[go: up one dir, main page]

RU2009138602A - Новые производные бензазепина - Google Patents

Новые производные бензазепина Download PDF

Info

Publication number
RU2009138602A
RU2009138602A RU2009138602/04A RU2009138602A RU2009138602A RU 2009138602 A RU2009138602 A RU 2009138602A RU 2009138602/04 A RU2009138602/04 A RU 2009138602/04A RU 2009138602 A RU2009138602 A RU 2009138602A RU 2009138602 A RU2009138602 A RU 2009138602A
Authority
RU
Russia
Prior art keywords
pharmaceutically acceptable
disease
acceptable salt
cyclobutyl
azepin
Prior art date
Application number
RU2009138602/04A
Other languages
English (en)
Other versions
RU2423353C1 (ru
Inventor
Марк Джеймс БАМФОРД (GB)
Марк Джеймс Бамфорд
Дэвид Кеннет ДИН (GB)
Дэвид Кеннет Дин
Санджит Сингх СЕХМИ (GB)
Санджит Сингх СЕХМИ
Дэвид Мэттью УИЛСОН (GB)
Дэвид Мэттью Уилсон
Джейсон ВИЗЕРИНГТОН (GB)
Джейсон Визерингтон
Original Assignee
Глэксо Груп Лимитед (GB)
Глэксо Груп Лимитед
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0229820A external-priority patent/GB0229820D0/en
Priority claimed from GB0312607A external-priority patent/GB0312607D0/en
Application filed by Глэксо Груп Лимитед (GB), Глэксо Груп Лимитед filed Critical Глэксо Груп Лимитед (GB)
Publication of RU2009138602A publication Critical patent/RU2009138602A/ru
Application granted granted Critical
Publication of RU2423353C1 publication Critical patent/RU2423353C1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

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

Abstract

1. Соединение общей формулы (I), которое представляет собой 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид !! или его фармацевтически приемлемая соль. ! 2. Фармацевтически приемлемая соль соединения по п.1, которая представляет собой кислотно-аддитивную соль, образованную 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамидом и кислотой. ! 3. Фармацевтически приемлемая соль соединения по п.2, где кислота представляет собой малеиновую, хлористоводородную, бромистоводородную, фосфорную, уксусную, фумаровую, салициловую, серную, лимонную, молочную, миндальную, винно-каменную и метансульфоновую кислоту. ! 4. Фармацевтическая композиция, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид ! ! или его фармацевтически приемлемую соль, и фармацевтически приемлемый носитель или эксцепиент. ! 5. Соединение по п.1, используемое в терапии. ! 6. Применение 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемой соли в получении лекарственного средства для лечения нейрологического заболевания или психиатрического расстройства. ! 7. Применение по п.6, где лекарственное средство предназначено для лечения: нейрологического заболевания, такого как болезнь Альцгеймера, деменцию, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических расстройств, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания

Claims (18)

1. Соединение общей формулы (I), которое представляет собой 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид
Figure 00000001
или его фармацевтически приемлемая соль.
2. Фармацевтически приемлемая соль соединения по п.1, которая представляет собой кислотно-аддитивную соль, образованную 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамидом и кислотой.
3. Фармацевтически приемлемая соль соединения по п.2, где кислота представляет собой малеиновую, хлористоводородную, бромистоводородную, фосфорную, уксусную, фумаровую, салициловую, серную, лимонную, молочную, миндальную, винно-каменную и метансульфоновую кислоту.
4. Фармацевтическая композиция, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид
Figure 00000001
или его фармацевтически приемлемую соль, и фармацевтически приемлемый носитель или эксцепиент.
5. Соединение по п.1, используемое в терапии.
6. Применение 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемой соли в получении лекарственного средства для лечения нейрологического заболевания или психиатрического расстройства.
7. Применение по п.6, где лекарственное средство предназначено для лечения: нейрологического заболевания, такого как болезнь Альцгеймера, деменцию, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических расстройств, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания с гиперактивностью, депрессию или привыкание.
8. Применение по п.6, где лекарственное средство используют для лечения ухудшения познавательной способности, вызванной заболеванием.
9. Применение по п.8, где лекарственное средство используют для лечения ухудшения познавательской способности, вызванной болезнью Альцгеймера, или родственного нейродегенеративного нарушения.
10. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль в качестве терапевтического вещества, используемого при лечении нейрологического заболевания или психиатрического расстройства.
11. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль по п.10 в качестве терапевтического вещества, используемого при лечении: нейрологического заболевания, такого как болезнь Альцгеймера, деменция, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических заболеваний, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания с гиперактивностью, депрессию и привыкание.
12. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль по п.10 в качестве терапевтического вещества, используемого для лечения ухудшения нарушения познавательной способности, вызванной заболеванием.
13. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид по п.12 или его фармацевтически приемлемая соль в качестве терапевтического вещества, используемого для лечения ухудшения познавательной способности, вызванной болезнью Альцгеймера или родственным нейродегенеративным нарушением.
14. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид по п.13 или его фармацевтически приемлемая соль в качестве терапевтического вещества используемого для лечения ухудшения познавательной способности, вызванной болезнью Альцгеймера.
15. Фармацевтическая композиция, предназначенная для лечения неврологического заболевания, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метил-никотинамид или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель или эксцепиент.
16. Фармацевтическая композиция по п.15, где неврологическим заболеванием является болезнь Альцгеймера, деменция, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсия, невропатическая боль, болезнь Паркинсона, рассеянный склероз или удар.
17. Способ получения соединения формулы (I) по п.1 или его фармацевтически приемлемой соли
Figure 00000002
I
где R1 представляет собой незамещенный циклобутил;
R2 представляет собой 2-пиридинил, замещенный СОN(H)(Me), и представляет собой 4-метиламинокарбонилпиридин-2-ил, который включает
а) взаимодействие соединения формулы (II)
Figure 00000003
где R1 определен выше,
с соединением формулы R2'-L1, где R2' такой, как определен выше для R2 или группа, превращаемая в него, a L1 обозначает подходящую уходящую группу, или
в) взаимодействие соединения формулы (III)
Figure 00000004
где R2 такой, как определено выше,
с соединением формулы R1'-L2, где R1' такой, как определено выше для R1 или группа, превращаемая в него, a L2 обозначает подходящую уходящую группу, или
с) взаимодействие соединения формулы (III), как определено выше, с кетоном формулы R1'=O, где R1' такой, как определен для R1 или группа, превращаемая в него, или
d) удаление защитной группы с защищенного соединения формулы (I).
18. Способ по п.17, где
на стадии а) R2' определен выше для R2 и L1 обозначает подходящую уходящую группу, такую как атом галогена или активированная гидроксильная группа, и
на стадии в) R1' определен выше для R1 и L2 обозначает подходящую уходящую группу, такую как атом галогена.
RU2009138602/04A 2002-12-20 2003-12-18 Новые производные бензазепина RU2423353C1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0229820.6 2002-12-20
GB0229820A GB0229820D0 (en) 2002-12-20 2002-12-20 Novel compounds
GB0312607.5 2003-06-02
GB0312607A GB0312607D0 (en) 2003-06-02 2003-06-02 Novel compounds

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
RU2005122932/04A Division RU2388752C2 (ru) 2002-12-20 2003-12-18 (3-ЦИКЛОАЛКИЛ-2,3,4,5-ТЕТРАГИДРО-1Н-БЕНЗО[d]АЗЕПИН-7-ИЛОКСИ)ПРОИЗВОДНЫЕ, ИХ ПРИМЕНЕНИЕ ДЛЯ ИНГИБИРОВАНИЯ Н3 РЕЦЕПТОРОВ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ПОЛУЧЕНИЯ

Publications (2)

Publication Number Publication Date
RU2009138602A true RU2009138602A (ru) 2011-04-27
RU2423353C1 RU2423353C1 (ru) 2011-07-10

Family

ID=32683982

Family Applications (2)

Application Number Title Priority Date Filing Date
RU2009138602/04A RU2423353C1 (ru) 2002-12-20 2003-12-18 Новые производные бензазепина
RU2005122932/04A RU2388752C2 (ru) 2002-12-20 2003-12-18 (3-ЦИКЛОАЛКИЛ-2,3,4,5-ТЕТРАГИДРО-1Н-БЕНЗО[d]АЗЕПИН-7-ИЛОКСИ)ПРОИЗВОДНЫЕ, ИХ ПРИМЕНЕНИЕ ДЛЯ ИНГИБИРОВАНИЯ Н3 РЕЦЕПТОРОВ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ПОЛУЧЕНИЯ

Family Applications After (1)

Application Number Title Priority Date Filing Date
RU2005122932/04A RU2388752C2 (ru) 2002-12-20 2003-12-18 (3-ЦИКЛОАЛКИЛ-2,3,4,5-ТЕТРАГИДРО-1Н-БЕНЗО[d]АЗЕПИН-7-ИЛОКСИ)ПРОИЗВОДНЫЕ, ИХ ПРИМЕНЕНИЕ ДЛЯ ИНГИБИРОВАНИЯ Н3 РЕЦЕПТОРОВ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ПОЛУЧЕНИЯ

Country Status (27)

Country Link
US (4) US7696193B2 (ru)
EP (3) EP1572215B1 (ru)
JP (2) JP4584831B2 (ru)
KR (2) KR100897642B1 (ru)
AR (1) AR042542A1 (ru)
AT (1) ATE441417T1 (ru)
AU (1) AU2003294909B2 (ru)
BR (1) BR0317483A (ru)
CA (1) CA2509413C (ru)
CY (1) CY1109558T1 (ru)
DE (1) DE60329123D1 (ru)
DK (1) DK1572215T3 (ru)
EG (1) EG25204A (ru)
ES (3) ES2401319T3 (ru)
IL (2) IL169091A (ru)
IS (1) IS2907B (ru)
MA (1) MA27582A1 (ru)
MX (1) MXPA05006567A (ru)
MY (1) MY138478A (ru)
NO (2) NO331068B1 (ru)
NZ (1) NZ540148A (ru)
PL (2) PL220722B1 (ru)
PT (1) PT1572215E (ru)
RU (2) RU2423353C1 (ru)
SI (1) SI1572215T1 (ru)
TW (1) TWI323256B (ru)
WO (1) WO2004056369A1 (ru)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100897642B1 (ko) * 2002-12-20 2009-05-14 글락소 그룹 리미티드 신경 장애 치료용 벤즈아제핀 유도체
EP1680127B1 (en) 2003-10-23 2008-10-15 F. Hoffmann-La Roche Ag Benzazepine derivatives as mao-b inhibitors
GB0329214D0 (en) * 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
GB0405628D0 (en) * 2004-03-12 2004-04-21 Glaxo Group Ltd Novel compounds
GB0408083D0 (en) * 2004-04-08 2004-05-12 Glaxo Group Ltd Novel compounds
TW200611701A (en) * 2004-06-18 2006-04-16 Glaxo Group Ltd Novel compounds
GB0418267D0 (en) * 2004-08-16 2004-09-15 Glaxo Group Ltd Novel compounds
CA2594383A1 (en) * 2005-01-07 2006-07-13 Glaxo Group Limited 6- (2 , 3 , 4 , 5-tetrahydro-lh-benzo [d] azepin-7-yloxy) -nicotamide derivatives as radiolabelled ligands
GB0513886D0 (en) 2005-07-06 2005-08-10 Glaxo Group Ltd Novel compounds
EP2275096A3 (en) 2005-08-26 2011-07-13 Braincells, Inc. Neurogenesis via modulation of the muscarinic receptors
WO2007045989A1 (en) * 2005-10-20 2007-04-26 Pfizer Limited Pyridyl derivatives useful as h3 ligands
CN101296902A (zh) * 2005-10-27 2008-10-29 Ucb医药有限公司 包含内酰胺或内酰胺衍生部分的化合物、制备它们的方法和它们的用途
DE602006017741D1 (de) * 2005-11-18 2010-12-02 Hoffmann La Roche Azaindol-2-carboxamid-derivate
EA015555B1 (ru) * 2006-05-30 2011-08-30 Янссен Фармацевтика Н.В. Замещенные пиридиламидные соединения в качестве модуляторов гистаминового h-рецептора
US20070293475A1 (en) * 2006-06-20 2007-12-20 Alcon Manufacturing Ltd. Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma
RU2449989C2 (ru) 2006-06-23 2012-05-10 Эбботт Лэборетриз Производные циклопропиламина в качестве модуляторов h3-гистаминового рецептора
US9108948B2 (en) * 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
GB2441014A (en) * 2006-09-14 2008-02-20 Glaxo Group Ltd Polymorphic form of 6-(3-cyclobuty1-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methyl-nicotinamide hydrochloride for use in therapy
CL2008000596A1 (es) * 2007-03-01 2008-09-05 Glaxo Group Ltd Forma de dosificacion que comprende 1-(6-[(3-ciclobutil-2,3,4,5-tetrahidro-1h-3-benzazepin-7-il)oxi]-3-piridinil)-2-pirrolidinona, un estabilizador, un excipiente; procedimiento de preparacion; y su uso para tratar enfermedades neurologicas.
CL2008000597A1 (es) * 2007-03-01 2008-09-05 Glaxo Group Ltd Forma de dosificacion que comprende 6-(3-ciclobutil-2,3,4,5-tetrahidro-1h-benzo[d]azepin-7-il oxi)-n-metil nicotinamida, un estabilizante y un excipiente; procedimiento de preparacion; y su uso para tratar enfermedades neurologicas.
KR101547705B1 (ko) 2007-05-22 2015-08-26 와이어쓰 엘엘씨 히드라지드의 개선된 제조 방법
WO2009030716A1 (en) * 2007-09-06 2009-03-12 Glaxo Group Limited Piperazine derivative having affinity for the histamine h3 receptor
US8383657B2 (en) 2007-12-21 2013-02-26 Abbott Laboratories Thiazolylidine urea and amide derivatives and methods of use thereof
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
WO2011051423A1 (en) 2009-11-02 2011-05-05 Glaxo Group Limited Treatment or prophylaxis of dementia, neurodegenerative disorders, schizophrenia, adhd, somnolence or epilepsy
WO2011083316A1 (en) * 2010-01-08 2011-07-14 Takeda Pharmaceutical Company Limited Benzazepine derivatives for the treatment of central nervous system disorders
WO2012037258A1 (en) 2010-09-16 2012-03-22 Abbott Laboratories Processes for preparing 1,2-substituted cyclopropyl derivatives
HRP20151003T1 (hr) * 2011-02-23 2015-10-23 Suven Life Sciences Limited Novi spojevi kao ligandi receptora histamina h3
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
DK2686310T5 (en) 2011-03-14 2018-07-09 Boehringer Ingelheim Int Benzodioxan-INHIBITORERAFLEUKOTRIEN PRODUCTION
WO2013012844A1 (en) 2011-07-19 2013-01-24 Boehringer Ingelheim International Gmbh Arylpyrazole ethers as inhibitors of leukotriene a4 hydrolase
BR112014017493A8 (pt) * 2012-01-16 2017-07-04 Glaxosmithkline Ip Dev Ltd usos terapêuticos
CN104114538B (zh) * 2012-01-16 2016-04-13 葛兰素史克知识产权发展有限公司 治疗用途
EA201400976A1 (ru) 2012-03-06 2015-02-27 Бёрингер Ингельхайм Интернациональ Гмбх Бензодиоксаны в комбинации с другими активными средствами для ингибирования продуцирования лейкотриена
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
EP2647377A1 (en) 2012-04-06 2013-10-09 Sanofi Use of an h3 receptor antagonist for the treatment of alzheimer's disease
US9403830B2 (en) 2012-07-17 2016-08-02 Boehringer Ingelheim International Gmbh Inhibitors of leukotriene production
WO2015009609A1 (en) 2013-07-15 2015-01-22 Boehringer Ingelheim International Gmbh Inhibitors of leukotriene production
JP2016523982A (ja) 2013-07-15 2016-08-12 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン生成の阻害剤
WO2016123629A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
EP4251148A1 (en) 2020-11-27 2023-10-04 Richter Gedeon Nyrt. Histamine h3 receptor antagonists/inverse agonists for the treatment of autism spectrum disorder
AU2022376563A1 (en) 2021-11-01 2023-12-07 Alkahest, Inc. Benzodioxane modulators of leukotriene a4 hydrolase (lta4h) for prevention and treatment of aging-associated diseases

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3393192A (en) * 1965-04-26 1968-07-16 Schering Corp Novel benzazepines
CA974989A (en) 1968-03-11 1975-09-23 Wallace And Tiernan Inc. Process for preparing 1,2,4,5-tetrahydro-3h,3-benzazepines and products obtained thereby
US4233217A (en) * 1968-03-11 1980-11-11 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H, 3 benzazepines
DE2207430C3 (de) 1972-02-14 1982-05-13 Pennwalt Corp., 19102 Philadelphia, Pa. 1,2,4,5-Tetrahydro-3H-3-benzazepin, ein Verfahren zu ihrer Herstellung und diese enthaltendes pharmazeutisches Mittel
US4210749A (en) * 1974-11-12 1980-07-01 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H,3 benzazepines
US4206210A (en) * 1977-01-19 1980-06-03 Smithkline Corporation Alkylthio-7,8-dihdroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having dopaminergic activity
US4843081A (en) * 1984-09-04 1989-06-27 Rorer Pharmaceutical Corporation Aryl and heteroaryl substituted cycloalkyl compounds
US5175157A (en) * 1985-11-27 1992-12-29 Boehringer Ingelheim Gmbh Cyclic amine derivatives, pharmaceutical compositions containing these compounds and methods for preparing them
DE3717561A1 (de) 1987-05-25 1988-12-08 Thomae Gmbh Dr K Indol-, isochinolin- und benzazepinderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
JPS6394239A (ja) 1986-10-08 1988-04-25 Konica Corp 色素画像の安定性を改良したハロゲン化銀写真感光材料
ZA882080B (en) * 1987-03-27 1989-04-26 Schering Corp Substituted benzazepines,their preparation and pharmaceutical compositions containing them
DK325188D0 (da) 1988-06-15 1988-06-15 Novo Industri As Hidtil ukendte benzazepinderivater
FR2642756B1 (fr) 1989-02-07 1994-03-04 Sanofi Derives cycloaminoalkoxyphenyle, leur procede de preparation ainsi que les compositions pharmaceutiques ou veterinaires en contenant
US4959374A (en) * 1989-07-06 1990-09-25 Beecham Group P.L.C. Novel compounds
AU8201591A (en) 1990-06-15 1992-01-07 Schering Corporation 8-lower alkyl-5-cycloalkyl or 5-cycloalkenyl substitued benzazepines and pharmaceutical compositions containing them
TW197435B (ru) 1990-11-22 1993-01-01 Takeda Pharm Industry Co Ltd
WO1993000094A2 (en) 1991-06-21 1993-01-07 Smithkline Beecham Plc Use of tetrahydrobenzazepine derivatives for the treatment of portal hypertension and migraine
GB9116824D0 (en) 1991-08-05 1991-09-18 Smithkline Beecham Corp Chemical compounds
GB9119467D0 (en) 1991-09-12 1991-10-23 Smithkline Beecham Corp Chemical compounds
JPH05194406A (ja) 1991-11-12 1993-08-03 Yoshitomi Pharmaceut Ind Ltd 新規アミド化合物
DK23392D0 (da) * 1992-02-24 1992-02-24 Novo Nordisk As Heterocykliske forbindelser, deres anvendelse og fremstilling
US5241065A (en) 1992-02-25 1993-08-31 Schering Corporation 2,3,4,5-tetrahydro-1h-3-benzazepines having anti-psychotic activity
JPH05239024A (ja) 1992-02-28 1993-09-17 Takeda Chem Ind Ltd 縮合複素環カルボン酸誘導体、その製造法、中間体および剤
CA2135644C (en) 1992-05-14 2009-01-27 Elisabetta Vegeto Mutated steroid hormone receptors, methods for their use and molecular switch for gene therapy
US5364791A (en) 1992-05-14 1994-11-15 Elisabetta Vegeto Progesterone receptor having C. terminal hormone binding domain truncations
DE4332168A1 (de) 1993-02-22 1995-03-23 Thomae Gmbh Dr K Cyclische Derivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
SE9300657D0 (sv) 1993-02-26 1993-02-26 Astra Ab New compounds
US5387685A (en) 1993-07-16 1995-02-07 American Cyanamid Co MDR reversal agents
EP0728003A1 (en) 1993-11-12 1996-08-28 Cell Therapeutics, Inc. Method for preventing tissue injury from hypoxia
WO1995014028A2 (en) 1993-11-18 1995-05-26 Washington University Compounds and pharmaceutical compositions for the treatment and prophylaxis of bacterial infections
DE4429079A1 (de) 1994-08-17 1996-02-22 Thomae Gmbh Dr K Cyclische Harnstoffderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19530996A1 (de) 1995-08-23 1997-02-27 Boehringer Mannheim Gmbh Cyclische Guanidine, Verfahren zu ihrer Herstellung und Arzneimittel
EP0920417A4 (en) 1996-08-15 1999-12-29 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
US5932590A (en) 1996-12-05 1999-08-03 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU5495398A (en) 1997-01-17 1998-08-07 Takeda Chemical Industries Ltd. Idebenone containing combination agent for treating alzheimer's disease
GB9724372D0 (en) 1997-11-18 1998-01-14 Smithkline Beecham Plc Novel compounds
CA2310330A1 (en) 1997-11-20 1999-06-03 Teijin Limited Biphenylamidine derivatives
JP3283032B2 (ja) 1998-02-02 2002-05-20 エルジ ケミカル リミテッド ピペリジン構造を有するファネシル転移酵素阻害剤及びその製造方法
EP0937723A1 (de) 1998-02-18 1999-08-25 Roche Diagnostics GmbH Neue Sulfonamide, Verfahren zu ihrer Herstellung sowie diese enthaltende Arzneimittel
ID26403A (id) 1998-04-20 2000-12-21 Basf Ag Amida baru yang tersubstitusi, pembuatan dan penggunaannya
BR9909994A (pt) 1998-04-29 2000-12-26 Smithkline Beecharm P L C Quinolinas usadas como inibidores de mrs e bactericidas
EP0982300A3 (en) 1998-07-29 2000-03-08 Societe Civile Bioprojet Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications
GB9816982D0 (en) 1998-08-05 1998-09-30 Smithkline Beecham Plc Novel compounds
AU761018B2 (en) 1998-10-08 2003-05-29 Smithkline Beecham Plc Tetrahydrobenzazepine derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents)
AU6123699A (en) 1998-10-16 2000-05-08 Takeda Chemical Industries Ltd. Nitrogenous fused heterocycle compounds, process for the preparation thereof andagents containing the same
AU778005B2 (en) 1998-12-24 2004-11-11 Bristol-Myers Squibb Pharma Company Succinoylamino benzodiazepines as inhibitors of Abeta protein production
GB9914255D0 (en) 1999-06-18 1999-08-18 Lilly Forschung Gmbh Pharmaceutical compounds
WO2001003680A2 (en) 1999-07-09 2001-01-18 Isis Innovation Limited Compounds for inhibiting diseases and preparing cells for transplantation
ES2209728T3 (es) * 1999-08-06 2004-07-01 F. Hoffmann-La Roche Ag Tetrahidro-benzo(d)azepinas y su uso como antagonistas de receptores de glutamato metabotropico.
CA2390376A1 (en) 1999-11-09 2001-05-17 William Leonard Scott .beta.-aminoacid compounds useful for inhibiting .beta.-amyloid peptide release and/or its synthesis
KR20020067937A (ko) 2000-01-26 2002-08-24 오노 야꾸힝 고교 가부시키가이샤 벤젠 축합 헤테로환 유도체 및 그 유도체를 유효성분으로서 함유하는 약제
JP2001226269A (ja) 2000-02-18 2001-08-21 Takeda Chem Ind Ltd メラニン凝集ホルモン拮抗剤
EP1148054B1 (en) 2000-04-21 2005-11-23 Pfizer Products Inc. Thyroid receptor ligands
MXPA02010452A (es) 2000-05-11 2003-06-06 Bristol Myers Squibb Co Analogos de tetrahidroisoquinolina utiles como secretagogos de la hormona del crecimiento.
JP2002371059A (ja) * 2000-05-16 2002-12-26 Takeda Chem Ind Ltd メラニン凝集ホルモン拮抗剤
AU2001256733A1 (en) 2000-05-16 2001-11-26 Takeda Chemical Industries Ltd. Melanin-concentrating hormone antagonist
US20040063699A1 (en) * 2000-07-04 2004-04-01 Naoki Tarui Gpr14 antagonist
EP1308513A4 (en) * 2000-08-10 2008-07-09 Takeda Pharmaceutical APPLICATION OF POLYPEPTIDES
US20030207863A1 (en) * 2000-08-25 2003-11-06 Hiroaki Fukumoto Preventives and remedies for central nervous system diseases
AU2002235277A1 (en) * 2000-10-23 2002-05-06 Smith Kline Beecham Corporation Compounds and methods
HUP0302264A2 (hu) 2000-11-14 2003-11-28 Smithkline Beecham P.L.C. Dopamin D3 receptorok modulátoraiként felhasználható tetrahidrobenzazepin-származékok és ezeket tartalmazó gyógyszerkészítmények
UA77165C2 (en) 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition
FR2819512B1 (fr) 2001-01-18 2003-02-21 Servier Lab Nouveaux composes cyclo[d] azepane, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DK1363705T3 (da) 2001-02-02 2012-09-24 Bristol Myers Squibb Co Sammensætning og antiviral aktivitet i substituerede azaindoloxoeddikesurpiperazin-derivater
US6649606B1 (en) 2001-11-09 2003-11-18 Bristol-Myers Squibb Co. Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
US7196108B2 (en) 2002-03-08 2007-03-27 Incyte San Diego Inc. Bicyclic heterocycles for the treatment of diabetes and other diseases
US6953787B2 (en) 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
AU2003223012A1 (en) 2002-04-26 2003-11-10 Pfizer Products Inc. Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors
WO2003091258A1 (en) 2002-04-26 2003-11-06 Pfizer Products Inc. N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
WO2004018432A1 (en) 2002-08-20 2004-03-04 Eli Lilly And Company Substituted azepines as histamine h3 receptor antagonists, preparation and therapeutic uses
ES2305491T3 (es) 2002-09-19 2008-11-01 Eli Lilly And Company Eteres de diarilo como antagonistas de receptores de opioides.
GB0224083D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
KR100897642B1 (ko) * 2002-12-20 2009-05-14 글락소 그룹 리미티드 신경 장애 치료용 벤즈아제핀 유도체
AU2003292625B2 (en) 2002-12-26 2008-07-24 Eisai R & D Management Co., Ltd. Selective estrogen receptor modulators
CA2515269A1 (en) 2003-02-07 2004-08-19 Warner-Lambert Company Llc Oxazolidinone derivatives n-substituted by a bicyclic ring, for use as antibacterial agents
CA2536659A1 (en) 2003-08-08 2005-02-17 Glaxo Group Limited Process
EP1680127B1 (en) 2003-10-23 2008-10-15 F. Hoffmann-La Roche Ag Benzazepine derivatives as mao-b inhibitors
GB0329214D0 (en) * 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
ES2375963T3 (es) 2003-12-18 2012-03-07 Abbott Gmbh & Co. Kg Tetrahidrobenzacepinas y su uso en la modulación del receptor d3 de la dopamina.
GB0405628D0 (en) * 2004-03-12 2004-04-21 Glaxo Group Ltd Novel compounds
GB0408083D0 (en) * 2004-04-08 2004-05-12 Glaxo Group Ltd Novel compounds
TW200611701A (en) * 2004-06-18 2006-04-16 Glaxo Group Ltd Novel compounds
GB0418267D0 (en) * 2004-08-16 2004-09-15 Glaxo Group Ltd Novel compounds

Also Published As

Publication number Publication date
KR20070089762A (ko) 2007-08-31
RU2005122932A (ru) 2006-04-10
US20070299056A1 (en) 2007-12-27
CA2509413C (en) 2012-05-01
US7799773B2 (en) 2010-09-21
US20100145040A1 (en) 2010-06-10
US7704994B2 (en) 2010-04-27
ATE441417T1 (de) 2009-09-15
KR100765027B1 (ko) 2007-10-09
NO20110408L (no) 2005-09-15
WO2004056369A1 (en) 2004-07-08
IS2907B (is) 2014-11-15
NO331068B1 (no) 2011-09-26
JP2006512412A (ja) 2006-04-13
US8207331B2 (en) 2012-06-26
NZ540148A (en) 2007-11-30
AU2003294909A1 (en) 2004-07-14
KR20050088195A (ko) 2005-09-02
JP2010248239A (ja) 2010-11-04
EP2133340B1 (en) 2013-01-16
RU2423353C1 (ru) 2011-07-10
NO20053384L (no) 2005-09-15
IL169091A0 (en) 2007-07-04
ES2401216T3 (es) 2013-04-17
SI1572215T1 (sl) 2010-01-29
AU2003294909B2 (en) 2007-05-17
EG25204A (en) 2011-11-14
EP2186516A1 (en) 2010-05-19
PL220722B1 (pl) 2015-12-31
NO332218B1 (no) 2012-07-30
MXPA05006567A (es) 2005-08-16
DE60329123D1 (de) 2009-10-15
EP1572215A1 (en) 2005-09-14
CY1109558T1 (el) 2014-08-13
ES2401319T3 (es) 2013-04-18
IS7941A (is) 2005-07-18
NO20053384D0 (no) 2005-07-12
US7696193B2 (en) 2010-04-13
AR042542A1 (es) 2005-06-22
MA27582A1 (fr) 2005-10-03
US20090105226A1 (en) 2009-04-23
EP1572215B1 (en) 2009-09-02
JP5315299B2 (ja) 2013-10-16
JP4584831B2 (ja) 2010-11-24
TW200500344A (en) 2005-01-01
HK1085647A1 (en) 2006-09-01
TWI323256B (en) 2010-04-11
DK1572215T3 (da) 2010-01-11
PT1572215E (pt) 2009-12-09
IL202827A (en) 2011-08-31
CA2509413A1 (en) 2004-07-08
PL377315A1 (pl) 2006-01-23
KR100897642B1 (ko) 2009-05-14
MY138478A (en) 2009-06-30
ES2333008T3 (es) 2010-02-16
RU2388752C2 (ru) 2010-05-10
BR0317483A (pt) 2005-11-16
EP2133340A1 (en) 2009-12-16
IL169091A (en) 2011-11-30
EP2186516B1 (en) 2013-01-16
US20060040918A1 (en) 2006-02-23
PL397229A1 (pl) 2012-02-27

Similar Documents

Publication Publication Date Title
RU2009138602A (ru) Новые производные бензазепина
EP1599462B1 (en) Process of preparing imatinib
ES2264060T3 (es) Derivado de 2-oxo-1-pirrolidina y sus usos farmaceuticos.
EP1072266B1 (en) Thienylazolylalcoxyethanamines, their preparation and their application as medicaments
UA83899C2 (ru) Соединения имидазола для лечения нейродегенеративных расстройств
MXPA05002420A (es) Compuestos de tiazol para el tratamiento de trastornos neurodegenerativos.
JP5957495B2 (ja) 新規ヘテロ環化合物およびその使用
EP2486002A1 (en) Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2005079802A8 (en) Bipyridyl amides as modulators of metabotropic glutamate receptor-5
CA2501799A1 (en) Pyrazole compounds for treatment of neurodegenerative disorders
JP6017496B2 (ja) 新規ヘテロ環化合物およびその使用
ATE367387T1 (de) Verwendung von oxindolderivaten zur behandlung von mit demenz in zusammenhang stehenden krankheiten, alzheimer-krankheit und mit glycogensynthasekinase-3 assoziierten leiden
CA2498945A1 (en) Process for the preparation of 2-amino-4,5,6,7-tetrahydro-6-aminobenzothiazoles from cyclohexanes and cyclohexanones as intermediates
TW200635589A (en) Therapeutic agents
JP2020520936A5 (ru)
TWI251594B (en) Preparation of substituted quinoxalines
RU2005126608A (ru) Производные ациламинотиазола, их получение и их применение в качестве ингибиторов продукции бета-амилоидного пептида
CN112521357B (zh) 一种长效低成瘾性hnk衍生物及其制备方法
ATE421961T1 (de) Piperidinderivate, verfahren zu deren herstellung und pharmazeutische zusammensetzung zur behandlung von alzheimer-krankheit, die diese derivate enthält
KR20230024383A (ko) 장기 작용성 및 저중독성 화합물 및 그의 제조 방법
JPH10182635A (ja) 光学活性ピペリジン誘導体及びその製造方法
JP2011102241A (ja) 新規１−アミノカルボニルピペリジン誘導体
JP2008537935A (ja) トルペリゾンの付加塩、その製造方法およびその使用
JP7579595B2 (ja) 長時間作用性の低嗜癖性ｈｎｋ誘導体及びその製造方法
CN112516130B (zh) 一种长效低成瘾性化合物在制备药物中的应用

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20181219