TWI228127B - Substituted imidazoles as histamine H3 or dual histamine H1 and H3 antagonists - Google Patents

Substituted imidazoles as histamine H3 or dual histamine H1 and H3 antagonists Download PDF

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Publication number
TWI228127B
TWI228127B TW090123022A TW90123022A TWI228127B TW I228127 B TWI228127 B TW I228127B TW 090123022 A TW090123022 A TW 090123022A TW 90123022 A TW90123022 A TW 90123022A TW I228127 B TWI228127 B TW I228127B
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Taiwan
Prior art keywords
compound
patent application
cns
scope
national standard
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TW090123022A
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English (en)
Chinese (zh)
Inventor
Neng-Yang Shih
Daniel M Solomon
John J Piwinski
Robert G Aslanian
Stuart B Rosenblum
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Schering Corp
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Publication of TWI228127B publication Critical patent/TWI228127B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/64Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW090123022A 2000-09-20 2001-09-19 Substituted imidazoles as histamine H3 or dual histamine H1 and H3 antagonists TWI228127B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US23403900P 2000-09-20 2000-09-20

Publications (1)

Publication Number Publication Date
TWI228127B true TWI228127B (en) 2005-02-21

Family

ID=22879625

Family Applications (1)

Application Number Title Priority Date Filing Date
TW090123022A TWI228127B (en) 2000-09-20 2001-09-19 Substituted imidazoles as histamine H3 or dual histamine H1 and H3 antagonists

Country Status (14)

Country Link
US (1) US6762186B2 (https=)
EP (1) EP1318996B1 (https=)
JP (1) JP2004514709A (https=)
CN (1) CN1461304A (https=)
AR (1) AR032894A1 (https=)
AT (1) ATE283853T1 (https=)
AU (1) AU2002241459A1 (https=)
CA (1) CA2422729A1 (https=)
DE (1) DE60107586T2 (https=)
ES (1) ES2233708T3 (https=)
HK (1) HK1052182B (https=)
MX (1) MXPA03002446A (https=)
TW (1) TWI228127B (https=)
WO (1) WO2002044141A2 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003268117A1 (en) * 2002-09-18 2004-04-08 Eli Lilly And Company Histamine h3 receptor antagonists, preparaton and therapeutic uses
US8063650B2 (en) 2002-11-27 2011-11-22 Rambus Inc. Testing fuse configurations in semiconductor devices
WO2004066960A2 (en) * 2003-01-28 2004-08-12 Schering Corporation Combination of h1, h3 and h4 receptor antagonists for treatment of allergic and non-allergic pulmonary inflammation, congestion and allergic rhinitis
EP1667955A2 (en) 2003-07-28 2006-06-14 SmithKline Beecham Corporation Cycloalkylidene compounds as modulators of the estrogen receptor
TWI290140B (en) * 2003-08-25 2007-11-21 Schering Corp 2-Substituted benzimidazole derivatives as selective melanin concentrating hormone receptor antagonists for thr treatment of obesity and related disorders
US20080306087A1 (en) * 2005-08-08 2008-12-11 Astrazeneca Ab Therapeutic Agents
US20100029681A1 (en) * 2006-05-26 2010-02-04 Hassan Pajouhesh Heterocyclic compounds as calcium channel blockers
JP5208962B2 (ja) 2006-12-22 2013-06-12 アベキサ・リミテッド 二環式ピリミジノンおよびその使用
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
CN110878069A (zh) * 2019-12-09 2020-03-13 南京杰运医药科技有限公司 一种4-吗琳基-2-乙基哌嗪的制备方法

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2586562B1 (fr) 1985-09-02 1989-03-10 Inst Nat Sante Rech Med Composition pharmaceutique contenant de l'a-methylhistamine
US4829065A (en) * 1987-04-24 1989-05-09 Syntex Pharmaceuticals, Ltd. Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives
GB8916947D0 (en) 1989-07-25 1989-09-13 Smith Kline French Lab Medicaments
DK0437645T3 (da) * 1990-01-15 1995-05-01 Heumann Pharma Gmbh & Co Imidazolylpropylguanidinderivat, fremgangsmåde til fremstilling deraf og lægemidler indeholdende denne forbindelse
DE59006842D1 (de) 1990-03-30 1994-09-22 Heumann Pharma Gmbh & Co Verwendung von Guanidinderivaten zur Herstellung eines Arzneimittels mit NPY-antagonistischer Wirkung.
FR2665160A1 (fr) * 1990-07-26 1992-01-31 Esteve Labor Dr Nouveaux derives de 1-diphenylmethylpiperazine, leur preparation et leur application en tant que medicaments.
GB9115740D0 (en) 1991-07-20 1991-09-04 Smithkline Beecham Plc Medicaments
DK0618905T3 (da) 1991-12-18 1995-12-04 Schering Corp Imidazolyl-alkyl-piperazin- og -diazepinderivater som histamin H3-agonister/antagonister
US5352707A (en) 1992-03-26 1994-10-04 Harbor Branch Oceanographic Institution, Inc. Method for treating airway congestion
HU213104B (en) * 1992-06-17 1997-02-28 Richter Gedeon Vegyeszet Process for producing 4-methyl-2-imidazolinone derivatives and pharmaceutical compositions containing them
JPH09505298A (ja) 1993-11-15 1997-05-27 シェーリング コーポレイション H▲下3▼‐レセプターアンタゴニストとしてのフェニル‐アルキルイミダゾール
FR2732017B1 (fr) 1995-03-21 2000-09-22 Inst Nat Sante Rech Med Nouveaux derives de l'imidazole antagonistes et/ou agonistes du recepteur h3 de l'histamine, leur preparation et leurs applications therapeutiques
EP1019050B1 (en) 1997-06-24 2002-03-20 Novo Nordisk A/S Use of somatostatin agonists and antagonists for treating diseases related to the eye
US5869479A (en) 1997-08-14 1999-02-09 Schering Corporation Treatment of upper airway allergic responses
US6133291A (en) * 1998-10-16 2000-10-17 Schering Corporation N-(imidazolylalkyl)substituted cyclic amines as histamine-H3 agonists or antagonists

Also Published As

Publication number Publication date
EP1318996B1 (en) 2004-12-01
DE60107586T2 (de) 2005-10-06
AR032894A1 (es) 2003-12-03
ATE283853T1 (de) 2004-12-15
US6762186B2 (en) 2004-07-13
HK1052182A1 (en) 2003-09-05
AU2002241459A1 (en) 2002-06-11
HK1052182B (en) 2005-04-01
EP1318996A2 (en) 2003-06-18
WO2002044141A3 (en) 2002-11-07
CN1461304A (zh) 2003-12-10
DE60107586D1 (de) 2005-01-05
ES2233708T3 (es) 2005-06-16
WO2002044141A2 (en) 2002-06-06
CA2422729A1 (en) 2002-06-06
MXPA03002446A (es) 2003-06-19
US20020082278A1 (en) 2002-06-27
JP2004514709A (ja) 2004-05-20

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