 or naphthalenyl; C3-6cycloalkyl; C3-6cycloalkenyl; C3-6alkenyl; C3-6alkenyl substituted with aryl1;C3-C6alkynyl; C3-6alkynyl substituted with aryl1;C1-4alkyloxyC1-4alkanediyl optionally substituted with aryl1;or when -Y1-Y2- is a radical of formula (a-1) then R1 may be taken together with Y2 to form a radical of formula -CH=CH-CH=CH- where each hydrogen may be optionally replaced by a substituent independently selected from the group consisting of C1-4alkyl, C1-4alkyloxy, polyhaloC1-4alkyl, halo, cyano, trifluoromethyl or aryl1;wherein aryl1 is phenyl; or phenyl substituted with one to five substituents each independently selected from the group consisting of C1-4alkyl, C1-4alkyloxy, polyhaloC1-4alkyl, halo, cyano or trifluoromethyl; R2 is hydrogen, C1-4alkyl or halo; A is C1-6alkanediyl; C1-6alkanediyl substituted with one or two groups selected from aryl2, heteroaryl1 and C3-8cycloalkyl; or provided that X3 represents CH, said radical A may also represent NH optionally substituted with aryl2, heteroaryl1 or C3-8cycloalkyl; where aryl2 is phenyl; or phenyl substituted with one to five substituents each independently selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo, cyano or trifluoromethyl; heteroaryl1 is furanyl, thienyl, pyridinyl, pyrazinyl, pyrimidinyl or pyridazinyl; and said heteroaryl1 is optionally substituted with one or two substituents each independently selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo, cyano or trifluoromethyl; B is N3R4, or OR9; wherein each R3 and R4 are independently selected from the group consisting of hydrogen, C1-8alkyl, C1-8alkyl substituted with one, two or three substituents each independently selected from the group consisting of hydroxy, halo, cyano, C1-4alkyloxy, C1-4alkyloxycarbonyl, C3-8cycloalkyl, polyhaloC1-4alkyl, NR5R6, CONR7R8, aryl3, polycyclic aryl or heteroaryl2;C3-8cycloalkyl; C3-8cycloalkyl; C3-8alkenyl; C3-8alkynyl; aryl3; polycyclic aryl; heteroaryl2; or R 3 and R 4 joined to the nitrogen atom bearing R 3 and R 4 can form an azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, azepanyl or azocanyl ring, each of these rings

HR20090085T 2004-03-10 2005-03-07 MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED BY 5-MEMBER HETEROCYCLIC RINGS HRP20090085T3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04075771 2004-03-10
US55633604P 2004-03-25 2004-03-25
PCT/EP2005/051010 WO2005085226A1 (en) 2004-03-10 2005-03-07 Mtp inhibiting aryl piperidines or piperazines substituted with 5-membered heterocycles

Publications (1)

Publication Number Publication Date
HRP20090085T3 true HRP20090085T3 (en) 2009-03-31

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Family Applications (1)

Application Number Title Priority Date Filing Date
HR20090085T HRP20090085T3 (en) 2004-03-10 2005-03-07 MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED BY 5-MEMBER HETEROCYCLIC RINGS

Country Status (4)

Country Link
CY (1) CY1108764T1 (en)
DE (1) DE602005011127D1 (en)
HR (1) HRP20090085T3 (en)
NO (1) NO337711B1 (en)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0013383D0 (en) * 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
JO2654B1 (en) * 2000-09-04 2012-06-17 شركة جانسين فارماسوتيكا ان. في Polyarylcarboxamides useful as lipid lowering agents

Also Published As

Publication number Publication date
DE602005011127D1 (en) 2009-01-02
CY1108764T1 (en) 2014-04-09
NO20064601L (en) 2006-10-10
NO337711B1 (en) 2016-06-06

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