EA015569B1 - Бензотиазолы, обладающие антагонистической активностью по отношению к h3-рецептору гистамина, и фармацевтические композиции, включающие эти соединения - Google Patents

Бензотиазолы, обладающие антагонистической активностью по отношению к h3-рецептору гистамина, и фармацевтические композиции, включающие эти соединения Download PDF

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Publication number
EA015569B1
EA015569B1 EA200870376A EA200870376A EA015569B1 EA 015569 B1 EA015569 B1 EA 015569B1 EA 200870376 A EA200870376 A EA 200870376A EA 200870376 A EA200870376 A EA 200870376A EA 015569 B1 EA015569 B1 EA 015569B1
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EA
Eurasian Patent Office
Prior art keywords
mmol
benzothiazole
mixture
isopropylpiperazin
cyclopropylpiperazin
Prior art date
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EA200870376A
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English (en)
Russian (ru)
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EA200870376A1 (ru
Inventor
Флоренсио Сарагоса Дервальд
Кнуд Эрик Андерсен
Рольф Хольвег
Инге Тогер Кристенсен
Яне Мари Лундбекк
Original Assignee
ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи
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Publication of EA200870376A1 publication Critical patent/EA200870376A1/ru
Publication of EA015569B1 publication Critical patent/EA015569B1/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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/14—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 three or more hetero rings

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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Nutrition Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
EA200870376A 2006-03-28 2007-03-22 Бензотиазолы, обладающие антагонистической активностью по отношению к h3-рецептору гистамина, и фармацевтические композиции, включающие эти соединения EA015569B1 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP06111820 2006-03-28
US78747806P 2006-03-30 2006-03-30
EP06112425 2006-04-10
US79428806P 2006-04-21 2006-04-21
EP06026875 2006-12-24
US90350307P 2007-02-26 2007-02-26
PCT/EP2007/052751 WO2007110364A1 (en) 2006-03-28 2007-03-22 Benzothiazoles having histamine h3 receptor activity

Publications (2)

Publication Number Publication Date
EA200870376A1 EA200870376A1 (ru) 2009-04-28
EA015569B1 true EA015569B1 (ru) 2011-10-31

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ID=43124961

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Application Number Title Priority Date Filing Date
EA200870376A EA015569B1 (ru) 2006-03-28 2007-03-22 Бензотиазолы, обладающие антагонистической активностью по отношению к h3-рецептору гистамина, и фармацевтические композиции, включающие эти соединения

Country Status (15)

Country Link
US (2) US8394842B2 (enExample)
EP (1) EP1999120B1 (enExample)
JP (1) JP2009531376A (enExample)
KR (1) KR101280333B1 (enExample)
CN (1) CN101410385B (enExample)
AU (1) AU2007229492B2 (enExample)
CA (1) CA2645581A1 (enExample)
EA (1) EA015569B1 (enExample)
ES (1) ES2388681T3 (enExample)
IL (1) IL193441A0 (enExample)
MX (1) MX2008011123A (enExample)
NZ (1) NZ570524A (enExample)
SG (1) SG170785A1 (enExample)
WO (1) WO2007110364A1 (enExample)
ZA (1) ZA200806985B (enExample)

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* Cited by examiner, † Cited by third party
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US20030236259A1 (en) * 2002-02-05 2003-12-25 Rolf Hohlweg Novel aryl- and heteroarylpiperazines
EP1902028A2 (en) * 2005-07-04 2008-03-26 Novo Nordisk A/S Histamine h3 receptor antagonists
JP2009537596A (ja) * 2006-05-23 2009-10-29 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー ６−（４−シクロプロピルピペリジン−１−イル）−２’−メチル−［３，４’］−ビピリジン及びその医薬としての使用
ATE538116T1 (de) * 2006-05-29 2012-01-15 High Point Pharmaceuticals Llc 3-(1,3-benyodioxol-5-yl)-6- (4- cyclopropylpiperazin-1-yl)-pyridazin, dessen salze und solvate und dessen verwendung als histamin-h3-rezeptorantagonist
EP2014656A3 (en) * 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8153813B2 (en) * 2007-12-20 2012-04-10 Abbott Laboratories Benzothiazole and benzooxazole derivatives and methods of use
WO2010109084A2 (fr) * 2009-03-24 2010-09-30 Sanofi-Aventis DERIVES D'AZACARBOLINES 9H-PYRROLO[2,3-b:5,4-c']DIPYRIDINE, LEUR PREPARATION ET LEUR UTILISATION THERAPEUTIQUE
US8481547B2 (en) * 2009-12-18 2013-07-09 Janssen Pharmaceutica Nv Substituted benzothiazole and benzoxazole derivatives useful as inhibitors of DPP-1
EA022746B1 (ru) * 2010-09-02 2016-02-29 Сувен Лайф Сайенсиз Лимитед Гетероциклические соединения в качестве лигандов гистаминовых hрецепторов
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
KR101913619B1 (ko) * 2011-06-09 2018-12-28 리젠 파마슈티컬스 소시에떼 아노님 Gpr-119의 조절제로서의 신규한 화합물
ES2586527T3 (es) * 2011-10-14 2016-10-17 Ambit Biosciences Corporation Compuestos heterocíclicos y uso de los mismos como moduladores del receptor de tirosina quinasas de tipo III
HK1220446A1 (en) * 2013-06-10 2017-05-05 Astellas Pharma Inc. Bicyclic nitrogen-containing aromatic heterocyclic amide compound
US10584118B2 (en) 2015-06-22 2020-03-10 Actelion Pharmaceuticals Ltd NADPH oxidase 4 inhibitors
CN116199700A (zh) * 2016-03-11 2023-06-02 Ac免疫有限公司 用于诊断和治疗的双环化合物
CN106588808A (zh) * 2017-02-26 2017-04-26 长沙深橙生物科技有限公司 一种苯并[d]恶唑衍生物的制备方法
JP7376471B2 (ja) 2017-06-05 2023-11-08 ピーティーシー セラピューティクス， インコーポレイテッド ハンチントン病を処置するための化合物
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