HUP9902827A2 - Muszkarin antagonista piperidin- és piperazinszármazékok, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Muszkarin antagonista piperidin- és piperazinszármazékok, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP9902827A2
HUP9902827A2 HU9902827A HUP9902827A HUP9902827A2 HU P9902827 A2 HUP9902827 A2 HU P9902827A2 HU 9902827 A HU9902827 A HU 9902827A HU P9902827 A HUP9902827 A HU P9902827A HU P9902827 A2 HUP9902827 A2 HU P9902827A2
Authority
HU
Hungary
Prior art keywords
alkyl
pipe
powder
hydrogen atom
ring
Prior art date
Application number
HU9902827A
Other languages
English (en)
Inventor
Theodros Asberom
Allen Barnett
Joel G. Berger
Craig D. Boyle
Margaret E. Browne
Samuel Chackalamannil
Wei K. Chang
Lian-Yong Chen
John W. Clader
Sundeep Dugar
Michael J. Green
Hubert B. Josien
Joseph A. Kozlowski
Derek B. Lowe
Stuart W. Mccombie
Robert Mcquade
Margaret Sherlock
Jayaram R. Tagat
Wing Tom
Wayne D. Vaccaro
Susan F. Vice
Yuguang Wang
Original Assignee
Schering Corp.
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 Schering Corp. filed Critical Schering Corp.
Publication of HUP9902827A2 publication Critical patent/HUP9902827A2/hu
Publication of HUP9902827A3 publication Critical patent/HUP9902827A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/24—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C07D295/116—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings with the doubly bound oxygen or sulfur atoms directly attached to a carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

A találmány tárgyát (I) általánős képletű N,N'-diszűbsztitűáltpiperazinők és 1,4-diszűbsztitűált piperidinek -, ahől Z és Y egyike nitrőgénatőm, a másik nitrőgénatőm, -CH- vagy -C(alkil)-képletű csőpőrt; X őxigén- vagy kénatőm, szűlfinil-, szűlfőnil- vagy metilén-csőpőrt, -CH(alkil)-, -C(alkil)2- vagy -CH(OH)- képletű vagy -NR20CO- általánősképletű csőpőrt, amelyben R20 hidrőgénatőm, aril- vagy alkilcsőpőrt ésmás csőpőrtők; R (f) vagy (g) általánős képletű vagy (h) képletű csőpőrt és máscsőpőrtők; R3 és R4 hidrőgénatőm vagy az arőmás gyűrűk szőkásősszűbsztitűenseinek valamelyike; R1 hidrőgénatőm, ciklőalkil- vagy alkilcsőpőrt, és R21 hidrőgénatőm(i), vagy a kettő együtt őxőcsőpőrt vagy abból kialakítőtt ciklűsősacetál; R2 (c) vagy (d) általánős képletű csőpőrt, amelyekben R29hidrőgénatőm, alkil-, alkil-karbőnil-, alkőxi-karbőnil-, karbamőil-,alkil-szűlfőnil-, aril-szűlfőnil- vagy szűlfamőilcsőpőrt, R30hidrőgénatőm vagy metilcsőpőrt, R31 és R32 hidrőgénatőm, R33 őrtő-szűbsztitűált (heterő)arilcsőpőrt, és R34 metilcsőpőrt; és R27 és R28 hidrőgénatőm vagy adőtt esetben szűbsztitűált alkilcsőpőrt,vagy együtt alkiléncsőpőrt - és ezeket tartalmazógyógyszerkészítmények és az acetilkőlinészteráz inhibitőrőkkalkőmbinációban való alkalmazásűk képezik. ŕ
HU9902827A 1996-08-08 1997-08-06 Piperidine and piperazine derivatives as muscarinic antagonists, pharmaceutical compositions containing the same and their use HUP9902827A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/700,628 US5889006A (en) 1995-02-23 1996-08-08 Muscarinic antagonists

Publications (2)

Publication Number Publication Date
HUP9902827A2 true HUP9902827A2 (hu) 2000-08-28
HUP9902827A3 HUP9902827A3 (en) 2001-03-28

Family

ID=24814273

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9902827A HUP9902827A3 (en) 1996-08-08 1997-08-06 Piperidine and piperazine derivatives as muscarinic antagonists, pharmaceutical compositions containing the same and their use

Country Status (26)

Country Link
US (2) US5889006A (hu)
EP (1) EP0938483B1 (hu)
JP (1) JP3748894B2 (hu)
KR (1) KR100344332B1 (hu)
CN (1) CN1084743C (hu)
AR (1) AR008285A1 (hu)
AT (1) ATE233260T1 (hu)
AU (1) AU724001B2 (hu)
BR (1) BR9711119A (hu)
CA (1) CA2261725C (hu)
CO (1) CO4900068A1 (hu)
CZ (1) CZ36699A3 (hu)
DE (1) DE69719354T2 (hu)
ES (1) ES2193391T3 (hu)
HK (1) HK1018776A1 (hu)
HU (1) HUP9902827A3 (hu)
ID (1) ID18003A (hu)
IL (1) IL128409A0 (hu)
NO (1) NO990551L (hu)
NZ (1) NZ333801A (hu)
PE (1) PE99598A1 (hu)
PL (1) PL331534A1 (hu)
SK (1) SK15599A3 (hu)
TR (1) TR199900255T2 (hu)
WO (1) WO1998005292A2 (hu)
ZA (1) ZA977011B (hu)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL117149A0 (en) 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
EP0988289A2 (en) * 1997-06-05 2000-03-29 Takeda Pharmaceutical Company Limited Heterocyclic compounds, their production and use
AU762726B2 (en) * 1998-03-31 2003-07-03 Acadia Pharmaceuticals, Inc. Compounds with activity on muscarinic receptors
US6528529B1 (en) 1998-03-31 2003-03-04 Acadia Pharmaceuticals Inc. Compounds with activity on muscarinic receptors
US6066636A (en) * 1998-06-30 2000-05-23 Schering Corporation Muscarinic antagonists
AU3126700A (en) 1998-12-18 2000-07-03 Du Pont Pharmaceuticals Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6331541B1 (en) 1998-12-18 2001-12-18 Soo S. Ko N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
AU780983B2 (en) * 1999-05-04 2005-04-28 Schering Corporation Piperidine derivatives useful as CCR5 antagonists
AU776541B2 (en) * 1999-05-04 2004-09-16 Schering Corporation Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
US6387930B1 (en) 1999-05-04 2002-05-14 Schering Corporation Piperidine derivatives useful as CCR5 antagonists
US6391865B1 (en) 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
US6689765B2 (en) 1999-05-04 2004-02-10 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
ES2244437T3 (es) * 1999-05-04 2005-12-16 Schering Corporation Derivados de piperazina utiles como antagonistas de ccr5.
CN1167682C (zh) * 1999-09-22 2004-09-22 先灵公司 毒蕈碱拮抗剂
US6294554B1 (en) 1999-09-22 2001-09-25 Schering Corporation Muscarinic antagonists
WO2001060369A1 (en) * 2000-02-18 2001-08-23 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
AU2001238424A1 (en) * 2000-02-18 2001-08-27 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
AR033517A1 (es) * 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
CA2413245A1 (en) 2000-06-30 2002-01-10 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity
JP2004529117A (ja) 2001-02-08 2004-09-24 シェーリング　コーポレイション 認知欠陥障害の処置における二重のｈ３／ｍ２アンタゴニストの使用
EP1373251A2 (en) 2001-03-13 2004-01-02 Schering Corporation Non-imidazole compounds as histamine h3 antagonists
US6720325B2 (en) * 2001-03-29 2004-04-13 Schering Corporation CCR5 antagonists useful for treating aids
ES2258642T3 (es) * 2001-07-02 2006-09-01 Astrazeneca Ab Derivados de piperidina utiles como moduladores de la actividad del receptor de quimiocina.
GB0120461D0 (en) * 2001-08-22 2001-10-17 Astrazeneca Ab Novel compounds
US20050020632A1 (en) * 2001-08-31 2005-01-27 Dominique Grimler Optical isomers of an iloperidone metabolite
GB0122503D0 (en) * 2001-09-18 2001-11-07 Astrazeneca Ab Chemical compounds
ES2269774T3 (es) 2001-10-10 2007-04-01 Schering Corporation Compuestos de piperidina como antagonistas muscarinicos.
US6914142B2 (en) * 2001-10-15 2005-07-05 Schering Corporation Synthesis of (4-bromopnenyl)(4-piperidyl)methanone-(Z)-O-ethyloxime and salts
KR100579813B1 (ko) * 2001-10-16 2006-05-12 주식회사 에스티씨나라 피페리딘 유도체, 이의 제조방법 및 이를 포함하는 치매치료용 약학적 조성물
WO2003059965A1 (en) * 2002-01-10 2003-07-24 University Of Washington Hydrogels formed by non-covalent linkages
SE0200844D0 (sv) * 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
SE0200843D0 (sv) 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
AU2003239128A1 (en) * 2002-03-29 2003-10-20 Schering Corporation Stereoselective alkylation of chiral 2-methyl-4-protected piperazines
JP4675103B2 (ja) 2002-06-14 2011-04-20 富山化学工業株式会社 脳機能を改善する医薬組成物および脳機能を改善するための方法
SE0202838D0 (sv) * 2002-09-24 2002-09-24 Astrazeneca Ab Chemical compounds
PL376149A1 (en) * 2002-10-03 2005-12-27 Vertex Pharmaceuticals Incorporated Piperazine and piperidine derivatives for treatment of neurological diseases
TW200504033A (en) * 2002-10-23 2005-02-01 Procter & Gamble Melanocortin receptor ligands
AU2003301552B2 (en) * 2002-10-23 2010-04-22 Janssen Pharmaceutica, N.V. Piperazinyl and diazapanyl benzamides and benzthioamides
PE20040769A1 (es) * 2002-12-18 2004-11-06 Schering Corp Derivados de piperidina utiles como antagonisas ccr5
CA2511726A1 (en) * 2002-12-23 2004-07-08 Ranbaxy Laboratories Limited Xanthine derivatives as muscarinic receptor antagonists
SE0300850D0 (sv) * 2003-03-25 2003-03-25 Astrazeneca Ab Chemical compounds
SE0300957D0 (sv) * 2003-04-01 2003-04-01 Astrazeneca Ab Chemical compounds
SE0301368D0 (sv) * 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
US20050020605A1 (en) * 2003-06-13 2005-01-27 Schering Aktiengesellschaft Quinolyl amide derivatives as CCR-5 antagonists
CA2526725A1 (en) 2003-06-30 2005-01-20 Schering Corporation Mch antagonists for the treatment of obesity
EP1660492B1 (en) * 2003-07-28 2008-08-20 Janssen Pharmaceutica N.V. Benzimidazole, benzthiazole and benzoxazole derivatives and their use as lta4h modulators
EP1687295B1 (en) * 2003-11-03 2011-08-17 Schering Corporation Bipiperidinyl derivatives useful as inhibitors of chemokine receptors
SE0302956D0 (sv) * 2003-11-07 2003-11-07 Astrazeneca Ab Chemical compounds
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
ATE428422T1 (de) * 2004-02-05 2009-05-15 Schering Corp Piperidin-derivate als ccr3-antagonisten
SE0400925D0 (sv) * 2004-04-06 2004-04-06 Astrazeneca Ab Chemical compounds
WO2006005980A1 (en) * 2004-06-16 2006-01-19 Ranbaxy Laboratories Limited Xanthine derivatives useful as muscarinic receptor antagonists
CA2594106A1 (en) * 2005-01-06 2006-07-13 Schering Corporation Preparation of ketone amides
EP1888527A1 (en) * 2005-05-27 2008-02-20 AstraZeneca AB Piperidines for the treatment of chemokine mediated diseases
WO2006138217A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
AR054617A1 (es) 2005-06-14 2007-07-04 Schering Corp Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden
AU2006259573A1 (en) 2005-06-14 2006-12-28 Pharmacopeia, Inc. Heterocyclic aspartyl protease inhibitors, preparation and use thereof
AR054510A1 (es) 2005-06-14 2007-06-27 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas y composiciones farmaceuticas que los comprenden.
WO2006138195A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Macrocyclic heterocyclic aspartyl protease inhibitors
EP2402316A1 (en) * 2005-07-21 2012-01-04 AstraZeneca AB (Publ) Piperidine derivatives
AU2006292598B2 (en) * 2005-09-16 2012-06-21 Janssen Pharmaceutica N.V. Cyclopropyl amines as modulators of the histamine H3 receptor
CA2637411A1 (en) * 2006-01-18 2007-07-26 Siena Biotech S.P.A. Modulators of alpha7 nicotinic acetylcholine receptors and therapeutic uses thereof
FR2899443B1 (fr) * 2006-04-07 2008-07-04 Salomon Sa Semelle de chaussure de ski de fond comportant des moyens perfectionnes d'ancrage d'un moyen de liaison et chaussure munie d'une telle semelle
KR20090087487A (ko) 2006-12-12 2009-08-17 쉐링 코포레이션 아스파르틸 프로테아제 억제제
AU2007332750A1 (en) * 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors containing a tricyclic ring system
TW200906396A (en) * 2007-02-14 2009-02-16 Janssen Pharmaceutica Nv LTA4H modulators and uses thereof
PE20090188A1 (es) * 2007-03-15 2009-03-20 Novartis Ag Compuestos heterociclicos como moduladores de la senda de hedgehog
WO2009032277A1 (en) 2007-09-06 2009-03-12 Schering Corporation Gamma secretase modulators
JP2011503002A (ja) 2007-11-05 2011-01-27 シェーリング コーポレイション γセクレターゼ調節剤
CN101945868A (zh) * 2007-12-11 2011-01-12 先灵公司 γ分泌酶调节剂
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
JP2011530559A (ja) * 2008-08-13 2011-12-22 ビーエーエスエフ ソシエタス・ヨーロピア ピペラジンジオン誘導体を調製する方法
JP5503663B2 (ja) 2008-11-13 2014-05-28 メルク・シャープ・アンド・ドーム・コーポレーション ガンマセクレターゼモジュレータ
CA2747750A1 (en) 2008-12-22 2010-07-01 Theodros Asberom Gamma secretase modulators
US8759337B2 (en) 2008-12-22 2014-06-24 Merck Sharp & Dohme Corp. Gamma secretase modulators
WO2010081851A1 (en) 2009-01-14 2010-07-22 Genoscience Pharma Piperidin-4-ylpiperazine compounds for the treatment of hcv infection
WO2010088392A1 (en) * 2009-01-28 2010-08-05 Rigel Pharmaceuticals, Inc. Carboxamide compounds and methods for using the same
US20120245158A1 (en) 2009-06-16 2012-09-27 Xianhai Huang Gamma secretase modulators
US20120232108A1 (en) 2009-06-16 2012-09-13 Xianhai Huang Gamma secretase modulators
WO2010147969A2 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
EP2536713A1 (en) 2010-02-16 2012-12-26 Pfizer Inc. (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors
WO2011143457A2 (en) 2010-05-12 2011-11-17 Northwestern University Compositions and methods for treating or preventing atrial fibrillation
SG11201402405QA (en) 2011-11-18 2014-09-26 Heptares Therapeutics Ltd Muscarinic m1 receptor agonists
WO2013112323A1 (en) 2012-01-23 2013-08-01 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as mgat - 2 inhibitors
US8993568B2 (en) 2012-01-31 2015-03-31 Eli Lilly And Company Morpholinyl derivatives useful as MOGAT-2 inhibitors
WO2014122474A1 (en) 2013-02-07 2014-08-14 Takeda Pharmaceutical Company Limited Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists
CN103242373B (zh) * 2013-05-24 2015-12-23 济南大学 一种四氧化三铁纳米粒子固载手性配体及其制备方法与应用
GB201417168D0 (en) * 2014-09-29 2014-11-12 Univ Hertfordshire Higher Education Corp Compounds
GB201519352D0 (en) * 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE963424C (de) * 1954-09-24 1957-05-09 Thomae Gmbh Dr K Verfahren zur Herstellung von therapeutisch wirksamen tertiaeren Aminen
US2792398A (en) * 1954-12-03 1957-05-14 Miles Lab Piperazine derivatives
NL93927C (hu) * 1954-12-28
GB807835A (en) * 1955-07-01 1959-01-21 Thomae Gmbh Dr K New tertiary amines and their salts and process for their preparation
US2819273A (en) * 1956-10-02 1958-01-07 Smith & Nephew Heterocyclic nitrogen-containing compounds having a 3:4:5-trimethoxybenzoyl substituent
GB840358A (en) * 1957-10-11 1960-07-06 British Drug Houses Ltd Improvements in or relating to the manufacture of n-mono-substituted piperazines
BE565570A (fr) * 1958-03-11 1960-07-15 H Morren Nouveau derie de la piperazine et sa preparation.
FR1532293A (fr) * 1967-01-11 1968-07-12 Rhone Poulenc Sa Nouveaux dérivés du dibenzocycloheptadiene et leur préparation
US3852455A (en) * 1970-11-27 1974-12-03 Richardson Merrell Inc 4-{8 4({60 hydroxybenzyl)piperidino{9 -4-fluorobutyrophenone derivatives as tranquilizers
DE2063384A1 (de) * 1970-12-23 1972-07-13 Farbwerke Hoechst AG, vormals Meister Lucius & Brüning, 6000 Frankfurt l-(l,2-Diphenyl-2-formylvinyl)-4methylpiperazin und seine physiologisch verträglichen Salze und Verfahren zu seiner Herstellung
JPS4961165A (hu) * 1972-10-23 1974-06-13
JPS604170B2 (ja) * 1974-03-29 1985-02-01 大日本製薬株式会社 １，２− ジフエニルエタノ−ルアミン誘導体の製法
JPS5431825Y2 (hu) * 1975-06-30 1979-10-04
US4251655A (en) * 1978-03-29 1981-02-17 Mcneilab, Inc. Substituted N-iminomethylpiperidines
AU523867B2 (en) * 1978-03-29 1982-08-19 Mcneil Lab Inc. Substituted n-iminomethylpiperidines
FI75816C (fi) * 1981-02-06 1988-08-08 Ucb Sa Foerfarande foer framstaellning av terapeutiskt aktiv 2-/4-(difenylmetyl)-1-piperazinyl/-aettiksyror eller dess amid.
GB8320701D0 (en) * 1983-08-01 1983-09-01 Wellcome Found Chemotherapeutic agent
DK623586A (da) * 1985-12-27 1987-06-28 Eisai Co Ltd Piperidinderivater eller salte deraf og farmaceutiske kompositioner indeholdende forbindelserne
IL85700A0 (en) * 1987-03-24 1988-08-31 Takeda Chemical Industries Ltd 1,4-disubstituted piperazine compounds,their production and use
FI95572C (fi) * 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
IL90279A (en) * 1988-05-24 1995-03-30 American Home Prod History of piperazinyl carboxamide, their preparation and the pharmaceutical preparations containing them
US5010078A (en) * 1988-05-24 1991-04-23 American Home Products Corporation Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity
ES2051927T3 (es) * 1988-06-14 1994-07-01 Searle & Co 1,2-diariletilaminas para el tratamiento de daños neurotoxicos.
GB9000305D0 (en) * 1990-01-06 1990-03-07 Pfizer Ltd Anticholinergic agents
GB9000301D0 (en) * 1990-01-06 1990-03-07 Pfizer Ltd Piperidine & pyrrolidine derivatives
GB9000304D0 (en) * 1990-01-06 1990-03-07 Pfizer Ltd Muscarinic receptor antagonists
JPH04202185A (ja) * 1990-11-30 1992-07-22 Terumo Corp ピペラジン誘導体及びこれを含有する医薬製剤
US5324832A (en) * 1991-07-03 1994-06-28 The United States Of America As Represented By The Department Of Health And Human Services Muscarinic antagonists
EP0612313A1 (en) * 1991-11-14 1994-08-31 Glaxo Group Limited Piperidine acetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
TW239127B (hu) * 1991-12-20 1995-01-21 Hoffmann La Roche
AU3171493A (en) * 1991-12-31 1993-07-28 Fujisawa Pharmaceutical Co., Ltd. Oxadiazole derivatives having acetylcholinesterase-inhibitory and muscarinic agonist activity
DK78692D0 (da) * 1992-06-12 1992-06-12 Lundbeck & Co As H Dimere piperidin- og piperazinderivater
EP0585500A1 (en) * 1992-09-04 1994-03-09 Merrell Dow Pharmaceuticals Inc. Diaryl piperazineacetamides as antimuscarinic agents
KR100299734B1 (ko) * 1993-07-28 2002-01-09 모리타 다카카즈 1,4-(디페닐알킬)피페라진유도체
TW397831B (en) * 1994-07-15 2000-07-11 Meiji Seika Kaisha The anti-platelet-agglutination hexahydrogenated pyridine and its derivatives
WO1996019223A1 (en) * 1994-12-22 1996-06-27 Smithkline Beecham Corporation Fibrinogen receptor antagonists
JPH10511356A (ja) * 1994-12-22 1998-11-04 スミスクライン・ビーチャム・コーポレイション フィブリノゲン受容体拮抗物質
US5700801A (en) * 1994-12-23 1997-12-23 Karl Thomae, Gmbh Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2207618A1 (en) * 1994-12-23 1996-07-04 Helmut Pieper Piperazine derivatives, medicaments comprising these compounds, their use and processes for their preparation
DE4446301A1 (de) * 1994-12-23 1996-06-27 Thomae Gmbh Dr K Piperazinderivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
IL117149A0 (en) * 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
TW429256B (en) * 1995-12-27 2001-04-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(benzimidazolyl- and imidazopyridinyl)-piperidine derivatives

Also Published As

Publication number Publication date
ATE233260T1 (de) 2003-03-15
IL128409A0 (en) 2000-01-31
DE69719354T2 (de) 2003-12-04
EP0938483B1 (en) 2003-02-26
PL331534A1 (en) 1999-07-19
PE99598A1 (es) 1998-12-28
CO4900068A1 (es) 2000-03-27
AU3899997A (en) 1998-02-25
NZ333801A (en) 2000-04-28
AR008285A1 (es) 1999-12-29
ID18003A (id) 1998-02-19
HUP9902827A3 (en) 2001-03-28
NO990551L (no) 1999-04-07
US6043255A (en) 2000-03-28
HK1018776A1 (en) 2000-01-07
AU724001B2 (en) 2000-09-07
JP3748894B2 (ja) 2006-02-22
CA2261725A1 (en) 1998-02-12
WO1998005292A2 (en) 1998-02-12
CZ36699A3 (cs) 1999-06-16
CN1084743C (zh) 2002-05-15
NO990551D0 (no) 1999-02-05
SK15599A3 (en) 2000-03-13
ZA977011B (en) 1998-02-06
KR100344332B1 (ko) 2002-11-29
BR9711119A (pt) 1999-11-23
EP0938483A2 (en) 1999-09-01
DE69719354D1 (de) 2003-04-03
JP2000501117A (ja) 2000-02-02
TR199900255T2 (xx) 1999-07-21
WO1998005292A3 (en) 1998-04-02
KR20000029947A (ko) 2000-05-25
ES2193391T3 (es) 2003-11-01
CN1232462A (zh) 1999-10-20
CA2261725C (en) 2005-10-25
US5889006A (en) 1999-03-30

Similar Documents

Publication Publication Date Title
HUP9902827A2 (hu) Muszkarin antagonista piperidin- és piperazinszármazékok, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0300138A2 (en) Cyclic amine derivatives as ccr5 antagonists, their production and use and pharmaceutical compositions containing them
HUP9904167A2 (hu) 1,4-Diszubsztituált piperazin- és piperidinszármazékok, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
AR012315A1 (es) Derivados de ditiolan y el uso de los mismos en la fabricacion de un medicamento.
HUP0302969A2 (hu) NPY Y5 antagonisták, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
CY1116183T1 (el) Πιπεραζινοδιονες ως ανταγωνιστες υποδοχεα οξυτοκινης
DK490288A (da) Substituerede thiazolidindionderivater
HUP0302508A2 (hu) Piridazinon- és triazinonszármazékok, valamint alkalmazásuk gyógyászati készítmények hatóanyagaiként
HUP0301607A2 (hu) Szelektív neurokinin antagonista hatású nitrogéntartalmú heterociklusos vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
ATE230729T1 (de) Benzamid-derivate und ihre verwendung als vasopressin-antagonisten
ID29452A (id) 4-okso-1,4-dihidro-3-quinolinkarboksamida sebagai agen-agen antivirus
HUP0204474A2 (hu) 1H-imidazopiridin-származékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
CA2423103A1 (en) N-acylsulfonamide apoptosis promoters
ATE282614T1 (de) Phenylharnstoff und phenylthioharnstoffderivate
HUP9904363A2 (hu) Muszkarin antagonista piperidin-éterek és az ezeket tartalmazó gyógyszerkészítmények
KR970704444A (ko) 트리아진 유도체 및 의약(triazine derivative and medicine)
CY1107703T1 (el) Υποκατεστημενες δικετοπιπεραζινες και χρηση αυτων ως ανταγωνιστες οξυτοκινης
TR200001463T2 (tr) P maddesi antagonistleri olarak, piperidinilaminometil-triflorometil-siklik eter bileşikleri
HUP0102071A2 (hu) A növekedési hormon felszabadulását előidéző 4,4- és 3,3diszubsztituált piperidin-származékok és ezeket tartalmazó gyógyászati készítmények
HUP9904622A2 (hu) 1,4-Diszubsztituált piperidinek mint muszkarin antagonisták
EA200101224A1 (ru) Производные пурина, способ их получения и содержащие их фармацевтические композиции
HUP0000729A2 (hu) Új amidszármazékok és ezeket tartalmazó gyógyszerkészítmények
KR950000692A (ko) 유기 물질의 광 안정화제, 열 안정화제 및 산화 안정화제로서 사용되는 피페리딘-트리아진 화합물
MX9400253A (es) Derivados de piperazina, proceso para su preparacion y composiciones farmaceuticas que los contienen.
HUP9904210A2 (hu) Kamptotecin-analógok, alkalmazásuk gyógyszerként és ilyen vegyületeket tartalmazó gyógyászati készítmények