ATE449090T1 - Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren - Google Patents

Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren

Info

Publication number
ATE449090T1
ATE449090T1 AT02742851T AT02742851T ATE449090T1 AT E449090 T1 ATE449090 T1 AT E449090T1 AT 02742851 T AT02742851 T AT 02742851T AT 02742851 T AT02742851 T AT 02742851T AT E449090 T1 ATE449090 T1 AT E449090T1
Authority
AT
Austria
Prior art keywords
histamine
diazepande
derivatives
receptor modulators
substituted piperazine
Prior art date
Application number
AT02742851T
Other languages
English (en)
Inventor
Florencio Doerwald
Knud Andersen
Jan Sorensen
Original Assignee
High Point Pharmaceuticals Llc
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 High Point Pharmaceuticals Llc filed Critical High Point Pharmaceuticals Llc
Application granted granted Critical
Publication of ATE449090T1 publication Critical patent/ATE449090T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56Amides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • C07D277/70Sulfur atoms
    • C07D277/74Sulfur atoms substituted by carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/20Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205Radicals derived from carbonic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D319/00Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/101,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/141,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/161,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18Ethylenedioxybenzenes, not substituted on the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrane Compounds (AREA)
AT02742851T 2001-07-02 2002-06-27 Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren ATE449090T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA200101046 2001-07-02
DKPA200101878 2001-12-14
PCT/DK2002/000438 WO2003004480A2 (en) 2001-07-02 2002-06-27 Substituted piperazine and diazepanes as histamine h3 receptor agonists

Publications (1)

Publication Number Publication Date
ATE449090T1 true ATE449090T1 (de) 2009-12-15

Family

ID=26069046

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02742851T ATE449090T1 (de) 2001-07-02 2002-06-27 Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren

Country Status (6)

Country Link
EP (1) EP1421071B1 (de)
JP (1) JP2005502623A (de)
AT (1) ATE449090T1 (de)
AU (1) AU2002344951A1 (de)
DE (1) DE60234453D1 (de)
WO (1) WO2003004480A2 (de)

Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040132715A1 (en) * 2002-09-06 2004-07-08 Dunford Paul J. Method to treat allergic rhinitis
PT1558595E (pt) 2002-10-23 2010-01-15 Janssen Pharmaceutica Nv Piperazinil e diazepanil benzamidas e benzotioamidas
US7226930B2 (en) * 2003-04-18 2007-06-05 Memory Pharmaceutical Corporation Phosphodiesterase 4 inhibitors
ATE402165T1 (de) 2003-04-23 2008-08-15 Glaxo Group Ltd Piperazin derivate und ihre verwendung für die behandlung von neurologischen und psychiatrischen krankheiten.
AU2004269892B2 (en) * 2003-09-09 2010-03-11 F. Hoffmann-La Roche Ag 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
WO2005097751A2 (en) 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Non-imidazole heterocyclic compounds as histamine h3-receptor ligands
US7423176B2 (en) * 2004-04-13 2008-09-09 Cephalon, Inc. Bicyclic aromatic sulfinyl derivatives
SI1828154T1 (sl) 2004-12-09 2009-08-31 Hoffmann La Roche Derivati fenil-piperazin metanona
MX2007006896A (es) 2004-12-15 2007-06-26 Hoffmann La Roche Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador 1 de glicina (glyt-1) para el tratamiento de la enfermedad de alzheimer.
DE602005010744D1 (de) * 2004-12-16 2008-12-11 Hoffmann La Roche Piperazinylpyridinderivate als mittel gegen adipositas
US7485637B2 (en) 2005-01-04 2009-02-03 Hoffmann-La Roche Inc. Benzoyl-tetrahydropiperidine derivatives
DE602005022113D1 (de) 2005-01-07 2010-08-12 Hoffmann La Roche Phenyl)methanon-derivate als glycin-transporter 1 (glyt-1) hemmer zur behandlung von neurologischen und neuropsychiatrischen erkrankungen
ATE435650T1 (de) 2005-01-18 2009-07-15 Hoffmann La Roche 2,5-disubstituierte phenylmethanonderivative als glycintransporter-1-inhibitoren (glyt-1) zur behandlung von neurologischen und neuropsychiatrischen störungen
KR100915472B1 (ko) 2005-01-26 2009-09-03 에프. 호프만-라 로슈 아게 페닐 메탄온 유도체 및 그의 글라이신 트랜스포터 1억제제로서의 용도
ES2334578T3 (es) 2005-02-07 2010-03-12 F. Hoffmann-La Roche Ag Fenil-metanonas sustituidas por heterociclo como inhibidores del transportador 1 de la glicina.
CN101142180B (zh) * 2005-03-17 2011-05-04 伊莱利利公司 作为组胺h3受体拮抗剂的吡咯烷衍生物
MX2007013986A (es) * 2005-05-13 2008-02-22 Lexicon Pharmaceuticals Inc Compuestos multiciclicos y metodos para su uso.
EP1896453B1 (de) * 2005-06-20 2009-12-02 Schering Corporation Kohlenstoffgebundene substituierte piperidine und derivate daraus als histamin-h3-antagonisten
CA2606004A1 (en) 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
ME01181B (me) 2005-09-16 2013-03-20 Janssen Pharmaceutica Nv Ciklopropil amini kao modulatori histaminskog h3 receptora
RU2008132966A (ru) * 2006-01-13 2010-02-20 Ф.Хоффманн-Ля Рош Аг (Ch) Производные циклогексилпиперазинилметанона и их применение в качестве модуляторов гистамин н3 рецептора
TW200734313A (en) * 2006-01-17 2007-09-16 Astrazeneca Ab Piperazines and piperidines as mGluR5 potentiators
WO2007143422A2 (en) * 2006-05-30 2007-12-13 Janssen Pharmaceutica N.V. Substituted pyridyl amide compounds as modulators of the histamine h3 receptor
CN101511807A (zh) * 2006-06-29 2009-08-19 詹森药业有限公司 组胺h3受体的取代的苯甲酰胺调节剂
US7977358B2 (en) 2007-07-26 2011-07-12 Hoffmann-La Roche Inc. Pyrazol derivatives
ES2442926T3 (es) 2007-08-22 2014-02-14 Astrazeneca Ab Derivados de ciclopropilamida `978
US8288389B2 (en) 2007-09-06 2012-10-16 Glaxo Group Limited Piperazine derivative having affinity for the histamine H3 receptor
WO2009067405A1 (en) * 2007-11-20 2009-05-28 Janssen Pharmaceutica N.V. Substituted pyrazinyl amide compounds as modulators of the histamine h3 receptor
KR101546712B1 (ko) 2007-11-20 2015-08-24 얀센 파마슈티카 엔.브이. 히스타민 h3 수용체의 조절제로서 사이클로알킬옥시- 및 헤테로사이클로알킬옥시피리딘 화합물
RU2010126842A (ru) 2007-12-05 2012-01-10 Астразенека Аб (Se) Производные пиперазина и их применение в качестве модуляторов рецептора лептина
WO2009126782A1 (en) * 2008-04-11 2009-10-15 High Point Pharmaceuticals, Llc Histamine h3 receptor ligands
US8691804B2 (en) 2008-05-08 2014-04-08 Evotec Ag Azetidines and cyclobutanes as histamine H3 receptor antagonists
WO2009143153A1 (en) * 2008-05-23 2009-11-26 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine h3 receptor
AU2009254547A1 (en) * 2008-06-04 2009-12-10 Astrazeneca Ab (Publ) New compounds V
US20120172375A1 (en) * 2008-11-07 2012-07-05 Bruce Trapp Compounds and methods of promoting oligodendrocyte precursor differentiation
JP5514831B2 (ja) 2008-11-17 2014-06-04 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病の治療のための置換二環式アミン
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
US20120220567A1 (en) 2009-07-23 2012-08-30 Shipps Jr Gerald W Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
NZ602110A (en) 2010-02-18 2014-09-26 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
WO2011137024A1 (en) 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
EP2568812B1 (de) 2010-05-11 2016-10-26 Merck Sharp & Dohme Corp. Neuartige prolylcarboxypeptidase-hemmer
EP2579873A4 (de) 2010-06-11 2013-11-27 Merck Sharp & Dohme Neuartige prolylcarboxypeptidase-hemmer
SG188212A1 (en) 2010-09-02 2013-04-30 Suven Life Sciences Ltd Heterocyclyl compounds as histamine h3 receptor ligands
US20150087628A1 (en) 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3280708B1 (de) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituierte chinazolin verbindungen und verfahren zu deren verwendung
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3364977A4 (de) 2015-10-19 2019-09-04 Araxes Pharma LLC Verfahren zum screening von inhibitoren von ras
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Rasの阻害剤としての複素環式化合物およびその使用方法
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2101081B1 (de) 1970-08-19 1974-01-11 Rhone Poulenc Sa
DE2304155A1 (de) * 1973-01-29 1974-08-01 Ichthyol Ges Cordes Hermanni & N-acylierte substituierte piperazinbzw. homopiperazinderivate, sowie verfahren zu ihrer herstellung
US4420477A (en) * 1979-11-30 1983-12-13 Fujisawa Pharmaceutical Co., Ltd. Cephem compounds
JPS56120669A (en) * 1980-02-27 1981-09-22 Res Inst For Prod Dev Allophanoylpiperazine compound and analgesic agent containing the same as active constituent
FR2514355A1 (fr) * 1981-10-14 1983-04-15 Fabre Sa Pierre Derives de biphenyl alcoyl carboxylates, leur procede de preparation et leur utilisation comme medicaments
US4457931A (en) * 1982-09-27 1984-07-03 Selvi & C. S.P.A. Piperazine derivatives with anticholinergic and/or antihistaminic activity
JPS6289676A (ja) * 1985-06-05 1987-04-24 Kuraray Co Ltd 3,4−ジヒドロベンゾピラン誘導体類及びその医薬用途
JPS63107968A (ja) * 1986-06-30 1988-05-12 Toyo Jozo Co Ltd 2−置換アルコキシ−3−置換−ピラジン類化合物
JPS6314774A (ja) * 1986-07-07 1988-01-21 Mitsubishi Chem Ind Ltd ピリダジノン誘導体又はその塩類
JPH0720929B2 (ja) * 1988-08-15 1995-03-08 三井東圧化学株式会社 ジヒドロカフェイン酸アミド化合物およびそれを有効成分として含有する治療剤
US5010080A (en) * 1988-12-02 1991-04-23 G. D. Searle & Co. Use of heterocyclic amides to inhibit tumor metastasis
EP0385043A1 (de) * 1989-02-28 1990-09-05 Fabrica Espanola De Productos Quimicos Y Farmaceuticos, S.A. (Faes) 4-Substituierte Piperazinderivate
JPH03275657A (ja) * 1989-07-05 1991-12-06 Kanegafuchi Chem Ind Co Ltd ケイ皮酸アミド誘導体
WO1993000342A1 (en) * 1991-06-21 1993-01-07 Boehringer Mannheim Italia S.P.A. 2-amino-4-aryl-thiazoles with antiasthmatic and anti-inflammatory activities on the respiratory tract
EP0524055A1 (de) * 1991-07-19 1993-01-20 Synthelabo Imidazo(2,1-b)benzothiazolderivate, Verfahren zu ihrer Herstellung und ihre therapeutische Verwendung
FR2722788B1 (fr) * 1994-07-20 1996-10-04 Pf Medicament Nouvelles piperazides derivees d'aryl piperazine, leurs procedes de preparation, leur utilisation a titre de medicament et les compositions pharmaceutiques les comprenant
CZ288002B6 (cs) * 1995-01-11 2001-03-14 Samjin Pharmaceutical Co., Ltd. Piperazinové deriváty a farmaceutický prostředek s protinádorovou aktivitou je obsahující
JP3081773B2 (ja) * 1995-03-31 2000-08-28 株式会社資生堂 N−アシルピペラジン誘導体及び抗菌剤、抗潰瘍剤
TR199800827T2 (xx) 1995-11-09 1999-02-22 Synthelabo 5-HT4, H3 resept�r ligandlar� olarak 5-fenil-3-(piperidin-4-il)-1,3,4-oksadiyazol-2(3H)-on t�revleri.
US6399618B1 (en) * 1997-07-09 2002-06-04 Cardiome Pharma Corp Compositions and methods for modulating sexual activity
GB9803536D0 (en) 1998-02-19 1998-04-15 Black James Foundation Histamine H,receptor ligands
JP2000086603A (ja) * 1998-07-15 2000-03-28 Yoshitomi Pharmaceut Ind Ltd 桂皮酸アミド誘導体および3―フェニルプロピオン酸アミド誘導体
EP0978512A1 (de) 1998-07-29 2000-02-09 Societe Civile Bioprojet Aryloxy- (oder Arylthio)alkylamine ohne Imidazolring als Histamin-H3-Antagonisten und deren therapeutische Anwendung
GB9905010D0 (en) * 1999-03-04 1999-04-28 Merck Sharp & Dohme Therapeutic agents
US6211182B1 (en) * 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
AU3957600A (en) 1999-04-26 2000-11-10 Boehringer Ingelheim International Gmbh Piperidyl-imidazole derivatives, their preparations and therapeutic uses
WO2001066534A2 (en) 2000-03-09 2001-09-13 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
GB0030304D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds
JP2002201178A (ja) * 2000-07-17 2002-07-16 Takeda Chem Ind Ltd スルホン誘導体、その製造法及び用途
US6316475B1 (en) 2000-11-17 2001-11-13 Abbott Laboratories Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
GB0031088D0 (en) * 2000-12-20 2001-01-31 Smithkline Beecham Plc Medicaments

Also Published As

Publication number Publication date
EP1421071A2 (de) 2004-05-26
DE60234453D1 (de) 2009-12-31
WO2003004480A2 (en) 2003-01-16
EP1421071B1 (de) 2009-11-18
JP2005502623A (ja) 2005-01-27
WO2003004480A3 (en) 2004-03-25
AU2002344951A1 (en) 2003-01-21

Similar Documents

Publication Publication Date Title
ATE449090T1 (de) Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
DE60329330D1 (de) Piperidin- und pyrrolidin-derivate alsantagonisten des histamin-h3-rezeptors
MEP53708A (en) 3-z-[1-(4-(n-((4-methyl-piperazin-1-yl)-methylcarbonyl) -n-methyl -amino) -anilino)-1- phenyl-methylene] -6-methoxycarbonyl -2-indolinone -monoethanesulphonate and the use thereof as a pharmaceutical composition
MY137053A (en) Pyrimidine derivatives and their use as cb2 modulators
BR0316350A (pt) Diaminotriazóis úteis como inibidores de proteìna cinases
BR0314393A (pt) Piperazinas heterocìclicas substituìdas para o tratamento de esquizofrenia
ATE450508T1 (de) Substituierte piperidinen mit selektiver bindungsfähigkeit zu histamin h3-rezeptoren
DE602004014117D1 (de) Thiazole zur verwendung als inhibitoren von protein-kinasen
ATE411985T1 (de) Substituierte piperazine als modulatoren des melanocortinrezeptors
ATE345329T1 (de) Pyridinderivate als modulatoren des cb2-rezeptors
EA200700118A1 (ru) Амидосоединения и их применение в качестве лекарственных средств
CY1111086T1 (el) Παραγωγα 2-αμινο-κιναζολινης χρησιμα ως αναστολεις της βητα-σεκρετασης (bace)
BRPI0514738A (pt) derivados de amida de 3-fenil-diidropirimido[4,5-d]pirimidinonas, sua fabricação e aplicação como agentes farmacêuticos
SE0302232D0 (sv) Novel Compounds
CY1111070T1 (el) Παραγωγα 2-αμινο-κουιναζολινης χρησιμα ως αναστολεις της β-σεκρετασης (bace)
DE60237528D1 (de) Neue aminoazetidin-, aminopyrrolidin- und aminopiperidinderivative
ATE355265T1 (de) Biphenylcarboxamidderivate und ihre verwendung als p38 kinase inhibitoren
BRPI0418255A (pt) derivados de piperazina e piperidina n-substituìdos
BRPI0417858A (pt) composto, composição farmacêutica, e, uso de uma composição farmacêutica
DE60101372D1 (de) Pyrimidinverbindungen und ihre verwendung als modulatoren der chemokin-rezeptor-aktivität
ATE524181T1 (de) Verwendung von 1,4-bis (3-aminoalkyl) piperazin- derivaten bei der behandlung von neurodegenerativen erkrankungen
AU2003260436A1 (en) Pyrimidine compounds
SE0300456D0 (sv) Novel compounds
MXPA05004273A (es) Derivados de fenilalquil y piridilalquil piperazina.
BR9608245A (pt) Derivados de piperazino como antagonistas de neurocinina

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties