EA200401455A1 - Производные бензоксазина в качестве модуляторов 5-htи их применение - Google Patents

Производные бензоксазина в качестве модуляторов 5-htи их применение

Info

Publication number
EA200401455A1
EA200401455A1 EA200401455A EA200401455A EA200401455A1 EA 200401455 A1 EA200401455 A1 EA 200401455A1 EA 200401455 A EA200401455 A EA 200401455A EA 200401455 A EA200401455 A EA 200401455A EA 200401455 A1 EA200401455 A1 EA 200401455A1
Authority
EA
Eurasian Patent Office
Prior art keywords
application
hty
benzoxazine
modulators
derivatives
Prior art date
Application number
EA200401455A
Other languages
English (en)
Other versions
EA009982B1 (ru
Inventor
Якоб Бергер
Робин Дуглас Кларк
Шухай Чжао
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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 Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA200401455A1 publication Critical patent/EA200401455A1/ru
Publication of EA009982B1 publication Critical patent/EA009982B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • 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
    • 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
    • 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
    • A61P25/22—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

В заявке описано соединение формулы I, которое обладает сродством к рецептору 5-HT, его фармацевтически приемлемая соль или пролекарство, где R, R, R, R, R, R, R, R, R, Y, Z, m, n и p имеют значения, указанные в описании заявки. Кроме того, настоящее изобретение включает композиции, включающие соединение формулы I, способы применения и способы получения соединения формулы I.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200401455A 2002-05-13 2003-05-05 Производные бензоксазина в качестве модуляторов 5-нт-6, способ их получения, фармацевтические композиции, содержащие эти производные, и их применение EA009982B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37800302P 2002-05-13 2002-05-13
PCT/EP2003/004671 WO2003095434A1 (en) 2002-05-13 2003-05-05 Benzoxazine derivatives as 5-ht6 modulators and uses thereof

Publications (2)

Publication Number Publication Date
EA200401455A1 true EA200401455A1 (ru) 2005-06-30
EA009982B1 EA009982B1 (ru) 2008-04-28

Family

ID=29420358

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401455A EA009982B1 (ru) 2002-05-13 2003-05-05 Производные бензоксазина в качестве модуляторов 5-нт-6, способ их получения, фармацевтические композиции, содержащие эти производные, и их применение

Country Status (37)

Country Link
US (4) US6867204B2 (ru)
EP (1) EP1506179B1 (ru)
JP (1) JP4307377B2 (ru)
KR (1) KR100636475B1 (ru)
CN (1) CN100429206C (ru)
AR (1) AR039988A1 (ru)
AT (1) ATE316523T1 (ru)
AU (1) AU2003233231B2 (ru)
BR (1) BRPI0310032B8 (ru)
CA (1) CA2485136C (ru)
DE (1) DE60303376T2 (ru)
DK (1) DK1506179T3 (ru)
EA (1) EA009982B1 (ru)
EC (1) ECSP045420A (ru)
EG (1) EG25683A (ru)
ES (1) ES2256744T3 (ru)
GT (1) GT200300108A (ru)
HK (1) HK1080846A1 (ru)
HR (1) HRP20041030B1 (ru)
IL (1) IL164928A0 (ru)
JO (1) JO2413B1 (ru)
MA (1) MA27118A1 (ru)
MX (1) MXPA04011254A (ru)
MY (1) MY139612A (ru)
NO (1) NO329380B1 (ru)
NZ (1) NZ536230A (ru)
PA (1) PA8573501A1 (ru)
PE (1) PE20040757A1 (ru)
PL (1) PL211057B1 (ru)
PT (1) PT1506179E (ru)
RS (1) RS51042B (ru)
TN (1) TNSN04225A1 (ru)
TW (1) TWI258479B (ru)
UA (1) UA76877C2 (ru)
UY (1) UY27803A1 (ru)
WO (1) WO2003095434A1 (ru)
ZA (1) ZA200408783B (ru)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2036547A3 (en) * 2001-07-20 2009-12-23 Psychogenics Inc. Treatment for Attention-Deficit Hyperactivity Disorder
IL164108A0 (en) 2002-03-27 2005-12-18 Glaxo Group Ltd Quinoline derivatives and their useas 5-ht6 ligands
CN100429206C (zh) * 2002-05-13 2008-10-29 弗·哈夫曼-拉罗切有限公司 作为5－ht6调节剂的苯并嗪衍生物及其用途
PL377770A1 (pl) 2002-11-08 2006-02-20 F. Hoffmann-La Roche Ag Podstawione benzoksazynony i ich zastosowanie
RS20060035A (en) 2003-07-22 2008-08-07 Arena Pharmaceuticals Inc., Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
ES2291984T3 (es) * 2003-12-09 2008-03-01 F. Hoffmann-La Roche Ag Derivados de benzoxazina y su empleo.
JP4533391B2 (ja) * 2004-01-16 2010-09-01 エフ．ホフマン−ラ ロシュ アーゲー 中枢神経系疾患の処置のための５−ヒドロキシトリプタミンレセプター（５−ｈｔ）のモジュレーターとしての、１−ベンジル−５−ピペラジン−１−イル−３，４−ジヒドロ−１ｈ−キナゾリン−２−オン誘導体、ならびにそれぞれの１ｈ−ベンゾ（１，２，６）チアジアジン−２，２−ジオキシドおよび１，４−ジヒドロベンゾ（ｄ）（１，３）オキサジン−２−オン誘導体
DE602005019562D1 (de) * 2004-05-05 2010-04-08 Hoffmann La Roche Zur modulation des 5-ht6-rezeptors, des 5-ht2a-rezeptors oder beider rezeptoren geeignete arylsulfonylbenzodioxane
CA2581921A1 (en) * 2004-09-30 2006-04-13 F. Hoffmann-La Roche Ag Benzoxazine and quinoxaline derivatives and uses
DE602005026543D1 (de) * 2004-09-30 2011-04-07 Hoffmann La Roche Zusammensetzungen und verfahren zur behandlung kognitiver störungen
US7378415B2 (en) * 2004-09-30 2008-05-27 Roche Palo Alto Llc Benzoxazine and quinoxaline derivatives and uses thereof
US7713954B2 (en) * 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
EP2508177A1 (en) 2007-12-12 2012-10-10 Glaxo Group Limited Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
US9126946B2 (en) 2008-10-28 2015-09-08 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
AR078770A1 (es) * 2009-10-27 2011-11-30 Elara Pharmaceuticals Gmbh Derivados de dihidrobenzo oxacinas y tiazinas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades inflamatorias e hiperproliferativas.
KR101293384B1 (ko) * 2010-10-13 2013-08-05 주식회사 대웅제약 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도
US9403800B2 (en) * 2012-01-24 2016-08-02 Chemregen, Inc. Compounds for inhibition of cancer cell proliferation
CA2935944A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
JP2018516992A (ja) 2015-06-12 2018-06-28 アクソファント サイエンシーズ ゲーエムベーハーＡｘｏｖａｎｔ Ｓｃｉｅｎｃｅｓ Ｇｍｂｈ レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体
BR112018000728A2 (pt) 2015-07-15 2018-09-04 Axovant Sciences Gmbh resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1029479C (zh) * 1989-11-08 1995-08-09 山之内制药株式会社 新型苯并噁嗪衍生物的制备方法
US5492914A (en) * 1994-07-28 1996-02-20 Syntex (U.S.A.) Inc. 2-(1-azabicyclo[2.2.2]oct-3 s-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[DE]is[2.2.2]oct-3's-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1h-benz [DE]isoquinolin-1-one and individual stereoisomers thereof
GB9507203D0 (en) 1995-04-07 1995-05-31 Smithkline Beecham Plc Novel compounds
DZ2376A1 (fr) * 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
HUP0001123A3 (en) 1997-04-18 2002-04-29 Smithkline Beecham Plc Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity
NZ501258A (en) 1997-07-11 2001-07-27 Smithkline Beecham P Benzenesulfonamide compounds with 5HT6 receptor antagonist activity for treating anxiety and/or depression
NZ502252A (en) * 1997-07-25 2001-09-28 H Indole and 2,3-dihydroindole derivatives useful for inhibiting serotonin reuptake and antagonism of 5-HT1a receptors
GB9801392D0 (en) 1998-01-22 1998-03-18 Smithkline Beecham Plc Novel compounds
EP1089997A1 (en) * 1998-06-19 2001-04-11 H.Lundbeck A/S 4,5,6 and 7-indole and indoline derivatives, their preparation and use
GB9818916D0 (en) * 1998-08-28 1998-10-21 Smithkline Beecham Plc Use
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US7067513B1 (en) * 1999-08-23 2006-06-27 Solvay Pharmaceuticals B.V. Phenylpiperazines
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
AU2001236606A1 (en) 2000-02-01 2001-08-14 Cor Therapeutics, Inc. 3,4-dihydro-2h-benzo(1,4)oxazine inhibitors of factor xa
CN100429206C (zh) * 2002-05-13 2008-10-29 弗·哈夫曼-拉罗切有限公司 作为5－ht6调节剂的苯并嗪衍生物及其用途

Also Published As

Publication number Publication date
ECSP045420A (es) 2005-01-03
EP1506179B1 (en) 2006-01-25
JP4307377B2 (ja) 2009-08-05
RS97004A (en) 2006-10-27
TNSN04225A1 (fr) 2007-03-12
BR0310032A (pt) 2005-02-15
TWI258479B (en) 2006-07-21
MA27118A1 (fr) 2004-12-20
GT200300108A (es) 2004-03-15
TW200400188A (en) 2004-01-01
NO329380B1 (no) 2010-10-04
JO2413B1 (en) 2007-11-11
KR20040106538A (ko) 2004-12-17
ZA200408783B (en) 2005-12-28
CA2485136A1 (en) 2003-11-20
AU2003233231A1 (en) 2003-11-11
UY27803A1 (es) 2003-11-28
BRPI0310032B8 (pt) 2021-05-25
DE60303376D1 (de) 2006-04-13
ES2256744T3 (es) 2006-07-16
PE20040757A1 (es) 2004-11-06
CN100429206C (zh) 2008-10-29
UA76877C2 (ru) 2006-09-15
DE60303376T2 (de) 2006-11-16
AR039988A1 (es) 2005-03-09
DK1506179T3 (da) 2006-06-06
EG25683A (en) 2012-05-16
HRP20041030A2 (en) 2005-06-30
IL164928A0 (en) 2005-12-18
NZ536230A (en) 2007-05-31
US8377931B2 (en) 2013-02-19
CN1653054A (zh) 2005-08-10
AU2003233231B2 (en) 2009-02-26
PT1506179E (pt) 2006-06-30
US6867204B2 (en) 2005-03-15
JP2005530774A (ja) 2005-10-13
CA2485136C (en) 2011-12-20
BRPI0310032B1 (pt) 2019-01-08
MXPA04011254A (es) 2005-01-25
RS51042B (sr) 2010-10-31
US20050130962A1 (en) 2005-06-16
HRP20041030B1 (hr) 2013-03-31
EP1506179A1 (en) 2005-02-16
US20130123251A1 (en) 2013-05-16
US20030232825A1 (en) 2003-12-18
PL211057B1 (pl) 2012-04-30
HK1080846A1 (en) 2006-05-04
PA8573501A1 (es) 2003-12-10
US20090325950A1 (en) 2009-12-31
MY139612A (en) 2009-10-30
NO20044665L (no) 2004-12-03
WO2003095434A1 (en) 2003-11-20
KR100636475B1 (ko) 2006-10-18
PL374019A1 (en) 2005-09-19
ATE316523T1 (de) 2006-02-15
EA009982B1 (ru) 2008-04-28

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