EA201170528A1 - Производные 1-бутил-2-гидроксиаралкилпиперазина и их применения в качестве лекарственного средства против депрессии - Google Patents

Производные 1-бутил-2-гидроксиаралкилпиперазина и их применения в качестве лекарственного средства против депрессии

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Publication number
EA201170528A1
EA201170528A1 EA201170528A EA201170528A EA201170528A1 EA 201170528 A1 EA201170528 A1 EA 201170528A1 EA 201170528 A EA201170528 A EA 201170528A EA 201170528 A EA201170528 A EA 201170528A EA 201170528 A1 EA201170528 A1 EA 201170528A1
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EA
Eurasian Patent Office
Prior art keywords
derivatives
butyl
effect
aralkylpiperazine
depression
Prior art date
Application number
EA201170528A
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English (en)
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EA020716B1 (ru
Inventor
Цзяньци Ли
На Лв
Хуа Цзинь
Чжицзе Вэн
Юнюн Чжен
Original Assignee
СиЭсПиСи ЧЖУНЦИ ФАРМАСЬЮТИКАЛ ТЕКНОЛОДЖИ (ШИЦЗЯЧЖУАН) КО., ЛТД.
Шанхай Инститьют Оф Фармасьютикал Индастри
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Application filed by СиЭсПиСи ЧЖУНЦИ ФАРМАСЬЮТИКАЛ ТЕКНОЛОДЖИ (ШИЦЗЯЧЖУАН) КО., ЛТД., Шанхай Инститьют Оф Фармасьютикал Индастри filed Critical СиЭсПиСи ЧЖУНЦИ ФАРМАСЬЮТИКАЛ ТЕКНОЛОДЖИ (ШИЦЗЯЧЖУАН) КО., ЛТД.
Publication of EA201170528A1 publication Critical patent/EA201170528A1/ru
Publication of EA020716B1 publication Critical patent/EA020716B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Изобретение раскрывает производные 1-бутил-2-гидроксиларалкилпиперазина и их применение в качестве антидепрессантов. Производные настоящего изобретения обладают тройным ингибирующим эффектом на обратный захват 5-НТ, NA и DA и могут вводиться пациентам, нуждающимся в этом, в форме композиции путем перорального введения, инъекции и т.п. По сравнению с имеющими в настоящее время клиническое применение антидепрессантами двойного назначения (такими как венлафаксин) указанные производные могут иметь более сильный эффект против депрессии, более широкие показания, более быстрое наступление эффекта и более низкие нейротоксичность и побочные реакции; и указанные производные имеют более высокую активность против депрессии, более низкую токсичность, более высокую биодоступность, более длительный период полувыведения и лучшие характеристики для лекарственного средства по сравнению с производными арилалканолпиперазина и их оптическими изомерами, раскрытыми в предшествующем уровне техники. Производное 1-бутил-2-гидроксиларалкилпиперазина представляет собой свободную щелочную форму или ее соль соединения формулы
EA201170528A 2008-10-07 2009-09-29 Производные 1-бутил-2-гидроксиаралкилпиперазина и их применение в качестве лекарственного средства против депрессии EA020716B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2008100438218A CN101712658B (zh) 2008-10-07 2008-10-07 1-丁基-2-羟基芳烷哌嗪衍生物及作为抗抑郁剂应用
PCT/CN2009/074314 WO2010040315A1 (zh) 2008-10-07 2009-09-29 1-丁基-2-羟基芳烷哌嗪衍生物及作为抗抑郁剂的应用

Publications (2)

Publication Number Publication Date
EA201170528A1 true EA201170528A1 (ru) 2012-03-30
EA020716B1 EA020716B1 (ru) 2015-01-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170528A EA020716B1 (ru) 2008-10-07 2009-09-29 Производные 1-бутил-2-гидроксиаралкилпиперазина и их применение в качестве лекарственного средства против депрессии

Country Status (14)

Country Link
US (1) US8252796B2 (ru)
EP (1) EP2351746B1 (ru)
JP (1) JP5486008B2 (ru)
KR (1) KR20110074574A (ru)
CN (1) CN101712658B (ru)
AP (1) AP2011005697A0 (ru)
AU (1) AU2009301530A1 (ru)
BR (1) BRPI0920885A2 (ru)
CA (1) CA2739877A1 (ru)
CO (1) CO6731066A2 (ru)
EA (1) EA020716B1 (ru)
IL (1) IL212164A0 (ru)
MX (1) MX2011003660A (ru)
WO (1) WO2010040315A1 (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102050801B (zh) * 2009-11-03 2013-05-29 石药集团中奇制药技术（石家庄）有限公司 一种芳烷哌嗪衍生物光学异构体的制备方法
CN102050800B (zh) * 2009-11-03 2013-05-29 石药集团中奇制药技术（石家庄）有限公司 一种1-丁基-2-羟基芳烷醇哌嗪衍生物光学异构体的制备方法
KR101380181B1 (ko) 2012-02-01 2014-03-31 한국과학기술연구원 단가아민 재흡수 억제 활성을 보이는 (1Ｓ,3ａＲ,9ｂＳ)-1-페닐-2,3,3ａ,4,5,9ｂ-헥사하이드로-1Ｈ-벤조［ｅ］인돌 유도체와 3,4-다이아릴피롤리딘-2-온 유도체
CN107586281A (zh) * 2016-07-06 2018-01-16 上海医药工业研究院 芳烷杂环类衍生物及其在多靶点抗抑郁症中的应用

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
DE3626837A1 (de) 1986-08-08 1988-02-11 Weinmann & Co Kg Drehverschluss fuer einen sportschuh, insbesondere skischuh
CN1181065C (zh) * 2002-05-08 2004-12-22 上海医药工业研究院 芳烷甲酰烷基哌嗪衍生物及其作为脑神经保护剂的应用
CN1172919C (zh) * 2002-06-03 2004-10-27 上海医药工业研究院 芳烷醇哌嗪衍生物及其在制备抗抑郁症药物中的应用
CN100415728C (zh) * 2005-10-10 2008-09-03 上海医药工业研究院 烷醇哌嗪衍生物光学异构体或其盐及其制备药物的应用

Also Published As

Publication number Publication date
EP2351746A4 (en) 2012-04-04
EA020716B1 (ru) 2015-01-30
EP2351746A1 (en) 2011-08-03
CN101712658B (zh) 2012-03-14
BRPI0920885A2 (pt) 2015-12-22
CA2739877A1 (en) 2010-04-15
WO2010040315A1 (zh) 2010-04-15
US20110183996A1 (en) 2011-07-28
JP5486008B2 (ja) 2014-05-07
JP2012505166A (ja) 2012-03-01
KR20110074574A (ko) 2011-06-30
AU2009301530A1 (en) 2010-04-15
IL212164A0 (en) 2011-06-30
EP2351746B1 (en) 2014-11-12
AP2011005697A0 (en) 2011-06-30
MX2011003660A (es) 2011-05-25
CO6731066A2 (es) 2013-08-15
CN101712658A (zh) 2010-05-26
US8252796B2 (en) 2012-08-28

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

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