EA200100709A1 - БЕНЗИЗОКСАЗОЛЫ И ФЕНОНЫ В КАЧЕСТВЕ α2-АНТАГОНИСТОВ - Google Patents

БЕНЗИЗОКСАЗОЛЫ И ФЕНОНЫ В КАЧЕСТВЕ α2-АНТАГОНИСТОВ

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Publication number
EA200100709A1
EA200100709A1 EA200100709A EA200100709A EA200100709A1 EA 200100709 A1 EA200100709 A1 EA 200100709A1 EA 200100709 A EA200100709 A EA 200100709A EA 200100709 A EA200100709 A EA 200100709A EA 200100709 A1 EA200100709 A1 EA 200100709A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
aryl
halogen
relates
phenyl
Prior art date
Application number
EA200100709A
Other languages
English (en)
Other versions
EA003606B1 (ru
Inventor
Людо Эдмонд Жозефин Кеннис
Йозефус Каролус Мертенс
Серж Мария Алойсиус Питерс
Original Assignee
Янссен Фармацевтика Н.В.
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 Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA200100709A1 publication Critical patent/EA200100709A1/ru
Publication of EA003606B1 publication Critical patent/EA003606B1/ru

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    • 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
    • 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
    • A61P25/14—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
    • A61P25/24—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I), их N-оксидным формам, фармацевтически приемлемым солям присоединения и стереохимически изомерным формам, где Alk представляет собой Cалкандиил; n равно 1 или 2; р равно 1 и q равно 2; или р равно 2 и q равно 1; X представляет собой -O-, -S-, -S(=O)-, -S(=O)- или NR; каждый Rнезависимо представляет собой водород, галоген, Cалкил, нитро, гидрокси или Cалкилокси; Rпредставляет собой водород, Cалкил, арил или Cалкил, замещенный арилом; арил представляет собой фенил или фенил, замещенный галогеном или Cалкилом; D представляет собой необязательно замещенный бензофенон или 3-бензизоксазолил, имеющие антагонистическую активность к центральному α-адренорецептору, кроме того изобретение относится к их получению, фармацевтическому применению и композициям.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100709A 1998-12-21 1999-12-14 1,5-ПЕНТАНДИИЛЗАМЕЩЕННЫЕ 1,2,3,4-ТЕТРАГИДРОБЕНЗО (ФУРО, АЗО И ТИО) [3,2-c] ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ α-АНТАГОНИСТОВ EA003606B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP98204358 1998-12-21
PCT/EP1999/010054 WO2000037466A1 (en) 1998-12-21 1999-12-14 BENZISOXAZOLES AND PHENONES AS α2-ANTAGONISTS

Publications (2)

Publication Number Publication Date
EA200100709A1 true EA200100709A1 (ru) 2001-12-24
EA003606B1 EA003606B1 (ru) 2003-06-26

Family

ID=8234508

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100709A EA003606B1 (ru) 1998-12-21 1999-12-14 1,5-ПЕНТАНДИИЛЗАМЕЩЕННЫЕ 1,2,3,4-ТЕТРАГИДРОБЕНЗО (ФУРО, АЗО И ТИО) [3,2-c] ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ α-АНТАГОНИСТОВ

Country Status (30)

Country Link
US (1) US6576640B1 (ru)
EP (1) EP1140934B1 (ru)
JP (1) JP4717216B2 (ru)
KR (2) KR20060093139A (ru)
CN (1) CN1154646C (ru)
AR (1) AR021924A1 (ru)
AT (1) ATE251622T1 (ru)
AU (1) AU765751B2 (ru)
BG (1) BG65162B1 (ru)
BR (1) BR9916427A (ru)
CA (1) CA2355716C (ru)
CZ (1) CZ294532B6 (ru)
DE (1) DE69911995T2 (ru)
EA (1) EA003606B1 (ru)
EE (1) EE200100329A (ru)
ES (1) ES2209553T3 (ru)
HK (1) HK1045686B (ru)
HR (1) HRP20010444A2 (ru)
HU (1) HUP0104812A3 (ru)
ID (1) ID28967A (ru)
IL (2) IL143830A0 (ru)
NO (1) NO317892B1 (ru)
NZ (1) NZ511411A (ru)
PL (1) PL196958B1 (ru)
SK (1) SK285560B6 (ru)
TR (1) TR200101813T2 (ru)
TW (1) TWI229673B (ru)
UA (1) UA71938C2 (ru)
WO (1) WO2000037466A1 (ru)
ZA (1) ZA200105067B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04000036A (es) 2001-07-05 2004-05-21 Upjohn Co Benzofuranos sustituidos con (hetero) arilo como ligandos 5-ht.
CA2480266C (en) * 2002-04-03 2011-07-12 Orion Corporation Use of an alpha2-adrenoreceptor antagonist for cns-related diseases
EP1757605A4 (en) * 2004-04-12 2007-12-19 Taisho Pharmaceutical Co Ltd CYCLIC AMINE COMPOUND
KR20080034171A (ko) * 2005-07-28 2008-04-18 브리스톨-마이어스 스큅 컴퍼니 세로토닌 수용체 효능제 및 길항제로서의 치환된테트라히드로-1ｈ-피리도[4,3,ｂ]인돌

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3419568A (en) * 1966-12-07 1968-12-31 Abbott Lab Derivatives of 1,2,3,4-tetrahydro-5h-pyrido[4,3b]indoles
US3382250A (en) * 1966-12-07 1968-05-07 Abbott Lab Aroylalkyl derivatives of 1, 2, 3, 4-tetrahydro-5h-pyrido[4, 3b]indoles
US3718657A (en) * 1970-12-03 1973-02-27 Abbott Lab Certain-2-substituted-1,2,3,4-tetrahydro-beta or gamma carbolines
JPS4729395U (ru) * 1971-04-26 1972-12-04
AR206812A1 (es) * 1974-04-01 1976-08-23 Pfizer Compuestos intermediarios de azaciclo(3,4-a)indoles 4- y 5-fenil substituidos desprovistos de actividad terapeutica
US4001263A (en) * 1974-04-01 1977-01-04 Pfizer Inc. 5-Aryl-1,2,3,4-tetrahydro-γ-carbolines
US4224329A (en) * 1979-01-23 1980-09-23 Pfizer Inc. 2-Substituted-trans-5-aryl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles
FR2570701B1 (fr) * 1984-09-27 1987-05-22 Synthelabo Derives de furo(3,2-c)pyridines, leur preparation et leur application en therapeutique
DE3522959A1 (de) * 1985-06-27 1987-01-08 Merck Patent Gmbh Indolderivate
EP0339959A3 (en) * 1988-04-27 1991-03-20 Glaxo Group Limited Lactam derivatives
WO1994008040A1 (en) * 1992-09-25 1994-04-14 Synaptic Pharmaceutical Corporation Dna encoding human alpha 1 adrenergic receptors and uses thereof
US5403847A (en) 1992-11-13 1995-04-04 Synaptic Pharmaceutical Corporation Use of α1C specific compounds to treat benign prostatic hyperlasia
US5508306A (en) * 1992-11-13 1996-04-16 Synaptic Pharmaceutical Corporation Aromatic amine derivatives
UA52681C2 (ru) * 1997-04-08 2003-01-15 Янссен Фармацевтика Н.В. Производные 1,2,3,4-тетрагидро-бензофуро [3,2,-c] пиридина

Also Published As

Publication number Publication date
HRP20010444A2 (en) 2002-06-30
WO2000037466A1 (en) 2000-06-29
CN1331692A (zh) 2002-01-16
IL143830A0 (en) 2002-04-21
EE200100329A (et) 2002-08-15
NO317892B1 (no) 2004-12-27
NO20012783D0 (no) 2001-06-06
HK1045686B (zh) 2005-04-01
CA2355716C (en) 2010-05-18
PL196958B1 (pl) 2008-02-29
AU2432700A (en) 2000-07-12
EP1140934B1 (en) 2003-10-08
DE69911995D1 (de) 2003-11-13
PL348421A1 (en) 2002-05-20
AR021924A1 (es) 2002-09-04
CA2355716A1 (en) 2000-06-29
EP1140934A1 (en) 2001-10-10
TWI229673B (en) 2005-03-21
HUP0104812A3 (en) 2003-12-29
BG105521A (en) 2001-12-29
KR20010075650A (ko) 2001-08-09
DE69911995T2 (de) 2004-09-02
NZ511411A (en) 2002-12-20
BR9916427A (pt) 2001-09-04
ATE251622T1 (de) 2003-10-15
ES2209553T3 (es) 2004-06-16
CZ20012120A3 (cs) 2001-10-17
BG65162B1 (bg) 2007-04-30
UA71938C2 (en) 2005-01-17
KR20060093139A (ko) 2006-08-23
EA003606B1 (ru) 2003-06-26
SK285560B6 (sk) 2007-03-01
AU765751B2 (en) 2003-09-25
US6576640B1 (en) 2003-06-10
SK8582001A3 (en) 2001-12-03
JP2002533341A (ja) 2002-10-08
KR100657540B1 (ko) 2006-12-14
TR200101813T2 (tr) 2001-12-21
HK1045686A1 (en) 2002-12-06
CN1154646C (zh) 2004-06-23
NO20012783L (no) 2001-06-06
ID28967A (id) 2001-07-19
CZ294532B6 (cs) 2005-01-12
ZA200105067B (en) 2002-06-20
HUP0104812A2 (hu) 2002-04-29
IL143830A (en) 2007-07-24
JP4717216B2 (ja) 2011-07-06

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): KZ

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU