HUP0004596A2 - Szerotonin 1A receptorra hatással lévő arilpiperazinok és a vegyületeket tartalmazó gyógyászati készítmények valamint intermedierjeik - Google Patents

Szerotonin 1A receptorra hatással lévő arilpiperazinok és a vegyületeket tartalmazó gyógyászati készítmények valamint intermedierjeik

Info

Publication number
HUP0004596A2
HUP0004596A2 HU0004596A HUP0004596A HUP0004596A2 HU P0004596 A2 HUP0004596 A2 HU P0004596A2 HU 0004596 A HU0004596 A HU 0004596A HU P0004596 A HUP0004596 A HU P0004596A HU P0004596 A2 HUP0004596 A2 HU P0004596A2
Authority
HU
Hungary
Prior art keywords
group
alkyl
carbon atoms
alkoxy
alkylthio
Prior art date
Application number
HU0004596A
Other languages
English (en)
Inventor
Alexander Glenn Godfrey
Daniel Timothy Kohlman
John Cunningham O'toole
Yao-Chang Xu
Tony Yantao Zhang
Original Assignee
Eli Lilly And Co.
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 Eli Lilly And Co. filed Critical Eli Lilly And Co.
Publication of HUP0004596A2 publication Critical patent/HUP0004596A2/hu
Publication of HUP0004596A3 publication Critical patent/HUP0004596A3/hu
Publication of HU226409B1 publication Critical patent/HU226409B1/hu

Links

Classifications

    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/004—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reaction with organometalhalides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/29—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation of hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/40—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation with ozone; by ozonolysis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/51—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition
    • C07C45/511—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups
    • C07C45/515—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups the singly bound functional group being an acetalised, ketalised hemi-acetalised, or hemi-ketalised hydroxyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/56—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds from heterocyclic compounds
    • C07C45/57—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds from heterocyclic compounds with oxygen as the only heteroatom
    • C07C45/59—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds from heterocyclic compounds with oxygen as the only heteroatom in five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/527—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings
    • C07C49/563—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/527—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings
    • C07C49/577—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/527—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings
    • C07C49/583—Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing —CHO groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/86—Ketones containing a keto group bound to a six-membered aromatic ring containing —CHO groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D295/104—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 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
    • C07D295/10—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
    • C07D295/104—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/108—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Anesthesiology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

A találmány (I) általános képletű arilpiperazin vegyületekrevonatkozik, melyek hatásos gyógyszerhatóanyagok a szerotonin 1Areceptorral összefüggő vagy azáltal befolyásolt állapotok kezelésére.A vegyületek alkalmasak a nikotin- vagy dohányelvonással járó tünetekenyhítésére. Az (I) általános képletben Ar' jelentése egy- vagykétgyűrűs aril- vagy heteroarilcsoport, mely 1-3 hidrogénatommal, 1-6szénatomos alkil-, 1-6 szénatomos alkoxi-, 1-6 szénatomos alkil-tio-,2-6 szénatomos alkenil-, 2-6 szénatomos alkinil-, halogénezett 1-6szénatomos alkil-, 3-8 szénatomos cikloalkil-, 3-8 szénatomoscikloalkenilcsoporttal vagy halogénatommal helyettesített; R1jelentése hidrogénatom, 1-6 szénatomos alkil-, 1-6 szénatomos alkoxi-,1-6 szénatomos alkil-tio-csoport; R2 jelentése fenil-, naftil- vagy 3-12 szénatomos cikloalkilcsoport, melyet 1-2 hidrogénatom, 1-6szénatomos alkil-, 1-6 szénatomos alkoxi-, 1-6 szénatomos alkil-tio-,2-6 szénatomos alkenil-, 2-6 szénatomos alkinil-, halogénezett, 1-6szénatomos alkil-, 3-8 szénatomos cikloalkil-, 3-8 szénatomoscikloalkenilcsoport vagy halogénatom helyettesít; R3 jelentésehidrogénatom, 1-6 szénatomos alkil-, 1-6 szénatomos alkoxi-, 1-6szénatomos alkil-tio-, 2-6 szénatomos alkenil-, 2-6 szénatomosalkinil-, halogénezett, 1-6 szénatomos alkilcsoport, 3-8 szénatomoscikloalkil-, 3-8 szénatomos cikloalkenilcsoport vagy halogénatom; Xjelentése -C(=O)-, -CHOH- vagy -CH2- képletű csoport. Ó
HU0004596A 1997-12-16 1998-12-08 Arylpiperazines having activity at the serotonin 1a receptor and pharmaceutical compositions containing them HU226409B1 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US6979197P 1997-12-16 1997-12-16
US6972297P 1997-12-16 1997-12-16
US8958998P 1998-06-17 1998-06-17
PCT/US1998/026008 WO1999031077A1 (en) 1997-12-16 1998-12-08 Arylpiperazines having activity at the serotonin 1a receptor

Publications (3)

Publication Number Publication Date
HUP0004596A2 true HUP0004596A2 (hu) 2001-11-28
HUP0004596A3 HUP0004596A3 (en) 2001-12-28
HU226409B1 HU226409B1 (en) 2008-11-28

Family

ID=27371593

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0004596A HU226409B1 (en) 1997-12-16 1998-12-08 Arylpiperazines having activity at the serotonin 1a receptor and pharmaceutical compositions containing them

Country Status (33)

Country Link
US (9) US6239135B1 (hu)
EP (2) EP1514559A1 (hu)
JP (2) JP2002508364A (hu)
KR (1) KR100539651B1 (hu)
CN (2) CN1227241C (hu)
AR (1) AR017864A1 (hu)
AT (1) ATE296296T1 (hu)
AU (1) AU747040B2 (hu)
BR (1) BR9814280A (hu)
CA (2) CA2315227C (hu)
CO (1) CO4980859A1 (hu)
DE (1) DE69830297T2 (hu)
DK (1) DK0924205T3 (hu)
EA (1) EA003703B1 (hu)
EG (1) EG23983A (hu)
ES (1) ES2244036T3 (hu)
HK (2) HK1020732A1 (hu)
HR (1) HRP20000406B1 (hu)
HU (1) HU226409B1 (hu)
ID (1) ID26930A (hu)
IL (3) IL136723A0 (hu)
MY (1) MY125868A (hu)
NO (1) NO317098B1 (hu)
NZ (1) NZ505220A (hu)
PE (1) PE20000134A1 (hu)
PL (1) PL193428B1 (hu)
PT (1) PT924205E (hu)
SV (1) SV1998000148A (hu)
TR (1) TR200001727T2 (hu)
TW (1) TW520366B (hu)
UA (1) UA66370C2 (hu)
WO (1) WO1999031077A1 (hu)
ZA (1) ZA9811473B (hu)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA66370C2 (en) * 1997-12-16 2004-05-17 Lilly Co Eli Arylpiperazines having activity to setotonin 1 receptors
DE122009000036I2 (de) 1999-09-03 2010-05-06 Apbi Holdings Llc Verwendung von Dapoxetin, ein selektiver Serotonin Aufnahme Inhibitor mit schnellem Wirkungseintritt, zur Behandlung von sexueller Dysfunktion
EP1286980A2 (en) * 2000-03-24 2003-03-05 Eli Lilly And Company Enantioselective process for preparing arylated lactones and derivatives
US6713479B2 (en) 2001-03-02 2004-03-30 Sepracor Inc. Piperidine-piperazine ligands for neurotransmitter receptors
DE10161644A1 (de) * 2001-12-14 2003-06-26 Gruenenthal Gmbh N,N'-disubstituierte Piperazin-Verbindungen
DE10161809A1 (de) * 2001-12-14 2003-06-26 Gruenenthal Gmbh Arzneimittel enthaltend N,N'-disubstituierte Piperazin-Verbindungen
DE10205721A1 (de) * 2002-02-12 2003-08-21 Biotronik Mess & Therapieg Führungsdraht und implantierbare Elektrodenleitung
US20030189215A1 (en) 2002-04-09 2003-10-09 Jong-Lam Lee Method of fabricating vertical structure leds
US7071197B2 (en) 2002-06-14 2006-07-04 Recordati S.A. N,N-disubstituted diazocycloalkanes
ITMI20021327A1 (it) * 2002-06-14 2003-12-15 Recordati Chem Pharm Nuove ossialchilpiperazine
US20040072839A1 (en) * 2002-06-14 2004-04-15 Amedeo Leonardi 1-Phenylalkylpiperazines
ITMI20021328A1 (it) * 2002-06-14 2003-12-15 Recordati Ind Chimica E Farma Nuove piperazine 1,4 - disostituite
ITMI20021329A1 (it) * 2002-06-14 2003-12-15 Recordati Chem Pharm Nuove ossialchilammine sostituite
WO2004019892A2 (en) * 2002-08-30 2004-03-11 Watson Pharmaceuticals, Inc. Drug delivery system for treating urinary incontinence
PL376789A1 (pl) * 2002-12-12 2006-01-09 Aventis Pharma S.A. Pochodne aminoindazoli i ich zastosowanie jako inhibitorów kinazy
GB0317370D0 (en) * 2003-07-24 2003-08-27 Synaptics Uk Ltd Magnetic calibration array
US20050165025A1 (en) * 2004-01-22 2005-07-28 Recordati Ireland Ltd. Combination therapy with 5HT 1A and 5HT 1B-receptor antagonists
PL2813225T3 (pl) * 2004-09-24 2018-11-30 University Of Maryland, Baltimore Sposób leczenia zatrucia związkami fosforoorganicznymi
US9132135B2 (en) * 2004-09-24 2015-09-15 University Of Maryland, Baltimore Method of treating organophosphorous poisoning
WO2007075964A2 (en) * 2005-12-22 2007-07-05 Schering Corporation Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
US20080081067A1 (en) * 2006-10-03 2008-04-03 Gupta Manishkumar Sustained release pharmaceutical compositions of venlafaxine and process for preparation thereof
WO2010065446A2 (en) * 2008-12-01 2010-06-10 The Procter & Gamble Company Perfume systems
MX2012005273A (es) * 2009-11-06 2012-06-19 Aerpio Therapeutics Inc Metodos para incrementar la estabilizacion de factor-1 alfa inducible por hipoxia.
DK3144394T3 (da) 2010-12-08 2019-05-13 Expression Pathology Inc SRM/MRM-test for trunkeret HER2
CN110713442A (zh) * 2018-07-11 2020-01-21 程先波 一种邻硝基苯甲醛的制备方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB230303A (hu) * 1900-01-01
US1013907A (en) * 1910-08-22 1912-01-09 David M Neuberger Engine.
GB1013907A (en) * 1962-09-13 1965-12-22 Ici Ltd Alkene derivatives
BE637389A (hu) * 1962-09-13
GB8909209D0 (en) 1989-04-22 1989-06-07 Wyeth John & Brother Ltd Piperazine derivatives
US5382583A (en) 1989-04-22 1995-01-17 John Wyeth & Brother, Limited Piperazine derivatives
US5340812A (en) 1989-04-22 1994-08-23 John Wyeth & Brother, Limited Piperazine derivatives
GB9021535D0 (en) 1990-10-03 1990-11-14 Wyeth John & Brother Ltd Piperazine derivatives
GB2248499A (en) 1990-10-05 1992-04-08 Richard Branson Seismic data interpretation digitising scanner
AU645681B2 (en) 1991-05-02 1994-01-20 John Wyeth & Brother Limited Piperazine derivatives
TW224974B (hu) 1991-07-02 1994-06-11 Hoffmann La Roche
CN1036395C (zh) 1992-03-19 1997-11-12 约翰韦恩兄弟有限公司 哌嗪衍生物的制备方法
GB9306103D0 (en) 1993-03-24 1993-05-12 Wyeth John & Brother Ltd Piperazine derivatives
JPH06293803A (ja) 1993-11-26 1994-10-21 Loctite Corp 光硬化性組成物
EP0661266A1 (en) 1993-12-27 1995-07-05 Toa Eiyo Ltd. Substituted cyclic amine compounds as 5HT2 antagonists
US5614523A (en) * 1995-01-17 1997-03-25 Eli Lilly And Company Compounds having effects on serotonin-related systems
GB9514384D0 (en) * 1995-07-13 1995-09-13 American Home Prod Medical treatment
UA66370C2 (en) * 1997-12-16 2004-05-17 Lilly Co Eli Arylpiperazines having activity to setotonin 1 receptors
EP1286980A2 (en) * 2000-03-24 2003-03-05 Eli Lilly And Company Enantioselective process for preparing arylated lactones and derivatives

Also Published As

Publication number Publication date
HUP0004596A3 (en) 2001-12-28
HU226409B1 (en) 2008-11-28
NO20003082L (no) 2000-08-02
UA66370C2 (en) 2004-05-17
CA2315227C (en) 2007-03-13
US20010003749A1 (en) 2001-06-14
US6514976B2 (en) 2003-02-04
PL193428B1 (pl) 2007-02-28
CA2315227A1 (en) 1999-06-24
EP0924205B1 (en) 2005-05-25
JP2008266337A (ja) 2008-11-06
HK1020732A1 (en) 2000-05-19
CN1227241C (zh) 2005-11-16
US20020169170A1 (en) 2002-11-14
ID26930A (id) 2001-02-22
IL174074A0 (en) 2006-08-01
ZA9811473B (en) 2000-06-14
AU747040B2 (en) 2002-05-09
BR9814280A (pt) 2001-10-30
US20040049083A1 (en) 2004-03-11
US6946579B2 (en) 2005-09-20
TR200001727T2 (tr) 2000-10-23
TW520366B (en) 2003-02-11
ES2244036T3 (es) 2005-12-01
PE20000134A1 (es) 2000-03-04
JP2002508364A (ja) 2002-03-19
AU1808399A (en) 1999-07-05
EA200000659A1 (ru) 2001-02-26
CO4980859A1 (es) 2000-11-27
KR100539651B1 (ko) 2005-12-29
NZ505220A (en) 2002-11-26
US7001908B2 (en) 2006-02-21
HRP20000406A2 (en) 2000-12-31
HRP20000406B1 (en) 2006-05-31
US6645967B2 (en) 2003-11-11
IL136723A (en) 2006-07-05
US6660859B2 (en) 2003-12-09
EP1514559A1 (en) 2005-03-16
WO1999031077A1 (en) 1999-06-24
DE69830297T2 (de) 2006-02-02
KR20010033143A (ko) 2001-04-25
US6358958B2 (en) 2002-03-19
PL342170A1 (en) 2001-05-21
US20030027831A1 (en) 2003-02-06
MY125868A (en) 2006-08-30
CN1743302A (zh) 2006-03-08
NO317098B1 (no) 2004-08-09
CN100355714C (zh) 2007-12-19
SV1998000148A (es) 1999-08-18
US20040044009A1 (en) 2004-03-04
EP0924205A1 (en) 1999-06-23
DE69830297D1 (de) 2005-06-30
IL136723A0 (en) 2001-06-14
CN1290258A (zh) 2001-04-04
EA003703B1 (ru) 2003-08-28
AR017864A1 (es) 2001-10-24
US20030008879A1 (en) 2003-01-09
PT924205E (pt) 2005-09-30
CA2506802A1 (en) 1999-06-24
US20060009464A1 (en) 2006-01-12
NO20003082D0 (no) 2000-06-15
US20050282817A1 (en) 2005-12-22
US7309702B2 (en) 2007-12-18
US6239135B1 (en) 2001-05-29
DK0924205T3 (da) 2005-09-26
ATE296296T1 (de) 2005-06-15
HK1034712A1 (en) 2001-11-02
EG23983A (en) 2008-02-27

Similar Documents

Publication Publication Date Title
HUP0004596A2 (hu) Szerotonin 1A receptorra hatással lévő arilpiperazinok és a vegyületeket tartalmazó gyógyászati készítmények valamint intermedierjeik
HUP9900172A2 (hu) Idegrendszeri elváltozások kezelésére alkalmas 10-aciloxi-10,11-dihidrobenz/b,f/azepin-5-karboxamid, előállítása és ezt tartalmazó gyógyszerkészítmény
HUP0204246A2 (hu) Új tiazolo[4,5-d]pirimidin-származékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP9902471A2 (hu) Piperazin- és piperidinvegyületek, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények
HUP0202490A2 (hu) Indazolszármazékok és ezeket tartalmazó protein-kináz gátló hatású gyógyszerkészítmények
HUP0301120A2 (hu) Szubsztituált fenilamino-kinazolin-származékok, alkalmazásuk rendellenes sejtnövekedés kezelésére és azokat tartalmazó gyógyszerkészítmények
HUP0102656A2 (hu) Elhízás és egyéb rendellenességek kezelésében hasznos, neuropeptid Y Y5 receptor ligandumaiként szolgáló N-helyettesített aminotetralinok és ezeket tartalmazó gyógyszerkészítmények
HUP0204245A2 (hu) Új N-aza-biciklo-amid-származékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0300565A2 (hu) PDE 5 inhibitor hatású 8-kinolin-xantin- és 8-izo-kinolin-xantin-származékok, alkalmazásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0001062A2 (hu) NAALADáz gátló hatású foszfinsavszármazékokat tartalmazó gyógyászati készítmények
MA26861A1 (fr) Inhibiteurs non peptidiques de la liaison cellulaire sous la dependance de vla-4 utiles dans le traitement des maladies inflammatoires, auto-immunes et respiratoires
HUP0303164A2 (hu) Kinazolinok mint MMP-13 gátlók, eljárás az előállításukra, intermedierjeik és a vegyületeket tartalmazó gyógyszerkészítmények
EA200600811A1 (ru) НОВЫЕ ПРОИЗВОДНЫЕ ТЕТРАГИДРОСПИРО {ПИПЕРИДИН-2,7'-ПИРРОЛО [3,2-b]ПИРИДИНА} И НОВЫЕ ПРОИЗВОДНЫЕ ИНДОЛА, ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ РАССТРОЙСТВ, СВЯЗАННЫХ С 5-HT-РЕЦЕПТОРОМ
YU59602A (sh) Aril fuzionisana azapoliciklična jedinjenja
CY1109558T1 (el) Παραγωγα βενζο[d]αζεπινης για την θεραπεια νευρολογικων διαταραχων
SE0104334D0 (sv) Therapeutic agents
TW200504047A (en) Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
HUP0401638A2 (hu) Daganatellenes hatású tiofén- és tiazolszulfonamid származékok, valamint ezeket tartalmazó gyógyászati készítmények
HUP0401886A2 (hu) Kemokin receptor aktivitás modulátorokként alkalmazható piperidinszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0002031A2 (hu) Benzotiofénszármazékok alkalmazása központi idegrendszeri betegségek kezelésére szolgáló gyógyszerkészítmények előállítására
EA200601194A1 (ru) Новые производные бензофурана, используемые для профилактики или лечения нарушений, связанных с 5-ht-рецептором
HUP0204458A2 (hu) Alfa-2-antagonista hatású kinolinszármazékok és ezeket tartalmazó gyógyszerkészítmények
HUP0301458A2 (hu) Benzoxazinonszármazékok, eljárás előállításukra és a vegyületek felhasználása
HUP0100024A2 (hu) Alzheimer-kór kezelésére szolgáló hatóanyagként karvedilolszármazékokat tartalmazó gyógyszerkészítmények
TW200508221A (en) New azetidine compounds

Legal Events

Date Code Title Description
MM4A Lapse of definitive patent protection due to non-payment of fees