UA80584C2 - Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-ил-пиперазина и их применение как антагонистов нейрокининов - Google Patents

Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-ил-пиперазина и их применение как антагонистов нейрокининов Download PDF

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UA80584C2
UA80584C2 UAA200505412A UA2005005412A UA80584C2 UA 80584 C2 UA80584 C2 UA 80584C2 UA A200505412 A UAA200505412 A UA A200505412A UA 2005005412 A UA2005005412 A UA 2005005412A UA 80584 C2 UA80584 C2 UA 80584C2
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alkyl
group
compound
amino
mono
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Франс Едуард Янссенс
Франсуа Марія Соммен
Бек Бенуа Крістіан Альберт Хіслен де
Йозеф Елізабет Леенартс
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Янссен Фармацевтика Н.В.
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Publication of UA80584C2 publication Critical patent/UA80584C2/ru

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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
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    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P25/04—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
    • A61P25/18—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
    • A61P25/22—Anxiolytics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • 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
    • C07D409/14—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
    • 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
    • C07D413/14—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
    • C07D417/14—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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Данное изобретение относится к замещенным производным 1-пиперидин-4-ил-4-пирролидин-3-ил-пиперазина, которые обладают антагонистической активностью в отношении нейрокининов, в частности антагонистической активностью в отношении NK1, комбинированной антагонистической активностью в отношении NK1/NK3 и комбинированной антагонистической активностью в отношении NK1/NK2/NK3, их получения, композиций, которые их содержат и к их применению как лекарственного средства, в частности, для лечения шизофрении, тревоги, депрессии, рвоты и СРК (IBS). Соединения, согласно изобретению, могут быть представлены общей формулой (I), где все заместители имеют значения, указанные в п. 1 и до них также относятся фармацевтически приемлемые аддитивные соли кислот или оснований, стереохимически изомерные формы, N-оксиды и прекурсоры таких соединений. EMBED ISISServer
UAA200505412A 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-ил-пиперазина и их применение как антагонистов нейрокининов UA80584C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0214831 2002-12-23
PCT/EP2003/051041 WO2004056799A2 (en) 2002-12-23 2003-12-17 Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists

Publications (1)

Publication Number Publication Date
UA80584C2 true UA80584C2 (ru) 2007-10-10

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UAA200505412A UA80584C2 (ru) 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-ил-пиперазина и их применение как антагонистов нейрокининов

Country Status (31)

Country Link
US (1) US7795261B2 (ru)
EP (1) EP1581518B1 (ru)
JP (1) JP4746878B2 (ru)
KR (1) KR101049073B1 (ru)
CN (1) CN100586945C (ru)
AR (1) AR042651A1 (ru)
AT (1) ATE500242T1 (ru)
AU (1) AU2003302488B2 (ru)
BR (1) BR0317658A (ru)
CA (1) CA2508657C (ru)
CL (1) CL2003002725A1 (ru)
CY (1) CY1112601T1 (ru)
DE (1) DE60336266D1 (ru)
DK (1) DK1581518T3 (ru)
EA (1) EA009078B1 (ru)
ES (1) ES2361161T3 (ru)
HK (1) HK1087703A1 (ru)
HR (1) HRP20050556B1 (ru)
IL (1) IL169336A (ru)
JO (1) JO2696B1 (ru)
MX (1) MXPA05006887A (ru)
MY (1) MY145135A (ru)
NO (1) NO331174B1 (ru)
NZ (1) NZ541035A (ru)
PA (1) PA8593301A1 (ru)
PL (1) PL376048A1 (ru)
PT (1) PT1581518E (ru)
SI (1) SI1581518T1 (ru)
TW (1) TWI329109B (ru)
UA (1) UA80584C2 (ru)
WO (1) WO2004056799A2 (ru)

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FR2847160A1 (fr) * 2002-11-20 2004-05-21 Oreal Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute
BRPI0509803A (pt) 2004-04-13 2007-09-18 Incyte Corp derivados de piperazinilpiperidina como antagonistas de receptor de quimiocina
WO2005123081A2 (en) * 2004-06-22 2005-12-29 Janssen Pharmaceutica N.V. (2-benzyl-4-{4-[1-(tetrahydrofuran-3-carbonyl)-pyrrolidin-3-yl]-piperazin-1-yl}-piperidin-1-yl)-(3,5-trifluoromethyl-phenyl))-methanone for the treatment of schizophrenia
WO2006071958A1 (en) * 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
BRPI0608847A2 (pt) 2005-03-08 2010-02-02 Janssen Pharmaceutica Nv derivados de diaza-espiro-[4,4]-nonano substituìdos e seu uso como antagonistas de neurocinina
DE102005038947A1 (de) * 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
MX2009005252A (es) * 2006-11-17 2009-05-28 Abbott Lab Aminopirrolidinas como antagonistas del receptor de quimiocina.
RU2442786C2 (ru) * 2007-03-31 2012-02-20 Интервет Интернэшнл Б.В. Способы получения зилпатерола и его солей
CA2679991C (en) * 2007-03-31 2013-02-26 Intervet International B.V. Processes for making zilpaterol and salts thereof
KR101240147B1 (ko) 2007-03-31 2013-03-08 인터벳 인터내셔널 비.브이. 질파테롤 및 이의 염의 제조 방법
CN101772513B (zh) 2007-06-04 2013-11-13 协同医药品公司 有效用于胃肠功能紊乱、炎症、癌症和其他疾病治疗的鸟苷酸环化酶激动剂
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EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
US8507535B2 (en) * 2010-07-07 2013-08-13 Hoffmann-La Roche Inc. Methyl-pyrrolidine ether derivatives
BR112015003376A8 (pt) * 2012-08-23 2018-01-23 Alios Biopharma Inc composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e usos de quantidade eficiente de composto ou sal farmaceuticamente aceitável do mesmo ou composição farmacêutica
JP2016514670A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
PL3297631T3 (pl) 2015-05-18 2020-03-31 Nerre Therapeutics Limited Antagoniści receptora NK-1/NK-3 do leczenia uderzeń gorąca
PL3765024T3 (pl) 2018-03-14 2024-08-05 KaNDy Therapeutics Limited <div>Nowa formulacja farmaceutyczna zawierająca podwójnych antagonistów receptora nk-1/nk-3</div>
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Also Published As

Publication number Publication date
AU2003302488A1 (en) 2004-07-14
US20060040950A1 (en) 2006-02-23
SI1581518T1 (sl) 2011-06-30
JO2696B1 (en) 2013-03-03
NO20053569D0 (no) 2005-07-21
CN100586945C (zh) 2010-02-03
PA8593301A1 (es) 2004-08-31
MY145135A (en) 2011-12-30
KR101049073B1 (ko) 2011-07-15
EP1581518A2 (en) 2005-10-05
MXPA05006887A (es) 2005-08-16
CA2508657A1 (en) 2004-07-08
HRP20050556B1 (hr) 2014-03-28
BR0317658A (pt) 2005-12-06
EA009078B1 (ru) 2007-10-26
NO20053569L (no) 2005-09-15
CL2003002725A1 (es) 2005-04-08
HK1087703A1 (en) 2006-10-20
AU2003302488B2 (en) 2009-10-08
TWI329109B (en) 2010-08-21
PT1581518E (pt) 2011-05-12
PL376048A1 (en) 2005-12-12
NO331174B1 (no) 2011-10-24
TW200500359A (en) 2005-01-01
WO2004056799A2 (en) 2004-07-08
EA200501041A1 (ru) 2005-12-29
ES2361161T3 (es) 2011-06-14
DE60336266D1 (de) 2011-04-14
KR20050085098A (ko) 2005-08-29
EP1581518B1 (en) 2011-03-02
AR042651A1 (es) 2005-06-29
WO2004056799A3 (en) 2004-08-12
US7795261B2 (en) 2010-09-14
NZ541035A (en) 2008-05-30
DK1581518T3 (da) 2011-06-06
HRP20050556A2 (en) 2006-07-31
IL169336A (en) 2013-01-31
ATE500242T1 (de) 2011-03-15
CA2508657C (en) 2013-02-19
CY1112601T1 (el) 2016-02-10
CN1726207A (zh) 2006-01-25
JP4746878B2 (ja) 2011-08-10
IL169336A0 (en) 2007-07-04
JP2006514027A (ja) 2006-04-27

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