WO2003066604A3 - Nouvelles aryl- et heteroarylpiperazines - Google Patents

Nouvelles aryl- et heteroarylpiperazines Download PDF

Info

Publication number
WO2003066604A3
WO2003066604A3 PCT/DK2003/000071 DK0300071W WO03066604A3 WO 2003066604 A3 WO2003066604 A3 WO 2003066604A3 DK 0300071 W DK0300071 W DK 0300071W WO 03066604 A3 WO03066604 A3 WO 03066604A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
heteroarylpiperazines
histamine
receptor
novel aryl
Prior art date
Application number
PCT/DK2003/000071
Other languages
English (en)
Other versions
WO2003066604A2 (fr
Inventor
Rolf Hohlweg
Florencio Zaragoza Doerwald
Henrik Stephensen
Ingrid Pettersson
Bernd Peschke
Original Assignee
Novo Nordisk As
Boehringer Ingelheim Int
Rolf Hohlweg
Florencio Zaragoza Doerwald
Henrik Stephensen
Ingrid Pettersson
Bernd Peschke
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
Priority to AU2003203148A priority Critical patent/AU2003203148A1/en
Priority to JP2003565978A priority patent/JP4607458B2/ja
Application filed by Novo Nordisk As, Boehringer Ingelheim Int, Rolf Hohlweg, Florencio Zaragoza Doerwald, Henrik Stephensen, Ingrid Pettersson, Bernd Peschke filed Critical Novo Nordisk As
Priority to IL16285903A priority patent/IL162859A0/xx
Priority to KR10-2004-7011995A priority patent/KR20040081177A/ko
Priority to BR0307429-3A priority patent/BR0307429A/pt
Priority to MXPA04007612A priority patent/MXPA04007612A/es
Priority to EP03701482A priority patent/EP1474401A2/fr
Priority to UA20040705946A priority patent/UA83187C2/ru
Priority to CA002474214A priority patent/CA2474214A1/fr
Priority to US10/383,310 priority patent/US20030236259A1/en
Publication of WO2003066604A2 publication Critical patent/WO2003066604A2/fr
Publication of WO2003066604A3 publication Critical patent/WO2003066604A3/fr
Priority to ZA2004/05694A priority patent/ZA200405694B/en
Priority to NO20043709A priority patent/NO328714B1/no
Priority to US12/367,952 priority patent/US20090264435A1/en
Priority to AU2010200135A priority patent/AU2010200135A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • C07D295/02—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • C07D295/02—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/033—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • 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
    • C07D295/08—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 singly bound oxygen or sulfur atoms
    • C07D295/084—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • 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
    • C07D295/08—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 singly bound oxygen or sulfur atoms
    • C07D295/096—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • 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
    • C07D295/10—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 doubly bound oxygen or sulphur atoms
    • C07D295/112—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 doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic 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
    • C07D401/02—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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Abstract

L'invention concerne de nouvelles aryl- et hétéroarylpiperazines, l'utilisation de ces composés comme compositions pharmaceutiques, les compositions pharmaceutiques comprenant les composés ainsi qu'une méthode thérapeutique utilisant ces composés et compositions. Les composés font preuve d'une forte affinité de liaison sélective avec le récepteur de l'histamine H3 indiquant une activité antagoniste du récepteur H3, agoniste inverse ou agoniste. Par conséquent, les composés sont utilisés dans le traitement de maladies et de troubles associés au récepteur de l'histamine H3.
PCT/DK2003/000071 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines WO2003066604A2 (fr)

Priority Applications (14)

Application Number Priority Date Filing Date Title
CA002474214A CA2474214A1 (fr) 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines
UA20040705946A UA83187C2 (en) 2002-02-05 2003-02-05 Aryl- and heteroarylpiperazines
IL16285903A IL162859A0 (en) 2002-02-05 2003-02-05 Novel aryl-and heteroarylpiperazines
JP2003565978A JP4607458B2 (ja) 2002-02-05 2003-02-05 新規なアリールおよびへテロアリールピペラジン
BR0307429-3A BR0307429A (pt) 2002-02-05 2003-02-05 Composto, uso do mesmo, composição farmacêutica, e, método para o tratamento de distúrbios ou doenças relacionadas com receptor de histamina h3
MXPA04007612A MXPA04007612A (es) 2002-02-05 2003-02-05 Aril- y heteroarilpiperazinas novedosas.
EP03701482A EP1474401A2 (fr) 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines
AU2003203148A AU2003203148A1 (en) 2002-02-05 2003-02-05 Novel aryl- and heteroarylpiperazines
KR10-2004-7011995A KR20040081177A (ko) 2002-02-05 2003-02-05 신규 아릴- 및 헤테로아릴피페라진
US10/383,310 US20030236259A1 (en) 2002-02-05 2003-03-07 Novel aryl- and heteroarylpiperazines
ZA2004/05694A ZA200405694B (en) 2002-02-05 2004-07-16 Novel aryl-and heteroarylpiperazines
NO20043709A NO328714B1 (no) 2002-02-05 2004-09-03 Aryl- og heteroarylpiperaziner, farmasoytiske preparater som omfatter minst en slik forbindelse, samt anvendelser av slike forbindelser til fremstilling av farmasoytiske preparater
US12/367,952 US20090264435A1 (en) 2002-02-05 2009-02-09 Novel Aryl- and Heteroarylpiperazines
AU2010200135A AU2010200135A1 (en) 2002-02-05 2010-01-13 Novel aryl-and heteroarylpiperazines

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
DKPA200200168 2002-02-05
DKPA200200168 2002-02-05
US35663002P 2002-02-08 2002-02-08
US60/356,630 2002-02-08
US39930402P 2002-07-26 2002-07-26
DKPA200201142 2002-07-26
DKPA200201142 2002-07-26
US60/399,304 2002-07-26

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/383,310 Continuation US20030236259A1 (en) 2002-02-05 2003-03-07 Novel aryl- and heteroarylpiperazines

Publications (2)

Publication Number Publication Date
WO2003066604A2 WO2003066604A2 (fr) 2003-08-14
WO2003066604A3 true WO2003066604A3 (fr) 2003-12-04

Family

ID=27739216

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2003/000071 WO2003066604A2 (fr) 2002-02-05 2003-02-05 Nouvelles aryl- et heteroarylpiperazines

Country Status (12)

Country Link
EP (1) EP1474401A2 (fr)
JP (1) JP4607458B2 (fr)
CN (1) CN1628109A (fr)
AU (2) AU2003203148A1 (fr)
BR (1) BR0307429A (fr)
CA (1) CA2474214A1 (fr)
IL (1) IL162859A0 (fr)
MX (1) MXPA04007612A (fr)
NO (1) NO328714B1 (fr)
PL (1) PL372390A1 (fr)
WO (1) WO2003066604A2 (fr)
ZA (1) ZA200405694B (fr)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7390813B1 (en) 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
AU2003287206A1 (en) 2002-10-23 2004-05-13 Janssen Pharmaceutica, N.V. Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators
KR20060054392A (ko) 2003-07-29 2006-05-22 노보 노르디스크 에이/에스 피리다지닐-피페라진 및 히스타민 ｈ３ 수용체 리간드로서그들의 사용
US7754711B2 (en) * 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
ES2375134T3 (es) 2003-07-30 2012-02-27 Xenon Pharmaceuticals Inc. Derivados de piperazina y su uso como agentes terapéuticos.
EP1651606B1 (fr) * 2003-07-30 2012-10-24 Xenon Pharmaceuticals Inc. Derives pyridyle et leur utilisation en tant qu'agents therapeutiques
EP2316826A1 (fr) 2003-07-30 2011-05-04 Xenon Pharmaceuticals Inc. Dérivés de pyridazine et utilisation de ceux-ci en tant qu'agents thérapeutiques
WO2005035521A1 (fr) * 2003-10-09 2005-04-21 Argenta Discovery Ltd. Quinoleines substituees, utilisees comme modulateurs de la mch
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
JP4596792B2 (ja) * 2004-02-24 2010-12-15 あすか製薬株式会社 ５−ｈｔ１ａ作動作用と５−ｈｔ３拮抗作用を併有する薬剤
WO2005097751A2 (fr) * 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Composes heterocycliques non-imidazole
EP1734963A4 (fr) 2004-04-02 2008-06-18 Merck & Co Inc Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
US20050256309A1 (en) * 2004-05-12 2005-11-17 Altenbach Robert J Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands
MXPA06015267A (es) * 2004-06-22 2007-03-15 Pfizer Prod Inc Antagonistas diazabiciclicos del receptor histamina-3.
CN101083994A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其用作硬脂酰CoA去饱和酶抑制剂的用途
MX2007003327A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa.
AU2005286648A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
JP5080256B2 (ja) 2004-09-20 2012-11-21 ゼノン・ファーマシューティカルズ・インコーポレイテッド 二環式複素環誘導体およびステアロイル−ＣｏＡデサチュラーゼ（ＳＣＤ）のインヒビターとしてのそれらの使用
TW200626592A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
TW200626138A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
TW200626139A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
JP5149009B2 (ja) 2004-09-20 2013-02-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヒトステアロイル−ＣｏＡデサチュラーゼを阻害するためのピリダジン誘導体
JP4958787B2 (ja) * 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヒトステアロイル−ＣｏＡデサチュラーゼを阻害するためのピリジン誘導体
AU2005302225B2 (en) * 2004-11-02 2012-05-24 Centre National De La Recherche Scientifique Pyridazine compounds, compositions and methods
WO2006094034A1 (fr) 2005-03-01 2006-09-08 Wyeth Composes de cinnoline et leur utilisation comme modulateurs du recepteur hepatique x
AU2006343359A1 (en) 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
WO2007003604A2 (fr) 2005-07-04 2007-01-11 Novo Nordisk A/S Medicaments
UA94052C2 (uk) * 2005-07-05 2011-04-11 Ф. Хоффманн-Ля Рош Аг Похідні піридазину
US8686002B2 (en) 2005-08-21 2014-04-01 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as binding partners for 5-HT5 receptors
GB0517184D0 (en) * 2005-08-22 2005-09-28 Glaxo Group Ltd Compounds
JP5185120B2 (ja) 2005-09-16 2013-04-17 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンｈ３受容体のモジュレーターとしてのシクロプロピルアミン
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
ES2388681T3 (es) * 2006-03-28 2012-10-17 High Point Pharmaceuticals, Llc Benzotiazoles con actividad de los receptores de histamina H3
MX2008013843A (es) * 2006-04-28 2008-11-10 Univ Northwestern Formulaciones que contienen compuestos de piridazina para tratar enfermedades neuroinflamatorias.
CA2653062A1 (fr) 2006-05-23 2007-11-29 Transtech Pharma, Inc. Nouveaux medicaments
PL2079732T3 (pl) 2006-05-29 2012-05-31 High Point Pharmaceuticals Llc 3-(1,3-benzodioksol-5-ylo)-6-(4-cyklopropylopiperazyn-1-ylo)-pirydazyna, jej sole i solwaty oraz jej zastosowanie jako antagonisty receptora histaminowego h3
JP2009538859A (ja) * 2006-05-30 2009-11-12 エフ．ホフマン−ラ ロシュ アーゲー ピペリジニルピリミジン誘導体
JP5285603B2 (ja) * 2006-05-30 2013-09-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンｈ３受容体のモジュレーターとしての置換ピリジルアミド化合物
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
CN103382174A (zh) 2006-06-23 2013-11-06 雅培制药有限公司 作为组胺h3受体调节物的环丙胺衍生物
AU2007271187A1 (en) * 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine H4 receptor
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
JO2849B1 (en) 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
US8933101B2 (en) 2007-04-23 2015-01-13 Janssen Pharmaceutica Nv Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
SI2148873T1 (sl) 2007-04-23 2013-01-31 Janssen Pharmaceutica, N.V. Derivati 4-alkoksipiridazina kot antagonisti receptorja dopamina 2 s hitro disociacijo
EP2155689B1 (fr) * 2007-05-31 2015-07-08 Boehringer Ingelheim International GmbH Antagonistes du récepteur ccr2 et leurs utilisations
EP2014656A3 (fr) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC Nouveaux antagonistes d'hétéocycliques h3
WO2009016088A1 (fr) * 2007-08-02 2009-02-05 F. Hoffmann-La Roche Ag Utilisation de dérivés de benzamide pour le traitement de troubles du snc
ES2384414T3 (es) 2007-09-06 2012-07-04 Glaxo Group Limited Derivado de piperazina que tiene afinidad por el receptor H3 de histamina
CA2706328C (fr) 2007-11-20 2016-04-19 Janssen Pharmaceutica N.V. Composes de cycloalkyloxy- et heterocycloalkyloxypyridine comme modulateurs du recepteur h3 de l'histamine
WO2009079593A1 (fr) * 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Dérivés pipérazinyle utiles comme modulateurs du récepteur du neuropeptide y2
WO2009079597A1 (fr) * 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Dérivés pipérazinyle utiles comme modulateurs du récepteur du neuropeptide y2
US8530474B2 (en) 2008-07-03 2013-09-10 Janssen Pharmaceutica Nv Substituted 6-(1-piperazinyl)-pyridazines as 5-HT6 receptor antagonists
CA2730774C (fr) 2008-07-31 2016-09-13 Janssen Pharmaceutica Nv Pyridines substituees par piperazin-1-yl-trifluoromethyle en tant qu'antagonistes des recepteurs d2 de la dopamine a dissociation rapide
PL2379525T3 (pl) 2008-12-19 2016-01-29 Centrexion Therapeutics Corp Cykliczne pirymidyno-4-karboksamidy jako antagoniści receptora CCR2 do leczenia stanów zapalnych, astmy oraz COPD
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
RS53555B1 (en) 2009-12-17 2015-02-27 Boehringer Ingelheim International Gmbh NEW CCR2 RECEPTOR ANTAGONISTS AND THEIR APPLICATIONS
ES2550667T3 (es) 2010-02-18 2015-11-11 Vtv Therapeutics Llc Derivados de fenilheteroarilo y métodos de uso de los mismos
EP2569295B1 (fr) 2010-05-12 2014-11-19 Boehringer Ingelheim International GmbH Nouveaux antagonistes du récepteur ccr2, son procédé de production et utilisation associée en tant que médicaments
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ｃｃｒ２受容体アンタゴニスト、その製造方法及び薬物としてのその使用
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
EP2576542B1 (fr) 2010-05-25 2015-04-22 Boehringer Ingelheim International GmbH Dérivés d'amide cycliques d'acides pyridazine-3-carboxyliques utiles dans le traitement de maladies respiratoires, liées à des douleurs, liées au système immunitaire et cardiovasculaires
WO2011151251A1 (fr) 2010-06-01 2011-12-08 Boehringer Ingelheim International Gmbh Nouveaux antagonistes du ccr2
US8853390B2 (en) 2010-09-16 2014-10-07 Abbvie Inc. Processes for preparing 1,2-substituted cyclopropyl derivatives
JP5786258B2 (ja) 2011-07-15 2015-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規かつ選択的なｃｃｒ２拮抗薬
WO2013151982A1 (fr) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Méthodes et composés utiles pour traiter le prurit, et procédés d'identification desdits composés
DK3177612T3 (da) 2014-08-04 2022-05-16 Nuevolution As Eventuelt fusionerede heterocyclylsubstituerede derivater af pyrimidin, der er anvendelige til behandling af inflammatoriske, metaboliske, onkologiske og autoimmune sygdomme
BR112017028492B1 (pt) 2015-07-02 2023-12-26 Centrexion Therapeutics Corporation Citrato de (4-((3r,4r)-3-metoxitetra-hidro-piran-4- ilamino)piperidin-1-il) (5- metil-6-(((2r, 6s)-6-(p-tolil) tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il) metanona, seu uso e seu método de preparação, e composição farmacêutica
JP2021098692A (ja) 2019-12-20 2021-07-01 ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ 核内受容体に対して活性の化合物
AU2021245397A1 (en) 2020-03-31 2022-10-20 Nuevolution A/S Compounds active towards nuclear receptors
JP2023519605A (ja) 2020-03-31 2023-05-11 ヌエヴォリューション・アクティーゼルスカブ 核内受容体に対して活性な化合物

Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB753166A (en) * 1953-05-22 1956-07-18 Miles Lab Improvements in or relating to substituted piperazines
US2993899A (en) * 1958-03-31 1961-07-25 Miles Lab Acetylenically unsaturated piperazine derivatives
US3309370A (en) * 1964-07-16 1967-03-14 Miles Lab Bicycloalkyl piperazine derivatives and process
DE2609746A1 (de) * 1975-04-07 1976-10-14 Parcor Piperazinverbindungen sowie arzneimittel, die diese verbindungen enthalten
EP0177392A1 (fr) * 1984-09-14 1986-04-09 Innothera Nouvelles (pyridyl-2)-1 pipérazines, leur procédé de préparation et leur application en thérapeutique
EP0236140A2 (fr) * 1986-03-05 1987-09-09 Otsuka Pharmaceutical Co., Ltd. Dérivés de carbostyrile et leurs sels et agents arythmiques les contenant
DE3803860A1 (de) * 1988-02-09 1989-08-17 Basf Ag N,n'-disubstituierte piperazine
EP0385237A2 (fr) * 1989-03-03 1990-09-05 Dainippon Pharmaceutical Co., Ltd. Dérivés de 2-(1-pipérazinyl)-4-phénylcycloalkynopyridines, procédés de préparation et compositions pharmaceutiques les contenant
AU639529B2 (en) * 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
WO1997002245A1 (fr) * 1995-07-06 1997-01-23 Japan Tobacco Inc. Derives de benzamidoxime et leur utilisation a des fins medicinales
WO1998027081A1 (fr) * 1996-12-19 1998-06-25 Smithkline Beecham Plc Derives de sulfamide, procede de preparation de ces derives et utilisation de ces derniers en tant que medicaments
EP1020445A1 (fr) * 1997-10-02 2000-07-19 Eisai Co., Ltd. Derives de pyridine condenses
WO2000066578A1 (fr) * 1999-04-30 2000-11-09 Pfizer Products Inc. Composes pour le traitement de l'obesite
WO2001044201A1 (fr) * 1999-12-16 2001-06-21 Schering Corporation Antagonistes du recepteur y5 au neuropeptide y a imidazoles substituees
WO2001064645A2 (fr) * 2000-03-01 2001-09-07 Orion Corporation Derives de quinoline utilises comme antagonistes alpha2

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4144346A (en) * 1977-01-31 1979-03-13 Janssen Pharmaceutica N.V. Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
US4163849A (en) * 1978-03-17 1979-08-07 Merck & Co., Inc. Piperazinylpyrazines
JPS56118074A (en) * 1980-02-22 1981-09-16 Tanabe Seiyaku Co Ltd Propane derivative and its preparation
US4339579A (en) * 1980-12-29 1982-07-13 American Home Products Corporation 2,6-Bis-(pyrrolopyrazinyl)pyrazines
US5001125A (en) * 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
JP2576862B2 (ja) * 1986-03-05 1997-01-29 大塚製薬 株式会社 カルボスチリル誘導体
GB9012316D0 (en) * 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
JPH0971564A (ja) * 1995-07-06 1997-03-18 Japan Tobacco Inc ベンズアミドオキシム誘導体及びその医薬用途
JP3989102B2 (ja) * 1997-10-02 2007-10-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合ピリジン誘導体
GB9926303D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
GB9926302D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
AU2002247149B2 (en) * 2001-01-31 2007-10-25 H. Lundbeck A/S Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
ATE356127T1 (de) * 2002-06-06 2007-03-15 Novo Nordisk As Substituierte hexahydropyrrolo(1,2-a)pyrazine, octahydropyrido(1,2-a)pyrazine und decahydropyrazino(1,2-a)azepine

Patent Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB753166A (en) * 1953-05-22 1956-07-18 Miles Lab Improvements in or relating to substituted piperazines
US2993899A (en) * 1958-03-31 1961-07-25 Miles Lab Acetylenically unsaturated piperazine derivatives
US3309370A (en) * 1964-07-16 1967-03-14 Miles Lab Bicycloalkyl piperazine derivatives and process
DE2609746A1 (de) * 1975-04-07 1976-10-14 Parcor Piperazinverbindungen sowie arzneimittel, die diese verbindungen enthalten
EP0177392A1 (fr) * 1984-09-14 1986-04-09 Innothera Nouvelles (pyridyl-2)-1 pipérazines, leur procédé de préparation et leur application en thérapeutique
EP0236140A2 (fr) * 1986-03-05 1987-09-09 Otsuka Pharmaceutical Co., Ltd. Dérivés de carbostyrile et leurs sels et agents arythmiques les contenant
AU639529B2 (en) * 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
DE3803860A1 (de) * 1988-02-09 1989-08-17 Basf Ag N,n'-disubstituierte piperazine
EP0385237A2 (fr) * 1989-03-03 1990-09-05 Dainippon Pharmaceutical Co., Ltd. Dérivés de 2-(1-pipérazinyl)-4-phénylcycloalkynopyridines, procédés de préparation et compositions pharmaceutiques les contenant
WO1997002245A1 (fr) * 1995-07-06 1997-01-23 Japan Tobacco Inc. Derives de benzamidoxime et leur utilisation a des fins medicinales
WO1998027081A1 (fr) * 1996-12-19 1998-06-25 Smithkline Beecham Plc Derives de sulfamide, procede de preparation de ces derives et utilisation de ces derniers en tant que medicaments
EP1020445A1 (fr) * 1997-10-02 2000-07-19 Eisai Co., Ltd. Derives de pyridine condenses
WO2000066578A1 (fr) * 1999-04-30 2000-11-09 Pfizer Products Inc. Composes pour le traitement de l'obesite
WO2001044201A1 (fr) * 1999-12-16 2001-06-21 Schering Corporation Antagonistes du recepteur y5 au neuropeptide y a imidazoles substituees
WO2001064645A2 (fr) * 2000-03-01 2001-09-07 Orion Corporation Derives de quinoline utilises comme antagonistes alpha2

Non-Patent Citations (26)

* Cited by examiner, † Cited by third party
Title
BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE, vol. 1, 1969, pages 319 - 324, ISSN: 0037-8968 *
CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 38, no. 5, 1990, pages 1286 - 1291, ISSN: 0009-2363 *
CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 39, no. 2, 1991, pages 367 - 371, ISSN: 0009-2363 *
COMPTES RENDUS DES SEANCES DE L'ACADEMIE DES SCIENCES, SERIE C: SCIENCES CHIMIQUE, vol. 267, no. 12, 1968, pages 724 - 727, ISSN: 0567-6541 *
DATABASE ZCAPLUS [online] BALLABEN E ET AL: "Reactivity of cyclopentanone enamines towards non-symmetric electrophilic diazenes.", XP002902956, retrieved from STN Database accession no. 1994:191665 *
DATABASE ZCAPLUS [online] HORI MANABU ET AL: "Novel 4-substituted 2-piperazinylquinazolines as potent anticonvulsive and antihypoxic agents.", XP002902958, retrieved from STN Database accession no. 1990:552359 *
DATABASE ZCAPLUS [online] HORI MANABU ET AL: "Potential nootropic agents, 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives.", XP002902957, retrieved from STN Database accession no. 1991:400232 *
DATABASE ZCAPLUS [online] MAZARGUIL H ET AL: "Enamines of N-methyl- and N- phenylpiperazine. I. Synthesis and physicochemical study.", XP002902959, retrieved from STN Database accession no. 1969:106472 *
DATABASE ZCAPLUS [online] MAZARGUIL H ET AL: "Enamines of N-methyl and N- phenylpiperazines. Synthesis of unsymmetrical N,N'-disubstituted and N-monosubstituted piperazines.", XP002902960, retrieved from STN Database accession no. 1969:20015 *
DATABASE ZCAPLUS [online] WU QIUYE ET AL: "Synthesis and platelet aggregation activity of 6-[4-substituted- piperazinyl)phenyl]-4,5-dihydro-3(2H)-pyridazinones.", XP002902955, retrieved from STN Database accession no. 1999:729780 *
DATABASE ZCAPLUS [online] XP002902943, retrieved from STN Database accession no. 2001:661394 *
DATABASE ZCAPLUS [online] XP002902944, retrieved from STN Database accession no. 2001:453029 *
DATABASE ZCAPLUS [online] XP002902945, retrieved from STN Database accession no. 2000:790496 *
DATABASE ZCAPLUS [online] XP002902946, retrieved from STN Database accession no. 1997:140310 *
DATABASE ZCAPLUS [online] XP002902947, retrieved from STN Database accession no. 1994:298482 *
DATABASE ZCAPLUS [online] XP002902948, retrieved from STN Database accession no. 1991:143438 *
DATABASE ZCAPLUS [online] XP002902949, retrieved from STN Database accession no. 1986:491334 *
DATABASE ZCAPLUS [online] XP002902950, retrieved from STN Database accession no. 1977:43741 *
DATABASE ZCAPLUS [online] XP002902951, retrieved from STN Database accession no. 1990:35892 *
DATABASE ZCAPLUS [online] XP002902952, retrieved from STN Database accession no. 1968:2915 *
DATABASE ZCAPLUS [online] XP002902953, retrieved from STN Database accession no. 1957:39516 *
DATABASE ZCAPLUS [online] XP002902954, retrieved from STN Database accession no. 1999:244638 *
DATABASE ZCAPLUS [online] XP002902961, retrieved from STN Database accession no. 1998:424243 *
DATABASE ZCAPLUS [online] XP002902965, retrieved from STN Database accession no. 1988:406428 *
GAZZETTA CHIMICA ITALIANA, vol. 123, no. 7, 1993, pages 387 - 391, ISSN: 0016-5603 *
ZHONGGUO YAOWU HUAXUE ZAZHI, vol. 9, no. 3, 1999, pages 172 - 175, 185, ISSN: 1005-0108 *

Also Published As

Publication number Publication date
MXPA04007612A (es) 2004-11-10
IL162859A0 (en) 2005-11-20
CA2474214A1 (fr) 2003-08-14
AU2003203148A1 (en) 2003-09-02
WO2003066604A2 (fr) 2003-08-14
AU2010200135A1 (en) 2010-02-04
NO20043709L (no) 2004-09-03
JP2005533747A (ja) 2005-11-10
EP1474401A2 (fr) 2004-11-10
NO328714B1 (no) 2010-05-03
ZA200405694B (en) 2005-09-28
BR0307429A (pt) 2004-12-28
JP4607458B2 (ja) 2011-01-05
PL372390A1 (en) 2005-07-25
CN1628109A (zh) 2005-06-15

Similar Documents

Publication Publication Date Title
WO2003066604A3 (fr) Nouvelles aryl- et heteroarylpiperazines
WO2003024928A3 (fr) Nouveau derives d'aminoazetidine, d'aminopyrrolidine et d'aminopiperidine
IL173161A0 (en) Pyridazinyl-piperazines and their use as histamine h3 receptor ligands
WO2006047516A3 (fr) Composes et compositions servant d'inhibiteurs d'activite de recepteur cannabinoide de type 1
WO2002072536A8 (fr) Derives d'uree ayant une activite antagoniste du recepteur vanilloide (vr1)
WO2005046603A3 (fr) Composes pyridiniques
WO2005000820A3 (fr) Derives de 4-cyanopyrazole-3-carboxamide, leur preparation et leur application comme antagonistes des recepteurs aux cannabinoides cb1
IL162834A0 (en) Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes
WO2004022537A3 (fr) Composes heterocycliques
WO2004108133A3 (fr) Modulateurs du recepteur vr1
WO2005086656A3 (fr) Derives d'heteroarylaminopyrazole utilises pour traiter le diabete
WO2004078116A3 (fr) Inhibiteurs de la p 38 et leurs procedes d'utilisation
AP2004003184A0 (en) Benzofused heteroaryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same and methods for their use.
DE60234616D1 (de) Substituierte piperidinen mit selektiver bindungsfähigkeit zu histamin h3-rezeptoren
WO2003084539A3 (fr) Nouvelles compositions pharmaceutiques a base d'anticholinergiques et d'inhibiteurs de la kinase p38
WO2003024401A3 (fr) Piperazinones de modulation de l'activite des recepteurs des chimiokines
WO2005030188A3 (fr) Derives de phenyl-piperazine en tant que modulateurs des recepteurs muscariniques
WO2007022947A3 (fr) Composes 5-cycle-heteroaromates et leur utilisation en tant que partenaires de liaison des recepteurs 5-ht5
AU2003270199A1 (en) Urea compounds active as vanilloid receptor antagonists for the treatment of pain
AU2003229535A1 (en) Substituted hexahydropyrrolo(1,2-a)pyrazines, octahydropyrido(1,2-a)pyrazines and decahydropyrazino(1,2-a)azepines
WO2005112923A3 (fr) Dérivés de 5-anilino-4-hétéroarylpyrazole utiles pour le traitement du diabete
WO2004110385A3 (fr) Modulateurs du recepteur des glucocorticoides et procede associe
WO2003072572A8 (fr) Agonistes du recepteur $g(b)3-adrenergique
WO2004087880A8 (fr) Composes et leur utilisation dans le traitement du diabete et troubles connexes
UA83187C2 (en) Aryl- and heteroarylpiperazines

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 10383310

Country of ref document: US

AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 162859

Country of ref document: IL

WWE Wipo information: entry into national phase

Ref document number: 2003203148

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2003701482

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2004/05694

Country of ref document: ZA

Ref document number: 200405694

Country of ref document: ZA

WWE Wipo information: entry into national phase

Ref document number: 2474214

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 1692/CHENP/2004

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 1020047011995

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 2003565978

Country of ref document: JP

Ref document number: 372390

Country of ref document: PL

WWE Wipo information: entry into national phase

Ref document number: PA/a/2004/007612

Country of ref document: MX

Ref document number: 20038033607

Country of ref document: CN

WWE Wipo information: entry into national phase

Ref document number: 2004126680

Country of ref document: RU

WWP Wipo information: published in national office

Ref document number: 2003701482

Country of ref document: EP