AR013153A1 - Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n. - Google Patents

Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n.

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Publication number
AR013153A1
AR013153A1 ARP980103175A ARP980103175A AR013153A1 AR 013153 A1 AR013153 A1 AR 013153A1 AR P980103175 A ARP980103175 A AR P980103175A AR P980103175 A ARP980103175 A AR P980103175A AR 013153 A1 AR013153 A1 AR 013153A1
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AR
Argentina
Prior art keywords
alkyl
derivatives
ring
alkoxy
substituted
Prior art date
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ARP980103175A
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English (en)
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Astrazeneca Ab
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Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR013153A1 publication Critical patent/AR013153A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de 2-arildihidropirimidina, que comprende la formula I incluyendo su forma tautomérica 3,4-dihidropirimidina en la cual: R1 representa un anillomonocíclico aromático que optativamente incorpora una o tres heteroátomos que pueden ser iguales o diferentes y que son elegidos entre N, O o S, anillo quepuede ser optativamente sustituido con halogeno, alquilo C1 a 6, alcoxi C1 a 6 trifluorometilo; R2 represena alquilo C1 a 6 o alquilo C2 a 6, optativamenteincluyendo O, o bien S, y que está sustituido con un anillo de fenilo o heteroarilo monocíclico, anillo aromático que está sustituido con uno o mássustituyentes seleccionados entre halogeno, alquilo C1 a 6 o alcoxi C1 a 6; R3 representa un anillo monocíclico o bicíclico optativamente incorpora un átomoseleccionado entre N, O o S, optativamente sustituido con uno o más sustituyentes independientemenete seleccionados entre, alquilo C1 a 6, alcoxiC1 a 6, ciano, trifluorometilo, amino, hidroxi, nitro o carbometoxi; R4 y R5 representan independientemente hidrogeno, alquilo C1 a 6 o bencilo; o el grupoNR4R5 junto representa piperidinilo, morfolinilo, 3,4-deshidropiperidinilo, tiomorfolinilo, perhidroazepinilo, pirrolidinilo, piperazinilo o piperaziniloque también esta sustituido en N-4 por alquilo C1 a 6; R6 y R7 representan independientemente alquilo C1 a 6 o cicloalquilo C3 a 6, o bencilo,optativamente sustituido en el anillo fenilo por alquilo C1 a 6 alcoxi C1 a 6 o halogeno; X representaO, S o NR6; R8 representa hidrogeno o alquilo C1 a 6; yn representa un entero de 2 a 4; y los isomeros opticos y racematos de los mismos, así como las sales farmacéuticamente aceptables; de los mismos,procesos para su preparacion, composicionesque los contienen y su uso como antagonistas de los canales de calcio neuronales tipo N que sirven para el
ARP980103175A 1997-07-02 1998-06-30 Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n. AR013153A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE9702564A SE9702564D0 (sv) 1997-07-02 1997-07-02 New compounds

Publications (1)

Publication Number Publication Date
AR013153A1 true AR013153A1 (es) 2000-12-13

Family

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Family Applications (1)

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ARP980103175A AR013153A1 (es) 1997-07-02 1998-06-30 Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n.

Country Status (9)

Country Link
US (1) US6218538B1 (es)
EP (1) EP0993450A1 (es)
JP (1) JP2002508780A (es)
AR (1) AR013153A1 (es)
AU (1) AU8249998A (es)
CA (1) CA2294746A1 (es)
SE (1) SE9702564D0 (es)
WO (1) WO1999001438A1 (es)
ZA (1) ZA985323B (es)

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DE19817265A1 (de) * 1998-04-18 1999-10-21 Bayer Ag Verwendung von Dihydropyrimidinen als Arzneimittel und neue Stoffe
DE19817264A1 (de) * 1998-04-18 1999-10-21 Bayer Ag Neue Dihydropyrimidine
US20040259866A1 (en) * 1998-06-30 2004-12-23 Snutch Terrance P. Calcium channel blockers comprising two benzhydril moieties
AU4289100A (en) * 1999-03-25 2000-10-16 Bayer Aktiengesellschaft Dihydropyrimidines and their use in the treatment of hepatitis
AU5568400A (en) 1999-06-23 2001-01-09 Ajinomoto Co., Inc. Novel dihydropyrimidine derivatives
DE10012824A1 (de) * 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10012823A1 (de) * 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013126A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
AU2001284504A1 (en) * 2000-09-14 2002-03-26 Ajinomoto Co., Inc. Novel pyrimidine derivative and novel pyridine derivative
US7314880B2 (en) * 2003-01-02 2008-01-01 Mount Cook Biosciences, Inc. Cardioprotective delta opioid receptor agonists and methods of using same
TW200418814A (en) * 2003-01-02 2004-10-01 Ardent Pharmaceuticals Inc Cardioprotective delta opioid receptor agonists and methods of using same
WO2006105670A1 (en) * 2005-04-08 2006-10-12 Neuromed Pharmaceuticals Ltd. Combination therapy comprising an n-type calcium channel blocker for the alleviation of pain
EP2019676A2 (en) * 2006-05-11 2009-02-04 Neuromed Pharmaceuticals, Ltd. Method for increasing the bioavailability of benzhydryl piperazine containing compounds
CN101225084A (zh) * 2007-01-16 2008-07-23 北京摩力克科技有限公司 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
MX2013010306A (es) 2011-03-08 2013-12-09 Zalicus Pharmaceuticals Ltd Formulaciones de dispersion solida y metodos de uso de las mismas.
US8409560B2 (en) 2011-03-08 2013-04-02 Zalicus Pharmaceuticals Ltd. Solid dispersion formulations and methods of use thereof
US20130267517A1 (en) 2012-03-31 2013-10-10 Hoffmann-La Roche Inc. Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
RU2014142598A (ru) * 2012-03-31 2016-05-27 Ф. Хоффманн-Ля Рош Аг Новые 4-метилдигидропиримидины для лечения и профилактики инфекции вируса гепатита в
JP6263533B2 (ja) 2012-08-24 2018-01-17 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． ジヒドロピリミジン化合物及び医薬におけるその適用
JP6113285B2 (ja) * 2012-09-10 2017-04-12 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂ型肝炎ウイルス感染症の治療及び予防用の６−アミノ酸ヘテロアリールジヒドロピリミジン
CA2920415A1 (en) 2013-11-19 2015-05-28 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and their application in pharmaceuticals
CN104672225B (zh) 2013-11-27 2019-02-12 广东东阳光药业有限公司 二氢嘧啶衍生物的制备方法及其中间体
KR20160133563A (ko) 2014-03-28 2016-11-22 선샤인 레이크 파르마 컴퍼니 리미티드 다이하이드로피리미딘 화합물 및 이의 약제학적 용도
TW201629054A (zh) 2015-02-07 2016-08-16 廣東東陽光藥業有限公司 二氫嘧啶衍生物的複合物及其在藥物中的應用

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DE3234684A1 (de) 1982-09-18 1984-03-22 Bayer Ag, 5090 Leverkusen Neue dihydropyrimidine, verfahren zu ihrer herstellung sowie ihre verwendung in arzneimitteln
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DE69500377T2 (de) 1994-08-19 1997-10-09 Mitsui Toatsu Chemicals Pyrimidin-Dion-Derivate und diese enthaltende antiarrhythmische Zusammensetzungen

Also Published As

Publication number Publication date
ZA985323B (en) 1999-01-11
CA2294746A1 (en) 1999-01-14
AU8249998A (en) 1999-01-25
SE9702564D0 (sv) 1997-07-02
EP0993450A1 (en) 2000-04-19
US6218538B1 (en) 2001-04-17
JP2002508780A (ja) 2002-03-19
WO1999001438A1 (en) 1999-01-14

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