CN1909909B - 作为5-羟色胺受体(5-ht)调节剂用于治疗中枢神经系统疾病的1-苄基-5-哌嗪-1-基-3，4二氢-1h-喹唑啉-2-酮衍生物和各个1h-苯并(1，2，6)噻二嗪-2，2-二氧化物和1，4-二氢-苯并(d)(1，3)*嗪-2-酮衍生物 - Google Patents

作为5-羟色胺受体(5-ht)调节剂用于治疗中枢神经系统疾病的1-苄基-5-哌嗪-1-基-3，4二氢-1h-喹唑啉-2-酮衍生物和各个1h-苯并(1，2，6)噻二嗪-2，2-二氧化物和1，4-二氢-苯并(d)(1，3)*嗪-2-酮衍生物 Download PDF

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CN1909909B
CN1909909B CN2005800026123A CN200580002612A CN1909909B CN 1909909 B CN1909909 B CN 1909909B CN 2005800026123 A CN2005800026123 A CN 2005800026123A CN 200580002612 A CN200580002612 A CN 200580002612A CN 1909909 B CN1909909 B CN 1909909B
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dihydro
piperazine
benzyl
base
chemical compound
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Expired - Fee Related
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Chinese (zh)
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CN1909909A (zh
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M·隋
S-H·赵
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F Hoffmann La Roche AG
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/20—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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • 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
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (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- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2005800026123A 2004-01-16 2005-01-07 作为5-羟色胺受体(5-ht)调节剂用于治疗中枢神经系统疾病的1-苄基-5-哌嗪-1-基-3，4二氢-1h-喹唑啉-2-酮衍生物和各个1h-苯并(1，2，6)噻二嗪-2，2-二氧化物和1，4-二氢-苯并(d)(1，3)*嗪-2-酮衍生物 Expired - Fee Related CN1909909B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US53708004P 2004-01-16 2004-01-16
US60/537,080 2004-01-16
PCT/EP2005/000095 WO2005067933A1 (en) 2004-01-16 2005-01-07 1-benzyl-5-piperazin-1-yl-3,4 dihydro-1h-quinazolin-2-one derivatives and the respective 1h-benzo(1,2,6)thiadiazine-2,2-dioxide and 1,4-dihydro-benzo(d) (1,3)oxazin-2-one derivatives as modulators of the 5-hydroxytryptamine receptor (5-ht) for the treatment of diseases of the central nervous system

Publications (2)

Publication Number Publication Date
CN1909909A CN1909909A (zh) 2007-02-07
CN1909909B true CN1909909B (zh) 2010-12-15

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CN2005800026123A Expired - Fee Related CN1909909B (zh) 2004-01-16 2005-01-07 作为5-羟色胺受体(5-ht)调节剂用于治疗中枢神经系统疾病的1-苄基-5-哌嗪-1-基-3，4二氢-1h-喹唑啉-2-酮衍生物和各个1h-苯并(1，2，6)噻二嗪-2，2-二氧化物和1，4-二氢-苯并(d)(1，3)*嗪-2-酮衍生物

Country Status (19)

Country Link
US (2) US7196087B2 (https=)
EP (1) EP1708713B1 (https=)
JP (1) JP4533391B2 (https=)
KR (1) KR100843053B1 (https=)
CN (1) CN1909909B (https=)
AR (1) AR047958A1 (https=)
AT (1) ATE388712T1 (https=)
AU (1) AU2005205016B2 (https=)
BR (1) BRPI0506909A (https=)
CA (1) CA2552681A1 (https=)
CO (1) CO5700763A2 (https=)
DE (1) DE602005005298T2 (https=)
ES (1) ES2302174T3 (https=)
IL (1) IL176631A0 (https=)
NO (1) NO20062791L (https=)
RU (1) RU2006129464A (https=)
TW (1) TW200530222A (https=)
WO (1) WO2005067933A1 (https=)
ZA (1) ZA200605434B (https=)

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CN102114244A (zh) * 2004-09-30 2011-07-06 弗·哈夫曼-拉罗切有限公司 治疗认知障碍的组合物和方法
US7713954B2 (en) * 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
AU2005316739A1 (en) * 2004-12-13 2006-06-22 Galileo Pharmaceuticals, Inc. Spiro derivatives as lipoxygenase inhibitors
BRPI0613430A2 (pt) * 2005-07-13 2011-01-11 Hoffmann La Roche compostos derivados de benzimidazol, uso dos mesmos, método para a preparação destes e composição farmacêutica
KR100817538B1 (ko) * 2006-07-05 2008-03-27 한국화학연구원 신규 치환된―１ｈ―퀴나졸린―２,４―디온 유도체, 이의제조방법 및 이를 함유하는 약학적 조성물
CN101600698B (zh) * 2006-09-11 2012-01-11 欧加农股份有限公司;药典有限责任公司 喹唑啉酮和异喹啉酮乙酰胺衍生物
WO2008073958A2 (en) 2006-12-12 2008-06-19 Wyeth Substituted benzothiadiazinedioxide derivatives and methods of their use
MX2010014394A (es) * 2008-06-20 2011-05-19 Rottapharm Spa Derivados de 6-1h-imidazo-quinazolina y quinolinas, nuevos inhibidores de monoamina oxidasa y ligandos del receptor de imidazolina.
EP2328881A1 (en) * 2008-09-08 2011-06-08 F. Hoffmann-La Roche AG 5-substituted benzoxazines
US20110288086A1 (en) 2010-05-21 2011-11-24 Jianqi Li Polycyclic quinazolines, preparation thereof, and use thereof
IL309982A (en) * 2016-11-15 2024-03-01 Univ Temple New modulators of 5-hydroxytryptamine receptor 7 and a method of using them
MX2021013135A (es) 2019-04-29 2021-11-25 Solent Therapeutics Llc Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4] tiadiazina como inhibidores de mrgx2.
JP7696354B2 (ja) * 2019-10-21 2025-06-20 アライリオン インコーポレイテッド 睡眠障害の治療のためのＨ１および５－ＨＴ２Ａ受容体調節物質としての３－（４－（１１Ｈ－ジベンゾ［ｂ，ｅ］［１，４］アゼピン－６－イル）ピペラジン－１－イル）－プロパン酸誘導体および３－（４－（ジベンゾ［ｂ，ｆ］［１，４］オキサゼピン／チアゼピン／ジアゼピン－１１－イル）ピペラジン－１－イル）－プロパン酸誘導体

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CN1042914A (zh) * 1988-11-22 1990-06-13 田辺制药株式会社 喹唑啉酮衍生物的制备方法
CN1015459B (zh) * 1985-06-06 1992-02-12 田边制药株式会社 喹唑啉酮化合物的制备方法
WO1999037643A1 (en) * 1998-01-26 1999-07-29 Yamanouchi Pharmaceutical Co., Ltd. Novel benzene-fused heterocyclic derivatives or salts thereof
WO2001032626A1 (en) * 1999-11-05 2001-05-10 Smithkline Beecham P.L.C. Isoquinoline and quinazoline derivatives having a combined 5ht1a, 5ht1b and 5ht1d receptor activity
WO2002102774A1 (en) * 2001-06-15 2002-12-27 F. Hoffmann-La Roche Ag 4-piperazinylindole derivatives with 5-ht6 receptor affinity
WO2003068772A1 (en) * 2002-02-18 2003-08-21 Glaxo Group Limited Heterocyclic compounds possessing affinity at 5ht1-type receptors and use thereof in therapy
WO2003095434A1 (en) * 2002-05-13 2003-11-20 F. Hoffmann-La Roche Ag Benzoxazine derivatives as 5-ht6 modulators and uses thereof

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JPS5271483A (en) 1975-12-11 1977-06-14 Sumitomo Chem Co Ltd Synthesis of 2(1h)-quinazolinone derivatives
WO1998018781A2 (en) 1996-10-28 1998-05-07 Versicor, Inc. Fused 2,4-pyrimidinedione combinatorial libraries, their preparation and the use of fused 2,4-pyrimidinediones derivatives as antimicrobial agents
AU6423298A (en) 1997-03-26 1998-10-20 Sumitomo Pharmaceuticals Company, Limited 4-arylmethylene-1,4-dihydro-2h-azine derivatives
DK1028950T3 (da) 1997-10-28 2003-09-01 Warner Lambert Co 7-substituerede quinazolin-2,4-dioner nyttige som antibakterielle midler
AU1626001A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)-quinazolin-2-ones and their use as csbp/p38 kinase inhibitors
WO2001044228A2 (fr) 1999-12-14 2001-06-21 Sanofi-Synthelabo Derives de quinazolinedione et phtalimide, leurs preparations et leurs applications en therapeutique
JP2004521892A (ja) * 2000-12-20 2004-07-22 メルク　エンド　カムパニー　インコーポレーテッド （ハロ−ベンゾカルボニル）複素環縮合フェニル系ｐ３８キナーゼ阻害剤
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CN1015459B (zh) * 1985-06-06 1992-02-12 田边制药株式会社 喹唑啉酮化合物的制备方法
CN1042914A (zh) * 1988-11-22 1990-06-13 田辺制药株式会社 喹唑啉酮衍生物的制备方法
WO1999037643A1 (en) * 1998-01-26 1999-07-29 Yamanouchi Pharmaceutical Co., Ltd. Novel benzene-fused heterocyclic derivatives or salts thereof
WO2001032626A1 (en) * 1999-11-05 2001-05-10 Smithkline Beecham P.L.C. Isoquinoline and quinazoline derivatives having a combined 5ht1a, 5ht1b and 5ht1d receptor activity
WO2002102774A1 (en) * 2001-06-15 2002-12-27 F. Hoffmann-La Roche Ag 4-piperazinylindole derivatives with 5-ht6 receptor affinity
WO2003068772A1 (en) * 2002-02-18 2003-08-21 Glaxo Group Limited Heterocyclic compounds possessing affinity at 5ht1-type receptors and use thereof in therapy
WO2003095434A1 (en) * 2002-05-13 2003-11-20 F. Hoffmann-La Roche Ag Benzoxazine derivatives as 5-ht6 modulators and uses thereof

Also Published As

Publication number Publication date
WO2005067933A1 (en) 2005-07-28
TW200530222A (en) 2005-09-16
US7365063B2 (en) 2008-04-29
NO20062791L (no) 2006-08-01
JP2007517826A (ja) 2007-07-05
KR100843053B1 (ko) 2008-07-01
CA2552681A1 (en) 2005-07-28
EP1708713A1 (en) 2006-10-11
ATE388712T1 (de) 2008-03-15
JP4533391B2 (ja) 2010-09-01
DE602005005298T2 (de) 2009-03-12
AR047958A1 (es) 2006-03-15
US20050165001A1 (en) 2005-07-28
AU2005205016A1 (en) 2005-07-28
CO5700763A2 (es) 2006-11-30
ES2302174T3 (es) 2008-07-01
RU2006129464A (ru) 2008-02-27
KR20060126720A (ko) 2006-12-08
CN1909909A (zh) 2007-02-07
ZA200605434B (en) 2008-02-27
IL176631A0 (en) 2006-10-31
EP1708713B1 (en) 2008-03-12
US20070149510A1 (en) 2007-06-28
AU2005205016B2 (en) 2010-07-15
BRPI0506909A (pt) 2007-05-29
US7196087B2 (en) 2007-03-27
DE602005005298D1 (de) 2008-04-24

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