ZA200502873B - Substituted piperazines (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists - Google Patents

Substituted piperazines (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists Download PDF

Info

Publication number
ZA200502873B
ZA200502873B ZA200502873A ZA200502873A ZA200502873B ZA 200502873 B ZA200502873 B ZA 200502873B ZA 200502873 A ZA200502873 A ZA 200502873A ZA 200502873 A ZA200502873 A ZA 200502873A ZA 200502873 B ZA200502873 B ZA 200502873B
Authority
ZA
South Africa
Prior art keywords
alkyl
optionally substituted
compound according
compound
formula
Prior art date
Application number
ZA200502873A
Other languages
English (en)
Inventor
Rachael Ancliff
Yvonne C Fogden
Thomas D Heightman
Simon T Hodgson
David M Wilson
Colin D Eldred
Ashley P Hancock
Heather Hobbs
Matthew J Lindon
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of ZA200502873B publication Critical patent/ZA200502873B/en

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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon 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
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • 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
    • C07D213/44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46Oxygen atoms
    • C07D213/50Ketonic 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
    • C07D213/60Heterocyclic 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/40Nitrogen atoms attached in position 8
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/46Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, 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
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/061,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
    • 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
    • C07D295/04Heterocyclic 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
    • C07D295/08Heterocyclic 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
    • C07D295/084Heterocyclic 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
    • C07D295/088Heterocyclic 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
    • 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
    • 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
    • C07D295/215Radicals derived from nitrogen analogues of carbonic acid
    • 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
    • C07D295/22Heterocyclic 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 hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
    • 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
    • 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
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans 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
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78Ring systems having three or more relevant rings
    • C07D311/80Dibenzopyrans; Hydrogenated dibenzopyrans
    • C07D311/82Xanthenes
    • C07D311/84Xanthenes 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 9
    • 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
    • C07D317/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38Carbon 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
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
ZA200502873A 2002-10-16 2005-04-08 Substituted piperazines (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists ZA200502873B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0224084.4A GB0224084D0 (en) 2002-10-16 2002-10-16 Novel compounds

Publications (1)

Publication Number Publication Date
ZA200502873B true ZA200502873B (en) 2006-07-26

Family

ID=9946029

Family Applications (2)

Application Number Title Priority Date Filing Date
ZA200502873A ZA200502873B (en) 2002-10-16 2005-04-08 Substituted piperazines (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists
ZA200603604A ZA200603604B (en) 2002-10-16 2006-05-05 Substituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists of histamine H3 reverse antagonists

Family Applications After (1)

Application Number Title Priority Date Filing Date
ZA200603604A ZA200603604B (en) 2002-10-16 2006-05-05 Substituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists of histamine H3 reverse antagonists

Country Status (18)

Country Link
US (2) US7615550B2 (OSRAM)
EP (1) EP1567511A1 (OSRAM)
JP (2) JP2006508935A (OSRAM)
KR (1) KR20050049553A (OSRAM)
CN (2) CN100400523C (OSRAM)
AU (1) AU2003280380A1 (OSRAM)
BR (1) BR0315283A (OSRAM)
CA (1) CA2502249A1 (OSRAM)
GB (1) GB0224084D0 (OSRAM)
IS (1) IS7782A (OSRAM)
MA (1) MA27482A1 (OSRAM)
MX (1) MXPA05004078A (OSRAM)
NO (1) NO20051689L (OSRAM)
NZ (2) NZ549963A (OSRAM)
PL (1) PL376477A1 (OSRAM)
RU (1) RU2328494C2 (OSRAM)
WO (1) WO2004035556A1 (OSRAM)
ZA (2) ZA200502873B (OSRAM)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842693B2 (en) 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
US20050256130A1 (en) * 2002-06-12 2005-11-17 Chemocentryx, Inc. Substituted piperazines
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
US20070293216A1 (en) * 2003-02-14 2007-12-20 Roamware Inc. Method and system for providing PLN service to inbound roamers in a VPMN using a standalone approach when no roaming relationship exists between HPMN and VPMN
CA2521000A1 (en) * 2003-04-03 2004-10-21 Kyowa Hakko Kogyo Co., Ltd. Preventive and/or therapeutic agent for neuropathic pain
US20060293298A1 (en) * 2003-04-10 2006-12-28 Bamford Mark J Compounds
GB0316915D0 (en) 2003-07-18 2003-08-20 Glaxo Group Ltd Compounds
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
CN1972914A (zh) * 2004-03-31 2007-05-30 詹森药业有限公司 作为组胺h3受体配合体的非咪唑杂环化合物
US7253168B2 (en) 2004-04-07 2007-08-07 Neurogen Corporation Substituted 1-benzyl-4-substituted piperazine analogues
AU2005240991A1 (en) * 2004-04-15 2005-11-17 Georgetown University Use of (4-alkylpiperazinyl) (phenyl) methanones in the treatment of Alzheimer's disease
US7632831B2 (en) * 2004-05-07 2009-12-15 Memory Pharmaceuticals Corporation 1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
US8158652B2 (en) * 2004-12-01 2012-04-17 Msd K.K. Substituted pyridone derivative
WO2006090142A1 (en) * 2005-02-24 2006-08-31 Glaxo Group Limited l-{4- [ (l-CYCLOBUTYL-4-PIPERIDINYL) OXY] PHENYL] -4-{ [4- (METHYLSULFONYL) PHENYL]CARBONYL PIPERAZINE AS HISTAMINE H3 ANTAGONIST
PT1861360E (pt) * 2005-03-17 2010-01-28 Lilly Co Eli Derivados de pirrolidina como antagonistas de receptores h3 de histamina
EP1717235A3 (en) * 2005-04-29 2007-02-28 Bioprojet Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
CN101228127B (zh) * 2005-05-30 2012-05-16 Msdk.K.公司 哌啶衍生物
ES2574014T3 (es) * 2005-05-30 2016-06-14 Msd K.K. Derivado de piperidina novedoso
GB0514812D0 (en) * 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
GB0514811D0 (en) * 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
GB0521563D0 (en) 2005-10-21 2005-11-30 Glaxo Group Ltd Novel compounds
CA2627234A1 (en) 2005-10-27 2007-05-03 Ucb Pharma, S.A. Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses
ATE485294T1 (de) * 2005-11-18 2010-11-15 Hoffmann La Roche Azaindol-2-carboxamid-derivate
EP1968967B1 (en) * 2005-11-30 2011-04-27 F. Hoffmann-La Roche AG 1,1-dioxo-thiomorpholinyl indolyl methanone derivatives for use as h3 modulators
AU2006319234B2 (en) * 2005-11-30 2012-01-19 F. Hoffmann-La Roche Ag 1,5-substituted indol-2-yl amide derivatives
JP2009519293A (ja) * 2005-12-16 2009-05-14 エフ.ホフマン−ラ ロシュ アーゲー H3レセプター調節剤としてのピロロ[2,3−b]ピリジン誘導体
PE20071068A1 (es) * 2005-12-20 2007-12-13 Glaxo Group Ltd Acido 3-(4-{[4-(4-{[3-(3,3-dimetil-1-piperidinil)propil]oxi}fenil)-1-piperidinil]carbonil}-1-naftalenil)propanoico o propenoico, sales de los mismos, como antagonistas de los receptores h1 y h3
KR20090007604A (ko) * 2006-04-20 2009-01-19 글락소 그룹 리미티드 히스타민 h1 및 h3 길항제로서의 2―치환된 4―벤질프탈라지논 유도체
AR060536A1 (es) 2006-04-20 2008-06-25 Glaxo Group Ltd Agonista del receptor de glucocorticoides y composiciones farmaceuticas
GB0609897D0 (en) * 2006-05-18 2006-06-28 Glaxo Group Ltd Compounds
EA015555B1 (ru) 2006-05-30 2011-08-30 Янссен Фармацевтика Н.В. Замещенные пиридиламидные соединения в качестве модуляторов гистаминового h-рецептора
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
BRPI0712823A2 (pt) 2006-06-23 2012-07-24 Abbott Lab derivados de ciclopropil amina como moduladores de receptor de histamina h3
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
EP2038269A1 (en) * 2006-06-29 2009-03-25 Janssen Pharmaceutica N.V. Substituted benzamide modulators of the histamine h3 receptor
KR101007469B1 (ko) 2006-12-22 2011-01-12 성균관대학교산학협력단 사스 코로나 바이러스의 rna 유사매듭구조에 결합하여 리보솜 틀 이동을 억제하는 호모피페라진계 화합물
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
CL2008002622A1 (es) 2007-09-06 2009-11-27 Glaxo Group Ltd 1-(1-metiletil)-4-{[4-(tetrahidro-2h-piran-4-iloxi)fenil]carbonil}piperazina y su sal hidrocloruro; formas cristalinas de la sal; proceso de preparacion; composicion farmaceutica; y uso para el tratamiento o profilaxis de deterioro cognitivo, fatiga o trastorno del sueno.
CA2697551C (en) 2007-09-20 2013-03-12 Irm Llc Piperidine derivatives as modulators of gpr119 activity
US8883776B2 (en) 2007-11-20 2014-11-11 Janssen Pharmaceutica N.V. Cycloalkyloxy- and heterocycloalkyloxypyridine compounds as modulators of the histamine H3 receptor
CA2720950A1 (en) * 2008-04-07 2009-10-15 Irm Llc Compounds and compositions as modulators of gpr119 activity
US20110160249A1 (en) 2008-05-23 2011-06-30 Schaab Kevin Murray 5-lipoxygenase-activating protein inhibitor
JP5502858B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド Pi3キナーゼの阻害剤として有用な4−カルボキサミドインダゾール誘導体
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
ES2542551T3 (es) 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
JP2012520257A (ja) 2009-03-10 2012-09-06 グラクソ グループ リミテッド Ikk2阻害剤としてのインドール誘導体
JP2012520845A (ja) 2009-03-17 2012-09-10 グラクソ グループ リミテッド Itk阻害剤として使用されるピリミジン誘導体
JP2012520685A (ja) 2009-03-19 2012-09-10 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたGATA結合タンパク質3(GATA3)遺伝子発現のRNA干渉媒介性阻害
JP2012520686A (ja) 2009-03-19 2012-09-10 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたシグナル伝達性転写因子6(STAT6)遺伝子発現のRNA干渉媒介性阻害
CA2755773A1 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of btb and cnc homology 1, basic leucine zipper transcription factor 1 (bach 1) gene expression using short interfering nucleic acid (sina)
WO2010107952A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP2012521763A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたシグナル伝達性転写因子1(STAT1)遺伝子発現のRNA干渉媒介性阻害
JP2012521764A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いた胸腺間質性リンパ球新生因子(TSLP)遺伝子発現のRNA干渉媒介性阻害
US20120004281A1 (en) 2009-03-27 2012-01-05 Merck Sharp & Dohme Corp RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) Gene Expression Using Short Interfering Nucleic Acid (siNA)
UY32571A (es) 2009-04-24 2010-11-30 Glaxo Group Ltd Compuestos derivados de pirazol amida
EP2421834A1 (en) 2009-04-24 2012-02-29 Glaxo Group Limited Pyrazole and triazole carboxamides as crac channel inhibitors
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
TWI516487B (zh) 2009-04-30 2016-01-11 葛蘭素集團有限公司 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途
WO2011002984A1 (en) 2009-07-02 2011-01-06 Cephalon, Inc. Substituted phenoxypropylcycloamine derivatives as histamine-3 (h3) receptor ligands
CA2774573A1 (en) * 2009-10-09 2011-04-14 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
US20120245171A1 (en) 2009-12-03 2012-09-27 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of pi3 kinases
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
WO2012025474A1 (en) 2010-08-24 2012-03-01 Glaxo Group Limited Indazole compounds
WO2012025473A1 (en) 2010-08-24 2012-03-01 Glaxo Group Limited Cc.chemokine receptor 4 antagonists
WO2012031383A1 (zh) * 2010-09-06 2012-03-15 中国科学院广州生物医药与健康研究院 酰胺类化合物
PL2614058T3 (pl) 2010-09-08 2015-12-31 Glaxosmithkline Ip Dev Ltd Polimorfy i sole n-[5-[4-(5-{[(2r,6s)-2,6-dimetylo-4-morfolinylo]-metylo}-1,3-oksazol-2-ilo)-1h-indazol-6-ilo]-2-(metyloksy)-3-pirydynylo]metanosulfonamidu
US8853390B2 (en) 2010-09-16 2014-10-07 Abbvie Inc. Processes for preparing 1,2-substituted cyclopropyl derivatives
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
US9149462B2 (en) 2010-10-21 2015-10-06 Glaxo Group Limited Pyrazole compounds acting against allergic, inflammatory and immune disorders
WO2012052458A1 (en) 2010-10-21 2012-04-26 Glaxo Group Limited Pyrazole compounds acting against allergic, immune and inflammatory conditions
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
JP2014507458A (ja) 2011-03-11 2014-03-27 グラクソ グループ リミテッド Sykインヒビターとしてのピリド[3,4−B]ピラジン誘導体
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
WO2012173952A1 (en) 2011-06-13 2012-12-20 Emory University Piperazine derivatives, compositions, and uses related thereto
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
WO2015042078A2 (en) 2013-09-22 2015-03-26 Calitor Sciences, Llc Substituted aminopyrimidine compounds and methods of use
US9233953B2 (en) * 2013-10-16 2016-01-12 Boehringer Ingelheim International Gmbh Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
CA2925064A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
CA2923995A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
WO2015069110A1 (en) * 2013-11-07 2015-05-14 Aapa B.V. Multiple d2 a(nta)gonists/h3 antagonists for treatment of cns-related disorders
JP6517318B2 (ja) 2014-03-28 2019-05-22 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されたヘテロアリール化合物および使用方法
WO2015173701A2 (en) 2014-05-12 2015-11-19 Glaxosmithkline Intellectual Property (No. 2) Limited Pharmaceutical compositions for treating infectious diseases
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
GB201602527D0 (en) 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
US20190161480A1 (en) 2016-08-08 2019-05-30 Glaxosmithkline Intellectual Property Development Limited Chemical Compounds
AU2017311691B2 (en) 2016-08-18 2021-12-02 Vidac Pharma Ltd. Piperazine derivatives, pharmaceutical compositions and methods of use thereof
GB201706102D0 (en) 2017-04-18 2017-05-31 Glaxosmithkline Ip Dev Ltd Chemical compounds
CN109232549B (zh) * 2017-07-11 2022-07-12 江苏恩华药业股份有限公司 一种治疗精神分裂症的化合物及其应用
GB201712081D0 (en) 2017-07-27 2017-09-13 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
AU2019209960B2 (en) 2018-01-20 2023-11-23 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
US11318144B2 (en) 2019-04-12 2022-05-03 LA PharmaTech Inc. Compositions and methods for treating Alzheimer's disease and Parkinson's disease
US10639314B1 (en) 2019-04-30 2020-05-05 LA PharmaTech Inc. Method of treating Alzheimer's disease
US10639315B1 (en) 2019-05-21 2020-05-05 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating Alzheimer's disease
US11690849B2 (en) 2019-04-12 2023-07-04 LA PharmaTech Inc. Method of treating dementia
US10966989B2 (en) 2019-04-12 2021-04-06 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating mental, behavioral, cognitive disorders
US11389458B2 (en) 2019-04-12 2022-07-19 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating parkinson's and huntington's disease
US10898493B2 (en) 2019-04-12 2021-01-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for psychiatric symptoms of patients with Alzheimer's disease
US11744833B2 (en) 2019-04-12 2023-09-05 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of insomnia
US11938139B2 (en) 2019-04-12 2024-03-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for anxiety, depression and other psychiatric disorders
CA3137393A1 (en) * 2019-04-30 2020-11-05 Jianmin Wang A method of treating mental, behavioral, cognitive disorders
CN116194114A (zh) 2020-03-26 2023-05-30 葛兰素史密斯克莱知识产权发展有限公司 用于防止或治疗病毒感染的组织蛋白酶抑制剂
US11351179B1 (en) 2021-08-05 2022-06-07 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of psychiatric disorders

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2401254A1 (de) 1974-01-11 1975-11-27 Boehringer Mannheim Gmbh Neue derivate von n hoch 6-substituierten adeninen
IL61897A (en) 1980-01-19 1984-01-31 Beecham Group Ltd Benzopyrano(2,3-d)-v-triazoles,their production and pharmaceutical compositions containing them
EP0745121B1 (en) 1992-05-14 2007-06-20 Baylor College Of Medicine Mutated steroid hormone receptors, methods for their use and molecular switch for gene therapy
US5364791A (en) 1992-05-14 1994-11-15 Elisabetta Vegeto Progesterone receptor having C. terminal hormone binding domain truncations
DE4410822A1 (de) 1994-03-24 1995-09-28 Schering Ag Neue Piperidin-Derivate
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
US5880128A (en) 1996-05-08 1999-03-09 Schering Corporation Carbonyl piperazinyl and piperidinyl compounds
WO1999041242A1 (fr) 1998-02-13 1999-08-19 Rhone-Poulenc Rorer S.A. Derives de naphtyl disubstitues, leur preparation, les compositions pharmaceutiques qui les contiennent
US6620839B2 (en) * 2000-07-13 2003-09-16 Abbott Laboratories 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
PT1301480E (pt) * 2000-07-13 2007-11-29 Abbott Lab Pirrolidinas 1,3-di-substituídas e 1,3,3-tri-substituídas úteis como ligandos do receptor de histamina-3 e suas aplicações terapêuticas
JP2004504300A (ja) 2000-07-18 2004-02-12 ビーエーエスエフ アクチェンゲゼルシャフト 1−アリール−4−ハロアルキル−2−[1h]ピリドン類
HUP0302893A3 (en) * 2000-08-08 2006-04-28 Ortho Mcneil Pharm Inc Non-imidazole aryloxypiperidines and pharmaceutical compositions containing them and their use
DK1313721T3 (da) * 2000-08-08 2006-06-26 Ortho Mcneil Pharm Inc Ikke-imidazol-aryloxyalkylaminer som H3-receptorligander
JP2002173426A (ja) 2000-12-05 2002-06-21 Ss Pharmaceut Co Ltd 血糖低下剤
JP2004520347A (ja) 2001-01-15 2004-07-08 グラクソ グループ リミテッド Ldl−受容体発現のインデューサーとしてのアリールピペリジンおよびピペラジン誘導体
WO2002076925A2 (en) * 2001-03-23 2002-10-03 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
JP4186518B2 (ja) * 2001-06-15 2008-11-26 アステラス製薬株式会社 フェニルピリジン誘導体
US7459461B2 (en) 2001-10-19 2008-12-02 Ortho-Mcneil Pharmaceutical, Inc. Phosphonic acid compounds as inhibitors of serine proteases
AU2003203148A1 (en) * 2002-02-05 2003-09-02 High Point Pharmaceuticals, Llc Novel aryl- and heteroarylpiperazines
US20060019964A1 (en) 2002-10-16 2006-01-26 Ancliff Ranchael A Compounds
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
GB0609897D0 (en) * 2006-05-18 2006-06-28 Glaxo Group Ltd Compounds

Also Published As

Publication number Publication date
ZA200603604B (en) 2007-04-25
CA2502249A1 (en) 2004-04-29
NO20051689D0 (no) 2005-04-05
NO20051689L (no) 2005-07-07
US7615550B2 (en) 2009-11-10
WO2004035556A1 (en) 2004-04-29
RU2005110061A (ru) 2006-01-20
CN100400523C (zh) 2008-07-09
AU2003280380A1 (en) 2004-05-04
JP2006508935A (ja) 2006-03-16
EP1567511A1 (en) 2005-08-31
IS7782A (is) 2005-03-31
CN101070309A (zh) 2007-11-14
NZ539446A (en) 2006-11-30
JP2007016041A (ja) 2007-01-25
PL376477A1 (en) 2005-12-27
US20100075953A1 (en) 2010-03-25
GB0224084D0 (en) 2002-11-27
MA27482A1 (fr) 2005-08-01
RU2328494C2 (ru) 2008-07-10
KR20050049553A (ko) 2005-05-25
US20060025404A1 (en) 2006-02-02
BR0315283A (pt) 2005-08-30
NZ549963A (en) 2008-03-28
MXPA05004078A (es) 2005-06-08
CN1726201A (zh) 2006-01-25

Similar Documents

Publication Publication Date Title
ZA200502873B (en) Substituted piperazines (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists
KR100742014B1 (ko) Gaba계 조절제
DE69232665T2 (de) Neue 4-arylpiperazine und 4-arylpiperidine
EP0129128B1 (de) 2-Pyrimidinyl-l-piperazin-Derivate, Verfahren zu ihrer Herstellung und diese enthaltende Arzneimittel
FI78296B (fi) Foerfarande foer framstaellning av terapeutiskt aktiva 2-substituerade 4-amino-6,7-dimetoxikinolinderivat.
DE60305484T2 (de) Verbindungen und deren verwendung als 5-ht inhibitoren
KR102221201B1 (ko) 치환된 바이사이클릭 디하이드로피리미디논 및 호중구 엘라스타제 활성의 억제제로서의 이의 용도
JP2016521722A (ja) 置換フェニル−2,3−ベンゾジアゼピン
WO2002076953A1 (en) New spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors
WO2011039344A1 (en) Pyrimidine derivatives as protein tyrosine kinase 2 inhibitors
CA2895426A1 (en) Bet-protein-inhibiting dihydroquinoxalinones
HUP0204458A2 (hu) Alfa-2-antagonista hatású kinolinszármazékok és ezeket tartalmazó gyógyszerkészítmények
EP1917245A1 (de) Heterocyclische verbindungen und ihre verwendung als bindungspartner für 5-ht5-rezeptoren
RU2002133208A (ru) Замещенные 1-аминоалкиллактамы и их применение в качестве антагонистов мускариновых рецепторов
JP2005513065A5 (OSRAM)
CN105358561A (zh) 磷酸二酯酶10a型的新型抑制剂化合物
DK171133B1 (da) 1-Pyridyl- eller -pyrimidyl-4-substitueret alkyl-piperaziner eller -homopiperaziner, fremstilling af disse, samt farmaceutiske præparater indeholdende disse
CA2953004C (en) Aromatic heterocyclic derivatives and pharmaceutical applications thereof
BG62350B2 (bg) N-заместени производни на 3-азабицикло/3.2.0/хептан като невролептици и други
AT398572B (de) Verfahren zur herstellung neuer disubstituierter 1,4-piperazinylderivate
KR20010015787A (ko) 테트라히드로피리도피리미디논의 제3 위치 치환 유도체,그의 제조 방법 및 용도
AU6280199A (en) 2-piperazino alkylamino benzoazole derivatives: dopamine receptor subtype specific ligands
JPH05194441A (ja) 新規な置換3−ピペラジニルアルキル−2,3−ジヒドロ−4h−1,3−ベンゾオキサジン−4−オン、その製造法および治療用途
TW200630371A (en) Halogen substituted benzodiazepine derivatives
RU2007110482A (ru) Композиции и способы для лечения когнитивных расстройств