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RU2006113600A - Неседативный а-2-агонист 1-(2,3-диметил-фенил)-этил-1,3-дигидро-имидазол-2-тион - Google Patents

Неседативный а-2-агонист 1-(2,3-диметил-фенил)-этил-1,3-дигидро-имидазол-2-тион Download PDF

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Publication number
RU2006113600A
RU2006113600A RU2006113600/04A RU2006113600A RU2006113600A RU 2006113600 A RU2006113600 A RU 2006113600A RU 2006113600/04 A RU2006113600/04 A RU 2006113600/04A RU 2006113600 A RU2006113600 A RU 2006113600A RU 2006113600 A RU2006113600 A RU 2006113600A
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Prior art keywords
selective agonist
agonist
brimonidine
stereoisomer
amide
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RU2006113600/04A
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RU2345987C2 (ru
Inventor
Кен ЧОУ (US)
Кен ЧОУ
Тод М. ХЕЙДЕЛБАУ (US)
Тод М. ХЕЙДЕЛБАУ
Джон Э. ДОНЕЛЛО (US)
Джон Э. ДОНЕЛЛО
Дэниел В. ДЖИЛ (US)
Дэниел В. ДЖИЛ
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Аллерган, Инк. (Us)
Аллерган, Инк.
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/04—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/84—Sulfur atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (6)

1. α-2А/α-1А селективный агонист, представляющий собой следующее соединение:
Figure 00000001
или его фармацевтически приемлемую соль, эфир, амид, стереоизомер или рацемическую смесь.
2. α-2А/α-1А селективный агонист по п.1, где указанный селективный агонист обладает α-1А эффективностью, меньшей по сравнению с бримонидином, и соотношением α-1А/α-2А эффективностей, большим по сравнению с бримонидином.
3. α-2А/α-1А селективный агонист по п.1, представляющий собой следующее соединение:
Figure 00000001
4. Фармацевтическая композиция, включающая фармацевтический носитель и терапевтически эффективное количество α-2А/α-1А селективного агониста, который представляет собой следующее соединение:
Figure 00000001
или его фармацевтически приемлемую соль, эфир, амид, стереоизомер или рацемическую смесь.
5. Фармацевтическая композиция по п.4, где указанный селективный агонист обладает α-1А эффективностью, меньшей по сравнению с бримонидином, и соотношением α-1А/α-2А эффективностей, большим по сравнению с бримонидином.
6. Фармацевтическая композиция по п.4, где указанный селективный агонист представляет собой следующее соединение:
Figure 00000001
RU2006113600/04A 2003-09-12 2004-08-20 Неседативный а-2-агонист 1-(2,3-диметилфенил)-этил-1,3-дигидроимидазол-2-тион RU2345987C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US50256203P 2003-09-12 2003-09-12
US60/502,562 2003-09-12
US10/891,953 2004-07-15
US10/891,953 US7141597B2 (en) 2003-09-12 2004-07-15 Nonsedating α-2 agonists
US10/891.953 2004-07-15

Publications (2)

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RU2006113600A true RU2006113600A (ru) 2007-11-10
RU2345987C2 RU2345987C2 (ru) 2009-02-10

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US (4) US7141597B2 (ru)
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CN (1) CN100417379C (ru)
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AU (1) AU2004279332B2 (ru)
BR (1) BRPI0413719A (ru)
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CO (1) CO5680444A2 (ru)
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DE (2) DE602004005720T2 (ru)
DK (2) DK1663206T3 (ru)
ES (1) ES2285522T3 (ru)
IL (1) IL173530A (ru)
MX (1) MXPA06002668A (ru)
NO (1) NO20060667L (ru)
NZ (1) NZ545181A (ru)
PL (2) PL379561A1 (ru)
PT (1) PT1663206E (ru)
RU (1) RU2345987C2 (ru)
SI (1) SI1663206T1 (ru)
TW (1) TWI337999B (ru)
WO (1) WO2005034946A1 (ru)
ZA (1) ZA200601002B (ru)

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US20050059721A1 (en) 2005-03-17
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CN100417379C (zh) 2008-09-10
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NO20060667L (no) 2006-04-06
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EP1800679A2 (en) 2007-06-27
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US8022226B2 (en) 2011-09-20
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IL173530A0 (en) 2006-07-05
AU2004279332A1 (en) 2005-04-21
RU2345987C2 (ru) 2009-02-10
EP1800679A3 (en) 2009-01-21
ZA200601002B (en) 2007-04-25
DE602004005720D1 (de) 2007-05-16
US20080176918A1 (en) 2008-07-24
US20070004790A1 (en) 2007-01-04
CA2537832C (en) 2012-01-24
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US7141597B2 (en) 2006-11-28
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